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Related Concept Videos

Pharmacokinetics: Drug–Drug Interactions01:25

Pharmacokinetics: Drug–Drug Interactions

Drug interactions occur when the pharmacological effect of one drug is altered by another substance, either enhancing or diminishing its activity. The drug whose activity is altered is known as the object drug, and the substance causing the alteration is called the agent drug or the precipitant. The net effects of these interactions are mostly undesirable, leading to decreased effectiveness or increased adverse effects. In rare cases, interactions can be beneficial, such as the enhanced...
Bioavailability: Influencing Factors01:22

Bioavailability: Influencing Factors

Bioavailability refers to the extent and rate at which a drug reaches systemic circulation in its active form. Extent refers to the amount of the drug that makes it into circulation, while rate is the speed at which it enters circulation. It is influenced by several factors critical for optimizing drug formulations, dosing regimens, and therapeutic outcomes.Physicochemical properties of drugs and formulationsThe solubility, stability, and dissolution rate of a drug significantly impact its...
Effect of Hepatic Disease on Pharmacokinetics: Dose Adjustments Due to Hepatic Impairment01:08

Effect of Hepatic Disease on Pharmacokinetics: Dose Adjustments Due to Hepatic Impairment

Hepatic impairment, characterized by decreased liver function, does not uniformly mandate adjustments in drug dosage. Whether dosage modifications are necessary depends on various factors related to the drug's metabolism and elimination pathways. If a drug is primarily excreted via the kidneys and bypasses significant hepatic processing, if it undergoes minimal metabolic transformation in the liver, or if it is volatile and primarily expelled through the lungs, dose adjustments may not be...
Drug toxicity: Drug–Drug Interaction01:30

Drug toxicity: Drug–Drug Interaction

Drug–drug interactions can precipitate toxicity through multiple mechanisms. Absorption interactions alter how drugs enter the body, exemplified when ranitidine increases the absorption of basic drugs, while cholestyramine decreases the levels of propranolol. Protein binding interactions occur when drugs share the same binding sites on plasma proteins. Drugs like aspirin and warfarin, when bound in excess, can lead to increased free drug concentrations, enhancing the potential for...
Anticoagulant Drugs: Vitamin K Antagonists and Direct Oral Anticoagulants01:18

Anticoagulant Drugs: Vitamin K Antagonists and Direct Oral Anticoagulants

Oral anticoagulants are vital tools in preventing and treating blood clotting disorders. This diverse class of medications can be categorized as vitamin K antagonists, exemplified by warfarin, and direct thrombin inhibitors (DTIs), such as dabigatran, as well as factor Xa inhibitors, including rivaroxaban.
Warfarin, a prominent vitamin K antagonist family member, exerts its effect by inhibiting the enzyme VKORC1 (vitamin K epoxide reductase complex 1). By hindering this enzyme, warfarin...
Factors Influencing Drug Absorption: Presystemic Elimination01:24

Factors Influencing Drug Absorption: Presystemic Elimination

The pharmacokinetic journey of oral drugs begins with a crucial first pass through the hepatic portal system, called the first-pass effect. This first pass significantly impacts bioavailability — the proportion of a drug that enters systemic circulation and is available for therapeutic action. The primary route sees the drug absorbed by intestinal membranes and then shunted to the liver via the hepatic portal vein. Here, pre-systemic elimination occurs as drugs face metabolism or biliary...

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Related Experiment Video

Updated: May 24, 2026

Metabolic Profiling to Determine Bactericidal or Bacteriostatic Effects of New Natural Products using Isothermal Microcalorimetry
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Metabolic Profiling to Determine Bactericidal or Bacteriostatic Effects of New Natural Products using Isothermal Microcalorimetry

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Decrease in the oral bioavailability of dabigatran etexilate after co-medication with rifampicin.

Sebastian Härtter1, Michael Koenen-Bergmann, Ashish Sharma

  • 1Boehringer Ingelheim Pharma GmbH & Co. KG, Biberach/Riss, Germany. sebastian.haertter@boehringer-ingelheim.com

British Journal of Clinical Pharmacology
|February 22, 2012
PubMed
Summary

Rifampicin significantly reduced dabigatran bioavailability by 67% in healthy volunteers. Dabigatran exposure returned to baseline after a 7-day washout, indicating no clinically relevant long-term effects.

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Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Clinical Pharmacology

Background:

  • Dabigatran etexilate is an oral prodrug of dabigatran, an anticoagulant.
  • CYP3A/P-glycoprotein inducers can affect dabigatran pharmacokinetics.
  • Understanding drug-drug interactions is crucial for safe and effective anticoagulation therapy.

Purpose of the Study:

  • To investigate the impact of rifampicin, a potent CYP3A/P-glycoprotein inducer, on the pharmacokinetics of dabigatran.
  • To assess the effect of rifampicin on dabigatran etexilate bioavailability and exposure.
  • To determine the washout period required for dabigatran pharmacokinetics to return to baseline after rifampicin co-administration.

Main Methods:

  • An open-label, fixed-sequence, four-period study was conducted in healthy volunteers.
  • Subjects received single doses of dabigatran etexilate alone and after 7 days of rifampicin administration.
  • Pharmacokinetic parameters, including AUC(0-∞) and C(max), were measured for total dabigatran.

Main Results:

  • Rifampicin administration significantly decreased the geometric mean area under the concentration-time curve (AUC(0-∞)) and maximal plasma concentration (C(max)) of total dabigatran by 67% and 65.5%, respectively.
  • The time to peak plasma concentration and terminal half-life of dabigatran were not significantly affected by rifampicin.
  • Dabigatran exposure returned to near baseline levels after 7 and 14-day washout periods, with reductions of 18% and 15% in AUC(0-∞), respectively, which were not considered clinically relevant.

Conclusions:

  • A 7-day administration of rifampicin significantly reduces the oral bioavailability of dabigatran.
  • Dabigatran exposure levels nearly returned to baseline after a 7-day washout period following rifampicin discontinuation.
  • The study highlights a significant drug-drug interaction between rifampicin and dabigatran etexilate, emphasizing the need for careful consideration in clinical practice.