DIOGYL®TABLETS (Metronidazole BP 200 mg)
Metronidazole is used in amoebiasis, giardiasis, trichomoniasis, helicobacter pylori eradication and anaerobic infections (after colorectal or pelvic surgery, appendectomy, osteomyelitis and abscesses of brain or lung).
Oral absorption of Diogyl is excellent. Bioavailability is at least 90%. Food decreases the rate, but not the extent of absorption. Diogyl is widely distributed into most body tissues and fluids including bone, bile, saliva, pleural and peritoneal fluids, vaginal and seminal fluids and the CSF. Protein binding of Diogyl is roughly 10% oral administration of 250mg, 500mg or 2g doses in healthy, fasting adults results in peak concentrations of 4.6-6.5ug/ml, and 30-45ug/ml, respectively, after 3 hours.
Peak serum concentration after oral administration of the 750mg extended release preparation is roughly 19.4ug/ml, in the fed state and 12.5ug/ml in the fasting state; AUC in the fed and fasting state is 211ug-hr/ml and 198ug-hr/ml, respectively.
Intravenous administration of 7.5mg/kg IV every 6 hours in healthy adults produces peak plasma concentration of 26ug/ml and troughs of 18ug/ml at steady state CSF concentrations of metronidazole are approximately 43% of plasma concentrations. The drug crosses the placenta and enters breast milk.
A significant amount of Diogyl (30-60) is metabolized in the liver by hydroxylation oxidation and glucuronide conjugation. The major metabolite is 2-hydroxymethyl metronidazole which has some antibacterial and antiprotozoal activity.
Within 24 hours, approximately 20% of Diogyl is excreted in the urine and 3% in feces. After 5 days the amount excreted in the urine increase 77% and that excreted in feces to 14%. Both unchanged drug and metabolites are excreted in the urine and the feces. Geriatric patients may have a decreased urinary excretion of metronidazole.
This medication is removed by hem dialysis but not by peritoneal dialysis and color the urine reddish brown due to water solute pigments formed during metabolism. The mean elimination half-life of metronidazole is roughly 8 hours.
Mode of action
Diogyl selectively blocks some of the functions within the bacterial cells and the parasites resulting in the death.
Invasive intestinal amoebiasis
Adults: 800mg every 8 hours for 5 days
Children: 1-3 years 200mg every 8 hours, 4-7 years 200mg every 6 hours, 8-10 years 400mg every 8 hours.
Intestinal amoebiasis in less susceptible people and chronic amoebic hepatitis.
Adults: 400mg every 8 hours for 5-10 days.
Children: 1-3 years 100mg every 8 hours, 4-7 years 100mg every 6 hours, 8-10 years 200mg every 8 hours.
Amoebic liver abscess and other forms environmental amoebiasis
Adults: 400mg every 8 hours for 5 days
For chronic hepatitis trichomonias
Adults: 200mg every 8 hours for 7 days
Children: 1-3 years 50mg every 8 hours, 4-7 years 100mg every 12 hours, 8-10 years 100mg every 8 hours.
Precautions and warnings
Use Dogyl with caution in decreased liver function, brain disease has occurred as a result of liver disease (hepatic encephalopathy). People with diseases of the brain or spinal cord and hereditary blood disorders called porphyries.
Do not drink alcohol while taking this medicine and for at least 48 hours after finishing the course as this can cause unpleasant symptoms such as hot flushes, abdominal cramps, nausea, vomiting, headache and palpitations.
This medicine may cause various side effects that could impair your mental or physical ability to safely drive or operate machinery. Although these are very rare, you should be aware of how you react to this medicine before driving or operating machinery.
If your course of treatment is longer than 10 days it is recommended that you are monitored by your doctor, who may carry out tests to check for side effects and that the medicine is working properly. Tell your doctor if you experience any pins and needles type of sensations, unsteadiness walking, dizziness, fits, severe abdominal pain or yellowing of your skin or whites of your eyes (jaundice) while taking the medicine.
Avoid using Diogyl in early pregnancy and chronic alcohol dependence
When given in conjunction with alcohol Diogyl may provoke Disulfiram like reaction in some individuals. Acute psychosis or confusion have been associated with the concomitant use of Diogyl and Disulfiram. Diogyl lowers plasma level of oral anticoagulants, phenobarbitone and corticosteroids when concomitantly administered with these drugs. Diogyl impairs the metabolism or excretion of several drugs such as warfarin, phenytoin and fluorouracil.
GIT disturbances, urticarial, angio-oedema, peripheral neuropathy and transient epileptiform seizure on intensive and or prolonged use.
Treatment of averdosage
Emesis or gastric lavage should be indicated as rapidly as possible followed by supportive measures.