Trichopolum
Active material: Metronidazol
When ATH: P01AB01
CCF: Antiprotozoal drug with antibacterial activity
ICD-10 codes (testimony): A06, A07.1, A40, A41, A59, i33, J15, J85, J86, K05, K12, K25, K26, K65.0, L01, L02, L03, L08.0, M00, M86, N70, N71, N73.0, Z29.2
When CSF: 07.01.01
Manufacturer: Pharmaceutical Works POLPHARMA S.A. (Poland)
Pharmaceutical form, composition and packaging
Pills white with a yellowish tinge, round, flat, with Valium; yellowing when exposed to light.
| 1 tab. | |
| metronidazol | 250 mg |
Excipients: potato starch, gelatin, starch stream, magnesium stearate.
10 PC. – blisters (2) – packs cardboard.
Pharmacological action
Antiprotozoal drug with antibacterial activity, 5-nitroimidazole derivative. The mechanism of action consists in biochemical restoration of 5-nitro group of metronidazole by intracellular transport proteins of anaerobic microorganisms and protozoa. The recovered 5-nitro group of metronidazole is reacted with the cellular DNA of microorganisms, inhibiting the synthesis of nucleic acids, that leads to the death of microorganisms.
Metronidazol active against Trichomonas vaginalis, Entamoeba histoiytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp., and obligate anaerobes Bacteroides spp . (incl. Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella (Prevotella crossroads, Prevotella mouth, Prevotella disiens); some Gram-positive microorganisms (Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp.). IPC for these strains is 0.125-6.25 ug / ml.
In combination with amoxicillin is active against Helicobacter pylori (amoxicillin suppresses the development of resistance to metronidazole).
Metronidazole has no bactericidal activity against most bacteria and facultative anaerobes, fungi and viruses. In the presence of mixed flora (aerobic and anaerobic) metronidazole exhibits synergism with antibiotics, effective in conventional aerobic.
Metronidazole increases the sensitivity of tumors to radiation, causing sensitization to ethanol (disulfiramopodobnyh action), It stimulates repair processes.
Pharmacokinetics
Absorption
After receiving the drug inside Metronidazole is rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability is not less than 80%. Cmax plasma metronidazole levels achieved after 1-3 no. Food intake and reduces the rate of absorption of Cmax metronidazole serum.
Distribution
Metronidazole binding to plasma proteins is less than 20%.
Metronidazole penetrates in most tissues and body fluids, including light, kidneys, liver, skin, cerebrospinal fluid, brain, bile, spittle, amniotic fluid, oral abscesses, vaginal secretions, semen, breast milk, penetrate the BBB and placental barrier. Vd in adults is about 0.55 l / kg, in newborn – 0.54-0.81 l / kg.
Metabolism
Metabolized in the liver about 30-60% Metronidazole by hydroxylation, oxidation and coupling with glucuronic acid. The major metabolite (2-oksimetronidazol) also has antiprotozoal and antibacterial action.
Deduction
T1/2 in normal liver function averages 8 no (from 6 h to 12 no).
Metronidazole is excreted by the kidneys – 60-80% (20% in unchanged form), through the intestine – 6-15%. Renal clearance of metronidazole 10.2 ml / min.
Pharmacokinetics in special clinical situations
T1/2 in alcoholic liver disease is 18 no (from 10 h to 29 no); in newborn, born at term pregnancy 28-30 weeks – about 75 no; 32-35 weeks – 35 no, 36-40 weeks – 25 h, respectively.
Metronidazole and main metabolites are quickly removed from the blood by hemodialysis (T1/2 is reduced to 2.6 no). In peritoneal dialysis, are displayed in small quantities.
In patients with impaired renal function after repeated dosing possible cumulation of metronidazole in blood serum (therefore, patients with severe renal insufficiency dosing frequency should be reduced).
Elderly patients reduced renal excretion of metronidazole.
Testimony
Treatment of infectious and inflammatory diseases, caused by sensitive microorganisms:
- Trichomoniasis;
- Bacterial vaginosis;
- All forms of amebiasis (intestinal diseases and extra-intestinal localization, including amebic liver abscess, amoebiasis, and asymptomatic amoebiasis);
- Giardiasis;
- Periodontal infections (incl. acute ulcerative gingivitis, acute odontogenic infection);
- Anaerobic bacterial infections (abdominal and gynecological infections of the CNS, bacteraemia, sepsis, endokardit, bone and joint infections, skin and soft tissue, respiratory tract infections), caused by Bacteroides spp., Clostridium spp., Eubacterium spp., Peptococcus spp., Peptostreptococcus spp. and
anaeroʙami, susceptible to metronidazole;
- Treatment of Helicobacter pylori infection in gastric ulcer or duodenal ulcer in conjunction with antibiotic drugs and bismuth, eg, amoksiцillinom.
Prophylactic before surgery on the digestive tract and reproductive organs.
Dosage regimen
The drug is prescribed inside, during or after a meal, The tablets are not liquid.
Trichomoniasis
Adults and children over 10 years appoint 250 mg (1 tab.) 3 times / day, or 500 mg (2 tab.) 2 times / day for 7 days. Women need to appoint additional metronidazole in the form of vaginal suppositories or tablets. If necessary, repeat the treatment. Between courses should take a break in 3-4 weeks of the repeat test laboratory studies.
Alternative therapies is the appointment 750 mg (3 tab.) morning and 1250 mg (5 tab.) or evening 2000 mg (8 tab.)/day one. The duration of treatment is 2 day. Treatment is carried out simultaneously in both sexual partners.
Children aged 3 to 7 years appoint 125 mg (1/2 tab.) 2 times / day; aged 7 to 10 years – 125 mg (1/2 tab.) 3 times / day. Course of treatment 7 days.
Bacterial vaginosis
Adults appoint 500 mg (2 tab.) 2 times / day for 7 days or 2000 mg (8 tab.)/day one. The simultaneous treatment of sexual partners is not required.
Ameʙiaz
At invasive forms of intestinal amebiasis in susceptible patients (incl. when amoebic dysentery) adults and children over 10 years appoint 750 mg (3 tab.) 3 times / day. Children aged 3 to 7 years – by 250 mg (1 tab.) 4 times / day; aged 7 to 10 years – by 375 mg (1.5 tab.) 3 times / day. The course of treatment is usually 5 days.
At intestinal amebiasis have less susceptible patients and chronic amoebic hepatitis adults and children over 10 years appoint 375 mg (1.5 tab.) 3 times / day. Children aged 3 to 7 years – po125 mg (1/2 tab.) 4 times / day; aged 7 to 10 years – 250 mg (1 tab.) 3 times / day. The duration of treatment is 5-10 days.
At amebic liver abscess and extra-intestinal amebiasis other forms adults and children over 10 years appoint 375 mg (1.5 tab.) 3 times / day. Children aged 3 to 7 years – by 125 mg (1/2 tablets) 4 times / day; aged 7 to 10 years – by 250 mg (1 tab.) 3 times / day. Course of treatment 5 days.
At bessimptomnom of carrier clean adults and children over 10 years appoint 375-750 mg (1.5-3 tab.) 3 times / day. Children aged 3 to 7 years – by 125 mg (1/2 tab.) 4 times / day; aged 7 to 10 years – by 250 mg (1 tab.) 3 times / day. The duration of treatment is 5-10 days.
Giardiasis
Adults and children over 10 years appoint 500 mg (2 tab.) 2 times / day for 5 -7 days; or 2000 mg (8 tab.) 1 times / day for 3 days.
Children aged 3 to 7 years – by 250-375 mg (1-1.5 tab.) 1 times / day for 5 days, or 500-750 mg (2-3 tab.) 1 times / day for 3 days. Children aged 7 to 10 years – by 250 mg (1 tab.) 2 times / day for 5 days, or 1000 mg (4 tab.) 1 times / day for 3 days.
Periodontal infections
At acute ulcerative gingivitis adults and children over 10 years appoint 250 mg (1 tab.) 3 times / day. Children aged 3 to 7 years – by 125 mg (1/2 tab.) 2 times / day; aged 7 to 10 years – by 125 mg (1 tab.) 3 times / day. The duration of treatment is 3 day.
At acute odontogenic infections adults and children over 10 years appoint 250 mg (1 tab.) 3 times / day for 3-7 days.
Infection, caused by anaerobic bacteria
Treatment of anaerobic infections usually begin with a / v infusion. Once it becomes possible, Treatment should be continued metronidazole in the form of tablets.
Adults and children over 10 years appoint 500 mg (2 tab.) 3-4 times / day. The duration of treatment should not exceed 7 days.
Children under 10 years in the treatment of anaerobic infections we recommend the use of metronidazole in the form of infusion solutions.
Helicobacter pylori eradication
Assign 500 mg (2 tab.) 3 times / day for 7 days (in a combination therapy, eg, with amoxicillin 2.25 g / day).
Infection prevention, caused by anaerobic bacteria (prior to surgery in the abdomen, in gynecology and obstetrics)
Adults and children over 12 years appoint 250-500 mg (1-2 tab.) 3 times / day for 3-4 days prior to surgery. Through 1-2 day after surgery (when it allowed the ingestion) appoint 250 mg (1 tab.) 3 times / day for 7 days.
In renal failure, severe (CC less than 10 ml / min) daily dose Trichopolum® should be reduced 2 times.
Side effect
From the digestive system: epigastric pain, nausea, vomiting, diarrhea, constipation, kišečnaâ how, decreased appetite, anorexia, taste disturbance, an unpleasant metallic taste in the mouth, dry mouth, glossitis, stomatitis; rarely – abnormal liver function tests, cholestatic hepatitis, jaundice, pancreatitis.
From the central and peripheral nervous system: prolonged use – headache, dizziness, dystaxia, ataxia, perifericheskaya neuropathy, hypererethism, irritability, depression, sleep disturbance, drowsiness, weakness; in some cases – confusion, hallucinations, convulsions; rarely – encephalopathy.
From the urinary system: dizurija, cystitis, polyuria, urinary incontinence, urine staining in red-brown color.
On the part of the reproductive system: excessive development of fungal vaginal flora (incl. vaginal candidiasis), colpodynia.
Allergic reactions: skin rash, itch, hives, erythema multiforme exudative, nasal congestion, fever.
On the part of the musculoskeletal system: mialgii, artralgii.
From the hematopoietic system: leukopenia; rarely – agranulocytosis, neutropenia, thrombocytopenia, pancytopenia.
Other: flattening of the T wave on the ECG; rarely – ototoxicity; empyesis.
Contraindications
- Leukopenia (incl. history);
- Organic CNS (incl. epilepsy);
- Liver failure (in the case of administration of the drug at high doses);
- I trimester of pregnancy;
- Lactation (breast-feeding);
- Children up to age 3 years;
- Hypersensitivity to metronidazole or other nitroimidazole derivatives.
FROM caution should be prescribed to patients with renal and / or hepatic insufficiency, in II-III trimesters of pregnancy.
Pregnancy and lactation
Metronidazole crosses the placental barrier, therefore Trichopolum® contraindicated for use in the I trimester of pregnancy. Use of the drug in the II and III trimester is possible only in cases, when the intended benefits to the mother outweighs the potential risk to the fetus.
Since metronidazole is excreted in breast milk, reaching concentrations therein, close to the plasma concentration, If necessary, use Trichopolum® lactation breastfeeding should be discontinued.
Cautions
Precautions should be prescribed Trichopolum® Patients with severe hepatic insufficiency, tk. as a result of slowing down the metabolism of the concentration of metronidazole and its metabolites in the plasma increases.
Caution is required when appointing Trichopolum® patients with depression of bone marrow hematopoiesis and the central nervous system, as well as elderly patients. The emergence of ataxia, dizziness and any other worsening of neurological status of patients required discontinuation of treatment.
When long-term therapy with metronidazole (more 10 days) should monitor picture peripheral blood and liver function.
At leucopenia the possibility of further treatment depends on the risk of infection.
Avoid the use of metronidazole in patients with porphyria.
In the treatment of Trichomonas vaginitis in women and Trichomonas urethritis in men should refrain from sex life. Be sure to simultaneous treatment of sexual partners. After the treatment of trichomoniasis should conduct pilot tests in three successive cycles before and after menstruation.
After treatment of giardiasis, if symptoms persist, through 3-4 a week is necessary to 3 fecal analysis every few days (some successfully treated patients with lactose intolerance, induced invasion, may persist for several weeks or months, Recalling the symptoms of giardiasis).
Patients should abstain from alcohol during treatment with metronidazole, as well as for, at least, 48 hours after treatment, because of the possibility of reactions disulfiramopodobnyh: abdominal pain, spastic nature, nausea, vomiting, headache, a sudden rush of blood to the face.
During treatment with metronidazole may acquire dark urine or reddish-brown color due to the presence of water-soluble dyes.
Trichopolum® can cause immobilization treponem, which leads to false positive test Nelson.
Use in Pediatrics
In combination with amoxicillin is not recommended Trichopolum® in children and adolescents under the age of 18 years.
Effects on ability to drive vehicles and management mechanisms
While taking the drug should avoid potentially hazardous activities, requiring a high concentration, psychomotor speed reactions, especially driving and maintenance mechanisms.
Overdose
Symptoms: increased side effects, mainly, nausea, vomiting and dizziness; in more severe cases ataxia, paresthesia and cramps. The lethal dose for humans is unknown.
Treatment: the holding of symptomatic and supportive therapy. The specific antidote is absent.
Drug Interactions
Metronidazole increases effect of warfarin and other coumarin anticoagulants (if this combination requires a reduction in dose of both drugs).
Cimetidine inhibits the metabolism of metronidazole, which may lead to an increase in its concentration in the blood plasma and increased risk of adverse reactions.
Co-administration of drugs, stimulating the activity of microsomal liver enzymes (phenobarbital, phenytoin), may accelerate the elimination of metronidazole, which leads to a decrease of its concentration in plasma.
Patients, receiving prolonged treatment with high doses of lithium, while taking metronidazole may increase the concentration of lithium in the blood plasma and the development of symptoms of intoxication.
It is not recommended to combine Metronidazole with nondepolarizing muscle relaxants (vekuroniya bromide).
In the combined receiving cyclosporine and metronidazole may be observed increase in the concentration of cyclosporine in the blood plasma.
Metronidazole reduces the clearance of fluorouracil, which may cause an increase in toxicity of the latter.
With simultaneous use of metronidazole may increase plasma concentrations of busulfan.
Sulfonamide enhance antimicrobial effects of metronidazole.
Similarly, disulfiram metronidazole is intolerant of ethanol. Concomitant use Trichopolum® disulfiram can lead to a variety of neurological symptoms (the interval between the application of these medications must be at least 2 weeks).
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored out of reach of children, dry, dark place at a temperature no higher than 25 ° C. Shelf life – 5 years.
