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

Dosage for the prepared suspension	100 mg / 5 ml	200 mg / 5 ml
Azithromycin dihydrate in terms of azithromycin	419.3 mg 400 mg	838.6 mg 800 mg
Excipients:
Sucrose (sugar)	14948.7 mg	14529.4 mg
Sodium carbonate (sodium carbonate anhydrous)	238.5 mg	238.5 mg
Xanthan gum (xanthan gum)	21.7 mg	21.7 mg
Giprolosa (Klucel EF)	25.4 mg	25.4 mg
Aromatizer "Banana"	119.2 mg	119.2 mg
Aromatizer "Cherry"	71.5 mg	71.5 mg
Aromatizer "Vanilla"	55.7 mg	55.7 mg

Description:

Crystalline or granular powder white or white with a yellowish or kremovatym tinge of color or light yellow with a faint fruity smell.

Description of the prepared suspension. Homogeneous suspension from white or light gray with a yellowish or creamy hue to a light yellow color with a characteristic fruity odor.

Pharmacotherapeutic group:Antibiotic-azalide

ATX: & nbsp

J.01.F.A.10 Azithromycin

Pharmacodynamics:

Azithromycin is a bacteriostatic broad-spectrum antibiotic from the group of macrolides-azalides. It has a wide spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of protein synthesis of a microbial cell. Linking to the 508 subunit of the ribosome, inhibits the peptidranslokase at the translation stage and suppresses protein synthesis, slowing the growth and multiplication of bacteria. In high concentrations has a bactericidal effect.

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

Sensitive microorganisms: aerobic gram-positive microorganisms - Staphylococcus aureus (methicillin-sensitive strains), Streptococcus pneumoniae (penicillin-sensitive strains), Streptococcus pyogenes, Streptococcus spp. (Group C, F and G); aerobic gram-negative microorganisms - Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae; anaerobic microorganisms - Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyriomonas spp.', other microorganisms - Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.

Microorganisms with acquired resistance to azithromycin: aerobic gram-positive microorganisms - Streptococcus pneumoniae (penicillin-resistant strains and strains with an average sensitivity to penicillin).

Microorganisms with natural resistance to azithromycin: aerobic gram-positive microorganisms - Enterococcus faecalis, Staphylococcus aureus (methicillin-resistant strains), Staphylococcus epidermidis (methicillin-resistant strains); anaerobic microorganisms - Bacteroides fragilis.

Cases of cross-resistance in Streptococcus pneumoniae, Streptococcus pyogenes (beta-hemolytic group streptococcus A), Enterococcus faecalis and Staphylococcus aureus (including methicillin-resistant strains) to erythromycin, other macrolides, lincosamides and azithromycin.

The sensitivity scale of microorganisms to azithromycin (Minimum inhibitory concentration (MIC), mg / L)

Microorganisms	MIC, mg / l
	Sensitive		Sustainable
Staphylococcus spp.	no more 1	more than 2
Streptococcus A, AT, C, G	not more than 0,25	more than 0.5
Streptococcus pneumoniae	not more than 0,25	more than 0.5
Haemophilus influenzae	not more than 0,12	more than 4
Moraxella catarrhal is	no more than 0.5	more than 0.5
Neisseria gonorrhoeae	not more than 0,25	more than 0.5

Pharmacokinetics:

After oral administration, the bioavailability is 37%, the maximum concentration in the blood plasma (Cmah) is created after 2-3 hours, the volume of distribution is 31.1 l / kg. Binding to blood proteins is inversely proportional to the concentration in the blood and is 7-50%.Penetrates through cell membranes (effective for infections caused by intracellular pathogens). It is transported by phagocytes, polymorphonuclear leukocytes and macrophages to the site of infection, where it is released in the presence of bacteria. Easily passes through the histohematological barriers and enters the tissues. The concentration in tissues and cells is 50 times higher than in plasma, and in the focus of infection - 24-34% more than in healthy tissues.

Has a long half-life of 2-4 days. The half-life of the tissues is much larger. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is output, basically, in the unchanged form - 50% of the intestine, 6% of the kidneys. In the liver, demethylated, losing activity.

In patients with severe renal failure (creatinine clearance less than 10 ml / min), the half-life of azithromycin increases by 33%.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to azithromycin, including:

- upper respiratory tract and ENT organs, including pharyngitis / tonsillitis, sinusitis, otitis media;

- lower respiratory tract, including acute bronchitis, exacerbation of chronic bronchitis and community-acquired pneumonia;

- urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis);

- infections of the skin and soft tissues (acne vulgaris (medium acne), erysipelas, impetigo, secondarily infected dermatoses);

- Lyme disease - the initial stage (migratory erythema - erythema migrans).

Contraindications:

Hypersensitivity to azithromycin, other macrolides or other components of the drug; severe hepatic dysfunction (no data on efficacy and safety); impaired renal function (CC less than 40 ml / min (no data on efficacy and safety)); deficiency of sugar / isomaltase, intolerance to fructose, glucose-galactose malabsorption; children's age up to 6 months; breastfeeding; simultaneous reception of ergotamine and dihydroergotamine.

Carefully:

With a mild violation of liver function; renal dysfunction (CC more than 40 ml / min); predisposition to arrhythmia and lengthening of the interval QT, joint application with antiarrhythmic drugs of classes IA, III, cisapride, in the presence of hypokalemia or hypomagnesemia, clinically significant bradycardia, arrhythmia or severe heart failure; simultaneous application of terfenadine, warfarin, digoxin, pregnancy, myasthenia gravis, diabetes mellitus.

Pregnancy and lactation:

In studies on animals, no damaging effects on the fetus have been identified, data on the efficacy and safety of the use of azithromycin in pregnant women are limited. Azithromycin is used during pregnancy only if the intended benefit to the mother exceeds the possible risk to the fetus. For the duration of treatment with azithromycin, breastfeeding should be discontinued.

Dosing and Administration:

Take inside, 1 hour before or 2 hours after meals 1 time per day.

For the preparation of a suspension in a bottle of powder add water (distilled or boiled and cooled) in an amount of 9.5 ml. Water should be measured with a pipette for dosing, attached to the vial. Vial contents thoroughly shake until a homogeneous suspension is obtained. The actual volume of the prepared suspension is 20 ml.

The prepared suspension should be stored in the original packaging for no more than 5 days at a temperature of no higher than 25 ° C. Do not freeze.

Before each use, the suspension must be shaken. To dispense the finished suspension, use a pipette for dosing or a measuring spoon. Immediately after taking the suspension, you need to drink a few sips of water to wash and swallow the remaining drug in the oral cavity. After use, a measuring spoon or pipette, which is previously disassembled, washed with running water, dried and stored together with the drug.

Children over 6 months old

In infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues (with the exception of migrating erythema): at the rate of 10 mg / kg body weight 1 time per day for 3 days (course dose 30 mg / kg).

Children with a body weight of up to 10 kg are advised to take the drug in powder form to prepare a suspension for oral administration at a concentration of 100 mg / 5 ml.

Patient's body weight	The required volume of suspension in ml (dose of azithromycin in mg) at one time
Patient's body weight	Suspension 100 mg / 5 ml	Suspension 200 mg / 5 ml
5 kg	2.5 ml (50 mg)
6 kg	3 ml (60 mg)	1.5 ml (60 mg)
7 kg	3.5 ml (70 mg)	1.8 ml (70 mg)
8 kg	4 ml (80 mg)	2 ml (80 mg)
9 kg	4.5 ml (90 mg)	2.3 ml (90 mg)
10-14 kg	5 ml (100 mg)	2.5 ml (100 mg)
15-24 kg		5 ml (200 mg)
25-34 kg		7.5 ml (300 mg)
35-44 kg		10 ml (400 mg)
More than 45 kg (prescribe doses for adults)		12.5 ml (500 mg)

When treating the initial stage of Lyme disease (migrating erythema - erythema migrans): once a day: the first day - at a dose of 20 mg / kg body weight, then from the 2nd to the 5th day at a dose of 10 mg / kg body weight. The course dose is 60 mg / kg body weight.

1st day
Patient's body weight	The required volume of suspension in ml (dose of azithromycin in mg) at one time
	Suspension 100 mg / 5 ml	Suspension 200 mg / 5 ml
5 kg	5 ml (100 mg)
6 kg	6 ml (120 mg)	3 ml (120 mg)
7 kg	7 ml (140 mg)	3.5 ml (140 mg)
8 kg	8 ml (160 mg)	4 ml (160 mg)
9 kg	9 ml (180 mg)	4.5 ml (180 mg)
10-14 kg	10 ml (200 mg)	5 ml (200 mg)
15-24 kg		10 ml (400 mg)
25-34 kg		15 ml (600 mg)
35-44 kg		20 ml (800 mg)
More than 45 kg (prescribe doses for adults)		25 ml (1.0 g)
From the 2nd to the 5th day
	Suspension 100 mg / 5 ml	Suspension 200 mg / 5 ml
5 kg	2.5 ml (50 mg)
6 kg	3 ml (60 mg)	1.5 ml (60 mg)
7 kg	3.5 ml (70 mg)	1.8 ml (70 mg)
8 kg	4 ml (80 mg)	2 ml (80 mg)
9 kg	4.5 ml (90 mg)	2.3 ml (90 mg)
10-14 kg	5 ml (100 mg)	2.5 ml (100 mg)
15-24 kg		5 ml (200 mg)
25-34 kg		7.5 ml (300 mg)
35-44 kg		10 ml (400 mg)
More than 45 kg (prescribe doses for adults)		12.5 ml (500 mg)

Adults.

With infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues (with the exception of migrating erythema): 500 mg once a day for 3 days (the course dose is 1.5 g).

The required volume of suspension in ml (dose of azithromycin in mg) at one time

Suspension 200 mg / 5 ml

12.5 ml (500 mg)

When treating the initial stage of Lyme disease (migrating erythema - erythema migrans):

1.0 g on the first day, then 500 mg / day daily from 2 to 5 days (course dose 3.0 g).

	The required volume of suspension in ml (dose of azithromycin in mg) per one reception
	Suspension 200 mg / 5 ml
1st day	25 ml (1.0 g)
From the 2nd to the 5th day	12.5 ml (500 mg)

In cases of urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis):

In uncomplicated urethritis / cervicitis - once 1.0 g.

The required volume of suspension in ml (dose of azithromycin in mg) for a single dose

Suspension 200 mg / 5 ml

25 ml (1.0 g)

In the treatment of acne (acne vulgaris) of moderate severity.

On the 1st, 2nd and 3rd day of treatment take 500 mg once a day, then take a break from the fourth to the seventh day, from the eighth day of treatment take 500 mg once a week for 9 weeks (course dose 6.0 g) .

The required volume of suspension in ml (dose of azithromycin in mg) at one time

Suspension 200 mg / 5 ml

12.5 ml (500 mg)

Patients with impaired renal function. If the kidney function is impaired (CC more than 40 ml / min) dose adjustment is not required.

Patients with impaired liver function. With a moderate violation of liver function, dose adjustment is not required.

Side effects:

Classification of the incidence of adverse events (WHO): very often (with a frequency of more than 1/10), often (with a frequency of at least 1/100, but less than 1/10),infrequently (with a frequency of at least 1/1000 but less than 1/100), rarely (with a frequency of at least 1/10000, but less than 1/1000), very rarely (with a frequency of less than 1/10 000), including individual messages.

From the system of the circulatory and lymphatic systems: often - lymphocytopenia, eosinophilia; infrequently - leukopenia, neutropenia; very rarely - thrombocytopenia, hemolytic anemia.

From the nervous system: often - dizziness, headache, paresthesia, anorexia; infrequently - nervousness, hyposthenia, insomnia, drowsiness; rarely - agitation; very rarely - fainting, convulsions, psychomotor hyperactivity, myasthenia gravis exacerbation gravis, anxiety, aggression.

From the sense organs: often - reduced hearing acuity, reduced visual acuity, impaired perception of gustatory sensations; infrequently - a noise in the ears, deafness; rarely - vertigo; very rare - anosmia, loss of taste, parasymia.

From the cardiovascular system: infrequent - a feeling of heartbeat; very rarely - arrhythmia, ventricular tachycardia, increased interval QT, arrhythmia such as "pirouette", lowering blood pressure.

From the digestive system: very often - nausea, diarrhea,abdominal pain, flatulence; often - vomiting, indigestion; infrequently - gastritis, constipation; very rarely - a discoloration of the tongue, pseudomembranous colitis, pancreatitis.

From the liver and biliary tract: infrequently - hepatitis, increased activity of "liver" transaminases, hyperbilirubinemia; rarely - a violation of liver function; very rarely - cholestatic jaundice, hepatic insufficiency, fulminant hepatitis, liver necrosis.

Allergic reactions: often - itchy skin, rash; infrequently - angioedema, hypersensitivity reactions, Stevens-Johnson syndrome, photosensitivity, urticaria; very rarely - anaphylactic reactions, toxic epidermal necrolysis, erythema multiforme.

From the musculoskeletal system: often - arthralgia.

From the urinary system: infrequently - increase in the concentration of urea and creatinine in the blood plasma; very rarely - interstitial nephritis, acute renal failure.

Other: often - weakness; infrequently - pain in the chest, peripheral edema, soreness, asthenia, vaginitis, candidiasis of various localizations.

Overdose:

When receiving high doses may occur amplification dose-related side effects: temporary hearing loss, severe nausea, vomiting, diarrhea. Treatment: the appointment of activated carbon, symptomatic therapy, control of vital functions.

Interaction:

Antacids (aluminum and magnesium-containing) does not affect the bioavailability of azithromycin, but reduce its Cmah 30%, and the drug should be taken at least one hour before or two hours after taking these drugs. Azithromycin It does not affect the concentration of carbamazepine, cimetidine, didanosine, efavirenz, fluconazole, indinavir, midazolam, theophylline, triazolam, trimethoprim / sulfamethoxazole, cetirizine, sildenafil, atorvastatin, rifabutin and blood, while the application of methylprednisolone.

If it is necessary to simultaneously use with cyclosporine, it is recommended to monitor the concentration of cyclosporine in the blood.

When simultaneous administration of digoxin and azithromycin is necessary to monitor the concentration of digoxin in the blood, as many macrolides digoxin enhance absorption in the gut, thereby increasing its CmOh.

With simultaneous use with derivatives of ergotamine and dihydroergotamine, toxic effects (vasospasm, dysesthesia) of the latter are possible.

If it is necessary to take an indirect action with anticoagulants at the same time (warfarin and other anticoagulants of the coumarin type) it is recommended to monitor prothrombin time.

It was established that simultaneous reception of terfenadine or cisapride and antibiotics of the macrolide class causes arrhythmia and lengthening of the interval QT. Proceeding from this, one can not exclude the aforementioned complication in the joint use of azithromycin and terfinadine.

With the joint administration of azithromycin and zidovudine, azithromycin does not affect the pharmacokinetic parameters of zidovudine in blood plasma or on the excretion of its and its metabolite glucuronide by the kidneys. Nevertheless, the concentration of the active metabolite - phosphorylated zidovudine in monocytes - increases.

At simultaneous application with nelfinavir it is possible to increase the incidence of adverse reactions of azithromycin (decrease in hearing, increase of activity of "liver" transaminases).

The possibility of inhibiting the isoenzyme should be considered CYP3A4 azithromycin with simultaneous application with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs, the metabolism of which occurs with the participation of this enzyme.

Special instructions:

When appointing patients with diabetes, as well as with a low-calorie diet, it should be taken into account that sucrose enters the suspension (3.7 g / 5 ml or 0.3 XE / 5 ml).

If you miss one dose of the drug - the missed dose should be taken as soon as possible, and the next - at intervals of 24 hours. It is necessary to follow the recommended in the instructions scheme and the duration of the drug.

Azithromycin is contraindicated in patients with severe impairment of liver function. Patients with moderate impaired hepatic function azithromycin should be administered with caution because of the possibility of developing fulminant hepatitis and severe hepatic insufficiency. In the presence of symptoms of impaired liver function (rapidly increasing asthenia, jaundice, darkening of the color of urine, a tendency to bleeding, hepatic encephalopathy) therapy with azithromycin should be discontinued and a study of the functional state of the liver.

With moderate renal failure (CC greater than 40 ml / min), azithromycin should be administered under the control of kidney function.

There is no data on the possible interaction between azithromycin and derivatives of ergotamine and dihydroergotamine, but because of the development of ergotism with the simultaneous administration of macrolides with derivatives of ergotamine and dihydroergotamine, this combination is contraindicated.

With prolonged use of azithromycin, the development of pseudomembranous colitis caused by Clostridium difficile, as in the form of mild diarrhea, and severe colitis. With the development of diarrhea against the background of taking azithromycin, and also 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded.

With the syndrome of delayed repolarization of the ventricles - the syndrome of lengthening the interval QT - against the background of taking macrolides, including azithromycin, the risk of arrhythmia increases. Caution when prescribing azithromycin should be observed in patients with lengthening interval QT, receiving antiarrhythmic drugs classes IA, III, cisapride, in the presence of hypokalemia or hypomagnesemia, clinically significant bradycardia,arrhythmia or severe heart failure.

The use of azithromycin may provoke the development of a myasthenic syndrome or cause an exacerbation of myasthenia gravis gravis.

Since 2010 azithromycin recommended by the International Union Against Sexually Transmitted Infections, together with the WHO European Office, as the first choice drug for the treatment of chlamydial infection during pregnancy.

As with the use of other antibacterial drugs, patients with azithromycin should regularly be examined for susceptible microorganisms and signs of development of superinfections, including fungal ones.

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

In the event of adverse reactions from the central nervous system, patients are advised to refrain from managing motor vehicles and practicing other potentially hazardous activities requiring increased concentration of attention, speed of psychomotor and motor reactions.

Form release / dosage:

Powder for the preparation of the suspension for ingestion 100 mg / 5 ml or 200 mg / 5 ml.

Packaging:

For 15.9 g in bottles with a capacity of 50 ml of dark (amber) glass. One bottle together with the instructions for use, a measuring spoon and a pipette for dosing are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

The prepared suspension should be stored at a temperature not exceeding 25 ° C. Do not freeze. Keep out of the reach of children.

Shelf life:

2 years. The prepared suspension is no more than 5 days.

At the end of the expiration date the drug should not be used.

Terms of leave from pharmacies:On prescription

Registration number:LP-002027

Date of registration:21.03.2013

The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-FORESTRY, OJSC Russia

Information update date: & nbsp26.10.2015

Illustrated instructions

Instructions

Azitrox® (Azitrox®)