Drug Mechanisms Of Action

Front 1

sulfonylureas

Back 1

block K+ channels of β cells --> depolarization --> ↑Ca+ --> release of insulin

Front 2

metformin

Back 2

↓ gluconeogenesis

Front 3

glitazones

Back 3

↑ target cell sensitivity to glucose via PPARs

Front 4

α-glucosidase inhibitors

Back 4

inhibit brush border α-glucosidase; acarbose, miglitol

Front 5

xenatide

Back 5

GLP-1 receptor full agonist --> augments insulin secretion

Front 6

orlistat

Back 6

inhibits pancreatic lipases; used in obesity

Front 7

sibutramine

Back 7

serotonin/norepinephrine reuptake inhibitor; obesity management

Front 8

propylthiouracil/methimazole

Back 8

inhibits organification and coupling

Front 9

anastrozole

Back 9

aromatase inhibitor --> ↓ estrogen synthesis

Front 10

clomiphene

Back 10

↓ feedback inhibition --> ↑FSH/LH --> ↑ovulation; fertility drug

Front 11

tamoxifen/raloxifene

Back 11

estrogen receptor agonist in bone; estrogen receptor antagonist in breast; partial agonist in endometrium

Front 12

mifepristone

Back 12

progesterone antagonist --> abortifacient

Front 13

flutamide

Back 13

androgen receptor blocker

Front 14

leuprolide

Back 14

GnRH analog

Front 15

finasteride

Back 15

5-α-reductase inhibitor --> ↓dihydrotestosterone

Front 16

biphosphonates

Back 16

hydroxyaptite analog increases bone formation

Front 17

antithrombin III

Back 17

activated by heparin; inactivates thrombin, IXa, Xa, XIa

Front 18

tPA

Back 18

tissue plasminogen activator; fibrinolytic; generates plasmin from plasminogen

Front 19

protein C

Back 19

inactivates factors Va and VIIIa --> anticoagulation

Front 20

heparin

Back 20

activates antithrombin III

Front 21

protamine sulfate

Back 21

binds negatively-charged heparin

Front 22

warfarin

Back 22

epoxide reductase inhibitor decreases vitamin K-dependant factors

Front 23

clopidogrel

Back 23

blocks platelet ADP receptors --> ↓platelet activation

Front 24

abciximab

Back 24

gpIIb/IIIa antagonist --> ↓platelet aggregation

Front 25

methotrexate

Back 25

inhibits dihydrofolate reductase --> ↓dTMP --> ↓DNA synthesis

Front 26

5-FU MOA

Back 26

inhibits thymidylate synthase --> ↓dTMP --> ↓DNA synthesis

Front 27

6-MP

Back 27

activated by HGPRTase --> blocks purine synthesis

Front 28

cytarabine (ara-C)

Back 28

DNA polymerase inhibitor

Front 29

cyclophosphamide

Back 29

alkylating agent ---> attacks guanine N7 --> denatures DNA;

Front 30

cisplatin

Back 30

alkylating agent cross-links DNA strands

Front 31

doxorubicin

Back 31

intercalates DNA inhibits topoisomerase II

Front 32

actinomycin D (dactinomycin)

Back 32

intercalates DNA inhibits topoisomerase

Front 33

bleomycin

Back 33

formation of free radicals cause breaks in DNA strands

Front 34

hydroxyurea

Back 34

inhibits ribonucleotidde reductase --> decreases DNA synthesis

Front 35

vincristine

Back 35

bind tubulin during M phase blocking polymerization of microtubules and formation of mitotic spindle

Front 36

cyclosporine

Back 36

binds cyclophillin --> ↓calcineurin --> ↓IL-2, IL-3, IFN-gamma; use in organ transplants

Front 37

tacrolimus

Back 37

inhibits calcineurin --> ↓IL-2, IL-3, IFN-gamma; use in organ transplants

Front 38

infliximab

Back 38

monoclonal Ig against TNF

Front 39

trastuzumab

Back 39

erb-B2 antagonist

Front 40

dacliximab

Back 40

blocks IL-2 receptors

Front 41

etanercept

Back 41

Recombinant TNF receptor binds TNF

Front 42

theophylline

Back 42

inhibits phosphodiesterase and increases cAMP --> bronchodilation

Front 43

ipratropium

Back 43

antimuscarinic

Front 44

cromolyn

Back 44

stabalizes mast cell membrane and inhibits degranulation

Front 45

zileuton

Back 45

5-lipoxygenase inhibitor --> decreases leukotrienes

Front 46

lukasts

Back 46

leukotriene receptor antagonists

Front 47

guainfenesin

Back 47

expectorant

Front 48

colchicine

Back 48

depolymerizes tubulin microtubules, prevents leukocyte chemotaxis and degranulation

Front 49

probenecid

Back 49

inhibits reabsorption of uric acid in PCT

Front 50

allopurinol

Back 50

inhibits xanthine oxidase and decreases uric acid

Front 51

isoniazid

Back 51

Inhibits mycolic acid synthesis; prodrug requires conversion by catalase; resistance: deletions if katG gene encodes catalase needed for activation; deletions in inhA gene encodes acyl carrier protein, the target

Front 52

rifampin

Back 52

Inhibits DNA-dependant RNA polymerase; resistance via change in enzyme

Front 53

ethambutol

Back 53

Inhibits synthesis of cell wall component arabingalactan

Front 54

polyenes

Back 54

Formation of artificial pores in the ergosterol membranes disrupts membrane permeability; ampB, nystatin

Front 55

azoles

Back 55

Fungicidal by inhibiting 14-alpha-demethylase which converts lanosterol to ergosterol

Front 56

Amantadine, enfurvitide

Back 56

block viral penetration and uncoating

Front 57

Acyclovir, foscarnet, ganciclovir

Back 57

inhibit viral DNA polymerases

Front 58

Foscarnet, ribavirin

Back 58

inhibit viral RNA polymerases

Front 59

Zidovudine, didanosine, zalcitabine, lamivudine, stavudine, nevirapine, delavirdine, efavirenz

Back 59

inhibit viral reverse transcriptase

Front 60

Indinavir, ritonavir, saquinavir, nelfinavir

Back 60

inhibt viral aspartate protease

Front 61

Zanamivir, oseltamivir

Back 61

inhibit viral neuraminidase

Front 62

fenoldopam

Back 62

D1 receptor agonist; relaxes renal vasculature; use in malignant hypertension

Front 63

cilostazol

Back 63

inhibits platelet aggregation and phosphodiesterase --> increases cAMP

Front 64

nitrates

Back 64

↑NO --> ↑guanylate cyclase and cGMP --> ↓Ca --> ↓myosin light chain kinase --> myosin dephosphorylation --> muscle relaxation

Front 65

nytroglycerin

Back 65

venodilation --> ↓preload --> ↓cardiac work

Front 66

imatimab

Back 66

inhibitor of BCR/Abl tyrosine kinase of CML without apoptosis

Front 67

rituximab

Back 67

monoclonal Ab against CD20 used in B-cell lymphomas

Front 68

lamotrigine

Back 68

blocks Na channels and glutamate receptors

Front 69

azathioprine

Back 69

6-MP precursor

Front 70

muronomab (okt3)

Back 70

CD3 antagonist blocks signal transduction complex

Front 71

anakinra

Back 71

IL-1 receptor antagonist