Butorphanol

Indications
 Nasal
Moderate to severe pain
Adult: Initially, 1 mg, repeated after 60-90 minutes if necessary; may be repeated after 3-4 hr when necessary. For severe pain, initial dose can be 2 mg, repeated only after 3-4 hr.
Elderly: Initial dose: 1/2 usual adult dose. Recommended dose interval: at least 6 hr.
Renal impairment: Initial dose: 1/2 usual adult dose. Recommended dose interval: at least 6 hr.
Hepatic impairment: Initial dose: 1/2 usual adult dose. Recommended dose interval: at least 6 hr.
Parenteral
Moderate to severe pain
Adult: 1-4 mg via IM inj or 0.5-2 mg IV inj every 3-4 hr.
Parenteral
Anaesthesia
Adult: As premedicant before surgery: 2 mg given via IM inj 60-90 minutes before surgery. As supplement in balanced anesth: Doses are given via IV admin; 2 mg shortly before induction and/or an incremental dose of 0.5-1 mg (up to 0.06 mg/kg) during anaesthesia. Total dose may vary but usually ranges from 4-12.5 mg.
Contraindications
 Opiate-dependent patients who have not been detoxified; acute resp depression; pregnancy.
Warnings / Precautions
 Elderly; renal and hepatic impairment; hypertensive patients (when used preoperatively); patients with acute MI; head injury; lactation; patients on MAOI or within 2 wk of treatment withdrawal.
Adverse Reactions
 Sedation, dizziness, physical dependence, with or without psychological dependence; dyspnoea, confusion, headache, nausea, vomiting, drowsiness, constipation; hallucinations, mental depression, HTN and paradoxical CNS excitation (especially in children); rash, syncope, tinnitus, vertigo, diaphoresis, withdrawal syndrome.
Potentially Fatal: Respiratory depression, convulsions.
Drug Interactions
 Additive depressant effects with other CNS depressants e.g. general anaesthetics, phenothiazines or other tranquilizers, sedatives, hypnotics, antihistamines or alcohols.
See Below for More butorphanol tartrate Drug Interactions
Mechanism of Actions
 Butorphanol is a phenanthrene derivative with opioid agonist and antagonist properties. It has central analgesic actions and produces generalised CNS depression. It also alters perception of and response to pain by binding to opiate receptors in the CNS.
Onset: IM or nasal admin: 10-15 minutes.
Duration: 3-4 hr (IM); 5 hr (nasal).
Absorption: Peak plasma concentrations after 0.5-1 hr (IM/nasal); 1-1.5 hr (oral).
Distribution: Crosses the placenta and enters breast milk. Protein-binding: 80%.
Metabolism: Hepatic; extensive 1st-pass metabolism.
Excretion: Mainly in the urine; 11-14% of parenteral dose excreted in bile; 3 hr (elimination half-life).
Storage Conditions
 Nasal: Store below 30°C. Parenteral: Store below 30°C.
Storage
 Nasal: Store below 30°C. Parenteral: Store below 30°C.
Available As
  • Butorphanol 1 mg
  • Butorphanol 2 mg

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