Alphagan P

Generic Name: brimonidine (Ophthalmic route)

bri-MOE-ni-deen

Commonly used brand name(s)

In the U.S.

• Alphagan P

Available Dosage Forms:

• Solution

Therapeutic Class: Antiglaucoma

Pharmacologic Class: Alpha-2 Adrenergic Agonist

Uses For Alphagan P

Brimonidine ophthalmic (eye) drops is used alone or together with other medicines to treat increased pressure in the eye that is caused by open-angle glaucoma or a condition called hypertension of the eye (ocular hypertension). This medicine is an alpha-adrenergic agonist.

This medicine is available only with your doctor's prescription.

Before Using Alphagan P

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of brimonidine eye drops in children 2 years of age and older. Because of brimonidine's toxicity, use in children younger than 2 years of age is not recommended.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of brimonidine eye drops in the elderly.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	B	Animal studies have revealed no evidence of harm to the fetus, however, there are no adequate studies in pregnant women OR animal studies have shown an adverse effect, but adequate studies in pregnant women have failed to demonstrate a risk to the fetus.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Depression or


• Heart attack, history of or


• Heart disease or


• Orthostatic hypotension (low blood pressure when standing up) or


• Raynaud disease (blood vessel disease) or


• Stroke, history of or


• Thromboangiitis obliterans (blood vessel disease)—Use with caution. May make these conditions worse.

Proper Use of Alphagan P

Use this medicine only as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered.

If your doctor ordered two different eye drops to be used together, wait at least 5 minutes after you put the first medicine in your eye to use the second medicine. This will prevent the second medicine from “washing out” the first one.

To use the eye drops:

• Wash your hands with soap and water before and after using this medicine.


• Shake the eye drops well just before each use.


• Tilt your head back and press your finger gently on the skin just beneath the lower eyelid. Pull the lower eyelid away from the eye to make a space. Drop the medicine into this space. Let go of the eyelid and gently close the eyes. Do not blink. Keep the eyes closed and apply pressure to the inner corner of the eye with your finger for 1 or 2 minutes to allow the medicine to be absorbed by the eye.


• If you think you did not get the drop of medicine into your eye properly, repeat the directions with a second drop.


• To keep the medicine as germ-free as possible, do not touch the applicator tip to any surface, including the eye. Keep the container tightly closed when you are not using the drops.


• If germs get in the bottle, your eye could become infected. Serious eye infections can cause blindness.


• The eye drops will normally be a clear liquid with a greenish-yellow color. If the color changes or the liquid becomes cloudy, do not use the medicine. Get a new bottle from the pharmacy.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For ophthalmic dosage form (eye drops):
  
  • For glaucoma or ocular hypertension:
    
    • Adults, teenagers, and children 2 years of age and older—One drop in the affected eye 3 times a day, about 8 hours apart.
    
    
    • Children younger than 2 years of age—Use is not recommended.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, apply it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using Alphagan P

The eye doctor will want to examine your or your child's eyes at regular visits to make sure the medicine is working properly and is not causing unwanted effects.

If itching, redness, swelling, or other signs of eye or eyelid irritation occur, stop using this medicine and check with your doctor. These symptoms may mean that you or your child are allergic to this medicine.

If you or your child have an eye injury or infection, or need to have eye surgery, talk with your doctor right away. You may need to change the medicine or stop using it.

This medicine may cause some people to become lightheaded, dizzy, drowsy, tired, or less alert than they are normally. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous if you are not alert.

This medicine may add to the effects of alcohol and other CNS depressants (medicines that make you drowsy or less alert). Some examples of CNS depressants are antihistamines or medicines for allergies; sedatives or sleeping medicine; prescription pain medicine or narcotics; medicine for seizures or barbiturates; muscle relaxants; or anesthetics, including some dental anesthetics. Check with your doctor before taking any of the above while you are using this medicine.

Brimonidine may cause your eyes to become more sensitive to light than they are normally. Wearing sunglasses and avoiding too much exposure to bright light may help lessen the discomfort.

Alphagan P Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

• Blurred or loss of vision


• burning, dry, or itching eyes


• discharge or excessive tearing


• disturbed color perception


• double vision


• halos around lights


• headache


• itching of the eye


• night blindness


• overbright appearance of lights


• redness of the eye or inner lining of the eyelid


• swelling of the eyelid


• tearing of the eye


• tunnel vision

Less common

• Ache or pain in the eye


• blindness


• bloody eye


• blurred vision or other change in vision


• change in color vision


• confusion


• decreased vision


• difficult or labored breathing


• difficulty seeing at night


• dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position


• drainage from the eye


• fainting


• fast heartbeat


• feeling of something in the eye


• gradual blurring or loss of vision


• increased blood pressure


• increased sensitivity of the eye to light


• mental depression


• muscle pain


• nausea or vomiting


• oozing in the eye


• redness, swelling, or itching of the eye or eyelid


• runny or stuffy nose


• seeing flashes or sparks of light


• seeing floating dark spots or material before eyes


• seeing floating spots before the eyes or a veil or curtain appearing across part of vision


• shortness of breath


• skin rash


• sneezing


• sweating


• swelling of the eye


• tightness in the chest


• unusual tiredness or weakness


• watery eyes


• wheezing

Incidence not known

• Bluish lips or skin


• chest pain or discomfort


• confusion


• fast, pounding, or irregular heartbeat or pulse


• feeling of warmth or heat


• flushing or redness of the skin, especially on the face and neck


• irregular, fast, slow, or shallow breathing


• low body temperature


• muscle aches or weakness


• shivering


• slow or irregular heartbeat


• weak or feeble pulse


• weight gain

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Burning, stinging, or tearing of the eye


• drowsiness or tiredness


• dryness of the mouth

Less common

• Acid or sour stomach


• anxiety


• bad, unusual, or unpleasant (after) taste


• belching


• body aches or pain


• change in taste


• chills


• congestion


• cough


• cough producing mucus


• crusting on eyelid or corner of eye


• diarrhea


• difficulty breathing


• discoloration of white part of the eye


• dryness of the eye


• dryness or soreness of the throat


• fever


• general feeling of discomfort or illness


• hoarseness


• indigestion


• joint pain


• lack or loss of strength


• large amounts of cholesterol in the blood


• lid disorder


• loss of appetite


• muscle aches and pains


• pain or tenderness around the eyes and cheekbones


• paleness of the eye or inner lining of the eyelid


• passing of gas


• pounding heartbeat


• rash


• shivering


• sleepiness or unusual drowsiness


• sleeplessness


• sneezing


• sore throat


• stomach discomfort, fullness, upset, or pain


• tender, swollen glands in the neck


• trouble with sleeping


• trouble with swallowing


• troubled breathing


• unable to sleep


• voice changes

Incidence not known

• Constricted, pinpoint, or small pupils (black part of the eye)


• redness of the skin


• sensitivity to light


• throbbing pain


• unusual drowsiness, dullness, tiredness, weakness, or feeling of sluggishness


• unusual weak feeling


• unusually warm skin

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Alphagan P side effects (in more detail)

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More Alphagan P resources

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

• Alphagan P Prescribing Information (FDA)


• Alphagan P Monograph (AHFS DI)


• Alphagan P MedFacts Consumer Leaflet (Wolters Kluwer)


• Alphagan Consumer Overview

Compare Alphagan P with other medications

• Glaucoma, Open Angle
• Intraocular Hypertension

Embeline Solution

Pronunciation: kloe-BAY-ta-sol
Generic Name: Clobetasol
Brand Name: Examples include Embeline and Temovate

Embeline Solution is used for:

Treating inflammation and itching of the scalp due to certain skin conditions. It is also used to treat moderate to severe psoriasis. It may also be used for other conditions as determined by your doctor.

Embeline Solution is a topical adrenocortical steroid. It works by reducing skin inflammation (eg, redness, swelling, itching, irritation) in a way that is not clearly understood.

Do NOT use Embeline Solution if:

• you are allergic to any ingredient in Embeline Solution or to other corticosteroids (eg, prednisone)

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

Before using Embeline Solution:

Some medical conditions may interact with Embeline Solution. 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 any kind of skin infection of the scalp, cuts, scrapes, or lessened blood flow to your skin


• if you have had a recent vaccination; have measles, tuberculosis, chickenpox, or shingles; or have had a positive tuberculosis test


• if you are taking prednisone or similar medicines

Some MEDICINES MAY INTERACT with Embeline Solution. Because little, if any, of Embeline Solution is absorbed into the blood, the risk of it interacting with another medicine is low.

Ask your health care provider if Embeline Solution 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 Embeline Solution:

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

• Wash and completely dry the affected area before applying Embeline Solution.


• Apply a small amount of Embeline Solution to the affected area. Gently rub the medicine in until it is evenly distributed. Wash your hands after applying Embeline Solution.


• If applying to an area with hair, part the hair when applying so that Embeline Solution reaches the skin.


• Do not bandage or cover the treated skin area unless directed by your doctor. Do not wear tight-fitting clothes over the treated area.


• If you miss a dose of Embeline Solution, apply it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not apply 2 doses at once.

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

Important safety information:

• Embeline Solution is for external use only. Do not get Embeline Solution in your eyes, nose, mouth, or on your lips. If contact is made with the eyes, flush them immediately with tap water.


• Use Embeline Solution with extreme caution if treating the face, groin, diaper area, or underarms.


• Do not use Embeline Solution to treat rosacea or conditions around the mouth.


• Do NOT take more than the recommended dose or use for longer than 2 weeks without checking with your doctor.


• If your symptoms do not get better within 2 weeks or if they get worse, check with your doctor.


• Do not use Embeline Solution to treat large areas of your body without first checking with your doctor.


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


• Check with your doctor before having vaccinations while using Embeline Solution.


• Do not use Embeline Solution for other skin conditions at a later time.


• Embeline Solution has a corticosteroid in it. Before you start any new medicine, check the label to see if it has a corticosteroid (eg, hydrocortisone) in it too. If it does or if you are not sure, check with your doctor or pharmacist.


• Embeline Solution is flammable. Do not store or use near an open flame or while smoking.


• Corticosteroids may affect growth rate in CHILDREN and teenagers in some cases. They may need regular growth checks while they use Embeline Solution.


• Embeline Solution should not be used in CHILDREN younger than 12 years old; safety and effectiveness in these 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 using Embeline Solution while you are pregnant. It is not known if Embeline Solution is found in breast milk after topical use. If you are or will be breast-feeding while you use Embeline Solution, check with your doctor. Discuss any possible risks to your baby.

Possible side effects of Embeline Solution:

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:

Dryness; itching; mild burning or stinging.

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); acne-like rash; burning, cracking, irritation, or peeling not present before you began using Embeline Solution; excessive hair growth; inflamed hair follicles; inflammation around the mouth; muscle weakness; numbness of fingers; thinning, softening, or discoloration of the skin; unusual weight gain, especially in the face.

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: Embeline 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 increased thirst or urination; muscle weakness; unusual weight gain, especially in the face.

Proper storage of Embeline Solution:

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

General information:

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


• Embeline Solution 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 Embeline Solution. 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 Embeline resources

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

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• Atopic Dermatitis
• Dermatitis
• Lichen Planus
• Lichen Sclerosus
• Psoriasis

Nicotine

Class: Autonomic Drugs, Miscellaneous
VA Class: AD900
Chemical Name: S-3-(1-Methyl-2-pyrrolidinyl)pyridine
Molecular Formula: C₁₀H₁₄N₂• x(C₁₀H₁₀•C₄H₆O₂)x
CAS Number: 54-11-5
Brands: Nicotrol NS, Nicotrol Inhaler, Nicoderm CQ, Commit, Nicorette

Introduction

Ganglionic (nicotinic) cholinergic-receptor agonist.^a

Uses for Nicotine

Smoking Cessation

Used for nicotine replacement therapy as a temporary adjunct in the cessation of cigarette smoking either unsupervised (self-medication)^{188 189 190 246 257} or in conjunction with a behavior modification program under clinician supervision.^{1 2 5 6 7 8 9 10 11 29 30 31 96 97 191 192 193 194 195 196 244 245 257 258 263}

Nicotine replacement therapy considered first-line therapy by USPHS for treatment for dependence on tobacco.²⁵⁷

Provides alternative sources of nicotine that help reduce the withdrawal symptoms associated with nicotine dependence.^{1 2 50 78 79 80 97 101 102 103 104} Chewing the resin complex-containing gum may act as a substitute oral activity in behavior modification.⁵

Ulcerative Colitis

Transdermal nicotine has been used in the management of ulcerative colitis†.^{125 204 205 206 207 208 209 210}

Nicotine Dosage and Administration

General

• 
  

  To increase smoking cessation rate,^{101 144 194 195 196} use as part of a comprehensive program of multiple treatment strategies, including behavioral modification.^{43 44 101 102 103 104 115 116 119 126 131 144 148 149 167 193 194 195 196 257 258 a}

  
  


• 
  

  Individualize duration of therapy based on patient response and degree of nicotine dependence.^{1 190 257 263 264 a}

  
  


• 
  

  Stop smoking prior to initiating nicotine replacement therapy;^{1 190 257 263 264} self-medication not recommended in patients who continue to smoke, chew tobacco, or use snuff or other nicotine-containing preparations.^{188 189 190}

  
  


• 
  

  Discontinue therapy in patients who continue to smoke 4 weeks after initiating treatment;^{101 102 103 104} may use nicotine replacement therapy again in subsequent attempts to quit smoking.^{101 102 103 104 121}

  
  

Administration

Administer nicotine percutaneously by topical application of a transdermal system.^{b i}

Administer nicotine transmucosally by oral inhalation using a special nicotine oral inhaler or intranasally using a metered-dose spray pump. ^{d 265 g}

Administer nicotine polacrilex intrabuccally (transmucosally) as a lozenge or chewing gum.^{c h}

May be administered as a single nicotine preparation (i.e., intrabuccally, intranasally, percutaneously, or by oral inhalation); however, if single therapy does not enable patients to quit smoking, use of transdermal nicotine may be combined with another form of nicotine replacement (i.e., either buccal nicotine polacrilex or nicotine nasal spray).²⁵⁷

Buccal Administration

Chewing Gum

Self-administer one piece of gum in response to the urge to smoke.¹

Chew gum very slowly until a distinctive peppery taste of nicotine, minty, cinnamon, or orange taste of the gum, or a slight tingling in the mouth is perceived (typically about 15 chews);¹ stop chewing gum and park between cheek and gum; once tingling is almost gone (about 1 minute), repeat chewing procedure.^{1 257} Continue for about 30 minutes or until taste dissipates.^{1 257} Do not swallow gum.¹

Do not eat or drink anything other than water for 15 minutes before and during chewing of gum.^{1 190 257}

Do not chew multiple pieces of gum simultaneously; do not chew too rapidly or chew pieces in succession.¹ May cause excessive release of nicotine and result in adverse effects (e.g., lightheadedness, nausea, vomiting, irritation of the throat and mouth, hiccups, indigestion).¹

Chew at least 9 pieces of gum daily to improve chances of quitting.^c

Do not attempt to discontinue nicotine polacrilex gum therapy until craving is satisfied by 1 or 2 pieces of the gum daily; but do not continue therapy for >6 months,¹ unless otherwise instructed by clinician.^{9 43 65}

4-mg strength gum recommended in highly dependent smokers because of evidence of increased efficacy.^a

Lozenges

Suck on lozenge until dissolved; do not swallow, bite, or chew.^{260 263 264} Allow to dissolve slowly in the mouth over 20–30 minutes, periodically moving the lozenge (e.g., with the tongue) from one side of the mouth to the other; minimize swallowing.^{263 264} A warm or tingling sensation may be perceived.^h

Do not eat or drink anything other than water for 15 minutes before and during sucking on the lozenge.^{257 263 264}

Use at least 9 lozenges daily for the first 6 weeks to improve chances of quitting.^h

Using >1 lozenge simultaneously or using one lozenge after another in uninterrupted sequence may result in adverse effects (e.g., hiccups, heartburn, nausea).^h

Self-administer lozenge in response to nicotine craving; decrease frequency of administration over time.^{263 264}

Topical Administration

Administer percutaneously by topical application of a transdermal system once daily.^{b i}

Apply at the same time each day, usually after awakening.^{101 102 103 104 129 167 188 189 257}

Expose the adhesive surface of the system by peeling and discarding the protective liner just prior to application and apply system immediately to avoid loss of nicotine through volatilization.^{101 102 103 104 129}

Apply transdermal system to a clean, dry, hairless area of intact skin^{43 101 129} on the trunk or upper outer arm^{101 102 103 104 129 167 188 189 257} by firmly pressing the system with the adhesive side touching the skin.^{101 129 167} Press system firmly in place with heel of hand for about 10 seconds, ensuring good contact, particularly around the edges.^{101 129 167 a} Do not apply to sites that are oily, damaged, or irritated;^{43 101 129} if necessary, hair may be clipped, but do not shave area.¹⁶⁷

System may be worn for 16 or 24 hours.^{b i} If cravings begin upon awakening, wear patch for 24 hours.^{189 b} If vivid dreams or sleep disruptions occur, wear patch for 16 hours; remove at bedtime and apply new patch upon awakening.^{189 257 b i}

If system inadvertently comes off during the period of use, apply a new system; ^{101 102 103 104 167 a} continue current application schedule or change so that the next system is applied 24 hours later.¹²⁹

Rotate application sites to minimize potential skin irritation; allow ≥1 week before reusing a given site.^{101 102 103 129} (See Dermatologic Effects under Cautions.)

Avoid unnecessary contact with transdermal systems.^{101 102 103 104} Avoid touching eyes after handling; wash hands with water alone as soap may enhance percutaneous absorption.^{101 102 103 104 167}

Intranasal Administration

Administer intranasally using a metered-dose spray pump.¹⁹¹

Prime spray pump prior to initial use by spraying into a tissue until a fine spray is seen (6–8 times); discard tissue.^d

If spray pump is not used for 24 hours, reprime pump by spraying into a tissue 1–2 times.^d

Clear nasal passages prior to administration.^d

Tilt the head back slightly;^{191 257 d} insert tip of bottle into one nostril as far as is comfortable.^d Breathe through the mouth and spray once into nostril; do not sniff, swallow or inhale through the nose while administering.^{191 257} Repeat this procedure for the other nostril.^d

If nose runs, sniff gently to keep nasal spray in nose; wait 2–3 minutes before blowing nose.^d

Avoid contact with skin, eyes, and mouth; if contact occurs, rinse with plain water immediately.^d If intranasal bottle breaks, wear protective gloves, wipe with paper towels, and wash surfaces thoroughly.^d

Oral Inhalation

Administer transmucosally as an inhaled vapor by oral inhalation using a special nicotine oral inhaler that mimics smoking cigarettes.^{244 245 246 247 248}

Hold the oral inhaler with two hands; separate the top and bottom pieces by pushing and turning the pieces until markings line up.^g Insert one nicotine cartridge and push the cartridge until it pops into place.^g Line up markings on the top and bottom pieces of the inhaler and push pieces together tightly; lock inhaler by turning pieces until markings do not line up.^g

Place the mouthpiece of the inhaler between lips and puff on the inhaler using rapid shallow sucking (“buccal mode”);^{244 248 257} alternatively, inhale slowly and deeply into back of throat (“pulmonary mode”).^{248 g} Nicotine is vaporized and absorbed in mouth and throat.^g (See Absorption under Pharmacokinetics.) Shallow puffing method generally is preferred.^{244 248 250 257} Deep inhalation technique requires considerable effort and does not result in substantially increased drug delivery or other benefits.²⁴⁸

Individualize orally inhaled dosage to the level of nicotine replacement required; optimum results generally achieved by frequent continuous puffing of the inhaler over 20 minutes.²⁴⁴

Nicotine is used up from cartridge after about four 5-minute sessions or one 20-minute session of active puffing.²⁵⁰

When cartridge is empty, remove top of mouthpiece; discard empty cartridge away from children and pets.^g Store with mouthpiece in locked position and cartridges in plastic case.^g Clean reusable mouthpiece regularly with soap and water.²⁴⁴

Use inhaler at temperatures >60°F; cold temperatures decrease the amount of nicotine inhaled.^g

Dosage

Chewing gum and lozenge available as nicotine polacrilex; dosage expressed in terms of nicotine.^{1 264}

Nicotine oral inhaler cartridges labeled as containing 10 mg of nicotine deliver ≤4 mg total with repeated inhalation.^{244 247 250 257} The amount of nicotine released depends on the volume and temperature of the air passing through the inhaler.^{244 245 246 247 248} An intensive inhalation regimen (80 deep inhalations over 20 minutes) releases approximately 4 mg of nicotine.²⁶⁵

Metered nasal spray delivers 0.5 mg of nicotine per metered spray and about 200 sprays (i.e., 100 doses) per 100-mg container.^{191 257}

Adults

Smoking Cessation

Buccal (Chewing Gum)

Patients who smoke <25 cigarettes daily: Chew a 2-mg piece of gum every 2 hours during weeks 1–6; chew a 2-mg piece every 2–4 hours during weeks 7–9; and chew a 2-mg piece every 4–8 hours during weeks 10–12 of therapy.^c Alternatively, chew a 2-mg piece of gum whenever the urge to smoke occurs; do not exceed 2 pieces (4 mg) per hour.¹

Patients who smoke ≥25 cigarettes daily: Chew a 4-mg piece of gum every 2 hours during weeks 1–6; chew a 4-mg piece every 2–4 hours during weeks 7–9; and chew a 4-mg piece every 4–8 hours during weeks 10–12 of therapy.^c Alternatively, chew a 4-mg piece whenever the urge to smoke occurs; do not exceed 2 pieces (8 mg) per hour.¹

Taper dosage by chewing each piece for only 10–15 minutes and gradually reducing the number of pieces chewed, or chew each piece for longer than 30 minutes but reduce the total pieces per day, or substitute regular chewing gum for some pieces.^c

Buccal (Lozenges)

Patients who smoke first cigarette >30 minutes after waking: One 2-mg lozenge every 1–2 hours during weeks 1–6; then one 2-mg lozenge every 2–4 hours during weeks 7–9; and once 2-mg lozenge every 4–8 hours during weeks 10–12.^{263 264 h}

Patients who smoke first cigarette ≤30 minutes after waking: One 4-mg lozenge every 1–2 hours during weeks 1–6; then one 4-mg lozenge every 2–4 hours during weeks 7–9; and one 4-mg lozenge every 4–8 hours during weeks 10–12.^{263 264 h}

Do not exceed 5 lozenges in 6 hours or 20 lozenges daily.^{263 264}

Discontinue therapy if mouth problems, persistent indigestion, severe sore throat, irregular heartbeat, palpitations or symptoms suggestive of overdosage (nausea, vomiting, dizziness, diarrhea, weakness, and rapid heartbeat) develop.²⁶⁴

Transdermal

Patients who smoke ≤10 cigarettes daily: Initially, 14 mg daily for 6 weeks, then 7 mg daily for 2 weeks, then discontinue.^{189 b i}

Patients who smoke >10 cigarettes daily: Initially, 21 mg daily for 4–6 weeks; then 14 mg daily for 2 weeks; then 7 mg daily for 2 weeks; then discontinue therapy.^{189 257 b i}

Intranasal

Initially, 1–2 sprays (0.5–1 mg) in each nostril per hour (1–2 mg per hour total); may increase up to a maximum of 5 sprays (5 mg) in each nostril per hour (10 mg total) or a maximum total of 80 sprays (40 mg) daily.^{191 257 e}

Initially, use at least 16 sprays (8 mg total) daily to increase chance of efficacy.^{191 257} Then, individualize dosage based on nicotine dependence and occurrence of symptoms of nicotine excess.¹⁹¹

Continue treatment in successfully abstinent patients for up to 8 weeks then discontinue over 4–6 weeks.¹⁹¹

Taper dosage by using only 1 spray at a time, using the spray less frequently, keeping a tally of daily usage, trying to meet a steadily reducing usage target, skipping a dose by not medicating every hour, or setting a planned “quit date” for stopping use of the spray.¹⁹¹ Some patients may not require tapering.¹⁹¹

Oral Inhalation

Initially, 6–16 cartridges daily for up to 12 weeks, then gradually decrease daily dosage over 6–12 weeks.^{244 245 246 257}

Use ≥6 cartridges daily for the first 3–6 weeks to increase chance of efficacy.²⁴⁴ Individualize dosage based on nicotine dependence and occurrence of symptoms of nicotine excess.²⁴⁴

Taper dosage by using less frequently, keeping a tally of daily usage, trying to meet a steadily reducing usage target, or setting a planned “quit date” for stopping use of the inhaler.²⁶⁵ Some patients may not require tapering.²⁶⁵

Prescribing Limits

Adults

Smoking Cessation

Buccal (Chewing Gum)

Maximum 2 pieces of 2-mg gum per hour (i.e., maximum 24 pieces [48 mg nicotine] daily).^c Maximum 12 weeks of therapy.^c

Maximum 2 pieces of 4-mg gum per hour (i.e., maximum 24 pieces [96 mg nicotine] daily).^c Maximum 12 weeks of therapy.^c

Clinician supervised: Maximum 30 pieces of 2-mg gum daily (i.e., 60 mg nicotine) or 24 pieces of 4-mg gum daily (i.e., 96 mg nicotine).^{1 190 195}

Buccal (Lozenges)

Maximum 5 lozenges in 6 hours or 20 lozenges daily.^h Maximum 12 weeks of therapy.^h

Transdermal

Patients who smoke ≤10 cigarettes daily: Maximum 8 weeks of therapy.^b

Patients who smoke >10 cigarettes daily: Maximum 10 weeks of therapy.^b

Continued therapy for periods longer than usually recommended may be appropriate for certain patients to promote extended abstinence.²⁵⁷ Continuation of therapy >12 weeks not recommended by manufacturer.^{101 102 103 104}

Intranasal

Maximum 5 sprays (5 mg) in each nostril per hour (maximum 10 mg total) or a maximum total of 80 sprays (40 mg) daily.^{191 257 e}

Manufacturer states that continuing therapy >12 weeks does not improve outcome.^e Safety of continuing therapy >6 months not established.^e

Oral Inhalation

Maximum 16 cartridges daily for up to 12 weeks.²⁶⁵

Manufacturer states that safety of continuing therapy >6 months not established.²⁶⁵

Special Populations

No special population dosage recommendations at this time.^{a b}

Cautions for Nicotine

Contraindications

• 
  

  Known hypersensitivity to nicotine, menthol (oral inhaler), or any ingredient in the formulation.^{101 102 103 104 191 244}

  
  


• 
  

  Nicotine polacrilex gum in patients with temporomandibular joint disease.^{101 102 103 104 191 244} (See Oral and Dental Effects under Cautions.)

  
  

Warnings/Precautions

Warnings

Nicotine Toxicity

Risk of nicotine toxicity (e.g., nausea, hypersalivation, abdominal pain, vomiting, diarrhea, perspiration, headache, dizziness, hearing and visual disturbances, mental confusion, weakness)^{1 4 36 97 191 244} and addiction.^{101 102 103 104 244} Sustained use of nicotine preparations is not recommended.^{1 81 101 102 103 104 244} Weigh risk of nicotine replacement against hazard of continued smoking concurrent with nicotine-replacement therapy and likelihood of smoking cessation without nicotine replacement.^{101 102 103 104 244}

Discontinue nicotine polacrilex lozenges if symptoms suggestive of overdosage (nausea, vomiting, dizziness, diarrhea, weakness, and rapid heartbeat) occur.²⁶⁴

Fetal/Neonatal Morbidity

Animal studies indicate fetal harm; pregnant women should attempt smoking cessation with educational and behavioral interventions before considering nicotine therapy.^{1 101 102 103 104 128 191 194 195 196 244 257 264 e}

Use during pregnancy only if the increased likelihood of smoking cessation justifies potential risk to the fetus and patient of nicotine replacement and possible continued smoking.^{1 101 102 103 104 128 191 194 195 196 244 257 264} If used during pregnancy or if patient becomes pregnant, apprise of potential fetal hazard.^{e 265}

General Precautions

Respiratory Effects

Possible exacerbation of bronchospasm.²⁴⁴ Use oral inhaler with caution in patients with bronchospastic disease;²⁴⁴ other dosage forms may be preferable.²⁴⁴

Intranasal nicotine is not recommended in patients with severe reactive airway disease.^{191 257}

Nasopharyngeal Effects

Nicotine nasal spray may irritate nasal mucosa;^e use of nasal spray not recommended in patients with a history of chronic nasal disorders (e.g., allergy, rhinitis, polyps, sinusitis).^{191 257}

Discontinue nicotine polacrilex lozenges if severe sore throat occurs.²⁶⁴

Cardiovascular Effects

Possible increased risk of adverse cardiovascular effects;^{144 149 164 165 211 212 213 214 215} however, causal relationship between nicotine replacement therapy and cardiac complications not established.^{101 102 103 104 144 148 149 191 244 257}

Discontinue therapy if irregular heartbeat or palpitations occur.^{264 b c h i}

Use with caution and only after careful evaluation in patients with coronary heart disease (i.e., history of MI, angina pectoris), serious cardiac arrhythmias, or vasospastic diseases (e.g., Buerger's disease, Prinzmetal's variant angina, Raynaud's phenomena).^{101 102 103 104 144 148 149 191 244 257} Benefit of nicotine replacement therapy must outweigh risks of continued cigarette smoking.^{43 257}

Self-medication not recommended in patients in the immediate post-MI period, with serious arhythmias, or with severe or worsening angina.^{188 189 190}

Endocrine Effects

Possible hyperinsulinemia and insulin resistance with prolonged nicotine replacement therapy.²⁵⁴ Use with caution in hyperthyroidism, pheochromocytoma, or insulin-dependent diabetes.^{101 102 103 104 191 244}

GI Effects

Possible delayed healing of peptic ulcer; use with caution.^{101 102 103 104 191 244}

Discontinue nicotine polacrilex lozenges if persistent indigestion develops.²⁶⁴

Use nicotine polacrilex gum with caution in patients with a history of esophagitis.^{1 97}

Hypertension

Possible increased risk of malignant hypertension in patients with accelerated hypertension; use with caution in such patients.^{1 101 102 103 104 191 244}

Possible perpetuation of hypertension; use with caution in patients with systemic hypertension.^a

Nicotine Dependence

Transference of dependence on nicotine may occur;^{1 81 87 88 90 96 97 98 191 195 244 257} potential for abuse and dependence on nicotine nasal spray appears to be greater than that for other formulations of nicotine (i.e., nicotine polacrilex gum, transdermal nicotine systems) but less than that of cigarettes.^{191 196 201 202 257}

To minimize withdrawal symptoms⁸⁷ and the risk of dependence on nicotine, withdraw gradually or discontinue use of nicotine polacrilex gum or transdermal or intranasal nicotine after 2–3 months of therapy.^{1 2 3 36 191 195 244}

Phenylketonuria

Commit nicotine polacrilex lozenges contain aspartame (NutraSweet), which is metabolized in the GI tract to provide 3.4 mg of phenylalanine per lozenge.²⁶⁴

Oral and Dental Effects

Risk of occlusal stress when nicotine polacrilex gum chewed for long periods of time; may result in displaced dental restorations or loosening of dental inlays or fillings.^{1 72} Gum may stick to dentures, dental caps, or partial bridges; if excessive sticking or damage to dental work occurs, discontinue gum and consult clinician.¹

Use nicotine polacrilex gum with caution in patients with a history of oral or pharyngeal inflammation, or dental conditions exacerbated by chewing gum.^{1 97}

Discontinue nicotine polacrilex lozenges if mouth problems develop.²⁶⁴

Dermatologic Effects

Possible skin reactions (e.g., urticaria, hives, rash) with transdermal systems.^{101 102 103 104 129} Increased risk of such reactions in patients with some dermatologic conditions (e.g., psoriasis, atopic or eczematous dermatitis).^{101 102 103 104}

If skin reaction occurs, discontinue transdermal system and contact clinician;^{101 102 103 104 129} topical corticosteroids and/or oral antihistamines recommended.^{43 112 144 149 195}

Risk of contact sensitization with transdermal systems; serious reaction may occur with re-exposure to smoking or other nicotine products.^{101 102 103 104}

Nervous System Effects

Potential adverse nervous system effects (e.g., insomnia,^{1 102 136 137} headache,^{1 68 101 102 103 104 109 111 118 137 244 246 263} dizziness, lightheadedness).^{1 27 104 109}

Specific Populations

Pregnancy

Category D.^{e 265} (See Fetal/Neonatal Morbidity under Cautions.)

Lactation

Distributed into milk.^{1 34 70 73 101 102 103 104 191 244 257} Use caution.^{1 34 70 73 101 102 103 104 191 244 257}

Weigh risk of exposure to nicotine in drug versus risk of nicotine and other components of tobacco smoke from cigarettes.^{1 101 102 103 104 191 244}

Pediatric Use

Safety and efficacy not established.^{1 101 102 103 104 191 196 244} However, the USPHS states that nicotine replacement therapy may be considered in adolescents when there is evidence of nicotine dependence and a desire to quit the use of tobacco.^{196 257}

Use or ingestion of used or unused nicotine replacement systems by children may cause poisoning or be fatal; keep used and unused containers out of reach of children.^{101 102 103 104 191 244}

Risk of choking if nicotine oral inhalers are swallowed; keep out of reach of children.²⁴⁴

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults;^{101 102 103 104 244} select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease.^{e 265}

Hepatic Impairment

Not studied in patients with hepatic impairment; use with caution.^{101 102 103 104 244}

Renal Impairment

Not studied in patients with renal impairment; clearance may be decreased in patients with severe renal impairment.^{44 101 102 103 104 244}

Common Adverse Effects

Buccal therapy (gum): Indigestion;^{1 7 27 85 96 257} nausea;^{1 6 9 27 68 85 95} hiccups;^{1 7 68 89 94 96 257} traumatic injury to oral mucosa and/or teeth;^{1 68 257} irritation and/or tingling of the tongue, mouth, and throat;^{1 5 9 27 29 68 85 89 95 96} oral mucosal ulceration;^{1 5 6 7 29 68 89 96} jaw-muscle ache;^{1 5 6 7 29 68} eructation;^{1 68 95} gum sticking to teeth;⁸⁹ unpleasant taste;^{5 85 95} dizziness;^{1 27} lightheadedness;^{1 27} headache;^{1 68} insomnia.¹

Buccal therapy (lozenge): Nausea,²⁶³ dyspepsia,²⁶³ flatulence,²⁶³ headache,²⁶³ upper respiratory tract infections.²⁶³

Transdermal therapy: Application site reactions (i.e., pruritus, burning, or erythema),^{101 102 103 104 113 114 115 118 126 136 137 195 257} diarrhea,^{101 102} dyspepsia,^{103 137} abdominal pain,¹⁰³ dry mouth.^{101 102 109 137}

Intranasal therapy: Runny nose,^{191 196 202 203} throat irritation,^{191 196 201 202 203} watery eyes,^{191 196 201}

Kinevac

sincalide

Dosage Form: injection, powder, lyophilized, for solution
Kinevac 5mcg

Description

 

Kinevac (Sincalide for Injection) is a cholecystopancreatic-gastrointestinal hormone peptide for parenteral administration. The agent is a synthetically-prepared C-terminal octapeptide of cholecystokinin. Each vial of sincalide provides a sterile nonpyrogenic lyophillized white powder consisting of 5 mcg sincalide with 170 mg mannitol, 30 mg arginine hydrochloride, 15 mg lysine hydrochloride, 9 mg potassium phosphate dibasic, 4 mg methionine, 2 mg pentetic acid, 0.04 mg sodium metabisulfite, and 0.005 mcg polysorbate 20. The pH is adjusted to 6.0 - 8.0 with hydrochloric acid and/or sodium hydroxide prior to lyophilization. Sincalide is designated chemically as L-α-aspartyl-O-sulfo-L-tyrosyl-L-methionylglycyl-L-tryptophyl-L-methionyl- L-α-aspartyl-L-phenylalaninamide. Graphic formula:

Clinical Pharmacology

When injected intravenously, sincalide produces a substantial reduction in gallbladder size by causing this organ to contract. The evacuation of bile that results is similar to that which occurs physiologically in response to endogenous cholecystokinin. The intravenous (bolus) administration of sincalide causes a prompt contraction of the gallbladder that becomes maximal in 5 to 15 minutes, as compared with the stimulus of a fatty meal which causes a progressive contraction that becomes maximal after approximately 40 minutes. Generally, a 40 percent reduction in radiographic area of the gallbladder is considered satisfactory contraction, although some patients will show area reduction of 60 to 70 percent.

Like cholecystokinin, sincalide stimulates pancreatic secretion; concurrent administration with secretin increases both the volume of pancreatic secretion and the out-put of bicarbonate and protein (enzymes) by the gland. This combined effect of secretin and sincalide permits the assessment of specific pancreatic function through measurement and analysis of the duodenal aspirate. The parameters usually determined are: volume of the secretion; bicarbonate concentration; and amylase content (which parallels the content of trypsin and total protein).

Both cholecystokinin and sincalide stimulate intestinal motility, and may cause pyloric contraction which retards gastric emptying.

Indications and Usage

Kinevac (Sincalide for Injection) may be used: (1) to stimulate gallbladder contraction, as may be assessed by various methods of diagnostic imaging, or to obtain by duodenal aspiration a sample of concentrated bile for analysis of cholesterol, bile salts, phospholipids, and crystals; (2) to stimulate pancreatic secretion (especially in conjunction with secretin) prior to obtaining a duodenal aspirate for analysis of enzyme activity, composition, and cytology; (3) to accelerate the transit of a barium meal through the small bowel, thereby decreasing the time and extent of radiation associated with fluoroscopy and x-ray examination of the intestinal tract.

Contraindications Section

The preparation is contraindicated in patients hypersensitive to sincalide and in patients with intestinal obstruction.

Warnings

Because of Kinevac’s effect on smooth muscle, pregnant patients should be advised that spontaneous abortion or premature induction of labor may occur (see Pregnancy Category B).

Precautions

General

The possibility exists that stimulation of gallbladder contraction in patients with small gallbladder stones could lead to the evacuation of the stones from the gallbladder, resulting in their lodging in the cystic duct or in the common bile duct. The risk of such an event is considered to be minimal because sincalide, when given as directed, does not ordinarily cause complete contraction of the gallbladder.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Long-term studies in animals have not been performed to evaluate carcinogenic or mutagenic potential, or possible impairment of fertility in males or females.

Teratogenic EffectsPregnancy Category B

Reproduction studies in rats in which sincalide was administered subcutaneously at doses up to 12.5 times the maximum recommended human dose revealed no evidence of harm to the fetus due to sincalide. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed (see WARNINGS).

Labor and Delivery

Sincalide should not be administered to pregnant women near term because of its effect on smooth muscle; the possibility of inducing labor prematurely exists. The effects of sincalide on labor, delivery and lactation in animals has not been determined (see WARNINGS).

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when sincalide is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in children have not been established.

Adverse Reactions

Reactions to sincalide are generally mild and of short duration. The most frequent adverse reactions were abdominal discomfort or pain, and nausea; rapid intravenous injection of 0.04 mcg sincalide per kg expectably causes transient abdominal cramping. These phenomena are usually manifestations of the physiologic action of the drug, including delayed gastric emptying and increased intestinal motility. These reactions occurred in approximately 20 percent of patients; they are not to be construed as necessarily indicating an abnormality of the billiary tract unless there is other clinical or radiologic evidence of disease.

The incidence of other adverse reactions, including vomiting, flushing, sweating, rash, hypotension, hypertension, shortness of breath, urge to defecate, headache, diarrhea, sneezing, and numbness was less than 1 percent; dizziness was reported in approximately 2 percent of patients. These manifestations are usually lessened by slower injection rate.

Overdosage

Although no overdosage reports have been received, gastrointestinal symptoms (abdominal cramps, nausea, vomiting and diarrhea) would be expected. Hypotension with dizziness or fainting might also occur. Overdosage symptoms should be treated symptomatically and should be of short duration. Starting with single bolus i.v. injection comparable to the human does of 0.4 mg/kg, sincalide caused hypotension and bradycardia in dogs. Higher doses injected once or repeatedly in dogs caused syncope and ECG changes in addition. These effects were attributed to sincalide-induced vagal stimulation in that all were prevented by pretreatment with atropine or bilateral vagotomy.

Dosage and Administration

Reconstitution and Storage

Sincalide for Injection may be stored at room temperature prior to reconstitution.

To reconstitute, aseptically add 5 mL of Sterile Water for Injection USP to the vial. This solution may be kept at room temperature and should be used within 8 hours of reconstitution, after which time any unused portion should be discarded.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

For prompt contraction of the gallbladder, a dose of 0.02 mcg sincalide per kg (1.4 mcg/70 kg) is injected intravenously over a 30- to 60-second interval; if satisfactory contraction of the gallbladder does not occur in 15 minutes, a second dose, 0.04 mcg sincalide per kg, may be administered. To reduce the intestinal side effects (see ADVERSE REACTIONS), an intravenous infusion may be prepared at a dose of 0.12 mcg/kg in 100 mL of Sodium Chloride Injection USP and given at a rate of 2 mL per minute; alternatively, an intramuscular dose of 0.1 mcg/kg may be given. When Kinevac (Sincalide for Injection) is used in cholecystography, roentgenograms are usually taken at five-minute intervals after the injection. For visualization of the cystic duct, it may be necessary to take roentgenograms at one-minute intervals during the first five minutes after the injection.

For the Secretin-Kinevac test of pancreatic function, the patient receives a dose of 0.25 units secretin per kg by intravenous infusion over a 60-minute period. Thirty minutes after the initiation of the secretin infusion, a separate IV infusion of Kinevac at a total dose of 0.02 mcg per kg is administered over a 30-minute interval. For example, the total dose for a 70 kg patient is 1.4 mcg of sincalide; therefore, dilute 1.4 mL of reconstituted Kinevac solution to 30 mL with Sodium Chloride Injection USP and administer at a rate of 1 mL per minute.

To accelerate the transit time of a barium meal through the small bowel, administer Kinevac after the barium meal is beyond the proximal jejunum. (Sincalide, like cholecystokinin, may cause pyloric contraction.) The recommended dose is 0.04 mcg sincalide per kg (2.8 mcg/70 kg) injected intravenously over a 30- to 60- second interval; if satisfactory transit of the barium meal has not occurred in 30 minutes, a second dose of 0.04 mcg sincalide per kg may be administered. For reduction of side effects, a 30-minute IV infusion of sincalide [0.12 mcg per kg (8.4 mcg/70 kg) diluted to approximately 100 mL with Sodium Chloride Injection USP] may be administered.

Sodium Chloride Injection dilutions may be kept at room temperature and should be used within one hour of dilution.

How Supplied

Kinevac (Sincalide for Injection) is supplied in packages of 10 vials containing 5 mcg of sincalide per vial (NDC 0270-0556-15).

Storage

Store at 25° C (77° F); excursions permitted to 15-30° C (59-86° F) [See USP Controlled Room Temperature].

U.S. Patent 6,803,046

Sample Outer label

Kinevac  sincalide  injection, powder, lyophilized, for solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 52584-556 (0270-0556) Route of Administration INTRAVENOUS DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength Sincalide (Sincalide) Sincalide 5 ug  in 5 mL

Inactive Ingredients Ingredient Name Strength Mannitol   Arginine hydrochloride   Lysine hydrochloride   Potassium phosphate, dibasic   Methionine   Pentetic acid   Sodium metabisulfite   Polysorbate 20

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 52584-556-15 1 VIAL In 1 BAG contains a VIAL 1 5 mL In 1 VIAL This package is contained within the BAG (52584-556-15)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NDA	NDA017697	11/05/2010

Labeler - General Injectables & Vaccines, Inc (108250663)

Revised: 11/2010General Injectables & Vaccines, Inc

More Kinevac resources

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

• Kinevac Concise Consumer Information (Cerner Multum)


• Kinevac Advanced Consumer (Micromedex) - Includes Dosage Information

Compare Kinevac with other medications

• Barium Meal Transit
• Gallbladder Contraction
• Pancreatic Secretion

Mountain Sickness / Altitude Sickness Medications

Definition of Mountain Sickness / Altitude Sickness: Acute mountain sickness is an illness that can affect mountain climbers, hikers, skiers, or travelers who ascend too rapidly to high altitude (typically above 8,000 feet or 2,400 meters). This is especially for persons who normally reside at or near sea level.

Drugs associated with Mountain Sickness / Altitude Sickness

The following drugs and medications are in some way related to, or used in the treatment of Mountain Sickness / Altitude Sickness. This service should be used as a supplement to, and NOT a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners.

Drug List:

Baycadron

De-Sone-La-Injection

Decadron

Dexacen-4-Injection

Dexacort-Phosphate-In-Turbinaire

Dexamethasone-Intensol

Dexasone-Injection

Dexasone-La-Injection

Dexpak-Tablets-Dose-Pack

Diamox

Diamox-Sequels-Sustained-Release-Capsules

Solurex-Injection

Solurex-La-Injection

Zema-Pak-10-Day

Zonegran

Generic Name: zonisamide (Oral route)

zoe-NIS-a-mide

Commonly used brand name(s)

In the U.S.

• Zonegran

Available Dosage Forms:

• Capsule


• Tablet

Therapeutic Class: Anticonvulsant

Chemical Class: Sulfonamide

Uses For Zonegran

Zonisamide is used together with other medicines to control partial seizures (convulsions) in the treatment of epilepsy. This medicine is an anticonvulsant that works in the brain tissue to stop seizures.

This medicine is available only with your doctor's prescription.

Before Using Zonegran

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of zonisamide in children below 16 years of age. Safety and efficacy have not been established.

Geriatric

Although appropriate studies on the relationship of age to the effects of zonisamide have not been performed in the geriatric population, geriatric-specific problems are not expected to limit the usefulness of zonisamide in the elderly. However, elderly patients are more likely to have age-related liver, kidney, or heart problems, which may require an adjustment in the dose for patients receiving zonisamide.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	C	Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Ketorolac


• Metformin


• Naproxen

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Ginkgo

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Blood or bone marrow problems (e.g., agranulocytosis, aplastic anemia) or


• Depression, history of—Use with caution. May make these conditions worse.

• Kidney disease or


• Liver disease—Use with caution. Effects may be increased because of slower removal of the medicine from the body.

Proper Use of Zonegran

Take this medicine only as directed by your doctor to help your condition as much as possible. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

This medicine comes with a medication guide and a patient information insert. Read and follow the instructions carefully. Ask your doctor if you have any questions.

Zonisamide may be taken with or without food, on a full or empty stomach. Swallow the capsule whole. Do not break, crush, or chew it.

It is important that you drink extra water every day while you take zonisamide to help prevent kidney stones.

This medicine will be used together with other seizure medicines. Keep using all of your medicines unless your doctor tells you to stop.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (capsules):
  
  • For seizures:
    
    • Adults and teenagers 16 years of age and older—At first, 100 milligrams (mg) once a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 400 mg per day.
    
    
    • Children and teenagers younger than 16 years of age—Use and dose must be determined by the doctor.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using Zonegran

It is very important that your doctor check your progress at regular visits to see if the medicine is working properly. Blood tests may be needed to check for unwanted effects.

It is important to tell your doctor if you become pregnant. Your doctor may want you to join a pregnancy registry for pregnant patients taking a seizure medicine.

This medicine may cause some people to become drowsy, dizzy, or less alert than they are normally. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous if you are dizzy or not alert.

This medicine will add to the effects of alcohol and other CNS depressants (medicines that make you drowsy or less alert). Some examples of CNS depressants are antihistamines or medicine for allergies or colds; sedatives, tranquilizers, or sleeping medicine; prescription pain medicines or narcotics; medicine for seizures or barbiturates; muscle relaxants; or anesthetics, including some dental anesthetics. Check with your medical doctor or dentist before taking any of the above while you are taking this medicine.

Contact your doctor immediately if you develop a skin rash, fever, sore throat, sores in your mouth, easy bruising, severe muscle pain or weakness, or worsening of your seizures.

Check with your doctor right away if you have sudden back pain, abdominal or stomach pain, pain while urinating, or bloody or dark urine. These may be symptoms of kidney stones.

Serious skin reactions can occur with this medicine. Stop using this medicine and check with your doctor right away if you have any of the following symptoms while taking this medicine: blistering, peeling, or loosening of the skin; chills; cough; diarrhea; itching; joint or muscle pain; red skin lesions, often with a purple center; sores, ulcers, or white spots in the mouth or on the lips; or unusual tiredness or weakness.

This medicine may make you sweat less, which causes your body temperature to increase. Use extra care not to become overheated during exercise or hot weather while you are taking this medicine. Overheating may result in heat stroke. Also, hot baths or saunas may make you dizzy or faint while you are taking this medicine.

Do not stop taking zonisamide without first checking with your doctor. Stopping the medicine suddenly may cause your seizures to return or to occur more often. Your doctor may want you to gradually reduce the amount of medicine you are taking before stopping it completely.

This medicine may cause some people to be agitated, irritable, or display other abnormal behaviors. It may also cause some people to have suicidal thoughts and tendencies or to become more depressed. If you or your caregiver notice any of these side effects, tell your doctor right away.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines, and herbal or vitamin supplements.

Zonegran Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

• Discouragement


• feeling sad or empty


• irritability


• lack of appetite


• loss of interest or pleasure


• mood or mental changes


• shakiness or unsteady walking


• tiredness


• trouble with concentrating


• trouble with sleeping

Less common

• Agitation


• bruising


• delusions


• hallucinations


• large, flat blue or purplish patches on the skin


• rash

Get emergency help immediately if any of the following symptoms of overdose occur:

Symptoms of overdose

• Difficult or labored breathing


• faintness


• loss of consciousness


• slow or irregular heartbeat

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Abdominal or stomach pain


• anxiety


• difficulty with memory


• dizziness


• double vision


• headache


• loss of appetite


• nausea


• restlessness


• sleepiness


• sleeplessness


• unusual drowsiness


• unusual tiredness or weakness

Less common

• Aching muscles or joints


• acid or sour stomach


• bad, unusual, or unpleasant taste in the mouth


• belching


• change in taste


• chills


• constipation


• diarrhea


• difficulty with speaking


• difficulty with thinking


• dry mouth


• fever


• general ill feeling


• headache


• heartburn


• indigestion


• mental slowness


• nervousness


• runny or stuffy nose


• sneezing


• tingling, burning, or prickly feelings on the skin


• uncontrolled, back and forth, or rolling eye movements


• weight loss

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Zonegran side effects (in more detail)

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

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More Zonegran resources

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

• Zonegran Prescribing Information (FDA)


• Zonegran Consumer Overview


• Zonegran Monograph (AHFS DI)


• Zonegran MedFacts Consumer Leaflet (Wolters Kluwer)


• Zonisamide Professional Patient Advice (Wolters Kluwer)

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