Block 5: Osteoporosis Med Chem Flashcards
What are the types of bone cells?
Osteogenic cells: Stem cells in the periosteum and endosteum
Osteoblasts: Produce new bone tissue
Osteocytes: Maintain bone tissue
Osteoclasts: Breakdown bone matrix
Describe Ca2+ homeostasis?
High Ca2+ - Calcitonin from thyroid inhibits osteoclasts
(opposing action to PTH)
Testosterone and estrogen stimulate osteoblasts
What are the drug classes for osteoporosis?
- Bisphosphonates
- SERMs
- Estrogens
- PTH analogues
- Monoclonal antibody
- Calcitonin
- Calcium supplements: requires water and Vitmin D for absorption
Describe the MOA of bisphosphonates?
Nitrogen-containing and Non-N: IPP is synthesized by FPP synthase to FPP
What is the endogenous substance bisphosphonates must mimic?
2 phosphates similar to IPP
What are the types of bisphosphonates?
- Pamidronic acid (pamidronate): Aredia
- Alendronic acid (alendronate): Fossamax
- Risedronic acid (risedronate): Actonel
- Ibandronic acid (ibandronate): Boniva
- Zoledronic acid (zoledronate): Reclast/Zometa
Pamidronate
Brand
Aredia
Alendronate
Brand, Dosing
Fossamax
Dosing: QD, QW
Risedronate
Brand, Dosing
Actonel
Dosing: QD, QW, QM
Ibandronate
Brand, Dosing
Boniva
Dosing: QD, QM
Zoledronate
Brand, Dosing
Reclast, Zometa
Dosing:
* QY or Q2Y (infusion for osteoporsis)
* Q4-12W for bone metastasis
What is the MOA for PTH?
What inhibits PTH?
Calcitonin
What are the PTH analogues?
- Teriparatide
- Abaloparatide
Teriparatide
Brand, MOA, Structure
Forteo
MOA: Net proremodeling, increasing osteoblast activity with minerals are present
Structure: 1st 34 of 84 amino acid sequence of PTH (the bioactive portion)
Denosumab
Brand, MOA, Indication
XGEVA
MOA: Bind to RANKL and neutralize its activity, reduces osteoclast activity and bone resorption
Indication: Bone metastasis
