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DRUGS USED IN
URINARY TRACT
INFECTION
For BSc Nursing
Dr. Pravin Prasad
1st Yr Resident, MD Clinical
Pharmacology
Maharajgunj medical Campus
2nd August, 2015 (17th Shrawan,
2072)
URINARY ANTISEPTICS
o Urinary antiseptics are oral agents that
o exert antibacterial activity in the urine
o but have little or no systemic antibacterial effects.
o Their usefulness is limited to lower urinary tract
infections.
o Why Urinary Antiseptic and not Urinary antibiotics?
DRUGS USED AS URINARY
ANTISEPTICS
 Nitrofurantoin
 Methenamine
 Nalidixic acid
NITROFURANTOIN
Primarily bacteriostatic
Activity limited to E. coli
Mechanism of Action:
Sensitive bacteria reduce the drug to an active agent that
inhibits various enzymes  damage bacterial DNA.
Antibacterial concentration is not attained in blood or tissues
Not to be used with Probenecid, azotemic patients: interferes
with tubular secretion of drug.
NITROFURANTOIN
Adverse Effects:
 Gastrointestinal Intolerance: Nausea, epigastric pain, diarrhoea
 Hypersensitivity : fever, chills
 Peripheral neuritis and other neurological effects with long term
use
 Hematologic disorders: leukopenia, granulocytopenia, Hemolytic
anemia in G6PD deficient patients
 Liver damage, pulmonary reaction with fibrosis on chronic use
 Contraindicated in renal impairment, pregnancy and neonates.
NITROFURANTOIN: USES
 Treatment for uncomplicated lower urinary
tract infection
 Not associated with prostatitis
 Supportive long term therapy
 Long term porphylaxis
 Following catheterization, instrumentation, in women
with recurrent cystitis
METHENAMINE (HEXAMINE)
 Prodrug
 Mechanism of Action:
 Decomposes slowly in acidic urine( Ph 5.5 or less) to release
formaldehyde which inhibits all bacteria
 No antimicrobial activty in blood and tissues.
 Needs to be administered with mandelic acid or
hippuric acid
METHENAMINE
 Use
 As Methenamine mandelate in
 Chronic and resistant UTI not involving kidneys.
 Not Effective for
 Acute UTI
 Catheter prophylaxis
METHENAMINE
 Side Effects:
 Gastritis
 Chemical cystitis, hematuria
 Occasional CNS Symptoms
NALIDIXIC ACID
 Nonfluorinated quinolone
 Bactericidal
 Mechanism of Action:
 Inhibit the replication of bacterial by interfering with
the action of DNA gyrase during bacterial growth
and development.
 Resistance Develops rather rapidly
NALIDIXIC ACID
 Uses:
 Second Line Drugs for UTI
 Recurrent cases
 On the basis of Sensitivity
Reports
 ADR
 Infrequent: GI upset, rashes
 Headache drowsiness,
vertigo, visual disturbances
 Seizures in children
 Nausea ,Vomiting and
abdominal pain
 Photosensitivity, urticaria and
Fever
Contraindicated in infants
PHENAZOPYRIDINE
 Urinary Analgesic
 Affords symptomatic relief from:
 Burning Micturation
 Dysuria
 Urgency
 No anti-bacterial property
 Side Effects:
 Nausea, Epigastric Pain
URINARY TRACT INFECTION:
TREATMENT
Mostly gram negative organisms
 Acute episode: single organism,
 Chronic/recurrent: mixed infection
Acute Infection: largely self limiting
 High urine flow rate
 Frequent bladder voiding
 Lower UTI: Single Dose Antibiotic or 3 Days Course Suffice
 Upper UTI: Longer Treatment
URINARY TRACT INFECTION:
TREATMENT
Bacterial Investigation very important
Smaller than usual doses required for treatment of Lower UTI
Upper UTI requires normal doses as for any other infection
Least Toxic and cheaper drugs should be chosen, for proper duration
Drug should not disrupt normal gut and perineal flora
Frequent recurrences: chronic suppressive treatment with co-
trimoxazole, nitrofurantoin, methenamine, cephalexin, norfloxacin
STATUS OF ANTIMICROBIAL
AGENTS OTHER THAN URINARY
ANTISEPTICS IN UTI
Sulfonamides:
 Decreased dependability for
acute UTI;
 Not used as single drug;
employed for suppressive or
prophylactic therapy
Cotrimoxazole:
 Declined responsiveness
 Employed empirically for acute
UTI (broad spectrum)
 Prophylaxis for recurrent cystitis
in women, catheterized patients
Quinolones:
 First generation FQs (norfloxacin
and ciprofloxacin)
Ampicillin/Amoxicillin
 Frequently used in the past
 Higher failure and relapse rates:
Unreliable for empericial
therapy
 Amoxicillin + Clavulanic Acid
used these days
 Coamoxiclav+ Gentamycin:
initial treatment for acute
STATUS OF ANTIMICROBIAL
AGENTS OTHER THAN URINARY
ANTISEPTICS IN UTI
Cephalosporin:
 Increasing use especially in nosocomial Klebsiella and Proteus
infection
 Employed on the basis of sensitivity report, employed for
community acquired infections as well
 Cephalexin: alternative for prophylaxis of recurrent UTI, especially
women likely to get pregnant
 Gentamycin:
 Sensitive against Pseudomonas
 Narrow margin of safety, parenteral administration: bacterial
sensitivity awaited
URINARY PH AND ANTI MICROBIAL
AGENTS
 Acidic urine required for Methenamine
 Inadequate response, in complicated cases: measurement and
correction of urinary pH may be attempted
 Urease positive Proteus infections: drugs acting at higher pH should
be administered
Favourable urinary pH for antimicrobial action
Acidic Alkaline pH immaterial
Nitrofurantion Cotrimoxazole Chloramphenicol
Methenamine Aminoglycosides Ampicillin
Cloxacillin Cephalosporin
Fluoroquinolone
URINARY TRACT INFECTIONS(UTI)
URINARY INFECTION IN
PATIENTS WITH RENAL
IMPAIRMENT
 Difficult to treat
 Drugs Contraindicated:
 Methamine mandelate,
 Tetracyclines,
 Cephalosporin (some)
 Drugs avoided:
 Nitrofurantion,
 Nalidixic acid,
 Aminoglycosides
 Potassium salts and acidifying agents contraindicated
THANK YOU

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Drugs Used in Urinary Tract Infection

  • 1. DRUGS USED IN URINARY TRACT INFECTION For BSc Nursing Dr. Pravin Prasad 1st Yr Resident, MD Clinical Pharmacology Maharajgunj medical Campus 2nd August, 2015 (17th Shrawan, 2072)
  • 2. URINARY ANTISEPTICS o Urinary antiseptics are oral agents that o exert antibacterial activity in the urine o but have little or no systemic antibacterial effects. o Their usefulness is limited to lower urinary tract infections. o Why Urinary Antiseptic and not Urinary antibiotics?
  • 3. DRUGS USED AS URINARY ANTISEPTICS  Nitrofurantoin  Methenamine  Nalidixic acid
  • 4. NITROFURANTOIN Primarily bacteriostatic Activity limited to E. coli Mechanism of Action: Sensitive bacteria reduce the drug to an active agent that inhibits various enzymes  damage bacterial DNA. Antibacterial concentration is not attained in blood or tissues Not to be used with Probenecid, azotemic patients: interferes with tubular secretion of drug.
  • 5. NITROFURANTOIN Adverse Effects:  Gastrointestinal Intolerance: Nausea, epigastric pain, diarrhoea  Hypersensitivity : fever, chills  Peripheral neuritis and other neurological effects with long term use  Hematologic disorders: leukopenia, granulocytopenia, Hemolytic anemia in G6PD deficient patients  Liver damage, pulmonary reaction with fibrosis on chronic use  Contraindicated in renal impairment, pregnancy and neonates.
  • 6. NITROFURANTOIN: USES  Treatment for uncomplicated lower urinary tract infection  Not associated with prostatitis  Supportive long term therapy  Long term porphylaxis  Following catheterization, instrumentation, in women with recurrent cystitis
  • 7. METHENAMINE (HEXAMINE)  Prodrug  Mechanism of Action:  Decomposes slowly in acidic urine( Ph 5.5 or less) to release formaldehyde which inhibits all bacteria  No antimicrobial activty in blood and tissues.  Needs to be administered with mandelic acid or hippuric acid
  • 8. METHENAMINE  Use  As Methenamine mandelate in  Chronic and resistant UTI not involving kidneys.  Not Effective for  Acute UTI  Catheter prophylaxis
  • 9. METHENAMINE  Side Effects:  Gastritis  Chemical cystitis, hematuria  Occasional CNS Symptoms
  • 10. NALIDIXIC ACID  Nonfluorinated quinolone  Bactericidal  Mechanism of Action:  Inhibit the replication of bacterial by interfering with the action of DNA gyrase during bacterial growth and development.  Resistance Develops rather rapidly
  • 11. NALIDIXIC ACID  Uses:  Second Line Drugs for UTI  Recurrent cases  On the basis of Sensitivity Reports  ADR  Infrequent: GI upset, rashes  Headache drowsiness, vertigo, visual disturbances  Seizures in children  Nausea ,Vomiting and abdominal pain  Photosensitivity, urticaria and Fever Contraindicated in infants
  • 12. PHENAZOPYRIDINE  Urinary Analgesic  Affords symptomatic relief from:  Burning Micturation  Dysuria  Urgency  No anti-bacterial property  Side Effects:  Nausea, Epigastric Pain
  • 13. URINARY TRACT INFECTION: TREATMENT Mostly gram negative organisms  Acute episode: single organism,  Chronic/recurrent: mixed infection Acute Infection: largely self limiting  High urine flow rate  Frequent bladder voiding  Lower UTI: Single Dose Antibiotic or 3 Days Course Suffice  Upper UTI: Longer Treatment
  • 14. URINARY TRACT INFECTION: TREATMENT Bacterial Investigation very important Smaller than usual doses required for treatment of Lower UTI Upper UTI requires normal doses as for any other infection Least Toxic and cheaper drugs should be chosen, for proper duration Drug should not disrupt normal gut and perineal flora Frequent recurrences: chronic suppressive treatment with co- trimoxazole, nitrofurantoin, methenamine, cephalexin, norfloxacin
  • 15. STATUS OF ANTIMICROBIAL AGENTS OTHER THAN URINARY ANTISEPTICS IN UTI Sulfonamides:  Decreased dependability for acute UTI;  Not used as single drug; employed for suppressive or prophylactic therapy Cotrimoxazole:  Declined responsiveness  Employed empirically for acute UTI (broad spectrum)  Prophylaxis for recurrent cystitis in women, catheterized patients Quinolones:  First generation FQs (norfloxacin and ciprofloxacin) Ampicillin/Amoxicillin  Frequently used in the past  Higher failure and relapse rates: Unreliable for empericial therapy  Amoxicillin + Clavulanic Acid used these days  Coamoxiclav+ Gentamycin: initial treatment for acute
  • 16. STATUS OF ANTIMICROBIAL AGENTS OTHER THAN URINARY ANTISEPTICS IN UTI Cephalosporin:  Increasing use especially in nosocomial Klebsiella and Proteus infection  Employed on the basis of sensitivity report, employed for community acquired infections as well  Cephalexin: alternative for prophylaxis of recurrent UTI, especially women likely to get pregnant  Gentamycin:  Sensitive against Pseudomonas  Narrow margin of safety, parenteral administration: bacterial sensitivity awaited
  • 17. URINARY PH AND ANTI MICROBIAL AGENTS  Acidic urine required for Methenamine  Inadequate response, in complicated cases: measurement and correction of urinary pH may be attempted  Urease positive Proteus infections: drugs acting at higher pH should be administered Favourable urinary pH for antimicrobial action Acidic Alkaline pH immaterial Nitrofurantion Cotrimoxazole Chloramphenicol Methenamine Aminoglycosides Ampicillin Cloxacillin Cephalosporin Fluoroquinolone
  • 19. URINARY INFECTION IN PATIENTS WITH RENAL IMPAIRMENT  Difficult to treat  Drugs Contraindicated:  Methamine mandelate,  Tetracyclines,  Cephalosporin (some)  Drugs avoided:  Nitrofurantion,  Nalidixic acid,  Aminoglycosides  Potassium salts and acidifying agents contraindicated

Editor's Notes

  1. Drugs, which in orally tolerated doses, attain antibacterial concentration only in urine, with little or no systemic antibacterial effect. lower urinary tract (urethritis, cystitis, and prostatitis) and the upper urinary tract (pyelonephritis)
  2. (Mandelate and hippurate)
  3. Primarily bacteriostatic, bactericidal at higher concentration and in acidic urine Previously, many gram negative bacteria were sensitive, now activity limited to E. coli Bactericidal antibiotics kill bacteria; bacteriostatic antibiotics slow their growth or reproduction.
  4. Pregnant women neonates and g6pd def more prone to hemolytic anemia
  5. Dose 50-100 mg TDS (5-7mg/kg) for 5-10 days, max 14 days f/by rest periods. Colors the urine brown.resistance more common Supportive long term therapy: 50 mg BD or 100 mg hS
  6. Hexamethylene-tetramine.. Decomposition takes 3 hrs. no resistance to formaldehyde .low ph alone bacteriostatic. proteus can raise PH BY urea-splitting. No antimicrobial activity in blood and tissues. hydrolysis is the decomposition reaction which leads to breaking down of chemical bonds by addition of water.. Prodrug- a compound that, on administration, must undergo chemical conversion by metabolic processes before becoming an active
  7. Not to b used in acte uti. Enteric coated tab used to prevent decomposing in stomach. Mandelamine: metehnamine mandelate tab 0.5, 1 g, tds or qid with fluid restriction.
  8. Contraindicated in hepatic def. (in addition to formation to formaldehyde,ammonium is produced in the bladder,becoz liver rapidly metabolize ammonia to form urea,so its c/I in hepatic insufficeincy,in which elevated levels of circulating ammonium ions would be toxic to the CNS) sulfonamides react with formaldehyde.
  9. Dose:
  10. Treatment more than 2 weeks seldom warranted
  11. Cotrimoxazole 480 mg hS FQ: Most potent action against gram negative bacilli and low cost; particularly valueable in complicated cases(prostatitis, indwelling catheter, cotrimoxazole/ampicillin resistance cases)
  12. Other AMA commonly used: Cloxacillin, Piperacillin/Carbenecillin, Chloramphenicol, Tetracycline