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Pharmacology

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Endocrinology

Question
86 out of 93
 

DOC for prevention of postmenopausal osteoporosis is: (AIIMS Nov 10)



A Raloxifene
B Tamoxifen

C Clomiphene
D Torimefen

Ans. A Raloxifene

(BG Katzung, Basic & Clinical Pharmacology’ 11th Edition’ 2010; pp-766)

  1. Raloxifen is a SERM having partial agonistic activity (agonist-antagonist) and is used for prevention of postmenopausal osteoporosis.
  2. Importantly, it has similar activity at bone and lipids but does not have similar action on the endometrium. That means, unlike tamoxifen it does not cause endometrial hyperplasia.
  3. Although, subjected to high first pass metabolism, the drug does have a volume of distribution. Therefore, the drug can be taken once a day.
  4. It is commonly regarded to be the drug of choice for prevention of postmenopausal osteoporosis.
  5. The drug is effective in reducing spine fractures but not hip fractures unlike bisphosphonates and teriparatide that can protect against both.
  6. Calcium or vitamin D could be added if the daily intake seems inadequate. The drug also reduces risk of breast cancer.
  7. Hot flashes and leg cramps are common. Risk of thromboembolic event is the major drawback. Calcitonin a calcinuric hormone librated by parafollicular C cells is also effective in postmenopausal osteoporosis.
  8. This drug is also effective in reducing risk of spine fractures but not in hip fractures. Bisphosphonates are potent inhibitors of bone resorption.
  9. These reduce fracture risk in spine, hip and other locations. Strontium increases new bone formation. Denosumab is an antibody to RANKL antibody and is interfere with osteoclast.
  10. Toremifen is SERM used for advanced breast cancer and is being evaluated for cancer if prostate. The drug has similar pharmacological spectrum as tamoxifen.
  11. Clomiphene is an older partial agonist partial agonist, a weak estrogen that also acts as a competitive inhibitor of endogenous estrogens.
  12. It is considered to be the drug of choice for inducing ovulation and is also used in azoospermia. Half-life of drug is 7 days and is eliminated in urine.

Endocrinology Flashcard List

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