Aprocitentan
Hypertension
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Drug Status
Government Approvals
US(FDA), UK(BNF)
WHO Essential Medicine
NO
Known Teratogen
No
Pharmaceutical Class
NA
Controlled Drug Substance
No
Aprocitentan
Summary
Aprocitentan is used to treat high blood pressure in adults when other medications have not been effective enough.
Aprocitentan works by blocking the action of a substance called endothelin, which causes blood vessels to narrow. This helps relax the blood vessels, reducing blood pressure and easing the heart's workload.
The usual dose for adults is 12.5 mg of Aprocitentan taken orally, once daily.
Common side effects of Aprocitentan include fluid retention, anemia, and headache. Serious effects include liver toxicity, fluid retention, and decrease in hemoglobin.
Aprocitentan is not recommended during pregnancy due to the risk of serious birth defects. It should also not be used by women of childbearing potential who are not using reliable contraception. It is contraindicated in patients with severe liver impairment and those allergic to its ingredients.
Indications and Purpose
How does Aprocitentan work?
Aprocitentan works by blocking the action of endothelin, a natural substance in the body that causes blood vessels to narrow. By inhibiting endothelin, Aprocitentan helps relax and widen blood vessels, which lowers blood pressure and reduces the heart's workload.
Is Aprocitentan effective?
Aprocitentan has been shown to effectively lower blood pressure in adults with hypertension not adequately controlled on other drugs. Clinical trials demonstrated a significant reduction in systolic and diastolic blood pressure compared to placebo, with the most substantial effect observed within the first two weeks of treatment.
What is Aprocitentan?
Aprocitentan is used to treat high blood pressure that has not responded to other medications. It belongs to a class of drugs called endothelin receptor antagonists, which work by blocking the action of endothelin, a substance that causes blood vessels to narrow. This helps relax blood vessels, reducing blood pressure and easing the heart's workload.
Directions for Use
For how long do I take Aprocitentan?
Aprocitentan is typically used as a long-term treatment for high blood pressure that has not responded to other medications. The duration of use will depend on the individual's response to the medication and should be determined by a healthcare provider.
How do I take Aprocitentan?
Aprocitentan should be taken orally once a day, with or without food. There are no specific food restrictions associated with this medication, but it is important to follow a healthy diet as part of a comprehensive plan to manage high blood pressure.
How long does it take for Aprocitentan to start working?
Most of the blood pressure-lowering effect of Aprocitentan occurs within the first two weeks of treatment. However, the full effect may take longer, and it is important to continue taking the medication as prescribed by your doctor.
How should I store Aprocitentan?
Store Aprocitentan tablets at room temperature, between 68°F to 77°F (20°C and 25°C). Keep the tablets in the original container, tightly closed, and protect them from light and moisture. Do not discard the desiccant packet inside the bottle.
What is the usual dose of Aprocitentan?
The usual daily dose of Aprocitentan for adults is 12.5 mg taken orally once a day. There is no established dose for children as the safety and efficacy of Aprocitentan in pediatric patients have not been established.
Warnings and Precautions
Can Aprocitentan be taken safely while breastfeeding?
Women are advised not to breastfeed while taking Aprocitentan due to the potential for serious adverse reactions in breastfed infants. It is unknown if Aprocitentan is excreted in human milk, but it has been found in the milk of lactating rats.
Can Aprocitentan be taken safely while pregnant?
Aprocitentan is contraindicated during pregnancy due to the risk of serious birth defects. Women of childbearing potential must use effective contraception and have regular pregnancy tests before, during, and after treatment. If pregnancy is detected, Aprocitentan should be discontinued immediately.
Can I take Aprocitentan with other prescription drugs?
Aprocitentan may interact with drugs that are substrates of OAT3, potentially increasing their plasma concentrations. Caution is advised when co-administering with drugs that have a narrow therapeutic index. Aprocitentan is also a substrate and inhibitor of UGT1A1 and UGT2B7, and it may affect the pharmacokinetics of other drugs metabolized by these enzymes.
Is Aprocitentan safe for the elderly?
Elderly patients may have a higher risk of experiencing side effects such as edema/fluid retention, heart failure, and anemia. It is recommended to monitor these patients closely for signs of fluid retention or heart failure. No dose adjustment is required for patients over the age of 65.
Who should avoid taking Aprocitentan?
Aprocitentan is contraindicated in pregnancy due to the risk of serious birth defects. It should not be used by individuals with severe hepatic impairment or those allergic to its ingredients. Patients should be monitored for hepatotoxicity, fluid retention, and anemia. Women of childbearing potential must use effective contraception during treatment.
