Drug Notebook

FDA Alerts

    Hepatotoxicity
  • Risk of developing serious hepatic injury. With close monitoring, unexplained hepatic cirrhosis and liver failure reported rarely after prolonged bosentan therapy (>12 months) during postmarketing surveillance.
  • Serum aminotransferase (AST/ALT) concentrations must be measured prior to initiation of therapy and monthly thereafter. (See Hepatic Effects under Cautions.)
  • In patients with adverse hepatic effects, dosage reduction or discontinuance of the drug may be necessary. (See Patients with Adverse Hepatic Effects under Dosage and Administration.)
  • Bosentan generally should be avoided in patients with elevated aminotransferases (>3 × ULN) at baseline (because monitoring for liver injury may be more difficult) and in those with preexisting moderate to severe hepatic impairment.

    Fetotoxicity
  • May cause fetal harm; contraindicated in pregnant women. Pregnancy must be excluded before start of treatment and prevented thereafter by use of reliable contraception. (See Fetal/Neonatal Morbidity and Mortality under Cautions.) Oral, injectable, transdermal, and implantable hormonal contraceptives may not be reliable when used concomitantly with bosentan and should not be used as the sole contraceptive method; additional forms of nonhormonal contraception should be used. (See Specific Drugs under Interactions.)

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What is the most important information I should know about bosentan?

This medication can cause birth defects in an unborn baby. Do not use if you are pregnant. Tell your doctor right away if you become pregnant during treatment. Use an effective barrier form of birth control (such as a condom or diaphragm with spermicide gel or inserts). Hormonal forms of contraception (such as birth control pills, injections, implants, skin patches, and vaginal rings) may not be effective enough to prevent pregnancy during your treatment.

Your doctor may have you take a pregnancy test before you start using this medicine, to make sure you are not pregnant. You may also be re-tested each month during your treatment.

Bosentan can cause severe liver problems. Symptoms include nausea, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes). Call your doctor at once if you have any of these symptoms. Your liver function will need to be tested before you start taking bosentan, and again each month during your treatment. Do not stop taking bosentan without first talking to your doctor. You may need to use less and less before you stop the medication completely.

What is Bosentan?

Bosentan prevents thickening of the blood vessels, especially those in the lungs and heart. Bosentan also lowers blood pressure in your lungs, helping your heart pump blood more efficiently.

Bosentan is used to treat pulmonary arterial hypertension (PAH). It improves your ability to exercise and prevents your condition from getting worse.

Bosentan may also be used for other purposes not listed in this medication guide.

What should I discuss with my healthcare provider before taking bosentan?

Do not use this medication if you are allergic to bosentan, or if you: Bosentan can cause severe liver problems. Symptoms include nausea, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes). Call your doctor at once if you have any of these symptoms. Your liver function will need to be tested before you start taking bosentan, and again each month during your treatment. FDA pregnancy category X. This medication can cause birth defects. Do not use bosentan if you are pregnant. Tell your doctor right away if you become pregnant during treatment. Use an effective barrier form of birth control (such as a condom or diaphragm with spermicide gel or inserts). Hormonal forms of contraception (such as birth control pills, injections, implants, skin patches, and vaginal rings) may not be effective enough to prevent pregnancy during your treatment.

Your doctor may have you take a pregnancy test before you start using this medicine, to make sure you are not pregnant. You may also be re-tested each month during your treatment.

It is not known whether bosentan passes into breast milk or if it could harm a nursing baby. Do not take this medication without telling your doctor if you are breast-feeding a baby.

How should I take bosentan?

Take bosentan exactly as it was prescribed for you. Do not take the medication in larger or smaller amounts, or take it for longer than recommended by your doctor.

Take each dose with a full glass (8 ounces) of water.

Bosentan can be taken with or without food.

Bosentan is usually taken twice a day, morning and evening.

Do not stop taking bosentan without first talking to your doctor. You may need to use less and less before you stop the medication completely. Store bosentan at room temperature away from moisture and heat.
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