Oral Chronic heart failure with reduced ejection fraction
Adult: To reduce the risk of CV death and heart failure hospitalisation in patients who are stabilised following a recent decompensation event requiring IV treatment: In conjunction with other heart failure treatments: Initially, 2.5 mg once daily, then double the dose approx every 2 weeks to the target maintenance dose of 10 mg once daily according to the patient's tolerance. If the patient experiences tolerability issues based on blood pressure, temporary dose reduction or discontinuation of therapy is recommended.
What are the brands available for Vericiguat in Philippines?
Vericiguat Should be taken with food. For patients w/ difficulty swallowing, tab may be crushed & mixed w/ water immediately before administration.
Contraindications
Pregnancy. Concomitant use with other soluble guanylate cyclase stimulators (e.g. riociguat).
Special Precautions
Patient with hypovolaemia, severe left ventricular outflow obstruction, autonomic dysfunction, resting hypotension, and history of hypotension. Not studied in patients with systolic blood pressure <100 mmHg at therapy initiation; some countries recommend that vericiguat should not be initiated if systolic blood pressure is <100 mmHg. Concomitant use with phosphodiesterase type 5 (PDE-5) inhibitors. Not recommended to be used in patients with severe hepatic impairment, eGFR <15 mL/min/1.73 m2 at treatment initiation, or those undergoing dialysis. Lactation.
Adverse Reactions
Significant: Symptomatic hypotension. Blood and lymphatic system disorders: Anaemia. Gastrointestinal disorders: Dyspepsia, nausea, vomiting, GERD. Nervous system disorders: Headache, dizziness.
PO: Z (Should not be used during pregnancy or contraindicated (manufacturer specific))
Patient Counseling Information
This drug may cause dizziness, if affected, do not drive or operate machinery. Women of childbearing potential must use proven birth control methods during therapy and for 1 month after stopping the treatment.
Monitoring Parameters
Verify pregnancy status in women of childbearing potential prior to treatment initiation. Monitor blood pressure and daily weights before and during therapy.
May enhance the adverse effects with other soluble guanylate cyclase stimulators (e.g. riociguat). May increase the risk of symptomatic hypotension with PDE-5 inhibitors (e.g. sildenafil).
Food Interaction
Increased bioavailability with food.
Action
Description: Mechanism of Action: Vericiguat is a stimulator of soluble guanylate cyclase (sGC), the essential enzyme in the nitric oxide (NO) signalling pathway. Heart failure is associated with impaired NO synthesis and reduced sGC activity causing a deficiency in sGC-derived cyclic guanosine monophosphate (cGMP), which in turn contributes to myocardial and vascular dysfunction. Vericiguat directly stimulates the sGC (independently and synergistically with NO), thereby enhancing the cGMP production. The increased levels of cGMP results in smooth muscle relaxation and vasodilation. Pharmacokinetics: Absorption: Increased bioavailability with food. Absolute bioavailability: 93% (with food). Time to peak plasma concentration: 4 hours (with food); 1 hour (fasted state). Distribution: Plasma protein binding: Approx 98%, mainly to serum albumin. Metabolism: Metabolised via glucuronidation primarily by UGT1A9 and to a lesser extent by UGT1A1 to form N-glucuronide (inactive metabolite). Excretion: Via urine (approx 53% as inactive metabolite); faeces (45% as unchanged drug). Elimination half-life: 30 hours.
Chemical Structure
Vericiguat Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 54674461, Vericiguat. https://pubchem.ncbi.nlm.nih.gov/compound/Vericiguat. Accessed July 29, 2024.