Orphenadrine

Indications
Oral
Muscle spasms
Adult: As citrate: 100 mg bid orally.
Oral
Parkinsonism and drug-induced extrapyramidal syndrome
Adult: As hydrochloride: Initially, 150 mg daily in divided doses; increase gradually by 50 mg every 2-3 days depending on response. Maintenance: 150-300 mg/day. Some patients may require up to 400 mg daily.
Max Dosage: 400 mg/day.
Parenteral
Muscle spasms
Adult: As citrate: 60 mg every 12 hr by IM or slow IV (over 5 min) inj.
Contraindications
Glaucoma, prostatic hypertrophy, GI obstruction, stenosing peptic ulcer, bladder neck obstruction, cardiospasm, myasthenia gravis.
Warnings / Precautions
Elderly; pregnancy and lactation. May impair ability to drive or operate machinery. CHF, cardiac decompensation, coronary insufficiency , tachycardia, or cardiac arrhythmias. History of drug abuse or acute alcoholism.
Adverse Reactions
Palpitation, tachycardia; agitation, drowsiness, dizziness, euphoria, hallucination, headache, mental confusion; pruritus, urticaria; constipation, gastric irritation, nausea, vomiting, xerostomia; urination hesitancy, urinary retention; aplastic anaemia (rare); tremor, weakness; blurred vision, increased intraocular pressure, nystagmus, pupil dilatation; nasal congestion; hypersensitivity.
Potentially Fatal: Anaphylactic reactions (rare).
Overdose Reactions
Symptoms: Blurred vision, tachycardia, confusion, seizures, respiratory arrest, dysrhythmias. 2-3 g may be lethal in adults. Management: Physostigmine 1-2 mg IV slowly may be given to reverse anticholinergic effects. Otherwise, treatment is symptomatic and supportive.
Drug Interactions
Reduced effect with acetylcholinesterase inhibitors e.g. donepezil, galantamine, rivastigmine, tacrine; may reduce effect of centrally-acting acetylcholinesterase inhibitors. Additive sedative effects with CNS depressants, alcohol. Pramlintide may increase anticholinergic effect on the GI tract. Increased risk of anticholinergic adverse effects with diphenhydramine, TCAs, phenothiazines.
See Below for More orphenadrine Drug Interactions
Food Interactions
Additive CNS depression may occur with valerian, St John's wort, kava kava, gotu kola.
Mechanism of Actions
Orphenadrine is a tertiary amine antimuscarinic which exerts antiparkinsonian action by inhibiting excess central cholinergic effects that occur due to dopamine deficiency. It reduces muscle spasms possibly by its atropine-like effect on the medulla or on cerebral motor centers.
Absorption: Readily absorbed from the GI tract and after IM inj.
Metabolism: Almost completely metabolised to at least 8 metabolites.
Excretion: Mainly via urine (as metabolites and traces of unchanged drug). Half-life: 14 hr.
Administration
May be taken with or without food. (May be taken w/ meals if GI upset occurs.)
Storage Conditions
Oral: Store at 15-30°C (59-86°F). Parenteral: Store at 15-30°C (59-86°F). Protect from light.
Storage
Oral: Store at 15-30°C (59-86°F). Parenteral: Store at 15-30°C (59-86°F). Protect from light.
Available As
  • Orphenadrine 35 mg
  • Orphenadrine 50 mg
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