Buprenorphine
Narcotic Analgesic · Opioid analgesic
Indications
Moderate to severe pain.
Dosage
Adults: Injection: 0.3-0.6 mg by IM or slow IV inj six or eight hourly. Tablets: 1-2 sublingually six to eight hourly or as required. Patch: Chronic pain (moderate to severe): Each patch is intended to be worn for 7 days. Apply patch to a hairless or nearly hairless skin site. For opioid experience patients: 7.5 mcg/hr, 10 mcg/hr, 15 mcg/hr and 20 mcg/hr. Max: 20 mcg/hr. For opioid naive patients: Initiate with a 5 mcg/hr patch. Dose adjustments may be made in 5 mcg/hr, 7.5 mcg/hr, or 10 mcg/hr increments by using no more than two patches of the 5 mcg/hr, 7.5 mcg/hr, or 10 mcg/hr. Max: 20 mcg/hr. For cessation of therapy, use a gradual downward titration of the dose every 7 days to prevent signs and symptoms of withdrawal in the physically dependent patient, consider introduction of an appropriate immediate-release opioid medication. Do not abruptly discontinue. Children: Sublingual…
Administration
Administer deep IM or by IV slowly, over a period of at least 2 min. Administer via-deep IM injection. Administer via IV route slowly over at least 2 min. Administer over 20-30 min preferred when managing opioid withdrawal in heroin-dependent hospitalized patients. Compatibility: Compatible with D5NS, D5W, NS and LR. Stability: Protect from excessive heat > 40°C. Protect from light.
Adverse Effects
Drowsiness, nausea, dizziness, sweating, erythema, pruritus, rash, GI upset, dry mouth, anorexia, headache, tremor, insomnia, confusion, depression, anxiety, paraesthesia, dyspnoea, orthostatic hypotension, oedema, fatigue, asthenia, miosis, respiratory depression, vasodilatation, chest pain.
Risk Factor (Pregnancy/Lactation)
Pregnancy: Risk cannot be ruled out. Lactation: Contraindicated or not recommended. Contraindications: Opioid dependence, severe respiratory or hepatic insufficiency, Myasthaenia gravis. Delirium tremens. Precautions: Narcotic dependence or previous large doses of narcotics. Impaired respiratory or hepatic function. Acute alcohol intoxication, history of seizures, head injury, shock, impaired consciousness, raised intracranial pressure or intracranial lesions, toxic psychosis, fever, prostatic hypertrophy, urinary tract obstruction, biliary tract disorders, hypothyroidism. Elderly or debilitated patients.
Interactions
MAOIs or CNS depressants, alcohol, benzodiazepines, inhibitors or inducers of CYP3A4, hepatotoxic drugs.
Advice to Patient
Do not swallow sublingual tablets. Place tablet under tongue and let it dissolve. If more than two tablets do not fit in mouth, place only two tablets at a time and let them dissolve. If you are self-administering injection of this medication, follow directions for administration and disposal of needles as prescribed. Contact prescriber if there is difficulty in breathing, unrelieved nausea or vomiting, unusual weakness, increased sleepiness, chest pain, fast heartbeat, palpitations Avoid alcohol during therapy. Do not take OTC medications especially tranquilizers, sedatives, antihistamines, pain medications without consulting prescriber. Change position slowly when rising from sitting or lying position. If constipation is unrelieved in few days, consult prescriber for suitable laxative or stool-softener.
Pharmacokinetics
Onset of action: Analgesic: Immediate-release IM: =15 mins. Peak effect: Immediate-release IM: Approx. 1 hr. Duration: Immediate-release IM: =6 hrs. Extended release SC: 28 days. Absorption: Immediate-release IM and SC: 30%-40%. Metabolism: Primarily hepatic; extensive first-pass effect. Bioavailability (relative to IV administration): Buccal film: 46%-65%. Immediate-release IM: 70%. Sublingual tab: 29%. Transdermal patch: Approx. 15%. Half-life elimination: Premature neonates (GA 27-32 wks): Immediate-release IV: 20 ± 8 hrs. Children 4-7 yrs: Immediate-release IV: Approx. 1 hr. Adults: IV: 2.2-3 hrs. Buccal film: 27.6 ± 11.2 hrs; Apparent terminal half-life: Sublingual tab: Approx. 37 hrs; Transdermal patch: Approx. 26 hrs. Time to peak, plasma: Buccal film: 2.5-3 hrs; Extended-release SC: 24 hrs, with steady state achieved after 4-6 mths; Subdermal implant: 12 hrs after insertion,…
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
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