Monograph
A04AA05 - Palonosetron |
Propably not porphyrinogenic |
PNP |
Rationale
Substrate of Cyps 2D6, 3A4 and 1A2. Water soluble drug, thus probably devoid of capacity for significant PXR-activation and subsequent Cyp-induction. Demonstrated in vitro not to be a Cyp-inhibitor or Cyp-inducer. The common side effect of constipation may worsen pre-existing porphyria-induced constipation in the patient.
Chemical description
Quinuclinidinyl-benz-isokinoline. Two cyclic tertiary amine functions in the molecule.
Therapeutic characteristics
Palonosetron is used for prevention of nausea in chemotherapy. It is a potent selective 5-HT receptor antagonist inhibiting reflexogenic nausea caused by 5-OH tryptamine.
Confounding side effects: constipation, diarrhoea.
Metabolism and pharmacokinetics
Metabolized mainly by Cyp 2D6, and to a minor extent by Cyp 3A4 and 1A2. In-vitro studies demonstrate abscence of capacity for Cyp-inhibition or induction.
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