DUZALLO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DUZALLO (DUZALLO).
DUZALLO (allopurinol) is a xanthine oxidase inhibitor that reduces uric acid production by inhibiting the conversion of hypoxanthine to xanthine and xanthine to uric acid.
| Metabolism | Primarily metabolized by aldehyde oxidase to oxipurinol, the active metabolite. Also metabolized via xanthine oxidase. Bioactivation requires hepatic metabolism. |
| Excretion | Primarily renal excretion (approximately 70% as unchanged drug); biliary/fecal excretion accounts for about 20%; the remainder undergoes hepatic metabolism. |
| Half-life | Terminal elimination half-life is approximately 12 hours (range 10–14 hours), allowing twice-daily dosing for steady-state achievement within 2–3 days. |
| Protein binding | Approximately 95% bound primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 0.3–0.5 L/kg, indicating distribution primarily into extracellular fluid and well-perfused tissues. |
| Bioavailability | Oral bioavailability is 60%–70% (first-pass metabolism); intravenous bioavailability is 100%. |
| Onset of Action | Oral: Onset of clinical effect occurs within 30–60 minutes; intravenous: within 5–10 minutes. |
| Duration of Action | Duration is approximately 8–12 hours after oral administration and 6–8 hours after IV; therapeutic effect may be prolonged in hepatic impairment. |
Adults: 200 mg orally twice daily.
| Dosage form | TABLET |
| Renal impairment | Not recommended in patients with severe renal impairment (eGFR < 30 mL/min/1.73 m²). No dose adjustment required for mild to moderate impairment (eGFR ≥ 30 mL/min/1.73 m²). |
| Liver impairment | No dose adjustment recommended 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 (< 18 years). |
| Geriatric use | No specific dose adjustment required; monitor renal function due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DUZALLO (DUZALLO).
| Breastfeeding | Allopurinol and its metabolite oxypurinol are excreted into breast milk. M/P ratio: 1.4 for allopurinol, 2.5 for oxypurinol. No adverse effects reported in infants; compatible with breastfeeding, but monitor infant for rash. |
| Teratogenic Risk | DUZALLO (allopurinol) is generally considered low risk. First trimester: limited data, no increased malformations. Second/third trimester: no known fetal harm. However, use only if clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
There is no FDA black box warning for DUZALLO.
| Serious Effects |
["Hypersensitivity to allopurinol or any component of the formulation","Concomitant use with didanosine"]
| Precautions | ["Hypersensitivity reactions including Stevens-Johnson syndrome and toxic epidermal necrolysis","Acute gout flare upon initiation; may require prophylactic anti-inflammatory therapy","Renal impairment: dose adjustment required","Hepatic toxicity may occur","Elevated risk of skin rash with concurrent amoxicillin or ampicillin use"] |
| Food/Dietary | Avoid grapefruit and grapefruit juice due to potential CYP3A4 inhibition increasing elagolix levels. High-fat meals may slightly increase elagolix absorption but no dose adjustment needed. No other significant food interactions reported. |
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| Monitor maternal serum uric acid levels, liver function, renal function (creatinine). Fetal ultrasound for growth if used in pregnancy. Watch for hypersensitivity reactions (e.g., rash, fever). |
| Fertility Effects | No known adverse effects on fertility in animal studies. Human data insufficient; unlikely to impair reproductive function. |
| Clinical Pearls | DUZALLO (elagolix/estradiol/norethindrone acetate) is a GnRH antagonist combination product for management of heavy menstrual bleeding in premenopausal women with uterine leiomyomas. Monitor bone mineral density with prolonged use beyond 6 months; avoid in patients with osteoporosis risk factors. Contraindicated with strong CYP3A4 inhibitors and in pregnancy. Assess for mood changes and depression. Use effective non-hormonal contraception during treatment. |
| Patient Advice | Take one tablet daily at approximately the same time with or without food. · Missing doses increases risk of pregnancy and reduces effectiveness for bleeding control. · Use effective non-hormonal contraception (e.g., condoms, copper IUD) during treatment and for 2 weeks after discontinuation. · Report severe headache, chest pain, or vision changes immediately (risk of thromboembolic events). · Notify your doctor if you suspect pregnancy or develop heavy bleeding, worsening depression, or jaundice. · Bone density may decrease; calcium and vitamin D supplementation is recommended. · Avoid grapefruit or grapefruit juice during treatment. |