Butorphanol + Tartrate information from DrugsUpdate  

Pharmacodynamics

Pharmacokinetics

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 hours (IM); 5 hours (nasal).

Absorption
Peak plasma concentrations after 0.5-1 hour (IM/nasal); 1-1.5 hour (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 hours (elimination half-life).

Butorphanol + Tartrate Indications / Butorphanol + Tartrate Uses

Information Not Available

Butorphanol + Tartrate Adverse Reactions / Butorphanol + Tartrate Side Effects

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.

Precautions

Monitor
Take vital signs and auscultate heart and lungs before administration.

Labor and Delivery
Rare reports of infant respiratory distress/apnea following butorphanol administration within 2 hours of delivery, multiple butorphanol doses, use with other analgesic/sedative drugs, or in preterm pregnancies. Use with caution in presence of abnormal fetal heart rate patterns.

Hazardous Tasks
May cause drowsiness, dizziness, or hypotension during first hour of dosing.

CV disease
Drug increases cardiac workload. Severe hypertension has occurred.

Drug dependency
Although potential for physical dependence is low, abuse may occur. Tolerance and psychological and physical dependence may occur with long-term use. Use in patients physically dependent on opiate agonists may precipitate withdrawal symptoms.

Head injury and increased intracranial pressure
May cause C0 2 retention and secondary elevation of CSF pressure, drug-induced miosis, and alterations in mental status that could obscure interpretation of clinical course of patients with head injuries.

Respiratory depression
May occur, especially in patients on other CNS drugs or in patients with CNS disease or respiratory impairment.

Special populations
Use with caution in patients with hepatic or renal disease.

Special Precautions

Elderly; renal and hepatic impairment; hypertensive patients (when used preoperatively); patients with acute MI; head injury; lactation; patients on MAOI or within 2 weeks of treatment withdrawal.

Other Drug Interactions

Additive depressant effects with other CNS depressants e.g. general anaesthetics, phenothiazines or other tranquilizers, sedatives, hypnotics, antihistamines or alcohols.

Other Interactions

Information Not Available

Dosage

Parenteral
Moderate to severe pain
Adult: 1-4 mg via IM injection or 0.5-2 mg IV injection every 3-4 hours.

Parenteral
Anaesthesia
Adult: As premedicant before surgery: 2 mg given via IM injection 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.

Nasal
Moderate to severe pain
Adult: Initially, 1 mg, repeated after 60-90 minutes if necessary; may be repeated after 3-4 hours when necessary. For severe pain, initial dose can be 2 mg, repeated only after 3-4 hours.
Elderly: Initial dose: 1/2 usual adult dose. Recommended dose interval: at least 6 hours.

Renal impairment
Initial dose: 1/2 usual adult dose. Recommended dose interval: at least 6 hours.

Hepatic impairment
Initial dose: 1/2 usual adult dose. Recommended dose interval: at least 6 hours.

Food(before/after)

Information Not Available

Butorphanol + Tartrate and Pregnancy

Contraindicated in pregnancy.

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

If prolonged use/high doses at term:
Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Butorphanol + Tartrate and Lactation

Caution when used during lactation

Butorphanol + Tartrate and Children

Safety and efficacy not established

Butorphanol + Tartrate and Geriatic

More sensitive to effects; reduce dose

Butorphanol + Tartrate and Other Contraindications

Opiate-dependent patients who have not been detoxified; acute resp depression; pregnancy.

Storage

Nasal
Store below 30°C.

Parenteral
Store below 30°C.

Lab interference

Nasal
Store below 30°C.

Parenteral
Store below 30°C.