alendronic acid / colecalciferol

Action and Spectrum

Actions and spectrum: 

alendronic acid: 

• Action: alendronic acid belongs to a class of medications called bisphosphonates. Its primary action is to inhibit bone resorption by osteoclasts. Osteoclasts breaks down bone tissue, and alendronic acid helps in slowing down this process, leading to an increase in bone density. 
• Spectrum: alendronic acid is used to treat osteoporosis in postmenopausal women and in men. It is also prescribed to manage osteoporosis associated with long-term glucocorticoid use. 

colecalciferol (Vitamin D3): 

• Action: colecalciferol, or vitamin D3, plays a crucial role in calcium and phosphate homeostasis. It enhances the calcium absorption in the small intestine and promotes the mineralization of bone. 
• Spectrum: Vitamin D deficiency can lead to impaired bone mineralization and a higher risk of fractures. colecalciferol supplementation is often combined with alendronic acid to ensure the supply of vitamin D, especially in individuals with insufficient exposure to sunlight or those at risk of vitamin D deficiency. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Headache 

Dyspepsia 

Diarrhoea 

abdominal distension 

musculoskeletal pain 

abdominal pain 

constipation 

flatulence 

Dysphagia 

acid regurgitation 

Black Box Warning

Black Box Warning: 

There were no specific black box warnings associated with the combination medication alendronic acid/colecalciferol. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals who have a known hypersensitivity or allergy to alendronic acid, colecalciferol, or any other components of the medication should avoid its use. 
• Inability to Stand or Sit Upright: Some formulations of alendronic acid require the patient to remain upright for a specific period after taking the medication. Individuals who cannot stand or sit upright for at least 30 minutes may have contraindications to specific formulations. 
• Abnormalities of the Esophagus: Conditions such as dysphagia, stricture, or other abnormalities of the esophagus may be contraindications, as alendronic acid can potentially cause irritation to the esophagus. 
• Pregnancy and Breastfeeding: The safety of alendronic acid/colecalciferol during pregnancy and breastfeeding is not well-established. It is avoided in pregnant and breastfeeding individuals unless the potential benefits outweigh the risks. 

Caution: 

• Gastrointestinal Disorders: Individuals with active upper gastrointestinal problems, such as gastritis, peptic ulcers, or active gastrointestinal bleeding, may require cautious use of alendronic acid to prevent potential irritation. 
• Calcium and Vitamin D Monitoring: Since colecalciferol (vitamin D3) is a component of the combination, caution is needed in individuals with hypercalcemia or conditions that may predispose them to elevated calcium levels. Regular monitoring of serum calcium and vitamin D levels is advisable. 
• Inability to Sit or Stand Upright: Some formulations of alendronic acid require patients to remain upright for a specified time after administration. Individuals who cannot comply with this requirement may need an alternative form of the medication. 

Comorbidities: 

• Renal Impairment: Individuals with pre-existing renal impairment may require dose adjustments or cautious use of alendronic acid/colecalciferol. Monitoring of renal function is typically recommended. 
• Esophageal Disorders: Individuals with esophageal disorders, including dysphagia or esophageal strictures, may be at an increased risk of adverse effects related to alendronic acid, and caution is advised. 
• Hypercalcemia: Conditions associated with hypercalcemia (elevated levels of calcium in the blood) may warrant caution when using colecalciferol (vitamin D3). Monitoring of serum calcium levels is important in such cases. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into human milk: unknown  

Pregnancy category: 

• 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 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: 

• alendronic Acid: It inhibits bone resorption by osteoclasts, responsible for breaking down bone tissue. alendronic acid binds to hydroxyapatite crystals in bone and is taken up by osteoclasts during bone resorption. This results in the inhibition of osteoclast activity and a reduction in bone turnover, leading to increased bone mineral density. 
• colecalciferol (Vitamin D3): Vitamin D plays a crucial role in calcium and phosphate homeostasis. colecalciferol is converted to its active form, calcitriol, in the liver and kidneys. Calcitriol enhances the absorption of dietary calcium in the small intestine and promotes the mineralization of bone. Adequate vitamin D is essential for maintaining bone health and preventing conditions such as osteoporosis.

Pharmacodynamics: 

alendronic Acid: 

• Inhibition of Bone Resorption: alendronic acid, a bisphosphonate, exerts its pharmacodynamic effects by inhibiting bone resorption. It is an analog of pyrophosphate that binds to hydroxyapatite crystals in bone, preferentially taken up by osteoclasts during bone resorption. 
• Osteoclast Inhibition: By localizing in bone, alendronic acid interferes with osteoclast activity, inhibiting their ability to break down bone tissue. This leads to a decrease in bone turnover and an increase in bone mineral density. 
• Fracture Risk Reduction: The primary clinical outcome is a reduction in the risk of fractures, particularly vertebral and hip fractures, in individuals with osteoporosis. 

colecalciferol (Vitamin D3): 

• Calcium Homeostasis: colecalciferol, or vitamin D3, plays a key role in calcium and phosphate homeostasis. It is converted to its active form, calcitriol, in the liver and kidneys. 
• Calcitriol’s Actions: Calcitriol enhances the absorption of dietary calcium in the small intestine, promoting calcium availability for bone mineralization. It also regulates calcium and phosphate levels in the blood. 
• Bone Health Support: Adequate vitamin D is essential for maintaining bone health. In the context of osteoporosis, colecalciferol supplementation supports the bone mineralization process and helps prevent fractures.

Pharmacokinetics: 

alendronic Acid: 

• Absorption: alendronic acid is poorly absorbed from the gastrointestinal tract, with reported bioavailability of less than 1%. To enhance absorption, it is recommended to take alendronic acid on an empty stomach with a full glass of water, and patients are advised to remain upright for 30 minutes after administration to minimize the risk of esophageal irritation. 
• Distribution: alendronic acid binds strongly to bone tissue, particularly hydroxyapatite crystals, where it is taken up by osteoclasts during bone resorption. 
• Metabolism: alendronic acid undergoes minimal metabolism. 
• Excretion: The majority of the absorbed drug that is not bound to bone is excreted unchanged in the urine. 

colecalciferol (Vitamin D3): 

• Absorption: colecalciferol is absorbed from the small intestine, and its absorption is dependent on bile salts and dietary fat. Absorption occurs in the presence of sunlight or ultraviolet (UV) light exposure. 
• Distribution: Vitamin D is transported in the bloodstream, bound to vitamin D-binding protein. 
• Metabolism: In the liver, colecalciferol is converted to 25-hydroxyvitamin D [25(OH)D], the major circulating form. Further hydroxylation occurs in the kidneys, resulting in the active form, calcitriol [1,25-dihydroxyvitamin D]. 
• Excretion: Metabolites of vitamin D are excreted in bile and undergo enterohepatic recirculation. 

Adminstartion

Administration: 

alendronic acid: 

• Timing of Administration: Take alendronic acid early in the morning, at least 30 minutes before food. 
• Administration with Water: Take alendronic acid with a full glass of water. Other beverages (including mineral water), foods, and medications can interfere with the absorption of alendronic acid. 

colecalciferol (Vitamin D3): 

• Dosage Instructions: The dosage of colecalciferol will depend on the specific formulation and the individual’s vitamin D status. Follow the prescribed dosage provided by the healthcare provider. 
• Sunlight Exposure: Adequate exposure to sunlight is important for the synthesis of vitamin D in the skin. Patients are encouraged to spend time outdoors in sunlight, but the duration may vary based on factors such as skin type and geographical location. 
• Dietary Considerations: Ensure an adequate intake of dietary sources of vitamin D, and follow any dietary recommendations provided by the healthcare provider. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: alendronic acid / colecalciferol 

Pronounced: (uh-LEN-droh-nik AS-id / kohl-kal-SIF-er-ol)  

Why do we use alendronic acid / colecalciferol? 

The combination medication is indicated for the treatment of osteoporosis in postmenopausal women. It is a condition characterized by decreased bone mineral density, leading to the increased risk of fractures, particularly in the hip and spine.

The combination may also be prescribed for the treatment of osteoporosis in men. While osteoporosis is more commonly associated with postmenopausal women, men can also experience bone loss and fractures, especially with age. The inclusion of colecalciferol (vitamin D3) in the combination addresses the importance of vitamin D in bone health.