- March 15, 2022
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Brand Name :
Adempas
Synonyms :
riociguat
Class :
Soluble Guanylate Cyclase Stimulators
Dosage forms & Strengths:
Adult:
Tablet
0.5 mg
1 mg
1.5 mg
2 mg
2.5 mg
Safety and efficacy are not seen in pediatrics
Refer to the adult dosing
riociguat: they may diminish the serum concentration of antacids
riociguat: they may diminish the serum concentration of antacids
riociguat: they may diminish the serum concentration of antacids
riociguat: they may diminish the serum concentration of antacids
riociguat: they may diminish the serum concentration of antacids
may have an increased hypotensive effect when combined with riociguat
may have an increased hypotensive effect when combined with riociguat
may have an increased hypotensive effect when combined with riociguat
may have an increased hypotensive effect when combined with riociguat
may have an increased hypotensive effect when combined with riociguat
may have an increased hypotensive effect when combined with nitroprusside
CYP3A strong enhancers of the small intestine may reduce the bioavailability of riociguat
amyl nitrite: they may increase the hypotensive effect when combined with riociguat
products containing roflumilast increase the effect of hypotension of riociguat
The presence of magnesium hydroxide lowers riociguat levels by inhibiting its gastrointestinal absorption
It may enhance the effect when combined with tafamidis meglumine
the effect of riociguat is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
Actions and Spectrum:
Stimulates (sGC) soluble guanylate cyclase
Nitric oxide binds to sGC, hence catalyzing the production of cGMP
>10%:
Dyspepsia and gastritis (21%)
Dizziness (20%)
Headache (27%)
Diarrhea (12%)
Nausea (14%)
1-10%:
Vomiting (10%)
Constipation (5%)
Hypotension (10%)
Heavy bleeding (2.4%)
Anemia (7%)
GERD (5%)
Hemoptysis (1%)
Black Box Warning:
It is essential to follow the dosage and administration instructions for the medication carefully.
Contraindication/Caution:
riociguat should not be used in people hypersensitive to the drug itself.
Pregnancy consideration:
Females of reproductive potential are advised not to become pregnant during the treatment.
Breastfeeding warnings:
No data is available regarding the presence of the drug in breast milk.
Pregnancy category:
Pharmacology
The pharmacology of riociguat is based on its ability to stimulate soluble guanylate cyclase (sGC). This enzyme is crucial in regulating blood vessel tone and blood flow. By increasing the production of (cGMP) in the body, riociguat relaxes the smooth muscles, leading to the dilation of the vessels. It improves blood flow to various organs, including the lungs, which can reduce the symptoms of pulmonary hypertension and CTEPH.
Pharmacodynamics:
riociguat is also found to have anti-inflammatory and anti-fibrotic effects, which may contribute to its therapeutic effects in pulmonary hypertension and CTEPH.
Pharmacokinetics:
The Pharmacokinetics of riociguat can be affected by certain drugs, such as potent inhibitors or inducers of CYP3A4, which can change the metabolism and elimination of the drug. Therefore it’s essential to monitor the patients who are taking those drugs and adjust the riociguat dose accordingly.
Absorption
The bioavailability of riociguat is 94%
Distribution
The volume of distribution is 30L
Metabolism
riociguat is metabolized in the liver by the cytochrome P450 enzymes, majorly by CYP3A4 and, minorly, by CYP2C8. The main metabolite of riociguat is N-desethyl-riociguat. This metabolite is pharmacologically active and has similar properties to the parent drug, but it has a longer half-life (around 10 hours) than riociguat.
Elimination and excretion
The half-life of the drug is 12 hours. The systemic clearance rate is 1.8L/hr. And the drug is excreted in urine and feces (40 and 53) %.
Administration:
riociguat is taken orally as tablets. If you miss a dose, continue it with the next scheduled dose.
If a missed dose gap is more than 3 days, re-titrate the dose.
Patient information leaflet
Generic Name: riociguat
Pronounced: rye-oh-sig-ue-at
Why do we use riociguat?
riociguat is used to treat Chronic-thromboembolic Pulmonary Hypertension or Arterial Pulmonary Hypertension.
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