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MDTI Memorization > MDTI drugs - Sheet1 > Flashcards

MDTI drugs - Sheet1 Flashcards

1
Q

rATG/eATG

A

polyclonal immunosuppressives. work on many signals. deplete cells. induction/rejection therapy. Problems: batch variability. risk of antibody reponse. Leuko, thrombo, anemia

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2
Q

belatacept

A

Immunosuppressive. Fusion protein blocks CD80/86 (signal 2). induces anergy/apoptosis. Monthly infusion. Problems: risk of PTLD, infection, anemia, leukopenia.

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3
Q

basiliximab

A

Immunosuppressive. mAb against IL-2R (Signal 3) or activated TCs. induction, not rejection.

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4
Q

sirolimus/everolimus

A

Immunosuppressives. mTOR inhibitors (signal 3). induce cell cycle arrest. CYP3A4 metabolizes. Problems: narrow TI, leuko, thrombo, anemia, proteniuria, wound healing, penomitis, edema.

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5
Q

Azathioprine, myophenolate, methotrexate

A

Immunosuppressives. Cell cycle inhibitors. problems: leuko, thrombo, anemia, liver/lung/GI disease (Azathioprine: skin cancer)

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6
Q

Corticosteroids

A

Immunosuppresives. inhibit TFs (NFAT)/cytokine expression. impair macrophages. high dose can cause apoptosis in lymphos. High dose for transplant/rejection, then tapered.

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7
Q

Tacrolimus, cyclosporine

A

Immunosuppresives. Inhibit calcineurin (signal 1). CYP3A4. Problems: Very narrow TI, nephrotoxicity, neurotoxicity, metabolic disturbance. hirsutism/gingival hyperplasia (cyclo only)

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8
Q

Cisplatin

A

DNA-crosslinking antineoplastic. stable in high Cl- (blood). unstable in cell. MoR: decreased uptake, enhanced repair, tolerance, thiols.

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9
Q

cyclophosphamide/Ifosfamide

A

DNA-alkylating antineoplastic. pro-drugs. MoR: DNA repair, decreased permeability, thiols.

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10
Q

doxorubicin

A

topoisomerase II antineoplastic. MoA: intercalation. MoR: mutx of topoisomerase, enhanced repair, thiols, p-glycoprotein

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11
Q

topotecan, irinotecan

A

topoisomerase I antineoplastic (S-phase specific). MoA: intercalation. MoR: mutx of topoisomerase, enhanced repair, thiols, p-glycoprotein

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12
Q

5-FU

A

uridine analog antineoplastic. MoA: competitively binds TS, S-phase arrest. MoR: increased TS expression.

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13
Q

methotrexate

A

DHFR inhibitor (pyramindine synthesis) antineoplastic. MoR: decreased transport, efflux, increase in DHFR expression

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14
Q

taxanes (paclitaxel)

A

anti-mitotic antineoplastic. MoA: stabilizes MTs. MoR: p-glycoprotein, MAPs impair binding

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15
Q

Vinas (vinblastine)

A

antimitotic antineoplastic. MoA: destabilize MTs. MoR: p-glycoprotein, tubulin mutx, altered tubulin isofomrs

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16
Q

bevaczumab

A

mAb antiangiogenic antineoplastic. MoA: binds VEGF

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17
Q

imatinib

A

Gleevec. RTKI antineoplastic. specificity for BCR-ABL, PDGFR, c-kit TKs

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18
Q

Coxib side effects

A

Reduced GI toxicity, renal and CV toxicity in some pts (NB: PGE is COX1/2 dependent

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19
Q

Clinical utility of NSAIDs

A

Antipyretic, analgesic, anti-inflammatory, antiplatelet (aspirin)

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20
Q

Aspirin MoA

A

Irreversible inhibition of COX by acetylation (all other NSAIDs are reversible)

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21
Q

Salicylate toxicity

A

Headache, tinnitus, dizziness, nausea (irritation of CN8)

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22
Q

Non-selectively inhibit COX

A

aspirin, ibuprofen, naproxen, ketorolac

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23
Q

Selectively (relative) inhibit COX2

A

Celecoxib, valdecoxib

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24
Q

PGF2a analogue as abortifacient, postpartum bleeding

A

Carbaprost

25
Q

PGE1 analogue used with RU486 as abortifacient and for gastric cytoprotection

A

Misoprostol

26
Q

PGE2 analogue used to induce labor

A

Dinoprostone

27
Q

Pegloticase (Krystexxa)

A

Recombinant uricase given for chronic gout

28
Q

Pyrazinamide

A

URAT-1 stimulator

29
Q

Nicotinate

A

URAT-1 stimulator

30
Q

Organic acids/anions

A

URAT-1 stimulator

31
Q

Probenecid

A

URAT-1 inhibitor

32
Q

Methotrexate

A

inhibits DHF. multiple possible mechanisms. Reduces TNFa, IL-1. first line for RA. Highly teratogenic

33
Q

Leflunomide

A

inhibits Orotic Acid Dehydrogenase. Similar to methotraxate. Liver Inflammation. Can’t use within 2 years of pregnancy

34
Q

Sulfasalazine

A

combo drug. GI intolerance, sulfa allergy, rash

35
Q

Hydroxychloqoquine

A

Anti-malarial. mechanism uncertain. GI, ocular complications

36
Q

NAME?

A

chimerical monoclonal Ab

37
Q

NAME?

A

humanized monoclonal Ab

38
Q

NAME?

A

fully human monoclonal Ab

39
Q

NAME?

A

receptor fusion protein

40
Q

Anti-TNF therapies

A

used in conjunction with or on failure of methotrexate for RA. evidence for first-line use growing. risks: infections (TB!!), tolerance

41
Q

tocilizumab

A

anti IL-6 therapy. Cholesterol/liver side effects, pregnancy

42
Q

Abatacept

A

Anti CD80/86 blocks signal 2. infections/anaphylaxis. pregnancy.

43
Q

rituximab

A

anti-CD20. depletes B cells. not first line.

44
Q

Belimumab

A

Anti-BlyS. Approved for SLE

45
Q

Allopurinol/Feboxustat

A

Inhibit xanthine oxidase. Decrease urate.

46
Q

Aspirin characteristics

A

Low dose preferential for COX1. High dose analgesic. Highest doses anti-inflammatory. Toxicity is dose-dependent. Reyes. Salicylism. Zero Order Kinetics!

47
Q

Kinetics of alcohol

A

zero order

48
Q

alprostadil (probably not on exam)

A

PGE analogue. Erectile dysfunction and to maintain PDA in neonates awaiting surgery

49
Q

latanoprost (probably not on exam)

A

PGF2a analogue. used topically to reduce intraocular pressure in glaucoma

50
Q

epoprostenol (probably not on exam)

A

PGI2 analogue. used for pulmonary vasodilation in primary pulmonary HTX

51
Q

heparin

A

proteoglycan. sythesized by mast cells. makes antithrombin more effective, inactivating IIa, IXa, Xa, XIa, XIIa. Acute TE, after non-hemmorhagic stroke, DIC. IV or SQ. narrow TI. safe for pregnancy

52
Q

LMW heparin

A

specifically inactivates Xa. longer half-life and more predictable kinetics. less likely to cause HIT, but patients with HIT can’t be given LMWH. supplanting standard heparin. for some reason does not prolong PTT in vitro

53
Q

HIT/HATT

A

anti-body mediated thrombocytopenia (with thrombosis). antibodies against heparin+platelt protein. 5-10 days after drug or 24 hrs if previously sensitized.

54
Q

Fondaprinux

A

synthetic pentasaccharide that binds antithrombin inhibits Xa not IIa. given SQ

55
Q

Lepirudin/argatroban

A

direct Xa/thrombin inhibitors given IV (Lepirudin can be SQ), used in HIT pts

56
Q

Rivaroxiban/apixaban

A

direct Xa inhibitors given orally. no way to reverse!

57
Q

warfarin/coumadin

A

blocks recycling of vitamin K. decreases 2, 7, 9, 10 (anticoag) and C/S (transient procoag). range of half-lifes. patients on Abx at risk for bleeding. binds to albumin, metabolized by P450. risk of bleeding, not safe with pregnancy. skin necrosis (induction with heparin). prolongs PT. target INR varies. higher INR = higher risk of bleeding.

58
Q

fibrinolytics

A

streptokinase, urokinase, t-PA. break up clots in PE, MI, arterial occlusion, DVT. bleeding, reactions (expecialy strepto). risk of bleeding.

MDTI Memorization (2 decks)

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