Drug/Small Molecule:
ethopropazine

2D structure

Overview

Generic Names: Aethopropropazin; Athapropazine; Athopropazin; Ethapropazine; Ethopromazine; Ethopropazine Hydrochloride; Etopropezina; Fempropazine; Fenpropazina; Isopthazine; Isotazin; Isothazine; Isothazine hydrochloride; Isothiazine; Phenopropazine; Phenoprozine; Prodierazine; Profenamina [INN-Spanish]; Profenamina [Italian]; Profenamine; Profenamine hydrochloride; Profenamine monohydrochloride; Profenaminum [INN-Latin]; Prophenamine; Prophenaminum
Trade Names: Dibutil; Lysivane; Parcidol; Pardidol; Pardisol; Parfezin; Parfezine; Parkin; Parkisol; Parphezein; Parphezin; Parsidan; Parsidol; Parsitan; Parsotil; Prodictazin; Rochipel; Rocipel; Rodipal; Tomil
PharmGKB Accession Id: PA449531

Description

Ethopropazine (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. (source: Drug Bank)

Indication

For use in the treatment of Parkinson's disease and also used to control severe reactions to certain medicines such as reserpine. (source: Drug Bank)

ATC Therapeutic Category

  • N04AA:Tertiary amines

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Ethopropazine's antiparkinson action can be attributed to its anticholinergic properties. Ethopropazine 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. Ethopropazine'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. (source: Drug Bank)

Pharmacology

Ethopropazine, 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. Ethopropazine also has a slight antihistaminic and local anesthetic effect. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Protein Binding

93% (source: Drug Bank)

Absorption

Well-absorbed from the gastrointestinal tract. (source: Drug Bank)

Toxicity

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. (source: Drug Bank)

Isomeric SMILES Code:

CCN(CC)C(C)CN1c2ccccc2Sc3c1cccc3 (source: Drug Bank)

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
CHRM1 Uncurated Annotation (source: Drug Bank)
GRIN3A Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00392
KEGG Drug ID:
D01118
PubChem Compound ID:
3290
PubChem Substance ID:
153942

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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