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Pharma > Antimicrobials: Protein Synthesis Inhibitors > Flashcards

Antimicrobials: Protein Synthesis Inhibitors Flashcards

1
Q

Inhibits formation of initiation complex

A

Aminoglycosides

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2
Q

Inhibits amino acid incorporation

A

Tetracycline

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3
Q

Inhibits formation of peptide bond

A

Chloramphenicol

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4
Q

Inhibits translocation

A

Macrolides

Lincosamide (Clindamycin)

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5
Q

Agents that bind to 30s ribosomal subunit

A

Aminoglycoside

Tetracycline

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6
Q

Agents that bind to 50s ribosomal subunits

A

Macrolides
Chloramphenicol
Lincosamide

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7
Q

Bactericidal

A

Aminoglycoside

Cell wall synthesis inhibitors

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8
Q

Bacteriostatic

A

Tetracycline
Macrolide
Chloramphenicol
Lincosamide

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9
Q

“mycin”

A

Derived from streptomyces

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10
Q

“Micin”

A

Derived from micromonospora

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11
Q

Inhibits protein synthesis at the 30s ribosomal subunit

Excreted unchanged by

A

Aminoglycoside

kidneys

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12
Q

Aminoglycoside examples

Excreted unchanged by kidneys

A 
Amikacin
Netilmicin
Neomycin
Tobramycin
Gentamicin
Streptomycin

TANGS

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13
Q

For UTI Gram negatives

Combined with penicillin and cephalosporin and or anti anaerobe
E coli
Enterobacter
Klebsiella
Pseudomonas
Tularemia
A

Aminoglycosides

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14
Q

DOC for tularemia

A

Streptomycin

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15
Q

Synergistic with beta lactam antibiotics
Bactericidal

Highly polar structure prevents adequate absorption after oral administration

All must be given IV to achieve serum levels except neomycin

A

Aminoglycoside

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16
Q

Only aminoglycoside given topically or orally

A

Neomycin

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17
Q

Aminoglycosides cause

A

Ototixicity
Nephrotoxicity

as well as Cisplatin

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18
Q

Aminoglycosides are bactericidal because

A

1 they bind to outer bacterial membrane thereby disrupting membrane integrity
2 bind to ribosomal 30s subunit

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19
Q

Interferes formation of initiation complex
Induce misreading of mRNA template
Cause polysomes to break up into monosomes
Concentration-dependent killing

A

Binding to 30s ribosomal subunit

Aminoglycosides

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20
Q

Explains why aminoglycosides can be given in single daily doses despite short half-life

A

Concentration dependent (post antibiotic effect)

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21
Q

2 days fluid diet, mechanical

Oral Metronidazole and Erythromycin 1 g and Neomycin

A

Nichols-Codon Bowel Prep for Colorectal Surgery

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22
Q

Aminoglycoside adverse effects:

A

Ototoxicity
Nephrotoxicity - Acute Tubular Necrosis
Neuromuscular blockade

“triple punch of a mean guy”

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23
Q

Aminoglycosides cause ototoxicity and nephrotoxicity because

A

they accumulate in the endolymph of the inner ear causing damage to hair cells in cochlea

and renal cortex

this is increased when taking diuretics

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24
Q

Aminoglycosides cause nephrotoxicity because

A

they accumulate in the renal cortex

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25
Q

Aminoglycosides cause neuromuscular blockade because

A

they decrease acetylcholine and decrease sensitivity to postsynaptic site

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26
Q

Aminoglycoside-induced neuromuscular blockade is reversed by

A

Ca gluconate

Neostigmine

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27
Q

Broadest spectrum of activity

A

Tetracycline

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28
Q 
Activity against gram positive
Gram negative
Spirochetes
Mycoplasma
Rickettsia
Chlamydia
A

Tetracyclines

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29
Q

Contains four fused rings with a system of conjugated double bonds
Inhibits protein synthesis at 30s ribosomal subunit

A

Tetracyclines

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30
Q

Tetracyclines Cannot be given with milk and antacids because

A

They form stable complexes with divalent and trivalent cations. Divalent cations inhibit its absorption in the gut.

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31
Q

Tetracylines cause Milk Alkali Syndrome:

A

Hypercalcemia
Alkalosis
Renal failure

inc Ca
inc pH
Renal failure

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32
Q

DOC for vibrio cholerae

A

Tetracycline

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33
Q

DOC for Mycoplasma

A

Macrolide

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34
Q

DOC for Rickettsia

A

Tetracycline

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35
Q 
Covers
Vibrio cholerae
Acne
Chlamydia
Ureaplasma
Urealyticum
Mycoplasma
Borrelia burgdorferi (Lyme disease)
Rickettsia
A

Tetracycline

VACUUM your Bed Room

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36
Q 
For psittacosis
inclusion conjunctivitis
trachoma
endocervical 
rectal infection and
non specific urethritis

all by Chlamydia

A

Tetracycline

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37
Q

DOC in syphillis if allergic to penicillin

A

Tetracycline

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38
Q

For Brucellosis
Cholera
Acne

A

Tetracycline

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39
Q

Most common adverse effect of tetracycline

A

Nausea and vomiting

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40
Q

Tetracycline advserse effects:

A

Deposition in bones and primary dentition causing DISCOLORATION AND HYPOPLASA

“teethracylcine”

Fanconi syndrome
Hepatotoxicity
Phototoxicity
Vestibular problems

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41
Q

Tetracycline may also cause this syndome

A

Fanconi’s syndrome nephrocalcinosis

rare renal tubule disorder causing excess amounts of glucose, bicarbonate, phosphates, uric acid, potassium, amino acids

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42
Q

Tetracyclines cause these symptoms

A

Enamel dysplasia

Inhibition of bone growth affecting epiphyseal plate also Quinolones

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43
Q

Tetracycline causing phototoxicity

A

Demeclocycline

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44
Q

Tetracycline causing vestibular problems

A

Minocycline

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45
Q

Only aminoglycoside given for Neisseria

A

Spectinomycin

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46
Q

Tetracycline with longest half life

and with highest protein binding

A

Doxycycline

cleared renally and fecally without liver metab

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47
Q

Tetracycline with best absorption and tissue penetration

A

Minocycline

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48
Q

Tetracycline contraindications:

A

Pregnant
Children under 8 years

Teratogen and teeth stainer

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49
Q

Covers gram negative: H influenzae, N meningitidis, N gonorrhea, Salmonella typhi, Brucella, Bordetella pertussis

Anaerobic gram positive cocci: C tetani, Mycoplasma

E coli, V. cholerae, Shigella, Chlamydia, Mycoplasma

Not effective against Pseudomonas, Histolytica, Entamoeba

A

Chloramphenicol

Chloromycetin

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50
Q 
Used for tyhpoid fever
Bacterial meningitis 
Anaerobic infections
Rickettsial disease (murine, scrub typhus, recrudescent typhus)
Rocky Mountain Spotted Fever
Q fever
Brucellosis
A

Chloramphenicol

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51
Q

Current DOC for typhoid

A

Ceftriaxone

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52
Q

Chloramphenicol resistance

A

Acetylation of chloramphenicol by acetyl-transferase enzyme (acetylated form cannot bind ribosome)
Decreased cellular permeability
Mutation leading to ribosomal insensitivity

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53
Q

Because of potential toxicity, this should only be employed with a well-defined and indicated condition

Acetylation by acetyl transferase - cannot bind ribosome, resistance

Decreased cellular permeability

A

Chloromycetin

Chloramphenicol

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54
Q

Chloramphenicol AR

A 
Anemia (dose dep) 
Aplastic anemia (dose INdep) 
Grey baby syndrome (lack of UDP- Glucoronyl transferase) ashen grey color of skin and lethargic eyes
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55
Q

Most important to toxicity of chloramphenicol is

A

Hematologic:
Bone marrow aplasia (benzene)
Idiosyncratic (aplastic anemia)
Dose-related reactions: erythroid supression of bone marrow (hypocellular aslo Vinblastin, Vincristine)

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56
Q

Chloramphenicol should not be given with a

A

phenobarbital (shortens half life)

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57
Q

inhibits protein synthesis at 50s ribosomal subunit

A

Macrolide

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58
Q

From streptomyces erythreus
Formerly Ilotycin

Alternative to penicillin if with allergy

Mainly for gram positives ineffective for gram neg

Bacteriostatic at low conc
Bactericidal at high conc

A

Erythromycin

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59
Q

Erythromycin activity

A

Static in low concentrations

Cidal in high concentrations

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60
Q

Covers Corynebacterium
Chlamydia
CAP (pneumococcus, mycoplasma, legionella)
Staph

Atypicals: Mycoplasma, Legionella
Gram neg: Neisseria, Bordatella

A

Erythromycin

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61
Q

Allergy with penicillin drug of choice

A

Erythromycin

62
Q

Allergy with erythromycin

A

Vancomycin IV

63
Q

Allergy with Vancomycin

64
Q

Erythromycin base can be inactivated by

A

gastric acid

65
Q

Esters of erythromycin base with improved acid stability and absorption less altered by food

A

stearate
estolate
ethylsuccinate

66
Q 
DOC for Legionnare’s disease
Mycoplasma 
Campylobacter
Chlamydial infection
Diptheria
Pertussis

Also covers for
Gram positives: pneumococci, legionella, chlamydia, listeria, helicobacter, mycobacteria

Gram negatives: neisseria, bordetella, bartonella, rickettsia, campylobacter, H influenzae (less susceptible)

A

Erythromycin

Macrolides

67
Q

Adverse effects of erythromycin

A

Epigastric distress
Cholestatic jaundice (estolate from erythromycin)
GI: anorexia, nausea, vomiting, diarrhea
Hepatitis, fever and rash

68
Q

Erythromycin causes diarrhea because

A

it directly stimulates gut motility

69
Q

IM injection of erythromycin may lead patient to experience

A

Pain for hours

Deafness (transient)

70
Q

Erythromycin is an enzyme

A

Inhibitor of CYP450

71
Q

Erythromcin increases levels of

A 
Theophylline
Oral anticoagulants
Cyclosporine
Digoxin
Statin 
Corticosteroids 
Carbamazepine
72
Q

Unique pharmacokinetic properties

Extensive tissue distribution
High drug concentration in cells (including phagocytes) resulting in greater tissue and secretion concentration compared to serum concentration

Half life of 3 days!

Does not inactivate CYP450

A

Azithromycin

73
Q

once a day dosing

should not be given with food

A

Azithromycin

74
Q

Used for nongonococcal urethritis caused by chlamydia, LRTI, PID, pharyngitis, Legionnaire

A

Azithromycin

75
Q

More active against staph and streph
Used in PUD antimicrobial protocol with omeprazole or lanzoprazole

Given with or without food but extended release form as once a day dosing (with food to improve bioavailability)

A

Clarithromycin

76
Q

Inhibits protein synthesis by binding to 50s ribosomal subunit of bacterial ribosome
Exhibits cross resistance with macrolides

A

Clindamycin

77
Q

Sulfur-containing antibiotics isolated from Streptomyces lincolnensis

Resemble macrolides in antibacterial spectrum and biochemical mechanism of action but has cross resistance

Inhibits 50s subunit

A

Lincomycin

78
Q

Potent agent available for non-spore forming anaerobic bacteria (Bacteroides fragilis)

But best for anaerobes like Bacteroides

A

Clindamycin

79
Q

Aspiration pneumoniae

Anaerobics DOC

A

Clindamycin

80
Q

Intraabdominal infection DOC

A

Metronidazole

81
Q

Covers

Gram positives: streptococci, staphylococci, pneumococci
Anaerobes: Gram positive and Gram negative Bacteroides

No activity against Enterococci, Gram negative aerobic bacteria

A

Clindamycin

82
Q

Drug inducing C difficile infection

A

Clindamycin
Ampicillin/Amoxicillin
Cephalosporin
Fluoroquinolone

83
Q

Treats anaerobic infection
Penetrating wounds of abdomen and gut
Female genital tract infections
Aspiration pneumonia*

A

Clindamycin

84
Q

Clindamycin AE

A

Diarrhea
Nausea
Skin rash
Pseudomembranous colitis*

85
Q

Patterned after Nalidixic acid

A

Quinolones

86
Q

Introduction of fluorine atom forming fluoroquinolones enhances antibacterial activity

A

Fluoroquinolone

87
Q

Most potent fluoroquinolone

A

Ciprofloxacin

88
Q

Fluoroquinolone inhibits DNA synthesis due to inhibition of

A

DNA Gyrase

Topoisomerase II and IV

89
Q

First Gen Quinilone

A

Nalidixic acid

Non-fluorinated

90
Q

Second Gen Quinolone

A

Ciprofloxacin -most potent fluorinated quinolone

Ofloxacin

91
Q

Third generation quinolone

A

Gatifloxacin flourinated

92
Q

Fluoroquinolone AE

A 
Diarrhea*
Nausea*
Closure of epiphyseal plates*
Headache
Dizziness
Nephrotoxicity
Phototoxicity*
93
Q

Fluoroquinolone absorption is decreased with

A

sucralfate
antacid containing aluminum and magnesium
iron and zinc

94
Q

Antibiotic that can cause seizure

A

Fluoroquinolone

95
Q 
For UTI
Skin
Bone
Soft tissue
Respiratory tract infection
Prostatitis
STDs
Diarrhea due to Campylobacter, salmonella, shigella, e coli
A

Fluoroquinolone

96
Q

Fluoroquinolone examples

A

Ciprofloxacin
Levofloxacin
Norfloxacin
Ofloxacin

97
Q

Fluoroquinolone SE

A 
Cartilage erosion in children (early closure of epiphyseal plate) *
Tendonitis and tendon rupture in adults*
Photosensitivity
Headache and dizziness
Insomnia
Diarrhea, nausea
98
Q

Used as urinary antiseptic
Pregnancy Category B
Contraindicated at term

A

Nitrofurantoin

99
Q

Nitrofurantoin should not be given to nursing mothers because

A

it enters breast milk

discontinue

100
Q

DOC for Chagas disease

A

Nifurtimox

101
Q

Paul Ehrlich’s discovery of the antisyphilitic Salvarsan paved way for the creation of this drug

A

Sulfonamide

102
Q

Metabolism of prontosil (bright red dye) in vivo to sulfanilamide (active drug)

A

Sulfonamide

103
Q

Structural analog of PABA

Competes with this substrate for enzyme Dihydropteroate synthetase preventing the synthesis of bacterial folic acid

A

Sulfonamide

104
Q

Sulfonamide inhibits the enzyme

A

Pteridine synthetase or

Dihydropteroate synthetase

105
Q

Trimethoprim inhibits formation of tetrahydrofolic acid by inhibiting the enzyme

A

Dihydrofolate reductase

106
Q

Tetrahydrofolic acid is converted to

A

Thymidine
Purine
Methionine

107
Q

Methotrexate inhibits the enzyme

A

dihydrofolate reductase

108
Q

Sulfonamide inhibits the conversion of

A

P aminobenzoic acid to Pteridine

109
Q

Trimethroprim inhibits the conversion of

Via enzyme

A

Dihydrofolic acid to tetrahydrofolic acid

Dihydrofolate reductase

110
Q

Essential cofactor for formation of Thymidine, Purines and Methionine

A

Folic acid

111
Q

Well absorbed orally
Displaces substances bound to albumin (bilirubin, warfarin)

For gram positive and gram negative Nocardia, Chlamydia, E coli, Klebsiella; Enterobacter

A

Sulfonamide

112
Q

UTI sulfonamide

A

Sulfamethoxsazole

113
Q

Ulcerative Colitis

Crohn’s

A

Sulfasalazine

114
Q

Burn infection

A

Silver sulfadiazine

115
Q

Ocular infection

A

Sulfacetamide

116
Q

Nocardiosis drug of choice

A

Sulfisoxazole

117
Q

Toxoplasmosis

A

Sulfadiazine with pyrimethamine

118
Q

Treatment of first attack of urinary tract infection

A

Co trimoxazole

119
Q

In burn therapy to prevent and treat bacterial infection

A

Silver sulfadiazine

Mafenide

120
Q

Treatment of conjunctivitis

Superficial ocular infections

A

Sodium sulfacetamide

121
Q

Treatment of chloroquine resistant malaria

A

Quinine
Pyrimethamine
Sulfadoxime

122
Q

Quinine
Pyrimethamine
Sulfadoxime

123
Q

DOC for pneumocystis carinii

A

Cotrimoxazole

Alternative drug: Pentamidine

124
Q

Sulfonamide can

A

displace substances bound to albumin

125
Q

Adverse Effects of Sulfonamide

A 
Crystalluria
Hematuria
Rashes (SJS)
Anemia (hemolytic) in patients with G6PD 
Nausea and vomiting
Kernicterus
126
Q

Sulfonamide is contraindicated in pregnancy because

A

it crosses placenta and breast milk

127
Q

Drugs that most commonly cause SJS

A

Sulfonamide
Aromatic Anticonvulsant
Allopurinol

128
Q

Mechanism of action is similar to sulfonamide

129
Q

Used to treat leprosy

A

Dapsone

Methemoglobinemia
Hemolytic anemia G6PD

130
Q

Associated with methemoglobinemia and hemolytic anemia G6PD

Competes with PABA to prevent dihydrofolate reducatase

131
Q

Dihydrofolate reductase inhibitor

Given with sulfamethoxazole

A

Trimethoprim

132
Q

DOC for Pneumocystis carinii PCP

Also used in complicated UTI, bacterial prostatitis, gonorrhea, sinusitis, AOM, pneumonia

Also effective in chancroid, shigellosis, tyhphoid fever, Nocardiosis

A

Trimpethoprim

133
Q

Trimethoprim SE

A

Leukopenia
Megaloblastic anemia
Granulocytopenia

134
Q

Severe hypoxemia in immunocompromised

A

Pneumocystis carinii

135
Q

prophylaxis for PCP is given if CD4 count is

136
Q

Prophylaxis for MAC is given is CD4 is

137
Q

Drugs CI in G6PD

A

Sulfonamides

Anti malarials

138
Q

Drugs that induce SLE

A

Hydralazine
Isoniazid
Methyldopa
Procainamide

139
Q

Confer antibiotic resistance

A

Bacterial plasmids

140
Q

Cidal = kills
Cell wall synthesis inhibitors
Narrow spectrum

A

Bactericidal

141
Q

Static inhibits growth
Protein synthesis inhibitors
Broad spectrum

A

Bacteriostatic

142
Q

Cell wall synthesis inhibitors

A

Penicillin
Cephalosporin
Carbapenem
Monobactam

143
Q

Aminoglycoside contraindicated in pregnancy:

A

Streptomycin

144
Q

Aminoglycoside is CI in patients with

A

Myesthenia gravis

145
Q

Tetracycline CI

A

Pregnant

Children under 8

146
Q

Erythromycin

A

Inbibits CYP450

Inc theophylline, digoxin

147
Q

C difficile drugs

A

Clindamycin
Ampicillin/Amoxicillin
Cephalosporin
Quinolone

148
Q

Meningococcemia

A

First line: rifampicin

Second line: ciprofloxacin

149
Q

Sulfonamide used to treat malaria

A

Fansidar (Sulfadoxine + Pyrimethamine)

150
Q

Sulfonamide SE

A 
Crystalluria hematuria
SJS
Anemia (hemolytic) in G6PD
Nausea and vomiting
Kernicterus
Crosses placenta and breast milk - contraindicated
151
Q

Loss of eyebrows, collapsed nasal bridge, aesthetic patches

Erythema nodosum leprosum and multibacillary leprosy

A

Leprosy

Give rifampin, dapsone, clofazimine

Pharma (26 decks)

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