Riociguat

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This is not a complete list of Riociguatdrug interactions. Ask your doctor or pharmacist for more information.

Riociguat lowers blood pressure in your lungs, helping your heart pump blood more efficiently.

Riociguat is used to treat chronic thromboembolic pulmonary hypertension (CTEPH) in people who cannot be treated with surgery, or in people who have undergone surgery but still have symptoms. Riociguat can treat certain symptoms of CTEPH and can improve your ability to exercise.

Riociguat is used to treat pulmonary arterial hypertension (PAH). Riociguat can improve your ability to exercise and help prevent PAH from getting worse.

Riociguat is available to women only under a special program from a certified pharmacy. You must be registered in the program and understand the risks and benefits of taking this medication.

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

Riociguat is available to women only under a special program from a certified pharmacy. You will need to have a negative pregnancy test before starting this treatment.

Riociguat can cause birth defects. Do not use if you are pregnant. Avoid getting pregnant while taking riociguat and for at least 1 month after your last dose. Do not have unprotected sex.

Tell your doctor about all your current medicines and any you start or stop using. Many drugs can interact with riociguat, and some drugs should not be used together.

Do not have unprotected sex while taking riociguat. You must use birth control to prevent pregnancy during treatment and for at least 30 days after you stop taking this medicine.

Riociguat can cause dizziness and may impair your thinking or reactions. Avoid driving or operating machinery until you know how the medicine will affect you. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.

Avoid taking an antacid within 1 hour before or after you take riociguat. Some antacids can make it harder for your body to absorb riociguat.

Smoking can make riociguat less effective. Tell your doctor if you start or stop smoking while you are taking this medicine. Your dose needs may need to be changed

Metabolized by CYP1A1, 3A, 2C8, and 2J2.1 Both drug and active metabolite are potent inhibitors of CYP1A1.19

Substrate of P-gp and BCRP.1

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

CYP3A4 inhibitors or inducers: Potential pharmacokinetic interaction (increased or decreased riociguat concentrations, respectively); caution is advised and dosage adjustments may be necessary.1 19

CYP1A1 inhibitors or inducers: Potential pharmacokinetic interaction (increased or decreased riociguat concentrations, respectively); caution is advised and dosage adjustments may be necessary.1 19

CYP1A1 substrates: Clinically important interactions are possible.19

Drugs Affecting Efflux Transport Systems

Pharmacokinetic interactions possible with inhibitors or inducers of P-gp and BCRP.1 19 (See Specific Drugs under Interactions.)

Drugs Affecting Hepatic Microsomal Enzymes and Efflux Transport Systems

Concomitant use of potent inhibitors of both CYP and P-gp/BRCP is expected to substantially increase exposure to riociguat and, thus, risk of hypotension.1 Dosage adjustments may be required.1 (See Dosage and Administration: Dosage.)

Specific Drugs

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Distribution of riociguat is restricted.1 (See Restricted Distribution Program under Dosage and Administration.)

Take riociguat as exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance of side effects.

riociguat should come with a Medication Guide. Read and follow these instructions carefully. Ask your doctor if you have any questions.

You may take riociguat with or without food.

If you have trouble swallowing the tablet, you may crush it and mix with water or soft foods (eg, applesauce) and take it immediately.

If you are using an antacid that contains aluminum or magnesium, take it 1 hour after taking riociguat.

Dosing

The dose of riociguat will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of riociguat. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (tablets):
  • For chronic thromboembolic pulmonary hypertension and pulmonary arterial hypertension:
    • Adults—At first, 1 milligram (mg) 3 times a day. Other patients may start at 0.5 mg 3 times a day. Your doctor may adjust your dose as needed and tolerated. However, the dose is usually not more than 2.5 mg 3 times a day.
    • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of riociguat, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

If you missed taking riociguat for 3 days, call your doctor right away.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

• Confusion
• dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
• nosebleeds
• unusual tiredness or weakness

• Abdominal or stomach pain or swelling
• bloating or swelling of the face, arms, hands, lower legs, or feet
• bloody or black, tarry stools
• bruising or purple areas on the skin
• coughing or spitting up blood
• decreased alertness
• fast, irregular, pounding, or racing heartbeat or pulse
• heavy non-menstrual vaginal bleeding
• rapid weight gain
• troubled breathing with exertion
• vomiting of blood or material that looks like coffee grounds

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Diarrhea
• headache
• heartburn or indigestion
• nausea or vomiting
• stuffy nose

• Difficulty having a bowel movement (stool)

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

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Higher exposure to riociguat

Store at 25°C (77°F); excursions are permitted from 15°C to 30°C (59°F to 86°F).