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Fluoroquinolones

CiprofloxacinNorfloxacinOfloxacinLomefloxacinTrovafloxacinLevofloxacinSparfloxacinGatifloxacin

Quinolones Nalidixic acid

Urinary tract antiseptics

MethenamineNitrofurantoin

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Mafenide Silver sulfadiazine Succinylsulfathiazole Sulfacetamide Sulfadiazine Sulfamethoxazole Sulfasalazine sulfisoxazole

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Pyrimethamine trimetoprim

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Co-trimoxazole

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First generation –nalidixic acid Second generation—ciprofloxacin,

norfloxacin, ofloxacin Third gen—gatifloxacin, levofloxacin,

moxifloxacin, sparfloxacin Fourth—trovefloxacin.

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Inhibit replication of bacterial DNA by blocking the action of DNA gyrase(topoisomerase-II) and topoisomerase IV resulting in death of the bacteria.

Are bactericidal and exhibit concentration dependent killing

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First generation: restricted to the treatment of infections of the urinary tract

Second generation: gram-ve, some gram +ve and atypical organisms

Third generation: gram-ve, some gram+ve and atypical organisms

Fourth generation: gram+ve, some gram-ve and anerobes

They are effective against gonorrhea but not syphilis.

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Ciprofloxacin-- Anthrax Pseudomonal infections UTI Gonorrhea Traveller’s diarrhea

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ROUTE : ORAL , IV ORAL –absorption Decreased by

sucralfate, calcium, antacids containing Mg , iron supplements, zinc…

DISTRIBUTION : CSF LESS Exception – OFLOXACINEXCRETION : RENAL

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NORFLOXACIN-Effective against both Gram positive and G negative organisms

Useful in treating UTIS and prostatitis.

LEVOFLOXACIN- An isomer of ofloxacin and has largely replaced it.

Useful in treatment of prostatitis due to E coli. STDs including gonorrhea EXCEPT syphilis

Good against respiratory infections due to S. Pneumonia and skin infections

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Mutation in bacterial DNA gyrase → decreased affinity for fluoroquinolones

Decreased intracellular concentration due to the presence of an efflux pump

Decreased number of porin proteins in the outer membrane

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Ciprofloxacin, ofloxacin can increase the serum levels of theophylline, warfarin and cyclosporin

Cimetidine interferes with the elimination of the fluoroquinolones

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NAUSEA, HEADACHE, DIARRHEA NEPHROTOXICITY PHOTO TOXICITY Liver toxicity-Trovafloxacin CNS – CARE FOR EPILEPSY Sparfloxacin and moxifloxacin- prolongs

QT interrval –CI in arrhythmias Cartilage erosions(in children) and

increase risk of tendon injury with previous Tendonitis(adults).

CI : preg, lactating, children 15

FOLATE ANTAGONISTS

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Inhibition of DNA/RNA synthesis/function through interference with folic acid production

MECH : analogs of PABA that COMPETES WITH PABA

ENZY : inhibits DIHYDRO-PTEROATE SYNTHETASE

AB SPECTRUM : BACTERIOSTATIC

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SILVER SULFA DIAZINE SULFACETAMIDE MAFENIDE SULFASALAZINE SULFISOXAZOLE SULFAMETHOXAZOLE

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ROUTE : MOSTLY ORAL TOPICAL: CREAMS OF MAFENIDE

ACETATE AND SILVER SULFADIAZINE USED IN BURNS

DISTRIBUTION : BBB, PLACENTA EXCRETION : RENAL

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HYPERSENSITIVITY reaction: rashes, angioedema, steven-Johnson syndrome

Cyrstalluria: due to depressed kidney function NEPHROTOXICITY BLOOD: hemolytic anemia in pts def in G6PD,

granulo and thrombocytopenia KERNICTERUS CI ; infants and newborns(< 2months of age),

PREGNANT(at term).

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Potentiation of the hypoglycemic effect of tolbutamide as well as the anticoagulant effect of warfarin due to their displacement from binding sites on albumin

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SILVER SULFA DIAZINE

SULFACETAMIDE MAFENIDE

SULFASALAZINE SULFISOXAZOLE

BURNS

IBD

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Other uses

NOCARDIOSIS-Nocardia asteroides UTI TRACHOMA

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TRIMETHOPRIM PYRIMETHAMINE - in combination with

sulfadiazine used to treat toxoplasmosis and and chloroquine resistant malaria)

METHOTREXATE – carcinoma

USES : UTI, PROSTATITIS, vaginitis SE : blood disorders RX ; FOLINIC ACID(leucovorin) to reverse

the blood disorder.

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TRIMETHOPRIM + SULFAMETHOXAZOLE PNEUMOCYSTIS CARINII (JIROVECI) PNEUMONIA MOA—Inhibition of 2 sequential steps in the

synthesis of tetrahydrofolic acid Sulfamethoxazole inhibits incorporation of PABA

into folic acid and trimethoprim prevents reduction of dihydrofolate to tetrahydofolate

USES : UTI, GENITAL, PROSTATE Shigellosis, nontyphoid salmonella, H-influenza

and alternative to Legionella and PCP in AIDS pts

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DERMATOLOGICALGIT—glossitis and stomatitisBLOOD- Anemia, Leukopenia,

Thrombocytp. Reverse using folinic acid(leucovorin)

DRUG INTERACTIONS- increased PT in Pts taking warfarin.

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Methenamine Needs acidic pH Mostly combined with mandelic acid Decomposes to Form formaldehyde

which is toxic for bacteria CI : hepatic failure, renal failure,

catheterized pt. & also with Sulfonamides.

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MethenamineRoute – oralExcretion – urine (renal)SE- GIT distress, at higher doses

albuminuria, hematuria and rashes.

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Bacteriostatic Antibiotic activity is greater in acidic

urine Sensitive bacteria reduce the drug to an

active agent that Inhibits various bacterial enzymes & damages DNA

Route – oral

Excretion – renal ( brown urine )30

SE GIT Pneumonitis Anemia : G 6 PD DEF. NEURO : DEMYELINATION.

CI : Pregnant & children

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