Treprostinil Sodium

Class: Vasodilating Agents, Miscellaneous
VA Class: CV900
Brands: Remodulin

Introduction

Vasodilator; a synthetic analog of prostacyclin.^{2 3 15}

Uses for Treprostinil Sodium

Pulmonary Arterial Hypertension

Used parenterally (as a continuous sub-Q or IV infusion) for treatment of pulmonary arterial hypertension (PAH) in patients with NYHA class II–IV symptoms to reduce symptoms associated with exercise.^{1 2 3} Also used parenterally to reduce rate of clinical deterioration in PAH patients who require conversion from epoprostenol therapy; carefully consider risks and benefits of each drug prior to transition.¹

Used by oral inhalation to improve walk distance in patients with WHO group I PAH and NYHA class III symptoms.^{15 16 17} Controlled clinical experience with orally inhaled treprostinil is based primarily on short-term trials in patients receiving the drug as add-on therapy to bosentan or sildenafil.^{13 15 16 17}

Sub-Q or IV treprostinil recommended by the American College of Chest Physicians (ACCP) as one of several options for treatment of PAH in patients with NYHA functional class II, III, or IV disease.^{12 13 25} Choice of PAH therapy should be individualized; consider factors such as disease severity, route of administration, potential adverse effects, and patient preference.^{12 13}

Designated an orphan drug by FDA for treatment of PAH.³¹

Treprostinil Sodium Dosage and Administration

Administration

Administer by continuous sub-Q or IV infusion, or by oral inhalation.^{1 15}

When administered parenterally, sub-Q route generally preferred; reserve IV use for patients who cannot tolerate sub-Q therapy (e.g., due to infusion-site pain or reaction) or in whom risks of IV therapy are considered warranted.¹

Sub-Q Administration

Administer undiluted drug solution by continuous sub-Q infusion via a self-inserted sub-Q catheter, using a controlled-infusion device (ambulatory infusion pump).¹ Consult manufacturer's labeling for pump specifications.¹

To avoid potential interruptions in drug delivery, patient must have immediate access to backup infusion pump and sub-Q infusion sets (since abrupt withdrawal or sudden, large dosage reductions may result in worsening of PAH symptoms).¹

For sub-Q use, administer as supplied without further dilution.¹ A single reservoir (syringe) of undiluted treprostinil may be administered for up to 72 hours at 37°C.¹

Rate of Administration

Calculate sub-Q infusion rates using the following formula:¹

sub-Q infusion rate (mL/hr) = [dose (ng/kg per minute) × wt (kg) × 0.00006] ÷ treprostinil dosage strength concentration (mg/mL)

IV Administration

For solution compatibility information, see Compatibility under Stability.

Must be diluted prior to IV administration.^{1 14} (See Dilution under Dosage and Administration.)

Administer diluted drug solution by continuous IV infusion through a permanent indwelling central venous catheter using a controlled-infusion device (ambulatory infusion pump).¹ Consult manufacturer's labeling for pump specifications.¹

A peripheral IV catheter (preferably placed in a large vein) may be used temporarily until central venous access can be established.¹

To avoid potential interruptions in drug delivery, patient must have immediate access to backup infusion pump and IV infusion sets (since abrupt withdrawal or sudden, large dosage reductions may result in worsening of PAH symptoms).¹

Consult manufacturer's labeling for additional information on administration of IV treprostinil.^{1 14}

Dilution

Must be diluted with sterile water for injection, 0.9% sodium chloride injection, or Flolan sterile diluent for injection prior to IV administration. Diluted solutions are stable at 37°C for ≤48 hours at concentrations as low as 0.004 mg/mL (4000 ng/mL).¹

Add appropriate amount of drug to a sufficient volume of diluent to fill pump reservoir (typical IV infusion system reservoirs have a total capacity of 50 or 100 mL).¹ Select an infusion rate that will allow for an infusion period of ≤48 hours, and calculate concentration and amount of treprostinil required for the dilution according to the following formulas:¹

Diluted IV treprostinil concentration (mg/mL) = [dose (ng/kg per minute) × wt (kg) × 0.00006] ÷ IV infusion rate (mL/hr)

Amount of treprostinil injection (mL) = [diluted IV treprostinil concentration (mg/mL) ÷ treprostinil vial strength (mg/mL)] × total reservoir volume (mL)

Consult manufacturer's labeling for additional information on preparation of IV treprostinil.¹

Oral Inhalation

Treprostinil inhalation solution is for oral inhalation only; do not ingest.¹⁵

Administer using only the Tyvaso Inhalation System (Optineb-ir Model ON-100/7 device and related accessories).¹⁵ Patients should have access to a back-up Optineb-ir device in the event of equipment malfunction.¹⁵ Instruct patients on proper administration (including dosing frequency), use, and maintenance of Optineb-ir device.¹⁵

Administer 4 times daily during waking hours at equally spaced intervals of approximately 4 hours.¹⁵

Prior to first inhalation session, transfer entire contents of a single 2.9-mL ampul of drug into medicine cup supplied by the manufacturer.¹⁵ One ampul should contain enough drug for one day of treatment.^{15 19} After each inhalation session, cap inhalation device and store upright with remaining drug inside for ≤24 hours.¹⁵ Discard medicine cup and any unused solution at end of each day and clean Optineb-ir device according to manufacturer's instructions.¹⁵

Do not mix with other drugs.¹⁵

Do not allow solution to come into contact with the eyes or skin.¹⁵

Dosage

Adults

PAH

Continuous Sub-Q or IV Infusion

Initially, 1.25 ng/kg per minute.¹ If initial dosage is not tolerated, reduce infusion rate to 0.625 ng/kg per minute.¹

Adjust dosage to achieve symptomatic improvement while minimizing adverse effects.¹ Increase infusion rate based on clinical response in increments of 1.25 ng/kg per minute at weekly intervals for the first 4 weeks and then 2.5 ng/kg per minute at weekly intervals for the remaining duration of the infusion.¹

Several months may be required to identify optimal dosage.^{2 8 14}

Oral Inhalation

Initially, 18 mcg (3 inhalations) per treatment session 4 times daily.¹⁵ If initial dosage not tolerated, reduce to 1 or 2 inhalations per treatment session, then increase up to 3 inhalations as tolerated.¹⁵ Continue to increase dose by 3 inhalations every 1–2 weeks until target maintenance dosage of 54 mcg (9 inhalations) per treatment session attained.¹⁵ If unable to titrate to target dosage, maintain patient on highest possible tolerated dosage.¹⁵

If a treatment session is missed or interrupted, resume therapy as soon as possible at usual dosage.¹⁵

Conversion from Epoprostenol to Sub-Q or IV Treprostinil Therapy

Sub-Q or IV

Perform transition in a hospital setting where patient can be closely monitored.¹

Initiate treprostinil at a dosage equivalent to 10% of the current epoprostenol dosage; gradually increase treprostinil dosage while simultaneously decreasing dosage of epoprostenol.¹ Manufacturer recommends the following titration protocol:¹

Step	Epoprostenol Dosage	Treprostinil Dosage
1	Unchanged	10% of starting epoprostenol dosage
2	80% of starting epoprostenol dosage	30% of starting epoprostenol dosage
3	60% of starting epoprostenol dosage	50% of starting epoprostenol dosage
4	40% of starting epoprostenol dosage	70% of starting epoprostenol dosage
5	20% of starting epoprostenol dosage	90% of starting epoprostenol dosage
6	5% of starting epoprostenol dosage	110% of starting epoprostenol dosage
7	0	110% of starting epoprostenol dosage + additional 5–10% increments as needed

Individually titrate treprostinil dosage to allow transition from epoprostenol therapy while balancing symptoms of PAH and prostacyclin-related adverse effects.¹ Manage any increase in PAH symptoms (e.g., shortness of breath) by initially increasing dosage of treprostinil; manage symptoms of excess prostacyclin (e.g., facial flushing, headache, jaw pain) by initially decreasing dosage of epoprostenol.¹

Other transition protocols have been used successfully.^{9 21 22 25} Limited data indicate that patients whose therapy is transitioned from epoprostenol to IV treprostinil appear to require higher average dosages of treprostinil to maintain the same clinical benefits.^{11 14 21 22 24 25}

Prescribing Limits

Adults

PAH

Parenteral

Limited experience with dosages >40 ng/kg per minute.¹

Oral Inhalation

Maximum 54 mcg (9 inhalations) per treatment session 4 times daily.¹⁵

Special Populations

Hepatic Impairment

In patients with mild to moderate hepatic impairment, decrease initial dosage of sub-Q or IV treprostinil to 0.625 ng/kg per minute (based on ideal body weight).¹

Titrate orally inhaled treprostinil slowly in patients with hepatic impairment because of the possibility of increased systemic exposure to the drug.¹⁵

Renal Impairment

Manufacturer makes no specific dosage recommendations for patients with renal impairment;¹ titrate dosage slowly because of the possibility of increased systemic exposure to the drug.^{1 15}

Geriatric Patients

Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy.^{1 15}

Cautions for Treprostinil Sodium

Contraindications

• 
  

  None known.¹

  
  

Warnings/Precautions

Warnings

Risk of Infection with IV Administration

Risk of serious and potentially fatal blood stream infections (BSI) and sepsis associated with drug delivery system (chronic indwelling central venous catheter).^{1 14 25 28} Patients must use strict aseptic technique in routine catheter care and in the preparation and administration of treprostinil.¹ Sub-Q route of administration is preferred when the drug is given parenterally.¹

Adequate Patient Evaluation and Monitoring

Use only under the supervision of a qualified clinician experienced in the diagnosis and management of PAH.¹

Initiate therapy in a setting with adequate medical personnel and equipment for providing physiologic monitoring and emergency care.¹

Therapy may be continued for prolonged periods; carefully consider patient's ability to administer the drug and care for an infusion system (when drug is given parenterally).¹

Precautions Related to Inhaled Treprostinil

Safety and efficacy of orally inhaled treprostinil not established in patients with lung disease (i.e., asthma, COPD).¹⁵ Monitor patients who develop acute pulmonary infections for any worsening of lung disease and loss of drug effect.¹⁵

Withdrawal of Therapy

Avoid abrupt withdrawal or sudden, large dosage reductions; may result in worsening of PAH symptoms.¹

Hematologic Effects

Possible increased risk of bleeding, particularly in patients receiving anticoagulant therapy.^{1 15} (See Specific Drugs under Interactions.)

Hypotensive Effects

Risk of symptomatic hypotension in patients with low systemic arterial pressure receiving orally inhaled treprostinil.¹⁵

Specific Populations

Pregnancy

Category B.^{1 15}

Lactation

Not known whether treprostinil is distributed into milk;^{1 15} use with caution in nursing women.^{1 15}

Pediatric Use

Parenteral treprostinil: Safety and efficacy not established in children or adolescents <16 years of age.^{1 8} Clinical studies did not include sufficient numbers of patients ≤16 years of age to determine whether pediatric patients respond differently than adults.¹ Titrate dosage carefully.⁸

Orally inhaled treprostinil: Safety and efficacy not established in patients <18 years of age.¹⁵

Geriatric Use

Clinical studies did not include sufficient numbers of patients ≥65 years of age to determine whether geriatric patients respond differently than younger patients.^{1 15}

Hepatic Impairment

Adjust dosage of sub-Q or IV treprostinil in patients with mild to moderate hepatic impairment.¹ (See Hepatic Impairment under Dosage and Administration.)

Not studied in patients with severe hepatic impairment.^{1 15}

Renal Impairment

Not studied in patients with renal impairment.^{1 15} However, possibility of reduced renal clearance of the drug in such patients.¹⁵

Common Adverse Effects

Sub-Q therapy: Infusion site pain and reaction (e.g., erythema, induration, rash).¹

IV therapy: Arm swelling, paresthesias, hematoma, pain.¹

Sub-Q and IV therapy: Headache, diarrhea, nausea, jaw pain, vasodilation, dizziness, edema, pruritus, hypotension.¹

Orally inhaled therapy: Cough and throat irritation; headache; GI effects; muscle, jaw, or bone pain; flushing; syncope.^{15 16}

Interactions for Treprostinil Sodium

Extensively metabolized in liver, principally by CYP2C8.^{1 29} Does not inhibit CYP1A2, 2A6, 2C8, 2C9, 2C19, 2D6, 2E1, or 3A in vitro.^{1 15} Does not induce CYP1A2, 2B6, 2C9, 2C19, or 3A in vitro.^{1 15} Pharmacokinetic interactions with drugs metabolized by the CYP enzyme system are considered unlikely.¹

Specific Drugs

Drug	Interaction	Comments
Acetaminophen	Pharmacokinetics of treprostinil not substantially affected1 15
Anticoagulants	Potential for increased risk of bleeding1 15 Warfarin: No clinically important interaction observed1 15
Antihypertensive agents	Additive hypotensive effect possible1 15
Bosentan	Pharmacokinetic interaction not observed with an oral formulation of treprostinil1 15 29
Diuretics	Additive hypotensive effect possible1 15
Fluconazole	Pharmacokinetics of treprostinil not substantially affected1 15
Gemfibrozil	Increased systemic exposure to an oral formulation of treprostinil; possible increased risk of adverse effects with treprostinil1 15
Rifampin	Decreased systemic exposure to an oral formulation of treprostinil; possible reduced efficacy of treprostinil1 15
Sildenafil	Pharmacokinetic interaction not observed with an oral formulation of treprostinil1 15
Vasodilating agents	Additive hypotensive effect possible1 15

Treprostinil Sodium Pharmacokinetics

Absorption

Bioavailability

Rapidly and completely absorbed after sub-Q infusion; absolute bioavailability of 100%.¹

Sub-Q and IV treprostinil are bioequivalent at steady-state dosage of 10 ng/kg per minute.^{1 9 30}

Mean absolute systemic bioavailability following oral inhalation is approximately 64 and 72% following doses of 18 and 36 mcg, respectively.¹⁵

Plasma Concentrations

Steady-state concentrations occur in approximately 10 hours following sub-Q administration.¹

Peak plasma concentrations of treprostinil achieved approximately 10–15 minutes after oral inhalation.¹⁸

Special Populations

Peak plasma concentrations increased by twofold or fourfold in patients with portopulmonary hypertension and mild or moderate hepatic impairment, respectively, compared with healthy individuals.¹

Distribution

Plasma Protein Binding

91%.^{1 15}

Elimination

Metabolism

Extensively metabolized in liver, principally by CYP2C8; 5 metabolites described thus far.^{1 15}

Elimination Route

Following sub-Q administration, excreted in urine (79%) and feces (13%).^{1 15}

Half-life

Biphasic; terminal half-life of approximately 4 hours.^{1 15}

Special Populations

In patients with hepatic insufficiency, clearance was reduced by up to 80% compared with healthy adults.^{1 15}

In patients with renal impairment, clearance may be reduced since treprostinil and its metabolites are eliminated principally by the kidneys.¹⁵

Stability

Storage

Parenteral

Injection

25°C (may be exposed to 15–30°C).¹

May use vial for ≤30 days after initial entry.¹

May store undiluted drug in a single reservoir (syringe) for ≤72 hours at 37°C.¹

Diluted solutions of treprostinil are stable at 37°C for ≤48 hours at concentrations as low as 0.004 mg/mL (4000 ng/mL).¹

Oral Inhalation

25°C (may be exposed to 15–30°C) for unopened ampuls in unopened foil pouch.¹⁵

Use ampuls within 7 days after opening foil pouch; store unopened ampuls in pouch until use because drug is light-sensitive.¹⁵

Once drug solution is placed in medicine cup in inhalation device, use within 24 hours.¹⁵ Discard any unused solution at end of day.¹⁵

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility

Compatible1 HID
Sodium chloride 0.9%
VariableHID
Dextrose 5%

Actions

• 
  

  Pharmacologic actions (e.g., vasodilation of pulmonary and systemic arterial vascular beds, inhibition of platelet aggregation) similar to those of epoprostenol.^{2 3}

  
  


• 
  

  In animals, vasodilatory effects reduce right and left ventricular afterload and increase cardiac output and stroke volume.¹

  
  


• 
  

  Causes dose-related negative inotropic and lusitropic effect.¹

  
  


• 
  

  Orally inhaled treprostinil exhibits high pulmonary selectivity and produces sustained pulmonary vasodilation without substantial systemic effects.¹⁸

  
  


• 
  

  Modest and temporary effects on QT_c interval observed following single oral inhalation doses; possibly an artifact of the rapidly changing heart rate produced by the drug.^{1 15} Effects of parenteral treprostinil on QT_c not studied.¹

  
  

Advice to Patients

• 
  

  Importance of advising patient that treprostinil is infused continuously through a self-inserted sub-Q or surgically placed indwelling central venous catheter, via an infusion pump, which will require a long-term commitment on the part of the patient.¹

  
  


• 
  

  Importance of advising patient to use sterile technique when preparing and administering drug.¹

  
  


• 
  

  Importance of advising patients that subsequent management of PAH may require therapy with an alternate IV prostacyclin therapy (e.g., epoprostenol).¹

  
  


• 
  

  Importance of understanding potential risks associated with therapy.¹

  
  


• 
  

  Importance of patients receiving adequate training in the proper administration and dosing of orally inhaled treprostinil, and on set-up, operation, and maintenance of the Optineb-ir device.¹⁵

  
  


• 
  

  Importance of having immediate access to a back-up pump and infusion sets (when administered parenterally) or a back-up Optineb-ir device (when administered via oral inhalation) in order to avoid potential interruptions in drug therapy secondary to drug delivery device failure or equipment malfunction.^{1 15}

  
  


• 
  

  Importance of advising patients that if a scheduled treatment session of orally inhaled treprostinil is missed, treatment should be resumed as soon as possible.¹⁵

  
  


• 
  

  Importance of advising patients to avoid skin or eye contact with treprostinil oral inhalation solution.¹⁵ If skin or eye contact occurs, instruct patient to immediately rinse the affected area with water.¹⁵

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.¹

  
  


• 
  

  Importance of informing patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Treprostinil Sodium

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	Injection, for continuous sub-Q or IV infusion via controlled-infusion device only	1 mg (of treprostinil) per mL	Remodulin	United Therapeutics
		2.5 (of treprostinil) per mL	Remodulin	United Therapeutics
		5 (of treprostinil) per mL	Remodulin	United Therapeutics
		10 (of treprostinil) per mL	Remodulin	United Therapeutics
Oral Inhalation	Solution, for nebulization	0.6 mg/mL (1.74 mg)	Tyvaso (available with Tyvaso Inhalation System)	United Therapeutics

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions August 04, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. United Therapeutics Corp. Remodulin (treprostinil sodium) injection prescribing information. Research Triangle Park, NC; 2010 Jan.

2. Simonneau G, Barst RJ, Galie N et al. Continuous subcutaneous infusion of treprostinil, a prostacyclin analogue, in patients with pulmonary arterial hypertension: a double-blind, randomized, placebo-controlled trial. Am J Respir Crit Care Med. 2002; 165:800-4. [IDIS 480255] [PubMed 11897647]

3. Fleming T, Lindenfeld J, Lipicky R et al. Report from the 93rd Cardiovascular and renal drugs advisory committee meeting, August 9-10, 2001. Circulation. 2001; 104:1742. [PubMed 11591605]

4. Vachiery JL, Hill N, Zwicke D et al. Transitioning from i.v. epoprostenol to subcutaneous treprostinil in pulmonary arterial hypertension. Chest. 2002; 121:1561-5. [IDIS 481609] [PubMed 12006444]

5. United Therapeutics Corporation. Cardiovascular and Renal drugs Advisory Committee presentation. NDA 21-272 Remodulin (treprostinil sodium) injection. Research Triangle Park, NC: 2001 Aug 21.

6. Newman JH. Treatment of primary pulmonary hypertension the next generation. N Engl J Med. 2002; 346:933-5. [IDIS 478527] [PubMed 11907295]

7. Food and Drug Administration. Cardiovascular and Renal Drugs Advisory Committee meeting. Rockville, MD; Aug 2001. From FDA web site.

8. United Therapeutics Corp., Research Triangle Park, NC; Personal communication.

9. Rubenfire M, McLaughlin VV, Allen RP et al. Transition from IV epoprostenol to subcutaneous treprostinil in pulmonary arterial hypertension: a controlled trial. Chest. 2007; 132:757-63. [PubMed 17400684]

10. Tapson VF, Gomberg-Maitland M, McLaughlin VV et al. Safety and efficacy of IV treprostinil for pulmonary arterial hypertension: a prospective, multicenter, open-label, 12-week trial. Chest. 2006; 129:683-8. [PubMed 16537868]

11. Gomberg-Maitland M, Tapson VF, Benza RL et al. Transition from intravenous epoprostenol to intravenous treprostinil in pulmonary hypertension. Am J Respir Crit Care Med. 2005; 172:1586-9. [PubMed 16151039]

12. Badesch DB, Abman SH, Simonneau G et al. Medical therapy for pulmonary arterial hypertension: Updated ACCP evidence-based clinical practice guidelines. Chest. 2007; 131:1917-28.

13. Barst RJ, Gibbs JS, Ghofrani HA et al. Updated evidence-based treatment algorithm in pulmonary arterial hypertension. J Am Coll Cardiol. 2009; 54(1 Suppl):S78-84. [PubMed 19555861]

14. Oudiz RJ, Farber HW. Dosing considerations in the use of intravenous prostanoids in pulmonary arterial hypertension: an experience-based review. Am Heart J. 2009; 157:625-35. [PubMed 19332188]

15. United Therapeutics Corp. Tyvaso (treprostinil) inhalation solution prescribing information. Research Triangle Park, NC; 2009 Jul.

16. McLaughlin VV, Benza RL, Rubin LJ et al. Addition of inhaled treprostinil to oral therapy for pulmonary arterial hypertension: a randomized controlled clinical trial. J Am Coll Cardiol. 2010; 55:1915-22. [PubMed 20430262]

17. Channick RN, Olschewski H, Seeger W et al. Safety and efficacy of inhaled treprostinil as add-on therapy to bosentan in pulmonary arterial hypertension. J Am Coll Cardiol. 2006; 48:1433-7. [PubMed 17010807]

18. Voswinckel R, Enke B, Reichenberger F et al. Favorable effects of inhaled treprostinil in severe pulmonary hypertension: results from randomized controlled pilot studies. J Am Coll Cardiol. 2006; 48:1672-81. [PubMed 17045906]

19. United Therapeutics Corp. Tyvaso inhalation system instructions for use. Research Triangle Park, NC; 2009 Aug.

20. Oudiz RJ, Schilz RJ, Barst RJ et al. Treprostinil, a prostacyclin analogue, in pulmonary arterial hypertension associated with connective tissue disease. Chest. 2004; 126:420-7. [PubMed 15302727]

21. Sitbon O, Manes A, Jais X et al. Rapid switch from intravenous epoprostenol to intravenous treprostinil in patients with pulmonary arterial hypertension. J Cardiovasc Pharmacol. 2007; 49:1-5. [PubMed 17261956]

22. Ivy DD, Claussen L, Doran A. Transition of stable pediatric patients with pulmonary arterial hypertension from intravenous epoprostenol to intravenous treprostinil. Am J Cardiol. 2007; 99:696-8. [PubMed 17317374]

23. Barst RJ, Galie N, Naeije R et al. Long-term outcome in pulmonary arterial hypertension patients treated with subcutaneous treprostinil. Eur Respir J. 2006; 28:1195-203. [PubMed 16899485]

24. Naeije R, Huez S. Expert opinion on available options treating pulmonary arterial hypertension. Expert Opin Pharmacother. 2007; 8:2247-65. [PubMed 17927481]

25. Skoro-Sajer N, Lang I. Treprostinil for the treatment of pulmonary hypertension. Expert Opin Pharmacother. 2008; 9:1415-20. [PubMed 18473715]

26. Feldman JP, Chakinala M, Torres F et al. Treprostinil sodium improves exercise capacity when added to existing oral pulmonary arterial hypertension therapy. Chest. 2007; 132 (suppl). Abstract No. 474b.

27. Gomberg-Maitland M, McLaughlin V, Gulati M et al. Efficacy and safety of sildenafil added to treprostinil in pulmonary hypertension. Am J Cardiol. 2005; 96:1334-6. [PubMed 16253609]

28. Centers for Disease Control and Prevention (CDC). Bloodstream infections among patients treated with intravenous epoprostenol or intravenous treprostinil for pulmonary arterial hypertension--seven sites, United States, 2003-2006. MMWR Morb Mortal Wkly Rep. 2007; 56:170-2. [PubMed 17332729]

29. Gotzkowsky SK, Dingemanse J, Lai A et al. Lack of a pharmacokinetic interaction between oral treprostinil and bosentan in healthy adult volunteers. J Clin Pharmacol. 2010; 50:829-34. [PubMed 20133511]

30. Laliberte K, Arneson C, Jeffs R et al. Pharmacokinetics and steady-state bioequivalence of treprostinil sodium (Remodulin) administered by the intravenous and subcutaneous route to normal volunteers. J Cardiovasc Pharmacol. 2004; 44:209-14. [PubMed 15243302]

31. US Food and Drug Administration. Orphan designations pursuant to Section 526 of the Federal Food and Cosmetic Act as amended by the Orphan Drug Act (P.L. 97-414). Rockville, MD; [August 6, 2010]. From FDA web site.

HID. Trissel LA. Handbook on injectable drugs. 16th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2011:1492-3.

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Benadryl Skin Allergy Relief Cream

1. Name Of The Medicinal Product

Benadryl Skin Allergy Relief Cream

Benadryl Allergy Skin Cream

2. Qualitative And Quantitative Composition

Benadryl Allergy Skin Cream contains:

1% w/v diphenhydramine hydrochloride Ph Eur

8% w/v zinc oxide Ph Eur

0.1% w/v racemic camphor Ph Eur.

3. Pharmaceutical Form

Cream.

4. Clinical Particulars

4.1 Therapeutic Indications

Benadryl Allergy Skin Cream is indicated for the relief of irritation associated with urticaria, herpes zoster and other minor skin affections and alleviate the discomforts of sunburn, prickly heat, insect bites and nettle stings. In infants it may be used for hives.

4.2 Posology And Method Of Administration

Adults:

Topical. Benadryl Allergy Skin Cream may be applied to the affected area, three or four times daily.

Children and Infants:

Topical. As for adults.

The Elderly:

Topical. As for adults.

4.3 Contraindications

Do not use on chicken pox or measles or exudative dermatoses, unless supervised by a doctor. Do not use on extensive areas of the skin except as directed by a doctor. Do not use any other drugs containing diphenhydramine while using this product.

4.4 Special Warnings And Precautions For Use

Benadryl Allergy Skin Cream should not be applied to raw, or broken surfaces or mucous membranes as this may result in percutaneous absorption giving rise to systemic effects. Avoid contact with the eyes. If a burning sensation or rash develops or if the condition persists, treatment should be discontinued. If necessary, remove by washing with soap and water.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

None known.

4.6 Pregnancy And Lactation

The safety of Benadryl Allergy Skin Cream in pregnancy and lactation has not been established. Like any medicine, Benadryl Allergy Skin Cream should only be used if the possible benefits outweigh the potential risks involved. Diphenhydramine is known to be absorbed through the skin. Diphenhydramine crosses the placental barrier and is secreted in breast milk.

4.7 Effects On Ability To Drive And Use Machines

None known.

4.8 Undesirable Effects

Rarely, sensitivity, eczematous reactions and photosensitivity have been reported after topical application of antihistamines. If this occurs, treatment should be discontinued.

4.9 Overdose

Symptoms and signs

Accidental ingestion or excessive absorption of Benadryl Allergy Skin Cream may lead to dose-related signs of diphenhydramine toxicity. These include drowsiness and sedation with anti-cholinergic symptoms prevailing. Camphor may produce nausea, vomiting and dizziness. At higher doses, delirium leading to coma, ataxia, increased muscle reflexes and cloniform convulsions may appear.

Treatment

The stomach should be emptied by lavage and aspiration. In cases of acute poisoning, activated charcoal may be useful. A sodium sulphate purgative may be given. Convulsions may be controlled with diazepam or thiopental sodium. In the case of camphor poisoning, lipid haemodialysis or resin haemoperfusion may be useful.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Benadryl Allergy Skin Cream contains diphenhydramine hydrochloride, zinc oxide and camphor. Diphenhydramine is a powerful antihistamine and local anaesthetic (antipruritic). In concentrations of between 0.1 – 3.0 %, camphor depresses cutaneous receptors and is an effective analgesic, anaesthetic and antipruritic, which provides a feeling of coolness when applied topically.

5.2 Pharmacokinetic Properties

Benadryl Allergy Skin Cream is intended only for topical application to the skin. At the recommended dose little of the active ingredients will be absorbed. Percutaneous penetration of diphenhydramine and camphor has been demonstrated during inappropriate use of these compounds separately, but has not been quantified.

5.3 Preclinical Safety Data

There are no preclinical data of relevance to the prescriber which are additional to that already included in other sections of the SPC.

6. Pharmaceutical Particulars

6.1 List Of Excipients

White ceresin

Cetostearyl alcohol

Ferric oxide red (E172)

Ferric oxide yellow (E172)

Sorbitan stearate

Propyl hydroxybenzoate

Propylene glycol

Polysorbate 60

Perfume oil soleil 78087

Purified water

6.2 Incompatibilities

None known.

6.3 Shelf Life

3 years.

6.4 Special Precautions For Storage

Do not store above 25°C.

6.5 Nature And Contents Of Container

Benadryl Allergy Skin Cream is stored in a 42 g epoxy phenolic-based lacquered aluminium tube with a white, polyethylene or polypropylene cap.

6.6 Special Precautions For Disposal And Other Handling

None applicable.

Administrative Data

7. Marketing Authorisation Holder

McNeil Products Limited

Foundation Park

Roxborough Way

Maidenhead

Berkshire SL6 3UG

United Kingdom

8. Marketing Authorisation Number(S)

PL 15513/0078

9. Date Of First Authorisation/Renewal Of The Authorisation

5^th January 2000

10. Date Of Revision Of The Text

2 December 2009

Aricept

Pronunciation: doe-NEP-e-zil
Generic Name: Donepezil
Brand Name: Aricept

Aricept is used for:

Treating dementia (eg, impairment of memory, judgment, and abstract thinking; changes in personality) in patients with moderate to severe Alzheimer disease.

Aricept is a cholinesterase inhibitor. It works by increasing the amount of a certain substance (acetylcholine) in the brain, which may help reduce the symptoms of dementia in patients with Alzheimer disease.

Do NOT use Aricept if:

• you are allergic to any ingredient in Aricept or to another piperidine derivative

Contact your doctor or health care provider right away if any of these apply to you.

Before using Aricept:

Some medical conditions may interact with Aricept. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances


• if you have a history of certain heart problems (eg, fast, slow, or irregular heartbeat; sick sinus syndrome), stomach or bowel problems (eg, ulcer, blockage), liver or kidney problems, lung or breathing problems (eg, asthma, chronic obstructive pulmonary disease [COPD]), or urinary blockage


• if you have brain lesions or tumors, increased pressure in the brain, a recent head injury, or a history of seizures (eg, epilepsy)


• if you have Parkinson disease, trouble swallowing tablets, or metabolism problems

Some MEDICINES MAY INTERACT with Aricept. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) (eg, ibuprofen) because the risk of stomach or bowel bleeding may be increased


• Cholinergic agents (eg, bethanechol), cholinesterase inhibitors (eg, galantamine), ketoconazole, or quinidine because they may increase the risk of Aricept's side effects


• Carbamazepine, dexamethasone, phenobarbital, phenytoin, or rifampin because they may decrease Aricept's effectiveness


• Anticholinergics (eg, scopolamine) because their effectiveness may be decreased by Aricept

This may not be a complete list of all interactions that may occur. Ask your health care provider if Aricept may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Aricept:

Use Aricept as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• An extra patient leaflet is available with Aricept. Talk to your pharmacist if you have questions about this information.


• Take Aricept by mouth in the evening right before bed, unless your doctor tells you otherwise. Take Aricept with or without food.


• Swallow Aricept whole. Do not break, crush, or chew before swallowing.


• Take Aricept on a regular schedule to get the most benefit from it.


• Taking Aricept at the same time each day will help you remember to take it.


• Continue to take Aricept even if you feel well. Do not miss any doses.


• If you miss a dose of Aricept, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once. Contact your doctor if you miss several doses (7 or more days) of Aricept. You may need to restart your medicine at a lower dose to avoid side effects.

Ask your health care provider any questions you may have about how to use Aricept.

Important safety information:

• Aricept may cause drowsiness, dizziness, or fainting. These effects may be worse if you take it with alcohol or certain medicines. Use Aricept with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.


• Do NOT take more than the recommended dose, change your dose, or stop taking Aricept without checking with your doctor.


• Aricept is not a cure for Alzheimer disease. Alzheimer disease will get worse over time in all patients who have it.


• Tell your doctor or dentist that you take Aricept before you receive any medical or dental care, emergency care, or surgery.


• Use Aricept with caution in patients who weigh less than 55 kg (121 lbs); they may be more sensitive to its effects, especially nausea, vomiting, and weight loss.


• Aricept should not be used in CHILDREN; safety and effectiveness in children have not been confirmed.


• PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of taking Aricept while you are pregnant. It is not known if Aricept is found in breast milk. Do not breast-feed while taking Aricept. Aricept is not approved for use in women who may be breast-feeding.

Possible side effects of Aricept:

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Diarrhea; dizziness; loss of appetite; muscle cramps; nausea; tiredness; trouble sleeping; vomiting; weight loss.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); bloody or black, tarry stools; chest pain; decreased, difficult, or painful urination; fainting; fever; flu-like symptoms (eg, headache, muscle aches, tiredness); mood or mental problems (eg, depression); new or worsening breathing problems (eg, shortness of breath); seizures; severe dizziness or headache; severe or persistent heartburn or stomach pain; slow or irregular heartbeat; swelling of the hands, ankles, or feet; tremor; unusual bruising; unusual tiredness or weakness; vomit that looks like blood or coffee grounds.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

See also: Aricept side effects (in more detail)

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include fainting; increased sweating or saliva production; loss of consciousness; muscle weakness; seizures; severe dizziness; severe nausea or vomiting; slow heartbeat; slow or shallow breathing.

Proper storage of Aricept:

Store Aricept at room temperature, between 59 and 86 degrees F (15 and 30 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Aricept out of the reach of children and away from pets.

General information:

• If you have any questions about Aricept, please talk with your doctor, pharmacist, or other health care provider.


• Aricept is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Aricept. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Aricept resources

• Aricept Side Effects (in more detail)
• Aricept Use in Pregnancy & Breastfeeding
• Drug Images
• Aricept Drug Interactions
• Aricept Support Group
• 11 Reviews for Aricept - Add your own review/rating

Compare Aricept with other medications

• Alzheimer's Disease
• Mild Cognitive Impairment

Pindolol

Pindolol Description

Pindolol, a synthetic beta-adrenergic receptor blocking agent with intrinsic sympathomimetic activity is 1-(Indol-4-yloxy)-3-(isopropylamino)-2-propanol.

C14H20N2O2    M.W. 248.32

Pindolol, USP is a white to off-white, crystalline powder having a faint odor which is practically insoluble in water; slightly soluble in methanol; and very slightly soluble in chloroform.

Each tablet for oral administration contains Pindolol and the following inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, magnesium stearate, microcrystalline cellulose, pregelatinized starch, and sodium lauryl sulfate.

Pindolol - Clinical Pharmacology

Pindolol is a nonselective beta-adrenergic antagonist (beta-blocker) which possesses intrinsic sympathomimetic activity (ISA) in therapeutic dosage ranges but does not possess quinidine-like membrane stabilizing activity.

PHARMACODYNAMICS

In standard pharmacologic tests in man and animals, Pindolol attenuates increases in heart rate, systolic blood pressure, and cardiac output resulting from exercise and isoproterenol administration, thus confirming its beta-blocking properties. The ISA or partial agonist activity of Pindolol is mediated directly at the adrenergic receptor sites and may be blocked by other beta-blockers. In catecholamine depleted animal experiments, ISA is manifested as an increase in the inotropic and chronotropic activity of the myocardium. In man, ISA is manifested by a smaller reduction in the resting heart rate (4 to 8 beats/min) than is seen with drugs lacking ISA. There is also a smaller reduction in resting cardiac output. The clinical significance of this observation has not been evaluated and there is no evidence, or reason to believe, that exercise cardiac output is less affected by Pindolol.

Pindolol has been shown in controlled, double-blind clinical studies to be an effective antihypertensive agent when used as monotherapy, or when added to therapy with thiazide-type diuretics. Divided dosages in the range of 10 mg to 60 mg daily have been shown to be effective. As monotherapy, Pindolol is as effective as propranolol, α-methyldopa, hydrochlorothiazide, and chlorthalidone in reducing systolic and diastolic blood pressure. The effect on blood pressure is not orthostatic, i.e., Pindolol was equally effective in reducing the supine and standing blood pressure.

In open, long-term studies up to 4 years, no evidence of diminution of the blood pressure lowering response was observed.

An average 3-pound increase in body weight has been noted in patients treated with Pindolol alone, a larger increase than was observed with propranolol or placebo. The weight gain appeared unrelated to blood pressure response and was not associated with an increased risk of heart failure, although edema was more common than in control patients. Pindolol does not have a consistent effect on plasma renin activity.

The mechanism of the antihypertensive effects of beta-blocking agents has not been established, but several mechanisms have been postulated: 1) an effect on the central nervous system resulting in a reduced sympathetic outflow to the periphery, 2) competitive antagonism of catecholamines at peripheral (especially cardiac) adrenergic receptor sites, leading to decreased cardiac output, 3) an inhibition of renin release. These mechanisms appear less likely for Pindolol than other beta-blockers in view of the modest effect on resting cardiac output and renin.

Beta-blockade therapy is useful when it is necessary to suppress the effects of beta-adrenergic agonists in order to achieve therapeutic goals. However, in certain clinical situations, (e.g., cardiac failure, heart block, bronchospasm), the preservation of an adequate sympathetic tone may be necessary to maintain vital functions. Although a beta-antagonist with ISA such as Pindolol does not eliminate sympathetic tone entirely, there is no controlled evidence that it is safer than other beta-blockers in such conditions as heart failure, heart block, or bronchospasm or is less likely to cause those conditions. In single-dose studies of the effects of beta-blockers on FEV1, Pindolol was indistinguishable from other non-cardioselective agents in its reduction of FEV1, and its reduction in the effectiveness of an exogenous beta-agonist.

Exacerbation of angina and, in some cases, myocardial infarction and ventricular dysrhythmias have been reported after abrupt discontinuation of therapy with beta-adrenergic blocking agents in patients with coronary artery disease. Abrupt withdrawal of these agents in patients without coronary artery disease has resulted in transient symptoms, including tremulousness, sweating, palpitation, headache, and malaise. Several mechanisms have been proposed to explain these phenomena, among them increased sensitivity to catecholamines because of increased numbers of beta receptors.

PHARMACOKINETICS AND METABOLISM

Pindolol is rapidly and reproducibly absorbed (greater than 95%), achieving peak plasma concentrations within 1 hour of drug administration. Pindolol has no significant first-pass effect. The blood concentrations are proportional in a linear manner to the administered dose in the range of 5 mg to 20 mg. Upon repeated administration to the same subject, variation is minimal. After a single dose, intersubject variation for peak plasma concentrations was about 4-fold (e.g., 45 to 167 ng/mL for a 20 mg dose). Upon multiple dosing, intersubject variation decreased to 2- to 2.5-fold. Pindolol is only 40% bound to plasma proteins and is evenly distributed between plasma and red cells. The volume of distribution in healthy subjects is about 2 L/kg.

Pindolol undergoes extensive metabolism in animals and man. In man, 35% to 40% is excreted unchanged in the urine and 60% to 65% is metabolized primarily to hydroxy-metabolites which are excreted as glucuronides and ethereal sulfates. The polar metabolites are excreted with a half-life of approximately 8 hours and thus multiple dosing therapy (q.8H) results in a less than 50% accumulation in plasma. About 6% to 9% of an administered intravenous dose is excreted by the bile into the feces.

The disposition of Pindolol after oral administration is monophasic with a half-life in healthy subjects or hypertensive patients with normal renal function of approximately 3 to 4 hours. Following t.i.d. administration (q.8H), no significant accumulation of Pindolol is observed.

In elderly hypertensive patients with normal renal function, the half-life of Pindolol is more variable, averaging about 7 hours, but with values as high as 15 hours.

In hypertensive patients with renal diseases, the half-life is within the range expected for healthy subjects. However, a significant decrease (50%) in volume of distribution (VD) is observed in uremic patients and VD  appears to be directly correlated to creatinine clearance. Therefore, renal drug clearance is significantly reduced in uremic patients, resulting in a significant decrease in urinary excretion of unchanged drug. Uremic patients with a creatinine clearance of less than 20 mL/min generally excreted less than 15% of the administered dose unchanged in the urine.

In patients with histologically diagnosed cirrhosis of the liver, the elimination of Pindolol was more variable in rate and generally significantly slower than in healthy subjects. The total body clearance of Pindolol in cirrhotic patients ranged from about 50 to 300 mL/min and was directly correlated to antipyrine clearance. The half-life ranges from 2.5 hours to greater than 30 hours. These findings strongly suggest that caution should be exercised in dosage adjustments of Pindolol in such patients.

The bioavailability of Pindolol is not significantly affected by coadministration of food, hydralazine, hydrochlorothiazide or aspirin. Pindolol has no effect on warfarin activity or the clinical effectiveness of digoxin, although small transient decreases in plasma digoxin concentrations were noted.

Indications and Usage for Pindolol

Pindolol tablets are indicated in the management of hypertension. It may be used alone or concomitantly with other antihypertensive agents, particularly with a thiazide-type diuretic.

Contraindications

Pindolol tablets are contraindicated in: 1) bronchial asthma; 2) overt cardiac failure; 3) cardiogenic shock; 4) second and third degree heart block; 5) severe bradycardia. (See WARNINGS.)

Warnings

Cardiac Failure

Sympathetic stimulation may be a vital component supporting circulatory function in patients with congestive heart failure, and its inhibition by beta-blockade may precipitate more severe failure. Although beta-blockers should be avoided in overt congestive heart failure, if necessary, Pindolol can be used with caution in patients with a history of failure who are well-compensated, usually with digitalis and diuretics. Both digitalis

glycosides and beta-blockers slow atrioventricular conduction and decrease heart rate. Concomitant use can increase risk of bradycardia. Beta-adrenergic blocking agents do not abolish the inotropic action of digitalis on heart muscle.

In Patients Without A History of Cardiac Failure

In patients with latent cardiac insufficiency, continued depression of the myocardium with beta-blocking agents over a period of time can in some cases lead to cardiac failure. At the first sign or symptom of impending cardiac failure, patients should be fully digitalized and/or be given a diuretic, and the response observed closely. If cardiac failure continues, despite adequate digitalization and diuretic, Pindolol therapy should be withdrawn (gradually, if possible).

Exacerbation of Ischemic Heart Disease Following Abrupt Withdrawal

Hypersensitivity to catecholamines has been observed in patients withdrawn from beta-blocker therapy; exacerbation of angina and, in some cases, myocardial infarction have occurred after abrupt discontinuation of such therapy. When discontinuing chronically administered Pindolol, particularly in patients with ischemic heart disease, the dosage should be gradually reduced over a period of 1 to 2 weeks and the patient should be carefully monitored. If angina markedly worsens or acute coronary insufficiency develops, Pindolol administration should be reinstituted promptly, at least temporarily, and other measures appropriate for the management of unstable angina should be taken. Patients should be warned against interruption or discontinuation of therapy without the physician’s advice. Because coronary artery disease is common and may be unrecognized, it may be prudent not to discontinue Pindolol therapy abruptly even in patients treated only for hypertension.

Nonallergic Bronchospasm (e.g., chronic bronchitis, emphysema) - Patients with Bronchospastic Diseases Should in General Not Receive Beta-Blockers

Pindolol should be administered with caution since it may block bronchodilation produced by endogenous or exogenous catecholamine stimulation of beta2 receptors.

Major Surgery

Because beta-blockade impairs the ability of the heart to respond to reflex stimuli and may increase the risks of general anesthesia and surgical procedures, resulting in protracted hypotension or low cardiac output, it has generally been suggested that such therapy should be gradually withdrawn several days prior to surgery. Recognition of the increased sensitivity to catecholamines of patients recently withdrawn from beta-blocker therapy, however, has made this recommendation controversial. If possible, beta-blockers should be withdrawn well before surgery takes place. In the event of emergency surgery, the anesthesiologist should be informed that the patient is on beta-blocker therapy.

The effects of Pindolol can be reversed by administration of beta-receptor agonists such as isoproterenol, dopamine, dobutamine, or norepinephrine. Difficulty in restarting and maintaining the heart beat has also been reported with beta-adrenergic receptor blocking agents.

Diabetes and Hypoglycemia

Beta-adrenergic blockade may prevent the appearance of premonitory signs and symptoms (e.g., tachycardia and blood pressure changes) of acute hypoglycemia. This is especially important with labile diabetics. Beta-blockade also reduces the release of insulin in response to hyperglycemia; therefore, it may be necessary to adjust the dose of antidiabetic drugs.

Thyrotoxicosis

Beta-adrenergic blockade may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism. Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-blockade which might precipitate a thyroid crisis.

Precautions

Impaired Renal or Hepatic Function

Beta-blocking agents should be used with caution in patients with impaired hepatic or renal function. Poor renal function has only minor effects on Pindolol clearance, but poor hepatic function may cause blood levels of Pindolol to increase substantially.

Information for Patients

Patients, especially those with evidence of coronary artery insufficiency, should be warned against interruption or discontinuation of Pindolol therapy without the physician’s advice. Although cardiac failure rarely occurs in properly selected patients, patients being treated with beta-adrenergic blocking agents should be advised to consult the physician at the first sign or symptom of impending failure.

Drug Interactions

Catecholamine-depleting drugs (e.g., reserpine) may have an additive effect when given with beta-blocking agents. Patients receiving Pindolol plus a catecholamine-depleting agent should, therefore, be closely observed for evidence of hypotension and/or marked bradycardia which may produce vertigo, syncope, or postural hypotension.

Pindolol has been used with a variety of antihypertensive agents, including hydrochlorothiazide, hydralazine, and guanethidine without unexpected adverse interactions.

Pindolol has been shown to increase serum thioridazine levels when both drugs are coadministered. Pindolol levels may also be increased with this combination.

Risk of Anaphylactic Reaction

While taking beta blockers, patients with a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic, or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reactions.

Carcinogenesis, Mutagenesis, Impairment of Fertility

In chronic oral toxicologic studies (1 to 2 years) in mice, rats, and dogs, Pindolol did not produce any significant toxic effects. In 2-year oral carcinogenicity studies in rats and mice in doses as high as 59 mg/kg/day and 124 mg/kg/day (50 and 100 times the maximum recommended human dose), respectively, Pindolol did not produce any neoplastic, preneoplastic, or nonneoplastic pathologic lesions. In fertility and general reproductive performance studies in rats, Pindolol caused no adverse effects at a dose of 10 mg/kg.

In the male fertility and general reproductive performance test in rats, definite toxicity characterized by mortality and decreased weight gain was observed in the group given 100 mg/kg/day. At 30 mg/kg/day, decreased mating was associated with testicular atrophy and/or decreased spermatogenesis. This response is not clearly drug-related, however, as there was no dose-response relationship within this experiment and no similar effect on testes of rats administered Pindolol as a dietary admixture for 104 weeks. There appeared to be an increase in prenatal mortality in males given 100 mg/kg but development of offspring was not impaired.

In females administered Pindolol prior to mating through day 21 of lactation, mating behavior was decreased at 100 mg/kg and 30 mg/kg. At these dosages there also was increased mortality of offspring. Prenatal mortality was increased at 10 mg/kg but there was not a clear dose-response relationship in this experiment. There was an increased resorption rate at 100 mg/kg observed in females necropsied on the 15th day of gestation.

Pregnancy

Teratogenic Effects. Category B

Studies in rats and rabbits exceeding 100 times the maximum recommended human doses, revealed no embryotoxicity or teratogenicity. Since there are no adequate and well controlled studies in pregnant women, and since animal reproduction studies are not always predictive of human response, Pindolol, as with any drug, should be employed during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers

Since Pindolol is secreted in human milk, nursing should not be undertaken by mothers receiving the drug.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

CLINICAL LABORATORY

Minor persistent elevations in serum transaminases (SGOT, SGPT) have been noted in 7% of patients during Pindolol administration, but progressive elevations were not observed. These elevations were not associated with any other abnormalities that would suggest hepatic impairment, such as decreased serum albumin and total proteins. During more than a decade of worldwide marketing, there have been no reports in the medical literature of overt hepatic injury. Alkaline phosphatase, lactic acid dehydrogenase (LDH), and uric acid are also elevated on rare occasions. The significance of these findings is unknown.

Adverse Reactions

Most adverse reactions have been mild. The incidences listed in the following table are derived from 12-week comparative double-blind, parallel design trials in hypertensive patients given Pindolol as monotherapy, given various active control drugs as monotherapy, or given placebo. Data for Pindolol and the positive controls were pooled from several trials because no striking differences were seen in the individual studies, with one exception. When considering all adverse reactions reported, the frequency of edema was noticeably higher in positive control trials (16% Pindolol vs. 9% positive control) than in placebo controlled trials (6% Pindolol vs. 3% placebo). The table includes adverse reactions either volunteered or elicited, and at least possibly drug-related, which were reported in greater than 2% of Pindolol patients and other selected important reactions.

ADVERSE REACTIONS WHICH WERE VOLUNTEERED OR ELICITED

* Active Controls: Patients received either propranolol, α-methyldopa or a diuretic (hydrochlorothiazide or chlorthalidone).
(and at least possibly drug-related)
	Pindolol (N = 322) %
Body System/      Adverse Reactions
Central Nervous System
Bizarre or Many Dreams	5
Dizziness	9
Fatigue	8
Hallucinations	< 1
Insomnia	10
Nervousness	7
Weakness	4
Autonomic Nervous System
Paresthesia	3
Cardiovascular
Dyspnea	5
Edema	6
Heart Failure	< 1
Palpitations	< 1
Musculoskeletal
Chest Pain	3
Joint Pain	7
Muscle Cramps	3
Muscle Pain	10
Gastrointestinal
Abdominal Discomfort	4
Nausea	5
Skin
Pruritus	1
Rash	< 1
	Active Controls* (N = 188) %
Body System/      Adverse Reactions
Central Nervous System
Bizarre or Many Dreams	0
Dizziness	11
Fatigue	4
Hallucinations	0
Insomnia	3
Nervousness	3
Weakness	2
Autonomic Nervous System
Paresthesia	1
Cardiovascular
Dyspnea	4
Edema	3
Heart Failure	< 1
Palpitations	1
Musculoskeletal
Chest Pain	1
Joint Pain	4
Muscle Cramps	1
Muscle Pain	9
Gastrointestinal
Abdominal Discomfort	4
Nausea	2
Skin
Pruritus	< 1
Rash	< 1
	Placebo (N = 78) %
Body System/      Adverse Reactions
Central Nervous System
Bizarre or Many Dreams	6
Dizziness	1
Fatigue	4
Hallucinations	0
Insomnia	10
Nervousness	5
Weakness	1
Autonomic Nervous System
Paresthesia	6
Cardiovascular
Dyspnea	6
Edema	1
Heart Failure	0
Palpitations	0
Musculoskeletal
Chest Pain	3
Joint Pain	4
Muscle Cramps	0
Muscle Pain	8
Gastrointestinal
Abdominal Discomfort	5
Nausea	1
Skin
Pruritus	0
Rash	1

The following selected (potentially important) adverse reactions were seen in 2% or fewer patients and their relationship to Pindolol is uncertain. CENTRAL NERVOUS SYSTEM: anxiety, lethargy; AUTONOMIC NERVOUS SYSTEM: visual disturbances, hyperhidrosis; CARDIOVASCULAR: bradycardia, claudication, cold extremities, heart block, hypotension, syncope, tachycardia, weight gain; GASTROINTESTINAL: diarrhea, vomiting; RESPIRATORY: wheezing; UROGENITAL: impotence, pollakiuria; MISCELLANEOUS: eye discomfort or burning eyes.

POTENTIAL ADVERSE EFFECTS

In addition, other adverse effects not aforementioned have been reported with other beta-adrenergic blocking agents and should be considered potential adverse effects of Pindolol.

Central Nervous System: Reversible mental depression progressing to catatonia; an acute reversible syndrome characterized by disorientation for time and place, short-term memory loss, emotional lability, slightly clouded sensorium, and decreased performance on neuropsychometrics.

Cardiovascular: Intensification of AV block. (See CONTRAINDICATIONS.)

Allergic: Erythematous rash; fever combined with aching and sore throat; laryngospasm; respiratory distress.

Hematologic: Agranulocytosis; thrombocytopenic and nonthrombocytopenic purpura.

Gastrointestinal: Mesenteric arterial thrombosis; ischemic colitis.

Miscellaneous: Reversible alopecia; Peyronie’s disease.

The oculomucocutaneous syndrome associated with the beta-blocker practolol has not been reported with Pindolol during investigational use and extensive foreign experience amounting to over 4 million patient-years.

Overdosage

No specific information on emergency treatment of overdosage is available. Therefore, on the basis of the pharmacologic actions of Pindolol, the following general measures should be employed as appropriate in addition to gastric lavage:

Excessive Bradycardia: administer atropine; if there is no response to vagal blockade, administer isoproterenol cautiously.

Cardiac Failure: digitalize the patient and/or administer diuretic. It has been reported that glucagon may be useful in this situation.

Hypotension: administer vasopressors, e.g., epinephrine or levarterenol, with serial monitoring of blood pressure. (There is evidence that epinephrine may be the drug of choice.)

Bronchospasm: administer a beta2 stimulating agent such as isoproterenol and/or a theophylline derivative.

A case of an acute overdosage has been reported with an intake of 500 mg of Pindolol by a hypertensive patient. Blood pressure increased and heart rate was ≥ 80 beats/min. Recovery was uneventful. In another case, 250 mg of Pindolol was taken with 150 mg diazepam and 50 mg nitrazepam, producing coma and hypotension. The patient recovered in 24 hours.

Pindolol Dosage and Administration

The dosage of Pindolol tablets should be individualized. The recommended initial dose of Pindolol tablets is 5 mg b.i.d. alone or in combination with other antihypertensive agents. An antihypertensive response usually occurs within the first week of treatment. Maximal response, however, may take as long as or occasionally longer than 2 weeks. If a satisfactory reduction in blood pressure does not occur within 3 to 4 weeks, the dose may be adjusted in increments of 10 mg/day at these intervals up to a maximum of 60 mg/day.

How is Pindolol Supplied

Pindolol Tablets, USP are available as 5 mg and 10 mg tablets.

The 5 mg tablets are white round scored tablets debossed with M above the score and 52 below the score on one side of the tablet and blank on the other side. They are available as follows:

NDC 0378-0052-01

bottles of 100 tablets

The 10 mg tablets are white round scored tablets debossed with M above the score and 127 below the score on one side of the tablet and blank on the other side. They are available as follows:

NDC 0378-0127-01

bottles of 100 tablets

Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]

Protect from light.

Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

Mylan Pharmaceuticals Inc.

Morgantown, WV 26505

REVISED JUNE 2010

PIND:R7

PRINCIPAL DISPLAY PANEL - 5 mg

NDC 0378-0052-01

Pindolol

TABLETS, USP

5 mg

100 TABLETS (Rx only)

Each tablet contains:

Pindolol, USP . . . . . 5 mg

Dispense in a tight, light-resistant

container as defined in the USP

using a child-resistant closure.

Keep container tightly closed.

Keep this and all medication

out of the reach of children.

Store at 20° to 25°C (68° to 77°F).

[See USP Controlled Room

Temperature.]

Protect from light.

Usual Adult Dosage: One tablet

twice daily. See accompanying

prescribing information.

Mylan Pharmaceuticals Inc.

Morgantown, WV 26505

RM0052A4

PRINCIPAL DISPLAY PANEL - 10 mg

NDC 0378-0127-01

Pindolol

TABLETS, USP

10 mg

100 TABLETS (Rx only)

Each tablet contains:

Pindolol, USP . . . . . 10 mg

Dispense in a tight, light-resistant

container as defined in the USP

using a child-resistant closure.

Keep container tightly closed.

Keep this and all medication

out of the reach of children.

Store at 20° to 25°C (68° to 77°F).

[See USP Controlled Room

Temperature.]

Protect from light.

Usual Adult Dosage: One tablet

twice daily. See accompanying

prescribing information.

Mylan Pharmaceuticals Inc.

Morgantown, WV 26505

RM0127A4

Pindolol  Pindolol  tablet

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0378-0052 Route of Administration ORAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength Pindolol (Pindolol) Pindolol 5 mg

Inactive Ingredients Ingredient Name Strength SILICON DIOXIDE   CROSCARMELLOSE SODIUM   MAGNESIUM STEARATE   CELLULOSE, MICROCRYSTALLINE   STARCH, CORN   SODIUM LAURYL SULFATE

Product Characteristics Color WHITE Score 2 pieces Shape ROUND Size 6mm Flavor Imprint Code M;52 Contains

Packaging # NDC Package Description Multilevel Packaging 1 0378-0052-01 100 TABLET In 1 BOTTLE, PLASTIC None

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
ANDA	ANDA074019	07/22/2010

Pindolol  Pindolol  tablet

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0378-0127 Route of Administration ORAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength Pindolol (Pindolol) Pindolol 10 mg

Inactive Ingredients Ingredient Name Strength SILICON DIOXIDE   CROSCARMELLOSE SODIUM   MAGNESIUM STEARATE   CELLULOSE, MICROCRYSTALLINE   STARCH, CORN   SODIUM LAURYL SULFATE

Product Characteristics Color WHITE Score 2 pieces Shape ROUND Size 8mm Flavor Imprint Code M;127 Contains

Packaging # NDC Package Description Multilevel Packaging 1 0378-0127-01 100 TABLET In 1 BOTTLE, PLASTIC None

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
ANDA	ANDA074019	07/22/2010

Labeler - Mylan Pharmaceuticals Inc. (059295980)

Registrant - Mylan Pharmaceuticals Inc. (059295980)

Revised: 06/2010Mylan Pharmaceuticals Inc.

More Pindolol resources

• Pindolol Side Effects (in more detail)
• Pindolol Dosage
• Pindolol Use in Pregnancy & Breastfeeding
• Drug Images
• Pindolol Drug Interactions
• Pindolol Support Group
• 0 Reviews for Pindolol - Add your own review/rating

Lexiva

Generic Name: fosamprenavir (FOS am pren a veer)

Brand Names: Lexiva

What is fosamprenavir?

Fosamprenavir is an antiviral medication in a group of HIV medicines called protease (PRO-tee-ayz) inhibitors. Fosamprenavir prevents human immunodeficiency virus (HIV) cells from multiplying in your body.

Fosamprenavir is used to treat HIV, which causes acquired immunodeficiency syndrome (AIDS). Fosamprenavir is not a cure for HIV or AIDS.

Fosamprenavir may also be used for purposes not listed in this medication guide.

What is the most important information I should know about fosamprenavir?

Do not take fosamprenavir with cisapride (Propulsid), pimozide (Orap), midazolam (Versed), triazolam (Halcion), or an ergot medicine such as Ergomar, Cafergot, Wigraine, D.H.E. 45, Migranal, Methergine, and others. Fosamprenavir should not be taken together with ritonavir (Norvir) if you are also using a heart rhythm medication called flecainide (Tambocor) or propafenone (Rythmol). Ask your doctor about taking a different medication for your heart rhythm disorder. These drugs can cause life-threatening side effects if you use them while you are taking fosamprenavir.

There are many other medicines that can cause serious interactions if you use them while taking fosamprenavir. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors.

HIV/AIDS is usually treated with a combination of different drugs. To best treat your condition, use all of your medications as directed by your doctor. Do not change your doses or medication schedule without advice from your doctor.

Avoid having unprotected sex or sharing needles, razors, or toothbrushes. Taking this medication will not prevent you from passing HIV to other people. Talk with your doctor about safe methods of preventing HIV transmission during sex.

What should I discuss with my healthcare provider before taking fosamprenavir?

Do not take this medication if you are allergic to fosamprenavir or a similar drug called amprenavir (Agenerase).

Do not take fosamprenavir together with cisapride (Propulsid), pimozide (Orap), midazolam (Versed), triazolam (Halcion), or ergot medicines such as ergotamine (Ergomar, Cafergot), dihydroergotamine (D.H.E. 45, Migranal Nasal Spray), ergonovine (Ergotrate), or methylergonovine (Methergine). Fosamprenavir should not be taken together with ritonavir (Norvir) if you are also using a heart rhythm medication called flecainide (Tambocor) or propafenone (Rythmol). Ask your doctor about taking a different medication for your heart rhythm disorder. These drugs can cause life-threatening side effects if you use them while you are taking fosamprenavir.

To make sure you can safely take fosamprenavir, tell your doctor if you have any of these other conditions:

• liver disease;


• kidney disease;


• 
  

  diabetes;

  
  


• 
  

  a bleeding disorder such as hemophilia;

  
  


• 
  

  heart disease, history of heart attack;

  
  


• 
  

  high cholesterol or triglycerides; or

  
  


• 
  

  if you have ever used a protease inhibitor in the past.

  
  

FDA pregnancy category C. It is not known whether fosamprenavir will harm an unborn baby. Tell your doctor if you are pregnant. HIV can be passed to your baby if you are not properly treated during pregnancy. Take all of your HIV medicines as directed to control your infection.

Your name may need to be listed on an antiviral pregnancy registry when you start using this medication.

Taking fosamprenavir together with another HIV medicine called ritonavir (Norvir) and also using birth control pills can increase you risk of liver problems. Ask your doctor about using a non-hormone method of birth control (such as a condom, diaphragm, spermicide) to prevent pregnancy while taking fosamprenavir and ritonavir. Women with HIV or AIDS should not breast-feed a baby. Even if your baby is born without HIV, the virus may be passed to the baby in your breast milk.

How should I take fosamprenavir?

Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Fosamprenavir tablets can be taken with or without food.

Fosamprenavir liquid should be taken with food in children and without food in adults.

Shake the oral suspension (liquid) well just before you measure a dose. Measure the liquid with a special dose-measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

Use fosamprenavir regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.

To be sure this medicine is helping your condition and is not causing harmful effects, your blood will need to be tested often. Your liver function may also need to be tested. Visit your doctor regularly.

HIV/AIDS is usually treated with a combination of drugs. Use all medications as directed by your doctor. Read the medication guide or patient instructions provided with each medication. Do not change your doses or medication schedule without your doctor's advice. Every person with HIV or AIDS should remain under the care of a doctor.

Store fosamprenavir tablets at room temperature away from moisture and heat. You may store fosamprenavir liquid in the refrigerator but do not allow it to freeze.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking fosamprenavir?

Taking this medication will not prevent you from passing HIV to other people. Avoid having unprotected sex or sharing razors or toothbrushes. Talk with your doctor about safe ways to prevent HIV transmission during sex. Sharing drug or medicine needles is never safe, even for a healthy person.

Fosamprenavir side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop taking fosamprenavir and call your doctor at once if you have any of these serious side effects:

• 
  

  chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, general ill feeling;

  
  


• 
  

  pale or yellowed skin, dark colored urine, fever, confusion or weakness;

  
  


• 
  

  increased urination or extreme thirst;

  
  


• 
  

  sudden and severe pain in your lower back or side, blood in your urine, pain or burning when you urinate;

  
  


• 
  

  signs of a new infection, such as fever or chills, cough, or flu symptoms;

  
  


• 
  

  easy bruising or bleeding; or

  
  


• 
  

  fever, sore throat, and headache with a severe blistering, peeling, and red skin rash.

  
  

Less serious side effects of fosamprenavir may include:

• 
  

  mild nausea, vomiting, diarrhea, stomach pain;

  
  


• 
  

  numbness or tingling, especially around your mouth;

  
  


• 
  

  headache, mood changes; or

  
  


• 
  

  changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist).

  
  

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect fosamprenavir?

Many other drugs can cause serious or life-threatening drug interactions if you use them while taking fosamprenavir. Tell your doctor if you are also using:

• 
  

  itraconazole (Sporanox) or ketoconazole (Nizoral);

  
  


• 
  

  heart rhythm medicine such as amiodarone (Cordarone, Pacerone), lidocaine, or quinidine (Quin-G);

  
  


• 
  

  an antidepressant such as amitriptyline (Elavil, Vanatrip, Limbitrol), imipramine (Janimine, Tofranil), or paroxetine (Paxil);

  
  


• 
  

  rifampin (Rifadin, Rimactane, Rifater);

  
  


• 
  

  steroid medicine such as dexamethasone (Cortastat, Dexasone, Solurex, DexPak) or fluticasone (Advair, Flonase, Flovent);

  
  


• 
  

  St. John's wort;

  
  


• 
  

  a blood thinner such as warfarin (Coumadin, Jantoven);

  
  


• 
  

  heart or blood pressure medicine such as amlodipine (Norvasc, Caduet, Exforge, Lotrel, Tekamlo, Tribenzor, Twynsta, Amturnide), diltiazem (Cartia, Cardizem), nifedipine (Nifedical, Procardia), verapamil (Calan, Covera, Isoptin, Verelan), and others;

  
  


• 
  

  cholesterol-lowering medicine such as atorvastatin (Lipitor, Caduet), lovastatin (Mevacor, Altoprev, Advicor), simvastatin (Zocor, Simcor, Vytorin);

  
  


• 
  

  drugs that weaken the immune system, such as cyclosporine (Gengraf, Neoral, Sandimmune), sirolimus (Rapamune), or tacrolimus (Prograf);

  
  


• 
  

  other HIV /AIDS medicine such as delavirdine (Rescriptor), efavirenz (Sustiva, Atripla), nevirapine (Viramune), lopinavir/ritonavir (Kaletra), or raltegravir (Isentress);

  
  


• 
  

  insulin or diabetes medication you take by mouth;

  
  


• 
  

  medicines to treat erectile dysfunction, such as sildenafil (Viagra), tadalafil (Cialis), or vardenafil (Levitra);

  
  


• 
  

  seizure medications such as carbamazepine (Carbatrol, Equetro, Tegretol), phenobarbital (Luminal, Solfoton), or phenytoin (Dilantin); or

  
  


• 
  

  stomach acid reducers such as cimetidine (Tagamet), famotidine (Pepcid), nizatidine (Axid), or ranitidine (Zantac).

  
  

This list is not complete and there are many other drugs that can interact with fosamprenavir. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor. Keep a list of all your medicines and show it to any healthcare provider who treats you.

More Lexiva resources

• Lexiva Side Effects (in more detail)
• Lexiva Use in Pregnancy & Breastfeeding
• Drug Images
• Lexiva Drug Interactions
• Lexiva Support Group
• 0 Reviews for Lexiva - Add your own review/rating

• Lexiva Prescribing Information (FDA)


• Lexiva Monograph (AHFS DI)


• Lexiva Advanced Consumer (Micromedex) - Includes Dosage Information


• Lexiva MedFacts Consumer Leaflet (Wolters Kluwer)


• Lexiva Consumer Overview

Compare Lexiva with other medications

• HIV Infection
• Nonoccupational Exposure

Where can I get more information?

• Your pharmacist can provide more information about fosamprenavir.

See also: Lexiva side effects (in more detail)

Isoramycin

Isoramycin may be available in the countries listed below.

Ingredient matches for Isoramycin

Fosfomycin

Fosfomycin is reported as an ingredient of Isoramycin in the following countries:

• Japan

International Drug Name Search

Seconal

Pronunciation: SEE-koe-BAR-bi-tahl
Generic Name: Secobarbital
Brand Name: Seconal

Seconal is used for:

Treating sleep disorders. It may also be used as a sedative prior to anesthesia for surgery.

Seconal is a barbiturate. It works by depressing the central nervous system, causing mild sedation or sleep, depending on the dose.

Do NOT use Seconal if:

• you are allergic to any ingredient in Seconal


• you have the blood disease porphyria or moderate to severe liver or lung problems


• you are taking sodium oxybate (GHB)

Contact your doctor or health care provider right away if any of these apply to you.

Video: Treatment for Depression

Treatments for depression are getting better everyday and there are things you can start doing right away.

Before using Seconal:

Some medical conditions may interact with Seconal. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances


• if you have liver problems, lung or respiratory tract disease, or a painful condition


• if you have a history of substance abuse or dependence, depression, or suicidal thoughts or behavior

Some MEDICINES MAY INTERACT with Seconal. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Monoamine oxidase inhibitors (MAOIs) (eg, phenelzine) or sodium oxybate (GHB) because they may increase the risk of Seconal's side effects


• Anticoagulants (eg, warfarin), beta-blockers (eg, atenolol), clozapine, corticosteroids (eg, prednisone), doxycycline, estrogens (eg, micronized estradiol), griseofulvin, metronidazole, oral contraceptives (birth control pills), phenytoin, quinidine, stiripentol, theophylline, or valproic acid because their effectiveness may be decreased by Seconal

This may not be a complete list of all interactions that may occur. Ask your health care provider if Seconal may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Seconal:

Use Seconal as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Seconal by mouth with or without food.


• If you miss a dose of Seconal and you are taking it regularly, take it as soon as possible. If several hours have passed or if it is nearing time for the next dose, do not double the dose to catch up, unless advised by your health care provider. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Seconal.

Important safety information:

• Seconal may cause drowsiness. This effect may be worse if you take it with alcohol or certain medicines. Use Seconal with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.


• Do not drink alcohol while you are taking Seconal.


• Check with your doctor before you take other medicine that may cause drowsiness (eg, sleep aids, muscle relaxers) while you are using Seconal; it may add to their effects. Ask your pharmacist if you have questions about which medicine may cause drowsiness.


• Do not take more than the recommended dose or take Seconal for longer than prescribed without checking with your doctor. Exceeding the recommended dose or taking Seconal for longer than prescribed may be habit-forming.


• Some patients taking Seconal have performed certain activities while they were not fully awake. These have included sleep-driving, making and eating food, making phone calls, and having sex. Patients often do not remember these events after they happen. Such an event may be more likely to occur if you use a high dose of Seconal. It may also be more likely if you drink alcohol or take other medicine that may cause drowsiness while you use Seconal. Tell your doctor right away if such an event happens to you.


• Before you have any medical or dental treatments, emergency care, or surgery, tell the doctor or dentist that you are using Seconal.


• Seconal may decrease the effectiveness of your birth control pill. To prevent pregnancy, be sure to use an additional form of birth control while using Seconal.


• Lab tests, including complete blood cell counts and kidney and liver function tests, may be performed while you use Seconal. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.


• Use Seconal with caution in the ELDERLY; they may be more sensitive to its effects, especially drowsiness, depression, or confusion.


• PREGNANCY and BREAST-FEEDING: If you think you may be pregnant, contact your doctor. You will need to discuss the benefits and risks of using Seconal while you are pregnant. Seconal is found in breast milk. If you are or will be breast-feeding while you use Seconal, check with your doctor. Discuss any possible risks to your baby.

When sleep medicines are used every night for more than a few weeks, they may lose their effectiveness to help you sleep. This is known as TOLERANCE. Sleep medicines should usually be used only for short periods of time, such as a few days and generally no longer than 1 or 2 weeks. If your sleep problems continue, contact your doctor.

When used for longer than a few weeks or at high doses, some people develop a need to continue taking Seconal. This is known as DEPENDENCE or addiction. If you suddenly stop taking Seconal, you may experience WITHDRAWAL symptoms, including anxiety, muscle twitching, trembling hands and fingers, weakness, dizziness, hallucinations, nausea, vomiting, sleeplessness, lightheadedness, or seizures.

Possible side effects of Seconal:

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Clumsiness; dizziness; excessive daytime drowsiness; lightheadedness.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); confusion; difficulty sleeping; fainting; fever; hallucinations; severe dizziness; trouble sleeping; unusual behavior; very slow breathing.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

See also: Seconal side effects (in more detail)

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include change in size of pupil; cold, clammy skin; deep sleep; incoordination; loss of consciousness; slowed or fast breathing; slurred speech; trouble walking; unusual eye movements.

Proper storage of Seconal:

Store Seconal at room temperature, between 59 and 86 degrees F (15 and 30 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Seconal out of the reach of children and away from pets.

General information:

• If you have any questions about Seconal, please talk with your doctor, pharmacist, or other health care provider.


• Seconal is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Seconal. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Seconal resources

• Seconal Side Effects (in more detail)
• Seconal Use in Pregnancy & Breastfeeding
• Seconal Drug Interactions
• Seconal Support Group
• 0 Reviews for Seconal - Add your own review/rating

Compare Seconal with other medications

• Insomnia
• Light Sedation
• Sedation