Drug information of Propylhexedrine

Propylhexedrine

Drug group:

Propylhexedrine is an alpha-adrenergic agonist often used in nasal decongestant inhalers. It is used to give temporary relief for nasal congestion from colds, allergic rhinitis, or allergies.

Mechanism of effect

Propylhexidrine causes the norepinephrine, dopamine, and serotonin (5HT) transporters to reverse their direction of flow. This inversion leads to a release of these transmitters from the vesicles to the cytoplasm and from the cytoplasm to the synapse. It also antagonizes the action of VMAT2, causing the release of more neurotransmitters.

Pharmacodynamic

Like other monoamine releasing stimulants propylhexedrine is active as a norepinephrine and dopamine releaser in the central nervous system. The acute effects of the drug closely resemble the physiological and psychological effects of an epinephrine-provoked fight-or-flight response, including increased heart rate and blood pressure, vasoconstriction (constriction of the arterial walls), bronchodilation, and hyperglycemia (increased blood sugar).

Pharmacokinetics

Absorption: Minimal systemic

Onset: 30 sec-5 min

Duration: 30 min-2 hr

Metabolism: Liver

Metabolites: Norpropylhexedrine, cyclohexylacetoxine, & 4-hydroxypropylhexedrine

Excretion: urine

Drug indications

nasal stuffiness

Dosage

Adult

Nasal Congestion

1-2 inhalations per nostril q2hr PRN; not to exceed 3 days

Pediatric

Nasal Congestion

<6 years: Not recommended

≥6 years: 1-2 inhalations per nostril q2hr PRN; not to exceed 3 days

Side effects

stinging , Rhinorrhea

Alerts

may be extracted & injected IV as amphetamine substitute by abusers: Potential for cardiomyopathy, dyspnea, death

Caution in cardiac disease (increase BP, HR, palpitations)

Points of recommendation

  • Importance of replacing or discarding inhaler 2–3 months after first use.
  • Importance of discontinuing drug and consulting a clinician if nasal congestion worsens or persists for >3 days.
  • Overuse of nasal inhaler may cause recurrence or exacerbation of nasal congestion; importance of not using more frequently than every 2 hours or for >3 days.
  • Importance of avoiding contamination of the inhaler. To minimize risk of spreading infections, do not share inhaler with other individuals.
  • Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed.
  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

Pregnancy level

Group c - Not adequate studies in pregnant women


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