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Riociguat (Oral)

Medically reviewed by Last updated on Sep 29, 2022.

Oral route(Tablet)

Do not administer riociguat to a pregnant female because it may cause fetal harm. Females of reproductive potential: Exclude pregnancy before start of treatment, monthly during treatment, and 1 month after treatment discontinuation. To prevent pregnancy, females of reproductive potential must use effective forms of contraception during treatment and for one month after stopping treatment. For all females, riociguat is available only through a restricted program called the Adempas REMS Program .

Commonly used brand name(s)

In the U.S.

  • Adempas

Available Dosage Forms:

  • Tablet

Therapeutic Class: Cardiovascular Agent

Pharmacologic Class: Soluble Guanylate Cyclase Stimulator

Uses for riociguat

Riociguat is used to treat adults with chronic thromboembolic pulmonary hypertension (CTEPH) that can be treated with surgery, or that cannot be treated with surgery.

Riociguat is also used to treat adults with pulmonary arterial hypertension (PAH), by relaxing these blood vessels and increasing the supply of blood to the lungs, which reduces the workload of the heart.

Riociguat is available only with your doctor's prescription and through a special restricted distribution program called the Adempas® REMS (Risk Evaluation and Mitigation Strategy) Program.

Before using riociguat

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For riociguat, the following should be considered:


Tell your doctor if you have ever had any unusual or allergic reaction to riociguat or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.


Appropriate studies have not been performed on the relationship of age to the effects of riociguat in the pediatric population. Safety and efficacy have not been established.


Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of riociguat in the elderly. However, elderly patients may be more sensitive to the effects of riociguat than younger adults, which may require caution in patients receiving riociguat.


There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking riociguat, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using riociguat with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

  • Aminophylline
  • Amyl Nitrite
  • Avanafil
  • Caffeine
  • Cobicistat
  • Dipyridamole
  • Dyphylline
  • Erythrityl Tetranitrate
  • Isosorbide Dinitrate
  • Isosorbide Mononitrate
  • Lopinavir
  • Nelfinavir
  • Nitric Oxide
  • Nitroglycerin
  • Papaverine
  • Pentaerythritol Tetranitrate
  • Pentoxifylline
  • Propatyl Nitrate
  • Ritonavir
  • Saquinavir
  • Sildenafil
  • Tadalafil
  • Telaprevir
  • Theophylline
  • Vardenafil
  • Vericiguat

Using riociguat with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Clarithromycin
  • Itraconazole

Interactions with food/tobacco/alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other medical problems

The presence of other medical problems may affect the use of riociguat. Make sure you tell your doctor if you have any other medical problems, especially:

  • Bleeding problems—Use with caution. May make this condition worse.
  • Heart or blood circulation problems, severe or
  • Hypotension (low blood pressure) or
  • Hypovolemia (low blood volume)—Use with caution. May increase risk for more serious side effects.
  • Kidney disease, severe or on dialysis or
  • Liver disease, severe or
  • Pulmonary veno-occlusive disease (lung problem)—Use is not recommended.
  • Pulmonary hypertension caused by idiopathic interstitial pneumonia—Should not be used in patients with this condition.

Proper use of riociguat

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 and mix it 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.


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.


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.

Precautions while using riociguat

It is very important that your doctor check your progress at regular visits to make sure riociguat is working properly and to check for unwanted effects. Blood tests may be needed to check for unwanted effects. Your blood pressure should be checked by your doctor every 2 weeks while taking riociguat.

Using riociguat while you are pregnant can cause very serious birth defects. Use a highly effective form of birth control or 2 forms of effective birth control to keep from getting pregnant while you are using riociguat and for at least 1 month after your last dose. The most effective forms of birth control are hormone birth control pills, patches, shots, vaginal rings, or implants, or a vasectomy (for men). One of these forms of birth control should be combined with a condom, a diaphragm, or a cervical cap. If a woman has had a tubal ligation or has an IUD, she does not need to use a second form of birth control. If you think you have become pregnant while using riociguat, tell your doctor right away.

If you are a woman who can get pregnant, you must have a negative pregnancy test before you will be allowed to take riociguat. You will also be required to have a pregnancy test every month during your treatment and for 1 month after treatment with riociguat. If you miss a period while you are using riociguat, tell your doctor right away.

Do not use riociguat together with a nitrate medicine (eg, nitroglycerin) or nitric oxide donor (eg, amyl nitrite). Do not use riociguat together with dipyridamole, theophylline, or medicine for impotence (eg, sildenafil, tadalafil, vardenafil). Using these medicines together may cause hypotension (low blood pressure).

Riociguat could lower your blood pressure and cause you to feel dizzy or lightheaded. Do not drive or do anything else that could be dangerous until you know how riociguat affects you. If you feel dizzy, lie or sit down so you do not faint.

Pulmonary edema (swelling in your lungs) may occur with riociguat. Check with your doctor right away if you have chest pain, difficult, fast, or noisy breathing, blue lips and fingernails, pale skin, increased sweating, coughing that sometimes produces a pink frothy sputum, or shortness of breath.

Tell your doctor if you smoke before taking riociguat.

Do not take other medicines unless thy have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (eg, St. John's wort) or vitamin supplements.

Riociguat side effects

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:

More common

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

Less common

  • 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
  • stomach pain or swelling
  • 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:

More common

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

Less common

  • Difficulty having a bowel movement

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.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.