Brown clear ampoule containing colorless solution.
Each ampoule (1 ml) contains: Butorphanol Tartrate 2.0 mg
Butorphanol is used to relief of moderate to severe pain, for pre-operative or pre-anesthetic medication as a supplement to balanced anesthesia, for relief of pain during labor.
Butorphanol has factors to be considered in determining the dose are age, body weight, physical status, underlying pathological condition, use of other drugs, type of anesthesia to be used, and surgical procedure involved. Use in the elderly, in patients with hepatic or renal disease, or in labor requires extra caution. The following doses are for patients who do not have impaired hepatic or renal function and who are not on CNS active agents.
Pain: Intravenous: The usual recommended single dose for IV administration is 1 mg repeated every 3 to 4 hours as necessary. The effective dosage range, depending on the severity of pain, is 0.5 mg to 2 mg repeated every 3 to 4 hours.
Intramuscular: The usual recommended single dose for IM administration is 2 mg in patients who will be able to remain recumbent, in the event drowsiness or dizziness occurs. This may be repeated every 3 to 4 hours. There are insufficient clinical data to recommend single doses above 4 mg.
Both expected efficacy and adverse reaction should be considered in dosage adjustment. The dose of this drug recommended for elderly patients, patients with hepatic or renal impairment should generally be half the recommended adult dose (0.5 mg IV and 1.0 mg IM). Repeat doses should be determined by the patient's response rather than at fixed intervals, but will generally be no less than 6 hours apart.
Use as Preoperative/Pre-anesthetic Medication: The preoperative medication dosage should be individualized. The usual adult dose is 2 mg IM, administered 60-90 minutes before surgery. This is approximately equivalent in sedative effect to 10 mg morphine or 80 mg meperidine.
Use in Balanced Anesthesia: The usual dose is 2 mg IV shortly before induction and/or 0.5 to 1.0 mg IV increments during anesthesia. The increment may be higher, up to 0.06 mg/kg (4 mg/70 kg), depending on previous sedative, analgesic and hypnotic drugs administered. The total dose of this drug will vary; however, patients seldom require less than 4 mg or more than 12.5 mg (approximately 0.06 to 0.18 mg/kg).
Opioid, including this drug, may not produce appropriate analgesic effect for every patient or every state during surgery. Analgesic fail during induction anesthesia can be judged to be general sympathetic nerve negative. Therefore, if heartbeat or blood pressure is continuously increased, intensive inhalation anesthetic or another IV should be considered.
Labor: In patients at full term or without fetal distress in early labor a 1-2 mg dose IV or IM may be administered and repeated after 4 hours. Dosage titration should be based on concurrent analgesics, sedatives, expected time of delivery and response of the first administration. If concomitant use of this drug with drugs that may potentiate its effects is deemed necessary, the lowest effective dose should be employed.
The clinical manifestations of butorphanol overdose are those of opioid drugs in general. The most serious symptoms are hypoventilation, cardiovascular insufficiency, coma and death.
The management of suspected butorphanol overdosage includes maintenance of adequate ventilation, peripheral perfusion, normal body temperature, and protection of the airway. Patients should be under continuous observation with adequate serial measures of mental state, responsiveness, and vital signs. Oxygen and ventilator assistance should be available with continual monitoring by pulse oximetry if indicated. In the presence of coma, placement of an artificial airway may be required. An adequate intravenous portal should be maintained to facilitate treatment if hypotension associated with vasodilation.
The use of a specific opioid antagonist such as naloxone should be considered. As the duration of butorphanol action usually exceeds the duration of action of naloxone, repeated dosing with naloxone may be required.
In managing cases of suspected butorphanol overdosage, the possibility of multiple drug ingestion should always be considered.
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 its opioid antagonist properties. This drug should be carefully administered to the following patients.
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.
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.
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.
When ampoules are cut, glass particles can be mixed with drug solution. Therefore, caution should be taken to prevent from mixing. In particular caution should be taken when it is used by elderly or children.
General Caution: Effects such as drowsiness or dizziness impair the mental and physical abilities required for the performance of potentially dangerous tasks such as driving a car or operating machinery.
Alcohol should not be consumed while using butorphanol.
Drugs having antagonistic action and effect of opioid less frequent than morphine but can be abused. Due to prolonged use of this drug, light withdrawal symptoms, excessive use and addition have been reported. Special care should be exercised in administering butorphanol to patients with a history of drug abuse or to patients receiving the drug on a continuous basis for an extended period.
Use for outpatients: Drowsiness and dizziness may occur. Caution should be taken until individual characteristic response to this drug is obtained.
Carcinogenesis, Mutagenesis, Impairment of Fertility: There was no evidence of carcinogenicity for this drug.
Butorphanol was not genotoxic in S. typhimurium of E. coli 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/m2) had a reduced pregnancy rate. However, a similar effect was not observed with a 2.5 mg/kg/day (14.75 mg/m2) subcutaneous dose.
Use in Children: Butorphanol is not recommended for use in patients below 18 years of age because safety and efficacy have not been established in this population.
Use in the Elderly: Due to changes in clearance, the mean half-life of butorphanol is increased by 25% (to over 6 hours) in patients over the age of 65 years. Elderly patients may be more sensitive to the side effects of butorphanol.
Pregnancy: Reproduction studies in mice, rats and rabbits during organogenesis did not reveal any teratogenic potential to butorphanol. However, pregnant rats treated subcutaneously with butorphanol at 1 mg/kg (5.9 mg/m2) had a higher frequency of stillbirths than controls. Butorphanol at 30 mg/kg/oral (360 mg/m2) and 60 mg/kg/oral (720 mg/m2) also showed higher incidences of post-implantation loss in rabbits. There are no adequate and well-controlled studies of this drug in pregnant women before 37 weeks of gestation. This drug 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 this drug during labor. The reports of respiratory distress/apnea have been associated with administration of a dose within 2 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 IV administration of 1 mg of this drug during labor was associated with transient sinusoidal fetal heart rate patterns, but was not associated with adverse neonatal outcomes. In the presence of an abnormal fetal heart rate pattern, this drug should be used with caution.
Nursing mothers: Butorphanol has been detected in milk following administration of this drug to nursing mothers. The amount an infant would receive is probable clinically insignificant (estimated 4μg/L of milk in a mother receiving 2 mg IM four times a day).
The most frequently reported adverse experiences across all clinical trials with this drug were somnolence (43%), dizziness (19%), nausea and/or vomiting (13%).
The following adverse experiences were reported at a frequency of 1% or greater in clinical trials.
Body as a whole: Asthenia/lethargy, headache, sensation of heat.
Digestive: Dry mouth, nausea and/or vomiting, stomach pain.
Nervous: Anxiety, confusion, dizziness, euphoria, floating feeling, nervousness, paresthesia, somnolence.
Skin and Appendages: Sweating/clammy, pruritus.
Special senses: Blurred vision.
The following adverse experiences were reported with a frequency of less than 1% in clinical trials.
Cardiovascular: Hypotension, syncope.
Nervous: Abnormal dreams, agitation, dysphoria, hallucinations, hostility.
Skin and Appendages: Rash/hives.
Urogenital: Impaired urination.
Concurrent use of butorphanol with central nervous system depressants (e.g. alcohol, barbiturates, tranquilizers and antihistamine) 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 actions of opioids.
It is not known if the effects of butorphanol are altered by other concomitant medications that affect hepatic metabolism of drugs (cimetidine, 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.
Store at temperatures not exceeding 30°C.
N02AF01 - butorphanol ; Belongs to the class of morphinan derivative opioids. Used to relieve pain.
Staldol soln for inj 2 mg/mL
1 mL x 10 × 1's
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