Benzatropina
Benzatropina Uses, Dosage, Side Effects, Food Interaction and all others data.
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.
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.
| Trade Name | Benzatropina |
| Generic | Benzatropine |
| Benzatropine Other Names | Benzatropina, Benzatropine, Benzatropinum, Benztropine, Tropine benzohydryl ether |
| Type | |
| Formula | C21H25NO |
| Weight | Average: 307.4293 Monoisotopic: 307.193614427 |
| Protein binding | About 95% of the administered dose of benztropine is found bound to plasma proteins. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Benzatropina is an anticholinergic drug used to treat Parkinson's disease (PD) and extrapyramidal symptoms, except tardive dyskinesia.
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.
Parkinsonism is a general term that refers to the group of neurological disorders that produce symptoms similar to Parkinson's disease such as tremors, slow movement, and stiffness. The parkinsonism includes a large number of disorders and some of them have not been clearly defined.
Benzatropina is also used to associated treatment for these conditions: Extrapyramidal disorder caused by neuroleptic drugs, Parkinsonism, Tardive Dyskinesia caused by neuroleptic drugs
How Benzatropina works
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.
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.
Food Interaction
- Avoid alcohol.
- Take with food. Food reduces irritation.
Volume of Distribution
Benztropine is expected to present a large volume of distribution between 12-30 L/kg.
Elimination Route
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.
Clearance
Extensive pharmacodynamic or pharmacokinetic studies have not been performed.
Elimination Route
Benztropine is mainly excreted in the urine but it is also found in the feces unchanged.
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