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Pharm Block 3 > Anti Protein Synthesis > Flashcards

Anti Protein Synthesis Flashcards

(78 cards)

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1
Q

bacterial ribosomes

A

30s

50s

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2
Q

bacterial start codon

A

formyl methionine

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3
Q

sequence upstream of start codon - helps bind mRNA to 16s ribosome

A

shine dalgarno

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4
Q

A site - acceptor - tRNA 1st attaches
P site - peptide - growing polypeptide chain
E site - exit - emptying tRNA

A

elongation of protein synthesis

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5
Q

peptide transformed from P site to A site by

A

peptide transferase

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6
Q

tRNA holding the polypeptide is translocated from A site to P site, opening A site

A

translocation

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7
Q

1) bind irreversibly to the 30s, inhibit initiation complex
2) misread mRNA
3) breakup polysomes into nonfunctional monosomes

A

aminoglycosides

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8
Q

1) bactericidal
2) work on aerobic gram negatives
3) coupled with cell wall active drugs (B lactams, vancomycin)

A

aminoglycosides

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9
Q

Ways of entry

1) passive diffusion
2) ATP and O2 dependent active transport

A

aminoglycosides

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10
Q

triple antibiotic ointment

A

neomycin
bacitracin
polymixin B

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11
Q

treats hepatic encephalopathy but lactulose is better and hepatic coma to decrease bacteria growth

A

neomycin

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12
Q

treats tularemia, TB, bubonic plague

A

streptomycin

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13
Q

Pharmacokinetics

1) poorly absorbed orally - always given parenterally - distributed mainly to ECF (14-20)
2) high [ ] in otic perilymph and renal cortical tissue

A

aminoglycosides

loop diuretics should not be used with aminoglycosides to prevent ototoxicity and nephrotoxicity

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14
Q

Mech. of Resistance

1) microorganism produces transferase enzyme or enzymes that inactivate aminoglycosides

A

acetylation
phosphorylation
adenylylation

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15
Q

what two aminoglycosides are resistant to inactivation by bacterial enzymes

A

netilmicin

amikacin

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16
Q

SE: ototoxicity, nephrotoxicity, acute tubular necrosis, NMJ blockade

A

aminoglycosides

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17
Q

Contraindications: in pregnancy (especially streptomycin) can cause deafness in newborn; avoid in sever renal dysfunction

A

aminoglycosides

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18
Q

displaces Ca2+ from nmj - leading to decrease Ach release

A

NMJ blockade

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19
Q

tubular damage, low GFR, results in loss of urinary [ ] capacity of tubules (ATN)

A

nephrotoxicity

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20
Q

causes acute proximal tubular necrosis (acute renal failure)

A

gentamicin

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21
Q

most nephrotoxic

A

gentamicin
neomycin
tobramycin

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22
Q

hearing loss, high frequency affected 1st then low frequency

A

cochlear ototoxicity

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23
Q

headache appears 1st followed by nausea, vomiting, dizziness, nystagmus, vertigo and ataxia

A

vestibular ototoxicity

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24
Q

most cochlear ototoxic agents

A

neomycin
kanamycin
amikacin

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25
most vestibulotoxic agents
streptomycin | gentamicin
26
bind reversibly to 30s blocks aminoacyl - tRNA enters A site bacteriostatic activity on gram + and - including anaerobes
tetracyclines
27
treats rickettsia, borrelia, vibrio, chlamydia, mycoplasma, and acne
tetracycline
28
Mech of resistance 1) development of efflux pump (Tet pump) 2) ribosomal protection proteins that displaces tetracycline 3) enzymatic inactivation of tetracycline
tetracycline
29
1st choice for rickettsia even in children
tetracycline
30
treatment for urethritis
tetracycline doxycycline, azithromycin and ceftriaxone for both sex partners
31
treatment for H pylori
bismuth, metronidazole, tetracycline and H2 blocker for 4 weeks
32
SE: calcium decreases absorption, causes tooth discoloration in young children, enamel dysplasia, skeletal deformities or growth retardation, hepatic necrosis especially in pregnant and Fanconi syndrome
tetracyclines
33
occurs from using expired tetracycline - renal tubular acidosis
Fanconi syndrome
34
Contraindications: can not be used in pregnancy or infants
tetracyclines
35
oral drug - absorbed un upper small intestine stays in intestine lumen - superinfections excreted in urine
tetracycline
36
excreted in stool can be used safely in px with renal dysfunction can cause vestibular toxicity (reversible)
doxycycline
37
inhibits renal actions of ADH used to treat ADH secretion tumors (SIADH) ADR: photosensitivity and nephrogenic DI
demeclocycline
38
``` IV only Tet pump insensitive bacteria broad spectrum (MRSA, VRSA) ineffective against proteus and pseudomonas eliminated through bile ```
tigecycline
39
acts on 50s, inhibiting translocation | bacteriostatic
macrolides
40
treat community acquired pneumonia cause by strep pneumonia, H flu, and moxraella and treats H pylori
azithromycin | clarithromycin
41
treat legionella pneumonia, chlamydia, urethritis and cervicitis, infections of bartonella, and mycobacterium avian and toxoplasma
macrolides
42
macrolides
azithromycin clarithromycin erythromycin
43
treats neonatal conjunctivitis and pneumonia caused by chlamydia trachoma's and diphtheria
erythromycin
44
SE: increased GI motility, acute cholestatic jaundice, prolonged QT interval, CYP450 inhibit (except azithromycin)
macrolides
45
1) gram +: production of methylase (methylation) | 2) gram -: resistance to esterase (hydrolyze)
Mech resistance of macrolides
46
highly affinity to 50s resistance used: only CAP SE: hepatotoxicity, exacerbation of MG Contraindication: MG
telithromycin - ketolides
47
acts on 50s, inhibiting translocation bacteriostatic anaerobe activity
clindamycin - lincosamide
48
activity against staph, strep, clostridium perfringens and MRSA treats S pyogenes and soft tissues infections, oral infections and aspiration pneumonia caused by bactericides fragilis and also actinomyces
clindamycin
49
SE: diarrhea, skin rashes, neutropenia, pseudomonas colitis caused by C Dif
clindamycin
50
methylation is mech of resistance
clindamycin
51
used also for: 1) active against pneumonia jiroveci with primaquine and toxoplasma gondii with pyrimethamine 2) prophylaxis of endocarditis in valvular heart disease before dental procedure if severe allergy to penicillin
clindamycin
52
binds to 50s, inhibits translocation methylation resistance only works on gram + cocci bactericidal
streptogramin
53
used in MRSA and VR enterococcus faecium given IV, 80% eliminated by biliary excretion
streptogramin
54
ADR: arthralgia and myalgia Potent: inhibitors of P450 CYP3A4
streptogramin
55
binds irreversibly to 50s, inhibits peptide bond formation and halting translation (inhibits peptidyl transferase) bacteriostatic
Chloramphenicol
56
very good activity against Salmonella typhi and useful for rocky mtn spotted fever in pregnant women, can also be used in s pneumo, h flu, n meningitis
Chloramphenicol
57
SE: anemia due to BM depression, aplastic anemia (irreversible), inhibits p450, gray baby
Chloramphenicol
58
accumulation of drug in babies due to ineffective glucuronic acid conjugation system - causes flaccidity, hypothermia, shock
gray baby
59
binds to unique 23s RNAs site of the 50s to inhibit initiation complex
linezolid
60
activity against gram + bacteria (cocci and rods), MRSA activity (nosocomial), and vancomycin resistant bacterial strains
linezolid
61
SE: thrombocytopenia, optic neuropathy, stocking glove peripheral neuropathy
linezolid
62
inhibit bacterial DNA gyrase (topoisomerase 2 (gram -) and 4 (gram +)) block relaxation of + supercoiled DNA (inhibit addition of - supercoil)
fluoroquinolones
63
treat UTI caused by pseudomonas
levofloxacin | ciprofloxacin
64
treat gram - causes gastroenteritis (shigella, e coli, salmonella) salmonella osteomyelitis (except norfloxacin) treats atypical pneumonia caused by legionella
fluoroquinolones
65
treat anthrax and prophylaxis pseudo aeruginosa
ciprofloxacin
66
treats CAP and mycoplasma pneumonia
levofloxacin
67
SE: Ca, Mg, iron decrease absorption - avoid with food, risk tendon and cartilage damage in elderly and children, photosensitivity, hypoglycemia, arthropathy in children
fluoroquinolones
68
High level - point mutation in quinolone binding region of topo
fluoroquinolones
69
ADR: 1) CNS - headache, dizziness, drowsiness 2) peripheral neuropathy 3) drug interaction: ciprofloxacin inhibits p450 4) may cause seizures by inhibiting theophylline metabolism Conta: children (cartilage develop), pregnancy, prolong QT
fluoroquinolones
70
antibacterial and antiprotozoa drug bacteriocidal
metronidazole
71
activity against giardia treats vaginitis and cervicitis caused by protozoal infection and bacterial vaginosis caused by gardenella Substitute for amoxicillin in triple therapy for H pylori in penicillin allergic px
metronidazole
72
treats pseudomembranous colitis caused by clostridium
metronidazole
73
SE: disulfuram like rxn
metronidazole
74
above the diaphragm below the diaphragm
clindamycin metronidazole
75
urinary antiseptic Tx: uncomplicated UTI attain high [ ] in urine ADR: pulmonary fibrosis and hypersensitivity G6PD def. hemolytic anemia and neutropenia
nitrofurantoin
76
cationic detergents gram - topical use B and C types
polymyxins
77
destabilizes gram - bacteria outer cell wall through ionic interactions
polymyxin B
78
from pseudomonas fluorescens gram + bacteria including MRSA inhibits staph isoleucyl tRNA synthetase ointment for topical use of minor skin infections
mupirocin

Pharm Block 3 (11 decks)

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