Buprenorphine Pharmacology


About Buprenorphine
Semi-synthetic opiate (thebaine derivative ), narcotic agonist(mu)-antagonist(kappa), opioid analgesic.
Mechanism of Action of Buprenorphine
It is a semi synthetic Opioid derivative. It has partial mu receptor agonistic action. So it gives a low level of physical dependence. It has analgesic action similar to morphine. At kappa receptors it has antagonistic action. So it is classified as narcotic agonist-antagonist
Pharmacokinets of Buprenorphine
Absorption-Well absorbed after intramuscular, intravenous and sublingual administration.
Distribution-96% is protein bound.
Metabolism- Metabolized in the liver by N- dealkylation and conjugation.
Excretion-Mainly through faeces and 30% excreted via urine as unchanged form.
Onset of Action for Buprenorphine
Intravenous- Immediate action after administration.
Intramuscular-15min after administration.
Sublingual-Immediate action after administration.
Duration of Action for Buprenorphine
Intravenous -6hrs.
Sublingual -6hrs.
Half Life of Buprenorphine
Plasma half life is about 3 hrs.
Side Effects of Buprenorphine
1. Nausea
2. Vomiting
3. Dizziness
4. Hypotension
5. Vertigo
6. Tachycardia
7. Bradycardia
8. Urinary retention
9. Diaphoresis
10. Withdrawal symptoms
Contra-indications of Buprenorphine
1.Hypersensitivity to this drug
2. Respiratory depression
3. Acute alcoholism
4. Increased intracranial pressure
5. Head injury
6. Pregnancy
Special Precautions while taking Buprenorphine
1.Hepatic dysfunction
2.Renal dysfunction
3.Respiratory depression
4.Adreno cortical insufficiency
6.Myasthenia gravis
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Children Related Information
Indications for Buprenorphine
2.Opioid dependant treatment
3. Pre operative analgesia
Interactions for Buprenorphine
Barbiturate anaesthetics: Cause respiratory and CNS depression due to additive activity.
Diazepam: Respiratory and cardiovascular collapse.
Alcohol, CNS depressants, MAOIs: Effects potentiated.
Narcotic addicts: May precipitate withdrawal.
Typical Dosage for Buprenorphine
300 to 600 mg i.m or slow i.v. repeated every 6-8 hrs.
Sublingual administration - 200 to 400mcg every 6-8hrs.
Children (>6 months)-
Intramuscular-3 to 6 mcg/kg every 6-8 hrs.
200-300 mcg for 37.5-50 kg
100-200 mcg for 25-37.5 kg.
100 mcg for 16-25kg
Schedule of Buprenorphine
Storage Requirements for Buprenorphine
Stored between 15 and 30 degree Celsius and protect from light.
Effects of Missed Dosage of Buprenorphine
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Buprenorphine
Provide symptomatic and supportive treatment. Establish respiratory exchange via artificial method. Administer narcotic antagonist naloxone for the reversal of respiratory depression. Repeated dosing is necessary because duration of buprinorphhine is longer than naloxone. Monitor vital signs and laboratory parameters closely.

Home Delivery for Buprenorphine in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including buprenorphine.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for buprenorphine and other medicines and health products. Home delivery services for buprenorphine may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take buprenorphine only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for buprenorphine before they complete the sale. You can get this information while placing the order for buprenorphine with the pharmacy.

Buprenorphine is a generic medicine name and there are several brands available for it. Some of the brands for buprenorphine might be better known than buprenorphine itself. If the pharmacy that's willing to deliver medicines to your home doesn't have buprenorphine in stock, you can ask for one of the branded alternatives for buprenorphine.