Buprenorphine
- Atc Codes:N02AE01
- CAS Codes:53152-21-9#52485-79-7
- PHARMGKB ID:53152-21-9#52485-79-7
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Subutex, Temgesic; Belgium: Subutex, Temgesic, Transtec; Cyprus: Temgesic; Czech Republic: Norspan, Subutex, Temgesic, Transtec; Denmark: Buprenorphin, Norspan, Subutex, Temgesic, Transtec; Estonia: Norspan, Subutex; Finland: Norspan, Subutex, Temgesic; France: Buprenorphine, Subutex, Temgesic; Germany: Buprenorphin, Norspan, Subutex, Temgesic, Transtec; Greece: Prenorvine, Subutex, Temgesic; Hungary: Norspan, Subutex, Transtec; Ireland: Butrans, Centradol, Subutex, Temgesic, Transtec; Italy: Subutex, Temgesic, Transtec; Lithuania: Norspan, Subutex; Luxembourg: Temgesic, Transtec; Netherlands: BuTrans, Buprenorfine, Subutex, Temgesic, Transtec; Poland: Bunondol, Temgesic, Transtec; Portugal: Buprenorfina, Buprex, Norspan, Subutex, Transtec, Triquisic; Slovakia: Norspan, Subutex, Temgesic, Transtec; Slovenia: Transtec; Spain: Buprenorfina, Buprex, Subutex, Transtec, Triquisic; UK: BuTrans, Temgesic, Transtec.
North America
Canada: Buprenex, Subutex; USA: Buprenex, Buprenorphine, Butrans, Subutex.
Latin America
Brazil: Temgesic; Mexico: Brospina, Temgesic, Transtec.
Asia
Japan: Lepetan, Zalba.
Drug combinations
Buprenorphine and Naloxone
Chemistry
Buprenorphine Hydrochloride: C~29~H~41~NO~4~ HCl. Mw: 504.10. (1) 6,14-Ethenomorphinan-7-methanol, 17-(cyclopropylmethyl)-α-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-α-methyl-, hydrochloride, [5α,7α(S)]-; (2) 21-Cyclopropyl-7α-[(S)-1-hydroxy-1,2,2-trimethylpropyl]-6,14-endo-ethano-6,7,8,14-tetrahydrooripavine hydrochloride. CAS-53152-21-9; CAS-52485-79-7 (buprenorphine)(1976).
Pharmacologic Category
Analgesics and Antipyretics; Opiate Partial Agonists. (ATC-Code: N02AE01).
Mechanism of action
Binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering perception of and response to pain. Produces generalized CNS depression. When used as recommended, buprenorphine acts as a classic μ-receptor agonist (like morphine).
Therapeutic use
Relief of moderate to severe pain. Management of opiate dependence.
Pregnancy and lactiation implications
Use only when the potential benefits to the mother justify the possible risks to the fetus. There have been reports of opiate withdrawal symptoms in neonates after maternal use for opiate dependence during pregnancy. Use not recommended during lactation.
Unlabeled use
Management of postoperative pain. Preoperative sedation and analgesia. As an adjunct to surgical anesthesia. As an antagonist to reverse fentanyl-induced anesthesia. Management of refractory endogenous depression.
Contraindications
Hypersensitivity to buprenorphine or any component of the formulation.
Warnings and precautions
May cause CNS depression. Use with extreme caution in head injury, intracranial lesions, or elevated intracranial pressure (risk of exaggerated elevation of ICP). Concurrent use of agonist/antagonist analgesics, or abrupt discontinuation of the drug, may precipitate withdrawal symptoms and/or reduced analgesic efficacy in patients following prolonged therapy with μ-opioid agonists. Buprenorphine has a longer duration of action than either morphine or meperidine. Avoid in labor. Possible psychological dependence on the opiate agonist activity of buprenorphine. May cause hypotension (caution in hypovolemia, cardiovascular disease, or hypotensive drugs). May obscure diagnosis or clinical course of acute abdominal conditions. Use with caution in biliary tract dysfunction (acute pancreatitis may cause constriction of sphincter of Oddi), history of ileus or bowel obstruction, hepatic impairment, in patients who are morbidly obese, in debilitated patients (greater potential for critical respiratory depression), adrenal insufficiency (including Addison’s disease), thyroid dysfunction, severe renal impairment, prostatic hyperplasia and/or urinary stricture, pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function (risk of critical respiratory depression). Use with caution in the elderly (higher sensitivity to adverse effects). Acute and chronic hypersensitivity reactions reported. Decreases in erythrocyte count, hematocrit, hemoglobin, sedimentation rate, and total serum protein concentration reported during prolonged administration. Serum alkaline phosphatase concentrations also decreased during prolonged buprenorphine therapy. Pain or sweating reported in patients receiving sublingual buprenorphine or buprenorphine in fixed combination with naloxone for the treatment of opiate dependence in clinical studies.