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Boards study > Pharm - Antibacterial, etc > Flashcards

Pharm - Antibacterial, etc Flashcards

1
Q

beta-lactam antimicrobial (antibacterial)

A
  • penicillin
  • ampicillin
  • methicillin
  • piperacillin
  • aztreonam
  • imipenem
  • cephalosporins
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2
Q

Protein synthesis inhibitors (antibacterial)

A 
50S inhibitors:
- chloramphenicol
- macrolides (eg. erythromycin)
- clindamycin
30S inhibitors:
- aminoglycosides (eg. gentamycin)
- tetracyclines
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3
Q

Antimycobacterial agents (antibacterial)

A
  • rifampicin
  • isoniazid
  • dapsone, ethambutol, and pyrazinamide
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4
Q

Other antibacterial agents

A
  • trimethoprim-sulfamethoxazole
  • fluoroquinolones (eg. ciprofloxacin)
  • vancomycin
  • metronidazole
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5
Q

Cephalosporin classes and antibacterial activity

A

1st gen: gram (+) cocci (pneumococci, strep, staph), Proteus mirabilis, E. coli, Klebsiella pneumonia
2nd gen: gram (+) cocci, Proteus, E. coli, Klebsiella sp., Enterobacter, Serratia, some anaerobes, H. flu
3rd gen: gram (-) bacteria (Serratia, Pseudomonas, Enterobacter, H. flu, Neisseria)
4th gen: gram (-) bacteria (same as 3rd gen), gram (+) bacteria (S. aureus, S. pneumonia)

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6
Q

Protein synthesis inhibitors

A

Aminoglycosides => 30S => inhib initiation complex -> mRNA misread
Tetracyclines => 30S => prevent tRNA attachment
Chloramphenicol => 50S => inhib peptidyl transferase (incorp new a.a. into strand)
Erythromycin, Lindomycin => 50S => block tRNA complex translocation
Clindamycin => 50S => block initiation complex formation and inhib tRNA complex translocation

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7
Q

Sulfonamides (sulfamethoxazole) and Trimethoprim

A
  • inhibit bacterial synthesis of folic acid
  • disrupts DNA synthesis (bacterial)
  • Sulfamethoxazole =| dihydropteroate synthase
  • Trimethoprim =| dihydrofolic acid reductase
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8
Q

antiretroviral agents

A
  • nucleoside reverse transcriptase inhibitors (eg. Zidovudine)
  • non-nucleoside reverse transcriptase inhibitors (eg. Nevirapine)
  • protease inhibitors (eg. Saquinivir)
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9
Q

antiviral agents

A
  • Acyclovir
  • Ganciclovir
  • Amantadine
  • Ribavirin
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10
Q

select Antiviral MOA

A
  • gamma-globulins => black adsorption and penetration
  • Amantadine => block uncoating of viral nucleic acid
  • reverse transcriptase inhib => block synth of nucleic acids
  • rifampin => block viral particle assembly
  • neuraminidase inhib => block release of viral particles from host cell
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11
Q

Antifungal agents

A
  • Flucytosine
  • Amphotericin B
  • Ketoconazole
  • Fluconazole
  • Griseofulvin
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12
Q

General Antifungal MOA

A
  • take advantage of different lipid content of mammalian and fungal membranes
  • fungal membranes have ergosterol, the target of most antifungal agents
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13
Q

select antifungal MOA

A
  • Amphotericin B => bind ergosterol -> holes in fungal membrane
  • Flucytosine => converted to nucleotide analogue by fungal enz then inhib DNA/RNA synth
  • Miconazole, fluconazole, clotrimazole => inhib fungal cytochrome P-450 -> reduce ergosterol synth
  • Caspofungin => disrupt fungal cell wall synth
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14
Q

Antiparasitic agents

A 
Antiprotozoan agents
- Chloroquine
- Primaquine
- Other antiprotozoan agents
Antihelminthic agents
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15
Q

Clinical uses of antiparasitic agents

A
  • Pentamidine => PCP pneumonia prophylaxis; alternate tx for T. brucei and Leishmaniasis
  • Nifurtimox => chagas disease (T. cruzi)
  • Suramin => T. brucei infection before CNS involvement
  • Melarsoprol => T. brucei infect after CNS involvement
  • Sodium stibogluconate => Leishmaniasis
  • Ivermectin => Onchocerciasis (river blindness)
  • Mebendazole/Albendazole/Thiabendazole => roundworm (Ascaris), whipworm (Trichuris), hookworm (Necator, Ancylostoma), pinworm (Enterobius)
  • Pyrantel pamoate => Roundworm, hookworm, pinworm
  • Praziquantel => Fluke (eg. schistosomes, Clonorchis, Paragonimus), agent of choice for cysticercosis
  • Niclosamide => tapeworm (eg. Diphyllobothrium latum, Taenia), except cysticerosis
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16
Q

Penicillin

A
  • similar: penicillin G (IV), penicillin V (oral)
  • MOA: block bacterial peptidoglycan cross-linking (bact cell wall synth)
  • Use: gram (+) cocci (strep, enterococci), gram (-) cocci (Neisseria), and spirochetes (eg. Treponema pallidum)
  • side FX: allergic rxn, Coombs’ (+) hemolytic anemia
17
Q

Ampicillin

A
  • similar: amoxicillin
  • MOA: block bacterial peptidoglycan cross-linking (bact cell wall synth)
  • Use: more than penicillin; gram (-) rods (H. flu, E. coli, Listeria monocytogenes, Proteus mirabilis, Salmonella), gram (+/-) cocci
  • side FX: nonallergenic skin rash
  • other: can be given orally; clavulanic acid and sulbactam inactivate beta-lactamases
18
Q

Methicillin

A
  • MOA: block bacterial peptidoglycan cross-linking (bact cell wall synth)
  • Use: S. aureus and other staph; inactive against enterococci, anaerobes, and gram (-)
  • side FX: interstitial nephritis
  • other: beta-lactamase resistant
19
Q

Piperacillin

A
  • MOA: block bacterial peptidoglycan cross-linking (bact cell wall synth)
  • Use: Pseudomonas and gram (-) rods (eg. Klebsiella)
  • other: susceptible to beta-lactams; with Tazobactam (anti beta-lactamase) can cover S. aureus and broader gram (-) coverage
20
Q

Aztreonam

A
  • MOA: block bacterial peptidoglycan cross-linking (bact cell wall synth)
  • Use: gram (-) rods (Klebsiella, Pseudomonas, Serratia); ineffective against gram (+) or anaerobes
  • side FX: NOT a cross-allergen of penicillin
  • other: relatively resistant to beta-lactamase, use to treat patients with Penicillin allergy or renal insufficiency
21
Q

Imipenem

A
  • MOA: block bacterial peptidoglycan cross-linking (bact cell wall synth)
  • Use: broad spectrum: Enterobacter, anaerobes, and Pseudomonas [also gram (+) cocci, enterococci, gram (-) rods (esp, drug-resistant Klebsiella)]; NOT for VRE or MRSA
  • side FX: seizure at high serum level
  • other: relatively beta-lactamase resistant; increased duration of action with Cilastatin (inhib renal dihydropeptidase I)
22
Q

Cephalosporins

A
  • MOA: block bacterial peptidoglycan cross-linking (bact cell wall synth)
  • Use: 1st gen: surgical prophylaxis or cellulitis
    2nd gen: sinusitis, otitis, pneumonia
    3rd/4th gen: treat serious gram (-) infections (eg. meningitis, Pseudomonas, Enterobacter)
  • side FX: hypersensitivity cross-reactive with Penicillin, disulfiram-like reaction with ethanol, nephrotoxic
  • other: relatively resistant to beta-lactamase
23
Q

Gentamicin

A
  • similar: aminoglycosides (eg. streptomycin, neomycin)
  • MOA: 30S protein synth inhib; inhib formation of initiation complex -> mRNA misread
  • Use: severe infection with gram (-) rods (eg. sepsis, chronic UTI, endocarditis [with vancomycin], pneumonia, Pseudomonas); Neomycin -> bowel surgery prep; Streptomycin -> TB; ineffective against anaerobes
  • side FX: nephrotoxic (ATN, esp with cephalosporin), ototoxic (esp with loop diuretic)
24
Q

Clindamycin

A
  • MOA: 50S port synth inhib; inhib formation of initiation complex
  • Use: some anaerobes (eg. Bacteroides fragilis, C. perfringens), some gram (+) cocci (strep, staph), and severe anaerobic infection above the diaphragm (eg. asp pneumonia, lung abscess)
  • side FX: C. diff colitis (pseudomembranous colitis)
25
Q

Chloramphenicol

A
  • MOA: 50S protein synth inhib
  • Use: broad-spectrum for gram (+/-) (H. flu, N. meningitidis, S. pneumonia, Bacteroides sp); rare use now b/c of side FX, but can be alternative to bacterial meningitis in penicillin intolerance or severe childhood rickettsial infect
  • side FX: myelosuppression (dose-dep anemia, dose-indep aplastic anemia); gray baby syndrome (vomiting, flaccid, gray skin, shock) from lack UDP glucuronyl transferase
26
Q

Erythromycin

A
  • similar: Macrolides
  • MOA: 50S protein synth inhib
  • Use: gram (+) cocci (strep, staph), Corynebacteria spp, atypical org (Mycoplasma, Legionella, Chlamydia spp);
    used to tx upper resp infect (eg. Mycoplasma, Legionnaires disease), STDs (Chlamydia, Neisseria, syph), H. pylori, Corynebacteria (eg. diphtheria)
  • side FX: GI upset, acute cholestatic hepatitis
  • other: inhib cytochrome P-450s -> incr serum warfarin, cyclosporine, and theophylline
27
Q

Tetracycline

A
  • similar: doxycycline, minocycline

- MOA: 30S prot synth inhib

28
Q

Trimethoprim-Sulfamethoxazole

A
  • MOA: inhibit bacterial folic acid synthesis (Trimethoprim -| dihydrofolate reductase; sulfamethoxazole [structural analogue of PABA] -| dihydropteroate synthase [competitive])
29
Q

Ciprofloxacin

A
  • similar: fluoroquinolones

- MOA: inhibit bacterial DNA topoisomerase II -> DNA strand breaks -> cell death

30
Q

Vancomycin

A
  • MOA: binds D-ala D-ala terminus of bacterial cell wall precursors -> inhibit transglycosylase -> weakened peptidoglycans in cell wall -> damage and lysis
31
Q

Metronidazole

A
  • MOA metabolized by bacterial proteins into reduced reactive compounds -> damage bact DNA, prot, memb -> cell death
32
Q

Rifampin

A
  • MOA: inhib bact DNA-dependent RNA polymerase -> decreased RNA synth
33
Q

Isoniazid

A
  • MOA: inhib synth of mycolic acids, which are major constituents of mycobacterial cell walls
34
Q

Other antimycobacterial agents: Dapsone (DAP), Ethambutol (ETH), and Pyrazinamide (PYR)

A
  • MOA:
    => DAP: PABA antag inhib folic acid synth (similar to sulfonazmides)
    => ETH: inhib mycobac arabinosyl transferase, which does cell wall synth
    => PYR: unknown
35
Q

Nucleoside reverse transcriptase inhib (NRTI): AZT, lamivudine, etc

A
  • MOA: inhibit HIV reverse transcriptase -> stops DNA synth; can also compete with nuc triphosphates for addition to DNA stand -> defective viral particle
36
Q

non-nucleoside reverse transcriptase inhib (NNRTI): nevirapine, efavirenz, delavirdine

A
  • MOA: bind HIV reverse transcriptase -> block DNA synth
37
Q

Protease inhibitors: saquinivir, ritonavir, indinavir, etc

A
  • MOA: inhib HIV protease enz -> can’t cleave precursor proteins into mature prot for virus core -> virus can’t replicate
38
Q

Acyclovir

A
  • MOA: phosphorylated by viral thymidine kinase into dGTP analogue -> inhib DNA synth thru incorporation
  • Use: HSV 1/2, VZV, EBV, genital herpes, herpes encephalitis
  • side FX: neurotoxic (tremor, delirium), nephrotoxic

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