Pharmacological properties of the drug Hiconcil
An antibiotic of the group of semisynthetic penicillins with a wide spectrum of bactericidal action. Active against gram-negative ( Haemophilus influenzae, Bordetella pertussis, Proteus mirabilis , Brucella strains , Neisseria gonorrhoeae , Neisseria meningitidis , most strains of salmonella, shigella, Escherichia coli and Borrelia burgdorferi Clostr strains , Streptococcus pneumoniae , Bacillus anthracis, Corynebacterium diphtheriae and most strains of enterococci) microorganisms. Does not affect bacteria that produce penicillinase. About 90% of the dose taken is absorbed in the small intestine. The maximum plasma level is reached 1–2 hours after oral administration. Concentration in blood plasma depends on the dose. The half-life is 60–90 minutes. In patients with renal failure, the half-life increases to 7 hours. The minimum concentration of amoxicillin in the blood plasma is determined another 8 hours after administration. Amoxicillin does not accumulate in the body. Approximately 15–20% of amoxicillin is bound to plasma proteins. Amoxicillin penetrates well into tissues and biological fluids of the body. The maximum concentration in biological fluids of the body is achieved 1 hour after reaching the maximum concentration in the blood plasma. Therapeutic concentrations are determined in the lungs, liver, lymph glands, uterus, ovaries, and mucous membrane of the paranasal sinuses. Penetrates into the exudate of the middle ear cavity. The concentration of amoxicillin in purulent exudate is higher than in the mucous secretion of the respiratory tract. The concentration of amoxicillin in bile is 10 times higher than in blood plasma. Amoxicillin penetrates poorly into brain tissue and cerebrospinal fluid. Does not penetrate prostate tissue. Amoxicillin is excreted mainly in the urine, 50–70% unchanged. About 10–20% of amoxicillin is metabolized. The beta-lactam ring is metabolized to penicillic acid, which is excreted in the urine. A minimal amount is excreted in bile. The pharmacokinetics of amoxicillin in children over 2 years of age is almost the same as in adults. In newborns, amoxicillin is excreted more slowly than in adults. Their half-life is 3.7–4 hours.
Hiconcil 250 mg/5 ml 100 ml por.d/susp. for oral administration
Trade name HICONCIL International nonproprietary name Amoxicillin Dosage form Powder for the preparation of suspension for oral administration 250 mg/5 ml Composition 5 ml of suspension contain the active substance - amoxicillin trihydrate 287.0 mg (equivalent to amoxicillin 250 mg) excipients: anhydrous citric acid, sodium benzoate, aspartame (E951), talc, sodium citrate anhydrous, lemon powder flavor, peach-apricot powder flavor, orange powder flavor, galactomannan guar gum, precipitated silicon dioxide Description Powder from white to slightly yellowish in color with a fruity odor. A suspension prepared in an appropriate amount of water is white to slightly yellowish in color with a fruity odor. Pharmacotherapeutic group Antimicrobials for systemic use. Beta-lactam antibacterial drugs. Broad-spectrum penicillins. Amoxicycline. ATC code J01CA04 Pharmacological properties Pharmacokinetics Absorption Amoxicillin is stable in the acidic environment of gastric juice, about 90% of the dose taken is absorbed in the small intestine. Eating does not affect the absorption of amoxicillin. The maximum plasma concentration is reached 1-2 hours after oral administration and is about 5 mcg/ml after taking a dose of 250 mg and 10 mcg/ml after taking a dose of 500 mg. The half-life of amoxicillin in patients with normal renal function is 60 to 90 minutes. In patients with renal failure, the half-life increases to 7 hours. The minimum concentration of amoxicillin in the blood plasma is detected 8 hours after administration. Distribution: 15–20% of amoxicillin is bound to plasma proteins. Amoxicillin penetrates well into tissues and biological fluids of the body. The maximum concentration in biological fluids of the body is achieved 1 hour after reaching the maximum concentration in the blood plasma. Therapeutic concentrations are determined in the lungs, liver, lymph glands, uterus, ovaries, and mucous membrane of the paranasal sinuses. Penetrates into the exudate of the middle ear cavity. The concentration of amoxicillin in purulent exudate is higher than in the mucous secretion of the respiratory tract. Amoxicillin also penetrates into the pleural and peritoneal fluids and is concentrated in saliva and tears. The concentration of amoxicillin in bile is 10 times higher than in blood plasma. In case of blockage of the bile ducts, amoxicillin penetrates minimally into the bile ducts. Amoxicillin weakly penetrates the blood-brain barrier (BBB) and cerebrospinal fluid, does not penetrate prostate tissue, penetration through the BBB increases during inflammatory processes. Amoxicillin penetrates the placental barrier and enters the fetal circulation. Approximately 50% of the amoxicillin concentration is determined in fetal blood and amniotic fluid compared to maternal blood plasma. Amoxicillin passes into breast milk in minimal quantities. Excretion Amoxicillin is excreted through the kidneys by glomerular filtration and tubular secretion. From 50% to 70% of an oral dose is excreted in unchanged active form in the urine, where after taking a dose of 250 mg, concentrations range from 0.3 to 1.3 g/l. Between 10% and 20% of amoxicillin is metabolized. The beta-lactam ring is metabolized to penicillic acid, which is excreted in the urine. A minimal amount of amoxicillin is excreted in the bile. Following a 3 g dose, mean bile concentrations were 19 mcg/mL. Enterohepatic circulation of amoxicillin is minimal. The maximum concentration of amoxicillin in breast milk, achieved 5 hours after ingestion of a dose of 1 g, is 0.81 mcg/ml. In severe renal failure, dose adjustment is necessary. Creatinine clearance ml/s (ml/min) 1.33–0.83 (80–50) 0.83–0.16 (50–10) <0.16 (<10) Amoxicillin dose 250 mg – 500 mg 8 hours 8–12 hours 12–24 hours When Peritoneal dialysis does not require dose adjustment. Hemodialysis removes 85% of amoxicillin and therefore the recommended dose should be administered after hemodialysis is stopped. Pharmacodynamics The effect of amoxicillin on bacterial cells Hiconcil suppresses the last phase of bacterial cell wall formation by inhibiting the action of transpeptidases, enzymes involved in the synthesis of peptidoglycan, which is an important component of the bacterial cell wall. Bacteria produce several types of penicillin-binding proteins (PBPs). Penicillin antibiotics inhibit the action of one or more transpeptidases. Impaired peptiglycan synthesis leads to the development of a defective cell wall, which is osmotically unstable and leads to the death of the bacterial cell. Penicillins also appear to be involved in bacterial wall disruption by inhibiting the action of an inhibitor of murein hydrolase, an enzyme that is associated with cell division. Thus, amoxicillin is a bactericidal antibiotic. The time it takes for the antibiotic concentration to reach the minimum inhibitory concentration (T>MIC) is a very important factor for the successful treatment of bacterial infections with beta-lactam antibiotics. When reaching 40% of the dosing time, the maximum clinical effect of amoxicillin may develop. Antibacterial spectrum of action Amoxicillin is effective against gram-positive and some gram-negative microorganisms. Compared to penicillin, amoxicillin is less effective against Streptococcus pyogenes, Streptococcus pneumoniae and Streptococcus agalactiae; however, penicillin is more effective against enterococci and Listeria monocytogenes. The effects of amoxicillin on gram-positive anaerobic bacteria and Neisseria species are the same as those of penicillin. Because beta-lactamases destroy amoxicillin, they are ineffective against beta-lactamase-producing strains and therefore have no effect on most strains of staphylococci. Strains of Haemophilus influenzae, Haemophilus parainfluenzae, E. coli, Salmonella species. and Shigella, which do not produce beta-lactamases, are sensitive to amoxicillin. Most other gram-negative bacteria are resistant to amoxicillin. Table 1. Bacteria sensitive to amoxicillin *: Gram-positive bacteria Gram-negative bacteria Streptococcus pneumoniae Haemophilus influenzae Streptococcus pyogenes pyogenes Escherichia coli Streptococcus viridans Proteus mirabilis Streptococcus agalactiae Salmonella spp. Staphylococcus aureus Shigella spp. Enterococcus faecalis Neisseria spp. Bacillus anthracis Bordetella pertussis Listeria monocytogenes Brucella spp. Corynebacterium spp. Vibrio cholerae Clostridium spp. Pasteurella septica
Use of the drug Hiconcil
Take orally with a sufficient amount of liquid 3 times a day, regardless of meals. Depending on the age (body weight) and severity of the infectious process, a single dose of the drug can be: for children aged 1–2 years (10 kg) - 2.5–5 ml of suspension (1/2–1 measuring spoon); 6 years (20 kg) - 1 capsule (250 mg) or 1-2 scoops of suspension; 10 years (30 kg) - 1 capsule (250 mg) or 2-3 scoops of suspension; 12 years (40 kg) - 250–500 mg (in capsules or the appropriate amount of suspension); for children weighing 40 kg and adults - 250–1000 mg (capsules).
Special instructions for the use of the drug Hiconcil
In case of severe allergic reactions, the drug is discontinued, antihistamines are prescribed, and, if necessary, epinephrine, corticosteroids. Skin rash most often occurs when the drug is prescribed to patients with infectious mononucleosis. In some cases, cross-hypersensitivity to cephalosporins and penicillins may occur. Microorganisms resistant to ampicillin often exhibit cross-resistance to amoxicillin. Caution is advised if severe diarrhea develops, as this may indicate the presence of pseudomembranous colitis. During treatment with Hiconcil, when determining blood glucose levels using the reduction method, the results may be distorted. In severe renal failure (glomerular filtration ≤10 ml/min), the interval between two successive doses should be increased to 12–24 hours. The drug should be used with caution during pregnancy and lactation.
Hiconcil caps 500 mg in blister pack. in pack №8x2
Name
Hiconcil caps 500 mg in blister pack. in pack №8x2
Description
Hard opaque gelatin capsules. The cap of the capsule is burgundy (brown-red), the body of the capsule is pink.
Main active ingredient
Amoxicillin
Release form
8 capsules in a blister. 2 blisters in a cardboard box along with instructions for use.
Dosage
500mg
special instructions
Use with caution in patients prone to allergic reactions. Amoxicillin in combination with metronidazole is not recommended for use in patients under 18 years of age; should not be used for liver diseases. During combination therapy with metronidazole, it is not recommended to drink alcohol.
pharmachologic effect
Hiconcil has a broad spectrum antibacterial and bactericidal effect. Blocks the synthesis of peptidoglycan and disrupts the formation of the cell wall of microorganisms. Hiconcil is a broad-spectrum semisynthetic penicillin antibiotic. Has a bactericidal effect. Active against aerobic gram-positive bacteria: Staphylococcus spp. (except for penicillinase-producing strains), Streptococcus spp; aerobic gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp., Salmonella spp., Klebsiella spp. Microorganisms that produce penicillinase are resistant to amoxicillin. Cross-resistance exists between amoxicillin and ampicillin.
Indications for use
Treatment: infectious and inflammatory diseases of the ENT organs, lower respiratory tract, urinary tract, gastrointestinal tract, skin and soft tissues, Lyme borreliosis (Lyme disease), gonorrhea. Prevention - bacterial endocarditis, surgical interventions in the oral cavity, on the upper respiratory tract. To continue therapy after treatment with parenteral forms of aminopenicillins.
Directions for use and doses
Hiconcil is taken orally, on an empty stomach or after meals (the powder for preparing the suspension and drops is pre-diluted and shaken before use). Adults - 500 mg 3 times a day; in severe cases, the dose is increased to 1000 mg 3 times a day; children: 5-10 years old - 250 mg 3 times a day, 2-5 years old - 125 mg 3 times a day, under 2 years old - 20 mg/kg/day in 3 divided doses. The course of treatment is 5-12 days.
Use during pregnancy and lactation
There was no negative effect of amoxicillin on the fetus. Pregnant women can be prescribed the drug if the doctor has carefully assessed the validity of its use. A small amount of the drug is excreted in breast milk; however, it can be prescribed during breastfeeding.
Precautionary measures
In case of severe renal dysfunction (Cl creatinine less than 10 ml/min), it is necessary to increase the interval between doses to 12–24 hours. Take with caution during pregnancy and lactation (only under medical supervision).
Interaction with other drugs
Amoxicillin reduces the effectiveness of oral contraceptives. When used together with allopurniol, the incidence of skin rash increases. Simultaneous use with clavulanic acid enhances the effect of amoxicillin. Bacteriostatic antibiotics reduce the effectiveness of amoxicillin. When used simultaneously with methotrexate, its toxicity increases. With concomitant use, the effectiveness of anticoagulants may increase, increasing the risk of bleeding. A false-positive Coombs test and a false-positive determination of glucose in urine are possible.
Contraindications
Hypersensitivity to penicillins and/or cephalosporins. Infectious mononucleosis, lymphocytic leukemia, severe gastrointestinal infections accompanied by diarrhea or vomiting, respiratory viral infections, allergic diathesis, bronchial asthma, hay fever.
Compound
1 capsule contains: Active substance: amoxicillin trihydrate - 292.1A mg or 585.48 mg, which is equivalent to 250 mg and 500 mg of amoxicillin. Excipients: colloidal anhydrous silicon dioxide, magnesium stearate. Capsule: titanium dioxide (E171), yellow iron oxide (E172), red iron oxide (E172), indigo carmine (E132), azorubine (E122), gelatin.
Overdose
Symptoms: nausea, vomiting, diarrhea, crystalluria, signs of central nervous system excitation, confusion, hallucinations, convulsions. Treatment: symptomatic. Taking a very large amount of the drug causes an increase in the concentration of amoxicillin in the urine. Patients with normal kidney function can avoid developing damage by drinking enough fluids. However, crystalluria may occur. In patients with impaired renal function, amoxicillin should be removed from the body by hemodialysis.
Side effect
Nausea, vomiting, diarrhea, pseudomembranous colitis, allergic reactions (rash, urticaria, etc., including anaphylactoid).
Storage conditions
Store at a temperature not exceeding 25°C. Store in original packaging to protect from light.
