Pharmacokinetic Characteristics of a Nifedipine and Lidocaine Fixed Combination in the Form of Rectal Cream: Two Decades Data Analysis


  • Raffaele Ottaiano New.Fa.Dem., S.r.l., Italy
  • Mara Sebastiano New.Fa.Dem., S.r.l., Italy
  • Larysa Bondarenko Institute of Pharmacology & Toxicology of NAMS of Ukraine, SI, Ukraine
  • Oleksandra Iudina UA PRO-PHARMA, LLC, Ukraine



nifedipine, lidocaine, fixed combination, pharmacokinetic characteristics


The creation of medicines' fixed combinations from compounds with complementary effects is one of the most popular directions in modern pharmacology and pharmaceutics. In case of nifedipine and lidocaine fixed combination such approach is quite obvious. The present review article is devoted to the analysis of clinical and non-clinical studies results on the assessment of the pharmacokinetic characteristics of these medicines. Although the oral route is the most convenient for drug administration, there are a number of circumstances where this is not possible from either a clinical or pharmaceutical perspective. In these cases, the rectal route may represent a practical alternative and can be used to administer drugs for both local and systemic actions. Research data of last decades suggested that nifedipine, a calcium channel blocker, could be effective in reducing anal resting pressure and in healing chronic anal fissure and acute thrombosed hemorrhoids. Another component of fixed combination lidocaine is a local anesthetic usually used to relieve pain of anal fissures and symptomatic hemorrhoids. In combinations lidocaine and nifedipine have complementary actions. Analysis of all available studies (during last 2 decades) which were aimed to investigate pharmacokinetic characteristics of a nifedipine and lidocaine fixed combination in the form of rectal cream showed that following topical application, the active ingredients nifedipine and lidocaine are absorbed into the bloodstream in only small quantities that have no major implications for the safety of the product, and systemic absorption, if any, was incomparably lower than absorption following per os administration of the two active ingredients.


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How to Cite

Ottaiano R, Sebastiano M, Bondarenko L, Iudina O. Pharmacokinetic Characteristics of a Nifedipine and Lidocaine Fixed Combination in the Form of Rectal Cream: Two Decades Data Analysis. Innov Biosyst Bioeng [Internet]. 2021Apr.6 [cited 2023Sep.23];5(1):27-36. Available from: