Melanez Suppositories 500 mg: Off white to light brown opaque bullet shaped suppository (Length: 26.7 mm, Width: 8.5±0.3 mm).
Each suppository contains Mesalazine 500 mg.
Melanez Suppositories 1 g: Off white to light brown opaque bullet shaped suppository (Length: 33.0 mm, Width: 10.4±0.3 mm).
Each suppository contains Mesalazine 1 g.
Pharmacotherapeutic group: Intestinal anti-inflammatory agents; aminosalicyclic aid and similar agents. ATC code: A07EC02.
Pharmacology: Pharmacodynamics: Mechanism action: The mechanism of the anti-inflammatory action is unknown. The results of in vitro studies indicate that inhibition of lipoxygenase may play a role.
Effects on prostaglandin concentrations in the intestinal mucosa have been demonstrated. Mesalazine (5-Aminosalicyclic acid/5-ASA) may also function as a radical scavenger of reactive oxygen compounds.
Pharmacodynamic effects: On reaching the intestinal lumen, rectally administered mesalazine has largely local effects on the intestinal mucosa and submucosal tissue.
Pharmacokinetics: General consideration of mesalazine: Absorption: Mesalazine absorption is highest in proximal gut regions and lowest in distal gut areas.
Biostransformation: Mesalazine is metabolized both pre-systematically by the intestinal mucosa and in the liver to the pharmacologically inactive N-acetyl-5-arninosalicylic acid (N-Ac-5-ASA). The acetylation seems to be independent of the acetylator phenotype of the patient. Some acetylation also occurs through the action of colonic bacteria. Protein binding of mesalazine and N-Ac-5-ASA is 43% and 78%, respectively.
Elimination: Mesalazine and its metabolite N-Ac-5-ASA are eliminated via the faeces (major part), renally (varies between 20 and 50%, dependent on kind of application, pharmaceutical preparation and route of mesalazine release, respectively) and biliary (minor part). Renal excretion predominantly occurs as N-Ac-5-ASA. About 1% of total orally administered mesalazine dose is excreted into the breast milk mainly as N-Ac-5-ASA.
Melanez Suppositories 500 mg specific: Distribution: Based on published data, technetium-labelled Melanez Suppositories 500 mg showed peak spread of the suppository that had melted due to body temperature after 2-3 hours. The spread was limited primarily to the rectum and rectosigmoid junction. Melanez Suppositories 500 mg are thus particularly suitable for treating proctitis (ulcerative colitis of the rectum).
Absorption: After both a single administration and after several weeks of long-term treatment with 500 mg mesalazine three times daily as Melanez Suppositories, peak plasma concentrations of 5-ASA were in the range of 0.1 to 1.0 ug/ml, those of the main metabolite N-Ac-5-ASA were in the range of 0.3 to 1.6 ug/ml. Peak plasma concentrations of 5-ASA are partially reached within the first hour of application.
Elimination: After a single rectal dose of 500 mg mesalazine, approximately 11% (within 72 hours) was recovered in the urine, and after several weeks of long-term treatment with 500 mg mesalazine three times daily as Melanez Suppositories, approximately 13% of the 5-ASA dose administered was recovered in the urine. Approximately 10% of a single administered dose was eliminated via the bile.
Melanez Suppositories 1 g specific: Distribution: Scintigraphic studies with a similar medicinal product, technetium-labelled Melanez Suppositories 500 mg showed peak spread of the suppository that had melted due to body temperature after 2-3 hours. The spread was limited primarily to the rectum and rectosigmoid junction. It is assumed that Melanez Suppositories l g act very similar and thus are particularly suitable for treating proctitis (ulcerative colitis of the rectum).
Absorption: Mean peak plasma concentration of 5-ASA after a single rectal dose of 1 g mesalazine (Melanez Suppositories 1 g) were 192±125 ng/ml (range 19-557 ng/ml), those of the main metabolite N-Ac-5-ASA were 402±211 ng/ml (range 57-1070 ng/ml). Time to reach the peak plasma concentration of 5-ASA was 7.1±4.9 h (range 0.3-24 h).
Elimination: After a single rectal dose of 1 g mesalazine (Melanez Suppositories 1 g) approx. 14% of the administered 5-ASA dose were recovered in the urine during 48 hours.
Melanez Suppositories 500 mg: Acute episodes of ulcerative colitis, proctitis and inflammation of the anal canal.
Melanez Suppositories 1 g: Treatment of ulcerative proctitis.
Posology: Adults and elderly: Melanez Suppositories 500 mg: One Mesalazine Suppositories 500 mg three times daily (equivalent to 1500 mg mesalazine daily) inserted into the rectum, according to the individual clinical requirement. As soon as remission has occurred, Mesalazine 500 mg gastro-resistant tablets can be used.
Melanez Suppositories l g: One Melanez Suppositories 1 g, 1-2 times daily inserted into the rectum.
Children and adolescents: There is little experience and only limited documentation for an effect in children.
Method of administration: When used three times daily, Mesalazine Suppositories 500 mg should be inserted into the rectum in the morning, at midday and at bedtime.
Melanez Suppositories l g should be administered preferably at bedtime.
Treatment with Melanez Suppositories must be administered regularly and consistently because only in this way can healing be successfully achieved.
The duration of use is determined by the physician.
Route of Administration: For rectal administration only.
Symptoms and Treatment of Overdosage: There are rare data on overdosage (e.g. intended suicide with high oral doses of mesalazine), which do not indicate renal or hepatic toxicity. There are no specific antidotes and treatment is symptomatic and supportive.
Melanez Suppositories are contraindicated in patients with: Known hypersensitivity to active substance, salicylates or to any of the excipients; Severe impairment of hepatic or renal function.
Blood tests (differential blood count; liver function parameters such as ALT or AST; serum creatinine) urinary status (dipsticks) should be determined prior to and during treatment at the discretion of the treating physician. As a guideline, follow-up tests are recommended 14 days after commencement of treatment, then a further two to three tests at intervals of 4 weeks.
If the findings are normal, follow-up tests should be carried out every 3 months. If additional symptoms occur, these tests should be performed immediately.
Caution is recommended in patients with impaired hepatic function.
Melanez Suppositories should not be used in patients with impaired renal function. Mesalazine-induced renal toxicity should be considered if renal function deteriorates during treatment.
Cases of nephrolithiasis have been reported with the use of mesalazine, including stones with a 100% mesalazine content. It is recommended to ensure adequate fluid intake during treatment.
Patients with pulmonary disease, in particular asthma, should be very carefully monitored during a course of treatment with Melanez Suppositories.
Severe cutaneous adverse reactions: Severe cutaneous adverse reactions (SCARs), including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), have been reported in association with mesalazine treatment.
Mesalazine should be discontinued at the first appearance of signs and symptoms of severe skin reactions, such as skin rash, mucosal lesions, or any other sign of hypersensitivity.
Patients with a history of adverse drug reactions to preparations containing sulphasalazine should be kept under close medical surveillance on commencement of a course of treatment with Melanez Suppositories. Should Melanez Suppositories cause acute intolerance reactions such as abdominal cramps, acute abdominal pain, fever, severe headache and rash, therapy should be discontinued immediately.
Photosensitivity: More severe reactions are reported in patients with pre-existing skin conditions such as atopic dermatitis and atopic eczema.
Effects on Ability to Drive and Use Machines: Melanez Suppositories have no or negligible influence on the ability to drive and use machines.
Pregnancy: There are no adequate data on the use of Melanez Suppositories in pregnant women. However, data on a limited number of exposed pregnancies indicate no adverse effect of mesalazine on the pregnancy or on the health of the foetus/newborn child. To date, no other relevant epidemiologic data are available. In one single case after long-term use of a high dose of mesalazine (2-4 g, orally) during pregnancy, renal failure in a neonate was reported.
Available published animal studies on oral mesalazine do not indicate direct or indirect harmful effects with respect to pregnancy, embryonic/foetal development, parturition or postnatal development.
Melanez Suppositories should only be used during pregnancy if the potential benefit outweighs the possible risk.
Breast-feeding: N-acetyl-5-aminosalicyclic acid and to a lesser degree, mesalazine are expected in breast milk. Only limited experience during lactation in women is available to date. Hypersensitivity reactions such as diarrhoea in the infant cannot be excluded. Therefore, Melanez Suppositories should only be used during breast-feeding, if the potential benefit outweighs the possible risk. If the infant develops diarrhoea, the breast-feeding should be discontinued.
(See table.)
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Severe cutaneous adverse reactions (SCARs), including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), have been reported in association with mesalazine treatment.
Specific interaction studies have not been performed. In patients, who are concomitantly treated with azathioprine, 6-mercaptopurine or thioguanine, a possible increase in the myelosuppressive effects of azathioprine, 6-mercaptopurine or thioguanine should be taken into account. There is weak evidence that mesalazine might decrease the anticoagulant effect of warfarin.
Incompatibilities: Not available.
Instruction for Use: 1. When practical, clean the area around the rectum with mild soap and warm water and rinse thoroughly.
Gently dry by patting or blotting with toilet tissue or a soft cloth.
2. Do not open suppository if it seems soft, hold the foil wrapper under cold water or place it in refrigerator for few minutes to harden it before removing the wrapper.
3. Position the patient to lie on one side with knees bent up to their abdomen or lie on back with feet and legs held up.
4. Detach the suppository by holding strip upright and carefully peel the wrapper evenly down both sides (moisten the suppository if dry).
5. Hold the suppository between index finger and thumb, locate the anus and gently insert suppository tip end first with the index finger. The suppository should be fully inserted into rectum against the wall of rectum.
6. Hold buttocks together while lying down for about 5 minutes to avoid having the suppository come out.
7. Discard used materials and wash hands thoroughly.
Store in a dry place below 30°C. Protect from light.
Shelf Life: 24 months.
A07EC02 - mesalazine ; Belongs to the class of aminosalicylic acid and similar antiinflammatory. Used in the treatment of intestinal inflammation.
Melanez supp 500 mg
6 × 5's
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