Urinary antisepetics
Dr SO Ogundele
Urinary antiseptics
• Oral UTI antiseptics have antibacterial activities in urine but little or
no systemic antibacterial activities
• Most UTI cases are caused by gram negative bacteria, especially E.Coli
• Acute UTIs are usually self limiting
• Upper UTI requires more aggresive and longer treatment than loer
UTI
• Organism causing UTI: E. Coli (85%), Staph Saprophutica, Proteus spp.,
Enterococcus, Staph Epidermides
UTI antisepetics
• Usefullness is limited to treatment of lower UTI
• Effective antibacterial levels are reached in the renal pelvices and
urinary bladder
• Use in chronic UTI where eradication of bacteria by short term
sytemic therapy is required is not proved
• Examples include; Nalidixic acid, oxolinic acid, nitrofurantoin,
phenazopyridine and methenamine
Nalidixic acid
• This drug is one of the earlier quinolones
• It does not achieve systemic antimicrobial leveland it is only useful for
the treatment of lowerUTI
• PK-
• it is well absorbed orally achieving a Bioavailability of 80-95%
• Well concentrated in body fluids, tissues and plasma
• Half life is 3-10 hours (allowwing for daily dosing)
• Oral absorption is impared by divalent cationic compounds (antacids)
• Serum concentration of IV is almost equal to that of oral route
• Excretion is by renal route (Glomerular filtration and tubular secretion)
Nalidixic acid
• MA: inhibition of DNA gyease and opoisomerase
• Indication
• Active against mainly gram negative organism
• Used to treat lower UTI
• Adverse effects
• GIT irritation
• Glycosuria
• Photosensitivities
• Visual disturbance
• Hepatic failure
• CNS stimulation
Nitrofurantoin
• It is both bacteriostaic or bacteriocidal for many gram positive and
negative bacterial especially E Coli
• It is a second line agent for treating UTI
• PK
• Well absorbed orally
• Rapidly metabolised and excreted through the kidney GF and TS
• No sytemic antibacterial activity
• It causes brown discouloration of urine
Nitrofurantoin
• Mechanism of action
• Rapid intracellular conversion into highly reactive intermediate by bactteria
reductase
• The intermdediate then react non-specifically with many ribosonal protein
and disrupt synthesis of protein, RNA, DNA and metabolic precursors
• Antibacterial spectrum cover include: E Coli, most Spp of proteus and
Pseudomonas
• Reistant to Enterobactria and Klebsiella
• Indication
• UTI
Nitrofurantoin
• Dosage: daily dosing for adults giving with food or milk
• Keep urinary PH at 5.5 to enhance drug activity
• Adverse effects
• GIT irritations (anorexia and vomiting)
• Skin rashes and hypersensitivity
• Neuropathies
• Heamolysis in G6PD deficiency
• Leucopenia
• Pneumonia
• Contraindications
• Pregnancy
• Impaired renal function
• Children less than a month old
Methenomines
• It is an hexa-methylene-tetramine
• It decomposis in water to form formaldehyde which is responsible for
its antibacterial activities
• Acidification of urine is required for this decomposition
• It is taken orally and excreted unchanged in urine
• Bacteriocidal for some gram negative bactrial when PH is less than 5.5
• Combination wwith sulfonamides leads to mutual antagonism
• Organism that makes urine strongly alkaline through release of
ammonia are usually resistant
Uses
• Effective against E. Coli, Staph Aureus, Staph Epidemides
• Use for chronic suppresive treatment of UTI
• Treatment of upper UTI like Pyelonephritis
Conclusion
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