CALDEROL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CALDEROL (CALDEROL).
Vitamin D analog; binds to vitamin D receptors, increasing calcium absorption in intestines and promoting bone mineralization.
| Metabolism | Hydroxylated in liver to 25-hydroxyvitamin D; further hydroxylated in kidney to active 1,25-dihydroxyvitamin D. |
| Excretion | Primarily fecal (biliary) as unchanged drug and metabolites (approx. 80%); renal excretion accounts for less than 20%. |
| Half-life | Terminal elimination half-life is approximately 20-30 hours; clinically, steady-state is achieved within 5-7 days. |
| Protein binding | Approximately 99% bound to serum proteins, primarily to vitamin D-binding protein (DBP) and albumin. |
| Volume of Distribution | Vd is approximately 0.4 L/kg; reflects distribution into total body water with negligible storage in fat. |
| Bioavailability | Oral bioavailability of calcitriol is approximately 70-90%. |
| Onset of Action | Oral: calcitriol peak serum levels at 3-6 hours; pharmacodynamic effects (e.g., intestinal calcium absorption) begin within 2-6 hours. |
| Duration of Action | Duration of pharmacodynamic effect (e.g., increased calcium absorption) lasts 24-48 hours after a single oral dose. |
Oral: 0.25-0.5 mcg once daily; titration up to 1 mcg daily based on serum calcium levels. Intravenous: 0.5-2 mcg bolus; maintenance 0.5-2 mcg daily.
| Dosage form | CAPSULE |
| Renal impairment | eGFR <30 mL/min/1.73m2: reduce dose by 50% and monitor calcium/phosphate levels; eGFR <15 mL/min/1.73m2: avoid use due to risk of hypercalcemia. |
| Liver impairment | Child-Pugh class B or C: reduce initial dose by 50% and titrate slowly; monitor calcium and albumin levels. |
| Pediatric use | For hypocalcemia: 0.05-0.1 mcg/kg/day PO, titrated in 0.05 mcg/kg increments every 2-4 weeks; not recommended for IV use in neonates. |
| Geriatric use | Start at the lowest adult dose (0.25 mcg PO daily); increase cautiously due to reduced renal function; monitor serum calcium and renal function frequently. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CALDEROL (CALDEROL).
| Breastfeeding | Excreted in breast milk; M/P ratio unknown. Potential for adverse vascular effects in infants. Contraindicated in breastfeeding due to risk of ductus arteriosus constriction. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: Potential for cardiac malformations (case reports). Second/third trimester: Risk of premature closure of ductus arteriosus, oligohydramnios, and pulmonary hypertension. Avoid use after 20 weeks gestation. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypercalcemia","Vitamin D toxicity","Malabsorption syndrome","Severe renal impairment"]
| Precautions | ["Hypercalcemia","Hypercalciuria","Renal impairment","Monitoring of serum calcium and phosphorus required"] |
| Food/Dietary | Avoid high-calcium foods or supplements unless directed. Vitamin D analogs may alter calcium absorption. No specific food restriction. |
| Clinical Pearls | Calderol (calcifediol) is a vitamin D analog used for renal osteodystrophy. Monitor serum calcium and phosphate levels; do not use with severe hypercalcemia or vitamin D toxicity. Dose adjustment needed in dialysis patients. |
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| Assess fetal echocardiography and amniotic fluid index before and during therapy. Monitor maternal renal function, blood pressure, and platelet count. Discontinue if ductal constriction or oligohydramnios develops. |
| Fertility Effects | In animal studies, high doses associated with impaired ovulation and fetal loss. Human data limited; may theoretically affect implantation due to anti-prostaglandin activity. |
| Patient Advice | Take exactly as prescribed; do not take extra doses. · Avoid calcium supplements and antacids without consulting your doctor. · Report symptoms of hypercalcemia: nausea, vomiting, constipation, weakness, confusion. · Not for use in children. · Store at room temperature away from light and moisture. |