Roksigeksal

General characteristics. Structure:

Tablets on 50 mg:
Active agent – рокситромицин 50 mg. Excipients: microcrystallic cellulose, K 30 povidone, half-oxameasures 188, magnesium stearate, isopropyl alcohol, the purified water, titanium dioxide, a gidroksipropilmetiltsellyuloz, PEG 400.

Tablets on 150 mg:
Active agent – рокситромицин 150 mg. Excipients: microcrystallic cellulose, K 30 povidone, half-oxameasures 188, magnesium stearate, isopropyl alcohol, the purified water, titanium dioxide, a gidroksipropilmetiltsellyuloz, PEG 400.

Tablets on 300 mg:
Active agent – рокситромицин 300 mg. Excipients: microcrystallic cellulose, K 30 povidone, half-oxameasures 188, magnesium stearate, isopropyl alcohol, the purified water, titanium dioxide, a gidroksipropilmetiltsellyulyoz, PEG 400.

Pharmacological properties:

Roksitromitsin – a semi-synthetic antibiotic of group of macroleads for intake.
Are usually sensitive to drug: Bordetella pertussis, Borrelia burgdorferi, Moraxella (Branhamella) catarrhalis, Campylobacter coli, Campylobacter jejuni, Chlamydia trachomatis, Chlamidia pneumoniae, Clostridium spp., including Clostridium perfringens, Corynebacterium diphtheriae, Enterococcus, Gardnerella vaginalis, Methi-S-Staphylococcus, Neisseria meningitides, Helicobacter pylori, Legionella multocida, Peptostreprococcus, Porphyromonas, Propionibacterium acnes, Rhodococcus egui, Streptococcus pneumoniae, Streptococcus spp.
Are moderately sensitive to drug: Haemophilus influenzae, Ureplasma urealyticum, Vibro cholerae, Staphylococcus aureus and epidermidis.
Are steady against drug: Acinetobacter spp., Bacteroides fragilis, Enterobacteria; Methi-R Staphylococcus, Pseudomonas spp., Fusobacterium, Mycoplasma hominis, Nocardia.

Pharmacokinetics. Absorption – bystry. The maximum concentration after intake of 150 mg – about 6,6 mg/l, time of achievement of the maximum concentration – 2,2 hours. The drug kinetics in relation to the accepted dose is not linear. The maximum concentration after intake of 300 mg – about 9,6 mg/l, time of achievement of the maximum concentration – 1,5 hours.
Children have the maximum concentration (at double reception of 2,5 mg/kg/days) – 8,7-10,1 mg/l and are reached in 2 hours. Reception at an interval of 12 h provides preservation of effective concentration in blood during 24 h.
At reception by adults of tablets 2 times with an interval of 12 hours in 24 hours still are determined by 150 mg of a roksitromitsin therapeutic active concentration. Equilibrium concentration in plasma at reception of 150 mg 2 times a day within 10 days is reached between 2 and 4 days and makes about 9,3 mg/l; at reception of 300 mg 2 times a day within 11 days – 10,9 mg/l.
Well gets into fabrics, especially into lungs (concentration of 5,6-3,7 mg/kg), palatine tonsils and a prostate, and also in cells, especially into neutrophilic leukocytes and monocytes, stimulating their phagocytal activity.
Practically does not get through a blood-brain barrier.
Distribution volume – 31,2 l.
Linkng with proteins (it is preferential with an acid glycoprotein, to a lesser extent – with albumine and lipoproteins) depends on concentration level that makes about 96% and decreases at increase in concentration of a roksitromitsin higher than 4 mg/l.
It is metabolized partially. An elimination half-life – 10,5-14 h, at children aged from 1 month up to 13 years – to 20 h.
Other part – kidneys (10%), lungs (15%) is removed preferential with a fecal masses (more than 50% of active agent). Less than 0,05% of the accepted dose are allocated with breast milk.
At a heavy chronic renal failure of T1/2 makes 25 h, and AUC increases, the renal clearance decreases.
At elderly patients (60-79 years) AUC and an elimination half-life increases, the renal clearance (depression of function of kidneys), however amount of the drug emitted by kidneys decreases does not change.
At patients with alcoholic cirrhosis the elimination half-life and the maximum concentration considerably increase.

Indications to use:

Infectious – the inflammatory diseases caused by microorganisms, sensitive to a roksitromitsin, including:

- infections of upper parts of respiratory tracts (acute pharyngitises, tonsillitis, sinusitis);
- infections of lower parts of respiratory tracts (pneumonia, bronchitis, bacterial infections at chronic obstructive diseases of lungs, atypical pneumonia);
- infections of skin and soft tissues;
- infections of an urogenital path (except for gonococcal infections), including uretrita, tservikovaginita.

Route of administration and doses:

Tablets on 50 mg:
To children with the body weight of 40 kg drug is appointed depending on body weight, a type of the activator and weight of infectious process. The recommended dose makes 5-8 mg/kg of body weight a day, treatment duration no more than 10 days.
Depending on weight the following dosages are recommended:
Children with the body weight from 7 to 13 kg: on ½ tablets in the morning and in the evening.
Children with the body weight from 14 to 26 kg: on 1 tablet in the morning and in the evening.
Children with the body weight from 27 to 40 kg: on 2 tablets in the morning and in the evening.
To children with body weight more than 40 kg are recommended to accept 2 times a day on 150 mg of a roksitromitsin (i.e. at most 300 mg of a roksitromitsin a day).
At a simultaneous renal and liver failure it is necessary to control the serumal level of a roksitromitsin and if necessary to carry out correction of doses.

Tablets on 150 and 300 mg:
The adult appoint 150 mg of drug 2 times a day, with an interval of 12 h. Purpose of 300 mg once in days is possible.
At elderly patients the dosage and a daily dose of a roksitromitsin do not change.
drug appoint in a dose 150 mg of 1 times a day.
Duration of reception of Roksigeksal depends on indications to use, weight of infectious process and activity of the activator – of 5-12 days at respiratory diseases and ENT organs, up to 2-2,5 months at chronic osteomyelitis; at Chlamidia and mycoplasmal pneumonia – 14 days, at legionellezny pneumonia – up to 21 days.
Roksitromitsin it is necessary to accept without chewing, washing down with enough water, approximately for a quarter of hour to food.

Features of use:

At a liver failure to exercise control of function of a liver.

Side effects:

Nausea, vomiting, anorexia, taste change, abdominal pains, lock/diarrhea (it is rare with blood), meteorism, increase in activity of "hepatic" transaminases and ShchF, giperkreatininemiya, cholestatic or hepatocellular acute hepatitis, pseudomembranous coloenteritis, dizziness, headache, paresthesias, vision disorder and sense of smell, a sonitus; Quincke's disease, bronchospasm, small tortoiseshell, weakness, acute anaphylaxis; rash, hyperemia, eczema; development of superinfection, candidiasis of an oral cavity and vagina, pigmentation of nails.

Interaction with other medicines:

Ergotamine and ergotaminopodobny vasoconstrictors lead to development of "ergotism", a necrosis of tissues of extremities.
Increases digoxin absorption.
Reduces efficiency of indirect anticoagulants.
Increases an elimination half-life of a midozalam (strengthening and increase in duration of action).
Increases concentration in plasma of theophylline, cyclosporine A (does not demand correction of the mode of dosing).
Increases serumal concentration of an astemizol, tsizaprid, Pimozidum that leads to lengthening of an interval of QT and/or heavy arrhythmias (control of an ECG is necessary).
Can force out Disopyramidum from communication with proteins of plasma, leading to increase in its concentration in serum.

Contraindications:

Hypersensitivity to macroleads, a concomitant use of drugs of derivatives of ergotamine and dihydroergotamine, pregnancy, the lactation period, chest age (up to 2 months)

With care – a liver failure.

Overdose:

In case of overdose wash out a stomach and carry out a symptomatic treatment. The specific antidote is absent. The hemodialysis is not effective.

Storage conditions:

List B.
At a temperature not above 25 °C.
In the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, on 50 mg:
On 10 tablets, coated, in a blister strip packaging from polyvinylchloride and aluminum foil. On 1 or 2 blister strip packagings in a cardboard box with the instruction for use.
Tablets, coated, on 150 mg:
On 10 tablets, coated, in a blister strip packaging from polyvinylchloride and aluminum foil. On 1 or 2 blister strip packagings in a cardboard box with the instruction for use.
Tablets, coated, on 300 mg:
On 7, 10 or 14 tablets, coated, in a blister strip packaging from polyvinylchloride and aluminum foil. On 1 blister strip packaging in a cardboard box with the instruction for use.