Orphenadrine

Orphenadrine

Basics

Orphenadrine is a centrally acting muscle relaxant and belongs to the group of H1 antihistamines. It is used to treat painful skeletal muscle tension and Parkinson's disease.

Orphenadrine is available by prescription and is usually given in the form of tablets or liquid preparations for ingestion. In some cases, it is also administered intravenously. It is available either as a monopreparation or in combination with paracetamol or diclofenac.

Effect

Pharmacodynamics

Orphenadrine is a so-called anticholinergic with an effect on the central nervous system. On the peripheral nervous system, orphenadrine has very little effect. In addition, it shows properties of an antihistamine as well as those of a local anaesthetic.

The mechanism of action is primarily based on a blockade of glutamate receptors. Glutamate is a very important excitatory neurotransmitter in the human brain. When blocked by orphenadrine, muscles become less excited and relaxation occurs.

Pharmacokinetics

Orphenadrine is absorbed into the blood mainly through the gastrointestinal tract. Plasma protein binding is 95% and plasma half-life is between 13-20 hours. Degradation of the drug occurs entirely in the cells of the liver.

Drug Interactions

The agents amantadine, quinidine, MAO inhibitors, and some tricyclic antidepressants may potentiate the anticholinergic effect of Orphenadrine. Orphenadrine may potentiate the effects of L-dopa. There is a risk of hypothermia if chlorpromazine is taken concomitantly. The consumption of alcohol should be avoided while taking Orphenadrine.

Toxicity

Toxicological data

Oral, mouse LD50 = 100 mg/kg; oral, rat LD50 = 255 mg/kg

Chemical & physical properties

Formula C18H23NO·HCl
Molar Mass (g·mol−1) 305,84 g
Physical State solid
Melting Point (°C) < 25
Boiling Point (°C) 195
PKS Value 8,91
CAS Number 341-69-5
PUB Number 4601
Drugbank ID DB01173

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

The content of this page is an automated and high-quality translation from DeepL. You can find the original content in German here.

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