Pronunciation:

rye-oh-SIG-ue-at

Brand Names:

• Adempas

Dosage Forms:

• Tablet

Warnings:

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 .

Classifications:

Therapeutic—

Cardiovascular Agent

Pharmacologic—

Soluble Guanylate Cyclase Stimulator

Uses of This Medicine:

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.

This medicine 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 This Medicine:

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 this medicine, the following should be considered:

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine 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.

Children—

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.

Older adults—

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 this medicine than younger adults, which may require caution in patients receiving riociguat.

Breast-feeding—

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.

Other 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 this medicine, 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 this medicine 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
• Cobicistat
• Dipyridamole
• Dyphylline
• Erythrityl Tetranitrate
• Isosorbide
• Isosorbide Dinitrate
• Isosorbide Mononitrate
• Lopinavir
• Nelfinavir
• Nitric Oxide
• Nitroglycerin
• Papaverine
• Pentaerythritol Tetranitrate
• Pentoxifylline
• Propatyl Nitrate
• Ritonavir
• Saquinavir
• Sildenafil
• Tadalafil
• Telaprevir
• Theophylline
• Vardenafil
• Vericiguat

Using this medicine 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.

• Avacopan
• Carbamazepine
• Clarithromycin
• Conivaptan
• Itraconazole
• Ketoconazole
• Letermovir
• Nirmatrelvir
• Tazemetostat

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Abacavir
• Mavacamten

Other interactions—

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. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is not recommended. Your doctor may decide not to treat you with this medication, change some of the other medicines you take, or give you special instructions about the use of food, alcohol, or tobacco.

• Caffeine

Other medical problems—

The presence of other medical problems may affect the use of this medicine. 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 This Medicine:

Take this medicine 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.

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

You may take this medicine 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.

Dosing—

The dose of this medicine 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 this medicine. 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 this medicine, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

If you missed taking this medicine 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.

Precautions While Using This Medicine:

It is very important that your doctor check your progress at regular visits to make sure this medicine 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 this medicine.

Using this medicine 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 this medicine 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 this medicine, 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 this medicine. You will also be required to have a pregnancy test every month during your treatment and for 1 month after treatment with this medicine. If you miss a period while you are using this medicine, tell your doctor right away.

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

This medicine 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 this medicine affects you. If you feel dizzy, lie or sit down so you do not faint.

Pulmonary edema (swelling in your lungs) may occur with this medicine. 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 this medicine.

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.

Side Effects of This Medicine:

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.