Buprenorphine is a long-acting, semi-synthetic opioid analgesic derived from thebaine. At the 20mg strength, it is primarily formulated as a sublingual tablet for the management of opioid dependence, functioning as a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. It is a cornerstone of Opioid Substitution Therapy (OST) in India, used for maintenance and detoxification.
Adult: Opioid Dependence (Induction & Maintenance): Individualized. Induction: Typically 2-8 mg sublingually on day 1, titrated upwards in increments of 2-4 mg to a maintenance dose of 12-24 mg/day. 20mg is within the common maintenance range. Maximum recommended single dose is 32 mg. Dosing is supervised at the center.
Note: For sublingual use only. Tablet must be placed under the tongue and allowed to dissolve completely. Patient should not chew, swallow, or talk until the tablet is fully dissolved (takes 2-10 minutes). Do not eat or drink until tablet is dissolved. Dosing is typically supervised at the OST clinic.
Buprenorphine binds with high affinity and slow dissociation to mu-opioid receptors in the central nervous system. As a partial agonist, it produces a sub-maximal analgesic and euphoric effect compared to full agonists (e.g., morphine, heroin). This property reduces abuse potential, attenuates withdrawal symptoms in dependent individuals, and blocks the effects of subsequently administered full opioid agonists. Its antagonist action at kappa receptors may contribute to a lower incidence of dysphoria and psychotomimetic effects.
Pregnancy: Pregnancy Category C (US FDA). Use only if potential benefit justifies potential fetal risk. Can cause neonatal opioid withdrawal syndrome (NOWS) if used chronically. However, for pregnant women with opioid dependence, medication-assisted treatment (MAT) with buprenorphine is preferred over untreated addiction or detoxification alone, as per WHO and Indian guidelines. Requires specialist management.
Driving: May impair mental and/or physical abilities required for driving or operating machinery, especially during initiation and dose adjustment. Patients should be cautioned.
| Benzodiazepines (e.g., Alprazolam, Diazepam) | Profound sedation, respiratory depression, coma, and death. | Major - CONTRAINDICATED for non-medical use. Extreme caution even with prescribed use. |
| Other CNS Depressants (Alcohol, Barbiturates, Sedative-hypnotics) | Additive CNS depression, increased risk of respiratory depression. | Major |
| CYP3A4 Inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin, Ritonavir, Grapefruit juice) | Increased buprenorphine plasma levels, risk of toxicity/overdose. | Moderate to Major |
| CYP3A4 Inducers (e.g., Rifampicin, Carbamazepine, Phenytoin, St. John's Wort) | Decreased buprenorphine plasma levels, risk of withdrawal symptoms and treatment failure. | Moderate to Major |
| Full Opioid Agonists (e.g., Morphine, Methadone, Heroin) | Buprenorphine may block effects or precipitate withdrawal if patient is dependent. | Major |
| MAO Inhibitors (e.g., Phenelzine, Selegiline) | Risk of serotonin syndrome or opioid toxicity (excitation, hyperpyrexia). | Major - CONTRAINDICATED |
| Serotonergic Drugs (SSRIs, SNRIs, TCAs, Tramadol) | Potential increased risk of serotonin syndrome. | Moderate |
Same composition (Buprenorphine (20mg)), different brands: