Tuesday, July 31, 2012

Neomycin,Polymyxin B Sulfates and Hydrocortisone




Neomycin and Polymyxin B Sulfates and Hydrocortisone OTIC Solution, USP

Sterile

DESCRIPTION


Neomycin and Polymyxin B Sulfates and Hydrocortisone OTIC Solution, USP is a sterile antibacterial and anti-inflammatory solution for otic use. Each mL contains: neomycin sulfate equivalent to 3.5 mg neomycin base, polymyxin B sulfate equivalent to 10,000 polymyxin B units, and hydrocortisone 10 mg (1%). The vehicle contains potassium metabisulfite 0.1% (added as a preservative) and the inactive ingredients glycerin, propylene glycol, hydrochloric acid, and Water for Injection.


Neomycin sulfate is the sulfate salt of neomycin B and C, which are produced by the growth of Streptomyces fradiae Waksman (Fam. Streptomycetaceae). It has a potency equivalent of not less than 600 mcg of neomycin standard per mg, calculated on an anhydrous basis. The structural formulae are:



Neomycin B (R1=H, R2=CH2NH2)


Neomycin C (R1=CH2NH2, R2=H)


Polymyxin B sulfate is the sulfate salt of polymyxin B1 and B2, which are produced by the growth of Bacillus polymyxa (Prazmowski) Migula (Fam. Bacillaceae). It has a potency of not less than 6,000 polymyxin B units per mg, calculated on an anhydrous basis. The structural formulae are:




Hydrocortisone, 11β,17,21-trihydroxypregn-4-ene-3, 20-dione, is an anti-inflammatory hormone. Its structural formula is:




CLINICAL PHARMACOLOGY


Corticoids suppress the inflammatory response to a variety of agents and they may delay healing. Since corticoids may inhibit the body's defense mechanism against infection, a concomitant antimicrobial drug may be used when this inhibition is considered to be clinically significant in a particular case.


The anti-infective components in the combination are included to provide action against specific organisms susceptible to them. Neomycin sulfate and polymyxin B sulfate together are considered active against the following microorganisms: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella-Enterobacter species, Neisseria species, and Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens and streptococci, including Streptococcus pneumoniae.The relative potency of corticosteroids depends on the molecular structure, concentration, and release from the vehicle.



INDICATIONS AND USAGE


For the treatment of superficial bacterial infections of the external auditory canal caused by organisms susceptible to the action of the antibiotics.



CONTRAINDICATIONS


This product is contraindicated in those individuals who have shown hypersensitivity to any of its components.


This product should not be used if the external auditory canal disorder is suspected or known to be due to cutaneous viral infection (for example, herpes simplex virus or varicella zoster virus).



WARNINGS


Neomycin can induce permanent sensorineural hearing loss due to cochlear damage, mainly destruction of hair cells in the organ of Corti. The risk of ototoxicity is greater with prolonged use; therefore, duration of therapy should be limited to 10 consecutive days (see PRECAUTIONS: General).


Patients being treated with eardrops containing neomycin should be under close clinical observation. Due to its acidity which may cause burning and stinging, Neomycin and Polymyxin B Sulfates and Hydrocortisone OTIC Solution should not be used in any patients with a perforated tympanic membrane.


Neomycin sulfate may cause cutaneous sensitization. A precise incidence of hypersensitivity reactions (primarily skin rash) due to topical neomycin is not known. Discontinue this product promptly if sensitization or irritation occurs. When using neomycin-containing products to control secondary infection in the chronic dermatoses, such as chronic otitis externa or stasis dermatitis, it should be borne in mind that the skin in these conditions is more liable than is normal skin to become sensitized to many substances, including neomycin. The manifestation of sensitization to neomycin is usually a low-grade reddening with swelling, dry scaling, and itching; it may be manifest simply as a failure to heal. Periodic examination for such signs is advisable, and the patient should be told to discontinue the product if they are observed. These symptoms regress quickly on withdrawing the medication. Neomycin-containing applications should be avoided for the patient thereafter.


Contains potassium metabisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than in nonasthmatic people.



PRECAUTIONS



General


As with other antibiotic preparations, prolonged use may result in overgrowth of nonsusceptible organisms, including fungi.


If the infection is not improved after 1 week, cultures and susceptibility tests should be repeated to verify the identity of the organism and to determine whether therapy should be changed.


Treatment should not be continued for longer than 10 days.


Allergic cross-reactions may occur which could prevent the use of any or all of the following antibiotics for the treatment of future infections: kanamycin; paromomycin; streptomycin; and possibly, gentamicin.



Information for Patients


Avoid contaminating the dropper with material from the ear, fingers, or other source. This caution is necessary if the sterility of the drops is to be preserved.


If sensitization or irritation occurs, discontinue use immediately and contact your physician.


Do not use in the eyes.



Laboratory Tests


Systemic effects of excessive levels of hydrocortisone may include a reduction in the number of circulating eosinophils and a decrease in urinary excretion of 17-hydroxycorticosteroids.



Carcinogenesis, Mutagenesis, Impairment of Fertility


Long-term studies in animals (rats, rabbits, mice) showed no evidence of carcinogenicity attributable to oral administration of corticosteroids.



Pregnancy



Teratogenic Effects


Pregnancy Category C. Corticosteroids have been shown to be teratogenic in rabbits when applied topically at concentrations of 0.5% on days 6 to 18 of gestation and in mice when applied topically at a concentration of 15% on days 10 to 13 of gestation. There are no adequate and well-controlled studies in pregnant women. Corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.



Nursing Mothers


Hydrocortisone appears in human milk following oral administration of the drug. Since systemic absorption of hydrocortisone may occur when applied topically, caution should be exercised when Neomycin and Polymyxin B Sulfates and Hydrocortisone OTIC Solution is used by a nursing woman.



Pediatric Use


The safety and effectiveness of Neomycin and Polymyxin B Sulfates and Hydrocortisone OTIC Solution in otitis externa have been established in the pediatric age group 2 years to 16 years of age. There is inadequate data to establish safety and effectiveness in otitis externa for pediatric patients under 2 years of age.1



Geriatric Use


Clinical studies of Neomycin and Polymyxin B Sulfates and Hydrocortisone OTIC Solution did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients.



ADVERSE REACTIONS


Neomycin occasionally causes skin sensitization. Ototoxicity and nephrotoxicity have also been reported (see WARNINGS). Adverse reactions have occurred with topical use of antibiotic combinations including neomycin and polymyxin B. Exact incidence figures are not available since no denominator of treated patients is available. The reaction occurring most often is allergic sensitization. In one clinical study, using a 20% neomycin patch, neomycin-induced allergic skin reactions occurred in two of 2,175 (0.09%) individuals in the general population.2 In another study, the incidence was found to be approximately 1%.3


The following local adverse reactions have been reported with topical corticosteroids, especially under occlusive dressings: burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, and miliaria. Stinging and burning have been reported when this product has gained access to the middle ear.



DOSAGE AND ADMINISTRATION


Therapy with this product should be limited to 10 consecutive days.


The external auditory canal should be thoroughly cleansed and dried with a sterile cotton applicator.


For adults, four drops of the solution should be instilled into the affected ear 3 or 4 times daily. For infants and children, three drops are suggested because of the smaller capacity of the ear canal.


The patient should lie with the affected ear upward and then the drops should be instilled. This position should be maintained for 5 minutes to facilitate penetration of the drops into the ear canal.


Repeat, if necessary, for the opposite ear.


If preferred, a cotton wick may be inserted into the canal and then the cotton may be saturated with the solution.


This wick should be kept moist by adding further solution every 4 hours. The wick should be replaced at least once every 24 hours.



HOW SUPPLIED


Bottle of 10 mL with sterilized dropper


NDC 61314-646-10


Store at 15° to 25°C (59° to 77°F).


Rx Only


Also Available: Neomycin and Polymyxin B Sulfates and Hydrocortisone OTIC Suspension, USP bottle of 10 mL with sterilized dropper.



REFERENCES


1. Jones, RN, Milazzo J, Seidlin, M. Ofloxacin Otic Solution for Treatment of Otitis Externa in Children and Adults. Arch Otolaryngol Head Neck Surg. 1997;123:1193-1200.


2. Leyden JJ, Kligman AM. Contact dermatitis to neomycin sulfate. JAMA. 1979;242:1276-1278.


3. Prystowsky SD, Allen AM, Smith RW, Nonomura JH, Odom RB, Akers WA. Allergic contact hypersensitivity to nickel, neomycin, ethylenediamine, and benzocaine: relationships between age, sex, history of exposure, and reactivity to standard patch tests and use tests in a general population. Arch Dermatol. 1979;115:959-962.


    



Dist. by:


FALCON Pharmaceuticals, Ltd.


Fort Worth, Texas 76134 USA


Mfd. by:


ALCON LABORATORIES, INC.


Fort Worth, Texas 76134 USA


Revised: September 2002


340109-0902


   



PRINCIPAL DISPLAY PANEL


NDC 61314-646-10      Rx Only


    


FALCON PHARMACEUTICALS®


  


NEOMYCIN AND


POLYMYXIN B SULFATES


AND HYDROCORTISONE


OTIC SOLUTION, USP


   


STERILE EAR SOLUTION


    


FOR USE IN EARS ONLY.


   


STERILE EAR SUSPENSION


10 mL (with Sterilized Dropper)


   


AFFILIATE OF


ALCON LABORATORIES, INC.











NEOMYCIN AND POLYMYXIN B SULFATES AND HYDROCORTISONE 
neomycin sulfate, polymyxin b sulfate and hydrocortisone  solution










Product Information
Product TypeHUMAN PRESCRIPTION DRUGNDC Product Code (Source)61314-646
Route of AdministrationAURICULAR (OTIC)DEA Schedule    














Active Ingredient/Active Moiety
Ingredient NameBasis of StrengthStrength
NEOMYCIN SULFATE (NEOMYCIN)NEOMYCIN3.5 mg  in 1 mL
POLYMYXIN B SULFATE (POLYMYXIN B)POLYMYXIN B10000 [iU]  in 1 mL
HYDROCORTISONE (HYDROCORTISONE)HYDROCORTISONE10 mg  in 1 mL














Inactive Ingredients
Ingredient NameStrength
POTASSIUM METABISULFITE 
GLYCERIN 
PROPYLENE GLYCOL 
HYDROCHLORIC ACID 
WATER 


















Product Characteristics
Color    Score    
ShapeSize
FlavorImprint Code
Contains      










Packaging
#NDCPackage DescriptionMultilevel Packaging
161314-646-1010 mL In 1 BOTTLENone










Marketing Information
Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
ANDAANDA06242303/18/2003


Labeler - Falcon Pharmaceuticals, Ltd. (874345820)

Registrant - Alcon Laboratories, Inc. (008018525)









Establishment
NameAddressID/FEIOperations
Alcon Laboratories, Inc.008018525MANUFACTURE
Revised: 08/2011Falcon Pharmaceuticals, Ltd.

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  • Otitis Externa
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Wednesday, July 25, 2012

Topiramate



Pronunciation: toe-PIR-a-mate
Generic Name: Topiramate
Brand Name: Topamax


Topiramate is used for:

Treating seizures in certain patients. It may be used alone or with other medicines. It is also used to prevent migraine headaches. It may also be used for other conditions as determined by your doctor.


Topiramate is an anticonvulsant that is also effective for preventing migraine headaches. It works by affecting several chemicals in the brain that help to reduce seizure activity and prevent migraine headaches from occurring.


Do NOT use Topiramate if:


  • you are allergic to any ingredient in Topiramate

  • you are taking a carbonic anhydrase inhibitor (eg, acetazolamide)

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



Before using Topiramate:


Some medical conditions may interact with Topiramate. Tell your health care provider 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 may become pregnant

  • if you have eye problems (eg, glaucoma), liver or kidney problems, kidney stones, or osteoporosis (weak bones) or soft bones; you drink alcohol regularly; you are on a ketogenic diet; or you are receiving kidney dialysis

  • if you have diarrhea, lung or breathing problems, low bicarbonate levels in the blood, or a growth problem, or you will be having surgery

  • if you have a history of status epilepticus (continuous seizure activity or a series of seizures without a full return to consciousness) or high blood acid levels (metabolic acidosis)

  • if you have a history of mental or mood problems (eg, depression), or suicidal thoughts or actions

  • if you take any other medicine for seizures

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


  • Anticholinergics (eg, benztropine), carbonic anhydrase inhibitors (eg, acetazolamide), haloperidol, or tricyclic antidepressants (eg, nortriptyline) because the risk of decreased sweating may be increased

  • Valproic acid because a serious side effect with symptoms of confusion, lethargy, and vomiting may occur

  • Metformin or pioglitazone because blood glucose control may be altered; monitor your blood sugar carefully if you use Topiramate with metformin or pioglitazone

  • Hydrochlorothiazide because it may increase the risk of Topiramate's side effects

  • Carbamazepine or hydantoins (eg, phenytoin) because they may decrease Topiramate's effectiveness

  • Amitriptyline because the risk of its side effects may be increased by Topiramate

  • Lithium because Topiramate may have an effect on lithium blood levels

  • Hormonal birth control (eg, birth control pills) or risperidone because their effectiveness may be decreased by Topiramate

This may not be a complete list of all interactions that may occur. Ask your health care provider if Topiramate 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 Topiramate:


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


  • Topiramate comes with an extra patient information sheet called a Medication Guide. Read it carefully. Read it again each time you get Topiramate refilled.

  • Take Topiramate by mouth with or without food.

  • Drink plenty of fluids while taking Topiramate to prevent kidney stones from forming.

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

  • Do not suddenly stop taking Topiramate. Suddenly stopping Topiramate may cause seizures to occur more often. If you need to stop Topiramate, your doctor will gradually lower your dose.

  • If you miss a dose of Topiramate, take it as soon as possible. If it is within 6 hours of your next dose, 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 more than 1 dose of Topiramate.

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



Important safety information:


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

  • Do not change your dose without checking with your doctor.

  • Do not drink alcohol while you take Topiramate.

  • Check with your doctor before you use medicines that may cause drowsiness (eg, sleep aids, muscle relaxers) while you are taking Topiramate; it may add to their effects. Ask your pharmacist if you have questions about which medicines may cause drowsiness.

  • Topiramate may reduce sweating, which could raise body temperature, especially in children. This risk is greater in hot weather and/or during vigorous exercise. Drink plenty of fluids. Dress lightly in hot climates or when exercising. Check carefully for signs of decreased sweating. If this occurs, promptly seek cooler or air-conditioned shelter and/or stop exercising. Seek medical attention right away if you have unexplained fever, mental or mood changes, headache, or dizziness.

  • Topiramate may cause high blood acid levels (metabolic acidosis). The risk may be greater in children and patients with kidney problems, severe breathing problems, or diarrhea. It may also be greater in patients who are taking certain other medicines (eg, acetazolamide), will be having surgery, or are on a ketogenic diet. Over a period of time, metabolic acidosis may cause kidney problems, bone problems, or decreased growth in children. Contact your doctor immediately if you experience fast breathing, unusual weakness or fatigue, sluggishness, persistent loss of appetite, or irregular heartbeat.

  • Patients who take Topiramate may be at increased risk of suicidal thoughts or actions. The risk may be greater in patients who have had suicidal thoughts or actions in the past. Watch patients who take Topiramate closely. Contact the doctor at once if new, worsened, or sudden symptoms such as depressed mood; anxious, restless, or irritable behavior; panic attacks; or any unusual change in mood or behavior occur. Contact the doctor right away if any signs of suicidal thoughts or actions occur.

  • Topiramate may cause serious eye problems that could lead to permanent loss of vision if not treated. Seek medical attention right away if you experience new eye symptoms (eg, blurred vision or other vision changes, eye pain or redness).

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

  • Hormonal birth control (eg, birth control pills) may not work as well while you are using Topiramate. To prevent pregnancy, use an extra form of birth control (eg, condoms). Discuss any questions or concerns with your doctor.

  • Lab tests, including serum bicarbonate levels, may be performed while you use Topiramate. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.

  • Use Topiramate with caution in the ELDERLY; they may be more sensitive to its effects.

  • Caution is advised when using Topiramate in CHILDREN; they may be more sensitive to its effects, especially decreased sweating and decreased bicarbonate levels.

  • Topiramate may affect growth rate in CHILDREN and teenagers in some cases. They may need regular growth checks while they take Topiramate.

  • Topiramate should be used with extreme caution in CHILDREN for migraines and in CHILDREN younger than 2 years for seizures; safety and effectiveness in these children have not been confirmed.

  • PREGNANCY and BREAST-FEEDING: Topiramate may cause birth defects if you take it while you are pregnant. Avoid becoming pregnant by using an effective form of birth control while you are taking Topiramate. If you think you may be pregnant or you are planning to become pregnant, contact your doctor. You will need to discuss the benefits and risks of taking Topiramate while you are pregnant. Topiramate is found in breast milk. If you are or will be breast-feeding while you take Topiramate, check with your doctor. Discuss any possible risks to your baby.


Possible side effects of Topiramate:


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:



Constipation; decreased sweating; diarrhea; dizziness; drowsiness; dry mouth; flu-like symptoms; headache; loss of appetite; nausea; nervousness; numbness or tingling of the skin; runny nose; sore throat; stomach pain or upset; taste changes; tiredness; trouble sleeping; 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); blood in the urine; blurred vision; bone pain; chest pain; confusion; decreased coordination; double vision or other vision changes; eye pain or redness; irregular heartbeat; loss of consciousness; memory problems; menstrual changes; muscle or joint pain, cramps, or weakness; new or worsening mental or mood changes (eg, aggressiveness, agitation, anxiety, depression, exaggerated feeling of well-being, hostility, impulsiveness, inability to sit still, irritability, panic attacks, restlessness); rapid, shallow breathing; red, swollen, blistered, or peeling skin; ringing in the ears; severe or persistent loss of appetite; severe stomach, side, or back pain; significant weight loss; speech problems; stupor; suicidal thoughts or actions; tremor; trouble thinking, concentrating, or remembering things; trouble walking; unexplained fever; unusual bruising or bleeding; unusual eye movements; unusual tiredness; vomiting.



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: Topiramate 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 agitation; depression; fainting; loss of coordination; mental impairment; seizures; severe drowsiness or dizziness; severe or persistent stomach pain; sluggishness; speech problems; stupor; vision problems (eg, blurred or double vision).


Proper storage of Topiramate:

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


General information:


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

  • Topiramate 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 Topiramate. 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 Topiramate resources


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


  • Topiramate Prescribing Information (FDA)

  • Topiramate Monograph (AHFS DI)

  • Topiramate Professional Patient Advice (Wolters Kluwer)

  • topiramate Advanced Consumer (Micromedex) - Includes Dosage Information

  • Topamax Prescribing Information (FDA)

  • Topamax Consumer Overview

  • Topiragen Prescribing Information (FDA)



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Monday, July 23, 2012

Solarcaine Lidocaine First Aid Spray Topical


Generic Name: lidocaine and prilocaine (Gingival route)


LYE-doe-kane, PRIL-oh-kane


Commonly used brand name(s)

In the U.S.


  • Oraqix

Available Dosage Forms:


  • Gel/Jelly

Therapeutic Class: Anesthetic, Amino Amide Combination


Chemical Class: Amino Amide


Uses For Solarcaine Lidocaine First Aid Spray


Lidocaine and prilocaine periodontal (gingival) gel is used on the gums to cause numbness or loss of feeling during dental procedures. This medicine contains a mixture of two topical local anesthetics (numbing medicines). It deadens the nerve endings in the gum.


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


Before Using Solarcaine Lidocaine First Aid Spray


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 lidocaine and prilocaine periodontal gel in the pediatric population. Safety and efficacy have not been established.


Geriatric


Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of lidocaine and prilocaine periodontal gel in the elderly. However, elderly patients are more likely to have age-related kidney or liver problems, which may require caution and an adjustment in the dose for patients receiving lidocaine and prilocaine periodontal gel.


Pregnancy








Pregnancy CategoryExplanation
All TrimestersBAnimal 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:


  • Glucose-6-phosphate dehydrogenase (G6PD) deficiency, history of or

  • Heart disease or

  • Heart rhythm problems—May cause side effects to become worse.

  • Methemoglobinemia (blood disorder), history of—Should not use in patients with this condition.

  • Liver disease, severe—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

Proper Use of lidocaine

This section provides information on the proper use of a number of products that contain lidocaine. It may not be specific to Solarcaine Lidocaine First Aid Spray. Please read with care.


A dentist or other trained health professional will give you this medicine in an office or clinic setting. The medicine is applied to the gums using a special dispenser.


Precautions While Using Solarcaine Lidocaine First Aid Spray


It is very important that your dentist check you closely for any problems or unwanted effects that may be caused by this medicine.


This medicine may cause serious types of allergic reactions, including anaphylaxis. Anaphylaxis can be life-threatening and requires immediate medical attention. Tell your dentist right away if you have a rash; itching; hoarseness; trouble with breathing; trouble with swallowing; or any swelling of your hands, face, or mouth after you receive the medicine.


This medicine may cause a rare, but serious blood problem called methemoglobinemia. Call your dentist right away if you develop a blue or bluish purple color on the lips, fingernails, or skin, or have headaches, dizziness, fainting, sleepiness, or trouble with breathing after you receive this medicine.


During the time that the gum feels numb, serious injury can occur. Be especially careful to avoid injury until the numbness wears off and you have normal feeling in the area. Avoid foods or liquids that are very hot or very cold. Do not chew gum or food while your mouth feels numb. You may accidentally bite your tongue or the inside of your cheeks.


Solarcaine Lidocaine First Aid Spray 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 or nurse immediately if any of the following side effects occur:


More common
  • Gum numbness that continues

  • gum swelling or irritation

  • nausea

Rare
  • Itching

  • hoarseness or trouble with swallowing

  • rash

  • shortness of breath

  • swelling of the eyelids, face, lips, or tongue

  • tightness in the chest

  • trouble with breathing

  • wheezing

Incidence not known
  • Blue or blue-purple color of lips, fingernails, mouth, or skin

  • blurred or double vision

  • convulsions

  • dark urine

  • dizziness or drowsiness

  • fainting

  • feeling hot, cold, or numb

  • headache

  • irregular or fast heartbeat

  • muscle twitching or trembling

  • nausea or vomiting

  • ringing or buzzing in the ears

  • shortness of breath or troubled breathing

  • unusual excitement, nervousness, or restlessness

  • unusual tiredness or weakness

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
  • Bad or bitter taste

  • headache

  • mouth pain or soreness

  • mouth ulcers

  • tiredness

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: Solarcaine Lidocaine First Aid Topical 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 Solarcaine Lidocaine First Aid Spray Topical resources


  • Solarcaine Lidocaine First Aid Spray Topical Side Effects (in more detail)
  • Solarcaine Lidocaine First Aid Spray Topical Use in Pregnancy & Breastfeeding
  • Solarcaine Lidocaine First Aid Spray Topical Support Group
  • 2 Reviews for Solarcaine Lidocaine First Aid Topical - Add your own review/rating


Compare Solarcaine Lidocaine First Aid Spray Topical with other medications


  • Anesthesia

Wednesday, July 18, 2012

TheraTears


Generic Name: ocular lubricant (OK yoo lar LOO bri kant)

Brand Names: Artificial Tears, Celluvisc, Clear Eyes CLR, Comfort Tears, Dry Eye Relief, GenTeal, Isopto Tears, Lacri-Lube S.O.P., Lacrisert, Lubricant Eye Drops, Moisture Drops, Oasis Tears, Opti-Free Rewetting Drops, optive, Refresh, Soothe, Sterilube, Systane, Systane Balance, Tears Again, Tears Naturale, Tears Renew, TheraTears, Ultra Fresh, Visine Tears


What is TheraTears (ocular lubricant)?

There are many brands and forms of ocular lubricant available and not all are listed on this leaflet.


Ocular lubricant is a solution specially formulated to moisten the eyes.


Ocular lubricant is used to relieve burning, irritation, and discomfort caused by dry eyes.

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


What is the most important information I should know about TheraTears (ocular lubricant)?


There are many brands and forms of ocular lubricant available and not all are listed on this leaflet.


You should not use an ocular lubricant if you are allergic to it. Ocular lubricant will not treat or prevent an eye infection.

Ask a doctor or pharmacist if it is safe for you to use this medicine if you have any type of infection in your eye.


Do not allow the dropper or tube tip to touch any surface, including the eyes or hands. If the dropper or tube becomes contaminated it could cause an infection in your eye, which can lead to vision loss or serious damage to the eye.


Stop using ocular lubricant and call your doctor if you have severe burning, stinging, irritation, eye pain, or vision changes.

This medication may cause blurred vision. Be careful if you drive or do anything that requires you to be able to see clearly.


Talk with your doctor if your symptoms do not improve or if they get worse while you are using ocular lubricant.

What should I discuss with my healthcare provider before using TheraTears (ocular lubricant)?


You should not use an ocular lubricant if you are allergic to it. Ocular lubricant will not treat or prevent an eye infection.

Ask a doctor or pharmacist if it is safe for you to use this medicine if you have any type of infection in your eye.


Ocular lubricant is not expected to harm an unborn baby. Ask a doctor or pharmacist about using ocular lubricant if you are pregnant. It is not known whether ocular lubricant passes into breast milk or if it could harm a nursing baby. Ask a doctor or pharmacist about using ocular lubricant if you are pregnant.

How should I use TheraTears (ocular lubricant)?


Use exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.


Do not use this medication while wearing contact lenses. Eye medication may contain a preservative that can discolor soft contact lenses. Wait at least 15 minutes after using this medication before putting your contact lenses in. Wash your hands before using ocular lubricant.

To apply the eye drops:



  • Tilt your head back slightly and pull down your lower eyelid to create a small pocket. Hold the dropper above the eye with the tip down. Look up and away from the dropper as you squeeze out a drop, then close your eye.




  • Use only the number of drops your doctor has prescribed.




  • Gently press your finger to the inside corner of the eye (near your nose) for about 1 minute to keep the liquid from draining into your tear duct. If you use more than one drop in the same eye, wait about 5 minutes before putting in the next drop.




  • Do not use the eye drops if the liquid has changed colors or has particles in it.



To apply the ointment:



  • Tilt your head back slightly and pull down your lower eyelid to create a small pocket. Hold the ointment tube with the tip pointing toward this pocket. Look up and away from the tip.




  • Squeeze out a ribbon of ointment 1/2-inch long into the lower eyelid pocket without touching the tip of the tube to your eye. Look down and close your eyes for a few minutes. Rolling your eyes around gently will help spread the ointment evenly.




  • After opening your eyes, you may have blurred vision for a short time. Avoid driving or doing anything that requires you to be able to see clearly.



Do not allow the dropper or tube tip to touch any surface, including the eyes or hands. If the dropper or tube becomes contaminated it could cause an infection in your eye, which can lead to vision loss or serious damage to the eye.


Talk with your doctor if your symptoms do not improve or if they get worse while you are using ocular lubricant. Store at room temperature away from moisture and heat. Do not freeze. Keep the bottle or tube tightly closed when not in use.

What happens if I miss a dose?


Since ocular lubricant is used on an as needed basis, you are not likely to miss a dose.


What happens if I overdose?


An overdose of ocular lubricant is not expected to be dangerous.


What should I avoid while using TheraTears (ocular lubricant)?


This medication may cause blurred vision. Be careful if you drive or do anything that requires you to be able to see clearly.


Avoid using other medications in your eyes during treatment with ocular lubricant unless your doctor tells you to.


TheraTears (ocular lubricant) 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 using ocular lubricant and call your doctor if you have a serious side effect such as:

  • severe burning, stinging, or eye irritation after using the medication;




  • eye pain; or




  • vision changes.



Less serious side effects may include:



  • mild eye burning or irritation;




  • itching or redness of your eyes;




  • watery eyes;




  • blurred vision; or




  • unpleasant taste in your mouth.



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 TheraTears (ocular lubricant)?


It is not likely that other drugs you take orally or inject will have an effect on ocular lubricant used in the eyes. But many drugs can interact with each other. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.



More TheraTears resources


  • TheraTears Use in Pregnancy & Breastfeeding
  • TheraTears Support Group
  • 1 Review for TheraTears - Add your own review/rating


  • FreshKote Drops MedFacts Consumer Leaflet (Wolters Kluwer)

  • Genteal Advanced Consumer (Micromedex) - Includes Dosage Information

  • Lacri-Lube S.O.P. Ointment MedFacts Consumer Leaflet (Wolters Kluwer)

  • Lacrisert Prescribing Information (FDA)

  • Lacrisert Insert MedFacts Consumer Leaflet (Wolters Kluwer)

  • Lacrisert Advanced Consumer (Micromedex) - Includes Dosage Information

  • Murine Tears Drops MedFacts Consumer Leaflet (Wolters Kluwer)

  • Murocel Eye Drops MedFacts Consumer Leaflet (Wolters Kluwer)

  • Refresh Redness Relief Drops MedFacts Consumer Leaflet (Wolters Kluwer)

  • Refresh liquigel



Compare TheraTears with other medications


  • Eye Dryness/Redness


Where can I get more information?


  • Your pharmacist can provide more information about ocular lubricant.


Tuesday, July 17, 2012

Sufentanil Citrate


Class: Opiate Agonists
VA Class: CN101
Chemical Name: N - [4 - (Methoxymethyl) - 1 - [2 - (2 - thieyl)ethyl] - 4 - piperidinyl] - N - phenylpropanamide2 - hydroxy - 1,2,3 - propanetricarboxylate (1:1)
Molecular Formula: C22H30N2O2S•O6H8O7
CAS Number: 60561-17-3
Brands: Sufenta

Introduction

Opiate agonist; synthetic phenylpiperidine derivative.1 3 4 5


Uses for Sufentanil Citrate


Anesthesia


As the analgesic component in the maintenance of balanced anesthesia (e.g., IV hypnotic and/or inhalation anesthetic, analgesic, skeletal muscle relaxant).1 17 34 36 41 46


As the primary anesthetic agent for induction and maintenance of general anesthesia when used in conjunction with 100% oxygen and a skeletal muscle relaxant (e.g., pancuronium bromide, succinylcholine chloride).1 10 11 12 13 15 16 18 35 37 38 39 43 44 45


Particularly useful when postoperative ventilation is anticipated and in providing favorable myocardial and cerebral oxygen balance.1 11 19 40 41 46


Cardiovascular parameters generally are more stable intraoperatively with use of sufentanil compared with inhalation agents.36 41 Incidence of postoperative hypertension and requirements for vasoactive agents or postoperative analgesics generally are decreased following use of moderate or high doses of sufentanil as compared with use of inhalation agents.1 36 38 41


Pain


Obstetric analgesia during labor and vaginal delivery.1 88


Sufentanil Citrate Dosage and Administration


General


Premedication



  • Selection of preanesthetic medication(s) should be based on the individual needs of the patient.1



Administration


Administer by IV injection, intermittent or continuous IV infusion, or epidural injection.1 4 7 8 10 11 12 13 19


IV Administration


For solution and drug compatibility information, see Compatibility under Stability.


Administration of small volumes may require use of a tuberculin syringe or equivalent.1


Rate of Administration

Administer by slow injection or intermittent or continuous infusion; individualize rate based on patient’s needs.1


Concomitant Administration of a Neuromuscular Blocking Agent

Risk of muscular rigidity (particularly of the truncal muscles) is related to the dose and rate of the infusion; however, administration of a neuromuscular blocking agent prior to sufentanil therapy can reduce the risk.1


The neuromuscular blocking agent used should be compatible with the patient’s condition, taking into account the hemodynamic effects of the drug, the cardiovascular status of the patient, existing drug therapy (e.g., preoperative use of β-adrenergic blocking agents), and the degree of skeletal muscle relaxation required.1











Administration of a Neuromuscular Blocking Agent with Sufentanil1

Sufentanil Dosage



Neuromuscular Blocking Agent Dosage



<8 mcg/kg



Administer up to 25% of the full paralyzing dose just prior to sufentanil1



>8 mcg/kg (titrated by slow IV infusion)



Administer a full paralyzing dose following loss of consciousness (e.g., loss of eyelash reflex, loss of response to voice command)1 61



>8 mcg/kg (rapidly administered anesthetic doses)



Administer a full paralyzing dose simultaneously with sufentanil1 or immediately after loss of consciousness61


Epidural Administration


For drug compatibility information, see Compatibility under Stability.


Specialized techniques are required for epidural administration; administration should be performed only by qualified individuals familiar with the techniques of administration, dosages, and special patient management problems associated with epidural administration.1


Dosage


Available as sufentanil citrate; dosage expressed in terms of sufentanil.1


Adjust dosage carefully according to body weight, individual requirements and response, physical status and underlying pathologic condition, premedication or concomitant medication(s), the anesthetic(s) being used, and the nature and duration of the surgery.1


Administer additional doses when patient movement and/or changes in vital signs indicate surgical stress or lightening of analgesia, and adjust according to individual requirements, response, and the anticipated remaining duration of the surgical procedure.1


Pediatric Patients


Anesthesia

General Anesthesia (as sole anesthetic agent) for Cardiovascular Surgery

IV

Children <12 years of age: Initially, 10–25 mcg/kg in conjunction with 100% oxygen and a skeletal muscle relaxant.1 8 61 Additional doses of up to 25–50 mcg each (or, alternatively, 1–2 mcg/kg each)61 may be given as needed based on response to the initial dose and as determined by changes in vital signs that indicate surgical stress or lightening of anesthesia.1


Neonates: Reduce dosage, especially in those with cardiovascular disease, according to the decrease in clearance.89 (See Pediatric Use under Cautions.)


Adults


Anesthesia

Analgesic Component of General Anesthesia

IV

Minor surgical procedures (expected duration of anesthesia is 1–2 hours): Total dosage of 1–2 mcg/kg in conjunction with nitrous oxide and oxygen; ≥75% of the total dosage may be given by slow injection or infusion prior to intubation.1 88 May administer supplemental doses of 10–25 mcg or administer intermittent or continuous maintenance infusions as necessary when movement and/or changes in vital signs indicate surgical stress or lightening of anesthesia; adjust maintenance infusion rate so that total dosage does not exceed 1 mcg/kg per hour of expected surgical time.1 88


Major surgical procedures (expected duration of anesthesia is 2–8 hours): Total dosage of 2–8 mcg/kg in conjunction with nitrous oxide and oxygen; ≤75% of the total dosage may be given by slow injection or infusion prior to intubation.1 88 May administer supplemental doses of 10–50 mcg or administer intermittent or continuous maintenance infusions as necessary when movement and/or changes in vital signs indicate surgical stress or lightening of anesthesia; adjust maintenance infusion rate so that total dosage does not exceed 1 mcg/kg per hour of expected surgical time.1 88


General Anesthesia (as sole anesthetic agent)

IV

Total dosage of 8–30 mcg/kg (by slow injection, infusion, or injection followed by infusion) in conjunction with oxygen and a skeletal muscle relaxant.1 88 Depending on the initial dose, may administer additional incremental doses of 0.5–10 mcg/kg by slow injection in anticipation of surgical stress (e.g., incision, sternotomy, cardiopulmonary bypass).1 88 Alternatively, may administer intermittent or continuous maintenance infusions as necessary as determined by changes in vital signs that indicate surgical stress and lightening of anesthesia; adjust maintenance infusion rate so that total dosage for the procedure does not exceed 30 mcg/kg.1 88


Pain

Obstetric Analgesia

Epidural

10–15 mcg (in combination with 10 mL of bupivacaine 0.125% with or without epinephrine).1 88 Doses may be repeated twice (for a total of 3 doses) at ≥1-hour intervals until delivery.1 88


Prescribing Limits


Adults


Anesthesia

Analgesic Component of General Anesthesia

IV

Minor or major surgical procedures: Total dose of ≤1 mcg/kg per hour of expected surgical time.1


General Anesthesia (as sole anesthetic agent)

IV

Total dose for procedure: ≤ 30 mcg/kg.1


Special Populations


Hepatic Impairment


Adjust dosage carefully; elimination of the drug may be decreased.1 60


Renal Impairment


Adjust dosage carefully; elimination of the drug may be decreased.1 60


Geriatric and Debilitated Patients


Reduce initial dosage;1 adjust additional doses according to the initial response and desired effect.1 61


Obese Patients


Base dosage on an estimate of ideal (lean) body weight if body weight exceeds ideal weight by >20%.1


Cautions for Sufentanil Citrate


Contraindications



  • Known hypersensitivity to sufentanil or intolerance to other opiate agonists.1



Warnings/Precautions


Warnings


Shares the toxic potentials of the opiate agonists; observe the usual precautions of opiate agonist therapy.1 4


Respiratory Depression

Respiratory function can be severely compromised.1


Consider the possibility of a recurrence of respiratory depression during recovery.4 A secondary rise in plasma concentrations may occur during the recovery period as blood perfusion to peripheral tissues increases and drug redistribution occurs.4


Administration of an opiate antagonist (e.g., naloxone) can reverse respiratory depression.1 The duration of respiratory depression produced by sufentanil may be longer than the duration of the opiate antagonist; therefore, continue appropriate patient monitoring following apparent initial reversal.1


Supervised Administration

Should be administered only by individuals experienced in the use of parenteral anesthetics and in the maintenance of an adequate airway and respiratory support.1


Opiate antagonist (e.g., naloxone) and facilities for intubation, administration of oxygen, and assisted or controlled respiration should be immediately available.1


Monitor vital signs routinely during administration; facilities for postoperative monitoring and assisted or controlled respiration should be available following administration of anesthetic doses of the drug (i.e., ≥8 mcg/kg).1


Major Toxicities


Musculoskeletal Effects

Possible skeletal muscle rigidity (e.g., of the truncal muscles); onset may be more rapid than with fentanyl.1 Administration of a neuromuscular blocking agent may be necessary.1 (See Concomitant Administration of a Neuromuscular Blocking Agent under Dosage and Administration.)


General Precautions


CNS Effects

Caution in patients with head injuries; sufentanil may obscure the clinical course.1


Impaired Respiration

Caution in patients with pulmonary disease, decreased respiratory reserve, or potentially compromised respiratory function.1 Further decreases in respiratory function and increases in airway resistance may occur.1


Cardiovascular Effects

Generally produces few cardiovascular effects.4 8 13 17 39 Possible hypotension1 8 10 34 36 39 40 or hypertension.1 8 10 18 35 37 38 40 41 42 Bradycardia occurs infrequently during anesthesia and may be corrected by administration of atropine.1


Specific Populations


Pregnancy

Category C.1


Used epidurally for analgesia during labor and delivery.1 88 Not recommended for IV use during labor and delivery; avoid epidural dosages in excess of the recommended dosage.1


Lactation

Not known whether sufentanil is distributed into milk.1 Caution if used in nursing women.1


Pediatric Use

Safety and efficacy documented in a limited number of children ≥1 day of age undergoing cardiovascular surgery.1 8 89


Use with caution in neonates because decreased clearance may result in increased blood concentrations of the drug.89 Clearance in healthy neonates is approximately one-half that reported in adults and children; may be further reduced by up to one-third in neonates with cardiovascular disease.89


Geriatric Use

Consider dosage reduction.1 61 (See Geriatric and Debilitated Patients under Dosage and Administration.)


Hepatic Impairment

Use with caution, since the drug undergoes metabolism in the liver.1


Renal Impairment

Use with caution, since the drug and its metabolites are eliminated mainly by the kidneys.1


Common Adverse Effects


Respiratory depression,1 38 skeletal muscle rigidity (e.g., truncal muscles, neck, extremities).1 4 13 38


Interactions for Sufentanil Citrate


Specific Drugs





















Drug



Interaction



Comments



β-Adrenergic blocking agents



Possible increased incidence and degree of bradycardia and hypotension during sufentanil induction in patients receiving chronic β-blocker therapy1



Patients with CAD receiving chronic preoperative β-blocker therapy appear to require lower initial and fewer supplemental doses of sufentanil during CABG surgery than do patients who have not received preoperative β-blocker therapy10



Calcium-channel blocking agents



Increased incidence and degree of bradycardia and hypotension during sufentanil induction in patients receiving chronic calcium-channel blocker therapy1



CNS depressants (e.g., opiate agonists, general anesthetics, tranquilizers, sedatives, hypnotics)



Potentiation of CNS and cardiovascular effects1



Use with caution; reduce dosage of at least one of the drugs when used concomitantly1



Nitrous oxide



Possible cardiovascular depression, manifested by bradycardia and decreases in mean arterial pressure and cardiac output, following concomitant administration of nitrous oxide with high doses of sufentanil1



Neuromuscular blocking agents



Possible tachycardia following administration of high doses of pancuronium during anesthesia with sufentanil and oxygen;1 4 38 hypertension and an increase in cardiac index may occur4


Bradycardia and hypotension reported during anesthesia during concomitant administration of neuromuscular blocking agents with sufentanil and oxygen; effects may be increased in patients also receiving calcium-channel blockers or β-blockers;1 bradycardia reported rarely following concomitant administration of sufentanil with succinylcholine1



To maintain a stable, lower HR and BP during anesthesia, use moderate doses of pancuronium or use a neuromuscular blocking agent with a lesser inhibitory effect on the vagus nerve 1


Sufentanil Citrate Pharmacokinetics


Absorption


Onset


Following IV administration, the onset of action as determined by time to unconsciousness (i.e., loss of response to voice command) is 1.2–3 minutes.4 10 13 15 16 18


Following epidural administration of 10–15 mcg and 0.125% bupivacaine with epinephrine 1:200,000 during the first stage of labor, the onset of action occurs within 10 minutes.1 88


Duration


The mean duration of anesthesia is 40 minutes following initial IV dose of 0.4 mcg/kg and 41–44 minutes following additional doses of 0.1 mcg/kg.20 Following administration of anesthetic doses (about 13–19 mcg/kg total), patient response to verbal command4 13 15 and adequate ventilation4 15 occurs at 0.6–1.8 and 5.6 hours, respectively.


Following IM administration of single doses of 0.15, 0.3, or 0.5 mcg/kg in patients with pain, the approximate duration of detectable analgesia was 2.3, 3.7, and 3.8 hours, respectively.21


Following epidural administration of 10–15 mcg and 0.125% bupivacaine with epinephrine 1:200,000 during the first stage of labor, the duration of action was 1–2 hours.1 88


Distribution


Extent


Distribution into human body tissues and fluids has not been fully characterized;14 however, the drug is highly lipophilic and is rapidly and extensively distributed in animals.4


Not known whether sufentanil crosses the placenta2 or distributes into milk.1 2


Plasma Protein Binding


Approximately 93% bound at plasma pH 7.41 4 6 14 (mainly to albumin; α-, α1-, β-, and γ-globulins; and α1-acid glycoprotein).6 14


Because a large portion of the drug appears to be bound to α1-acid glycoprotein, binding may be affected by disease states in which this protein is altered.4 6 14 24


Binding in plasma is independent of plasma drug concentration within the therapeutic range (i.e., 0.1–10 ng/mL);4 6 however, binding is affected by changes in plasma pH.4 6 14 Increases in plasma pH from 7.4 to 7.8 increase sufentanil binding by about 30%; decreases in plasma pH from 7.4 to 7 decrease binding by about 30%.6


Elimination


Metabolism


Appears to be metabolized mainly in the liver and small intestine1 2 via N-dealkylation and O-demethylation.4


The O-demethylated metabolite appears to have about 10% of the analgesic activity of the unchanged drug.4


Elimination Route


Excreted principally in urine and also in feces via biliary elimination;1 2 60 only 2% of a dose is excreted unchanged in urine and feces.1 2


Half-life


Triphasic; plasma concentrations decline rapidly secondary to redistribution.1 2 4 5 14 22


In adults with normal renal and hepatic function, the plasma half-life averages 0.72–1.2 minutes in the initial (distribution) phase, 13.7–17 minutes in the second (redistribution) phase, and 140–158 minutes in the terminal (elimination) phase.1 2 4 5 14 22 23


Elimination half-life is longer (434 minutes) in neonates but shorter in infants and children (97 minutes), compared with adults and adolescents.89


Stability


Storage


Parenteral


Injection

15–25°C; protect from light.1


Compatibility


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


Parenteral


Sufentanil citrate is hydrolyzed in acidic solutions.60


Solution Compatibilitya






Compatible



Dextrose 5% in water



Variable



Sodium chloride 0.9%


Drug Compatibility




Admixture Compatibilitya

Compatible



Bupivacaine HCl



























Y-Site Compatibilitya

Compatible



Amphotericin B cholesteryl sulfate complex



Atropine sulfate



Dexamethasone sodium phosphate



Diazepam



Diphenhydramine HCl



Etomidate



Gatifloxacin



Haloperidol lactate



Hetastarch in lactated electrolyte injection (Hextend)



Hydroxyzine HCl



Ketorolac tromethamine



Linezolid



Metoclopramide HCl



Midazolam HCl



Phenobarbital sodium



Prochlorperazine edisylate



Propofol



Remifentanil HCl



Scopolamine HBr



Incompatible



Lorazepam



Phenytoin sodium



Thiopental sodium


ActionsActions



  • A potent analgesic;1 shares the actions of the opiate agonists.1 4 29




  • Precise mechanism of action has not been fully elucidated; opiate agonists act at several CNS sites, involving several neurotransmitter systems to produce analgesia.b




  • Pain perception is altered in the spinal cord and higher CNS levels (e.g., substantia gelatinosa, spinal trigeminal nucleus, periaqueductal gray, periventricular gray, medullary raphe nuclei, hypothalamus).26 b




  • Opiate agonists do not alter the threshold or responsiveness of afferent nerve endings to noxious stimuli, nor peripheral nerve impulse conduction.26




  • Opiate agonists act at specific receptor binding sites in the CNS and other tissues; opiate receptors are concentrated in the limbic system, thalamus, striatum, hypothalamus, midbrain, and spinal cord.b




  • High affinity and selectivity for the μ-opiate receptor in the CNS; reportedly is more selective and binds more tightly to this receptor than does fentanyl.4 9 12 25 49 52




  • Produces dose-related analgesia;1 2 4 at doses up to 8 mcg/kg, the drug has a potent analgesic effect, but higher doses usually produce substantial CNS depression resulting in hypnosis and anesthesia.1 2 4 9 10 11 12 13 19




  • Analgesic potency appears to be 5–12 times that of fentanyl on a weight basis.1 12 23 39 40 47 48 50




  • Appears to have little effect on histamine release.1 7 53 54 61




  • May have a centrally mediated vagal effect.4 60 61



Advice to Patients



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




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


Subject to control under the Federal Controlled Substances Act of 1970 as a schedule II (C-II) drug.1


* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name


















Sufentanil Citrate

Routes



Dosage Forms



Strengths



Brand Names



Manufacturer



Parenteral



Injection



50 mcg (of sufentanil) per mL*



Sufenta (C-II; preservative-free)



Akorn



Sufentanil Citrate Injection (C-II; preservative-free)



Baxter, Hospira



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 October 2006. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.




References



1. Taylor Pharmaceuticals. Sufenta injection prescribing information. Decatur, IL: 1998 Aug.



2. Janssen Pharmaceutica. Product information form for American Hospital Formulary Service on Sufenta. Piscataway, NJ; 1984 Apr 5.



3. Windholz M, ed. The Merck index. 10th ed. Rahway, NJ: Merck & Co., Inc.; 1983:APP-3.



4. Rosow CE. Sufentanil citrate: a new opioid analgesic for use in anesthesia. Pharmacotherapy. 1984; 4:11-9. [IDIS 393492] [PubMed 6230606]



5. Michiels M, Hendriks R, Heykants J. Radioimmunoassay of the new opiate analgesics alfentanil and sufentanil. Preliminary pharmacokinetic profile in man. J Pharm Pharmacol. 1983; 35:86-93. [IDIS 165823] [PubMed 6131992]



6. Meuldermans WEG, Hurkmans RMA, Heykants JJP. Plasma protein binding and distribution of fentanyl, sufentanil, alfentanil and lofentanil in blood. Arch Int Pharmacodyn Ther. 1982; 257:4-19. [PubMed 6214227]



7. Rosow CE, Philbin DM, Keegan CR et al. Hemodynamics and histamine release during induction with sufentanil or fentanyl. Anesthesiology. 1984; 60:489-91. [IDIS 185009] [PubMed 6201089]



8. Hickey PR, Hansen DD. Fentanyl- and sufentanil-oxygen-pancuronium anesthesia for cardiac surgery in infants. Anesth Analg. 1984; 63:117-24. [IDIS 180669] [PubMed 6229197]



9. Rosenbaum JS, Holford NH, Richards ML et al. Discrimination of three types of opioid binding sites in rat brain in vivo. Mol Pharmacol. 1984; 25:242-8. [PubMed 6321946]



10. Stanley TH, de Lange S, Boscoe MJ et al. The influence of chronic preoperative propranolol therapy on cardiovascular dynamics and narcotic requirements during operation in patients with coronary artery disease. Can Anaesth Soc J. 1982; 29:319-24. [IDIS 154371] [PubMed 6213289]



11. de Lange S, Boscoe MJ, Stanley TH et al. Antidiuretic and growth hormone responses during coronary artery surgery with sufentanil-oxygen and alfentanil-oxygen anesthesia in man. Anesth Analg. 1982; 61:434-8. [IDIS 151510] [PubMed 6461279]



12. de Lange S, Stanley TH, Boscoe MJ et al. Catecholamine and cortisol responses to sufentanil-O2 and alfentanil-O2 anaesthesia during coronary artery surgery. Can Anaesth Soc J. 1983; 30:248-54. [IDIS 170873] [PubMed 6242846]



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31. Keykhah MM, Smith DS, Englebach I et al. Effects of naloxone on cerebral blood flow and metabolism. Anesthesiology. 1983; 59:A309.



32. Bovill JG, Sebel PS. Pharmacokinetics of high-dose fentanyl: a study in patients undergoing cardiac surgery. Br J Anaesth. 1980; 52:795-801. [IDIS 123648] [PubMed 7426257]



33. Lunn JK, Stanley TH, Eisele J et al. High dose fentanyl anesthesia for coronary artery surgery: plasma fentanyl concentrations and influence of nitrous oxide on cardiovascular responses. Anesth Analg. 1979; 58:390-5. [IDIS 105685] [PubMed 314761]



34. Flacke JW, Kripke BK, Bloor BC et al. Intraoperative effectiveness of sufentanil, fentanyl, meperidine, or morphine in balanced anesthesia: a double-blind study. Anesth Analg. 1983; 62:259-60.



35. Howie MB, Lingam RP, Lee JJ et al. Sufentanil-oxygen compared with fentanyl-oxygen anesthesia for coronary artery surgery. Anesthesiology. 1982; 57:A292.



36. Fahmy NR. Clinical evaluation of sufentanil-N2O and isoflurane-N2O anesthesia during major orthopedic surgical procedures. In: Advances in anesthesia: a new synthetic narcotic for the 80s; proceedings of a symposium; 1983 Oct 8; Atlanta, GA.



37. Khoury GF, Estafanous FG, Zurick AM et al. Sufentanil/pancuronium versus sufentanil/metocurine anesthesia for coronary artery surgery. Anesthesiology. 1982; 57:A47.



38. Khoury GF, Estafanous FG, Samonte AF et al. Evaluation of sufentanil-O2 versus halothane-N2O/O2 anesthesia for coronary artery surgery. Anesthesiology. 1982; 57:A290.



39. Sebel PS, Bovill JG. Cardiovascular effects of sufentanil anesthesia. Anesth Analg. 1982; 61:115-9. [IDIS 152035] [PubMed 6119930]



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43. Smith NT, Dec-Silver H, Sanford TJ Jr et al. EEGs during high-dose fentanyl-, sufentanil-, or morphine-oxygen anesthesia. Anesth Analg. 1984; 63:386-93. [IDIS 183550] [PubMed 6230952]



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45. Sebel PS, Bovill JG, Wauquier A. Total narcotic anesthesia with sufentanil. Anesth Analg. 1981; 60:276.



46. McKay RD, Varner PD, Hendricks PL et al. The evaluation of sufentanil-N2O-O2 vs. fentanyl-N2O-O2 anesthesia for craniotomy. Anesth Analg. 1984; 63:250.



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53. Flacke JW, Van Etten A, Flacke WE. Greatest histamine release from meperidine among four narcotics: double-blind study in man. Anesthesiology. 1983; 59:A51.



54. Flacke WE, Van Etten AP, Flacke JW et al. Plasma histamine levels during sufentanil anesthesia for coronary bypass graft surgery. Anesth Analg. 1983; 62:260-1.



55. Bovill JG, Sebel PS, Fiolet JWT et al. The influence of sufentanil on endocrine and metabolic responses to cardiac surgery. Anesth Analg. 1983; 62:391-7. [IDIS 168279] [PubMed 6219596]



56. Young ML, Smith DS, Greenberg J et al. Effects of sufentanil on regional cerebral glucose metabolism in rats. Anesthesiology. 1983; 59:A335.



57. Keykhah MM, Smith DS, C et al. Effects of sufentanil on cerebral blood flow and oxygen consumption. Anesthesiology. 1982; 57:A248.



58. C.dtdson C, Keykhah M, Smith DS et al. Influence of high dose fentanyl on cerebral blood flow and metabolism. Acta Physiol Scand. 1981; 113:271-2.



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60. King W (Janssen Pharmaceutica, Piscataway, NJ): Personal communication; 1984 October 19 and 31.



61. Reviewer’s comments (personal observations); 1984 October.



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63. Sebel PS, Bovill JG, Schellekens APM et al. Hormonal responses to high-dose fentanyl anaesthesia: a study in patients undergoing cardiac surgery. Br J Anaesth. 1981; 53:941-8. [IDIS 140705] [PubMed 7025877]



64. Howie MB, Smith DF, Harrington K et al. Serum concentrations of sufentanil and fentanyl in the post-operative course in cardiac surgery patients. Anesthesiology. 1984; 61:A131.



65. Mummaneni N, Rao TL, Montoya A. Awareness and recall with high-dose fentanyl-oxygen anesthesia. Anesth Analg. 1980; 59:948-9. [IDIS 129874] [PubMed 7192516]



66. Gosselin RE, Hodge HC, Smith RP et al. Clinical toxicology of commercial products. 5th ed. Baltimore: Williams & Wilkins Co.; 1984: III-284-9.



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68. Howie MB, Smith DF, Dasta JF et al. Pharmacokinetic comparison of sufentanil and fentanyl during anesthesia for cardiac surgery. Anesthesiology. 1984; 61:A377.



69. Helgenberg JC. Intraoperative awareness during high-dose fentanyl oxygen anesthesia. Anesthesiology. 1981; 54:341-3. [IDIS 133978]