alendronate

Action and Spectrum

Actions and Spectrum:

The primary action of alendronate is to inhibit the activity of osteoclasts, which are cells responsible for breaking down bone tissue. By slowing down bone resorption, alendronate helps to maintain or increase bone density, reducing the risk of fractures.

alendronate is also used to treat Paget’s disease of bone, a condition in which the bones become enlarged and weak, and to prevent glucocorticoid-induced osteoporosis, a type of osteoporosis caused by long-term use of corticosteroid medications.

The spectrum of alendronate includes the following:

• Treatment of osteoporosis: alendronate is used to treat and prevent osteoporosis in postmenopausal women and to reduce the risk of fractures in both men and women with osteoporosis.
• Management of bone metastases: alendronate can be used to manage bone metastases in cancer patients, helping to reduce pain and the risk of fractures.
• Treatment of Paget’s disease of bone: alendronate is also used to treat Paget’s disease of bone, a condition in which the bones become enlarged and weak.

Drug Interaction

Adverse Reaction

Frequency defined:  

1-10% 

Daily dosing 

• Abdominal pain (2.1-6.6%) 
• Musculoskeletal (bone, muscle, or joint) pain (4.1%) 
• Acid regurgitation (2-4.1%) 
• Flatulence (2.6-4.1%) 
• Nausea (0.6-3.6%) 
• Dyspepsia (3.4-3.6%) 
• Constipation (1.3-3.1%) 
• Vomiting (1%) 
• Dysphagia (1%) 
• Abdominal distention (1%) 

Weekly dosing 

• Abdominal pain (1.7-3.7%) 
• Musculoskeletal pain (2.9%) 
• Dyspepsia (1.9-2.7%) 
• Acid regurgitation (1.4-1.9%) 
• Nausea (1.4-1.9%) 
• Abdominal distention (1%) 

<1% 

Daily dosing 

• Gastroesophageal reflux disease (0.7%) 
• Senses taste perversion (0.5%) 
• Gastritis (0.5%) 

Weekly dosing 

• Musculoskeletal pain (0.8%) 
• Constipation (0.8-0.9%) 
• Flatulence (0.4%) 
• Gastritis (0.2%) 
• Muscle pain (0.2%) 
• Abdominal distention (0.2%)

Post-marketing report 

• Pruritus 
• alopecia severe skin reactions 
• Stevens-Johnson syndrome

Black Box Warning

Black Box Warning:

The black box warning for alendronate states that the medication can cause irritation, inflammation, or ulceration of the esophagus, the tube that connects the mouth to the stomach. This can cause difficulty swallowing, chest pain, and heartburn.

Contraindication / Caution

Be cautious in conditions with hypersensitivity and hypocalcemia. 

Pregnancy / Lactation

Pregnancy consideration: 

The drug is not recommended during pregnancy as it may affect the fetus  

Pregnancy category: C 

Lactation: The excretion of the drug in human breast milk is unknown  

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 the risks over benefits. These category drugs should be prohibited for pregnant women. 
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology:

alendronate is a medication that belongs to a class of drugs known as bisphosphonates. bisphosphonates are used to treat and prevent osteoporosis, a condition characterized by thinning and weakening of bones.

Pharmacodynamics:

Its mechanism of action involves inhibiting the activity of osteoclasts, which are cells responsible for breaking down bone tissue.

Pharmacokinetics:

Absorption

alendronate is usually taken orally in the form of a tablet. It is poorly absorbed from the gastrointestinal tract, with only about 0.6% of an oral dose being absorbed. The bioavailability of alendronate is further reduced by food, which can decrease absorption by up to 90%.

Distribution

alendronate is distributed mainly to bone tissue, where it is taken up by osteoclasts (cells responsible for breaking down bone tissue). The drug has a low volume of distribution, indicating that it is largely confined to the extracellular fluid.

Metabolism

alendronate is not metabolized in the body and is excreted unchanged.

Elimination and Excretion

alendronate is excreted primarily in the urine. The drug has a half-life of approximately 10 years in bone tissue, indicating that it is slowly released from bone over time.

Adminstartion

Administration:

The administration of alendronate is typically once a week, taken in the morning on an empty stomach with a full glass of water, at least 30 minutes before eating, drinking, or taking any other medications. It is important to remain upright, sitting or standing, for at least 30 minutes after taking the medication to reduce the risk of side effects such as irritation or ulcers of the esophagus.

Patient Information Leaflet

Patient information leaflet 

Generic Name: alendronate 

Pronounced: [uh·len·droh·nayt] 

Why do we use alendronate? 

alendronate is used to treat and prevent osteoporosis in postmenopausal women and men. Osteoporosis is a condition where bones become weak and brittle, increasing the risk of fractures, especially in the hip, spine, and wrist.

alendronate belongs to a class of drugs called bisphosphonates, which work by slowing down the activity of osteoclasts, cells that break down bone tissue. By reducing bone resorption, alendronate can increase bone density and strength, reducing the risk of fractures.