medicalmeds.eu Medicines Antibacterial agents for system use. Beta лактамные antibiotics, penicillin. Оспамокс

Оспамокс

Producer: Sandoz Gmbh (Sandoz Gmbh) Germany

Code of automatic telephone exchange: J01CA04

Release form: Firm dosage forms. Tablets.

Indications to use: Upper respiratory tract infections. Lower respiratory tract infections. Infections of urinogenital system. Digestive tract infections.

General characteristics. Structure:

Active ingredient: amoxicillin.

Pharmacological properties:

Pharmacodynamics. Active ingredient of drug of Ospamoks — amoxicillin — a semi-synthetic aminopenicillinic antibiotic of a broad spectrum of activity for oral administration. Works bakteritsidno, breaking synthesis of components of a bacterial cell. It is active in the relation of both gram-positive, and gram-negative microorganisms. Such species of microorganisms are sensitive to drug:

gram-positive aerobes: Corinebacterium diphteriae, Enterococcus faecalis, Listeria monocytogenes, Streptococcus agalactiae, Streptococcus bovis, Streptococcus pyogenes;

gram-negative aerobes: Helicobacter pylori;

anaerobe bacterias: Peptostreptococci;

others: Borrelia.

Changeably sensitive (the acquired resistance can become a problem): Corinebacterium spp., Enterococcus faecium, Streptococcus pneumoniae, Streptococcus viridans, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Proteus mirabilis, Prevotella, Fusobacterium spp.

Rezistentna such types, as: Staphylococcus aureus, Acinetobacter, Citrobacter, Enterobacter, Klebsiella, Legionella, Morganella morganii, Proteus vulgaris, Providencia, Pseudomonas, Serratia, Bacteroides fragilis, Chlamidia, Mycoplasma, Rickettsia.

Pharmacokinetics. Absorption. After oral administration amoxicillin is soaked up in a small intestine quickly and almost completely (85–90%). Meal practically does not influence drug absorption. After reception of a single dose of 500 mg concentration of amoxicillin in a blood plasma made 6–11 mg/l. Cmax of active agent in a blood plasma is reached in 1–2 h.

Distribution. About 20% of amoxicillin contact proteins of a blood plasma. Amoxicillin gets into mucous membranes, a bone tissue and intraocular liquid, a phlegm in therapeutic effective concentration. Concentration of amoxicillin in bile exceeds its concentration in blood by 2–4 times. Amoxicillin badly diffuses in SMZh; however at an inflammation of a meninx (for example at meningitis) concentration in SMZh makes about 20% that in a blood plasma.

Metabolism. Amoxicillin is partially metabolized, the majority of its metabolites are inactive.

Removal. Amoxicillin is emitted preferential with kidneys. About 60-80% of the accepted dose eliminirut in 6 h in not changed look. Т½ amoxicillin makes 1–1,5 h. At renal failure Т½ of amoxicillin increases and reaches 8,5 h at an anury. Т½ amoxicillin does not change at an abnormal liver function.

Indications to use:

The infections caused by microorganisms, sensitive to amoxicillin:

- respiratory organs;

- bodies of urinogenital system;

- bodies of a digestive tract;

- skin and soft tissues.

Route of administration and doses:

Doses of amoxicillin establish individually depending on age, body weight and a condition of kidneys of the patient, and also from sensitivity of microorganisms and localization of infectious process.

Meal does not influence amoxicillin absorption. It is necessary to swallow of a tablet and the capsule whole (the tablet can be divided into parts) not to chew, wash down with 1 glass of water. The tablet of Ospamoks of DT can be dissolved in water and to drink the received suspension. Suspension of Ospamoks should be accepted not divorced, washing down with water.

Dosing. In case of infectious and inflammatory diseases easy and moderately severe to adults and children aged> 500–750 mg 2 times a day or 500 mg 3 times a day are recommended to accept 12 years (with body weight> 40 kg). Usually daily dose for children makes 30 mg/kg, divided into 2–3 receptions.

At treatment of chronic diseases, a recurrence, heavy infections the dose of drug can be raised and it is recommended to be distributed on 3 receptions: the adult appoint 750–1000 mg 3 times a day; to children aged> 12 years — to 60 mg/kg/days distributed on 3 receptions.

For children aged up to 12 years (with the body weight <40 kg) the daily dose makes 30 mg/kg, divided into 2–3 receptions.

Usually to children at the age of 1–3 years appoint 250 mg 2 times a day or 125 mg 3 times a day. To children aged from 3 up to 12 years appoint 250 mg 3 times a day. Exact daily doses are calculated according to the body weight of the child, but not his age!

At treatment of chronic diseases, a recurrence, infections of a heavy current it is recommended to raise a dose to 60 mg/kg/days in 3 receptions (but no more than 3 g/days).

Use duration. In case of infections easy and moderately severe drug is accepted for 5–7 days. However in case of the infections caused by a streptococcus, duration of treatment has to make not less than 10 days.

At treatment of chronic diseases, local infectious defeats, heavy infections duration of treatment needs to be determined proceeding from a clinical picture of a disease.

Administration of drug should be continued for 48 h after disappearance of symptoms of a disease.

The patient with renal failures (clearance of creatinine <30 ml/min.) the dose of drug is reduced or increase an interval between receptions:

Adults and children with body weight> 40 kg

Clearance of creatinine, Dose, mg the Interval between

ml/min. use, h

> 30 Dose adjustments are not required

10-30 500 12

<10 500 24

In case of a hemodialysis it is necessary to apply 500 mg of amoxicillin at the end of the procedure.

Children with body weight <40 kg

Clearance of creatinine, Dose, mg the Interval between

ml/min. use, h

> 30 Dose adjustments are not required

10-30 15 12

<10 15 24

Patients with an abnormal liver function. Patients with an abnormal liver function do not need dose adjustment.

Suspension preparation. To stir up a bottle that powder separated from walls and a bottom. To add drinking water in 2 portions (at first to ⅔, and then to a tag on a bottle), stirring up every time. Before each use it is good to shake up. For measuring off of suspension the measured spoon of 5 ml with tags of 1,25 and 2,5 ml is applied.

Features of use:

Before therapy amoxicillin needs to be made the test for probability of emergence of reaction of hypersensitivity for penicillin and cephalosporins. There can be a cross hypersensitivity and cross resistance (10–15%) between penicillin and cephalosporins.

Heavy and sometimes lethal cases of hypersensitivity (anaphylactic reaction) noted at the patients receiving penicillinic therapy. Such reactions arise more often at patients with the known heavy allergic reactions in the anamnesis. Treatment by drug needs to be stopped and replaced with another. There can be a need for elimination of symptoms of anaphylactic reaction, for example, immediate introduction of Epinephrinum, steroids (in/in) and emergency treatment of respiratory insufficiency.

Patients with heavy disorders of a GIT which are followed by diarrhea and vomiting should not apply Ospamoks of DT because of risk of decrease in absorption.

At patients with a renal failure removal of amoxicillin is slowed down and, depending on extent of disturbance, it is necessary to stop use of amoxicillin or to lower the general daily dose of drug.

Prolonged use of drug can lead to the excess growth of resistant microorganisms or barmy mushrooms. Emergence of superinfection is possible, it demands careful observation of such patients.

At use of drug in high doses it is necessary to use enough liquid for prevention of a crystalluria which can be caused by amoxicillin. Existence of high concentration of amoxicillin in urine can cause loss of a deposit of drug in an uric catheter therefore it should be checked visually through certain intervals of time.

When developing the heavy diarrhea characteristic of pseudomembranous colitis (in most cases the caused Clostridium difficile), it is recommended to stop use of drug and to take the appropriate measures. Use antiperistaltic means is contraindicated.

Amoxicillin is not recommended to be applied to treatment of patients with viral infections, an acute lymphoid leukosis or infectious mononucleosis in connection with the increased risk of an erythematic enanthesis.

During therapy by high doses it is necessary to control blood indicators regularly.

Therapy by amoxicillin in high doses of patients with a renal failure or patients with epilepsy and meningitis in the anamnesis can lead to spasms in some cases.

Emergence of a generalized erythema with fever and pustules in an initiation of treatment can demonstrate development of an acute generalized eczematic pustulez, therefore, therapy by amoxicillin should be stopped.

With extra care patients should apply suspension with a fenilketonuriya as drug contains aspartame.

Оспамокс in the form of suspension contains benzoate and sodium citrate that patients who adhere to a diet with the limited content of sodium need to consider at purpose of drug.

Use during pregnancy and feeding by a breast. Amoxicillin gets through a placental barrier and its concentration in a blood plasma of a fruit makes about 25-30% of concentration in a blood plasma of mother. The insignificant number of data on use of amoxicillin during pregnancy confirm lack of undesirable influence on the fruit/newborn. Drug during pregnancy it is possible to appoint advantage/risk after careful assessment of a ratio.

Amoxicillin in insignificant quantity gets into breast milk therefore it is impossible to exclude risk of development of hypersensitivity in the child which is on breastfeeding. Ospamoks's use during this period is possible only in that case when the expected advantage for mother exceeds potential risk for the child. Feeding by a breast should be stopped if the newborn had gastrointestinal frustration (diarrhea, candidiasis or skin rash).

Children. Оспамокс, suspension, appoint to children since the birth. For children 12 years the recommended dosage forms are aged more senior capsules and tablets are.

Ability to influence speed of response at control of vehicles or work with other mechanisms. Before identification of individual reaction to drug (dizziness is possible) it is recommended to be careful at control of vehicles or work with difficult mechanisms.

Side effects:

Criteria for evaluation of frequency of development of side reactions: often (≥1/100, <1/10), sometimes (≥1/1000, <1/100), it is rare (≥1/10 000, <1/1000), is very rare (<1/10 000).

From a GIT: often — diarrhea, nausea, a meteorism, soft kcal, an itch in the field of an anus, loss of appetite, an enantem (especially on the site of a mouth), dryness in a mouth, taste disturbance; sometimes — vomiting; seldom — pseudomembranous and hemorrhagic colitis; very seldom — intestines candidiasis, coloring of teeth, coloring of language in black color. These side effects generally not heavy also pass during treatment or right after completion of therapy. Emergence of such side effects can be prevented if to apply amoxicillin during food.

From skin and hypodermic cellulose: often — skin rash; sometimes — urticaria, an itch; very seldom — a multiformny erythema, Stephens's syndrome — Johnson, a toxic epidermal necrolysis, violent or exfoliative dermatitis and acute generalized exanthematous пустулез, a Lyell's disease. Sudden emergence of a small tortoiseshell indicates allergic reaction to amoxicillin, in this case therapy by drug should be stopped immediately.

From kidneys and urinary system: seldom — intersticial nephrite, a crystalluria.

From system of blood and lymphatic system: seldom — an eosinophilia, hemolitic anemia, thrombocytopenia; very seldom — a leukopenia, a heavy neutropenia, an agranulocytosis, a pancytopenia, a miyelosupressiya, a granulocytopenia, and also lengthening of the period of bleeding and a prothrombin time. These phenomena are reversible on condition of the treatment termination.

From immune system: very seldom — heavy allergic reactions, including a Quincke's disease (Quincke's edema), an anaphylaxis, a serum disease, an allergic vasculitis, throat hypostasis, an acute anaphylaxis.

From gepatobiliarny system: very seldom — hepatitis, cholestatic jaundice, moderate and short-term increase in concentration of liver enzymes (ASAT, ALAT).

From TsNS: very seldom — a hyperkinesia, a hyperactivity, dizziness and spasms.

Infections and invasions: very seldom — long or repeated use of drug can lead to development of superinfections and colonization of resistant microorganisms or barmy mushrooms which cause oral or vaginal candidiasis.

Others: seldom — fever.

Interaction with other medicines:

Probenetsid, phenylbutazone, оксифенбутазон, acetylsalicylic acid (to a lesser extent) and Sulfinpyrazonum suppress tubular secretion of drugs of a penicillinic row that leads to increase Т½ and concentration of amoxicillin in a blood plasma.
The drugs possessing bacteriostatic action (antibiotics of a tetracycline row, macroleads, chloramphenicol) can neutralize bactericidal effect of amoxicillin. Parallel use of aminoglycosides is possible (synergy effect).
Unrecommended combinations
Allopyrinolum. Simultaneous use with amoxicillin promotes emergence of allergic skin reactions.
Digoxin. Digoxin absorption therefore correction of its dose is necessary increases.
Disulfiramum. Simultaneous use with amoxicillin is contraindicated.
Anticoagulants. Simultaneous use of amoxicillin and anticoagulants of a class of coumarins can extend a bleeding time. Dose adjustment of anticoagulants is necessary. Patients who received amoxicillin had messages on increase in activity of peroral anticoagulants.
Methotrexate. Use of amoxicillin with a methotrexate leads to increase in toxic action of the last. Amoxicillin reduces renal clearance of a methotrexate therefore it is necessary to check the level of its concentration in a blood plasma.
Amoxicillin should be applied with care together with oral hormonal contraceptives — the plasma level of estrogen and progesterone can temporarily decrease, and it can reduce efficiency of hormonal contraceptives. Therefore it is recommended to use additional non-hormonal contraceptives.
Other types of interactions. The artificial diuresis leads to decrease in concentration of amoxicillin in a blood plasma by increase in its elimination.
Emergence of diarrhea can lead to reduction of absorption of other medicines and it is adverse to influence their efficiency.
Influence on results of diagnostic laboratory testings: at a research on availability of glucose in urine it is recommended to use an enzymatic glyukozooksidazny method. When using chemical methods usually note false positive result.
Amoxicillin can reduce amount of estriol in urine at pregnant women.
At high concentration of amoxicillin glycemia level in a blood plasma can decrease. Amoxicillin can influence protein definition by a colorimetric method.

Contraindications:

Hypersensitivity to amoxicillin and other β-laktamny antibiotics, medicines of a penicillinic and tsefalosporinovy row, and also to any of drug substances. Infectious mononucleosis and leukemoid tests of lymphatic type.

Overdose:

Symptoms: dysfunction of a GIT — nausea, vomiting, diarrhea; disturbance of water and electrolytic balance. It was reported about crystalluria cases that sometimes led to a renal failure.

Treatment: there is no specific antidote. It is necessary to cause vomiting or to wash out a stomach then to accept absorbent carbon and osmotic purgatives. It is necessary to support water and electrolytic balance. Amoxicillin is not removed by means of a hemodialysis.

Storage conditions:

In original packaging. Оспамокс tablets, capsules, powder for suspension preparation — at a temperature up to 25 °C. Ready suspension should be applied for 14 days in densely closed bottle. Оспамокс DT — at a temperature not above 30 °C.