Unbound MEDLINE

Once daily nifedipine: the formulation dictates the pharmacokinetic characteristics and the therapeutic responses.

Abstract

Nifedipine as a pharmacologic agent for treating hypertension and angina pectoris has been available worldwide since the early 1980's. However, the formulation of nifedipine has undergone a number of modifications over time to improve the pharmacokinetic profile and administration regimen from 3 times daily to once daily. Nifedipine Gastrointestinal Therapeutic System (GITS) is the most widely studied of the once daily formulations from both a pharmacokinetic and clinical perspective. Nifedipine GITS was registered in most major countries worldwide based on both clinical pharmacology and clinical trial data in adequately powered studies. Moreover, outcome trials in both hypertension (INSIGHT) and angina pectoris (ACTION) have been completed and published. Other once daily modified release nifedipine formulations are available in a number of countries but limited published data is available on these formulations. A Pubmed (Medline) search using the terms "nifedipine pharmacokinetics" yielded 162 articles of which 7 provided detailed pharmacokinetic values in head to head comparisons of nifedipine GITS and another once a day formulation. These published pharmacokinetic studies have failed to show that any of the other formulations is consistently bioequivalent to the reference formulation, nifedipine GITS. In addition, other Pubmed searches yielded limited data from comparative clinical studies, which show significant differences in favor of the nifedipine GITS formulation in terms of blood pressure control and activation of the sympathetic nervous system. With limited data comparing once daily formulations of nifedipine to nifedipine GITS and no data comparing between other once a day formulations, for both pharmacokinetic and therapeutic reasons, the evidence indicates that patients should not be switched between once daily formulations of nifedipine.

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  • Publisher Full Text
  • Authors

    Toal CB, Meredith PA, Elliott HL

    Source

    International journal of clinical pharmacology and therapeutics 50:3 2012 Mar pg 202-17

    MeSH

    Calcium Channel Blockers
    Chemistry, Pharmaceutical
    Delayed-Action Preparations
    Drug and Narcotic Control
    Humans
    Hypertension
    Nifedipine
    Sympathetic Nervous System

    Pub Type(s)

    Journal Article

    Language

    eng

    PubMed ID

    22373833