Name of drug
ROZEX GEL (metronidazole 7.5 mg/g)
Common name Metronidazole
Molecular formula C 6H 9N 3O 3
Molecular weight 171.2
Chemical class Antiprotozoal and antibacterial agent.
Chemical structure N
N CH 2CH 2OH
O 2N CH 3
C 6H 9N 3O 3; M r 171.16
Composition
Metronidazole 7.5 mg/g in an aqueous gel containing methyl and propyl hydroxybenzoates, propylene glycol, carbomer 940 and disodium edetate.
同学会发言Description
Metronidazole is 1- (2 hydroxyethyl)-2-methyl-5-nitroimidazole. It is a white to brownish crystalline powder that is soluble in water.
腊八节的意义Actions
Metronidazole is an antiprotozoal (trichomoniasis, amoebiasis, giardiasis) and anaerobic antibacterial agent. However the mechanisms by which Rozex acts in reducing inflammatory lesions of rosacea are unknown, but may include an antibacterial and / or anti-inflammatory effect.
Pharmacokinetics . The absorption of metronidazole following topical administration is negligible. Studies on the topical administration of 1 gram of Rozex (7.5 mg of metronidazole) to the face of 10 r
osacea patients showed a maximum rum concentration of 66 nanogram/mL in one patient. This concentration is approximately 100 times less than concentrations afforded by a single 250 mg tablet. The rum metronidazole concentrations were below the detectable limits of the assay at the majority of time points in all patients. Three of the patients had no detectable rum concentrations of metronidazole at any time point. The mean do of gel applied during clinical studies was 600 mg, which reprents 4.5 mg of metronidazole per application. Therefore under normal usage levels, the formulation affords minimal rum concentrations of metronidazole.
蛋白质结构
Indications
类别英语Treatment of inflammatory papules, pustules and erythema of rosacea.
Contraindications
Contraindicated in individuals with a history of hypernsitivity to metronidazole, hydroxybenzoates or other ingredients of the formulation.
Precautions
Rozex has been reported to irritate the eyes (watering), therefore contact with the eyes and mucous
membranes should be avoided. If a reaction suggesting local irritation occurs, patients should be directed to u the medication less frequently, discontinue u temporarily or discontinue u until further instructions. Metronidazole is a nitroimidazole compound and should be ud with care in patients with evidence or a history of blood dyscrasia.
Patients should be advid to avoid or minimize exposure of areas treated with topical metronidazole to sunlight or other sources of UV light (e ction: carcinogenicity, mutagenicity and impairment of fertility). Unnecessary or prolonged u of this medication should be avoided, as the long-term safety of topical metronidazole is unknown.
U in pregnancy and lactation. (Category B2)
短片小说集There is no experience to date with the u of Rozex in pregnancy. Metronidazole cross the placental barrier and rapidly enters the foetal circulation. There is inadequate evidence of the safety of metronidazole in human pregnancy. In animal studies metronidazole was not teratogenic or embryotoxic unless administered at extremely high dos. Becau there are no well-controlled studies of therapy with Rozex gel in pregnant women, Rozex gel should not be ud during pregnancy.
After oral administration metronidazole is excreted in breast milk in concentrations similar to tho found in the plasma. Metronidazole blood levels from topical application are significantly lower than tho achieved after oral metronidazole. A decision should be made to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
U in children
Rozex (metronidazole 0.75%) cream has not been studied in children. Rosacea is a skin disorder which principally affects adults.
Carcinogenicity, mutagenicity and impairment of fertility
Animal studies with oral metronidazole showed incread incidences of tumour in the lung, liver, testes, reticulum, mammary gland and pituitary gland in certain rodent species. Evidence of photocarcinogenicity of metronidazole has also been reported in mice. Although there is no evidence to date of a carcinogenic effect in humans it is prudent to avoid unnecessary and prolonged u of Rozex cream and to avoid or to minimi exposure of sites treated with Rozex cream to the sun.
Metronidazole has shown evidence of mutagenic activity in veral bacterial systems. In addition, a do respon increa in the frequency of micronuclei was obrved in mice after
intraperitoneal injection and an increa in chromosome aberrations has been found in human lymphocyte cultures. The benefit/risk ratio should therefore be carefully assd in each ca particularly in relation to the verity of the dia and the age of the patient.
Oral metronidazole caud hypospermatogenesis, infertility and abnormal spermatozoa in mice and rats with a NOEL in rats being about 200 times the estimated human metronidazole do contained in the Rozex cream, bad on body surface area.
Interactions with other drugs
我心目中的小学
Drug interactions are less likely with topical administration but should be kept in mind when Rozex is prescribed for patients who are receiving anticoagulent treatment. Oral metronidazole has been reported to potentiate the anticoagulent effect of coumarin and warfarin resulting in a prolongation of prothrombin time.
Adver reactions
悠扬悦耳的近义词Becau of the minimal absorption of metronidazole and conquently its insignificant plasma concentration after topical administration, the adver experiences reported with the oral form of the
drug have not been reported with Rozex. Adver reactions reported with Rozex include eye irritation (watering) if the gel is applied too cloly to this area, transient redness, mild dryness, burning and skin irritation. None of the side effects exceeded an incidence of 2% of patients.
Post-marketing experience
The following non-rious adver experiences have been reported s ince 1995: contact dermatitis/allergic reaction; local irritation, erythema, pruritis, burning, dryness, tightness, discomfort, rash; hyperpigmentation, pigmentation disorders, hypertrichosis; facial oedema; eyelid oedema; treatment failure (worning of rosacea); watery eyes; metallic taste; tingling or numbness in the extremities; naua; other (zoster lesion, pustules on the no and vesicular bullous eruptions). The causal relationship with topical metronidazole has not been unequivocally established for the adver experiences.
Dosage and administration
Adults. Apply and rub in a thin film of gel twice daily, morning and evening, to entire affected areas after washing.
Elderly. The dosage recommended in the elderly is the same as that recommended in adults. Children. Not recommended.
Areas to be treated should be cleand before application of gel. Patients may u cosmetics after application of the product.
Significant therapeutic results should be noted within three weeks. Clinical studies have demonstrated continuing improvement over nine weeks of therapy.
Overdosage
There is no human experience with overdosage of Rozex. The acute oral toxicity of the Rozex formulation was determined to be greater than 5g/kg (the highest do given) in albino rats.
Prentation Gel : 15g, 30g, 50g
Storage Store below 25°C (room temperature) Name and Address of Sponsor
Galderma Australia
13B Narabang Way
Belro NSW 2085
Marketing Authorisation Number: AUST R 15211. TGA approved 08/02/93
计算机二级一年可以考几次Latest amendment June 2003
