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Buprenorphine information from DrugsUpdate  

See Available Brands of Buprenorphine in India

P - Cautioned while taken during pregnancy
L - Cautioned while taken during lactation

Buprenorphine is a semi-synthetic opiate with partial agonist and antagonist actions. Buprenorphine hydrochloride was first marketed in the 1980s by Reckitt & Colman (now Reckitt Benckiser) as an analgesic, available generally as Temgesic 0.2mg sublingual tablets, and as Buprenex in a 0.3mg/ml injectable formulation. In October 2002, the Food and Drug Administration (FDA) of the United States of America additionally approved Suboxone and Subutex, buprenorphine's high-dose sublingual pill preparations for opioid addiction, and as such the drug is now also used for this purpose. In the European Union, Suboxone and Subutex, buprenorphine's high-dose sublingual pill preparations were approved for opioid addiction treatment in September 2006. In the Netherlands, Buprenorphine is a List II drug of the Opium Law, though special rules and guidelines apply to its prescription and dispensation. In the USA, it has been a Schedule III drug under the United Nations' Convention on Psychotropic Substances since it was rescheduled from Schedule V just before FDA approval of Suboxone and Subutex.[1] In recent years, buprenorphine has been introduced in most European countries as a transdermal formulation for the treatment of chronic pain.

Pharmacodynamics

Pharmacokinetics

Buprenorphine exerts its analgesic effect by binding to the mu-opioid receptors in the CNS. It has a longer duration of analgesic action than morphine. Its partial agonist activity gives it a low level of physical dependence. Buprenorphine and morphine show similar dose-related resp depressant effect.
Absorption: Rapidly absorbed through the muscles (IM), buccal mucosa (sublingual); peak plasma concentrations after 90 minutes (sublingual).
Distribution: Enters breast milk. Protein-binding: 96%.
Metabolism: Minimal 1st-pass effect; converted to N-dealkylbuprenorphine and conjugated metabolites. There is enterohepatic recirculation.
Excretion: Via faeces (mainly unchanged), via urine (small amounts as unchanged); 1.2-7.2 hr (elimination half-life).

Buprenorphine Indications / Buprenorphine Uses

Information Not Available

Buprenorphine Adverse Reactions / Buprenorphine Side Effects

Sedation, nausea, dizziness, vertigo, hypotension, miosis, headache, hypoventilation, resp or CNS depression; tachycardia, bradycardia, urinary retention, coma, vomiting, drowsiness, sweating, confusion, dry mouth, diaphoresis, withdrawal syndrome.

Precautions

Information Not Available

Special Precautions

Hepatic or renal disease; pregnancy, lactation; hypothyroidism; adrenocortical insufficiency; asthma; prostatic hyperplasia; shock; hypotension; inflammatory or obstructive bowel disorders; myasthaenia gravis; infants/neonates. Reduce dose in elderly and debilitated patients. May precipitate withdrawal symptoms in narcotic addicts.

Other Drug Interactions

Plasma-buprenorphine concentrations may be affected when co-administered with drugs that induce or inhibit cytochrome P450 isoenzyme CYP3A4. Enhanced depressant effects with other CNS depressants e.g. alcohol, anaesthetics, anxiolytics, hypnotics, TCAs and antipsychotics.
Potentially Fatal: Diazepam may produce resp and cardiac collapse.

Other Interactions

Information Not Available

Dosage

Sublingual
Moderate to severe pain
Adult: 200-400 mcg every 6-8 hr.
Child: >6 yr: 37.5-50 kg: 200-300 mcg; 25-37.5 kg: 100-200 mcg; 16-25 kg: 100 mcg. To be given every 6-8 hr.
Intravenous
As a perioperative analgesic supplement
Adult: 300-450 mcg via slow IV inj.
Intramuscular
Premedication before anaesthesia
Adult: 300 mcg. May also be given sublingually at 400 mcg.
Parenteral
Moderate to severe pain
Adult: 300-600 mcg IM or slow IV Inj repeated every 6-8 hr if needed.
Child: >6 mth: 3-6 mcg/kg every 6-8 hr. Max: 9 mcg/kg every 6-8 hr.

Food(before/after)

Information Not Available

List of Contraindications

Buprenorphine and Pregnancy

Cautioned when used in pregnancy

Buprenorphine and Lactation

Cautioned when used in lactation

Buprenorphine and Children

Breathing problems may be especially likely to occur in children younger than 2 years of age. These children are usually more sensitive than adults to the effects of narcotic analgesics. Also, unusual excitement or restlessness may be more likely to occur in children receiving these medicines. Hydromorphone extended-release capsules should not be used in children younger than 18 years of age.

Buprenorphine and Geriatic

Elderly people are especially sensitive to the effects of narcotic analgesics. This may increase the chance of side effects, especially breathing problems, during treatment.

Buprenorphine and Other Contraindications

Acute alcoholism; convulsive disorders; head injuries; increased intracranial pressure; comatose patients; resp depression and obstructive airway disease; patients on established opioid agonists.

Storage

Intramuscular: Store at 15-30°C.
Intravenous: Store at 15-30°C.
Parenteral: Store at 15-30°C.
Sublingual: Store at 15-30°C.

Lab interference

Intramuscular: Store at 15-30°C.
Intravenous: Store at 15-30°C.
Parenteral: Store at 15-30°C.
Sublingual: Store at 15-30°C.

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