Afenoxin instructions for use
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Afenoxin - Indications for use
Infections of the respiratory and urogenital tracts, the abdominal cavity, ENT organs, bones and joints, skin and soft tissues.
Afenoxin has a broad spectrum of antimicrobial activity, is most active against gram-negative bacteria, less pronounced effect on anaerobes.
It acts on Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Campylobacter jejuni, Citrobacter diversus, Citrobacter freundii, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Morganella morganii, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri , Providencia stuartii, Pseudomonas aeruginosa, Salmonella typhi, Serratia marcescens, Shigella flexneri, Shigella sonnei, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Acinetobacter spp., Acinetobacter calcoaceticus, Aeromonas caviae, Aeromonas hydrophila, Brucella melitensis, Campylobacter coli, Edwardsiella tarda, Enterobacter aerogenes, Haemophilus ducreyi, Klebsiella oxytoca, Legionella pneumophila, Moraxella (Branhamella) catarrhalis, Neisseria meningitidis, Pasteurella multocida, Salmonella enteritidis, Vibrio cholerae, Vibrio parahaemolyticus, Vibrio vulnificus, Yersinia enterocolitica, Chlamydia trachomatis, Mycobacterium tuberculosis. In an acidic environment, activity decreases.
The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin. Ciprofloxacin is moderately sensitive to Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly).
Most strains of Burkholderia cepacia and some strains of Stenotrophomonas maltophilia, as well as Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides are resistant to ciprofloxacin. Ineffective against Treponema pallidum.
Resistance develops slowly and gradually ("multistage" type). There is no cross-resistance with penicillins, cephalosporins, aminoglycosides.
When ingestion is quickly and fairly fully absorbed from the digestive tract, absorption is mainly in the duodenum and jejunum. Absolute bioavailability is 60-80%. Cmax is achieved after 1-1.5 hours and at doses of 250, 500 and 750 mg is 0.1; 0.2 and 0.4 μg / ml, respectively.
Eating slows down absorption, but does not alter Cmax and bioavailability. After 60 min IV infusion in doses of 200 and 400 mg Cmax - 2.1 and 4.6 μg / ml, the plasma concentration in 12 hours is 0.1 and 0.2 μg / ml, respectively. The binding with plasma proteins is 20-40%.
Penetrates into tissues, liquids and cells, creating high concentrations in the kidneys, gall bladder, liver, lungs, mucous membranes and sinuses, female genitalia, phagocytic cells (polynuclears, macrophages), urine, sputum, bile, blister fluid; is found in the prostate gland, cerebrospinal fluid (less than 10% of the plasma level, with meningitis - up to 45% or more), saliva, skin, adipose tissue, muscles, bones, cartilage, passes through the placenta. T1 / 2 for oral administration - 3,5-5 h, with iv introduction - 5-6 hours. Total Cl - about 35 l / h.
Biotransformiruetsya in the liver (15-30%) with the formation of low-activity metabolites (deethylciprofloxacin, sulphociprofloxacin, oxociprofloxacin, formyl ciprofloxacin).
It is excreted mainly by the kidneys (by glomerular filtration and tubular secretion) in unchanged form (with oral administration - 40-50%, after intravenous administration - 50-70%) and in the form of metabolites (ingestion - 15%, with / in the introduction - 10%), the rest - through the digestive tract (with bile and feces); a small amount is excreted by lactating mammary glands.
Concentrations in the urine greatly exceed the MIC for most pathogens of urinary tract infections. There was no cumulation after oral administration at a dose of 500 mg twice a day for 5 days or in / in the administration of 100, 150 and 200 mg twice a day for 7 days.
With chronic cirrhosis of the liver, pharmacokinetics does not change; in patients with renal insufficiency, T1 / 2 is prolonged.
Afenoxin in pregnancy
Contraindicated in pregnancy (safety and efficacy in women during pregnancy is not established).
Afenoxin - Contraindications
Hypersensitivity, pregnancy , lactation, age (up to 12 years).
Afenoxin - Side effects
Dizziness , anxiety, hallucinations, tremor, convulsive attacks, dyspepsia , nausea, gastralgia, tachycardia , hypotension , coronary insufficiency, thrombosis, arthralgia, gout , renal dysfunction, increased hepatic transaminase activity, superinfection (candidiasis), allergic reactions.
Afenoxin - Administration and dosage
Inside, 250-500-750 mg every 12 hours.
Afenoxin - Interaction with other drugs
Activity increases when combined with beta-lactam antibiotics, aminoglycosides, vancomycin, clindamycin, metronidazole. Sucralfate, bismuth preparations, antacids containing aluminum, magnesium or calcium ions, cimetidine, ranitidine, vitamins with trace elements, iron sulfate, zinc, didanosine (recommended 2 hours before or 4 hours after these preparations) reduce absorption.
Probenecid, azlocillin increase the concentration in the blood. Reduces clearance and increases plasma levels of caffeine, aminophylline and theophylline (the probability of side effects increases).
Strengthens the effect of warfarin and other oral anticoagulants (prolongs bleeding time).
Increases the nephrotoxicity of cyclosporine, the risk of increased CNS excitability and convulsive reactions against the background of NSAIDs.
Drugs alkalinizing urine (citrates, sodium bicarbonate, inhibitors of carbonic anhydrase), reduce solubility (the probability of crystalluria increases).
Infusion solutions of ciprofloxacin ready for use can be combined with infusion solutions: 0.9% sodium chloride, Ringer's solution, Ringer lactate, 5 and 10% dextrose solution, 10% fructose solution, and also a solution containing 5% dextrose with 0.225 or 0.45% sodium chloride. Incompatible with solutions having a pH above 7.
Afenoxin - Precautions
In connection with the threat of the development of adverse reactions from the central nervous system, ciprofloxacin should be used only for vital signs in the pathology of the central nervous system in the past: organic brain damage, epilepsy, lowering the convulsive threshold, severe cerebral artery atherosclerosis (risk of blood supply, stroke), in old age, with severe violations of the kidney and liver (you need to monitor the concentration in the blood plasma).
In patients with allergic reactions to fluoroquinolone derivatives, a history of reaction to ciprofloxacin is possible. During the treatment with Afenoxin, sun and UV irradiation, intensive physical exertion, drinking regime control, urine pH should be avoided.
Cases of crystalluria have been reported, especially in patients with an alkaline urine reaction (pH 7 or higher). To avoid the development of crystalluria, exceeding the recommended daily dose is inadmissible, adequate fluid intake and maintenance of acid urine reaction are also necessary.
When pain occurs in the tendons or the appearance of the first signs of tendovaginitis treatment should be discontinued (individual cases of inflammation or rupture of the tendon during treatment with fluoroquinolones are described).
It can reduce the speed of psychomotor reactions, especially against the background of alcohol, which should be taken into account by patients working with potentially dangerous mechanisms or driving vehicles. If severe diarrhea develops, pseudomembranous colitis should be excluded (in which ciprofloxacin is contraindicated). Simultaneous IV administration of barbiturates requires control of cardiovascular function (heart rate, blood pressure, ECG parameters). Adolescents under 18 years of age are prescribed only in the case of resistance of the pathogen to other chemotherapeutic drugs.
The solution in the form of eye drops is not intended for intraocular injections. When using other ophthalmic agents, the interval between administrations should be at least 5 minutes.
In a cool, dark place.
Shelf life 24 months.
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