Description

Simple

A medication used to treat constipation caused by opioid drugs.

Clinical

An opioid antagonist used to to treat opioid-induced constipation.

Overview

Naldemedine is an opioid receptor antagonist [FDA Label]. It is a modified form of [DB00704] to which a side chain has been added to increase molecular weight and polar surface area resulting in restricted transport across the blood brain barrier. Naldemedine was approved in 2017 in both the US and Japan for the treatment of Opioid-induced Constipation.

Pharmacology

Indication

For the treatment of opioid-induced constipation [FDA Label].

Pharmacodynamic

Naldemedine is an opioid receptor antagonist with restricted movement across the blood brain barrier [FDA Label]. This allows it to antagonize the periperal effects of opioid drugs such as constipation without interfering with the effects on the central nervous system.

Mechanism of action

Naldemedine binds to and antagonizes mu-, delta-, and kappa-opioid receptors [FDA Label]. The binding of opioid agonists to peripheral mu-opioid receptors slows the transit of feces through the intestine resulting in constipation. By antagonizing mu-opioid receptors, naldemedine inhibits this effect... Read more

Absorption

Tmax is 0.75 h [FDA Label]. Administration with a high-fat meal reduces Cmax by 35% and increases Tmax to 2.5 h.

Protein binding

Naldemedine is 93-94% bound to human plasma proteins [FDA Label].

Volume of distribution

The apparent volume of disribution during the terminal phase is 155 L [FDA Label]

Clearance

Information currently not available.

Half life

The terminal elimination half life is 11 h [FDA Label].

Route of elimination

57% of naldemedine is excreted in the urine with 16-18% as the parent compound and 35% is excreted in the feces [FDA Label].

Toxicity

The most common adverse effects of naldemedine are abdominal pain (11%), diarrhea (7%), nausea (6%), vomiting (3%), and gastroenteritis (3%) [FDA Label].

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Gastrointestinal obstruction
      • Drugbank Id: DBCOND0010786
  • Regions: US
  • Patient Conditions:
      • Name: Increased risk of recurrent gastrointestinal obstruction
      • Drugbank Id: DBCOND0108997
  • Regions: US
  • Patient Conditions:
      • Name: Suspected gastrointestinal obstruction
      • Drugbank Id: DBCOND0107630

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Abacavir
Abacavir may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Acarbose
Acarbose may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Acetaminophen
Acetaminophen may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Acetazolamide
Acetazolamide may increase the excretion rate of Naldemedine which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid
Acetylsalicylic acid may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Aclidinium
Aclidinium may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Acrivastine
Acrivastine may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Acyclovir
Acyclovir may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Adefovir
Adefovir may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Adefovir dipivoxil
Adefovir dipivoxil may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Albutrepenonacog alfa
Naldemedine may decrease the excretion rate of Albutrepenonacog alfa which could result in a higher serum level.
Alclofenac
Alclofenac may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Aldesleukin
Aldesleukin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Alfentanil
The therapeutic efficacy of Alfentanil can be decreased when used in combination with Naldemedine.
Allopurinol
Allopurinol may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Allylestrenol
Allylestrenol may decrease the excretion rate of Naldemedine which could result in a higher serum level.
Almasilate
Naldemedine may decrease the excretion rate of Almasilate which could result in a higher serum level.
Alminoprofen
Alminoprofen may decrease the excretion rate of Naldemedine which could result in a higher serum level.