Antibiotics/Antifungals/Antivirals Flashcards

(126 cards)

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
Virus associated with Merkel cell carcinoma
Polyomavirus
26
Virus associated with primary CNS lymphoma
EBV
27
Virus associated with squamous cell anal cancer
HPV
28
Mechanism of action of echinocandins
Inhibits B-1, 3-D-glucan synthesis
29
Mechanism of action of polyenes (amphotericin B, nystatin)
Bind to membrane ergosterol, altering membrane integrity
30
Mechanism of imidazoles (ketoconazole) and triazoles (fluconazole, itraconazole)
Inhibits CYP450 enzyme lanosterol14 demethylase, results in decreased ergosterol production
31
Mechanism of action of terbinafine
Inhibits squalene epoxidase with resultant decrease in lanosterol and ergosterol production
32
Mechanism of action of griseofulvin
Inhibits fungal mitosis by binding to intracellular microtubular protein
33
Mechanism of action of 5-flucytosine
Converted to 5-fluorouracil, incorporated into fungal RNA inhibiting protein synthesis
34
Mechanism of action of B lactams
Binds to penicillin-binding-proteins --> decreases crosslinking of peptidoglycan layer
35
Examples of B lactam
Penicillin Cephalosporins Carbapenems Monobactams
36
Generations of beta lactams
1st - cephalexin 2nd - cefaclor 3rd - cefixime 4th - cefepime 5th - ceftaroline
37
Mechanism of resistance for beta lactams
Cleavage of beta lactam ring by beta-lactamases
38
Mechanism of resistance for MRSA
PBP mutations
39
Mechanism of action for glycopeptides e.g. vancomycin, teicoplanin
Bind to D-alanyl-D-alanine section of peptidoglycan precursor --> inhibited peptidoglycan synthesis
40
Mechanism of resistance of vancomycin
Reduced penetration in gram negative bacteria Change in peptidoglycan precursor structure
41
Mechanism of action for fosfomycin
Inactivate enolpyruvate transferase --> inhibition of N-acetylmuramic acid formation --> disruption of peptidoglycan synthesis
42
Adverse effects of carbapenems
Secondary fungal infections CNS toxicity - highest risks of imipenem GI upset Rash Thrombophlebitis
43
Adverse effects of cephalosporins
Potential cross-reactivity in pts with penicillin allergies AIHA Vitamin K deficiency Disulfiram-like reaction Increases nephrotoxic effect of aminoglycosides Neurotoxicity
44
Mechanism of action of aminoglycosides
Inhibits protein synthesis - 30S ribosomal subunit
45
Mechanism of resistance of aminoglycosides
Inactivating enzymes e.g. acetylation, phosphorylation, adenylation Removal by efflux pumps Mutation of bacterial ribosome binding site Reduced penetrance Anaerobic bacteria Acidic environment
46
Mechanism of action of tetracycline
Inhibition of protein synthesis - 30S ribosomal subunit Block incoming aminoacyl-tRNA with amino acids --> decrease protein synthesis
47
Mechanism of resistance of tetracycline
Reduced cell wall penetration Removal by efflux pump Production of protein that protects ribosome
48
Clinical use of daptomycin
Gram positive bacteria S. aureus especially MRSA VRE
49
Adverse effects of daptomycin
Reversible myopathy Rhabdomyolysis Allergic pneumonitis
50
Clinical use of colistin
Polymyxin Severe gram negative bacteria that are multidrug resistant
51
Adverse effects of colistin
Nephrotoxicity Neurotoxicity Urticaria, eosinophilia and/or anaphylactoid reactions Respiratory failure
52
Adverse effects of aminoglycosides
Nephrotoxicity Ototoxicity and vestibulotoxicity NM blockade Teratogenecity
53
Contraindications of aminoglycoside
MG Botulism Pregnancy
54
Clinical use of tetracyclines
Bacteria that lack cell wall i.e. Mycoplasma Intracelluar bacteria i.e. Rickettsia, Chlamydia, Anaplasma Borrelia burgdorferi
55
Adverse effects of tetracyclines
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
Mechanism of action of macrolides
Bind to 23S rRNA --> inhibition of transpeptidation, translocation and chain elongation --> decrease protein synthesis
57
Mechanism of resistance of macrolides
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
Mechanism of clindamycin
Impair transpeptidation --> inhibition of chain elongation --> decrease protein synthesis Increase opsonisation and phagocytosis Inhibits alpha toxin expression
59
Mechanism of resistance of clindamycin
Reduced penetration Mutation of bacterial ribosome binding site
60
Mechanism of action of oxazolidinones i.e. linezolid
Prevents association of 50S with 30S subunit --> impairment of initiation complex formation --> early interruption of protein synthesis
61
Mechanism of resistance of oxazolidinones
Point mutation of 23S rRNA Methylation of ribosomal subunit
62
Mechanism of action of chloramphenicol
Prevent binding of amino acid-containing aminoacyl-tRNA --> inhibition of peptidyltransferase --> reduce protein synthesis
63
Mechanism of resistance of chloramphenicol
Reduced penetration Enzymatic inactivation by acetyltransferase (plasmid encoded)
64
Mechanism of action of fluoroquinolones i.e. ciprofloxacin, norfloxacin
Inhibit prokaryotic toposiomerase II (DNA gyrase) and topoisomerase IV --> inhibited DNA synthesis
65
Mechanism of resistance of fluoroquinolones
Mutations in DNA gyrase and topoisomerase IV Reduced cell wall permeability Efflux pumps (plasmid-encoded resistance)
66
Mechanism of action of metronidazole
Disruption of DNA integrity via free radical formation
67
Mechanism of resistance of metronidazole
Reduced activation due to decreased enzymatic activity
68
Mechanism of action of rifamycins (rifampin, rifabutin, rifaximin)
Blocks mRNA synthesis via inhibition of bacterial DNA-dependent RNA-polymerase --> reduce protein synthesis
69
Mechanism of resistance of rifamycins
Mutated RNA-polyermase --> reduce binding of rifamycins
70
Mechanism of action of isoniazid
Inhibits mycolic acid synthesis --> reduce cell wall synthesis
71
Mechanism of resistance of isoniazid
Mutation causing reduce KatG --> reduce expression of catalase-peroxidase
72
Mechanism of resistance of pyrazinamide
Mutations in RpsA gene coding for ribosomal protein S1
73
Mutation of action of ethambutol
Inhibits arabinosyltransferase --> reduce cell wall synthesis
74
Mechanism of resistance of ethambutol
Mutations in EmbCAB gene coding for arabinosyltransferase --> inability of drug to inhibit enzyme
75
Mechanism of action of dapsone
Competitive antagonism of para-aminobenzoic acid --> inhibited dihydrofolic acid synthesis
76
Mechanism of resistance of dapsone
Mutations in folP1 gene coding for dihydropteroate synthase --> reduced expression of dihydroteroate synthase
77
Mechanism of action of nitrofurantoin
Bind to bacterial ribosomes --> inhibition of DNA, RNA, and protein synthesis
78
Mechanism of resistance of nitrofurantoin
Enzyme-mediated reduction Efflux pumps
79
Clinical use of tigecycline
Gram positive aerobes MRSA VRE Anaerobes (broad spectrum) Partially effective against gram-negative aerobes
80
Adverse effects of tigecycline
GI upset Hepatotoxicity Deposition in bones and teeth Photosensitivity
81
Adverse effects of macrolides
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
Drug reactions of macrolides
Enhances effect of oral anticoagulants Erythromycin and clarithromycin - increased theophylline serum concentrations, CYP3A4 inhibition
83
Antibiotics associated with pseudomembranous colitis
Clindamycin Fluoroquinolones 3rd and 4th generation cephalosporins
84
Adverse effects of clindamycin
GI upset Pseudomembranous colitis Fever Teratogenicity
85
Adverse effects of oxazolidinones I.e. linezolid
GI upset Pancytopenia due to BM suppression Peripheral neuropathy Serotonin syndrome - partially inhibits monoamine oxidase
86
Generations of fluoroquinolones
1st - nalidixic acid 2nd - norfloxacin, ciprofloxacin, ofloxacin 3rd - levofloxacin 4th - moxifloxacin, gemifloxacin
87
Adverse effects of fluoroquinolones
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
Adverse effects of metronidazole
Headache Disulfiram-like reaction Metallic taste Peripheral neuropathy (prolonged used) Vestibular dysfunction
89
Mechanism of action of diaminopyrimidine e.g. amifampridine
Inhibits dihydrofolate reductase Uses NADPH to reduce dihydrofolate acid to tetrahydrofolic acid Used to treat congenital myasthenia syndromes and LEMS
90
Mechanism of action of sulfonamides e.g. sulfomethoxazole
Inhibits dihydropteroate synthase
91
Adverse effects of sulfonamides
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
Adverse effects of diaminopyrimidine derivatives
Megaloblastic anaemia Leukopenia, granulocytopenia Hyperkalaemia Increased creatinine - caused by decreased tubular secretion
93
Adverse effects of nitrofurantoin
Nitrofurantoin induced lung disease Pulmonary fibrosis Haemolytic anaemia GI upset Reversible peripheral neuropathy
94
Adverse effects of rifampicin
Red-orange discolouration of body fluids Flu-like symptoms Minor hepatotoxicity CYP450 induction False positive urine opiate screening
95
Adverse effects of isoniazid
Hepatotoxicty Anion gap metabolic acidosis Drug induced lupus erythematous Benzo-refractory seizures Vitamin B6 deficiency - peripheral neuropathy, sideroblastic anaemia, aplastic anaemia, thrombocytopenia, pellagra
96
Adverse effects of pyrazinamide
Hyperuricaemia Hepatotoxicity
97
Adverse effects of ethambutol
Optic neuropathy Hyperuricaemia
98
Adverse effects of dapsone
Methemoglobinemia Haemolytic anaemia in G6Pd deficiency Agranulocytosis GI upset Peripheral neuropathy
99
Mechanism of action of interferon alfa and -a
Antiviral and immunomodulatory effect via intercellular and intracellular mechanisms
100
Adverse effects of pegylated interferon alfa and -a
Flu like symptoms BM suppression CNS - depressive mood, seizures Induction of autoantibodies Myopathy
101
Mechanism of action of tenofovir
Nucleoside analogue - premature termination of DNA transcription via phosphorylation to triphosphate in hepatic cells
102
Adverse effects of tenofovir/adefovir
Nephrotoxicity Headache and abdominal pain
103
Mechanism of action of entecavir, lamivudine, telbivudine
Nucleoside analogue - inhibition of reverse transcriptase
104
Adverse effects of entecavir, lamivudine, telbivudine
GI symptoms Fever Headache Vasculitides Neuropathies Neutropenia Lactic acidosis
105
Aciclovir, valaciclovir relationship
Valaciclovir is prodrug of aciclovir Has greater oral bioavailability
106
Penciclovir, famciclovir relationship
Famciclovir is prodrug of penciclovir with greater bioavailability
107
Mechanism of action of aciclovir, valaciclovir, penciclovir, famciclovir
Guanosine analogue Phosphylated drug is incorporated into replicating viral DNA strand --> inhibition of viral DNA polymerase via chain termination
108
Adverse reaction of aciclovir
Obstructive crystal-induced nephropathy AKI TTP GI symptoms Increases transminases
109
Mechanism of action of ganciclovir, valganciclovir
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
Adverse effects of ganciclovir, valganciclovir
Myelotoxicity Nephrotoxicity GI symptoms CNS - headache, confusion, parasthesias
111
Mechanism of action of foscarnet
Pyrophosphate analogue
112
Adverse effects of foscarnet
Nephrotoxicity GI symptoms CNS - headache, confusion, seizures due to electrolyte abnormalities, parasthesias Haemotological abnormalities - leukopenia, neutropenia
113
Mechanism of action of amantadine
M2 ion channel blocker Weak NMDA receptor antagonist
114
Adverse effects of amantadine
Neurological - ataxia, anxiety GI - nausea, vomiting Livedo reticularis Peripheral oedema
115
Mechanism of action of oseltamivir
Neuraminidase inhibitor
116
Adverse effects of oseltamivir
Pulmonary - URTI GI - nausea, vomiting Headache
117
Mechanism of action of ketoconazole
Inhibits 17a-hydroxylase/17,20-lyase
118
Adverse effects of amphotericin B
Arrhythmias Nephrotoxicity Fever, chills IV phlebitis Hypokalaemia, hypomagnesemia
119
Adverse effects of nystatin
GI symptoms Contact dermatitis SJS
120
Adverse effects of azoles
Hepatotoxicity CYP450 inhibition Local burning sensation Gynaecomastia - ketoconazole
121
Adverse effects of terbinafine
Headache Hepatotoxicity Dysgeusia GI upset
122
Adverse effects of echinocandins
Flushing Hepatotoxicity GI upset
123
Adverse effects of griseofulvin
Hepatotoxicity Carcinogenic Teratogenic CYP450 induction Confusion, headaches Disulfarim-like reactions
124
Adverse effects of flucytosine
BM suppression Hepatic injury Renal failure
125
Which antibiotics do not cross the blood brain barrier?
Aminoglycosides Erythromycin Tetracyclines Clindamycin First generation cephalosporins
126
Carbapenems are inactive against which bacteria
MRSA VRE Enterococcus faecium Mycoplasma Chlamydia Stenotrophonomas maltophilia