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

Core: corn starch (88.86 mg), lactose monohydrate (78.43 mg), calcium hydrophosphate dihydrate (30.00 mg), magnesium stearate (9.71 mg), talc (5.00 mg), silicon dioxide colloid (11 , 43 mg), sodium glycolate (6.57 mg);

Sheath: hypromellose (5.00 mg), talc (7.14 mg), titanium dioxide (1.71 mg), macrogol 4000 (2.14 mg).

Description:White round biconvex tablets.

Pharmacotherapeutic group:antibiotic-macrolide.

ATX: & nbsp

J.01.F.A Macrolides

J.01.F.A.06 Roxithromycin

Pharmacodynamics:

Semisynthetic antibiotic group of macrolides for oral administration.Bacteriostatic action: binding to the 50S ribosomal subunit, inhibits the translocation and transpeptidation reaction, the formation of peptide bonds between the amino acids and the peptide chain inhibits protein synthesis by ribosomes, resulting in inhibiting the growth and reproduction of bacteria.

In vitro, the drug is sensitive to: Streptococcus agalactiae, Streptococcus pneumoniae (Pneumococcus), Neisseria meningitides (Meningococcus), Listeria monocytogenes, Mycoplasma pneumoniae, Chlamydia trachomatis, Ureaplasma urealyticum, Legionella pneumophila, Helicobacter pylori (Campylobacter), Gardnerella vaginalis, Bordetella pertussis, Moraxella catarrhalis (Branhaniella catarrhalis), Haemophilus ducreyi.

The following microorganisms. Variable sensitivity demonstrated in vitro: beta-hemolytic Streptococcus group A (Streptococcus pyogenes), Staphylococcus aureus, Haemophilus influenziae, Staphylococcus epidermidis.

Pharmacokinetics:

Absorption is fast. The maximum concentration in the blood plasma after ingestion is 150 mg to 6.6 mg / l, the time to reach the maximum concentration is 2.2 hours, after taking 300 mg to 9.6 mg / l and 1.5 hours, respectively. In children, the maximum plasma concentration (at 2-fold reception of 2.5 mg / kg / day) - 8.7-10.1 mg / l is reached after 2 hours from the reception interval of 12h maintains the effective concentration in blood for 24 hours. The. The equilibrium concentration in the plasma with admission 150 mg twice a day for 10 days is reached between 2 and 4 days and is 9.3 mg / l; when taken 300 mg twice a day for 11 days, 10.9 mg / l.

It penetrates well into the lungs (concentration 5.6-3.7 mg / kg), in palatine tonsils (2.6-1.7 mg / kg) and in the prostate gland (2.8-2.4 mg / kg), inside cells, especially in neutrophilic leukocytes and monocytes, stimulating their phagocytic activity. Virtually does not penetrate the hemato-encephalic barrier. The volume of distribution is 31.2 liters. The connection with plasma proteins (mainly with acidic glycoprotein, to a lesser degree - with albumins and lipoproteins) - 96%, Wears saturable and decreases at concentrations above 4 mg / l.

It is partially metabolized. The elimination half-life is 10.5-14 hours, in children from 1 month to 13 years old it is up to 20 hours. It is excreted mainly with calcified masses (more than 50% of the active substance), the rest - kidneys (10%), lungs (15%) . Less than 0.05% of the dose given is excreted in breast milk.

In severe chronic renal failure, the elimination half-life is 25 hours and the area under the concentration curve increases, and the kidney clearance decreases. In elderly patients (60-79 years), the area under the concentration curve and half-life increases, renal clearance decreases (renal function decreases), however, the amount of the drug released by the kidneys does not change.

In patients with alcoholic cirrhosis of the liver, the half-life and the maximum concentration in the blood plasma increase significantly.

Indications:

Infections of mild and moderate severity caused by drug-susceptible pathogens:

- lower respiratory tracts - acute bronchitis, pneumonia caused by Streptococcus pneumoniae, atypical pneumonia caused by Mycoplasma pneumoniae;

- LOP organs - pharyngitis, tonsillitis, sinusitis, otitis media caused by beta-hemolytic streptococcus of group A and Streptococcus pneumoniae;

- skin and soft tissues - erysipelas, pyoderma caused by Staphylococcus aureus and beta-hemolytic group A streptococcus;

- urinary tract - urethritis in men, caused by Chlamydia trachomatis and Ureaplasma urealyticum.

Contraindications:

Hypersensitivity, simultaneous reception of ergotamine, dihydroergotamine (risk of developing symptoms of "ergotism"), cisapride, pimozide, astemizole and terfenadine; pregnancy, lactation, Children under 12 years of age and weighing less than 40 kg, taking into account the given dosage regimen.

For medicinal forms containing lactose (optional): lactose intolerance.

Carefully:Hepatic insufficiency (cirrhosis of the liver with jaundice and / or ascites), renal failure, elderly age, simultaneous reception with colchicine,dopaminimulants - alkaloids of ergot (including bromocriptine, cabergoline, lisuride, pergolide), cyclosporin, theophylline.

Pregnancy and lactation:

Dosing and Administration:

Inside, adults -150 mg 2 times a day, morning and evening, before meals or 300 mg once. The course of treatment is determined individually, depending on the indications, the severity of the infection process and the activity of the pathogen; for infections caused by beta-hemolytic streptococcus, the course of treatment should be at least 10 days. With hepatic insufficiency, -150 mg once a day.

Children and adolescents older than 12 years with a body weight above 40 kg - both for adults.

Side effects:Nausea, vomiting, decreased appetite, changes in taste and / or smell, epigastric pain, diarrhea, increased activity of "liver" transaminases and alkaline phosphatases, cholestatic or hepatocellular acute hepatitis, pancreatitis; dizziness, headache, paresthesia, allergic reactions (bronchospasm, urticaria, rash, purpura, angioedema, anaphylactic shock), development of superinfection.

Overdose:Treatment: gastric lavage, symptomatic treatment, there is no specific antidote.

Interaction:

Increases the absorption of digoxin, increasing the risk of its toxic effects (requires ECG monitoring and digoxin concentrations in blood plasma). Clinically significant interaction with warfarin was not revealed. An increase in prothrombin time or the International Normalized Relationship (MHO) has been reported with simultaneous intake with vitamin K antagonists, so during the treatment period it is necessary to monitor MHO.

Increases the half-life and area under the concentration curve of midazolam (increased and prolonged duration of action). Increases the concentration in the plasma of theophylline, cyclosporine.

Increases serum; the concentration of astemizole, cisapride, pimozide, which leads to an extension of the Q-T interval and / or severe arrhythmias (ECG monitoring is necessary).

Can displace the disopyramide from the connection with plasma proteins, leading to an increase in its concentration in the serum-blood (requires monitoring of the ECG and the concentration of disopyramide in the blood plasma).

Ergotamine and ergotamine-like vasoconstrictive drugs lead to the development of "ergotism", necrosis of limb tissues.

Special instructions:

With liver failure during the period of treatment, it is necessary to monitor the function of the liver.

With the development of superinfection or pseudomembranous colitis roxithromycin should immediately be abolished and appropriate therapy prescribed.

If the course of treatment lasts more than 14 days, it is necessary to regularly monitor the liver function and renal function, as well as the blood picture.

Effect on the ability to drive transp. cf. and fur:Patients taking the drug should refrain from potentially dangerous activities associated with the need for concentration and increased speed of psychomotor reactions.

Form release / dosage:

The tablets covered with a cover of 150 mg.

Packaging:For 10 tablets in PVC-aluminum blister. For 1, 2 blisters in a cardboard box along with instructions for use.

Storage conditions:In the dark place at a temperature of no higher than 25 ° C. In a place inaccessible to children.

Shelf life:

2 years. Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-010986/09

Date of registration:31.12.2009/30.05.2016

The owner of the registration certificate:Esparma GmbHEsparma GmbH Germany

Manufacturer: & nbsp

LINDOPHARM, GmbH Germany

Representation: & nbspESPARMA GmbH ESPARMA GmbH Germany

Information update date: & nbsp12.06.2016

Illustrated instructions

Instructions

Esparoxy (Esparoxy)