Description

Simple

A medication used to prevent and treat bone loss (typically caused by osteoporosis).

Clinical

A bisphosphonate drug that prevents osteoclastic bone resorption and is used for the prevention and treatment of osteoporosis.

Overview

Alendronic acid is a second generation bisphosphonate that is used for the treatment of some forms of osteoperosis and Paget's disease[FDA Label][1,5]. It functions by preventing resorption of bone[FDA Label][1].

Pharmacology

Indication

Alendronic acid is indicated for the treatment and prevention of osteoporosis in men and postmenopausal women, treatment of glucocorticoid-induced osteoporosis, and Paget's disease of bone[FDA Label][ Read more

Pharmacodynamic

Alendronic acid tablets have a very low oral bioavialability[FDA Label][2]. After adminis... Read more

Mechanism of action

Alendronic acid binds to bone hydroxyapatite[FDA Label]. Bone resorption causes local acidification, releasing alendronic acid which is that taken into osteoclasts by fluid-phase endocytosis[ Read more

Absorption

Mean oral bioavailability of alendronic acid in women is 0.64% and in men is 0.59%[FDA Label][ Read more

Protein binding

78%[FDA Label]. Studies in rats show that plasma protein binding increases with decreasing alendronic acid plasma concentration[ Read more

Volume of distribution

28L[FDA Label].

Clearance

71mL/min[FDA Label].

Half life

Due to alendronic acid being incorporated into the skeleton, the terminal half life is estimated to be over 10 years[FDA Label].

Route of elimination

Administration of radiolabeled alendronic acid results in 50% recovery in urine within 72 hours[FDA Label][ Read more

Toxicity

In clinical studies, ≥3% of patients experience abdominal pain, acid regurgitation, constipation, diarrhea, dyspepsia, musculoskeletal pain, and nausea[FDA Label].

No information for treatment of overdose is available, however patients should be given milk or antacids to bind alendronic acid and... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Upper gastrointestinal adverse reactions US
  • adult
  • seniors
  • Kind: experimental
    • Percent: 18%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Abdominal Pain US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 2-7%
  • Kind: placebo
    • Percent: 2-5%
  • Clinical Trial
    Musculoskeletal Pain US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Acid Regurgitation US
    • postmenopausal
  • Kind: experimental
    • Percent: 1-5%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Musculoskeletal Pain US
    • adult
    • seniors
  • Kind: experimental
    • Percent: ≤4%
  • Kind: placebo
    • Percent: ≤3%
  • Clinical Trial
    Acid Regurgitation US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 1-2%
  • Kind: placebo
    • Percent: 1-4%
  • Clinical Trial
    Acid Regurgitation US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Flatulence US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Abdominal Pain US
    • postmenopausal
  • Kind: experimental
    • Percent: 2-4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Dyspepsia US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 1-4%
  • Kind: placebo
    • Percent: 1-4%
  • Clinical Trial
    Nausea US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 1-4%
  • Kind: placebo
    • Percent: 2-4%
  • Clinical Trial
    Headache US
    • adult
    • seniors
  • Kind: experimental
    • Percent: <3%
  • Kind: placebo
    • Percent: <2%
  • Clinical Trial
    Diarrhea US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1-2%
  • Clinical Trial
    Flatulence US
    • adult
    • seniors
  • Kind: experimental
    • Percent: ≤3%
  • Kind: placebo
    • Percent: ≤1%
  • Clinical Trial
    Gastroesophageal Reflux Disease US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Dyspepsia US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 2-3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Nausea US
    • postmenopausal
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Constipation US
    • adult
    • seniors
  • Kind: experimental
    • Percent: ≤3%
  • Kind: placebo
    • Percent: ≤2%
  • Clinical Trial
    Acid Regurgitation US
  • Kind: experimental
    • Percent: 2-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 2-3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Abdominal Pain US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Esophageal ulcer US
    • adult
    • seniors
  • Kind: experimental
    • Percent: ≤2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Musculoskeletal Pain US
    • postmenopausal
  • Kind: experimental
    • Percent: 1-2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dyspepsia US
    • postmenopausal
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Diarrhea US
    • postmenopausal
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Constipation US
    • postmenopausal
  • Kind: experimental
    • Percent: 1-2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Nausea US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Gastritis US
    • adult
    • seniors
  • Kind: experimental
    • Percent: <1%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Abdominal distension US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Gastric Ulcer US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Muscle Cramp US
    • adult
    • seniors
  • Kind: experimental
    • Percent: ≤1%
  • Kind: placebo
    • Percent: ≤1%
  • Clinical Trial
    Taste perversion US
    • adult
    • seniors
  • Kind: experimental
    • Percent: <1%
  • Kind: placebo
    • Percent: ≤1%
  • Clinical Trial
    Dysphagia US
    • adult
    • seniors
  • Kind: experimental
    • Percent: ≤1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Vomiting US
    • adult
    • seniors
  • Kind: experimental
    • Percent: ≤1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Abdominal distension US
    • postmenopausal
  • Kind: experimental
    • Percent: ≤1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Melena US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Diarrhea US
    • adult
    • seniors
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 0%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Angioedema US
    Post Marketing
    Urticaria US
    Post Marketing
    Bone pain US
    Post Marketing
    Joint Pain US
    Post Marketing
    Gastric Ulcer US
    Post Marketing
    Duodenal Ulcer US
    Post Marketing
    Esophageal Perforation US
    Post Marketing
    Oropharyngeal ulceration US
    Post Marketing
    Esophageal ulcer US
    Post Marketing

    Contraindications

    • Route:
      • Oral
    • Dose Form:
      • Tablet
    • Sex Group: all
    • Regions: US
    • Patient Conditions:
        • Name: Inability to stand or sit upright for at least 30 minutes
        • Drugbank Id: DBCOND0118757
    • Route:
      • Oral
    • Dose Form:
      • Tablet
    • Sex Group: all
    • Regions: US
    • Patient Conditions:
        • Name: Achalasia
        • Drugbank Id: DBCOND0032922
    • Route:
      • Oral
    • Dose Form:
      • Tablet
    • Sex Group: all
    • Regions: US
    • Patient Conditions:
        • Name: Stricture
        • Drugbank Id: DBCOND0057158
    • Route:
      • Oral
    • Dose Form:
      • Tablet
    • Sex Group: all
    • Regions: US
    • Patient Conditions:
        • Name: Abnormalities of the esophagus
        • Drugbank Id: DBCOND0108189
    • Route:
      • Oral
    • Dose Form:
      • Tablet
    • Sex Group: all
    • Regions: US
    • Patient Conditions:
        • Name: Aspiration
        • Drugbank Id: DBCOND0019548
    • Route:
      • Oral
    • Dose Form:
      • Tablet
    • Hypersensitivity:
      • true
    • Sex Group: all
    • Regions: US
    • Regions: US
    • Patient Conditions:
        • Name: Hypocalcemia
        • Drugbank Id: DBCOND0020582

    Food Interactions

    Administer vitamin supplements. Patients may require supplemental vitamin D.

    Avoid multivalent ions. Calcium, antacids, and divalent ions may interfere with the absorption of this medication.

    Take before a meal. Take 30-60 minutes before breakfast.

    Take with a full glass of water.