Triconex Forte

Triconex Forte

metronidazole

Manufacturer:

Multicare

Distributor:

Zuellig
Full Prescribing Info
Contents
Metronidazole.
Action
Amoebicide/Antiprotozoal.
Pharmacology: Metronidazole, a synthetic 5-nitroimidazole, has an antibiotic action that is based on the modification of the genetic substance of microorganisms. Its spectrum contains anaerobic bacteria (Bacteroides fragilis, clostridia, fusobacteria, peptococci, peptostreptococci), certain other bacteria (eg, Gardnerella vaginalis) and protozoas (Giardia lamblia, Entamoeba hystolytica, Trichomonas vaginalis). Bactericidal tissue concentrations are achieved in the central nervous system, in the liver and the bile ducts, in the bones, in vaginal secretions and in the pelvic organs.
Pharmacokinetics: Absorption: Metronidazole is rapidly absorbed following oral administration, at least 80% in <1 hr. The peak serum concentrations achieved following oral administration are similar to those obtained following IV administration of equivalent doses. The oral bioavailability is 100% and is not modified by simultaneous ingestion of food.
Distribution: Approximately 1 hr after a single-dose administration of 500 mg of metronidazole, the peak serum concentration is on average 10 mcg/mL. The plasma t½ is between 8-10 hrs. The protein binding is low, <20%. The volume of distribution is large, on average 40 L (ie, 0.66 L/kg). Diffusion of the drug is rapid and extensive with concentrations close to serum levels in the lungs, kidneys, liver, skin, bile, cerebrospinal fluid, saliva, seminal fluid and vaginal secretion. Metronidazole crosses the placental barrier and is excreted in breast milk.
Metabolism: Metronidazole is primarily metabolized in the liver. Oxidation yields 2 main metabolites: The alcoholic metabolites, the primary metabolite, with a bactericidal activity against anaerobic bacteria equal to approximately 30% that of metronidazole and with an elimination t½ of 11 hrs. The acid metabolite in small amounts and with bactericidal activity approximately equal to 5% that of metronidazole.
Elimination: High liver and biliary concentration. Low concentration in the colon. Little fecal elimination. Excretion is primarily urinary, shown by the fact that the metronidazole and its oxidation metabolites excreted in the urine account for approximately 35-85% of the administered dose.
Indications/Uses
Metronidazole is the drug of choice for the symptomatic intestinal and extraintestinal amoebiasis as well as infections with Trichomonas vaginalis and Giardia lamblia. Metronidazole is also indicated in the treatment of trichomoniasis in both male and female patients when the presence of trichomonas has been demonstrated by wet smear or culture and for sexual partners of those patients who have recurrence of infections. It is quickly and reliably effective against Gardnerella vaginosis.
Curative treatment of medico-surgical infections due to susceptible anaerobic pathogens.
Prophylaxis against infections caused by susceptible anaerobic pathogens in high-risk surgical contents.
Conversion from prophylactic or curative injectable treatment of infections due to susceptible anaerobic pathogens. Anaerobic infections (eg, cerebral abscesses, intra-abdominal abscesses, gynecological infections of the pelvic organs, soft tissue infections, osteomyelitis) are well documented indications. Metronidazole also has an advantageous effect on parodontopathy. Anaerobic infections of the lower respiratory tract respond better to penicillin or clindamycin. Metronidazole is combined with a 2nd antibiotic for the treatment of mixed infections with aerobic germs and for preoperative infection prophylaxis (colorectal and gynecological interventions). It can be an alternative to vancomycin in the treatment of mucous colitis. Imidazoles are also used against Helicobacter pylori in which case one has to expect resistant germs. Metronidazole is sometimes more efficient than sulfasalazine for Crohn's disease, however, the tolerance of long-term administration is not established.
Applied topically, metronidazole has proven effective against rosacea, acne and foul-smelling skin lesions (tumours, decubitus ulcer).
Dosage/Direction for Use
Adults: Amoebiasis, Balantidiasis and Blastocystis hominis Infections: 3-4 tablets in divided doses for 5-7 days or 2 g daily as a single dose for 3 days.
Giardiasis: 1 tablet twice a day for 5 days.
Children: 40-50 mg/kg body weight daily for 5 days.
Trichomoniasis: 4 tablets once daily or 1 tablet twice daily for 7 days.
Bacterial Vaginosis: 4 tablets once daily or 1 tablet twice daily for 5-7 days.
Anaerobic Bacterial Infections: 1 tablet thrice a day for 5 days or longer when needed.
Children: 20-30 mg/kg/day.
Prevention of Postoperative Anaerobic Bacterial Infections: 1 tablet thrice a day for 3 days preoperative, followed postoperative by 1 tablet thrice a day up to the 7th day.
Contraindications
Hypersensitivity to imidazole.
Use in pregnancy: Metronidazole should be avoided in the 1st trimester even if there are no clear indications of teratogenic effects.
It should not be administered to patients with active neurological disorders or history of blood dyscrasias, hypothyroidism and hypoadrenalism.
Warnings
Metronidazole has been shown to be carcinogenic in mice. Unnecessary use of the drug should be reserved for conditions described in the indications.
The use of this drug in the 1st trimester of pregnancy should be avoided. During the 2nd trimester of pregnancy, its use should be restricted to those patients in whom topical measures have been proven inadequate. Metronidazole is secreted in the breast milk when administered to nursing mothers. Its use should be avoided although there is no reported effect to the newborn.
Special Precautions
When there is clinical evidence of trichomonal infection, the sexual partner should be treated concomitantly to avoid re-infestations. Although, no persistent hematologic abnormalities have been reported in clinical studies, total and differential leukocyte counts should be made before and after treatment especially if a 2nd course of therapy is needed. Treatment should be discontinued if ataxia or any CNS symptoms occur.
Metronidazole has been shown to be carcinogenic in mice. Unnecessary use of the drug should be reserved for conditions described in the indications.
Patients with Renal Failure: Dose reduction is recommended because of the biologically active metabolite.
Patients with Hepatic Insufficiency: Increase in plasma levels are likely because of the predominantly hepatic metabolism. Reduce dose.
Use in pregnancy & lactation: The use of metronidazole in the 1st trimester of pregnancy should be avoided. During the 2nd trimester of pregnancy, its use should be restricted to those patients in whom topical measures have been proven inadequate. Metronidazole is secreted in the breast milk when administered to nursing mothers. Its use should be avoided although there is no reported effect to the newborn. Relatively high concentrations are found in the breast milk (like in plasma). Nursing is possible 24 hrs after a single dose.
Use in the elderly: Caution with neurological diseases (risk of cramps). Generally no dose adjustment necessary.
Use In Pregnancy & Lactation
The use of metronidazole in the 1st trimester of pregnancy should be avoided. During the 2nd trimester of pregnancy, its use should be restricted to those patients in whom topical measures have been proven inadequate. Metronidazole is secreted in the breast milk when administered to nursing mothers. Its use should be avoided although there is no reported effect to the newborn. Relatively high concentrations are found in the breast milk (like in plasma). Nursing is possible 24 hrs after a single dose.
Adverse Reactions
High doses or long-term administration of metronidazole can cause peripheral neuropathy with sensory disturbances eg, at the hands and feet. Neuropathy is often only slowly reversible or not reversible at all. Neutropenia can also develop. Metallic taste in the mouth, nausea, upper abdominal pain or headaches sometimes occur following usual therapeutic doses. Convulsions, ataxia, skin problems (skin rashes, urticaria) and vaginal candidiasis are not as common. Isolated cases of pancreatitis, cystitis, mucous colitis and hemolysis have been observed. Mutagenic effects have been observed in animal experiments, no carcinogenic effect has yet been demonstrated in humans.
Drug Interactions
Metronidazole can reinforce the effect of oral anticoagulants. A combination with cimetidine results in higher metronidazole levels. Antabuse reactions were observed when combined with alcohol. Concomitant administration of disulfiram can cause psychotic reactions.
Storage
Store at temperatures not exceeding 30°C.
ATC Classification
J01XD01 - metronidazole ; Belongs to the class of imidazole derivative antibacterials. Used in the systemic treatment of infections.
Presentation/Packing
Tab 500 mg x 100's.
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