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ID > Walsh drugs > Flashcards

Walsh drugs Flashcards

1
Q

macrolides structure

A

macrocyclic lactone ring of 14-16 carbons with deoxy sugars attached

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2
Q

macrolide mechanism

A

inhibits protein synthesis via binding to 50S ribosomal RNA which prevents elongation

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3
Q

metronidazole chemistry

A

a synthetic derivative of 5-nitroimidazole

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4
Q

metronidazole mechanism

A

selectively absorbed by anaerobic bacteria and sensitive protozoa in unionized form–> nonenzymatically reduced by reacting with ferredoxin–> results are toxic products that accumulate in cells–> taken up into bacterial DNA–> unstable molecules that are highly reactive–> bactericidal

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5
Q

sulfonamides chemistry

A

structurally related to p-aminobenzoic acid (PABA)

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6
Q

sulfonamides mechanism

A

as structural analogs of PABA, they inhibit dihydropteroate synthase and thus folate production

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7
Q

trimethoprim mechanism

A

inhibits dihydrofolate reductase

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8
Q

fluoroquinolones structure

A

synthetic fluorinated analogs of nalidixic acid

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9
Q

fluoroquinolones mechanism

A

block bacterial DNA synthesis by inhibiting topoisomerase II (DNA gyrase) and IV

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10
Q

nitrofurantoin structure

A

aromatic xenobiotic compound with 2 main pharmacophores: nitro group attached to furan ring at 5 position, hydrazone moiety

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11
Q

nitrofurantoin mechanism

A

undergoes rapid intracellular conversion to highly reactive intermediates by bacterial reductases–> these intermediates react non-specifically with many ribosomal proteins and disrupt the synthesis of proteins, RNA, DNA, and metabolic processes

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12
Q

fosfomycin structure

A

phosphoenolpyruvate analogue, contains a phosphonic group and an epoxide ring

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13
Q

fosfomycin mechanism

A

inhibits cytoplasmic enzyme enolpyruvate transferase (MurA) by covalently binding to the cysteine residue of the active site. blocks the addition of phosphoenolpyruvate–> UDP-N-acetylglucosamine (which is the first step in the formation of UDP-N-acetyluramic acid, the precursor to N-acetylmuramic acid, which is only found in bacterial cell walls). thus, inhibits a very early stage of bacterial cell wall synthesis

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14
Q

macrolides solubility

A

poorly soluble in water but dissolve in organic solvent (so they are dispensed as esters and salts)

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15
Q

macrolides preferred pH

A

enhanced activity at alkaline pH (inactivated in highly acidic environments)

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16
Q

macrolides renal

A

no renal dose adjustments; not removed by dialysis

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17
Q

macrolides distribution

A

distributed widely except CNS and CSF; traverses placenta

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18
Q

macrolides major ADE

A

GI intolerance due to direct motilin agonists/disrupt normal gut flora. also may prolong QT interval

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19
Q

which macrolide has the highest tendency of prolonging QT interval

A

erythromycin

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20
Q

which macrolide has the lowest tendency of prolonging QT interval

A

azithromycin

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21
Q

what side effect can erythromycin produce

A

acute cholestatic hepatitis (fever, jaundice, etc)

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22
Q

metronidazole distribution

A

wide; penetrates well into the CNS and CSF

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23
Q

how is metronidazole metabolized

A

hepatically; may accumulate in hepatic insufficiency

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24
Q

major ADE for metronidazole

A

disulfiram-like reaction due to accumulation of acetaldehyde: avoid alcohol also for 3 days after treatment

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25
Q

3 major groups of sulfonamides

A

PO absorbable, PO nonabsorbable, topical

26
Q

major groups within PO absorbable sulfonamides

A

short, intermediate, long acting

27
Q

what classification is sulfamethoxazole

A

intermediate acting

28
Q

sulfonamides renal

A

renal dose adjustments at severe reduction in kidney function

29
Q

sulfonamides major ADE

A

cross allergy?, urinary tract disturbances: crystalluria, hematuria, urinary obstruction. fever, rash, photosensitivity, urticaria, n/v/d, SJS, nephrosis, allergic nephritis, hematopoietic disturbances

30
Q

sulfonamides taken near end of pregnancy

A

increased risk of kernicterus in newborns (a type of brain damage secondary to high levels of bilirubin)

31
Q

how to treat crystalluria from sulfonamides and why

A

sodium bicarb–> it alkalizes the urine, helps make it more soluble

32
Q

trimethoprim important PK

A

it is more lipid soluble than sulfamethoxazole; higher volume of distribution

33
Q

ratio of sulfa to TMP

A

5:1

34
Q

renal dose adjustment in bactrim?

A

yes

35
Q

TMP major ADRs

A

megaloblastic anemia, leukopenia, granulocytopenia. patients with AIDS and pneumocystis pneumonia experience high frequency of fever, rash, leukopenia, diarrhea, elevations of hepatic enzymes, hyperkalemia, hypernatremia

36
Q

fluoroquinolones absorption

A

impaired by divalent and trivalent cations, including those found in OTC antacids like tums: dose 2 hours before or 4 hours after any products containing these cations

37
Q

fluoroquinolones major ADE

A

GI events including antibiotic-associated colitis. QT prolongation. may damage growing cartilage and cause arthropathy: not rec. for <18 years. avoid in pregnancy. Peripheral neuropathy/CNS effects (concern for elders)

38
Q

nitrofurantoin important PK

A

doesn’t work systemically, is a urinary antiseptic

39
Q

nitrofurantoin major ADR

A

anorexia, n/v, neuropathies, hemolytic anemia in patients with glucose 6 phosphate deficiency. hypersensitivity

40
Q

Nitrofurantoin antagonizes the action of ____

A

nalidixic acid

41
Q

fosfomycin major ADE

A

hematuria and dysuria, counsel patients to drink plenty of water

42
Q

how does food impact clarithromycin absorption

A

ER form: increases. IR form: no effect

43
Q

how does food impact azithromycin and erythromycin absorption

A

decreases

44
Q

what is different about the chemistry of clarithromycin

A

the addition of a methyl group: improves acid stability and oral absorption.

45
Q

how does clarithromycin compare to erythromycin in terms of antibacterial activity

A

it is more active against mycobacterium avium

46
Q

what is different about the PK of clarithromycin

A

longer half life so twice daily dosing

47
Q

dose adjustments for clarithromycin

A

reduce at CrCl< 30 ml/min

48
Q

advantages of clarithromycin over erythromycin

A

lower incidence of GI intolerance, less frequent dosing, better tissue penetration

49
Q

what is different about the chemistry of azithromycin

A

addition of a methylated nitrogen to the lactone ring

50
Q

azithromycin is highly active against

A

chlamydia species

51
Q

what is different about azithromycin PK

A

longest half life of all agents: once daily dosing and shortening duration of therapy

52
Q

azithromycin with meals

A

1 hour before or 2 hours after

53
Q

when is nitrofurantoin contraindicated

A

CrCL <60 mL/min

54
Q

what is the difference between macrobid and macrodantin

A

macrobid contains 25% macrocrystal and 75% monohydrate. macrodantin contains only macrocrystal

55
Q

erythromycin inhibits ____

A

CYP3A4, can increase concentrations of drugs. clarithromycin does this less, and azithromycin does not participate at all.

56
Q

erythromycin increases serum concentration of ____

A

PO digoxin by increasing bioavailability

57
Q

how is macrobid taken

A

bid

58
Q

how is macrodantin taken

A

qid

59
Q

which is the least active fluoroquinolone for gram + and -

A

norfloxacin

60
Q

which fluoroquinolones have excellent gram - and good gram +

A

ciprofloxacin, levofloxacin, ofloxacin

61
Q

which fluoroquinolones have improved activity against gram +

A

gemifloxacin and moxifloxacin

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