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294 Cards in this Set

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Antimicrobials: Combinations used(general)?
Additive (1+1=2)
Synergist (1+1>2)
Antagonist (1+1<2)
Antimicrobial combination: Synergistic combinations?
Synergistic combination=
(Cidal + Cidal)
Antimicrobial combination: Antagonistic combinations?
Penicillins + Tetracyclins
(Cidal+ Static)
Cidal + Static drugs ____(should/should not) be combined
Should not

Bacterial cell wall synthesis inhibitors: Name the drugs/drug classes?
1. Penicillins
2. Cephalosporins
3. Imipenem
4. Meropenem
5. Aztreonam
6. Vancomycin
Bacterial protein synthesis inhibitors: Name the drugs/drug classes?
1. Aminoglycosides
2. Chloramphenicol
3. Macrolides
4. Tetracyclines
5. Streptogramins
6. Linezolid

Bacterial nucleic acid synthesis inhibitors: Name the drug/drug classes?
1. Fluoroquinolones
2. Rifampin
Bacterial folic acid synthesis inhibitors: Name the drug/drug classes?
1. Sulfonamides
2. Trimethoprim
3. Pyrimethamine
Mechanism of resistance against penicillin and cephalosporins?
1. Beta lactamases production
2. Change in PBP structure
3. Change in porins
Mechanism of resistance against aminoglycosides?
Formation of enzymes that inactivate the drug through the process of ______ via
1. _____
2. _____
3. _____
Through the process of "conjugation" via:
1. Acetylation
2. Adenylylation
3. Phosphorylation
Mechanism of resistance against Macrolides?
1. Methyltransferase formation--> Alters binding site on 50S ribosomal subunit
2. Active transport out of the cell
Mechanism of resistance against Tetracyclines?
Increased P-glycoprotein pump that pumps drugs out of the cell
Mechanism of resistance against Sulfonamides?
1. Altered enzyme sensitivity to action of binding drug
2. Use of exogenous folic acid
3. Increased formation of PABA
Mechanism of resistance against Fluoroquinolones?
1. Altered enzyme sensitivity to action of binding drug
2. Increased activity of transport system to promote drug efflux
All bacterial cell wall synthesis inhibitors are _____ (bactericidal/bacteriostatic)?
Penicillins: MOA?
1. Bind to PBP
2. Inhibition transpeptidation -->
3. Inhibition of cross-linking
Microbes associated with:
1. Penicllinase activity?
2. PBP structure alteration?
3. Porin structure alteration?
1. Penicillinase: Staph
2. PBP alteration: Pneumococci, MRSA
3. Porins: Pseudomonas
Narrow spectrum b-lactamase sensitive group of penicillin drugs: Name em.
1. Penicillin G
2. Penicillin V
Narrow spectrum b-lactamase sensitive group of penicillin drugs: Spectrum of activity?
2. Streptococci
3. Pneumococci
4. Meningococci
Narrow spectrum b-lactamase resistant group of penicillin drugs: Name em.
1. Methicillin
2. Nafcillin
3. Oxacillin
4. Cloxacillin
Broad spectrum b-lactamase sensitive group of penicillin drugs: Name em.
1. Amoxicillin
2. Ampicillin
Broad spectrum b-lactamase sensitive group of penicillin drugs:
Spectrum of activity?
1. All gram +ves(except staph)
2. E-coli
3. H.influenza
4. Listeria monocytogenes
5. Borellia burgdorferi
6. H.pylori
Ampicillin/amoxicillin not effective against _____ (gram +ve cocci)
Listeria monocytogenes: DOC- ____(Ampicillin/amoxicillin)

"LASER- listeria amplification"
H.Pylori: DOC-
Borellia burgdorferi: DOC- ____(Ampicillin/amoxicillin)
Extended spectrum b-lactamase sensitive group of penicillin drugs
1. Ticarcillin
2. Piperacillin
3. Azlocillin
4. Carbenicillin

Extended spectrum activity against?
Suicide inhibitors:
Name em.
Clavulanic acid

MOA: Irreversibly inhibits b-lactamase
Penicillin group of drugs- synergy observed with?
Penicillins -mechanism of elimination?
Active tubular secretion in kidney

Renal excretion implies dose reduction in renal failure

1. Nafcillin
2. Oxacillin

(Nafcillin Oxacillin: NO are NOT excreted through kidneys.
Mechanism of elimination of Nafcollin and Oxacillin?
Through bile

Nafcillin and Oxacillin cannot be used in liver dysfunction
Penicillin available in repository form?
Benzathine penicilline G
Penicillin with long half life?
Benzathine penicillin

T1/2: 2 weeks
Penicillin hypersenstivity: type?
ALL types

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
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
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
Penicillins: Adverse reactions?
1. Hypersensitivity reactions (I thru IV)
2. Interstitial nephritis
3. NVD
4. Jarisch-Herxheimer reaction
Interstitial nephritis commonly observed with which penicillin?
Jarisch herxheimer reaction commonly observed with which penicillin?
In rx with penicillin for syphilis
GI distress commonly observed with which penicillin?

Ampicillin is poorly absorbed in the gut
Jarisch Herxheimer reaction?
Observed in treatment of syphilis: Immune response observed after destruction of t.pallidum and release of antigens

1. Fever
2. Swelling
3. Joint pain
Very long acting penicillin?
Benzathine penicillin

How is it adminstered (what form)?
1. IM- thick suspension slow release
(Slow release)

"BenzaThick penicillin- thick slow release suspension"--> Long t1/2
Cephalosporin: MOA?
1. Bind to PBP
2. Inhibition transpeptidation -->
3. Inhibition of cross-linking
First generation cephalosporin: Name em?
1. Cefazolin
2. Cephalexin

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

Spectrum of activity?
1. Gram +ve COCCI
2. Ecoli
3. Kliebsella
4. Proteus

Evade the Problematic Fight Klub
Cephalosporin generation I: unique pharmacokinetic property?
Do not enter the CNS
Cephalosporin generation I:
In surgical prophylaxis (due to its broad spectrum of activity)
Cephalosporin generation II: Name em?

increased -ve coverage
Cephalosporin generation II drug that crosses the BBB?
Cephalosporin generation III: Name em?
1. Cephtriaxone
2. Cephotaxime
3. Cephoperazone
4. Cefdinir

"Tried tax per dinar"
Cephalosporin: elimination?
All eliminated through active tubular secretion via kidneys except
1. Ceftriaxone
2. Cefoperazone

Eliminated in bile
Cephalosporins: Side effects?
1. Hypersensitivity reactions etc
same as penicillins

2. Disulfiram like effects observed with
1. Cefotetan
2. Cefoperazone
Drug fever _____common/uncommon with cepahlosporins?
Cephalosporin generation III: drug that does not cross the BBB?
Cpehalosporin generation III: Use?
Empiric management of:
1. Meningitis
2. Sepsis
Cephalosporin generation IV: properties?
1. Wide spectrum
2. B-lactamase resistant
3. Crosses BBB
Organisms not covered by cephalosporins?
Imipenem/meropenem: MOA?
Similar to penicillin
Imepenem and meropenem are beta-lactamase _____sensitive/resistant?
Imepenem/meropenem: spectrum of activity?
1. Effective against all microbes
2. Gram +ve cocci
3. Gram -ve rods
4. Anaerobes
Imepenem/meropenem: use?
In severe life-threatening infections
Imipenem is always administered with ____?

Cilastin inhibits renal de-hydrpeptidase(breaks down imepenem-->nephrotoxic compound)
1. Increases half life of imepenem
2. Also prevents nephrotoxicity
Drugs used in empiric Rx of life threatening sepsis/meningitis?
1. IIIrd generation cephalosporins
2. Imipenem/Meropenem
Imipenem/meropenem: elimination?
Through the kidney
Imepenem/meropenem: adverse effects?
1. GI distress
2. Drug fever
3. CNS effects- (seizures with imipenem)
Aztreonam : MOA?
Same as penicillins
Penicillin/related drugs resistant to beta-lactamase
1. Nafcillin/cloxacillin/oxacillin/Methicillin
2. Cefapime(IV generation cephalosporin)
3. Imepenem/meropenem
4. Aztreonam
Penicillin/cephalosporin/related drugs cleared through bile?
1. Nafcillin
2. Oxacillin
3. Ceftriaxone
4. Cefoperazone
Penicillin/cephalosprin/related drugs safe in renal impairment?
1. Nafcillin
2. Oxacillin
3. Ceftriaxone
4. Cefoperazone
Cephalosporins that do not have CNS entry?
1. Ist generation cephalosporins
2. IInd generation cephalosporins (except cefuroxime)
3. Cefoperazone
Cephalosporins used in empirical treatment of meningitis/sepsis?
IIIrd generation cephalosporin
Wide spectrum cephalosporin?

Mode of administration?
IIIrd generation cephalosporins: modes of administration of each drug?
1. Ceftriaxone: IM
2. Cefotaxime: Parenteral
3. Cefoperazone: ?
4. Cefdinir: Oral
5. Cefixim: Oral
Cephalosporins used for surgical prophylaxis?
Ist generation
Cell wall synthesis inhibitor associated with seizures?

Also associated with?
Cell wall synthesis inhibitor active mainly against gram -ve rods?
Cell wall synthesis inhibitor that has no cross-reactions with penicillins therefore can be used in patients with hypersensitivity to penicillins?
Aztreonam: Mode of administration?
Vancomycin : MOA?
1. Binding to D-ALA D-ALA muramyl pentapeptide
2. Inhibits transglycosylation-->
3. Inhibition of peptidoglycan chains.
Vancomycin spectrum of activity?
2. Enterococci
3. Clostridium difficile
Pseudomembranous colitis: DOC?
#1 Metronidazole
#2 Vancomycin
Vancomycin resistance?
Change of D-ALA to D-Lactate

"D-luck shields"
Vancomycin: Administration?
Vancomycin ____(can/cannot) cross the BBB?
Vancomycin : elimination?
Through kidneys
Vancomycin: Side effects?
1. Red man syndrome
2. Ototoxicity
3. Nephrotoxicity

Red man syndrome?
Hypersensitivity type?
Red discoloration of skin due to flushing from histamine release

Type I hypersensitivity
Protein synthesis inhibitor associated with inhibition of initiation complex formation?
1. Aminoglycoside
2. Linezolid
Protein synthesis inhibitor associated with inteterference with t-rna attachment to A-site?
1. Tetracyclines
2. Dalfopristine
3. Quinopristine
Protein synthesis inhibitor associated with inhibition of peptidyl transferase enzyme(peptide bond formation?
Protein synthesis inhibitor associated with inhibition of translocation?
1. Macrolides
2. Clindamycin
Sites of attachment (50s or 30s) for:
1. Aminoglycosides
2. Tetracylines
3. Quinupristine
4. Linezolid
5. Dalfopristine
6. Chloramphenicol
7. Macrolides
8. Clindamycin
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"
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)?
Prevents binding of aminoacyl tRNA to acceptor site


Site of binding(30s/50s)?
1. Inhibits formation of peptide bond
2. Inhibits activity of peptidyltranserase


Site of binding(30s/50s)?
Inhibit translocation of peptidyl-tRNA from acceptor to donor site (-static)


Site of binding(30s/50s)?
Aminoglycosides: spectrum of activity?
Gram -ve rods

Aminoglycosides are effective/ineffective against anaerobes?
Ineffective against anaerobes

Since AG utilize O2 dependent pump for uptake by the bacteriae(only present in aerobes)
Absent in anaerobes therefore they are innately resistant
Aminoglycosides are DOCs for?
1. Tularemia
2. Bubonic plague

(Imagine: Rabbits and baboons eating protein-sugar)
Aminoglycosides are used synergistically for _____(organism/infection) with _____(antibiotic)
(2 organisms with 1 combo each)
Enterococci: PenicillinG + AG
Pseudomonas: Extended spectrum penicillin
Aminoglycosides: administration?
Only IV

Since they are sugars they are water soluble therefore not absorbed orally
Aminoglycosides: elimination?
Through kidneys
Aminoglycosides: Side effects?
1. Nephrotoxicity
2. Ototoxicity
3. Neuromuscular blockade
Aminoglycoside drug interaction in relation to nephrotoxicity?
1. Vancomycin
2. Cispatin
3. Amphotericin B
4. Cyclosporin
Aminoglycoside drug interaction in relation to ototoxicity?
1. Loop diuretics
Aminoglycoside: Ototoxicity?
1. Hair cell damage
2. Vestibular dysfunction
Aminoglycoside: dosing?
Once-daily dosing
Aminoglycoside: Nephrotoxicity?
1. Proteinuria
2. Hypokalemia
3. Acidosis
4. Acute tubular necrosis
Aminoglycoside : NM blockade?
1. Decreased release of ACh.
(Similar mechanism to botulinus toxin)

2. Enhance effect of skeletal muscle relaxants
Prevents attachment of t-RNA to A site.

Therefore prevent ELONGATION of proteins

Aminoglycosides : Name em?
1. Gentamicin
2. Tobramicin
3. Amikacin
4. Streptomycin
Aminoglycoside used topically?
Neomycin in preparation "neopsorin"
Aminoglycosides: resistance?
Production of conjugase enzyme--> faster elimination
Phototoxicity: Associated antibacterial drugs?
1. Tetracyclines
2. Sulfonamides
3. Fluoroquinolones
Tetracyclines: DOCs for?
1. Borellia burgdorferi
2. Ricketssiae

Imagine: "Tet attack on boris yeltsin with a racket"
Tetracyclines: other uses?
1. Atypicals(superseeded by macrolides)
2. H.pylori
3. Borellia burgdorferi(DOC)
4. Ricketssia(DOC)
Tetracycline used in prostatitis?

(doXXycycline for prostatitis)
Tetracycline used in meningococcal carrier state?
(MINocycline used in MENingitis or MINd/brain/CNS infection)

Since minocycline attains high concentration in saliva and tears
Tetracycline used in SIADH?

Blocks ADH receptor functions in distal tubule
Tetracycline used in soft tissue infetions/intestinal infections/resistant infections?
Tetracycline used in gingivitis?
Tetracycline elimination?
Through kidneys except ____?
(eliminated via liver)
Tetracycline safe in renal impariment?

(eliminated through liver)
Tetracycline: pharmacokinetics?
Chelation reduces absorption-
Divalent cations
1. Ca
2. Mg
3. Fe

therefore should not be taken with foods-
dairy products etc
Tetracyclines: Advere effects?
1. Tooth-enamel dysplasia
2. Reduced bone growth
3. GI distress
4. Liver dysfunction
5. Vestibular dysfunction
Why are tetracyclines C/I in pregnancy?
D/T liver dysfunction
Macrolides: DOCs for?
1. Atypicals- Chlamydia, Mycoplasma, Ureoplasma,
2. MAC
3. Legionella pneumophilia
4. H.pylori: Clarithromycin
Macrolides : Other microbes covered?
Gram +ves except ___?
Macrolides: Side effects?
1. GI distress
2. Reversible deafness at high doses
Macrolides: GI distress due to?
Stimulation of motilin receptors
Macrolides more commonly associated with GI distress?
1. Erythromycin
2. Azithromycin

(You "thro" up with aziTHRO and eryTHROmycins)
1. Telithromycin
2. Used in macrolide resistant S.pneumonia
Clindamycin : MOA?
Same as macrolide
Prevents translocation
Clindamycin: spectrum of activity?
Gram +ve cocci
Is clindamycin effective against MRSA?
Clindamycin: one good use?
Osteomyelitis: since it achieves good concentration in bone
(and effective against gram +ve cocci- stapj aureus- MCC of osteomyelitis)
Clindamycin: Side effects?
***Pseudomembranous colitis***
MCC of pseudomembranous colitis? (which specific antimicrobial agent)
Macrolide resistance?
Bases of rRNA get methylated therefore macrolide fails to recognize the binding site.

(Macrolide resistance thru Methylation of bases)
Drugs used in osteomyelitis?
1. Staph aureus: clindamycin
2. Salmonella: Quinolones
3. Pseudomonas: Quinolones

(Salmonella in sickle cell anemia)
(Pseudomonas in diabetics and IV drug abusers)
Macrolide safe in pregnancy?

(since its water soluble it does not cross the placental barrier)
Chloramphenicol: MOA?
Inhibits peptidyl transferase
(binds 50S)

Chloramphenicol: Use?
Back up drug for -
1. S.typhi
2. B.fragilis
3. Ricketssia
Chloramphenicol: pharmacokinetics?
Metabolized by hepatic glucoronidation
therefore dose reduction required in liver dysfunction

***Inhibition of P450***
Adverse effects?
1. Gray baby syndrome
2. BM suppression (aplastic anemia)
3. Kernicterus (displaces bilirubin from binding site)-- therefore C/i in children
Grey baby syndrome?
Observed as an adverse effect of chloramphenicol toxicity in neonates

Chloramphenicol metabolized by glucoronidation in liver.
In neonates the glucoronyl transferase enzyme is relatively deficient-->excess chloramphenicol
Linezolid: MOA?
Inhibits formation of initiation complex (prevents formation of N-formymethionine-tRNA-mRNA complex)
Linezolid: use?
Adverse effects?
2. VRE
3. Drug resistant pneumococci

Adverse effects:
1. Bone marrow suppression- platelets--> bleeding problems
Antimicrobials associated with BM toxicity?
1. Tetracyclines
2. Choramphenicol
3. Linezolid(plateles)
4. Trimethoprim
5. Pyrimethamine
Quinupristine/Dalfopristine: MOA?
1. Similar to tetracycline
2. Prevent interaction between amino-acyl tRNA with acceptor site
3. Stimulate 50S(?) dissociation from tertiary complex
Quinupristine/Dalfopristine: Use?
Used together parenterally in rx of:
2. VRE
Quinupristine/Dalfopristine: Side effects?
Folic acid synthesis inhibitors?
1. Sulfonamides
2. Trimethoprim
3. Pyrimethamine
4. Methotrexate
Sulfonamides inhibit _____ enzyme?
Dihydropteroate synthetase
DHF reductase inhibited by?
1. Trimethoprim
2. Pyrimethamine
3. Methotrexate
Sulfonamides always used in combinations: why?
Because of multiple resistance
When are sulfonamides used in combinations?
1. Sulfasalazine: Ulcerative colitis and RA
2. Ag-sulfadiazine: burns
Sulfasalazine: MOA?
sulfasalazine--colonic bacteriae-->
5-ASA(ulcerative colitis)
Uses of trimethoprim-sulfamethoxazole:
DOC for?
1. Nocardia
2. P.Jirovecci prophylaxis
3. Toxoplasma gondii
4. Back up for listeria

Gram -ve: Ecoli, salmonella, shigella, H.influenza
Gram +ve: staph (including MRSA)
Sulfonamides: pharmacokinetics?
Hepatically acetylated
Renally excreted
High protein binding--> kernicterus
Kernicterus causing antimicrobial drugs?
1. Chloramphenicol
MRSA effective antimicrobials?
1. Vancomycin
2. Clindamycin
Sulfonamides: toxicity?
1. SJS
2. Hemolysis in G6PD deficiency
3. Phototoxicity
4. BM suppression
Pneumocystis jirovecci: Drugs used?
1. Cotrimoxazole
2. Pentamidine
3. Atovaquone
Nucleic acid synthesis inhibitors?
Fluoroquinolones: MOA?
1. Inhibition of DNA gyrase/Topoisomerase II
2. Inhibition of Topoisomerase IV

FQs are cidal

Topoisomerase IV: function?
Prevents sister chromatids from twisting and recombining
Fluoroquinolones used in?
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
Drug resistant pneumococci?
1. Fluoroquinolone (levofloxacin)
2. Telethromycin
Soft tissue infections: drugs used?
1. Tigecycline
2. Fluoroquinolones

(soFT tissure infections- fluoroquinolones tigecycline
Fluoroquinolones: elimination?
Eliminated thru active secretion in kidney
(avoid probenicid)
(Dose reduction in renal failure)
Fluoroquinolones: side effects?
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)
Drugs whose absorption gets limited due to divalent cations (Fe, Ca)
1. Tetracycline
2. Fluoroquinolones
production of free radicals

Metronidazole is effective against _____(aerobes/anaerobes) ?
Metronidazile effective against ____(gram +ve/-ve)
gram -ve
Effective against which gram +ve?
Metronidazole DOC for?
Clostridium difficile
(Pseudomembranous colitis)
Metrinodazole: Side effects?
1. Metallic taste(d/t gingivitis)
2. Disulfiram effect
A/tb drugs: Name em?
1. Isoniazid
2. Rifampin
3. Ethambutol
4. Pyrazinamide
5. Streptomycin
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
Isoniazid: side effects?
1. Hepatitis(elevated AST and ALT)
2. Peripheral neuritis
3. Sideroblastic anemia
4. SLE(in slow acetylators)
Rifampin: MOA?
Inhibition of DNA dependent RNA polymerase
(Nucleic acid synthesis inhibitor)
Rifampin: Side effects?
1. Red orange urine/saliva
2. Hepatitis
3. Induction of P450
Ethambutol: MOA?
Inhibition of arabinogalactan synthesis(cell wall component)
A/tb drug requiring conversion by catalase? (prodrug)
Ethambutol: Side effects?
1. Dose dependent retrobulbar neuritis
2. Decreased visual acuity
(red-green discrimination)
Pyrizinamide: MOA?
Pyrizinamide: side effects?
1. Hepatitis
2. Hyperuricemia
Streptomycin: MOA?
AG: initiation complex formation inhibition
misreading of genetic code
Streptomycin: adverse effects?
1. Vestibular toxicity
2. Deafness
3. Nephrotoxicity
4. NM blockade
A/tb drug associated with hepatitis?
1. Isoniazid
2. Rifampin
3. Pyrizinamide
A/tb drug which is a prodrug?
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
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
Isoniazid prophylaxis offered to which patient population
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)
Amphotericin B: MOA
Interaction with cell membrane--->Pore formation(polyene)
Amphotericin B: Spectrum of activity/DOC for?
Wide spectrum: DOC for- 1.Aspergillus 2.Candida 3.Cryptococcus 4. Histoplasma 5.Mucor
Polyenes: Name em?
Amphotericin B
Nystatin: MOA?
Polyene: "interact with fungal cell membrane" ---> "pore" formation altering membrane permeability
Amphotericin B: MOA
Interaction with cell membrane--->Pore formation(polyene)
“Polyenes produce Pores in membranes”
Amphotericin B: Spectrum of activity/DOC for?
Wide spectrum: DOC for-
4. Histoplasma
6. Sporothrix
Amphotericin B: MOA has synergistic action with _____?
Flucytosine in _____ and _____ fungal infections
1. Candida
2. Cryptococcus
Nystatin : Uses?
Used in topical infections only

Why cannot it be used systemically?
Because of its high toxicity- cannot be used systemically
Amphotericin B : Pharmacokinetics? (unique)
1. Given IV(poor absorption)
2. Poor CNS penetration
3. Can be administered intra-thecally
4. Slow clearance- long T1/2
Amphotericin B: Side effects?
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
Azoles: MOA?
Inhibition of P-450 enzyme 14-alpha-demethylase
Function of 14-alpha-demethylase: function?
Converts lanosterole-->erogsterole
Azoles: Resistance development?
Decreased intracellular accumulation of azoles (Formation of pumps)
DOC for paracocidioides?

Other uses of ketoconazole?
Other uses:
1. Back up for histoplasma
2. Mucocutaneous candidiasis
3. Dermatophytoses
4. Back up for blastomyces
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?
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
Flucanazole: DOC for?
1. Esophageal candidiasis
2. Invasive candidiasis
3. Coccidiodomycosis
4. Fungal meningitis (cryptococcal)
Itraconazole/Voriconaxole: DOC for?
1. Blastomycosis
2. Sporotrichosis
3. Aspergillosis

(Imagine casper near a volcanic blast from the spore crater)
Azoles used topically?
1. Clotrimazole
2. Miconazole
Azoles that penetrate CNS?
Only flucanazole
Absorption of ketoconazole is interfered by ____?
Azole whose absorption is increased by food?
Azoles metabolized by liver enzymes?
Ketoconazole and itraconazole
Azole that is eliminated from liver in an unchanged form?
Azoles: side effects?
I. Decreased synthesis of steroids(cortisol/testorsterone)-->
1. Decreased libido
2. Gynecomastia
3. Menstrual abnormality

II. Hepatotoxicity: Increased LFTs
Flucytosine: the 2 MOAs?
1. Formation of 5-FU--(triphosphorylation)--->incorporated into fungal RNA
2. 5-FU---->5-fd-UMP (inhibits thymidylate synthase)--->decreased thymine
Flucytosine always used in combination with ______?
Amphotericin B

Due to rapid development of resistance
Flucytosine and amphotericin B combination used in _____ and _____fungal infections
Cryptococcal and Candidal
Flucytosine: side effects?
Bone marrow toxicity
Griseofulvin: MOA?
Disrupts microtubule structures of _____?
Griseofulvin attains maximum concentration in _____(body part/structure)
Griseofulvin: side effect?
Disulfiram like reaction
Terbanafine: MOA?
Inhibits squalene epoxide ---> decreased ergosterole synthesis
(cell wall synthesisn inhibitor)
Terbanafine: Side effects?
1. GI distress
2. Hepatotoxicity (increased LFT)
Caspofungin/Micafungin: MOA?
Inhibit glucan synthesis needed in cell wall synthesis
Caspofungin/Micafungin: Uses?
1. Invasive candidiasis
2. Aspergillosis
Caspofungin/Micafungin: Side effects?
1. GI distress
2. Flushing
Antivirals that inhibit viral penetration?
1. Enfuvirtide
2. Maraviroc
3. Amantadine
Antivirals that inhibit uncoating?
Antivirals that inhibit DNA-polymerase?
1. Acyclovir
2. Foscarnet
3. Ganciclovir
Antivirals that inhibit RNA-polymerase?
2. Ribavarin
Antivirals that inhibit viral reverse trascriptase?
1. Zidovudine
2. Didanosine
3. Zalcitabine
4. Lamivudine
5. Stavudine
6. Lamivudine
7. Nevirapine
8. Efavirenz
Antivirals that inhibit aspartate protease?
1. Indinavir
2. Ritanavir
3. Saquinavir
4. Nelfinavir
Antivirals that inhibit neuraminidase?
1. Zanamavir
2. Oseltamavir
Acyclovir: MOA?
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
Acyclovir: Resistance?
1. Changes in DNA polymerase
2. Decreased/complete inactivity of thymidine kinase (TK-)
Acyclovir: use/antiviral?
1. HSV
2. VZV only
Acyclovir: effect in HSV/VZV?
1. Reduces viral shedding(genital herpes)
2. Reduces acute neuritis in shingles
3. Reduces symptoms in chicken pox
4. Prophylactic in immunocompromised patients
Acyclovir is ineffective against ______?(herpes condition/symptom)
Post herpetic neuralgia
Acyclovir: Side effects?
1. Crystalluria
2. Neurotoxicity (headache, confusion, seizures)
Crystalluria observed as acyclovir side effect can be minimized by?
Maintaining hydration
Is acyclovir hematotoxic?
Antivirals with DNA-polymerase activity that are used in acyclovir resistant cases?
1. Foscarnet
2. Valacyclovir
Foscarnet and valacyclovir can be used in TK-ve strains: true/false?
Foscarnet and valacyclovir: pharmacologoc advantage over acyclovir?
Have a longer T1/2
Ganciclovir: MOA?
1. First step: phophorylation by Thymdine kinase/UL-97----> activated form--->incorporated into DNA--->termination
2. Activated gancyclovir inhibits DNA polymerase directly
Ganciclovir: Resistance?
1. Change in DNA polymerase
2. TK-ve strains
Ganciclovir: Side effects?
1. Hematotoxicity(leukopenia/thrombocytopenia)
2. Crystalluria
3. Mucositis
4. Fever
5. Rash
6. Siezures in overdose
Foscarnet: MOA?
Inhibits DNA and RNA polymerase
Antiviral used in prophylaxis and rx of CMV infections?
Ganciclovir (CMV retinitis in AIDS and transplant patients)
Ganciclovir: Uses?
1. HSV
2. VZV
3. CMV
Foscarnet: Side effect?
1. Nephrotoxicity: ATN
2. Hypocalcemia: tetany
3. Seizures(hypocalcemia)
Foscarnet should be avoided with _____ drug
IV pentamidine

To avoid life threatening nephrotoxicity and hypocalcemia
Nucleoside reverse transcriptase inhibitors:
Antiviral drug that is not an antimetabolite?
Activated by nonspecific phosphorylation---> competes with natural nucleotides---> incorporated into DNA---> termination
2. Activated/phosphorylated compound inhibits reverse trancriptase
NRTIs: Name em
1. Zidovudine 2. Didanosine 3. Zalcitabine 4. Lamivudine 5. Stavudine 6. Lamivudine 7. Nevirapine 8. Efavirenz
NRTIs: Resistance?
Occurs due to mutation in gene that encodes for reverse trancriptase
NRTI associated with:
1. Myopathy
2. Peripheral neuropathy
3. Pancreatitis
4. Hematotoxicity
5. GI distress
6. Liver dusfunction
7. Neutropenia?
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
Least toxic of all NRTIs?
Protease inhibitors: MOA?
Inhibit aspartate protease (required for cleaving pre-proteins into proteins of mature virus
Protease inhibitors: resistance?
Mutation in pol gene
Is cross resistance observed amongst protease inhibitors?
NO cross resistance between protease inhibitors
Is cross resistance observed amongst NRTIs?
NO cross resistance between NRTIs
Protease inhibitors: Name em?
1. Indinavir 2. Ritanavir 3. Saquinavir 4. Nelfinavir
2 protease inhibitors always used in combination?
Indinavir and ritanavir

To avoid resistance
NRTI combinations to be avoided? Why?
1. Didanosine + Zalcitabine(additive toxicity- pancreatitis)
2. Zidovudine + Stavudine(competition for activation)
Least toxic of all protease inhibitors?
Protease inhibitor associated with crystalluria?
Ritonavir: side effect?
Induction of CYPA12. Inhibition of all other P450 enzymes
Protease inhibitors: side effect in general?
Lipid and carb metab disorder-->obesity, insulin resistance
Antiviral that inhibits integrase enzyme (HIV)?
Enfuvirtide: MOA?
Fusion inhibitor: binds to gp41
Maraviroc: MOA?
Inhibition of CCR-5 protein

Location of CCR-5 protein?
CD4+ T cell
Amantadine: MOA?
Prevents attachment, penetration and uncoating of infuenza A virus
Amantadine: side effects?
1. Insomnia
2. Seizures
3. Nervousness
4. Livedo reticularis
5. Atropine like side effects
Amantadine: Uses?
Mainly for prophylaxis purposes
Zanamavir/oseltamavir: MOA?
Inhibit neuraminidase

Neuraminidase : function?
Prevent clumping of virus particles so that more may be available for infection
Neuraminidase inhibitors: name em?
Neuraminidase inhibitors: uses?
Used for prophylaxis
Ribavarin: MOA?
1. Monophosphorylated form inhibits IMP dehydrogenase
2. Triphosphate inhibits RNA polymerase and end capping of viral RNA
Ribavarin: Clinical uses?
1. Hepatitis C (Adjunct to alpha interferon)
2. RSV
3. Lassa fever
4. Hanta virus
Ribavarin: side effects?
1. Hemotoxic
2. Teratogenic
Interferon used in
1. Chronic granulomatous disease
2. Multiple sclerosis
3. Hepatitis?
1. CGD: IFN-gamma
2. MS: IFN-beta
3. Hepatitis: IFN-alpha
Uses of alpha IFN?
1. Hepatitis
2. Multiple myeloma
3. Renal cell carcinoma
4. Kaposi's sarcoma
5. Chronic myelogenous leukemia
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?
1. Zidovudine+Lamivudine
2. Zidovudine+Lamivudine+Indinavir
3. ZDV full dose in 2nd and 3rd trimester
4. Zidovudine
5. Nevirapine
DOC for:
1. Amebiasis
2. Giardiasis
3. Trichomoniasis
4. Toxoplasmosis
5. Leishmaniasis
6. Trypanosomiasis
1. Amebiasis: Metronidazole
2. Giardiasis: Metronidazole
3. Trichomoniasis: Metronidazole
4. Toxoplasmosis: Pyrimethamine + sulfadiazine
5. Leishmaniasis: Stibogluconate
6. Trypanosomiasis: Nifurtimox
african: arsenic componds
Antimalarials: Chloroquine sensitive: prophylaxis:
Chloroquine + primaquine
Antimalarials: Back up drugs?
1. Hydroxychloroquine
2. Primaquine
3. Pyrimethamine-sulfadoxine
DOC for:
1. P.falciparum
2. P.malaraie
3. P.vivax
4. P. ovale
1. P.falciparum: Chloroquine
2. P.malariae: Chloroquine
3. P.vivax: Chloroquine + Primaquine
4. P.ovale: Chloroquine + Primaquine
Antimalarials: side effects?
Hemolysis in G6PD deficiency
Cinchonism with quinine
Mebendazole: MOA?
1. Decreased glucose uptake
2. Distorts microtubule structure
Antimicrobials that distort microtubule structure?
1. Mebendazole
2. Griseofulvin
Mebendazole: uses?
For intestinal nematodes
Praziquantel: MOA?
1. Increases Ca influx
2. Increases vacuolization
Praziquantel: Use?
Most cestodes and trematodes