Naldemedine


Description

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. Na...

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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... Read more

Mechanism of action

Naldemedine binds to and antagonizes mu-, delta-, and kappa-opioid receptors [FDA Label]. The bindin... Read more

Absorption

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

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 i... Read more

Toxicity

The most common adverse effects of naldemedine are abdominal pain (11%), diarrhea (7%), nausea (6%),... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Abdominal Pain US
  • adult
  • Kind: experimental
    • Percent: 8-11%
  • Kind: placebo
    • Percent: 2-5%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 2-3%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Gastroenteritis US
    • adult
  • Kind: experimental
    • Percent: 2-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Opioid Withdrawal US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Vomiting US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Rash US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Bronchospasm US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial

    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

    Type in a drug name to check for interaction with Naldemedine

    Abacavir may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Acarbose may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Aceclofenac may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Acemetacin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Acetaminophen may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Acetazolamide may increase the excretion rate of Naldemedine which could result in a lower serum level and potentially a reduction in efficacy.
    Acetylsalicylic acid may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Aclidinium may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Acrivastine may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Acyclovir may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Adefovir may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Adefovir dipivoxil may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Naldemedine may decrease the excretion rate of Albutrepenonacog alfa which could result in a higher serum level.
    Alclofenac may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Aldesleukin may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    The therapeutic efficacy of Alfentanil can be decreased when used in combination with Naldemedine.
    Allopurinol may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Allylestrenol may decrease the excretion rate of Naldemedine which could result in a higher serum level.
    Naldemedine may decrease the excretion rate of Almasilate which could result in a higher serum level.
    Alminoprofen may decrease the excretion rate of Naldemedine which could result in a higher serum level.

    References

      Information currently not available.

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