Pharmacology Flashcards
1
Q
What are the first line treatments for osteporosis?
A
- bisphosphonates, Denosumab, SERMs (raloxifene), hormone-replacement therapy (HRT), and strontium ranelate
2
Q
Which drugs are anti-resportive in nature? Anabolic/bone-forming? Which have a dual action?
A
- anti-resorptive: bisphosphanates, Denosumab, HRT, raloxifene (SERM), Odanacatib
- bone-forming: teriparatide (synthetic PTH)
- dual action: strontium ranelate
3
Q
Bisphosphanates
A
- “-dronate” (etidronate, aldendronate, risedronate)
- anti-resportive drugs used to treat osteoporosis and paget disease
- MOA: the drug gets taken up in large amounts and is stored in bone; when osteoclasts come in contact with the drug, they undergo apoptosis
- etidronate (older form): resembles PPi and generates cytotoxic ATP
- aldendronate/risendronate (newer form): much more potent; contains nitrogen and interferes with protein trafficking
- side effects: esophageal irritation, dyspepsia, heartburn, nausea (these are swallowed), osteonecrosis of the jaw
4
Q
Zolderonic Acid
A
- an IV form of bisphosphanates
- avoid the side effects of the oral forms, but has its own side effects: flu-like symptoms and osteonecrosis of the jaw)
5
Q
Denosumab
A
- an anti-resorptive drug used to treat osteoporosis
- MOA: monoclonal antibody against RANKL; prevents osteoclast activation
- side effects: hives, difficulty breathing, swelling of the face and lips, osteonecrosis of the jaw
6
Q
Teriparatide
A
- synthetic PTH; a bone-forming drug used to treat osteoporosis
- MOA: PTH analog; in small, intermittent doses, it promotes osteoblast activity without activating osteoclasts
- side effects: if used too long, osteoclast activation will dominate; increased risk for osteosarcoma if used longer than 18 months
7
Q
Hormone Replacement Therapy (HRT)
A
- anti-resorptive drugs used to treat osteoporosis in post-menopausal women
- estrogen is re-introduced to the body, increasing it protective effects against bone loss
- side effects: increased risk for CAD, thromboembolism, and breast cancer
8
Q
Raloxifene (a SERM)
A
- SERM: selective estrogen receptor modulator; an anti-resorptive drug used to treat osteoporosis in women
- MOA: acts like estrogen, but for specific bone receptors only, thus avoiding the increased risk of breast cancer seen with HRT
- only works on the vertebrae
- side effects: venous thromboembolism and CAD
9
Q
Strontium Ranelate
A
- a drug used to treat osteoporosis
- MOA: stimulates osteoblast activity and induces osteoclast apoptosis
10
Q
Odanacatib
A
- an anti-resorptive drug used to treat osteoporosis
- MOA: inhibits cathepsin (the enzyme used by osteoclasts to degrade the organic component of bone matrix)
11
Q
” -dronate “
A
- bisphosphanate
12
Q
What treatments are available for rheumatoid arthritis?
A
- analgesics for pain
- NSAIDs for pain and stiffness and some anti-inflammation
- corticosteroids for anti-inflammation
- DMARDs and biological agents (TNF inhibitors) for anti-inflammation (these are the mainstay of treatment)
13
Q
NSAIDs
A
- reverse inhibition of cyclooxygenase (both COX-1 and COX-2) blocks prostaglandin synthesis to provide an analgesic and anti-inflammatory action
- used to provide relief in rheumatoid arthritis, gout, seronegative spondyloarthropathies, etc.
- often given with PPIs as prophylaxis for gastric ulcers
- (the NSAID Indomethacin is given to close PDA!)
14
Q
Aspirin
A
- irreversibly inhibits cyclooxygenase (both COX-1 and COX-2) to block prostaglandin synthesis; a type of NSAID
- in small doses: decreased platelet aggregation
- in intermediate doses: anti-pyretic and analgesic
- in high doses: anti-inflammatory
15
Q
DMARDs
A
- disease modifying anti-rheumatic drugs
- the mainstay of treatment for rheumatoid arthritis
- Methotrexate, Sulfasalazine, hydroxychloroquine, Leflunomide
- alleviate inflammation to greatly improve joint function
