PEMEFLOX
-
Chemical Name:
Pefloxacin (Mesilate Dihydrate) -
Therapeutic Category:
Antimicrobial -
Pharmacologic Category:
Antibiotic, Quinolone -
Pharmaceutical Form:
Ampoule -
Composition:
Pefloxacin (Mesilate Dihydrate) 400mg/5ml
PEMEFLOX
Injection (Ampoule)
Pefloxacin Mesilate
1-PHARMACOLOGY:
Synthetic bactericidal antibiotic belonging to the quinoline group.
The antibacterial spectrum of Pefloxacin is as follows:
-Usually susceptible strains (M.I.C. equal to or less than 1 µg/ml): Escherichia coli, Klebsiella, Enterobacter, Serratia, Proteus mirabilis, Proteus indo+, Citrobacter, Salmonella, Shigella, Haemophilus, Staphylococcus, Neisseria gonorrhea.
-Inconstantly susceptible strains: Streptococci and Pneumococci, Pseudomonas, Acinetobacter, Clostridium perfringens, Mycoplasma, Chlamydiae.
-Usually resistant strains: (M.I.C. more than 4 µg/ml): Gram negative anaerobic microorganisms, Spirochetes, Mycobacterium tuberculosis.
2-PHARMACOKINETICS:
Distribution (concentrations in serum):
-Single dose:
The maximum concentration in serum after single administration of 400 mg is around 4 µg/ml at the end of perfusion (1 h)
Serum half-time of elimination is around 12 hours.
-Repeated doses:
After parenteral administration of 400 mg every 12 hours, the following characteristics are observed after the 9th dose: maximum concentration in serum around 10 µg/ml.
Serum half-time of elimination around 12 hours.
30 % binding to plasma proteins.
Diffusion in tissues:
Distribution volume: about 1.7 liter/kg after administration of a single dose of 400 mg.
After repeated administrations, concentrations in tissues are good and varies between 5,6 µg/g in muscle and 11,4 µg/g in thyroid gland.
Biotransformation:
It is mainly metabolized in the liver. Both major metabolites are demethylated norfloxacin and pefloxacin-N-oxide.
Excretion:
-In individual with normal renal and hepatic functions: Half the administered dose of Pefloxacin is excreted unchanged in urine.
-Urine concentrations of unchanged Pefloxacin reach 25 µg/ml between the 1st and 2nd hour after administration.
-In patients suffering from renal insufficiency: significant changes are not observed in serum concentrations of Pefloxacin even when the disease is severe. Pefloxacin is poorly dialyzed (mean extraction coefficient: 23%)
-In patients suffering from hepatic insufficiency: changes in the pharmacokinetics of Pefloxacin are observed in a trial using a single dose of 8 mg/kg body weight in patients suffering from cirrhosis: significantly reduced drug clearance in plasma leading to significant increase in the half-time of elimination (3 to 5 times greater) as well as a significant increase in urine excretion of unchanged Pefloxacin (3 to 4 times greater).
3-INDICATIONS:
In adults, they are restricted to severe infections with gram-negative bacilli and staphylococci that are susceptible; namely in their following manifestations:
- Septicemic, endocarditic, meningeal, respiratory, otorhinolaryngologic, renal and urinary,
gynecologic, abdominal, hepatic, biliary, osteoarticular, cutaneous.
4-CONTRA-INDICATIONS:
-Allergy to quinolone.
-Children under 15 years of age.
-Deficiency in glucose-6-phosphate dehydrogenase.
-Pregnancy and lactation.
5-PRECAUTIONS:
-Severe hepatic insufficiency: Dosage should be adjusted accordingly.
-The patient must not be exposed to sunlight nor UV light during treatment because of the risk of photosensitization.
-Streptococci and pneumococci are not always susceptible to Pefloxacin. The antibiotic must therefore not be used as the primary treatment of non-nosocomial respiratory infections, in the absence of any specific bacteriologic study.
6-DRUG INTERACTIONS:
It is advised not to use the drug with anti-acids.
7-ADVERSE REACTIONS:
It may rarely cause:
Photosensitization and cutaneous eruptions, muscular and/or joint pain, headaches, insomnia, gastric pain, nausea and vomiting.
All these disorders are reversible upon discontinuation of treatment.
8-DOSAGE & ADMINISTRATION:
Intravenously: Injections of PEMEFLOX must be prescribed in slow intravenous infusion (1 hour) after dilution of the 400 mg ampoule into 250 ml of 5% glucose solution (2 injections per day in the morning and evening). Saline solution (NaCl) or any other solution containing chlorine ions must not be added because of the risk of precipitation.
Dosage:
-In adults with normal hepatic function: average of 800 mg/day.
A first dose of 800 mg may be indicated to reach efficacious blood levels more rapidly.
-In adults with hepatic insufficiency: The daily dose must be adapted in patients suffering from severe hepatic insufficiency or reduced hepatic blood flow by increasing the interval in between two administration.
A more specific method may be recommended for intravenous injections: 8 mg/kg body weight in 1 hour infusion:
-Twice a day in the absence of absence of icterus or ascites.
-Once a day in the presence of icterus.
-Every 36 hours in the presence of ascites.
-Every other day in the presence of both icterus and ascites.
9-PACKAGING & COMPOSITION:
PEMEFLOX – Injection: A pack of 5 or 25 ampoules of 5mL in a carton. Each Ampoule (5mL) contains Pefloxacin Mesilate Dihydrate equiv. to Pefloxacin 400 mg.
10-STORAGE CONDITIONS:
Ampoules of PEMEFLOX must be protected from light.
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