Final- Drug MOA and distinguishing characteristics

Question 1

MOA of chloroquine? what is it used to tx? Distinguishing characteristics? be careful to use in what 2 populations?

Answer 1

MOA: inhibit reproduction via damaging parasitic DNA; damages membrane of infected RBC and inactivates enzymes of plasmodium that normally polymerizes heme that is released as the parasite digests host Hgb- this leads to soluble heme which is toxic to the parasite
txs malaria
DCs: given PO, rapidly absorbed, given early can allow for cure in less than 1 wk, now some resistance reported; caution in pts w/hepatic dysfxn and can cause severe hemolysis in pts w/G6PD deficiency

Question 2

MOA of metronidazole? what is it used to tx? Distinguishing characteristics? caution in what pts? C/Is?

Answer 2

MOA: inhibits reproduction, binds to protozoan or anaerobic bacterial DNA which halts DNA cell division
txs: ambeiasis, protozoa, trichomoniasis
DCs: inhibits aldehyde dehydrogenase in liver, highly lipid soluble, can cause metallic taste
C/Is: EtOH, caution in pts w/ G6PD deficiency as it can cause severe hemolysis

Question 3

MOA of mebendazole? what is it used to tx? Distinguishing characteristics?

Answer 3

MOA: destroys microtubules
tx: helminthic infxns
MOST COMMONLY USED OF ALL ANTI-HELMINTHICS

Question 4

MOA of ivermectin? what is it used to tx? avoid with what? cidal or static?

Answer 4

MOA: increases GABA transmission which hyperpolarizes excitable tissues so can’t have AP’s appropriately, overall inhibits the inhibitory mechanism of overexcitation which leads to tetany
tx: anti-helminthic
avoid using with benzodiazepines and barbituates
cidal to helminths

Question 5

MOA of pyrethrins? what is it used to tx? source?

Answer 5

MOA: sustain open Na2+ channels in insects which causes tetany- repeated and extended nerve d/c from insects, insect seizures before death, replaced irreversible cholinesterase inhibitor
tx: parasitic infxns, insecticide, insect repellant
from chrysanthemum flower

Question 6

MOA of artemisinin? what is it used to tx? Distinguishing characteristics?

Answer 6

MOA: schizonticide in all malaria forms, possibly via free radical formation
tx: malaria
DCs: derivative of Chinese herbal med- qinghao su; limited resistance so emerging as first line drug over quinine derivatives to tx malaria

Question 7

MOA of cisplatin? what is it used to tx? SEs?

Answer 7

MOA: platinum based drug- platinum reacts w/DNA of rapidly dividing cells which binds to and causes cross-linking of DNA–> apoptosis
tx: neoplasms- carcinomas, sarcomas, small cell lung CA, ovarian CA, lymphomas, germ cell tumors, solid tumors, bladder CA, metastatic testicular carcinoma
SEs: high nephrotoxicity, high frequency hearing loss, tinnitus, possible BM suppression, anaphylaxis

Question 8

MOA of cyclophosphamide? what is it used to tx? Distinguishing characteristics?

Answer 8

MOA: alkylating agent- introduces alkyl group to DNA which prevents DNA or RNA replication and inhibits nucleic acid fxn
txs: neoplasms- acute lymphocytic leukemia, Hodgkin’s dz, non-Hodgkin’s, breast, ovarian, lung CA, MM, sarcomas, CLL

Question 9

MOA of metotrexate? what is it used to tx? Distinguishing characteristics?

Answer 9

MOA: antimetabolite- interferes w/formation of DNA or RNA by preventing access to key metabolic components, DMARD, immunosuppressive, competitively inhibits dihydrofolate reductase
tx: neoplasms- lung, breast CA, leukemia, Hodgkin’s and non-Hodgkin’s, cutaneous T cell lymphoma, head and neck CA, osteosarcoma
DCs: renal excretion is primary route of elimination, inhibits S phase

Question 10

MOA of doxorubicin? what is it used to tx? Distinguishing characteristics? SEs?

Answer 10

MOA: antibiotic-like drug, breaks DNA during replication and inhibits protein synthesis
tx: neoplasms
DCs: most efficacious for broadest spectrum, must be administered rapid IV or risk tissue necrosis at site of injection
SEs: cardiotoxicity, alopecia, anorexia, red urine dt pigment in drug and renal excretion

Question 11

MOA of paclitaxel? what is it used to tx? source? SEs?

Answer 11

MOA: microtubule inhibitor, reversibly binds to microtubules which prevents cell division, inhibits M (mitosis) phase
tx: advanced ovarian CA, metastatic breast CA
source: Pacific Yew Tree
SEs: N/V, anorexia, arthralgia, alopecia

Question 12

MOA of tamoxifin? what is it used to tx? SEs?

Answer 12

MOA: hormonal inhibitor- reduces natural stimulation of tissue growth and proliferation; specifically an estrogen antagonist; blocks RNA synthesis
tx: early breast CA
SEs: hot flashes and other menopausal sxs, increased risk for uterine CA

Question 13

MOA of trastuzumab? what is it used to tx? Distinguishing characteristics? SE?

Answer 13

MOA: binds to HER2 sites in breast CA tissue which inhibits proliferation of cells that overexpress HER2 protein
tx: metastatic breast CA
DCs: molecule too lg to cross BBB, administer IV
SE: cardiotoxicity

Question 14

MOA of acetylcholine? what is it used to tx? Distinguishing characteristics?

Answer 14

MOA: muscarinic and nicotinic agonist
tx: possible opthalmic use but other products are better
DCs: quaternary ammonium group= too lg to cross BBB b/c lipid insoluble

Question 15

MOA of acyclovir? what is it used to tx? Distinguishing characteristics? static or cidal?

Answer 15

MOA: guanosine analog that is incorporated into viral DNA and inhibits further viral synthesis
tx: herpes (HSV 1, 2), encephalitis, meningitis, varicella whne given in high enough doses
DCs: can cross BBB, resistance is increasing
static= only works against viruses that are actively replicating

Question 16

MOA of albuterol? what is it used to tx? Distinguishing characteristics? SEs?

Answer 16

MOA: B2 receptor agonist, SABA
tx: asthma, COPD (relief only)
DCs: effective orally or by inhalation, limited CV effects, specific for bronchial system so no effects on myocardium really
SEs: weak and occasional tachycardia, vasodilation

Question 17

MOA of amiodarone? what is it used to tx? SE?

Answer 17

MOA: class 3 anti-arrhythmic= K+ channel blockers
tx: arrhythmias
SE: QT prolongation

Question 18

MOA of amoxicillin-clavulinate? what is it used to tx? cidal or static? SEs?

Answer 18

MOA: penicillin aspect and beta-lactamase inhibitor component- affects cell wall synthesis of beta-lactam ring and neutralizes beta-lactamase
bacteriocidal
SE: c. diff colitis

Question 19

MOA of amphotericin B? what is it used to tx? Distinguishing characteristics?

Answer 19

MOA: effects ergosterol synthesis in cell wall of fungus
tx: mycoses
GOLD STANDARD to tx mycotic infxn

Question 20

MOA of atenolol? what is it used to tx? effects on target organ? Distinguishing characteristics? SE of abrupt discontinuation?

Answer 20

MOA: selective beta-1 antagonist
tx: arrhythmias, prophylaxis, MI, HTN, angina
effects on heart: blunts cardiac stimulation, prevents reflex tachycardia, decreases HR, contractility and BP
DCs: specificity for the heart so no problem for asthmatics or diabetics to use; slows down the heart and decreases force of contractions (negative ionotropic and chronotropic effects)
abrupt discontinuation causes reflex tachycardia

Question 21

MOA of atorvastatin? what is it used to tx? SEs? how to offset SEs? CYP it utilizes?

Answer 21

MOA: inhibits rate limiting step in formation of cholesterol (HmgCoA) so liver can’t produce as much cholesterol and therefore has to increase uptake from blood stream by upregulating # of LDL receptors on liver
tx: first line tx for primary and secondary prevention of ASCVD, familial hypercholesterolemia
SEs: myalgias, can give CoQ10 to help with myalgia
utilizes CYP450, 3A4

Question 22

MOA of atropine? what is it used to tx? Distinguishing characteristics? SEs?

Answer 22

MOA: muscarinic receptor antagonist, inhibits SLUD, dilates bronchus
tx: diarrhea, once used to tx asthma, mydriasis and cycloplegia
DC: tertiary ammonium compound= can cross BBB
SEs: inhibits SLUD, can cause toxicity esp in children even after just ophthalmic use

Question 23

MOA of azithromycin? what is it used to tx? Distinguishing characteristics? SEs? static or cidal?

Answer 23

MOA: binds reversibly to 50s ribosome subunit
tx: bacterial infxn- respiratory, chlamydia, gonorrhea, sinusitis, bronchitis, COPD, atypical respiratory pathogens
DCs: concentration dependent so have to give the 1st dose as a loading dose, THE leading selling abx in N. America
SEs: QT prolongation, diarrhea
bacteriostatic

Question 24

MOA of bethanechol? what is it used to tx? Distinguishing characteristics?

Answer 24

MOA: muscarinic agonist
tx: gastroparesis, urinary bladder paresis, paralytic bowel, urinary retention, xerostomia, ocular diagnostic
DCs: not metabolized by esterase enzymes, relatively long 1/2 life, quaternary ammonium compound, particular affinity for gut and bladder SM, use to keep Ach in synapse longer

Question 25

MOA of carvedilol? what is it used to tx? Distinguishing characteristics? C/Is? effects on end organ?

Answer 25

MOA: both alpha and beta antagonist activities tx: anti-arrhythmic, CHF, MI w/rEF, prophylactic, HTN, angina (off-label use) DCs: shield myocardium from chronically toxic effects of NE levels, return myocardial density to normal C/Is: cardiogenic shock, symptomatic bradycardia, 2nd or 3rd degree heartblock w/o pacemaker, severe reactive airway dz, DO NOT USE IN THOSE W/ASTHMA OR ACTIVE BRONCHOSPASM effects on heart: blunts cardiac stimulation, prevents reflex tachycardia, decreases HR, contractility and BP

Question 26

MOA of cephalexin? what is it used to tx? Distinguishing characteristics?

Answer 26

MOA: beta-lactam ring which inhibits formation of bacterial cell wall, cephalosporin, 1st generation, most activity against G(+) bugs tx: UTIs, skin infxns, some respiratory, surgical prophylaxis DCs: alt to PNC, does NOT cover enterococcus spp

Question 27

MOA of clopidogrel? what is it used to tx? Distinguishing characteristics?

Answer 27

MOA: inhibits aggregation of platelets; irreversibly blocks P2Y12 component on ADP receptors on platelet surface tx: post-NSTEMI, ACS, CVA, PCI and arterial occlusive dz to prevent clots DCs: duration lasts for lifespan of platelet

Question 28

MOA of digoxin? what is it used to tx? Distinguishing characteristics? SEs? source?

Answer 28

MOA: cardiac glycoside, Na-K-ATP-ase inhibitor, likely dt benefits from neurohormonal inhibition tx: arrhythmias, CHF, SVT/SVA, indicated w/concurrent a. fib DCs: very narrow therapeutic range, NO SURVIVAL BENEFIT SEs: diuresis, changes in yellow/green perception, anorexia, N/V, diarrhea, constipation, bradycardia source: fox glove

Question 29

MOA of diltiazem? what is it used to tx? C/I? SEs?

Answer 29

MOA: calcium channel blocker, class IV anti-arrhythmic, prevents release of Ca2+ which prevents contraction of SM, d/c of impulses in conduction system of heart tx: atrial arrhythmias, HTN, SVT, angina C/I in those w/hypotension, reduced LVEF, AV block, Wolff Parkinson White arrhythmia

Question 30

MOA of doxycycline? what is it used to tx? Distinguishing characteristics? SEs? cidal or static?

Answer 30

MOA: inhibits protein synthesis by attaching to 30s ribosomal subunit, tetracycline abx tx: respiratory, intracellular infxns, acne, rosacea, chlamydia, SSTIs DCs: increasing resistance SEs: teeth discoloration in children, chelation w/Ca2+, photosensitivity, skin discoloration bacteriostatic

Question 31

MOA of epinephrine? what is it used to tx? Distinguishing characteristics? SEs?

Answer 31

MOA: alpha 1, 2; beta 1, 2 stimulation (G protein which facilitates 2nd messengers) tx: anaphylaxis, adjunct to local anesthesia (alpha 1), arrhythmias, cardiac emergencies, bronchospasms DCs: more B and less A activity than NE, ineffective orally, very short 1/2 life SEs: tachycardia, increased CO, HTN

Question 32

MOA of ezetimibe? what is it used to tx?

Answer 32

MOA: inhibits absorption of dietary and biliary chol form gut, reduces absorption of chol, disrupts chylomicron formation, ultimately upregulates LDL receptors on the liver and lowers LDL-c tx: adjunctive tx in homozygous familial hypercholesterolemia and primary hyperlipidemia

Question 33

MOA of fluconazole? what is it used to tx? Distinguishing characteristics?

Answer 33

MOA: effects ergosterol formation tx: mycotic infxns DCs: #1 prescribed -azole compound as an anti-mycotic

Question 34

MOA of furosemide? what is it used to tx? SEs?

Answer 34

MOA: loop diuretic- inhibits Na-K-Cl cotransporter in thick ascending limb of loop of henle to inhibit Na2+ and Cl- reabsorption so as to decrease overall fluid load and CO tx: HTN, CHF SEs: hypokalemia

Question 35

MOA of genatmycin? what is it used to tx? Distinguishing characteristics? SEs? cidal or static? don't administer along with what and why?

Answer 35

MOA: binds to ribosomal subunit (irreversibly) so as to inhibit protein synthesis tx: topical abx therapy of bacterial conjunctivitis DCs: broad spectrum SEs: VERY TOXIC! don't use unless most other abx have failed, MC of all aminoglycosides used, nephrotoxicity, ototoxicity bacteriocidal don't administer w/diuretics b/c they change the composition of endoline which affects protein synthesis w/in cochlea and vestibular appartus

Question 36

MOA of hydralazine? what is it used to tx? Distinguishing characteristics? SEs?

Answer 36

MOA: vasodilator, antioxidant (inhibits destruction of NO), arteriole dilator tx: HTN, CHF DCs: not recommended unless unable to tolerate ACE I, consider in African American population SEs: reflex tachycardia

Question 37

MOA of hydrochlorothiazide? what is it used to tx? SEs?

Answer 37

MOA: increase the osmolality w/in the nephron so Na2+ will stay in nephron which will draw water into the lumen and excrete it, active in DCT SEs: hypokalemia

Question 38

MOA of ipratropium? what is it used to tx? Distinguishing characteristics?

Answer 38

MOA: muscarinic antagonist tx: rhinorrhea, COPD, asthma DCs: quaternary ammonium compound= can't get into CNS

Question 39

MOA of latanoprost? what is it used to tx? Distinguishing characteristics?

Answer 39

MOA: prostaglandin analog so increase aqueous outflow tx: open angle glaucoma (1st line tx or can tx w/Beta blocker as well) DCs: PGs don't have single target tissues- also receptors in myometrium SM so can cause uterine contractions

Question 40

MOA of lisinopril? what is it used to tx? SEs?

Answer 40

MOA: blocks convsersion of angiotensin 1 to angiotensin 2; inhibiting one of the most potent vasoconstrictors we are capable of producing tx: HTN, high peripheral resistance, CHF, used in all pts w/reduced EF to prevent HF SEs: cough, reflex tachycardia, hypotension, angioedema, teratogenic, hyperkalemia

Question 41

MOA of metoprolol? what is it used to tx? Distinguishing characteristics? SEs?

Answer 41

MOA: B1 receptor antagonist, cardioselective tx: prophylactic HF, blunts cardiac stimulation, prevents reflex tachycardia, decreases HR, contractility, BP, MI, CHF, angina, HTN DCs: anti-HTN w/o risk to asthmatics and diabetics b/c no beta 2 activity

Question 42

MOA of metronidazole? what is it used to tx? Distinguishing characteristics? SEs?

Answer 42

MOA: inhibits nucleic acid synthesis tx: only tx anaerobes, no G(+) or G(=)s DCs: cannot use w/EtOH, metallic taste, "disulfiram rxn"

Question 43

MOA of montelukast? what is it used to tx? Distinguishing characteristics? SEs?

Answer 43

MOA: LTR antagonist (blocks receptor), inhibits inflammation tx: asthma DCs: metabolized in the liver, drug interactions and liver effects not evident

Question 44

MOA of mupirocin? what is it used to tx? Distinguishing characteristics? SEs?

Answer 44

MOA: exerts antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis tx: bacterial skin infxn, prevention, MRSA DCs: go to drug when looking for something that is topical

Question 45

MOA of nitroglycerine? what is it used to tx? Distinguishing characteristics? SEs?

Answer 45

MOA: vasodilator, stimulates NO receptors, relaxation of vascular SM leading to reduced preload and reduced O2 consumption tx: angina, more specific to venous dilation, prevention of stress induced angina DCs: short 1/2 life b/c broken down so quickly, metabolized before gets out of gut so can't take orally, sublingual is the MC way to take it, most destroyed on first pass in liver, immediate sx relief SEs: hypotension, H/A, flushing, light headedness

Question 46

MOA of phenylephrine? what is it used to tx? Distinguishing characteristics? SEs?

Answer 46

MOA: alpha 1 agonist tx: hemorrhoids, nasal congestion, mydriatic (pupillary constriction) DCs: limited access to CNS, effective orally SEs: rebound congestion, increased peripheral resistance, reflex bradycardia

Question 47

MOA of propranolol? what is it used to tx? Distinguishing characteristics? avoid in what pts?

Answer 47

MOA: beta 1 and 2 antagonist (non-selective) tx: MI, HTN, angina, migraine prophylaxis, blunts cardiac stimulation, prevents reflex tachycardia, decreases HR, contractility and BP, SVA DCs: abrupt discont. will cause reflex bradycardia, significant 1st pass metabolism avoid in pts w/heart block or severe bradycardia

Question 48

MOA of quinidine? what is it used to tx? Distinguishing characteristics? SEs?

Answer 48

``` MOA: Na channel blocker, class 1 anti-arrhythmic, moderate block of both Na and K channels, slows phase 0 depolarization and slows conduction tx: ventricular tachyarrhythmias, paroxysmal recurrent a. fib, WPW syndrome DCs: class 1a anti-arrhythmic ```

Question 49

MOA of spironolactone? what is it used to tx? Distinguishing characteristics? SEs?

Answer 49

MOA: inhibits aldosterone responsible for regulating Na and K, diuretic tx: HTN DCs: potassium sparing effect! use more often since doesn't affect K levels

Question 50

MOA of sulfamethoxazole/trimethoprim? what is it used to tx? Distinguishing characteristics? SEs?

Answer 50

MOA: anti-metabolite, prevents formation of folic acid w/in bacteria tx: CA-MRSA, UTIs, OM, sinusitis, bronchitis, pneumocytis prophylaxis, SSTI DCs: increasing resistance SEs: increases effects of warfarin, Steven Johnson's Syndrome, (=) SEs in those w/sulfa allergy

Question 51

MOA of tetracycline? what is it used to tx? Distinguishing characteristics? SEs? static or cidal

Answer 51

MOA: inhibits protein synthesis by binding to 30s ribosomal subunit tx: CA-MRSA, respiratory, intracellular infxns, acne, rosacea, chlamydia, SSTIs DCs: increased resistance limits their use; alt tx for those PNC allergic, can be used in renal failure SEs: photosensitivity, tooth discoloration in children bacteriostatic

Question 52

MOA of theophylline? what is it used to tx? Distinguishing characteristics? SEs?

Answer 52

MOA: phosphodiesterase inhibitor, inhibits breakdown of c-AMP, methylxanthine and mild stimulant, bronchodilatory or anti-inflammatory or diaphragmatic inotrope? think of mostly as a reliever tx: asthma, COPD SEs: toxicity- hyperstimulation that includes diarrhea, GI cramping, tremor, tachycardia, may progress to seizures

Question 53

MOA of vancomycin? what is it used to tx? Distinguishing characteristics? SEs?

Answer 53

MOA: inhibits 2nd stage of cell wall synthesis of susceptible bacteria, may also alter the permeability of the cell membrane and selectively inhibits ribonucleic acid synthesis tx: MRSA, SSTI, pneumonia, bacteremia, endocarditis DCs: delivered IV, PO only for c. diff colitis