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a salt or ester of lactic acid

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/11/18 05:40:21」(JST)

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Biperiden is an antiparkinsonian agent^[1] of the anticholinergic type.^[2] The original brand name, which still exists and is manufactured by BASF/Knoll Pharma, is Akineton. Generics are available worldwide, one of them is Dekinet manufactured by Rafa Laboratories.

Uses

Biperiden is used for the adjunctive treatment of all forms of Parkinson's disease and for reduced sweating in methadone users (postencephalitic, idiopathic, and arteriosclerotic). It seems to exert better effects in the postencephalitic and idiopathic than in the arteriosclerotic type.

Biperiden is also commonly used to improve parkinsonian signs and symptoms related to antipsychotic drug therapy.

It relieves muscle rigidity, reduces abnormal sweating related with Clozapine and Methadone use^[3]^[4] and salivation, improves 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.^[5]

Contraindications and cautions

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

Special groups

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.

Pediatric patients

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

Side effects

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

CNS : Drowsiness, vertigo, headache, and dizziness are frequent. With high doses nervousness, agitation, anxiety, delirium, and confusion are noted. Biperiden may be abused due to a short acting mood-elevating and euphoriant effect. The normal sleep architecture may be altered (REM sleep depression). Biperiden may lower the seizure-threshold. Some instances of dementia have been noted to correlate with chronic administration of anticholinergic medications such as Biperiden for Parkinson's disease.^[6]
Peripheral side effects : Blurred vision, dry mouth, impaired sweating, abdominal discomfort, and obstipation are frequent. Tachycardia may be noted. Allergic skin reactions may occur. Parenteral use may cause orthostatic hypotension.
Eyes : Biperiden causes mydriasis with or without photophobia. It may precipitate narrow angle glaucoma.

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 bioavailability is only 33 +/- 5% due to extensive first-pass metabolism. In young, healthy volunteers, peak plasma concentrations following a single oral 4 mg immediate-release dose are reached after 1.5 hours. The 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 atropine-like blocking effect on all peripheral structures which are parasympathetic-innervated (e.g. cardiovascular and visceral organs). It also has a prominent central blocking effect on M1 receptors. Biperiden does also act as FIASMA (functional inhibitor of acid sphingomyelinase).^[7]

History

Biperiden was synthesized by the German chemist W. Klavehn from Knoll AG, Germany. In March 1953 a patent was applied for in Germany and subsequently in many other countries.

References

^ Jackisch R, Kruchen A, Sauermann W, Hertting G, Feuerstein TJ (October 1994). "The antiparkinsonian drugs budipine and biperiden are use-dependent (uncompetitive) NMDA receptor antagonists". Eur. J. Pharmacol. 264 (2): 207–11. doi:10.1016/0014-2999(94)00528-1. PMID 7851484.
^ Pehl C, Wendl B, Kaess H, Pfeiffer A (October 1998). "Effects of two anticholinergic drugs, trospium chloride and biperiden, on motility and evoked potentials of the oesophagus". Aliment. Pharmacol. Ther. 12 (10): 979–84. doi:10.1046/j.1365-2036.1998.00398.x. PMID 9798802.
^ Richardson C, Kelly DL, Conley RR (August 2001). "Biperiden for excessive sweating from clozapine". Am J Psychiatry 158 (8): 1329–30. doi:10.1176/appi.ajp.158.8.1329-a. PMID 11481174.
^ Caflisch C, Figner B, Eich D (February 2003). "Biperiden for excessive sweating from methadone". Am J Psychiatry 160 (2): 386–7. doi:10.1176/appi.ajp.160.2.386. PMID 12562595.
^ Shim, TM; McDonough JH (May 2000). "Efficacy of biperiden and atropine as anticonvulsant treatment for organophosphorus nerve agent intoxication". Archives of Toxicology 74 (3): 165–172. doi:10.1007/s002040050670. PMID 10877003.
^ Nishiyama K, Mizuno T, Sakuta M, Kurisaki H (1993). "Chronic dementia in Parkinson's disease treated by anticholinergic agents. Neuropsychological and neuroradiological examination.". Adv Neurol 60: 479–83. PMID 8420174.
^ Kornhuber J, Muehlbacher M, Trapp S, Pechmann S, Friedl A, Reichel M, Mühle C, Terfloth L, Groemer T, Spitzer G, Liedl K, Gulbins E, Tripal P (2011). "Identification of novel functional inhibitors of acid sphingomyelinase". PLoS ONE 6 (8): e23852. doi:10.1371/journal.pone.0023852. PMC 3166082. PMID 21909365.

UpToDate Contents

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English Journal

Cholinergic gating of hippocampal auditory evoked potentials in freely moving rats.

Klinkenberg I1, Sambeth A, Blokland A.
European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology.Eur Neuropsychopharmacol.2013 Aug;23(8):988-97. doi: 10.1016/j.euroneuro.2012.08.014. Epub 2012 Sep 10.
As perturbations in auditory filtering appear to be a candidate trait marker of schizophrenia, there has been considerable interest in the development of translational rat models to elucidate the underlying neural and neurochemical mechanisms involved in sensory gating. This is the first study to in
PMID 22974558

Midazolam-induced acute dystonia reversed by diazepam.

Komur M1, Arslankoylu AE, Okuyaz C.
Journal of anaesthesiology, clinical pharmacology.J Anaesthesiol Clin Pharmacol.2012 Jul;28(3):368-70. doi: 10.4103/0970-9185.98346.
Midazolam can induce acute dystonia in childhood. We report the development of acute dystonia in a 6-year-old girl after receiving midazolam as a sedative. Dystonic contractions persisted despite flumazenil and biperiden lactate injections and the patient was treated with diazepam. Acute dystonia wa
PMID 22869948

Gluteal abscess following intramuscular injection of dissolved biperiden tablets.

Ozucelik DN, Yucel N, Coskun S, Cobanoglu M, Kunt MM.
International journal of clinical practice.Int J Clin Pract.2007 Aug;61(8):1417-8.
PMID 17627718

Japanese Journal

抗精神病薬による薬剤性口顎ジストニアの1例

日本顎関節学会雑誌 26(1), 15-19, 2014
NAID 130004567847

「biperiden hydrochloride」

Systematic (IUPAC) name
	(1RS,2SR,4RS)-1-(bicyclo[2.2.1]hept-5-en-2-yl)-1-phenyl-3-(piperidin- 1-yl)propan-1-ol
Clinical data
AHFS/Drugs.com	monograph
MedlinePlus	a699058
Pregnancy cat.	AU: B2; US: C;
Legal status	US: ℞-only;
Routes	Oral, IM, IV
Pharmacokinetic data
Bioavailability	33 ± 5% (oral)
Protein binding	60%
Metabolism	Hepatic hydroxylation
Half-life	18 to 24 hours
Excretion	Renal
Identifiers
CAS number	514-65-8
ATC code	N04AA02
PubChem	CID 2381
DrugBank	DB00810
ChemSpider	2289
UNII	0FRP6G56LD
KEGG	D00779
ChEBI	CHEBI:3112
ChEMBL	CHEMBL1101
Chemical data
Formula	C21H29NO
Mol. mass	311.461 g/mol
	SMILES OC(c1ccccc1)(CCN2CCCCC2)C4C3\C=C/C(C3)C4;
	InChI 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 ; Key:YSXKPIUOCJLQIE-UHFFFAOYSA-N ;
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