Butorphanol Tartrate

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Overview

What is Butorphanol Tartrate?

Butorphanol tartrate is a synthetically derived opioid agonist-antagonist analgesic of the phenanthrene series. The chemical name is ( – )-17-(cyclobutylmethyl)morphinan-3,14-diol D- ( – ) - tartrate (1:1) (salt). The molecular formula is CHNO•CHO, which corresponds to a molecular weight of 477.55 and the following structural formula:

Butorphanol tartrate is a white crystalline substance. The dose is expressed as the tartrate salt. One milligram of the salt is equivalent to 0.68 mg of the free base. The n-octanol/ aqueous buffer partition coefficient of butorphanol is 180:1 at pH 7.5.

Butorphanol tartrate injection is a sterile, parenteral, aqueous solution of butorphanol tartrate for intravenous or intramuscular administration. In addition to 1 or 2 mg of butorphanol tartrate, each mL contains 3.3 mg of citric acid, 7.29 mg sodium citrate dihydrate (equivalent to 6.4 mg sodium citrate, anhydrous), and 6.4 mg of sodium chloride, and 0.1 mg benzethonium chloride (in multiple dose vial only) as a preservative. The pH range is 3.0 to 5.5.

What does Butorphanol Tartrate look like?

What are the available doses of Butorphanol Tartrate?

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What should I talk to my health care provider before I take Butorphanol Tartrate?

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How should I use Butorphanol Tartrate?

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What interacts with Butorphanol Tartrate?

Butorphanol tartrate injection is contraindicated in patients hypersensitive to butorphanol tartrate or the preservative benzethonium chloride in the multiple dose vial.

What are the warnings of Butorphanol Tartrate?

Patients Dependent on Narcotics

Because of its opioid antagonist properties, butorphanol is not recommended for use in patients dependent on narcotics. Such patients should have an adequate period of withdrawal from opioid drugs prior to beginning butorphanol therapy. In patients taking opioid analgesics chronically, butorphanol has precipitated withdrawal symptoms such as anxiety, agitation, mood changes, hallucinations, dysphoria, weakness and diarrhea.

Because of the difficulty in assessing opioid tolerance in patients who have recently received repeated doses of narcotic analgesic medication, caution should be used in the administration of butorphanol to such patients.

Drug Abuse and Dependence

Drug Abuse:

Physical Dependence, Tolerance, and Withdrawal:

Note:

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What are the precautions of Butorphanol Tartrate?

Head Injury and Increased Intracranial Pressure

As with other opioids, the use of butorphanol in patients with head injury may be associated with carbon dioxide retention and secondary elevation of cerebrospinal fluid pressure, drug-induced miosis, and alterations in mental state that would obscure the interpretation of the clinical course of patients with head injuries. In such patients, butorphanol should be used only if the benefits of use outweigh the potential risks.

Disorders of Respiratory Function or Control

Butorphanol may produce respiratory depression, especially in patients receiving other CNS active agents, or patients suffering from CNS diseases or respiratory impairment.

Hepatic and Renal Disease

In patients with hepatic or renal impairment, the initial dose of butorphanol tartrate injection should generally be half the recommended adult dose (0.5 mg IV and 1 mg IM). Repeat doses in these patients should be determined by the patient’s response rather than at fixed intervals but will generally be no less than 6 hours apart ( and sections).

Cardiovascular Effects

Because butorphanol may increase the work of the heart, especially the pulmonary circuit, the use of butorphanol in patients with acute myocardial infarction, ventricular dysfunction, or coronary insufficiency should be limited to those situations where the benefits clearly outweigh the risk ().

Severe hypertension has been reported rarely during butorphanol therapy. In such cases, butorphanol should be discontinued and the hypertension treated with antihypertensive drugs. In patients who are not opioid dependent, naloxone has also been reported to be effective.

Use in Ambulatory Patients

Drug Interactions

Concurrent use of butorphanol with central nervous system depressants (e.g., alcohol, barbiturates, tranquilizers, and antihistamines) may result in increased central nervous system depressant effects. When used concurrently with such drugs, the dose of butorphanol should be the smallest effective dose and the frequency of dosing reduced as much as possible when administered concomitantly with drugs that potentiate the action of opioids.

It is not known if the effects of butorphanol are altered by other concomitant medications that affect hepatic metabolism of drugs (erythromycin, theophylline, etc.), but physicians should be alert to the possibility that a smaller initial dose and longer intervals between doses may be needed.

No information is available about the use of butorphanol concurrently with MAO inhibitors.

Information for Patients

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Carcinogenesis, Mutagenesis, Impairment of Fertility

Two-year carcinogenicity studies were conducted in mice and rats given butorphanol tartrate in the diet up to 60 mg/kg/day (180 mg/m for mice and 354 mg/m for rats). There was no evidence of carcinogenicity in either species in these studies.

Butorphanol was not genotoxic in or assays or in unscheduled DNA synthesis and repair assays conducted in cultured human fibroblast cells.

Rats treated orally with 160 mg/kg/day (944 mg/m) had a reduced pregnancy rate. However, a similar effect was not observed with a 2.5 mg/kg/day (14.75 mg/m) subcutaneous dose.

Pregnancy

Teratogenic Effects: Pregnancy Category C:

There are no adequate and well-controlled studies of butorphanol tartrate in pregnant women before 37 weeks of gestation. Butorphanol tartrate should be used during pregnancy only if the potential benefit justifies the potential risk to the infant.

Labor and Delivery

There have been rare reports of infant respiratory distress/apnea following the administration of butorphanol tartrate injection during labor. The reports of respiratory distress/apnea have been associated with administration of a dose within two hours of delivery, use of multiple doses, use with additional analgesic or sedative drugs, or use in preterm pregnancies ().

In a study of 119 patients, the administration of 1 mg of IV butorphanol tartrate during labor was associated with transient (10 to 90 minutes) sinusoidal fetal heart rate patterns, but was not associated with adverse neonatal outcomes. In the presence of an abnormal fetal heart rate pattern, butorphanol tartrate should be used with caution.

Nursing Mothers

Butorphanol has been detected in milk following administration of butorphanol tartrate injection to nursing mothers. The amount an infant would receive is probably clinically insignificant (estimated 4 mcg/L of milk in a mother receiving 2 mg IM four times a day).

Pediatric Use

Butorphanol is not recommended for use in patients below 18 years of age because safety and efficacy have not been established in this population.

Geriatric Use

Of the approximately 1500 patients treated with butorphanol tartrate injection in clinical studies, 15% were 61 years of age or older and 1% were 76 years or older.

Due to changes in clearance, the mean half-life of butorphanol is increased by 25% in patients over the age of 65 years. (section). Elderly patients may be more sensitive to the side effects of butorphanol. There are insufficient efficacy data for patients ≥65 years to determine whether they respond differently from younger patients.

The initial dose of butorphanol tartrate injection recommended for elderly patients should generally be half the recommended adult dose (0.5 mg IV and 1 mg IM). Repeat dose should be determined by the patient’s response rather than at fixed intervals, but will generally be no less than 6 hours apart (section).

Butorphanol and its metabolites are known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection.

What are the side effects of Butorphanol Tartrate?

Clinical Trial Experience

A total of 2446 patients were studied in premarketing clinical trials of butorphanol. Approximately half received butorphanol tartrate injection with the remainder receiving butorphanol tartrate nasal spray. In nearly all cases the type and incidence of side effects with butorphanol by any route were those commonly observed with opioid analgesics.

The adverse experiences described below are based on data from short-term and long-term clinical trials in patients receiving butorphanol by any route. There has been no attempt to correct for placebo effect or to subtract the frequencies reported by placebo-treated patients in controlled trials.

The most frequently reported adverse experiences across all clinical trials with butorphanol tartrate injection and nasal spray were somnolence (43%), dizziness (19%), nausea and/or vomiting (13%). In long-term trials with the nasal spray only, nasal congestion (13%) and insomnia (11%) were frequently reported.

The following adverse experiences were reported at a frequency of 1% or greater in clinical trials and were considered to be probably related to the use of butorphanol:

Body as a Whole:

Cardiovascular:

Digestive:

Nervous:

Respiratory:

Skin and Appendages:

Special Senses:

The following adverse experiences were reported with a frequency of less than 1% in clinical trials and were considered to be probably related to the use of butorphanol.

Cardiovascular:

Nervous:

Skin and Appendages:

Urogenital:

The following infrequent additional adverse experiences were reported in a frequency of less than 1% of the patients studied in short-term butorphanol tartrate nasal spray trials and under circumstances where the association between these events and butorphanol administration is unknown. They are being listed as alerting information for the physician.

Body as a Whole:

Cardiovascular:

Nervous:

Respiratory:

Postmarketing Experience

Postmarketing experience with butorphanol tartrate has shown an adverse event profile similar to that seen during the premarketing evaluation of butorphanol by all routes of administration. Adverse experiences that were associated with the use of butorphanol tartrate nasal spray or butorphanol tartrate injection and that are not listed above have been chosen for inclusion below because of their seriousness, frequency of reporting, or probable relationship to butorphanol. Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made. These adverse experiences include apnea, convulsion, delusion, drug dependence, excessive drug effect associated with transient difficulty speaking and/or executing purposeful movements, overdose, and vertigo. Reports of butorphanol overdose with fatal outcome have usually but not always been associated with ingestion of multiple drugs.

What should I look out for while using Butorphanol Tartrate?

Butorphanol tartrate injection is contraindicated in patients hypersensitive to butorphanol tartrate or the preservative benzethonium chloride in the multiple dose vial.

What might happen if I take too much Butorphanol Tartrate?

How should I store and handle Butorphanol Tartrate?

Store at controlled room temperature 20° to 25°C (68° to 77°F)Rx onlyManufactured by:Yung Shin Pharmaceutical Industrial Co., Ltd.Tachia, TaichungTaiwan, ROCRevision: April 2007Store at controlled room temperature 20° to 25°C (68° to 77°F)Rx onlyManufactured by:Yung Shin Pharmaceutical Industrial Co., Ltd.Tachia, TaichungTaiwan, ROCRevision: April 2007Store at controlled room temperature 20° to 25°C (68° to 77°F)Rx onlyManufactured by:Yung Shin Pharmaceutical Industrial Co., Ltd.Tachia, TaichungTaiwan, ROCRevision: April 2007Store at controlled room temperature 20° to 25°C (68° to 77°F)Rx onlyManufactured by:Yung Shin Pharmaceutical Industrial Co., Ltd.Tachia, TaichungTaiwan, ROCRevision: April 2007Store at controlled room temperature 20° to 25°C (68° to 77°F)Rx onlyManufactured by:Yung Shin Pharmaceutical Industrial Co., Ltd.Tachia, TaichungTaiwan, ROCRevision: April 2007Butorphanol Tartrate Injection USP, for IM or IV use is available as follows: 2 mg/mL, 2-mL vial, 10 vials per carton1 mg/mL, 1-mL vial, 10 vials per carton 2 mg/mL, 1-mL vial, 10 vials per carton 2 mg/mL, 10-mL multiple dose vial, individually cartoned. Butorphanol Tartrate Injection USP, for IM or IV use is available as follows: 2 mg/mL, 2-mL vial, 10 vials per carton1 mg/mL, 1-mL vial, 10 vials per carton 2 mg/mL, 1-mL vial, 10 vials per carton 2 mg/mL, 10-mL multiple dose vial, individually cartoned. Butorphanol Tartrate Injection USP, for IM or IV use is available as follows: 2 mg/mL, 2-mL vial, 10 vials per carton1 mg/mL, 1-mL vial, 10 vials per carton 2 mg/mL, 1-mL vial, 10 vials per carton 2 mg/mL, 10-mL multiple dose vial, individually cartoned. Butorphanol Tartrate Injection USP, for IM or IV use is available as follows: 2 mg/mL, 2-mL vial, 10 vials per carton1 mg/mL, 1-mL vial, 10 vials per carton 2 mg/mL, 1-mL vial, 10 vials per carton 2 mg/mL, 10-mL multiple dose vial, individually cartoned. Butorphanol Tartrate Injection USP, for IM or IV use is available as follows: 2 mg/mL, 2-mL vial, 10 vials per carton1 mg/mL, 1-mL vial, 10 vials per carton 2 mg/mL, 1-mL vial, 10 vials per carton 2 mg/mL, 10-mL multiple dose vial, individually cartoned.

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Clinical Information

Chemical Structure

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Clinical Pharmacology

Butorphanol is a mixed agonist-antagonist with low intrinsic activity at receptors of the µ-opioid type (morphine-like). It is also an agonist at κ-opioid receptors.

Its interactions with these receptors in the central nervous system apparently mediate most of its pharmacologic effects, including analgesia.

In addition to analgesia, CNS effects include depression of spontaneous respiratory activity and cough, stimulation of the emetic center, miosis and sedation. Effects possibly mediated by non-CNS mechanisms include alteration in cardiovascular resistance and capacitance, bronchomotor tone, gastrointestinal secretory and motor activity and bladder sphincter activity.

In an animal model, the dose of the butorphanol tartrate required to antagonize morphine analgesia by 50% was similar to that for nalorphine, less than that for pentazocine and more than that for naloxone.

The pharmacological activity of butorphanol metabolites has not been studied in humans; in animal studies, butorphanol metabolites have demonstrated some analgesic activity.

In human studies of butorphanol (), sedation is commonly noted at doses of 0.5 mg or more. Narcosis is produced by 10 to 12 mg doses of butorphanol administered over 10 to 15 minutes intravenously.

Butorphanol, like other mixed agonist-antagonists with a high affinity for the κ-receptor may produce unpleasant psychotomimetic effects in some individuals.

Nausea and/or vomiting may be produced by doses of 1 mg or more administered by any route.

In human studies involving individuals without significant respiratory dysfunction, 2 mg of butorphanol IV and 10 mg of morphine sulfate IV depressed respiration to a comparable degree. At higher doses, the magnitude of respiratory depression with butorphanol is not appreciably increased; however, the duration of respiratory depression is longer. Respiratory depression noted after administration of butorphanol to humans by any route is reversed by treatment with naloxone, a specific opioid antagonist section).

Butorphanol tartrate demonstrates antitussive effects in animals at doses less than those required for analgesia.

Hemodynamic changes noted during cardiac catheterization in patients receiving single 0.025 mg/kg intravenous doses of butorphanol have included increases in pulmonary artery pressure, wedge pressure and vascular resistance, increases in left ventricular end diastolic pressure and in systemic arterial pressure.

Non-Clinical Toxicology

Butorphanol tartrate injection is contraindicated in patients hypersensitive to butorphanol tartrate or the preservative benzethonium chloride in the multiple dose vial.

Concurrent use of butorphanol with central nervous system depressants (e.g., alcohol, barbiturates, tranquilizers, and antihistamines) may result in increased central nervous system depressant effects. When used concurrently with such drugs, the dose of butorphanol should be the smallest effective dose and the frequency of dosing reduced as much as possible when administered concomitantly with drugs that potentiate the action of opioids.

It is not known if the effects of butorphanol are altered by other concomitant medications that affect hepatic metabolism of drugs (erythromycin, theophylline, etc.), but physicians should be alert to the possibility that a smaller initial dose and longer intervals between doses may be needed.

Array

No information is available about the use of butorphanol concurrently with MAO inhibitors.

As with other opioids, the use of butorphanol in patients with head injury may be associated with carbon dioxide retention and secondary elevation of cerebrospinal fluid pressure, drug-induced miosis, and alterations in mental state that would obscure the interpretation of the clinical course of patients with head injuries. In such patients, butorphanol should be used only if the benefits of use outweigh the potential risks.

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72

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Interactions

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