HECTOROL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for HECTOROL (HECTOROL).
Synthetic vitamin D analog that binds to vitamin D receptors (VDR), increasing intestinal absorption of calcium and phosphate, and promoting bone mineralization. Also suppresses parathyroid hormone (PTH) production.
| Metabolism | Hepatic via CYP27A1 and CYP3A4; undergoes further metabolism to active and inactive metabolites. |
| Excretion | Primarily hepatic metabolism followed by biliary excretion; renal excretion accounts for <2% of unchanged drug. |
| Half-life | Terminal elimination half-life is approximately 5.0 hours in healthy adults; prolonged in patients with hepatic impairment. |
| Protein binding | ≥99.9% bound to plasma proteins, primarily vitamin D-binding protein (DBP). |
| Volume of Distribution | 1.4 L/kg; indicates extensive distribution into tissues, including bone and parathyroid glands. |
| Bioavailability | Oral: approximately 70%; limited data available for other routes. |
| Onset of Action | Oral: 2-6 hours for elevation of serum calcium; intravenous: within 12 hours for suppression of PTH. |
| Duration of Action | Oral: 1-2 days for maximal effect on serum calcium; intravenous: up to 4 days for PTH suppression. |
| Molecular Weight | 418.6 |
0.5 to 1.5 mcg intravenously three times weekly during hemodialysis; adjust to maintain serum intact PTH within target range (1.5 to 3 times upper limit of normal). Initial dose: 0.5 mcg three times weekly; may increase by 0.25 to 0.5 mcg at 2- to 4-week intervals.
| Dosage form | CAPSULE |
| Renal impairment | No dose adjustment required for GFR-based impairment; HECTOROL is indicated for patients on chronic hemodialysis. In predialysis CKD, use is not recommended. No specific GFR-based adjustments provided. |
| Liver impairment | No specific dose adjustments for hepatic impairment based on Child-Pugh classification have been established. Use with caution in severe hepatic impairment due to potential altered vitamin D metabolism. |
| Pediatric use | Safety and effectiveness in pediatric patients have not been established; no recommended pediatric dosing available. |
| Geriatric use | No specific dose adjustments for geriatric patients; clinical studies did not include sufficient numbers of subjects aged 65 and over to determine differences in response. Use with monitoring of serum calcium, phosphorus, and intact PTH. |
| 1st trimester | Avoid use during first trimester due to risk of fetal harm based on animal studies; consider alternative therapy. |
| 2nd trimester | Use only if clearly needed; may cause fetal hypercalcemia and suppression of parathyroid function. |
| 3rd trimester | Use only if clearly needed; monitor maternal and fetal serum calcium levels closely; risk of fetal hypercalcemia. |
Clinical note
Comprehensive clinical and safety monograph for HECTOROL (HECTOROL).
| Placental transfer | Crosses placenta in animal studies; in humans, expected to cross due to molecular weight and lipophilicity; evidence limited. |
| Breastfeeding | Excreted in human milk at low levels; monitor infant for signs of hypercalcemia (e.g., vomiting, constipation, irritability). Caution is advised; benefit should outweigh risk. |
■ FDA Black Box Warning
None.
| Serious Effects |
HypercalcemiaVitamin D toxicityKnown hypersensitivity to doxercalciferol or any component
| Precautions | Hypercalcemia and hyperphosphatemia risk; monitor serum calcium and phosphorus levels., Adynamic bone disease with oversuppression of PTH., Digitalis toxicity potentiated by hypercalcemia., Aluminum hydroxide and magnesium-containing antacids may bind to the drug. |
| Food/Dietary | Avoid excessive intake of foods high in calcium (dairy products) and phosphorus (processed foods, cola, nuts) as they may affect therapy. Do not take with antacids containing magnesium or aluminum. Limit alcohol intake as it may interfere with vitamin D metabolism. |
Loading safety data…
| Lactation Rating |
| L3 (Moderately Safe) |
| Teratogenic Risk | Category C. First trimester: Potential risk of hypercalcemia-related fetal harm; limited human data. Second/third trimesters: Risk of fetal hypercalcemia, suppression of fetal parathyroid function, and possible craniofacial malformations at high doses. |
| Fetal Monitoring | Monitor maternal serum calcium, phosphorus, and alkaline phosphatase every 1-2 weeks; fetal ultrasound for signs of hypercalcemia (e.g., nephrocalcinosis, growth restriction); adjust dose to maintain normocalcemia. |
| Fertility Effects | No known direct adverse effects on fertility in animal studies; clinical data insufficient to assess impact on human fertility. |
| Clinical Pearls |
| HECTOROL (doxercalciferol) is a vitamin D2 analog used to manage secondary hyperparathyroidism in chronic kidney disease. Monitor serum calcium, phosphorus, and PTH levels closely; goal is to suppress PTH without causing hypercalcemia or hyperphosphatemia. Do not use with other vitamin D preparations due to additive toxicity. Adjust dose based on PTH and calcium-phosphorus product. |
| Patient Advice | Take exactly as prescribed; do not change dose or stop without consulting your doctor. · Notify your doctor immediately if you experience nausea, vomiting, confusion, or irregular heartbeat (signs of hypercalcemia). · Avoid taking any other vitamin D supplements or medications containing calcium without doctor approval. · Adhere to dietary restrictions on phosphorus and calcium intake as advised by your dietitian. · Keep all laboratory appointments for blood tests to monitor calcium, phosphorus, and PTH levels. |