CYP3A4gátlók

CYP3A4gátlók refer to substances that inhibit the activity of the cytochrome P450 enzyme CYP3A4. CYP3A4 is a crucial enzyme primarily located in the liver and intestines, responsible for metabolizing a significant proportion of drugs and other xenobiotics. Inhibiting its activity can lead to increased plasma concentrations of drugs that are substrates for CYP3A4. This can potentiate their therapeutic effects or, more commonly, lead to adverse drug reactions due to supratherapeutic levels.

CYP3A4gátlók can be broadly classified into reversible and irreversible inhibitors. Reversible inhibitors bind to the enzyme and then dissociate, while irreversible inhibitors form a permanent covalent bond, permanently inactivating the enzyme. The clinical significance of CYP3A4 inhibition lies in its potential to cause drug-drug interactions. For example, co-administration of a potent CYP3A4 inhibitor with a drug that is a CYP3A4 substrate can significantly increase the substrate drug's exposure, potentially leading to toxicity.

Common examples of CYP3A4 inhibitors include certain antifungal medications (like ketoconazole and itraconazole), macrolide antibiotics (like erythromycin and clarithromycin), protease inhibitors used in HIV treatment, and grapefruit juice. The extent of inhibition varies depending on the specific inhibitor and its concentration. Understanding CYP3A4 inhibition is vital for safe and effective pharmacotherapy, guiding dose adjustments and avoiding potentially dangerous combinations of medications.