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. |
| Molecular Weight | 365.38 |
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 | No adequate human data; animal studies show no teratogenicity at clinically relevant doses. Use only if clearly needed. |
| 2nd trimester | No adequate human data; animal studies show no teratogenicity. Use only if clearly needed. |
| 3rd trimester | No adequate human data; animal studies show no teratogenicity. Use only if clearly needed. |
Clinical note
Comprehensive clinical and safety monograph for VOQUEZNA (VOQUEZNA).
| Placental transfer | Unknown in humans; molecular weight (365.38 Da) suggests potential for placental transfer. |
| Breastfeeding | No human data on excretion in breast milk; consider risk vs benefit. Because of potential for adverse effects in infant, caution advised. |
| Lactation Rating |
■ FDA Black Box Warning
No FDA black box warnings.
| Serious Effects |
History of 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) |
| Food/Dietary | VOQUEZNA may be taken with or without food. Avoid excessive consumption of foods that trigger acid reflux (e.g., spicy, fatty, acidic) during treatment. No specific food-drug interactions reported. |
Loading safety data…
| L3 - Moderately Safe |
| 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. |
| 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. |
| Clinical Pearls | VOQUEZNA (vonoprazan) is a potassium-competitive acid blocker (PCAB) with rapid onset and sustained acid suppression; it does not require activation by gastric acid. Avoid use with atazanavir, nelfinavir, rilpivirine. May increase digoxin levels; monitor. Assess for Clostridioides difficile infection risk with prolonged use. Consider hypomagnesemia with extended therapy (>1 year). |
| Patient Advice | Take VOQUEZNA exactly as prescribed, usually once daily with or without food. · Swallow tablets whole; do not crush or chew. · Notify your healthcare provider if you experience severe diarrhea, rash, or signs of low magnesium (muscle cramps, irregular heartbeat). · Avoid taking with HIV medications (atazanavir, nelfinavir, rilpivirine). · Report any unexpected bruising or bleeding (possible interaction with warfarin). · Do not take over-the-counter acid reducers without consulting your doctor. |