Buprenorphine (buprenorphine hydrochloride)
Also sold as: Buprigesic, Norspan patch, Subutex (sublingual), Suboxone (buprenorphine + naloxone)
Pregnancy
Cat C
Lactation
Avoid
Schedule
NDPS
Forms
injection 0.3mg/mL (1mL ampoule — IM/slow IV) +3
Indications
- Moderate-to-severe acute pain (parenteral buprenorphine injection)
- Chronic moderate pain (transdermal patch — Norspan)
- Opioid Use Disorder (OUD) — opioid dependence treatment and maintenance (sublingual buprenorphine or buprenorphine+naloxone)
- Opioid withdrawal management (sublingual buprenorphine)
- Cancer pain in patients with renal failure (preferred over morphine — no renally-cleared active metabolites)
Adult Dosing
Acute pain — IM or slow IV injection
0.2–0.4 mg every 6–8 hours as needed
Maximum 1.2 mg/day (parenteral)
Acute pain — sublingual
0.2–0.4 mg sublingually every 6–8 hours
Allow tablet to dissolve completely under tongue; do not swallow
Chronic pain — transdermal patch (Norspan)
Initiate at 5 mcg/h; escalate to 10 mcg/h then 20 mcg/h based on pain control
Change patch every 7 days
Opioid Use Disorder (OUD) — induction (sublingual)
2–4 mg SL on day 1; then 8–16 mg SL on day 2; stabilise on 8–24 mg SL once daily
Once daily; induction on day 1 and 2 only
Patient MUST have COWS score ≥8 (mild-to-moderate withdrawal) before first dose to avoid precipitating severe withdrawal.
Opioid Use Disorder (OUD) — maintenance with Suboxone
8–24 mg buprenorphine / 2–6 mg naloxone SL once daily
Once daily maintenance; review at least monthly
Pediatric Dosing
Specialist supervision required. OUD treatment not approved <16yr; ≥16yr under addiction medicine specialist.
Renal Dose Adjustment
| CrCl / eGFR | Dose Adjustment |
|---|---|
| Any (including CKD and ESRD) | No dose adjustment required — buprenorphine and its metabolites are primarily excreted in feces (biliary route), not renally. Preferred opioid in renal failure; transdermal patch and SL formulations preferred over parenteral |
Hepatic Adjustment
Buprenorphine is extensively metabolized by CYP3A4 in the liver. Moderate hepatic impairment (Child-Pugh B): use with caution; monitor for excess sedation. Severe hepatic impairment (Child-Pugh C): significantly reduced clearance — contraindicated for OUD induction (monitoring challenges), use with great caution for analgesia only under specialist supervision. Hepatitis and transaminase elevations observed with SL formulations — monitor LFTs in OUD treatment.
Pregnancy & Lactation
Pregnancy: Category C
Category C. Preferred agent for OUD treatment during pregnancy (over methadone in some guidelines, as it is associated with milder Neonatal Opioid Withdrawal Syndrome). Use buprenorphine monotherapy (NOT Suboxone/buprenorphine+naloxone) in pregnancy as naloxone safety data is limited. Neonatal opioid withdrawal syndrome (NOWS) is expected — neonatology involvement is mandatory.
Lactation: Avoid
Buprenorphine and metabolites are excreted in breast milk. However, WHO and some guidelines support breastfeeding in stable OUD patients on buprenorphine maintenance (benefits of breastfeeding may outweigh risks). Avoid in high-dose analgesia settings. Discuss individual risk-benefit with obstetric and lactation specialists.
Top Drug Interactions
| Interacting Drug | Effect | Severity |
|---|---|---|
| CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir, clarithromycin, erythromycin) | Significantly increase buprenorphine plasma levels, increasing risk of sedation and respiratory depression. Reduce buprenorphine dose by 25–50% when adding a CYP3A4 inhibitor; monitor respiratory function closely. | Major |
| CYP3A4 inducers (rifampicin, carbamazepine, phenytoin) | Reduce buprenorphine levels significantly, causing inadequate analgesia or precipitating withdrawal in OUD patients. Increase buprenorphine dose when adding inducer; titrate carefully when inducer is discontinued. | Major |
| Benzodiazepines / CNS depressants / Alcohol | Additive respiratory depression and sedation — potentially fatal combination, particularly in OUD patients who misuse benzodiazepines concurrently with Suboxone. FDA black box warning. Counsel patients explicitly about this combination. If concurrent use is unavoidable (e.g., anxiety disorder requiring benzodiazepine), use lowest effective doses with close monitoring. | Major |
| Naloxone (in Suboxone formulation) | Naloxone in Suboxone is poorly absorbed sublingually — this is intentional to prevent IV abuse (IV naloxone would precipitate acute withdrawal). If Suboxone is crushed and injected by an opioid-dependent patient, naloxone is fully active and precipitates severe acute opioid withdrawal. | Major |
| Full opioid agonists (morphine, fentanyl, oxycodone) | Buprenorphine has very high mu-receptor affinity and can displace full agonists, precipitating acute withdrawal if given to a patient NOT yet in withdrawal. When transitioning from full agonist to buprenorphine, patient must have COWS score ≥8 (mild withdrawal) before first buprenorphine dose. | Major |
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Side Effects
Common
- Headache
- Nausea and vomiting
- Constipation (less severe than full agonists due to ceiling effect)
- Sweating (particularly in OUD treatment doses)
- Insomnia
- Sedation and dizziness (especially on initiation)
- Sublingual formulation: oral numbness, taste disturbance, dry mouth
- Transdermal patch: local skin reactions (erythema, pruritus at site)
Serious / Discontinue If
- Precipitated opioid withdrawal — if administered to an opioid-dependent patient who is NOT yet in withdrawal, buprenorphine displaces the full agonist from opioid receptors (due to high affinity) and precipitates severe acute withdrawal: severe agitation, vomiting, diarrhea, piloerection, diaphoresis, muscle cramps. Management: supportive care; do NOT give more opioids — this worsens precipitated withdrawal.
- Respiratory depression — less than full agonists due to ceiling effect (theoretical safety advantage), but REAL RISK at high doses especially with concurrent CNS depressants or in opioid-naive patients
- Hepatotoxicity — transaminase elevations reported, particularly with high-dose SL formulations in OUD treatment; monitor LFTs at baseline and during treatment
- QTc prolongation — less than methadone, but monitor in patients with cardiac risk factors or on other QT-prolonging drugs
- Neonatal Opioid Withdrawal Syndrome (NOWS) — expected in neonates born to mothers on maintenance therapy; planned and managed with neonatology team
- Adrenal insufficiency with chronic use (opioid endocrinopathy)
Contraindications
- Acute respiratory depression (without resuscitative support)
- Severe hepatic impairment (OUD induction setting)
- Paralytic ileus
- Hypersensitivity to buprenorphine or naloxone (for Suboxone)
- Concurrent MAOI therapy (within 14 days)
- NDPS Act compliance mandatory for all formulations in India — register, record-keeping, prescription limits
Available Indian Brands
| Brand | Manufacturer | Price (approx) |
|---|---|---|
| Buprigesic 0.3mg/mL injection | Sun Pharma | ₹28/vial |
| Norspan 5mcg/h patch (7-day) | Mundipharma | ₹385/patch |
| Suboxone 2mg/0.5mg sublingual film | Indivior | ₹125/7 tab |
Monitoring Required
- COWS (Clinical Opioid Withdrawal Scale) score before first OUD induction dose — must be ≥8
- Urine drug screen (UDS) at baseline and periodically during OUD treatment (compliance and concurrent substance use)
- Liver function tests (ALT, AST) at baseline, 1 month, then quarterly during OUD treatment
- Respiratory rate and oxygen saturation — especially on initiation and dose changes
- Pain score (analgesic use)
- Mental health assessment (depression, anxiety — common in OUD patients)
- QTc interval at baseline and if on concurrent QT-prolonging drugs
- Body weight and nutritional status
- Treatment retention and social functioning (OUD context)
- Skin at patch application sites (Norspan — rotate weekly)
Patient Counseling Points
- For OUD treatment: Do NOT take your first buprenorphine dose until you feel withdrawal symptoms — sweating, yawning, goosebumps, runny nose, stomach cramps. Taking it too early will cause severe withdrawal immediately.
- For sublingual tablets/films: Place under the tongue or inside the cheek. Do not chew, swallow, or crush. Allow to dissolve completely (5–10 minutes). Do not eat or drink for 30 minutes before or after taking it.
- For Suboxone: The naloxone in this medicine is there to prevent misuse. If you try to inject it, you will go into immediate, severe withdrawal. Suboxone is for under-tongue (sublingual) use only.
- CRITICAL: Do NOT take benzodiazepines (like diazepam, clonazepam) or alcohol with this medicine — the combination can stop your breathing. This is a leading cause of overdose deaths.
- For the Norspan patch: apply to upper outer arm, chest, or back — clean, dry, hairless skin. Change every 7 days at the same time. Fold used patch and flush.
- Tell your doctor about ALL medicines you take, especially antifungals (like fluconazole, ketoconazole) and antibiotics (like clarithromycin) — they interact with buprenorphine.
- Constipation and sweating are common side effects. Increase water and fiber intake. A laxative may be needed.
- If you develop persistent nausea, yellowing of eyes/skin, or dark urine — contact your doctor immediately (rare liver side effect).
- If you are pregnant or planning pregnancy, inform your doctor — buprenorphine is one of the recommended treatments for OUD during pregnancy, but requires specialist management and neonatal monitoring.
- Do not share your medicine. This medicine is for your prescription only and is a controlled substance under Indian NDPS law.
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Clinically reviewed by: Dr. Arun Bhaskar, MD, DM Palliative Medicine, Tata Memorial Hospital Mumbai
Last reviewed: 2026-04-01
References
- SAMHSA. Clinical Practice Guideline for the Treatment of Opioid Use Disorder. 2023.
- WHO. Guidelines for the Pharmacologically Assisted Treatment of Opioid Dependence. 2009.
- Indivior. Suboxone (buprenorphine/naloxone) Prescribing Information. 2023.
- Mundipharma. Norspan (buprenorphine transdermal) Prescribing Information. 2022.
- Ministry of Health, India. National Drug Dependence Treatment Centre (NDDTC) OST Guidelines. 2021.