Orphenadrine citrate, paracetamol.
Each tablet contains orphenadrine citrate 35 mg and paracetamol 450 mg.
Orphenadrine citrate is the citrate salt of orphenadrine (2-dimethylaminoethyl 2-methylbenzhydryl ether citrate) and closely related to diphenhydramine.
Pharmacology: Orphenadrine is a centrally-acting potent skeletal muscle relaxant by blocking reticular facilitation whose hyperactivity leads to spasticity, rigidity and muscle spasm. It does not affect normal muscle tone and voluntary movement. Action is rapid in onset and relatively prolonged. It also possesses anticholinergic properties and this acts by blocking the effect of acetylcholine in CNS.
The combination of anticholinergic effects and CNS penetration make orphenadrine useful for pain of all etiologies including pain from radiculopathy, muscle pain, headaches and many others.
Paracetamol has antipyretic, analgesic and weak anti-inflammatory properties by inhibiting prostaglandin synthesis in CNS and peripheral tissues.
Pharmacokinetics: Orphenadrine is readily absorbed from the GIT and has bioavailability of 90%. The t½ is approximately 13-20 hrs and it is metabolized in the liver by hepatic demethylation. Excretion is via renal and biliary tracts.
Paracetamol is rapidly absorbed from the GIT primarily in small gut by passive transport. It is metabolized primarily by 1st order kinetics. Massive plasma levels occur within 20-90 min after ingestion. It is metabolized in the liver by conjugation with glucuronic acid and to a lesser extent with sulfuric acid. Paracetamol appear to be distributed throughout most body fluid except fat and cerebrospinal fluid. The biological t½ of paracetamol in normal adults is about 2-3 hrs in usual dosage range.
Painful muscular conditions, tension headache, non-articular rheumatism, acute and traumatic conditions of the limbs and trunk: sprains, strains, prolapsed intervertebral disc.
Orphenadrine shows some anticholinergic activity and should not be used in patients with glaucoma, prostatic hypertrophy or obstruction at the bladder neck or myasthenia gravis.
Norgetex should be used with caution in patients with tachycardia, cardiac decompensation, coronary insufficiency and cardiac arrhythmias.
Safety of continuous long-term therapy with orphenadrine has not been established. Therefore if orphenadrine is prescribed for prolonged use, periodic monitoring of blood, urine and liver function is recommended. Orphenadrine may cause transient episodes of lightheadedness, dizziness or syncope. Patients should observe caution while driving or performing other tasks requiring alertness, coordination or physical dexterity.
Use in pregnancy: Pregnancy Category C. Animal reproduction studies have not been conducted with orphenadrine. It is also not known whether orphenadrine can cause fetal harm when administered to pregnant women or can affect reproduction capacity. Orphenadrine should be given to a pregnant woman only if clearly needed.
Use in children: Safety and effectiveness in pediatric patients have not been established.
Use in pregnancy: Pregnancy Category C. Animal reproduction studies have not been conducted with orphenadrine. It is also not known whether orphenadrine can cause fetal harm when administered to pregnant women or can affect reproduction capacity. Orphenadrine should be given to a pregnant woman only if clearly needed.
Side effects rarely occur at the recommended dosage. Those encountered are associated with anticholinergic activity and may include dry mouth, nausea, blurring of vision. Rarely, rash or drowsiness may occur. These symptoms disappear rapidly with a reduction in dosage or cessation of medication. No toxic effects have been observed.
M03BC51 - orphenadrine, combinations ; Belongs to the class of ethers. Used as centrally-acting muscle relaxants.
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