thyme creeping herb extract, Ciprofloxacin | Cyprolet A tablets are coated. 600 mg + 500 mg 10 pcs.

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SKU
BID465421
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Latin name

Ciprolet A
Latin name

Ciprolet A

Release form

Tablets.

Packaging

In a blister pack of 10 tablets.

In a cardboard box 1 blister.

Pharmacological action

Pharmacodynamics

Combined drug whose action is due to the components that make up its composition.

tinidazole an antiprotozoal and antimicrobial agent, an imidazole derivative, is effective against Trichomonas vaginalis, Entamoeba histolitica, Lamblia, as well as causative agents of anaerobic infections (Clostridium spp., Bacteroides fragilis, Bacteroides melaninogenicus, Eubacter spp., peppococococcus pococcus. )

Being a highly lipophilic drug, it penetrates into Trichomonas and anaerobic microorganisms, where it is restored by nitroreductase, inhibits synthesis and damages the structure of DNA.

ciprofloxacin a broad-spectrum antimicrobial agent, a derivative of fluoroquinolone, inhibits 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 wall and membranes) and the rapid death of a bacterial cell.

Acts bactericidal on gram-negative organisms during dormancy and division (since it affects not only DNA gyrase, but also causes cell wall lysis), gram-positive microorganisms only during the division period.

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 rappenissa marciensiens, ., 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 left, and on the other bacterial cells have no inactivating enzymes.

Resistant to the drug: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. He is effective against Treponema pallidum.

Pharmacokinetics

Absorption:

Both ciprofloxacin and tinidazole are well absorbed in the gastrointestinal tract after oral administration.

Food intake slows down absorption, but does not change the value of the maximum concentration (Cmax) and bioavailability.

Distribution: Tinidazole. Bioavailability 100%, communication with plasma proteins 12%, time to reach maximum concentration (TCmax) after oral administration 2 hours, Cmax after oral administration of 500 mg 47.7 mcg / ml.

ciprofloxacin. Bioavailability 50-85%, distribution volume 2-3.5 l / kg, communication with plasma proteins 20-40%, TCmax after oral administration 60-90 minutes Cmax after oral administration of 500 mg 0.2 mcg / ml.

Metabolism and excretion: Tinidazole penetrates into the cerebrospinal fluid at a concentration equal to that in plasma, and undergoes reverse absorption in the renal tubules. The half-life (T1 / 2) 12-14 hours

Tinidazole is metabolized in the liver by the cytochrome P450 enzyme system (CYP3A4).

About 50% is excreted with bile, 25% kidneys, 12% in the form of metabolites.

Reverse absorption in the renal tubules.

Ciprofloxacin penetrates well into body fluids and tissues (excluding tissue rich in fats, such as nerve tissue). The concentration in tissues is 2–12 times higher than in plasma.

Therapeutic concentrations are achieved in saliva, tonsils, liver, gall bladder, 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.

It enters the cerebrospinal fluid in a small amount, where its concentration in the absence of inflammation of the meninges is 6-10% of serum, and in case of inflammation 14-37%.

Ciprofloxacin also penetrates well 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.

Activity decreases slightly at pH values ​​less than 6.

Metabolized in the liver (15-30%) with the formation of inactive metabolites (diethylcycrofloxacin, sulfociprofloxacin, oxociprofloxacin, formylciprofloxacin). T1 / 2 about 4 hours.

It is excreted mainly by the kidneys by tubular filtration and tubular secretion unchanged (40-50%) and as 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 (CC) above 22 ml / min) do not differ from those in healthy patients.

In ciprofloxacin with chronic renal failure, T1 / 2 increases to 12 hours.

In chronic renal failure (CC above 20 ml / min), the percentage of drug excreted through the kidneys 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: - respiratory tract infections (acute and chronic (in the acute stage) bronchitis, pneumonia, bronchiectasis - srd) organs (otitis media, sinusitis, frontal sinusitis, sinusitis, mastoiditis, tonsillitis, pharyngitis)

- infections of the oral cavity (acute ulcerative gingivitis, periodontitis, periostitis)

- kidney and urinary infections of the canal tracts (cystitis, pyelonephritis)

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

- intraabdominal 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, bedsores)

- infections of bones and joints (osteomyelitis, septic arthritis)

- postoperative infections.

Contraindications

Hypersensitivity (including to derivatives of fluoroquinolone or imidazole)

blood diseases (history)

bone marrow hemopoiesis suppression

organic CNS diseases

short term pregnancy (low risk of pregnancy)

acute porphyria

children under 18 years of age.

Precautions: severe vascular atherosclerosis derivatives of fluoroquinolone or imidazole)

blood diseases (history)

bone marrow hematopoiesis suppression

organic diseases of the central nervous system

pregnancy

lactation period

concomitant use with tizanidine (risk of a pronounced decrease in blood pressure, drowsiness, 18 years old, drowsiness).

Precautions: severe vascular atherosclerosis derivatives of fluoroquinolone or imidazole)

blood diseases (history)

bone marrow hematopoiesis suppression

organic diseases of the central nervous system

pregnancy

lactation period

concomitant use with tizanidine (risk of a pronounced decrease in blood pressure, drowsiness, 18 years old, drowsiness).

Precautions: severe vascular atherosclerosisbrain

cerebrovascular accident

mental illness

epilepsy seizures history

severe renal and / or liver failure

elderly.

Use during pregnancy and lactation

Since tinidazole and ciprofloxacin are excreted in breast milk,

should be discontinued during the treatment period with the drug,

because tinidazole can have a mutagenic and carcinogenic effect.

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

microcrystalline 20.33 mg,

sodium carboxymethyl starch (type A) 5 mg,

silicon dioxide 93.5 mg palladium stearate 7 mg

shell composition:

Opadry 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%).

Dosage and administration

Inside, 1 hour before meals or 2 hours after meals, with plenty of water.

Do not crush, chew, or break the tablet.

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

Side effects

Side effects are presented in accordance with the classification of side effects of the World Health Organization. Their frequency is defined 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 (<1/10000 appointments). Undesirable reactions, which were recorded only during post-marketing observations, the frequency of which was not evaluated, are indicated as “frequency unknown”.

Ciprofloxacin

From the central and peripheral nervous system: infrequently - psychomotor hyperactivity / agitation, sleep disturbances, dizziness, headache rarely - tremor, anxiety, “nightmare” dreams, confusion, disorientation, depression (which can lead to self-harming behavior, such as suicidal behavior / thoughts, as well as suicide attempt or successful suicide), hallucinations, paresthesia and dysesthesia, hypesthesia, convulsions (including epilepsy attacks), vertigo very rarely - increased intracranial pressure (including benign intracranial hyper tension), psychotic reactions (which can lead to self-damaging behavior, such as suicidal behavior / thoughts, as well as suicide attempt or successful suicide), migraine, impaired coordination of movements, impaired gait, hyperesthesia, frequency is unknown - peripheral neuropathy and polyneuropathy.

On the part of the sensory organs:

rarely - impaired vision, tinnitus, hearing loss is very rare - impaired smell, hearing impairment, impaired color perception.

On the part of the cardiovascular system: rarely - tachycardia, vasodilation, lowering blood pressure, a sensation of a "rush" of blood to the face is very rare - vasculitis frequency is unknown - lengthening the QT interval, ventricular arrhythmias (including pirouette type).

From the digestive system: often - nausea, diarrhea infrequently - vomiting, abdominal pain, dyspepsia, flatulence, decreased appetite and the amount of food consumed rarely - impaired liver function, cholestatic jaundice (especially in patients with past 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 kidneys and urinary tract: infrequently - impaired renal function rarely - renal failure, hematuria, crystalluria, tubulointerstitial nephritis.

From the respiratory system, chest and mediastinal organs: rarely - respiratory failure (including bronchospasm).

From the side of musculoskeletal and connective tissue: infrequently - arthralgia rarely - increased muscle tone, muscle cramps, arthritis, tendovaginitis, myalgia is very rare - tendon ruptures (mainly Achilles), muscle weakness, exacerbation of symptoms of myasthenia gravis.

On the part of the immune system:

infrequently - skin itching, 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: infrequently - pain syndrome of non-specific etiology, general malaise, fever, superinfection (candidiasis) rarely - edema, hyperhidrosis, pseudomembranous colitis (in very rare cases with possible fatal outcome), photosensitivity, very rarely blistering - petechiae, erythema multiforme forms, erythema nodosum, Stevens-Johnson syndrome (malignant exudative erythema), including potentially life-threatening, Lyell's syndrome (toxic epidermal necrolysis) frequency is 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.

From the nervous system: fatigue, ataxia, cramps, dizziness, headache, hypesthesia, paresthesia, peripheral neuropathy, sensory disturbance, vertigo.

Allergic reactions: hypersensitivity reactions in the form of skin rash, itching, urticaria, angioedema.

Other: “flushes” of blood to the skin of the face, fever, transient leukopenia, dark urine.

Drug Interaction

Effects caused by tinidazole

Cyprolet A enhances the effect of indirect anticoagulants.

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

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

Ciprolet A is not recommended at the same time as ethionamide.

Effects caused by ciprofloxacin

Due to the decreased activity of microsomal oxidation processes in hepatocytes, it increases the concentration and lengthens T1 / 2 of theophylline and other xanthines, incl. caffeine, oral hypoglycemic drugs, indirect anticoagulants, contributes to a decrease in the prothrombin index.

Increases the nephrotoxic effect of cyclosporine, an increase in serum creatinine is noted, such patients need to be monitored twice a week.

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

Therefore Ciprolet A should be given 1-2 hours before or 4 hours after taking these medicines.

Concomitant use with NSAIDs (excluding acetylsalicylic acid) increases the risk of convulsions.

Metoclopramide accelerates the absorption of ciprofloxacin, leading to a decrease in Tmax.

Co-administration of uricosuric drugs leads to a slowing of elimination (up to 50%) and an increase in the plasma concentration of ciprofloxacin.

Ciprofloxacin increases Cmax 7-fold (4 to 21-fold) and tizanidine AUC, which increases the risk of marked BP and drowsiness.

Ciprolet A is compatible with sulfanilamides and antibiotics (beta-lactam antibiotics, aminoglycosides, erythromycin, rifampicin, cephalosporins), with which synergism is commonly observed.



overdose Symptoms:

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

Treatment:

vomiting induction, gastric lavage.

Symptomatic, supportive therapy (including adequate hydration of the body).

There is no specific antidote.

With hemo- or peritoneal dialysis, tinidazole can be completely eliminated and ciprofloxacin insignificantly (less than 10%).

Storage conditions

At a temperature not higher than 25 C.

Keep out of the reach of children!

Expiration

3 years.

Dosage form

Dosage form

tablets

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