Cefalexin

General characteristics. Structure:

Active agent: cefalexin monohydrate of 263 mg that corresponds to the content of cefalexin of 250 mg

Excipients: magnesium stearate, cellulose microcrystallic PH 102.

Structure of a cover of the capsule: titanium dioxide (E171), dye ferrous oxide yellow (E172), indigo carmine (Indigotin I) (E132), gelatin.
 
Active agent: cefalexin monohydrate of 525.9 mg that corresponds to the content of cefalexin of 500 mg

Excipients: magnesium stearate, cellulose microcrystallic PH 102.

Structure of a cover of the capsule: titanium dioxide (E171), dye ferrous oxide yellow (E172), dye ferrous oxide black (E172), indigo carmine (Indigotin I) (E132), gelatin.

Pharmacological properties:

Tsefalosporinovy antibiotic of the I generation. Works bakteritsidno, breaks synthesis of a cell wall of microorganisms. It is steady against lactamelements.
Has a broad spectrum of activity. It is active concerning gram-positive microorganisms - Staphylococcus spp., (including Staphylococcus aureus strains producing and not producing a penicillinase, penicillin - sensitive strains of Staphylococcus epidermidis), Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes), Corynebacterium diphtheriae; gram-negative microorganisms - Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp., Salmonella spp., Escherichia coli, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella catarrhalis, Proteus mirabilis; Treponema spp., radiant mushrooms.
Proteus spp is inefficient concerning Pseudomonas aeruginosa. (indolpositive strains), Morganella morganii, Mycobacterium tuberculosis, Enterococcus faecalis, Haemophilus spp., Enterobacter spp., Serratia spp., Pseudomonas spp., Aeromonas spp., Acinetobacter spp., Methicillinum resistant strains, anaerobic microorganisms.
It is steady against a penicillinase of stafilokokk, but collapses tsefalosporinazy gram-negative microorganisms.

Pharmacokinetics. After intake it is quickly and well soaked up. Bioavailability - 90-95%, meal slows down absorption, but does not influence its completeness. Time of achievement of Cmax after intake 0.25, 0.5 or 1 g - 1 h, the size Cmax - 9, 18 and 32 mkg/ml, respectively.
Therapeutic concentration remains during 4-6 h. Communication with proteins of plasma - 10-15%. Vd - 0.26 l/kg.
It is distributed rather evenly in various fabrics and liquids of an organism: lungs, liver, heart, kidneys, bile, gall bladder, bones, joints, respiratory tracts. Badly gets through not changed GEB. Passes through a placenta, in a small amount it is allocated with breast milk, it is found in amniotic liquid.
It is not metabolized.
T1/2 is 0.9-1.2 h. The general clearance - 380 ml/min. It is removed by kidneys - 70-89% in not changed look (2/3 - glomerular filtering, 1/3 - canalicular secretion); with bile - 0.5%. Renal clearance - 210 ml/min.
At disturbance of secretory function of kidneys concentration in blood increases, and removal time is extended with kidneys, T1/2 after intake is 5-30 h. It is moderately removed by means of a hemodialysis, it is good - by means of peritoneal dialysis.

Indications to use:

— infections of upper and lower respiratory tracts (pharyngitis, average otitis, sinusitis, quinsy, bronchitis, acute and exacerbation of chronic pneumonia, bronchial pneumonia, empyema and abscess of lungs);
— infections of urinogenital system (pyelonephritis, cystitis, urethritis, prostatitis, epididymite, endometritis, gonorrhea, vulvovaginitis);
— infections of skin and soft tissues (furunculosis, abscess, phlegmon, pyoderma, lymphadenitis, lymphangitis);
— infections of bones and joints (including osteomyelitis).

Route of administration and doses:

Inside, in 30-60 min. prior to food, washing down with water.
The average dose for adults and children is more senior than 10 years - on 250 - 500 mg each 6 h. The daily dose of drug has to make not less than 1-2 g, if necessary can be increased to 4 g. Duration of a course of treatment - 7-14 days. At the infections caused by a beta and hemolitic streptococcus of group A, the minimum duration of treatment makes 10 days.
To adult patients with a renal failure the daily dose is reduced taking into account KK value: at KK of 5-20 ml/min. the maximum daily dose makes 1.5 g/days; at KK less than 5 ml/min. - 0.5 g/days. The daily dose is divided into 4 receptions.
To children aged up to 10 years drug is recommended to appoint in the form of suspension for intake. At body weight less than 40 kg an average daily dose - 25-100 mg/kg of body weight; frequency rate of reception - 4 At average otitis - a dose of 75 mg/kg/days, frequency rate of reception - 4 times/days. At streptococcal pharyngitis, infections of skin and soft tissues frequency rate of reception - 2 times/days. At the heavy course of infections the daily dose can be increased to 100 mg/kg of body weight, and frequency rate of reception - to 6 times/days.
Suspension preparation: to add water to risks to a bottle and it is good to shake up. The prepared suspension is stable at the room temperature within 14 days. Before each use suspension needs to be shaken up. 5 ml of ready suspension contain 250 mg of cefalexin.

Features of use:

Patients with allergic reactions to penicillin and karbapenema in the anamnesis can have hypersensitivity to tsefalosporinovy antibiotics.
During treatment by cefalexin positive forward reaction of Koombs, and also false positive reaction of urine to glucose is possible.
During treatment it is not recommended to use ethanol.
At patients with a renal failure cumulation is possible (correction of the mode of dosing is required).
At a staphylococcal infection there is a cross resistance between cephalosporins and izoksazolilpenitsillina.

Side effects:

Allergic reactions: rash, urticaria, a Quincke's edema, an erythema, it is rare - an eosinophilia, a toxic epidermal necrolysis, Stephens-Johnson's syndrome, an acute anaphylaxis.

From the alimentary system: pain in a stomach, dryness in a mouth, anorexia, nausea, vomiting, diarrhea, toxic hepatitis, cholestatic jaundice, increase in activity of hepatic transaminases and an alkaline phosphatase, candidiasis of intestines, an oral cavity, a pseudomembranous coloenteritis.

From a nervous system: dizziness, weakness, headache, excitement, hallucinations, spasms.

From urinogenital system: intersticial nephrite, an itch of generative organs and an anus, a vaginitis, allocations from a vagina, candidiasis of generative organs.

From bodies of a hemopoiesis: leukopenia, neutropenia, thrombocytopenia.

From a musculoskeletal system: arthralgia, arthritis.

Laboratory indicators: increase in a prothrombin time.

Interaction with other medicines:

At simultaneous use with furosemide, Acidum etacrynicum, nefrotoksichny antibiotics (for example, aminoglycosides) the risk of damage of kidneys increases.

Salicylates and indometacin slow down cefalexin removal.

Cefalexin reduces a prothrombin ratio, strengthens effect of indirect anticoagulants.

Contraindications:

— children's age up to 3 years (for a dosage form - the capsule);
— hypersensitivity (including to others beta лактамным to antibiotics).

With care - a renal failure, pseudomembranous colitis (in the anamnesis), pregnancy, the lactation period, chest age (up to 6 months - for suspension).

Use of the drug CEFALEXIN at pregnancy and feeding by a breast
Use of drug at pregnancy and in the period of a lactation perhaps only in that case when the estimated advantage for mother exceeds potential risk for a fruit.
In need of purpose of drug in the period of a lactation it is necessary to stop breastfeeding.

Use at renal failures
To adult patients with a renal failure the daily dose is reduced taking into account KK value: at KK of 5-20 ml/min. the maximum daily dose makes 1.5 g/days; at KK less than 5 ml/min. - 0.5 g/days. The daily dose is divided into 4 receptions.

Use for children
Contraindication: children's age up to 3 years (for a dosage form - the capsule). To children aged up to 10 years drug is recommended to appoint in the form of suspension for intake.

Overdose:

Symptoms: vomiting, nausea, pains in epigastriums, diarrhea, a hamaturia.

Treatment: absorbent carbon (is more effective, than lavage), maintenance of passability of respiratory tracts, monitoring - the vital functions, blood gases, electrolytic balance.

Storage conditions:

List B. To store in the place, unavailable to children, at a temperature from 15 °C to 25 °C.

Issue conditions:

According to the recipe

Packaging:

Капс. 250 mg: 16 pieces.

Капс. 500 mg: 16 pieces.