Aprepitant
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DRUG STATUS
Approvals
US(FDA), UK(BNF)
Essential Medicine
YES
Teratogenicity
N/A
Pharmaceutical Class
Substance P/Neurokinin-1 Receptor Antagonist
Aprepitant
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Click HereSummary
Aprepitant is used to prevent nausea and vomiting associated with chemotherapy and postoperative situations in adults. It's also used for chemotherapy-related nausea and vomiting in children aged 12 and older.
Aprepitant works by blocking neurokinin, a chemical in the brain that causes nausea and vomiting. It provides protection for both acute (0-24 hours) and delayed (25-120 hours) phases of vomiting.
For chemotherapy, on day 1, take one 125 mg capsule an hour before treatment. On days 2 and 3, take one 80 mg capsule. For surgery, take a 40 mg capsule within 3 hours before the operation. You can take it with or without food.
Common side effects include tiredness, diarrhea, weakness, indigestion, stomach pain, and hiccups. Less common but serious side effects include allergic reactions and dehydration.
Avoid Aprepitant if you're allergic to its components or if you're taking certain medications like Pimozide. It's also not recommended for breastfeeding women, pregnant women unless necessary, and people with liver conditions. Also, inform your doctor about all medications you take before starting Aprepitant.
Indications and Purpose
What is Aprepitant used for?
Aprepitant is indicated for preventing nausea and vomiting associated with highly and moderately emetogenic chemotherapy (including cisplatin-based regimens) and for the prevention of postoperative nausea and vomiting in adults.
How does Aprepitant work?
Aprepitant stops nausea and vomiting. It does this by blocking neurokinin, a chemical in the brain that causes these symptoms. Doctors usually prescribe it for three days during chemotherapy. However, the exact dose and how long you take it will depend on your doctor's instructions. It's very important to take it exactly as prescribed – don't change the dose or how often you take it. * **Neurokinin:** A type of chemical messenger in the brain and body involved in sending signals, including those related to nausea and vomiting. * **Chemotherapy:** A type of cancer treatment using drugs to kill cancer cells.
Is Aprepitant effective?
Aprepitant's effectiveness in preventing nausea and vomiting caused by strong (highly emetogenic chemotherapy or HEC) or moderately strong (moderately emetogenic chemotherapy or MEC) chemotherapy has been shown in a study of children 12 and older. The study included 95 children in this age group, along with younger children. Aprepitant was given with ondansetron (another anti-nausea medicine) and sometimes dexamethasone (a steroid that can also help with nausea). Side effects were similar to those seen in adults. However, how well aprepitant works in children under 6 months old isn't known. * **Highly emetogenic chemotherapy (HEC):** Chemotherapy drugs very likely to cause severe nausea and vomiting. * **Moderately emetogenic chemotherapy (MEC):** Chemotherapy drugs somewhat likely to cause nausea and vomiting. * **Ondansetron:** A medicine to prevent and treat nausea and vomiting. * **Dexamethasone:** A steroid medicine with many uses, including reducing nausea and vomiting.
How does one know if Aprepitant is working?
The studies measured how well the drug prevented nausea and vomiting after chemotherapy and surgery. **Chemotherapy Study:** The main goal was to see how many patients had *no vomiting, retching (the urge to vomit), or needed extra anti-nausea medicine* within 25-120 hours after chemo (this is called a "complete response"). They also looked at complete response in the first 24 hours and up to 120 hours, and just the absence of vomiting up to 120 hours. **Surgery Study:** The main goal was to see how many patients had *no vomiting* and a complete response (no vomiting, no extra medicine) in the first 24 hours after surgery. They also checked for no vomiting in the first 48 hours. In short, the studies measured the drug's success in preventing nausea and vomiting at different times after treatment.
Directions for Use
What is the usual dose of Aprepitant?
Aprepitant is used to prevent nausea and vomiting. For adults and children 12 and older getting chemotherapy, the typical dose is 125mg on the first day, then 80mg on days two and three. If chemo isn't on days two and three, take the 80mg dose in the morning. To prevent nausea and vomiting after surgery, the dose is 40mg within 30 hours before the surgery. *Chemotherapy* is a cancer treatment using drugs. *Hepatic impairment* means the liver isn't working perfectly. *Renal impairment* means the kidneys aren't working perfectly. The dosage usually doesn't need to be changed for mildly or moderately impaired livers, or for any level of kidney impairment.
How do I take Aprepitant?
Aprepitant is a medicine.For chemotherapy: On day 1, take one 125 mg (milligram – a unit of weight) white and pink capsule an hour before your chemo treatment. On days 2 and 3, take one 80 mg white capsule an hour before chemo, or in the morning if you don't have chemo that day. Chemotherapy is cancer treatment using drugs.For surgery: Your doctor will tell you if you need to take a 40 mg capsule within 3 hours before your surgery. Surgery is a medical operation.You can take aprepitant with or without food if you're having chemotherapy. There are no other special diet instructions.
For how long do I take Aprepitant?
Aprepitant is typically used only for the first three days of chemotherapy cycles or as a single dose before surgery. Chronic or continuous use is not recommended as it hasn’t been studied and may increase the risk of drug interactions.
How long does it take for Aprepitant to start working?
Aprepitant begins working within a few hours, effectively preventing nausea and vomiting during chemotherapy or after surgery. It provides protection for both acute (0–24 hours) and delayed (25–120 hours) phases of emesis.
How should I store Aprepitant?
Capsules should be stored at room temperature, away from moisture and heat. Oral suspensions must be refrigerated and used within 72 hours of preparation.
Warnings and Precautions
Who should avoid taking Aprepitant?
Aprepitant is contraindicated in individuals allergic to its components or those taking medications like Pimozide due to the risk of severe drug interactions. Women using hormonal contraceptives should use alternative methods during and for 1 month after taking Aprepitant.
Can I take Aprepitant with other prescription drugs?
Aprepitant interacts significantly with other medications. It affects how the liver processes some drugs. Taking it with strong CYP3A4 inhibitors (drugs that slow down liver processing, like ketoconazole and diltiazem) can raise aprepitant levels in your blood, increasing side effects. Conversely, strong CYP3A4 inducers (drugs that speed up liver processing, like rifampin) can lower aprepitant's effectiveness. Aprepitant can also weaken warfarin (a blood thinner), needing closer monitoring of your blood clotting levels (INR). It might also make hormonal birth control less effective, so a backup method is advised. Never take aprepitant with pimozide (a psychiatric medication) as it's dangerous. Always tell your doctor about all medications you take before starting aprepitant.
Can I take Aprepitant with vitamins or supplements?
There are no known significant interactions with common vitamins or supplements. However, it’s essential to inform your doctor of all supplements being used to avoid potential interactions.
Can Aprepitant be taken safely while pregnant?
Limited studies exist on Aprepitant’s safety during pregnancy. Animal studies did not show fetal harm, but it is generally recommended to use Aprepitant only if clearly needed during pregnancy.
Can Aprepitant be taken safely while breastfeeding?
It is unknown whether Aprepitant is excreted in human milk. Breastfeeding women should weigh the benefits of the medication against potential risks to the infant and consult their doctor before use.
Is Aprepitant safe for the elderly?
Clinical studies indicate no major differences in response between older and younger patients. However, elderly individuals should use it cautiously, especially if they have other medical conditions or take multiple medications.
Is it safe to exercise while taking Aprepitant?
Exercise is generally safe, but patients should avoid strenuous activity if experiencing side effects like dizziness or fatigue. Moderate exercise can help maintain energy levels during treatment.
Is it safe to drink alcohol while taking Aprepitant?
Drinking alcohol while taking Aprepitant can worsen side effects like dizziness or nausea. It’s best to avoid alcohol during treatment for optimal safety.
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