Generic
Buprenorphine
1 brands available in the market
At a glance
Buprenorphine is a partial opioid agonist used in the treatment of moderate to severe pain and opioid dependence. It provides pain relief by binding to mu-opioid receptors in the CNS and helps prevent withdrawal symptoms in patients stopping other opioids.
Description
Buprenorphine is a partial opioid agonist used for moderate to severe pain and opioid dependence. It binds to mu-opioid receptors in the CNS to relieve pain. Due to its partial agonist activity, it has a lower risk of physical dependence and life-threatening respiratory depression compared to full agonists like morphine.
Buprenorphine is available as sublingual tablets/films, transdermal patches, and injections. Sublingual forms are rapidly absorbed and used for acute pain and opioid dependence. Transdermal patches provide slow, steady release for chronic pain management.
Indications
- Moderate to severe pain
- Opioid dependence
Therapeutic class
Opioid Analgesic
Pharmacological class
Partial Opioid Agonist
Pharmacology
Buprenorphine is a partial opioid agonist that binds to mu-opioid receptors to relieve pain. Its partial agonist activity results in lower respiratory depression risk compared to full agonists. In opioid dependence, it replaces other opioids, reducing withdrawal symptoms and helping to eliminate dependence.
Mechanism of action
Buprenorphine binds to mu-opioid receptors in the CNS, blocking pain signal transmission. As a partial agonist, it produces less physical dependence than full agonists. In opioid dependence, it blocks other opioid effects and reduces withdrawal symptoms.
Dosage
Adults (Sublingual, Pain): 200-400 mcg every 6-8 hours.
Adults (IV/IM, Pain): 300-600 mcg every 6-8 hours.
Adults (Perioperative Analgesia, IV): 300-450 mcg slow IV injection.
Adults (Anesthesia Premed, IM): 300 mcg.
Elderly (Moderate-to-Severe Pain): 0.15 mg IV/IM q6hr (slow IV over 2 minutes).
Children (12 years): As in adults.
Hepatic impairment: Not recommended in serious liver disease; caution required.
Renal impairment: Caution in severe kidney disease; dose adjustment may be needed.
Administration
Take as advised by your doctor. Sublingual tablets should be placed under the tongue and allowed to dissolve; do not swallow, chew, or crush. May be taken with or without food.
Missed dose
If you miss a dose, take it as soon as you remember. Skip the missed dose if it is almost time for your next dose. Do not double the dose.
Side effects
Common side effects: Weakness, opioid withdrawal syndrome, anxiety, nervousness, dizziness, headache, sleepiness, diarrhea, nausea, vomiting, abdominal pain.
Serious side effects: Respiratory depression (especially with first use, dose increases, elderly, or lung disease).
Withdrawal symptoms (if stopped suddenly): Nausea, vomiting, diarrhea, muscle aches, sweating, anxiety.
Precautions & warnings
- Opioid medicines can cause respiratory depression; special caution needed with first use and dose increases.
- Do not stop abruptly (may cause withdrawal symptoms); gradually reduce dose with your doctor's guidance.
- May cause dizziness and sleepiness; avoid driving or tasks requiring concentration.
- Using with alcohol or other sedative medications increases risk of respiratory depression and overdose.
- Caution during pregnancy and lactation.
- Avoid use in serious liver disease; caution in hepatic and renal impairment.
Contraindications
- Acute alcoholism
- Convulsive disorders
- Head injuries
- Increased intracranial pressure
- Comatose patients
- Respiratory depression and obstructive airway disease
- Patients on established opioid agonists
Drug interactions
- CYP3A4 inhibitors (atazanavir, ritonavir): May increase buprenorphine plasma concentrations; dose adjustment may be needed.
- Other CNS depressants (alcohol, anesthetics, anxiolytics, hypnotics, TCAs, antipsychotics): Enhanced depressant effects.
- Diazepam: May cause respiratory and cardiac collapse (potentially fatal).
Food interactions
Alcohol consumption is unsafe (increases risk of respiratory depression and overdose).
Use in pregnancy
May be unsafe during pregnancy (Category C). Limited human data; animal studies show adverse fetal effects. Prolonged opioid use during pregnancy may cause neonatal opioid withdrawal syndrome (NOWS). Your doctor will weigh benefits and risks.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Probably unsafe during breastfeeding. Limited human data suggests the drug may pass into breast milk and harm the baby.
Pediatric use
Children 12 years: Same as adult dose. Safety in children under 12 years has not been established.
Geriatric use
Elderly patients require dose adjustment (higher risk of respiratory depression).
Renal / hepatic impairment
Hepatic impairment: Not recommended in serious liver disease; caution required.
Overdose effects
Overdose symptoms: Respiratory depression, extreme drowsiness, confusion, muscle weakness, cold and clammy skin, pinpoint pupils. Seek immediate medical attention if overdose is suspected.
Storage conditions
Store below 30°C, away from light and moisture. Keep out of reach of children.
Chemical structure
Buprenorphine Hydrochloride