Orphenate

Orphenate Uses, Dosage, Side Effects, Food Interaction and all others data.

A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.

Orphenate is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculoskeletal conditions. Orphenate 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. Orphenate 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.

Trade Name Orphenate
Availability Prescription only
Generic Orphenadrine
Orphenadrine Other Names Orfenadrina, Orphenadrine, Orphenadrinum
Related Drugs cyclobenzaprine, tizanidine, diazepam, methocarbamol, Flexeril, Soma
Weight 100mg,
Type Oral Tablet, Extended Release, Injection
Formula C18H23NO
Weight Average: 269.3813
Monoisotopic: 269.177964363
Protein binding

95%

Groups Approved
Therapeutic Class
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Orphenate
Orphenate

Uses

Orphenate is a muscarinic antagonist used as an adjunct for the symptomatic relief of musculoskeletal pain and discomfort.

Indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculo skeletal conditions.

Orphenate is also used to associated treatment for these conditions: Back Pain Lower Back, Fever, Menstrual Distress (Dysmenorrhea), Mild pain, Muscle Spasms, Mild Musculoskeletal Disorder, Mild to moderate pain, Moderate Musculoskeletal Disorder, Moderate Pain

How Orphenate works

Orphenate binds and inhibits 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.

Toxicity

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

Food Interaction

  • Avoid alcohol.
  • Take with or without food. Food does not significantly affect absorption.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Orphenate Disease Interaction

Major: anticholinergic effects

Elimination Route

Orphenate is almost completely absorbed in the gastrointestinal tract.

Half Life

13-20 hours

Innovators Monograph

You find simplified version here Orphenate

*** Taking medicines without doctor's advice can cause long-term problems.
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