CIPROFLOXACIN
Introduction
DRUG : Ciprofloxacin
BRAND NAME : Baycip
Company name : Bayer
CATEGORY : Antibiotic
Description:- Ciprofloxacin is a
synthetic chemotherapeutic antibio
tic of the fluoroquinolone drug class. It
is a second-generation
fluoroquinolone antibacterial
Ciprofloxacin: Chemical Structure
Ciprofloxacin is a 4-quinolone antibacterial durg
Effective against gram- O
positive and gram-
negative pathogens. F CO2H
N
N
Ciprofloxacin
HN
Effective against Confers potent
pseudomonas antimicrobial activity
Ref : Drugs 1988 (35: 373-447)
Mechanism of Action:
Mechanism of Action
Ciprofloxacin inhibits DNA gyrase enzyme which
is responsible for super coiling of DNA.
It acts as bactericidal in bacteria which are
actively multiplying and even those which are
stationary.
Ciprofloxacin gets concentrated in all the tissues
as the volume of distribution of drug is high,
sufficient to eradicate infections.
PHARMACOKINETICS
Oral bioavailability – good
Good volume of distribution.
Eliminated from body in short time and
hence no cumulation.
Less plasma protein binding and therefore
more drug available at tissue sites.
CIPROFLOXACIN: ANTIBACTERIAL SPECTRUM
Antibacterial spectrum ciprofloxacin has in vitro activity against a wide range of gram-negative, gram-
positive and atypical pathogens.
Gram-positive Gram-negative Atypical
S.epidermidis E.coli, L.pneumophila
S.pneumoniae H.influenzae M.pneumoniae
S.pyogenes K.pneumoniae C.trachomatis
N.gonorrhoeae
P.mirabilis
S.typhii
Serratia,
Shigella
M.catarrhalis
Pseudomonas
Others: Mycobacterium tuberculosis
Market Formulations & Strenghts:
Ciprofloxacin is available as:
Tablets (100 mg, 250 mg, 500 mg, 750 mg
or 1000 mg)
Intravenous solutions (5% and 10%, 100
mL)
Eye and ear drops
Dosage and Administration:
RECOMMENDED STARTING AND MAINTENANCE DOSES FOR
PATIENTS WITH IMPAIRED RENAL FUNCTION
Creatinine Clearance (mL/min) Dose
50 Usual Dosage.
30 – 50 250 – 500 mg q 12 h
5 – 29 250 – 500 mg q 18 h
Patients on hemodialysis 250 – 500 mg q 24 h
or Peritoneal dialysis (after dialysis)
Dosage Administration:
Infection Severity Dose Frequency Usuaual
Duration
Urinary Tract Acute Uncomplicated 250 mg q 12 h 3 days
Mild/Moderate 250 mg q 12 h 7 to 14
days
Severe/Complicated 500 mg q 12 h 7 to 14
days
Indications:
On promotion:
Multi drug resistant-typoih and paratyphoid fever.
Urinary tract infections
Surgical prophylaxis
Surgical bound infections
Otitis media
Acute sinusitis.
Indications:
General indications:
LRTI
ENT infections
Infectious diarrhea, dysentery and typhoid fever
Paratyphoid fever
Cholera
UTI (acute, sub acute and chronic)
Skin and soft tissue infections
Orthopedic infections
Gynecological infections
Gall bladder infections
Gonorrhea
Chancroid
Contraindications :
Hypersensitivity to the drug
Epilepsy or convulsions
Pregnancy, lactation.
Overdose:
Overdose of ciprofloxacin may result in reversible
renal toxicity. Treatment of overdose includes
emptying of the stomach via induced vomiting or
by gastric lavage. Administration of magnesium,
aluminum, or calcium containing antacids can
reduce the absorption of ciprofloxacin.
Side Effects:
dizziness, fainting, fast or pounding heartbeat;
sudden pain or swelling near your joints (especially in your arm or
ankle);
diarrhea that is watery or bloody;
confusion, hallucinations, depression, unusual thoughts or behavior;
seizure (convulsions);
pale or yellowed skin, dark colored urine, fever, weakness;
numbness, tingling, or unusual pain anywhere in your body;
fever, sore throat, and headache with a severe blistering, peeling, and
red skin rash; or
the first sign of any skin rash, no matter how mild.
Adverse Effects:
Gastro Intestinal Tract – All quinolones have varying
degrees of GIT irritation ranging from mild nausea to
severe gastritis which can be limited by administering ½ hr
after food.
Central Nervous System effects The Pharmacodynamic
Drug interactions with NSAIDs manifest sometimes as
convulsions.
Cardio Vascular System Toxicity.
Phototoxicity.
Leading Manufacturing Companies:
Brand Company
Cifron-CT Ranbaxy
Ciplox-TZ Cipla
Zoxin- TZ FDC
Ciprolets-A Dr. Reddys
Alcipro-TN Alkem
Quintor TZ Torrent
Ciprobid TZ Zy.alidac
HIGHLIGHTS OF CIPROFLOXACIN
The most potent fluorinated quinolone
Has a very broad spectrum of antibacterial activity
Ensures rapid bactericidal activity at very low
concentrations
Is rapidly distributed and adequate levels are achieved in
most tissues and body fluids with high intracellular
concentrations in the phagocytes
Good bioavailability with an extended half-life of elimination
CIPROFLOXACIN: A SUCCESS STORY
Ciprofloxacin, has become a remarkable
success story in the pharmaceutical industry,
not only for being the first oral antimicrobial
drug with broad spectrum that can be used to
treat day-today as well as serious infections,
but also for its penetration into the
commercial market place.