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Medicine information : RELISTOR Solution for Injection
| Drug class description : | Solution for Injection |
| Generic Name : | Methylnaltrexone bromide |
| Drug description : | Solution for injection. Sterile, clear solution, colourless to paleyellow, essentially free from visible particulates. |
| Presentation : | Relistor 12 mg /0.6 ml solution for injection. Each vial of 0.6 ml contains 12 mg methylnaltrexone bromide. One ml of solution contains 20 mg methylnaltrexone bromide. |
| Indications : | Treatment of opioidinduced constipation in advanced illness patients who are receiving palliative care when response to usual laxative therapy has not been sufficient. |
| Adult Dosage : | For adults only. RELISTOR should be added to induce prompt bowel movements when response to usual laxative therapy has been insufficient. The recommended dose of methylnaltrexone bromide is 8 mg (0.4 ml RELISTOR) (for patients weighing 3861 kg) or 12 mg (0.6 ml RELISTOR) (for patients weighing 62114 kg). The usual administration schedule is one single dose every other day. Doses may also be given with longer intervals, as per clinical need. Patients may receive two consecutive doses 24 hours apart, only when there has been no response (bowel movement) to the dose on the preceding day. Patients whose weight falls outside of the ranges should be dosed at 0.15 mg/kg. The injection volume for these patients should be calculated: Dose (ml) = patient weight (kg) x 0.0075 Renal patients In patients with severe renal impairment (creatinine clearance less than 30 ml/min), the dose of methylnaltrexone bromide should be reduced from 12 mg to 8 mg (0.4 ml RELISTOR) for those weighing 62 to 114 kg, or from 0.15 mg/kg to 0.075 mg/kg for those whose weight falls outside the 62 to 114 kg range. There are no data available from patients with end-stage renal impairment on dialysis, and RELISTOR is not recommended in these patients (See Special Precuations). Hepatic impairment No dose adjustment is necessary in patients with mild to moderate hepatic impairment. There are no data available from patients with severe hepatic impairment (Child-Pugh Class C), and RELISTOR is not recommended in these patients (See Special Precuations). Administration RELISTOR is given as a subcutaneous injection. It is recommended to rotate injection sites. It is not recommended to inject into areas where the skin is tender, bruised, red, or hard. Areas with scars or stretch marks should be avoided. The three areas of the body recommended for injection of RELISTOR are upper legs, abdomen, and upper arms. RELISTOR can be injected without regard to food. |
| Child Dosage : | There is no experience in children under the age of 18. Therefore, methylnaltrexone should not be used in the paediatric age group until further data become available. |
| Elderly Dosage : | No dose adjustment is recommended based on age . |
| Contra Indications : | Hypersensitivity to the active substance or to any of the excipients. Use of methylnaltrexone bromide in patients with known or suspected mechanical gastrointestinal obstruction or acute surgical abdomen is contraindicated. |
| Special Precautions : | The activity of methylnaltrexone bromide has been studied in patients with constipation induced by opioids. Therefore, RELISTOR should not be used for treatment of patients with constipation not related to opioid use. If severe or persistent diarrhoea occurs during treatment, patients should be advised not to continue therapy with RELISTOR and consult their physician. Data from clinical trials suggest treatment with methylnaltrexone bromide can result in the rapid onset (within 30 to 60 minutes on average) of a bowel movement. Methylnaltrexone bromide treatment has not been studied in clinical trials for longer than 4 months, and should therefore only be used for a limited period. RELISTOR should only be used in patients who are receiving palliative care. It is added to usual laxative treatment. RELISTOR is not recommended in patients with severe hepatic impairment or with endstage renal impairment requiring dialysis (See Adult Dosage). Use of methylnaltrexone bromide in patients with colostomy, peritoneal catheter, active diverticular disease or fecal impaction has not been studied. Therefore, RELISTOR should only be administered with caution in these patients. This medicinal product contains less than 1 mmol sodium (23 mg) per dose, i.e., essentially sodium-free). |
| Interactions : | Methylnaltrexone does not affect the pharmacokinetics of medicinal products metabolised by cytochrome P450 (CYP) isozymes. Methylnaltrexone is minimally metabolised by CYP isozymes. In vitro metabolism studies suggest that methylnaltrexone does not inhibit the activity of CYP1A2, CYP2E1, CYP2B6, CYP2A6, CYP2C9, CYP2C19 or CYP3A4, while it is a weak inhibitor of the metabolism of a model CYP2D6 substrate. In a clinical drug interaction study in healthy adult male subjects, a subcutaneous dose of 0.3 mg/kg of methylnaltrexone did not significantly affect the metabolism of dextromethorphan, a CYP2D6 substrate. The organic cation transporter (OCT)-related drug-drug interaction potential between methylnaltrexone and an OCT inhibitor was studied in 18 healthy subjects by comparing the single-dose pharmacokinetic profiles of methylnaltrexone before and after multiple 400 mg doses of cimetidine. The renal clearance of methylnaltrexone was reduced following multiple-dose administration of cimetidine (from 31 l/h to 18 L/h). However, this resulted in a small reduction in total clearance (from 107 L/h to 95 l/h). Consequently, no meaningful change in AUC of methylnaltrexone, in addition to Cmax, was observed before and after multiple-dose administration of cimetidine. Pregnancy: There are no adequate data with the use of methylnaltrexone bromide in pregnant women. Studies in animals have shown reproductive toxicity at high doses. The potential risk for humans is unknown. RELISTOR should not be used during pregnancy unless clearly necessary. Lactation: It is unknown whether methylnaltrexone bromide is excreted in human breast milk. Animal studies have shown excretion of methylnaltrexone bromide in breast milk. A decision on whether to continue/discontinue breastfeeding or to continue/discontinue therapy with RELISTOR should be made, taking into account the benefit of breast-feeding to the child and the benefit of RELISTOR therapy to the woman. |
| Adverse Reactions : | The most common drugrelated adverse reactions in all patients exposed to methylnaltrexone bromide during all phases of placebo-controlled studies were abdominal pain, nausea, diarrhoea and flatulence. Generally, these reactions were mild or moderate. The adverse reactions are classified as: Very common (=1/10); Common (=1/100 to <1/10); Uncommon (=1/1,000 to <1/100); Rare (1/10,000 to <1/1,000); Very rare (<1/10,000), unknown (cannot be estimated from the available data). Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness: Nervous system disorders Common: Dizziness Gastrointestinal disorders Very common: Abdominal pain, nausea, flatulence, diarrhoea Skin and subcutaneous tissue disorders Common: Injection site reactions (e.g. stinging, burning, pain, redness, oedema) |
| Manufacturer : | Wyeth |
| Drug Availability : | (POM) |
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