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44 Cards in this Set

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What is the MOA of sulfonamides?
inhibit DHP synthase, the "bacterial enzyme" responsible for the incorporation of PABA into dihydropteroic acis, the immediate precursor of folic acid.

Selective for bacteria
What is the MOA of trimethoprim?
It inhibits DHFR which reduces dihydrofolate to tetrahydrofolate (one carbon transfers for pyrimidine and purine synthesis)

note: REASONABLE selective for bacteria (4 to 5 times more sensitive than mammals)
Sulfisoxazole (Gantrisin) is marketed in combination with what for treatment of otitis media in kids?
with Erythromycin

- Pediazole, Eryzole, Pediagen
Azo Gantrisin and Azo Ganatol are combinations of what two drugs and what do they treat?
Phenazopyridine
+ Sulfisoxazole = Gantrisin
+ Sulfamethoxazole = Ganatol

used as an antiseptic and analgesic to treat urinary tract inf.

- pee turns orange red!
Crystalluria is associated with what kind of drugs?
Sulfonamides (sulfadiazine)

- adequate urine output is necessary to avoid or give Na bicarbonate to reduce
Which sulfonamide is used to treat both inflammation and infection?
Sulfasalazine
Sulfasalazine is broken down by the intestinal bacteria to what?
Sulfapyridine, an active sulfonamide and 5-aminosalicylate, (antiinflammatory - management of IBD)
Which sulfonamide is topically used for ophthalmic infections because it is non-irritating to the eyes even at high concentrations?
SulFACE(eyes)tamide
Which sulfonamide is used topically for the prevention of infection of burns?
Silver sulfadiazine

note: side effects - burning, rash, itching
Which combination of sulfonamides are used to treat bacterial vaginosis caused by Hemophilus (Gardnerella) vaginalis?
Sulfabenzamide, Sulfacetamide, Sulfathiazole

( sultrin, dayto sulf, gynesulf, triple sulfa, trysul)
Which topical sulfonamide is effective in preventing the colonization of burns ?
Mafenide (sulfamylon)
Which long acting sulfonamide is combined with pyrimethamine for prophylaxis and treatment of Mefloquine resistant Plasmodium falciparum (Malaria) ?
Sulfadoxine!

note: only used in high risk cases because may cause Steven-Johnson syndrome!
ORAL trimethoprim-sulfamethoxazole combination (TMP-SMZ) is effective for what?
Pneumocystis Jeroecii pneumonia (low dose for prophylaxis in AIDS and neutropenic patients, May cause rash, leukopenia, and hepatitis) ...

-Shigellosis, Salmonella inf (SLD for Typhoid fever)

- UTI

-Bact. respiratory inf - acute otitis media, chronic bronchitis, maxillary sinusitis. respiratory pathogens (Hemophilus, Moraxella catarrhalis, and klebsiaella pneumonia), MRSA.

-prostatitis, non TB mycobacterial infections.
What is IV trimethoprim-sulfamethoxazole used for?
Management of PJP in AIDS patients.

Also, G(-) spesis caused by multi drug resistant species such as enterobacter and Serratia, Shigellosis, typhoid fever, and UTI
Sulfonamides is combined with what to treat Leishmaniasis and Taxoplasmosis (protozoans)?
ORAL Pyrimethamine
Proguanil (PLASMODIAL folate reductase inhibitor) and Atavaquine (Malarone) are used in combination for treatment of what?
Malaria.
What are the adverse reactions of sulfonmides?
- Hypersensitivity

- Steven-Johnson

-GI disturbance

- Mild hepatic dysfunction

- Acute hemolytic anemia in G6PDH deficient patients.

-Rarely granulocytopenia, thrombocytopenia, and aplastic anemia

-Crystalluria and hematuria

-Drug interactions with methotraxate and warfarin b/c it competes for binding site

-Kernicterus in neonate (bilirubin displacement from plasma binding site)
Trimethoprim may cause hematological disorders that can be ameliorated with what?
supplementary folinic acid (leucovorin)
Trimethoprim may cause hematological disorders that can be ameliorated with what?
supplementary folinic acid (leucovorin)
What sulfonamides is used to treat NOCARDIOSIS ( G+ filamentous nonmotile - w/ primary pulmonary lesions with or without hematogenous spread to deep viscera and CNS)
Sulfadiazine
What is the MOA of Fluoroquinolones?
Inhibits gyrase mediated DNA supercoiling - topoisomerase II and IV - by binding to the A subunit that carries out the strand cutting.

At high concentrations it inhibits eukaryotic topoisomerase
T/F: Floroquinolones are bacteriostatic
False.

Bactericidal!
Norfloxacin, Cirpofloxacin, Ofloxacin, and TMP-SMX are equally efficacious in treatment of what?
UTIs.

Cipro #1.
Fluoroquinolones have NO activity against what STD causing organism?
Treponema Pallidum = SYPHILIS.
Flouroquinolones are CONTRAndicated in what kind of patients?
PREGNANT and UNDER 18!
What is the #1 treatment for Anthrax?
Cipro
What gen. of fluoroquinolones have good activity against Strep Pneumonia and aerobic bacteria?
4th gen - Moxifloxacin, Gatifloxacin, Lomefloxacin
What are side effects of flouroquinolones?
Athralgia, joint swelling, tendonitis, tendon rupture (don't exercise!)

- CI in pregnant and <18 yo
What is the use and CI of Nitrofurantoin?
UTI infections.

CI in pregnant and neonates due to hemolytic anemia. May cause hemolysis in G6PDH deficient patients.
What is the use and CI of Methanamine?
UTI, chronic suppresice therapy- decomposes ad acidic PH to produce formaldehyde. (inactive against proteus)

CI with sulfonamides (complexes), renal insufficient pts, and hepatic insufficient pts (NH3 production)
What is the cell wall of mycobacteria composed of?
High lipid content with long-chain (C70-90) fatty acids.
What does XDR TB mean?
Extensive drug resistance - TB that is resistant to isoniazid and rifampin, plus any fluoroquinolones and at least one of three injectable SLD (amikacin, kanamycin, capreomycin)
What is the MOA of isoniazid?
Inhibits synthesis of enzymes needed for mycolic acid synthesis via oxygen dependent pathways such as catalase-peroxidase aciton
What is a major side effect of Isoniazid?
Hepatotoxicity (age dependent) and neurotoxicity (alleviated by Pyridoxine)
What is DOC for prophylaxis of TB?
Isoniazid
What is the MOA of rifampin?
Blocks bacterial RNA synthesis by bindng to DNA dependent RNA polymerase (B subunit) in Mycobacteia.
What is the clinical use of Rifampin?
Tx for TB AND Leprosy! Also, meningococcal and staphyococcal carrier states)

(Isoniazid is TB only)
What drug can be tested for compliance by examining the color of body fluids?
Rifampin - oragne-red color.
Rifampin can't be used with what other type of drug in HIV patients?
Protease inhibitors.
What is the first line agent in patients taking retroviral drugs (HIV)?
Rifapentine (1x weekly) and Rifabutin


*Also contraincated in pts taking protease inhibitors but not as serious as Rifampin
What is the MOA of ethambutol?
blocks arabino-galactin (cell wall component of mycoB)
What FLD for TB causes visual disturbances (green blindness) and retinal damage (retrobulbar optic neuritis), headache, and confusion.
ethambutol
What flouroquinolones are used as SLD for TB?
Cipro and Levo
What is the use of Dapsone?
Most effective drug for M. Leprea.

note: If used in US, it is for PJP in immune suppresed.