INFORMATION FOR HEALTH PROFESSIONALS
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DYZOLE is available as white round biconvex film-coated tablets coded with dp one side & 500 on the other, containing 500mg tinidazole. Tablets are approximately 12mm in diameter.
The mode of action of tinidazole against anaerobic bacteria and protozoa involves penetration of the compound into the cell of the microorganism and subsequent damage of DNA strands or inhibition of their synthesis.
Tinidazole is active against both protozoa and obligate anaerobic bacteria. The activity against protozoa involves Trichomonas vaginalis, Entamoeba histolytica and Giardia lamblia.
Tinidazole is active against most anaerobic bacteria including Bacteroides fragilis, Bacteroides melaninogenicus, Bacteroides spp., Clostridium spp., Eubacterium spp., Fusobacterium spp., Gardnerella vaginalis, Peptococcus spp., Peptostreptococcus spp., and Veillonella spp.
Tinidazole is rapidly and completely absorbed after oral therapy. Peak serum levels usually occur within two hours after administration and decline slowly, with an elimination half-life of 12 to 14 hours.
In healthy volunteers, peak plasma concentrations at 2 hours after a single oral 2g dose vary between 40-51 mcg/mL. At 24 hours the values are between 11-19 mcg/mL. Detectable levels of approximately 1 mcg/mL are still observed up to 72 hours.
In healthy volunteers, tinidazole 1600mg given as a single intravenous infusion over 10-15 minutes gives peak plasma concentrations of 32 mcg/mL decreasing to 8.6 mcg/mL at 24 hours, 2.1 mcg/mL at 48 hours and 0.5 mcg/mL at 72 hours.
In healthy volunteers, tinidazole 800mg given as a single intravenous infusion over 10-15 minutes gives peak plasma concentrations of between 14-21 mcg/mL. At 24 hours postinfusion the values are between 4-5 mcg/mL, justifying once daily dosage administration.
Studies with labelled tinidazole in humans show that tinidazole is excreted mainly in the urine and to a lesser extent in faeces in a proportion of 5 to 1 measured as radioactivity excreted after 5 days.
In humans, about 37% of an intravenously administered dose has been recovered from urine: 25% as unchanged compound, about 2% as the 2-hydroxymethyl metabolite and its glucuronide conjugate, and approximately 10% as an unidentified compound. The manner in which the rest of the compound is eliminated from the body has yet to be clarified.
In patients with moderate to severe renal impairment the pharmacokinetic characteristics are not markedly changed in comparison with those in normal volunteers. Thus modification of the dosage in patients with impaired renal function is not necessary.
The plasma protein binding is approximately 12%.
Following dosing with tinidazole the compound is well distributed into body tissues in clinically effective concentrations and effectively passes the blood brain barrier.
Adult: A single oral dose of 2g approximately 12 hours before surgery.
Children less than 12 years: Data are not available to allow dosage recommendations for children below the age of 12 years in the prophylaxis of anaerobic infections.
Adults: An initial oral dose of 2g the first day followed by 1g daily given as a single dose or as 500mg twice daily.
Treatment for 5 to 6 days will generally be adequate but clinical judgement must determine the duration of therapy, particularly when eradication of infection from certain sites may be difficult.
Regular clinical and laboratory observation is advised if it is considered necessary to continue therapy for more than 7 days.
Children less than 12 years: Data are not available to allow dosage recommendations for children below the age of 12 years in the treatment of anaerobic infections.
Adults: Nonspecific vaginitis has been successfully treated with a single oral dose of 2g. Higher cure rates have been achieved with 2g single daily doses on two consecutive days (total dosage 4g).
Adults: A single oral dose of 2g.
When infection with Trichomonas vaginalis is confirmed, simultaneous treatment of the consort is recommended.
Adults: A single oral dose of 2g.
Children: A single dose of 50 to 75 mg/kg of body weight. It may be necessary to repeat this dose once in some cases.
Use the recommended DYZOLE oral regimen for urogenital trichomoniasis, plus one Nystatin vaginal tablet inserted twice daily for 7 to 14 days.
Adults: A single dose of 2g orally.
Children: A single dose of 50 to 75 mg/kg of body weight. It may be necessary to repeat this dose once in some cases.
Adults: A single daily dose of 2g orally for 2 to 3 days or 600 mg orally twice daily for 5 days.
In the occasional instance where a three day single daily dose is ineffective, treatment may be continued for up to 6 days and where the five day twice daily course is ineffective, treatment may be continued for up to a total of 10 days.
Children: A single daily dose of 50 to 60mg/kg of body weight on each of three successive days.
Adults: Total dosage varies from 4.5 to 12g, depending on the virulence of the Entamoeba histolytica.
Treatment should be initiated with 1.5 to 2g orally as a single daily dose for 3 days. In the occasional instance where a three-day course is ineffective, treatment may be continued for up to a total of 6 days.
As an alternative, 600mg twice daily may be given for 5 days. In the occasional instance where the five day course is ineffective, treatment may be continued for up to a total of 10 days.
Children: A single daily dose of 50 to 60 mg/kg of body weight on each of five successive days.
In amoebic involvement of the liver, the aspiration of pus may be required in addition to therapy with DYZOLE
It is recommended that oral DYZOLE be taken during or after a meal.
As with other compounds of similar structure, tinidazole, is contraindicated in patients having, or with a history of, blood dyscrasias although no persistent haematological abnormalities have been noted in clinical or animal studies. Tinidazole should be avoided in patients with organic neurological disorders.
Tinidazole crosses the placental barrier and is present in the breast milk when administered to nursing mothers.
Since the effects of compounds of this class on foetal development and in newborn are not definitely known, tinidazole is contraindicated during the first trimester of pregnancy and in nursing mothers during the neonatal period.
Tinidazole should not be administered to patients with known hypersensitivity to the compound.
Compounds of similar chemical structure have produced various neurological disturbances such as dizziness, vertigo, uncoordination, and ataxia. If, during therapy with tinidazole, abnormal neurological signs develop, therapy should be discontinued.
Tinidazole is contraindicated during the first trimester of pregnancy. While there is no evidence that tinidazole is harmful during the late stages of pregnancy, its use during the last two trimesters requires that the potential benefits outweigh the possible risk to mother and foetus.
Reported side effects have generally been infrequent, mild and self-limiting. Side effects from the gastrointestinal tract include nausea, vomiting, anorexia, diarrhoea and metallic taste.
Hypersensitivity reactions, occasionally severe, may occur in rare cases in the form of skin rash, pruritis, urticaria and angioneurotic oedema.
As with related compounds, tinidazole may produce transient leukopenia. Other rarely reported side-effects are headache, tiredness, furry tongue and dark urine.
Tinidazole and related compounds when taken together with alcoholic beverages have caused abdominal cramps, flushing and vomiting.
Closely related chemical compounds enhance the activity of warfarin. If DYZOLE is given to patients receiving warfarin or other anticoagulants, the dosage of the latter should be recalibrated.
Nil
Store below 30°C
Prescription Medicine
Outer carton each containing 10 blisters of 4 individual tablets.
DYZOLE brand of tinidazole is a derivative of the substituted imidazole compounds with antiprotozoal and antianaerobic activity. The chemical name of tinidazole is 1-(2(ethylsulfonyl)ethyl)-2-methyl-5 nitroimidazole. It is a pale-yellow, crystalline solid that is relatively insoluble in water and soluble in organic solvents such as methanol and chloroform.
Other ingredients of the tablets are: Maize cornflour, Alginic acid, Microcrystalline cellulose, Magnesium stearate, Sodium lauryl sulphate, Opadry white (Y-1-7000B) and Hydroxypropylmethyl cellulose.
Lincoln Pharmaceuticals
A Division of Douglas Pharmaceuticals Ltd
Central Park Drive
Lincoln
PO Box 45027
AUCKLAND 8
NEW ZEALAND.
Phone: (09) 835-0660
Toll Free: 0800 744 844
Fax: (09) 835-0665
1 September 1999