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M2 Fall > Pharmocolgy Unit 4 > Flashcards

Pharmocolgy Unit 4 Flashcards

1
Q

penicillin G

A

penicillin; acid labile (IV or IM, not oral); procaine/benzathine forms -> water insoluble -> slow release over weeks; spectrum: gram+ and some gram- cocci (not gram- rods) adverse: allergies, neurotoxic, seizures, stevens-johnson syndrome (rash, swelling, blistering around mouth); uses: non penicillinase producing microbes

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2
Q

penicillin V

A

penicillin; acid stable (orally effective-65% absorbed vs 35% for pen G)

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3
Q

oxacillin

A

b-lactamase resistant; acid stable; food interferes w absorption; can be parenteral; spectrum/use: penicillinase-producing Staph and Strep; resistance: MRSA (BPB w low affinity for drugs); adverse: less than PenG,V, hepatitis at high dose

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4
Q

amoxicillin

A

extended spectrum aminopenicillin; acid stable (oral - not affected by food); spectrum/use: non-lactamase gram- rods (E coli, H influenza, Salmonella, Shigella, not sub for penG,V), prophylaxis against bacterial endocarditis

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5
Q

ampicillin

A

extended spectrum aminopenicillin; acid stable (oral); spectrum/use: non-lactamase gram- rods (E coli, H influenza, Salmonella, Shigella, not sub for penG,V),

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6
Q

piperacillin

A

extended spectrum ureidopenicillin; parenteral admin; anti-pseudomonal; reserved for serious Klebsiella or Pseudomonas; combi w aminoglycosides to prevent resistance

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7
Q

ticarcillin

A

extended spectrum caboxypenicillin; parenteral admin; antipseudomonal (rarely used alone)

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8
Q

clavulonic acid

A

b-lactamase suicide inhibitor; no abx activity alone; used combi w extended spectrum penicillins (w amoxicllin = augmentin)

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9
Q

sulbactam

A

b-lactamase suicide inhibitor; no abx activity alone; used combi w extended spectrum penicillins

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10
Q

tazobactam

A

b-lactamase suicide inhibitor; no abx activity alone; used combi w extended spectrum penicillins

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11
Q

1st gen cephalosporin/cephalexin

A

cephalosporin; most acid stable (oral); spectrum/use: broadest against gram+ (surgical prophylaxis, some gram- bacilli

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12
Q

2nd gen cephalosporin/cefuroxime

A

cephalosporin; IV, IM; adverse: antabuse effect; spectrum/use: only group with significant activity against anaerobes (sinusitis, otitis, peritonitis, diverticulitis

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13
Q

3rd gen cephalosporin/ceftazidime

A

cephalosporin: IV, IM; adverse: antabuse effect; resistance: induce AmpC; spectrum/use: anti-pseudomonal, -pneumococcal, serious gram- infections (meningitis, pneumonia, gonorrhea); used in children/infants with severe infection; pentrates CNS

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14
Q

4th gen cephalosporin/cefepime

A

cephalosporin; IV, IM; resistance: indice AmpC; spectrum/use: anti-pseudomonal, high resistance to B-lactamases: useful in treating penicillin-resistant steptococci and enterobacter

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15
Q

imipenem

A

carbapenem; has B-lactam ring-> blocks PDG x-linking; more efficient binding to PBPs than pcn or ceph; penetrates OM of gram-; broadest spectrum B-lactam drug (NOT MRSA, VRE); resistant to most B-lactamases but induces those that inactivate pcns and cephs; resistance: alterations in PBP; parenteral admin; renal metabolism and inactivation (admin w dehydropeptidase cilastatin); adverse: cross-allergenic w pcn, rare GI effects, superinfections, neurotoxic; uses: 2nd line therpay for serious nosocomial infection (klebsiella, E cloi)

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16
Q

meropenem

A

carbapenem

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17
Q

cilastatin

A

dehydropeptidase inhibitor

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18
Q

aztreonam

A

monobactam; binds PBPs; relative resistance to B-lactamases; IV, IM use only (poor oral absorption); No X-reactitivity w pcns; spectrum: narrow, gram- aerobes (pseudomonas) NOT gram+, anaerobes; uses: gram- UTIs, lower RTIs, systemic infxn

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19
Q

bacitracin

A

non-b-lactam PDG inhibitor; deple3tes lipid carrier for PDG synthesis; topical use only (poor absorption); narrow spectrum: gram+, Neisseria, T pallidum; toxicity: nephrotoxic; uses: skin and ophthalmic infection, combi w/ polymyxin B

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20
Q

D-cycloserine

A

non-b-lactam PDG inhibitor; analog of D-ala, blocks D-ala addition (step2); good CNS penetration, oral, broad spectrum; toxicity: serious CNS effects; uses: 2nd line Tb drug

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21
Q

daptomycin

A

cyclic lipopeptide, membrane depolarization; bactericidal; IV admin, renal excretion; spectrum/use: like vancomycin (gram+ including MRSA, ALSO TREATS VRE; adverse: myopathy $$$

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22
Q

fosfomycin

A

non-b-lactam PDG inhibitor; analog of PEP, blocks step1 of PDG synthesis; broad spectrum; resistance: after multiple doses; toxicity: diarrhea, vaginitis; Uses: single dose oral tx for UTI by E. faecalis and E. coli

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23
Q

vancomycin

A

non-b-lactam PDG inhibitor; binds D-ala terminus (substrate) and blocks X-linking of PDG; bacericidal in dividing cultures (except static in enterococci); IV admin (no IM) oral rarely (poor absorption); distributes to bone, meninges; renal excretion; narrow spectrum: gram+ (most MRSA); resistance: VRenterococci van genes, VRSA overexpress D-ala; toxicity: red man syndrome (too fast IV), ototoxic, nephrotoxic; uses: MRSA, pcn resistant S. pneumo (serious gram+ infections), combi w/ aminoglycosides-> expands spectrum to gram+

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24
Q

amikacin

A

aminoglycoside; derivative of kanamycin but less toxic; treats bacteria resistant to genta/tobra, treats Mycobacteria Tb in combi therapy

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25
Q

gentamicin

A

aminoglycoside. resistance: poor drug uptake; synergistic w/ vanco or pcn -> extends use to gram+; main use: SEVERE GM- INFECTIONS (pseudomonas, klebsiella in HIV), topical for burns, wounds, skin lesions; adverse: ototoxic, mainly vestibular/ irreversible

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26
Q

neomycin (kanamycin)

A

aminoglycoside; limited to topical and oral use; widespread resistance; significant toxicity

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27
Q

tobramycin

A

aminoglycoside; very similar to gentamicin; more active against pseudomonas; uses: pseudomonas RTI in CF

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28
Q

streptomycin

A

aminoglycoside; high resistance linits use; uses: mycobacterial Tb (no longer 1st line bc of incr resistance); adverse: deafness in newborns when taken during pregnancy

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29
Q

spectinomycin

A

aminocyclitol; binds 30S->protein synthesis inhibitor->bacteriostatic; spectrum: mostly Gm- but also many Gm+; used in MRSA and enterococci, abx-resistant gonorrhea; given IM->rapid

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30
Q

tigecycline

A

first glycylglcine; tetracycline analog; similar to tetracycline but binds 30S higher affinity; uses: strains that are tetracycline-resistant and Hershey isolate of MRSA (VRSA); adverse: well tolerated, n/v

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31
Q

tetracycline

A

tetracycline; reversible bind 30S->bacteriostatic; deposits in bone in anactive form -> teeth discoloration, poor bone development in children; can cross placenta; excreted by kidneys; spectrum: very broad -> superinfections; uses: acne, rickettsia, chlamydia, mycoplasma, yersinia, borrelia; adverse: Gi irritation, C. diff colitis, heptotoxic, nephrotoxic; DONT give to pregnant women or children<8yo

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32
Q

doxycycline

A

tetracycline; best absorption among tetracyclines; photosensitivity; eliminated as inactive chelate in feces -> no affect on normal flora=safer

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33
Q

minocycline

A

tetracycline; vestibular disturbance in women; metabolized by liver ->feces

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34
Q

azithromycin

A

macrolide; more effective than erythromycin against anaerobes; unclear mechanism of excretion; adverse: structurally different from other macrolides and does NOT induce CYP3A4

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35
Q

clarithromycin

A

macrolide; more effective than erythromycin against anaerobes; metabolized in liver -> excreted by kidney; inhibits CYP3A4 -> affect on mulitple drugs: theophylline, warfarin, carbamazepine,

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36
Q

erythromycin

A

macrolide; only acid labile; penetrates into abscesses; excretion in bile; hepatotoxic: cholestatic hepatitis with erythromycin estolate (reversible); inhibits CYP3A4 -> affect on mulitple drugs: theophylline, warfarin, carbamazepine,

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37
Q

telithromycin

A

1st member of new drug class; semi-synthetic erythromycin derivative; increased acid stability, increased 50S affinity, reduces induction of resistance, not induce cross-R; binds 50S at 2 sites; conc-dependant bacericidal vs S. pneumoniae; oral -> well absorbed; hepatic metabolism, renal excretion; MLS-typeB is resistant to drug; uses: S pneumonia, H influenza, M catarrhalis, S aureus; CA-RTIs (pneumonia), bacterial sinusitis, chronic bronchitis; adverse: GI, diarrhea, nausea, abd pain, exacerbation of disease in myasthenia gravis; competes for CYP3A4 with other drugs

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38
Q

clindamycin

A

lincosamide; binds 50S (MLS-B resistance); spectrum: most Gm+, better than macrolides vs anaerobes, esp B. fragilis (non-CNS), NOT Gm-; bacteriostatic; Resistance: slow, stepwise from methylase(MLS-B (erm), does not induce methylase expression; oral or parenteral; wide distribution including bone (active) low [] in CNS; metabolized by liver-> bile, renal excretion IMPAIRED IN HEPATIC FAILURE; uses: RTIs by anaerobes, GAS, MRSA, osteomyelitis; adverse: pseudomembranous colitis, rash, steven-johnson syndrome, anaphylaxis

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39
Q

quinupristin/dalfopristin (synercid)

A

streptogramins; IV; quinupristin binds 50S, dalfopristin enhances binding (bactericidal effect together, bacteriostatic individually); uses: MRSA, serious vanco-resistant Gm+ VRE, VRSA, S. pneumonia; adverse: pain, phlebitis at IV site; affects CYPs; resistance: quinupristin (erm-encoded methylase-> modify 50S ->MLS-B resistance, vgb-encoded lactonase -> modify drug); dalfopristin (vat/sat-encoded acetyltransferase ->modify drug, vga/vgb-encoded efflux pump)

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40
Q

sulfamethoxazole

A

sulfonamide; first abx used in US; competitively inhibits binding PABA to DHPS (high PABA (pus) inhibits activity); bacteriostatic; Selective: DHPS only function in bacteria, bacteria must synthesize folic acid; oral or IV; distributes all over incl CNS/CSF; hepatic metabolized -> renal excretion; spectrum: broad (many Gm+/-) also some arasites (plasmodium, toxoplasma) NOT rickettsia; Resistance: Staph, Strep, Enterobacteriaceae, Neisseria; X-resistance to all sufa: overproduce PABA, mutatnt DHPS, incr efflux; adverse: GI, rash, hemolytic anemia in G6PD deficiency, kernicterus in infants (compete w bili for albumin -> incr unconjugated bili}, stevens-johnson syndrome, marrow/hepatic toxic (uncommon) Uses: malaria, CNS toxoplasmosis, combi w trimethorpim for common infections

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41
Q

chloramphenicol

A

reversible binds 50S (subject to MLS-B resistance); bacteriostatic (-cidal from H influeza, N meningitidis; spectrum: very broad, most anaerobes, Gm- bacilli; resistance: drug modification, MLS-B); oral,parenteral; cross placenta; penetrates CNS; metabolized in liver-> renal excretion; uses: FEW, due to toxicity, those normally treated by tetracyclines that cant take them; adverse: hematologic, aplastic anemia, hypersensitivity, gray baby syndrome, inhibits CYPs

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42
Q

linezolid

A

binds novel site in 23S rRNA of 50S subunit (no MLS-B resistance); bacteriostatic; oral ->100% bioavailable; uses: tx MRSA, VREf, multi-drug resistant S. pneumoniae; No X-resistance w other protein synthesis inhibitors

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43
Q

mupirocin

A

topical use only; uses: impetigo from MRSA, GAS; inhibits isoleucyl tRNA synthase; rapidly metabolized to inactive (topical only); resistance reare

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44
Q

Trimethoprim

A

inhibits bacterial DHFR 100,000X better than humn DHFR; bacteriostatic alone;

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45
Q

tmp-sulfa

A

synergistic; bactericidal; oral; wide distribution; excreted in urine; spectrum: many Gm+/-, NOT pseudomonas, anaerobes, atypical bacteria; resistance: overexpress DHFR, mutant DHFR (plasmid); adverse: same as sulfas,bone marrow suppression and neutropenia, cause anti-folate effect; Uses: UTIs (decr efficacy among E coli); pneumocystis pneumonia in AIDS/transplant, sinusitis, otitis media, CA-MRSA

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46
Q

ciprofloxacin

A

fluoroquinolone; better for Gm- (incl pseudomonas); 2nd line anti-Tb

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47
Q

levofloxacin

A

fluoroquinolone; same for Gm+/-

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48
Q

moxifloxacin

A

fluoroquinolone; better for Gm+ (incl Strep)

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49
Q

amphotericin B

A

polyene; binds ergosterol-> forms pores-> ion leak -> cell death; broadest spectrum antifungal; uses: most life-threathening systemic infections (candida, aspergillus, cryptococcus) initial therapy; fungicidal; adverse: cholesterol binding accounts for toxicity; resistance: decreased ergosterol (azole tx); poor oral absorption -> used orally for GI topical tx, topical for superficial infxn, parenteral for systemic; extensive metabolism->excreted over 2 weeks by kidney; distribution in RE in lipid formulation ->liver, lung, spleen; NOT kidney (reduce toxicity), CSF (not for fungal mieningitis); adverse: local irritation, IV->immediate rxn to infusion: fever, chills, spasm, headache, hypotn, anaphylaxis, thrombophlebitis; IV->nephrotoxicity (reversible); drug interactions: incr digitalis toxicity, antagonize azoles, enhanced nephrotoxicity w aminoglycosides, cyclosporine

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50
Q

nystatin

A

polyene; similar to AmpB; narrower spectrum than AmpB; TOO toxic for parenteral use; not metabolized; topical only (not well absorbed by GI, skin, mucous membranes; uses: topical for superficial mucosal, skin, vaginal candida; drug of choice for oral cavity infections; adverse: mild but bitter and unpleasant taste

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51
Q

clotrimazole

A

imidazole; restricted to oral/topical use; effective and more palatable than alternative nystatin; drug of choice for oropharyngeal candidiasis in AIDS; swallowed drug mild Gii upset->metabolized by liver

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52
Q

ketoconazole

A

imidazole; GREATEST propensity to inhibit mammal CYPs -> inhibit adrenal/gonadal steroig synthesis, interfere with other drug metabolism; cause symptomatic hepatitis; availability of safer drugs makes use limited

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53
Q

miconazole

A

imidazole; use limited by toxicity: thrombophlebitis p IV; effective topically vs candidiasis; uses: oropharyngeal candidiasis

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54
Q

fluconazole

A

triazole; similar to ketoconazole (more selctive for fungal CYPs); best CNS penetration (cryptococcal meningitis); resistance: Candida krusei (instrinsic) glabrata (common), NOT active against aspergllus mold; good oral bioavailablility (water soluble), IV available; uses: most common systemic antifungal; 1st line for invasive candida (not krusei), cryptococcal meningitis

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55
Q

itraconazole

A

triazole; broader spectrum than flconazole: includes dimorphic (histoplasma, blastomyces, coccidioidses, and aspergillus mold); absrobed well orally, IV available; uses: aspergillus and fluconazole-resistant candida

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56
Q

posaconazole

A

tirazole; newest azole; similar to voriconazole but only azole w activity vs zygomycoses (rhizopus, mucor); good oral bioavail; toxicity: rash, incr hepatic enzymes, no visual effects; numerous drug interactions; FDA approved for prophylaxis of invasive fungal infections (BMT w GvsHD, hematologic malignancy, and neutropenia)

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57
Q

voriconazole

A

triazole; same spectrum as itraconazole, more potent vs yeast and molds; excellent oral bioavail; low toxicity (transient visual side effects, rash, incr hepatc enzymes (inhibits CY3A4); uses: immunoompromised pts, aspergillosis (better survival vs AmpB, new standard of care?) fusarium infection, fluconazole-resistant candida

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58
Q

terbinafine

A

allylamine; inhibits ergosterol synthesis blocking aqualene epoxidase; fungicidal (elevated squalene=toxic); spectrum: dermatophytes (same as griseofluvin); topical or oral->good absorption-> accumulates in skin, nails, and fatty tissue (dermatophyte sites of infection); drug interactions: admin w rifampin doubles clearance of terbinafine, admin w cimetidine decr clearance by 1/3; uses: mainstay for skin, nail infections, unusual, refractory infetions.

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59
Q

anidulafungin

A

glucan synthesis inhibitor

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60
Q

caspofungin

A

glucan synthesis inhibitor-> weakens cell wall->lysis; spectrum: primarily aspergillus, azole-resistant candida; given IV; uses: (well tolerated) invasive candida, aspergillus, molds

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61
Q

micafungin

A

glucan synthesis inhibitor

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62
Q

flucytosin

A

5-fluorocytosine; orally effective for systemic cadida/cryptococcus meningitis; fungistatic; converted to 5-FU-> inhibits thymidylate synthetase->blocks DNA synthesis and protein synthesis; human cells inefficienty convert to 5-FU; uses: combi w fluconazole, AmpB ->synergistic effect (allows for reduced AmpB dose); resistance: common, enzyme mutations; high oral biovailable, good CNS penetration, renal excretion; adverse: GI intolerance, marrow depression->anemia, lukopenia, thrombocytopenia

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63
Q

griseofluvin

A

assoc w polymerized microtubules -> blocks mitosis; only use: oral/systemic tx for dermatophytosis (limited use); induces various CYPs -> alters warfarin, oral contraception, etc.

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64
Q

ferrous fumurate

A

iron

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65
Q

ferrous gluconate

A

iron

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66
Q

ferrous sulfate

A

iron

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67
Q

deferasirox

A

chelator

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68
Q

deferoxamine

A

chelator

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69
Q

Vit B12

A

vit

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70
Q

erythropoietin

A

growth factor; stimulates proliferation, maturation, and hemoglobin formation by erythroid progenitors; acts synergistically w IL-3 and GM-CSF; stimulates relsease of reticulocytes from marrow to circulation; uses: anemia of chronic renal failure, anemia in AIDS pts treated w AZT, anemia w cancer chemo, preoperatively for autologous transfusion; adverse: increased clotting, HTn, seizures, allergic rxn mild

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71
Q

G-CSF

A

growth factor; stimulates granulocyte colonies and neutrophi production

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72
Q

GM-CSF

A

growth factor; w IL-3 stimulates proliferation of granulocytes, monocytes, and megakaryocytes

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73
Q

ethambutol

A

1st line antiTb; active gainst mulitplying bacilli; blocks cell wall synthesis; resistance from embB gene mutation (arabinosyl transferase); adverse: optic neuritis (decr VA, red-green color blindness)

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74
Q

isoniazid (INH)

A

1st line antiTb; kills actively growing bacteria; passive penetration; used as single drug for latent Tb; prodrug activated by Tb enzyme; inhibits fatty acid synthase type II system; adverse: peripheral neuropathy (give vit B6), elevated liver enzymes, fatal hepatitis (pregnant/postpartum women)

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75
Q

pyrazinamide

A

1st line antiTb; prodrug -> intracellular PZA; kills less metabolically active when low proton pump action

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76
Q

rifampin

A

1st line antiTb, anti-leprosy; active against rapidly growoing and slow metabolizing bacilli, good penetration; inhibits prokaryotic RNA polymerase; broad spectrum Gm+/-; resistance by mutation in rpoB gene; adverse: orange color in urine, sweat, tears, rash, thrombocytopenia, nephritis, hepatitis, and drug interactions

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77
Q

streptomycin

A

1st line antiTb

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78
Q

capreomycin

A

2nd line antiTb

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79
Q

kanamycin

A

2nd line antiTb; blocks protein synthesis (16S rRNA)

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80
Q

rifabutin

A

anti MAC

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81
Q

dapsone

A

anti-leprosy; used in MDT form leprosy; inhibits synthesis of dihydrofolic acid-> blocking DNA/RNA synthesis; adverse: hemolysis, hepatitis, nausea and rash

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82
Q

aspart

A

rapid acting insulin (faster than wild type) aa sequence change (B28 pro->asp) promotes absorption by preventing self-assoc

83
Q

detemir

A

long acting insulin; aa sequence change (c-terminus thr deleted, myristic acid added to c-terminus lys) incr self aggregation and binding to albumin

84
Q

glargine

A

long acting insulin; aa sequence change (A21 asn->gly, arg added at B31,32) makes insulin soluble in acidic solution but precipitate at neutral pH, decr absorption

85
Q

glulisine

A

rapid acting insulin (faster than wild type) aa sequence change (B3, B29 asn->lys, lys->glu) promotes absorption by preventing self-assoc

86
Q

lispro

A

rapid acting insulin (faster than wild type) aa sequence change (B28,B29 pro->lys, lys->pro) promotes absorption by preventing self-assoc

87
Q

NPH

A

intermediate acting insulin (slower than wild-type) wild-type sequence suspended in protamine -> forms complex that decr absorption (use waning in favor of long-acting)

88
Q

regular crystalline insulin

A

short acting insulin (slower than wild-type) with wild-type

89
Q

exenatide

A

incretin agonist; SQ injection; adverse: nausea, anorexia, headache, diarrhea, pancreatitis

90
Q

sitagliptin

A

inhibitor of incretin degredation; oral; adverse: headaches, increased rate of infections, pancreatitis

91
Q

pramlintide

A

synthetic amylin analog; SQ; used in DMII; given w insulin in DMI; inhibits glucagon secretion and has CNS-mediated anorectic effects; adverse: hypoglycemia, nausea, vomiting, anorexia

92
Q

chlorpropamide

A

1st gen sulfonylurea; ~60 hr duration

93
Q

glipizide

A

2nd gen sulfonylurea; 10-24 hr duration

94
Q

glyburide

A

2nd gen sulfonylurea; 10-24 hr duration

95
Q

glimepiride

A

2nd gen sulfonylurea; 12-24 hr duration

96
Q

tolbutamide

A

1st gen sulfonylurea; 6-12 hr duration

97
Q

repaglinide

A

meglitinide; same mechanism as sulfonylureas; more potent than 2nd gen sulfonylureas but shorter durtion (4-5 hr); adverse: hypoglycemia, use caution in renal/hepatic failure

98
Q

nateglinide

A

D-phenylalanine analog; same mechanism as sulfonylureas/meglitinides; more potent but less sustained; adverse: hyoglycemia and other effects less pronounced than in meglitinides; safer in renal failure

99
Q

metformin

A

biguanide; activate AMP-activated protein kinase (energy sensor); reduces hepatic glucose output; first choice drug for DM II; adverse: Gi discomfort, lactic acidosis, NO hypoglycemia

100
Q

rosiglitazone

A

thiazolidinedione; increase insulin sensitivity in liver, fat, muscle: adverse: increase risk of heart failure and stroke *restricted by FDA

101
Q

pioglitazone

A

thiazolidinedione; increase insulin sensitivity in liver, fat, muscle: adverse: increase risk of heart failure and bladder cancer

102
Q

acarbose

A

a-glucosidase inhibitor; reduce carbohydrate absorption from gut

103
Q

miglitol

A

a-glucosidase inhibitor; reduce carbohydrate absorption from gut

104
Q

bromocriptine

A

D2 selective agonist; oral; incr morning dopaminergic activity -> incr insulin sensitivity and decr hepatic glucose output; adverse: nausea, fatigue; dizziniess, vomiting, headache, NO hypoglycemia or wt gain; ?? efficacy

105
Q

canagliflozin

A

inhibitor of glucose/Na cotransport (SGLT2) in convoluted tubule in kidney->inhibit glucose reabsorption; oral; adverse: UTIs, increased urination

106
Q

thyroxine

A

T4; potency=1; half-life 7days; less expensive; converted to T3 in periphery; oral IV, IM, tx lifelong

107
Q

triiodothyronine

A

T3; potency=4; half-life 1 day; more expensive; oral, IM, IV for emergency myxedema coma; adverse: thyrotoxicosis, stress on CV system

108
Q

propylthiouracil

A

thioamine; inhibits thyroid peroxidase: oxidation, iodination, coupling; also inhibits T4->T3 conversion; faster than MMI but less potent and shorter duration; treatment for pregnant women (instead of MMI)

109
Q

methimazole

A

thioamine inhibits thyroid peroxidase: oxidation, iodination, coupling; slower but more potent than PTU; not used in hyperthyroid pregnant women during 1st tri

110
Q

potassium iodide

A

inhibits release of T3 and T4; inhibits synthesis of T3 and T4; oral; course is fast but effect is transient; not sole therapy; adverse: safe and reversible, rash, swollen salivary glands; used to prevent I131 after nuclear accident

111
Q

radioactive iodine

A

I131; concentrates in thyroid and causes local radiation damage; oral; adverse: delayed hypothyroidism, radiation exposure; time course slow (weeks); NOT used in pregnant/nursing mothers

112
Q

propranolol

A

B blocker; alleviate symptoms of incr CV activity from hyperthyroid

113
Q

cortisol

A

glucocorticoid; oral, injectable, topical; some MC activity

114
Q

dexamethasone

A

pure glucocorticoid (no MC activity); oral, injectable, topical

115
Q

prednisolone

A

glucocorticoid; oral, injectable; decr MC activity

116
Q

fludrocortisone

A

Only mineralocorticoid; oral only; has GC activity; only useful as replacement therapy in adrenal insufficiency; adverse: fluid/electrolyte abnormalities, hypertension

117
Q

spironolocatone

A

mineralocorticoid ; also androgen antagonist

118
Q

eplerenone

A

mineralocorticoid antagonist; no anti-androgen activity

119
Q

aminoglutethimide

A

inihibits conversion of cholesterol to pregnenolone (first step) t treat cushings

120
Q

metyrapone

A

inhibits conversion of 11-deoxy to cortisol and corticosterone to treat cushings syndrome

121
Q

ketoconazole

A

inhibits many steps in steroid synthesis to treat cushings

122
Q

progestin+estrogen as contraception

A

discontinuous or continuous admin; main effect pituitary/hypothalamus; predictable menstrual periods;

123
Q

ethinyl estradiol

A

estrogen in progestin+estrogen contraception

124
Q

estrone sulfate

A

estrogen

125
Q

diethylstilbestrol

A

estrogen; among first non-steroidal estrogens used; not used any more

126
Q

tamoxifen

A

SERM; agonist everywhere but breast; PM symtoms, osteoporosis, E-dependant Breast CA

127
Q

raloxifene

A

SERM; antagonist in breast and endometrium, neutral in vag epithelium; PM symptoms, osteoporosis, E-dependant breast CA

128
Q

ospemifene

A

SERM; antagonist breast neutral in endometrium; approved for tx of vaginal atrophy in PM women

129
Q

clomiphene

A

estrogen receptor antagonist; ovulation induction

130
Q

fulvestrant

A

estrogen receptor antagonist; ovulation induction

131
Q

anastrozole

A

non-steroidal aromatase inhibitor; tx estrogen-dependant breast CA; ovulation induction; adverse: hot flushes, plasma lipids and bone resorption

132
Q

exemestane

A

steroidal aromastase inhibitor; tx estrogen-dependant breast CA; ovulation induction; adverse: hot flushes, plasma lipids and bone resorption

133
Q

drospirenone

A

progestin; enhanced acitivity as mineralocorticoid and androgen antagonists; also as progestin in progestin+estrogen oral contraception

134
Q

progesterone only contraception

A

continuous admin; prevents fertilization by decreasing amount and increasing viscosity of cervical mucus; prevent ovulation by inhibiting HPO axis; adverse: headache, abnormal menstrual bleeding

135
Q

medroxyprogesterone acetate

A

progestin only contraaception; IM injection every 3 months (depo-provera)

136
Q

norethindrone

A

progestin only contraception; oral daily; IUD 5 yrs; also in progestin+estrogen oral contraception

137
Q

norgestrel

A

progestin only contraception; oral daily; IUD 5yrs; postcoital contraception (higher dose, effective within 72 hrs of intercourse) NON PRESCRIPTION->adverse: n/v, headache, breast tenderness, abd cramps

138
Q

ulipristal

A

SPRM; can be agonist or antagonist, depending on tissue; postcoital contraception; effective within 5 days of intercourse; inhibits ovulation by progesterone antagonism; prescription needed; drug of choice in ER

139
Q

RU-486 (mifepristone)

A

progestin receptor antagonist; abortion w prostaglandin; also glucocorticoid antagonist used in cushings and DM II

140
Q

FSH

A

gonadotropin; induce follicular growth

141
Q

CG

A

gonadotropin; induce ovulation (like LH); diagnostic marker of pregnancy

142
Q

gonadorelin

A

GnRH; stimulate gonadotropin secretion to treat delayed puberty in boys or girls and anovulatory women; admin as single injection fo via pump (pulsatile)

143
Q

luprolide

A

GnRH agonist; after initial stimulation secretion is suppressed (desensitization) used as antiandrogen like antagonist

144
Q

cetrorelix

A

GnRH antagonist; treat precocious puberty in boys and girls and androgen excess in males; treat endometriosus and dysmenorrhea; stop GnRh in ovulation-inductionprotocol

145
Q

testosterone

A

androgen

146
Q

testosterone propionate

A

androgen

147
Q

methyltestosterone

A

17a-alkylated androgen; orally active

148
Q

danazol

A

17a-alkylated androgen; orally active but more side effects (hepatotoxic)

149
Q

dutasteride

A

5a-reductase inhibitor; antiandrogen

150
Q

finasteride

A

5a-reductase inihibitor; antiandrogen

151
Q

bicalutamide

A

androgen receptor antagonist

152
Q

flutamide

A

androgen receptor antagonist

153
Q

nilutamide

A

androgen receptor antagonist

154
Q

progestin (noncontraception use)

A

suppress HPO axisto treat dysmenorrhea and endometriosis; P+E replacment therapy in ovarian dysfunction ad postmenopausal

155
Q

growth hormone

A

human growth hormon; recombinant; SQ once daily or IM once/twice a month

156
Q

sermorelin acetate

A

synthetic GHRH analog; for functioning pituitary

157
Q

IGF-1

A

human, recombinant; used only in syndromes of GH resistance

158
Q

pegvisomant

A

GH antagonist; SQ injection; nine aa mutation from wild-type GH; binds GH receptor but doesnt allow dimerization

159
Q

ocreatide

A

somatostatin agonist; IM or SQ injection; selective for somatostatin receptor in pituitary; inhibit GH release; adverse: nausea, flatulence, ad pain, gallstones (20-30% incidence)

160
Q

lanreotide

A

somatostatin agonist; IM or SQ injection; selective for somatostatin receptor in pituitary; inhibit GH release; adverse: nausea, flatulence, ad pain, gallstones (20-30% incidence)

161
Q

bromocriptine

A

D2 agonist; oral; treat hyperprolactinemia -> amerorrhea, galactorrhea, infertility; adverse: nausea, headaches, orthostatic hypotension (adrenergic response)

162
Q

cabergoline

A

D2 agonist; oral; treat hyperprolactinemia -> amerorrhea, galactorrhea, infertility; adverse: nausea, headaches, orthostatic hypotension (adrenergic response)

163
Q

desmopressin

A

synthetic vasopressin

164
Q

oxytocin

A

from post pituitary; modulates ion channels in myometrium to induce smooth muscle contraction in uterus; induces labor; V1-> or IM

165
Q

vasopressin

A

acts on V1 -> vasoconstriction; V2 -> renal collecting tubule water resorption; replcement therapy for diabetes insipidus; oral, IV, SQ, or intranasal

166
Q

Vit D

A

incr calcium absortion for GI tract

167
Q

Vit D2 (ergocalciferol)

A

incr calcium absortion for GI tract

168
Q

Vit D3 (calcitriol)

A

incr calcium absortion for GI tract

169
Q

PTH/teriparatide

A

PTH;normally stimulate bone resorption; given at daily low dose leads to osteoblast stimulation and new bone formation;

170
Q

calcitonin

A

from thyroid C cells; SQ, IM, intranasal; inhibit bone resorption and incr calcium excretion by kidneys -> decr serum calcium

171
Q

alendronate

A

bisphosphonate; oral or parenteral; inhibits bone resorption

172
Q

etidronate

A

bisphosphonate; retards dissolution of hydroxyapatite; slows osteoclasst resorption of bone; parenteral

173
Q

pamidronate

A

bisphosphonate; parenteral; inhbits bone resorption

174
Q

risedronate

A

bisphosphonate; oral or parenteral; inhibits bone resorption

175
Q

tiludronate

A

bisphosphonate; oral or parenteral; inhibits bone resorption

176
Q

denosumab

A

RANKYL antibody; inhibits bone resorption by binding RANKligand and prevent binding to RANK; RANK is osteoclast receptor that stimulates resorptive activity

177
Q

enfuvirtide

A

HIV antiviral, entry inhibitor; injection; peptide mimic binds to HIV gp41 -> blocks membrane fusion; adverse: immunogenic->inflammation; resistance form gp41 mutations

178
Q

maraviroc

A

HIV antiviral, entry inhibitor; small molecule inhibitor; binds CCR5 allosterically preventing HIV gp120/CCR5 interaction; testing for CXCR4 efficacy; resistance: gp120 mutations; salvage therapy; microbicide to block sexual transmission

179
Q

AZT (zidovudine)

A

HIV antiviral, NRT inhibitor

180
Q

emtricitabine

A

HIV antiviral, NRT inhibitor

181
Q

lamivudine

A

HIV, hepatitis B antviral, NRT inhibitor

182
Q

tenofovir

A

HIV antiviral, NtRT inhibitor; adverse: competes with other drugs for kidney tubule secretion; other hiv and herpes antiviral will elevate tenofovir in serum

183
Q

efavirenz

A

HIV antiviral, NNRT inhibitor

184
Q

nevirapine

A

HIV antiviral, NNRT inhibitor

185
Q

ralgravir

A

HIV antiviral, integrase inhibitor; resistance from aa changes in integrase

186
Q

ritonavir

A

HIV antiviral, protease inhibitor; blocks CYP 3A4

187
Q

saquinavir

A

HIV antiviral, protease inhibitor; combination w ritonavir incr availability; many known drug interactions

188
Q

palivizumab

A

RSV antiviral ab, entry inhibitor; prophylaxis for infants/children >2 yrs with CLD

189
Q

ribavarin

A

guanosine analog; inhibits inosine monophosphate dehydrogenase resulting in GTP depletion (decr 5 capping of RNA); can base pair with cytidine or uridine -> mutations -> highly defective viral genome; mutations can bestow resistance; causes shift in Th1 to Th2 pheotype of CD4+ cells; Best broad spectrum antiviral available; treat hospitalized infant with RSV; standard of care for Hep C w IFNa

190
Q

pegylated interferon

A

generates antiviral state in virally infected and nearby cells; HBV sensitive to antiviral state; standard of care for Hep C w ribavarin

191
Q

acyclovir

A

a-herpes antiviral, nucleoside analog; effective 1st line drug; prodrug selectively activated by viral nucleoside kinase; no 3-OH; uses: tx HSV, VZ (immunocompromised), prophylaxis in BMT, HSV encephalitis (not very successful); short half-life, poor oral absorption; (elevate tenofovir levels

192
Q

cidofovir

A

a,B,gamma-herpes antiviral, nucleoside analog; acycic nucleoside phosphonate derivate of cytosine; converted to active ANP-diphosphate by cellular kinase (no need for viral kinase and retain activity against TK (kinase) negative/altered HSV); competitive inhibitor of viral DNA polymerase and act as chain terminator

193
Q

famciclovir

A

a-herpes antiviral, nucleoside analog; prodrug of penciclovir; oral

194
Q

penciclovir

A

a-herpes antiviral, nucleoside analog; acyclic guanine derivative w 3-OH -.allows short chain extension but still causes termination

195
Q

valacyclovir

A

a-herpes antiviral, nucleoside analog; effective 1st line drug; prodrug selectively activated by viral nucleoside kinase; no 3-OH; uses: tx HSV, VZ (immunocompromised), prophylaxis in BMT, HSV encephalitis (not very successful); povides more sustaing and higher levels in serum than acyclovir; (elevate tenofovir levels)

196
Q

foscarnet

A

a,B,gamma-herpes antiviral, non-nucleoside analog of pyrophosphate -> binds to pyrophosphate -binding site on viral DNA polymerase -> noncompetitive inhibits polymerase activeity; 100X more selective for viral vs cellular polymerase

197
Q

docosanol

A

a-herpes antiviral, non-nucleoside analog; saturates fatty alcohol that is approved as topical cream; mixed evidence of efficacy

198
Q

ganciclovir

A

B,gamma-herpes antiviral, nucleoside analog; hydroxymethylated derivative of acyclovir; IV for life-threatening CMV infection (retinitis); effect beter than acyclovir on HSV, VZV, and CMV but TOXIC; adverse: granulocytopenia, thrombocytopenia, may not be reversible

199
Q

fomivirsen

A

B,gamma-herpes antiviral, antisense RNA against CMV that can be used against CMV retinitis in immunocompromised pts

200
Q

amantadine

A

influenza antiviral, uncoating inhibitor (resistance is widespread); block acidification of virion in endosome by binding M2; only works with influenza A; must be administered withine 48 hrs of onset, and prophylaxis; antiparkinson drug

201
Q

oseltamivir (tamiflu)

A

influenza antiviral, neuraminidase inhibitor; blocks release of virion; works for A nd B; oral

202
Q

zanamivir

A

influenza antiviral, neuraminidase inhibitor; blocks release of virion from cel; works with A and B; aerosol

203
Q

telaprevir

A

hepatitis C antiviral, protease inhibitor; 12 week course parallel w IFNa and ribavarin; adverse: rashes, anemia and elevates statins in blood when taken together

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