Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Ointment, Rectal, as hydrochloride:
GRX Hemorrhoidal: 0.25% (43 g) [contains benzoic acid, methylparaben, propylparaben]
Hemorrhoidal: 0.25% (56 g) [contains benzoic acid, cetyl alcohol, methylparaben, propylparaben]
Hemorrhoidal: 0.25% (57 g) [contains benzoic acid, methylparaben, propylparaben]
Major-Prep Hemorrhoidal: 0.25% (57 g) [contains benzoic acid, methylparaben, propylparaben]
Major-Prep Hemorrhoidal: 0.25% (57 g [DSC]) [contains methylparaben, propylparaben]
Preparation H: 0.25% (28 g, 57 g) [contains benzoic acid, methylparaben, propylparaben]
Suppository, Rectal, as hydrochloride:
Anu-Med: 0.25% (12 ea [DSC])
GoodSense Hemorrhoidal: 0.25% (12 ea) [contains methylparaben, propylparaben]
Hemorrhoidal: 0.25% (12 ea) [contains corn starch, methylparaben, propylparaben]
Hemorrhoidal: 0.25% (12 ea, 24 ea) [contains methylparaben, propylparaben]
Preparation H: 0.25% (12 ea, 24 ea, 48 ea) [contains corn starch, methylparaben, propylparaben]
Rectacaine: 0.25% (12 ea)
Pharmacology
Mechanism of Action
Potent, direct-acting alpha-adrenergic agonist with virtually no beta-adrenergic activity; produces local vasoconstriction.
Use: Labeled Indications
For OTC use as treatment of hemorrhoids
Contraindications
Hypersensitivity to phenylephrine or any component of the formulation; hypertension; ventricular tachycardia
Dosage and Administration
Dosing: Adult
Hemorrhoids: Rectal:
Ointment: Apply to clean, dry area up to 4 times/day
Suppository: Insert 1 suppository rectally up to 4 times/day
Dosing: Geriatric
Refer to adult dosing.
Dosing: Pediatric
Hemorrhoids, anorectal protection: Children ≥12 years and Adolescents:
Ointment: Topical or rectal: Apply to rectal area or by applicator into rectum up to 4 times daily (eg, morning, night, and after bowel movements)
Suppository: Rectal: Insert 1 suppository into rectum up to 4 times daily (eg, morning, night, and after bowel movements)
Drug Interactions
Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha1-Agonists. Similarly, Alpha1-Agonists may antagonize Alpha1-Blocker vasodilation. Monitor therapy
AtoMOXetine: May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. Monitor therapy
Cocaine (Topical): May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Consider therapy modification
Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Monitor therapy
Ergot Derivatives: May enhance the hypertensive effect of Alpha1-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha1-Agonists. Exceptions: Ergoloid Mesylates; Nicergoline. Avoid combination
Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Monitor therapy
Iobenguane Radiopharmaceutical Products: Alpha1-Agonists may diminish the therapeutic effect of Iobenguane Radiopharmaceutical Products. Management: Discontinue all drugs that may inhibit or interfere with catecholamine transport or uptake for at least 5 biological half-lives before iobenguane administration. Do not administer these drugs until at least 7 days after each iobenguane dose. Avoid combination
Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in patients receiving linezolid. Specific dose adjustment recommendations are not presently available. Consider therapy modification
Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of Alpha1-Agonists. While linezolid is expected to interact via this mechanism, management recommendations differ from other monoamine oxidase inhibitors. Refer to linezolid specific monographs for details. Exceptions: Linezolid. Avoid combination
Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Tricyclic Antidepressants: May enhance the therapeutic effect of Alpha1-Agonists. Tricyclic Antidepressants may diminish the therapeutic effect of Alpha1-Agonists. Monitor therapy
Adverse Reactions
Rare systemic effects may occur.
Warnings/Precautions
Disease-related concerns:
- Cardiovascular disease, including ischemic heart disease: Use caution.
- Diabetes mellitus: Use caution.
- Hyperthyroidism: Use caution.
Special populations:
- Elderly: Use caution.
Other warnings/precautions:
- Use with caution in patients with increased intraocular pressure or prostatic hyperplasia. Notify healthcare provider if symptoms do not improve within 7 days or if bleeding occurs.
Pregnancy
Pregnancy Considerations
When administered intravenously, phenylephrine crosses the placenta. Refer to the Phenylephrine (Systemic) monograph for details. There is limited information available supporting the use of topical agents for the treatment of hemorrhoids. Products containing phenylephrine should be used with caution in pregnant women, especially patients with hypertension or diabetes.
Patient Education
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Have patient report immediately to prescriber rectal bleeding or rectal pain (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
