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Titolo:
PHARMACOKINETICS AND PHARMACODYNAMICS OF PAROXETINE
Autore:
HIEMKE C;
Indirizzi:
UNIV MAINZ,PSYCHIAT KLIN,UNTERE ZAHLBACHER STR 8 D-55101 MAINZ GERMANY
Titolo Testata:
Fortschritte der Neurologie, Psychiatrie
, volume: 62, anno: 1994,
pagine: 2 - 8
SICI:
0720-4299(1994)62:<2:PAPOP>2.0.ZU;2-O
Fonte:
ISI
Lingua:
GER
Soggetto:
SPARTEINE OXIDATION POLYMORPHISM; ELDERLY DEPRESSED-PATIENTS; RAT-BRAIN; SEROTONIN REUPTAKE; PLASMA 10-HYDROXYNORTRIPTYLINE; ANTI-DEPRESSANTS; ANTIDEPRESSANT; FLUVOXAMINE; FLUOXETINE; DESIPRAMINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
70
Recensione:
Indirizzi per estratti:
Citazione:
C. Hiemke, "PHARMACOKINETICS AND PHARMACODYNAMICS OF PAROXETINE", Fortschritte der Neurologie, Psychiatrie, 62, 1994, pp. 2-8

Abstract

Paroxetine is a trans-isomeric phenylpiperidine with antidepressant properties induced by selective inhibition of the neuronal high affinity uptake of serotonin. In comparison with other selective serotonin uptake inhibitors paroxetine is 2 to 23 times more potent. With the exception of a low affinity to muscarinic receptors, which is not relevantfor therapeutic effects, it does not interact directly with monoamineneurotransmitter receptors. Paroxetine is applied orally at single daily doses of 20 to 50 mg and well absorbed from the gastrointestinal tract. It undergoes a partially saturated first pass metabolism which reduces the bioavailability at therapeutic doses to about 30-60%. Maximal blood levels are reached 2 to 8 hours after oral administration. Inthe plasma 95 % of the drug are bound to protein. Paroxetine is eliminated after transformation in the liver into pharmacologically inactive metabolites. High affinity to the cytochrome P450 isoenzyme CYP2D6 indicates that interferences occur with other drugs which are metabolized via the same isoenzyme. Although clinical practice has not reportedproblematic drug interactions so far, comedications with tricyclic antidepressants should be avoided. The most frequent side effects of paroxetine concern nausea and somnolescence. Since cardiotoxicity or other toxic side effects are much less frequent than under tricyclic antidepressants paroxetine seems advantageous in elderly patients. The onset of antidepressant effects requires several weeks as known for all currently available antidepressants. The pharmacokinetic and pharmacodynamic properties of paroxetine taken together indicate that this selective serotonin uptake inhibitor seems advantageous to other antidepressant agents because of its high selectivity and poor toxicity.

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Documento generato il 21/01/20 alle ore 06:56:17