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)
| Systematic (IUPAC) name | |
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(1RS,2SR,4RS)-1-(bicyclo[2.2.1]hept-5-en-2-yl)-1-phenyl-3-(piperidin- 1-yl)propan-1-ol
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| Clinical data | |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a699058 |
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| Routes of administration |
Oral, IM, IV |
| Legal status | |
| Legal status |
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| 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 Y |
| ATC code | N04AA02 (WHO) |
| PubChem | CID 2381 |
| IUPHAR/BPS | 7128 |
| DrugBank | DB00810 Y |
| ChemSpider | 2289 Y |
| UNII | 0FRP6G56LD Y |
| KEGG | D00779 Y |
| ChEBI | CHEBI:3112 Y |
| ChEMBL | CHEMBL1101 Y |
| Chemical data | |
| Formula | C21H29NO |
| Molar mass | 311.461 g/mol |
| 3D model (Jmol) | Interactive image |
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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.
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]
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.
Dose-dependent side effects are frequent. Particularly geriatric patients may react with confusional states or develop delirium.
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.
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.
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]
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]
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| リンク元 | 「ビペリデン」「biperiden lactate」 |
| 関連記事 | 「hydrochloride」 |