Description

Simple

A medication used to treat congestion and a runny nose.

Clinical

An alpha and beta adrenergic agonist used to treat nasal and sinus congestion, as well as allergic rhinitis.

Overview

Pseudoephedrine is structurally related to [ephedrine] but exerts a weaker effect on the sympathetic nervous system.[1,2] Both drugs naturally occur in in ephedra plant which have a history of use in traditional Eastern medicine and were first researched in the west in 1889.[2] The decongestant effect of pseudoephedrine was described in dogs in 1927.[2]

Pharmacology

Indication

Pseudoephedrine is a sympathomimetic amine used for its decongestant activity.[11, Read more

Pharmacodynamic

Pseudoephedrine causes vasoconstriction which leads to a decongestant effect.[2, Read more

Mechanism of action

Pseudoephedrine acts mainly as an agonist of alpha adrenergic receptors[6] and less stro... Read more

Absorption

A 240mg oral dose of pseudoephedrine reaches a Cmax of 246.3±10.5ng/mL fed and 272.5±13.4ng/mL fasted, with a Tmax of 6.60±1.38h fed and 11.87±0.72h fasted, with an AUC of 6862.0±334.1ng\*h/mL fed and 7535.1±333.0ng\*h/mL fasted.[ Read more

Protein binding

-pseudoephedrine is 6.6±0.4% bound to human serum albumin and 22.5±3.2% protein bound in serum.[ Read more

Volume of distribution

The apparent volume of distribution of pseudoephedrin is 2.6-3.3L/kg.[11]

Clearance

A 60mg oral dose of pseudoephedrine has a clearance of 5.9±1.7mL/min/kg.[13]

Half life

The mean elimination half life of pseudoephedrine is 6.0h.[11]

Route of elimination

55-75% of an oral dose is detected in the urine as unchanged pseudoephedrine.[13]

Toxicity

The oral LD50 of pseudoephedrine is 2206mg/kg in rats and 726mg/kg in mice.[13]

Patients experiencing an overdose of pseudoephedrine may prese... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • Kind: experimental
    • Percent: 19
  • Kind: experimental
    • Percent: 18
  • Kind: comparator
    • Percent: 19
  • Kind: comparator
    • Percent: 19
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 10
  • Kind: comparator
    • Percent: 13
  • Kind: comparator
    • Percent: 3
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 6
  • Kind: experimental
    • Percent: 12
  • Kind: comparator
    • Percent: 8
  • Kind: comparator
    • Percent: 12
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 11
  • Kind: experimental
    • Percent: 8
  • Kind: comparator
    • Percent: 2
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 8
  • Kind: comparator
    • Percent: 9
  • Kind: comparator
    • Percent: 8
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 8
  • Kind: comparator
    • Percent: 2
  • Kind: comparator
    • Percent: 8
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 5
  • Kind: experimental
    • Percent: 8
  • Kind: comparator
    • Percent: 1
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 6
  • Kind: experimental
    • Percent: 7
  • Kind: comparator
    • Percent: 5
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 2
  • Kind: experimental
    • Percent: 7
  • Kind: comparator
    • Percent: 5
  • Kind: comparator
    • Percent: 3
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 4
  • Kind: experimental
    • Percent: 1
  • Kind: comparator
    • Percent: 6
  • Kind: comparator
    • Percent: 1
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 4
  • Kind: comparator
    • Percent: 2
  • Kind: comparator
    • Percent: 2
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 3
  • Kind: comparator
    • Percent: 2
  • Kind: comparator
    • Percent: 4
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: 3
  • Kind: experimental
    • Percent: 1
  • Kind: comparator
    • Percent: 4
  • Kind: comparator
    • Percent: 2
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 4
  • Kind: placebo
    • Percent: 0.6
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 3.6
  • Kind: placebo
    • Percent: 0.4
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 2
  • Kind: comparator
    • Percent: 3
  • Kind: comparator
    • Percent: 1
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 3
  • Kind: comparator
    • Percent: 2
  • Kind: comparator
    • Percent: 2
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 3
  • Kind: comparator
    • Percent: 3
  • Kind: comparator
    • Percent: 3
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 2
  • Kind: experimental
    • Percent: 3
  • Kind: comparator
    • Percent: 3
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 2
  • Kind: experimental
    • Percent: 3
  • Kind: comparator
    • Percent: 1
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 3
  • Kind: experimental
    • Percent: 3
  • Kind: comparator
    • Percent: 2
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 3
  • Kind: experimental
    • Percent: 3
  • Kind: comparator
    • Percent: 2
  • Clinical Trial
    Dysmenorrhea US
  • Kind: experimental
    • Percent: 1
  • Kind: experimental
    • Percent: 2
  • Kind: comparator
    • Percent: 2
  • Kind: comparator
    • Percent: 3
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 3
  • Kind: experimental
    • Percent: 2
  • Kind: comparator
    • Percent: 1
  • Kind: comparator
    • Percent: 1
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 2
  • Kind: experimental
    • Percent: 2
  • Kind: comparator
    • Percent: 3
  • Kind: comparator
    • Percent: 2
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 2
  • Kind: experimental
    • Percent: 2
  • Kind: comparator
    • Percent: 3
  • Kind: comparator
    • Percent: 3
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 2
  • Kind: experimental
    • Percent: 3
  • Kind: comparator
    • Percent: 3
  • Kind: comparator
    • Percent: 3
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 2.4
  • Kind: placebo
    • Percent: 0.9
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 2
  • Kind: comparator
    • Percent: 0
  • Kind: comparator
    • Percent: 2
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 2
  • Kind: experimental
    • Percent: 2
  • Kind: comparator
    • Percent: 0
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 2
  • Kind: experimental
    • Percent: 2
  • Kind: comparator
    • Percent: 1
  • Clinical Trial
    Psychomotor hyperactivity US
  • Kind: experimental
    • Percent: 2
  • Kind: experimental
    • Percent: 2
  • Kind: comparator
    • Percent: 0
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: 1
  • Kind: experimental
    • Percent: 2
  • Kind: comparator
    • Percent: 1
  • Clinical Trial
    Cough increase US
  • Kind: experimental
    • Percent: 1
  • Kind: experimental
    • Percent: 2
  • Kind: comparator
    • Percent: 2
  • Kind: comparator
    • Percent: 1
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 1
  • Kind: experimental
    • Percent: 2
  • Kind: comparator
    • Percent: 1
  • Kind: comparator
    • Percent: 2
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 1.9
  • Kind: placebo
    • Percent: 0.1
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 1.7
  • Kind: placebo
    • Percent: 1.1
  • Clinical Trial
    Epistaxis US
  • Kind: experimental
    • Percent: 1.1
  • Kind: placebo
    • Percent: 0.9
  • Clinical Trial
    Accidental injury US
  • Kind: experimental
    • Percent: 1.1
  • Kind: placebo
    • Percent: 0.4
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 1.1
  • Kind: placebo
    • Percent: 0.1
  • Clinical Trial
    Sinusitis US
  • Kind: experimental
    • Percent: 1
  • Kind: placebo
    • Percent: 0.6
  • Clinical Trial
    Urticaria US
    Post Marketing
    Puritus US
    Post Marketing
    Rash US
    Post Marketing
    Dyspnea US
    Post Marketing
    Palpitations US
    Post Marketing
    Tachycardia US
    Post Marketing
    Acute Generalized Exanthematous Pustulosis US
    Post Marketing
    Erythema multiforme US
    Post Marketing
    Bronchospasm US
    Post Marketing

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Severe Hypertension
        • Drugbank Id: DBCOND0058109
        • Modification Of:
          • Base:
            • Name: Hypertension
            • Drugbank Id: DBCOND0020037
          • Severity:
            • Includes:
              • severe
    • Regions: US
    • Patient Conditions:
        • Name: Urinary Retention
        • Drugbank Id: DBCOND0001412
    • Regions: US
    • Patient Conditions:
        • Name: Narrow-angle glaucoma
        • Drugbank Id: DBCOND0095646
    • Regions: US
    • Patient Conditions:
        • Name: Severe Coronary Artery Disease
        • Drugbank Id: DBCOND0037446
        • Modification Of:
          • Base:
            • Name: Coronary Artery Disease
            • Drugbank Id: DBCOND0000554
          • Severity:
            • Includes:
              • severe
    • Regions: US
    • With Categories Coadmin:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996
    • Hypersensitivity:
      • true
    • Regions: US

    Food Interactions

    Take with or without food. The absorption is unaffected by food.