Aprepitant

Aprepitant : Introduction

Aprepitant is a medication used to treat nausea and vomiting caused by chemotherapy. It belongs to a class of medications called neurokinin-1 (NK-1) receptor antagonists. Aprepitant is available in capsule and injection form.

Uses for Aprepitant

Aprepitant is used to treat the nausea and vomiting caused by chemotherapy and radiation treatments. It may also be used to prevent nausea and vomiting during and after surgery. It is usually taken in combination with other medications to treat nause.

Brand Name	Aprepitant
Type
Weight
Generic	Aprepitant
Manufacturer
Available in	English বাংলা

Mechanism of Action

Aprepitant works by blocking NK-1 receptors, which are involved in the vomiting reflex. By blocking these receptors, aprepitant decreases the vomiting reflex and helps to prevent nausea and vomiting caused by chemotherapy or radiation.

How Long Does It Take to Work?

Aprepitant begins to work within an hour of taking the medication. It is usually taken one to four hours before chemotherapy or radiation treatments, or two to four hours before surgery.

Absorption

Aprepitant is rapidly absorbed after oral administration and reaches peak plasma concentrations within 1-2 hours. It is approximately 40% bound to plasma proteins.

Route of Elimination

Aprepitant is primarily metabolized by cytochrome P450 3A4 (CYP3A4). It is mostly eliminated in feces as unchanged drug or as metabolites. A small amount is excreted in urine.

Dosage and Administration

Aprepitant is available in both capsule and injection forms. The recommended dosage of aprepitant varies depending on the indication. For the prevention of nausea and vomiting caused by chemotherapy, the recommended dose is 125 mg taken one to four hours before chemotherapy, followed by 80 mg daily for three consecutive days.

For the prevention of nausea and vomiting caused by radiation therapy, the recommended dose is 80 mg taken two to four hours before radiation therapy, followed by 80 mg daily for four consecutive days.

For the prevention of nausea and vomiting during and after surgery, the recommended dose is 80 mg taken two to four hours before surgery, followed by 80 mg daily for three consecutive days.

Side Effects

The most common side effects associated with aprepitant include headache, fatigue, diarrhea, constipation, and dizziness. Other side effects may include nausea, rash, vomiting, and fever.

Toxicity

Aprepitant is generally well-tolerated, but may cause serious side effects if taken in excess. Overdose symptoms may include nausea, vomiting, headache, and dizziness. If an overdose is suspected, seek medical attention immediately.

Precaution

Aprepitant should not be used in patients with known hypersensitivity to the drug. Before taking aprepitant, patient should let their doctor know if they have liver or kidney problems, as the dosage may need to be adjusted. It should be used with caution in patients with severe asthma or COPD.

Interactions

Drugs that interact with aprepitant include: warfarin, diltiazem, carbamazepine, phenytoin, rifampin, dexamethasone, elbasvir/grazoprevir, and phenobarbital. It may also interact with certain herbal products such as St. John's Wort. Patients should inform their doctor of all medications they are taking before starting aprepitant.

Disease Interactions

Aprepitant may interact with certain disease states, such as liver or kidney disease. Patients with these conditions should be monitored closely while taking aprepitant. Caution should also be used in patients with asthma or COPD.

Drug Interactions

Aprepitant can interact with other drugs, such as warfarin, diltiazem, carbamazepine, phenytoin, rifampin, dexamethasone, elbasvir/grazoprevir, and phenobarbital. Patients should inform their doctor of all medications they are taking before starting aprepitant. In some cases, the dosage of other medications may need to be adjusted.

Food Interactions

Aprepitant can interact with certain foods and beverages. Patients should avoid alcohol, grapefruit juice, and spicy or fatty foods while taking aprepitant.

Pregnancy Use

Aprepitant is not recommended for use during pregnancy, as the safety of the drug has not been established. Women who are pregnant or planning to become pregnant should talk to their doctor before taking aprepitant.

Lactation Use

It is not known if aprepitant is excreted in breastmilk. Women who are breastfeeding or plan to breastfeed should talk to their doctor before taking aprepitant.

Acute Overdose

If an overdose of aprepitant is suspected, seek medical attention immediately. Overdose symptoms may include nausea, vomiting, headache, and dizziness.

Contraindication

Aprepitant should not be used in patients with known hypersensitivity to the drug.

Use Direction

The recommended dosage of aprepitant varies depending on the indication. Patients should take the medication according to their doctor’s instructions.

Storage Condition

Aprepitant should be stored at room temperature, away from moisture and direct light.

Volume of Distribution

The volume of distribution of aprepitant is approximately 17 L.

Half Life

The plasma half-life of aprepitant is approximately 18-22 hours.

Clearance

The clearance of aprepitant is approximately 5.6 L/hr.

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Some Frequently Asked Questions About Aprepitant