Amosin, 250 mg/3 g 10 pcs.

Pharmacotherapeutic group

Antibiotic, semi-synthetic penicillin

ATC code: J01CA04

Pharmacodynamics:

A broad-spectrum antibacterial bactericidal acid-resistant agent from the group of semisynthetic penicillins. It inhibits transpeptidase disrupts synthesis of peptidoglycan (support protein of cell wall) during division and growth causing lysis of bacteria. Active against aerobic Gram-positive bacteria: Staphylococcus spp. (except for penicillinase-producing strains) Streptococcus spp; and aerobic Gram-negative bacteria: Neisseria gonorrhoeae Neisseria meningitidis Escherichia coli Shigella spp. Salmonella spp. Klebsiella spp. Microorganisms producing penicillinase are resistant to the action of amoxicillin. Action develops 15-30 minutes after administration and lasts for 8 hours.

Pharmacokinetics:

Absorption – fast high (93%) food intake has no effect on absorption is not destroyed in the acidic environment of the stomach. When administered orally in doses of 125 and 250 mg, the maximum concentration is 1.5-3 mcg/ml and 3.5-5 mcg/ml, respectively. Time to maximum concentration after oral administration is 1-2 hours. It has a large volume of distribution – high concentrations are found in plasma sputum bronchial secretion (poor distribution in purulent bronchial secretion) pleural and peritoneal fluid urine contents of skin blister tissue lung tissue intestinal mucosa female genital organs prostate middle ear fluid bone adipose tissue gallbladder (with normal liver function) fetal tissues.

The concentration also increases by a factor of 2 when the dose is increased by a factor of 2. The concentration in bile is 2-4 times higher than in plasma. In amniotic fluid and umbilical cord vessels, the concentration of amoxicillin is 25-30% of the level in plasma of a pregnant woman. Poorly penetrates through the blood-brain barrier in inflammation of the meninges (meningitis), the concentration in cerebrospinal fluid is about 20%. Binding with plasma proteins is 17%.

Partially metabolized to form inactive metabolites. Half-life period is 1-1.5 hours. It is eliminated 50-70% unchanged by kidneys through tubular excretion (80%) and glomerular filtration (20%) by liver – 10-20%. A small amount is excreted with breast milk. Half-life in premature infants and children up to 6 months is 3-4 hours. With impaired renal function (creatinine clearance less than or equal to 15 ml/min) the half-life is increased to 8.5 hours. Amoxicillin is eliminated with hemodialysis.

Indications

Active ingredient

Composition

How to take, the dosage

Overly before or after meals.

Adults and children over 10 years of age (with body weight over 40 kg) are prescribed 0.5 g 3 times a day; in severe course of infection – 0.75-1 g 3 times a day. Children under 5-10 years of age are prescribed 0.25 g 3 times daily; 2-5 years of age – 0.125 g 3 times daily; under 2 years of age – 20 mg/kg 3 times daily. The course of treatment is 5-12 days.

In acute uncomplicated gonorrhea 3 g is prescribed once; when treating women the repeated administration of the indicated dose is recommended.

In acute infectious diseases of the gastrointestinal tract (paratyphoid typhoid) and biliary tract in gynecological infectious diseases in adults 1.5-2 g 3 times a day or 1-1.5 g 4 times a day.

In leptospirosis in adults – 0.5-0.75 g 4 times a day for 6-12 days.

In case of salmonella carriage in adults – 1.5-2 g 3 times a day for 2-4 weeks.

In prophylaxis of endocarditis during minor surgical interventions in adults – 3-4 g 1 hour before the procedure. If necessary a second dose is administered after 8-9 hours. In children the dose is reduced by half.

In patients with impaired renal function and in creatinine clearance of 15-40 ml/min the interval between doses is increased up to 12 hours; in creatinine clearance less than 10 ml/min the dose is reduced by 15-50%; in anuria – maximum dose 2 g/day.

Preparation of suspension.

One-dose bag.

In a clean beaker, pour boiled and cooled water (see table) then pour the contents of one bag and stir until a homogeneous suspension is obtained.

After intake, rinse the beaker with water to dry and store in a clean dry place.

Vial or jar.

In a vial or jar containing 5 g of amoxicillin 62 ml of boiled and cooled water or distilled water is added. 1 ml of the ready-made suspension contains 50 mg of amoxicillin. The suspension is shaken before use. The suspension is dosed with a double-sided spoon: the large spoon contains 5 ml (025g), the small one 25 ml (0125g) or with a spoon with two marks: the lower one corresponds to 25 ml (0125g) and the upper one to 5 ml (025g).

Interaction

Antacids glucosamine laxatives food aminoglycosides – slow down and reduce absorption; ascorbic acid increases absorption.

Bactericidal antibiotics (including aminoglycosides cephalosporins cycloserine vancomycin rifampicin) – synergistic effect; bacteriostatic drugs (macrolides chloramphenicol lincosamides tetracyclines sulfonamides) – antagonistic.

Increases the effectiveness of indirect anticoagulants (by suppressing intestinal microflora it reduces the synthesis of vitamin K and prothrombin index); reduces the effectiveness of estrogen-containing oral contraceptives drugs in the metabolism of which para-aminobenzoic acid ethinyl estradiol is formed – the risk of bleeding “breakthrough”.

Diuretics allopurinol oxyphenbutazone phenylbutazone non-steroidal anti-inflammatory drugs; drugs that block tubular secretion – reducing tubular secretion increases the concentration.

Allopurinol increases the risk of skin rash.

Decreases clearance and increases toxicity of methotrexate.

It increases the absorption of digoxin.

Special Instructions

During the course of treatment it is necessary to monitor the hematopoietic function of the liver and kidneys.

The development of superinfection due to the growth of microflora insensitive to it is possible, which requires appropriate changes in antibiotic therapy.

When treating patients with bacteremia a bacteriolysis reaction may develop (Jarisch-Herxheimer reaction).

In patients with hypersensitivity to penicillins cross-allergic reactions with cephalosporin antibiotics are possible.

In the treatment of mild diarrhea, antidiarrheal medications that decrease intestinal peristalsis should be avoided; kaolin- or attapulgit-containing antidiarrheal medications may be used. If the diarrhea is severe, a physician should be consulted.

The treatment must be continued for an additional 48-72 hours after clinical signs of illness have disappeared.

In case of concomitant use of estrogen-containing oral contraceptives and amoxicillin, other or additional contraceptive methods should be used if possible.

Contraindications

Hypersensitivity (including to other penicillins cephalosporins carbapenems) allergic diathesis bronchial asthma pollinosis infectious mononucleosis lympholeukosis liver failure gastrointestinal diseases in the history (especially colitis associated with antibiotic use) lactation period.

Pregnancy renal failure bleeding in the history.

Side effects

Allergic reactions: possible urticaria hyperemic skin erythema angioneurotic edema rhinitis conjunctivitis; rarely – fever joint pain eosinophilia exfoliative dermatitis erythema polyformic exudative erythema Stevens-Johnson syndrome; serum-like reactions; in single cases – anaphylactic shock.

Digestive system disorders: dysbacteriosis change of taste vomiting diarrhea stomatitis glossitis impaired liver function moderate increase in “hepatic” transaminase activity pseudomembranous enterocolitis.

Nervous system disorders: agitation anxiety insomnia ataxia confusion altered behavior depression peripheral neuropathy headache dizziness seizure reactions.

Laboratory findings: leukopenia neutropenia thrombocytopenic purpura anemia.

Others: difficulty breathing tachycardia interstitial nephritis vaginal candidiasis superinfection (especially in patients with chronic disease or reduced body resistance).

Overdose

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