VOQUEZNA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VOQUEZNA (VOQUEZNA).
Potassium-competitive acid blocker (PCAB) that reversibly inhibits the H+/K+ ATPase pump in gastric parietal cells, suppressing both fasting and stimulated gastric acid secretion.
| Metabolism | Primarily metabolized by CYP3A4 and to a lesser extent by CYP2B6, CYP2C19, and CYP2D6. |
| Excretion | Primarily renal (approximately 90% of absorbed dose excreted unchanged in urine) with minimal biliary/fecal elimination (<5%). |
| Half-life | Terminal elimination half-life is approximately 2-3 hours in adults; no clinically relevant accumulation with once-daily dosing. |
| Protein binding | Approximately 98% bound to serum proteins, primarily albumin and alpha1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 12-18 L (0.15-0.25 L/kg in adults), indicating minimal extravascular distribution and limited tissue penetration. |
| Bioavailability | Absolute oral bioavailability is approximately 80-90% after oral administration, with no clinically relevant food effect. |
| Onset of Action | Onset of acid suppression occurs within 30-60 minutes after oral administration; maximal effect on intragastric pH is observed within 2-3 days of repeated dosing. |
| Duration of Action | Duration of acid suppression lasts approximately 12-24 hours with once-daily dosing, allowing for pH control over 24 hours; longer duration seen in CYP2C19 poor metabolizers. |
10 mg orally once daily; may increase to 20 mg once daily if inadequate response after 8 weeks.
| Dosage form | TABLET |
| Renal impairment | No dosage adjustment required for mild to moderate renal impairment. Not recommended in severe renal impairment (eGFR <30 mL/min/1.73 m²). |
| Liver impairment | No dosage adjustment for mild hepatic impairment (Child-Pugh A). Not recommended in moderate or severe hepatic impairment (Child-Pugh B or C). |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No dosage adjustment required; monitor for adverse effects in elderly patients with reduced renal or hepatic function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for VOQUEZNA (VOQUEZNA).
| Breastfeeding | No data on presence in human milk, effects on breastfed infant, or milk production. Vonoprazan is excreted in rat milk at concentrations similar to maternal plasma; M/P ratio unknown. Due to potential for adverse reactions in nursing infants (e.g., diarrhea, metabolic alkalosis), advise against breastfeeding or discontinue drug, considering importance to mother. |
| Teratogenic Risk | No adequate and well-controlled studies in pregnant women. Animal reproduction studies with vonoprazan fumarate (the active ingredient) have not been conducted at clinically relevant exposures. Based on its mechanism of acid suppression, theoretical risk of fetal electrolyte and metabolic disturbances exists if maternal acid-base balance is altered. In first trimester, avoid unless clearly needed; second and third trimesters, use only if potential benefit justifies fetal risk, as no evidence of structural anomalies. Limited human data preclude definitive risk assessment. |
■ FDA Black Box Warning
No FDA black box warnings.
| Serious Effects |
["Hypersensitivity to vonoprazan or any component of the formulation"]
| Precautions | ["Acute interstitial nephritis","Clostridioides difficile-associated diarrhea","Bone fracture (with high dose or prolonged use)","Cutaneous and systemic lupus erythematosus","Cyanocobalamin (vitamin B12) deficiency with prolonged use","Hypomagnesemia with prolonged use","Interference with laboratory tests (e.g., chromogranin A, secretin stimulation testing)","Increased risk of gastric cancer (from long-term use, based on observational studies)","Severe cutaneous adverse reactions (e.g., Stevens-Johnson syndrome)"] |
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| Fetal Monitoring | Monitor maternal acid-base status, electrolytes, and renal function if used chronically in pregnancy. In infants exposed in utero, observe for signs of electrolyte imbalance (e.g., hypocalcemia, hypomagnesemia) and metabolic alkalosis postnatally. |
| Fertility Effects | Animal studies with vonoprazan showed no impairment of fertility in male or female rats at doses up to 6 mg/kg/day (approximately 1.7 times human AUC at 20 mg). No human data on fertility effects. |