High Quality 99% Pharmaceutical White Powder Aprepitant CAS 170729-80-3

Aprepitant More Info

Aprepitant is a neurokinin-1 (NK1) receptor antagonist used primarily as an antiemetic to prevent nausea and vomiting associated with chemotherapy and surgery. It works by blocking the action of substance P, a neuropeptide involved in the vomiting reflex, thereby reducing the likelihood of emesis (vomiting).

Mechanism of Action

Aprepitant selectively binds to and inhibits NK1 receptors located in the central nervous system. By blocking these receptors, it prevents substance P from exerting its effects, which include:
Inhibition of Vomiting Reflex: Aprepitant reduces both acute and delayed phases of nausea and vomiting induced by cytotoxic chemotherapeutic agents like cisplatin.
Enhanced Efficacy with Other Antiemetics: It is often used in combination with other antiemetic medications, such as 5-HT3 receptor antagonists (e.g., ondansetron) and corticosteroids (e.g., dexamethasone), to improve overall antiemetic effects.

Applications

Chemotherapy-Induced Nausea and Vomiting (CINV): Particularly effective in patients undergoing highly emetogenic chemotherapy.
Postoperative Nausea and Vomiting (PONV): Used to prevent nausea and vomiting following surgical procedures.

Routes of Administration

Aprepitant is available in several formulations:
Oral Capsules: Commonly used for outpatient settings.
Intravenous Formulation: Used in hospital settings for immediate effect.

Safety and Side Effects

Common Side Effects
Commonly reported side effects include:
Fatigue
Headaches
Dizziness
Constipation
Nausea
Loss of appetite
Hiccups
Indigestion
Serious Side Effects
Serious adverse reactions can occur, including:
Allergic Reactions: Symptoms may include hives, difficulty breathing, or swelling of the face, lips, tongue, or throat.
Cardiovascular Issues: Such as irregular heartbeats or hypotension.
Severe Skin Reactions: Including skin peeling or blisters.
Neutropenia: Low white blood cell counts may increase infection risk.
Patients are advised to report any severe side effects or unusual symptoms to their healthcare provider immediately.

Pharmacokinetics

Absorption and Distribution
Aprepitant has an oral bioavailability of approximately 60–65%. It reaches peak plasma concentrations within 3 to 4 hours after administration. The volume of distribution is around 70 L, indicating extensive tissue distribution.
Metabolism and Excretion
Aprepitant is primarily metabolized by the liver through cytochrome P450 enzymes, particularly CYP3A4. The drug has a half-life of approximately 9 to 13 hours, allowing for once-daily dosing in most cases. A significant portion of the drug is excreted in urine as metabolites.