Phenylephrine Monograph

Pharmacologic Category
Alpha-Adrenergic Agonist

Dosing:
Ocular procedures Instill 1 drop of 2.5% solution and repeat 10-60 minutes as needed or OTC 1-2 drops of 0.12% solution 4 times a day Hypotension/shock: I.V. bolus: 100-500 mcg/dose every 10-15 minutes as needed (initial dose should not exceed 500 mcg) I.V. infusion: Initial dose: 100-180 mcg/minute. Nasal congestion: Oral: 10 mg every 4 hours as needed for 7 days (maximum: 60 mg/24 hours)

Use\ Indications:
As mydriatic, in treatment of glaucoma; eye irritation, hypotension, vascular failure in shock; as a vasoconstrictor in regional analgesia; supraventricular tachycardia (Note: Not for routine use in treatment of supraventricular tachycardias); as a decongestant [OTC]

Contraindications
Hypersensitivity to phenylephrine or any component of the formulation; hypertension; ventricular tachycardia; narrow-angle glaucoma

Warnings/Precautions:
Notify healthcare provider if symptoms do not improve within 3 days (for ophthalmic preparation) 7 days (for systemic preparation) or are accompanied by fever, vision changes, and redness of the eye. Sulfites: Some products contain sulfites which may cause allergic reactions in susceptible individuals. In patients with heart failure or cardiogenic shock, asthma, hyperthyroidism, diabetes mellitus, cardiovascular disease, ischemic heart disease, hypertension, increased intraocular pressure, prostatic hyperplasia or in the elderly. Discontinue and contact healthcare provider if nervousness, dizziness, or sleeplessness occur. Sympathomimetics, AtoMOXetine (for ADHD); Ergot Derivatives (for migraine), MAO Inhibitors (for depression); Tricyclic Antidepressants, Iobenguane I-123 (radiolabeled molecule similar to noradrenaline)

Drug Interactions

Mechanism of Action
Potent, direct-acting alpha-adrenergic agonist is linked with Gq-protien which activates IP3 signal transduction pathway in smooth muscles and produces local vasoconstriction. Such increases in systemic vascular resistance result in dose dependent increases in systolic and diastolic blood pressure

Pharmacodynamics/Kinetics
Ophthalmic: Rapid Onset of action causing Mydriasis and duration of action is long (40-50mins approx.) Absorption: Minimal systemic absorption Systemic: Onset of action: I.M., SubQ: 10-15 minutes; I.V.: Immediate Oral: 15-30 minutes Duration: I.M.: 1-2 hours; I.V.: ~15-20 minutes; SubQ: 50 minutes Oral: 4 hours Absorption: Oral: Rapid and complete Metabolism: Hepatic via oxidative deamination Undergoes sulfation and some glucuronidation; forms inactive metabolites Excretion: Urine (mostly as inactive metabolites)

Adverse Reactions
Cardiovascular: Arrhythmia (rare), hypertension, myocardial infarction (rare), subarachnoid hemorrhage (rare), syncope (rare) decreased cardiac output, hypertension, discomfort, bradycardia, severe peripheral and visceral vasoconstriction Ocular: Burning, irritation, vision changes, rebound miosis, floaters (transient) Endocrine & metabolic: Metabolic acidosis Gastrointestinal: Gastric irritation, nausea Neuromuscular & skeletal: tremor, weakness Renal: Decreased renal perfusion, reduced urine output Respiratory: Respiratory distress Central nervous system: Anxiety, dizziness, excitability, headache, insomnia, nervousness, restlessness Brand Names Sudafed PE Neo-Synephrine Vicks Sinex Albalon Relief