Ciprolet A - instructions for use, dose, side effects, contraindications

Active substanceTinidazole + CiprofloxacinTinidazole + Ciprofloxacin

Similar drugsTo uncover

Ciprolet® A

pills inwards

Dr. Reddy's Laboratories Ltd. India

Cyfran® ST

pills inwards

Ranbaxy Laboratories Limited India

Dosage form: & nbspfilm coated tablets

Composition:

Each tablet contains:

Active ingredients: ciprofloxacin hydrochloride monohydrate (equivalent to 500 mg 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, silicon dioxide colloid 3.952 mg, talc 8.952 mg, magnesium stearate 7 mg; composition of the shell:

Ramp-off 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%).

Description:

The tablets, covered with a film shell from white to almost white, are oval in shape, with a separating risk on one side and smooth on the other.

View on cross-section: from white to light yellow.

Pharmacotherapeutic group:antimicrobial agent combined

ATX: & nbsp

J.01.R.A Combinations of antibacterial drugs

J.01.R.A.11 Ciprofloxacin and Tinidazole

Pharmacodynamics:

Combined drug, the effect of which is due to the components that make up its composition.

Tinidazole, an antiprotozoal and antimicrobial agent derived from imidazole, is effective against Trichomonas vaginalis, Entamoeba histolitica, Lamblia, and causative agents of anaerobic infections (Clostridium spp., Bacteroides fragilis, Bacteroides melaninogenicus, Eubacter spp., Fusobacterium spp., Peptococcus spp., And Peptostreptococcus spp). As vysokolipofilnym drug penetrates the trichomonas and anaerobic microorganisms, which recovers nitroreductase inhibits the synthesis and structure damages DNA.

Ciprofloxacin - antimicrobial broad spectrum fluoroquinolone derivative inhibits bacterial DNA gyrase (topoisomerase II and IV, are responsible for the process of the chromosomal DNA supercoiling around nuclear RNA that is necessary for reading the genetic information) gives DNA synthesis, growth and division of bacteria; causes significant morphological changes (including the cell wall and membranes) and the rapid death of the bacterial cell.

Bactericidal effect on gram-negative organisms in a rest period and division (because not only affects DNA gyrase, but also causes lysis of the cell wall) for gram-positive microorganisms - only during division. Low toxicity for macroorganism cells is explained by the absence of DNA-gyrase in them. On the background of admission

, ciprofloxacin does not parallel develop resistance to other antibiotics that do not belong to the group of inhibitors of gyrase, which makes it highly effective against bacteria resistant to aminoglycosides, penicillins, cephalosporins, tetracyclines and many other antibiotics.

Gram-negative aerobic bacteria are sensitive 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).

The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin. Resistance develops extremely slowly, since 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 of its inactivating. For drug resistant: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. It is effective against Treponema pallidum.

Pharmacokinetics:

Suction:

how ciprofloxacin, and tinidazole well absorbed in the gastrointestinal tract after oral administration. Eating slows down absorption, but does not change the maximum concentration (C max) and bioavailability.

Distribution:

Tinidazole. Bioavailability - 100%, connection with plasma proteins - 12%, time to reach the maximum concentration (TCmax) after ingestion -2 hours, Cmax after oral administration 500 mg - 47.7 μg / ml.

Ciprofloxacin. Bioavailability is 50-85%, the volume of distribution is 2-3.5 l / kg, the connection with plasma proteins is 20-40%, Tesha after oral administration is 60-90 min, Cmax after oral administration 500 mg - 0.2 mcg / ml.

Metabolism and excretion:

Tinidazole penetrates into the cerebrospinal fluid at a concentration equal to that in the plasma and is reabsorbed in the renal tubules. The half-life (T1 | 2) is 12-14 hours. Tinidazole is metabolized in the liver with the participation of the cytochrome P450 enzyme system (CYP3A4). About 50% is excreted with bile, 25% - kidneys, 12% - in the form of metabolites. It is reversed in the renal tubules.

Ciprofloxacin well penetrates into fluid media and body tissues (excluding tissue rich in fats, for example, nerve tissue). Concentration in tissues is 2-12 times higher than in plasma.Therapeutic concentrations are achieved in saliva, tonsils, liver, gall bladder, bile, intestine, abdominal and pelvic organs, uterus, seminal fluid, prostate tissue, endometrium, fallopian tubes and ovaries, kidney and urinary organs, pulmonary tissue, bronchial secretion, bone tissue, muscles, synovial fluid and articular cartilage, peritoneal fluid, skin. Spinal fluid penetrates in a small amount, where its concentration, in the absence of inflammation of the meninges, is 6-10% of the serum, and when inflamed - 14-37%. Ciprofloxacin well penetrates also into the eye fluid, bronchial secretion, pleura, peritoneum, lymph, through the placenta. The concentration of ciprofloxacin in blood neutrophils is 2-7 times higher than in blood plasma. The activity decreases slightly at pH values below 6. Metabolised in the liver (15-30%) with the formation of low-activity metabolites (diethylciprofloxacin, sulfosiprofloxacin, oxocycrofloxacin, formyl ciprofloxacin). T1 / 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.Kidney 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 ones.

In ciprofloxacin in chronic renal failure, T1 / 2 increases to 12 hours. In chronic renal failure (CC above 20 ml / min), the percentage of kidney-excreted drug decreases, but cumulation 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:

infection of the respiratory tract (acute and chronic (at the stage of exacerbation) bronchitis, pneumonia, bronchiectatic disease);

infection of the ENT organs (otitis media, sinusitis, frontal sinitis, sinusitis, mastoiditis, tonsillitis, pharyngitis);

Infection of the oral cavity (acute ulcerative gingivitis, periodontitis, periostitis).

infection of the kidneys and urinary tract (cystitis, pyelonephritis);

infections of the pelvic organs and genital organs (prostatitis, adnexitis, salpingitis, oophoritis, endometritis, tubular abscess, pelvioperitonitis);

intra-abdominal infections (infections of the gastrointestinal tract, biliary tract, intraperitoneal abscesses);

infections of the skin and soft tissues (infected ulcers, wounds, burns, abscesses, phlegmon, ulcerative skin lesions with "diabetic foot syndrome," pressure sores);

infection of bones and joints (osteomyelitis, septic arthritis);

postoperative infections.

Contraindications:

Hypersensitivity (including fluoroquinolone or imidazole derivatives), blood diseases (in anamnesis), oppression of bone marrow hematopoiesis, organic diseases of the central nervous system, pregnancy, lactation period, simultaneous reception with tizanidine (risk of pronounced decrease in blood pressure, drowsiness), acute porphyria, children under 18 years.

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulation disorder, mental illness, epilepsy, history of convulsions, marked renal and / or hepatic insufficiency, elderly age.

Pregnancy and lactation:

Because the tinidazole and ciprofloxacin are excreted into breast milk, then for the period of drug treatment it is necessary to stop breastfeeding, since tinidazole may have a mutagenic and carcinogenic effect.

Dosing and Administration:

Inside, 1 hour before meals or 2 hours after meals, with enough water. Do not break, chew or destroy the pill.

The recommended dose is 1 tablet 2 times a day for 5-10 days.

Side effects:

From the digestive system: loss of appetite, dryness of the oral mucosa, "metallic" aftertaste in the mouth, nausea, vomiting, diarrhea, abdominal pain, bloating, cholestatic jaundice (especially in patients with liver disease migrated), hepatitis, gepatonekroz.

From the nervous system: headache, dizziness, fatigue, impaired coordination of movements (including locomotor ataxia), dysarthria, peripheral neuropathy, rarely - seizures, weakness, anxiety, tremor, insomnia, "nightmarish" dream, peripheral paralgeziya (anomaly perception of pain), increased intracranial pressure,confusion, depression, hallucinations, as well as other manifestations of psychotic reactions, migraine, fainting, thrombosis of the cerebral arteries, increased sweating.

From the senses: a violation of taste and smell, visual impairment (diplopia, change in color perception), noise in the ears, hearing loss.

From the cardiovascular system: tachycardia, arrhythmia, lowering blood pressure.

On the part of the hemopoiesis: leukopenia, granulocytopenia, anemia (including hemolytic), thrombocytopenia, leukocytosis, thrombocytosis.

From the urinary system: hematuria, crystalluria (with alkaline urine and diuresis), glomerulonephritis, dysuria, polyuria, urinary retention, albuminuria, decreased renal nitrogen function, interstitial nephritis. Allergic reactions: skin itching, urticaria, skin rash, drug fever, petechiae, angioedema, dyspnea, eosinophilia, photosensitivity, vasculitis, erythema nodosum, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome) .

From the laboratory parameters: hypoprothrombinemia, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, hyperglycemia.

Other: arthralgia, arthritis, tendovaginitis, tendon ruptures, asthenia, myalgia,

superinfection (candidiasis, pseudomembranous colitis), "tides" of blood to the face.

Overdose:

Symptoms: in cases of acute overdose, the symptoms of a reversible lesion of the urinary system will prevail, cramps are possible.

Treatment: induction of vomiting, gastric lavage. Symptomatic, maintenance 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 (less than 10%).

Interaction:

Effects caused by tinidazole. Strengthens the effect of indirect anticoagulants. To reduce the risk of developing bleeding, the dose of Ciprolet ® A is reduced by 50%. Strengthens the action of ethanol (disulfiram-like reactions). Phenobarbital accelerates the metabolism of tinidazole. Ciprolet ® A is not recommended for use with ethionamide.Effects caused by ciprofloxacin. Due to a decrease in the activity of microsomal oxidation in hepatocytes, it increases the concentration and lengthens Tx of theophylline and other xanthines, including caffeine, oral hypoglycemic drugs, indirect anticoagulants, helps to reduce prothrombin

. index. Increases the nephrotoxic effect of cyclosporine, there is an increase in serum creatinine, in such patients monitoring of this indicator is required 2 times a week. Oral administration together with Fe-containing drugs, sucralfate and antacid drugs containing Mg2 +, Ca2 +, A13 +, didanosine leads to a decrease in the absorption of ciprofloxacin. Therefore, the drug Ciprolet ® A is prescribed 1-2 hours before or 4 hours after the administration of the above medicines. Non-steroidal anti-inflammatory drugs (excluding acetylsalicylic acid) increase the risk of seizures. Metoclopramide accelerates absorption, which leads to a decrease in TCaxax. The combined use of uricosuric medicines leads to a delay in excretion (up to 50%) and an increase in the plasma concentration of ciprofloxacin.Increases Cmax 7-fold (4 to 21 times) and AUC (area under the pharmacokinetic curve) of tizanidine, which increases the risk of pronounced reduction in blood pressure and drowsiness.

The drug Ciprolet ® A is compatible with sulfonamides and antibiotics (beta-lactam antibiotics, aminoglycosides, erythromycin, rifampicin, cephalosporins), when combined with which, usually, there is synergy.

Special instructions:

Consider the possibility of cross-allergic reactions. In patients with hypersensitivity to other imidazole derivatives, cross-sensitivity may also develop tinidazole; development of a cross-allergic reaction to ciprofloxacin it is also possible in patients with hypersensitivity to other derivatives of fluoroquinolones.

During treatment, avoid contact with direct sunlight. If photosensitisation reactions occur, discontinue use immediately.

During treatment 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).

To avoid the development of crystalluria, the recommended daily dose should not be exceeded, sufficient fluid intake and maintenance of acid urine reaction is also necessary. Causes dark staining of urine, which has no clinical significance.

Patients with epilepsy, seizures in history, vascular diseases and organic brain damage, in connection with the threat of development of adverse reactions from the central nervous system, the drug should be prescribed only for "vital" indications.

^ If a severe and prolonged diarrhea occurs during or after treatment, the diagnosis of pseudomembranous colitis should be ruled out, which requires immediate discontinuation of the drug and the appointment of appropriate treatment.

If pain occurs in the tendons or when the first signs of tendovaginitis appear, treatment should be stopped.

In the treatment of more than 6 days should monitor the picture of peripheral blood.

Effect on the ability to drive transp. cf. and fur:Impact on the ability to drive vehicles and manage mechanisms. During treatment, one should refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

The tablets covered with a film cover, 500 + 600 mg. For 10 tablets in PVC / aluminum blister. For 1 blister in a pack of cardboard with instructions for use.

Packaging:

The tablets covered with a film cover, 500 + 600 mg. For 10 tablets in PVC / aluminum blister. For 1 blister in a pack of cardboard with instructions for use.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children!

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-002404/10

Date of registration:24.03.2010

The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India

Manufacturer: & nbsp

DR. REDDY`S LABORATORIES, LTD. India

Representation: & nbspDR REDDY'S LABORATORIS LTD. DR REDDY'S LABORATORIS LTD. India

Information update date: & nbsp05.09.2015

Illustrated instructions

Instructions

Ciprolet® A (Ciprolet A)