Emplex may be available in the countries listed below.
Ingredient matches for Emplex
Methotrexate
Methotrexate is reported as an ingredient of Emplex in the following countries:
- Slovakia
International Drug Name Search
Sunday, 25 July 2010
Tuesday, 20 July 2010
Levofloxacin Sandoz
Levofloxacin Sandoz may be available in the countries listed below.
Ingredient matches for Levofloxacin Sandoz
Levofloxacin
Levofloxacin hemihydrate (a derivative of Levofloxacin) is reported as an ingredient of Levofloxacin Sandoz in the following countries:
- Switzerland
International Drug Name Search
Bell Homatropine
Bell Homatropine may be available in the countries listed below.
Ingredient matches for Bell Homatropine
Homatropine
Homatropine Hydrobromide is reported as an ingredient of Bell Homatropine in the following countries:
- India
International Drug Name Search
Monday, 19 July 2010
Novatec
Novatec may be available in the countries listed below.
Ingredient matches for Novatec
Lisinopril
Lisinopril is reported as an ingredient of Novatec in the following countries:
- Luxembourg
International Drug Name Search
Tuesday, 13 July 2010
Flox
Flox may be available in the countries listed below.
Ingredient matches for Flox
Norfloxacin
Norfloxacin is reported as an ingredient of Flox in the following countries:
- Brazil
International Drug Name Search
Saturday, 10 July 2010
Duac
Dosage Form: topical gel
Duac® (clindamycin phosphate and benzoyl peroxide) Gel, 1.2%/5%
For Dermatological Use Only.
Not for Ophthalmic Use.
Rx Only
Duac Description
Duac® Gel contains clindamycin phosphate, (7(S)-chloro-7-deoxylincomycin-2-phosphate), equivalent to 1% clindamycin, and 5% benzoyl peroxide.
Clindamycin phosphate is a water soluble ester of the semi-synthetic antibiotic produced by a 7(S)-chloro-substitution of the 7(R)-hydroxyl group of the parent antibiotic lincomycin.
Clindamycin phosphate is C18H34ClN2O8PS. The structural formula for clindamycin phosphate is represented below:
Clindamycin phosphate has a molecular weight of 504.97 and its chemical name is methyl 7 - chloro - 6,7,8 - trideoxy - 6 - (1 - methyl - trans - 4 - propyl - L - 2 - pyrrolidinecarboxamido) - 1 - thio - L - threo - α - D - galacto - octopyranoside 2-(dihydrogen phosphate).
Benzoyl peroxide is C14H10O4. It has the following structural formula:
Benzoyl peroxide has a molecular weight of 242.23.
Each gram of Duac® Gel contains 10 mg (1%) clindamycin, as phosphate, and 50 mg (5%) benzoyl peroxide in a base consisting of carbomer homopolymer (type C), dimethicone, disodium lauryl sulfosuccinate, edetate disodium, glycerin, methylparaben, poloxamer 182, purified water, silicon dioxide, and sodium hydroxide.
Duac - Clinical Pharmacology
A comparative study of the pharmacokinetics of Duac® Gel and 1% clindamycin solution alone in 78 patients indicated that mean plasma clindamycin levels during the four week dosing period were < 0.5 ng/ml for both treatment groups.
Benzoyl peroxide has been shown to be absorbed by the skin where it is converted to benzoic acid. Less than 2% of the dose enters systemic circulation as benzoic acid.
Microbiology
Mechanism of Action
Clindamycin binds to the 50S ribosomal subunits of susceptible bacteria and prevents elongation of peptide chains by interfering with peptidyl transfer, thereby suppressing protein synthesis.
Benzoyl peroxide is a potent oxidizing agent.
In Vivo Activity
No microbiology studies were conducted in the clinical trials with this product.
In Vitro Activity
The clindamycin and benzoyl peroxide components individually have been shown to have in vitro activity against Propionibacterium acnes, an organism which has been associated with acne vulgaris; however, the clinical significance of this is not known.
Drug Resistance
There are reports of an increase of P. acnes resistance to clindamycin in the treatment of acne. In patients with P. acnes resistant to clindamycin, the clindamycin component may provide no additional benefit beyond benzoyl peroxide alone.
Clinical Studies
In five randomized, double-blind clinical studies of 1,319 patients, 397 used Duac® Gel, 396 used benzoyl peroxide, 349 used clindamycin and 177 used vehicle. Duac® Gel applied once daily for 11 weeks was significantly more effective than vehicle, benzoyl peroxide, and clindamycin in the treatment of inflammatory lesions of moderate to moderately severe facial acne vulgaris in three of the five studies (Studies 1, 2, and 5).
Patients were evaluated and acne lesions counted at each clinical visit: weeks 2, 5, 8, 11. The primary efficacy measures were the lesion counts and the investigator’s global assessment evaluated at week 11. Patients were instructed to wash the face, wait 10 to 20 minutes, and then apply medication to the entire face, once daily, in the evening before retiring. Percent reductions in inflammatory lesion counts after treatment for 11 weeks in these five studies are shown in the following table:
Study 1 (n=120) | Study 2 (n=273) | Study 3 (n=280) | Study 4 (n=288) | Study 5 (n=358) | |
| Duac® Gel | 65% | 56% | 42% | 57% | 52% |
| Benzoyl Peroxide | 36% | 37% | 32% | 57% | 41% |
| Clindamycin | 34% | 30% | 38% | 49% | 33% |
| Vehicle | 19% | -0.4% | 29% | 29% | |
The Duac® Gel group showed greater overall improvement in the investigator’s global assessment than the benzoyl peroxide, clindamycin and vehicle groups in three of the five studies (Studies 1, 2, and 5).
Clinical studies have not adequately demonstrated the effectiveness of Duac® Gel versus benzoyl peroxide alone in the treatment of non-inflammatory lesions of acne.
Indications and Usage for Duac
Duac® Gel is indicated for the topical treatment of inflammatory acne vulgaris.
Duac® Gel has not been demonstrated to have any additional benefit when compared to benzoyl peroxide alone in the same vehicle when used for the treatment of non-inflammatory acne.
Contraindications
Duac® Gel is contraindicated in those individuals who have shown hypersensitivity to any of its components or to lincomycin. It is also contraindicated in those having a history of regional enteritis, ulcerative colitis, pseudomembranous colitis, or antibiotic-associated colitis.
Warnings
ORALLY AND PARENTERALLY ADMINISTERED CLINDAMYCIN HAS BEEN ASSOCIATED WITH SEVERE COLITIS WHICH MAY RESULT IN PATIENT DEATH. USE OF THE TOPICAL FORMULATION OF CLINDAMYCIN RESULTS IN ABSORPTION OF THE ANTIBIOTIC FROM THE SKIN SURFACE. DIARRHEA, BLOODY DIARRHEA, AND COLITIS (INCLUDING PSEUDOMEMBRANOUS COLITIS) HAVE BEEN REPORTED WITH THE USE OF TOPICAL AND SYSTEMIC CLINDAMYCIN. STUDIES INDICATE A TOXIN(S) PRODUCED BY CLOSTRIDIA IS ONE PRIMARY CAUSE OF ANTIBIOTIC-ASSOCIATED COLITIS. THE COLITIS IS USUALLY CHARACTERIZED BY SEVERE PERSISTENT DIARRHEA AND SEVERE ABDOMINAL CRAMPS AND MAY BE ASSOCIATED WITH THE PASSAGE OF BLOOD AND MUCUS. ENDOSCOPIC EXAMINATION MAY REVEAL PSEUDOMEMBRANOUS COLITIS. STOOL CULTURE FOR Clostridium difficile AND STOOL ASSAY FOR Clostridium difficile TOXIN MAY BE HELPFUL DIAGNOSTICALLY. WHEN SIGNIFICANT DIARRHEA OCCURS, THE DRUG SHOULD BE DISCONTINUED. LARGE BOWEL ENDOSCOPY SHOULD BE CONSIDERED TO ESTABLISH A DEFINITIVE DIAGNOSIS IN CASES OF SEVERE DIARRHEA. ANTIPERISTALTIC AGENTS SUCH AS OPIATES AND DIPHENOXYLATE WITH ATROPINE MAY PROLONG AND/OR WORSEN THE CONDITION. DIARRHEA, COLITIS AND PSEUDOMEMBRANOUS COLITIS HAVE BEEN OBSERVED TO BEGIN UP TO SEVERAL WEEKS FOLLOWING CESSATION OF ORAL AND PARENTERAL THERAPY WITH CLINDAMYCIN.
Mild cases of pseudomembranous colitis usually respond to drug discontinuation alone. In moderate to severe cases, consideration should be given to management with fluids and electrolytes, protein supplementation and treatment with an antibacterial drug clinically effective against Clostridium difficile colitis.
Precautions
General
For dermatological use only; not for ophthalmic use. Concomitant topical acne therapy should be used with caution because a possible cumulative irritancy effect may occur, especially with the use of peeling, desquamating, or abrasive agents.
The use of antibiotic agents may be associated with the overgrowth of nonsusceptible organisms, including fungi. If this occurs, discontinue use of this medication and take appropriate measures.
Avoid contact with eyes and mucous membranes.
Clindamycin and erythromycin containing products should not be used in combination. In vitro studies have shown antagonism between these two antimicrobials. The clinical significance of this in vitro antagonism is not known.
Information for Patients
Patients using Duac® Gel should receive the following information and instructions:
- Duac® Gel is to be used as directed by the physician. It is for external use only. Avoid contact with eyes, and inside the nose, mouth, and all mucous membranes, as this product may be irritating.
- This medication should not be used for any disorder other than that for which it was prescribed.
- Patients should not use any other topical acne preparation unless otherwise directed by their physician.
- Patients should report any signs of local adverse reactions to their physician. Patients who develop allergic symptoms such as severe swelling or shortness of breath should discontinue use and contact their physician immediately.
- Duac® Gel may bleach hair or colored fabric.
- Duac® Gel can be stored at room temperature up to 25°C (77°F) for up to 2 months. Do not freeze. Keep tube tightly closed. Keep out of the reach of small children. Discard any unused product after 2 months.
- Before applying Duac® Gel to affected areas, wash the skin gently, rinse with warm water, and pat dry.
- Excessive or prolonged exposure to sunlight should be limited. To minimize exposure to sunlight, a hat or other clothing should be worn.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Benzoyl peroxide has been shown to be a tumor promoter and progression agent in a number of animal studies. Benzoyl peroxide in acetone at doses of 5 and 10 mg administered twice per week induced squamous cell skin tumors in transgenic TgAC mice in a study using 20 weeks of topical treatment. The clinical significance of this is unknown.
In a 2-year dermal carcinogenicity study in mice, treatment with Duac® Gel at doses up to 8000 mg/kg/day (16 times the highest recommended adult human dose of 2.5 g Duac® Gel, based on mg/m2) did not cause an increase in skin tumors. However, topical treatment with another formulation containing 1% clindamycin and 5% benzoyl peroxide at doses of 100, 500, or 2000 mg/kg/day caused a dose-dependent increase in the incidence of keratoacanthoma at the treated skin site of male rats in a 2-year dermal carcinogenicity study in rats.
In a 52-week photocarcinogenicity study in hairless mice (40 weeks of treatment followed by 12 weeks of observation), the median time to onset of skin tumor formation decreased and the number of tumors per mouse increased relative to controls following chronic concurrent topical treatment with Duac® Gel and exposure to ultraviolet radiation.
Genotoxicity studies were not conducted with Duac® Gel. Clindamycin phosphate was not genotoxic in Salmonella typhimurium or in a rat micronucleus test. Benzoyl peroxide has been found to cause DNA strand breaks in a variety of mammalian cell types, to be mutagenic in Salmonella typhimurium tests by some but not all investigators, and to cause sister chromatid exchanges in Chinese hamster ovary cells.
Studies have not been performed with Duac® Gel or benzoyl peroxide to evaluate the effect on fertility. Fertility studies in rats treated orally with up to 300 mg/kg/day of clindamycin (approximately 120 times the amount of clindamycin in the highest recommended adult human dose of 2.5 g Duac® Gel, based on mg/m2) revealed no effects on fertility or mating ability.
Pregnancy
Teratogenic Effects
Pregnancy Category C
Animal reproduction studies have not been conducted with Duac® Gel or benzoyl peroxide. It is also not known whether Duac® Gel can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Duac® Gel should be given to a pregnant woman only if clearly needed.
Developmental toxicity studies performed in rats and mice using oral doses of clindamycin up to 600 mg/kg/day (240 and 120 times the amount of clindamycin in the highest recommended adult human dose based on mg/m2, respectively) or subcutaneous doses of clindamycin up to 250 mg/kg/day (100 and 50 times the amount of clindamycin in the highest recommended adult human dose based on mg/m2, respectively) revealed no evidence of teratogenicity.
Nursing Women
It is not known whether Duac® Gel is secreted into human milk after topical application. However, orally and parenterally administered clindamycin has been reported to appear in breast milk. Because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric Use
Safety and effectiveness of this product in pediatric patients below the age of 12 have not been established.
Adverse Reactions
During clinical trials, all patients were graded for facial erythema, peeling, burning, and dryness on the following scale: 0 = absent, 1 = mild, 2 = moderate, and 3 = severe. The percentage of patients that had symptoms present before treatment (at baseline) and during treatment were as follows:
| Before Treatment (Baseline) | During Treatment | |||||
| Mild | Moderate | Severe | Mild | Moderate | Severe | |
| Erythema | 28% | 3% | 0 | 26% | 5% | 0 |
| Peeling | 6% | <1% | 0 | 17% | 2% | 0 |
| Burning | 3% | <1% | 0 | 5% | <1% | 0 |
| Dryness | 6% | <1% | 0 | 15% | 1% | 0 |
(Percentages derived by # subjects with symptom score/# enrolled Duac® Gel subjects, n = 397).
Anaphylaxis, as well as allergic reactions leading to hospitalization, has been reported in post-marketing use with Duac® Gel. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to a drug exposure.
Duac Dosage and Administration
Duac® Gel should be applied once daily, in the evening or as directed by the physician, to affected areas after the skin is gently washed, rinsed with warm water and patted dry.
How is Duac Supplied
Duac® (clindamycin phosphate and benzoyl peroxide), 1.2%/5% Gel is available in:
- 45 gram tube NDC 0145-2371-05
Prior to Dispensing: Store in a cold place, preferably in a refrigerator, between 2°C and 8°C (36°F and 46°F). Do not freeze.
Dispensing Instructions for the Pharmacist: Dispense Duac® Gel with a 60 day expiration date and specify “Store at room temperature up to 25°C (77°F). Do not freeze.”
Keep tube tightly closed. Keep out of the reach of small children.
©2011 Stiefel Laboratories, Inc.
Stiefel Laboratories, Inc.
Research Triangle Park, NC 27709
DUA:4PI
Rev. July 2011
Duac is a registered trademark of Stiefel Laboratories, Inc.
Principal Display Panel
NDC 0145-2371-05
Duac®
(clindamycin phosphate and benzoyl peroxide) Gel, 1.2%/5%
45 grams
Rx only
For external use only
DEVCOMP-0001937
Principal Display Panel
NDC 0145-5371-61
Duac®
(clindamycin phosphate and benzoyl peroxide) Gel, 1.2%/5%
20 x 5 g
Professional Samples
Rx only
For external use only.
Available in 45 gram tubes
DEVCOMP-0001935
Principal Display Panel
NDC 0145-2367-01
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| Marketing Information | |||
| Marketing Category | Application Number or Monograph Citation | Marketing Start Date | Marketing End Date |
| NDA | NDA050741 | 10/22/2007 | |
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| Marketing Information | |||
| Marketing Category | Application Number or Monograph Citation | Marketing Start Date | Marketing End Date |
| NDA | NDA050741 | 03/01/2011 | |
| Duac clindamycin phosphate and benzoyl peroxide gel | ||||||||||||||||||||||||
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| Marketing Information | |||
| Marketing Category | Application Number or Monograph Citation | Marketing Start Date | Marketing End Date |
| NDA | NDA050741 | 10/22/2007 | 12/31/2012 |
| Labeler - Stiefel Laboratories Inc (808842343) |
Friday, 9 July 2010
Butorphanol Tartrate
Class: Opiate Partial Agonists
VA Class: CN101
CAS Number: 58786-99-5
Brands: Stadol, Stadol NS
Introduction
Opiate partial agonist; phenanthrene derivative.a b d
Uses for Butorphanol Tartrate
Pain
Relief of moderate to severe pain such as that associated with acute and chronic medical disorders including cancer, neuropathic or spastic conditions, orthopedic problems, burns, renal colic, and surgery.d
Preoperative sedation and analgesia and as a supplement to surgical anesthesia.a
Obstetric analgesia during labor.a
Management of pain associated with migraine headache.113 114 116 122
In equianalgesic doses, parenteral butorphanol is as effective as morphine, meperidine, and pentazocine, but relative potential for abuse reportedly is less than that of codeine or propoxyphene.d
Butorphanol Tartrate Dosage and Administration
Administration
Administer IM, by IV injection, or by nasal inhalation.113
Nasal Administration
Assemble the nasal solution spray pump according to the manufacturer’s instructions.113 Prior to initial use, fully prime the spray pump; reprime pump whenever it has not been used for ≥48 hours.113
Consult the manufacturer’s patient instructions regarding use of the nasal solution spray pump.113 124
The nasal solution spray pump is an open delivery system; aim the pump spray away from the patient, other individuals, or animals to minimize environmental exposure.113
IV Administration
For drug compatibility information, see Compatibility under Stability.
Dosage
Available as butorphanol tartrate; dosage expressed in terms of the salt.a b
After initial priming, the nasal solution spray pump delivers about 14–15 metered doses containing 1 mg per spray.a If repriming of the pump is necessary, the spray pump will deliver about 8–10 metered doses, depending on the extent of repriming.113
Adults
Pain
IV
Initially, 1 mg; may repeat dose every 3–4 hours as necessary.a Usual effective dosage, depending on severity of pain, is 0.5–2 mg repeated every 3–4 hours.a
IM
Initially, 2 mg in patients able to remain recumbent; may repeat dose every 3–4 hours as necessary.a Usual effective dosage, depending on severity of pain, is 1–4 mg repeated every 3–4 hours.a
Intranasal
Initially, 1 mg (1 spray in 1 nostril); if adequate analgesia is not achieved, may give an additional 1-mg dose within 60–90 minutes.113 May repeat this initial dose sequence in 3–4 hours, if needed.113
For management of severe pain: Initially, 2 mg (1 spray in each nostril) in patients who can remain recumbent if drowsiness or dizziness occurs.113 Do not administer additional 2-mg doses at intervals <3–4 hours, since the incidence of adverse effects may be increased.113
Preoperative Sedation and Analgesia
IM
Usual dosage is 2 mg administered 60–90 minutes before surgery.a
Supplement to Surgical Anesthesia
IV
2 mg shortly before induction of anesthesia and/or 0.5–1 mg administered during anesthesia in increments up to 0.06 mg/kg (depending on previous administration of sedatives, analgesics, and hypnotic agents).a Usual total dose is 4–12.5 mg (approximately 0.06–0.18 mg/kg).a
Obstetric Analgesia
IV or IM
1–2 mg administered in patients at full term in early labor; may repeat after 4 hours.a Use alternative analgesia if delivery expected within 4 hours.a
Prescribing Limits
Adults
Pain
IM
Maximum 4 mg as a single dose.a
Special Populations
Hepatic Impairment
Pain
IV
Initially, 0.5 mg.113 If necessary, repeat dose at an interval of ≥6 hours.113
IM
Initially, 1 mg.113 If necessary, repeat dose at an interval of ≥6 hours.113
Intranasal
Initially, 1 mg (1 spray in 1 nostril); may give an additional 1-mg dose within 90–120 minutes, if necessary.113 May repeat this initial dose sequence at an interval of ≥6 hours.113
Renal Impairment
Patients with renal impairment may receive the same IV, IM, or intranasal dosages as patients with hepatic impairment.113
Geriatric Patients
Geriatric patients may receive the same IV, IM, or intranasal dosages as patients with hepatic impairment.113
Cautions for Butorphanol Tartrate
Contraindications
Known hypersensitivity to butorphanol or benzethonium chloride (contained in the multiple-dose vials of the injection or in the nasal solution).a b
Warnings/Precautions
Warnings
Abuse Potential
Possible tolerance, psychologic dependence, and physical dependence.a b d Episodes of abuse associated with all routes of administration, especially nasal administration.a b
Patients with a history of drug or alcohol dependence or abuse are at risk of habituation or dependence; use only with careful surveillance in such patients.a b
Patients Dependent on Opiates
Partial opiate antagonist; not recommended for use in patients physically dependent on opiatesa because of the potential to precipitate symptoms of withdrawal (e.g., anxiety, agitation, mood changes, hallucinations, dysphoria, weakness, diarrhea).128 129
Use with caution in patients who recently received repeated doses of opiate analgesics; allow an adequate period of withdrawal from opiates before initiation of butorphanol therapy.128 129
General Precautions
Head Injury and Increased Intracranial Pressure
Adverse effects of opiates may obscure the existence, extent, or course of intracranial pathology.113 Use in patients with head injury only if the potential benefits justify the possible risks.113
Respiratory Effects
Possible respiratory depression, especially in patients with impaired respiration caused by other drugs, uremia, severe infection, severely limited respiratory reserve, bronchial asthma, respiratory obstruction, or cyanosis.a b d Use with caution and in lower dosages in these patients.a b d
Cardiovascular Effects
Possible increased myocardial workload; use in patients with AMI, ventricular dysfunction, or coronary insufficiency only if the potential benefits justify the possible risks.a b
Severe hypertension reported rarely.a b If hypertension occurs, discontinue and administer a hypotensive agent as necessary; butorphanol-induced hypertension reportedly has been managed with naloxone in patients who were not opiate dependent.113
Use cautiously before surgery or anesthesia in hypertensive patients.d
Possible hypotension associated with syncope in patients receiving nasal solution; caution patients against performing activities that may pose risks if hypotension were to occur.113
CNS Depression
Performance of activities requiring mental alertness and physical coordination may be impaired.a b
Concurrent use of other CNS depressants may potentiate CNS depression.a b (See Specific Drugs under Interactions.)
Biliary Tract Surgery
Safe use in patients about to undergo biliary tract surgery has not been established; use with caution.d
Specific Populations
Pregnancy
Category C.a b
Use of intranasal spray not recommended during labor and delivery.
Lactation
Distributed into milk following parenteral administration, but not in clinically important amounts at usual therapeutic dosages.113
No experience with use of nasal solution in nursing women; estimated that amount of drug distributed into milk will be similar to that when administered parenterally.113 b
Pediatric Use
Safety and efficacy not established in children <18 years of age.a b
Geriatric Use
Select dosage with caution.113 (See Geriatric Patients under Dosage and Administration.)
Possible increased sensitivity to the drug in some geriatric individuals.113
Insufficient experience with the nasal solution in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.b
Hepatic Impairment
Use with caution.a b (See Hepatic Impairment under Dosage and Administration.)
Renal Impairment
Use with caution.a b (See Renal Impairment under Dosage and Administration.)
Common Adverse Effects
Sedation, dizziness, nausea and/or vomiting.a b
Interactions for Butorphanol Tartrate
Not known whether drugs that affect hepatic microsomal enzymes may interfere with metabolism of butorphanol.113
Specific Drugs
Drug | Interaction | Comments |
|---|---|---|
Cimetidine | Pharmacokinetic interaction unlikelyb | |
CNS depressants (e.g., alcohol, antihistamines, general anesthetics, hypnotics, phenothiazines, sedatives, tranquilizers, barbiturates) | Additive CNS effectsa b | Reduce dose and frequency of butorphanol administration113 |
Erythromycin | Potential for decreased metabolism of butorphanol is unknown113 a b | Consider reducing dose and increasing interval between doses of butorphanol113 a b |
Oxymetazoline | Possible decreased rate of absorption of intranasal butorphanol; extent of absorption appears to be unchanged113 b | Slower onset of analgesic action if butorphanol is administered intranasally with or immediately after oxymetazoline113 |
Pancuronium | Increased conjunctival changesd | |
Sumatriptan | Reduced analgesic effect of butorphanol nasal spray when administered shortly after sumatriptan nasal spray; possible increased BPb | Reduction in analgesic effect is minimal if butorphanol is administered≥30 minutes after sumatriptanb |
Theophylline | Potential for decreased metabolism of butorphanol is unknown113 b | Consider reducing dose and increasing interval between doses of butorphanol113 b |
Butorphanol Tartrate Pharmacokinetics
Absorption
Bioavailability
Rapidly absorbed following IM injection; peak plasma concentrations usually attained within 30–60 minutes.a d
Following nasal inhalation, peak blood concentrations are achieved in about 30–60 minutes.113 114 Absolute bioavailability of nasally administered butorphanol is 60–70% and appears to be unchanged in patients with allergic rhinitis.a
Completely absorbed from the GI tract following oral administration; however, after first-pass metabolism, bioavilability is only 5–17%.a b
Onset
Onset of analgesic activity occurs in a few minutes after IV administration or within 15 minutes after IM administration;a b peak analgesic effect achieved within 30–60 minutes after IV or IM administration.a
After nasal inhalation in postoperative patients, onset of analgesia occurs within 15 minutes;113 114 125 peak analgesic effect achieved within 1–2 hours.b
Duration
After IV or IM administration, duration of analgesia is 3–4 hours.a b
After nasal inhalation in postoperative patients, duration of analgesia is approximately 2.5–5 hours.113 114 125
Distribution
Extent
Highest concentrations of butorphanol and its metabolites in animals are found in the liver, kidneys, and intestine; drug concentrations are higher in the lungs, spleen, heart, endocrine tissues, blood cells, and fat tissue than in plasma; brain concentrations are lower than plasma concentrations.d
Rapidly crosses the placenta and is distributed into milk.a b
Plasma Protein Binding
About 80%.a b
Elimination
Metabolism
Extensively metabolized in the liver, principally by hydroxylation; N-dealkylation and conjugation of butorphanol and its metabolites also occur.a b d Metabolites have no analgesic activity.d
Elimination Route
Excreted prinicipally in urine (70–80%) mainly as metabolites; also excreted in feces (15%).a b
Half-life
About 4.6–4.7 hours following intranasal or IV administration.113 114
Special Populations
In patients with hepatic impairment, elimination half-life of 16.8 hours reported.b
In patients with renal impairment (Clcr <30 mL/minute), elimination half-life of 10.5 hours reported.113
In geriatric individuals, elimination half-life reported to be about 5.6 hours (range 3.3–8.8 hours) or 6.6 hours (range: 3.8–9.2 hours) following IV or intranasal administration, respectively.113
Stability
Storage
Nasal
Solution
25°C.b
Parenteral
Injection
15–30°C; protect from light.a
Compatibility
For information on systemic interactions resulting from concomitant use, see Interactions.
Drug Compatibility
Compatible |
|---|
Allopurinol sodium |
Amifostine |
Aztreonam |
Bivalirudin |
Cefepime HCl |
Cladribine |
Dexmedetomidine HCl |
Docetaxel |
Doxorubicin HCl liposome injection |
Enalaprilat |
Esmolol HCl |
Etoposide phosphate |
Fenoldopam mesylate |
Filgrastim |
Fludarabine phosphate |
Gemcitabine HCl |
Granisetron HCl |
Hetastarch in lactated electrolyte injection (Hextend) |
Labetalol HCl |
Linezolid |
Melphalan HCl |
Nicardipine HCl |
Oxaliplatin |
Paclitaxel |
Pemetrexed disodium |
Piperacillin sodium–tazobactam sodium |
Propofol |
Remifentanil HCl |
Sargramostim |
Teniposide |
Thiotepa |
Vinorelbine tartrate |
Incompatible |
Amphotericin B cholesteryl sulfate complex |
Lansoprazole |
Midazolam HCl |
ActionsActions
Analgesic effect is believed to result from an interaction with an opiate receptor site in the CNS (probably in or associated with the limbic system).a
Opiate antagonistic effect may result from competitive inhibition at the opiate receptor, but other mechanisms probably also are involved.d Butorphanol exerts antagonistic114 115 126 or partially antagonistic113 effects at μ opiate receptor sites; it appears to exerts agonistic effects principally at κ and Σ opiate receptors.101 102 103 104
Produces respiratory depression, sedation, miosis and, in animals, antitussive effect.a
Slightly increases pulmonary artery pressure, pulmonary wedge pressure, left ventricular end-diastolic pressure, systemic arterial pressure, pulmonary vascular resistance, and cardiac index.a
In animals, inhibits GI motility slightly, causes little increase in duodenal smooth muscle activity, and has little or no effect on bile duct flow.d
Advice to Patients
Potential for butorphanol to impair mental alertness or physical coordination; do not drive or operate machinery for ≥1 hour after receiving the drug or until effects on individual are known.a b
Patients receiving the nasal solution should not perform activities that may pose risks if hypotension were to occur.113
Importance of taking only as prescribed; do not increase dosage or duration of therapy unless otherwise instructed by a clinician.a b
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and alcohol consumption.a b Importance of avoiding alcohol while receiving the drug.a b
Importance of women informing their clinician if they are or plan to become pregnant or to breast-feed.a b
Importance of advising patients of other important precautionary information.a b (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 IV (C-IV) drug.127 128 129
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Nasal | Solution | 1 mg/metered spray (10 mg/mL)* | Butorphanol Tartrate Nasal Spray ( C-IV) | Mylan, Novex, Roxane |
Stadol NS ( C-IV) | Bristol-Myers Squibb, (also promoted by Cephalon) | |||
Parenteral | Injection | 1 mg/mL* | Butorphanol Tartrate Injection ( C-IV; available as single-dose vials and prefilled syringes) | Apotex, Baxter, Bedford, Hospira, Mayne |
Stadol ( C-IV) | Sandoz | |||
2 mg/mL* | Butorphanol Tartrate Injection ( C-IV; available as single-dose vials, multiple-dose vials, and pre-filled syringes) | Apotex, Baxter, Bedford, Hospira, Mayne | ||
Stadol ( C-IV) | Sandoz |
Disclaimer
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions August 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
References
Only references cited for selected revisions after 1984 are available electronically.
100. The United States pharmacopeia, 21st rev, and The national formulary, 16th ed. Rockville, MD: The United States Pharmacopeial Convention, Inc; 1985:141-2.
101. Jaffe JH, Martin WR. Opioid analgesics and antagonists. In: Gilman AG, Goodman LS, Rall TW et al, eds. Goodman and Gilman’s the pharmacological basis of therapeutics. 7th ed. New York: Macmillan Publishing Company; 1985:491-531.
102. Martin WR. Pharmacology of opioids. Pharmacol Rev. 1983; 35:283-323. [IDIS 182771] [PubMed 6144112]
103. Zola EM, McLeod DC. Comparative effects and analgesic efficacy of the agonist-antagonist opioids. Drug Intell Clin Pharm. 1983; 17:411-7. [IDIS 171471] [PubMed 6861632]
104. Lewis JR. Evaluation of new analgesics: butorphanol and nalbuphine. JAMA. 1980; 243:1465-7. [IDIS 112206] [PubMed 7359723]
105. Evans WS, Bowen JN, Giordano FL et al. A case of Stadol dependence. JAMA. 1985; 253:2191-2. [IDIS 198247] [PubMed 3974108]
106. Smith SG, Davis WM. Nonmedical use of butorphanol and diphenhydramine. JAMA. 1984; 252:1010. [IDIS 188728] [PubMed 6748202]
107. Brown GR. Stadol dependence: another case. JAMA. 1985; 254:910. [IDIS 203557] [PubMed 4021020]
108. Austin RP. Diversion of butorphanol. Am J Hosp Pharm. 1983; 40:1306. [PubMed 6614013]
109. Hoover RC, Williams RB. Survey of butorphanol and nalbuphine diversion in U.S. hospitals. Am J Hosp Pharm. 1985; 42:1111-3. [PubMed 4003423]
110. Butorphanol. In: WHO Expert Committee on Drug Dependence. 25th report. Technical report series 775. Geneva: World Health Organization; 1989:24-6.
111. Preston KL, Bigelow GE, Liebson IA. Butorphanol-precipitated withdrawal in opioid-dependent human volunteers. J Pharmacol Exp Ther. 1988; 246:441-8. [IDIS 245408] [PubMed 2457074]
112. Preston KL, Bigelow GE, Liebson IA. Butorphanol-precipitated withdrawal in opioid-dependent human volunteers. NIDA Res Monogr. 1987; 76:157-61. [PubMed 2449617]
113. Mead Johnson. Stadol (butorphanol tartrate) injectable and Stadol NS (butorphanol tartrate) nasal spray prescribing information. Princeton, NJ; 1995 Jan.
114. Gillis JC, Benfield P, Goa KL. Transnasal butorphanol: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in acute pain management. Drugs. 1995; 50:157-75. [PubMed 7588085]
115. Jaffe JH, Martin WR. Opioid analgesics and antagonists. In: Gilman AG, Rall TW, Nies AS et al, eds. Goodman and Gilman’s the pharmacological basis of therapeutics. 8th ed. New York: Pergamon Press; 1990:485-521.
116. Anon. Drugs for migraine. Med Lett Drugs Ther. 1995; 37:17-20. [PubMed 7862023]
117. Joyce TH, Kubicek MF, Skjonsby BS et al. Efficacy of transnasal butorphanol tartrate in postepisiotomy pain: a model to assess analgesia. Clin Ther. 1993; 15:160-7. [PubMed 8458045]
118. Shyu WC, Morgenthien EA, Pittman KA et al. The effects of age and sex on the systemic availability and pharmacokinetics of transnasal butorphanol. Eur J Clin Pharmacol. 1994; 47:57-60. [IDIS 339323] [PubMed 7988625]
119. Shyu WC, Pittman KA, Robinson DS et al. The absolute bioavailability of transnasal butorphanol in patients experiencing rhinitis. Eur J Clin Pharmacol. 1993; 45:559-62. [IDIS 326431] [PubMed 8157043]
120. Shyu WC, Mayol RF, Pfeffer M et al. Biopharmaceutical evaluation of transnasal, sublingual, and buccal disk dosage forms of butorphanol. Biopharm Drug Dispos. 1993; 14:371-9. [IDIS 317491] [PubMed 8218955]
121. Shyu WC, Pittman KA, Robinson D et al. Multiple-dose phase I study of transnasal butorphanol. Clin Pharmacol Ther. 1993; 54:34-41. [IDIS 319110] [PubMed 8330463]
122. Hoffert MJ, Couch JR, Diamond S et al. Transnasal butorphanol in the treatment of acute migraine. Headache. 1995; 35:65-9. [PubMed 7737863]
123. Bristol-Myers Squibb, Princeton, NJ: Personal communication.
124. Mead Johnson. Stadol NS (butorphanol tartrate) nasal spray patient instructions. Princeton, NJ; 1992.
125. Schwesinger WH, Reynolds JC, Harshaw DH et al. Transnasal butorphanol and intramuscular meperidine in the treatment of postoperative pain. Adv Ther. 1992; 9:123-9.
126. Chen JC, Smith ER, Cahill M et al. The opioid receptor binding of dezocine, morphine, fentanyl, butorphanol and nalbuphine. Life Sci. 1992; 52:389-96.
127. Code of federal regulations. Part 1308. Schedules of controlled substances, revised as of April 1, 1998.
128. Bristol-Myers Squibb. Stadol NS (butorphanol tartrate) nasal spray prescribing information. Priceton, NJ; 1999 May.
129. Bristol-Myers Squibb, Priceton, NJ: Personal communication.
130. Matchar DB, Young WB, Rosenberg JH et al. Evidence-based guidelines for migraine headache in the primary care setting: pharmacological management of acute attaks. St. Paul, MN; 2001. From the American Academy of Neurology web site: ().
a. Bedford Laboratories. Butorphanol tartrate injection prescribing information. Bedford OH; 1999 Dec.
b. Bristol-Myers Squibb. Stadol NS (butorphanol tartrate) nasal spray prescribing information. Priceton, NJ; 2002 Mar
HID. Trissel LA. Handbook on injectable drugs. 14th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2007:233-7.
d. AHFS Drug Information 2004. McEvoy GK, ed. Butorphanol. Bethesda, MD: American Society of Health-System Pharmacists; 2004:2075-7.
More Butorphanol Tartrate resources
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Friday, 2 July 2010
Daivonex
Daivonex may be available in the countries listed below.
Ingredient matches for Daivonex
Calcipotriol
Calcipotriol is reported as an ingredient of Daivonex in the following countries:
- Argentina
- Australia
- Bahrain
- Bangladesh
- Bulgaria
- Chile
- China
- Colombia
- Costa Rica
- Czech Republic
- Denmark
- Dominican Republic
- Ecuador
- El Salvador
- Estonia
- Finland
- France
- Germany
- Guatemala
- Honduras
- Hong Kong
- Hungary
- Iceland
- India
- Indonesia
- Israel
- Italy
- Latvia
- Lithuania
- Luxembourg
- Malaysia
- Malta
- Mexico
- Netherlands
- New Zealand
- Norway
- Oman
- Panama
- Philippines
- Poland
- Portugal
- Romania
- Russian Federation
- Singapore
- Slovenia
- Spain
- Sri Lanka
- Switzerland
- Taiwan
- Thailand
- Tunisia
- Vietnam
Calcipotriol monohydrate (a derivative of Calcipotriol) is reported as an ingredient of Daivonex in the following countries:
- Belgium
- Netherlands
- Sweden
- Switzerland
International Drug Name Search
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