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Drug Action II > Block 5: Osteoporosis Med Chem > Flashcards

Block 5: Osteoporosis Med Chem Flashcards

1
Q

What are the types of bone cells?

A

Osteogenic cells: Stem cells in the periosteum and endosteum
Osteoblasts: Produce new bone tissue
Osteocytes: Maintain bone tissue
Osteoclasts: Breakdown bone matrix

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2
Q

Describe Ca2+ homeostasis?

A

High Ca2+ - Calcitonin from thyroid inhibits osteoclasts
(opposing action to PTH)

Testosterone and estrogen stimulate osteoblasts

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3
Q

What are the drug classes for osteoporosis?

A
  1. Bisphosphonates
  2. SERMs
  3. Estrogens
  4. PTH analogues
  5. Monoclonal antibody
  6. Calcitonin
  7. Calcium supplements: requires water and Vitmin D for absorption
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4
Q

Describe the MOA of bisphosphonates?

A

Nitrogen-containing and Non-N: IPP is synthesized by FPP synthase to FPP

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5
Q

What is the endogenous substance bisphosphonates must mimic?

A

2 phosphates similar to IPP

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6
Q

What are the types of bisphosphonates?

A
  1. Pamidronic acid (pamidronate): Aredia
  2. Alendronic acid (alendronate): Fossamax
  3. Risedronic acid (risedronate): Actonel
  4. Ibandronic acid (ibandronate): Boniva
  5. Zoledronic acid (zoledronate): Reclast/Zometa
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7
Q

Pamidronate

Brand

A

Aredia

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8
Q

Alendronate

Brand, Dosing

A

Fossamax
Dosing: QD, QW

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9
Q

Risedronate

Brand, Dosing

A

Actonel
Dosing: QD, QW, QM

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10
Q

Ibandronate

Brand, Dosing

A

Boniva
Dosing: QD, QM

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11
Q

Zoledronate

Brand, Dosing

A

Reclast, Zometa
Dosing:
* QY or Q2Y (infusion for osteoporsis)
* Q4-12W for bone metastasis

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12
Q

What is the MOA for PTH?

A
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13
Q

What inhibits PTH?

A

Calcitonin

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14
Q

What are the PTH analogues?

A
  1. Teriparatide
  2. Abaloparatide
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15
Q

Teriparatide

Brand, MOA, Structure

A

Forteo
MOA: Net proremodeling, increasing osteoblast activity with minerals are present
Structure: 1st 34 of 84 amino acid sequence of PTH (the bioactive portion)

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16
Q

How many aa is in a PTH sequence?

17
Q

Abaloparatide

Brand

A

Tymlos
No pharm difference than Forteo

18
Q

What are the types of monoclonal antibodies for osteoporosis?

A
  1. Denosumab (XGEVA)
  2. Remosozumab-aqqg (Evenity)
19
Q

Denosumab

Brand, MOA, Indication

A

XGEVA
MOA: Bind to RANKL and neutralize its activity, reduces osteoclast activity and bone resorption
Indication: Bone metastasis

20
Q

Remosozumab-aqqg

Brand, MOA

A

Evenity
MOA: DUAL MECHANISM
* Increases osteoblastic activity and bone formation by increasing sP1NP marker
* Decreases osteoclastic activity and bone resorption by decreasing sCTX marker

Drug Action II (28 decks)

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