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Benzatropine | CAS No: 86-13-5 | GMP-certified suppliers
A medication that serves as adjunct therapy for all forms of parkinsonism and manages extrapyramidal symptoms caused by neuroleptic drugs.
Therapeutic categories
Primary indications
- Benztropine is indicated to be used as an adjunct in the therapy of all forms of parkinsonism
- It can also be used for the control of extrapyramidal disorders due to neuroleptic drugs
- The extrapyramidal symptoms are defined as drug-induced disorders that include symptoms of dystonia, akathisia, parkinsonism, bradykinesia, tremors, and dyskinesia
Product Snapshot
- Benzatropine is available as oral tablets and injectable solutions suited for both parenteral and oral administration
- It is primarily used as an adjunct therapy for parkinsonism and to manage extrapyramidal symptoms induced by neuroleptic drugs
- The product is approved for use in the US and Canadian markets
Clinical Overview
Pharmacodynamically, benztropine acts by selectively inhibiting dopamine reuptake transporters in the presynaptic nerve terminals, leading to a dose-dependent increase in synaptic dopamine concentrations. This dopaminergic effect typically manifests clinically within 1 to 2 hours following oral administration and within minutes after intramuscular injection, with an approximate duration of action of 24 hours. In addition to its dopaminergic activity, benztropine exhibits anticholinergic effects through high affinity antagonism at muscarinic M1 receptors predominantly located in the striatum, helping to restore the dopaminergic-cholinergic balance disrupted in Parkinson’s disease. The compound also has notable antihistaminic activity comparable to pyrilamine and shares structural and functional similarities with atropine.
The mechanism of action thus combines dopamine transporter inhibition with muscarinic and histamine receptor antagonism, contributing to symptom alleviation in Parkinsonian and drug-induced movement disorders. Clinically, benztropine is associated with a pronounced sedative effect, and safety considerations include the potential for anticholinergic-related adverse events such as dry mouth, blurred vision, urinary retention, and cognitive impairment, particularly in elderly patients. It is also classified among agents that can prolong the QT interval, necessitating caution in at-risk populations.
Benztropine was developed by USL Pharma and received FDA approval in 1996. Pharmacokinetic profiles indicate renal excretion as the main elimination pathway. As a cytochrome P450 CYP2D6 substrate, potential pharmacokinetic interactions should be considered during formulation and clinical use.
For API sourcing, quality control should ensure adherence to established pharmacopoeial standards regarding purity, enantiomeric composition, and residual solvents due to benztropine’s complex synthesis. Suppliers must provide documentation of compliance with relevant Good Manufacturing Practices (GMP), impurity profiles, and batch-to-batch consistency to meet global regulatory requirements.
Identification & chemistry
| Generic name | Benzatropine |
|---|---|
| Molecule type | Small molecule |
| CAS | 86-13-5 |
| UNII | 1NHL2J4X8K |
| DrugBank ID | DB00245 |
Pharmacology
| Summary | Benztropine acts primarily as a selective inhibitor of presynaptic dopamine transporters, increasing synaptic dopamine levels. It also exhibits antagonistic activity at muscarinic acetylcholine M1 receptors and histamine H1 receptors, contributing to correction of the dopaminergic-cholinergic imbalance in parkinsonism. These combined pharmacodynamic effects underpin its use as an adjunct treatment for parkinsonism and neuroleptic-induced extrapyramidal symptoms. |
|---|---|
| Mechanism of action | Benztropine is an agent with anti-muscarinic and antihistaminic effects. Its main mechanism of action is presented by the selective inhibition of dopamine transporters but it also presents affinity for histamine and muscarine receptors. It is widely known that benztropine is a potent inhibitor of presynaptic carrier-mediated dopamine transport. As well, it is known to be an analog of atropine and hence, it has a large affinity for muscarinic receptors M1 in the human brain. Once bound, benztropine blocks the activity of the muscarinic receptors mainly in the striatum. The increased advantage of benztropine lays on the antagonism of acetylcholine activity which corrects the imbalance between dopamine and acetylcholine in Parkinson patients. |
| Pharmacodynamics | The inhibition of dopamine reuptake by benztropine produces a dose-dependent increase of dopamine in the nerve terminal of the dopaminergic system. Clinically the activity of benztropine is observed after 1-2 hours of oral administration and after a few minutes of intramuscular administration with a last-longing effect of about 24 hours. Reports have indicated that benztropine has a very large sedative effect. The antihistaminic effect of benztropine is very similar to the effect found in [pyrilamine] and the anticholinergic activity was found to be equal to [atropine] _ex vivo_ and of about 50% activity _in vivo_. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Muscarinic acetylcholine receptor M1 | Humans | antagonist |
| Sodium-dependent dopamine transporter | Humans | inhibitor |
| Histamine H1 receptor | Humans | antagonist |
ADME / PK
| Absorption | Oral administration of 1.5 mg of benztropine is slowly absorbed in the gastrointestinal tract and it reaches a peak concentration of 2.5 ng/ml in about 7 hours. It has an approximate oral bioavailability of 29%. |
|---|---|
| Half-life | The elimination half-life of benztropine is very variable and it is reported to be of around 36 hours. |
| Protein binding | About 95% of the administered dose of benztropine is found bound to plasma proteins. |
| Metabolism | Benztropine has been shown to undergo metabolism mainly marked by N-oxidation, N-dealkylation and ring hydroxylation. The extensive metabolism of benztropine produces eight phase-I metabolites plus four glucuronide conjugates. |
| Route of elimination | Benztropine is mainly excreted in the urine but it is also found in the feces unchanged. |
| Volume of distribution | Benztropine is expected to present a large volume of distribution between 12-30 L/kg. |
| Clearance | Extensive pharmacodynamic or pharmacokinetic studies have not been performed. |
Formulation & handling
- Benzatropine is a small molecule API suitable for both oral and parenteral (intramuscular, intravenous) formulations.
- Low water solubility and high LogP indicate potential challenges in aqueous formulation and bioavailability enhancement.
- Administration with food is recommended to reduce gastrointestinal irritation; avoid co-administration with alcohol.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is approaching patent expiry in key markets including the US and Canada, indicating a transition towards increased generic competition and greater market maturity. This phase typically involves expanded availability and pricing adjustments. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The benzotropine manufacturing landscape comprises multiple originator and generic manufacturers with a diverse global footprint, including established companies producing branded and generic forms primarily in the US and Canadian markets. The presence of various branded products across these regions indicates sustained brand recognition, while the inclusion of numerous generic manufacturers suggests that patent expiry has allowed for existing generic competition. This dynamic supports a well-established supply chain with broad market participation. |
|---|
Safety
| Toxicity | The oral LD50 of benztropine is reported to be of 940 mg/kg in rats.[MSDS] In the presence of overdose with benztropine, it has been observed symptoms of circulatory collapse, cardiac arrest, respiratory depression, respiratory arrest, psychosis, shock, coma, seizure, ataxia, combativeness, anhidrosis, hyperthermia, fever, dysphagia, decreased bowel sounds and sluggish pupils. |
|---|
- Benztropine exhibits an oral LD50 of approximately 940 mg/kg in rats, indicating moderate acute toxicity
- Exposure to overdose conditions may result in severe central nervous system and cardiopulmonary effects, including respiratory depression, circulatory collapse, and seizures
- Handling requires precautions to prevent ingestion and limit exposure due to potential for neurotoxic and systemic adverse effects
Benzatropine is a type of Anticholinergics/Parasympathemimetics
Anticholinergics/Parasympathomimetics are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the medical field. These compounds exhibit specific pharmacological actions by targeting the cholinergic system in the body.
Anticholinergics are drugs that block the action of acetylcholine, a neurotransmitter that regulates various bodily functions. By inhibiting the activity of acetylcholine, anticholinergics can have diverse therapeutic effects, including reducing muscle spasms, decreasing gastrointestinal motility, and alleviating symptoms associated with certain respiratory conditions.
On the other hand, parasympathomimetics, also known as cholinomimetics, mimic the action of acetylcholine by stimulating cholinergic receptors. These compounds enhance the parasympathetic nervous system, which is responsible for the "rest and digest" functions of the body. Parasympathomimetics are commonly used to treat conditions such as glaucoma, urinary retention, and Alzheimer's disease.
The use of anticholinergics/parasympathomimetics requires careful consideration and medical supervision due to their potential side effects, which can include dry mouth, blurred vision, urinary retention, constipation, and cognitive impairment. These medications are available in various forms, including tablets, capsules, patches, and inhalers, and their dosage is determined by the specific medical condition being treated.
Overall, anticholinergics/parasympathomimetics play a vital role in modern medicine, providing targeted therapeutic effects by modulating the cholinergic system. Their usage has significantly improved patient outcomes in various medical conditions and continues to be an important category of pharmaceutical APIs.
Benzatropine (Anticholinergics/Parasympathemimetics), classified under Autonomic Nervous System Agents
Autonomic Nervous System Agents are a crucial category of pharmaceutical active ingredients (APIs) that target the autonomic nervous system (ANS). The ANS plays a vital role in regulating essential bodily functions such as heart rate, blood pressure, digestion, and respiratory rate. This category of pharmaceutical APIs encompasses a wide range of drugs designed to modulate the activity of the ANS.
One subcategory within Autonomic Nervous System Agents is the Sympathomimetic agents, which mimic the effects of the sympathetic nervous system. These drugs are often used to treat conditions such as asthma, nasal congestion, and hypotension by stimulating specific adrenergic receptors.
Conversely, Sympatholytic agents act to inhibit or block the sympathetic nervous system. They are employed to treat hypertension, anxiety, and certain cardiac conditions by reducing sympathetic activity.
Another subcategory is Parasympathomimetic agents, which mimic the effects of the parasympathetic nervous system. These drugs are commonly used to treat glaucoma, urinary retention, and certain gastrointestinal disorders by stimulating cholinergic receptors.
Parasympatholytic agents, on the other hand, act to block the parasympathetic nervous system. They find applications in the treatment of conditions such as overactive bladder and irritable bowel syndrome by inhibiting cholinergic receptors.
The Autonomic Nervous System Agents API category includes various drugs with distinct mechanisms of action that enable healthcare professionals to fine-tune the balance of the autonomic nervous system. By targeting specific receptors and pathways, these pharmaceutical APIs provide valuable therapeutic options for managing a wide range of medical conditions related to autonomic dysfunction.
Benzatropine API manufacturers & distributors
Compare qualified Benzatropine API suppliers worldwide. We currently have 7 companies offering Benzatropine API, with manufacturing taking place in 5 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 |
|---|---|---|---|---|---|
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Arch Pharmalabs | Producer | India | India | CoA, USDMF | 19 products |
| Cedarburg Pharma | Producer | United States | United States | CoA, USDMF | 12 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, FDA, GMP, MSDS, USDMF, WC | 170 products |
| Fine Chemicals | Producer | South Africa | South Africa | CoA, USDMF | 14 products |
| Harman Finochem | Producer | India | India | CoA, FDA, GMP, USDMF | 34 products |
| NAVINTA | Producer | United States | Unknown | CoA, USDMF | 15 products |
When sending a request, specify which Benzatropine 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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