Esparoxy, 150 mg 10 pcs

Pharmacodynamics

Esparoxy is a semi-synthetic oral macrolide antibiotic. It has bacteriostatic action: by binding to 50S subunit of ribosomes it inhibits translocation and transpeptidation reactions, formation of peptide bonds between amino acids and peptide chain, inhibits protein synthesis by ribosomes and as a result inhibits bacterial growth and reproduction.

In vitro to the drug are sensitive: Streptococcus agalactiae, Streptococcus pneumoniae (Pneumococcus), Neisseria meningitidis (Meningococcus), Listeria monocytogenes, Mycoplasma pneumoniae, 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 in vitro: group A beta-haemolytic streptococcus (Streptococcus pyogenes), Staphylococcus aureus, Haemophilus influenzae, Staphylococcus epidermidis.

Pharmacokinetics

Absorption is fast. C_max in plasma after oral administration of 150 mg is 6.6 mg/L, T_max is 2.2 h, after administration of 300 mg is 9.6 mg/L and 1.5 h respectively. In children, C_max in plasma (at 2 times administration of 2.5 mg/kg/day) is 8.7-10.1 mg/l and is reached after 2 h.

Administration at 12-hour intervals ensures that effective blood concentrations are maintained for 24 hours. C_ss in plasma when 150 mg twice daily for 10 days is reached between days 2 and 4 and is 9.3 mg/L; when 300 mg twice daily for 11 days is 10.9 mg/L.

It penetrates well into the lungs (concentrations are 5.6-3.7 mg/kg), the palatine tonsils (2.6-1.7 mg/kg) and prostate (2.8-2.4 mg/kg), inside cells, especially neutrophil leukocytes and monocytes, stimulating their phagocytic activity.

It practically does not penetrate through the GEB. V_d is 31.2 l. Binding with plasma proteins (mainly with acidic glycoprotein, to a lesser extent with albumin and lipoprotein) is 96%, has a saturable character and decreases at concentrations above 4 mg/L.

It is partially metabolized. T_1/2 is 10.5-14 h, in children aged 1 month to 13 years, up to 20 h. It is eliminated mainly in the faeces (more than 50% of the active substance), the rest in the kidneys (10%) and lungs (15%). Less than 0.05% of the taken dose is excreted with the breast milk.

In severe chronic renal failure T_1/2 – 25 h and AUC increases, renal clearance decreases. In elderly patients (60-79 years), AUC and T_1/2 increase, renal clearance decreases (decreased renal function), but the amount of drug excreted by the kidneys does not change.

In patients with alcoholic cirrhosis, T_1/2 and C_max in plasma are significantly increased.

Indications

Respiratory tract infections, Urinary tract infections, Infectious diseases, Skin infections

Infections of mild to moderate severity caused by pathogens sensitive to the drug:

• lower respiratory tract – acute bronchitis, pneumonia caused by Streptococcus pneumoniae, atypical pneumonia caused by Mycoplasma pneumoniae;
• loral organs – pharyngitis, tonsillitis, sinusitis, otitis media caused by group A beta-haemolytic streptococcus and Streptococcus pneumoniae;
• skin and soft tissue – rye, pyoderma caused by Staphylococcus aureus and group A beta-hemolytic streptococcus;
• renal tract – urethritis in men caused by Chlamydia trachomatis and Ureaplasma urealyticum.

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Active ingredient

Roxithromycin

Composition

1 coated tablet contains:

the active substance:

• roxithromycin 150 mg,

excipients:

• corn starch – 88.86 mg;

• lactose monohydrate – 78.43 mg;

• calcium hydrophosphate dihydrate – 30 mg;

• Magnesium stearate – 9.71 mg;

• talk – 5 mg;

• Colloidal silicon dicoside – 11.43 mg;

• sodium glycolate – 6.57 mg

coating:

Hypromellose, 5 mg; talc, 7.14 mg; titanium dioxide, 1.71 mg; macrogol 4000, 2.14 mg

How to take, the dosage

Esparoxy is taken orally, adults – 150 mg 2 times a day, morning and evening, before a meal, or 300 mg once. The course of treatment is determined individually, depending on the indications, the severity of the infectious process and the activity of the pathogen; in infections caused by beta-haemolytic streptococcus, the course of treatment should be at least 10 days. In case of hepatic insufficiency – 150 mg once a day.

Children and adolescents over 12 years of age with a body weight of more than 40 kg – as for adults.

Interaction

It increases the absorption of digoxin, increasing the risk of its toxic effects (ECG and plasma concentrations of digoxin should be monitored). No clinically significant interaction with warfarin has been found. Increased PV or MHO have been reported when concomitantly administered with vitamin K antagonists, so MHO should be monitored during treatment.

increases T_1/2 and AUC of midazolam (increasing and prolonging the duration of action). Increases plasma concentrations of theophylline, cyclosporine.

increases serum concentrations of astemisol, cisapride, pimozide, which leads to prolongation of the QT interval and/or severe arrhythmias (ECG monitoring is required).

May displace disopyramide from plasma protein binding, leading to increased serum concentrations (ECG and plasma disopyramide concentrations should be monitored).

Ergotamine and ergotamine-like vasoconstrictors lead to the development of “ergotism”, necrosis of limb tissues.

Special Instructions

In case of hepatic insufficiency, liver function should be monitored during treatment. If superinfection or pseudomembranous colitis develops, roxithromycin should be immediately discontinued and appropriate therapy should be prescribed.

If the course of treatment lasts more than 14 days, liver and kidney function tests and blood counts should be monitored regularly.

Impact on the ability to drive a car or perform work requiring increased speed of physical and mental reactions. Patients taking the drug should refrain from potentially hazardous activities requiring concentration and increased speed of psychomotor reactions.

Contraindications

• Hypersensitivity;
• current use of ergotamine, dihydroergotamine (risk of ergotism symptoms), cisapride, pimozide, astemizole and terfenadine;
• pregnancy;
• lactation period;
• children under 12 years of age and with a body weight less than 40 kg.

For dosage forms containing lactose (optional), lactose intolerance.

With caution: liver failure (cirrhosis with jaundice and/or ascites), renal failure, advanced age, simultaneous use with colchicine, dopamine stimulants – ergot alkaloids (including bromocriptine, cabergoline, lisuride, pergolide), cyclosporine, theophylline.

Side effects

• Nausea,
• vomiting,
• decreased appetite,
• change in taste and/or sense of smell,
• pigastric pain,
• diarrhea,
• decreased liver transaminase activity,

alkaline phosphateepigastric pain,

• diarrhea,
• increased liver transaminase and alkaline phosphatase activity,
• cholestatic or hepatocellular acute hepatitis,
• pancreatitis;
• dizziness,
• headache,
• paresthesias,allergic reactions (bronchospasm, urticaria, rash, purpura, angioedema, anaphylactic shock),
• development of superinfection.

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Overdose

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

Similarities

Roxithromycin