Propylhexedrine

Class: Vasoconstrictors
ATC Class: R03AA01
VA Class: RE102
Chemical Name: N,α-dimethyl-cyclohexylethylamine
Molecular Formula: C10 H21 N
CAS Number: 101-40-6
Brands: Benzedrex

Introduction

Vasoconstrictor, an aliphatic amine.a

Uses for Propylhexedrine

Nasal Congestion

Self-medication for temporary relief of nasal congestion associated with the common cold, hay fever, or other allergies.101 a b

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As effective as other topical vasoconstrictors.a

Topical nasal decongestants often preferred for short-term treatment; oral agents preferred for prolonged treatment.a (See Overuse under Cautions.)

Reduce swelling and facilitate visualization of nasal and pharyngeal membranes prior to surgery or diagnostic procedures.a

Open obstructed eustachian ostia in patients with ear inflammation.a

Propylhexedrine Dosage and Administration

Administration

Intranasal Administration

Administer topically to the nasal mucosa as an inhalation.a b

Avoid contamination of the inhaler tip; inhaler is for single-patient use only.a b

Warm drug container in the hands prior to use to increase drug volatility.a

Inhale vapor through each nostril while head is erect; blow nose thoroughly after 3–5 minutes.a

Supervise use by children 6–12 years of age.b

Dosage

The Benzedrex propylhexedrine inhaler delivers 0.4–0.5 mg of the drug in each 800 mL of air.b

Pediatric Patients

Nasal Congestion
Intranasal

Children ≥6 years of age: 2 inhalations (0.4–0.5 mg) in each nostril no more than every 2 hours.a b

If symptoms are not improved after 3 consecutive days, consult a clinician.a b (See Overuse under Cautions.)

Adults

Nasal Congestion
Intranasal

2 inhalations (0.4–0.5 mg) in each nostril no more than every 2 hours.a b

If symptoms are not improved after 3 consecutive days, consult a clinician.a b (See Overuse under Cautions.)

Prescribing Limits

Pediatric Patients

Nasal Congestion
Intranasal

Children ≥6 years of age: Maximum of every 2 hours; maximum duration of 3 consecutive days.a b

Adults

Nasal Congestion
Intranasal

Maximum of every 2 hours; maximum duration of 3 consecutive days.a b

Special Populations

No special populations dosage recommendations at this time.a b

Cautions for Propylhexedrine

Warnings/Precautions

General Precautions

Overuse

Possible irritation of nasal mucosa and adverse systemic effects (particularly in children) with excessive dosage and/or prolonged or too frequent use.a Possible rebound congestion (rhinitis, chronic redness and swelling of the nasal mucosa); avoid prolonged use.a b (See Advice to Patients.)

Overdosage following oral ingestion may result in psychotic reactions, palpitation, ventricular extrasystoles, and shock.a

Sympathomimetic Effects

Possible headache, hypertension, nervousness, and increased ventricular rate.a Use with caution in patients with thyroid disease (e.g., hyperthyroidism), heart disease, hypertension, or diabetes mellitus.a

Specific Populations

Pregnancy

Safety during pregnancy not established.a

Pediatric Use

Safety and efficacy not established in children <6 years of age.a b

Possible irritation of nasal mucosa and adverse systemic effects associated with excessive dosage, prolonged or too frequent use, or inadvertent ingestion of nasal solution.a

Common Adverse Effects

Burning, stinging, sneezing, increase in nasal discharge. a b

Interactions for Propylhexedrine

Specific Drugs

Drug

Interaction

Comments

MAO inhibitors

Potential for enhanced sympathomimetic effects a

Interaction unlikely; however, use concomitantly with cautiona

Propylhexedrine Pharmacokinetics

Absorption

Bioavailability

Occasionally, absorption may be sufficient to produce systemic effects.a

Onset

Following intranasal administration, local vasoconstriction usually occurs within 0.5–5 minutes.a

Duration

Following intranasal administration, local vasoconstriction persists for 30–120 minutes.a

Elimination

Metabolism

Metabolized in the liver.a

Elimination Route

Excreted in urine as unchanged drug and metabolites.a

Stability

Storage

Intranasal

Inhaler

Tight container at 15–30°C.b Avoid excessive heat.a

Inhaler remains potent for 2–3 months after first use, depending on the degree of use.a b

Actions

  • Structurally and pharmacologically related to amphetamine.a

  • Exact mechanism of action unknown but thought to be similar to amphetamine.a

  • Indirectly stimulates α-adrenergic receptors of the sympathetic nervous system; exerts a minor stimulant effect on β-adrenergic receptors.a

  • Intranasal application constricts dilated arterioles, reduces nasal blood flow and congestion, and may open obstructed eustachian ostia.a Temporarily improves nasal ventilation and aeration.a

Advice to Patients

  • Importance of replacing or discarding inhaler 2–3 months after first use.a b

  • Importance of discontinuing drug and consulting a clinician if nasal congestion worsens or persists for >3 days.a b

  • 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.a b

  • Importance of avoiding contamination of the inhaler.a b To minimize risk of spreading infections, do not share inhaler with other individuals.a b

  • Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed.a

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.a

  • Importance of informing patients of other important precautionary information.a (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Propylhexedrine

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Nasal

Inhalant

250 mg

Benzedrex Inhaler

Ascher

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions June 1, 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

Only references cited for selected revisions after 1984 are available electronically.

101. Food and Drug Administration. Cold, cough, allergy, bronchodilator, and antiasthmatic drug products for over-the-counter human use; amendment of final monograph for over-the-counter nasal decongestant drug products. 21 CFR Parts 310 and 341. Final rule. [Docket No. 2004N- 0289] Fed Regist. 2005; 70:58974-7.

102. Spector SL, Bernstein IL, Li JT et al for the Joint Task Force on Practice Parameters et al. Parameters for the diagnosis and management of sinusitis. J Allergy Clin Immunol. 1998; 102(Suppl):S107-44.

103. American Academy of Pediatrics: subcommittee on management of sinusitis and committee on quality improvement. Clinical practice guideline: Management of sinusitis. Pediatrics. 2001; 108:798-808. [PubMed 11533355]

a. AHFS drug information 2007. McEvoy GK, ed. Propylhexedrine. Bethesda, MD: American Society of Health-Systems Pharmacists; 2007:2867.

b. B.F. Ascher Pharmaceuticals. Benzedrex (propylhexedrine) inhaler patient information. Lenaxa, KS. Available at: . Accessed 2008 Mar 5.

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