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Buprenorphine-an opioid used to treat opioid addiction, moderate acute pain and moderate chronic pain

Buprenorphine is used in medication-assisted treatment (MAT) to help people reduce or quit their use of heroin or other opiates More

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Description

Buprenorphine is used in medication-assisted treatment (MAT) to help people reduce or quit their use of heroin or other opiates

Generic Name

Buprenorphine-an opioid used to treat opioid addiction, moderate acute pain and moderate chronic pain

Chemical names

Buprenex; Temgesic; Buprenorfina; Buprenorphinum

Brand names

Addnok, Bunogesic, Buprigesic, Buprine, Buprinor, Norphin, Pentorel, Qudict, Tidigesic.

IUPAC name

(1S,2R,6S,14R,15R,16R)-3-(cyclopropylmethyl)-16-[(2S)-2-hydroxy-3,3-dimethylbutan-2-yl]-15-methoxy-13-oxa-3-azahexacyclo[13.2.2.1²,?.0¹,?.0?,¹?.0?,¹²]icosa-7,9,11-trien-11-ol.

Pharmacokinetics

Actions

Buprenorphine's analgesic effect is due to partial agonist activity at mu-opioid receptors. Buprenorphine is also a kappa-Opioids receptor antagonist, binding to kappa and mu receptors results in hyper polarization and reduced neuronal excitability. Furthermore, buprenorphine slowly dissociates from its receptor. 

Dosage/Dosage form

The recommended dose is 0.3 to 0.6 mg by IM/IV/SC routes.0.2 to 0.4 mg ¾ times a day sublingual.

Therapeutic uses

Prescribed for moderate to severe pain.

Adverse effects/Side effects

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

Interaction

·       Enhanced depressant effects with other CNS depressants e.g. anaesthetics, alcohol, anxiolytics, hypnotics, TCAs and antipsychotics. Diazepam may produce respiratory and cardiac collapse.

·       Plasma-buprenorphine concentrations may be affected when co-administered with drugs that induce or inhibit cytochrome P450 isoenzyme CYP3A4.

Contraindications

  • Convulsive disorders; head injuries; comatose patients; increased intracranial pressure; respiratory depression and obstructive airway disease; patients on established Opioids agonists.
  • Acute alcoholism; 

Storage

Store at 15-30°C.

Information

Molecular weight

467.6401

Molecular formula

C29H41NO4

CAS number

52485-79-7

Precautions

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