Drugs acting on
Genitourinary System
Dip. Clinical Med:2.2
KMTC MWINGI
MR. NYAMAI S.M
Urinary antiseptics
are oral agents that exert antibacterial activity in the
urine but have little or no systemic antibacterial effect.
Their usefulness is limited to lower urinary tract
infections.
Nitrofurantoin
At therapeutic doses, nitrofurantoin is bactericidal for
many Gram-positive and Gram-negative bacteria;
however, P aeruginosa and many strains of Proteus are
inherently resistant.
Nitrofurantoin has a complex mechanism of action that
is not fully
Drugs used on Urinary System
Classified into;
• Urinary Antiseptics.
• Antidiuretics.
• Cholinergics & Anticholinergics.
• Acidifiers & Alkalanizers.
Urinary Antiseptics
Drugs used for urinary tract infects which kill
or inhibit the growth of microorganism.
Attain antibacterial concentration only in
urine. There4 no systemic antibacterial
effect
Include:
Nitrofuratoin
Methenamine
nitrofuratoin
Primarily bacteriostatic in high urine conc its
bacteriocidal(its activity enhaced in lower PH)
Mode of action:
Taken by susceptible bacteria, enzymatically
metabolized to produce intermediates that
damage DNA and protein synthesis.
Activity currently restricted to E.coli
Does not develop resistance during continued
therapy.no cross resistance with other anti
microbials known
It antagonizes bactericidal action of Nalidixic Acid
pharmacokinetics
Well absorbed
Rapidly metabolized in liver
Less than half excreated in urine unchanged
T1/2 30min-60mins
Renal excreation reduced in Azotemia pt: NOT
used renal failure due to accumulation in body
Probenacid inhibits its tubular
secretion:reducing its antiseptic action in
urine
Contraindicated in neonates,pregnacy 38-
42wks,renal failure
Adverse effects
GI-intolerance;nausea
vomiting,diarrhea,abd pains
Fevr,chills,leucopenia occasionally
Longterm use:peripheral
neuritis/neurological effects
In G6PD-hemolytic anemia
Hepatotoxic/pulmonary rxn with fibrosis
Urine turn dark brown when exposed to
light
Uses
uncomplicated UTI
Infections of E.coli 50mg-100mg tds x 5-
10days
Suppressive longterm rx of lower uti
Prophylaxis of UTI following
catheterization/instrumentation
Methenamine
Drugs;methenamine
mandelate,methanamine hippurate
Hexamethylene tetramine inactive in such
Decomposes in urine to release
formaldehyde-inhibits bacteria
Acidic urine is essential for its action ph<5.5
Thus administered with organic acid e.g
mandelic,hippuric or ascorbic acid
Adm as enteric coated tabs to protect from
gastic juices and limit fluid intake to maintain
low ph in urine
uses
Resistant UTI not involving kidneys
Not efective for acute UTI or
catherterization prophylaxis
Adverse effects
Gastritis,chemical cystitis and hematuria
Antidiuretics
Def: are the agent(s) that reduce urine
volume, opposing diuresis.
Mechanism of Action:
Reduces urine flow by acting reabsorption of
water by kidney tubules
Indication & Uses:
1. Cranial Diabetes insipidus.
2. Primary nocturnal enuresis (bed wetting)
3. Nocturia associated with multiple
sclerosis.
Ct Antidiuretics
Drugs;
Antidiuretic Hormone (Vasopressin) 5-10units IM/ SC
Desmopressin 100-400mcg orally 1-4mcg IV.
Contraindication & Precautions:
Hypersensitivity, impaired renal function, with
ongoing diuretic treatment, Caution in CV disease,
edema, hypertension, cystic fibrosis, fluid and
electrolyte imbalance, pregnancy and lactation.
Adverse effect: Nasal irritation, Rhinitis,
Abdominal cramps, Urge defecate, fluid retention,
congestion, Ulceration, nausea, pallor, Backache in
females (due to uterine contraction)
Acidifiers & Alkalanizers
Urinary acidifiers;sodium citrate,pottasium
citrate,tartaric acid
Urinary alkalanizers;sodium
bicarbonate,acetazolamide
AntiMicrobials ;
Acidic;Nitrofuratoin,methenamine,Tetracycli
nes,cloxacillin
Alkaline:cotrimoxazole,aminoglycosisdes,c
ephalosporins,flouroquinolones
PH immaterial: chloramphenicol,ampicillin
Cholinergics and
anticholinergics
These drugs are used for retention and enuresis
Cholinergic effect: contract detruser muscle(m3
receptor) and relaxes internal sphincter.
Drugs: bethanechol
Has specific affinity for cholinergic receptors of
bladder
Indication:
non-obstructive post-op
postpartum urine retention(neurogenic bladder atony)
neurogenic bladder for children above 8yrs
Anticholinergic effect:(inhibition of
cholinergic action)relaxation of
detruser,contraction of internal sphincter
Drugs:oxybutynin
Indication:
Urine incontinence(urine involutarily leaves
bladder.
Overactive bladder(OAB)
Others:COPD,OPP,drooling e.t.c
Drugs acting on uterus
Stimulants
Oxytocin
Prostaglandin;e.g Misoprostol
Others:
Ergometrine and Ethacridine
Relaxants/tocolytics
Calcium channel blockers e.g nifedipine
Beta2 agonists e.g salbutamol,terbutaline,ritodrine
Magnesium sulphate
Others:
Oxytocin receptor antagonist:atosiban
Prostaglandin synthase: indomethecin, ibuprofen,asprin (beware of
premature closure of ductus arteriosus,ulceration,bleeding)
oxytocin
Not absorbed orally:administer
im/iv/intranasal/sublingual
T1/2 10-15mins
Metabolised in liver,kidney & circulating oxytocinase
Effects
Mammary gland;Milk letdown
Cvs-bolus injection-vasodilator-hypotension
Kidney:antiduretic activity-water retention-water
intoxication-nausea-vomiting,anorexia,weight
gain,lethargy.
Uterine rupture,fetal distress,maternal injury
To curb above-always give slow infusion.
oxytocin
Indications
Induction/augmentation of term labor;mother&fetus must
be continously monitored
Mild preeclampsia
Uterine inertia
Prevent PPH;I.M after delivery of placenta
Missed abortion,incomplete abtn
Post maturity
To promote milk ejection
Contraindication:
prematurity,hypersensitivity,breech,evidence of fetal
distress,cpd,Ecclampsia
Precautions:multiple pregnacy,prev-c/s,hypertension
prostagladins
Misoprostol(PGE1),dinoprotone(PGE2),carbo
prost
MOA;contracts uterine smooth muscle
Comparison with oxytocin
Pgs contract uterine smooth muscles
throught pregnacy unlike oxytocin that
works better at term.
Pgs best softens cervix than oxytocin
Pgs have longer duration of action than
oxytocin
Indication
Induction of abortion
Induction of labor(low dose)
PPH
Adverse effects
Nausea,vomiting, abd pains,
diarrhea,bronchospasms,flushing
Contraindication:CPD,fetal distress,risk of
uterine rupture(prev c/s)
Precaution:astham,multiple pg,glaucoma,old
prev c/s
Tocolytics
Inhibits uterine contraction/prevent premature
labor
Indication:uncomplicated premature labor
Relaxants/tocolytics
Calcium channel blockers e.g nifedipine
Beta2 agonists e.g
salbutamol,terbutaline,ritodrine
Magnesium sulphate
Others:
Oxytocin receptor antagonist:atosiban
Prostaglandin synthase: indomethecin, ibuprofen,asprin
(beware of premature closure of ductus arteriosus,ulceration,bleeding)
Tocolytics
Contraindications
Labour more than 36wks,Fetus >2.5kg,
fetal distress,cervix dilatation>4cm,
ruptured membranes,PPH
