Pharmacology: Antimicrobials/antibiotics(Usmle Step1)

Front 1

Antimicrobials: Combinations used(general)?

Back 1

Additive (1+1=2)
Synergist (1+1>2)
Antagonist (1+1<2)

Front 2

Antimicrobial combination: Synergistic combinations?

Back 2

Synergistic combination=
Penicillins+Aminogycosides
(Cidal + Cidal)

Front 3

Antimicrobial combination: Antagonistic combinations?

Back 3

Penicillins + Tetracyclins
(Cidal+ Static)

Front 4

Cidal + Static drugs ____(should/should not) be combined

Back 4

Should not

NEVER COMBINE STATIC+CIDAL

Front 5

Bacterial cell wall synthesis inhibitors: Name the drugs/drug classes?

Back 5

1. Penicillins
2. Cephalosporins
3. Imipenem
4. Meropenem
5. Aztreonam
6. Vancomycin

Front 6

Bacterial protein synthesis inhibitors: Name the drugs/drug classes?

Back 6

1. Aminoglycosides
2. Chloramphenicol
3. Macrolides
4. Tetracyclines
5. Streptogramins
6. Linezolid

(CLE TAG)

Front 7

Bacterial nucleic acid synthesis inhibitors: Name the drug/drug classes?

Back 7

1. Fluoroquinolones
2. Rifampin

Front 8

Bacterial folic acid synthesis inhibitors: Name the drug/drug classes?

Back 8

1. Sulfonamides
2. Trimethoprim
3. Pyrimethamine

Front 9

Mechanism of resistance against penicillin and cephalosporins?

Back 9

1. Beta lactamases production
2. Change in PBP structure
3. Change in porins

Front 10

Mechanism of resistance against aminoglycosides?

Back 10

Formation of enzymes that inactivate the drug through the process of ______ via
1. _____
2. _____
3. _____

Hint 10

Through the process of "conjugation" via:
1. Acetylation
2. Adenylylation
3. Phosphorylation

Front 11

Mechanism of resistance against Macrolides?

Back 11

1. Methyltransferase formation--> Alters binding site on 50S ribosomal subunit
2. Active transport out of the cell

Front 12

Mechanism of resistance against Tetracyclines?

Back 12

Increased P-glycoprotein pump that pumps drugs out of the cell

Front 13

Mechanism of resistance against Sulfonamides?

Back 13

1. Altered enzyme sensitivity to action of binding drug
2. Use of exogenous folic acid
3. Increased formation of PABA

Front 14

Mechanism of resistance against Fluoroquinolones?

Back 14

1. Altered enzyme sensitivity to action of binding drug
2. Increased activity of transport system to promote drug efflux

Front 15

All bacterial cell wall synthesis inhibitors are _____ (bactericidal/bacteriostatic)?

Back 15

Bactericidal

Front 16

Penicillins: MOA?

Back 16

1. Bind to PBP
2. Inhibition transpeptidation -->
3. Inhibition of cross-linking

Front 17

Microbes associated with:
1. Penicllinase activity?
2. PBP structure alteration?
3. Porin structure alteration?

Back 17

1. Penicillinase: Staph
2. PBP alteration: Pneumococci, MRSA
3. Porins: Pseudomonas

Front 18

Narrow spectrum b-lactamase sensitive group of penicillin drugs: Name em.

Back 18

1. Penicillin G
2. Penicillin V

Front 19

Narrow spectrum b-lactamase sensitive group of penicillin drugs: Spectrum of activity?

Back 19

1. TREPONEMA PALLIDUM
2. Streptococci
3. Pneumococci
4. Meningococci

Front 20

Narrow spectrum b-lactamase resistant group of penicillin drugs: Name em.

Back 20

1. Methicillin
2. Nafcillin
3. Oxacillin
4. Cloxacillin

Front 21

Broad spectrum b-lactamase sensitive group of penicillin drugs: Name em.

Back 21

1. Amoxicillin
2. Ampicillin

Front 22

Broad spectrum b-lactamase sensitive group of penicillin drugs:
Spectrum of activity?

Back 22

1. All gram +ves(except staph)
2. E-coli
3. H.influenza
4. Listeria monocytogenes
5. Borellia burgdorferi
6. H.pylori

Front 23

Ampicillin/amoxicillin not effective against _____ (gram +ve cocci)

Back 23

Staph

Front 24

Listeria monocytogenes: DOC- ____(Ampicillin/amoxicillin)

Back 24

Ampicillin

"LASER- listeria amplification"

Front 25

H.Pylori: DOC-
____(Ampicillin/amoxicillin)

Back 25

Amoxicillin

Front 26

Borellia burgdorferi: DOC- ____(Ampicillin/amoxicillin)

Back 26

Amoxicillin

Front 27

Extended spectrum b-lactamase sensitive group of penicillin drugs

Back 27

1. Ticarcillin
2. Piperacillin
3. Azlocillin
4. Carbenicillin

Extended spectrum activity against?

Hint 27

Pseudomonas

Front 28

Suicide inhibitors:
Name em.
MOA?

Back 28

Clavulanic acid
Sulbactam
Tazobactam

MOA: Irreversibly inhibits b-lactamase

Front 29

Penicillin group of drugs- synergy observed with?

Back 29

Aminoglyosides

Front 30

Penicillins -mechanism of elimination?
Implication?

Back 30

Active tubular secretion in kidney

Renal excretion implies dose reduction in renal failure

Exceptions?

Hint 30

Exceptions:
1. Nafcillin
2. Oxacillin

(Nafcillin Oxacillin: NO are NOT excreted through kidneys.

Front 31

Mechanism of elimination of Nafcollin and Oxacillin?

Back 31

Through bile

Implication?

Hint 31

Nafcillin and Oxacillin cannot be used in liver dysfunction

Front 32

Penicillin available in repository form?

Back 32

Benzathine penicilline G

Front 33

Penicillin with long half life?

Back 33

Benzathine penicillin

T1/2: 2 weeks

Front 34

Penicillin hypersenstivity: type?

Back 34

ALL types
Type I,II,III,IV

Type I:
1. Laryngospasm
2. Anaphylaxis
3. Angioedema

Type II:
1. Vasculitis
2. Neutropenia
3. Positive coomb's

Type III:
1. Vasculitis
2. Serum sickness
3. Interstitial nephritis

Type IV:
1. Urticarial/Maculopapular rash.
2. SJS

Front 35

Identify type of hypersensitivity for:
1. Urticaria
2. Positive Coomb's test
3. Angioedema
4. Serum sickness
5. SJS
6. Interstitial nephritis
7. Vasculitis
8. Laryngospasm
9. Neutropenia
10. Anaphylaxis
11. Maculopapular rash

Back 35

1. Urticaria: Type IV
2. Positive Coomb's: Type II
3. Angioedema: Type I
4. Serum sickness: Type III
5. SJS: Type IV
6. Interstitial nephritis: Type III
7. Vasculitis: Type II and Type III
8. Layngospasm: Type I
9. Neutropenia: Type II
10. Anaphylaxis: Type I
11. Maculopapular rash: Type IV

Front 36

Penicillins: Adverse reactions?

Back 36

1. Hypersensitivity reactions (I thru IV)
2. Interstitial nephritis
3. NVD
4. Jarisch-Herxheimer reaction

Front 37

Interstitial nephritis commonly observed with which penicillin?

Back 37

Methicillin

Front 38

Jarisch herxheimer reaction commonly observed with which penicillin?

Back 38

In rx with penicillin for syphilis

Front 39

GI distress commonly observed with which penicillin?

Back 39

Ampicillin

Why?

Hint 39

Ampicillin is poorly absorbed in the gut

Front 40

Jarisch Herxheimer reaction?

Back 40

Observed in treatment of syphilis: Immune response observed after destruction of t.pallidum and release of antigens

1. Fever
2. Swelling
3. Joint pain

Front 41

Very long acting penicillin?

Back 41

Benzathine penicillin

How is it adminstered (what form)?

Hint 41

1. IM- thick suspension slow release
(Slow release)

"BenzaThick penicillin- thick slow release suspension"--> Long t1/2

Front 42

Cephalosporin: MOA?

Back 42

1. Bind to PBP
2. Inhibition transpeptidation -->
3. Inhibition of cross-linking

Front 43

First generation cephalosporin: Name em?

Back 43

1. Cefazolin
2. Cephalexin

All Cephalosporins with "ph"s instead of "f"s

Spectrum of activity?

Hint 43

1. Gram +ve COCCI
2. Ecoli
3. Kliebsella
4. Proteus

Evade the Problematic Fight Klub

Front 44

Cephalosporin generation I: unique pharmacokinetic property?

Back 44

Do not enter the CNS

Front 45

Cephalosporin generation I:
Use?

Back 45

In surgical prophylaxis (due to its broad spectrum of activity)

Front 46

Cephalosporin generation II: Name em?

Back 46

Cefotetan
Cerfuroxime
Cefaclor

Spectrum?

Hint 46

increased -ve coverage

Front 47

Cephalosporin generation II drug that crosses the BBB?

Back 47

Cefuroxime

Front 48

Cephalosporin generation III: Name em?

Back 48

1. Cephtriaxone
2. Cephotaxime
3. Cephoperazone
4. Cefdinir

"Tried tax per dinar"

Front 49

Cephalosporin: elimination?

Back 49

All eliminated through active tubular secretion via kidneys except
______?

Hint 49

1. Ceftriaxone
2. Cefoperazone

Eliminated in bile

Front 50

Cephalosporins: Side effects?

Back 50

1. Hypersensitivity reactions etc
same as penicillins

2. Disulfiram like effects observed with

Hint 50

1. Cefotetan
2. Cefoperazone

Front 51

Drug fever _____common/uncommon with cepahlosporins?

Back 51

common

Front 52

Cephalosporin generation III: drug that does not cross the BBB?

Back 52

Cefoperazone

Front 53

Cpehalosporin generation III: Use?

Back 53

Empiric management of:
1. Meningitis
2. Sepsis

Front 54

Cephalosporin generation IV: properties?

Back 54

1. Wide spectrum
2. B-lactamase resistant
3. Crosses BBB

Front 55

Organisms not covered by cephalosporins?

Back 55

Listeria
Atypicals(mycoplasma/chlamydia)
MRSA
Enterococci

Front 56

Imipenem/meropenem: MOA?

Back 56

Similar to penicillin

Front 57

Imepenem and meropenem are beta-lactamase _____sensitive/resistant?

Back 57

Resistant

Front 58

Imepenem/meropenem: spectrum of activity?

Back 58

1. Effective against all microbes
2. Gram +ve cocci
3. Gram -ve rods
4. Anaerobes

Front 59

Imepenem/meropenem: use?

Back 59

In severe life-threatening infections

Front 60

Imipenem is always administered with ____?

Back 60

Cilastin

why?

Hint 60

Cilastin inhibits renal de-hydrpeptidase(breaks down imepenem-->nephrotoxic compound)
1. Increases half life of imepenem
2. Also prevents nephrotoxicity

Front 61

Drugs used in empiric Rx of life threatening sepsis/meningitis?

Back 61

1. IIIrd generation cephalosporins
2. Imipenem/Meropenem

Front 62

Imipenem/meropenem: elimination?

Back 62

Through the kidney

Front 63

Imepenem/meropenem: adverse effects?

Back 63

1. GI distress
2. Drug fever
3. CNS effects- (seizures with imipenem)

Front 64

Aztreonam : MOA?

Back 64

Same as penicillins

Front 65

Penicillin/related drugs resistant to beta-lactamase

Back 65

1. Nafcillin/cloxacillin/oxacillin/Methicillin
2. Cefapime(IV generation cephalosporin)
3. Imepenem/meropenem
4. Aztreonam

Front 66

Penicillin/cephalosporin/related drugs cleared through bile?

Back 66

1. Nafcillin
2. Oxacillin
3. Ceftriaxone
4. Cefoperazone

Front 67

Penicillin/cephalosprin/related drugs safe in renal impairment?

Back 67

1. Nafcillin
2. Oxacillin
3. Ceftriaxone
4. Cefoperazone

Front 68

Cephalosporins that do not have CNS entry?

Back 68

1. Ist generation cephalosporins
2. IInd generation cephalosporins (except cefuroxime)
3. Cefoperazone

Front 69

Cephalosporins used in empirical treatment of meningitis/sepsis?

Back 69

IIIrd generation cephalosporin

Front 70

Wide spectrum cephalosporin?

Back 70

Cefepime

Mode of administration?

Hint 70

IV

Front 71

IIIrd generation cephalosporins: modes of administration of each drug?

Back 71

1. Ceftriaxone: IM
2. Cefotaxime: Parenteral
3. Cefoperazone: ?
4. Cefdinir: Oral
5. Cefixim: Oral

Front 72

Cephalosporins used for surgical prophylaxis?

Back 72

Ist generation

Front 73

Cell wall synthesis inhibitor associated with seizures?

Back 73

Imipenem

Also associated with?

Hint 73

Nephrotoxicity

Front 74

Cell wall synthesis inhibitor active mainly against gram -ve rods?

Back 74

Aztreonam

Front 75

Cell wall synthesis inhibitor that has no cross-reactions with penicillins therefore can be used in patients with hypersensitivity to penicillins?

Back 75

Aztreonam

Front 76

Aztreonam: Mode of administration?

Back 76

IV

Front 77

Vancomycin : MOA?

Back 77

1. Binding to D-ALA D-ALA muramyl pentapeptide
2. Inhibits transglycosylation-->
3. Inhibition of peptidoglycan chains.

Front 78

Vancomycin spectrum of activity?

Back 78

1. MRSA
2. Enterococci
3. Clostridium difficile

Front 79

Pseudomembranous colitis: DOC?

Back 79

#1 Metronidazole
#2 Vancomycin

Front 80

Vancomycin resistance?

Back 80

Change of D-ALA to D-Lactate


"D-luck shields"

Front 81

Vancomycin: Administration?

Back 81

IV

Front 82

Vancomycin ____(can/cannot) cross the BBB?

Back 82

Cannot

Front 83

Vancomycin : elimination?

Back 83

Through kidneys

Front 84

Vancomycin: Side effects?

Back 84

1. Red man syndrome
2. Ototoxicity
3. Nephrotoxicity

Red man syndrome?
Hypersensitivity type?

Hint 84

Red discoloration of skin due to flushing from histamine release

Type I hypersensitivity

Front 85

Protein synthesis inhibitor associated with inhibition of initiation complex formation?

Back 85

1. Aminoglycoside
2. Linezolid

Front 86

Protein synthesis inhibitor associated with inteterference with t-rna attachment to A-site?

Back 86

1. Tetracyclines
2. Dalfopristine
3. Quinopristine

Front 87

Protein synthesis inhibitor associated with inhibition of peptidyl transferase enzyme(peptide bond formation?

Back 87

Chloramphenicol

Front 88

Protein synthesis inhibitor associated with inhibition of translocation?

Back 88

1. Macrolides
2. Clindamycin

Front 89

Sites of attachment (50s or 30s) for:
1. Aminoglycosides
2. Tetracylines
3. Quinupristine
4. Linezolid
5. Dalfopristine
6. Chloramphenicol
7. Macrolides
8. Clindamycin

Back 89

1. Aminoglycoside: 30s
2. Tetracyclines: 30s
3. Quinupristine: 50s
4. Linezolid: 50s
5. Dalfopristine: 50s
6. Chloramphenicol: 50s
7. Macrolides: 50s
8. Clindamycin: 50s

"CLEan TAg"

Front 90

Aminoglycoside:
MOA?
Cidal/static?

Back 90

1. Interferes with initiation complex formation
i. Blocks association of 30s with 50s(static)
ii. Causes misreading of code(cidal)-->
incorporation of from amino acid in protein formation

Site of binding (30s/50s)?

Hint 90

30s

Front 91

Tetracyclines:
MOA?
Cidal/static?

Back 91

Prevents binding of aminoacyl tRNA to acceptor site

Static

Site of binding(30s/50s)?

Hint 91

30s

Front 92

Chloramphenicol:
MOA?
Cidal/static?

Back 92

1. Inhibits formation of peptide bond
2. Inhibits activity of peptidyltranserase

Static

Site of binding(30s/50s)?

Hint 92

50s

Front 93

Macrolides:
MOA?
Cidal/static?

Back 93

Inhibit translocation of peptidyl-tRNA from acceptor to donor site (-static)

Static

Site of binding(30s/50s)?

Hint 93

50s

Front 94

Aminoglycosides: spectrum of activity?

Back 94

Gram -ve rods

exceptions?

Hint 94

Anaerobes

Front 95

Aminoglycosides are effective/ineffective against anaerobes?

Back 95

Ineffective against anaerobes

Why?

Hint 95

Since AG utilize O2 dependent pump for uptake by the bacteriae(only present in aerobes)
Absent in anaerobes therefore they are innately resistant

Front 96

Aminoglycosides are DOCs for?

Back 96

1. Tularemia
2. Bubonic plague

(Imagine: Rabbits and baboons eating protein-sugar)

Front 97

Aminoglycosides are used synergistically for _____(organism/infection) with _____(antibiotic)
(2 organisms with 1 combo each)

Back 97

Enterococci: PenicillinG + AG
Pseudomonas: Extended spectrum penicillin

Front 98

Aminoglycosides: administration?
why?

Back 98

Only IV

Since they are sugars they are water soluble therefore not absorbed orally

Front 99

Aminoglycosides: elimination?

Back 99

Through kidneys

Front 100

Aminoglycosides: Side effects?

Back 100

1. Nephrotoxicity
2. Ototoxicity
3. Neuromuscular blockade

Front 101

Aminoglycoside drug interaction in relation to nephrotoxicity?

Back 101

1. Vancomycin
2. Cispatin
3. Amphotericin B
4. Cyclosporin

Front 102

Aminoglycoside drug interaction in relation to ototoxicity?

Back 102

1. Loop diuretics

Front 103

Aminoglycoside: Ototoxicity?

Back 103

1. Hair cell damage
2. Vestibular dysfunction

Front 104

Aminoglycoside: dosing?

Back 104

Once-daily dosing

Front 105

Aminoglycoside: Nephrotoxicity?

Back 105

1. Proteinuria
2. Hypokalemia
3. Acidosis
4. Acute tubular necrosis

Front 106

Aminoglycoside : NM blockade?

Back 106

1. Decreased release of ACh.
(Similar mechanism to botulinus toxin)

2. Enhance effect of skeletal muscle relaxants

Front 107

Tetracyclines:
MOA?

Back 107

Prevents attachment of t-RNA to A site.
-->

Therefore prevent ELONGATION of proteins


Static

Front 108

Aminoglycosides : Name em?

Back 108

1. Gentamicin
2. Tobramicin
3. Amikacin
4. Streptomycin

Front 109

Aminoglycoside used topically?

Back 109

Neomycin in preparation "neopsorin"

Front 110

Aminoglycosides: resistance?

Back 110

Production of conjugase enzyme--> faster elimination

Front 111

Phototoxicity: Associated antibacterial drugs?

Back 111

1. Tetracyclines
2. Sulfonamides
3. Fluoroquinolones

Front 112

Tetracyclines: DOCs for?

Back 112

1. Borellia burgdorferi
2. Ricketssiae

Imagine: "Tet attack on boris yeltsin with a racket"

Front 113

Tetracyclines: other uses?

Back 113

1. Atypicals(superseeded by macrolides)
2. H.pylori
3. Borellia burgdorferi(DOC)
4. Ricketssia(DOC)

Front 114

Tetracycline used in prostatitis?

Back 114

Doxycycline


(doXXycycline for prostatitis)

Front 115

Tetracycline used in meningococcal carrier state?

Back 115

Minocycline
(MINocycline used in MENingitis or MINd/brain/CNS infection)

Why?

Hint 115

Since minocycline attains high concentration in saliva and tears

Front 116

Tetracycline used in SIADH?

Back 116

Demeclocycline

MOA?

Hint 116

Blocks ADH receptor functions in distal tubule

Front 117

Tetracycline used in soft tissue infetions/intestinal infections/resistant infections?

Back 117

Tigecycline

Front 118

Tetracycline used in gingivitis?

Back 118

Minocycline

Front 119

Tetracycline elimination?

Back 119

Through kidneys except ____?

Hint 119

Demeclocycline
(eliminated via liver)

Front 120

Tetracycline safe in renal impariment?

Back 120

Demeclocycline

(eliminated through liver)

Front 121

Tetracycline: pharmacokinetics?

Back 121

Chelation reduces absorption-
Divalent cations
1. Ca
2. Mg
3. Fe

therefore should not be taken with foods-
dairy products etc

Front 122

Tetracyclines: Advere effects?

Back 122

1. Tooth-enamel dysplasia
2. Reduced bone growth
3. GI distress
4. Liver dysfunction
5. Vestibular dysfunction

Front 123

Why are tetracyclines C/I in pregnancy?

Back 123

D/T liver dysfunction

Front 124

Macrolides: DOCs for?

Back 124

1. Atypicals- Chlamydia, Mycoplasma, Ureoplasma,
2. MAC
3. Legionella pneumophilia
4. H.pylori: Clarithromycin

Front 125

Macrolides : Other microbes covered?

Back 125

Gram +ves except ___?

Hint 125

MRSA

Front 126

Macrolides: Side effects?

Back 126

1. GI distress
2. Reversible deafness at high doses

Front 127

Macrolides: GI distress due to?

Back 127

Stimulation of motilin receptors

Front 128

Macrolides more commonly associated with GI distress?

Back 128

1. Erythromycin
2. Azithromycin

(You "thro" up with aziTHRO and eryTHROmycins)

Front 129

Ketolide?
Use?

Back 129

1. Telithromycin
2. Used in macrolide resistant S.pneumonia

Front 130

Clindamycin : MOA?

Back 130

Same as macrolide
Prevents translocation

Front 131

Clindamycin: spectrum of activity?

Back 131

Gram +ve cocci
Anaerobes

Front 132

Is clindamycin effective against MRSA?

Back 132

Yes

Front 133

Clindamycin: one good use?

Back 133

Osteomyelitis: since it achieves good concentration in bone
(and effective against gram +ve cocci- stapj aureus- MCC of osteomyelitis)

Front 134

Clindamycin: Side effects?

Back 134

***Pseudomembranous colitis***

Front 135

MCC of pseudomembranous colitis? (which specific antimicrobial agent)

Back 135

Clindamycin

Front 136

Macrolide resistance?

Back 136

Bases of rRNA get methylated therefore macrolide fails to recognize the binding site.

(Macrolide resistance thru Methylation of bases)

Front 137

Drugs used in osteomyelitis?

Back 137

1. Staph aureus: clindamycin
2. Salmonella: Quinolones
3. Pseudomonas: Quinolones

(Salmonella in sickle cell anemia)
(Pseudomonas in diabetics and IV drug abusers)

Front 138

Macrolide safe in pregnancy?

Back 138

Azithromycin

(since its water soluble it does not cross the placental barrier)

Front 139

Chloramphenicol: MOA?

Back 139

Inhibits peptidyl transferase
(binds 50S)

Bacteriostatic

Front 140

Chloramphenicol: Use?

Back 140

Back up drug for -
1. S.typhi
2. B.fragilis
3. Ricketssia

Front 141

Chloramphenicol: pharmacokinetics?

Back 141

Metabolized by hepatic glucoronidation
therefore dose reduction required in liver dysfunction

***Inhibition of P450***

Front 142

Chloramphenicol:
Adverse effects?

Back 142

1. Gray baby syndrome
2. BM suppression (aplastic anemia)
3. Kernicterus (displaces bilirubin from binding site)-- therefore C/i in children

Front 143

Grey baby syndrome?

Back 143

Observed as an adverse effect of chloramphenicol toxicity in neonates

Reason?

Hint 143

Chloramphenicol metabolized by glucoronidation in liver.
In neonates the glucoronyl transferase enzyme is relatively deficient-->excess chloramphenicol

Front 144

Linezolid: MOA?

Back 144

Inhibits formation of initiation complex (prevents formation of N-formymethionine-tRNA-mRNA complex)

Front 145

Linezolid: use?
Adverse effects?

Back 145

Use:
1. VRSA
2. VRE
3. Drug resistant pneumococci

Adverse effects:
1. Bone marrow suppression- platelets--> bleeding problems

Front 146

Antimicrobials associated with BM toxicity?

Back 146

1. Tetracyclines
2. Choramphenicol
3. Linezolid(plateles)
4. Trimethoprim
5. Pyrimethamine

Front 147

Quinupristine/Dalfopristine: MOA?

Back 147

1. Similar to tetracycline
2. Prevent interaction between amino-acyl tRNA with acceptor site
3. Stimulate 50S(?) dissociation from tertiary complex

Front 148

Quinupristine/Dalfopristine: Use?

Back 148

Used together parenterally in rx of:
1. VRSA
2. VRE

Front 149

Quinupristine/Dalfopristine: Side effects?

Back 149

Unknown(?)

Front 150

Folic acid synthesis inhibitors?

Back 150

1. Sulfonamides
2. Trimethoprim
3. Pyrimethamine
4. Methotrexate

Front 151

Sulfonamides inhibit _____ enzyme?

Back 151

Dihydropteroate synthetase

Front 152

DHF reductase inhibited by?

Back 152

1. Trimethoprim
2. Pyrimethamine
3. Methotrexate

Front 153

Sulfonamides always used in combinations: why?

Back 153

Because of multiple resistance

Front 154

When are sulfonamides used in combinations?

Back 154

1. Sulfasalazine: Ulcerative colitis and RA
2. Ag-sulfadiazine: burns

Front 155

Sulfasalazine: MOA?

Back 155

sulfasalazine--colonic bacteriae-->
5-ASA(ulcerative colitis)
sulfapyridine(RA)

Front 156

Uses of trimethoprim-sulfamethoxazole:
DOC for?
others?

Back 156

DOC:
1. Nocardia
2. P.Jirovecci prophylaxis
3. Toxoplasma gondii
4. Back up for listeria

Others:
Gram -ve: Ecoli, salmonella, shigella, H.influenza
Gram +ve: staph (including MRSA)

Front 157

Sulfonamides: pharmacokinetics?

Back 157

Hepatically acetylated
Renally excreted
High protein binding--> kernicterus

Front 158

Kernicterus causing antimicrobial drugs?

Back 158

1. Chloramphenicol
2. TMP/SMX

Front 159

MRSA effective antimicrobials?

Back 159

1. Vancomycin
2. Clindamycin
3. TMP/SMX

Front 160

Sulfonamides: toxicity?

Back 160

1. SJS
2. Hemolysis in G6PD deficiency
3. Phototoxicity
4. BM suppression

Front 161

Pneumocystis jirovecci: Drugs used?

Back 161

1. Cotrimoxazole
2. Pentamidine
3. Atovaquone

Front 162

Nucleic acid synthesis inhibitors?

Back 162

Fluroquinolones

Front 163

Fluoroquinolones: MOA?
cidal/static?

Back 163

1. Inhibition of DNA gyrase/Topoisomerase II
2. Inhibition of Topoisomerase IV


FQs are cidal

Topoisomerase IV: function?

Hint 163

Prevents sister chromatids from twisting and recombining

Front 164

Fluoroquinolones used in?

Back 164

1. UTIs- cotri resistant strains
2. STDs-chlamyida gonorrhea
3. PIDs
4. Gram -ve infections
5. Diarrhea(shigella salmonella)
6. Soft tissue infections
7. Drug-resistant pneumococci

Front 165

Drug resistant pneumococci?

Back 165

1. Fluoroquinolone (levofloxacin)
2. Telethromycin

Front 166

Soft tissue infections: drugs used?

Back 166

1. Tigecycline
2. Fluoroquinolones

(soFT tissure infections- fluoroquinolones tigecycline

Front 167

Fluoroquinolones: elimination?

Back 167

Eliminated thru active secretion in kidney
(avoid probenicid)
(Dose reduction in renal failure)

Front 168

Fluoroquinolones: side effects?

Back 168

1. Tendon rupture
2. Phototoxicity
3. Headache/insomnia/dizziness
4. Inhibition of chondrogenesis
5. Prolongation of QT interval
6. Seizures

(tendonitis, phototoxicity
chodrogenesis, QT increase, seizures)

Front 169

Drugs whose absorption gets limited due to divalent cations (Fe, Ca)

Back 169

1. Tetracycline
2. Fluoroquinolones

Front 170

Metronidazole:
MOA?
Cidal/static?

Back 170

Unknown
production of free radicals

Cidal

Front 171

Metronidazole is effective against _____(aerobes/anaerobes) ?

Back 171

anaerobes

Front 172

Metronidazile effective against ____(gram +ve/-ve)

Back 172

gram -ve
Effective against which gram +ve?

Hint 172

Clostridium

Front 173

Metronidazole DOC for?

Back 173

Clostridium difficile
(Pseudomembranous colitis)

Front 174

Metrinodazole: Side effects?

Back 174

1. Metallic taste(d/t gingivitis)
2. Disulfiram effect

Front 175

A/tb drugs: Name em?

Back 175

1. Isoniazid
2. Rifampin
3. Ethambutol
4. Pyrazinamide
5. Streptomycin

Front 176

Isoniazid
MOA?
Resistance?

Back 176

Inhibits mycolic acid synthesis (cell wall synthesis)

Resistance by: Deletions in Kat gene(catalase gene)--> no catalase production ---> no more conversion of isoniazid to active form

Front 177

Isoniazid: side effects?

Back 177

1. Hepatitis(elevated AST and ALT)
2. Peripheral neuritis
3. Sideroblastic anemia
4. SLE(in slow acetylators)

Front 178

Rifampin: MOA?

Back 178

Inhibition of DNA dependent RNA polymerase
(Nucleic acid synthesis inhibitor)

Front 179

Rifampin: Side effects?

Back 179

1. Red orange urine/saliva
2. Hepatitis
3. Induction of P450

Front 180

Ethambutol: MOA?

Back 180

Inhibition of arabinogalactan synthesis(cell wall component)

Front 181

A/tb drug requiring conversion by catalase? (prodrug)

Back 181

Isoniazid

Front 182

Ethambutol: Side effects?

Back 182

1. Dose dependent retrobulbar neuritis
2. Decreased visual acuity
(red-green discrimination)

Front 183

Pyrizinamide: MOA?

Back 183

Unknown

Front 184

Pyrizinamide: side effects?

Back 184

1. Hepatitis
2. Hyperuricemia

Front 185

Streptomycin: MOA?

Back 185

AG: initiation complex formation inhibition
misreading of genetic code

Front 186

Streptomycin: adverse effects?

Back 186

1. Vestibular toxicity
2. Deafness
3. Nephrotoxicity
4. NM blockade

Front 187

A/tb drug associated with hepatitis?

Back 187

1. Isoniazid
2. Rifampin
3. Pyrizinamide

Front 188

A/tb drug which is a prodrug?

Back 188

Isoniazid

Front 189

A/tb drug which is associated with:
1. Retrobulbar neuritis
2. Red-orange metabolites
3. Hyperuricemia
4. Peripheral neuritis
5. Deafness
6. Sideroblastic anemia
7. Induction of P450

Back 189

1. Retrobulbar neuritis: Ethambutol
2. Red orange metabs: Rifampin
3.Hyperuricemia: Pyrizinamide
4. Peripheral neuritis: Isoniazid
5. Deafness: Streptomycin
6. Sideroblastic anemia: Isoniazid
7. Induction of P450: Rifampin

Front 190

Isoniazid prophylaxis offered to which patient population
?

Back 190

1. Young children on exposure even if TST negative
2. TST conversion in past 2 years
3. Tuberculin reactors with high risk (diabetes/HIV/leukemia/prolonged glucocorticoid)

Front 191

Amphotericin B: MOA

Back 191

Interaction with cell membrane--->Pore formation(polyene)

Front 192

Amphotericin B: Spectrum of activity/DOC for?

Back 192

Wide spectrum: DOC for- 1.Aspergillus 2.Candida 3.Cryptococcus 4. Histoplasma 5.Mucor

Front 193

Polyenes: Name em?

Back 193

Amphotericin B
Nystatin

Front 194

Nystatin: MOA?

Back 194

Polyene: "interact with fungal cell membrane" ---> "pore" formation altering membrane permeability

Front 195

Amphotericin B: MOA

Back 195

Interaction with cell membrane--->Pore formation(polyene)
“Polyenes produce Pores in membranes”

Front 196

Amphotericin B: Spectrum of activity/DOC for?

Back 196

Wide spectrum: DOC for-
1.Aspergillus
2.Candida
3.Cryptococcus
4. Histoplasma
5.Mucor
6. Sporothrix

Front 197

Amphotericin B: MOA has synergistic action with _____?

Back 197

Flucytosine in _____ and _____ fungal infections

Hint 197

1. Candida
2. Cryptococcus

Front 198

Nystatin : Uses?

Back 198

Used in topical infections only

Why cannot it be used systemically?

Hint 198

Because of its high toxicity- cannot be used systemically

Front 199

Amphotericin B : Pharmacokinetics? (unique)

Back 199

1. Given IV(poor absorption)
2. Poor CNS penetration
3. Can be administered intra-thecally
4. Slow clearance- long T1/2

Front 200

Amphotericin B: Side effects?

Back 200

1. Fever/chills
2. Hypotension (d/t histamine)
3. Nephrotoxicity(dose dependent)
4. Anemia (due to less erythropoetin)
5. Renal tubular acidosis and hyperkalemia(nephrotoxicity)

Precautions to observed

Front 201

Azoles: MOA?

Back 201

Inhibition of P-450 enzyme 14-alpha-demethylase
Function of 14-alpha-demethylase: function?

Hint 201

Converts lanosterole-->erogsterole

Front 202

Azoles: Resistance development?

Back 202

Decreased intracellular accumulation of azoles (Formation of pumps)

Front 203

DOC for paracocidioides?

Back 203

Ketoconazole

Other uses of ketoconazole?

Hint 203

Other uses:
1. Back up for histoplasma
2. Mucocutaneous candidiasis
3. Dermatophytoses
4. Back up for blastomyces

Front 204

DOC for:
1. Sporotrichoses
2. Aspergillosis
3. Paracoccidioides
4. Histoplasmosis
5. Candida(systemic)
6. Candida(mucocutaneous)
7. Blastomycosis
8. Cryptococcosis
9. Aspergillosis
10. Mucor
11. Coccidiodomycosis
12. Candida(topical)
13. Meningeal fungal (any)
14. Used in combination with amphotericin B
15. Esophageal candidiasis?

Back 204

1. Sporotrichosis: Itraconazole/Voriconazole
2. Aspergillosis: Itraconazole/Voriconazole
3. Paracoccidioides: Ketoconazole
4. Histoplasmosis: Amphotericin B
5. Candida (systemic): Amphotericin B
6. Candida (muco-cutaneous): Flucanazole
7. Blastomycosis:Itraconazole/voriconazole
8. Cryptococcosis: Amphotericin B
9. Aspergillosis: Itraconazole/voriconazole
10. Mucor: Amphotericin B
11. Coccidiodomycosis: Flucanazole
12. Candida (topical): Clotrimazole/nicomazole
13. Meningeal fungal(any): Flucanazole
14. Used in combination with amphotericin B: Flucytosine
15. Esophageal candidiasis: Flucanazole

Front 205

Flucanazole: DOC for?

Back 205

1. Esophageal candidiasis
2. Invasive candidiasis
3. Coccidiodomycosis
4. Fungal meningitis (cryptococcal)

Front 206

Itraconazole/Voriconaxole: DOC for?

Back 206

1. Blastomycosis
2. Sporotrichosis
3. Aspergillosis

(Imagine casper near a volcanic blast from the spore crater)

Front 207

Azoles used topically?

Back 207

1. Clotrimazole
2. Miconazole

Front 208

Azoles that penetrate CNS?

Back 208

Only flucanazole

Front 209

Absorption of ketoconazole is interfered by ____?

Back 209

Antacids

Front 210

Azole whose absorption is increased by food?

Back 210

Itraconazole

Front 211

Azoles metabolized by liver enzymes?

Back 211

Ketoconazole and itraconazole

Front 212

Azole that is eliminated from liver in an unchanged form?

Back 212

Flucanazole

Front 213

Azoles: side effects?

Back 213

I. Decreased synthesis of steroids(cortisol/testorsterone)-->
1. Decreased libido
2. Gynecomastia
3. Menstrual abnormality

II. Hepatotoxicity: Increased LFTs

Front 214

Flucytosine: the 2 MOAs?

Back 214

1. Formation of 5-FU--(triphosphorylation)--->incorporated into fungal RNA
2. 5-FU---->5-fd-UMP (inhibits thymidylate synthase)--->decreased thymine

Front 215

Flucytosine always used in combination with ______?

Back 215

Amphotericin B

Why?

Hint 215

Due to rapid development of resistance

Front 216

Flucytosine and amphotericin B combination used in _____ and _____fungal infections

Back 216

Cryptococcal and Candidal

Front 217

Flucytosine: side effects?

Back 217

Bone marrow toxicity

Front 218

Griseofulvin: MOA?

Back 218

Disrupts microtubule structures of _____?

Hint 218

Dermatophytes

Front 219

Griseofulvin attains maximum concentration in _____(body part/structure)

Back 219

Keratin

Front 220

Griseofulvin: side effect?

Back 220

Disulfiram like reaction

Front 221

Terbanafine: MOA?

Back 221

Inhibits squalene epoxide ---> decreased ergosterole synthesis
(cell wall synthesisn inhibitor)

Front 222

Terbanafine: Side effects?

Back 222

1. GI distress
2. Hepatotoxicity (increased LFT)

Front 223

Caspofungin/Micafungin: MOA?

Back 223

Inhibit glucan synthesis needed in cell wall synthesis

Front 224

Caspofungin/Micafungin: Uses?

Back 224

1. Invasive candidiasis
2. Aspergillosis

Front 225

Caspofungin/Micafungin: Side effects?

Back 225

1. GI distress
2. Flushing

Front 226

Antivirals that inhibit viral penetration?

Back 226

1. Enfuvirtide
2. Maraviroc
3. Amantadine

Front 227

Antivirals that inhibit uncoating?

Back 227

Amantadine

Front 228

Antivirals that inhibit DNA-polymerase?

Back 228

1. Acyclovir
2. Foscarnet
3. Ganciclovir

Front 229

Antivirals that inhibit RNA-polymerase?

Back 229

1.Foscarnet
2. Ribavarin

Front 230

Antivirals that inhibit viral reverse trascriptase?

Back 230

1. Zidovudine
2. Didanosine
3. Zalcitabine
4. Lamivudine
5. Stavudine
6. Lamivudine
7. Nevirapine
8. Efavirenz

Front 231

Antivirals that inhibit aspartate protease?

Back 231

1. Indinavir
2. Ritanavir
3. Saquinavir
4. Nelfinavir

Front 232

Antivirals that inhibit neuraminidase?

Back 232

1. Zanamavir
2. Oseltamavir

Front 233

Acyclovir: MOA?

Back 233

1. Monophosphorylated by viral thymidine kinase-->bioactivated by host cell kinase--->triphosphate-->incorporated into DNA-->chain termination (since it lacks 3'hydroxyl group)
2. Acyclovir directly inhibits viral DNA polymerase

Front 234

Acyclovir: Resistance?

Back 234

1. Changes in DNA polymerase
2. Decreased/complete inactivity of thymidine kinase (TK-)

Front 235

Acyclovir: use/antiviral?

Back 235

1. HSV
2. VZV only

Front 236

Acyclovir: effect in HSV/VZV?

Back 236

1. Reduces viral shedding(genital herpes)
2. Reduces acute neuritis in shingles
3. Reduces symptoms in chicken pox
4. Prophylactic in immunocompromised patients

Front 237

Acyclovir is ineffective against ______?(herpes condition/symptom)

Back 237

Post herpetic neuralgia

Front 238

Acyclovir: Side effects?

Back 238

1. Crystalluria
2. Neurotoxicity (headache, confusion, seizures)

Front 239

Crystalluria observed as acyclovir side effect can be minimized by?

Back 239

Maintaining hydration

Front 240

Is acyclovir hematotoxic?

Back 240

No

Front 241

Antivirals with DNA-polymerase activity that are used in acyclovir resistant cases?

Back 241

1. Foscarnet
2. Valacyclovir

Front 242

Foscarnet and valacyclovir can be used in TK-ve strains: true/false?

Back 242

FALSE

Front 243

Foscarnet and valacyclovir: pharmacologoc advantage over acyclovir?

Back 243

Have a longer T1/2

Front 244

Ganciclovir: MOA?

Back 244

1. First step: phophorylation by Thymdine kinase/UL-97----> activated form--->incorporated into DNA--->termination
2. Activated gancyclovir inhibits DNA polymerase directly

Front 245

Ganciclovir: Resistance?

Back 245

1. Change in DNA polymerase
2. TK-ve strains

Front 246

Ganciclovir: Side effects?

Back 246

1. Hematotoxicity(leukopenia/thrombocytopenia)
2. Crystalluria
3. Mucositis
4. Fever
5. Rash
6. Siezures in overdose

Front 247

Foscarnet: MOA?

Back 247

Inhibits DNA and RNA polymerase

Front 248

Antiviral used in prophylaxis and rx of CMV infections?

Back 248

Ganciclovir (CMV retinitis in AIDS and transplant patients)

Front 249

Ganciclovir: Uses?

Back 249

1. HSV
2. VZV
3. CMV

Front 250

Foscarnet: Side effect?

Back 250

1. Nephrotoxicity: ATN
2. Hypocalcemia: tetany
3. Seizures(hypocalcemia)

Front 251

Foscarnet should be avoided with _____ drug

Back 251

IV pentamidine

Why?

Hint 251

To avoid life threatening nephrotoxicity and hypocalcemia

Front 252

NRTIs?

Back 252

Nucleoside reverse transcriptase inhibitors:
1. NNRTI
2. NRTI

Front 253

Antiviral drug that is not an antimetabolite?

Back 253

Foscarnet

Front 254

NRTIs: MOA?

Back 254

Activated by nonspecific phosphorylation---> competes with natural nucleotides---> incorporated into DNA---> termination
2. Activated/phosphorylated compound inhibits reverse trancriptase

Front 255

NRTIs: Name em

Back 255

1. Zidovudine 2. Didanosine 3. Zalcitabine 4. Lamivudine 5. Stavudine 6. Lamivudine 7. Nevirapine 8. Efavirenz

Front 256

NRTIs: Resistance?

Back 256

Occurs due to mutation in gene that encodes for reverse trancriptase

Front 257

NRTI associated with:
1. Myopathy
2. Peripheral neuropathy
3. Pancreatitis
4. Hematotoxicity
5. GI distress
6. Liver dusfunction
7. Neutropenia?

Back 257

1. Myopathy: Zidovudine
2. Peripheral neuropathy: Zidovudine, Zalcitabine, Didanosine, Stavudine
3. Pancreatitis: Zalcitabine, Didanosine
4. Hematotoxicity: Zidovudine
5. GI distress: Lamivudine, Zalcitabine
6. Liver dysfunction: Didanosine
7. Neutropenia: Lamivudine, Zalcitabine

Front 258

Least toxic of all NRTIs?

Back 258

Lamivudine

Front 259

Protease inhibitors: MOA?

Back 259

Inhibit aspartate protease (required for cleaving pre-proteins into proteins of mature virus

Front 260

Protease inhibitors: resistance?

Back 260

Mutation in pol gene

Front 261

Is cross resistance observed amongst protease inhibitors?

Back 261

NO cross resistance between protease inhibitors

Front 262

Is cross resistance observed amongst NRTIs?

Back 262

NO cross resistance between NRTIs

Front 263

Protease inhibitors: Name em?

Back 263

1. Indinavir 2. Ritanavir 3. Saquinavir 4. Nelfinavir

Front 264

2 protease inhibitors always used in combination?

Back 264

Indinavir and ritanavir

Why?

Hint 264

To avoid resistance

Front 265

NRTI combinations to be avoided? Why?

Back 265

1. Didanosine + Zalcitabine(additive toxicity- pancreatitis)
2. Zidovudine + Stavudine(competition for activation)

Front 266

Least toxic of all protease inhibitors?

Back 266

Saquinavir

Front 267

Protease inhibitor associated with crystalluria?

Back 267

Indinavir

Front 268

Ritonavir: side effect?

Back 268

Induction of CYPA12. Inhibition of all other P450 enzymes

Front 269

Protease inhibitors: side effect in general?

Back 269

Lipid and carb metab disorder-->obesity, insulin resistance

Front 270

Antiviral that inhibits integrase enzyme (HIV)?

Back 270

Raltegravir

Front 271

Enfuvirtide: MOA?

Back 271

Fusion inhibitor: binds to gp41

Front 272

Maraviroc: MOA?

Back 272

Inhibition of CCR-5 protein

Location of CCR-5 protein?

Hint 272

CD4+ T cell

Front 273

Amantadine: MOA?

Back 273

Prevents attachment, penetration and uncoating of infuenza A virus

Front 274

Amantadine: side effects?

Back 274

1. Insomnia
2. Seizures
3. Nervousness
4. Livedo reticularis
5. Atropine like side effects

Front 275

Amantadine: Uses?

Back 275

Mainly for prophylaxis purposes

Front 276

Zanamavir/oseltamavir: MOA?

Back 276

Inhibit neuraminidase

Neuraminidase : function?

Hint 276

Prevent clumping of virus particles so that more may be available for infection

Front 277

Neuraminidase inhibitors: name em?

Back 277

Zanamavir/oseltamivir

Front 278

Neuraminidase inhibitors: uses?

Back 278

Used for prophylaxis

Front 279

Ribavarin: MOA?

Back 279

1. Monophosphorylated form inhibits IMP dehydrogenase
2. Triphosphate inhibits RNA polymerase and end capping of viral RNA

Front 280

Ribavarin: Clinical uses?

Back 280

1. Hepatitis C (Adjunct to alpha interferon)
2. RSV
3. Lassa fever
4. Hanta virus

Front 281

Ribavarin: side effects?

Back 281

1. Hemotoxic
2. Teratogenic

Front 282

Interferon used in
1. Chronic granulomatous disease
2. Multiple sclerosis
3. Hepatitis?

Back 282

1. CGD: IFN-gamma
2. MS: IFN-beta
3. Hepatitis: IFN-alpha

Front 283

Uses of alpha IFN?

Back 283

1. Hepatitis
2. Multiple myeloma
3. Renal cell carcinoma
4. Kaposi's sarcoma
5. Chronic myelogenous leukemia

Front 284

antiretroviral combinations used in:
1. HIV prophylaxis for needle stick injury
2. HIV prophylaxis for high risk exposure
3. HIV in pregnancy
4. Intrapartum
5. During delivery?

Back 284

1. Zidovudine+Lamivudine
2. Zidovudine+Lamivudine+Indinavir
3. ZDV full dose in 2nd and 3rd trimester
4. Zidovudine
5. Nevirapine

Front 285

DOC for:
1. Amebiasis
2. Giardiasis
3. Trichomoniasis
4. Toxoplasmosis
5. Leishmaniasis
6. Trypanosomiasis

Back 285

1. Amebiasis: Metronidazole
2. Giardiasis: Metronidazole
3. Trichomoniasis: Metronidazole
4. Toxoplasmosis: Pyrimethamine + sulfadiazine
5. Leishmaniasis: Stibogluconate
6. Trypanosomiasis: Nifurtimox
african: arsenic componds

Front 286

Antimalarials: Chloroquine sensitive: prophylaxis:

Back 286

Chloroquine + primaquine

Front 287

Antimalarials: Back up drugs?

Back 287

1. Hydroxychloroquine
2. Primaquine
3. Pyrimethamine-sulfadoxine

Front 288

DOC for:
1. P.falciparum
2. P.malaraie
3. P.vivax
4. P. ovale

Back 288

1. P.falciparum: Chloroquine
2. P.malariae: Chloroquine
3. P.vivax: Chloroquine + Primaquine
4. P.ovale: Chloroquine + Primaquine

Front 289

Antimalarials: side effects?

Back 289

Hemolysis in G6PD deficiency
Cinchonism with quinine

Front 290

Mebendazole: MOA?

Back 290

1. Decreased glucose uptake
2. Distorts microtubule structure

Front 291

Antimicrobials that distort microtubule structure?

Back 291

1. Mebendazole
2. Griseofulvin

Front 292

Mebendazole: uses?

Back 292

For intestinal nematodes

Front 293

Praziquantel: MOA?

Back 293

1. Increases Ca influx
2. Increases vacuolization

Front 294

Praziquantel: Use?

Back 294

Most cestodes and trematodes