Loperamide


Description

One of the long-acting synthetic antidiarrheals; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.

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Pharmacology

Indication

For the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associa... Read more

Pharmacodynamic

Loperamide is a synthetic anti-diarrheal indicated for the control and symptomatic relief of acute n... Read more

Mechanism of action

In vitro and animal studies show that Loperamide acts by slowing intestinal motility and by a... Read more

Absorption

Not significantly absorbed from the gut

Protein binding

97%

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

9.1 to 14.4 hours (average 10.8 hours)

Route of elimination

Excretion of the unchanged loperamide and its metabolites mainly occurs through the feces.

Toxicity

Oral, mouse: LD50 = 105 mg/kg. Symptoms of overdose include constipation, drowsiness, let... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Constipation US
  • Kind: experimental
    • Percent: 2-5%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Abdominal Cramps US
  • Kind: experimental
    • Percent: 3%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 3%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Colic US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Abdominal cramp US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Abdominal cramp US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Colic US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Meteorism US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: ≥1%
  • Clinical Trial
    Rash US
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    Pruritus US
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    Urticaria US
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    Abdominal Distention US
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    Abdominal Pain US
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    Nausea US
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    Abdominal Discomfort US
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    Flatulence US
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    Vomiting US
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    Constipation US
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    Dyspepsia US
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    Bullous eruption US
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    Angioedema US
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    Toxic Epidermal Necrolysis US
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    Stevens-Johnson Syndrome US
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    Anaphylactic shock US
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    Allergic Reactions US
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    Dry Mouth US
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    Anaphylactoid reactions US
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    Toxic megacolon US
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    Urinary Retention US
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    Paralytic Ileus US
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    Megacolon US
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    Fatigue US
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    Drowsiness US
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    Dizziness US
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    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Abdominal pain without diarrhea
        • Drugbank Id: DBCOND0108046
    • Regions: US
    • Below Age:
      • Amount: 24
      • Unit: month
    • Regions: US
    • Patient Conditions:
        • Name: Use as primary therapy for acute ulcerative colitis
        • Drugbank Id: DBCOND0108048
    • Regions: US
    • Patient Conditions:
        • Name: Use as primary therapy for acute dysentery
        • Drugbank Id: DBCOND0108047
    • Regions: US
    • Patient Conditions:
        • Name: Use as primary therapy for pseudomembranous colitis
        • Drugbank Id: DBCOND0108050
    • Regions: US
    • Patient Conditions:
        • Name: Use as primary therapy for bacterial enterocolitis
        • Drugbank Id: DBCOND0108049

    Food Interactions

    • Take without regard to meals. Increase liquid intake.

    Interactions

    Type in a drug name to check for interaction with Loperamide

    The serum concentration of (R)-warfarin can be increased when it is combined with Loperamide.
    The serum concentration of (S)-Warfarin can be increased when it is combined with Loperamide.
    The risk or severity of hypoglycemia can be increased when Loperamide is combined with 2,4-thiazolidinedione.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Loperamide.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Loperamide.
    The metabolism of 4-Methoxyamphetamine can be decreased when combined with Loperamide.
    The metabolism of 5-androstenedione can be decreased when combined with Loperamide.
    The metabolism of Loperamide can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Loperamide.
    The metabolism of 7-ethyl-10-hydroxycamptothecin can be decreased when combined with Loperamide.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Loperamide.
    The therapeutic efficacy of Abafungin can be increased when used in combination with Loperamide.
    The metabolism of Loperamide can be increased when combined with Abatacept.
    The metabolism of Abemaciclib can be decreased when combined with Loperamide.
    The risk or severity of QTc prolongation can be increased when Loperamide is combined with Abexinostat.
    The metabolism of Abiraterone can be decreased when combined with Loperamide.
    The metabolism of Loperamide can be decreased when combined with Acalabrutinib.
    The risk or severity of hypoglycemia can be increased when Loperamide is combined with Acarbose.
    The risk or severity of QTc prolongation can be increased when Loperamide is combined with Acebutolol.
    The risk or severity of hyperkalemia can be increased when Loperamide is combined with Aceclofenac.

    References

      Information currently not available.

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