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| '''Biperiden''' is an ] agent<ref name="pmid7851484">{{cite journal |author=Jackisch R, Kruchen A, Sauermann W, Hertting G, Feuerstein TJ |title=The antiparkinsonian drugs budipine and biperiden are use-dependent (uncompetitive) NMDA receptor antagonists |journal=Eur. J. Pharmacol. |volume=264 |issue=2 |pages=207–11 |year=1994 |month=October |pmid=7851484 |doi= |url=http://linkinghub.elsevier.com/retrieve/pii/0014-2999(94)00528-1}}</ref> of the ] type.<ref name="pmid9798802">{{cite journal |author=Pehl C, Wendl B, Kaess H, Pfeiffer A |title=Effects of two anticholinergic drugs, trospium chloride and biperiden, on motility and evoked potentials of the oesophagus | |
'''Biperiden''' is an ] agent<ref name="pmid7851484">{{cite journal |author=Jackisch R, Kruchen A, Sauermann W, Hertting G, Feuerstein TJ |title=The antiparkinsonian drugs budipine and biperiden are use-dependent (uncompetitive) NMDA receptor antagonists |journal=Eur. J. Pharmacol. |volume=264 |issue=2 |pages=207–11 |year=1994 |month=October |pmid=7851484 |doi= 10.1016/0014-2999(94)00528-1|url=http://linkinghub.elsevier.com/retrieve/pii/0014-2999(94)00528-1}}</ref> of the ] type.<ref name="pmid9798802">{{cite journal |author=Pehl C, Wendl B, Kaess H, Pfeiffer A |title=Effects of two anticholinergic drugs, trospium chloride and biperiden, on motility and evoked potentials of the oesophagus | | ||
| ==Pharmacokinetics== | |||
| The oral ] is only 33 +/- 5% due to extensive ]. In young, healthy volunteers peak plasma concentrations following an oral single dose of 4mg in immediate release form are reached after 1.5 hours. The ] has been determined as 18.4 hours, and may be prolonged in geriatric patients. After ] dosing of 4mg the elimination half-life is approximately 24 hours. | |||
| ==Pharmacology== | |||
| Biperiden has an ]-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 ]s. | |||
| ==Uses== | |||
| Biperiden is used for the adjunctive treatment of all forms of ] (postencephalitic, ], 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 ] drug therapy. | |||
| It relieves ], reduces ]<ref name="pmid11481174">{{cite journal |author=Richardson C, Kelly DL, Conley RR |title=Biperiden for excessive sweating from clozapine |journal=Am J Psychiatry |volume=158 |issue=8 |pages=1329–30 |year=2001 |month=August |pmid=11481174 |doi= |url=http://ajp.psychiatryonline.org/cgi/pmidlookup?view=long&pmid=11481174}}</ref><ref name="pmid12562595">{{cite journal |author=Caflisch C, Figner B, Eich D |title=Biperiden for excessive sweating from methadone |journal=Am J Psychiatry |volume=160 |issue=2 |pages=386–7 |year=2003 |month=February |pmid=12562595 |doi= |url=http://ajp.psychiatryonline.org/cgi/pmidlookup?view=long&pmid=12562595}}</ref> and ], improves ], and to lesser extent, ]. | |||
| ==Contraindications and cautions== | |||
| * Hypersensitivity to biperiden | |||
| * Narrow angle ] | |||
| * ] | |||
| * Caution : Patients with obstructive diseases of the urogenital tract, patients with a known history of seizures and those with potentially dangerous ] | |||
| * It can cause an acute organic psychosyndrome if used in about twice above prescribed dose.{{Fact|date=November 2008}} Due to that, many drug addicts make use of it as a one-time substitute for drugs of abuse.{{Who|date=November 2008}} | |||
| ==Special patient 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 ]s are frequent. Particularly geriatric patients may react with confusional states or develop ]. | |||
| * CNS : ], ], ], and ] are frequent. With high doses nervousness, agitation, ], 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 (] depression). Biperiden may lower the seizure-threshold. Some instances of dementia have been noted to correllate with chronic administration of ] medications such as Biperiden for ].<ref>{{cite journal | author = Nishiyama K, Mizuno T, Sakuta M, Kurisaki H | title = Chronic dementia in Parkinson's disease treated by anticholinergic agents. Neuropsychological and neuroradiological examination. | journal = Adv Neurol | volume = 60 | issue = | pages = 479–83 | year = 1993 | pmid = 8420174}}</ref> | |||
| * 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 ] with or without ]. It may precipitate narrow angle glaucoma. | |||
| ==Interactions== | |||
| * Other anticholinergic drugs (e.g. spasmolytics, ]s, TCAs) : Side effects of biperiden may be increased. | |||
| * ] : Increased anticholinergic action (particular on AV conduction). | |||
| * Antipsychotics : Long term use of biperiden may mask or increase the risk of ]. | |||
| * ] (meperidine) : Central effects and side effects of pethidine may be increased. | |||
| * ] : Action of metoclopramide is decreased. | |||
| * Alcohol : Risk of serious intoxication. | |||
| ==Dosage== | |||
| Strictly individual. Oral, and in some countries, IV and ] use is possible. The usual oral daily doses are between 2 and 16mg. If possible, patients should be started with a low initial dose which is increased slowly. | |||
| ==Overdose== | |||
| Biperiden mimics an atropine intoxication with mydriasis, dryness of mucous membranes, red face, atonic states of bowels and bladder, and ] 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 ] which combines a peripheral and a central action. ] 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. | |||
| ==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== | |||
| {{reflist|2}} | |||
| {{Anticholinergics}} | |||
| {{Anti-parkinson anticholinergic agents}} | |||
| ] | |||
| ] | |||
| ] | |||
| ] | |||
| ] | |||
Revision as of 21:59, 16 April 2009
Pharmaceutical compound | |
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| Clinical data | |
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| Pregnancy category |
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| Routes of administration | Oral, IM, IV |
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| Pharmacokinetic data | |
| Bioavailability | 33 ± 5% (oral) |
| Protein binding | 60% |
| Metabolism | Hepatic hydroxylation |
| Elimination half-life | 18 to 24 hours |
| Excretion | Renal |
| Identifiers | |
IUPAC name
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.007.441  |
| Chemical and physical data | |
| Formula | C21H29NO |
| Molar mass | 311.461 g/mol g·mol |
| 3D model (JSmol) | |
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Biperiden is an antiparkinsonian agent of the anticholinergic type.<ref name="pmid9798802">{{cite journal |author=Pehl C, Wendl B, Kaess H, Pfeiffer A |title=Effects of two anticholinergic drugs, trospium chloride and biperiden, on motility and evoked potentials of the oesophagus |
- Jackisch R, Kruchen A, Sauermann W, Hertting G, Feuerstein TJ (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.
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