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

Excipients: citric acid anhydrous, sodium benzoate, aspartame, talc, anhydrous trisodium citrate, cyamopsis of four-bladed (guar) gum (guar galactomannic), silicon dioxide precipitated; Flavors (powdery) - lemon, peach-apricot, orange.

Description:

Powder: white or white with a yellowish tinge powder with a characteristic fruity odor.

Ready-to-use suspension: white or white with a yellowish tinge suspension with a characteristic fruity smell, bitter-sweet to taste.

Pharmacotherapeutic group:Antibiotic, penicillin semisynthetic.

ATX: & nbsp

J.01.C.A.04 Amoxicillin

Pharmacodynamics:

Amoxicillin is an aminobenzyl penicillin,It has a bactericidal effect by inhibiting the synthesis of the bacterial cell wall.

Thresholds MIC for various sensitive organisms vary. Enterobacteriaceae spp. it is considered to be sensitive when inhibited at a concentration of <8 μg / ml amoxicillin and resistant - at a concentration of> 32 m kg / ml.

In accordance with the recommendations CLSI and when used CLSI-the indicated methods M.catarrhalis (β-lactamase negative) and N. influenzae (β-lactamase negative) are regarded as sensitive at concentrations <1 μg / ml and resistant at> 4 μg / ml; Str. pneumoniae are considered to be sensitive MIC <2 μg / ml and resistant at> 8 μg / ml.

The prevalence of resistant strains varies geographically and at different times, so it is advisable to focus on local information on resistance, especially when treating severe infections.

Sensitive:

Gram-positive aerobes The frequency of resistance in the EU countries

(if> 10%) (extreme values)

Bacillus anthracis

Corynebacterium spp ^§

Enterococcus faecalis^§

Listeria monocytogenes

Streptococcus agalactiae

Streptococcus bovis

Streptococcus pneumoniae # * 4.6-51.4 %

Streptococcus pyogenes # *

Streptococcus viridans^§

Gram-negative aerobes:

Brucella spp #

Escherichia coli * 46.7%

Haemophilus influenzae * 2-31.7 %^e

Haemophilus para-influenzae * 15.3%

Neisseria gonorrhoeae^§12- 80%> ^ь

Neisseria meningitidis #

Proteus mirabilis 28%

Salmonella spp^§

Shigella spp^§

Vibrio cholerae

Anaerobes

Bacteroides melaninogenicus^§

Clostridium spp

Fusobacterium spp}

Peptostreptococci

Resistant

Gram-positive aerobes

Staphylococcus (βlactamase-producing strains)

Gram-negative aerobes

Acinetobacter spp

Citrobacter spp

Enterobacter spp

Klebsiella spp

Moraxella catarrhalis *

Proteus spp (indol positive)

Proteus vulgaris

Providencia spp

Pseudomonas spp

Serratia spp

Anaerobes

Bacteroides fragilis

Other

Chlamydia

Mycoplasma Rickettsia

a) % production of β-lactamase

(b) % penicillin resistance (including intermediate resistance)

# To date, there have been no reports of the appearance of β-lactamase-producing strains.

^§ Inconsistent sensitivity; Sensitivity can not be predicted without sensitivity testing.

* Clinical efficacy was shown for sensitive strains when used according to indications.

Bacteria may have resistance to amoxicillin (and hence ampicillin) as a result of the production of beta-lactamases, hydrolyzing aminopenicillins (which can be inhibited by clavulanic acid), changes in penicillin binding proteins, impaired permeability to the drug, or the operation of special pump pumps that pump the drug out of the cell . In one microorganism, several mechanisms of resistance can be present simultaneously,which explains the existence of variable and unpredictable cross-resistance to other betalactams and antibacterial drugs from other groups.

Pharmacokinetics:

Suction:

Absorption - fast, high (93%), food intake does not affect absorption, does not break down in the acidic environment of the stomach. When administered orally in the form of a suspension in a dose of 125 and 250 mg Cmah - 1.5-3 and 3.5-5 μg / ml, respectively. Maximum plasma concentrations are observed 1 to 2 hours after taking the drug.

Distribution:

About 17% of amoxicillin is in the plasma-bound state.

It has a large volume of distribution: in high concentrations it is found in plasma, sputum, bronchial secretion (in the purulent bronchial secretion the distribution is weak), pleural and peritoneal fluid, urine, skin blisters, lung tissue, intestinal mucosa, female genital organs, prostate gland, medium ear fluid (with its inflammation), bones, adipose tissue, gall bladder (with normal liver function), fetal tissues. When the dose is doubled, the concentration also doubles.Concentration in bile exceeds the concentration in plasma by 2-4 times. In amniotic fluid and vessels of the umbilical cord, the concentration of amoxicillin is 25-30% of the level in the plasma of a pregnant woman. Poor penetration through the BBB, with inflammation of the meninges, the concentration in the CSF is about 20% of the plasma level. Amoxicillin passes through the placenta and is found in small amounts in breast milk.

Biotransformation and elimination:

Partially metabolized with the formation of inactive metabolites. T1 / 2 - 1-1.5 hours. It is excreted by 50-70% kidneys in unchanged form (by tubular secretion - 80% and glomerular filtration - 20%), liver - 10-20%. In small amounts excreted in breast milk. T1 / 2 in preterm, newborns and children up to 6 months - 3-4 hours. renal dysfunction (CK less than or equal to 15 ml / min) T1 / 2 increases to 8.5 h. Amoxicillin is removed during hemodialysis.

Indications:

Ospamox® is indicated for oral therapy of the following bacterial infections caused by amoxicillin-sensitive Gram-positive and Gram-negative pathogens:

- Upper respiratory tract infections, including ear, nose and throat infections: acute otitis media, acute sinusitis and bacterial pharyngitis.

- Infections of the lower respiratory tract: exacerbation of chronic bronchitis, community-acquired pneumonia.

- Infections of the gastrointestinal tract: bacterial enteritis, infections caused by H. Pylori.

- Infections of the genitourinary system: cystitis, pyelonephritis, prostatitis, epididymitis, urethritis, uncomplicated gonorrhea.

- Infections of the skin and subcutaneous tissue.

- Endocarditis: prevention of endocarditis in patients at risk for developing endocarditis - for example, in the conduct of dental procedures.

Contraindications:

Hypersensitivity to penicillins.

Carefully:

- It is necessary to consider the possibility of cross-allergy with other beta-lactam antibiotics, such as cephalosporins and carbapenems.

- Ospamox® should be used with caution in patients with viral infections, acute lymphoblastic leukemia and infectious mononucleosis (due to an increased risk of erythematous skin rash).

Pregnancy and lactation:

The use of amoxicillin during pregnancy and breastfeeding is only possible if the intended benefit to the mother exceeds the potential risk to the fetus or infant.

Dosing and Administration:

The drug is intended for oral use. Absorption of amoxicillin does not decrease with simultaneous intake of food.

For the preparation of a suspension fill the bottle with drinking water about 1 cm before reaching the mark, close the bottle and shake it thoroughly. After the foam settles, add water exactly to the mark. Shake thoroughly again.

After that, the suspension is ready for use.

Before each use, shake the bottle thoroughly.

Therapy of infections:

Typically, therapy is recommended to continue for 2-3 days after the disappearance of symptoms. In the case of infections caused by beta-hemolytic streptococcus, complete eradication of the pathogen requires a therapy for at least 10 days.

Adults doses (including elderly patients):

Standard dose:

The standard dose is from 750 mg to 3 grams of amoxicillin per day, divided into several doses.

Children's dosages (children under 12 years of age or less than 40 kg of body weight)

The daily dose for children is 25-50 mg / kg / day in 3 divided doses (maximum 60 mg / kg / day), depending on the indication and severity of the disease.

Children over 12 years of age or with a body weight above 40 kg should receive an adult dosage.

Dosing in renal failure:

In patients with severe renal failure, the dose should be reduced. For renal clearance less than 30 ml / min, an interval between doses or a decrease in subsequent doses is recommended.

Adults (including patients of senile age):

Creatinine clearance ml / mi	Dose	Interval between administrations
> 30	Dose changes are not required.
10-30	500 mg	12 h
< 10	500 mg	24 h

When hemodialysis: 500 mg should be administered after the end of the procedure.

Impaired renal function in children weighing less than 40 kg:

Creatinine clearance ml / min	Dose	Interval between administrations
>30	Dose changes are not required.
10-30	15 mg / kg	12 h
< 10	15 mg / kg	24 h

Prophylaxis of endocarditis

For the prevention of endocarditis, 3 g of amoxicillin should be prescribed 1 hour before the operation and, if necessary, another 3 g after 6 hours.

Children should be prescribed amoxicillin at a dose of 50 mg / kg.

Side effects:

Side effects are classified as follows:

Often: 10%, or less often, but more often 1%

Infrequently: 1%, or less often, but more often 0.1%

Rarely: 0.1% or less, but more often 0.01%

Very rarely, including isolated cases: 0.01% or less.

Changes in the blood and lymphatic system.

Rarely: eosinophilia and hemolytic anemia.

Rarely: single cases of leukopenia, granulocytopenia, thrombocytopenia, anemia.All changes were reversible upon discontinuation of therapy.

Changes from the immune system.

Rarely: laryngeal edema, serum sickness, allergic vasculitis, anaphylaxis and anaphylactic shock in rare cases.

Neurological disorders.

Rarely: aseptic meningitis.

Gastrointestinal disorders.

Often: discomfort, nausea, loss of appetite, vomiting, flatulence, diarrhea, dry mouth, dyspnoea, dysbacteriosis. As a rule, the listed effects are characterized by mild severity and often disappear as the therapy continues or very quickly after its termination.

With the development of severe persistent diarrhea, it is necessary to take into account the possibility of a very rare complication, pseudomembranous colitis. In these cases, the prescription of drugs that suppress peristalsis is contraindicated.

Changes in the liver and biliary system.

Infrequently: a transient increase in the level of hepatic enzymes.

Changes in the skin and subcutaneous fat.

Often: skin reactions in the form of hyperemia of the skin, itching, exanthema,urticaria; a typical exanthema appears on days 5-11 after the initiation of therapy. Immediate development of urticaria indicates an allergic reaction to amoxicillin and requires discontinuation of therapy.

Rarely: angioedema (Quincke's edema), exudative erythema multiforme, acute exanthematous pustular eruptions, Stevens-Johnson syndrome, toxic epidermal necrolysis, bullous and exfoliative dermatitis, stomatitis.

Changes in the urinary system.

Rarely: acute interstitial nephritis.

General disorders.

Rarely: drug fever.

Overdose:

Symptoms.

Amoxicillin usually does not cause acute toxic effects, even with the occasional use of high doses. Overdose may manifest symptoms of gastrointestinal disorders, a violation of the water-electrolyte balance.

Therapy.

It is necessary to stop taking amoxicillin.

There is no specific antidote to amoxicillin.

Therapy includes the introduction of activated charcoal (indications for gastric lavage, as a rule, no) or symptomatic measures. Particular attention should be paid to maintaining the water-electrolyte balance.It is possible to use hemodialysis.

Interaction:

Joint use is not recommended:

Allopurinol.

Joint application with allopurinol can lead to the development of allergic skin reactions.

Digoxin

It is possible to increase absorption of digoxin against amoxicillin therapy.

Anticoagulants

Amoxicillin, suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index, and thereby increases the effectiveness of indirect anticoagulants.

Other antibiotics

Pharmaceutically incompatible with aminoglycosides (to avoid mutual inactivation it is impossible to mix).

Ospamox should not be used concomitantly in combination with bacteriostatic antibiotics (macrolides, tetracyclines), sulfonamides because of a possible decrease in activity (antagonistic action); bactericidal antibiotics (including aminoglycosides, cephalosporins) have a synergistic effect.

Methotrexate

Amoxicillin reduces clearance and increases the toxicity of methotrexate.

FROM caution should be applied amoxicillin with the following preparations:

Oral hormonal contraceptives

Amoxicillin reduces the effectiveness of estrogen-containing oral contraceptives.The use of amoxicillin can lead to a transient decrease in the concentration of estrogen and progesterone in the blood and reduce the effectiveness of hormonal contraceptives. In this regard, it is recommended to additionally use non-hormonal methods of contraception for the duration of amoxicillin treatment.

Special instructions:

Before beginning therapy with amoxicillin it is important to make sure that there is no hypersensitivity reaction to penicillins and cephalosporins in the anamnesis, which can cause a cross allergic reaction (10-15%).

Long-term use of amoxicillin in some cases may lead to an increase in resistant bacteria and fungi.

Ospamox powder for oral suspension contains aspartame (E951) and should be administered with caution to patients with phenylketonuria. In homozygous patients with phenylketonuria, the amount of phenylalanine, the source of which is aspartame, should be included in the calculation of the consumption of phenylalanine.

The composition of this medical product includes sodium benzoate and sodium citrate, which is important to consider patients on a diet with limited sodium intake.The sodium content in the maximum daily dose does not exceed 200 mg.

In the development of severe persistent diarrhea, the probability of pseudomembranous colitis caused by Clostridium difficile.

In course treatment it is necessary to monitor the status of the functions of the organs of hematopoiesis, liver and kidneys.

When using amoxicillin in high doses in order to minimize the risk of amoxicillin crystals, it is important to monitor the adequacy of consumption and elimination of fluid.

When determining the presence of glucose in urine amoxicillin therapy is recommended to use enzymatic glucose oxidant methods. When using chemical methods, a high concentration of amoxicillin in urine can cause false positive results.

Form release / dosage:

Powder for the preparation of a suspension for ingestion 125 mg / 5 ml.

Packaging:

Primary packaging. By 5.1 g or 8.5 g of powder to prepare a suspension for ingestion in vials of dark glass. The vials have a circular mark. The bottle is sealed with a sealing gasket and covered with a childproof cover with a childproof cover and a first tamper-evident control ring.

Secondary packaging.For 1 bottle of dark glass, complete with a measuring spoon and instructions for medical use in a pack of cardboard. Powder for the preparation of the suspension for oral administration 250 mg / 5 ml Primary packaging 6.6 g or 11.0 g powder for the preparation of a suspension for oral administration in vials of dark glass. The vials have a circular mark. The bottle is sealed with a sealing gasket and covered with a screw cap PE / PP cover with child protection and a control ring of the first opening.

Secondary packaging. For 1 bottle of dark glass, complete with a measuring spoon and instructions for medical use in a pack of cardboard. Powder for suspension for oral administration 500 mg / 5 ml

Primary packaging. For 12 g or 20 g powder for the preparation of a suspension for oral administration in vials of dark glass. The vials have a circular mark. The bottle is sealed with a sealing gasket and covered with a screw cap PE / PP cover with child protection and a control ring of the first opening.

Secondary packaging. For 1 bottle of dark glass, complete with a measuring spoon and instructions for medical use in a pack of cardboard. Packaging for hospitals (for all dosages) For 40 bottles of dark glass (with a capacity of 60 ml or 100 ml) with instructions for medical use in a carton box.

Storage conditions:

At a temperature of no higher than 25 ° C.

The finished suspension is stored at a temperature of 2 to 8 ° C in a tightly closed vial. Keep out of the reach of children.

Shelf life:

3 years.

Finished suspension: 14 days.

Do not use the drug after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-002012

Date of registration:12.03.2012

The owner of the registration certificate:Sandoz GmbHSandoz GmbH Austria

Manufacturer: & nbsp

SANDOZ, GmbH Austria

Representation: & nbspSANDOZ SANDOZ Switzerland

Information update date: & nbsp14.04.2015

Illustrated instructions

Instructions

Ospamox® (Ospamox®)