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Phenylephrine (topical): Drug information

Phenylephrine (topical): Drug information
(For additional information see "Phenylephrine (topical): Patient drug information" and see "Phenylephrine (topical): Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Avedana Hemorrhoid Pain Relief [OTC];
  • Avedana Hemorrhoidal [OTC];
  • Avedana Hemorroidal Cooling [OTC];
  • GRX Hemorrhoidal [OTC] [DSC];
  • Hemorrhoidal Cooling [OTC];
  • Hemorrhoidal [OTC];
  • Major-Prep Hemorrhoidal [OTC] [DSC];
  • Preparation H [OTC]
Pharmacologic Category
  • Alpha-Adrenergic Agonist;
  • Antihemorrhoidal Agent
Dosing: Adult
Hemorrhoids, anorectal pain/itch

Hemorrhoids, anorectal pain/itch:

Note: Combine with dietary modifications, bowel hygiene, and warm sitz baths for best results (Ref). General dosing guidelines provided; refer to specific product labeling for dosing instructions.

Ointment: Topical, rectal: Apply to rectal area or by applicator into rectum, as needed, up to 4 times/day (eg, morning, night, after bowel movements).

Suppository: Rectal: Insert 1 suppository, as needed, up to 4 times/day (eg, morning, night, after bowel movements).

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric

(For additional information see "Phenylephrine (topical): Pediatric drug information")

Hemorrhoids, anorectal protection

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)

Adverse Reactions

Rare systemic effects may occur.

Warnings/Precautions

Other warnings/precautions:

• Self-medication (OTC use): For external use only. When used for self-medication (OTC), notify health care provider prior to use if you have diabetes, heart disease, high BP, thyroid disease, difficultly in urination due to enlargement of the prostate gland, or are currently taking medications for high BP or depression. Discontinue use and notify health care provider if condition worsens or does not improve within 7 days or if bleeding occurs; or if introduction of applicator into rectum causes additional pain.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Gel, External, as hydrochloride:

Avedana Hemorroidal Cooling: 0.25% (25.5 g) [contains edetate (edta) disodium, methylparaben, polysorbate 80, propylene glycol, propylparaben]

Hemorrhoidal Cooling: 0.25% (51 g) [contains methylparaben, polysorbate 80, propylene glycol, propylparaben]

Preparation H: 0.25% (26 g, 51 g) [contains edetate (edta) disodium, methylparaben, polysorbate 80, propylene glycol, propylparaben]

Ointment, Rectal, as hydrochloride:

Avedana Hemorrhoid Pain Relief: 0.25% (57 g) [contains benzoic acid, corn oil, methylparaben, propylparaben]

GRX Hemorrhoidal: 0.25% (43 g [DSC]) [contains benzoic acid, methylparaben, propylparaben]

Hemorrhoidal: 0.25% (56 g, 57 g) [contains benzoic acid, cetyl alcohol, methylparaben, propylparaben]

Hemorrhoidal: 0.25% (56 g, 57 g) [contains benzoic acid, methylparaben, propylparaben]

Major-Prep Hemorrhoidal: 0.25% (57 g [DSC]) [contains benzoic acid, methylparaben, propylparaben]

Preparation H: 0.25% (28 g, 57 g) [contains benzoic acid, methylparaben, propylparaben]

Suppository, Rectal, as hydrochloride:

Avedana Hemorrhoidal: 0.25% (12 ea, 24 ea) [contains corn starch, 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 methylparaben, propylparaben]

Preparation H: 0.25% (12 ea, 24 ea, 48 ea) [contains corn starch, methylparaben, propylparaben]

Generic Equivalent Available: US

Yes

Pricing: US

Gel (Avedana Hemorroidal Cooling External)

0.25-50% (per gram): $0.10

Gel (Preparation H External)

0.25-50% (per gram): $0.23

Ointment (Avedana Hemorrhoid Pain Relief Rectal)

0.25-14-74.9% (per gram): $0.05

Ointment (Preparation H Rectal)

0.25-14-74.9% (per gram): $0.20

Suppository (Avedana Hemorrhoidal Rectal)

0.25-88.44% (per each): $0.31

Suppository (Preparation H Rectal)

0.25% (per each): $0.65

0.25-88.44% (per each): $0.44

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Ointment: Topical or rectal: For external and/or intrarectal use only. Prior to application, cleanse affected area by patting or blotting with appropriate cleansing wipe; gently dry by patting with a tissue or soft cloth prior to use. When using applicator for intrarectal use, remove protective cover from applicator and attach to tube. Lubricate applicator well, then gently insert into rectum. Thoroughly cleanse applicator after each use and replace protective cover.

Suppository: For rectal use only. Prior to use, cleanse affected area by patting or blotting with appropriate cleansing wipe; gently dry by patting with a tissue or soft cloth prior to insertion. Remove foil wrapper.

Administration: Pediatric

Ointment: Topical or rectal: For external and/or intrarectal use only. Prior to application, cleanse affected area by patting or blotting with appropriate cleansing wipe. Apply ointment to clean and dry rectal area at night, in the morning, and/or after each bowel movement (up to 4 times daily). When using applicator for intrarectal use, remove protective cover from applicator and attach to tube. Lubricate applicator well, then gently insert into rectum. Thoroughly cleanse applicator after each use and replace protective cover.

Suppository: For rectal use only. Cleanse affected area by patting or blotting with appropriate cleansing wipe; gently dry by patting with a tissue or soft cloth prior to insertion. Remove foil wrapper. Insert into rectum at night, in the morning, and/or after each bowel movement (up to 4 times daily).

Use: Labeled Indications

Hemorrhoids, anorectal pain/itch: Temporary relief of burning, local itching, and discomfort associated with hemorrhoids.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha1-Agonists. Similarly, Alpha1-Agonists may antagonize Alpha1-Blocker vasodilation. Risk C: Monitor therapy

Atomoxetine: May enhance the hypertensive effect of Sympathomimetics. Atomoxetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy

Atropine (Systemic): May enhance the hypertensive effect of Alpha1-Agonists. Risk C: Monitor therapy

Bromocriptine: May enhance the hypertensive effect of Alpha1-Agonists. Management: Consider alternatives to this combination when possible. If combined, monitor for hypertension and tachycardia, and do not coadminister these agents for more than 10 days. Risk D: Consider therapy modification

Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Risk C: 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. Risk D: Consider therapy modification

Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Risk C: Monitor therapy

Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): May enhance the vasoconstricting effect of Alpha1-Agonists. Risk X: Avoid combination

Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Risk C: 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. Risk X: Avoid combination

Kratom: May enhance the adverse/toxic effect of Sympathomimetics. Risk X: Avoid combination

Levothyroxine: May enhance the adverse/toxic effect of Sympathomimetics. Specifically, the risk of coronary insufficiency may be increased in patients with coronary artery disease. Levothyroxine may enhance the therapeutic effect of Sympathomimetics. Sympathomimetics may enhance the therapeutic effect of Levothyroxine. Risk C: Monitor therapy

Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Consider initial dose reductions of sympathomimetic agents, and closely monitor for enhanced blood pressure elevations, in patients receiving linezolid. Risk D: Consider therapy modification

Lisuride: May enhance the hypertensive effect of Alpha1-Agonists. Risk X: Avoid combination

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. Risk X: Avoid combination

Ozanimod: May enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy

Pergolide: May enhance the hypertensive effect of Alpha1-Agonists. Risk C: Monitor therapy

Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Sympathomimetics may enhance the tachycardic effect of Solriamfetol. Risk C: Monitor therapy

Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy

Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy

Tricyclic Antidepressants: May enhance the therapeutic effect of Alpha1-Agonists. Tricyclic Antidepressants may diminish the therapeutic effect of Alpha1-Agonists. Risk C: Monitor therapy

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.

Breastfeeding Considerations

It is not known if phenylephrine is excreted into breast milk.

Mechanism of Action

Potent, direct-acting alpha-adrenergic agonist with virtually no beta-adrenergic activity; produces local vasoconstriction.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AU) Australia: Neo synephrine;
  • (IT) Italy: Isonefrine;
  • (PR) Puerto Rico: Anu-med | Grx hemorrhoidal | Neo synephrine;
  • (RU) Russian Federation: Relief;
  • (ZA) South Africa: I-glo
  1. Brown S, Girling C, Thapa Magar H, et al. Guidelines, guidelines and more guidelines for haemorrhoid treatment: a review to sort the wheat from the chaff. Colorectal Dis. 2022;24(6):764-772. doi:10.1111/codi.16078 [PubMed 35119707]
  2. Davis BR, Lee-Kong SA, Migaly J, Feingold DL, Steele SR. The American Society of Colon and Rectal Surgeons clinical practice guidelines for the management of hemorrhoids. Dis Colon Rectum. 2018;61(3):284-292. doi:10.1097/DCR.0000000000001030 [PubMed 29420423]
  3. Preparation H ointment (phenylephrine topical) [prescribing information]. Madison, NJ: Pfizer; June 2019.
  4. Preparation H suppository (phenylephrine topical) [prescribing information]. Madison, NJ: Pfizer; received September 2019.
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