Riociguat (Oral Route)

Riociguat is used for treating pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension by reducing blood pressure in the lungs, helping the heart pump blood much better.

Overview

Riociguat (brand name Adempas) helps lower blood pressure in the lungs, allowing the heart to pump blood more effectively.

It is used for treating pulmonary arterial hypertension as well as chronic thromboembolic pulmonary hypertension in people who’ve had surgery but symptoms still remain, or those who can’t be treated through surgery. In both cases, Riociguat can improve the symptoms of both conditions and help you exercise.

Adempas is available to female patients only under a certain special program from certified pharmacies. To access the medication, you must be enrolled in that program and know the pros and cons of using this medication.

Riociguat can also be taken for other reasons not covered in this medicine guide.

Women must not be pregnant before starting Riociguat treatment. They’ll have to test for pregnancy.

Riociguat may trigger birth defects. Don’t take it if you’re pregnant. Be sure to prevent pregnancy while using the medicine and for about one month after your final dose. Don’t have sex without a condom.

Tell your healthcare professional about all your current medications and any you stop or start taking. Many medications may interact with Adempas, and some medications shouldn’t be taken together. Your doctor might need to alter your treatment program if you take any of these medications:

  • Theophylline
  • Dipyridamole
  • Erectile dysfunction medication such as Cialis, Viagra, Levitra, etc.
  • A nitrate medication for heart problems or chest pain (nitroglycerin, amyl nitrite, etc.)
  • Other medications to treat PAH (pulmonary arterial hypertension) such as Revatio, Adcirca

You shouldn’t use Adempas if you’re allergic to it.

Don’t use Adempas if you have pulmonary arterial hypertension associated with a condition known as idiopathic interstitial pneumonias, or simply PH-IIP.

To ensure that you can safely take Riociguat, inform your physician:

  • If you have low blood pressure
  • If you have blood circulation problems or heart disease
  • If you have pulmonary veno-occlusive disease
  • If you have kidney disease (or are on dialysis)
  • If you have liver disease
  • If you’ve recently coughed up blood or bled from your lungs
  • If you’re dehydrated
  • If you smoke cigarettes

Conditions Treated

  • Pulmonary arterial hypertension
  • Chronic pulmonary hypertension following pulmonary embolism

Type of Medicine

  • Cardiovascular agent

Side Effects

Unusual tiredness, fainting, heartburn, dizziness, headache, lightheadedness, nausea, vomiting, indigestion, or diarrhea can happen. If any of the above effects worsen or continue, inform your pharmacist or physician promptly.

To lower the risk of lightheadedness and dizziness, get up slowly from your chair or bed.

Remember that your healthcare professional has prescribed Riociguat because he/she has deemed its benefit to be greater than the potential for side effects. The majority of people taking Riociguat don’t develop serious side effects.

The medication rarely causes severe bleeding. If you have any of these rare but serious symptoms of bleeding, report them to your doctor immediately:

  • Unusual vaginal bleeding
  • Coughing up blood
  • Signs of intestinal/stomach bleeding (e.g. bloody/black stools, vomit that has blood or resembles coffee grounds)
  • Bleeding around catheter area
  • Symptoms of bleeding in your brain (e.g. severe headache, vision problems, weakness on the side of your body, confusion, slurred speech)

Riociguat rarely triggers a severe allergic reaction. However, seek medical assistance promptly if you have any of these symptoms of a severe allergic reaction:

  • Rash
  • Itching or swelling (mainly of the throat/tongue/face)
  • Troubled breathing
  • Severe dizziness

Some people may suffer different side effects to those listed above. See your healthcare specialist if you have any symptom that concerns you while you’re using Riociguat.

This isn’t a full list of potential Riociguat side effects. If you experience other effects not mentioned here, call up your doctor and pharmacist.

Dosage

The recommended starting Riociguat dose is 1 milligram taken thrice a day for 14 days. You can take Riociguat with food or without, but you should space it about 6-8 hours apart. Your physician will increase the dose gradually provided your blood pressure doesn’t drop drastically or other effects aren’t tolerated. Your total dose per day shouldn’t exceed 7.5 milligrams (2.5 milligrams taken thrice a day).

Many factors may affect the Riociguat dose you need, including other medicines, other medical conditions, and body weight. If your healthcare provider has recommended a different dose from the ones mentioned here, don’t change your way of taking Riociguat without your doctor’s knowledge.

It’s very important to take Riociguat exactly as instructed by your healthcare provider. Don’t suddenly stop taking Riociguat, unless you’re suffering serious side effects. Talk to your doctor about discontinuing this medication if you feel it’s necessary to do so.

If you’ve missed a dose, continue with your normal dosing schedule and skip that dose. Don’t take double doses to offset missed doses. If you don’t know what to do when you’ve missed a dose, seek advice from your doctor. If your Riociguat treatment has been disrupted by at least 3 days, contact your healthcare provider before resuming treatment.

If you have problems with swallowing a Riociguat tablet, crush it and then mix with applesauce or water. Take it immediately.

If you’re taking an antacid that has magnesium or aluminum, take it an hour after taking Adempas.

Use Riociguat regularly to maximize its benefit. Take it at similar intervals daily so you can remember.

Don’t use Riociguat more times than prescribed or increase your dose. Your condition won’t improve any quicker, and your risk for side effects will go up.

Tell your healthcare professional if your condition worsens or doesn’t improve.

Interactions

Riociguat may interact with any of the medications listed below:

  • Amiodarone
  • Oxcarbazepine
  • Phenytoin
  • Anagrelide
  • Bosentan
  • Carvedilol
  • Dabrafenib
  • Rifabutin
  • Primidone
  • Quinidine
  • Cyclosporine
  • Clarithromyocin
  • Rifampin
  • Roflumilast
  • Tacrolimus
  • Tamoxifen
  • Deferasirox
  • St John’s wort
  • Telaprevir
  • Theophylline
  • Tocilizumab
  • Dexamethasone
  • Gefitinib
  • Erlotinib
  • Enzalutamide
  • Grapefruit juice
  • Verapamil
  • Milrinone
  • Nitrates (nitroglycerin, isosorbide dinitrate)
  • HIV protease inhibitors (ritonavir, indinavir, atazanavir)
  • “Azole” antigungals (ketoconazole, voriconazole, itraconazole)
  • Proton pump inhibitors (omeprazole, lansoprazole)
  • Phosphodiesterase 5 inhibitors (tadalafil, sildenafil, vardenafil)
  • Tyrosine kinase inhibitors (imatinib, erlotinib)

When two drugs interact, it doesn’t necessarily mean you must discontinue one of them. Consult your healthcare provider about how any medicine interactions should be controlled or how they’re being controlled.

Drugs other than those mentioned above can interact with Riociguat. Report all kinds of medications you’re using to your doctor. Also report any supplements you’re using. Since alcohol, cigarettes, caffeine, or street drugs may interact with many medicines and affect their action, please inform your prescriber if you take them.

Warnings

It’s crucially important that your healthcare provider monitors your progress regularly to ensure Riociguat is working well and to test for undesirable effects. You may need blood tests to test for undesirable effects. Your doctor should check your blood pressure every 14 days while you’re using Riociguat.

Using Riociguat while you’re pregnant may lead to severe birth defects. Make use of two effective birth control forms to prevent pregnancy while you’re taking Riociguat and for around a month after you complete the treatment.

The most effective birth control forms include hormone-based birth control pills, vaginal rings, shots, patches, or implants for women, and vasectomy for males. You should combine one of these methods with a condom, a cervical cap, or a diaphragm. If you have an IUD or a tubal ligation, you don’t have to use another birth control method. If you think you’ve gotten pregnant while using Riociguat, inform your doctor promptly.

If you’re a woman of child-bearing age, your pregnancy test must be negative before you’re allowed to use Riociguat. In addition, you must take a pregnancy test every month you’re under treatment and a month after discontinuing treatment. If you don’t see your period while taking Riociguat, inform your doctor immediately.

Tell your pharmacist and physician what other medications (prescription and non-prescription), nutritional supplements, herbal products, and vitamins you’re using or plan to use. Make sure to state any of these: certain antifungal medications such as ketoconazole (Xolegel, Extina, Nizoral), itraconazole (Sporanox, Onmel); certain seizure medications like Carbamazepine (Equetro, Epitol, Tegretol, etc.), Phenytoin (Phenytek, Dilantin), and Phenobarbital; HIV protease inhibitors like Ritonavir (in Kaletra, Norvir); and blood pressure medications. Your healthcare provider may need to adjust your doses of drugs or carefully check on you for side effects.

Don’t take this medication together with nitric oxide donor (e.g. amyl nitrite) or other nitrate medication like nitroglycerin. Don’t take Riociguat together with theophylline, dipyridamole, or impotence medicine (such as vardenafil, sildenafil, or tadalafil). Using these medications together may lead to low blood pressure, also known as hypotension.

Riociguat may make your blood pressure go down and make you feel lightheaded or dizzy. Avoid using machines, driving a vehicle, or doing any task that might be hazardous until you understand how Riociguat affects you. And if you’re feeling dizzy after taking Riociguat, sit or lie down so you don’t faint.

This medicine may cause pulmonary edema. See your doctor straight away if you suffer chest pain, noisy, fast, or difficult breathing occasionally with wheezing, pale skin, blue fingernails and lips, increased sweating, shortness of breath, or coughing that occasionally produces pink foamy sputum.

If you’re using antacids containing magnesium hydroxide (Mylanta, Maalox, Tums, etc.) or aluminum hydroxide, use them one hour prior to or after using Riociguat.

Report all herbal products you’re using to your doctor, particularly St John’s wort.

If you have pulmonary hypertension related to idiopathic interstitial pneumonia, or PH-IIP in short, tell your doctor. He or she will likely tell you to stop taking Riociguat.

Let your healthcare professional know if you smoke now or stop or start smoking during treatment. In addition, let the healthcare professional know if you’ve recently had vomiting, diarrhea, or profuse sweating which may have led to dehydration (significant loss of body fluids); if you have hypotension, if you’ve recently bled in your lungs; if you have liver, kidney, or heart disease; if you have pulmonary veno-occlusive disease (blocked veins in your lungs); or if you’ve had treatment to stop coughing blood.

If you’re breastfeeding, inform your doctor. You should never breastfeed while taking Riociguat. The drug gets into breast milk and can affect your baby.

Don’t use other medications unless you’ve discussed them with your healthcare specialist. This includes over-the-counter (OTC) or prescription medicines, vitamin supplements, or herbal products like St John’s wort.

Storage

Keep Riociguat in a sealed container. Keep the medicine at room temperature. Protect Riociguat from direct light, moisture, and heat, and protect the medicine from freezing.

Keep Riociguat away from children and don’t keep medicines you no longer use or outdated ones. Find out from your healthcare provider how you should discard any medicine you don’t use.

Summary

Riociguat is only given to women under a special plan from a certified chemist. You must not be pregnant before you start this treatment.

Don’t give Riociguat to anybody else, regardless of whether they show symptoms like yours. It may be hazardous for anyone to take Riociguat if their healthcare provider hasn’t prescribed it.

Your doctor may recommend Riociguat for other conditions not discussed in this medication guide. If you have no idea why you’re taking Riociguat or haven’t discussed it with your doctor, please talk to him or her. Don’t stop using Riociguat without your healthcare provider’s knowledge.

Medical and/or lab tests (for example pregnancy, blood pressure tests) must be carried out periodically to check on your progress or for side effects. For more details, consult your healthcare provider.

Don’t miss any appointment with your healthcare provider. Your doctor will regularly check your blood pressure during your Riociguat treatment.

Always use protection during sex if you’re taking Riociguat. You must prevent pregnancy with birth control during your treatment and for a month after you stop using Riociguat.

If you’re the guardian or parent of a female kid taking Riociguat, make sure to speak to the doctor as soon as you spot signs of puberty (such as pubic hair or breast development), even if monthly periods haven’t started yet.

Riociguat can bring about dizziness and may affect your reactions and thinking. Do not operate any machine or drive until you have an idea of how Riociguat affects you. Don’t get up too quickly from your chair or bed or you could feel dizzy. Just rise slowly and stabilize yourself to avoid a fall.

Smoking may make this medication less effective. Inform your doctor if you stop or start smoking while you’re using Riociguat. Your doctor may need to adjust your dose.

This medicine can be taken for other reasons. For more information, consult your doctor and pharmacist.

 

Resources
Last Reviewed:
January 29, 2018
Last Updated:
February 10, 2018
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