Riociguat Case Study

Long Island University

Riociguat
(Adempas,Bayer)

Therapeutic class: Cardiovascular Agent, Soluble Guanylate Cyclase Stimulators

Clinical Pharmacology: Sensitizes soluble guanylate cyclase (sGC) to endogenous nitric oxide (NO) by stabilizing the NO-sGC binding. It also directly stimulates sGC independent of NO. Riociguat stimulates the NO-sGC–cyclic guanosine monophosphate (cGMP) pathway and leads to increased generation of cGMP with subsequent vasodilation

Pharmacokinetics:
Absorption:
Time to peak, plasma: 1.5 hours
Bioavailability: Approximately 94%
Distribution:
Volume of distribution is approximately 30 L
Protein binding, plasma: Approximately 95%
Metabolism:
Mainly cleared by metabolism by CYP1A1, CYP3A, CYP2C8, …show more content…
Present most pertinent information concisely for the study using the table format below. There should be 1 study summarized in the table in the completed …show more content…
Consult appropriate manufacturer labeling. Consider therapy modification
- Dabrafenib: May decrease the serum concentration of CYP3A4,2C8 Substrates. Management: Seek alternatives to the CYP3A4,2C8 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification.
- Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Riociguat. Avoid Combination
- Vasodilators (Organic Nitrates): May enhance the hypotensive effect of Riociguat. Avoid combination

Adverse Reactions:
Common:
- Cardiovascular: Hypotension (3-10%)
- CNS: Dizziness (20%), Headache (27%)
- GI: Diarrhea (12%), Dyspepsia (13-19%), Nausea (14%), Vomiting (10%)

Dosage and Administration:
-Adults:
Chronic thromboembolic pulmonary hypertension:
Initial dosage:
1 mg three times daily; 0.5 mg three times daily in patients who may not tolerate the hypotensive effects.
Dosage