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Orphenadrine | CAS No: 83-98-7 | GMP-certified suppliers
A medication that provides adjunctive relief for acute musculoskeletal pain and manages rigidity and tremor in drug-induced parkinsonism through central muscle relaxation and anticholinergic effects.
Therapeutic categories
Primary indications
- Indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculo skeletal conditions
Product Snapshot
- Orphenadrine is available in multiple formulations including oral tablets (immediate, extended, delayed release, coated, film coated, multilayer), capsules, solutions, and injectable forms suitable for intramuscular, intravenous, and parenteral administration
- It is primarily indicated for adjunctive use in the relief of discomfort associated with acute painful musculoskeletal conditions
- Orphenadrine is approved for use in regulatory markets including the United States and Canada
Clinical Overview
Pharmacodynamically, orphenadrine exerts predominantly central anticholinergic effects with relatively weak peripheral activity. Its therapeutic impact arises from restoring the balance between cholinergic and dopaminergic neurotransmission in the basal ganglia, which is disrupted in Parkinson’s disease and related syndromes due to dopamine deficiency. It also possesses mild antihistaminic and local anesthetic properties that may contribute to its symptomatic effects. The medication additionally inhibits histamine H1 receptors and N-methyl-D-aspartate (NMDA) receptors, which may influence motor manifestations and provide relief from neuroleptic-induced hyperkinesia.
The mechanism of action involves antagonism of muscarinic receptors, counteracting excessive cholinergic stimulation resulting from striatal dopamine depletion. This action reduces muscle rigidity and tremor and may mediate a relaxing effect on skeletal muscle spasms. The drug’s mood-elevating properties have been noted, though these are not fully characterized.
Key pharmacokinetic parameters include metabolism mediated by cytochrome P450 enzymes, notably CYP1A2, CYP2B6, CYP2D6, CYP2E1, and CYP3A4, with orphenadrine acting as an inhibitor and substrate across several of these isoforms. This enzymatic involvement underscores the potential for drug-drug interactions and necessitates careful consideration during polypharmacy.
Safety considerations involve monitoring for anticholinergic side effects such as tachycardia, dry mouth, blurred vision, and confusion, particularly in elderly or vulnerable populations. Orphenadrine is listed among potential QTc-prolonging agents, indicating the requirement for caution in patients at risk of cardiac arrhythmias.
From a formulation and sourcing perspective, quality assurance should focus on verifying the chemical purity consistent with diphenylmethane derivatives and ensuring compliance with pharmacopeial standards. Given its metabolic profile, stability and impurity profiles must be rigorously controlled to maintain safety and efficacy in finished dosage forms.
Identification & chemistry
| Generic name | Orphenadrine |
|---|---|
| Molecule type | Small molecule |
| CAS | 83-98-7 |
| UNII | AL805O9OG9 |
| DrugBank ID | DB01173 |
Pharmacology
| Summary | Orphenadrine acts primarily as an antagonist of histamine H1 and NMDA receptors, with additional anticholinergic activity that modulates central cholinergic-dopaminergic balance. It is used to alleviate motor disturbances related to dopamine deficiency and to reduce skeletal muscle spasms in acute musculoskeletal conditions. The drug's pharmacodynamic profile includes central anticholinergic, mild antihistaminic, and local anesthetic effects. |
|---|---|
| Mechanism of action | Orphenadrine 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. |
| Pharmacodynamics | Orphenadrine is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculoskeletal conditions. Orphenadrine 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. Orphenadrine 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. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Glutamate receptor ionotropic, NMDA 2D | Humans | antagonist |
| Glutamate receptor ionotropic, NMDA 1 | Humans | antagonist |
| Glutamate receptor ionotropic, NMDA 3B | Humans | antagonist |
ADME / PK
| Absorption | Orphenadrine is almost completely absorbed in the gastrointestinal tract. |
|---|---|
| Half-life | 13-20 hours |
| Protein binding | 95% |
| Metabolism | Biotransformation occurs mainly in the liver. Pharmacologically active metabolites are N-demethyl orphenadrine and N,N-didemethyl orphenadrine. |
Formulation & handling
- Orphenadrine is a small molecule suitable for both oral and parenteral (intramuscular and intravenous) administration.
- The compound exhibits low water solubility and moderate lipophilicity (LogP 4.17), necessitating formulation strategies to enhance bioavailability for oral or injectable forms.
- Food intake does not significantly affect absorption, but alcohol should be avoided during use.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is currently off-patent in both the US and Canada, with generic versions available in these markets. The product is in a mature phase of its lifecycle, characterized by established competition and stabilized demand. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Orphenadrine includes numerous packagers, primarily serving the US and Canadian markets, indicating a broad base of generic manufacturers. The presence of several originator or branded products, such as Norflex and Disipal, shows established branded formulations mainly in North America. Patent expirations have led to wide generic availability, suggesting existing generic competition rather than imminent entry. |
|---|
Safety
| Toxicity | Oral, mouse LD<sub>50</sub> = 100 mg/kg; oral, rat LD<sub>50</sub> = 255 mg/kg |
|---|
- Handle with appropriate personal protective equipment to avoid ingestion and minimize exposure, due to low oral LD50 values in rodent studies
- Avoid inhalation or skin contact as the compound may pose systemic toxicity risks at low doses
- Use in well-ventilated areas and follow established industrial hygiene practices to prevent accidental exposure
Orphenadrine is a type of Muscle relaxants
Muscle relaxants are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) commonly used to alleviate muscle spasms and promote muscle relaxation. These medications act on the central nervous system (CNS) or directly on muscle fibers to reduce muscle tone and tension.
Muscle relaxants can be classified into two main groups: spasmolytics and neuromuscular blockers. Spasmolytics primarily target the CNS to inhibit the transmission of nerve signals, thus reducing muscle spasms. They are often prescribed for conditions such as back pain, muscle strains, and spasms caused by neurological disorders.
Neuromuscular blockers, on the other hand, act at the neuromuscular junction to prevent the transmission of nerve impulses, resulting in temporary paralysis of skeletal muscles. These medications are primarily used during surgical procedures to induce muscle relaxation and facilitate intubation.
Commonly prescribed muscle relaxants include benzodiazepines, such as diazepam and lorazepam, which have sedative properties and can provide relief from muscle spasms. Another class of muscle relaxants is the centrally acting skeletal muscle relaxants, including carisoprodol and cyclobenzaprine, which work by affecting neurotransmitters in the CNS.
It is important to note that muscle relaxants can cause side effects such as drowsiness, dizziness, and impaired coordination. They should only be used under the guidance of a healthcare professional, and the dosage and duration of treatment should be strictly followed to avoid dependence or other complications.
In conclusion, muscle relaxants are pharmaceutical APIs used to alleviate muscle spasms and promote muscle relaxation. They are available in different forms and can target the CNS or directly act on muscle fibers. It is crucial to consult a healthcare professional for proper diagnosis, prescription, and monitoring when using muscle relaxants.
Orphenadrine (Muscle relaxants), classified under Skeletal muscle relaxants
Skeletal muscle relaxants are a category of pharmaceutical active pharmaceutical ingredients (APIs) that are commonly used in the treatment of musculoskeletal conditions characterized by muscle spasms, stiffness, or tension. These medications work by targeting the central nervous system to reduce muscle activity and promote relaxation.
Skeletal muscle relaxants act on various receptors in the central nervous system, such as gamma-aminobutyric acid (GABA) receptors, to inhibit the transmission of nerve impulses and decrease muscle tone. This results in a reduction in muscle spasms, pain relief, and improved mobility.
There are different classes of skeletal muscle relaxants, including benzodiazepines, antispasmodics, and centrally acting muscle relaxants. Benzodiazepines, such as diazepam and lorazepam, exert their muscle relaxant effects by enhancing the activity of GABA receptors. Antispasmodics like cyclobenzaprine work by inhibiting the release of certain neurotransmitters involved in muscle contractions. Centrally acting muscle relaxants, such as baclofen and tizanidine, directly target the spinal cord to reduce muscle hyperactivity.
Skeletal muscle relaxants are commonly prescribed for conditions like muscle spasms, back pain, fibromyalgia, and multiple sclerosis. However, they are typically used for short-term treatment due to their potential side effects, including drowsiness, dizziness, and sedation.
It is important to note that skeletal muscle relaxants should only be used under the supervision and prescription of a qualified healthcare professional. Proper dosage and duration of treatment should be determined based on the patient's condition and medical history to ensure safe and effective use of these medications.
Orphenadrine API manufacturers & distributors
Compare qualified Orphenadrine API suppliers worldwide. We currently have 2 companies offering Orphenadrine API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Albemarle | Producer | United States | United States | CoA, USDMF | 17 products |
| Procos | Producer | Italy | Italy | CoA, USDMF | 22 products |
When sending a request, specify which Orphenadrine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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