calcifediol

Action and Spectrum

Actions and Spectrum 

Actions of calcifediol include:  

• Regulating calcium and phosphate levels: calcifediol helps to maintain the balance of calcium and phosphate in the body by activating the production of calcitriol (the active form of vitamin D). This helps to absorb calcium from the intestines and increase the uptake of calcium from the bone into the blood.  
• Maintaining bone health: calcifediol plays a key role in bone formation and bone resorption (the process of breaking down and rebuilding bone). It helps to promote the formation of new bone tissue and prevent bone loss.  
• Regulating the immune system: calcifediol has immune-modulatory effects and can help to regulate the immune system. It has been shown to have anti-inflammatory effects and may help to reduce the risk of certain autoimmune diseases.  
• Reducing the risk of certain cancers: Some studies have shown that higher levels of calcifediol may be associated with a reduced risk of certain types of cancer, including breast, colon, and prostate cancer.  

The spectrum of calcifediol includes its various actions and effects on the body, including its role in regulating calcium and phosphate levels, maintaining bone health, regulating the immune system, and potentially reducing the risk of certain cancers.  

Drug Interaction

Adverse Reaction

Frequency Defined  

>10%  

Hyperphosphatemia (44%)  

1-10%  

Increased blood creatinine (4.9%)  

Nasopharyngitis (4.9%)  

Dyspnea (4.2%)  

Cough (3.5%)  

Congestive heart failure (3.5%)  

Bronchitis (2.8%)  

Constipation (3.2%)  

Hyperkalemia (2.5%)  

Anemia (4.9%)  

Hyperuricemia (1.8%)  

Osteoarthritis (2.1%)  

Contusion (1.8%)  

COPD (1.4%)  

Pneumonia (1.4%)  

<1%  

Hyperphosphatemia (0.4%)

Black Box Warning

Contraindication / Caution

Contraindications/ Cautions  

Contraindications:  

• Hypersensitivity to calcifediol or any other ingredients in the medication  
• Severe hypercalcemia  
• Severe kidney failure or impaired kidney function  
• Active vitamin D-dependent hypercalcemia  

Cautions:  

• Use with caution in patients with liver disease or impaired liver function, as calcifediol may increase liver enzymes and worsen liver function  
• Use with caution in patients with heart disease, as calcifediol may increase the risk of hypercalcemia and potentially worsen heart function  
• Use with caution in patients with a history of kidney stones, as calcifediol may increase the risk of developing kidney stones  
• Use with caution in patients with high blood pressure, as calcifediol may increase the risk of hypertension  
• Use with caution in patients taking medications that can interact with calcifediol, such as diuretics, anticonvulsants, and antacids. It is important to inform your healthcare provider about all medications you are taking before starting calcifediol.

Pregnancy / Lactation

Pregnancy warnings:     

US FDA pregnancy category: N/A 

Lactation:   

Excreted into human milk is unknown  

Pregnancy Categories:         

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.    

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.     

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.     

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.     

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology:  

Calcifediol, also known as 25-hydroxyvitamin D, is a hormone produced in the liver and released into the bloodstream. It plays a key role in calcium and phosphate metabolism, helping to regulate the concentration of these minerals in the body.  

Pharmacodynamics:  

The pharmacodynamics of calcifediol involves the regulation of calcium and phosphate metabolism and the maintenance of normal bone structure and function. It also has several other effects on various bodily systems, including the immune system, endocrine system, and cardiovascular system.  

The primary mechanism of action of calcifediol is through its ability to bind to vitamin D receptors (VDRs) in the intestine, bone, and kidney. When calcifediol binds to VDRs in the intestine, it stimulates the production of calcium-binding proteins, which increases calcium absorption from the diet. In the bone, calcifediol stimulates the production of osteocalcin, a protein that is involved in bone mineralization. In the kidney, calcifediol stimulates the production of the enzyme 1-alpha-hydroxylase, which converts calcifediol to 1,25-dihydroxyvitamin D, a more active form of vitamin D that is involved in the regulation of calcium and phosphate levels in the body.  

Calcifediol has several other pharmacodynamic effects in the body, including the regulation of immune function, insulin secretion, and blood pressure. It has also been shown to have anti-inflammatory and anti-tumor effects.  

Pharmacokinetics:  

Absorption  

The absorption of calcifediol is typically high when taken orally.   

The serum total 25-hydroxyvitamin D levels stabilize after around three months.  

Distribution  

It is mainly protein bound in the blood and has a large volume of distribution, with a steady-state Vd of 8.8 L in healthy volunteers and 30.1 L in individuals with stage 4 chronic kidney disease.  

Metabolism   

Calcifediol is metabolized by the 1-alpha-hydroxylase enzyme to produce calcitriol, the active form of vitamin D, in the kidney and other tissues. It is also catabolized by the CYP24A1 enzyme to inactive metabolites.  

Elimination and excretion  

Calcifediol is primarily excreted through the biliary fecal route  

Adminstartion

Administration:  

Oral Administration:  

When taking calcifediol orally, it is important to swallow the capsule whole and not crush or chew it.   

Missed dose  

If a dose is missed, patients should skip the missed dose and resume taking the medication at the next regularly scheduled time. It is not necessary to take an extra dose to compensate for a missed one.  

Storage:  

Calcifediol should be stored at controlled room temperature, between 20-25°C (68-77°F). It is permitted to have excursions in temperatures between 15-30°C (59-86°F). It is important to keep the medication away from moisture and heat and to store it out of reach of children.  

Patient Information Leaflet

Patient information leaflet 

Generic Name: calcifediol  

Why do we use calcifediol? 

calcifediol is a form of vitamin D that is used to treat vitamin D deficiency. It is often used in people who have conditions that interfere with the absorption of vitamin D, such as Crohn’s disease, celiac disease, or cystic fibrosis. calcifediol is also used to treat rickets, a condition that causes softening and weakening of the bones in children. In addition, calcifediol may be used to treat osteomalacia, a condition that causes weak bones in adults. It may also be used to increase calcium levels in people with low calcium levels due to certain medical conditions.