Pharmacology of Orphenadrine (Norflex); Mechanism of action, pharmacokinetics, pharmacodynamics

Orphenadrine is a centrally acting muscle relaxant and anticholinergic agent used to relieve musculoskeletal pain and discomfort. Here's an overview of its pharmacology:

Mechanism of Action
Orphenadrine works by blocking muscarinic acetylcholine receptors in the central nervous system, which helps reduce muscle spasms.

It also has antihistaminic and analgesic properties, contributing to its pain-relieving effects.

Additionally, it may act as an N-methyl-D-aspartate (NMDA) receptor antagonist, which could enhance its analgesic effects.

Pharmacokinetics
Absorption: Well-absorbed after oral administration.

Bioavailability: Approximately 90%.

Metabolism: Extensively metabolized in the liver via demethylation.

Half-Life: 13–20 hours.

Excretion: Primarily eliminated through the kidneys (renal excretion).

Clinical Applications
Used as an adjunct to rest and physical therapy for the relief of discomfort associated with acute musculoskeletal conditions.

Sometimes used to manage symptoms of drug-induced parkinsonism.

Adverse Effects
Common side effects include dry mouth, drowsiness, dizziness, constipation, and blurred vision.

Rare but serious effects include urinary retention, confusion, and tachycardia

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