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Flashcards in Drugs Deck (28):
1

Ibuprofen

NSAID: reversibly inhibits COX-1 and COX-2; blocks prostaglandin synthesis
Toxicity: renal damage, fluid retention, aplastic anemia, GI distress, ulcers

2

Naproxen

aka Alleve
NSAID
can use in acute gout treatment

3

NSAIDs

ibuprofen, naproxen, indomethacin, ketrolac
Mechanism: reversibly inhibit COX-1 and COX-2; block prostaglanding synthesis
Use: antipyretic, analgesic, anti-inflammatory. Can use NSAIDs in acute gout treatment.
EtToxicity: renal damage, fluid retention, aplastic anemia, GI distress, ulcers

4

Indomethacin

NSAID
can be used to close a PDA

5

Celecoxib

COX-2 inhibitor; reversibly inhibits COX-2, but spares COX-1 (so maintains gastric mucosa)
Use: rheumatoid and osteoarthritis; patients with gastritis or ulcers
Toxicity: increased risk of thrombosis; Sulfa allergy; less toxicity to GI mucosa than NSAIDs

6

Acetaminophen

Mechanism: reversibly inhibits COX, mostly in the CNS; is inactivated peripherally
Toxicity: overdose leads to hepatic necrosis; acetaminophen metabolite depletes glutathione and forms toxic tissue adducts in the liver

7

antidote to acetaminophen?

N-acetylcysteine (regenerates glutathione, which is depleted by acetaminophen metabolite)

8

Bisphosphonates:
-Mechanism?
-Use?
-Toxicity?

Etidronate, Pamidronate, Alendronate, Risedronate, Zoledronate (IV)
Mechanism: inhibit osteoclastic activity, reduces formation and resorption of hydroxyapatite
Use: malginancy-associated hypercalcemia, Paget's disease of bone, postmenopausal osteoporosis
Toxicity: corrosive esophagitis (not zoledronate though), nausea, diarrhea, osteonecrosis of the jaw

9

Etidronate

a bisphosphonate

Mechanism: inhibit osteoclastic activity, reduces formation and resorption of hydroxyapatite
Use: malginancy-associated hypercalcemia, Paget's disease of bone, postmenopausal osteoporosis
Toxicity: corrosive esophagitis (not zoledronate though), nausea, diarrhea, osteonecrosis of the jaw

10

pamidronate

a bisphosphonate:

Mechanism: inhibit osteoclastic activity, reduces formation and resorption of hydroxyapatite
Use: malginancy-associated hypercalcemia, Paget's disease of bone, postmenopausal osteoporosis
Toxicity: corrosive esophagitis (not zoledronate though), nausea, diarrhea, osteonecrosis of the jaw

11

alendronate

a bisphosphonate:

Mechanism: inhibit osteoclastic activity, reduces formation and resorption of hydroxyapatite
Use: malginancy-associated hypercalcemia, Paget's disease of bone, postmenopausal osteoporosis
Toxicity: corrosive esophagitis (not zoledronate though), nausea, diarrhea, osteonecrosis of the jaw

12

Risedronate

a bisphosphonate:

Mechanism: inhibit osteoclastic activity, reduces formation and resorption of hydroxyapatite
Use: malginancy-associated hypercalcemia, Paget's disease of bone, postmenopausal osteoporosis
Toxicity: corrosive esophagitis (not zoledronate though), nausea, diarrhea, osteonecrosis of the jaw

13

Zoledronate

a bisphosphonate (IV):

Mechanism: inhibit osteoclastic activity, reduces formation and resorption of hydroxyapatite
Use: malginancy-associated hypercalcemia, Paget's disease of bone, postmenopausal osteoporosis
Toxicity: corrosive esophagitis (not zoledronate though), nausea, diarrhea, osteonecrosis of the jaw

14

Probenecid

treatment for chronic gout; lowers urate levels by inhibiting reabsorption of uric acid in PCT; (also, inhibits secretion of penicillin)

15

Allopurinol

drug for chronic gout treatment; lowers urate by inhibiting xanthane oxidase, so decreases conversion of xanthine to uric acid.
Also, used in lymphoma and leukemia to prevent tumor lysis-associated urate nephropathy.
Get increased concentrations of azathioprine and 6-MP, which are both normally metabolized by xanthine oxidase

16

Febuxostat

drug for chronic gout treatment; inhibits xanthine oxidase

17

Colchicine

acute gout drug;
binds and stabilized tubulin to inhibit polymerization, impairing leukocyte chemotaxis and degranulation; GI side effects (diarrhea...) if given orally

18

Etanercept

TNF-alpha inhibitor;
Mechanism: recombinant fornm of human TNF receptor that binds TNF (etanerCEPT is a TNF decoy reCEPTor)
Clinical use: rheumatoid arthritis, psoriasis, ankylosing spondalitis

19

Infliximab

TNF-alpha inhibitor
Mechanism: anti-TNF antibody
Use: Crohn's disease, rheumatoid arthritis, ankylosing spondilitis
("INFLIXimab INFLIX pain on TNF" :))

20

Adalimumab

TNF-alpha inhibitor
Mechanism: anti-TNF antibody
Clinical use: rheumatoid arthritis, psoriasis, ankylosing spondylitis

21

What do TNF-alpha inhibitors predispose to?

All TNF-alpha inhibitors (ie etanercept, infliximab, adalimumab) predispose to infection including reactivation of latent TB, because TNF blockade prevents activation of macrophages and destruction of phagocytosed microbes

22

Leuprolide

GnRH analogue:
-acts like an agonist if used in a pulsatile fashion
-acts as an antagonist when used in continuous fashion (so downregulates GnRH receptor in pituitary so decreased FSH/LH)
Use: infertility (if given pulsatile), prostate cancer (if given continuous, along with flutamide), uterine fibroids
Toxicity: anti-androgen, nausea, vomiting

23

Finasteride

anti-androgen
5-alpha-reductase inhibitor (so blocks Testosterone --> DHT);
Use: BPH; promotes hair growth (so can treat male-pattern balndess) (soooo encourages female breast growth, and prevents male hair loss!)

24

Flutamide

anti-androgen
nonsteroidal competitive inhibitor of androgens at the testosterone receptor
Use: prostate carcinoma

25

Ketoconazole

anti-androgen
inhibits steroid synthesis (inhibits desmolase)
Use: PCOS to prevent hirsutism
Side effects: gynecomastia, amenorrhea

26

Spironolactone

anti-androgen; inhibits steroid binding
Use: PCOS to prevent hirsutism
Side effects: gynecomastia and amenorrhea

Also: K+ sparing diuretic = competitive aldosterone receptor antagonist in the cortical collecting tubule
Use: hyperaldosteronism, K+ depletion, CHF
Toxicity: hyperkalemia (can lead to arrhythmias), endocrine effects with aldosterone antagonists (gynecomastia, anti-androgen effects)

27

Ethinyl estradiol, DES, mestranol

All are estrogens; all bind estrogen receptors
Uses: hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women; men with androgen-dependent prostate cancer
Toxicity: increased risk of endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, increased risk of thrombi
Contraindications: ER-positive breast cancer, history of DVTs

28

Females exposed to DES in utero?

increased risk of clear cell adenocarcinoma of vagina in females esposed to DES (an estrogen) in utero.