Micro AntiMicrobials Flashcards

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1
Q

Blocks cell wall synthesis by inhibiting peptidoglycan cross-linking

A

Penicillin, Methicillin, Ampicillin, Piperacillin, Cephalosporins, Aztreonam, Imipenem

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2
Q

Blocks peptidoglycan synthesis

A

Bacitracin, Vancomycin

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3
Q

Inhibits Folic Acid Synthesis (involved in methylation)

A

Sulfonamides, Trimethoprim

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4
Q

Blocks DNA topoisomerase

A

Fluoroquinolones

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5
Q

Blocks mRNA synthesis

A

Rifampin

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6
Q

Damages DNA

A

Metronidazole

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7
Q

Blocks protein synthesis at 50S ribosome

A

Chloramphenicol, Macrolides, Clindamycin, Streptogamins (Quinupristin, dalfopristin), Linezolid

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8
Q

Blocks protein synthesis at 30S ribosome

A

Aminoglycosides, Tetracycline

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9
Q
Penicillin 
Names? Class? 
MoA
Use? Bactericidal for...
Tox
Resistance
A

G (IV and IM), V (oral). β-lactam Antibiotic
Binds PBP (transpeptidiases) and blocks its cross-linking of peptidoglycan
Gram+, N meningitidis, T pallidum, Syphilis
Bactericidal for Gram+ cocci, Gram+ rods, Gram- cocci, Spirochetes
Hypersensitivity rxn, Hemolytic anemia
β-lactamase cleaves β-lactam ring

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10
Q
Penicillinase-Resistent Penicillins 
Names 
Spectrum 
MoA
Use
Tox
A

Oxacillin, Nafcillin, Dicloxacillin
Narrow spectrum
Same as penicillin but bulk R group blocks β-lactamase access
S aureus (except MRSA)
Hypersensitivity reaction. Interstitial nephritis

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11
Q
Aminopenicillins 
Names? Spectrum? 
MoA
Availability 
Use
Tox
Resistance
A

Ampicillin and Amoxicillin. Wide spectrum
Same as penicillin.
AmOxicillin has greater Oral availability
“HELPSS kill Enterococci “
H influenzae, E coli, Listeria, Proteus, Salmonella, Shigella, Enterococci
Hypersensitivity rxn, Ampicillin rash, Pseudomembranous colitis
Penicillinase sensitive. Combine w/ Clavulanic acid to protect against β-lactamase

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12
Q
Antipseudomonals 
Names
MoA? Spectrum? 
Use
Tox
Resistance
A
Ticarcillin and Peperacillin 
Same as penicillin. Extended spectrum 
Pseudomonas and Gram- rods
Hypersensitivity rxn
Penicillinase. Use with Clavulanic acid
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13
Q

β-lactamase Inhibitors

A

“CAST”

Clavulanic Acid, Sulbactam, Tazobactam

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14
Q
Cephalosporins 
MoA
Resistance 
What does it do to bacteria 
What bacteria can in kill? 
Tox
A

β-lactam
Less susceptible to penicillinase
Does not kill “LAME” bugs
Listeria, Atypicals (chlamydia, Mycoplasma, MRSA, Enterococci
Ceftaroline covers MRSA
Hypersensitivity, VitK deficiency. ↑ nephrotoxicity of aminoglycosides

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15
Q

1st gen Cephalosporins
Names
Uses

A

Cefazolin, Cephalexin
Gram+ cocci, Proteus, E coli, Klebsiella
“PEcK”
Cefazolin used prior to surgery to prevent S aureus wound infection

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16
Q

2nd gen Cephalosporins
Names
Uses

A

Cefoxitin, Cefaclor, Cefuroxime
Gram+ cocci, Haemophilus, Enterobacter aerogenes, Neisseria, Proteus, E coli, Klebsiella, Serratia
“HEN PEcKS”

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17
Q

3rd gen Cephalosporins
Names
Uses

A

Ceftriaxone, Cefotaxime, Ceftazidime
Serous Gram- infections resistant to other β-lactam
Ceftriazone: Meningitis and Gonorrhea
Ceftazidime: Pseudomonas

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18
Q

4th gen Cephalosporins
Names
Uses

A

Cefepime

Pseudomonas and Gram+

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19
Q
Aztreonam 
MoA
Resistance
Use
Tox
A

Monobactam. Prevents peptidoglycan cross-linking by binding PBP3
Resistant to β-lactamase
Gram- rods only. No activity against Gram+ or anaerobes (pseudomonas)
Used for penicillin allergy pts and those with renal insufficiency who cannot tolerate aminoglycosides
Generally nontoxic. Possible GI upset.

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20
Q
Carbapenems
Names
MoA
Co-administration w/... 
Resistance 
Use
Tox
A

Imipenem, Meropenem, Ertapenem, Doripenem
Broad spectrum β-lactam.
I is coadministered w/ Cilastatin (inhibitor of renal dehydropeptidase I) to ↓ inactivation of drug in renal tubules. M resistent to inactivation
Resistent to β-lactamase
Gram+ cocci, Gram- rods, and anaerobes
Only used when all else fails or life threatening
GI distress, Skin rash, CNS tox (seizures)

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21
Q
Vancomycin 
MoA
What does it do to bacteria?
Use
Tox
Resistance
A

Inhibits cell wall peptidoglycan formation by binding D-ala D-ala portion of cell wall precursors
Bactericidal
Gram+ only. Multi-drug resistant organisms: MRSA, enterococci, C diff
“NOT so bad”
Nephrotoxic, Ototoxic, Thrombophlebitis (inflammation of a vein caused by a blood clot), Diffuse flushing - Red Man Syndrome (prevented by pretreatment with antihistamines and slow infusion rate)
Mutation of 2nd D-ala to D-lac

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22
Q

Protein Synthesis inhibitors

A

“Buy AT 30, CCEL (sell) at 50”
30S inhibitors:
Aminoglycosides (bactericidal), Tetracyclines (bacteristatic)
50S inhibitors (bacteristatic):
Chloramphenicol, Clindamycin, Erythromycin (macrolides), Linezolid (variable)

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23
Q
Aminoglycosides 
Names 
What does it do to bacteria?
MoA
Uptake
A

“Mean GNATS caNNOT kill Anaerobes”
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
Bactericidal
Inhibits formation of initiation complex and causes misreading. Blocks translocation
Needs O2 for uptake thus ineffective against anaerobes

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24
Q

Aminoglycosides
Use
Tox
Resistance

A

“Mean GNATS caNNOT kill Anaerobes”
Severe Gram- rods. Synergistic w/ β-lactams. N for bowel surgery
Nephrotoxic (esp w/ cephalosporins), Neuromuscular blockade, Ototoxic (esp w/ loops diuretics), Teratogen
Transferase enzyme that inactivates the drug by acetylation, phosphorylation or adenylation

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25
Q
Tetracylcines 
Names 
What does it do to bacteria?
MoA
Elimination 
Do not take w/
A

Tetracycline, Doxycycline, Demeclocycline, Minocycline
Bacteriostatic
Binds 30S and prevents attachment of aminoacyl-tRNA
Demeclocycline is an ADH antagonist used to treat SIADH
Doxycycline fecally eliminated so it can be given to pts with renal failure
Do not take with milk, antaacids, iron b. divalent cations inhibit gut absorption

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26
Q
Tetracylcines
Use
Tox
Contraindications 
Resistance
A

Borrelia burgdorferi, M pneumoniae, Rickettsia, and Chlamydia (accumulates in cells so good at killing last 2)
GI distress, discoloration of teeth and inhibition of bone growth in children. Photosensitivity
Pregnancy
↓ Uptake or ↑ efflux by plasmid encoded pump

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27
Q
Macrolides 
Names
What does it do to bacteria 
MoA
Use
A
Azithromycin, Clarithromycin, Erythromycin 
Bacteriostatic
Blocks translocation ("macroSLIDES"). Binds 23S rRNA of 50S ribosome 
Atypical pneumonia (Mycoplasma, Chlamydia, Legionella), STDs (Chlamydia), Gram+ cocci (strep in pts allergic to penicillin)
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28
Q

Macrolides
Tox
Resistance

A

“MACRO”
Motility issues, Arrhythmia (long QT), acute Cholestatic hepatitis, Rash, eOsinophilia. Increased serum concentration of theophyllines and oral anticoagulants
Methylation of 23S rRNA binding site

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29
Q
Chloramphenicol 
What does it do to bacteria?
MoA
Use
Tox
Resistance
A

Bacteriostatic. Blocks peptidyltransferase at 50S
Meningitis (Haemophilus, N meningitidis, Strep pneumoniae)
Anemia, Aplastic anemia, Gray baby syndrome (in premies b/c lack of UDP glucuronyl transferase)
Plasmid encoded acetyltransferase inactivates drug

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30
Q
Clindamycin 
What does it do to bacteria?
MoA
Use
Tox
A

Bacteriostatic. Blocks peptide transfer (transpeptidation) at 50S ribosomal subunit
Anaerobes (Bacteroides fragilis, C perfringens) in aspiration pneumonia or lung abscesses. Oral infections with mouth anaerobes
“Anaerobes above the diaphragm”
Pseudomembranous colitis (C diff overgrowth), Fever, Diarrhea

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31
Q
Sulfonamides 
Names
What does it do to bacteria?
MoA
Use
Tox
Resistance
A

Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine
Bacteriostatic
PABA antimetabolite inhibits dihydropteroate syntahse
Gram+, Gram-, Nocardia, Chlamydia, UTIs
Hypersensitivity, Hemolysis (G6PD deficiency), Nephrotoxic (tubulointerstitial nephritis), Photosensitivity, Kernicterus (infants), Displace other drugs from albumin (warfarin)
Altered dihydropteronate synthase, ↓ uptake, ↑ PABA synthesis

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32
Q

Bacterial DNA, RNA, and Protein Synthesis

A

PABA + Pteridine –> [Dihydropteroate Synthase] –> Dihydropteroic acid –> Dihydrofolic acid –> [Dihydrofolate reductase] –> THF –> N methylene THF –> Purines (DNA and RNA), Thymidine (DNA), and Methionine (proteins)

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33
Q
Trimethoprim 
What does it do to bacteria? 
MoA
Used w/
Use
Tox
A

Bacteriostatic
Inhibits bacterial DHF reductase
Combined with SMX
UTIs, Shigella, Salmonella, Pneumocystis jirovecii pneumonia (treatment and prophylaxis)
“TMP: Treats Marrow Poorly”
Megaloblastic anemia, Leukopenia, Granulocytopenia. May alleviate w/ supplemental folic acid (Leucovorin rescue)

34
Q
Fluoroquinolones 
Names 
What does it do to bacteria 
Co-administration 
MoA
Resistance
A

Ciprofloxacin, Norfloxacin, Levofloxacin, Olfoxacin, Sparfloxacin, Moxifloxacin, Gatifloxacin, Enoxacin. Nalidixic acid (quinolone)
Bactericidal. Do not take with antacids
Inhibits DNA gyrase (topoisomerase II) and topoisomerase IV
Chromosome-encoded mutation in DNA gyrase, Plasmid-mediated resistance, efflux pumps

35
Q

Fluoroquinolones
Use
Tox
Contraindications

A

Gram- rods of Urinary and GI tracts (including Pseudomonas), Neisseria, Some Gram+ organisms
“LONES hurt your BONE attachments”
GI upset, Super-infections, Skin rashes, Headache, Dizziness. Tendonitis, Tendon rupture, Leg cramps, Myalgias, Long QT
Pregnant women, Children (damage to cartilage)

36
Q
Metronidazole 
What does it do to pathogens? 
MoA
Use
Tox
A

Bactericidal. Antiprotozoal
Free radicals
“GET GAP on the METRO”
Giardia, Entamoeba, Trichomanas, Gardnerella vaginalis, Anaerobes below the diaphragm (Bacteroides, C diff), H pylori (w/ PPI and Clarithromycin)
Disulfiram-like reaction w/ EtOH, Headache, Metallic taste

37
Q

Antimycobacterial Drugs

A

Tuberculosis
Prophylaxis: Isoniazid. Treatment: “RIPE” Rifampin, Isoniazid, Pyrazinamide, Ethambutol
M avium-intracellulare
Prophylaxis: Azithromycin. Treatment: Azithromycin, Rifampin, Ethambutol, Streptomycin
Leprae
Treatment: Tuberculoid form w/ Dapsone and Rifampin. Add Clofazimine for Lepromatous form

38
Q
Isoniazid 
Activation 
MoA
Use
Tox
A
Bacterial catalase-peroxidase (KatG) converts INH into active metabolite 
↓ synthesis of mycolic acids
TB
Neurotoxicity and Hepatotoxicity. Lupus 
VitB6 prevents neurotoxicity
39
Q

Rifampin
MoA
Use
Tox

A

“4Rs” RNA pol, Revs up P450, Red/Orange fluid, Rapid resistance if used alone
Inhibits DNA-dependent RNA pol
TB. Delays resistance to dapsone in leprosy. Meningococcal prophylaxis and chemoprophylaxis in contacts of children with Haemophilus influenzae type B
Hepatotoxic. Drug interactions (↑ P450). Orange body fluid

40
Q

Pyrazinamide
MoA
Use
Tox

A

Acidifies intracellular environment
TB
Hyperuricemia, Hepatotoxic

41
Q

Ethambutol
MoA
Use
Tox

A

↓ carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltranferase
TB
Optic neuropathy (Red-Green Color Blindess)

42
Q

Meningococcal infection prophylaxis

A

Ciprofloxacin or Rifampin (for children)

43
Q

Gonorrhea prophylaxis

A

Ceftriaxone

44
Q

Syphilis prophylaxis

A

Benzathine Penicillin G

45
Q

History of recurrent UTI prophylaxis

A

TMP-SMX

46
Q

Endocarditis with surgical or dental procedures prophylaxis

A

Penicillins

47
Q

Pregnant woman carrying GBS prophylaxis

A

Ampicillin

48
Q

Strep Pharyngitis in child with prior RF prophylaxis

A

Oral penicillin

49
Q

Post-surgical infection due to S aureus prophylaxis

A

Cefazolin

50
Q

Gonococcal or Chlamydial conjunctivitis in newborns prophylaxis

A

Erythromycin ointment

51
Q

HIV prophylaxis for CD4 less than 200

A

TMP-SMX for Pneumocystis pneumonia

Aerosolized pentamidine used if pt cannot tolerate TMP-SMX but this may not prevent toxoplasmosis

52
Q

HIV prophylaxis for CD4 less than 100

A

TMP-SMX for Pneumocystis pneumonia and Toxoplasmosis

Aerosolized pentamidine used if pt cannot tolerate TMP-SMX but this may not prevent toxoplasmosis

53
Q

HIV prophylaxis for CD4 less than 50

A

Azithromycin for Mycobacterium avium complex

54
Q

Treatment of MRSA and VRE (enterococci)?

A

MRSA: Vancomycin
VRE: Linezolid and Streptogramins (quinupristin/dafopristin)

55
Q
Amphotericin B
MoA
Use
Route
Supplement
Tox
How to reduce tox?
A

Binds ergosterol forming pores in membrane
Cryptococcus (w/ or w/o Flucytosine), Blastomyces, Coccidioides, Histoplasma, Candida, Mucor
Intrathecally for fungal meningitis
K and Mg to change renal tubule permeability
Fever/Chills (“shake and bake”), Hypotension, Nephrotoxic, Arrhythmias, Anemia, IV phlebitis
Hydration (for kidneys) and Liposomal form reduces tox

56
Q

Nystatin
MoA
Use

A

Binds ergosterol forming pores in membrane

“Swish and swallow” for oral candidiasis (thrush). Topical for diaper rash or vaginal candidiasis

57
Q
Azoles 
Names
MoA
Use
Tox
A

Fluconazole, Ketoconazole, Clotimazole, Miconazole, Itraconazole, Voriconazole
Inhibits fungal sterol (ergosterol) synthesis by inhibiting P450 that converts Lanosterol to Ergosterol
F for chronic suppression of Crytococcal meningitis in AIDS and Candidal infection of all types
I for Blastomyces, Coccidioides, Histoplasma
C and M for topical fungal infections
Inhibits Testosterone synthesis (gynecomastia), Liver dysfunction

58
Q

Flucytosine
MoA
Use
Tox

A

Inhibits DNA and RNA synthesis by conversion to 5FU by cytosine daminase
Systemic fungal infections (esp miningitis by Cryptococcus) w/ Amphotericin B
Bone marrow suppression

59
Q

Caspofungin, Micafungin
MoA
Use
Tox

A

Inhibits cell wall synthesis by inhibiting β-glucan
Invasive aspergillosis, Candida
GI upset, Flushing (by histamine release)

60
Q

Terbinafine
MoA
Use
Tox

A

Inhibits fungal enzyme Squalene Epoxide
Dermatophytoses (onychomycosis)
LFTs, visual disturbances

61
Q
Griseofulvin
MoA
Where does it accumulate?
Use
Tox
A

Interferes to MT function disrupting mitosis
Oral treatment for superficial infection.
Deposits in keratin containing tissues (nails)
Inhibits growth of dermatophytes (tinea, ringworm)
Teratogenic, Carcinogenic, Confusion, Headaches, ↑ P450 (warfarin metabolism)

62
Q

Antiprotozoan Therapy

A

Pyrimethamine (toxoplasmosis), Suramin and Melarsoprol (Trypanosoma brucei), Nifurtimox (T cruzi), Sodium Stibogluconate (Leishmaniasis)

63
Q
Chloroquine 
MoA
Resistance 
Use
Tox
A

Blocks detoxification of Heme into Hemozoin. Heme accumulates and is toxic to Plasmodia
Plasmodial species other than P falciparum
Membrane pump that ↓ intracellular concentration
Retinopathy

64
Q

Treatment for Plasmodia falciparum

A

Artemether/lumifantrine or Atovaquone/Proguanil

65
Q

Treatment for life-threatenting malaria

A

Quinidine (in US), Quinine (Elsewhere), Artisunate

66
Q

Anti-Helminthic Therapy
Names
MoA

A

Mebendazole, Pyrantel Pamoate, Ivermectin, Diethylcarbamazine, Praziquantel (for flukes like Schistosoma)
Imobilizes helminths

67
Q

Zanamivir, Oseltamivir
MoA
Use

A

Inhibits Influenza Neuraminidase decreasing release of progeny
Treatment and Prevention of Influenza A and B

68
Q

Ribavirin
MoA
Use
Tox

A

Inhibits synthesis of Guanine by competitively inhibiting IMP dehydrogenase
RSV, HCV (chronic)
Hemolytic anemia, Teratogen

69
Q
Acyclovir 
MoA
Use
Better version?
Tox
Resistance
A

Guanosine analog that inhibits viral DNA pol by chain termination
HSV and VZV. Weak activity against EBV
HSV induced mucocutaneous or genital lesions and encephalitis. Prophylaxis for immunocompromised pts
No effect on latent HSV or VZV
Vanacyclovir has better bioavailability
Few toxicities
Mutated viral Thymidine kinase

70
Q

Treatment for Herpes Zoster (Shingles)

A

Famciclovir

71
Q
Ganciclovir 
MoA
Use
Better version?
Tox
Resistance
A

Guanosine analog that inhibits viral DNA pol
CMV
Valganiciclovir is a prodrug with better bioavailability
Leukopenia, Neutropenia, Thrombocytopenia, Renal toxicity
Mutated CMV DNA pol or lack of viral kinase

72
Q
Foscarnet 
MoA
Use
Tox
Resistance
A

Pyrophosphate analog. Viral DNA pol inhibitor
CMV retinitis (when ganciclovir fails), HSV (when acyclovir fails)
Nephrotoxic
Mutated DNApol

73
Q
Cidofovir 
MoA
Use
Half life 
Tox
Co-administration
A

Inhibits viral DNA pol
CMV retinitis, HSV (when acyclovir fails)
Long half-life
Nephrtoxic
Probenecid and IV saline to reduce toxicity

74
Q

HAART
When is it initiated?
Regimen

A

AIDS-defining illness, low CD4 (below 500), High vial load

2 nucleoside RT inhibitors + 1 non-nucleoside RT inhibitor OR Protease inhibitor OR Integrase inhibitor

75
Q

Protease inhibitors
Names
MoA
Tox

A

“Navir tease a protease”
-navir (Lopi, Ataza, Daru, Fosampre, Saqui, Rito, Indi)
Protease cleaves products of HIV mRNA into functional parts
Ritonavir can boost other [drug] by inhibiting P450
Hyperglycemia, GI intolerance (nausea, diarrhea), Lipodystrophy
Indinavir: Nephropathy and Hematuria

76
Q
NRTI
Names 
MoA
Activation 
Uses 
Tox
A

“Have you DINED with my NUCLEAR family”
Tenofovir (TDF), Emtricitabine (FTC), Abacavir (ABC), Lamivudine (3TC), Zidovudine (ZDV, AZT), Didanosine (ddl), Stavudine (d4T)
Competitive NT that gets used by RT but has not 3’ OH –> early chain termination
TDF does not need activation. The rest need to phosphorylated
ZDV used as prophylaxis during pregnancy
Bone marrow suppression (reversible w/ G-CSF and EPO), Peripheral neuropathy, Lactic Acidosis, Anemia (ZDV)

77
Q
NNRTIs
Names
MoA
Activation 
Tox
A

Nevirapine, Efaverenz, Delavirdine
Inhibits RT
Does not require phosphorylation
Bone marrow suppression (reversible w/ G-CSF and EPO), Peripheral neuropathy, Rash, Anemia (ZDV)

78
Q

Integrase Inhibitors
Names
MoA
Tox

A

Raltegravir
Inhibits HIV genome integration into host cell chromosome
Hypercholesterolemia

79
Q
Interferons 
What is it? What produces it?
MoA
Use
Tox
A

Glycoprotein synthesized by virus-infected cells.
Blocks replication of both RNA and DNA viruses
IFNα: chronic HBV or HCV, Kaposi sarcoma
IFNβ: MS
IFNγ: NADPH oxidase deficiency
Neutropenia, Myopathy

80
Q

Antibiotics to avoid during pregnancy

A

“SAFe Children Take Really Good Care”

Sulfonamides (Kernicterus), Aminoglycosides (Ototoxic), Fluoroquinolones (Cartilage damage), Clarithromycin (Embryotoxic), Tetrocycline (Discolored teeth, inhibition of bone growth), Ribavirin (teratogenic), Griseofulvin (Teratogenic), Chloramphenicol (gray baby)

81
Q

Killed Influenza Vaccine

A

Generates Abs to H preventing entry of viral particles into the cells