Buprenorphine

Buprenorphine is a unique opioid medication used for the treatment of severe pain and opioid addiction. It has distinct pharmacokinetic and pharmacodynamic properties.

Aspect	Details about Buprenorphine
Classification	Partial mu-opioid receptor agonist and kappa-opioid receptor antagonist.
Clinical Use	• Treatment of severe pain. • Alternative to methadone for severe opioid addiction.
Formulation & Combination	• Suboxone: Combination with naloxone (4:1 fixed-dose) to reduce abuse potential. • Poorly absorbed gastrointestinally, formulated as sublingual tablet.
Pharmacokinetics & Dynamics	• Long duration of action (24-36 hours). • Slow dissociation from opioid receptors. • "Ceiling effect" at higher doses.
Dosage Forms	• Sublingual (SL): 200-400 µg t.d.s. (three times a day). • Transdermal matrix patch: 5, 10, 20 µg/h (once weekly); 35, 52.5, 70 µg/h (alternate every 3 or 4 days).
Dosage Equivalence	400 µg t.d.s. sublingual dose equivalent to 10-15 mg morphine every 4 hours.
Advantages Over Other Opioids	• Less effect on Qtc interval prolongation. • Fewer drug interactions and sexual side effects. • Lower risk of overdose and respiratory depression.
Transdermal Patch Pharmacokinetics	• 7-day patches: Analgesic effect evaluated after at least 3 days; 50% decrease in plasma concentration 12 hours after removal. • 4-day patches: Analgesic effect evaluated after at...

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