URINARY ANTISEPTICS
These areorally administered AMAs which attain antibacterial concentration
only in urine, with no systemic antibacterial effect.
They are concentrated in the kidney tubules, and are useful in lower urinary tract
infection ((UTI).
They have been called urinary antiseptics because this may be considered as a
form of local therapy.
Nitrofurantoin and methenamine are two such agents; infrequently used now.
3.
URINARY TRACT INFECTION(UTI)
Upper urinary tract infection It infects kidney and ureters.
Symptoms - loin pain,
fever
Lower urinary tract infection Burning micturition
(burning sensation while passing the
urine),
Increased frequency of micturition,
Fever
4.
Nitrofurantoin
It isprimarily bacteriostatic, but may be cidal at higher concentrations and
in acidic urine, because its activity is enhanced at lower pH.
No cross resistance with any other Antimicrobial agents.
It is mainly effective against E.coli.
Many gram-negative bacteria except Ps. aeruginosa and proteus were
susceptible.
Methenamine (Hexamine)
Itis inactive (prodrugs)as such; but decomposes slowly in acidic urine to
release formaldehyde which inhibits all bacteria.
This drug exerts no antimicrobial activity in blood and tissues.
Acidic urine is essential for its action.
9.
MECHANISM OF ACTIONOF METHENAMINE
METHENAMINE (PRODRUGS)
STOMACH (ENTERIC COATED)
GET ABSORBED IN INTESTINE AND ENTER IN KIDNEY
UNDER ACIDIC CONDITION (URINE IS ACIDIC) THE DRUGS
GETS CONVERTED INTO A TOXIC COMPOUND
FORMALDEHYDE.
FORMALDEHYDE KILLS BACTERIA
Empirical antimicrobial regimensFor
upper UTI (pyelonephritis)
the same drugs may be given for 2 weeks.
Nitrofurantoin is not suitable for pyelonephritis.
12.
The status ofAMAs (other than urinary
antiseptics) in urinary tract infections
1. Cotrimoxazole
employed empirically in acute UTI without bacteriological data,
because majority of urinary pathogens, including Chlamydia trachomatis,
are covered by cotrimoxazole.
It should not be used to treat UTI during pregnancy.
13.
2. Quinolones
Thefirst generation FQs, especially
ciprofloxacin and ofloxacin are highly effective and currently the most popular
drugs, because of potent action against gram-negative bacilli and low cost.
The FQs should not be given to pregnant women.
14.
3. Ampicillin/Amoxicillin
Amoxicillin+ clavulanic acid is more frequently employed.
Parenteral coamoxiclav is often combined with gentamicin for initial
treatment of acute pyelonephritis
6. Gentamicin
Itis very effective against most urinary pathogens including Pseudomonas
In acute pyelonephritis
gentamicin + parenteral amoxicillinclavulanate, may be initiated empirically
before bacteriological report becomes available
18.
Urinary pH inrelation to use of AMAs
Certain AMAs act better in acidic urine, while others in
alkaline urine
ACIDIC ALKALINE pH immaterial
Nitrofurantoin Cotrimoxazole Chloramphenicol
Methenamine Aminoglycosides Ampicillin
Tetracyclines (Gentamicin, etc.)
Cloxacillin Cephalosporins
Fluoroquinolones
19.
Prophylaxis for urinarytract infection
The most frequently used drugs for prophylaxis or long-term suppressive
treatment of lower UTI are:
• Cotrimoxazole 480 mg* OD P/O HS
• Nitrofurantoin 100 mg* OD P/O HS
• Norfloxacin 400 mg* OD P/O HS
• Cephalexin 250 mg* OD P/O HS
* All drugs are given once daily at bed time.