SlideShare a Scribd company logo
Prepared by :- Ruchita V Bhavsar
1st sem M.Pharm
Guided by :- Mr. Samaresh Pal Roy
HOD of Pharmacology,
SDPC, Kim
 Introduction
 History
 Classification
 Mechanism of Action
 Resistance
 Pharmacokinetics
 Use
 Adverse Effects
 Interaction
2
 The quinolones are a family of synthetic,
broad-spectrum antibiotic with bactericidal
activity.
 The term quinolone refers to potent
synthetic chemotherapeutic antibacterial
agent.
3
 The 1st generation of the quinolones begins with
Nalidixic acid in 1962 for the treatment of
Urinary Tract Infections in humans.
 Nalidixic acid was discovered by George Lesher
and co-workers in a distillate during an attempt
at chloroquine synthesis.
4
 Quinolones (1st generation)
 Highly protein bound
 Mostly used in UTI
 Fluoroquinolones (2nd, 3rd, 4th generation)
 Modified 1st generation quinolones
 Not highly protein bound
 Wide distribution to urine and other tissues
 Limited CSF penetration
5
Generation Drugs Antibacterial spectrum
First
Nalidixic acid
Cinoxacin
Gram –ve bacteria
Aerobic
Second
Norfloxacin
Ciprofloxacin
Ofloxacin
Lomefloxacin
Enoxacin
Gram +ve bacteria
Aerobic
Improved activity against
Gram –ve bacteria
Third
Levofloxacin
Sparfloxacin
Gatifloxacin
Gemifloxacin
Good activity against
Anaerobic
Gram +ve bacteria
particularly pneumococci
Fourth
Trovafloxacin
Moxifloxacin
Clinafloxacin
Sitafloxacin
Anaerobic
Increased activity against
pneumococci
6
 The first-generation agents include cinoxacin
and nalidixic acid, which are the oldest and least
often used quinolones.
 Because minimal serum levels are achieved, use
of these drugs has been restricted to the
treatment of uncomplicated urinary tract
infections.
 They are more susceptible to the development
of bacterial resistance.
 These agents are not recommended for use in
patients with poor renal function because of
significantly decreased urine concentrations.
7
 The second-generation quinolones have increased
gram-negative activity, as well as some gram-
positive and atypical pathogen coverage.
 Compared with first-generation drugs, these agents
have broader clinical applications in the treatment
of complicated urinary tract infections and
pyelonephritis, sexually transmitted diseases,
selected pneumonias and skin infections.
 They include ciprofloxacin, lomefloxacin,
norfloxacin, ofloxacin and enoxacin.
 Ciprofloxacin and ofloxacin are the most widely
used because of their availability in oral and
intravenous formulations.
8
 The third-generation quinolones currently include
levofloxacin, gatifloxacin, moxifloxacin and
sparfloxacin.
 These agents are separated into a third class
because of their expanded activity against gram-
positive organisms, particularly penicillin-sensitive
and penicillin-resistant S. pneumoniae, and
atypical pathogens such as Mycoplasma
pneumoniae and Chlamydia pneumoniae.
 Although the third-generation quinolones retain
broad gram-negative coverage, they are less active
than ciprofloxacin against Pseudomonas species.
9
10
 Because of their expanded antimicrobial spectrum,
they are useful in the treatment of community-
acquired pneumonia, acute sinusitis and acute
exacerbations of chronic bronchitis.
 The FDA recommends that all of these drugs should
be avoided in patients who are taking drugs that
are known to prolong the QT interval, such as
tricyclic antidepressants, phenothiazines and class
I antiarrhythmics. In contrast, levofloxacin does
not affect the QT interval.
 Trovafloxacin, the current member of the fourth-
generation class, adds significant antimicrobial
activity against anaerobes while maintaining the
gram-positive and gram-negative activity of the
third-generation quinolones. It also retains activity
against Pseudomonas species comparable to that of
ciprofloxacin.
 Because of concern about hepatotoxicity,
trovafloxacin therapy should be reserved for life-
or limb-threatening infections requiring inpatient
treatment and the drug should be taken for no
longer than 14 days.
11
 Delafloxacin (developmental code name RX-
3341) is a fluoroquinolone antibiotic being
developed.
 It is more active than other quinolones
against Gram-Positive bacteria.
 Phase II clinical trials have been completed and
Phase III trial for ACUTE BACTERIAL SKIN AND
SKIN STRUCTURE INFECTIONS (ABSSSI) is due to
begin.
12
13
 The fluoroquinolones are a relatively new group
of antibiotics.
 They were first introduced in 1986, but they are
really modified quinolones, a class of antibiotics,
whose accidental discovery occured in the early
1960.
14
15
 It blocks bacterial DNA synthesis by
 Inhibition of bacterial Topoisomerase II (DNA
Gyrase)
 Inhibition of Topoisomerase IV
 Inhibition of ATP dependent DNA gyrase; which
nicks doule stranded DNA, introduces negative
supercoils and then reseals the nicked ends. This
is required to prevent excessive positive
supercoiling of DNA strands when they seperate
to permit replication or transcription.
16
17
 Inhibition of DNA gyrase also prevents the
relaxation of positively supercoiled DNA.
 Inhibition of DNA nicking–closing enzyme
responsible for DNA elongation, which leads to
break in double stranded DNA.
 Inhibition of topoisomerase IV interferes with the
separation of replicated chromosomal DNA into
respective daughter cells during cell division.
18
 The critical imbalance in cellular metabolism
resulting from the inhibition of enzymes
precipitates a sequence of cellular events which
may lead to :
1. Premature cell division
2. Delayed cell division
3. Total failure of cell division leading to lysis of
the cell
19
20
 Resistance appears to be the result of :
 Alteration in the quinolone enzymatic targets
(DNA gyrase), decreased outer membrane
permeability or the development of efflux
mechanisms.
 One or more point mutations in the quinolone
binding region of the target enzyme
(Topoisomerase) or from a change in the
permeability of the organism.
21
22
23
24
 Absorption : Well absorbed orally with
bioavailability 80-95% Oral absorption is impaired
by divalent cations
 Distribution : Widely distributed in body fluids
and tissues but limited CSF penetration. It can
pass the placenta reaching to the foetus
 Half life : 3-8 hours in serum
 Elimination : 30-50% from urine by tubular
secretion or glomerular filtration and some
amount in bile – faeces.
25
26
1. RTI (Respiratory Tract Infection) :
 EMPYEMA : The collection of pus in a cavity of
the body, especially in the pleural cavity (the
area between the lungs and the inner surface of
the chest wall)
 PNEUMONIA : Infection of the lungs that caused
by bacteria, viruses, fungi or parasites
 LUNG ABSCESS : Bacterial infection that occurs
in the lung tissue causing tissue to die and pus to
collect in that space
2. MENINGITIS : Inflammation of the lining of the
brain and spinal cord
27
3. UTI (Urinary Tract Infection) :
 PYELONEPHRITIS : A type of urinary tract
infection (UTI) that affects one or both kidneys
caused by a bacterium mainly Escherichia coli or
virus infection. It causes the kidneys to swell
and may permanently damage them.
 EPIDIDYMITIS : Inflammation of the epididymis, a
tube near the testicles that stores and carries
sperm in men
 PROSTATITIS : Inflammation of
the prostate gland due to a
urine infection in men
 CYSTITIS : Inflammation of the
bladder usually caused by a
urine infection in women
28
4. GIT (Gastro Intestinal Tract) infection :
 ENTERIC FEVER : A potentially fatal
multisystemic illness caused primarily by
Salmonella species
 BACTERIAL DIARRHOEA : Caused by
Campylobacter, salmonellae, and shigella
organisms
5. Skin & soft tissue infections :
 INFECTED ULCERS : Shallow wound that
develops on the skin
 INFECTED BURNS : Red coloured and warm to
touch due to an infection
29
6. GONORRHEA : A venereal disease involving
inflammatory discharge from the urethra or
vagina.
7. CHANCROID : Bacterial infection that causes open
sores on or around the genitals of men and women
8. TUBERCULOSIS : Infectious bacterial disease
characterized by the growth of nodules (tubercles)
in the tissues, especially the lungs
9. CONJUCTIVITIS : Inflammation of the outermost
layer of the white part of the eye and the inner
surface of the eyelid
30
CNS (Central Nervous System)
 Quinolones may displace the neuroinhibitor GABA,
resulting in CNS stimulation
 Dizziness
 Headache
 Insomnia
 Restlessness
Phototoxicity
 Skin damage after exposure to UV light due to
toxic reactions.
 These included second-degree burns, discoloration
and sometimes permanent discoloration and
scarring of the skin. 31
32
33
Gastrointestinal
 Depletion of magnesium and disruption of cellular
enzyme function
 Disruption of mitochondrial function and energy
production
 Other common side effects are :
 Nausea
 Vomiting
 Anorexia
 Diarrhea
1. NSAIDs :
 Enhance the CNS toxicity of quinolones
2. Theophylline, Caffeine or Warfirine
 Plasma concentration is increased by
Ciprofloxacin
3. Antacid or Iron salts
 Reduce the absorption of quinolones
34
 2nd generation fluoroquinolone
 Most potent fluoroquinolone against P.
aeruginosa
 Not effective against Gram +ve and anaerobes
 Mainly effective against Gram –ve bacteria :
Enterobacteriacae H. Influenzae
Campylobacter M. Catarrhalis
Pseudomonas N. Gonorrhea
 Intracellular Pathogen :
M. Tuberculosis Mycoplasma
Chlamydia Legionella
Brucella
35
36
CLINICAL USE :
 Urinary Tract Infections
 Travellers’ diarrhoea
 Anthrax
 Diabetic foot infections
UNIQUE QUALITIES :
 It binds to divalent cations which decreases
absorption.
 Because of its good penetration into bone, orally
administered ciprofloxacin is a useful alternative to
parenterally administered antibiotics for the
treatment of osteomyelitis caused by susceptible
organisms.
37
MARKETED PREPARATIONS :
 Ciplox eye drop / Ciloxan eye drop or
ointment : Used in conjuctivitis, corneal ulcer
and before opthalmic surgery
38
 Neocip 500 mg :
Cipla
 C-flox 250 mg :
Intas
 Ciprodac 500 mg :
Cadila
 3rd generation fluoroquinolone
 Levo-isomer
 100% oral bioavailability
 Effective against Gram +ve and Gram –ve
bacteria
 Also effective against Pathogen :
Legionella pneumophila
Atypical respiratory pathogens
Mycobacterium tuberculosis
39
40
CLINICAL USE :
 Urinary tract infections
 Chronic bronchitis
 Nosocomial pneumonia
 Intra-abdominal infections
UNIQUE QUALITY :
 It binds to divalent cations which decreases
absorption
41
MARKETED
PREPARATIONS :
 Levoslog tablet
 Levotec tablet
 Wecure ablet
42

More Related Content

What's hot

Chloramphenicol
ChloramphenicolChloramphenicol
Chloramphenicol
JagirPatel3
 
Quinolones
QuinolonesQuinolones
Quinolones
JagirPatel3
 
Tetracycline
TetracyclineTetracycline
Tetracycline
uptu
 
Beta lactamase inhibitors
Beta lactamase inhibitorsBeta lactamase inhibitors
Beta lactamase inhibitors
JagirPatel3
 
Anthelmintic drugs
Anthelmintic drugsAnthelmintic drugs
Anthelmintic drugs
Subramani Parasuraman
 
Macrolide antibiotics.pptx
Macrolide antibiotics.pptxMacrolide antibiotics.pptx
Macrolide antibiotics.pptx
Subramani Parasuraman
 
Ciprofloxacin Antibiotic
Ciprofloxacin AntibioticCiprofloxacin Antibiotic
Ciprofloxacin Antibiotic
Mosese HULKSTAH Tuapati JNR
 
Tetracyclines
TetracyclinesTetracyclines
Tetracyclines
kencha swathi
 
Anthelmintic Drugs
Anthelmintic DrugsAnthelmintic Drugs
Anthelmintic Drugs
Mr.S.SEETARAM SWAMY
 
9.ANTIPROTOZOAL DRUGS
9.ANTIPROTOZOAL DRUGS9.ANTIPROTOZOAL DRUGS
9.ANTIPROTOZOAL DRUGS
Saminathan Kayarohanam
 
Anti Amoebic Drugs
Anti Amoebic DrugsAnti Amoebic Drugs
Anti Amoebic Drugs
Dr Renju Ravi
 
Urinary Tract Infection
Urinary Tract InfectionUrinary Tract Infection
Urinary Tract InfectionRahul Kunkulol
 
Antimalarial drugs
Antimalarial drugsAntimalarial drugs
Antimalarial drugs
ANUSHA SHAJI
 
Antiviral drugs
Antiviral drugsAntiviral drugs
Antiviral drugs
SnehalChakorkar
 
Sulfonamides
SulfonamidesSulfonamides
Sulfonamides
Shruthi Rammohan
 
Tetracyclines
Tetracyclines Tetracyclines
Tetracyclines
abdul waheed
 
Antileprotic drugs
Antileprotic drugsAntileprotic drugs
Antileprotic drugs
Dr. Pramod B
 
Polyene and polypeptide antibiotics
Polyene and polypeptide antibioticsPolyene and polypeptide antibiotics
Polyene and polypeptide antibiotics
Narasimha Kumar G V
 
Antimalarial Drugs Pharmacology
Antimalarial Drugs PharmacologyAntimalarial Drugs Pharmacology
Antimalarial Drugs Pharmacology
http://neigrihms.gov.in/
 
Antitubercular drugs
Antitubercular drugsAntitubercular drugs
Antitubercular drugs
Dr. Pramod B
 

What's hot (20)

Chloramphenicol
ChloramphenicolChloramphenicol
Chloramphenicol
 
Quinolones
QuinolonesQuinolones
Quinolones
 
Tetracycline
TetracyclineTetracycline
Tetracycline
 
Beta lactamase inhibitors
Beta lactamase inhibitorsBeta lactamase inhibitors
Beta lactamase inhibitors
 
Anthelmintic drugs
Anthelmintic drugsAnthelmintic drugs
Anthelmintic drugs
 
Macrolide antibiotics.pptx
Macrolide antibiotics.pptxMacrolide antibiotics.pptx
Macrolide antibiotics.pptx
 
Ciprofloxacin Antibiotic
Ciprofloxacin AntibioticCiprofloxacin Antibiotic
Ciprofloxacin Antibiotic
 
Tetracyclines
TetracyclinesTetracyclines
Tetracyclines
 
Anthelmintic Drugs
Anthelmintic DrugsAnthelmintic Drugs
Anthelmintic Drugs
 
9.ANTIPROTOZOAL DRUGS
9.ANTIPROTOZOAL DRUGS9.ANTIPROTOZOAL DRUGS
9.ANTIPROTOZOAL DRUGS
 
Anti Amoebic Drugs
Anti Amoebic DrugsAnti Amoebic Drugs
Anti Amoebic Drugs
 
Urinary Tract Infection
Urinary Tract InfectionUrinary Tract Infection
Urinary Tract Infection
 
Antimalarial drugs
Antimalarial drugsAntimalarial drugs
Antimalarial drugs
 
Antiviral drugs
Antiviral drugsAntiviral drugs
Antiviral drugs
 
Sulfonamides
SulfonamidesSulfonamides
Sulfonamides
 
Tetracyclines
Tetracyclines Tetracyclines
Tetracyclines
 
Antileprotic drugs
Antileprotic drugsAntileprotic drugs
Antileprotic drugs
 
Polyene and polypeptide antibiotics
Polyene and polypeptide antibioticsPolyene and polypeptide antibiotics
Polyene and polypeptide antibiotics
 
Antimalarial Drugs Pharmacology
Antimalarial Drugs PharmacologyAntimalarial Drugs Pharmacology
Antimalarial Drugs Pharmacology
 
Antitubercular drugs
Antitubercular drugsAntitubercular drugs
Antitubercular drugs
 

Viewers also liked

Quinolones | drug develoupment | mechanism of action | future
Quinolones | drug develoupment | mechanism of action | futureQuinolones | drug develoupment | mechanism of action | future
Quinolones | drug develoupment | mechanism of action | future
Arun Geetha Viswanathan
 
Quinolones and fluoroquinolones
Quinolones and fluoroquinolonesQuinolones and fluoroquinolones
Quinolones and fluoroquinolones
Koppala RVS Chaitanya
 
A presentation on quinolones
A presentation on quinolonesA presentation on quinolones
A presentation on quinolones
Protic Jodder
 
Macrolide
MacrolideMacrolide
Quinolones
QuinolonesQuinolones
Quinolones
Gopi sankar
 
Quinolones and misc. antibiotics
Quinolones and misc. antibioticsQuinolones and misc. antibiotics
Quinolones and misc. antibioticspctebpharm
 
Chemical bond
Chemical bondChemical bond
Chemical bond
Nasib Bin Mahbub Shuvo
 
Quinolones
QuinolonesQuinolones
Quinolones
Medhat Saleh
 
Effect Of Quinolones On Induced Bacterial Resistance1
Effect Of Quinolones On Induced Bacterial Resistance1Effect Of Quinolones On Induced Bacterial Resistance1
Effect Of Quinolones On Induced Bacterial Resistance1a08kalch
 
F1 Safety in the 21st Century
F1 Safety in the 21st CenturyF1 Safety in the 21st Century
F1 Safety in the 21st Century
Max Mosley
 
Ozone layer depletion
Ozone layer depletionOzone layer depletion
Ozone layer depletion
Nasib Bin Mahbub Shuvo
 
QUINOLONES IN CARTIs
QUINOLONES IN CARTIsQUINOLONES IN CARTIs
QUINOLONES IN CARTIsJohnScreen
 
20% tercer corte ultimo
20% tercer corte ultimo20% tercer corte ultimo
20% tercer corte ultimo
DuayChavezpsm
 
Actividad en clase 2015 grupo iii
Actividad en clase 2015 grupo iiiActividad en clase 2015 grupo iii
Actividad en clase 2015 grupo iii
ginafda
 
Fap psicoterapia-analitica-funcional
Fap psicoterapia-analitica-funcionalFap psicoterapia-analitica-funcional
Fap psicoterapia-analitica-funcional
Alex Sandro
 
Trastornos graves de_conducta
Trastornos graves de_conductaTrastornos graves de_conducta
Trastornos graves de_conducta
Daniel Hernández H
 
The wonder drug --Quinolones.
The wonder drug --Quinolones.The wonder drug --Quinolones.
The wonder drug --Quinolones.
dranjalivyas
 

Viewers also liked (20)

Quinolones | drug develoupment | mechanism of action | future
Quinolones | drug develoupment | mechanism of action | futureQuinolones | drug develoupment | mechanism of action | future
Quinolones | drug develoupment | mechanism of action | future
 
Quinolones and fluoroquinolones
Quinolones and fluoroquinolonesQuinolones and fluoroquinolones
Quinolones and fluoroquinolones
 
Quinolones
QuinolonesQuinolones
Quinolones
 
Quinolones
QuinolonesQuinolones
Quinolones
 
A presentation on quinolones
A presentation on quinolonesA presentation on quinolones
A presentation on quinolones
 
Macrolide
MacrolideMacrolide
Macrolide
 
Macrolide (l)
Macrolide (l)Macrolide (l)
Macrolide (l)
 
Quinolones
QuinolonesQuinolones
Quinolones
 
Quinolones and misc. antibiotics
Quinolones and misc. antibioticsQuinolones and misc. antibiotics
Quinolones and misc. antibiotics
 
Chemical bond
Chemical bondChemical bond
Chemical bond
 
Quinolones
QuinolonesQuinolones
Quinolones
 
Effect Of Quinolones On Induced Bacterial Resistance1
Effect Of Quinolones On Induced Bacterial Resistance1Effect Of Quinolones On Induced Bacterial Resistance1
Effect Of Quinolones On Induced Bacterial Resistance1
 
F1 Safety in the 21st Century
F1 Safety in the 21st CenturyF1 Safety in the 21st Century
F1 Safety in the 21st Century
 
Ozone layer depletion
Ozone layer depletionOzone layer depletion
Ozone layer depletion
 
QUINOLONES IN CARTIs
QUINOLONES IN CARTIsQUINOLONES IN CARTIs
QUINOLONES IN CARTIs
 
20% tercer corte ultimo
20% tercer corte ultimo20% tercer corte ultimo
20% tercer corte ultimo
 
Actividad en clase 2015 grupo iii
Actividad en clase 2015 grupo iiiActividad en clase 2015 grupo iii
Actividad en clase 2015 grupo iii
 
Fap psicoterapia-analitica-funcional
Fap psicoterapia-analitica-funcionalFap psicoterapia-analitica-funcional
Fap psicoterapia-analitica-funcional
 
Trastornos graves de_conducta
Trastornos graves de_conductaTrastornos graves de_conducta
Trastornos graves de_conducta
 
The wonder drug --Quinolones.
The wonder drug --Quinolones.The wonder drug --Quinolones.
The wonder drug --Quinolones.
 

Similar to Quinolones

DIVYA KALE [ QUINOLES ]
DIVYA KALE  [ QUINOLES ]DIVYA KALE  [ QUINOLES ]
DIVYA KALE [ QUINOLES ]
DIVYAKALE14
 
quinolones-170308055400.pdf
quinolones-170308055400.pdfquinolones-170308055400.pdf
quinolones-170308055400.pdf
HakeemUllah7
 
quinolones-170308055400.pptx
quinolones-170308055400.pptxquinolones-170308055400.pptx
quinolones-170308055400.pptx
HakeemUllah7
 
quinolones 08767565455688-Dr Sumera.pptx
quinolones 08767565455688-Dr Sumera.pptxquinolones 08767565455688-Dr Sumera.pptx
quinolones 08767565455688-Dr Sumera.pptx
HakeemUllah7
 
POWERPOINT PRESENTATION ON QUINOLINE
POWERPOINT PRESENTATION ON QUINOLINE  POWERPOINT PRESENTATION ON QUINOLINE
POWERPOINT PRESENTATION ON QUINOLINE
ayesharuqsar
 
Quinolone resistance
Quinolone resistanceQuinolone resistance
Quinolone resistance
SheemaKhanam
 
Resistance of quinolone
Resistance of quinoloneResistance of quinolone
Resistance of quinolone
SheemaKhanam
 
fluoroquinolones medchem- oriental college of pharmacy
fluoroquinolones medchem- oriental college of pharmacyfluoroquinolones medchem- oriental college of pharmacy
fluoroquinolones medchem- oriental college of pharmacy
Kaushik Kuche
 
Quinolones & fluoroquinolones-medicinal chemistry.
Quinolones & fluoroquinolones-medicinal chemistry.Quinolones & fluoroquinolones-medicinal chemistry.
Quinolones & fluoroquinolones-medicinal chemistry.
AishwaryaKshirsagar4
 
Fluoroquinolones
FluoroquinolonesFluoroquinolones
Fluoroquinolones
Zainab&Sons
 
Fluoroquinolones
FluoroquinolonesFluoroquinolones
Fluoroquinolones
Zainab&Sons
 
Antibacterials 2
Antibacterials 2Antibacterials 2
Antibacterials 2pavelbd
 
Quinolones & fluoroquinolones
Quinolones & fluoroquinolonesQuinolones & fluoroquinolones
Quinolones & fluoroquinolones
Ameena Kadar
 
Antibiotics resistant infections
Antibiotics resistant infectionsAntibiotics resistant infections
Antibiotics resistant infections
Abdalrahman Rashed
 
Fluroquinolones 2
Fluroquinolones 2Fluroquinolones 2
Fluroquinolones 2VIJAI KUMAR
 
Chemotherapy
ChemotherapyChemotherapy
Quinolones and Fluoroquinolone MOA,ADME,Spectrum of activity of Quinolones.
Quinolones and Fluoroquinolone MOA,ADME,Spectrum of activity of Quinolones.Quinolones and Fluoroquinolone MOA,ADME,Spectrum of activity of Quinolones.
Quinolones and Fluoroquinolone MOA,ADME,Spectrum of activity of Quinolones.
FahimAnwarRizwi
 
Quinolone
QuinoloneQuinolone
Quinolone
Rawan Adnan
 
Class quinolones
Class quinolonesClass quinolones
Class quinolones
Raghu Prasada
 

Similar to Quinolones (20)

DIVYA KALE [ QUINOLES ]
DIVYA KALE  [ QUINOLES ]DIVYA KALE  [ QUINOLES ]
DIVYA KALE [ QUINOLES ]
 
quinolones-170308055400.pdf
quinolones-170308055400.pdfquinolones-170308055400.pdf
quinolones-170308055400.pdf
 
quinolones-170308055400.pptx
quinolones-170308055400.pptxquinolones-170308055400.pptx
quinolones-170308055400.pptx
 
quinolones 08767565455688-Dr Sumera.pptx
quinolones 08767565455688-Dr Sumera.pptxquinolones 08767565455688-Dr Sumera.pptx
quinolones 08767565455688-Dr Sumera.pptx
 
POWERPOINT PRESENTATION ON QUINOLINE
POWERPOINT PRESENTATION ON QUINOLINE  POWERPOINT PRESENTATION ON QUINOLINE
POWERPOINT PRESENTATION ON QUINOLINE
 
Quinolone resistance
Quinolone resistanceQuinolone resistance
Quinolone resistance
 
Resistance of quinolone
Resistance of quinoloneResistance of quinolone
Resistance of quinolone
 
fluoroquinolones medchem- oriental college of pharmacy
fluoroquinolones medchem- oriental college of pharmacyfluoroquinolones medchem- oriental college of pharmacy
fluoroquinolones medchem- oriental college of pharmacy
 
Quinolones & fluoroquinolones-medicinal chemistry.
Quinolones & fluoroquinolones-medicinal chemistry.Quinolones & fluoroquinolones-medicinal chemistry.
Quinolones & fluoroquinolones-medicinal chemistry.
 
Fluoroquinolones
FluoroquinolonesFluoroquinolones
Fluoroquinolones
 
Fluoroquinolones
FluoroquinolonesFluoroquinolones
Fluoroquinolones
 
Antibacterials 2
Antibacterials 2Antibacterials 2
Antibacterials 2
 
Quinolones & fluoroquinolones
Quinolones & fluoroquinolonesQuinolones & fluoroquinolones
Quinolones & fluoroquinolones
 
Antibiotics resistant infections
Antibiotics resistant infectionsAntibiotics resistant infections
Antibiotics resistant infections
 
Fluroquinolones 2
Fluroquinolones 2Fluroquinolones 2
Fluroquinolones 2
 
Chemotherapy
ChemotherapyChemotherapy
Chemotherapy
 
Quinolones and Fluoroquinolone MOA,ADME,Spectrum of activity of Quinolones.
Quinolones and Fluoroquinolone MOA,ADME,Spectrum of activity of Quinolones.Quinolones and Fluoroquinolone MOA,ADME,Spectrum of activity of Quinolones.
Quinolones and Fluoroquinolone MOA,ADME,Spectrum of activity of Quinolones.
 
Antifungal agents
Antifungal agentsAntifungal agents
Antifungal agents
 
Quinolone
QuinoloneQuinolone
Quinolone
 
Class quinolones
Class quinolonesClass quinolones
Class quinolones
 

More from Ruchita Bhavsar

Inflammatory bowel disease
Inflammatory bowel diseaseInflammatory bowel disease
Inflammatory bowel disease
Ruchita Bhavsar
 
Hypertension
HypertensionHypertension
Hypertension
Ruchita Bhavsar
 
Endothelin
EndothelinEndothelin
Endothelin
Ruchita Bhavsar
 
Glycine receptor
Glycine receptorGlycine receptor
Glycine receptor
Ruchita Bhavsar
 
Senna
SennaSenna
Anatomical planes & cavities
Anatomical planes & cavitiesAnatomical planes & cavities
Anatomical planes & cavities
Ruchita Bhavsar
 
Schizophrenia
SchizophreniaSchizophrenia
Schizophrenia
Ruchita Bhavsar
 

More from Ruchita Bhavsar (7)

Inflammatory bowel disease
Inflammatory bowel diseaseInflammatory bowel disease
Inflammatory bowel disease
 
Hypertension
HypertensionHypertension
Hypertension
 
Endothelin
EndothelinEndothelin
Endothelin
 
Glycine receptor
Glycine receptorGlycine receptor
Glycine receptor
 
Senna
SennaSenna
Senna
 
Anatomical planes & cavities
Anatomical planes & cavitiesAnatomical planes & cavities
Anatomical planes & cavities
 
Schizophrenia
SchizophreniaSchizophrenia
Schizophrenia
 

Recently uploaded

Eukaryotic Transcription Presentation.pptx
Eukaryotic Transcription Presentation.pptxEukaryotic Transcription Presentation.pptx
Eukaryotic Transcription Presentation.pptx
RitabrataSarkar3
 
NuGOweek 2024 Ghent programme overview flyer
NuGOweek 2024 Ghent programme overview flyerNuGOweek 2024 Ghent programme overview flyer
NuGOweek 2024 Ghent programme overview flyer
pablovgd
 
THEMATIC APPERCEPTION TEST(TAT) cognitive abilities, creativity, and critic...
THEMATIC  APPERCEPTION  TEST(TAT) cognitive abilities, creativity, and critic...THEMATIC  APPERCEPTION  TEST(TAT) cognitive abilities, creativity, and critic...
THEMATIC APPERCEPTION TEST(TAT) cognitive abilities, creativity, and critic...
Abdul Wali Khan University Mardan,kP,Pakistan
 
Phenomics assisted breeding in crop improvement
Phenomics assisted breeding in crop improvementPhenomics assisted breeding in crop improvement
Phenomics assisted breeding in crop improvement
IshaGoswami9
 
Bob Reedy - Nitrate in Texas Groundwater.pdf
Bob Reedy - Nitrate in Texas Groundwater.pdfBob Reedy - Nitrate in Texas Groundwater.pdf
Bob Reedy - Nitrate in Texas Groundwater.pdf
Texas Alliance of Groundwater Districts
 
Deep Software Variability and Frictionless Reproducibility
Deep Software Variability and Frictionless ReproducibilityDeep Software Variability and Frictionless Reproducibility
Deep Software Variability and Frictionless Reproducibility
University of Rennes, INSA Rennes, Inria/IRISA, CNRS
 
Topic: SICKLE CELL DISEASE IN CHILDREN-3.pdf
Topic: SICKLE CELL DISEASE IN CHILDREN-3.pdfTopic: SICKLE CELL DISEASE IN CHILDREN-3.pdf
Topic: SICKLE CELL DISEASE IN CHILDREN-3.pdf
TinyAnderson
 
mô tả các thí nghiệm về đánh giá tác động dòng khí hóa sau đốt
mô tả các thí nghiệm về đánh giá tác động dòng khí hóa sau đốtmô tả các thí nghiệm về đánh giá tác động dòng khí hóa sau đốt
mô tả các thí nghiệm về đánh giá tác động dòng khí hóa sau đốt
HongcNguyn6
 
What is greenhouse gasses and how many gasses are there to affect the Earth.
What is greenhouse gasses and how many gasses are there to affect the Earth.What is greenhouse gasses and how many gasses are there to affect the Earth.
What is greenhouse gasses and how many gasses are there to affect the Earth.
moosaasad1975
 
The debris of the ‘last major merger’ is dynamically young
The debris of the ‘last major merger’ is dynamically youngThe debris of the ‘last major merger’ is dynamically young
The debris of the ‘last major merger’ is dynamically young
Sérgio Sacani
 
如何办理(uvic毕业证书)维多利亚大学毕业证本科学位证书原版一模一样
如何办理(uvic毕业证书)维多利亚大学毕业证本科学位证书原版一模一样如何办理(uvic毕业证书)维多利亚大学毕业证本科学位证书原版一模一样
如何办理(uvic毕业证书)维多利亚大学毕业证本科学位证书原版一模一样
yqqaatn0
 
Shallowest Oil Discovery of Turkiye.pptx
Shallowest Oil Discovery of Turkiye.pptxShallowest Oil Discovery of Turkiye.pptx
Shallowest Oil Discovery of Turkiye.pptx
Gokturk Mehmet Dilci
 
Orion Air Quality Monitoring Systems - CWS
Orion Air Quality Monitoring Systems - CWSOrion Air Quality Monitoring Systems - CWS
Orion Air Quality Monitoring Systems - CWS
Columbia Weather Systems
 
Nucleophilic Addition of carbonyl compounds.pptx
Nucleophilic Addition of carbonyl  compounds.pptxNucleophilic Addition of carbonyl  compounds.pptx
Nucleophilic Addition of carbonyl compounds.pptx
SSR02
 
Nucleic Acid-its structural and functional complexity.
Nucleic Acid-its structural and functional complexity.Nucleic Acid-its structural and functional complexity.
Nucleic Acid-its structural and functional complexity.
Nistarini College, Purulia (W.B) India
 
Unveiling the Energy Potential of Marshmallow Deposits.pdf
Unveiling the Energy Potential of Marshmallow Deposits.pdfUnveiling the Energy Potential of Marshmallow Deposits.pdf
Unveiling the Energy Potential of Marshmallow Deposits.pdf
Erdal Coalmaker
 
Chapter 12 - climate change and the energy crisis
Chapter 12 - climate change and the energy crisisChapter 12 - climate change and the energy crisis
Chapter 12 - climate change and the energy crisis
tonzsalvador2222
 
Medical Orthopedic PowerPoint Templates.pptx
Medical Orthopedic PowerPoint Templates.pptxMedical Orthopedic PowerPoint Templates.pptx
Medical Orthopedic PowerPoint Templates.pptx
terusbelajar5
 
20240520 Planning a Circuit Simulator in JavaScript.pptx
20240520 Planning a Circuit Simulator in JavaScript.pptx20240520 Planning a Circuit Simulator in JavaScript.pptx
20240520 Planning a Circuit Simulator in JavaScript.pptx
Sharon Liu
 
aziz sancar nobel prize winner: from mardin to nobel
aziz sancar nobel prize winner: from mardin to nobelaziz sancar nobel prize winner: from mardin to nobel
aziz sancar nobel prize winner: from mardin to nobel
İsa Badur
 

Recently uploaded (20)

Eukaryotic Transcription Presentation.pptx
Eukaryotic Transcription Presentation.pptxEukaryotic Transcription Presentation.pptx
Eukaryotic Transcription Presentation.pptx
 
NuGOweek 2024 Ghent programme overview flyer
NuGOweek 2024 Ghent programme overview flyerNuGOweek 2024 Ghent programme overview flyer
NuGOweek 2024 Ghent programme overview flyer
 
THEMATIC APPERCEPTION TEST(TAT) cognitive abilities, creativity, and critic...
THEMATIC  APPERCEPTION  TEST(TAT) cognitive abilities, creativity, and critic...THEMATIC  APPERCEPTION  TEST(TAT) cognitive abilities, creativity, and critic...
THEMATIC APPERCEPTION TEST(TAT) cognitive abilities, creativity, and critic...
 
Phenomics assisted breeding in crop improvement
Phenomics assisted breeding in crop improvementPhenomics assisted breeding in crop improvement
Phenomics assisted breeding in crop improvement
 
Bob Reedy - Nitrate in Texas Groundwater.pdf
Bob Reedy - Nitrate in Texas Groundwater.pdfBob Reedy - Nitrate in Texas Groundwater.pdf
Bob Reedy - Nitrate in Texas Groundwater.pdf
 
Deep Software Variability and Frictionless Reproducibility
Deep Software Variability and Frictionless ReproducibilityDeep Software Variability and Frictionless Reproducibility
Deep Software Variability and Frictionless Reproducibility
 
Topic: SICKLE CELL DISEASE IN CHILDREN-3.pdf
Topic: SICKLE CELL DISEASE IN CHILDREN-3.pdfTopic: SICKLE CELL DISEASE IN CHILDREN-3.pdf
Topic: SICKLE CELL DISEASE IN CHILDREN-3.pdf
 
mô tả các thí nghiệm về đánh giá tác động dòng khí hóa sau đốt
mô tả các thí nghiệm về đánh giá tác động dòng khí hóa sau đốtmô tả các thí nghiệm về đánh giá tác động dòng khí hóa sau đốt
mô tả các thí nghiệm về đánh giá tác động dòng khí hóa sau đốt
 
What is greenhouse gasses and how many gasses are there to affect the Earth.
What is greenhouse gasses and how many gasses are there to affect the Earth.What is greenhouse gasses and how many gasses are there to affect the Earth.
What is greenhouse gasses and how many gasses are there to affect the Earth.
 
The debris of the ‘last major merger’ is dynamically young
The debris of the ‘last major merger’ is dynamically youngThe debris of the ‘last major merger’ is dynamically young
The debris of the ‘last major merger’ is dynamically young
 
如何办理(uvic毕业证书)维多利亚大学毕业证本科学位证书原版一模一样
如何办理(uvic毕业证书)维多利亚大学毕业证本科学位证书原版一模一样如何办理(uvic毕业证书)维多利亚大学毕业证本科学位证书原版一模一样
如何办理(uvic毕业证书)维多利亚大学毕业证本科学位证书原版一模一样
 
Shallowest Oil Discovery of Turkiye.pptx
Shallowest Oil Discovery of Turkiye.pptxShallowest Oil Discovery of Turkiye.pptx
Shallowest Oil Discovery of Turkiye.pptx
 
Orion Air Quality Monitoring Systems - CWS
Orion Air Quality Monitoring Systems - CWSOrion Air Quality Monitoring Systems - CWS
Orion Air Quality Monitoring Systems - CWS
 
Nucleophilic Addition of carbonyl compounds.pptx
Nucleophilic Addition of carbonyl  compounds.pptxNucleophilic Addition of carbonyl  compounds.pptx
Nucleophilic Addition of carbonyl compounds.pptx
 
Nucleic Acid-its structural and functional complexity.
Nucleic Acid-its structural and functional complexity.Nucleic Acid-its structural and functional complexity.
Nucleic Acid-its structural and functional complexity.
 
Unveiling the Energy Potential of Marshmallow Deposits.pdf
Unveiling the Energy Potential of Marshmallow Deposits.pdfUnveiling the Energy Potential of Marshmallow Deposits.pdf
Unveiling the Energy Potential of Marshmallow Deposits.pdf
 
Chapter 12 - climate change and the energy crisis
Chapter 12 - climate change and the energy crisisChapter 12 - climate change and the energy crisis
Chapter 12 - climate change and the energy crisis
 
Medical Orthopedic PowerPoint Templates.pptx
Medical Orthopedic PowerPoint Templates.pptxMedical Orthopedic PowerPoint Templates.pptx
Medical Orthopedic PowerPoint Templates.pptx
 
20240520 Planning a Circuit Simulator in JavaScript.pptx
20240520 Planning a Circuit Simulator in JavaScript.pptx20240520 Planning a Circuit Simulator in JavaScript.pptx
20240520 Planning a Circuit Simulator in JavaScript.pptx
 
aziz sancar nobel prize winner: from mardin to nobel
aziz sancar nobel prize winner: from mardin to nobelaziz sancar nobel prize winner: from mardin to nobel
aziz sancar nobel prize winner: from mardin to nobel
 

Quinolones

  • 1. Prepared by :- Ruchita V Bhavsar 1st sem M.Pharm Guided by :- Mr. Samaresh Pal Roy HOD of Pharmacology, SDPC, Kim
  • 2.  Introduction  History  Classification  Mechanism of Action  Resistance  Pharmacokinetics  Use  Adverse Effects  Interaction 2
  • 3.  The quinolones are a family of synthetic, broad-spectrum antibiotic with bactericidal activity.  The term quinolone refers to potent synthetic chemotherapeutic antibacterial agent. 3
  • 4.  The 1st generation of the quinolones begins with Nalidixic acid in 1962 for the treatment of Urinary Tract Infections in humans.  Nalidixic acid was discovered by George Lesher and co-workers in a distillate during an attempt at chloroquine synthesis. 4
  • 5.  Quinolones (1st generation)  Highly protein bound  Mostly used in UTI  Fluoroquinolones (2nd, 3rd, 4th generation)  Modified 1st generation quinolones  Not highly protein bound  Wide distribution to urine and other tissues  Limited CSF penetration 5
  • 6. Generation Drugs Antibacterial spectrum First Nalidixic acid Cinoxacin Gram –ve bacteria Aerobic Second Norfloxacin Ciprofloxacin Ofloxacin Lomefloxacin Enoxacin Gram +ve bacteria Aerobic Improved activity against Gram –ve bacteria Third Levofloxacin Sparfloxacin Gatifloxacin Gemifloxacin Good activity against Anaerobic Gram +ve bacteria particularly pneumococci Fourth Trovafloxacin Moxifloxacin Clinafloxacin Sitafloxacin Anaerobic Increased activity against pneumococci 6
  • 7.  The first-generation agents include cinoxacin and nalidixic acid, which are the oldest and least often used quinolones.  Because minimal serum levels are achieved, use of these drugs has been restricted to the treatment of uncomplicated urinary tract infections.  They are more susceptible to the development of bacterial resistance.  These agents are not recommended for use in patients with poor renal function because of significantly decreased urine concentrations. 7
  • 8.  The second-generation quinolones have increased gram-negative activity, as well as some gram- positive and atypical pathogen coverage.  Compared with first-generation drugs, these agents have broader clinical applications in the treatment of complicated urinary tract infections and pyelonephritis, sexually transmitted diseases, selected pneumonias and skin infections.  They include ciprofloxacin, lomefloxacin, norfloxacin, ofloxacin and enoxacin.  Ciprofloxacin and ofloxacin are the most widely used because of their availability in oral and intravenous formulations. 8
  • 9.  The third-generation quinolones currently include levofloxacin, gatifloxacin, moxifloxacin and sparfloxacin.  These agents are separated into a third class because of their expanded activity against gram- positive organisms, particularly penicillin-sensitive and penicillin-resistant S. pneumoniae, and atypical pathogens such as Mycoplasma pneumoniae and Chlamydia pneumoniae.  Although the third-generation quinolones retain broad gram-negative coverage, they are less active than ciprofloxacin against Pseudomonas species. 9
  • 10. 10  Because of their expanded antimicrobial spectrum, they are useful in the treatment of community- acquired pneumonia, acute sinusitis and acute exacerbations of chronic bronchitis.  The FDA recommends that all of these drugs should be avoided in patients who are taking drugs that are known to prolong the QT interval, such as tricyclic antidepressants, phenothiazines and class I antiarrhythmics. In contrast, levofloxacin does not affect the QT interval.
  • 11.  Trovafloxacin, the current member of the fourth- generation class, adds significant antimicrobial activity against anaerobes while maintaining the gram-positive and gram-negative activity of the third-generation quinolones. It also retains activity against Pseudomonas species comparable to that of ciprofloxacin.  Because of concern about hepatotoxicity, trovafloxacin therapy should be reserved for life- or limb-threatening infections requiring inpatient treatment and the drug should be taken for no longer than 14 days. 11
  • 12.  Delafloxacin (developmental code name RX- 3341) is a fluoroquinolone antibiotic being developed.  It is more active than other quinolones against Gram-Positive bacteria.  Phase II clinical trials have been completed and Phase III trial for ACUTE BACTERIAL SKIN AND SKIN STRUCTURE INFECTIONS (ABSSSI) is due to begin. 12
  • 13. 13
  • 14.  The fluoroquinolones are a relatively new group of antibiotics.  They were first introduced in 1986, but they are really modified quinolones, a class of antibiotics, whose accidental discovery occured in the early 1960. 14
  • 15. 15
  • 16.  It blocks bacterial DNA synthesis by  Inhibition of bacterial Topoisomerase II (DNA Gyrase)  Inhibition of Topoisomerase IV  Inhibition of ATP dependent DNA gyrase; which nicks doule stranded DNA, introduces negative supercoils and then reseals the nicked ends. This is required to prevent excessive positive supercoiling of DNA strands when they seperate to permit replication or transcription. 16
  • 17. 17  Inhibition of DNA gyrase also prevents the relaxation of positively supercoiled DNA.  Inhibition of DNA nicking–closing enzyme responsible for DNA elongation, which leads to break in double stranded DNA.  Inhibition of topoisomerase IV interferes with the separation of replicated chromosomal DNA into respective daughter cells during cell division.
  • 18. 18  The critical imbalance in cellular metabolism resulting from the inhibition of enzymes precipitates a sequence of cellular events which may lead to : 1. Premature cell division 2. Delayed cell division 3. Total failure of cell division leading to lysis of the cell
  • 19. 19
  • 20. 20
  • 21.  Resistance appears to be the result of :  Alteration in the quinolone enzymatic targets (DNA gyrase), decreased outer membrane permeability or the development of efflux mechanisms.  One or more point mutations in the quinolone binding region of the target enzyme (Topoisomerase) or from a change in the permeability of the organism. 21
  • 22. 22
  • 23. 23
  • 24. 24
  • 25.  Absorption : Well absorbed orally with bioavailability 80-95% Oral absorption is impaired by divalent cations  Distribution : Widely distributed in body fluids and tissues but limited CSF penetration. It can pass the placenta reaching to the foetus  Half life : 3-8 hours in serum  Elimination : 30-50% from urine by tubular secretion or glomerular filtration and some amount in bile – faeces. 25
  • 26. 26 1. RTI (Respiratory Tract Infection) :  EMPYEMA : The collection of pus in a cavity of the body, especially in the pleural cavity (the area between the lungs and the inner surface of the chest wall)  PNEUMONIA : Infection of the lungs that caused by bacteria, viruses, fungi or parasites  LUNG ABSCESS : Bacterial infection that occurs in the lung tissue causing tissue to die and pus to collect in that space 2. MENINGITIS : Inflammation of the lining of the brain and spinal cord
  • 27. 27 3. UTI (Urinary Tract Infection) :  PYELONEPHRITIS : A type of urinary tract infection (UTI) that affects one or both kidneys caused by a bacterium mainly Escherichia coli or virus infection. It causes the kidneys to swell and may permanently damage them.  EPIDIDYMITIS : Inflammation of the epididymis, a tube near the testicles that stores and carries sperm in men  PROSTATITIS : Inflammation of the prostate gland due to a urine infection in men  CYSTITIS : Inflammation of the bladder usually caused by a urine infection in women
  • 28. 28 4. GIT (Gastro Intestinal Tract) infection :  ENTERIC FEVER : A potentially fatal multisystemic illness caused primarily by Salmonella species  BACTERIAL DIARRHOEA : Caused by Campylobacter, salmonellae, and shigella organisms 5. Skin & soft tissue infections :  INFECTED ULCERS : Shallow wound that develops on the skin  INFECTED BURNS : Red coloured and warm to touch due to an infection
  • 29. 29 6. GONORRHEA : A venereal disease involving inflammatory discharge from the urethra or vagina. 7. CHANCROID : Bacterial infection that causes open sores on or around the genitals of men and women 8. TUBERCULOSIS : Infectious bacterial disease characterized by the growth of nodules (tubercles) in the tissues, especially the lungs 9. CONJUCTIVITIS : Inflammation of the outermost layer of the white part of the eye and the inner surface of the eyelid
  • 30. 30
  • 31. CNS (Central Nervous System)  Quinolones may displace the neuroinhibitor GABA, resulting in CNS stimulation  Dizziness  Headache  Insomnia  Restlessness Phototoxicity  Skin damage after exposure to UV light due to toxic reactions.  These included second-degree burns, discoloration and sometimes permanent discoloration and scarring of the skin. 31
  • 32. 32
  • 33. 33 Gastrointestinal  Depletion of magnesium and disruption of cellular enzyme function  Disruption of mitochondrial function and energy production  Other common side effects are :  Nausea  Vomiting  Anorexia  Diarrhea
  • 34. 1. NSAIDs :  Enhance the CNS toxicity of quinolones 2. Theophylline, Caffeine or Warfirine  Plasma concentration is increased by Ciprofloxacin 3. Antacid or Iron salts  Reduce the absorption of quinolones 34
  • 35.  2nd generation fluoroquinolone  Most potent fluoroquinolone against P. aeruginosa  Not effective against Gram +ve and anaerobes  Mainly effective against Gram –ve bacteria : Enterobacteriacae H. Influenzae Campylobacter M. Catarrhalis Pseudomonas N. Gonorrhea  Intracellular Pathogen : M. Tuberculosis Mycoplasma Chlamydia Legionella Brucella 35
  • 36. 36 CLINICAL USE :  Urinary Tract Infections  Travellers’ diarrhoea  Anthrax  Diabetic foot infections UNIQUE QUALITIES :  It binds to divalent cations which decreases absorption.  Because of its good penetration into bone, orally administered ciprofloxacin is a useful alternative to parenterally administered antibiotics for the treatment of osteomyelitis caused by susceptible organisms.
  • 37. 37 MARKETED PREPARATIONS :  Ciplox eye drop / Ciloxan eye drop or ointment : Used in conjuctivitis, corneal ulcer and before opthalmic surgery
  • 38. 38  Neocip 500 mg : Cipla  C-flox 250 mg : Intas  Ciprodac 500 mg : Cadila
  • 39.  3rd generation fluoroquinolone  Levo-isomer  100% oral bioavailability  Effective against Gram +ve and Gram –ve bacteria  Also effective against Pathogen : Legionella pneumophila Atypical respiratory pathogens Mycobacterium tuberculosis 39
  • 40. 40 CLINICAL USE :  Urinary tract infections  Chronic bronchitis  Nosocomial pneumonia  Intra-abdominal infections UNIQUE QUALITY :  It binds to divalent cations which decreases absorption
  • 41. 41 MARKETED PREPARATIONS :  Levoslog tablet  Levotec tablet  Wecure ablet
  • 42. 42