Esparoks

General characteristics. Structure:

Active ingredient: 150 mg of a roksitromitsin.

Excipients: kernel: starch corn, lactoses monohydrate, hydrophosphate calcium dihydrate, magnesium stearate, talc, silicon dioxide colloid, sodium glycollate; cover: gipromelloza, talc, titanium dioxide, macrogoal 4000.

Pharmacological properties:

Pharmacodynamics. A semi-synthetic antibiotic of group of macroleads for intake. Has bacteriostatic action: communicating with 50ssubjedinitsey ribosomes, suppresses reactions of a translocation and transpeptidation, process of formation of peptide bonds between amino acids and a peptide chain, slows down protein synthesis by ribosomes therefore growth and reproduction of bacteria oppresses.

Invitro are sensitive to drug: Streptococcus agalactiae, Streptococcus pneumoniae (Pneumococcus), Neisseria meningitides (Meningococcus), Listeria monocytogenes, Mycoplasma pneumonia, Chlamydia trachomatis, Ureaplasma urealyticum, Legionella pneumophila, Helicobacter pylori (Campylobacter), Gardnerella vaginalis, Bordetella pertussis, Moraxella catarrhalis(Branhamella catarrhalis), Haemophilus ducreyi.

The following microorganisms showed variable sensitivity of invitro: beta and hemolitic streptococcus of group A (Streptococcus pyogenes), Staphylococcus aureus, Haemophilus influenzae, Staphylococcus epidermidis.

Pharmacokinetics. Absorption — bystry. The maximum concentration in a blood plasma after intake of 150 mg — 6.6 mg/l, time of achievement of the maximum concentration — 2.2 h, after reception of 300 mg — 9.6 mg/l and 1.5 h respectively. Children have the maximum concentration in a blood plasma (at 2-fold reception of 2.5 mg/kg/days) — 8.7–10.1 mg/l and are reached in 2 h. Reception at an interval of 12 h provides preservation of effective concentration in blood during 24 h. 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 9.3 mg/l; at reception of 300 mg 2 times a day within 11 days — 10.9 mg/l.

Well gets into lungs (concentration of 5.6-3.7 mg/kg), into palatine tonsils (2.6–1.7 mg/kg) and a prostate (2.8–2.4 mg/kg), 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. Communication with proteins of plasma (it is preferential with an acid glycoprotein, to a lesser extent — with albumine and lipoproteins) — 96%, has saturable character and decreases at concentration over 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 an elimination half-life — 25 h and the area under a concentration curve increases, decreases renal clearance. At elderly patients (60–79 years) the area under a concentration curve 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 in a blood plasma considerably increase.

Indications to use:

Infections easy and moderate severity, caused by activators, sensitive to drug:
• the lower respiratory tracts — the acute bronchitis, pneumonia caused by Streptococcus;
• pneumoniae, the atypical pneumonia caused by Mycoplasma pneumoniae;
• ENT organs — the pharyngitis, tonsillitis, sinusitis, average otitis caused by a beta and hemolitic streptococcus of group A and Streptococcus pneumoniae;
• skin and soft tissues — the ugly face, a pyoderma caused by Staphylococcus aureus and a beta and hemolitic streptococcus of group A;
• urinary tract — the urethritis at men caused by Chlamydia trachomatis and Ureaplasma urealyticum.

Route of administration and doses:

Inside, adult — 150 mg 2 times a day, in the morning and in the evening, to food or 300 mg once. The course of treatment is defined individually depending on indications, weight of infectious process and activity of the activator; at the infections caused by a beta hemolitic streptococcus, the course of treatment has to make not less than 10 days. At a liver failure — 150 mg of 1 times a day.

To children and teenagers 12 years with body weight higher than 40 kg — as for adults are more senior.

Features of use:

At a liver failure during treatment it is necessary to control function of a liver.

At development of superinfection or pseudomembranous colitis рокситромицин it is necessary to cancel and appoint the corresponding therapy immediately.

If the course of treatment lasts over 14 days, it is regularly necessary to control indicators of function of a liver and kidneys, and also a blood picture.

Influence on ability to participate in traffic and to operate the vehicles and mechanisms. The patients accepting drug should refrain from potentially dangerous types of activity connected with need of concentration of attention and the increased speed of psychomotor reactions.

Side effects:

Nausea, vomiting, loss of appetite, change of taste and/or sense of smell, pain in epigastric area, diarrhea, increase in activity of "hepatic" transaminases and alkaline phosphatases, a cholestatic or hepatocellular acute hepatitis, pancreatitis; dizziness, headache, paresthesias, allergic reactions (bronchospasm, urticaria, rash, purpura, Quincke's disease, acute anaphylaxis), development of superinfection.

Interaction with other medicines:

Increases digoxin absorption, increasing risk of development of its toxic action (control of an ECG and concentration of digoxin in a blood plasma is necessary). Clinically significant interaction with warfarin is not revealed. It was reported about increase in a prothrombin time or the International Normalized Relation (MHO) at a concomitant use with antagonists of vitamin K therefore during treatment it is necessary to monitorirovat MHO.

Increases an elimination half-life and the area under a concentration curve of midazolam (strengthening and increase in duration of action). Increases concentration in plasma of theophylline, cyclosporine.

Increases serumal concentration of an astemizol, tsizaprid, Pimozidum that leads to lengthening of an interval of Q-T 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 blood serum (control of an ECG and concentration of Disopyramidum in a blood plasma is necessary).

Ergotamine and ergotaminopodobny vasoconstrictive medicines lead to development of "ergotism", a necrosis of tissues of extremities.

Contraindications:

Hypersensitivity, concomitant use of ergotamine, dihydroergotamine (risk of development of symptoms of "ergotism"), tsizaprida, Pimozidum. astemizola and terfenadina; pregnancy, the lactation period, children up to 12 years and with body weight less than 40 kg, taking into account the given dosing mode.

For the dosage forms containing lactose (in addition): lactose intolerance.

With care. A liver failure (cirrhosis with jaundice and/or with ascites), a renal failure, advanced age, a concomitant use with colchicine, dofaminostimulyator — ergot alkaloids (including Bromocriptinum, kabergoliny, lisuridy, pergolidy), cyclosporine, theophylline.

Overdose:

Treatment: the gastric lavage, a symptomatic treatment, a specific antidote does not exist.

Storage conditions:

In the place protected from light, at a temperature not above 25 °C. In the place, unavailable to children. A period of validity - 2 years. Not to use after the term specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated 150 mg. On 10 tablets in the PVC-aluminum blister. On 1, 2 blisters in a cardboard pack together with the application instruction.