| Common Brands | Emend |
|---|---|
|
Drug Class |
NK1 receptor antagonist |
|
Controlled Substance Classification |
Not a controlled medication |
|
Generic Status |
Lower-cost generic available |
|
Availability |
Prescription only |
Aprepitant is generally used for the prevention of nausea and vomiting associated with chemotherapy, especially highly emetogenic chemotherapy, as well as postoperative settings. Brand names include Emend. Aprepitant is typically used in combination with other antiemetic drugs like 5-HT3 receptor antagonists (for example, ondansetron) and corticosteroids (for example, dexamethasone) to achieve optimal control of nausea and vomiting.
Being an NK1 receptor antagonist, aprepitant is a drug that blocks the action of substance P, a neurotransmitter involved in the vomiting reflex. It thereby inhibits this pathway, thereby reducing the occurrence of nausea and vomiting, especially during conditions where such symptoms are likely to arise, such as chemotherapy or post-surgical recovery.
Aprepitant is administered orally, usually in the form of a capsule or tablet. To achieve the best outcome, follow these general guidelines:
Take as directed: Take the medication exactly as directed by your doctor. Aprepitant should be taken one hour before chemotherapy or surgery, depending on the reason for the treatment.
Food and Timing: Aprepitant can be taken with or without food. However, taking it on an empty stomach may sometimes result in faster absorption.
Follow-up therapy: If aprepitant is part of chemotherapy treatment, it may be taken in combination with other antiemetic drugs such as ondansetron and dexamethasone. It is advisable to carry out the full course for better results.
Missed dose: If you are missed a dose of aprepitant, seek your physician for advice on what you can do next.
Aprepitant works by blocking the NK1 receptors in the central nervous system, which play a key role in the process of vomiting. Here’s how it works:
Inhibition of Substance P: Substance P is a neuropeptide that binds to NK1 receptors, initiating the vomiting reflex. Aprepitant prevents substance P from binding to these receptors, effectively stopping the cascade of events that lead to nausea and vomiting.
Action on the Brain: The vomiting center in the brainstem receives signals from different areas of the body when nausea or vomiting is triggered. By blocking the NK1 receptors, aprepitant reduces the activation of this center and prevents the feeling of nausea and the act of vomiting.
Combination Therapy: Although aprepitant can be used alone, it is often combined with other drugs, such as 5-HT3 antagonists and steroids, to achieve a more complete prevention of nausea and vomiting, especially in chemotherapy-induced cases.
Aprepitant targets the nausea pathways of the central nervous system to help alleviate severe nausea and vomiting in high-risk situations, such as chemotherapy and surgery.
Although aprepitant has been found to be largely well tolerated, it produces side effects. Common adverse effects include:
Allergic reactions: including rash, itching, and swelling
Liver problems: Aprepitant can influence liver function, and you must have your liver enzymes monitored.
Severe abdominal pain or vomiting: These can be symptoms of a severe gastrointestinal condition and should be evaluated promptly.
If you are experiencing any severe or strange symptoms, you must call your doctor right away.
Important Precautions before Applying Aprepitant
It should be kept in mind that:
Pregnancy is one of the considerations about its category. Category B as regarded, and so by inference, it is deemed appropriate when pregnant, though under careful and prudent health professionals to apply when not utterly inevitable.
Liver impairment.The drug dose is considered essential especially when there are a pathological state in a disease due to impaired liver diseases. Liver enzyme needs careful, and frequent followup as required.
Aprepitant can interact with a variety of drugs, affecting either the efficacy of this drug or the efficacy of other concomitant drugs. It is known to have the following interactions:
CYP3A4 inhibitors (e.g., ketoconazole, ritonavir): Aprepitant is metabolized by CYP3A4 enzymes, and inhibitors can increase the concentration of aprepitant in the body, raising the risk of side effects.
CYP3A4 inducers (e.g., rifampin, carbamazepine): These drugs can decrease the levels of aprepitant, making it less effective.
Anticoagulants (e.g., warfarin): Aprepitant may affect the anticoagulant effects of warfarin, increasing the risk of bleeding. Close monitoring of blood clotting parameters is recommended.
Chemotherapy-induced nausea and vomiting: The typical dose is 125 mg on Day 1 and 80 mg on Day 2 and Day 3. It should be administered one hour prior to chemotherapy.
Postoperative nausea and vomiting: A single dose of 40 mg is usually administered 3 hours before surgery.
Aprepitant can only be acquired with a prescription from a healthcare provider. It is important to observe the doctor’s prescription and communicate your complete medical history as well as the medications that you are on. Follow-ups may be necessary to track its effectiveness and any possible side effects.
Aprepitant is primarily used to prevent nausea and vomiting caused by chemotherapy in cancer patients, and it can also be used for postoperative nausea and vomiting.
Aprepitant works as a neurokinin-1 (NK1) receptor antagonist, blocking the action of substance P, a neuropeptide involved in the emetic (vomiting) response.
Common side effects include fatigue, dizziness, nausea, diarrhea, and loss of appetite. Severe side effects can occur but are less common.
Aprepitant can interact with many medications. Always consult a healthcare provider before using it with other drugs, especially anticoagulants, antidepressants, and steroids.
Aprepitant is categorized as Pregnancy Category B, indicating that it is not expected to harm an unborn baby. However, it should only be used if necessary and prescribed by a healthcare provider.
Aprepitant can be administered orally in capsule form and is typically taken one hour before chemotherapy treatment. There is also an injectable form used in some cases.
Aprepitant should not be used in individuals with a known allergy to the drug or any of its components. It is also contraindicated in some conditions affecting liver function.
Aprepitant has been shown to be highly effective in preventing acute and delayed nausea and vomiting related to chemotherapy when used in combination with other anti-emetic agents.
Yes, aprepitant can be used in pediatric patients aged 6 months and older for nausea and vomiting related to chemotherapy. Dosage adjustments are necessary based on age and weight.
If a dose is missed, take it as soon as possible. If it’s already time for the next dose, skip the missed dose and continue with the regular schedule. Do not take two doses at once.
Avoid alcohol and grapefruit juice, as they can interact with aprepitant and potentially increase side effects or reduce its effectiveness.
Individuals with liver disease should use aprepitant with caution. Dosage adjustments may be necessary, and close monitoring by a healthcare professional is recommended.
An overdose of aprepitant may cause an increase in side effects. If an overdose is suspected, seek medical attention immediately.
The anti-emetic effects of aprepitant can last for several days, depending on the dosage and the specific chemotherapy regimen used.
Aprepitant is not typically used for motion sickness. Other medications are more commonly recommended for that purpose.
While fatigue can be a side effect, aprepitant generally does not cause significant drowsiness in most patients. However, individual reactions may vary.
The usual recommended dose for adults is 125 mg taken orally one hour before chemotherapy on the first day, followed by 80 mg daily for the next two days.
Store aprepitant at room temperature, away from moisture and heat. Keep it out of reach of children.
Aprepitant capsules should not be crushed or broken. They should be swallowed whole for proper delivery of the medication.
Discuss your complete medical history, current medications, any allergies, and your chemotherapy regimen to ensure that aprepitant is safe and appropriate for you.
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