Opioid-induced constipation

Active Ingredient: Methylnaltrexone

Indication for Methylnaltrexone

Population group: only adults (18 years old or older)

Methylnaltrexone is indicated for the treatment of opioid-induced constipation when response to laxative therapy has not been sufficient in adult patients, aged 18 years and older.

For this indication, competent medicine agencies globally authorize below treatments:

8-12 mg once a day or every other day

Route of admnistration

Subcutaneous

Defined daily dose

8 - 12 mg

Dosage regimen

From 8 To 12 mg once every 2 day(s)

Detailed description

Opioid-induced constipation in adult patients with chronic pain (except palliative care patients with advanced illness)

The recommended dose of methylnaltrexone bromide is 12 mg (0.6 mL of solution) subcutaneously, as needed, given as at least 4 doses weekly, up to once daily (7 doses weekly).

In these patients, the treatment with usual laxatives should be stopped when commencing treatment with methylnaltrexone.

Opioid-induced constipation in adult patients with advanced illness (palliative care patients)

The recommended dose of methylnaltrexone bromide is 8 mg (0.4 mL of solution) (for patients weighing 38-61 kg) or 12 mg (0.6 mL of solution) (for patients weighing 62-114 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 as follows:

Dose (mL) = patient weight (kg) x 0.0075

In palliative care patients, methylnaltrexone is added to usual laxative treatment.

Dosage considerations

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 methylnaltrexone are upper legs, abdomen, and upper arms.

Methylnaltrexone can be injected without regard to food.

8-12 mg once a day or every other day

Route of admnistration

Subcutaneous

Defined daily dose

8 - 12 mg

Dosage regimen

From 8 To 12 mg once every 2 day(s)

Detailed description

Opioid-induced constipation in adult patients with chronic pain (except palliative care patients with advanced illness)

The recommended dose of methylnaltrexone bromide is 12 mg (0.6 mL of solution) subcutaneously, as needed, given as at least 4 doses weekly, up to once daily (7 doses weekly).

In these patients, the treatment with usual laxatives should be stopped when commencing treatment with methylnaltrexone.

Opioid-induced constipation in adult patients with advanced illness (palliative care patients)

The recommended dose of methylnaltrexone bromide is 8 mg (0.4 mL of solution) (for patients weighing 38-61 kg) or 12 mg (0.6 mL of solution) (for patients weighing 62-114 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 as follows:

Dose (mL) = patient weight (kg) x 0.0075

In palliative care patients, methylnaltrexone is added to usual laxative treatment.

Dosage considerations

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 methylnaltrexone are upper legs, abdomen, and upper arms.

Methylnaltrexone can be injected without regard to food.

Active ingredient

Methylnaltrexone

Methylnaltrexone bromide is a selective antagonist of opioid binding at the mu-receptor. As a quaternary amine, the ability of methylnaltrexone bromide to cross the blood-brain barrier is restricted. This allows methylnaltrexone bromide to function as a peripherally acting mu-opioid antagonist in tissues such as the gastrointestinal tract, without impacting opioid-mediated analgesic effects on the central nervous system.

Read more about Methylnaltrexone

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