Antibiotics for CNS infections Flashcards

1
Q

Ceftriaxone (3rd generation cephalosporin)

A
  • Cell wall inhibitor, binds to penicillin binding proteins, good CNS penetration
  • N. gonorrhoeae conjunctivitis
  • Empiric treatment of bacterial meningitis: Ceftriaxone + vancomycin
  • Definitive, Prophylactic treatment of Neisseria meningitis
  • Empiric treatment of brain abscess: Ceftriaxone + metronidazole
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2
Q

Penicillin

A
  • Cell wall inhibitor, binds to penicillin binding proteins
  • High levels of beta-lactam antibiotics in CNS block binding of GABA to receptors. The tissue becomes more excitable and prone to seizures.
  • Gram positive only, intrapartum prophylaxis for Streptococcus agalactiae (Strep B)
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3
Q

Amoxicillin, Ampicillin

A

Cell wall inhibitor, binds to penicillin binding proteins

Add clavulanate to inactivate enzymatic degradation by Beta-lactamases

Otitis media and sinusitis: Amoxicillin

Listeria monocytogenes meningitis: Ampicillin + Gentamicin (unless pregnant)

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4
Q

Aztreonam

A
  • Cell wall inhibitor, binds to penicillin binding proteins
  • Empiric treatment of meningitis if beta-lactam allergy: Aztreonam + Vancomycin
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5
Q

Vancomycin

A
  • Cell wall inhibitor, binds to the D-ala-D-ala shielding it from the transpeptidation reaction
  • Gram positives including MRSA, Empiric treatment of meningitis with ceftriaxone
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6
Q

Rifampin

A
  • inhibits DNA-dependent RNA polymerase, increases P-450 levels decreasing activity of other drugs
  • Meningococcal prophylaxis for H. influenza type B, Mycobacterium tuberulcolosis
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7
Q

Gentamicin, Amikacin (Aminoglycosides)

A
  • Protein synthesis inhibitor, binds 30S ribosomal subunit, ototoxicity
  • Listeria monocytogenes meningitis: Gentamicin + Ampicillin (unless pregnant)
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8
Q

Acyclovir, Gancyclovir- guanosine analog

A
  • Prodrugs must be phosphorylated by viral thymidine kinase leading to its selectivity
  • Inhibits viral DNA polymerase and leads to chain termination
  • Not effective against latent virus
  • HSV-1, HSV-2(Acyclovir), CMV(Gancyclovir)
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9
Q

Foscarnet

A
  • Phosphonoformate binds viral DNA and RNA polymerases
  • Nephrotoxic
  • CMV and gancyclovir-resistant strains
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10
Q

Trifluridine

A
  • Prodrug must be phosphorylated by cellular kinases leading to its toxicity
  • Inhibits viral DNA polymerase and leads to chain termination
  • Topical use for HSV keratoconjunctivitis
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11
Q

Amphotericin B

A
  • Disrupts the plasma membranes allowing the leakage of electrolytes,
  • Liposomal form enters CNS
  • Nephrotoxic
  • Also used for visceral leishmaniasis
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12
Q

Flucytosine (5-FC)

A
  • DNA synthesis inhibitor conversion to 5-fluorouracil
  • Combined with amphotericin B to treat Cryptococcus, Candida infections
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13
Q

Fluconazole

A
  • Decreases ergosterol synthesis
  • Used to treat fungal otitis externa caused by Candida
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14
Q

Combine the following 4 drugs for the treatment of Mycobacterium tuberculosis

A
  • Rifampin- inhibits DNA-dependent RNA polymerase
  • Isoniazid- mycolic acid inhibitor, difference in drug half-life depending on if the individual is a fast or slow acetylator
  • Pyrazinamide- Unknown
  • Ethambutol- cell wall inhibitor, binds arabinosyl transferase
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15
Q

Pentamidine

A
  • Binds DNA minor groove, mitochondrial as well as nuclear genome replication is affected
  • Trypanosoma brucei
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16
Q

Suramin

A
  • Unknown mechanism, highly toxic
  • Trypanosoma brucei
17
Q

Melarsaprol

A

An arsenical, crosses BBB, so will treat stage 2 T. brucei infection. Super toxic!!!!

18
Q

Eflornithine

A
  • ornithine decarboxylase inhibitor, crosses BBB, so will treat stage 2 T. brucei infection.
19
Q

Nifurtimox

A
  • oxidative stress, impairment of membrane potential
  • Trypanosoma cruzi (also Benznidazole, also a nitroaromatic), or T. brucei co-treatment with eflornithine
20
Q

Sodium stibogluconate & Meglumine antimoniate

A
  • Organic antimonials
  • Targets are glycolysis and fatty acid beta-oxidation
  • Leishmania
21
Q

Miltefosine

A
  • Mechanism unknown
  • Leishmania
22
Q

Sulfadiazine+Pyrimethamine

A
  • folate synthesis inhibitors, dangerous to use in pregnancy. The macrolide Spiramycin may be more appropriate in certain pregnancy situations but not approved in US so must acquire from FDA
  • Toxoplasmosis
23
Q

Albendazole (roundworms, tapeworms)

A
  • microtubule inhibitor
  • Taenia solium- cysticercosis, Echinococcus granulosis, Toxocara cati