Riociguat

Drug #2331

Riociguat is methyl 4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo [3,4-b]pyridin-3-yl]-5-pyrimidinyl(methyl carbamate. It is a soluble guanylate cyclase (sGC) stimulator indicated for the treatment of adults with Persistent/recurrent Chronic Thromboembolic Pulmonary Hypertension (CTEPH) (WHO Group 4) after surgical treatment or inoperable CTEPH to improve exercise capacity and WHO functional class.It is also indicated for Pulmonary Arterial Hypertension (PAH) (WHO Group 1) to improve exercise capacity, improve WHO functional class and to delay clinical worsening.

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Primary Characteristics

It is of Synthetic origin.

Molecular Weight: 422.42 · Solubility in Water: soluble at 35C · Non-proprietary name: Riociguat.

Pharmacokinetics

Absorption: Riociguat has an oral bioavailability is 94%.

Distribution: Riociguat has a volume of distribution is 30L. plasma protein binding is 95%.

Elimination: it is metabolised via hepatic, plasma half-life is 7-12hrs, renal excretion is 40% ib urine, 53% in feces.

Indications

Riociguat is primarily indicated in conditions like Chronic thromboembolic pulmonary hypertension, Pulmonary hypertension.

Contraindications

None recorded.

Dosage

Riociguat's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
0 – 0.5 mg	—	Every 8h	PO	For patients who may not tolerate the hypotensive effect of riociguat
1 mg	1 mg	Every 8h	PO	recommended starting dose
2.5 mg	2.5 mg	Every 8h	PO	highest tolerated dose
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

7 interactions

Major3 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Riociguat is known to cause more or less tolerable side effects which are usually transient. These include Anemia, Constipation , Diarrhea, Dizziness, dyspepsia, Gastritis, GI reflux, Headache, Hypotension, Nausea, Vomiting .

Warnings / Precautions

Symptomatic hypotension , Bleeding , Pulmonary edema in patients with pulmonary veno-occlusive disease. If confirmed, discontinue treatment.

Available Brands

None recorded.

Storage Conditions

Riociguat should be stored Tablet.

Drug Classification

1.12.3.7 — Direct vasodilators