doxercalciferol

Action and Spectrum

Actions and spectrum: 

doxercalciferol is a synthetic analog of vitamin D that is used in the treatment of secondary hyperparathyroidism in patients with chronic kidney disease. It helps to increase the absorption of calcium from the intestines, which in turn helps to regulate parathyroid hormone (PTH) levels.

doxercalciferol is also used to treat low levels of calcium in the blood (hypocalcemia) and to prevent and treat bone disease in patients with chronic kidney disease. 

Drug Interaction

Adverse Reaction

Frequency not defined: 

Edema 

Chills 

Headache 

Nausea 

Hypercalcemia 

Anorexia 

Dyspepsia 

Edema 

Sleep disorder 

Palpitation 

Dizziness 

Malaise 

Vomiting 

Hypercalciuria 

Constipation 

Arthralgia 

Weight increase 

Dyspnea Pruritus  

Post marketing Reports 

Hypersensitivity reactions 

Black Box Warning

Contraindication / Caution

Contraindication/Caution 

Contraindication 

doxercalciferol is contraindicated in patients with hypercalcemia, vitamin D toxicity, or known hypersensitivity to any component of the formulation. It has to be used in patients with evidence of vitamin D toxicity or hypersensitivity to the drug. It should not be used concomitantly with vitamin D supplements, calcium supplements, or other vitamin D analogs, as it can increase the risk of hypercalcemia.  

Caution 

doxercalciferol, like other vitamin D analogs,in patients with known hypersensitivity it should be used with caution to vitamin D or its analogs. It should also be used cautiously in evidence of vitamin D toxicity or patients with hypercalcemia, as it may exacerbate these conditions. 

caution should be taken when using doxercalciferol in patients with impaired liver function, as the drug is metabolized in the liver. Finally, doxercalciferol should be used with caution in patients with malabsorption syndromes, as these patients may not absorb the drug adequately.  

Comorbidities 

• Hypersensitivity to vitamin D or doxercalciferol: Patients who are allergic to vitamin D or doxercalciferol should not take this medication. 
• High calcium levels: doxercalciferol can increase calcium levels in the blood, so patients with high calcium levels should be closely monitored. 
• Liver disease: Patients with liver disease may have impaired liver function, which can affect the metabolism of doxercalciferol. 
• Pregnancy and breastfeeding: doxercalciferol is classified as pregnancy category C and should be used with caution in pregnant or breastfeeding women. 
• Malabsorption syndromes: Patients with malabsorption syndromes such as celiac disease or inflammatory bowel disease may have difficulty absorbing doxercalciferol and may require higher doses or alternative treatments. 
• Hyperphosphatemia: doxercalciferol can also increase phosphorus levels in the blood, so patients with high phosphorus levels should also be closely monitored. 
• Cardiovascular disease: Patients with cardiovascular disease may be at increased risk for adverse effects of doxercalciferol, such as hypercalcemia and hyperphosphatemia. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category C 

Lactation: safety and efficacy not established  

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

doxercalciferol is a synthetic vitamin D2 analog that is activated in the liver to form the active hormone calcitriol (1,25-dihydroxy vitamin D3). Calcitriol acts as a ligand for the vitamin D receptor (VDR), which is expressed in many tissues, including the intestines, bone, and parathyroid glands. 

In the intestines, calcitriol promotes calcium and phosphate absorption. In bone, calcitriol enhances bone formation by increasing osteoblast activity and decreasing osteoclast activity. In the parathyroid gland, calcitriol suppresses parathyroid hormone (PTH) synthesis and secretion.  

Pharmacodynamics: 

doxercalciferol is an active vitamin D analog that regulates calcium and phosphorus homeostasis. It works by increasing the absorption of calcium and phosphorus from the gastrointestinal tract, enhancing bone mineralization, and reducing parathyroid hormone (PTH) levels. 

doxercalciferol binds to the vitamin D receptor (VDR) in the intestine, parathyroid gland, and bone, leading to the transcription of genes responsible for calcium absorption and bone mineralization. It also inhibits the secretion of PTH by the parathyroid gland, which helps to decrease serum calcium and phosphorus levels.  

Pharmacokinetics: 

Absorption 

doxercalciferol is administered orally and is absorbed in the small intestine. The absorption of doxercalciferol is dependent on the presence of dietary fat. 

Distribution  

The distribution of doxercalciferol is mainly in the blood and it binds to vitamin D-binding protein (VDBP) and albumin. 

Metabolism 

doxercalciferol undergoes hepatic metabolism to form its active form, 1α, 25-dihydroxy vitamin D2. 

Elimination 

The elimination half-life of doxercalciferol is approximately 30 hours. The drug and its metabolites are eliminated mainly in the bile and feces, with a small amount eliminated in the urine. 

Adminstartion

Administration 

doxercalciferol is available as an oral solution, oral capsules, and injection. The oral solution and capsules should be taken by mouth with or without food. The injection is administered either into a vein or into a muscle. The dose and duration of treatment may vary depending on the individual’s condition, response to treatment, and other factors. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: doxercalciferol 

Pronounced: [dock-sir-kal-SIH-fer-all]  

Why do we use doxercalciferol? 

doxercalciferol is a synthetic vitamin D analog that is used to treat secondary hyperparathyroidism. It helps in reducing the levels of parathyroid hormone (PTH) by increasing the absorption of calcium and phosphorus in the intestine and by reducing the release of PTH from the parathyroid gland.

It is also used to treat vitamin D deficiency in patients with liver disease or malabsorption syndrome and in those who are on chronic steroid therapy.