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Hectorol
Overview
What is Hectorol?
Doxercalciferol, the active ingredient in Hectorol, is a synthetic vitamin D analog that undergoes metabolic activation to form 1α,25-dihydroxyvitamin D (1α,25-(OH)D), a naturally occurring, biologically active form of vitamin D. Hectorol is available as a sterile, clear, colorless aqueous solution for intravenous injection.
Hectorol single-use injection is supplied in a stoppered 2 mL amber glass vial containing either 4 mcg/2 mL or 2 mcg/mL. Each vial includes an aluminum seal and yellow (4 mcg/2 mL) or green (2 mcg/mL) flip-off cap. Each milliliter (mL) of solution contains doxercalciferol, 2 mcg; ethanol, 100%, 0.05 mL; Polysorbate 20, 10 mg; sodium chloride, 1.5 mg; butylated hydroxytoluene, 0.02 mg; sodium phosphate dibasic, heptahydrate, 14.4 mg; sodium phosphate monobasic, monohydrate, 1.8 mg; and disodium edetate, 1.1 mg.
Hectorol is also supplied as a multi-dose injection contained within a stoppered 2 mL amber glass vial containing 4 mcg/2 mL. Each vial includes an aluminum seal and an orange plastic flip-off cap. Each milliliter (mL) of solution contains doxercalciferol, 2 mcg; ethanol, 100%, 0.075 mL; Polysorbate 20, 10 mg; sodium chloride, 1.5 mg; butylated hydroxytoluene, 0.02 mg; sodium phosphate dibasic, heptahydrate, 14.4 mg; sodium phosphate monobasic, monohydrate, 1.8 mg; and disodium edetate, 1.1 mg.
Doxercalciferol is a colorless crystalline compound with a calculated molecular weight of 412.66 and a molecular formula of CHO. It is soluble in oils and organic solvents, but is relatively insoluble in water. Chemically, doxercalciferol is (1α,3β,5Z,7E,22E)-9,10-secoergosta-5,7,10(19),22-tetraene-1,3-diol and has the structural formula presented in Figure 1.
Other names frequently used for doxercalciferol are 1α-hydroxyvitamin D, 1α-OH-D, and 1α-hydroxyergocalciferol.
What does Hectorol look like?
What are the available doses of Hectorol?
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What should I talk to my health care provider before I take Hectorol?
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How should I use Hectorol?
Hectorol is indicated for the treatment of secondary hyperparathyroidism in patients with chronic kidney disease on dialysis.
For intravenous use only. The optimal dose of Hectorol must be carefully determined for each patient.
The recommended initial dose of Hectorol is 4 mcg administered intravenously as a bolus dose three times weekly (approximately every other day). The initial dose should be adjusted, as needed, in order to lower blood iPTH into the range of 150 to 300 pg/mL. The dose may be increased at 8-week intervals by 1 to 2 mcg if iPTH is not lowered by 50% and fails to reach the target range. Dosages higher than 18 mcg weekly have not been studied. Drug administration should be suspended if iPTH falls below 100 pg/mL and restarted one week later at a dose that is at least 1 mcg lower than the last administered dose. During titration, iPTH, serum calcium, and serum phosphorus levels should be obtained weekly. If hypercalcemia, hyperphosphatemia, or a serum calcium times phosphorus product greater than 55 mg/dL is noted, the dose of Hectorol should be decreased or suspended and/or the dose of phosphate binders should be appropriately adjusted. If suspended, the drug should be restarted at a dose that is 1 mcg lower.
Dosing must be individualized and based on iPTH levels with monitoring of serum calcium and serum phosphorus levels. Table 5 presents a suggested approach in dose titration.
What interacts with Hectorol?
Hectorol should not be given to patients with a tendency towards hypercalcemia or current evidence of vitamin D toxicity.
Hectorol Injection is contraindicated in patients with previous hypersensitivity to doxercalciferol or any of its ingredients (see and ).
What are the warnings of Hectorol?
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Overdosage of any form of vitamin D, including Hectorol is dangerous (see ). Progressive hypercalcemia due to overdosage of vitamin D and its metabolites may be so severe as to require emergency attention. Acute hypercalcemia may exacerbate tendencies for cardiac arrhythmias and seizures and may potentiate the action of digitalis drugs. Chronic hypercalcemia can lead to generalized vascular calcification and other soft-tissue calcification. The serum calcium times serum phosphorus (Ca X P) product should be maintained at <55 mg/dL in patients with chronic kidney disease. Radiographic evaluation of suspect anatomical regions may be useful in the early detection of this condition.
Since doxercalciferol is a precursor for 1α,25-(OH)D, a potent metabolite of vitamin D, pharmacologic doses of vitamin D and its derivatives should be withheld during Hectorol treatment to avoid possible additive effects and hypercalcemia.
Oral calcium-based or other non-aluminum-containing phosphate binders and a low phosphate diet should be used to control serum phosphorus levels in patients undergoing dialysis. Uncontrolled serum phosphorus exacerbates secondary hyperparathyroidism and can lessen the effectiveness of Hectorol in reducing blood PTH levels. If hypercalcemia occurs after initiating Hectorol therapy, the dose of Hectorol and/or calcium-containing phosphate binders should be decreased. If hyperphosphatemia occurs after initiating Hectorol, the dose of Hectorol should be decreased and/or the dose of phosphate binders increased. (See dosing recommendations for Hectorol under ).
Magnesium-containing antacids and Hectorol should not be used concomitantly in patients on chronic renal dialysis because such use may lead to the development of hypermagnesemia.
Serious hypersensitivity reactions, including fatal outcome, have been reported post marketing in patients on hemodialysis following administration of Hectorol Injection. Hypersensitivity reactions include anaphylaxis with symptoms of angioedema (involving face, lips, tongue and airways), hypotension, unresponsiveness, chest discomfort, shortness of breath, and cardiopulmonary arrest. These reactions may occur separately or together.
Monitor patients receiving Hectorol Injection upon initiation of treatment for hypersensitivity reactions. Should a hypersensitivity reaction occur, discontinue Hectorol, monitor and treat if indicated (see ).
What are the precautions of Hectorol?
General
The principal adverse effects of treatment with Hectorol Injection are hypercalcemia, hyperphosphatemia, and oversuppression of PTH (iPTH less than 150 pg/mL). Prolonged hypercalcemia can lead to calcification of soft tissues, including the heart and arteries, and hyperphosphatemia can exacerbate hyperparathyroidism. Oversuppression of PTH may lead to adynamic bone syndrome. All of these potential adverse effects should be managed by regular patient monitoring and appropriate dosage adjustments. During treatment with Hectorol, patients usually require dose titration, as well as adjustment in co-therapy (i.e., dietary phosphate binders) in order to maximize PTH suppression while maintaining serum calcium and phosphorus levels within prescribed ranges.
In two open-label, single-arm, multi-centered studies, the incidence of hypercalcemia and hyperphosphatemia increased during therapy with Hectorol Injection (see ). The observed increases during Hectorol treatment underscore the importance of regular safety monitoring of serum calcium and phosphorus levels throughout treatment. Patients with higher pre-treatment serum levels of calcium (> 10.5 mg/dL) or phosphorus (> 6.9 mg/dL) were more likely to experience hypercalcemia or hyperphosphatemia. Therefore, Hectorol should not be given to patients with a recent history of hypercalcemia or hyperphosphatemia, or evidence of vitamin D toxicity.
| Study | Hypercalcemia(per 100 patient weeks) | Hyperphosphatemia(per 100 patient weeks) | |||
|---|---|---|---|---|---|
| Washout(Off Treatment) | Open-Label(Treatment) | Washout(Off Treatment) | Open-Label(Treatment) | ||
| Study C | 0.9 | 0.9 | 0.9 | 2.4 | |
| Study D | 0.3 | 1.0 | 1.2 | 3.7 |
Information for the Patient
The patient, spouse, or guardian should be informed about adherence to instructions about diet, calcium supplementation, and avoidance of the use of nonprescription drugs without prior approval from the patient's physician. Patients should also be carefully informed about the symptoms of hypercalcemia (see ).
Laboratory Tests
Serum levels of iPTH, calcium, and phosphorus should be determined prior to initiation of Hectorol treatment. During the early phase of treatment (i.e., first 12 weeks), serum iPTH, calcium, and phosphorus levels should be determined weekly. For dialysis patients in general, serum or plasma iPTH and serum calcium, phosphorus, and alkaline phosphatase should be determined periodically.
Drug Interactions
Specific drug interaction studies have not been conducted. Magnesium-containing antacids and Hectorol should not be used concomitantly because such use may lead to the development of hypermagnesemia (see ). Although not examined specifically, enzyme inducers (such as glutethimide and phenobarbital) may affect the 25-hydroxylation of Hectorol and may necessitate dosage adjustments. Cytochrome P450 inhibitors (such as ketoconazole and erythromycin) may inhibit the 25-hydroxylation of Hectorol. Hence, formation of the active Hectorol moiety may be hindered.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Long-term studies in animals to evaluate the carcinogenic potential of doxercalciferol have not been conducted. No evidence of genetic toxicity was observed in an bacterial mutagenicity assay (Ames test) or a mouse lymphoma gene mutation assay. Doxercalciferol caused structural chromatid and chromosome aberrations in an human lymphocyte clastogenicity assay with metabolic activation. However, doxercalciferol was negative in an mouse micronucleus clastogenicity assay. Doxercalciferol had no effect on male or female fertility in rats at oral doses up to 2.5 mcg/kg/day (approximately 3 times the maximum recommended human oral dose of 60 mcg/wk based on mcg/m body surface area).
Use in Pregnancy
Pregnancy Category B
Reproduction studies in rats and rabbits, at doses up to 20 mcg/kg/day and 0.1 mcg/kg/day (approximately 25 times and less than the maximum recommended human oral dose of 60 mcg/week based on mcg/m body surface area, respectively) have revealed no teratogenic or fetotoxic effects due to doxercalciferol. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Nursing Mothers
It is not known whether doxercalciferol is excreted in human milk. Because other vitamin D derivatives are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from doxercalciferol, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric Use
Safety and efficacy of Hectorol in pediatric patients have not been established.
Geriatric Use
Of the 70 patients treated with Hectorol Injection in the two Phase 3 clinical studies, 12 patients were 65 years or over. In these studies, no overall differences in efficacy or safety were observed between patients 65 years or older and younger patients.
Hepatic Insufficiency
Studies examining the influence of hepatic insufficiency on the metabolism of Hectorol were inconclusive. Since patients with hepatic insufficiency may not metabolize doxercalciferol appropriately, the drug should be used with caution in patients with impaired hepatic function. More frequent monitoring of iPTH, calcium, and phosphorus levels should be done in such individuals.
What are the side effects of Hectorol?
Hectorol Injection has been evaluated for safety in 70 patients with chronic renal disease on hemodialysis (who had been previously treated with oral Hectorol) from two 12-week, open-label, single-arm, multi-centered studies. (Dosage titrated to achieve target plasma iPTH levels, see .)
Because there was no placebo group included in the studies of Hectorol Injection, Table 4 provides the adverse event incidence rates from placebo-controlled studies of oral Hectorol.
Potential adverse effects of Hectorol are, in general, similar to those encountered with excessive vitamin D intake. The early and late signs and symptoms of vitamin D intoxication associated with hypercalcemia include:
| Adverse Event | Hectorol (n=61)% | Placebo (n=61)% | Body as a Whole |
|---|---|---|
| Abscess | 3.3 | 0.0 |
| Headache | 27.9 | 18.0 |
| Malaise | 27.9 | 19.7 | Cardiovascular System |
| Bradycardia | 6.6 | 4.9 | Digestive System |
| Anorexia | 4.9 | 3.3 |
| Constipation | 3.3 | 3.3 |
| Dyspepsia | 4.9 | 1.6 |
| Nausea/Vomiting | 21.3 | 19.7 | Musculo-Skeletal System |
| Arthralgia | 4.9 | 0.0 | Metabolic and Nutritional |
| Edema | 34.4 | 21.3 |
| Weight increase | 4.9 | 0.0 | Nervous System |
| Dizziness | 11.5 | 9.8 |
| Sleep disorder | 3.3 | 0.0 | Respiratory System |
| Dyspnea | 11.5 | 6.6 | Skin |
| Pruritus | 8.2 | 6.6 |
Early
Weakness, headache, somnolence, nausea, vomiting, dry mouth, constipation, muscle pain, bone pain, metallic taste, and anorexia.
Late
Polyuria, polydipsia, anorexia, weight loss, nocturia, conjunctivitis (calcific), pancreatitis, photophobia, rhinorrhea, pruritus, hyperthermia, decreased libido, elevated blood urea nitrogen (BUN), albuminuria, hypercholesterolemia, elevated serum aspartate transaminase (AST) and alanine transaminase (ALT), ectopic calcification, hypertension, cardiac arrhythmias, sensory disturbances, dehydration, apathy, arrested growth, urinary tract infections, and, rarely, overt psychosis.
Postmarketing Experience
Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to estimate their frequency or to establish a causal relationship to drug exposure.
Hypersensitivity reactions, including fatal outcome, have been reported in patients on hemodialysis following administration of Hectorol Injection. Hypersensitivity reactions include anaphylaxis with symptoms of angioedema (involving face, lips, tongue and airways), hypotension, unresponsiveness, chest discomfort, shortness of breath, cardiopulmonary arrest, pruritus and skin burning sensation (see ). These reactions may occur separately or together.
What should I look out for while using Hectorol?
Hectorol should not be given to patients with a tendency towards hypercalcemia or current evidence of vitamin D toxicity.
Hectorol Injection is contraindicated in patients with previous hypersensitivity to doxercalciferol or any of its ingredients (see and ).
Overdosage of any form of vitamin D, including Hectorol is dangerous (see ). Progressive hypercalcemia due to overdosage of vitamin D and its metabolites may be so severe as to require emergency attention. Acute hypercalcemia may exacerbate tendencies for cardiac arrhythmias and seizures and may potentiate the action of digitalis drugs. Chronic hypercalcemia can lead to generalized vascular calcification and other soft-tissue calcification. The serum calcium times serum phosphorus (Ca X P) product should be maintained at <55 mg/dL in patients with chronic kidney disease. Radiographic evaluation of suspect anatomical regions may be useful in the early detection of this condition.
Since doxercalciferol is a precursor for 1α,25-(OH)D, a potent metabolite of vitamin D, pharmacologic doses of vitamin D and its derivatives should be withheld during Hectorol treatment to avoid possible additive effects and hypercalcemia.
Oral calcium-based or other non-aluminum-containing phosphate binders and a low phosphate diet should be used to control serum phosphorus levels in patients undergoing dialysis. Uncontrolled serum phosphorus exacerbates secondary hyperparathyroidism and can lessen the effectiveness of Hectorol in reducing blood PTH levels. If hypercalcemia occurs after initiating Hectorol therapy, the dose of Hectorol and/or calcium-containing phosphate binders should be decreased. If hyperphosphatemia occurs after initiating Hectorol, the dose of Hectorol should be decreased and/or the dose of phosphate binders increased. (See dosing recommendations for Hectorol under ).
Magnesium-containing antacids and Hectorol should not be used concomitantly in patients on chronic renal dialysis because such use may lead to the development of hypermagnesemia.
Serious hypersensitivity reactions, including fatal outcome, have been reported post marketing in patients on hemodialysis following administration of Hectorol Injection. Hypersensitivity reactions include anaphylaxis with symptoms of angioedema (involving face, lips, tongue and airways), hypotension, unresponsiveness, chest discomfort, shortness of breath, and cardiopulmonary arrest. These reactions may occur separately or together.
Monitor patients receiving Hectorol Injection upon initiation of treatment for hypersensitivity reactions. Should a hypersensitivity reaction occur, discontinue Hectorol, monitor and treat if indicated (see ).
What might happen if I take too much Hectorol?
Administration of Hectorol to patients in excess doses can cause hypercalcemia, hypercalciuria, hyperphosphatemia, and over-suppression of PTH secretion leading in certain cases to adynamic bone disease. High intake of calcium and phosphate concomitant with Hectorol may lead to similar abnormalities. High levels of calcium in the dialysate bath may contribute to hypercalcemia.
How should I store and handle Hectorol?
LUGOL’S is supplied in 8 ml glass single-use bottles.
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Calcitriol (1α,25-(OH)D) and 1α,25-(OH)D regulate blood calcium at levels required for essential body functions. Specifically, the biologically active vitamin D metabolites control the intestinal absorption of dietary calcium, the tubular reabsorption of calcium by the kidney and, in conjunction with parathyroid hormone (PTH), the mobilization of calcium from the skeleton. They act directly on bone cells (osteoblasts) to stimulate skeletal growth, and on the parathyroid glands to suppress PTH synthesis and secretion. These functions are mediated by the interaction of these biologically active metabolites with specific receptor proteins in the various target tissues. In uremic patients, deficient production of biologically active vitamin D metabolites (due to lack of or insufficient 25-hydroxyvitamin D-1-alpha-hydroxylase activity) leads to secondary hyperparathyroidism, which contributes to the development of metabolic bone disease in patients with renal failure.
Non-Clinical Toxicology
Hectorol should not be given to patients with a tendency towards hypercalcemia or current evidence of vitamin D toxicity.Hectorol Injection is contraindicated in patients with previous hypersensitivity to doxercalciferol or any of its ingredients (see and ).
Overdosage of any form of vitamin D, including Hectorol is dangerous (see ). Progressive hypercalcemia due to overdosage of vitamin D and its metabolites may be so severe as to require emergency attention. Acute hypercalcemia may exacerbate tendencies for cardiac arrhythmias and seizures and may potentiate the action of digitalis drugs. Chronic hypercalcemia can lead to generalized vascular calcification and other soft-tissue calcification. The serum calcium times serum phosphorus (Ca X P) product should be maintained at <55 mg/dL in patients with chronic kidney disease. Radiographic evaluation of suspect anatomical regions may be useful in the early detection of this condition.
Since doxercalciferol is a precursor for 1α,25-(OH)D, a potent metabolite of vitamin D, pharmacologic doses of vitamin D and its derivatives should be withheld during Hectorol treatment to avoid possible additive effects and hypercalcemia.
Oral calcium-based or other non-aluminum-containing phosphate binders and a low phosphate diet should be used to control serum phosphorus levels in patients undergoing dialysis. Uncontrolled serum phosphorus exacerbates secondary hyperparathyroidism and can lessen the effectiveness of Hectorol in reducing blood PTH levels. If hypercalcemia occurs after initiating Hectorol therapy, the dose of Hectorol and/or calcium-containing phosphate binders should be decreased. If hyperphosphatemia occurs after initiating Hectorol, the dose of Hectorol should be decreased and/or the dose of phosphate binders increased. (See dosing recommendations for Hectorol under ).
Magnesium-containing antacids and Hectorol should not be used concomitantly in patients on chronic renal dialysis because such use may lead to the development of hypermagnesemia.
Serious hypersensitivity reactions, including fatal outcome, have been reported post marketing in patients on hemodialysis following administration of Hectorol Injection. Hypersensitivity reactions include anaphylaxis with symptoms of angioedema (involving face, lips, tongue and airways), hypotension, unresponsiveness, chest discomfort, shortness of breath, and cardiopulmonary arrest. These reactions may occur separately or together.
Monitor patients receiving Hectorol Injection upon initiation of treatment for hypersensitivity reactions. Should a hypersensitivity reaction occur, discontinue Hectorol, monitor and treat if indicated (see ).
Specific drug interaction studies have not been conducted. Magnesium-containing antacids and Hectorol should not be used concomitantly because such use may lead to the development of hypermagnesemia (see ). Although not examined specifically, enzyme inducers (such as glutethimide and phenobarbital) may affect the 25-hydroxylation of Hectorol and may necessitate dosage adjustments. Cytochrome P450 inhibitors (such as ketoconazole and erythromycin) may inhibit the 25-hydroxylation of Hectorol. Hence, formation of the active Hectorol moiety may be hindered.
The principal adverse effects of treatment with Hectorol Injection are hypercalcemia, hyperphosphatemia, and oversuppression of PTH (iPTH less than 150 pg/mL). Prolonged hypercalcemia can lead to calcification of soft tissues, including the heart and arteries, and hyperphosphatemia can exacerbate hyperparathyroidism. Oversuppression of PTH may lead to adynamic bone syndrome. All of these potential adverse effects should be managed by regular patient monitoring and appropriate dosage adjustments. During treatment with Hectorol, patients usually require dose titration, as well as adjustment in co-therapy (i.e., dietary phosphate binders) in order to maximize PTH suppression while maintaining serum calcium and phosphorus levels within prescribed ranges.
In two open-label, single-arm, multi-centered studies, the incidence of hypercalcemia and hyperphosphatemia increased during therapy with Hectorol Injection (see ). The observed increases during Hectorol treatment underscore the importance of regular safety monitoring of serum calcium and phosphorus levels throughout treatment. Patients with higher pre-treatment serum levels of calcium (> 10.5 mg/dL) or phosphorus (> 6.9 mg/dL) were more likely to experience hypercalcemia or hyperphosphatemia. Therefore, Hectorol should not be given to patients with a recent history of hypercalcemia or hyperphosphatemia, or evidence of vitamin D toxicity.
Hectorol Injection has been evaluated for safety in 70 patients with chronic renal disease on hemodialysis (who had been previously treated with oral Hectorol) from two 12-week, open-label, single-arm, multi-centered studies. (Dosage titrated to achieve target plasma iPTH levels, see .)
Because there was no placebo group included in the studies of Hectorol Injection, Table 4 provides the adverse event incidence rates from placebo-controlled studies of oral Hectorol.
Potential adverse effects of Hectorol are, in general, similar to those encountered with excessive vitamin D intake. The early and late signs and symptoms of vitamin D intoxication associated with hypercalcemia include:
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
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