Biperiden

Source: Wikipedia, the free encyclopedia.
Biperiden
Clinical data
Trade namesAkineton
AHFS/Drugs.comMonograph
MedlinePlusa699058
License data
Pregnancy
category
  • AU: B2
Routes of
administration		By mouth, intramuscular injection (IM), intravenous therapy (IV)
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability33 ± 5% (by mouth)
Protein binding60%
MetabolismLiver hydroxylation
Elimination half-life18 to 24 hours
ExcretionKidney
Identifiers
  • (1RS,2SR,4RS)-1-(bicyclo[2.2.1]hept-5-en-2-yl)-1-phenyl-3-(piperidin- 1-yl)propan-1-ol
JSmol)
  • OC(c1ccccc1)(CCN2CCCCC2)C4C3\C=C/C(C3)C4
  • InChI=1S/C21H29NO/c23-21(19-7-3-1-4-8-19,11-14-22-12-5-2-6-13-22)20-16-17-9-10-18(20)15-17/h1,3-4,7-10,17-18,20,23H,2,5-6,11-16H2 checkY
  • Key:YSXKPIUOCJLQIE-UHFFFAOYSA-N checkY
  (verify)

Biperiden, sold under the brand name Akineton among others, is a medication used to treat

muscle.[2][3]

Common side effects include blurred vision, dry mouth, sleepiness, constipation, and confusion.[2] It should not be used in people with a bowel obstruction or glaucoma.[2] It is unclear if use in pregnancy or breastfeeding is safe.[4] Biperiden is in the anticholinergic family of medication.[2]

Biperiden was approved for medical use in the United States in 1959.[2] It is on the World Health Organization's List of Essential Medicines.[5] Biperiden is no longer marketed in the United States.[6][7][8]

Medical uses

Biperiden is used for the adjunctive treatment of all forms of

idiopathic, and arteriosclerotic Parkinson's) and for reduced sweating in methadone
users. It seems to exert better effects in the postencephalitic and idiopathic than in the arteriosclerotic type.

Biperiden is also commonly used to improve acute extrapyramidal side effects related to antipsychotic drug therapy, such as akathisia.

It relieves

abnormal gait, and to lesser extent, tremor
.

In its role as a synthetic acetylcholine antagonist, biperiden has been analyzed as an alternative anticonvulsant for usage in the treatment of intoxication by organophosphorus nerve agents, such as sarin.[11]

It was also suggested by IV route for neuroleptic malignant syndrome.[12]

Pregnancy and lactation

  • Pregnancy : In animal studies biperiden had no embryo- or fetotoxic effects. There is no sufficient clinical data on pregnant women. The drug should therefore be used cautiously during pregnancy.
  • Lactation : Biperiden is found in the milk of lactating women. No sufficient clinical data exists regarding effects for the newborns. Additionally, biperiden may decrease maternal milk production. It is therefore recommended that biperiden is not used during lactation.

Children

Children and adolescents aged 1 year and older may be treated. The clinical experience is mainly on the short-term treatment of acute drug induced dystonic reactions. Doses should be reduced according to the weight of the patients.[citation needed]

Contraindications

  • Hypersensitivity to biperiden
  • Narrow angle glaucoma
  • Ileus
  • Caution: People with obstructive diseases of the urogenital tract, people with a known history of seizures and those with potentially dangerous tachycardia

Side effects

Dose-dependent side effects are frequent. Particularly geriatric patients may react with confusional states or develop delirium.

Interactions

  • Other anticholinergic drugs (e.g. spasmolytics, antihistamines, TCAs) : Side effects of biperiden may be increased.
  • Quinidine : Increased anticholinergic action (particular on AV conduction).
  • Antipsychotics : Long-term use of biperiden may mask or increase the risk of tardive dyskinesia.
  • Pethidine (meperidine) : Central effects and side effects of pethidine may be increased.
  • Metoclopramide : Action of metoclopramide is decreased.
  • Alcohol : Risk of serious intoxication.

Overdose

Biperiden mimics an atropine intoxication with mydriasis, dryness of mucous membranes, red face, atonic states of bowels and bladder, and hyperthermia in high doses. Central consequences are agitation, confusion, and hallucinations. An untreated overdose may be fatal, particular in children. Premortal signs are respiratory depression and cardiac arrest. A specific antagonist is physostigmine which combines a peripheral and a central action. Carbachol can be used to treat atonic bowels and bladder. The vital functions should be monitored and stabilized. It may be necessary to treat hyperthermia with cooling blankets.

Pharmacokinetics

The oral

elimination half-life
has been determined as 18.4 hours, and may be prolonged in geriatric patients. After a 4 mg intravenous dose, the elimination half-life is approximately 24 hours.

Pharmacology

Biperiden has an

M1 receptors. Biperiden does also act as FIASMA (functional inhibitor of acid sphingomyelinase).[14]

History

Biperiden was synthesized by the German chemist W. Klavehn from Knoll AG, Germany. In March 1953 a patent was applied for in Germany[15] and subsequently in many other countries. A US patent application was filed in March 1954 and granted in April 1957.[16]

One website reported that it was not commercially available in the United States as of 2017.[17]

References

  1. ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
  2. ^ a b c d e f "Biperiden Hydrochloride". The American Society of Health-System Pharmacists. Archived from the original on 21 December 2016. Retrieved 8 December 2016.
  3. ^
    ISBN 9789241547659
    .
  4. ^ "Biperiden Use During Pregnancy | Drugs.com". www.drugs.com. Archived from the original on 21 December 2016. Retrieved 15 December 2016.
  5. hdl:10665/325771
    . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  6. ^ "Akineton (biperiden hydrochloride): FDA-Approved Drugs". U.S. Food and Drug Administration. Retrieved 2 July 2020.
  7. ^ "Akineton (biperiden lactate): FDA-Approved Drugs". U.S. Food and Drug Administration. Retrieved 2 July 2020.
  8. ^ "Akineton Tablets (biperiden hydrochloride)". DailyMed. Retrieved 2 July 2020.
  9. PMID 11481174. Archived from the original
    on 2012-09-21. Retrieved 2008-11-12.
  10. PMID 12562595
    .
  11. S2CID 13749842. Archived from the original
    on September 23, 2017.
  12. S2CID 2457321
    .
  13. PMID 8420174
    .
  14. PMID 21909365
    .
  15. ^ DE 1005067, Klavehn W, "Verfahren zur Herstellung von bicyclisch substituierten Aminopropanolen", issued 1957, assigned to Knoll AG. 
  16. ^ US 2789110, Klavehn W, "Amino alcohols substituted by bicycloalkyl residues and a process of making same", issued 1957, assigned to Knoll AG. 
  17. ^ "Biperiden". Davis's Drug Guide. Archived from the original on 10 September 2017. Retrieved 6 July 2017.
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