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BPT Flashcards > Antibiotics/Antifungals/Antivirals > Flashcards

Antibiotics/Antifungals/Antivirals Flashcards

1
Q

Cell wall inhibitors

A

Penicillins
Cephalosporins
Carbapenems
Vancomycin
Bacitracin
Fosfomycin
Isoniazid

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2
Q

Acts on cell membrane

A

Polymyxins
Daptomycin

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3
Q

Antibiotics that inhibits DNA replication and transcription

A

Quinolones

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4
Q

Inhibits RNA polymerase

A

Rifampin

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5
Q

Acts on 50S subunit

A

Erythromycin
Clindamycin
Synercid
Pleuromutilins

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6
Q

Acts on 30S subunit

A

Aminoglycosides - gentamycin, streptomycin
Tetracycline
Glycylcyclines

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7
Q

Acts on both 30S and 50S

A

Linezolid

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8
Q

Acts on folic acid synthesis in cytoplasm

A

Sulfonamides
Trimethoprim

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9
Q

Mechanism of action of meropenem

A

Binds penicillin binding protein to inhibit cell wall synthesis

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10
Q

Mechanism of action of ciprofloxacin

A

Inhibits DNA topoisomerase

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11
Q

Mechanism of action of trimethoprim

A

Disruption of dihydrofolate reductase

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12
Q

Mechanism of action of erythromycin

A

Inhibition of translocation of tRNA at 50S ribosomal subunit

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13
Q

Mechanism of action of rifampicin

A

Inhibits DNA-dependent RNA-polymerase

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14
Q

Mechanism of action of colistin

A

Disruption of cell membrane via LPS and phospholipids

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15
Q

Mechanism of action of sulfamethoxazole

A

Inhibition of de novo folate biosynthesis

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16
Q

Mechanism of action of doxycycline

A

Competition with A site on 50S ribosomal subunit

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17
Q

Mechanism of resistance of VRE

A

Modification of drug target
van gene

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18
Q

Mechanism of aminoglycoside E. coli resistance

A

Enzymatic alterations of binding site

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19
Q

Mechanism of ESBL

A

Beta lactamases
Destruction of antibiotics

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20
Q

Mechanism of staph aureus with intermediate sensitivity to vancomycin

A

Global cell adaptation to antibiotic effects

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21
Q

Mechanism of action of entecavir

A

Guanosine analogue phosphorylated within virally infected cells into triphosphate that then incorporates into viral DNA - halts replication process

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22
Q

Mechanism of action of famciclovir

A

Guanosine derivative phosphorylated within virally infected cells to triphosphate that inhibits DNA polymerase

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23
Q

Mechanism of action of ritonavir

A

Inhibition of viral protease

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24
Q

Virus associated Kaposi’s sarcoma

A

HHV-8

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25
Q

Virus associated with Merkel cell carcinoma

A

Polyomavirus

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26
Q

Virus associated with primary CNS lymphoma

A

EBV

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27
Q

Virus associated with squamous cell anal cancer

A

HPV

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28
Q

Mechanism of action of echinocandins

A

Inhibits B-1, 3-D-glucan synthesis

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29
Q

Mechanism of action of polyenes (amphotericin B, nystatin)

A

Bind to membrane ergosterol, altering membrane integrity

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30
Q

Mechanism of imidazoles (ketoconazole) and triazoles (fluconazole, itraconazole)

A

Inhibits CYP450 enzyme lanosterol14 demethylase, results in decreased ergosterol production

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31
Q

Mechanism of action of terbinafine

A

Inhibits squalene epoxidase with resultant decrease in lanosterol and ergosterol production

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32
Q

Mechanism of action of griseofulvin

A

Inhibits fungal mitosis by binding to intracellular microtubular protein

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33
Q

Mechanism of action of 5-flucytosine

A

Converted to 5-fluorouracil, incorporated into fungal RNA inhibiting protein synthesis

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34
Q

Mechanism of action of B lactams

A

Binds to penicillin-binding-proteins –> decreases crosslinking of peptidoglycan layer

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35
Q

Examples of B lactam

A

Penicillin
Cephalosporins
Carbapenems
Monobactams

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36
Q

Generations of beta lactams

A

1st - cephalexin
2nd - cefaclor
3rd - cefixime
4th - cefepime
5th - ceftaroline

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37
Q

Mechanism of resistance for beta lactams

A

Cleavage of beta lactam ring by beta-lactamases

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38
Q

Mechanism of resistance for MRSA

A

PBP mutations

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39
Q

Mechanism of action for glycopeptides e.g. vancomycin, teicoplanin

A

Bind to D-alanyl-D-alanine section of peptidoglycan precursor –> inhibited peptidoglycan synthesis

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40
Q

Mechanism of resistance of vancomycin

A

Reduced penetration in gram negative bacteria
Change in peptidoglycan precursor structure

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41
Q

Mechanism of action for fosfomycin

A

Inactivate enolpyruvate transferase –> inhibition of N-acetylmuramic acid formation –> disruption of peptidoglycan synthesis

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42
Q

Adverse effects of carbapenems

A

Secondary fungal infections
CNS toxicity - highest risks of imipenem
GI upset
Rash Thrombophlebitis

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43
Q

Adverse effects of cephalosporins

A

Potential cross-reactivity in pts with penicillin allergies
AIHA
Vitamin K deficiency
Disulfiram-like reaction
Increases nephrotoxic effect of aminoglycosides
Neurotoxicity

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44
Q

Mechanism of action of aminoglycosides

A

Inhibits protein synthesis - 30S ribosomal subunit

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45
Q

Mechanism of resistance of aminoglycosides

A

Inactivating enzymes e.g. acetylation, phosphorylation, adenylation
Removal by efflux pumps
Mutation of bacterial ribosome binding site
Reduced penetrance
Anaerobic bacteria
Acidic environment

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46
Q

Mechanism of action of tetracycline

A

Inhibition of protein synthesis - 30S ribosomal subunit
Block incoming aminoacyl-tRNA with amino acids –> decrease protein synthesis

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47
Q

Mechanism of resistance of tetracycline

A

Reduced cell wall penetration
Removal by efflux pump
Production of protein that protects ribosome

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48
Q

Clinical use of daptomycin

A

Gram positive bacteria
S. aureus especially MRSA
VRE

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49
Q

Adverse effects of daptomycin

A

Reversible myopathy
Rhabdomyolysis
Allergic pneumonitis

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50
Q

Clinical use of colistin

A

Polymyxin
Severe gram negative bacteria that are multidrug resistant

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51
Q

Adverse effects of colistin

A

Nephrotoxicity
Neurotoxicity
Urticaria, eosinophilia and/or anaphylactoid reactions
Respiratory failure

52
Q

Adverse effects of aminoglycosides

A

Nephrotoxicity
Ototoxicity and vestibulotoxicity
NM blockade
Teratogenecity

53
Q

Contraindications of aminoglycoside

A

MG
Botulism
Pregnancy

54
Q

Clinical use of tetracyclines

A

Bacteria that lack cell wall i.e. Mycoplasma
Intracelluar bacteria i.e. Rickettsia, Chlamydia, Anaplasma
Borrelia burgdorferi

55
Q

Adverse effects of tetracyclines

A

Hepatotoxicity
Deposition in bones and teeth –> inhibition of bone growth and discolouration of teeth
Damage to mucous membranes i.e. oesophagitis
Photosensitivity
Fanconi syndrome
Pseudotumour cerebri

56
Q

Mechanism of action of macrolides

A

Bind to 23S rRNA –> inhibition of transpeptidation, translocation and chain elongation –> decrease protein synthesis

57
Q

Mechanism of resistance of macrolides

A

Reduced penetration
Efflux pumps
Methylation of 23S rRNA binding site –> inhibits binding of macrolides
Cross-resistance with clindamycin and streptogramins
Mutation of bacterial ribosome binding site

58
Q

Mechanism of clindamycin

A

Impair transpeptidation –> inhibition of chain elongation –> decrease protein synthesis
Increase opsonisation and phagocytosis
Inhibits alpha toxin expression

59
Q

Mechanism of resistance of clindamycin

A

Reduced penetration
Mutation of bacterial ribosome binding site

60
Q

Mechanism of action of oxazolidinones i.e. linezolid

A

Prevents association of 50S with 30S subunit –> impairment of initiation complex formation –> early interruption of protein synthesis

61
Q

Mechanism of resistance of oxazolidinones

A

Point mutation of 23S rRNA
Methylation of ribosomal subunit

62
Q

Mechanism of action of chloramphenicol

A

Prevent binding of amino acid-containing aminoacyl-tRNA –> inhibition of peptidyltransferase –> reduce protein synthesis

63
Q

Mechanism of resistance of chloramphenicol

A

Reduced penetration
Enzymatic inactivation by acetyltransferase (plasmid encoded)

64
Q

Mechanism of action of fluoroquinolones i.e. ciprofloxacin, norfloxacin

A

Inhibit prokaryotic toposiomerase II (DNA gyrase) and topoisomerase IV –> inhibited DNA synthesis

65
Q

Mechanism of resistance of fluoroquinolones

A

Mutations in DNA gyrase and topoisomerase IV
Reduced cell wall permeability
Efflux pumps (plasmid-encoded resistance)

66
Q

Mechanism of action of metronidazole

A

Disruption of DNA integrity via free radical formation

67
Q

Mechanism of resistance of metronidazole

A

Reduced activation due to decreased enzymatic activity

68
Q

Mechanism of action of rifamycins (rifampin, rifabutin, rifaximin)

A

Blocks mRNA synthesis via inhibition of bacterial DNA-dependent RNA-polymerase –> reduce protein synthesis

69
Q

Mechanism of resistance of rifamycins

A

Mutated RNA-polyermase –> reduce binding of rifamycins

70
Q

Mechanism of action of isoniazid

A

Inhibits mycolic acid synthesis –> reduce cell wall synthesis

71
Q

Mechanism of resistance of isoniazid

A

Mutation causing reduce KatG –> reduce expression of catalase-peroxidase

72
Q

Mechanism of resistance of pyrazinamide

A

Mutations in RpsA gene coding for ribosomal protein S1

73
Q

Mutation of action of ethambutol

A

Inhibits arabinosyltransferase –> reduce cell wall synthesis

74
Q

Mechanism of resistance of ethambutol

A

Mutations in EmbCAB gene coding for arabinosyltransferase –> inability of drug to inhibit enzyme

75
Q

Mechanism of action of dapsone

A

Competitive antagonism of para-aminobenzoic acid –> inhibited dihydrofolic acid synthesis

76
Q

Mechanism of resistance of dapsone

A

Mutations in folP1 gene coding for dihydropteroate synthase –> reduced expression of dihydroteroate synthase

77
Q

Mechanism of action of nitrofurantoin

A

Bind to bacterial ribosomes –> inhibition of DNA, RNA, and protein synthesis

78
Q

Mechanism of resistance of nitrofurantoin

A

Enzyme-mediated reduction
Efflux pumps

79
Q

Clinical use of tigecycline

A

Gram positive aerobes
MRSA
VRE
Anaerobes (broad spectrum)
Partially effective against gram-negative aerobes

80
Q

Adverse effects of tigecycline

A

GI upset
Hepatotoxicity
Deposition in bones and teeth
Photosensitivity

81
Q

Adverse effects of macrolides

A

Increased intestinal motility –> GI upset
QT interval prolongation
Acute cholestatic hepatitis
Eosinophilia
Rash
Increased risk of hypertrophic pylroic stenosis in infants up to 6 weeks og ageD

82
Q

Drug reactions of macrolides

A

Enhances effect of oral anticoagulants
Erythromycin and clarithromycin - increased theophylline serum concentrations, CYP3A4 inhibition

83
Q

Antibiotics associated with pseudomembranous colitis

A

Clindamycin
Fluoroquinolones
3rd and 4th generation cephalosporins

84
Q

Adverse effects of clindamycin

A

GI upset
Pseudomembranous colitis
Fever
Teratogenicity

85
Q

Adverse effects of oxazolidinones I.e. linezolid

A

GI upset
Pancytopenia due to BM suppression
Peripheral neuropathy
Serotonin syndrome - partially inhibits monoamine oxidase

86
Q

Generations of fluoroquinolones

A

1st - nalidixic acid
2nd - norfloxacin, ciprofloxacin, ofloxacin
3rd - levofloxacin
4th - moxifloxacin, gemifloxacin

87
Q

Adverse effects of fluoroquinolones

A

GI upset
Neurological symptoms - mild headache, dizziness, mood changes, peripheral neuropathy, lowers seizure threshold
Hyper/hypoglycaemia
QT prolongation
Photosensitivity
Skin rash
Superinfection
Muscle ache, leg cramps, tendinitis, tendon rupture

88
Q

Adverse effects of metronidazole

A

Headache
Disulfiram-like reaction
Metallic taste
Peripheral neuropathy (prolonged used)
Vestibular dysfunction

89
Q

Mechanism of action of diaminopyrimidine e.g. amifampridine

A

Inhibits dihydrofolate reductase
Uses NADPH to reduce dihydrofolate acid to tetrahydrofolic acid
Used to treat congenital myasthenia syndromes and LEMS

90
Q

Mechanism of action of sulfonamides e.g. sulfomethoxazole

A

Inhibits dihydropteroate synthase

91
Q

Adverse effects of sulfonamides

A

Drug interactions due to CYP450 inhibition
Displacement of other drugs from albumin
Nephrotoxicity esp. ATN
GI upset
Hyperkalaemia
Agranulocytosis
Aplastic anaemia, thrombocytopenia, pancytopenia
Haemolytic anaemia in G6PD-deficient patients
SJS
Hypersensitivity reactions
Photosensitivity
Fever

92
Q

Adverse effects of diaminopyrimidine derivatives

A

Megaloblastic anaemia
Leukopenia, granulocytopenia
Hyperkalaemia
Increased creatinine - caused by decreased tubular secretion

93
Q

Adverse effects of nitrofurantoin

A

Nitrofurantoin induced lung disease
Pulmonary fibrosis
Haemolytic anaemia
GI upset
Reversible peripheral neuropathy

94
Q

Adverse effects of rifampicin

A

Red-orange discolouration of body fluids
Flu-like symptoms
Minor hepatotoxicity
CYP450 induction
False positive urine opiate screening

95
Q

Adverse effects of isoniazid

A

Hepatotoxicty
Anion gap metabolic acidosis
Drug induced lupus erythematous
Benzo-refractory seizures
Vitamin B6 deficiency - peripheral neuropathy, sideroblastic anaemia, aplastic anaemia, thrombocytopenia, pellagra

96
Q

Adverse effects of pyrazinamide

A

Hyperuricaemia
Hepatotoxicity

97
Q

Adverse effects of ethambutol

A

Optic neuropathy
Hyperuricaemia

98
Q

Adverse effects of dapsone

A

Methemoglobinemia
Haemolytic anaemia in G6Pd deficiency
Agranulocytosis
GI upset
Peripheral neuropathy

99
Q

Mechanism of action of interferon alfa and -a

A

Antiviral and immunomodulatory effect via intercellular and intracellular mechanisms

100
Q

Adverse effects of pegylated interferon alfa and -a

A

Flu like symptoms
BM suppression
CNS - depressive mood, seizures
Induction of autoantibodies
Myopathy

101
Q

Mechanism of action of tenofovir

A

Nucleoside analogue - premature termination of DNA transcription via phosphorylation to triphosphate in hepatic cells

102
Q

Adverse effects of tenofovir/adefovir

A

Nephrotoxicity
Headache and abdominal pain

103
Q

Mechanism of action of entecavir, lamivudine, telbivudine

A

Nucleoside analogue - inhibition of reverse transcriptase

104
Q

Adverse effects of entecavir, lamivudine, telbivudine

A

GI symptoms
Fever
Headache
Vasculitides
Neuropathies
Neutropenia
Lactic acidosis

105
Q

Aciclovir, valaciclovir relationship

A

Valaciclovir is prodrug of aciclovir
Has greater oral bioavailability

106
Q

Penciclovir, famciclovir relationship

A

Famciclovir is prodrug of penciclovir with greater bioavailability

107
Q

Mechanism of action of aciclovir, valaciclovir, penciclovir, famciclovir

A

Guanosine analogue
Phosphylated drug is incorporated into replicating viral DNA strand –> inhibition of viral DNA polymerase via chain termination

108
Q

Adverse reaction of aciclovir

A

Obstructive crystal-induced nephropathy
AKI
TTP
GI symptoms
Increases transminases

109
Q

Mechanism of action of ganciclovir, valganciclovir

A

Guanosine analogue
Phosphorylation to 5’ monophosphate by CMV coded UL97 kinase –> further phosphorylation to triphosphate by cellular kinases
Inhibition of viral DNA polymerase –> termination of viral DNA synthesis

110
Q

Adverse effects of ganciclovir, valganciclovir

A

Myelotoxicity
Nephrotoxicity
GI symptoms
CNS - headache, confusion, parasthesias

111
Q

Mechanism of action of foscarnet

A

Pyrophosphate analogue

112
Q

Adverse effects of foscarnet

A

Nephrotoxicity
GI symptoms
CNS - headache, confusion, seizures due to electrolyte abnormalities, parasthesias
Haemotological abnormalities - leukopenia, neutropenia

113
Q

Mechanism of action of amantadine

A

M2 ion channel blocker
Weak NMDA receptor antagonist

114
Q

Adverse effects of amantadine

A

Neurological - ataxia, anxiety
GI - nausea, vomiting
Livedo reticularis
Peripheral oedema

115
Q

Mechanism of action of oseltamivir

A

Neuraminidase inhibitor

116
Q

Adverse effects of oseltamivir

A

Pulmonary - URTI
GI - nausea, vomiting
Headache

117
Q

Mechanism of action of ketoconazole

A

Inhibits 17a-hydroxylase/17,20-lyase

118
Q

Adverse effects of amphotericin B

A

Arrhythmias
Nephrotoxicity
Fever, chills
IV phlebitis
Hypokalaemia, hypomagnesemia

119
Q

Adverse effects of nystatin

A

GI symptoms
Contact dermatitis
SJS

120
Q

Adverse effects of azoles

A

Hepatotoxicity
CYP450 inhibition
Local burning sensation

Gynaecomastia - ketoconazole

121
Q

Adverse effects of terbinafine

A

Headache
Hepatotoxicity
Dysgeusia
GI upset

122
Q

Adverse effects of echinocandins

A

Flushing
Hepatotoxicity
GI upset

123
Q

Adverse effects of griseofulvin

A

Hepatotoxicity
Carcinogenic
Teratogenic
CYP450 induction
Confusion, headaches
Disulfarim-like reactions

124
Q

Adverse effects of flucytosine

A

BM suppression
Hepatic injury
Renal failure

125
Q

Which antibiotics do not cross the blood brain barrier?

A

Aminoglycosides
Erythromycin
Tetracyclines
Clindamycin
First generation cephalosporins

126
Q

Carbapenems are inactive against which bacteria

A

MRSA
VRE
Enterococcus faecium
Mycoplasma
Chlamydia
Stenotrophonomas maltophilia

BPT Flashcards (32 decks)

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