Pseudoephedrine

Mechanism of Action

• Acts on α- and β2-adrenergic receptors
  • Alpha-adrenergic activation causes vasoconstriction of blood vessels
    • Decreases fluid leaving the blood vessels and entering the nose, throat and sinus linings
    • Decreases inflammation of nasal membranes
    • Decreased mucus production
  • Beta-adrenergic activation cause relaxation of smooth muscle in the bronchi
    • Increases bronchial dilation
    • Decreases non-fluid congestion and difficulty breathing

Treatment

• Nasal/sinus decongestant
• Stimulant
• Urinary incontinence (off label)

Brand Names

• Sudafed
• SudoGest
• Valu-Tapp Decongestant
• Silfedrine
• Wal-phed
• Sudogest

Other Medicines

• May be included in many over-the-counter medications
  • Either as a single ingredient or in combination with other medicines
• Antihistamines (Zyrtec D, Semprex-D, Claritin-D, Allegra-D)
• Guaifenesin (Mucinex D)
• Dextromethorphan (Wal-Tussin Cough, Creomulsion Adult Formula, Vicks DayQuil Cough)
• Acetaminophen
• Aspirin
• Ibuprofen

Interactions

• Monoamine oxidase inhibitor (MOI)
  • Use within 14 days of Pseudoephedrine can cause hypertensive crises (Livingston 1995)
• Methyldopa, reserpine, beta-blockers
  • As a sympathomimetic, pseudoephedrine may decrease the antihypertensive effects of medications (Jones & Barlett 2011)
• Digitalis
  • Pseudoephedrine can increase of ectopic pacemaker activity (PDR 2005)
    • AKA: ectopic focus, or premature heartbeat outside the normally functioning SA node
• Antacids
• Increase rate of pseudoephedrine absorption (Lucarotti 1972)

Effect on Exercise and Rest

• Heart Rate
  • Small yet significant increase in heart rate (2.83 beats/min) (Solemo 2005)
  • Generally no effect on heart rate during rest or exercise (ACSM 2013)
    • A heart rate increase may be seen (ACSM 2013)
      • The effect may become attenuated after continued use
• Blood Pressure
  • Small yet significant increase of systolic blood pressure (0.99 mm Hg) (Solemo 2005)
  • Non-significant increase of Diastolic blood pressure (0.63 mm Hg) (Solemo 2005)
  • Generally no effect on blood pressure during rest or exercise (ACSM 2013)
    • Increase in Systolic blood pressure may be seen (ACSM 2013)
      • The effect may become attenuated after continued use.
  1. May produce premature ventricular contractions (PVC) (ACSM 2013)
  2. No change in performance (ACSM 2013)

Populations Not Recommend

• Pregnant women
• Diabetes mellitus
• Cardiovascular disease
• Severe or uncontrolled hypertension
• Severe coronary artery disease
• Prostatic hypertrophy
• Hyperthyroidism
• Closed-angle glaucoma

Banned Status

• Banned by World Anti-doping Agency
• Permitted under NCAA

References

American College of Sports Medicine (2013). Guidelines for Exercise Testing and Prescription, William & Wilkins, 9, 401.

Jones & Barlett (2011) Nurse's Handbook of Combination Drugs, Jones & Bartlett Publishers, 10th Edition.

Livingston MG. (1995). Interactions with selective MAOIs. Lancet, 345(8952):804.

Lucarotti RL, Colaizz JL, Barry H, Paust RI (1972). Enhanced pseudoephedrine absorption by concurrent administration of aluminum hydroxide gel in humans. Journal of Pharmaceutical Science, 61(6), 903–905.

PDR Staff (2005). Physicians' Desk Reference Companion Guide. 59th Edition. Pg 61.

Salerno SM1, Jackson JL, Berbano EP. (2005). Effect of oral pseudoephedrine on blood pressure and heart rate: a meta-analysis. Arch Intern Med. 165(15):1686-94.