UTI and Drugs fro 6 sem B.Pharm as per new PCI Syllabus 2018

1. URINARY TRACT ANTI-
INFECTIVE AGENTS

2. • Urinary tract infections mainly caused by
E -coli , Staphulococcus etc
• It affects the various part of urinary system
kidney , urethra , bladder .
symptoms
Burning senation during urination
pain in pelvic area
Red or pink coloured urine
Continuous urge to urinate

3. • Urinary tract infections can be treated with
many drugs like sulfoamides , quinolones and
other agents .
• These agents are mainly concentrated in
urine after administration
• Effective in eradicating urinary tract
infections

4. Classification
QUNINOLONES
Nalidixic acid
Norfloxacin
Ciprofloxacin
Sparfloxacin
Ofloxacin
Gemifloxacin

5. • Quinolones constitute a large class of
synthetic antimicrobial agents that are
highly effective in the treatment of
many types of infectious diseases,
particularly those caused by bacteria.
• Quinolones are potent, broad-spectrum
antibacterial agents.

6. • Mode of action:
• Quinolones inhibit the action of bacterial
DNA gyrase enzyme.
• This enzyme is responsible for supercoiling
and compacting bacterial DNA molecules into
the bacterial cell during replication.
• This action is accomplished by modifying the
topology of DNA via supercoiling and twisting
of these macromolecules to permit DNA
replication or transcription.

7. QNINOLONES
4-OXO,1,4- DIHYDROQUNILONE MOIETY
SAR

8. (8-aza-4-quinoline)
Prototype drug is Nalidixic acid

9. • 1,4-Dihydro-4-oxa-3-pyridine carboxylic
moiety
• Presence of -COOH group at C3 is
essential for Gyrase binding and bacterial
transport.
• Modification or removal of this group
abolishes the activity.
• Introduction of fluorine at C-6 & Piprazine
ring at C-7 gives highly potent drugs. For
ex: Norfloxacin, Ciprofloxacin ,

11. • Substitution at C-7 & C-8 controls potency
and Pharmacokinetic of the drug.
• Introduction of Fluorine at C-6 and C-8
gives Sparfloxacin. Which has broad
spectrum of activity.

12. • Substitution at positions 5.6.7. and 8 of the
annulated ring produced good effects.
• Substitution at position 6 with fluorine atom
significantly enhance the activity.
• Alkly substitution at position 1 is essential for
activity by lower alkyl groups have greater
potency.
• Aryl substitution at position 1 is consistent
with activity and 2.4-di fluoro phenyl group
has optimum potency.

13. • Ring condensations at (1,8), (5,6), (6,7)
positions leads to active compounds.

14. MOA
• Quninolines acts as a anti-infectives agents
and treats UTI
• By Inhibiting the A – subunit of DNA gyrase
enzyme (topoisomerase)
• which is required for reproduction of bacterial
DNA.
• The agents inhibits DNA replication pathway.
• DNA gyrase causes unwinding of DNA in the
bacteria.
• Quinolines inhibit this enzyme by binding to
its A-subunit as a result of which bacteria is
not able to replicate.

15. NALIDIXIC ACID
1-ETHYL- 7 METHYL-1,4-OXO ( 1,8) NAPH THYRIDINE- 3
CARBOXYLIC ACID

16. MOA
• It inhibits bacterial replication by binding to
the A – subunit of the enzyme DNA gyrase.
USES
• used for lower UTI caused by E-Coli

17. 1-ETHYL -6-FLURO—1,4-DIHYDRO-4-OXO-7-(1-
PIPERAZINYL) -3-QUINOLINE CARBOXYLIC ACID
NORFLOXACIN

18. MOA
• It inhibit the enzymes topoisomerase II and IV
( DNA gyrase )
• Essential for replication, transcription, repair
and recombination of bacterial DNA.

19. USES
• Treatment of UTI’s caused by E-Coli
• Gasteroenteritis
• Enzyme inhibitor
• Nucleic acid synthesis inhibitor

20. Enoxacin
MOA: Enoxacin functions by inhibiting bacterial DNA
gyrase and topoisomerase IV. The inhibition of these
enzymes prevents bacterial DNA replication,
transcription, repair and recombination
USES: It is used in UTI infection caused by E coli.
It is used in the treatment of Diarrhoea and respiratory
tract Infections.

21. 1-cyclopropyl -6-fluoro- 1,4-dihydro-4-oxo-7-(1- piperazinyl)-3-
quinoline carboxylic acid
CIPROFLOXACIN

22. USES
• Recurrent UTI
• Chronic Prostatitis
• Pneumonia
• Skin infection
• Meningitis
• Combination with Metronidazole ( for
Complicated abdominal infection )

23. Sparfloxacin
5-AMINO-1-CYCLOPROPYL-7-(3R,5S)-3,5-DIMETHYLPIPERAZIN-1-YL)
-6,8-DIFLUORO-4-OXO-QUINOLINE-3- CARBOXYLIC ACID

24. MOA
• It inhibit the enzymes topoisomerase II and IV
( DNA gyrase )
• Essential for replication, repair and
recombination of bacterial DNA.
• Inhibition of cell growth
• cell lysis .

25. USES
• UTI
• Bacterial infection
• Bronchitis
• Lower respiratory tract infections

26. OFLOXACIN
9-Fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-
oxo-3,7-dihydro-2H-[1,4]oxazino[2,3,4-
ij]quinoline-6-carboxylic acid

27. • It is one of the most promising newer
members of the fluoroquionolone family.
• In this product, N-methyl moiety has been
made rigid by incorporation into a heterocyclic
ring.
• It is useful in the treatment of genitourinary,
respiratory, gastrointestinal, skin, soft tissue
infections, periodonitis, and gonorrhoea.

28. GATIFLOXACIN
inhibits the bacterial enzymes DNA
gyrase and topoisomerase IV.

29. • oral broad-spectrum quinolone antibacterial
agent used in the treatment of acute bacterial
infections
• In chronic bronchitis and mild-to-moderate
pneumonia.

30. LOMEFLOXACIN
It inhibits the bacterial enzymes DNA
gyrase and topoisomerase IV.
USES: It is used in UTI infection caused by E coli.
It is used in the treatment of Diarrhoea and respiratory tract
Infections.

31. MOXIFLOXACIN
It inhibits the bacterial enzymes DNA
gyrase and topoisomerase IV.
USES: It is used in UTI infection.
It is used in the treatment of conjuctivitis

32. FURAZOLIDINE
MOA: It exerts its effect by cross linking with bacterial DNA
USES: It is used to treat diarrhoea and enteritis caused by bacterial
infection including travelers diaahoea and cholera
Furazolidine has also been used for treating giardiasis amoebiasis
Being antibacterial it is also used in the treatment of UTI’s

33. NITROFURANTOIN
MOA: It causes inhibition of DNA, RNA,
protein, and cell wall synthesis. This leads
to inhibition of bacterial growth or cell
death
USES: it is used in the prophylaxis of UTI

35. METHENAMINE
MOA: It gets converted into
formaldehyde in the body
which has an antibacterial
action
USES: it is used in the prophylaxis of UTI