Melperone

4-fluoro- 4-( 4-methyl- piperidino) - butyrophenone

  • 3575-80-2 ( melperone )
  • 1622-79-3 ( melperone · hydrochloride)

N05AD03

  • Neuroleptic
  • Butyrophenones

Blockade of postsynaptic D2 receptors in the mesolimbic and mesocortical system

209-211 ° C ( melperone · hydrochloride)

Template: Infobox chemical / molecular formula search available

Melperone is a medium potent neuroleptic agent from the class of butyrophenones. Pharmacologically, it is assigned to the typical neuroleptics. The antipsychotic potency (Reference is chlorpromazine ) is inferior to the sedative component. In higher doses to write to melperone a sleeping abutting ( hypnotic ) effect component. It is mainly used for excitation, voltage, and sleep disorders. Melperone has a very low incidence of the so-called EPS ( extrapyramidal disorders ), it has in comparison with other Central and low-potency neuroleptics a small influence on the cardiovascular system and a very low delirium - inducing effect, so that it is often in geriatric psychiatry patients will use.

Pharmacology

Indications

As already mentioned, melperone find V.A. at excitation, stress, and sleep disorders insert ( v. doses of 10-100 mg / day or the night to ), but it is (50-200 mg / day Dv) also used in a state of confusion and delirium alcoholic. Another indication is an additional medication in anxious - depressed patients with sleep disturbance ev ( doses 25-75 mg / day and at night ). An antipsychotic ( acting against positive symptoms ) effect is achieved only at high doses ( approximately 200-400 mg / day) and melperone is hardly used in this indication.

Pharmacodynamics

Melperone acts relatively weak antidopaminerg by the blockade of postsynaptic D2 receptors in the mesolimbic and mesocortical areas; Moderate to high affinity and binding only briefly ( so-called "hit - and-run Effect" ); the nigrostriatal region of the D2 antagonism is still low, so low incidence of EPS. A serotonin contributes to the blocking effect.

Melperone also acts clearly antinoradrenerg ( α1 - blockade ), which probably contributes to the sedative effect, but this is short term and the possible hypotensive effect only weakly.

Pharmacokinetics

After oral administration, Cmax achieved within 1-3 hours; Volume of distribution Vd = 7-10 l · kg -1. Plasma protein binding about 50%. Half-life Tβ (1/ 2) = 6-8 hours ( steady-state ). Elimination mainly renal ( kidney through ), mostly as metabolites ( intensive metabolism ).

Production

The synthesis is carried out from 4- methylpiperidine and 4-chloro -4'- fluorobutyrophenone by a nucleophilic substitution.

Trade names

Buronil (A), Eunerpan (D), Melneurin (D ), numerous generics (D), Bunil (P)

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