Unikpef - instructions for use, dose, side effects, contraindications

Auxiliary substances: corn starch, microcrystalline cellulose, sodium carboxymethyl starch (type A), silicon dioxide colloid, magnesium stearate, dye Opaprai II white 85F28751 (polyvinyl, partially hydrolysed, alcohol, titanium dioxide, macrogol 4000 / PEG 3000, talc).

Description:white or yellowish-white tablet in a film shell in the form of a capsule with a risk on one side.

Pharmacotherapeutic group:antimicrobial agent, fluoroquinolone.

ATX: & nbsp

J.01.M.A.03 Pefloxacin

Pharmacodynamics:

Antimicrobial agent from the group of fluoroquinolones. It has a bactericidal effect, blocks DNA gyrase, replicates the A-subunit of DNA, RNA and disrupts the synthesis of bacterial proteins.

With respect to Gram-negative strains effectively acts as dividing cells, and cells in the resting stage; in the case of gram-positive strains - only on cells that are in the process of mitotic division. Has a wide range of action.

It is active against most aerobic gram-negative bacteria: Escherichia coli, Klebsiella spp., indole-positive and indole-negative Proteus spp., at. t.ch. Proteus mirabilis, Enterobacter spp., Morganella morgana, Yersinia enterocolitica, Vibrio cholerae, Vibrio parahaemolyticus, Neiserii gonorrhoeae, Neiserii meningitidis, Haemophilus influenzae, Pseudomonas aeruginosa, Moraxella catarrhalis, Pasteurella multocida, Campylobacter spp., Serratia spp., Citrobacter spp., Salmonella spp., Shigella spp., Haemophilus spp., Neisseria gonorrhoeae.

Aerobic Gram-positive bacteria: Staphylococcus spp., (including, producing and not producing penicillinase and methicillin-resistant), Streptococcus spp., in t.ch. Streptococcus pyogenes, Streptococcus agalactiae, Corynebacterium diphtheriae, Listeria monocytogenes, intracellular bacteria: Legionella spp in t.ch. Legionella pneumophila, Brucella spp., Chlamidia spp., as well as against bacteria that produce beta-lactamase. Suppresses vital functions Mycoplasma spp and Helicobacter.

Moderately sensitive microorganisms: Pneumococcus, Acinetobacter spp., Clostridium perfringens, Pseudomonas spp., Chlamydia trachomatis.

Stable microorganisms: gram-negative anaerobes, Treponema spp., Mycobacterium tuberculosis.

Pharmacokinetics:

Absorption - high, 20 minutes after ingestion of a single dose (400 mg) absorbed 90%.

The time to reach the maximum concentration (4 μg / ml) is 90 to 120 minutes, the therapeutic concentration is held for 12 to 15 hours. After repeated administration, the maximum concentration in the blood is 10 μg / ml; concentration in bronchial mucosa - 5 mcg / ml; the ratio between the concentration in the mucosa and the blood is 100%. Connection with plasma proteins - 25 - 30%.

Well penetrates into tissues and body fluids, including. in the bronchial secretion, the lungs, the prostate gland, spinal fluid and bone tissue. Volume of distribution

- 1.5 - 1.8 l / kg. Concentration in the cerebrospinal fluid after a triple intake of 400 mg - 4.5 μg / ml, with an increase in the dose of up to 800 mg - 9.8 μg / ml; the ratio between the concentration in the plasma and the liquid is 89%. Concentration in other organs and tissues 12 hours after the last dose: thyroid gland 11.4 μg / g, salivary glands 2.2 μg / g, skin 7.6 μg / g, nasopharyngeal 6 μg / g, amygdala 9 μg / g , muscle - 5.6 mcg / g.

Metabolised in the liver by methylation to dimethylphexlocacin (has significant antibacterial activity), oxidized to Noxide and conjugated with glucuronic acid to form pefloxacin-glucuronide.

The half-life is 8-10 hours, with repeated administration, 12-13 hours. It is excreted by the kidneys - 60%, with bile - 30% unchanged; partially in the form of metabolites. The content of unchanged drug in the urine after 1 to 2 hours after administration is 25 μg / ml, after 12-24 hours - 15 μg / ml. Unchanged pefloxacin and its metabolites are detected in urine within 84 hours after the last administration. Poor dialysis (extraction ratio - 23%).

Indications:

Treatment of infections caused by microorganisms sensitive to the drug: infections of the kidneys and urinary tract, gastrointestinal tract (including salmonellosis, typhoid fever), infections of the gallbladder and bile ducts (cholecystitis, cholangitis, empyema of the gallbladder), infection of the pelvic organs (in including adnexitis and prostatitis); bones, joints, skin and soft tissues, infection of the lower respiratory tract and ENT organs (middle ear and paranasal sinuses, pharynx and larynx), eye infections; intra-abdominal abscesses, peritonitis; sepsis, septicemia, endocarditis, meningoencephalitis, osteomyelitis, gonorrhea, chlamydia, prostatitis, epididymitis, soft chancre; surgical and nosocomial infections, prevention of surgical infection.

Contraindications:

Hypersensitivity, epilepsy, hemolytic anemia, deficiency of glucose-6-phosphate dehydrogenase, pregnancy, lactation period, children's age (under 18 years).

Carefully:atherosclerosis of cerebral vessels, cerebral circulation disorder, organic CNS lesions, convulsive syndrome of unknown etiology, renal and / or hepatic insufficiency.

Pregnancy and lactation:contraindicated

Dosing and Administration:

Inside, on an empty stomach, the doses are selected individually, depending on the localization and severity of the infection, as well as the sensitivity of microorganisms.

In uncomplicated infections - 0.4 g 2 times a day, the average daily dose - 0.8 g in 2 divided doses. Tablets are swallowed without chewing and drinking with a lot of water.

In patients with impaired liver function, correction of the dosing regimen is required: with minor violations, the drug is prescribed at a dose of 0.4 g / day; with more severe violations - every 36 hours; with severe liver pathology, the interval between administrations is extended to 2 days. The course of treatment - no more than 30 days.

Patients with impaired renal function (with creatinine clearance below 20 ml / min) single dose should be 50% of the average dose - with a multiplicity of appointment 2 times a day, or a full single dose administered once a day.For elderly people, the dose of the drug is reduced by about 1/3.

Side effects:

From the nervous system: depression, headache, dizziness, fatigue, insomnia, increased convulsive alertness, anxiety, agitation, tremor, rarely - convulsions.

On the part of the digestive system: nausea, vomiting, diarrhea, abdominal pain, anorexia, flatulence, pseudomembranous colitis, transient increase in "liver" transaminases, cholestatic jaundice, hepatitis, necrosis of the liver.

From the urinary system: crystalluria, rarely - glomerulonephritis, dysuria.

Allergic reactions: skin rash, skin itch, urticaria, skin hyperemia, photosensitivity, rarely - Quincke's edema, bronchospasm, arthralgia.

From the hematopoietic system: leukopenia, neutropenia, thrombocytopenia (at doses of 1600 mg / day), agranulocytosis, eosinophilia.

Other: tachycardia, myalgia, tendonitis, tendon rupture, candidiasis.

Overdose:

Treatment: the specific antidote is unknown. Symptomatic therapy, with necessity - hemodialysis and peritoneal dialysis.

Interaction:

Cimetidine and others.inhibitors of microsomal oxidation increase the half-life, reduce overall clearance, but do not affect the volume of distribution and renal clearance.

Pefloxacin reduces the metabolism of theophylline in the liver, which leads to an increase in the concentration of theophylline in the plasma and central nervous system (in order to avoid the development of intoxication, the dose of theophylline should be reduced).

Significantly reduces the prothrombin index (in patients taking indirect anticoagulants - a continuous monitoring of the blood picture is necessary).

Covering agents slow absorption.

The simultaneous use of beta-lactam antibiotics can prevent the development of resistance during the treatment of staphylococcal infection. Aminoglycosides, piperacillin, azlocillin, ceftazidime increase the antibacterial effect (including infection with Pseudomonas aeruginosa).

Drugs that block tubular secretion, slow the excretion of pefloxacin.

Special instructions:

With smigazhyh infections, perforativnyh processes in the abdominal cavity, with infections of the pelvic organs - combined with drugs that are active against anaerobes (metronidazole, clindamycin).

During treatment, patients should receive a large amount of fluid (to prevent crystalluria).

Due to the possible appearance of photosensitization, during the treatment period one can not be exposed to UV radiation.

For patients with severe liver and kidney disease, dose adjustment is required, in proportion to the degree of damage.

If serious and persistent diarrhea occurs during or after treatment with pefloxacin, the development of pseudomembranous colitis should be ruled out (immediate withdrawal of the drug and the appropriate treatment).

Effect on the ability to drive transp. cf. and fur:During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 400 mg. 10 tablets in a blister AL / PVC; 2 or 10 blisters together with instructions for use are placed in a cardboard box.

Packaging:(10) - packings cellular planimetric (10) - packs cardboard
(10) - packings, cellular, outline (2) - packs, cardboard

Storage conditions:

Store in a dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N012529 / 01

Date of registration:17.01.2008

The owner of the registration certificate:Unik Pharmaceutical Laboratories Unik Pharmaceutical Laboratories India

Manufacturer: & nbsp

UNIQUE PHARMACEUTICAL Laboratories India

Information update date: & nbsp30.08.2015

Illustrated instructions

Instructions

Unicpef® (Unikpef®)