CNS Infections Review Drugs Flashcards Preview

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Flashcards in CNS Infections Review Drugs Deck (23):
1

Ceftriaxone

(3rd generation cephalosporin)
• 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

2

Penicillin

• 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)

3

Amoxicillin, Ampicillin

• 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)

4

Aztreonam

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

5

Vancomycin

• 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

6

Rifampin

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

7

Gentamicin, Amikacin (Aminoglycosides)

• Protein synthesis inhibitor, binds 30S ribosomal subunit, ototoxicity
• Listeria monocytogenes meningitis: Gentamicin + Ampicillin

8

Acyclovir, Gancyclovir

guanosine analog
• 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)

9

Foscarnet

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

10

Trifluridine

• 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

11

Amphotericin B

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

12

Flucytosine (5-FC)

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

13

Fluconazole

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

14

Antimycobacteria

Combine the following 4 drugs for the treatment of Mycobacterium tuberculosis
• 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

15

Pentamidine

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

16

Suramin

• Unknown mechanism, highly toxic
• Trypanosoma brucei

17

Melarsaprol

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

18

Eflornithine

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

19

Nifurtimox

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

20

Sodium stibogluconate & Meglumine antimoniate

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

21

Miltefosine

• Mechanism unknown
• Leishmania

22

Sulfadiazine+Pyrimethamine

• 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

Albendazole (roundworms, tapeworms)

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