3. 3
RAQSHAN JABEEN
ANTI-URINARY TRACT INFECTION
DEFINATION:
-A urinary tract infection (UTI) is an infection in any part of urinary system – kidney, ureters, bladder and
urethra.
- UTI can be defined as "INFECTION of KIDNEY,URETER,BLADDER or URETHRA ,mainly
associated with DYSURIA,FREQUENT URINATION,FLANK PAINand BURNINGSENSATION
WHILE URINATING..."
-It is define as the presence of at least 1 lakh bacteria per ml of urine (normal bacterial count= 1000 per ml
of urine)
- Most infections involve the lower urinary tract the bladder and the urethra.
- It is common disorder at all ages in both sexes.
EPIDEMOLOGY:-
UTI is the 2nd most common infections presentation in community practices.
Worldwide, about 150 million people are diagnosed with UTI each year .
Prevalence 35% of healthy women suffer symptoms of UTI at some time in their life Common in women
ETIOLOGY:-
1. The causative organism causing UTI are:-
E.coli, Pseudomonas aeroginosa, streptococcus faecalis, staphylococcus epidermis and proteus mirabilis.
- Klebsiella, Proteus, Candida species
2. Waiting for long to urinate.
3. Sexual transmitted diseases [STD] like gonorrhea causes urethritis .
4. Following can cause germs to enter into bladder or kidney and cause UTI:-
- Having bubble bath
- Wearing tight fiting clothes
5. Risk factors :-
- Being pregnant .
- Wearing tight fitting clothes.
- Diabetic.
- Presence of tumor/ stones/ foreign bodies in urinary tract.
SINGS & SYMPTOMS:-
1) Abrupt onset of micturation.
2) Pain in urethra during voiding.
3) Supra pubic pain and tenderness.
4) Haematuria (blood in urine).
5) Dysuria .
6) Fever , Feeling tired, apathy, shaky.
7) Pressure in lower belly.
4. 4
RAQSHAN JABEEN
CLASSIFICATION:-
UTI may present itself in acute and chronic form.
1. Acute infection
2. Chronic infection
1. Acute infection: -
Infection localized to the urethra and bladder (cysto-urethritis, lower uti) causes increased
frequency and urgency of micturation, dysuria and pain in the perineum, fever, chills and
leucocytosis are generally absent. Such infections are generally self limiting. If the kidneys are
also involved (Pyelonephritis - upper UTI).The patient may have loin pain, fever, chills and
leucocytosis urine is usually loaded with pus cells.
2. Chronic infection: -
Patient with chronic infection may have few urinary symptoms unless renal failure has
supervened. When polyuria and nocturnal frequency may be present. Generally loss of health and
weight anemia and hypertension are frequently present and even urine may show pus cells.
UTI are generally classified as complicated and uncomplicated, depending upon the factors that
trigger the infections.
Primary / Recurrent,
It depending on whether the infection is occurring for the first time or is a repeated
event.
UNCOMPLICATED UTI :-
The uncomplicated UTI are due to bacterial infection most often E.COLI. they
affect much more in men.
COMPLICATED UTI :-
Complicated infection which occurs in men and women of any age are also caused
by bacteria but they tend to be more severe more difficult to treat and recurrent.
Recurrent UTI: -
Most women’s who have had an uncomplicated uti have occasionalrecurrence.
5. 5
RAQSHAN JABEEN
TREATMENT
Treatment / Drug therapy
1. SULPHAMETHOXAZOLE / TRIMETROPRIM :-
Trimetroprim
This medication is a combination of two antibiotics sulfamethonazole & trimethoprim. It is used
to treat a wide Varity of bacterial infections.
SULFAMETHOXAZOLE:[GANTANOL][5-methyl-3-isonazolyl]-sulfanilamide.
SYNTHESIS:
S.NO AGENTS EXAMPLES
1 Bacteriostatics agents Sulfonamides
Tetracycline
Nitrofurantion
2 Bactericidal agents Cotrimoxazole
Ampicillin
Fluroquinolones
Cephalosporins
Aminoglycosides
3 Urinary Antiseptic Nitrofurantoin.
Nalidixic acid .
Methanamine
Mandelate.
6. 6
RAQSHAN JABEEN
PROPERTIES:
-It is a white, odourless , crystalline powder and is bitter in taste .It is employed principally in
lower urinary track & systemic infections caused by E.COLI.
USES:-
- Nocardia (DOC), Mycobacteria, Gram –ve infections, Gram +ve infections, Fungus – Pneumocystis
carinii, Protozoa – Toxoplasma gondii.
- Sulfonamides are conjugated in the liver and their metabolites are excreted in the kidney which can cause
crystalluria.
They are high protein bounding drugs. Can cause kernicterus in neonates.
- It is used in treatment of seberal infections including AIDS.
DOSAGE: -
oral:-500mg or 1g tablets, suspension (100mg/1ml)
DOSE:-
oral 2g , followed by 1g every 8 hrs.
MOA: -
Sulfamethoxazole, a sulfanilamide, is a structural analog of para-aminobenzoic acid (PABA).
They compete with PABA to bind to dihydropteroate synthetase and inhibit conversion of PABA
and dihydropteroate diphosphate to dihydrofolic acid, or dihydrofolate. Inhibiting the production
of dihydrofolate intermediate interferes with the normal bacterial synthesis of folic acid (folate).
Folate is an essential metabolite for bacterial growth and replication because it is used in DNA
synthesis, primarily at thymidylate and purine biosynthesis, and amino acids synthesis, including
serine, glycine and methionine. Hence, blockage of folate production inhibits the folate-dependent
metabolic processes for bacterial growth. Since it inhibits bacterial growth, sulfamethoxazole is
considered a bacteriostatic antibiotic.
Sulfonamides are selective against bacteria because they interfere with the synthesis of folate, a
process which does not occur in humans. Human do not synthesize folate, and must acquire it
through diet.
7. 7
RAQSHAN JABEEN
ADVERSE DRUG REACTIONS:-
Itching , Rash , Diarrhea, Headache , loss of appetite , hepatitis, stevnes. Johson syndrome ,
bloody urine, allergic reactions ,decrease blood platelets , hemolytic anemia , depression,
drowsiness.
2. NITROFURMINTOIN:- [Furandanti, Furalan] ; 1-[(5-nitro-2-furanyl)methylene] amino 1-2,4-
imidazolidinedione.
SYNTHESIS:-
PROPERTIES and USES: -
It is a lemon yellow odourless with a bitter taste powder. It is very slightly soluble in water. It is a white
anti-bacterial spectrum both gram+ve and gram-ve bacteria. It is also active against many strains of Ecoli
and Enterococci. Mainly used in the treatment of uncomplicated UTI. Plasma half life is 0.3 – 1 hour.
DOSAGE: -
Oral for adults :- 50-100 mg every 6 hours with meals and at bed time .
MOA: -
The MOA of nitrofuratonin is unique and complex the drug works by damaging bacteria DNA since it
reduced form is highly reactive. This is made possible by rapid reduction of nitrofuratonin inside the
bacterial cell by flavoproteins to multiply reactive intermediators that acts on ribosomal proteins. The
broads mechanism of action for this drug likely is responsible for the low development of resistance to its
effect as a drug effects many different processes important to bacterial cells.
ADVERSE EFFECTS: -
Nausea, vomiting, intestinal fibrosis, may occur in chronic therapy, jaundice also occur.
Preparations: -
Include tablets/ capsules 50&100 mg & a suspension 25mg 15ml .
A microcrystallines preparation (macrodantin)which may be less nauseating is available in capsules 25-
150mg.
8. 8
RAQSHAN JABEEN
3. TETRACYCLINES:-
-Tetracycline isagroupof antibioticthatobtainedbyfermentationfromstreptomycesspp.Orbychemical
transformationof natural products.
-Theyare derivativesof anoctahydronaphthacene ,ahydrocarbonsystem thatcomprisesfourannulated
six memberrings.
Formula: C22H24N2O8
IUPAC ID: (4S,6S,12aS)-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-
pentahydroxy-6-methyl-1,11-dioxonaphthacene-2-carboxamide.
PROPERTIES:-
Colour /Crystalline: cr (+3w)
Molecular weight: 444.44
Melting Point: 170-173°C (with decomposition)
USES:-
First-Line Drug: it is used as first line drug to treat venerealdiseases,cholera, relapsing fever.
Second-Line Drug: Penicillin for leptospirosis.
• They are used in urinary tract infections in which causative organism are sensitive.
• As a prophylactic in chronic obstructive lung diseases.
SYNTHESIS:-
9. 9
RAQSHAN JABEEN
DOSAGES:-
1g daily in 2-4 divided doses.
Storage:-
In light , light resistant container.
MOA:-
They act by inhibiting protein synthesis.They bind to the 30S subunits of ribosomes and inhibit the
binding of aminoacyl tRNA to the mRNA-ribosomal complex. This leads to the inhibition of transfer of
genetic information from tRNA to mRNA. Hence ,no translation or protein synthesis occur at the mRNA-
Ribosomal complex.
ADR’S:-
Hypersensitivity like rashes, urticaria, pruritus, glossitis, vulva, and dermatitis.
Prolonged usage in diabetes, leucopenia causes super infections.
Ataxia, Vertigo are produced when minocycline is discontinued.
4. FLUROQUINOLES:-
1. CIPROFLOXACIN:-
PROPERTIES:-
It isveryeffective forthe treatmentof UTI.
USES:-
To Treat endocarditis,gastroenteritis,malignantotitisenterna,respiratorytract infectionsetc.
DOSAGES:-
Tab:- 250,500 or 750 mg.
UTI:- 250mg twice daily.
MOA:-
It’sa broadspectrumantibioticof the fluoroquinoloneclass. Itisactive againstbothgram positive and
negative bacteria.ItfunctionsbyinhibitingDNA gyraseandtype lltopisomerase,topisomerase lV ,
necessarytoseparate bacterial DNA therebyinhibitingcell division(t1/2=3-4hrs).
ADR’S:-
Diarrhoea, bloody1 blackstools,change inskincolour, chestpainor discomfort, confusion, coughing/
spittingupblood.Increase heartbeat,jointpains.
10. 10
RAQSHAN JABEEN
SYNTHESIS:-
2. OFLOXACIN:-
PROPERTIES AND USES:-
It is one of the most promising newer member of the fluroquinoline family. In this product, the N-ethyl
moiety has been made rigid by incorporation into a heterocyclic ring. It is useful in the treatment of genito-
urinary, respiratory , gastrointestinal, skin and soft tissue infection and gonorrhea. It is contraindicated for
children below 16yrs, pregnant and lactating women and history of epilepsy.
DOSAGES:-
100, 200mg tablets;200-450 mg dailyusuallyfor5-7 days.
MOA:-
It inhibitsthe enzymebacterial DNA gyrase andpreventsandreplicationof bacterial DNA duringbacterial
growthand reproduction.
12. 12
RAQSHAN JABEEN
Oral availability % = >90
T(1/2)= 6-8 hrs
It is used treat a number of bacterial infections including sinusitis , pneumonia , urinary tract infections,
pelvic infections.
DOSAGES:-
500mg. OD for 7-14 days.
MOA:-
Inhibiting bacterial DNA gyrase primarily in gram negative bacteria
Inhibiting bacterial topoisomerase IV primarily in gram positive bacteria.
ADR’S:-
nausea,diarrhea, trouble sleeping
Major:- tendon rupture or inflammation , seizures , psychosis , peripherial nerve damage.
5. CEPHALOSPORINS
1. CEPHALEXIN [KEFLEX]:-
PROPERTIES:-
White,crystals.P.ka:5.2, 7.3 verysoluble inwater,dilute aqueoussolution,insoluble inorganicsolvents.
The alpha -aminogroupof cephaleninrenderitsacidstable andthe 3- methyl groupisresponsible for
metabolicstability.
13. 13
RAQSHAN JABEEN
USES:-
ParticularlyrecommendedforUTIand sometimesemployedforupperrespiratorytractinfections.
SYNTHESIS:-
DOSAGES:-
ORAL- 200-500 mg every6 hrs.
Children's- 18.8-25 mg/kgevery6hrs.
MOA:-
It acts by inhibitingbacterial cell wall synthesis,lackof bacterial cell wallresultsindeathdue tolysisof
bacteria.
ADR’S:-
Diarrhea,dyspepsia,gastritis,fatigue,headache,abdomendiscomfort,rash,agitation,dizzinessand
angioedema.
2. CEFTRIAZONE:-
PROPERTIES AND USES:-
White , crystals,meltingpointabout -155°verysoluble inwater.Itenhibitexcellentboardspectrum
antibacterial activityagainst bothgram positive,negative organisms. It isan antibioticuseful for
treatmentof an number of bacterial infectionssuchasintra abdominal infections.Itisalsouse to
reduce the risk of post operative infections.
DOSAGES:-
Children: 50–75mg/kg per day in equally divided doses every 12hrs;max 2g/day.
Adult: 1–2g IM or IV once daily or in 2 equally divided doses; max 4g/day.
14. 14
RAQSHAN JABEEN
SYNTHESIS:-
MOA:-
It isan third generation antibioticfromthe cephalosporinfamily.Itselectivelyaanirreversibly inhibits
bacterial cell wall synthesisbybindingtotranspeptidase,alsocalledastransamidase whichare penicillin
bindingproteinsthatcatalyse the crosslinkingof the peptidoglycanpolymersformingthe bacterial cell
wall .
ADR’S:-
liverenzyme ,nausea,vomiting,itchiness,headache,dizziness.
15. 15
RAQSHAN JABEEN
HOME REMEDIES FOR UTI :
1. WATER AND JUICES:
- Drinkplenty of water
- Have plentyof juices,like CRANBERRYJUICE
- CRANBERRYJUICE ➡ one of the bestremediestocombatUTI....
2. RAISINS:
- Boil 25 grams of RAISINSin250 ml of water ➡Boil,until waterreducestohalf of itsoriginal volume ➡
have thismixture twice adaywithsugar
- Consideredtobe aneffectiveremedy......
3. BOTTLE GOURD :
- Drinka freshglassof bottle guardjuice,alongwithateaspoonof LIME JUICE.......
4. TENDER COCONUT:
- Have tendercoconutwaterdailyfor15 days...
5. PARSLEY:
- Possessesnatural diureticproperties
- Helpstocleanbladderof infectiousorganisms
- Take half teaspoonof coarselychoppedfreshparsley ➡boil in2.5litresof waterin a coveredpotfor 10
min➡strainit ➡ drinkthisteaovera periodof 3 hours ➡ helpful influshingoutbladder........
6. CUCUMBER:
- Drink1 cup of cucumberjuice + 1 teaspoonof HONEY + 1 teaspoonof FRESH LIME JUICE thrice daily
- Thiscombinationactsas a diuretic........
7. RADISH LEAVES :
- Drink1 cup of RADISH LEAF JUICE inmorningfor15 days........
8. SPINACH :
- Take half cup freshspinachjuice mixedwithhalfcupof tendercoconutwatertwice a day.......
16. 16
RAQSHAN JABEEN
9 . CARROT :
- Take half glassof carrot juice mixedwithanequal quantityof water(if there isnofever).........
10. SANDALWOOD OIL:
- Possessesanti-bacterial anddiureticproperties
- Take 5 dropsin the beginning ➡increase totendropsina cup of waterwith/without2gramsginger
juice...
11. SANDALWOOD BATH :
- Aromatherapybath ➡helpsease PELVICDISCOMFORTthatarisesdue tobladderinfection
- Add10 drops of SANDALWOODESSENTIALOILto a bathof warm water ➡ soakfor 20 minutes ➡eases
pelvicdiscomfort...
- Repeatdailyuntil infectionsubsides...
.
17. 17
RAQSHAN JABEEN
REFERENCES
BOOKS :-
1. P.PARIMOO-A TEXT BOOK OF MEDICINAL CHEMISTRY
2. RAMARAONADENDLA- 2ND EDITION, MEDICINAL CHEMISTRY
3. Dr. ANEES AHMAD SIDDIQUI -VOL-2- A TEXT BOOK OF MEDICINAL
CHEMISTRY
4. S.N PANDEYA – VOL-2 TEXT BOOK OF MEDICINAL CHEMISTRY
5. S.S.KADAM-VOL-1- PRINCIPLES OF MEDICINAL CHEMISTRY
6. R.S SATOSKAR – Revised 22nd EDITION -Pharmacology and
Pharmacotherapeutics
"Sulfamethoxazole". En.wikipedia.org. N.p., 2016. Web. 20 Nov. 2016
"Cephalexin Uses, Side Effects & Dosage Guide - Drugs.Com". Drugs.com. N.p.,
2016. Web. 20 Nov. 2016.
Singh, Jaskeerat. "Antibacterial Drugs". The Medical Post. N.p., 2016. Web. 20
Nov. 2016.
Tetracycline - Biosynthesis". Chm.bris.ac.uk. N.p., 2016. Web. 20 Nov. 2016.
"14 Natural Home Remedies For UTI Pain & Discomfort | Everyday
Roots". Everyday Roots. N.p., 2016. Web. 20 Nov. 2016
"7 Home Remedies For Urinary Tract Infection (UTI)
Symptoms". EverydayHealth.com. N.p., 2016. Web. 24 Nov. 2016.
"LECTURE 10 Classification Of Heterocyclic Compounds On The Basis Of Their
Chemical Structure. Derivatives Of 5-Nitrofuran As Antimicrobial Agents
Associate. - PptDownload". Slideplayer.com. N.p., 2016. Web. 24 Nov. 2016.