塩酸ビペリデン

関: biperiden、biperiden lactate

WordNet

a complex consisting of an organic base in association with hydrogen chloride

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/11/16 00:01:56」(JST)

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Biperiden, sold under the brandname Akineton among others, is a medication used to treat Parkinson disease.^[1] It is of the anticholinergic type.^[2] It is on the WHO Model List of Essential Medicines, the most important medications needed in a basic health system.^[3] It is available as a generic medication.

Medical 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, such as akathisia.

It relieves muscle rigidity, reduces abnormal sweating related with clozapine and methadone use^[4]^[5] 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.^[6]

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 shortterm treatment of acute drug induced dystonic reactions. Doses should be reduced according to the weight of the patients.

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.

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.^[7]
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).^[8]

History

Biperiden was synthesized by the German chemist W. Klavehn from Knoll AG, Germany. In March 1953 a patent was applied for in Germany^[9] and subsequently in many other countries. A US patent application was filed in March 1954 and granted in April 1957.^[10]

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.
^ "19th WHO Model List of Essential Medicines (April 2015)" (PDF). WHO. April 2015. Retrieved May 10, 2015.
^ 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.
^ Espacenet - Bibliographic data
^ United States Patent: 2789110^{[permanent dead link]}

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 統合失調症に対するクロザピン投与のガイドライン guidelines for prescribing clozapine in schizophrenia
2. 薬物乱用頭痛：治療および予後 medication overuse headache treatment and prognosis
3. パーキンソン病の薬理学的治療 pharmacologic treatment of parkinson disease
4. 第一世代（定型）抗精神病剤中毒 first generation typical antipsychotic medication poisoning
5. 反社会性人格障害の治療 treatment of antisocial personality disorder

English Journal

Do traditional anti-seizure drugs have a future? A review of potential anti-seizure drugs in clinical development.

Zaccara G1, Schmidt D2.
Pharmacological research.Pharmacol Res.2016 Feb;104:38-48. doi: 10.1016/j.phrs.2015.12.011. Epub 2015 Dec 12.
Currently information is available for 20 potential anti-seizure drugs in clinical development. They include candidates with mechanisms of action similar to those of marketed AEDs (allopregnanolone, brivaracetam, ganaxolone, ICA-105665, NS1209, selurampanel); those with new mechanisms of action (bep
PMID 26689774

The Controversial Case of Biperiden: From Prescription Drug to Drug of Abuse.

Affaticati A1, Gerra ML, Amerio A, Inglese M, Antonioni MC, Marchesi C.
Journal of clinical psychopharmacology.J Clin Psychopharmacol.2015 Dec;35(6):749-50. doi: 10.1097/JCP.0000000000000421.
PMID 26479221

Acute dystonic reaction due to dexketoprofen trometamol.

Kayipmaz AE1, Giray TA1, Tasci SS1, Tasci SS1, Kavalci C1, Kocalar UG1.
JPMA. The Journal of the Pakistan Medical Association.J Pak Med Assoc.2015 Nov;65(11):1231-2.
Dexketoprofentrometamol (DKP), is a tromethamine salt of the water-soluble S-enantiomer of ketoprofen. As with all other non-steroidal anti-inflammatory agents, the most common side effect of DKP is gastric complications. In this paper, we report a case of dystonic reaction after intravenous DKP use
PMID 26564300

Japanese Journal

院内製剤の品質確保に関する研究(第5報)院内製剤0.2%塩酸ビペリデン液に関する検討

植田敦子,上村慎子,栗田浩幸 [他]
静岡県環境衛生科学研究所報告 (47), 31-35, 2004
NAID 40007129469

Pharmacokinetic and Pharmacodynamic Interactions among Haloperidol, Carteolol Hydrochloride and Biperiden Hydrochloride

ISAWA Shinano,MURASAKI Mitsukuni,MIURA Sadanori,YOSHIOKA Masaya,UCHIUMI Mitsutomo,KUMAGAI Yuji,AOKI Shigeru,HISAZUMI Hidefumi,KUDO Shoji
日本神経精神薬理学雑誌 = Japanese journal of psychopharmacology 19(3), 111-118, 1999-06-25
NAID 10017038926

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★リンクテーブル★

リンク元	「ビペリデン」「biperiden lactate」
関連記事	「hydrochloride」

「ビペリデン」

Biperiden
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; category	AU: B2; US: C (Risk not ruled out); ;
Routes of; administration	Oral, IM, IV
Legal status
Legal status	US: ℞-only;
Pharmacokinetic data
Bioavailability	33 ± 5% (oral)
Protein binding	60%
Metabolism	Hepatic hydroxylation
Biological half-life	18 to 24 hours
Excretion	Renal
Identifiers
CAS Number	514-65-8
ATC code	N04AA02 (WHO)
PubChem	CID 2381
IUPHAR/BPS	7128
DrugBank	DB00810
ChemSpider	2289
UNII	0FRP6G56LD
KEGG	D00779
ChEBI	CHEBI:3112
ChEMBL	CHEMBL1101
Chemical data
Formula	C21H29NO
Molar mass	311.461 g/mol
3D model (Jmol)	Interactive image
	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 ;
(verify)

　　[★]

英: biperiden
化: 塩酸ビペリデン biperiden hydrochloride
商: アキネトン、アキリデン、タスモリン、ビカモール
関: トリヘキシフェニジル、プロサイクリディン

三級アミン
抗コリン作用薬
血液脳関門を通過する
パーキンソン病治療薬

ドパミン系機能とアセチルコリン系機能とを平衡させる

軽症のもので、特に振戦に効く

副作用 (SPC.191)

視力障害、口渇、尿閉、便秘、混乱、せん妄

「biperiden lactate」

　　[★]

乳酸ビペリデン

関: biperiden、biperiden hydrochloride

「hydrochloride」

　　[★] 塩酸塩、ハイドロクロライド　

[pmid7851484-1] 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.

[pmid9798802-2] 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.

[WHO2015E-3] "19th WHO Model List of Essential Medicines (April 2015)" (PDF). WHO. April 2015. Retrieved May 10, 2015.

[pmid11481174-4] 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.

[pmid12562595-5] 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.

[6] 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.

[7] 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.

[pmid18504571-8] 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.

[9] Espacenet - Bibliographic data

[10] United States Patent: 2789110^{[permanent dead link]}

匿名

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案内

案内

biperiden hydrochloride