Instructions for Opticef tablets 400 mg No. 14
Composition
active ingredient: cefixime;
1 film-coated tablet contains cefixime 400 mg (as cefixime trihydrate 447.630 mg);
excipients: microcrystalline cellulose (type 101), calcium hydrogen phosphate dihydrate, pregelatinized starch, microcrystalline cellulose (type 102), magnesium stearate;
Opadry Y-1-7000 white film-forming coating: hypromellose, macrogol/PEG 400, titanium dioxide (E 171).
Dosage form
Film-coated tablets.
Main physicochemical properties: oblong biconvex tablets, film-coated from white to light cream color with a score on one side.
Pharmacotherapeutic group
Antibacterials for systemic use. Beta-lactam antibiotics. Third-generation cephalosporins. ATX code J01D D08.
Pharmacological properties
Pharmacodynamics
Cefixime is a third-generation cephalosporin antibiotic for internal use. In vitro, it has significant bactericidal activity against a wide range of gram-positive and gram-negative microorganisms.
Clinically effective in the treatment of infections caused by the most common pathogens, including Streptococcus pneumoniae, Streptococcus pyogenes, E.coli, Proteus mirabilis, Klebsiella species, Haemophilus influenzae (beta-lactamase positive and negative), Branhamella catarrhalis (beta-lactamase positive and negative) and Enterobacter species. Has a high degree of stability in the presence of beta-lactamases.
Most strains of enterococci (Streptococcus faecalis, group D Streptococci) and Staphylococci (including coagulase-positive, coagulase-negative and methicillin-resistant strains) are resistant to cefixime. In addition, most strains of Pseudomonas, Bacteroides fragilis, Listeria monocytogenes and Clostridia are resistant to cefixime.
Pharmacokinetics
Absorption. The absolute bioavailability of cefixime after oral administration is 22-54%. Since the presence of food does not significantly affect absorption, cefixime can be administered without regard to meals. The maximum serum level after taking the recommended doses for adults or children is 1.5 to 3 μg/ml. With repeated dosing, slight accumulation of cefixime is possible.
Distribution: Cefixime is almost completely bound to albumin, with an average free fraction of approximately 30%.
Metabolism: Metabolites of cefixime have not been isolated from human serum or urine.
Excretion: Cefixime is excreted mainly unchanged in the urine. The predominant mechanism is glomerular filtration.
There is no data on the penetration of cefixime into breast milk.
Indication
Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:
upper respiratory tract infections (including otitis media) and other upper respiratory tract infections (sinusitis, pharyngitis, tonsillitis of bacterial etiology) in case of known or suspected resistance of the pathogen to other commonly used antibiotics, or in case of risk of treatment failure;
lower respiratory tract infections (including acute bronchitis and exacerbation of chronic bronchitis);
urinary tract infections (including cystitis, cystourethritis, uncomplicated pyelonephritis).
Clinically effective in the treatment of infections caused by the most common pathogens, including Streptococcus pneumoniae, Streptococcus pyogenes, E.coli, Proteus mirabilis, Klebsiella species, Haemophilus influenzae (beta-lactamase positive and negative), Branhamella catarrhalis (beta-lactamase positive and negative) and Enterobacter species. Has a high degree of stability in the presence of beta-lactamases.
Most strains of enterococci (Streptococcus faecalis, group D Streptococci) and Staphylococci (including coagulase-positive, coagulase-negative and methicillin-resistant strains) are resistant to cefixime. In addition, most strains of Pseudomonas, Bacteroides fragilis, Listeria monocytogenes and Clostridia are resistant to cefixime.
Contraindication
Confirmed hypersensitivity to cephalosporin antibiotics or to other components of the drug; hypersensitivity to penicillins; porphyria.
Interaction with other medicinal products and other types of interactions
Blockers of tubular secretion (allopurinol, probenecid, diuretics) increase the maximum concentration of cefixime in the blood serum, slowing down the excretion of cefixime by the kidneys, which may lead to symptoms of overdose.
Salicylic acid increases free cefixime by 50% due to displacement of cefixime from protein binding sites; this effect is concentration-dependent.
Concomitant use with carbamazepine may cause an increase in its plasma concentration, therefore it is advisable to monitor the level of carbamazepine in the blood plasma.
When cefixime is used in combination with potentially nephrotoxic substances (aminoglycosides, colistin, polymyxin, viomycin) or potent diuretics (ethacrynic acid, furosemide), there is an increased risk of developing renal failure.
Nifedipine increases bioavailability, but clinical interactions have not been determined.
Potentially, like other antibiotics, the use of the drug may reduce the effectiveness of combined oral contraceptives.
As with other cephalosporins, increases in prothrombin time have been reported in some patients, therefore caution should be exercised in patients receiving anticoagulant therapy.
Cefixime should be used with caution in patients receiving coumarin-type anticoagulants, such as warfarin potassium. Since cefixime may potentiate the effects of anticoagulants, an increase in prothrombin time with or without clinical bleeding may occur.
During treatment with cefixime, a false-positive direct Coombs test and a false-positive reaction to glucose in the urine when using copper sulfate tablets, Benedict's or Fehling's solutions are possible. It is recommended to use a glucose oxidase test to determine glucose in the urine.
Application features
Beta-lactams, including cefixime, increase the risk of encephalopathy (which may include seizures, confusion, movement disorders, impaired consciousness) in patients, especially in cases of overdose and renal failure.
Severe cutaneous adverse reactions, such as toxic epidermal necrolysis, Stevens-Johnson syndrome, drug rash with eosinophilia and systemic symptoms (DRESS syndrome) and acute generalized exanthematous pustulosis (AGEP), have been reported in some patients with cefixime. If severe cutaneous adverse reactions occur, cefixime should be discontinued and appropriate treatment should be initiated.
Before using cefixime, careful inquiry should be made regarding the patient's history of hypersensitivity reactions to penicillins and cephalosporins or to other drugs.
Cefixime should be used with caution in patients with a history of allergic reactions to penicillins. Cross-allergic reactions between penicillins and cephalosporins have been reported in both in vivo (in humans) and in vitro studies. These cases have been reported rarely and have been of the anaphylactic type, particularly after parenteral administration.
Antibiotics should be used with caution in patients with a history of any form of hypersensitivity reactions, especially after the use of drugs. If an allergic reaction occurs, the drug should be discontinued immediately and appropriate therapy should be prescribed.
Cases of drug-induced hemolytic anemia, including severe cases with fatal outcome, have been described with cephalosporins. Hemolytic anemia has also been reported after repeated use of cephalosporins (including cefixime).
Neutropenia and agranulocytosis may occur with beta-lactam antibiotics, especially with prolonged treatment. If neutropenia develops, cefixime treatment should be discontinued.
With long-term use of the drug (more than 10 days), blood parameters should be monitored.
Cefixime should be used with caution in patients with significant renal impairment (see Renal impairment).
As with other cephalosporins, cefixime may cause acute renal failure, including tubulointerstitial nephritis as the underlying pathological condition. If acute renal failure occurs, cefixime should be discontinued and appropriate therapy and/or measures should be taken.
Caution should be exercised when prescribing the drug in cases of bleeding, gastrointestinal diseases, especially ulcerative colitis, regional enteritis or colitis on the background of use, as well as in cases of impaired liver function.
The safety of cefixime in premature infants or neonates has not been established.
Prolonged use of antibacterial drugs may lead to the growth of non-susceptible microorganisms and disruption of the normal intestinal flora, which may lead to excessive growth of Clostridium difficile and the development of pseudomembranous colitis. In mild forms of pseudomembranous colitis caused by the use of antibiotics, discontinuation of the drug may be sufficient. If the symptoms of colitis do not improve after discontinuation, oral vancomycin, which is the antibiotic of choice in the event of pseudomembranous colitis, should be prescribed.
In case of moderate or severe colitis, electrolytes and protein solutions should be added to the treatment. Concomitant use of drugs that reduce intestinal peristalsis should be avoided.
In case of simultaneous use of cefixime with aminoglycosides, polymyxin B, colistin, loop diuretics (furosemide, ethacrynic acid) in high doses, it is necessary to carefully monitor renal function. After prolonged use of cefixime, the state of hematopoiesis function should be checked.
For infections caused by group A beta-hemolytic streptococcus, the course of treatment should be at least 10 days to prevent acute rheumatic fever.
During treatment, a positive direct Coombs test and a false-positive urine test for glucose are possible.
Cephalosporins increase the toxicity of alcohol, so it is not recommended to drink alcoholic beverages during treatment with cefixime.
Use during pregnancy or breastfeeding
In reproductive studies in mice and rats, at doses approximately 400 times the human dose, no evidence of impaired fertility or foetal harm was found in cefixime. In rabbits, at doses up to 4 times the human dose, there was no evidence of teratogenicity; a high incidence of abortions and maternal mortality was observed, which is expected given the known sensitivity of rabbits to changes in gut microflora caused by antibiotics.
There are no data on the use of the drug during pregnancy. Cefixime crosses the placenta.
The drug should not be used during pregnancy or breastfeeding, except in cases of extreme necessity as prescribed by a doctor.
Ability to influence reaction speed when driving vehicles or other mechanisms
Patients who experience central nervous system adverse reactions (e.g., convulsions, dizziness, impaired consciousness, movement disorders) while taking Opticef should refrain from driving or operating other machinery.
Method of administration and doses
Food intake does not affect the absorption of cefixime. Usually the course of treatment is 7 days, if necessary - up to 14 days. In the treatment of uncomplicated cystitis, the course of treatment is 3 days.
Adults and children over 12 years of age with a body weight of more than 50 kg: the recommended dose is 400 mg (one tablet) per day once or 200 mg (half a tablet) every 12 hours, depending on the severity of the disease.
Elderly patients: prescribe the drug in the recommended adult dose. Renal function should be monitored and the dose adjusted in severe renal insufficiency (see "Renal insufficiency").
Renal impairment: Cefixime can be used in cases of renal impairment. For patients with creatinine clearance of 20 ml/min or higher, the usual dose and dosing regimen should be used. For patients with creatinine clearance below 20 ml/min, it is not recommended to exceed a dose of 200 mg (half a tablet) once daily. This also applies to patients on continuous ambulatory peritoneal dialysis or hemodialysis.
Children.
Children under 12 years of age are recommended to use the drug in a different dosage form.
Overdose
There is a risk of encephalopathy with the use of beta-lactam antibiotics, including cefixime, especially in cases of overdose and renal failure.
Adverse reactions recorded when using the drug in doses up to 2 g in healthy volunteers did not differ from adverse reactions observed in patients taking the drug in recommended doses.
Symptoms: increased manifestation of adverse reactions.
Treatment: gastric lavage, symptomatic and supportive therapy. There is no specific antidote. Hemodialysis or peritoneal dialysis only slightly contributes to the removal of cefixime from the body.
Side effects
From the blood and lymphatic system: eosinophilia, hypereosinophilia, agranulocytosis, leukopenia, neutropenia, granulocytopenia, hemolytic anemia, thrombocytopenia, thrombocytosis, hypoprothrombinemia, thrombophlebitis, increased thrombin and prothrombin time, purpura.
On the part of the digestive system: stomach cramps, abdominal pain, diarrhea*, dyspepsia, nausea, vomiting, flatulence, dysbacteriosis, candidiasis of the oral mucosa, stomatitis, glossitis.
Liver and biliary tract: jaundice, hepatitis, cholestasis.
Infectious and parasitic diseases: pseudomembranous colitis.
Laboratory indicators: increased aspartate aminotransferase (AST), increased alanine aminotransferase (ALT), increased blood bilirubin, increased blood urea, increased serum creatinine.
Metabolism and nutrition disorders: anorexia (loss of appetite).
Nervous system: headache, dizziness, dysphoria; cases of convulsions have been reported with the use of cephalosporins, including cefixime (frequency unknown).
Beta-lactams, including cefixime, increase the risk of encephalopathy (which may include seizures, confusion, movement disorders, impaired consciousness) in patients, especially in cases of overdose and renal failure (frequency unknown).
Hearing disorders: hearing loss.
Respiratory, thoracic and mediastinal disorders: dyspnea.
Renal and urinary disorders: acute renal failure, including tubulointerstitial nephritis as the underlying pathological condition, hematuria.
Immune system disorders: anaphylactic reaction, serum sickness-like reactions, drug fever, arthralgia.
Skin and subcutaneous tissue disorders: urticaria, skin rash, pruritus, fever, facial edema, angioedema, drug rash with eosinophilia and systemic symptoms (DRESS), Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, acute generalized exanthematous pustulosis (AGEP) (see section "Special warnings and precautions for use").
Reproductive system and breast disorders: genital itching, vaginitis caused by Candida.
* Diarrhea is usually associated with higher doses. Moderate to severe diarrhea has been reported. Cefixime should be discontinued if severe diarrhea occurs.
Reporting adverse reactions after the registration of a medicinal product is important. This allows monitoring of the benefit/risk ratio when using this medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of the medicinal product via the Automated Information System for Pharmacovigilance at the link: https://aisf.dec.gov.ua.
Expiration date
3 years.
Storage conditions
In the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
7 tablets in a blister, 1 or 2 blisters in a pack.
Vacation category
According to the recipe.
Producer
Limited Liability Company "Agropharm".
Limited Liability Company "Natur+".
Location of the manufacturer and address of its place of business.
Ukraine, 08200, Kyiv region, Irpin, Centralna st., 113-A
Ukraine, 08200, Kyiv region, Irpin, Tarasa Shevchenko str., 3.
