1. fluoroquinolones ciprofloxacin norfloxacin ofloxacin lomefloxacin trovafloxacin levofloxacin...
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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
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FOLATE ANTAGONISTS
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Inhibition of DNA/RNA synthesis/function through interference with folic acid production
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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
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SE GIT Pneumonitis Anemia : G 6 PD DEF. NEURO : DEMYELINATION.
CI : Pregnant & children
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