Riociguat

Riociguat is a  prescription medication used for the treatment of Chronic-thromboembolic Pulmonary Hypertension (CTEPH)/ Arterial Pulmonary Hypertension (PAH).

• Riociguat is available under the following different brand names: Adempas

Common side effects of Riociguat include:

• headache,
• dizziness,
• indigestion,
• upset stomach or stomach pain,
• swelling of the legs and feet,
• nausea,
• diarrhea,
• nausea,
• vomiting,
• dizziness,
• low blood pressure (hypotension),
• low levels of iron in the blood (anemia),
• gastroesophageal reflux disease (GERD),
• constipation,
• palpitations,
• stuffy nose,
• nosebleed,
• difficulty swallowing,
• abdominal bloating, and
• swelling of the extremities.

Serious side effects of Riociguat include:

• hives,
• difficult breathing
• swelling of the face, lips, tongue, or throat.
• a light-headed feeling,
• abnormal vaginal bleeding, or any other unusual bleeding,
• vomiting or coughing up bright red blood, or vomit that looks like coffee grounds,
• low red blood cells (anemia)--pale skin, unusual tiredness, feeling light-headed or short of breath, cold hands and feet,
• a build-up of fluid in the lungs--anxiety, sweating, pale skin, severe shortness of breath, wheezing, gasping for breath, cough with foamy mucus, chest pain, fast or uneven heart rate.

Rare side effects of Riociguat include:

• none 

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablet

• 0.5mg
• 1mg
• 1.5mg
• 2mg
• 2.5mg

Chronic-thromboembolic Pulmonary Hypertension (CTEPH)/ Arterial Pulmonary Hypertension (PAH)

Adult dosage

• Initial dose: 1 mg orally thrice a day; consider 0.5 mg orally thrice a day if the patient may not tolerate the hypotensive effect
• If systolic blood pressure is above 95 mmHg and no symptoms of hypotension, up-titrate the dose by 0.5 mg orally thrice a day with dose increases no sooner than 2 weeks apart to the highest tolerated dose (not to exceed 2.5 mg orally thrice a day)
• If symptoms of hypotension occur, decrease the dose by 0.5 mg thrice daily

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first

• Riociguat has severe interactions with the following drugs:
  • amyl nitrite
  • avanafil
  • dipyridamole
  • isosorbide dinitrate
  • isosorbide mononitrate
  • nitroglycerin IV
  • nitroglycerin PO
  • nitroglycerin sublingual
  • nitroglycerin transdermal
  • nitroglycerin translingual
  • sildenafil
  • tadalafil
  • theophylline
  • vardenafil
  • vericiguat
• Riociguat has serious interactions with at least 71 other drugs.
• Riociguat has moderate interactions with at least 77 other drugs.
• Riociguat has minor interactions with the following drug:
  • ribociclib

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Pregnancy (see Black Box Warnings)
• Coadministration with nitrates or nitric oxide donors (e.g., amyl nitrite), PDE inhibitors (e.g., avanafil, sildenafil, tadalafil, vardenafil), or nonspecific PDE inhibitors (e.g., dipyridamole, theophylline) because of additive hypotension
• Administration within 24 hours of sildenafil
• Concomitant use of another soluble guanylate cyclase (sGC) stimulators
• Tadalafil 24 hours before or within 48 hours after riociguat
• Patients with pulmonary hypertension associated with idiopathic interstitial pneumonia

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Riociguat?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Riociguat?”

Cautions

• May cause fetal harm when administered during pregnancy and is contraindicated for use in women who are pregnant (see Black Box Warnings and Contraindications); because of this, females may only receive riociguat via a restricted access program
• Reduces blood pressure; consider the potential for symptomatic hypotension or ischemia in patients with hypovolemia, severe left ventricular outflow obstruction, resting hypotension, or autonomic dysfunction; dose reduction may be required
• Coadministration with strong CYP and P-gp/BCRP inhibitors increases riociguat systemic exposure and increases the risk for hypotension; dose reduction may be required
• Serious bleeding was reported including hemoptysis, vaginal bleeding, catheter site hemorrhage, subdural hematoma, hematemesis, and intra-abdominal hemorrhage
• Pulmonary vasodilators may significantly worsen the cardiovascular status of patients with pulmonary veno-occlusive disease; avoid use in these patients and discontinue if signs of pulmonary edema occur and are confirmed

Adempas REMS Program

• Females can only receive drugs through the Adempas Risk Evaluation and Mitigation Strategy (REMS) Program, a restricted distribution program
• Important requirements of the Adempas REMS Program include the following:
• Prescribers must be certified with the program by enrolling and completing training.
• All females, regardless of reproductive potential, must enroll in Adempas REMS Program before initiating therapy
• Male patients are not enrolled in the Adempas REMS Program
• Female patients of reproductive potential must comply with the pregnancy testing and contraception requirements
• Pharmacies must be certified with the program and must only dispense to patients who are authorized to receive Adempas
• Further information, including a list of certified pharmacies, is available at www.AdempasREMS.com or 1-855-4 ADEMPAS

Pregnancy & Lactation

• Based on data from animal reproduction studies, therapy may cause embryo-fetal toxicity and miscarriage when administered to a pregnant woman and is contraindicated during pregnancy; in reproduction studies with pregnant rabbits, oral administration during organogenesis caused abortions and fetal toxicity at exposures approximately 4 times and 13 times, respectively, the maximum recommended human (MRHD); advise pregnant women of the potential risk to a fetus
• Females of reproductive potential must have a negative pregnancy test before initiation, monthly during, and 1 month after discontinuation of treatment; contraception must also be used during and for 1 month after treatment (see Boxed Warning)
• If pregnancy is suspected, contact a healthcare provider immediately

Lactation

• There are no data on the presence of riociguat in human milk, its effects on the breastfed infant, or milk production; the drug is present in rat milk; because of the potential for serious adverse reactions, such as hypotension, in breastfed infants, advise women not to breastfeed during therapy