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Related Concept Videos

Pharmacokinetics: Drug–Drug Interactions01:25

Pharmacokinetics: Drug–Drug Interactions

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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...
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Pharmacokinetics: Drug–Food and Drug–Viral Interactions01:26

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A drug interaction occurs when the concurrent use of another drug, food, or an external substance alters the pharmacological activity of a drug. This interaction can modify the action of the original drug, affecting its effectiveness and safety.Drug–food interactions are significant as they impact drug absorption, metabolism, and excretion. For example, grapefruit juice is a well-known disruptor of drug metabolism. It inhibits the cytochrome P450 3A4 enzyme, crucial for the metabolism of...
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Drug toxicity: Drug–Drug Interaction01:30

Drug toxicity: Drug–Drug Interaction

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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...
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Factors Affecting Protein-Drug Binding: Drug Interactions01:23

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Drug interactions are a critical aspect of pharmacology and can occur when two or more drugs compete for the same binding site. This competition can result in one drug displacing another, altering the effect of the displaced drug. Drug interactions are complex processes that rely heavily on how much of the displacer drug is present and how strongly it can bind to the same sites as the displaced drug.
Displacement interactions can have varying outcomes, ranging from toxicity to virtually...
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Pharmacokinetic–Pharmacodynamic Relationship: Duration of Dose-Effect Relationship01:14

Pharmacokinetic–Pharmacodynamic Relationship: Duration of Dose-Effect Relationship

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For drugs producing a quantal response, onset occurs when plasma concentration reaches a minimum effective level (Cmin). The drug's action duration depends on how long the plasma concentration remains above Cmin.Two primary factors influence this duration: dose size and the rate of drug removal from the action site. Both depend on the drug's redistribution to poorly perfused tissues and elimination processes. A larger dose promotes rapid onset and prolongs the effect's duration.Consider a...
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Nonlinear Pharmacokinetics: Dependence of Elimination Half-Life and Dose Clearance01:23

Nonlinear Pharmacokinetics: Dependence of Elimination Half-Life and Dose Clearance

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The elimination half-life and drug clearance of drugs following nonlinear kinetics can vary with dosage. The Michaelis-Menten parameters and drug concentration influence these factors. As the dose increases, the elimination half-life tends to lengthen, resulting in a reduction in clearance and a disproportionately larger area under the curve. The total clearance can be derived from the Michaelis-Menten equation for drugs following a one-compartment model.
A study on guinea pigs examined the...
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[Pharmacokinetic interactions].

Piedad Arazo Garcés1, Ignacio de los Santos Gil

  • 1Servicio de Medicina Interna, Unidad de Enfermedades Infecciosas, Hospital Universitario Miguel Servet, Zaragoza, España.

Enfermedades Infecciosas Y Microbiologia Clinica
|November 21, 2013
PubMed
Summary
This summary is machine-generated.

Rilpivirine (RPV), a potent nonnucleoside reverse transcriptase inhibitor (NNRTI), shows significant drug interactions via the CYP450 system. Food intake enhances RPV absorption, crucial for effective antiviral therapy.

Keywords:
Drug interactionsHIV infectionInfección VIHInteracciones medicamentosasRilpivirinaRilpivirine

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Area of Science:

  • Pharmacology
  • Virology
  • Drug Metabolism

Background:

  • Rilpivirine (RPV) is an approved nonnucleoside reverse transcriptase inhibitor (NNRTI) for treatment-naïve patients.
  • RPV exhibits potent antiviral activity with a distinct adverse effect profile compared to earlier NNRTIs.

Purpose of the Study:

  • To elucidate the pharmacological interactions of RPV.
  • To understand RPV's metabolic pathways and transporter interactions.
  • To provide guidance on co-administration with other antiretrovirals and medications.

Main Methods:

  • In vitro assessment of RPV's interaction with the CYP450 system, specifically CYP3A4.
  • Evaluation of RPV's inhibitory effects on P-glycoprotein (P-gp).
  • Analysis of known drug interaction data with protease inhibitors, NNRTIs, and drugs affecting gastric pH or CYP3A4.

Main Results:

  • RPV is a substrate and mild inducer of CYP3A4 and inhibits P-gp in vitro.
  • Clinically significant interactions occur with protease inhibitors and other NNRTIs (efavirenz, nevirapine).
  • Contraindicated co-administration with gastric acid reducers (omeprazole) and CYP3A4 inducers (rifampicin) due to reduced RPV levels.
  • Concomitant use with CYP3A4 inhibitors (clarithromycin) may increase RPV levels.

Conclusions:

  • RPV's pharmacokinetic profile is influenced by the CYP450 system and drug transporters.
  • Careful consideration of concomitant medications is essential to optimize RPV efficacy and safety.
  • Administration with food is recommended to ensure adequate plasma concentrations and therapeutic benefit.