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PharmGeneral Flashcards

1
Q

MOA and indications for fomepizole

A

inhibits alcohol dehydrogenase, and is an antidone for methanol or ethylene glycol poisoning

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2
Q

MOA and indications for disulfiram

A

inhibits acetaldehyde dehydrogenase, used for alcoholics

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3
Q

Abx that block cell wall synthesis by inhibition of peptidoglycan cross linkin

A

penicillin, methicillin, ampicillin, piperacillin, cephalosporins, aztreonam, imipenem

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4
Q

Abx that block peptidoglycan synthesis

A

bacitracin, vancomycin

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5
Q

abx that block nucleotide synthesi by inhibiting folic acid syntehsis

A

sulfonamides,trimethoprim

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6
Q

abx that block DNA topoisomerases

A

fluoroquinolones

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7
Q

abxs that block mRNA synthesis

A

rifmpin

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8
Q

abx that damage DNA

A

metronidazole

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9
Q

abx that block protein synthesis at 50S ribosomal subunit

A

chloramphenicol, macrolides, clindamycin, linezolid

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10
Q

abx that block protein synthesis at 30s ribosomal subunit

A

aminoglycosides,tetracyclines

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11
Q

MOA, clinical use, and toxicity for Penicillin

A

-Bind penicillin-binding proteins (transpeptidases)
Block transpeptidase cross-l inking of peptidoglycan
Activate autolytic enzymes

-Mostly used for gram-positive organisms (S. pneumoniae, S. pyogenes, Actinomyces) . Also used for
Neisseria meningitidis, Treponema pallidum, and syphilis . Bactericidal for gram-positive cocc i ,
gram-positive rods, gram-negative cocci, and spirochetes . Not penicillinase resistant.

-Hypersensitivity reactions, hemolytic anemia.

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12
Q

MOA, indications, and toxicity for oxacillin, nafcillin, dicloxacillin

A

-Bind penicillin-binding proteins (transpeptidases)
-Block transpeptidase cross-l inking of peptidoglycan
-Activate autolytic enzymes
-penicillinase resistant because bulky R group
blocks access of B-lactamase to B-lactam ring.

Use: S.au reus (except MRSA; resistant because of
altered penicill in-binding protein target site) .

-Hypersensitivity reactions, interstitial nephritis.

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13
Q

MOA, clinical use, and toxicit for amoxicillin, ampicillin

A

-Bind penicillin-binding proteins (transpeptidases)
-Block transpeptidase cross-l inking of peptidoglycan
-Activate autolytic enzymes
Penicillnase sensitive

AmOxicillin has better oral bioavailability than ampicillin

USe against: Haemophilus Influenza, EColi, Listeria monocytogenes, Poteus mirabilis, Salmonella, shigella,enterococci

Toxicity: Hypersensitivity reactions ; ampicillin rash ;
pseudomembranous colitis.

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14
Q

MOA, clinical use, and toxicity for ticacilllin, piperaclin

A
  • Bind penicillin-binding proteins (transpeptidases)
  • Block transpeptidase cross-linking of peptidoglycan
  • Activate autolytic enzymes

Used for pseudomonas, gram negative rods

Tox: hypersensitivty reactions

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15
Q

Beta lactamase inhibitors:

A

Clavulanic acid, sulbactam, tazobactam

use these to protect abx from destruction by B-lactamase (penicillinase)

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16
Q

Cephalosporins MOA and toxicity

A

Blactam drugs that inhibit cell wall synthesisnbut are less susceptible to penicillinases.
Bactericidal

Toxicity: hypersensitivty reaction, VitK deficiney, disulfuram like reaction, increases nephrotoxicity of aminoglycosides

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17
Q

Ceph 1st gen drugs and uses

A 
1st generation (cefazol i n , cephalexin) -gram- positive cocci, Proteus mirabilis, E. coli,Klebsiella pnewnoniae. Cefazol in used prior to
surgery to prevent S. aureus wound infections .
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18
Q

Ceph 2nd gen drugs and uses

A 
2nd generation (cefoxitin, cefaclor, cefuroxime) - gram-positive cocci , Haemophilus influenzae, Enterobacter
aerogenes, Neisseria spp., Proteus mirabilis,E. coli, Klebsiella pneumoniae, Serratiammarcescens.

2nd generation - HEN PEcKS.

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19
Q

3rd gen ceph drugs and uses

A 
3rd generation (ceftriaxone, cefotaxime, cefdinir, ceftazidime) - serious gram-negative infections
resistant to other B-lactam
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20
Q

4th gen ceph drug and use

A 
4th generation (cefepime) -increased activity against
Pseudomonas and gram-positive organisms.
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21
Q

Aztreonam MOA, use, toxicity

A

Prevents peptidoglycan cross-l inking by binding to PBP3. Synergistic with aminoglycosicles. No cross-allergenicity with penicillins.

  • Gram-negative (PEKS) rods only, for those with renal insufficinecy and PCN allergy
  • usually nontoxic
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22
Q

imipenem/cilastin, meropenem MOA, use, toxicity

A

Broad spetrum B lactamase, binds to PBP

use: gram + cocci, gram - rods, pseudomonas
no MRSA coverage

Tox: imipenem can be metabolized by renal dehdropeptiase I,so give cilastin to inhibit this renal inactivation

Gi distress, skin rash, CNS toxicit

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23
Q

Vancomycin MOA,use, toxicity

A

inhibits cell wall peptidogylcan formation by binding D-ala D-ala portion of cell wall.

Gram + only

Toxicity: NOT (nephro, ototoxicity, thrombophlebitis)

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24
Q

Protein syntehsis inhibitors

A

30S: aminoglycosides,tetracycline
50S: chloramphenicol,clindamycin, eryhtromycin, linezolid

buy AT 30,CCELL at 50

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25
Q

Aminoglycosides use, toxicity

A

Gentamycin, neomycin, tobramycin

use: severe gram neg rods, tox: nephrotoxic, neuromusuclar blockade, ototoxic, teratogen

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26
Q

Tetracyclines use, toxicity, and contraindications

A

Tetracycline, doxycycline, demeclocycline

use for borrelia burgdorferi, mycoplasma pneumoniae, rickettsia, chlaymdia

Tox: GI distress, teeth discoloration

DO NOT TAKE with mlk,antacids,or Fe containig preps because it inhibits its absorption
DONT use in kids or pregnancy

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27
Q

Macrolides use, toxicity

A

Erythromycin, clarithromycin

Use: atypical PNA (mycoplasma,chlamydia, legionella), STDs (chlamydia), gram + (strep infxns if allergic to PCN)

Toxic: CREAM

motility issues,arrthymia via porlonged QT, cholestatic hepatitis, rash, eopsinophilae

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28
Q

Nitrofurantoin MOA and use

A

bacterocidal, inacativates bacterial ribosomes

safe in pregnancy, used for UTI and cystitis

Ecoli, staph saprophyticus

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29
Q

Chloramphenicol MOA,clinical use, toxicity`

A

blocks peptidyltransferase at 50S ribosomal subunit

Use for meningitis (hFlu, neisseria, strep pneumo)
Toxic: anemia,aplastic anemia,gray baby syndrome

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30
Q

Clindamycin clinical use and toxicity

A

Anaerobic infxns in aspiration PNA or lung abscess or mouth anaerobes

toxic: pseudomembranous collitis

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31
Q

Sulfonamides MOA, use, toxicity

A

Sulfamethaxole, sulfisoxazole, sulfadiazene

PABA antmetabolites inhibit dihydropeptide synthase, causing decreased folic acid

Use: gram + gram -, nocardia, chlamydia

Tox: hypersensitivity rxns, hemolysis if G6pD deficient, nephrotoxic,photosensitvity, SJS

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32
Q

Trimethoprim:

MOA, use, toxicity

A

Inhibit bacterial dihydrofolate reductase, decreasing folic acid synthesis

used for UTIs, MRSA, andShigella, salmonella, and PCP tx/ppx if CD < 200

Can cause megaloblastic anemia, leukopenia, granulocytopenia

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33
Q

Fluroquinolons: ciprofloxacin, norloxacin,levofloxacin,etc..

A

MOA: inhibit DNA Gyrase (toposiomerase II)
-DONT AKE WITH ANTACIDS/supplement
Use for gram negative rods of urinary and GI tracts including pseudomonas, some gram +

Tox: GI upset, skin rashes, tendonitis,~prolonged QT

DONT USE IN PREGNANCY

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34
Q

metronidazole MOA, use, tox

A

MOA: forms free radical damage

treats: giardia,entamoema,trichomonas, garneralla,anaerobes,Cdiff/clostridum

GET GAP on the METRO

Tox: disfuliram like rxn

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35
Q

Antimycobacterial PPX and tx for:

  • TB
  • MAC/MAI
  • MLeprae
A

PPx/Tx as…
TB: Isoniazid // Rifampin, Isoniazid, Pyrazinamide, Ethambutol
MAC: Azithromycin // azithromycin, rifampin, ethambutol, streptomycin
Leprae: none, long term tx with dapsone and rifampin for tuberculoid, andd clofazimine for lepromatous form

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36
Q

Abx to avoid in pregnancy (and their cause)

A 
Sulfonamides - kernicterus
Aminoglycosides - ototoxicity
Fluorquinlones - cartilage toxicity
Clarithromycin - embryotoxic
tetracyclines - discolored teeth, inhibit bone growth
ribavirin - teratogenic
Griseofulvin - teratogenic
metronidazole - mutagenic
Chloramphenicol - gray baby

SAFe Children May Take Really Good Care

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37
Q

Isoniazid MOA, toxicity

A

decreases synthesis of mycolic acid. Needs bacterial ctalase peroxidase to convert INH to active metaolite

Neurotoxic,hepatotoxic,and need to give pyridoxine (vitB6), can prevent neurotoxicity and drug induced lupus

38
Q

Rifampn MOA, use, toxicity

A

inhibits DNA dependent RNA polymerase
used for TB and leprosy, used for meningococcal prophylaxis and chemoprphylaxis for children with HFlu type B

Tox: hepatotoxicity, increases p450, orange body fluids

39
Q

Pyrazinamide MOA and toxicity

A

Inhibits mycolic acid prdxn
effective in pH of phagolysosomes where TB engulfed by macrophage is fund

Hyperuricemia, hepatotoxicity

40
Q

Ethambutol MOA and toxicity

A

Decrease carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase

Tox: optic neuropathy (color blindedness)

41
Q

Abx ppx for meningococal infection

A

ciprofloxacin for adults, or rifampin for children

42
Q

Abx ppx for HFlu meningitis

A

rifampin

43
Q

HIV PPX for <200, 150,100,and 50, and against what drugs?

A

200: bactrim,PCP
150: itaconazole, histoplamosis
100: bactrimfor PCP/toxoplasmosis
50: azithromycin, MAC

44
Q

Amphotericin B MOA, use, and toxicity

A

binds ergosterol, forming pores that allow leakage of electrolytes

use for serious systemicmycoses, cryptococcus infxns, blastomyces, coccidoides,hitoplasma, candida, mucor

**supplement afx with K and Mg
Tox: fevers,chills, hypoTN, HypoK, nephrotoxicity, arrhytmia, IV phlebitis, anemia

45
Q

Nystatin:

MOA and use

A

binds ergoserol and creates membrane pores, allowing leakage. USe as topical form only

use for oral candidiasis and topical for vaginal candidiasis/diaper rash

46
Q

Azoles

MOA, use, toxicity

A

-Fluconazole, ketoconazole, clotrimazole, m iconazole, itraconazole, voriconazole.

-I n h ibit fungal sterol (ergosterol) synthesis, by inhibiting the P-45 0 enzyme that converts lanosterol
to ergosterol.
Local and less serious systemic mycoses. Fluconazole for chronic suppression of cryptococcal
meningitis i n AIDS patients and candidal infections of all types. Itraconazole for Blastomyces,
Coccidioides, Histoplasma. Clotrimazole and miconazole for topical fungal i n fections.

-Testosterone synthesis inh ibition (gynecomastia, esp. with ketoconazole ) , l iver dysfunction (inhibits
cytochrome P-4 5 0 ) .

47
Q

Flucytosone MOA,use, toxicity

A

-Inhibits DNA and RNA biosynthesis by conversion to 5 -fluorouracil by cytosine deaminase.

-Used i n systemic fungal infections (esp. men ingitis caused by Cryptococcus) i n combination with
amphotericin B .

-Bone marrow suppression.

48
Q

Griseofulvin MOA, use, and toxicity?

A

Interferes with microtubule function ; disrupts mitosis. Deposits in keratin-containing tissues (e.g.,
nails ) .

USE: Oral treatment of superficial infections; inhibits growth of derm atophytes (tinea, ringworm) .

TOXICITY: Teratogenic, carcinogenic, confusion , headaches, increases P-450 and warfarin metabolism.

49
Q

tx for toxoplasmosis

A

pyrimethamine

50
Q

tx for trypanosoma brucei

A

suramin and melarsoprol

51
Q

tx for T Cruzii

A

nifurtimox

52
Q

tx for leishmaniasis

A

sdium stibogluconate

53
Q

chloroquine mOA, use, toxicity

A

blocks detoxification of heme into hemozoin, heme accumulates and becomes toxic to plasmodia

Tx for plasmodial species other than P falciparaum.

Tox: retinopathy

54
Q

tx for P falciparum

A

atovaquone/proguanil

55
Q

Tx for life threatening malaria

A

quinidine in US, quinine elsewhere

56
Q

Antihelminthic therapy

A

Mebendazole, pyrantel pamoate, ivermecti n, diethylcarbamazine, praziquantel ; immobil ize
helminths

57
Q

tx against flukes

A

Use praziquantel against flukes (trematodes) such as Schistosoma.

58
Q

Antiviral drugs that block:

  • Viral adsorptin
  • Nucleic acid synthesis
  • Protein synthhesis/processing
  • packaging and assembly
  • release of packaging
A
  • gamma globulins
  • purine/pyrimidine analogs, and Reverse transcriptase inhibitors
  • protease inhibitiors
  • rifampin
  • neuraminidase inhibitors (flu)
59
Q

Zanamir, Oseltamavir MOA and use

A

Inhibit influenza neuraminidase, decreasing the release of progeny virus.
Treatment and prevention of both influenza A and B.

60
Q

Ribavirin MOA,use, toxicity

A

Inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase.

Use: RSV, chronic hepatitis C.

Tox: Hemolytic anemia. Severe teratogen

61
Q

Valacyclovir/Acyclovir: MOA, use, tox

A

Monophosphrylated by HSV/VZV thymidine kinase, guanosine analog, inhibits viral DNA polymerase by chain termination

Use: HSV1/2, VZV, weak against EBV
tox: very few

62
Q

Tx for herpes zoster?

A

Famcyclovir

Guanosine nucleoside analog,relies on viral thymidine kinase
HSV1/HSV2, VZV

63
Q

Ganciclovir MOA, use, toxicity

A

5’ monophosphate formed by CMV viral kinase (CMV doesnt have thymidine kinase ). Guanosine analog. Triphophate formed by cellular kinases. Inhibits viral DNA polymerase

Use:CMV, especially in immunocompromsed

Valganciclovir is prodrug with better oral bioavailability

Tox: leukopenia, neutropenia, thrommbocytopenia, renal toxicity

64
Q

Foscarnet/Cidofovir MOA, use, toxicity

A

Viral DNA polymerase inhibitor that binds to the pyrophosphate-binding site of the enzyme.
Does not require activation by viral kinase.
Use: CMV retinitis in immunocompromised patientswhen ganciclovir fails; acyclovir-resistant HSV.

Tox: Nephrotoxicity

65
Q

HIV therapy

A 
HAART
3 drugs (2 nucleoside reverse transcriptase inhibitors) + (1 non-nucleoside reverase transcriptasse inhibitor OR protease inhibitor OR integrase inhibitor)

2NRTI + (1 NNRTI/PI/II)

66
Q

Protease inhibitors drugs, MOA, Toxicity

A

Lopinavir, Atazanavir, Darunavir, Fosamprenavir, Saquinavir, Ritonavi r, lndinavir

MOA: assembly of viron depends on HIV-1 protease, which is inhibited by these.

Tox: Ritonavir can boost other drug mechanisms by inhibiting P450. hyperglycemia, GI intolerase, hyperlipidemia,nephropathy

Nephrolithiasis: indinavir, atazanavir

67
Q

NRTI drugs, MOA, and tox:

A 
Tenofovir (TDF)
Emtricitabine (FTC)
Abacavir (ABC)
Lamivudine (3TC)
Zidovudine (ZDV,
formerly AZT)
Didanosine (ddl)
Stavudine ( d4T)

MOA: competitively inhibit nucleotide binding to reverse transcriptase and terminate DNA chain - most (except tenofovir) need to be phosphorylated by thymidine kinase to be active

Tox: bone marrow suppression (reverse with GCsf, EPO), peripheral neuropathy, lactic acidosis, rash, and anemia (ZDV)

68
Q

NNRTIs Drugs, MOA, tox

A

Nevirapine
Efavirenz
Delavirdine
Etravirine

binds to reverse transcriptase as a non competitive inhibitor, does not require phoshphorylation

Tox: Rash, bone marrow suppression, periph neuopathy

69
Q

Integrase inhibitors Drug, MOA, tox

A

Raltegravir

Inhibits HIV geneome integration into host cell by inhibiting HIV integrase.

Tox: hypercholesterolemia,nausea, rash, myopathy

70
Q

Fusion inhibitor MOA,MOA

A

Enfuvirtide

Fusion inhibiotr that inhibits HIV GP41

71
Q

Maraviron MOA

A

CCR5 antagonist (mostly found on macrophages)

-Drug inhibits binding where Gp120 normally inds

72
Q

IFNa MOA, use, toxicity

A

inhibit DNA/RNA virus replication

chronic hep B and C, kaposis sarcoma

tox: neutropenia, myopathy

73
Q

IFNB MOA, use, toxicity

A

MS

Neutropenia, myopathy

74
Q

IFNy use

A

NADPH oxidase deficiency

75
Q

Cyclosporine MOA, use, toxicity

A

binds to cyclophilins in T cells, whichblocks differentiation and activation of T cells by inhibiting calcineuron, thus preventing Il2 production

Use: suppress organ rejectin, some AI disorders (RA,psoriasis)

Tox: nephrotoxicity,HTN, hyperlipid/TG, increase viral infxns, lymphomas

76
Q

Tacrolimus MOA,clinical use/Tox

A

MOA: inhibits calcineurin and secretion of IL-2

Use: immunosuppresion

Tox: nephrotoxic, neurotoxic,HTN

77
Q

Sirolimus MOA,use, tox

A

inhibits mTOR and T cell proiferation in response to IL2

use: imunosuppresion, esp after renal transplants

Tox: hyperipidemiea,thrombcytopenia, luekopenia

78
Q

Azathiprine: MOA, use, toxicity

A

Antimetabolite precursoe of 6-MU interferes with synthesis of nucleic acids, toxic to proliferating lymphocytes

Use: autoimmune do and kidney transplantation

Tox: bone marrow suppression, **metabolized by xanthine oxidase and thus patients on allopurinol worsen this toxicity

79
Q

Muromonab-CD3 (OKT3)

A

monoclonal Ab against CD3,blocks T cell signal tranduction

Use: immunosuppresion after kidney transplant

Tox: cytokine release,hypersenstiivty

80
Q

Mycophenylate MOA

A

inhibits IMP dehydrogenase,prevents syntehsis of guanine, prevents rapid proliferation of B/T cells

81
Q

Use for aldesluekin

A

RCC,metastaic melanoma (IL2 recombinant)

82
Q

Use for epoetin alfa

A

Anemias, in renal failure

83
Q

Use for filgrastim

A

Recovery of bone marrow (GSCF recombinant)

84
Q

Sargramostin use

A

recovery of bone marrow (GMCSF recombinant)

85
Q

Infliximab target and use

A

TNFa, Chrons disease, RA, Psoriatic arthritis, ankylosing spodylitis

86
Q

Adalimumab target and use

A

TNFa, Chrons disease, RA, Psoriatic arthritis, ankylosing spodylitis

87
Q

Abciximab target and use

A

GpIIbIIIa inhibitor, used for reventing cardiac ischemia

88
Q

Trastuzumab (herceptin) target and use

A

HER2 receptor, used for Her2 overexpressing breast cancers

89
Q

Rituximab target and use

A

CD20 used for B cell NHL

90
Q

Omalizumab target and use

A

IgE target used for severe asthma

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