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 |
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 Drug Interaction
Moderate: diphenhydramine, diphenhydramine, duloxetine, duloxetine, pregabalin, pregabalin, alprazolam, alprazolam, cetirizine, cetirizineUnknown: celecoxib, celecoxib, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Orphenate Disease Interaction
Elimination Route
Orphenate is almost completely absorbed in the gastrointestinal tract.
Half Life
13-20 hours
Innovators Monograph
You find simplified version here Orphenate
