Benzatropine

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Benztropine
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Benzatropine
Clinical data
Trade namesCogentin, others
Other namesbenzatropine (BAN UK), benztropine (USAN US)
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • AU: B2
Routes of
administration
By mouth, IM, IV
ATC code
Legal status
Legal status
Pharmacokinetic data
MetabolismLiver
Elimination half-life12–24 hours
ExcretionUrine
Identifiers
  • (3-endo)-3-(Diphenylmethoxy)-8-methyl-8-azabicyclo[3.2.1]octane
JSmol)
  • CN4[C@@H]1CC[C@H]4C[C@H](C1)OC(c2ccccc2)c3ccccc3
  • InChI=1S/C21H25NO/c1-22-18-12-13-19(22)15-20(14-18)23-21(16-8-4-2-5-9-16)17-10-6-3-7-11-17/h2-11,18-21H,12-15H2,1H3/t18-,19+,20+ checkY
  • Key:GIJXKZJWITVLHI-PMOLBWCYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Benzatropine (

muscle.[3] Benefits are seen within two hours and last for up to ten hours.[4][5]

Common side effects include dry mouth, blurry vision, nausea, and constipation.

Benzatropine was approved for medical use in the United States in 1954.

generic medication.[3] In 2020, it was the 229th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[7][8] It is sold under the brand name Cogentin among others.[3]

Medical uses

Benzatropine is used to reduce

bradykinesia.[9] 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.

Adverse effects

These are principally anticholinergic:

While some studies suggest that use of anticholinergics increases the risk of tardive dyskinesia (a long-term side effect of antipsychotics),[10][11] other studies have found no association between anticholinergic exposure and risk of developing tardive dyskinesia,[12] although symptoms may be worsened.[13]

Drugs that decrease cholinergic transmission may impair storage of new information into long-term memory. Anticholinergic agents can also impair time perception.[14]

Pharmacology

Benzatropine is a centrally acting anticholinergic/antihistamine agent. It is a selective M1 muscarinic acetylcholine receptor antagonist. Benzatropine partially blocks cholinergic activity in the basal ganglia and has also been shown to increase the availability of dopamine by blocking its reuptake and storage in central sites, and as a result, increasing dopaminergic activity. Animal studies have indicated that anticholinergic activity of benzatropine is approximately one-half that of atropine, while its antihistamine activity approaches that of mepyramine. Its anticholinergic effects have been established as therapeutically significant in the management of Parkinsonism. Benzatropine antagonizes the effect of acetylcholine, decreasing the imbalance between the neurotransmitters acetylcholine and dopamine, which may improve the symptoms of early Parkinson's disease.[15]

Benzatropine analogues are atypical

dopamine reuptake inhibitors,[16] which might make them useful for people with akathisia secondary to antipsychotic therapy.[17]

Benzatropine also acts as a functional inhibitor of acid sphingomyelinase (FIASMA).[18]

Benzatropine has been also identified, by a high throughput screening approach, as a potent differentiating agent for

muscarinic receptors. In preclinical models for multiple sclerosis, benzatropine decreased clinical symptoms and enhanced re-myelination.[19]

Other animals

In veterinary medicine, benzatropine is used to treat priapism in stallions.[20]

Naming

Since 1959, benzatropine is the official

Latin (all medications are assigned a Latin name by WHO).[2]

"Benztropine" is the official United States Adopted Name (USAN), the medication naming system coordinated by the USAN Council, co-sponsored by the American Medical Association (AMA), the United States Pharmacopeial Convention (USP), and the American Pharmacists Association (APhA). It is also the Japanese Accepted Name (JAN)[22] and was used in Australia until 2015, when it was harmonized with the INN.[21]

Both names may be modified to account for the

methanesulfonate salt as which the medication is formulated: the modified INN (INNm) and BAN (BANM) is benzatropine mesilate, while the modified USAN is benztropine mesylate.[23] The modified JAN is a hybrid form, benztropine mesilate.[22]

The misspelling benzotropine is also occasionally seen in the literature.

See also

References

  1. ^ a b World Health Organization (December 1959). "International Non-Proprietary Names for Pharmaceutical Preparations). Recommended International Non-Proprietary Names (Rec. I.N.N.): List 3º" (PDF). WHO Chronicle. 13 (12): 464. Retrieved 2020-12-01.
  2. ^ a b c World Health Organization. "INN: Benzatropine". WHO MedNet. Retrieved 2020-12-01.[permanent dead link]
  3. ^ a b c d e f g h i "Benztropine Mesylate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 9 April 2019.
  4. .
  5. .
  6. ^ "Benztropine (Cogentin) Use During Pregnancy". Drugs.com. Retrieved 9 April 2019.
  7. ^ "The Top 300 of 2020". ClinCalc. Retrieved 7 October 2022.
  8. ^ "Benztropine - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.
  9. PMID 5066
    .
  10. .
  11. .
  12. .
  13. .
  14. .
  15. ^ MIMS Australia Pty Ltd. MIMS.
  16. PMID 24194527
    .
  17. .
  18. .
  19. .
  20. .
  21. ^ a b "Updating medicine ingredient names - list of affected ingredients". Therapeutic Goods Administration. 2015-11-23. Retrieved 2020-12-01.
  22. ^ a b Compound D00778 at KEGG Pathway Database.
  23. .

External links

  • "Benzatropine". Drug Information Portal. U.S. National Library of Medicine.