Sumamed, 100 mg/5 ml 20.925 g strawberry flavor

Pharmacotherapeutic group: antibiotic-azolid

ATCode: J01FA10

Pharmacological properties

Pharmacodynamics.

Azithromycin is a bacteriostatic broad-spectrum antibiotic of the group of macrolide-azalid. It has a broad spectrum of antimicrobial action. Azithromycin mechanism of action is associated with inhibition of microbial cell protein synthesis. Binding to 50S-subunit of ribosome, it inhibits peptide translocase at the translation stage and inhibits protein synthesis, slowing down the growth and reproduction of bacteria. In high concentrations it has a bactericidal effect.

It has activity against a number of Gram-positive, Gram-negative, anaerobic, intracellular and other microorganisms.

Microorganisms can be resistant to the antibiotic from the start or they can become resistant to it.

In most cases, susceptible microorganisms

1. Gram-positive aerobes

Staphylococcus aureus methicillin-sensitive Streptococcus pneumoniae Streptococcus pyogenes

2. Gram-negative aerobes Haemophilus influenzae Haemophilus parainfluenzae Legionella pneumophila Moraxella catarrhalis

Pasteurella multocidaPasteurella multocida Neisseria gonorrhoeae

3. Anaerobes Clostridium perfringens Fusobacterium spp. Prevotella spp. Porphyriomonas
4. Other microorganisms.Chlamydia trachomatis Chlamydia pneumoniae Chlamydia psittaci Mycoplasma pneumoniae Mycoplasma hominis

Borrelia burgdorferi

Microorganisms capable of developing resistance to azithromycin Gram-positive aerobes

Streptococcus pneumoniae penicillin-resistant Initially resistant microorganisms Gram-positive aerobes

Enterococcus faecalis

Staphylococci (methicillin-resistant Staphylococcus aureus has a very high frequency of acquired resistance to macrolides)

Gram-positive bacteria that are resistant to erythromycin.

Anaerobes

Bacteroides fragilis

Pharmacokinetics.

Azithromycin is well absorbed and rapidly distributed in the body after oral administration. After a single dose of 500 mg bioavailability is 37% (first pass effect), maximum concentration (0.4 mg/l) in blood is achieved after 2-3 hours, the volume of distribution is 31.1 l/kg, binding to proteins is inversely proportional to the concentration in blood and is 7-50%. It penetrates through cell membranes (effective in infections caused by intracellular pathogens). It is transported by phagocytes to the site of infection, where it is released in the presence of bacteria. Easily passes the histohematic barriers and enters the tissues. Concentration in tissues and cells is 10-50 times higher than in plasma, and in the focus of infection it is 24-34% higher than in healthy tissues.

Asithromycin has a very long half-life of 35-50 h. The tissue elimination half-life is much longer. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is mainly excreted unchanged – 50% by the intestine, 6% by the kidneys. In the liver it is demethylated, losing activity.

Indications

Bronchitis, Urethritis, Respiratory tract infections, Otitis, Angina, Lung inflammation (pneumonia), Infectious diseases, Skin infections, Pharyngitis, Tonsillitis, Guaymonitis

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

• Infections of the upper respiratory tract and ENT organs (pharyngitis/tonsillitis, sinusitis, otitis media);

• Infections of the lower respiratory tract: Acute bronchitis, exacerbation of chronic bronchitis, pneumonia, incl.ч.

• Infections of the skin and soft tissues (rye, impetigo, secondary infected dermatosis);

• The initial stage of Lyme disease (borreliosis) – erythema migrans (erythema migrans).

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Active ingredient

Azithromycin

Composition

1 g powder for oral suspension preparation contains:

Active ingredient:

azithromycin dihydrate* – 25.047 mg, in terms of azithromycin 23.895 mg;

excipients:

sucrose* 929.753 mg,

sodium phosphate 20.00 mg,

hyprolose 1.60 mg,

xanthan gum 1.60 mg,

How to take, the dosage

Ingestion, once a day, 1 hour before or 2 hours after a meal. After taking Sumamed^® the child should always be offered a few sips of water so that he can swallow the rest of the suspension.

Before each administration of the drug the contents of the bottle should be shaken thoroughly until a homogeneous suspension is obtained. If the desired volume of suspension has not been withdrawn from the bottle within 20 minutes after shaking, the suspension should be shaken again, the desired volume taken away and given to the child.

The required dose is taken using a 1 ml syringe with a nominal capacity of 5 ml (100 mg azithromycin) of suspension or a measuring spoon with a nominal capacity of 2.5 ml (50 mg azithromycin) or 5 ml (100 mg azithromycin) of suspension placed in the carton box with the bottle.

After use, the syringe (previously disassembled) and the measuring spoon are washed with running water, dried and stored in a dry place until the next administration of Sumamed^®.

Infections of the upper and lower respiratory tract, ENT organs, skin and soft .tissues

At the rate of 10 mg/kg body weight once a day for 3 days (course dose 30 mg/kg).

In pharyngitis/tonsillitis caused by Streptococcus pyogenes, Sumamed^® is used at a dose of 20 mg/kg/day for 3 days (course dose 60 mg/kg). The maximum daily dose is 500 mg.

In Lyme disease (initial stage of borreliosis) – erythema migrans (erythema migrans): on day 1 at a dose of 20 mg/kg/day, then from day 2 to day 5 at a dose of 10 mg/kg/day (course dose 60 mg/kg).

In patients with impaired renal function: In patients with a GFR of 10 – 80 ml/min, no dose adjustment is required.

In impaired hepatic function: When used in patients with mild to moderate hepatic impairment, no dose adjustment is required.

Elderly patients: Dose adjustment is not required. In elderly patients, special caution is recommended with Sumamed^® due to the possible presence of proarrhythmogenic factors that may increase the risk of cardiac and pirouette arrhythmias.

Method of preparation and storage of suspension

The contents of the bottle intended for preparation of 20 ml of suspension (nominal volume) are added to 12 ml of water using a syringe for dispensing. Shake until a homogeneous suspension is obtained. The volume of the resulting suspension will be about 25 ml, which exceeds the nominal volume by about 5 ml. This is to compensate for the unavoidable loss of suspension during dosing the drug. The prepared suspension can be stored at a temperature not exceeding 25 °C for not more than 5 days.

Interaction

Antacid drugs

The antacid drugs do not affect the bioavailability of azithromycin, but decrease the maximum blood concentration by 30%, so the drug should be taken at least one hour before or two hours after taking these

drugs and meals.

Cetirizine

Concomitant use for 5 days in healthy volunteers of azithromycin with cetirizine (20 mg) did not result in a pharmacokinetic interaction or significant change in QT interval.

Didanosine (didezoxynosine)

The concomitant use of azithromycin (1200 mg/day) and didanosine (400 mg/day) in 6 HIV-infected patients showed no change in the pharmacokinetic readings of didanosine compared with the placebo group.

Digoxin (P-glycoprotein substrates)

. Concomitant use of macrolide antibiotics, including azithromycin, with P-glycoprotein substrates such as digoxin results in higher serum P-glycoprotein substrate concentrations. Thus, when concomitant use of azithromycin and digoxin is necessary to consider the possibility of increasing the concentration of digoxin in the blood serum.

Zidovudine

The concomitant use of azithromycin (single administration of 1000 mg and multiple administration of 1200 mg or 600 mg) has little effect on pharmacokinetics, including renal excretion of zidovudine or its glucuronide metabolite. However, azithromycin administration caused an increase in the concentration of phosphorylated zidovudine, the clinically active metabolite, in peripheral blood mononuclear cells.

The clinical significance of this finding is unclear.

Asithromycin interacts weakly with cytochrome P450 isoenzymes.

Azithromycin has not been found to be involved in pharmacokinetic interactions similar to those of erythromycin and other macrolides. Azithromycin is not an inhibitor and inducer of cytochrome P450 isoenzymes.

Sorgonum alkaloids

In view of the theoretical possibility of ergotism, concomitant use of azithromycin with derivatives of ergot alkaloids is not recommended.

Pharmacokinetic studies have been performed on the concomitant use of azithromycin and drugs metabolized by cytochrome P450 isoenzymes.

Atorvastatin

Concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in plasma concentrations of atorvastatin (based on HMK-CoA reductase inhibition analysis). However, in the post-registration period there were isolated reports of cases of rhabdomyolysis in patients receiving azithromycin and statins simultaneously.

Carbamazepine

Pharmacokinetic studies with healthy volunteers showed no significant effect on plasma concentrations of carbamazepine and its active metabolite in patients receiving azithromycin concomitantly.

Cimetidine

In pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin, no changes in the pharmacokinetics of azithromycin were found, provided that cimetidine was used 2 hours before azithromycin.

Indirect-acting anticoagulants (coumarin derivatives)

In pharmacokinetic studies, azithromycin did not affect the anticoagulant effect of a single dose of 15 mg warfarin taken by healthy volunteers. Potentiation of anticoagulant effect has been reported after concomitant use of azithromycin and indirect anticoagulants (coumarin derivatives). Despite the fact that causal relationship has not been established, the need for frequent monitoring of prothrombin time when using azithromycin in patients receiving oral anticoagulants of indirect action (coumarin derivatives) should be considered.

Cyclosporine

. In a pharmacokinetic study involving healthy volunteers who took oral azithromycin (500 mg/day once) for 3 days followed by cyclosporine (10 mg/kg/day once), a significant increase in the maximum plasma concentration (Cmax) and area under the concentration-time curve (AUC0-5) of cyclosporine was found. Caution should be exercised when concomitant use of these drugs. If concomitant use of these drugs is necessary, plasma concentrations of cyclosporine should be monitored and the dose should be adjusted accordingly.

Efavirenz

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

Fluconazole

Concomitant use of azithromycin (1200 mg once daily) did not alter the pharmacokinetics of fluconazole (800 mg once daily). Total exposure and half-life of azithromycin were not altered by concomitant use of fluconazole, but there was a decrease in Cmax of azithromycin (by 18%), which had no clinical significance.

Indinavir

The concomitant use of azithromycin (1200 mg once) had no statistically significant effect on the pharmacokinetics of indinavir (800 mg three times daily for 5 days).

Methylprednisolone

Asithromycin has no significant effect on the pharmacokinetics of methylprednisolone.

Nelfinavir

The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times daily) causes increased equilibrium serum concentrations of azithromycin. No clinically significant adverse effects have been observed and no dose adjustment of azithromycin is required when used concomitantly with nelfinavir.

Rifabutin

The concomitant use of azithromycin and rifabutin has no effect on the serum concentrations of either drug. Neutropenia was sometimes observed when azithromycin and rifabutin were used concomitantly. Although neutropenia has been 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.

Sildenafil

When used in healthy volunteers, there is no evidence of an effect of azithromycin (500 mg/day daily for 3 days) on the AUC and Cmax of sildenafil or its major circulating metabolite.

Terfenadine

In pharmacokinetic studies there has been no evidence of interaction between azithromycin and terfenadine. Single cases have been reported in which the possibility of such an interaction could not be completely ruled out, but there has been no specific evidence that such an interaction has occurred.

The concomitant use of terfenadine and macrolides has been found to cause arrhythmias and prolongation of the QT interval.

Theophylline

No interaction between azithromycin and theophylline has been identified.

Triazolam/midazolam

There are no significant changes in pharmacokinetic parameters when azithromycin is used simultaneously with triazolam or midazolam in therapeutic doses.

Trimethoprim/sulfamethoxazole

The concomitant use of trimethoprim/sulfamethoxazole with azithromycin showed no significant effect on Cmax, total exposure or renal excretion of trimethoprim or sulfamethoxazole. Serum azithromycin concentrations were consistent with those found in other studies.

Special Instructions

When using Sumamed^® in patients with diabetes mellitus and also on a low-fat diet, note that the suspension contains sucrose (0.32 IU/ 5 ml).

If a dose of Sumamed^® is missed, the missed dose should be taken as soon as possible and the next ones should be taken 24 hours apart.

Sumamed^® should be taken at least one hour before or two hours after taking antacids.

The drug Sumamed^® should be used with caution in patients with mild to moderate hepatic impairment because of the possibility of fulminant hepatitis and severe hepatic impairment.

In the presence of symptoms of hepatic impairment, such as rapidly increasing asthenia, jaundice, darkened urine, bleeding tendency, hepatic encephalopathy, therapy with Sumamed^® should be stopped and liver function testing should be performed.

In patients with impaired renal function: In patients with a GFR of 10 – 80 ml/min, no dose adjustment is necessary.

As with other antibacterials, therapy with Sumamed^® should routinely screen patients for the presence of non-susceptible microorganisms and signs of superinfections, including fungal infections.

The drug Sumamed^® should not be used for longer courses than directed, since the pharmacokinetic properties of azithromycin recommend a short and simple dosing regimen.

There are no data on possible interaction between azithromycin and ergotamine and dihydroergotamine derivatives, but because of the development of ergotism when using macrolides with ergotamine and dihydroergotamine derivatives simultaneously, this combination is not recommended.

Long-term use of Sumamed^® may result in pseudomembranous colitis caused by Clostridium difficile, both as mild diarrhea and severe colitis. If antibiotic-associated diarrhea develops against the background of Sumamed^® therapy, as well as 2 months after the end of therapy, clostridial

pseudomembranous colitis should be excluded. Do not use drugs that inhibit intestinal peristalsis.

In treatment with macrolides, including azithromycin, prolongation of cardiac repolarization and QT interval have been observed, increasing the risk of cardiac arrhythmias, including pirouette arrhythmias, which may lead to cardiac arrest.

We should use Sumamed^® with caution in patients with proarrhythmogenic factors (especially elderly patients), including congenital or acquired prolongation of the QT interval; in patients taking class IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol) antiarrhythmic drugs, cisapride, terfenadine, antipsychotics (pimozide), antidepressants (citalopram) fluoroquinolones (moxifloxacin and levofloxacin), with disorders of fluid and electrolyte balance, especially in case of hypokalemia or hypomagnesemia, clinically significant bradycardia, cardiac arrhythmia or severe heart failure.

The use of Sumamed^® may provoke myasthenic syndrome or worsen myasthenia gravis.

Impact on driving and operating ability

In case of adverse effects on the nervous system and eyesight, caution should be exercised when performing activities requiring increased concentration and rapid psychomotor reaction.

Synopsis

White to yellowish-white powder with characteristic odor of strawberries. After dissolving in water – homogeneous suspension of yellowish-white color with a characteristic odor of strawberries.

Contraindications

Hypersensitivity to azithromycin, erythromycin, other macrolides or ketolides, or other drug components; severe hepatic impairment; sucrose/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption; childhood age <6 months; simultaneous use of ergotamine and dihydroergotamine.

With caution

Myasthenia; mild to moderate hepatic impairment; terminal renal failure with a GFR (glomerular filtration rate) less than 10 ml/min; in patients with proarrhythmogenic factors (especially in older patients): with congenital or acquired prolongation of the QT interval, in patients receiving therapy with antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with electrolyte balance disorders, especially in case of hypokalemia or hypomagnesemia, clinically significant bradycardia, cardiac arrhythmia, or severe heart failure; concomitant use of digoxin, warfarin, cyclosporine, diabetes mellitus.

Side effects

The frequency of side effects is classified in accordance with the recommendations of the World Health Organization: very frequently – at least 10%; frequently – at least 1%, but less than 10%; infrequently – at least 0.1%, but less than 1%; rarely – at least 0.01%, but less than 0.1%; very rarely – less than 0.01%; unknown frequency – cannot be estimated based on available data.

Infectious diseases: infrequent – candidiasis, including oral mucosa, vaginal infection, pneumonia, fungal infection, bacterial infection, pharyngitis, gastroenteritis, respiratory disease, rhinitis; unknown frequency – pseudomembranous colitis.

With the blood and lymphatic system: infrequent – leukopenia, neutropenia, eosinophilia; very rare – thrombocytopenia, hemolytic anemia.

Metabolism and nutrition: infrequent – anorexia.

Allergic reactions: infrequent – angioedema, hypersensitivity reaction; unknown frequency – anaphylactic reaction.

Nervous system disorders: Frequent – headache; infrequent – dizziness, impaired sense of taste, paresthesias, drowsiness, insomnia, nervousness; rare

agitation; unknown frequency – hypoesthesia, anxiety, aggression, syncope, seizures, psychomotor hyperactivity, loss of smell, perverse sense of smell, loss of sense of taste, myasthenia, delirium, hallucinations.

Visual organ: infrequent visual impairment.

Hearing organ and labyrinth disorders: infrequent – hearing disorder, vertigo; unknown frequency – hearing disorder, including deafness and/or tinnitus.

Cardiovascular system: infrequent – palpitations,

“rushes” of blood to the face; unknown frequency – lowering of blood pressure, increased QT interval in the electrocardiogram, arrhythmia type “pirouette”, ventricular tachycardia.

Respiratory system disorders: infrequently – shortness of breath, nasal bleeding.

Gastrointestinal tract: very often – diarrhea; often – nausea, vomiting, abdominal pain; infrequently – flatulence, dyspepsia, constipation, gastritis, dysphagia, bloating, dry oral mucosa, belching, oral mucosa ulcers, increased salivary gland secretion; very rarely – color change of tongue, pancreatitis.

Hepatic and biliary tract: infrequent – hepatitis; rare – impaired liver function, cholestatic jaundice; unknown frequency – liver failure (in rare cases – with fatal outcome, mainly with severe liver impairment); liver necrosis, fulminant hepatitis.

Skin and subcutaneous tissue: infrequent – skin rash, itching, urticaria, dermatitis, dry skin, sweating; rare – photosensitization reaction; unknown frequency – Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, drug rash with eosinophilia and systemic manifestations (DRESS syndrome).

Musculoskeletal system: infrequent osteoarthritis, myalgia, back pain, neck pain; unknown frequency – arthralgia.

Kidney and urinary tract disorders: infrequent dysuria, renal pain; unknown frequency – interstitial nephritis, acute renal failure.

Gender and mammary gland disorders: infrequent – metrorrhagia, impaired testicular function.

Others: infrequent – edema, asthenia, malaise, feeling of fatigue, facial edema, chest pain, fever, peripheral edema.

Laboratory findings: frequent – decreased lymphocyte count, increased eosinophil count, increased basophil count, increased monocyte count, increased neutrophil count, decreased plasma bicarbonate concentration; infrequent – increased activity of aspartate aminotransferase, alanine aminotransferase, increased concentration of bilirubin in blood plasma, increased concentration of urea in blood plasma, increased concentration of creatinine in blood plasma, changes in plasma potassium, increased plasma alkaline phosphatase activity, increased plasma chloride concentration, increased blood glucose concentration, increased platelet count, decreased hematocrit, increased plasma bicarbonate concentration, change in plasma sodium concentration.

Overdose

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

Treatment:symptomatic therapy.

Pregnancy use

During pregnancy and breast-feeding use the drug only if the expected benefits to the mother exceed the potential risk to the fetus and child. If it is necessary to use the drug during breastfeeding, it is recommended to suspend breastfeeding.

Similarities

Azithromycin, Chemomycin, Azitral, Zifactor, Azitrox, Ecomed (Azithromycin), Sumamed, AzitRus, Sumamed forte, Zitrolide forte