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Benzatropine

Generic Name
Benzatropine
Brand Names
Cogentin
Drug Type
Small Molecule
Chemical Formula
C21H25NO
CAS Number
86-13-5
Unique Ingredient Identifier
1NHL2J4X8K
Background

Benztropine, with the chemical formula 3alpha-diphenylmethoxytropane, is a tropane-based dopamine inhibitor used for the symptomatic treatment of Parkinson's disease. It is a combination molecule between a tropane ring, similar to cocaine, and a diphenyl ether from the dialkylpiperazines determined to be a dopamine uptake inhibitor since 1970. The generation of structure-activity relationships proved that benztropine derivatives with the presence of a chlorine substituent in the para position in one of the phenyl rings produces an increased potency for dopamine uptake inhibition as well as a decreased inhibition of serotonin and norepinephrine. Benztropine was developed by USL Pharma and officially approved by the FDA on 1996.

Indication

用于治疗帕金森病。也用于药物引起的锥体外系疾患,口服1小时起效,肌肉或静脉注射数分钟内起效,作用持续24小时。具有抗胆碱及抗组胺作用,并有轻度局部麻醉作用。

Associated Conditions
Parkinsonism

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• The FDA has approved Amneal Pharmaceuticals' Brekiya, the first and only dihydroergotamine (DHE) autoinjector for acute treatment of migraine and cluster headaches in adults. • Brekiya provides patients with the same medication used in hospitals and emergency rooms in a convenient, self-administered form that requires no refrigeration, assembly, or priming. • The approval addresses significant unmet needs, as headache is the fourth most common reason for ER visits, affecting approximately 39 million Americans with migraine and up to 1 million with cluster headache.

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• The FDA approved KarXT (Cobenfy) on September 26, 2024, marking the first new mechanism of action for schizophrenia treatment since 1954. • KarXT combines xanomeline and trospium to modulate brain circuits via muscarinic cholinergic receptors, offering a nondopaminergic approach to managing schizophrenia symptoms. • Clinical trials (EMERGENT-1, -2, -3, -4, -5) demonstrated significant improvements in PANSS scores and supported the long-term safety and efficacy of KarXT. • Cobenfy's unique mechanism and adverse event profile necessitate prescriber education to optimize its use as a novel treatment option for schizophrenia.

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FDA Approves Cobenfy, a Novel Schizophrenia Treatment Targeting Cholinergic Receptors

• The FDA has approved Cobenfy (xanomeline and trospium chloride) as the first new class of drug for schizophrenia in over 30 years, offering a novel approach to treatment. • Cobenfy targets muscarinic receptors, unlike traditional antipsychotics that focus on dopamine, potentially reducing side effects like weight gain and movement disorders. • Clinical trials demonstrated Cobenfy significantly reduced schizophrenia symptoms compared to placebo, marking a transformative moment in managing this challenging condition. • Expected to launch in late October, Cobenfy offers a new option for adults with schizophrenia, with ongoing studies exploring its potential in Alzheimer's psychosis and other conditions.
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