Spheromycinum

General characteristics. Structure:

Active ingredient: 1,5 or 3 million ME of Spheromycinum.

Auxiliary components: starch corn, croscarmellose sodium, povidone, magnesium stearate, silicon dioxide colloid anhydrous, cellulose microcrystallic.

Structure of a cover: gipromelloza, talc, titanium dioxide (Е 171), macrogoal 400.

Antibacterial agent of group of macroleads of a broad spectrum of activity, the rendering bactericidal and bacteriostatic effect.

Pharmacological properties:

Pharmacodynamics: Active ingredient Spheromycinum is an antibiotic from group of macroleads. The mechanism of antibacterial action is caused by braking of synthesis of protein in a microbic cell due to linkng with the catalytic peptidiltransferazny center of 50S-subunit of ribosomes.

Usually sensitive microorganisms (MPK - the minimum overwhelming concentration of ≤1 mg/l): Streptococcus spp., Staphylococcus spp. (Methicillinum - sensitive strains), Enterococcus spp., Rhodococcus equi, Bacillus cereus, Branhamella catarrhalis, Bordetella pertussis, Helicobacter pylori, Campylobacter spp., Legionella spp., Corynebacterium diphtheriae, Moraxella spp., Mycoplasma pneumoniae, Coxiella spp., Chlamydia spp., Treponema pallidum, Borrelia burgdorferi, Leptospira spp., Propionibacterium acnes, Actinomyces spp., Eubacterium spp., Porphyromonas spp., Mobiluncus spp., Bacteroides spp., Peptostreptococcus spp., Prevotella spp., Toxoplasma gondii.

Moderately sensitive microorganisms (MPK of 1-4 mg/l): Neisseria gonorrhoeae, Ureaplasma urealyticum, Clostridium perfringens. Concerning these activators the antibiotic is moderately active in vitro, positive takes can be noted at concentration of an antibiotic in the inflammation center above, than MPK.

Steady microorganisms (MPK> of 4 mg/l): at least, 50% of strains are steady - Staphylococcus spp. (Methicillinum - resistant strains), Enterobacter spp., Pseudomonas spp., Acinetobacter spp., Nocardia asteroides, Fusobacterium spp., Haemophilus spp., Mycoplasma hominis, Corynebacterium jekeium.
Note: activity of Spheromycinum concerning Toxoplasma gondii is proved to in vitro and in vivo; due to the lack of clinical indications some kinds of bacteria in a range are not specified.

Spheromycinum gets and collects in phagocytes (polynuclear neutrophils, monocytes, peritoneal and alveolar macrophages). At the person of concentration of drug in phagocytes are rather high. These properties explain activity of Spheromycinum in relation to intracellular bacteria.
Pharmacokinetics: Absorption: Absorption of Spheromycinum happens quickly, but is incomplete also with big variability (from 10% to 60%). At joint reception with food bioavailability decreases by 50% and time of achievement of the maximum concentration in plasma increases.
Distribution: After administration of drug inside in a dose of 6 million ME the maximum concentration of Spheromycinum in blood serum (Cmax) makes about 3,3 mkg/ml. Later in/in introductions of 1,5 million ME of Spheromycinum by hourly infusion of Cmax makes 2,3 mkg/ml. At introduction of 1,5 million ME each 8 h Css it is reached by the end of the second day (Cmax about 3 mkg/ml and Cmin about 0,5 mkg/ml).
Linkng with proteins of plasma low (about 10%). The maximum concentration of Spheromycinum in blood serum (Tmax) at receipt in 1 g (3 million ME) is reached in 3 hours (3-4 hours) and receipt of 2 g (6 million ME) - in 4 hours (2-5 hours). Spheromycinum does not get into cerebrospinal fluid; it is allocated with breast milk, but passes through a placental barrier (concentration in blood of a fruit makes about 50% of concentration in blood serum of mother). Concentration in a placenta is 5 times higher, than the corresponding concentration in blood serum.              Vd about 383 l. Drug well gets into saliva and fabrics (concentration in lungs makes 20-60 mkg/g, in almonds - 20-80 mkg/g, in the infected bosoms - 75-110 mkg/g, in bones - 5-100 mkg/g). 10 days later after the end of treatment concentration of Spheromycinum in a spleen, a liver, kidneys makes 5-7 mkg/g.
Metabolism: Spheromycinum is metabolized in a liver with formation of active metabolites with unspecified chemical structure.
Removal: It is removed mainly with bile (concentration 15-40 times higher, than in serum). Renal excretion of active Spheromycinum makes about 10% of the entered dose. Small amounts of Spheromycinum are found in excrements. The elimination half-life after reception of 3 million ME of Spheromycinum inside makes about 8 h of blood (T1/2). Later in/in infusion of T1/2 makes about 5 h.
Pharmacokinetics in special clinical cases: T1/2 is extended at elderly people. Correction of the mode of dosing with an impaired renal function is not required from patients. Pregnant women: features of pharmacokinetics of Spheromycinum with pregnant women and its transfer to the child through a placenta remain up to the end not found out.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug:
— quinsies caused by a beta and hemolitic streptococcus of group A as an alternative to treatment beta лактамными antibiotics, especially, if they cannot be applied;
— acute sinusitis (irrespective of a microbiological profile of the activator, macroleads are applied when treatment beta лактамными is not shown by antibiotics);
— superinfection at an acute bronchitis;
— exacerbation of chronic bronchitis;
— not hospital (extra hospital) pneumonia at persons without risk factors, without heavy clinical symptoms, with lack of clinical factors which testify to a pneumococcal etiology of a disease.

At suspicion of atypical pneumonia macroleads are shown regardless of disease severity and the anamnesis.
— skin infections with a high-quality current: impetigo, an impetignization at various dermatosis, an ecthyma, infected dermogipodermit (in particular, an erysipelatous inflammation or эризипелоид), an erythrasma;
— infections of an oral cavity;
— not gonococcal genital infections;
— chemoprophylaxis of a recurrence of rheumatism in cases when beta лактамные antibiotics are contraindicated;
— a toxoplasmosis at pregnant women;
— prevention of a spotted fever at persons to whom rifampicin use is contraindicated.

• for an eradikation of a microorganism (Neisseria meningitidis) in a nasopharynx;
• after treatment and before return to public life;
• at the persons which had contact with a sick spotted fever at which oropharyngeal secretion (expectoration) in 10 days prior to its hospitalization was observed.

Spheromycinum is not intended for treatment of a spotted fever.

Route of administration and doses:

The adult appoint in from 6 to 9 million ME a day in 2 or 3 receptions (2-3 tablets on 3 million ME or 4-6 таб. on 1,5 million ME). The maximum daily dose makes 9 million ME. Correction of a dose is not required from elderly people.

To children appoint in 150 - 300 thousand ME to 1 kg of weight a day in 2-3 receptions. The maximum daily dose for children makes 300 thousand ME on 1 kg of weight a day. The course of treatment of quinsy makes 10 days.

At newborns use of Spheromycinum is not recommended because of the insufficient number of data on its therapeutic effectiveness at them, including at an inborn toxoplasmosis.

For prevention of a spotted fever drug is appointed within 5 days the adult on 3 million ME in 12 hours, to children on 75 thousand ME to 1 kg of body weight in 12 hours.

To pregnant women with a toxoplasmosis appoint a day 9 million ME of drug in 3 receptions till the birth of the child or confirmation of the diagnosis of a toxoplasmosis at a fruit. Then purpose of a combination of Pyrimethaminum and Sulfadiazinum follows.

With renal failures in connection with small renal excretion of Spheromycinum of change of a dose it is not required to patients.

Pill is taken inside entirely, washing down with enough water.

Features of use:

Pill should not be taken to those children up to 6 years which can choke at reception of a tablet form of medicine.

With care patients should appoint medicine with abnormal liver functions and kidneys. In the presence of chronic diseases of a liver it is necessary to carry out regular control of hepatic indicators of blood serum. As medicine is removed with urine in small amounts, patients should appoint correction of a dose only with a serious renal failure.

It was reported about very exceptional cases of development of hemolitic anemia in patients with insufficiency of a glyukozo-6-phosphate-dehydrogenase. For this reason for such patients reception of medicine is not recommended.

If the patient has any associated disease, then he has to report about it to the doctor and consult with it.

Influence on ability of control of vehicles and other difficult mechanisms. There are no data on an adverse effect of Spheromycinum on the speed of psychomotor reaction at persons of various professions including requiring special attention and coordination of movements (drivers, drivers, operators, etc.).

Side effects:

Undesirable effects are given according to the following gradation of frequency of their emergence: very frequent (≥10%), frequent (≥1% and <10%), infrequent (≥0.1% and <1%), rare (≥0.01% and <0.1%), very rare (<0.01%, including isolated cases), frequency is unknown (according to the available data it is not possible to establish emergence frequency).

From the alimentary system: abdominal pain, nausea, vomiting, diarrhea; very seldom - pseudomembranous colitis, changes of functional trials of a liver and development of cholestatic hepatitis; in isolated cases - an ulcer esophagitis and acute colitis. Also the possibility of development of acute injury of a mucous membrane of intestines in patients about AIDS at use of Spheromycinum in high doses concerning a cryptosporidiosis is noted (only 2 cases

From TsNS and peripheral nervous system: rare and tranzitorny paresthesias.

From system of a hemopoiesis: very seldom – hemolitic anemia, acute hemolysis and thrombocytopenia.

From cardiovascular system: lengthening of an interval of QT on an ECG is possible.

Allergic reactions: skin rash, small tortoiseshell, skin itch; very seldom - a Quincke's disease of Quincke, an acute anaphylaxis.

Others: in some cases - a vasculitis, including Shenleyn-Genokh's purpura.

At emergence of side effects it is necessary to cancel administration of drug. In cases of aggravation of the side effects specified in the instruction or emergence of the side effects which are not mentioned in the instruction, the patient has to be warned about need to inform on it the attending physician.

Interaction with other medicines:

Care at combined use is required: At simultaneous use with the medicines containing a combination of a levodopa and a karbidopa decrease in level of a levodopa in plasma was observed (clinical control and on it correction of a dose of a levodopa is necessary).

Influence on a hemostasis (MNO - the international normalized relation): it was reported about numerous cases of a superactivity of peroral anticoagulants at the patients receiving an antibioticotherapia. The expressed infection (inflammation), age and the general condition of patients are risk factors. It complicates definition of impact of an infection (its treatment) on development of an imbalance of a hemostasis. Some classes of antibiotics and antibacterial agents exert impact on a hemostasis more than the others. Ftorkhinolona, macroleads, tsiklina, co-trimoxazole, and some cephalosporins concern to them.

Contraindications:

Allergy to Spheromycinum

Feeding period breast.

Use to the patients belonging to risk group of increase in duration of a QT interval:
- The known hereditary syndrome of the extended QT-of an interval or existence in the family anamnesis of the hereditary syndrome extended with QT-of an interval (if the electrocardiogram did not yield other results);
- Or known acquired, caused by reception of medicines, lengthening of QT-of an interval.

In combination with the medicines causing ventricular tachycardia like pirouette:
- Antiarrhytmic means of the class Ia (quinidine, hydroquinidine, Disopyramidum);
- Antiarrhytmic means of a class III (Amiodaronum, соталол, дофетилид, ибутилид);
- Sultoprid (neuroleptic of group of benzamides);
- Other medicines: bepridit, цизаприд, difemanit, мизоластин, Vincaminum, erythromycin (see the section "Interaction with Other Medicines");
- Certain neuroleptics of group of fenotiazin (thioridazine, Chlorpromazinum, levomepromazinum, циамемазин), neuroleptics of group of benzamides (амисульприд, Sulpiridum, тиаприд), neuroleptics of group of phenyl propyl ketones (haloperidol, Droperidolum) and other neuroleptics (Pimozidum);
- Galofantrin, pentamidine, moxifloxacin.

Pregnancy and lactation: SPIRAMITSIN-FT can appoint at pregnancy according to indications. Numerous use of drugs of Spheromycinum during pregnancy did not reveal the data indicating manifestations of phototoxicity or developing of malformations at a fruit so far. Teratogenic action of Spheromycinum is not revealed. The risk of transfer of a toxoplasmosis to a fruit during pregnancy decreases from 25% to 8% when using drug in the I trimester, from 54% to 19% - in the II trimester and from 65% to 44% - in the III trimester.

At purpose of drug SPIRAMITSIN-FT in the period of a lactation it is necessary to stop breastfeeding. Spheromycinum is excreted in breast milk. It was reported about emergence of gastrointestinal frustration at newborns when breastfeeding by mothers receiving Spheromycinum drugs.

Overdose:

Symptoms: the toxic dose and cases of overdose by Spheromycinum are unknown. Nausea, vomiting, diarrhea can be possible symptoms after use of high doses. In case of overdose it is necessary to define QT interval, in particular with other risk factors (a hypopotassemia, inborn lengthening of an interval of QT, reception of other medicines extending QT and/or causing a torsade de pointes of ventricles).

Treatment: if necessary carry out symptomatic therapy. The specific antidote does not exist.

Storage conditions:

To store at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 2 years.

Issue conditions:

According to the recipe

Packaging:

Coated tablets of 1,5 million ME in a blister strip packaging No. 8×2 and in banks No. 16 and 3,0 of one million ME in a blister strip packaging No. 5×2 and in banks No. 10. Together with a leaf insert two blister strip packagings or one bank are placed in a pack from a cardboard.