Aprepitant

5 - {[ (2S, 3R ) -2 - [ (1R ) -1 - [3,5- bis (trifluoromethyl) - phenyl] ethoxy] -3 - ( 4-fluorophenyl) morpholin-4 -yl] methyl} -1,2- dihydro-1 ,2,4-triazol- 3-one

A04AD12

Antiemetic

NK1 antagonist

Template: Infobox chemical / molecular formula search available

Aprepitant (trade name: Emend ®, manufacturer MSD Sharp & Dohme ) is a drug from the group of neurokinin -1 receptor antagonists ( NK1 receptor antagonist ), which used as an antiemetic for the prevention of acute and delayed nausea and vomiting associated with highly emetogenic chemotherapy will.

• 2.1 Mechanism of action ( pharmacodynamics )
• 2.2 Absorption and distribution in the body ( pharmacokinetics )

Clinical information

Areas of application (indications )

Aprepitant ( Postoperative nausea and vomiting, PONV) is approved for the prevention of nausea and vomiting after chemotherapy and after surgery. Here aprepitant is often used in combination with 5 -HT3 antagonists and glucocorticoids. Aprepitant is in the form of hard capsules 40 mg (PONV ), 80 and 125 mg ( chemotherapy) available.

Side effects

One of the unwanted side effects include malaise, loss of appetite, fatigue, headache, liver involvement ( elevated transaminases ).

Contraindications

Aprepitant should not be given in case of hypersensitivity to the drug. It must not be taken during pregnancy. In lactation, treatment with aprepitant is not recommended.

Interactions with other drugs

Aprepitant is a series of interactions with other drugs that are to be observed in the application. This medicine is particularly problematic, which are also metabolized by CYP3A4, or induce or inhibit this. For example, should not be given in combination with terfenadine aprepitant.

Pharmacological properties

Mechanism of action ( pharmacodynamics )

Aprepitant acts as an antagonist of the neurokinin NK1 receptor, by preventing the binding of the natural ligands for NK1, substance P,. The binding of substance P to the NK1 receptor, which is localized to cells in the vomiting center in the brainstem, triggers the nausea; this is reduced by aprepitant.

In addition, aprepitant exists with the drug, fosaprepitant, a prodrug of aprepitant, a substance more with this mechanism of action. Fosaprepitant is approved for use by infusion into drugs under the trade name Ivemend ®.

Uptake and distribution in the body ( pharmacokinetics )

Aprepitant is metabolized primarily by CYP3A4. This drug is also a moderate inhibitor and inducer of the cytochrome.

Swell

• Aprepitant - a new class of antiemetic (PZ )
• Neurokinin receptor antagonists ( ÖAZ ) ( version of 18 June 2009 at the Internet Archive )
• Infomed pharma criticism entry aprepitant
• Karow, General and special pharmacology and toxicology.