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phenylephrine (Neo-Synephrine, Mydrifin, sudafed PE, PE)

Tradename: Neo-Synephrine, sudafed PE [6]. Indications: 1) oral agent (OTC oral phenylephrine to be removed from U.S. market [2] - treatment of vascular failure in shock syndromes (hypotension) including hypertrophic cardiomyopathy [8] - vasoconstriction to allow for regional spinal anesthesia - paroxysmal supraventricular tachycardia (PSVT) uncontrolled by standard therapy - decongestant for eustachian tube congestion 2) topical agent - hemorrhoids, rectal pain, proctitis, anal pruritus 3) nasal spray - symptomatic relief from cold symptoms* - nasal congestion, rhinitis, rhinorrhea, sneezing, cough - allergic rhinitis* - seasonal allergic rhinitis 3) ophthalmic agent: - mydriasis in ophthalmic procedures - treatment of glaucoma (wide-angle) secondary to pupil block caused by aphakia or posterior synechiae - prevention of echothiophosphate-induced iris cysts - determination of refraction errors - diagnosis of Horner's & Raeder's syndromes - prevention & treatment of posterior synechiae in patients with anterior uveitis - allergic conjunctivitis * on list of medications to avoid for treatment of allergic rhinitis & viral rhinitis [11] - cardiovascular risk cited Contraindications: narrow-angle glaucoma Dosage: 1) hypotension a) adults - 2-5 mg SC every 1-2 hours PRN - 0.1-0.5 mg IV every 10-15 min PRN - 100-200 ug IV for severe hypotension - IV infusion: 0.1-0.5 ug/kg/min - infusion: 20 mg in 250 mL D5W (80 ug/mL) at 40-180 ug/min or 1-3 ug/kg/min (35-160 mL/hr) b) children - 0.1 mg/kg SC every 1-2 hours PRN; max 5 mg/dose - 5-20 ug/kg IV every 10-15 min PRN - IV infusion: - mix 10 mL in 250 mL of D5W or normal saline (40 ug/mL) - start at 100-180 ug/min (2-5 mL/min) - maintenance (after blood pressure has stabilized) 40-60 ug/min (0.8-1.2 mL/min) 2) PSVT: 0.25-0.5 mg over 20-30 seconds 3) nasal congestion: 2-3 sprays per nostril every 3-4 hours 4) Oral decongestant: 10 mg every 4 hours PRN (Sudafed PE) [6] 5) ophthalmic agent a) ophthalmoscopy & retinal photography: - 1 drop - may repeat as needed in 10-60 minutes b) refraction: - instill 1 drop of 2.5% solution in between the administration of a cycloplegic drug c) diagnosis of Horner's & Raeder's syndromes - use appropriate concentration to perform testing d) ocular surgery: - 1-2 drops into the eye 30-60 minutes before surgery - usually used in conjunction with another mydriatic agent (i.e. atropine) - 1 drop of 10% solution into the eye TID along with atropine e) glaucoma secondary to pupil block: - 1 drop of 10% solution into the eye TID along with atropine for synergistic effect - may be given QID if needed - apply finger pressure to the lacrimal sac during & for 1-2 minutes following application to reduce frequency of systemic adverse effects f) mydriasis: 1 drop QD-TID for 5 days Nasal spray: 0.125%, 0.25%, 0.5%, 1%. Ophthalmic agent: Tradenames: Neo-synephrine, Mydrifin. Ophthalmic agent: 2.5% (15 mL) 10% (5 mL). Injection: 10 mg/mL (1 mL). Pharmacokinetics: 1) topical (intraocular, nasal) administration a) onset of action within minutes b) duration of action is 0.5 to 4 hours 2) IV administration a) immediate onset of action b) duration of action is 20-50 minutes c) metabolized by monoamine oxidase (MAO) Adverse effects: 1) Nasal a) common (> 10%) - nasal burning - rebound congestion (after 3-10 days) - sneezing b) less common (1-10%) - stinging, dryness 2) Ophthalmic a) common (> 10%) - transient stinging b) less common (1-10%) - headache, blurred vision, photophobia, lacrimation, browache 3) Systemic a) common (> 10%) - tremor b) less common (1-10%) - peripheral vasoconstriction, hypertension, angina, reflex bradycardia, arrhythmias, restlessness, excitability 4) other [3,4] - insomnia - tachycardia - headache - blurred vision Drug interactions: 1) alpha-adrenergic receptor antagonists antagonize effects of phenylephrine 2) tricyclic antidepressants & MAO inhibitors increase the pressor effects of phenylephrine 3) acetaminophen may increase plasma levels of phenylephrine Mechanism of action: 1) alpha-1 adrenergic receptor agonist [8] 2) potent vasoconstriction 3) dose-related increase in peripheral vascular resistance 4) elevation of blood pressure 5) sinus bradycardia associated with vagal reflexes 6) topical administration results in arteriole constriction 7) reduction in blood flow & nasal congestion * NOT as effective of pseudoephedrine [7] * NOT effective [12]

Interactions

drug interactions drug adverse effects (more general classes)

General

alpha-1 adrenergic receptor agonist mydriatic agent vasoconstrictor agent or vasopressor

Properties

AGONIST-FOR: alpha-1 adrenergic receptor MISC-INFO: elimination route PLASMA pregnancy-category C safety in lactation - ? ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Faga LJ, American Family Physician 58:1795-1802, 1998
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Mangione CM, In: UCLA Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 12-15, 2001
  6. Prescriber's Letter 12(3): 2005 Sudafed PE Nasal Decongestant Detail-Document#: 210310 (subscription needed) http://www.prescribersletter.com
  7. Prescriber's Letter 13(12): 2006 Changes to OTC cough and Cold products Detail-Document#: 221207 (subscription needed) http://www.prescribersletter.com
  8. Medical Knowledge Self Assessment Program (MKSAP) 16, 17. American College of Physicians, Philadelphia 2012, 2015
  9. Deprecated Reference
  10. Atkinson HC et al Increased Phenylephrine Plasma Levels with Administration of Acetaminophen. N Engl J Med 2014; 370:1171-1172March 20, 2014 PMID: 24645960 http://www.nejm.org/doi/full/10.1056/NEJMc1313942
  11. Therapeutics Letter #108. Therapeutics Initiative Drugs to Avoid. http://www.ti.ubc.ca/2018/01/04/108-drugs-avoid/
  12. DePeau-Wilson M FDA Plans to Ban Popular Cold Med. Data review shows that oral phenylephrine is not effective as a decongestant, agency says. MedPage Today November 7, 2024 https://www.medpagetoday.com/publichealthpolicy/fdageneral/112779

Component-of

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chlorpheniramine/phenylephrine/phenylpropanolamine/phenyltoloxamine (Naldecon, Naldelate, Par Decon) chlorpheniramine/phenylephrine/phenyltoloxamine chlorpheniramine/phenylephrine/pyrilamine (Triotann) chlorpheniramine/phenylephrine/scopolamine citrate/guaifenesin/phenylephrine cocoa butter/phenylephrine cocoa butter/phenylephrine/shark liver oil codeine/dexchlorpheniramine/phenylephrine codeine/dexchlorpheniramine/phenylephrine/phosphate codeine/diphenhydramine/phenylephrine codeine/diphenhydramine/phenylephrine/phosphate codeine/guaifenesin/phenylephrine codeine/guaifenesin/phenylephrine/phosphate codeine/phenylephrine codeine/phenylephrine/phosphate codeine/phenylephrine/phosphate/promethazine codeine/phenylephrine/phosphate/pyrilamine codeine/phenylephrine/promethazine (Phenergan with phenylephrine & codeine) codeine/phenylephrine/pyrilamine codeine/phenylephrine/triprolidine cyclopentolate/phenylephrine (Cyclomydril) dexbrompheniramine/dextromethorphan/guaifenesin/phenylephrine 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