Parfezine - General Information
Parfezine (also known as profenamine hydrochloride) is a medication derived from phenothiazine. It is primarily used as an antidyskinetic to treat parkinsonism. It is sold under the trade names Parsidol in the United States and Parsidan in Canada.
Pharmacology of Parfezine
Parfezine, a phenothiazine and antidyskinetic, is used in the treatment of Parkinson's disease. By improving muscle control and reducing stiffness, this drug permits more normal movements of the body as the disease symptoms are reduced. It is also used to control severe reactions to certain medicines such as reserpine, phenothiazines, chlorprothixene, thiothixene, loxapine, and haloperidol. Unlike other NMDA antagonists, ethopropazine — because of its anticholinergic action — is largely devoid of neurotoxic side effects. Parfezine also has a slight antihistaminic and local anesthetic effect.
Parfezine for patients
Several conditions may affect the use of this medicine including a history of sensitivity to antidyskinetics, breast feeding (as this drug may inhibit lactation), use in children (as children are more susceptible to anticholinergic effects), and use in the elderly (as the elderly are predispositioned to glaucoma with chronic use).
When taking this medicine, it is importance not to take more medication than the amount prescribed. If gastric irritation is experienced, taking the drug with food may relieve this condition. If you miss a dose, take it as soon as possible, but not within 2 hours of the next dose. Do not double dose. Regular visits to physician to check progress during prolonged therapy; eye examination may be needed while you are taking this medicine. Avoid alcohol or other CNS depressants. Also, avoiding use of antidiarrheal medications within 1 or 2 hours of taking this medication.
Ethopropazine may interact with alcohol or other CNS depressants, causing increased sedative effects. It may also interact with amantadine or other anticholinergic drugs or MAOIs, which may intensify the anticholinergic action. Ethopropazine can interact with chlorpromazine, increasing the metabolism of chlorpromazine.
Ethopropazine is contraindicated for the treatment of patients with cardiovascular instability, as it may increase the risk of cardiac arrhythmias. Ethopropazine may aggravate tardive dyskinesia, may cause a mydriatic effect resulting in increased intraocular pressure and may precipitate an acute attack of angle-closure glaucoma, and is also contraindicated for patients with hepatic impairment, as the drug's metabolism may be altered. Ethopropazine may also aggravate hypertension, myasthenia gravis, urinary retention, and moderate to severe prostatic hypertrophy.
Additional information about Parfezine
Parfezine Indication: For use in the treatment of Parkinson's disease and also used to control severe reactions to certain medicines such as reserpine.
Mechanism Of Action: Parfezine's antiparkinson action can be attributed to its anticholinergic properties. Parfezine partially blocks central (striatal) cholinergic receptors, thereby helping to balance cholinergic and dopaminergic activity in the basal ganglia; salivation may be decreased, and smooth muscle may be relaxed. Drug-induced extrapyramidal symptoms and those due to parkinsonism may be relieved, but tardive dyskinesia is not alleviated and may be aggravated by anticholinergic effects. Parfezine's local anesthetic effect is due to its antagonism of the NMDA glutamate receptor. Glutamate is recognized as an important transmitter in nociceptive pathways, and the N-methyl-D-aspartate (NMDA) subtype of the glutamate receptor, in particular, has been implicated in the mediation of neuropathic pain. Excessive release of glutamate at NMDA receptors on dorsal horn neurons of the spinal cord results in hyperactivation and hypersensitivity of these receptors (perceived as hyperalgesia), thought to be an integral feature of neuropathic pain.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Ethopropazine
Synonyms: Ethopropazine Hydrochloride; Ethapropazine; Ethopromazine; Etopropezina; Aethopropropazin; Athapropazine; Athopropazin; Isothazine hydrochloride; Isothazine; Isotazin; Isopthazine; Fenpropazina; Isothiazine; Profenaminum [Inn-Latin]; Profenamine monohydrochloride; Profenamine hydrochloride; Profenamine; Profenamina [Italian]; Profenamina [Inn-Spanish]; Prophenamine; Prophenaminum; Prodierazine; Phenoprozine; Phenopropazine; Fempropazine
Drug Category: Antiparkinson Agents; Antidyskinetics
Drug Type: Small Molecule; Approved
Absorption: Well-absorbed from the gastrointestinal tract.
Toxicity (Overdose): Symptoms of overdose include severe clumsiness or unsteadiness, severe drowsiness, severe dryness of mouth, nose, or throat, fast heartbeat, shortness of breath or troubled breathing, and warmth, dryness, and flushing of skin.
Protein Binding: 93%
Biotransformation: Not Available
Half Life: 1 to 2 hours
Dosage Forms of Parfezine: Tablet Oral
Chemical IUPAC Name: N,N-diethyl-1-phenothiazin-10-ylpropan-2-amine
Chemical Formula: C19H24N2S
Ethopropazine on Wikipedia: https://en.wikipedia.org/wiki/Ethopropazine
Organisms Affected: Humans and other mammals