Azole | Medicines for fungal infection

Azole

Azoles (anti-fungal agents) interfere with the synthesis of ergosterol at a later stage than allylamines. They have an inhibitory effect on fungal growth (fungistatic). Classification and application: With the azoles (means against fungal diseases) one differentiates active substances, which can be applied only locally, i.e.

locally (e.g. as cream or ointment) from active substances, with which local and systemic gifts are possible. For example, clotrimazole (Canesten®) is used as a local active ingredient for fungal infections of the skin, oral mucosa, genitals and skin folds. Other locally applied active ingredients are ketoconazole (Nizoral®), bifonazole (Mycospor®), miconazole (Daktar®), isoconazole (Travocort®), oxiconazole (Myfungar®) and fenticonazole (Fenizolan®).

Active ingredients that can also be administered systemically include fluconazole (Diflucan®), itraconazole (Sempera®), posaconazole (Noxafil®) and voriconazole (Vfend®).They are quite broad, i.e. they are effective against various types of fungi (remedies against fungal diseases). Side effects and contraindications: The most likely adverse effects are gastrointestinal tract disorders such as nausea or abdominal pain. Headaches, dizziness or skin rashes may also occur.

Only rarely the liver is also affected, which can result in an increase in liver values (liver enzymes), but can also lead to severe functional disorders. Patients with liver disease and children in general should not be treated with azoles. Drug interactions through azoles: Azoles (drugs for fungal diseases) influence certain enzymes in the liver that belong to the so-called cytochrome P450 system (CYP450 enzymes).

On the one hand, azoles are metabolised by CYP450 enzymes, on the other hand, azoles also inhibit some of these enzymes. Thus, these antimycotics (agents against fungal diseases) influence the activation or degradation of some other drugs. If other active substances such as rifampicin, phenytoin, carbamazepine or phenobarbital are administered at the same time, they are broken down more quickly by azoles, which leads to a loss of efficacy of these substances.

On the other hand, azoles should not be given with drugs that alter stomach acid. This leads to a reduced absorption of the azoles from the gastrointestinal tract. These include H2-blockers such as ranitidine or drugs to neutralize the acidic gastric juice (antacids). The active ingredients itraconazole and voriconazole can lead to cardiac arrhythmia if terfenadine, an allergy medication (antihistamine), is administered simultaneously.