ANTIBIOTIK DAN

ANTISEPTIK
SALURAN KEMIH
dr. Ave Olivia Rahman, MSc.
Bagian Farmakologi FKIK UNJA

Antibioti
cs

Antisepti
cs

Empirical Antibiotics for

UTIs
Trimethoprimsulfamethoxazole
Fluoroquinolones: Ciprofloxacin,
Levofloxacin
Beta-lactams : penicillins and
Cephalosporins. amoxicillin
clavulanate, cefdinir, cefaclor, and
cefpodoximeproxetil.
Macrolide: clarithromycin,
azithromycin, erytromycin used in
STD-caused UTIs.

Antiseptic
METHANAMINE, NITROFURANTOIN
The urinary tract antiseptics are
concentrated in the renal tubules
inhibit growth of many bacteria.
Cannot be used to treat systemic
infections effective concentrations
are not achieved in plasma with safe
doses.
As local therapy only in kidney and
bladder

Methenamine
Prodrug
Generate formaldehyde that have
antibacterial action.
Acidification of the urine promotes
the generate of formaldehyde
should strive to keep the pH below
5.5

Continue...Antimicrobial
Activity
Nearly all bacteria are sensitive to
free formaldehyde, at concentrations
20 g/ml.
Urea-splitting microorganisms (e.g.,
Proteus spp.) tend to raise the pH of
the urine inhibit the release of
formaldehyde.
Microorganisms do not develop
resistance to formaldehyde

Continue...Pharmacology
Absorbed orally. 10-30% decomposes in
the gastric juice (unless protected by an
enteric coating)
Produce ammonia contraindicated in
hepatic insufficiency.
MIC for most urinary tract pathogens : 18
to 60 g/ml, achived with a daily dose of
2 g at urine pH is 6 and the daily urine
volume is 1000 to 1500 ml
The acids commonly used are mandelic
acid and hippuric acid (UREX, HIPREX).

Continue...Toxicology
Gastrointestinal distress
Painful and frequent micturition,
albuminuria, hematuria, and rashes.
CONTRAINDICATION: in renal
insufficiency can occur crystalluria
Methenamine combines with
sulfamethizole mutual
antagonism.

Continue...Therapeutic Uses and

Status
Not a primary drug for the treatment
of acute urinary tract infections, but it
is of value for chronic suppressive
treatment.
Most useful for E. coli, the common
gram-negative offenders and often S.
aureus and S. epidermidis .
Enterobacter aerogenes and Proteus
vulgaris are usually resistant.

Nitrofurantoin

A synthetic nitrofuran
Formed highly reactive intermediates
damage DNA.
Active against E. Coli and enterococci.
Resistant for Proteus, Pseudomonas,
Enterobacter and Klebsiella.
The antibacterial activity is higher in an
acidic urine.
Bacterial resistance to nitrofurantoin is
frequent .
Not recommended for treatment of
pyelonephritis or prostatitis.

Continue...Pharmacology
Absorbed rapidly and completely from the
GI tract.
Drug is eliminated rapidly Antibacterial
concentrations are not achieved in plasma.
Plasma half-life is 0.3 to 1 hour. 40% is
excreted unchanged into the urine.
In impaired glomerular function
efficacy of the drug and systemic
toxicity.
Nitrofurantoin colors the urine brown.

Continue...Toxicology
Gastrointestinal upset,
Hypersensitivity reactions,
leukopenia, hemolytic anemia
[associated with G6PD),
hepatocellular damage, Acute
pneumonitis, Interstitial pulmonary
fibrosis, Megaloblastic anemia,
neurologic disturbance.
CONTRAINDICATION : Pregnant
women (>36 week), impaired renal
function (creatinine clearance < 40

Dosing of Nitrofurantoin
Adults dose : 4x 50 to 100 mg/day,
with meals and at bedtime.
Child dose : 5 to 7 mg/kg in 4 divided
doses (max 400 mg).
Prevent recurrences : A single 50100mg dose at bedtime .
A course of therapy should not exceed
14 days, and repeated courses should
be separated by rest periods.

Acute cystitis in pregnancy

Nitrofurantoin: 4 x 50 mg (avoid at > 36
weeks)
Trimethoprim: 1x 300 mg (avoid in the
first trimester)
Cephalexin: 2x 500 mg.
Paracetamol can be used to relieve pain
associated with acute cystitis.
Recurrent UTIs require antibiotic
prophylaxis.