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MODA > Chemotherapy: Antibiotics > Flashcards

Chemotherapy: Antibiotics Flashcards

1
Q

D-cycloserine

A

Inhibits cell wall biosynthesis
Structural analogue of D-Ala; prevents synthesis of pentapeptide by inhibiting L-Ala racemase, D-Ala-D-Ala synthetase and D-Ala-D-Ala/ muramyl tripetide ligase

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2
Q

Fosfomycin

Used in treatment of?

A

Inhibits cell wall biosynthesis
Inhibits puruvyl transferase required for conversion of NAG into NAM
Treatment of UTI

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3
Q

Bacitracin

Active against Gram positive or gram negative?

A

Inhibits cell wall biosynthesis
Cyclic polypeptide
Forms a tight complex with Mg2+ and bactoprenol pyrophoasphate; inhibits dephosphorylation to bactoprenol phosphate (lipid carrier for NAM-NAG unit)
Active against Gram-positive bacteria

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4
Q

Penicillin

A

Inhibits cell wall biosynthesis
beta-lactam antibiotic
Inhibits peptidoglycan-crosslinking transpeptidase enzymes by covalent & irreversible binding as a pseudosubstrate.

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5
Q

Ampicillin

A

Inhibits cell wall biosynthesis
beta-lactam antibiotic
Inhibits peptidoglycan-crosslinking transpeptidase enzymes by covalent & irreversible binding as a pseudosubstrate.

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6
Q

Amoxicillin

A

Inhibits cell wall biosynthesis
beta-lactam antibiotic
Inhibits peptidoglycan-crosslinking transpeptidase enzymes by covalent & irreversible binding as a pseudosubstrate.

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7
Q

Methicillin

A

Inhibits cell wall biosynthesis
beta-lactam antibiotic
Inhibits peptidoglycan-crosslinking transpeptidase enzymes by covalent & irreversible binding as a pseudosubstrate.

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8
Q

Clavulanate

A

beta-lactamase inhibitor

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9
Q

Augmentin

A

Combination of amoxicillin and clavulanate

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10
Q

Vancomycin

Used to treat which bacteria?

A

Inhibits cell wall biosynthesis
Glycopeptide antibiotic
Binds D-Ala-D-Ala termini of the pentapeptide in peptidoglycan- preventing its cross-linking to another peptidoglycan strand.
Effective against clostridium difficile, used intravenously against gram positive cocci e.g enterococcus, staphylococcus

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11
Q

Isoniazid

A

Inhibits biosynthesis of mycolic acids in cell envelope of Mycobacterium Tuberculosis
Used in prevention and treatment of TB

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12
Q

Chloramphenicol

Uses?

A

Acts on protein synthesis
Blocks aminoacyl tRNA binding to 50S subunit of ribosome
V effective broad spectrum antibiotic but use restricted due to bone marrow suppression in some cases. Indicated in e.g meningitis

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13
Q

Tetracycline

Used against?
Side effects?

A

Acts on protein synthesis
Polyketide antibiotic
Binds to 16rRNA in 30S subunit of ribosome, inhibits mvt of amino-acyl tRNA into A site.
Effective against a wide range of bacteria, including mycoplasma and cholera.
Toxicity associated with binding of calcium in bones and teeth.

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14
Q

Erythromycin

Spectrum/ uses?

A

Acts on protein synthesis
14-membered macrolide antibiotic
Binds to 23SrRNA in 50S subunit, and blocks polypeptide exit tunnel.
Similar antibacterial spectrum as penicillin, used as second-line drug for patients allergic to penicillin.

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15
Q

Fusidic acid

Spectrum?

A

Acts on protein synthesis
Inhibits elongation factor G- and hence the movement of 30S subunit by one unit along the mRNA
Narrow spectrum, used against staphylococcal infections

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16
Q

Streptomycin

Side effects?
Used against?

A

Acts on protein synthesis
Aminoglycoside antibiotic
Target 30S subunit of ribosome & decrease fidelity of mRNA translation.
Exhibits nephrotoxicity and ototoxicity
Used against gram negative rods: e.g pseudomanas, proteus

17
Q

Gentamycin

Side effects?
Used against?
Interaction with penicillin?

A

Acts on protein synthesis
Aminoglycoside antibiotic
Target 30S subunit of ribosome & decrease fidelity of mRNA translation.
Less nephrotoxicity & ototoxicity than streptomycin
Used vs gram -ve rods: e.g Pseudomanas, Proteus
Most streptococci (gram +ve) are resistant because cannot penetrate the cell
Synergistic effect against some streptococci with penicillin.

18
Q

Ciprofloxacin

Uses?

A

Fluoroquinolone antibiotic
Inhibits type II DNA topoisomerases (DNA gyrase & topo IV)- hence inhibits changes in supercoiling required for replication & gene expression.
Used vs bacillus anthrax (anthrax infections), and in Pseudomonas infections where oral therapy is preferred- e.g respiratory tract infections in CF patients.

19
Q

Rifampin

Uses?

A

Binds beta subunit of DNA-dependent RNA polymerase- inhibits initiation of RNA synthesis
Used vs mycobacterium

20
Q

Daunomycin

Uses?

A

Planar polycyclic anthracycline antibiotic
Intercalates in dsDNA and causes local unwinding
Used as anticancer agent

21
Q

Bleomycin

A

Metal-chelating glycopeptide antibiotic

Generates superoxide and hydroxyl radicals- causing single & double-stranded breaks in DNA

22
Q

Mitomycin C

A

Aziridine-containing antibiotic

Alkylates & cross-links DNA, thereby preventing strand separation during DNA replication and transcription

23
Q

Sulfamethoxazole

A

Acts as an antimetabolite
Sulfa drug
p-aminobenzoate analogue, competitively inhibits DHPS in biosynthesis of tetrahydrofolate (methyl carrier required for synthesis of dTMP)

24
Q

Trimethoprim

A

Acts as antimetabolite

Inhibits DHFR in biosynthesis of tetrahydrofolate

25
Q

Co-trimoxazole

Uses?

A

Combination of sulfamethoxazole and trimethoprim.
Used in AIDS patients with fungal Pneumocystis carinii infections
Withdrawn as routine anti-bacterial due to being implicated in cases of Steven-Johnson syndrome (severe & sometimes fatal allergic reaction)

26
Q

Valinomycin

A

Targets membrane
Cyclic peptide antibiotic
Binds K+ and facilitates K+ diffusion across membrane

27
Q

Granmicidin A

A

Targets membrane
Linear polypeptide antibiotic
Forms homodimeric complex that acts as an ion channel in the membrane

28
Q

Polymixin

A

Targets membrane
Cationic detergent antibiotic containing cyclic peptide and hydrophobic tail
Binds to membrane & alters its ion permeability

29
Q

Amphotericin B

Used against

A

Targets membrane
Polyene antifungal and antiparasitic drug
Forms pores in membrane by an ergosterol-dependent mechanism
Used against most systemic mycoses; active vs Cryptococcus, Candida, Aspergillus

30
Q

Fluconazole

Used to treat

A

Targets membrane
Triazole antifungal drug
Inhibits ergosterol biosynthesis
Treatment of athletes foot & vaginal candidiasis

31
Q

Miconazole

A

Triazole antifungal drug

Inhibits ergosterol biosynthesis

MODA (27 decks)

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