Biperiden

The Parkinson agent biperiden causes psychotic states at high dose rates (10-15 mg/day). Abuse of this drug was at one time rare, but drug-dependent and medicament-dependent people now sometimes use it. The deliberate production of a Parkinsonoid state by the neuroleptic effects of biperiden has also been described. 

Chemical Name a-bicyclo[2.2.1 ] hept-5-en-2-yl-a-phenyl-1-piperidinepropanol 

Trede Name Manufacturer Country Year Introduced 

The reaction mixture is boiled for half an hour under reflux. Thereafter the ether is removed by distillation, until the inside temperature reaches 65°-70°C. The resulting benzene solution is added to 95 cc concentrated hydrochloric acid containing ice for further processing. Thereby, 3-piperidino-1-phenyl-1-[A5-bicyclo-(2,2,1 )-heptenyl-2]-propanol-1 of the summary formula CjiH gON is obtained. The compound melts at 101°C and its chloro-hydrate has a melting point of about 238°C. The compound is difficultly soluble in water, slightly soluble in ethanol, and readily soluble in methanol. 

Klavehr, W. U.S. Patent 2,789,110 April 16, 1957 assigned to Knoll AG Chemische Fabri-ken, Germany 

Chemical Name 4,4 -(2-pyridylmethylene)bisphenol diacetate Common Name — 

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Algestone acetophenide Biperiden Eprozinol Fendiline HCl Phenindamine tartrate Procyclidine HCl Pyrrobutamine Tridihexethyl iodide Trihexyphenidyl HCl m-Acetoxy acetophenone Norfenefrine... 

Fluoro uracil mercury Tegafur Formaldehyde Biperiden Bronopol Cortivazol Edetate disodium Glaziovine Hexetidine Meptazinol Metampicillin sodium Methylol riboflavin Nifurfoline Nifurtoinol Noxytiolin Oxymetazoline HCI Phenindamine tartrate Pipebuzone Thihexinol Timonacic sodium Triclobisonium chloride T romethamine Tyloxapol Formamide Cimetide Primidone Protriptyline Razo xane Spiperone Formic acid Bupivacaine... 

AChs are an effective treatment (see Table 71-4). Benztropine has a half-life that allows once- to twice-daily dosing. Dose increases above 6 mg/day must be slow because of nonlinear pharmacokinetics. Trihexyphenidyl, diphenhydramine, and biperiden usually require three-times-daily dosing. Diphenhydramine produces more sedation, but all of the AChs have been abused for euphoriant effects. 

Bethanechol (U recholine) Biperiden (Akineton) Bisacodyl (Dulcolax)... 

Anticholinergics. Antagonists at muscarinic cholinoceptors, such as betuatropine and biperiden (p. 106), suppress striatal cholinergic overactivity and thereby relieve rigidity and tremor however, akinesia is not reversed or is even exacerbated. Atropinelike peripheral side effects and impairment of cognitive function limit the tolerable dosage. 

Acute dystonias occur immediately after neuroleptization and are manifested by motor impairments, particularly in the head, neck, and shoulder region. After several days to months, a parkinsonian syndrome (pseudoparkinsonism) or akathisia (motor restlessness) may develop. All these disturbances can be treated by administration of antiparkin-son drugs of the anticholinergic type, such as biperiden (i.e., in acute dystonia). As a rule, these disturbances disappear after withdrawal of neuroleptic medication. Tardive dyskinesia may become evident after chronic neuroleptization for several years, particularly when the drug is discontinued. It is due to hypersensitivity of the dopamine receptor system and can be exacerbated by administration of anticholinergics. 

Biperiden Biperiden, l-(5-norbomen-2-yl)-l-phenyl-3-piperidinopropan-l-ol (10.2.4), is also synthesized according to the method of making trihexyphenidyl, except by reacting 2-(l-piperidino)propiophenone (10.2.1) with 5-norbomen-2-ylmagnesiumbromide [33,34],... 

Biperiden has the same properties as the aforementioned drugs. A synonym of this drug is akineton. 

The therapeutic value of these drags is relatively small, and they are nsed either in combination with levodopa, or in cases of minor Parkinsonism. Drags described in Chapter 10—trihexyphenidyl (10.2.2), procyclidine (10.2.3), biperiden (10.2.4), benztropine (10.2.6), ethopropazine (10.2.7), and others belong to this gronp of drugs. 

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