Description
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.
Uses
Benzatropine is used to reduce extrapyramidal side effects of antipsychotic treatment. Benzatropine is also a second-line drug for the treatment of Parkinson's disease. It improves tremor, and may alleviate rigidity and bradykinesia.Benzatropine is also sometimes used for the treatment of dystonia, a rare disorder that causes abnormal muscle contraction, resulting in twisting postures of limbs, trunk, or face.
Side effects
These are principally anticholinergic:Dry mouth;Blurred vision;Cognitive changes;Drowsiness;Constipation;Urinary retention;Tachycardia;Anorexia;Severe delirium and hallucinations (in overdose).
Toxicity
The oral LD50 of benztropine is reported to be of 940 mg/kg in rats.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.
Definition
ChEBI: Tropane in which a hydrogen at position 3 is substituted by a diphenylmethoxy group (endo-isomer). An acetylcholine receptor antagonist, it is used (particularly as its methanesulphonate salt) in the treatment of Parkinson's disease, and to re
uce parkinsonism and akathisia side effects of antipsychotic treatments.
brand name
Cogentin (Merck).
Safety Profile
Poison by subcutaneous andintravenous routes. When heated to decomposition itemits toxic fumes of NOx.
in vivo
Benztropine (5 μM, 4 weeks) inhibits tumor-initiating potential in a 4T1 mouse model[1].
| Animal Model: | Balb/c mice bearing 4T1 breast tumors[1] |
| Dosage: | 1.5 mg/kg |
| Administration: | Injection; 3 weeks |
| Result: | Reduced the tumor size and weight significantly without body weight changing. |
