Ciprolet A, pills 600mg + 500mg 10pcs

Composition

Each tablet contains: Active ingredients: ciprofloxacin hydrochloride monohydrate (equivalent to 500 mg of ciprofloxacin) – 582.285 mg and tinidazole-600,000 mg; Excipients: corn starch 35 mg, croscarmellose sodium 27.476 mg, microcrystalline cellulose 20.33 mg, sodium carboxymethyl starch (type A) 5 mg, colloidal silicon dioxide 3.952 mg, talc 8.952 mg, magnesium stearate 7 mg; shell composition: Opadray white 40 mg (hypromellose 55.46%, talc 19.84%, titanium dioxide 11.93%, macrogol-6000 11.09%, polysorbate-80 0.84%, sorbic acid 0.84%).

Pharmacological action

Pharmacodynamiccombinated drug, the action of which is due to the components that make up its composition. Tinidazole is an antiprotozoal and antimicrobial agent derived from imidazole, effective against Trichomonas vaginalis, Entamoeba histolitica, Lamblia, as well as pathogens of anaerobic infections (Clostridium spp., Bacteroides fragilis, Bacteroides melaninogenicus, Eubacter spp., Fusobacterium spp., Peptococcus spp. and Peptostreptococcus spp. ). Being a highly lipophilic drug, it penetrates into trichomonads and anaerobic microorganisms, where it is restored by nitroreductase, inhibits synthesis and damages the structure of DNA. Ciprofloxacin, a broad-spectrum antimicrobial agent derived from fluoroquinolone, suppresses bacterial DNA gyrase (topoisomerases II and IV, responsible for the supercoiling of chromosomal DNA around nuclear RNA, which is necessary for reading genetic information), disrupts DNA synthesis, bacterial growth and division; causes pronounced morphological changes (including cell walls and membranes) and rapid bacterial cell death. It acts bactericidal on gram-negative organisms during dormancy and division (since it affects not only DNA gyrase, but also causes lysis of the cell wall), on gram-positive microorganisms-only during division. Low toxicity to macroorganism cells is explained by the absence of DNA gyrase in them. While taking ciprofloxacin, there is no parallel development of resistance to other antibiotics that do not belong to the group of gyrase inhibitors, which makes it highly effective against bacteria resistant to aminoglycosides, penicillins, cephalosporins, tetracyclines and many other antibiotics. Gram − negative aerobic bacteria are susceptible to ciprofloxacin: Enterobacteria (Escherichia coli, Salmonella spp., Shigella spp., Citrobacter spp., Klebsiella spp., Enterobacter spp., Proteus mirabilis, Proteus vulgaris, Serratia marcescens, Hafnia alvei, Edwardsiella tarda, Providencia spp., Morganella morganii, Vibrio spp., Yersinia spp. ), other gram-negative bacteria (Haemophilus spp., Pseudomonas aeruginosa, Moraxella catarrhalis, Aeromonas spp., Pasteurella multocida, Plesiomonas shigelloides, Campylobacter jejuni, Neisseria spp. ), some intracellular pathogens-Legionella pneumophila, Brucella spp., Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii; gram-positive aerobic bacteria: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae). Most methicillin-resistant staphylococci are also resistant to ciprofloxacin. Resistance develops extremely slowly, because, on the one hand, after the action of ciprofloxacin, there are practically no persistent microorganisms, and on the other hand, bacterial cells do not have enzymes that inactivate it. Resistant to the drug: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. He is effective against Treponema pallidum. Pharmacokineticsabsorption:  Both ciprofloxacin and tinidazole are well absorbed in the gastrointestinal tract after oral use. Food intake slows down absorption, but does not change the maximum concentration (Cmax) and bioavailability. Distribution: Tinidazole. Bioavailability-100%, plasma protein binding-12%, time to reach the maximum concentration (TCmax) after oral use-2 hours, Cmax after oral use of 500 mg-47.7 mcg / ml. Ciprofloxacin. Bioavailability − 50-85%, volume of distribution-2-3.5 l / kg, plasma protein binding-20-40%, TCmax after oral use-60-90 min, Cmax after oral use of 500 mg-0.2 mcg / ml. Metabolism and elimination: Tinidazole penetrates the cerebrospinal fluid in a concentration equal to that in plasma, and undergoes reabsorption in the renal tubules. The elimination half-life (T1 / 2) is 12-14 hours. Tinidazole is metabolized in the liver by the cytochrome P450 (CYP3A4) enzyme system. About 50% is excreted in the bile,25% in the kidneys, and 12% in the form of metabolites. It is reabsorbed in the renal tubules. Ciprofloxacin penetrates well into fluids and body tissues (excluding fat-rich tissue, such as nerve tissue). The concentration in tissues is 2-12 times higher than in plasma. Therapeutic concentrations are achieved in saliva, tonsils, liver, gallbladder, bile, intestines, abdominal and pelvic organs, uterus, seminal fluid, prostate tissue, endometrium, fallopian tubes and ovaries, kidneys and urinary organs, lung tissue, bronchial secretions, bone tissue, muscles, synovial fluid and articular cartilage, peritoneal fluid, skin. In the cerebrospinal fluid penetrates in a small amount, where its concentration in the absence of inflammation of the meninges is 6-10% of the serum, and with inflamed-14-37%. Ciprofloxacin also penetrates well into the eye fluid, bronchial secretions, pleura, peritoneum, lymph, and through the placenta. The concentration of ciprofloxacin in blood neutrophils is 2-7 times higher than in blood plasma. Its activity decreases slightly at pH values less than 6. It is metabolized in the liver (15-30%) with the formation of low-level metabolites (diethylcyprofloxacin, sulfocyprofloxacin, oxocyprofloxacin, formylcyprofloxacin). T 1/2 − about 4 hours. It is mainly excreted by the kidneys by tubular filtration and tubular secretion in unchanged form (40-50%) and in the form of metabolites (15%), the rest − through the gastrointestinal tract. A small amount is excreted in breast milk. Renal clearance − 3-5 ml/min/kg; total clearance − 8-10 ml/min/kg. In special cases: The pharmacokinetic parameters of tinidazole in patients with chronic renal failure – CRF (creatinine clearance above 22 ml / min) do not differ from those in healthy subjects. Ciprofloxacin in chronic renal failure increases T 1/2 to 12 hours. With CRF (creatinine clearance above 20 ml / min), the percentage of the drug excreted through the kidneys decreases, but accumulation in the body does not occur due to a compensatory increase in the metabolism of the drug and its excretion through the gastrointestinal tract.

Indications

Mixed bacterial infections caused by sensitive gram-positive and gram-negative microorganisms, in association with anaerobic microorganisms and / or protozoa:

• respiratory tract infections (acute and chronic (in the acute stage) bronchitis, pneumonia, bronchiectasis);
• infections of ENT organs (otitis media, sinusitis, frontal sinusitis, sinusitis, mastoiditis, tonsillitis, pharyngitis);
• mouth infections (acute ulcerative gingivitis, periodontitis, periostitis);
• and infections of the kidneys and urinary tract (cystitis, pyelonephritis);
• infection of the pelvic organs and genital organs (prostatitis, adnexitis, salpingitis, oophoritis, endometritis, tubular abscess, pelvioperitonit);
• intra-abdominal infections (infections of the gastrointestinal tract, biliary tract, intra-abdominal abscesses);
• infections of skin and soft tissue (infected ulcers, wounds, burns, abscesses, cellulitis, ulcerated skin lesions in the diabetic foot, pressure ulcers);
• infections of bones and joints (osteomyelitis, septic arthritis);
• postoperative infection.

Use during pregnancy and lactation

Since tinidazole and ciprofloxacin are excreted in breast milk,

breast-feeding should be discontinued for the duration of treatment with the drug,

since tinidazole can have a mutagenic and carcinogenic effect.

Contraindications

• Hypersensitivity (including to derivatives of fluoroquinolone or imidazole);
• blood diseases (in the anamnesis);
• suppression of bone marrow hematopoiesis;
• organic diseases of the central nervous system;
• pregnancy;
• lactation;
• simultaneous use with tizanidine (risk of a pronounced decrease in blood pressure, drowsiness);
• acute porphyria;
• children under 18 years of age.

With caution: severe atherosclerosis of the cerebral vessels;

impaired cerebral circulation;

mental illnesses; epilepsy; convulsions in the anamnesis;

severe renal and/or liver failure;

elderly age.

Side effects

Side effects are presented according to the World Health Organization classification of Side Effects.Their frequency is determined as follows: very often (>1/10 appointments), often (1/10-1/100 appointments); infrequently (1/100-1/1000 appointments); rarely (1/1000-1/10000 appointments); very rarely (>Adverse reactions that were recorded only in the course of post-marketing observations, the frequency of which was not estimated, are indicated- “frequency unknown”. Ciprofloxacin from the central and peripheral nervous system: infrequently – psychomotor hyperactivity / agitation, sleep disorders, dizziness, headache; rarely – tremor, anxiety, “nightmarish” dreams, confusion, disorientation, depression (which can lead to self – harming behavior, such as suicidal actions / thoughts, as well as suicide attempt or successful suicide), hallucinations, paresthesia and dysesthesia, hypesthesia, convulsions (including seizures epilepsy), vertigo; very rarely – increased intracranial pressure (including benign intracranial hypertension), psychotic reactions (which can lead to self-injurious behavior, such as suicidal actions / thoughts, as well as suicide attempt or successful suicide), migraines, impaired coordination of movements, gait disorders, hyperesthesia; frequency unknown-peripheral neuropathy and polyneuropathy. From the side of the senses: rarely-visual impairment, tinnitus, hearing loss; very rarely-olfactory impairment, hearing impairment, color perception impairment. From the cardiovascular system: rarely-tachycardia, vasodilation, decreased blood pressure, a feeling of “rush” of blood to the face; very rarely-vasculitis; frequency unknown-prolongation of the QT interval, ventricular arrhythmias (including the “pirouette” type). From the digestive system:often – nausea, diarrhea; infrequently-vomiting, abdominal pain, dyspepsia, flatulence, decreased appetite and the amount of food consumed; rarely-liver function disorders, cholestatic jaundice (especially in patients with previous liver diseases), hepatitis; very rarely – pancreatitis, hepatonecrosis. From the hematopoietic system:infrequently – eosinophilia; rarely-leukopenia, leukocytosis, thrombocytopenia, thrombocytosis, anemia, neutropenia; very rarely-hemolytic anemia, agranulocytosis, pancytopenia (life-threatening), bone marrow depression (life-threatening). From the side of the kidneys and urinary tract: infrequently-impaired renal function; rarely-renal failure, hematuria, crystalluria, tubulointerstitial nephritis. Respiratory, thoracic and mediastinal disorders: rarely – respiratory disorders (including bronchospasm). Musculoskeletal and connective tissue disorders:infrequently-arthralgia; rarely-increased muscle tone, muscle cramps, arthritis, tendovaginitis, myalgia; very rarely-tendon tears (mainly Achilles), muscle weakness, exacerbation of myasthenia gravis symptoms. From the immune system:infrequently-pruritus, rash, urticaria; rarely-allergic reactions, allergic edema / angioedema; very rarely-anaphylactic reactions, anaphylactic shock (life-threatening), serum sickness. Changes in laboratory parameters: infrequently-increased activity of “hepatic” transaminases and alkaline phosphatase, increased bilirubin concentration; rarely-changes in prothrombin content, increased amylase activity, hyperglycemia, hypoglycemia. Other services: infrequently – pain syndrome of non – specific etiology, general malaise, fever, superinfections (candidiasis); rarely – edema, hyperhidrosis, pseudomembranous colitis (in very rare cases with a possible fatal outcome), photosensitization, blistering; very rarely-petechiae, erythema multiforme, erythema nodosum, Stevens – Johnson syndrome (malignant exudative erythema), including potentially life-threatening Lyell’s syndrome (toxic epidermal necrolysis); frequency unknown-acute generalized pustular exanthema, increased international normalized ratio (in patients receiving vitamin K antagonists). Tinidazole from the digestive system:abdominal pain, anorexia, diarrhea, hairy tongue, glossitis, nausea, stomatitis, vomiting, metallic taste. Nervous system disorders:fatigue, ataxia, seizures, dizziness, headache, hypesthesia, paresthesia, peripheral neuropathy, sensory impairment, vertigo. Allergic reactions: hypersensitivity reactions in the form of skin rash, pruritus, urticaria, angioedema. Other services:”flushes” of blood to the skin of the face, fever, transient leukopenia, dark urine.

Interaction

Tinidazole-related effects.

Enhances the effect of indirect anticoagulants.

To reduce the risk of bleeding, the dose of Ciprolet A is reduced by 50%.

Enhances the effect of ethanol (disulfiram-like reactions). Phenobarbital accelerates the metabolism of tinidazole.

Ciprolet A is not recommended for use with ethionamide.

Ciprofloxacin-related effects.

Due to a decrease in the activity of microsomal oxidation processes in hepatocytes, it increases the concentration and lengthens T_1/2 of theophylline and other xanthines, including caffeine, oral hypoglycemic drugs, indirect anticoagulants, and helps to reduce the prothrombin index. Increases the nephrotoxic effect of cyclosporine, there is an increase in serum creatinine, in such patients it is necessary to monitor this indicator 2 times a week.

Oral use together with iron-containing drugs, sucralfate and antacid drugs containing Mg2+, Ca2+, Al3+, didanosine leads to a decrease in the absorption of ciprofloxacin.

Therefore, the drug Ciprolet is prescribed 1-2 hours before or 4 hours after taking the above drugs. NSAIDs (excluding acetylsalicylic acid) increase the risk of seizures.

Metoclopramide accelerates absorption, which leads to a decreasein tmax. Co-use of uricosuric drugs leads to a slowdown in excretion (up to 50%) and an increase in the plasma concentration of ciprofloxacin.

Increases the_cmax by 7 times (from 4 to 21 times) and the AUC of tizanidine, which increases the risk of a pronounced decrease in blood pressure and drowsiness.

Ciprolet A is compatible with sulfonamides and antibiotics (beta-lactam antibiotics, aminoglycosides, erythromycin, rifampicin, cephalosporins), with which synergy is usually observed.

How to take, course of use and dosage

Inside,1 hour before a meal or 2 hours after a meal, with a sufficient amount of water.

Do not break, chew or destroy the tablet. The recommended dose is 1 tablet 2 times a day for 5-10 days.

Overdose

Symptoms:

in cases of acute overdose, symptoms of reversible damage to the urinary system will prevail, and convulsions may occur.

Treatment:

induction of vomiting, gastric lavage. Symptomatic, supportive therapy (including adequate hydration of the body).

There is no specific antidote.

With the help of hemo – or peritoneal dialysis, tinidazole can be completely eliminated from the body, and ciprofloxacin — slightly (

Special instructions

The possibility of cross-allergic reactions should be considered. Patients with hypersensitivity to other imidazole derivatives may also develop cross-sensitivity to tinidazole; patients with hypersensitivity to other fluoroquinolone derivatives may also develop a cross-allergic reaction to ciprofloxacin. Sometimes, after the first dose of ciprofloxacin, allergic reactions may develop, which should be immediately reported to the attending physician. During treatment, it is recommended to avoid contact with direct sunlight. If photosensitization reactions occur, the drug should be discontinued immediately. During the treatment period and at least 3 days after discontinuation of the drug, it is not recommended to take ethanol (the risk of developing disulfiram-like reactions against the background of tinidazole, which is part of the drug). Paroxysmal seizures and peripheral neuropathy, characterized mainly by numbness or paresthesia of the extremities, have been reported in patients treated with tynidazole. If any neurological symptoms occur, tinidazole therapy should be discontinued immediately and a doctor should be consulted. To avoid the development of crystalluria, you should not exceed the recommended daily dose, as well as sufficient fluid intake and maintaining an acidic urine reaction. Causes dark staining of the urine, which is not clinically relevant. Cases of epileptic status have been reported with ciprofloxacin. Ciprofloxacin, like other fluoroquinolones, can provoke seizures and reduce the threshold of convulsive readiness, if seizures occur, the drug should be discontinued. Patients with epilepsy, convulsions in the anamnesis, vascular diseases and organic brain damage due to the threat of adverse reactions from the central nervous system, the drug should be prescribed only for “vital” indications. Mental reactions may occur even after the first use of fluoroquinolones, including ciprofloxacin. In rare cases, depression or psychotic reactions may progress to suicidal thoughts and self-harming behavior, such as suicide attempts, including committed ones. if the patient develops one of these reactions, stop taking the drug and inform your doctor. If severe and prolonged diarrhea occurs during or after treatment, the diagnosis of pseudomembranous colitis should be excluded, which requires immediate discontinuation of the drug and appropriate treatment. The use of drugs that inhibit intestinal motility is contraindicated.When using ciprofloxacin, cases of tendinitis and tendon rupture (mainly Achilles tendon), sometimes bilateral, may occur within the first 48 hours after the start of therapy. Inflammation and tendon rupture may occur even several months after discontinuation of ciprofloxacin treatment. There is an increased risk of developing tendinopathy in elderly patients and in patients with tendon diseases who are simultaneously treated with glucocorticosteroids. If there is pain in the tendons or if the first signs of tendovaginitis appear, treatment should be discontinued, and a doctor should be consulted. When treating for more than 6 days, the peripheral blood picture should be monitored. Given that women have a longer average QT interval than men, they are more sensitive to drugs that cause prolongation of the QT interval; ciprofloxacin should be used with caution in combination with drugs that prolong the QT interval (for example, antiarrhythmic drugs of classes IA and III, tricyclic antidepressants, macrolides, neuroleptics), in patients with an increased risk of prolongation of the QT interval or the development of arrhythmia of the “pirouette” type (for example, congenital QT prolongation syndrome, heart diseases (heart failure, myocardial infarction, bradycardia), electrolyte imbalance (for example, hypokalemia, hypomagnesemia)). Liver necrosis and life-threatening liver failure have been reported with ciprofloxacin. If you have symptoms of liver disease, such as anorexia, jaundice, dark urine, itching, abdominal pain, the use of ciprofloxacin should be discontinued. Ciprofloxacin should be used with caution in patients with severe myasthenia gravis, as symptoms may worsen. Cases of sensory or sensorimotor polyneuropathy, hypesthesia, or weakness have been reported with ciprofloxacin. If symptoms such as pain, burning, tingling, numbness, or weakness occur, patients should inform their doctor before continuing to use the drug. Caution should be exercised when ciprofloxacin is co-administered with drugs that are metabolized by CYP450 1A2 isoenzymes, such as ropinirole, olanzapine. During treatment, you should refrain from engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Film-coated tablets

Storage conditions

At a temperature not exceeding 25 C. Keep out of reach of children!

Shelf

life is 3 years.

Active ingredient

Tinidazole, Ciprofloxacin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Biliary Tract Infections, Sinusitis, Adnexitis, Otitis Media, Pharyngitis, Tonsillitis, Osteomyelitis, Periodontitis, Pneumonia, Bedsores, Intestinal Infections, Purulent Wounds, Urinary Tract Infections, Bronchitis, Skin Infections, Prostatitis