Antiflex - General Information
A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.
Pharmacology of Antiflex
Antiflex is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculoskeletal conditions. Antiflex is an anticholinergic with a predominantly central effect and only a weak peripheral effect. In addition, it has mild antihistaminic and local anaesthetic properties. Parkinson's syndrome is the consequence of a disturbed balance between cholinergic and dopaminergic neurotransmission in the basal ganglia caused by a decrease in dopamine. Antiflex restores the physiological equilibrium and has a favourable effect on the rigidity and tremor of Parkinson's disease and Parkinsonian syndromes. The effect is somewhat less on bradykinesia.
Antiflex for patients
No information provided.
Contraindicated in patients with glaucoma, pyloric or duodenal obstruction, stenosing peptic ulcers, prostatic hypertrophy or obstruction of the bladder neck, cardiospasm (megaesophagus) and myasthenia gravis.
Contraindicated in patients who have demonstrated a previous hypersensitivity to the drug.
Additional information about Antiflex
Antiflex Indication: Indicated for the treatment of Parkinson's disease.
Mechanism Of Action: Antiflex binds to both histamine H1 receptors and NMDA receptors. It restores the motor disturbances induced by neuroleptics, in particular the hyperkinesia. The dopamine deficiency in the striatum increases the stimulating effects of the cholinergic system. This stimulation is counteracted by the anticholinergic effect of orphenadrine. It may have a relaxing effect on skeletal muscle spasms and it has a mood elevating effect.
Drug Interactions: Docetaxel The agent increases the serum levels and toxicity of docetaxel
Donepezil Possible antagonism of action
Galantamine Possible antagonism of action
Rivastigmine Possible antagonism of action
Food Interactions: Not Available
Generic Name: Orphenadrine
Synonyms: O-Methyldiphenhydramine; Orphenadrine Citrate; Orphenadine; Orphenadrin; Orphenate; Orphenedrine; Mephenamine
Drug Category: Antiparkinson Agents; Antidyskinetics; Skeletal Muscle Relaxants
Drug Type: Small Molecule; Approved
Other Brand Names containing Orphenadrine: Antiflex; Banflex; Biorphen; Brocadisipal; Brocasipal; Disipal; Flexoject; Mio-Rel; Myolin; Myotrol; Norflex; Orfro;
Absorption: Orphenadrine is almost completely absorbed in the gastrointestinal tract.
Toxicity (Overdose): Oral, mouse LD50 = 100 mg/kg; oral, rat LD50 = 255 mg/kg
Protein Binding: 95%
Biotransformation: Biotransformation occurs mainly in the liver. Pharmacologically active metabolites are N-demethyl orphenadrine and N,N-didemethyl orphenadrine.
Half Life: 13-20 hours
Dosage Forms of Antiflex: Tablet, extended release Oral
Chemical IUPAC Name: N,N-dimethyl-2-[(2-methylphenyl)-phenylmethoxy]ethanamine
Chemical Formula: C18H23NO
Orphenadrine on Wikipedia: http://en.wikipedia.org/wiki/Orphenadrine
Organisms Affected: Humans and other mammals