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 grampositive and gramF negative pathogens.
O CO2H

N
Ciprofloxacin

HN

Effective against pseudomonas

Confers potent 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 Usual Dosage.

50

30 50
5 29 Patients on hemodialysis or Peritoneal dialysis

250 500 mg q 12 h
250 500 mg q 18 h 250 500 mg q 24 h (after dialysis)

Dosage Administration:

Infection

Severity

Dose

Frequency

Usuaual

Duration
Urinary Tract Acute Uncomplicated 250 mg q 12 h 3 days

Mild/Moderate
Severe/Complicated

250 mg q 12 h
500 mg q 12 h

7 to 14 days
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 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
Ciplox-TZ Zoxin- TZ

Ranbaxy
Cipla FDC

Ciprolets-A
Alcipro-TN Quintor TZ

Dr. Reddys
Alkem 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.