Sumaclide - instructions for use, doses, side effects, contraindications

hypromellose (hydroxypropylmethylcellulose) - 0.0126 g
sodium lauryl sulfate - 0.0018 g
calcium stearate - 0.0144 g
sodium stearyl fumarate - 0.0144 g
sodium croscarmellose - 0.0432 g
calcium phosphate disubstituted two-water (calcium hydrogen phosphate dihydrate) until the mass of the core is 1.2 g

Shell accessories:

hypromellose (hydroxypropylmethylcellulose) 0.029535 g

titanium dioxide (titanium dioxide) - 0.0025 g
polysorbate-80 (tween-80) 0.0029 g
colourant "Ponso 4R", E 124 0.000065 g

Description:The tablets covered with a film cover, pink color of the oblong form with biconcave surfaces. On the cross-section, two layers are visible: the outer layer is pink, the inner one is white or almost white.

Pharmacotherapeutic group:Antibiotic - azalide

ATX: & nbsp

J.01.F.A.10 Azithromycin

Pharmacodynamics:

Antibacterial agent of a wide spectrum of action, azalide, acts bacteriostatically. Communicating with 50S subunit of ribosomes, inhibits peptidranslokase at the stage of translation, suppresses protein synthesis, slows the growth and multiplication of bacteria, has a bactericidal effect at high concentrations. Effects on extracorporeal and intracellular pathogens.

It is active against Gram-positive aerobic microorganisms: Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes, Staphylococcus aureus (methicillin-sensitive); Gram-negative aerobic organisms: Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Legionella pneumophila, Neisseria gonorrhoeae, Pasteurella multocida; some anaerobic microorganisms: Prevotella spp., Clostridium perlringens, Fusobacterium spp., Porphyriomonas spp.; a also Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.

Microorganisms that can develop resistance to azithromycin: gram-positive aerobes (Streptococcus pneumoniae (penicillin-resistant). Initially, stable microorganisms: gram-positive aerobes (Enterococcus faecalis, Staphylococcus spp. (methicillin-resistant staphylococci exhibit a very high degree of resistance to macrolides), Gram-positive bacteria resistant to erythromycin); anaerobes (Bacteroides lragilis).

Inactive against Gram-positive bacteria, resistant to erythromycin.

Pharmacokinetics:

Azithromycin is rapidly absorbed from the gastrointestinal tract, which is due to its stability in an acidic environment and lipophilicity. Bioavailability after a single dose of 0.5 g - 37% (the effect of "first passage" through the liver), the maximum concentration of the drug in the plasma after oral intake of 0.5 g - 0.4 mg / l, the time to reach the maximum concentration of the drug in plasma - 2 , 5-2.9 h; in tissues and cells the concentration is 10-50 times higher than in serum, the volume of distribution is 31.1 l / kg. Easily passes the histohematological barriers. It penetrates well into the respiratory tract, urino-genital organs and tissues, into the prostate gland, into the skin and soft tissues; accumulates in a medium with low pH, in lysosomes (which is especially important for the eradication of intracellular pathogens). It is also transported by phagocytes, polymorphonuclear leukocytes and macrophages. It penetrates the membranes of cells and creates high concentrations in them.

The concentration in the foci of infection is significantly higher (by 24-34%) than in healthy tissues, and correlates with the severity of the inflammatory edema.In the focus of inflammation persists in effective concentrations within 5-7 days after taking the last dose. The connection with plasma proteins is 7-50% (inversely proportional to the concentration in the blood).

In the liver demethylated, the metabolites formed are not active. Plasma clearance - 630 ml / min: the half-life of the drug between 8 and 24 hours after admission is 14-20 hours, the half-life of the drug in the interval from 24 to 72 hours is 41 hours. 50% is excreted with bile in unchanged form, 6% kidneys.

Eating significantly changes the pharmacokinetics: the maximum concentration of the drug in the plasma increases (by 31%), the area under the concentration-time curve does not change. In elderly men (65-85 years) pharmacokinetic parameters do not change, in women the maximum concentration of the drug in plasma increases (by 30-50%).

Indications:

Urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis).

Contraindications:

Hypersensitivity to azithromycin, other macrolides, other components of the drug, increased sensitivity to erythromycin; ketolides; simultaneous administration with ergotamine and dihydroergotamine, severe impairment of liver function (Child-Pugh class C); severe impairment of the function of the lobes (creatinine clearance less than 40 ml / min); the period of breastfeeding, children under 18 years (for a given dosage).

Carefully:

Myasthenia gravis, mild and moderate liver function disorders, disorders functions of the lobes of light and moderate severity (creatinine clearance more than 40 ml / min), in patients with proarrhythmogenic factors (especially in elderly patients): with congenital or acquired lengthening of the interval QT, in patients receiving antiarrhythmic drug therapy classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with disturbances of water-electrolyte balance, especially in case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure; simultaneous use of digoxin, warfarin, cyclosporine.

Pregnancy and lactation:

Use during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

For the duration of treatment, breastfeeding should be discontinued (no data on penetration into breast milk).

Dosing and Administration:

Inside, without chewing, 1 hour before or 2 hours after eating 1 time per day.

In cases of urinary tract infections caused by Chlamydia trachomatis (Urethritis, cervicitis): uncomplicated urethritis / cervicitis - 1 g (1 tablet of 1000 mi^-) once.

When used in patients with impaired renal function of mild and moderate severity, a dose adjustment ns is required.

When used in patients with impaired liver function of mild and moderate severity, in elderly patients a dose adjustment ns is required.

Side effects:

- From the digestive system: anorexia, nausea, vomiting, changes in the language of color, dry mucous membranes of the mouth, burping, ulcer oral mucosa, increased secretion of the salivary glands, abdominal pain, flatulence, constipation, dyspepsia, dysphagia, bloating, diarrhea, pseudomembranous colitis, melena , pancreatitis, increased activity "liver" transaminases, bilirubin, hepatitis, cholestatic jaundice, fulminant hepatitis, hepatic failure (possibly fatal), hepatic necrosis; in addition, a decrease in appetite, gastritis.

- From the cardiovascular system: heart palpitations, chest pain, lowering blood pressure, increasing the interval QT an electrocardiogram, an arrhythmia of the type "pirouette", a ventricular tachycardia, "tides" of blood to the face.

- On the part of the hematopoiesis system: leukopenia, neutropenia, eosinophilia, thrombocytopenia, hemolytic anemia.

- From the nervous system: dizziness, headache, vertigo, drowsiness, paresthesia, agitation, fatigue, tinnitus, hyperkinesia, anxiety, neurosis, sleep disorders, sweating, insomnia, hypnosis, aggression, fainting, convulsions, psychomotor hyperactivity, nervousness, agitation, delirium, hallucinations.

- From the sense organs: visual impairment, conjunctivitis, reversible hearing impairment down to deafness, hearing disorder, taste disorders, loss of taste sensations, perversion of smell, loss of smell.

- From the genitourinary system: vaginal candidiasis, dysuria, pain in the kidney, interstitial nephritis, acute renal failure, metrorrhagia, dysfunction of the testes.

- Allergic reactions: rash, hives, itching of the skin, angioedema, anaphylactic reaction, Stevens-Johnson syndrome, necrolysis, erythema multiforme.

- From the skin: dermatitis, dry skin, photosensitization.

- From the musculoskeletal system: myasthenia gravis, myalgia, back pain, neck pain, arthralgia, osteoarthritis.

- From the respiratory system: shortness of breath, nosebleed.

- Infectious diseases: rhinitis, pharyngitis, respiratory diseases, pneumonia, gastroenteritis, candidamycosis of the oral mucosa.

- Other: asthenia, face swelling, fever, peripheral edema.

- Laboratory data: in blood plasma: an increase in the number of basophils, monocytes, neutrophils, a decrease or increase in the concentration of bicarbonates, an increase in the activity of alkaline phosphatase, an increase in the content of chlorine, an increase in the concentration of glucose, an increase in the number of platelets, an increase in hematocrit, a change in sodium content, increased urea concentration, the content of potassium.

Overdose:

Symptoms: severe nausea, temporary loss of hearing, vomiting, diarrhea.

Treatment: gastric lavage, symptomatic therapy.

Interaction:

Antacids (A13 + and Mg2 + -containing), ethanol and food slow down and reduce the absorption of azithromycin (for oral forms), so the interval between their intake should be 1 hour before or 2 hours after ingestion and these medications.

With the simultaneous use of warfarin and azithromycin (in usual doses), no changes in prothrombin time have been detected, however, considering that the interaction of macrolides and warfarin may enhance the anticoagulation effect, patients need careful monitoring of prothrombin time.

Azithromycin weakly interacts with cytochrome P450 isoenzymes, it was revealed that azithromycin participates in pharmacokinetic interactions similar to erythromycin and other macrolides, azithromycin It is not an inducer and inhibitor of cytochrome P450 isoenzymes.

In contrast to macrolides, no interaction with theophylline, terfenadine, carbamazepine, triazolam, digoxin was noted.

Care should be taken when using terfenadine and azithromycin concurrently, since it has been established that simultaneous use of terfenadine and various types of antibiotics causes arrhythmia and lengthening of the duration of the ventricular complex, reflecting the duration of the ventricular systole.Proceeding from this, it is impossible to exclude the aforementioned complications in the joint use of terfenadine and azithromycin.

Ergotamine and dihydroergotamine: increased toxic effect (vasospasm, dysesthesia). Macrolides slow down excretion, increase plasma concentrations and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, and drugs that undergo microsomal oxidation (carbamazepine, terfenadine, ciclosporin, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic drugs), however, no such interaction was observed with the use of azalides (including azithromycin).

Lincosamides weaken, and tetracycline and chloramphenicol increase the effectiveness of azithromycin.

With cetirizine: simultaneous use for 5 days in healthy volunteers azithromycin with cetirizine (20 mg) did not lead to a pharmacokinetic interaction and a significant change in the interval QT.

With Didanosine: simultaneous use of azithromycin (1200 mg / day) and didanosine (400 mg / day) in 6 HIV-infected patients showed no change in the pharmacokinetic indications of didanosine compared with the placebo group.

With zidovudine: simultaneous use of azithromycin (a single dose of 1000 mg and repeated administration of 1200 mg or 600 mg) has little effect on the pharmacokinetics, including kidney excretion, zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear.

With atorvastatin: simultaneous use of atorvastatin (10 mg per day daily) and azithromycin (500 mg daily) did not cause changes in the concentrations of atorvastatin in blood plasma (based on the inhibition of GMA-CoA reductase). However, separate reports of cases of rhabdomyolysis in patients simultaneously receiving azithromycin and statins.

With cimetidine: according to the results of a study aimed at determining the effect of a single dose of cimetidine, taken 2 hours before taking azithromycin, on its pharmacokinetics, no changes were detected.

With efavirenz: simultaneous use of azithromycin (600 mg / day once) and efavirenz (400 mg / day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction.

With fluconazole: simultaneous use of azithromycin (1200 mg once) did not change the pharmacokinetics of fluconazole (800 mg once). The total exposure and the half-life of azithromycin did not change with the simultaneous use of fluconazole, but a decrease in the maximum concentration of azithromycin by 18% was observed, which was not clinically significant.

With indinavir: simultaneous use of azithromycin (1200 mg once) did not cause a statistically significant effect on the pharmacokinetics of indinavir (800 mg three times a day for 5 days).

With nelfinavir: the simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the equilibrium concentration of azithromycin in the blood plasma, clinically significant side effects were not observed and dosage adjustment of azithromycin when used simultaneously with nelfinavir is not required.

With rifabutin: with simultaneous use of azithromycin and rifabutin, neutropenia was sometimes observed, despite the fact that neutropenia was associated with the use of rifabutin, a causal relationship between the use of a combination of azithromycin and rifabutin and neutropenia has not been established.

With sildenafil: when used in healthy volunteers, there is no evidence of the effect of azithromycin (500 mg / day for 3 days) with combined application does not affect the area under the pharmacokinetic curve "concentration-time" (AUC), the maximum concentration (Cmax), time to reach the maximum concentration ( Cmax), rate of elimination rate and half-life of sildenafil or its main circulating metabolite.

With trimethoprim / sulfamethoxazole: simultaneous use of trimethoprim / sulfamethoxazole with azithromycin did not reveal a significant effect on the maximum concentration, total exposure or renal excretion of trimethoprim or sulfamethoxazole. The concentrations of azithromycin in the serum corresponded to those detected in other studies.

With the simultaneous use of azithromycin and cyclosporine, a dose adjustment of cyclosporine is necessary.

Special instructions:

In case of missed dose, the missed dose should be taken as soon as possible, and the subsequent dose should be taken at intervals of 24 hours.

It is necessary to observe a break of 2 hours with simultaneous use of antacids. Azithromycin should be used with caution in patients with impaired liver function of mild and moderate severity due to the possibility of developing fulminant hepatitis and hepatic insufficiency; in patients with impaired renal function of mild and moderate severity (under the control of the state of kidney function).

In the presence of symptoms of liver dysfunction (rapidly increasing asthenia, jaundice, darkening of the urine, a tendency to bleeding, hepatic encephalopathy) therapy with azithromycin should be discontinued and an examination of the functional state of the liver should be carried out.

Contraindicated simultaneous administration of azithromycin with derivatives of ergotamine and dihydroergotamine because of the possible development of ergotism.

As with the use of other antibacterial drugs, with drug therapy azithromycin should regularly monitor patients for the presence of non-susceptible microorganisms and signs of development of superinfections, including fungal.

When taking the drug azithromycin possibly the development of pseudomembranous colitis caused by Clostridium difficile, as in the form of mild diarrhea, hack and severe colitis. With the development of antibiotic-associated diarrhea against the background of taking the drug azithromycin, and also 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded. During the treatment with azithromycin, taking drugs that inhibit the intestinal peristalsis is contraindicated.

Effect on the ability to drive transp. cf. and fur:

It is necessary to refrain from activities related to the need for high concentration of attention and rapid psychomotor reactions (including driving) during drug treatment.

Form release / dosage:

Tablets, film-coated, 1000 mg.

Packaging:

3 tablets in a planar cell packaging made of polyvinylchloride film and aluminum foil printed lacquered.

3 tablets in a polymer can.

1 jar or 1 contour mesh package with instructions but applied in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not apply but the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003007

Date of registration:01.06.2015

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp20.08.2015

Illustrated instructions

Instructions

Sumaclide (Sumaklid)