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Step 1 Pharm > Antimicrobials > Flashcards

Antimicrobials Flashcards

1
Q

Beta-lactams

Mechanism

A

Block cell wall synthesis

Inhibit peptidoglycan cross-linking

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

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2
Q

Bacitracin, vancomycin

Mechanism

A

Block peptidoglycan synthesis

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3
Q

TMP, sulfonamides

Mechanism

A

Block nucleotide synthesis-

Inhibit folic acid synthesis

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4
Q

Fluoroquinolones

Mechanism

A

Block DNA topoisomerases

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5
Q

Rifampin

Mechanism

A

Block mRNA synthesis

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6
Q

Metronidazole

Mechanism

A

Damage DNA

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7
Q

Chloramphenicol, macrolides, clindamycin, streptogramins, linezolid

Mechanism

A

50S ribosomal subunit inhibitor

Chloramphenicol, macrolides, clindamycin, streptogramins (quinupristin, dalfopristin), linezolid

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8
Q

Aminoglycosides, tetracyclines

Mechanism

A

30S ribosomal subunit inhibitor

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9
Q

Bind transpeptidases

Gram-positives, gram-neg cocci, spirochetes

Hypersensitivity, hemolytic anemia

Beta-lactamases for resistance

A

Penicillin G (IV,IM)

Penicillin V (oral)

Penicillinase susceptible

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10
Q

Penicillinase resistant

S. aureus

Hypersensitivity, interstitial nephritis

A

Oxacillin, nafcillin, dicloxacillin

(naf for staph)

bulky -R group

blocks beta-lactamase access to b-lactam ring

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11
Q

MRSA

Mechanism of resistance

A

Altered penicillin-binding protein target site

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12
Q

HELPSS kill enterococci

Hypersensitivity, rash, pseudomembranous colitis

Combined with clavulanic acid

A

Aminopenicillins

Ampicillin, amoxiciliin

amoxi > bioavailability

penicillinase susceptible (add clavulate)

HELPSS:

Haemophilus, E. coli, Listeria, Proteus, Salmonella, Shigella

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13
Q

Gram-neg rods, Pseudomonas

Combined with clavulanate

Hypersensitivity

A

Antipseudomonals

Ticarcillin, piperacillin

Susceptible to penicillinase

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14
Q

Beta-lactamase inhibitors

A

CAST

Clavulanic acid, sulbactam, tazobactam

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15
Q

Covers everything but LAME

(Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA, Enterococci)

A

Cephalosporins

except ceftaroline covers MRSA

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16
Q

Can cause

Hypersensitivity, Vit K deficiency, increased nephrotoxicity of aminoglycosides

A

Cephalosporins

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17
Q

Gram-pos cocci

PEcK

(Proteus, E. coli, Klebsiella)

A

1st gen cephalosporins

Cefazolin, Cephalexin

Cefazolin - prior to surgery to prevent

S. aureus wound infections

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18
Q

Gram-pos cocci

HEN PEcKS

(Haemophilus, Enterobacter aerogenes, Neisseria, Proteus, E. coli, Klebsiella, Serratia marcescens)

A

2nd gen cephalosporins

Cefoxitin, Cefaclor, Cefuroxime

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19
Q

Serious gram-neg infections

(meningitis, gonorrhea)

resistant to other beta-lactams

A

3rd gen cephalosporins

Ceftriaxone- meningitis, gonorrhea

Ceftazidime- Pseudomonas

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20
Q

Gram-neg rods only

monobactam (resistant to beta-lactamases)

No penicillin cross-allergenicity

Binds PBP3

A

Aztreonam

Binding to PBP3 prevents peptidoglycan cross-linking

Syngeristic with aminoglycosides

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21
Q

Beta-lactamase resistant

Inactivation in renal tubules prevented by cilastatin

Wide spectrum- serious infections

GI distress, seizures, rash

A

Imipenem/cilastatin

meropenem

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22
Q

Binds D-ala portion of cell wall precursors

Gram-pos only

Red man syndrome

A

Vancomycin

Red man syndrome:

Nephrotoxicity, ototoxicity, thrombophlebitis,

diffuse flushing

(pretreat w/ antihistamine, do slow infusion)

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23
Q

Result of

D-ala D-ala

change to

D-ala D-lac

in cell wall precursor

A

Vancomycin resistance

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24
Q

Inhibits intiation complex formation

Ineffective against anaerobes

Nephrotoxic, ototoxic, teratogen, neuromuscular block

Inactivated by acetylation, phosphorylation, adenylation

A

Aminoglycosides

(gentamicin, neomycin, amikacin, tobramycin, streptomycin)

Cause misreading of mRNA

Requires O2 for uptake

Resistance: transferase enzymes

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25
Q

Prevents aminoacyl-tRNA attachment to 30S

Divalent cations inhibit absorption in gut

GI distress, discoloration of teeth, inhibits bone growth in children, photosensitivity. Contraindication: pregnancy

Resistance: plasmid-encoded transport pumps

A

Tetracyclines

(tetracycline, doxycycline, demeclocycline, minocycline)

Intracellular accumulation- effective against:

B. burgdorferi, M.pneumoniae, Rickettsia, Chlamydia

Divalent cations in milk, antacids, iron-preps

Demeclocycline- ADH antagonist. SIADH- first line

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26
Q

Blocks translocation by binding 23S subunit (of 50S)

Atypical pneumonias, Chlamydia, gram-pos cocci

Motility issues, long QT arrythmia, acute cholestatic hepatitis, rash, eosinophilia

Resistance: methylation of 23S binding site

A

Macrolides

Azithromycin, clarithromycin, erythromycin

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27
Q

Blocks peptidyltransferase at 50S

Meningitis (3rd world)

Anemia, gray baby syndrome

A

Chloramphenicol

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28
Q

Blocks peptide transfer at 50S

Anaerobic infections- aspiration pneumonia, oral infections

Pseudomembranous colitis, fever, diarrhea

A

Clindamycin

Clindamycin- anaerobes above diaphragm

Metronidazole- anaerobes below diaphragm

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29
Q

Inhibit dihydropteroate synthase

Nocardia, Chlamydia, UTIs

Hypersensitivity, hemolysis, nephrotoxicity, kernicterus

A

Sulfonamides

Sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine

PABA antimetabolites inhibit enzyme

Hemolysis in G6PD deficiency

30
Q

Inhibit dihydrofolate reductase

UTI, Shigella, Salmonella, Pneumocystis jirovecii

Megaloblastic anemia, leukopenia, granulocytopenia

A

Trimethoprim

Leucovorin reverses folate deficiency due to TMP

31
Q

Reverses side-effects of Trimethoprim

A

Leucovorin

(Supplemental folinic acid)

32
Q

Inhibit DNA gyrase (topo II) and topo IV

Gram-neg rods in urinary, GI. Neisseria, Pseudomonas.

Rarely tendon rupture, leg cramps, myalgias.

Contra: pregnant, children (cartilage damage)

A

Fluoroquinolones

(ciprofloxacin, norfloxacin, levofloxacin, ofloxacin, sprafloxacin, moxifloxacin, gatifloxacin, enoxacin, nalidixic acid)

No antacids

33
Q

Free radical metabolites damage DNA

Anaerobes, protozoa (Giardia, Entamoeba, Trichomonas, Gardernella)

Reacts with EtOH, metallic taste

A

Metronidazole

Treats anerobes below the diaphragm

34
Q

Mycobacterium tuberculosis

A

RIPE

Rifampin, isoniazid, pyrazinamide, ethambutol

Prophylaxis: Isoniazid

35
Q

Mycobacterium avium-intracellulare

A

ARES

Azithromycin, rifampin, ethambutol, streptomycin

Prophylaxis: Azithromycin

36
Q

Mycobacterium leprae

A

Tuberculoid- dapsone, rifampin

Lepromatous- dapsone, rifampin, clofazimine

No prophylaxis

37
Q

Active metabolite decreases sythesis of mycolic acids

Bacterial catalase-peroxidase (KatG) creates metabolite

Solo prophylaxis against TB

Neurotoxicity, hepatotoxicity, lupus.

A

Isoniazid

INH- Injures Neurons and Hepatocytes

pyridoxine (B6) can prevent neurotoxicity

38
Q

Inhibits DNA-dependent RNA Pol

TB, leprosy, meningococcal prophylaxis

Activates P450, orange body fluids

A

Rifampin

Meningococcal prophylaxis in contacts of children with Haemophilus influenzae B

Delays resistance to dapsone in leprosy.

39
Q

Uncertain mechanism

Active in pH of phagolysosome

TB

Hyperuricemia, hepatotoxicity

A

Pyrazinamide

40
Q

Blocks arabinosyltransferase

Decreased carbohydrate polymerization in cell wall

TB

Optic neuropathy (red-green colorblindness)

A

Ethambutol

41
Q

HIV prophylaxis

CD4 < 200

CD4 < 100

CD4 < 50

A

TMP-SMX (Pneumocystis)

TMP-SMX (Pneumocystis and toxoplasmosis)

Azithromycin (M. avium complex)

42
Q

Vancomycin resistant enterococcus (VRE)

A

Linezolid

Streptogramins (quinupristin, dalfopristin)

43
Q

Binds ergosterol

Forms membrane pores

(2)

A

Amphotericin B

Nystatin

44
Q

Inhibits fungal ergosterol synthesis

A

-azoles

Fluconazole, itraconazole, voriconazole

45
Q

Inhibits synthesis of beta-glucan

Inhibits fungal cell wall synthesis

A

Caspofungin

46
Q

Inhibits squalene epoxidase

Disrupts lanosterol synthesis

A

Terbinafine, Naftifine

47
Q

Inhibits fungal DNA and RNA biosynthesis

A

5-Flucytosine

By conversion to 5-fluorouracil

by cytosine deaminase

48
Q

Bind ergosterol

Systemic mycoses: Cryptococcus, Blastomyces, Coccidioides, Histoplasma, Candida, Mucor, meningitis

Fever/chills, nephrotoxic, arrhytmias, IV phlebitis, anemia

A

Amphotericin B

Supplement K+ and Mg2+

(altered renal tubule permeability)

Hydration reduces nephrotoxicity

Liposomal reduces toxicity

49
Q

Binds ergosterol

Topical

Oral candidiasis, diaper rash, vaginal candidiasis

A

Nystatin

50
Q

Blocks conversion of lanosterol to ergosterol

(inhibits P450)

AIDS- cryptococcal meningitis suppression, candida

Blastomyces, Coccidioides, Histoplasma

Testosterone synth inhibition, liver dysfunction

A

Fluconazole

Itraconazole

Gynecomastia- ketoconazole

51
Q

Inhibits DNA, RNA biosynthesis

Systemic infections, Cyptoccal meningitis

Bone marrow suppression

A

Flucytosine

Active metabolite: 5-fluorouracil

by cytosine deaminase

52
Q

Inhibits fungal cell wall synthesis

(beta-glucan)

Invasive aspergillosis, candida

GI upset, flushing (histamine)

A

Caspofungin, micafungin

53
Q

Inhibits squalene epoxidase

Dermtophytoses (i.e. onychomycosis)

Abnormal liver function tests, visual disturbances

A

Terbinafine

54
Q

Disrupts microtubule formation, mitosis

Deposits in keratin-containing tissues (nails)

Oral Tx of superficial infections (tinea, ringworm)

Teratogen, carcinogen, increases P450

A

Griseofulvin

55
Q

Blocks detox of heme to hemozoin

Plasmodium (other than falciparum)

Retinopathy

Resistance: membrane pump

A

Chloroquine

Heme accumulates, is toxic to Plasmodia.

Life-threatening malaria in US: quinidine

56
Q

Flukes- such as Schistosoma

A

Praziquantel

57
Q

Pyrimethamine

Suramin and melarsoprol

Nifurtimox

Sodium stibogluconate

A

Antiprotozoans

Pyrimethamine- toxoplasmosis

Suramin and melarsoprol- Trypanosoma brucei

Nifurtimox- Trypanosoma cruzi

Sodium stibogluconate- Leishmaniasis

58
Q

Mebendazole

Pyrantel pamoate

Ivermectin

Diethylcarbamazepine

Praziquantel

A

Antihelminthic

59
Q

Inhibits neuraminidase

Influenza A and B

A

Oseltamivir, Zanamivir

60
Q

Inhibits synthesis of guanine nucleotides

(competitive IMP dehydrogenase inhibition)

Respiratory synctial virus, chronic HCV

Hemolytic anemia, severe teratogen

A

Ribavirin

61
Q

Guanosine analog

Monophosphorylation by viral thymidine kinase

DNA Pol chain termination

Herpes simplex virus, Varicella zoster virus

A

Acyclovir

Prophylaxis in immunocompromised

Valacyclovir (prodrug) better bioavailability

For herpes zoster- famiciclovir

62
Q

Guanosine analog

Converted to monophosphate by viral kinase

Inhibits viral DNA Pol

Cytomegalovirus

Leukopenia, neutropenia, thrombocytopenia, renal toxicity

A

Ganciclovir

Valganciclovir (prodrug)- better oral bioavailability

63
Q

Inhibits viral DNA Pol

by binding pyrophosphate binding site

No activation by viral kinase

CMV retinitis in immunocompromised

(when ganciclovir fails)

Acyclovir-resistant HSV

Nephrotoxicity

A

Foscarnet

Pyrophosphate analog

64
Q

Inhibits viral DNA Pol

No activation by viral kinase

CMV retinitis in immunocompromised

Acyclovir-resistant HSV

Long half-life

Nephrotoxicity

A

Cidofovir

Codminister with probenecid and IV saline

to reduce toxicity

65
Q

HIV therapy

A

2 nucleoside reverse transcriptase inhibitors (NRTIs)

+

1 non-NRTI

or

1 protease inhibitor

or

1 integrase inhibitor

66
Q

Prevent cleavage of HIV proteins into functional parts

Hyperglycemia, GI intolerance, lipodystrophy

A

Protease inhibitors

Lopinavir, atazanavir, darunavir, fosamprenavir, saquinavir, ritonavir, indinavir

-navir tease a protease

67
Q

Protease inhibitor

Nephropathy, hematuria

A

Indinavir

68
Q

Competitive inhibition of nucleotide binding to RT

DNA chain termination

(lack 3’ OH group)

Most need to be phosphorylated

Bone marrow suppression, peripheral neuropathy, lactic acidosis, rash, anemia

A

Nucleoside reverse transcriptase inhibitors

Tenofovir, emtricitabine, abacavir, lamivudine, zidovudine, didanosine, stavudine

Tenofovir- doesnt need phosphylation

(a nucleo_tide)_

Zidovudine- prophylaxis during pregnancy

69
Q

Competitive inhibition of nucleotide binding to RT

No phosphorylation

Bone marrow suppression, peripheral neuropathy, lactic acidosis, rash, anemia

A

Non-nucleoside reverse transcriptase inhibitors

Nevirapine, efavirenz, delavirdine

70
Q

Inhibits HIV genome integration into host cell

Reversible inhibition

Hypercholesterolemia

A

Integrase inhibitors

Raltegravir

Reversible inhibition of HIV integrase

71
Q

Block both DNA, RNA viral replication

Glycoproteins synthesized by infected cells

Chronic HBV, HCV, Kaposi’s sarcoma

Multiple sclerosis

NADPH oxidase deficiency

Neutropenia, myopathy

A

Interferons

IFN-alpha

IFN-beta

IFN-gamma

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