Tb, Antifungals, And Antivirals

Front 1

First Line TB Drugs:

Back 1

Rifampin
Isoniazid
Pyrazinamide
Ethambutol
"Streptomycin"

Hint 1

RIPE

Front 2

First Line TB Drugs:

Back 2

Rifampin
Isoniazid
Pyrazinamide
Ethambutol
"Streptomycin"

Hint 2

RIPE

Front 3

Isoniazid (INH)MoA:

Back 3

Inhibits synthesis of mycolic acids and mycobacterial cell wall

Front 4

Isoniazid (INH)MoA:

Back 4

Inhibits synthesis of mycolic acids and mycobacterial cell wall

Front 5

Isoniazid (INH) Route:

Back 5

PO/IM
Good PO absorption

Front 6

Isoniazid (INH) Route:

Back 6

PO/IM
Good PO absorption

Front 7

Isoniazid (INH) Metabolism:

Back 7

Metabolized by N-acetyltransferase in the liver

Slow acetylators have increased toxicity

Front 8

Isoniazid (INH) AEs:

Back 8

Hepatotoxic (AST, ALT)

Neurotoxicity (B6 defenciency; given prophyllaxis)

Front 9

Rifampin MoA & PK

Back 9

MoA: Inhibits DNA-dependent RNA polymerase and inhibits RNA synthesis

Extremely bactericidal (never monotherapy)

IV/PO
Well absorbed/widely distributed
Excreted into bile
Enterohepatic recirc.
Excretion via feces

Front 10

Rifampin AEs:

Back 10

Hepatotoxic
n/v
rash
Red-orange discoloration of fluids

POTENT 2D6 & 3A4 INHIBITOR

Front 11

Pyrazinamide MoA & PK:

Back 11

Prodrug converted to pyrainoic acid by mycobacteria

Bactericidal

PO Only (well absorbed)
Widely dist.
Extensive hepat. metab.
Metabolites renally excreted

Front 12

Pyrazinamide AEs:

Back 12

Hepatotoxic, hyperuricemia (gout), n/v

Front 13

Ethambutol only TB agent not:

Back 13

metabolized primarily metabolized in liver

Front 14

Ethambutol MoA, PK:

Back 14

Inhibits cell wall, bacteriostatic

PO only (well absorbed)
Primarily excreted in urine

Front 15

Ethambutol AEs:

Back 15

Optic neuritis (dose related)

Cat C

Front 16

Streptomycin is an:

Back 16

aminoglycoside

Front 17

Streptomycin MoA, PK:

Back 17

Inhibits protein synthesis

Bactericidal against rapidly dividing EC organisms

IM/IV
Eliminated renally

Front 18

Streptomycin AEs:

Back 18

Ototoxicity (can be permanent)
Nephrotoxicity (reversible)

Cat D

Front 19

First Line TB Drugs:

Back 19

Rifampin
Isoniazid
Pyrazinamide
Ethambutol
"Streptomycin"

Hint 19

RIPE

Front 20

First Line TB Drugs:

Back 20

Rifampin
Isoniazid
Pyrazinamide
Ethambutol
"Streptomycin"

Hint 20

RIPE

Front 21

Isoniazid (INH) Metabolism:

Back 21

Metabolized by N-acetyltransferase in the liver

Slow acetylators have increased toxicity

Front 22

Isoniazid (INH) AEs:

Back 22

Hepatotoxic (AST, ALT)

Neurotoxicity (B6 defenciency; given prophyllaxis)

Front 23

Isoniazid (INH)MoA:

Back 23

Inhibits synthesis of mycolic acids and mycobacterial cell wall

Front 24

Rifampin MoA & PK

Back 24

MoA: Inhibits DNA-dependent RNA polymerase and inhibits RNA synthesis

Extremely bactericidal (never monotherapy)

IV/PO
Well absorbed/widely distributed
Excreted into bile
Enterohepatic recirc.
Excretion via feces

Front 25

Isoniazid (INH)MoA:

Back 25

Inhibits synthesis of mycolic acids and mycobacterial cell wall

Front 26

Rifampin AEs:

Back 26

Hepatotoxic
n/v
rash
Red-orange discoloration of fluids

POTENT 2D6 & 3A4 INHIBITOR

Front 27

Isoniazid (INH) Route:

Back 27

PO/IM
Good PO absorption

Front 28

Isoniazid (INH) Route:

Back 28

PO/IM
Good PO absorption

Front 29

Pyrazinamide MoA & PK:

Back 29

Prodrug converted to pyrainoic acid by mycobacteria

Bactericidal

PO Only (well absorbed)
Widely dist.
Extensive hepat. metab.
Metabolites renally excreted

Front 30

Pyrazinamide AEs:

Back 30

Hepatotoxic, hyperuricemia (gout), n/v

Front 31

Ethambutol only TB agent not:

Back 31

metabolized primarily metabolized in liver

Front 32

Ethambutol MoA, PK:

Back 32

Inhibits cell wall, bacteriostatic

PO only (well absorbed)
Primarily excreted in urine

Front 33

Ethambutol AEs:

Back 33

Optic neuritis (dose related)

Cat C

Front 34

Streptomycin is an:

Back 34

aminoglycoside

Front 35

Streptomycin MoA, PK:

Back 35

Inhibits protein synthesis

Bactericidal against rapidly dividing EC organisms

IM/IV
Eliminated renally

Front 36

Streptomycin AEs:

Back 36

Ototoxicity (can be permanent)
Nephrotoxicity (reversible)

Cat D

Front 37

Isoniazid (INH) Metabolism:

Back 37

Metabolized by N-acetyltransferase in the liver

Slow acetylators have increased toxicity

Front 38

Isoniazid (INH) Metabolism:

Back 38

Metabolized by N-acetyltransferase in the liver

Slow acetylators have increased toxicity

Front 39

Isoniazid (INH) AEs:

Back 39

Hepatotoxic (AST, ALT)

Neurotoxicity (B6 defenciency; given prophyllaxis)

Front 40

Isoniazid (INH) AEs:

Back 40

Hepatotoxic (AST, ALT)

Neurotoxicity (B6 defenciency; given prophyllaxis)

Front 41

Rifampin MoA & PK

Back 41

MoA: Inhibits DNA-dependent RNA polymerase and inhibits RNA synthesis

Extremely bactericidal (never monotherapy)

IV/PO
Well absorbed/widely distributed
Excreted into bile
Enterohepatic recirc.
Excretion via feces

Front 42

Rifampin AEs:

Back 42

Hepatotoxic
n/v
rash
Red-orange discoloration of fluids

POTENT 2D6 & 3A4 INHIBITOR

Front 43

Rifampin MoA & PK

Back 43

MoA: Inhibits DNA-dependent RNA polymerase and inhibits RNA synthesis

Extremely bactericidal (never monotherapy)

IV/PO
Well absorbed/widely distributed
Excreted into bile
Enterohepatic recirc.
Excretion via feces

Front 44

Rifampin AEs:

Back 44

Hepatotoxic
n/v
rash
Red-orange discoloration of fluids

POTENT 2D6 & 3A4 INHIBITOR

Front 45

Pyrazinamide MoA & PK:

Back 45

Prodrug converted to pyrainoic acid by mycobacteria

Bactericidal

PO Only (well absorbed)
Widely dist.
Extensive hepat. metab.
Metabolites renally excreted

Front 46

Pyrazinamide MoA & PK:

Back 46

Prodrug converted to pyrainoic acid by mycobacteria

Bactericidal

PO Only (well absorbed)
Widely dist.
Extensive hepat. metab.
Metabolites renally excreted

Front 47

Pyrazinamide AEs:

Back 47

Hepatotoxic, hyperuricemia (gout), n/v

Front 48

Ethambutol only TB agent not:

Back 48

metabolized primarily metabolized in liver

Front 49

Ethambutol MoA, PK:

Back 49

Inhibits cell wall, bacteriostatic

PO only (well absorbed)
Primarily excreted in urine

Front 50

Pyrazinamide AEs:

Back 50

Hepatotoxic, hyperuricemia (gout), n/v

Front 51

Ethambutol AEs:

Back 51

Optic neuritis (dose related)

Cat C

Front 52

Ethambutol only TB agent not:

Back 52

metabolized primarily metabolized in liver

Front 53

Streptomycin is an:

Back 53

aminoglycoside

Front 54

Ethambutol MoA, PK:

Back 54

Inhibits cell wall, bacteriostatic

PO only (well absorbed)
Primarily excreted in urine

Front 55

Ethambutol AEs:

Back 55

Optic neuritis (dose related)

Cat C

Front 56

Streptomycin is an:

Back 56

aminoglycoside

Front 57

Streptomycin MoA, PK:

Back 57

Inhibits protein synthesis

Bactericidal against rapidly dividing EC organisms

IM/IV
Eliminated renally

Front 58

Streptomycin AEs:

Back 58

Ototoxicity (can be permanent)
Nephrotoxicity (reversible)

Cat D

Front 59

Streptomycin MoA, PK:

Back 59

Inhibits protein synthesis

Bactericidal against rapidly dividing EC organisms

IM/IV
Eliminated renally

Front 60

Streptomycin AEs:

Back 60

Ototoxicity (can be permanent)
Nephrotoxicity (reversible)

Cat D

Front 61

Amphotericin B MoA:

Back 61

Bind to ergosterol in the fungal cell membrane (pokes holes)

Hint 61

Swiss Cheese

Front 62

Amphotericin B PK:

Back 62

IV in D5W sol over 2-4 hrs
Widely dist. in tissues
Excreted extremely slowly in urine (half life 24 hrs-14 days)

Front 63

Amphotericin B AEs:

Back 63

Infusion-related rxns (fever, chills, vomitting, headache)

Nephrotoxicity (lipid formulations less nephrotoxic)

Lowered Mg2+ & K+

Front 64

Flucytosine (5-FC = 5-fluorocytosine) MoA, PK, AEs:

Back 64

MoA: Inhibits DNA synthesis (nvr monotherapy)

PK: PO only; renal excretion

AE: Bone marrow suppression

Front 65

Caspofungin, micafungin, anidulafungin are all members of what drug class?

Back 65

Echinocandins

Front 66

Echinocandins MoA, PK, AE:

Back 66

MoA: Inhibit fungal cell wall synthesis; target Beta-(1,3)-D-glucan synthase enzyme

PK: IV only, hepatic metabolism

AE: Extremely well tolerated; Thrombophlebitis, abnormal liver enzymes possible

Front 67

Terbinafine is what kind of antifungal?

Back 67

Allylamine

Front 68

Terbinafine MoA, PK, AEs:

Back 68

MoA: Inhibits ergosterolsynthesis; Inhibits enzyme squalene epoxidase

PK: Topical and PO; 40% bioavailability due to first-pass metabolism; Long half-life of 200-400 hrs (slow release from tissues)

AEs: GI, hepatotoxicity

Hint 68

1st and Long

Front 69

Azole antifungal MoA, PK:

Back 69

MoA: Inhibit synthesis of ergosterol(fungal cell
membrane component); Inhibit enzyme 14-demethylase

PK: Variable absorption when administered orally Fluconazole>> voriconazole, posaconazole>>
itraconazole Most undergo hepatic metabolism via CYP450 3A4 Not posaconazolewhich is glucuronidatedin liver Exception = fluconazole(excreted in the urine)

Front 70

Azole Interactions:

Back 70

They're CYP450 inhibitors (including 3A4)

Front 71

Azole AEs:

Back 71

Hepatotoxicity, visual disturbances (voriconazole only)

Front 72

Nucleoside Analogues MoA:

Back 72

Prodrugs

Phosphorylated by viral and host kinases to form active triphosphateform (thymidinekinase)

Compete with endogenous nucleoside
triphosphatesand competitively inhibit
viral DNA polymerase

Inhibition of viral DNA polymerase
prevents the synthesis of viral DNA

Front 73

Ganciclovir AE:

Back 73

Bone marrow suppression

Front 74

Cidofovir AE:

Back 74

VERY TOXIC

Bone marrow suppression and nephrotoxicity

Probenecid and hydration are co-administered with each dose Probenecid decreases cidofovirsecretion into kidney

Front 75

Foscarnet MoA:

Back 75

Blocks pyrophosphate-binding sites on viral DNA polymerase and prevents attachment of nucleotide precursors to DNA

No activation needed

Front 76

Foscarnet PK & AE:

Back 76

IV only; renal excretion

Nephrotoxicity

Front 77

WHich is the only IV NSAID?

Back 77

toradol