Nonlinear Pharmacokinetics: Role of Transporters

Drug kinetics, under nonlinear changes influenced by transporter proteins, are pivotal in drug distribution.

These cellular transporters in cells modulate local drug concentrations through facilitated influx or efflux.

For instance, xenobiotic transporter expression, susceptible to age and gender influences, can potentially impact the pharmacokinetic linearity of the drug.

Polymorphisms in drug transporters contribute to variations in drug toxicity and efficacy, altering pharmacokinetics.

In the liver, the interplay between drug transporters and enzymes can significantly impact the pharmacokinetic linearity of hepatic drugs.

In the intestine, ABC transporters influence bioavailability and linearity of absorption, while bile acid transporters regulate drug movement and elimination.

Various organic anion and cation drug transporters in the kidney can alter the linearity of systemic drug elimination.

The action of breast cancer resistance proteins is considered to achieve pharmacokinetic linearity and suitable dosing in cancer therapy.

Understanding the impact of transporters on pharmacokinetics can improve the safety and efficacy of drug dosing.