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Updated On: 27-02-2024

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Methylnaltexone Bromide- Opioid Antagonist- Antialcoholic

Drug Name:
Methylnaltexone Bromide- Opioid Antagonist- Antialcoholic

List Of Brands:

RELISTOR*

Indication Type Description:

Indication

Adverse Reaction

Contra-Indications

Dosages/ Overdosage Etc

Patient Information

Pharmacology/ Pharmacokinetics

Pregnancy and lactation

Indication:

Opioid Induced Constipation

Adverse Reaction:

CNS- dizziness 7%

GI- abdominal pain 28% diarrhea 5% flatulence 13% nausea 11%

Contra-Indications:

In patients with known or suspeceted mechanical GI obstruction

Special Precautions-

Severe or persistent diarrhea- if severe or persistent diarrhea occurs advice patients

to discontinue therapy and consult the doctor

Peripheral catheters- use of methynaltexone has not been studied with peripherl catheters

Renal function impairment- dose reduction of one-half is recommended in patients with

severe renal function impairment (CrCl less than 30mL/min)

Pregnancy- use methylnatrexone only if absolutely needed

Lactation- excercise caution when methynatrexone is administered to breast-feeding

woman.

Children- Safety for use in children have not establishd

Dosages/ Overdosage Etc:

Indication-

Opioid Induced constipation

Dosage-

8mg for patients weighing 38 or less than 62kg (84 to less than 136 lb) or

12mg for patients weighing 62 to 114kg (136 to 251 lb)

The usual schedule is 1 dose every other day as needed but no more frequently than

1 dose in a 24 hour period.

Patients falling outside this range should be dosed at 0.15mg/kg

Patient Information:

1. Instruct patients the usual schedule of 1 dose every other day as needed, but no

more frequently than 1 dose in 24 hours period

2.In about 30% of patients in clinical trials, laxation was reported within 30 minutes of

administering the drug. Advice patients to be within close proximity of toilet facitites

once the drug is administered

3.Advice patients not to continue taking the drug if they experience severe or persistent

diarrhea

4. Instruct patients to discontinue mthylnatrexone if they stop taking their opioid

pain medication

Pharmacology/ Pharmacokinetics:

Ref - Drug Facts and Comparison (2010)

Pharmacology-

Methylnatrexone is a selective antagonist of opioid binding the muopioid receptor.

As a quaternary amine , the ability of methylnatrexone to cross the blood-brain barier

is restricted. This allows methynaltrexone to function as peripherally acting mucopioid

receptor antagonist in tissues such as GI tract, thereby decreasing the constipating

effects of opioid without impacting opioid mediated analgesic effects on the CNS

Pharmacokinetics

Following subcutaneous admin methylnaltrexone is absorbed rapidly with peak

concentration Cmax acheived at approx 0.5 hrs . Across the range of doses evaluated

peak concentration and area under curve (AUC) increase in a dose proportional

manner as indicated-

Pharmacokinetic Parameters of Methynaltrexone

following single Subcutaneous doses

Parameter 0.15mg/kg 0.3mg/kg 0.5mg/kg

Cmax 9ng/mL) 117(32.7) 239(62.2) 392(147.9)

Tmax (hours) 0.5(0.25 to 0.75) 0.5(0.25 to 0.75) 0.5 (0.25 to 0.75)

AUC 9ng*h/mL) 175(36.6) 382(63.8) 582(111.2)

Pregnancy and lactation:

Pregnancy- use methylnatrexone only if absolutely needed

Lactation- excercise caution when methynatrexone is administered to breast-feeding

woman.

Children- Safety for use in children have not establishd

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