Drugs

Question 1

Ibuprofen

Answer 1

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

Question 2

Naproxen

Answer 2

aka Alleve
NSAID
can use in acute gout treatment

Question 3

NSAIDs

Answer 3

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

Question 4

Indomethacin

Answer 4

NSAID

can be used to close a PDA

Question 5

Celecoxib

Answer 5

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

Question 6

Acetaminophen

Answer 6

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

Question 7

antidote to acetaminophen?

Answer 7

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

Question 8

Bisphosphonates:

• Mechanism?
• Use?
• Toxicity?

Answer 8

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

Question 9

Etidronate

Answer 9

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

Question 10

pamidronate

Answer 10

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

Question 11

alendronate

Answer 11

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

Question 12

Risedronate

Answer 12

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

Question 13

Zoledronate

Answer 13

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

Question 14

Probenecid

Answer 14

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

Question 15

Allopurinol

Answer 15

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

Question 16

Febuxostat

Answer 16

drug for chronic gout treatment; inhibits xanthine oxidase

Question 17

Colchicine

Answer 17

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

Question 18

Etanercept

Answer 18

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

Question 19

Infliximab

Answer 19

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

Question 20

Adalimumab

Answer 20

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

Question 21

What do TNF-alpha inhibitors predispose to?

Answer 21

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

Question 22

Leuprolide

Answer 22

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

Question 23

Finasteride

Answer 23

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!)

Question 24

Flutamide

Answer 24

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

Question 25

Ketoconazole

Answer 25

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

Question 26

Spironolactone

Answer 26

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)

Question 27

Ethinyl estradiol, DES, mestranol

Answer 27

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

Question 28

Females exposed to DES in utero?

Answer 28

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