PMS Benztropine

PMS Benztropine 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 PMS Benztropine
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
PMS Benztropine
PMS Benztropine

Uses

PMS Benztropine 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.

PMS Benztropine is also used to associated treatment for these conditions: Extrapyramidal disorder caused by neuroleptic drugs, Parkinsonism, Tardive Dyskinesia caused by neuroleptic drugs

How PMS Benztropine 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.

Innovators Monograph

You find simplified version here PMS Benztropine

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0002448
http://classyfire.wishartlab.com/tax_nodes/C0002279
http://classyfire.wishartlab.com/tax_nodes/C0000369
http://classyfire.wishartlab.com/tax_nodes/C0000369
http://classyfire.wishartlab.com/tax_nodes/C0000492
http://classyfire.wishartlab.com/tax_nodes/C0002542
http://classyfire.wishartlab.com/tax_nodes/C0000195
http://classyfire.wishartlab.com/tax_nodes/C0003449
http://classyfire.wishartlab.com/tax_nodes/C0002239
http://classyfire.wishartlab.com/tax_nodes/C0001167
http://classyfire.wishartlab.com/tax_nodes/C0004139
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0004150
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:3048
http://www.hmdb.ca/metabolites/HMDB0014390
http://www.genome.jp/dbget-bin/www_bget?drug:D07511
http://www.genome.jp/dbget-bin/www_bget?cpd:C06846
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=1201549
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505349
https://www.chemspider.com/Chemical-Structure.16736541.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50366775
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=1424
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=3048
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1201203
https://zinc.docking.org/substances/ZINC000100036536
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP001460
http://www.pharmgkb.org/drug/PA448591
https://www.ebi.ac.uk/pdbe-srv/pdbechem/chemicalCompound/show/CXQ
http://www.rxlist.com/cgi/generic2/benztrop.htm
https://www.drugs.com/cdi/benztropine.html
https://en.wikipedia.org/wiki/Benzatropine
*** Taking medicines without doctor's advice can cause long-term problems.
Share