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Acetaminophen and phenylephrine: Drug information

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Acetaminophen and phenylephrine: Drug information
Copyright 1978-2011 Lexicomp, Inc. All rights reserved.

(For additional information see “Acetaminophen and phenylephrine: Patient drug information”)

Brand Names: U.S.

  • Alka-Seltzer Plus® Sinus Formula [OTC];
  • Cetafen Cold® [OTC];
  • Contac® Cold + Flu Maximum Strength Non-Drowsy [OTC];
  • Excedrin® Sinus Headache [OTC];
  • Mapap® Sinus Congestion and Pain Daytime [OTC];
  • Sinus Pain & Pressure [OTC];
  • Sinutab® Sinus [OTC];
  • Sudafed PE® Pressure + Pain [OTC];
  • Tylenol® Sinus Congestion & Pain Daytime [OTC];
  • Vicks® DayQuil® Sinus [OTC]
Pharmacologic Category

  • Analgesic, Miscellaneous;
  • Decongestant
Dosing: AdultSinus pain/pressure: Oral: General dosing guidelines, refer to specific product labeling: Acetaminophen 325 mg and phenylephrine 5 mg/caplet: Take 2 caplets every 4 hours as needed; maximum: 12 caplets/24 hours

Dosing: PediatricChildren ≥12 years: Refer to adult dosing.

Dosing: GeriatricRefer to adult dosing.

Dosage Forms: U.S.Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Caplet, oral:

Contac® Cold + Flu Maximum Strength Non Drowsy: Acetaminophen 500 mg and phenylephrine hydrochloride 5 mg

Excedrin® Sinus Headache: Acetaminophen 325 mg and phenylephrine hydrochloride 5 mg

Mapap® Sinus Congestion and Pain Daytime, Sinutab® Sinus, Sudafed PE® Pressure + Pain: Acetaminophen 325 mg and phenylephrine hydrochloride 5 mg

Tylenol® Sinus Congestion & Pain Daytime: Acetaminophen 325 mg and phenylephrine hydrochloride 5 mg [Cool Burst™ flavor]

Capsule, liquicap, oral:

Vicks® DayQuil® Sinus: Acetaminophen 325 mg and phenylephrine hydrochloride 5 mg [ethanol free]

Gelcap, oral:

Tylenol® Sinus Congestion & Pain Daytime: Acetaminophen 325 mg and phenylephrine hydrochloride 5 mg

Gelcap, rapid release, oral:

Tylenol® Sinus Congestion & Pain Datyime: Acetaminophen 325 mg and phenylephrine hydrochloride 5 mg

Tablet for solution, oral [effervescent]:

Alka-Seltzer Plus® Sinus Formula: Acetaminophen 250 mg and phenylephrine hydrochloride 5 mg [contains sodium 477 mg/tablet and phenylalanine 4.2 mg/tablet; lemon zest flavor]

Tablet, oral:

Cetafen Cold®: Acetaminophen 500 mg and phenylephrine hydrochloride 5 mg

Sinus Pain & Pressure: Acetaminophen 500 mg and phenylephrine hydrochloride 5 mg

Generic Equivalent Available: U.S.Yes: Caplet

AdministrationCaplets and gelcaps should be swallowed whole; do not crush, chew, or dissolve. Effervescent tablets should be dissolved in 4 ounces of water.

UseTemporary relief of sinus/nasal congestion and pressure, headache, and minor aches and pains

Adverse Reactions SignificantSee individual agents.

ContraindicationsHypersensitivity to acetaminophen, phenylephrine, or any component of the formulation; with or within 14 days of MAO inhibitor therapy

Warnings/Precautions Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with cardiovascular disease (including hypertension and ischemic heart disease).

• Diabetes: Use with caution in patients with diabetes mellitus.

• Ethanol use: Use with caution in patients with alcoholic liver disease; consuming ≥3 alcoholic drinks/day may increase the risk of liver damage.

• Hepatic impairment: Use caution in patients with hepatic impairment; acetaminophen may cause severe hepatic toxicity with acute overdose.

• Prostatic hyperplasia/urinary obstruction: Use with caution in patients with prostatic hyperplasia and/or GU obstruction.

• Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.

Special populations:

• Elderly: Use with caution in the elderly; more likely to experience adverse reactions to sympathomimetics.

• Pediatrics: Use with caution in children; do not exceed pediatric dosing recommendations. Not for OTC use in children <12 years of age.

Dosage form specific issues:

• Phenylalanine: Some products may contain phenylalanine.

• Sodium: Some products may contain sodium; use with caution in sodium restricted patients.

Other warnings/precautions:

• Dosage limit: Limit acetaminophen dose to <4 g/day.

• Self-medication (OTC use): When used for self-medication (OTC), notify healthcare provider if symptoms do not improve within 7 days or are accompanied by fever lasting >3 days. Discontinue and contact healthcare provider if nervousness, dizziness, or sleeplessness occur.

Metabolism/Transport EffectsAcetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)

Drug Interactions

(For additional information: Launch Lexi-Interact™ Drug Interactions Program )

Anticonvulsants (Hydantoin): May increase the metabolism of Acetaminophen. This may 1) diminish the effect of acetaminophen; and 2) increase the risk of liver damage. Risk C: Monitor therapy

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

Barbiturates: May increase the metabolism of Acetaminophen. This may 1) diminish the effect of acetaminophen; and 2) increase the risk of liver damage. Risk C: Monitor therapy

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Benzylpenicilloyl Polylysine: Alpha1-Agonists may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Consider use of a histamine skin test as a positive control to assess a patient’s ability to mount a wheal and flare response. Risk D: Consider therapy modification

Cannabinoids: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy

CarBAMazepine: May increase the metabolism of Acetaminophen. This may 1) diminish the effect of acetaminophen; and 2) increase the risk of liver damage. Risk C: Monitor therapy

Cholestyramine Resin: May decrease the absorption of Acetaminophen. Effect is minimal if cholestyramine is administered 1 hour after acetaminophen. Risk D: Consider therapy modification

Conivaptan: May increase the serum concentration of CYP3A4 Substrates (Low risk). Risk C: Monitor therapy

Cyproterone: May decrease the serum concentration of CYP1A2 Substrates. Risk C: Monitor therapy

Cyproterone: May decrease the serum concentration of CYP2E1 Substrates. Risk C: Monitor therapy

Dasatinib: Acetaminophen may enhance the hepatotoxic effect of Dasatinib. Dasatinib may increase the serum concentration of Acetaminophen. Risk D: Consider therapy modification

FentaNYL: Alpha1-Agonists may decrease the serum concentration of FentaNYL. Specifically, fentanyl nasal spray serum concentrations may decrease and onset of effect may be delayed. Risk C: Monitor therapy

Imatinib: Acetaminophen may enhance the hepatotoxic effect of Imatinib. Imatinib may increase the serum concentration of Acetaminophen. Risk D: Consider therapy modification

Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Risk X: Avoid combination

Isoniazid: May enhance the adverse/toxic effect of Acetaminophen. Risk C: Monitor therapy

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

Metyrapone: May increase the serum concentration of Acetaminophen. More importantly, by inhibiting the conjugative metabolism of acetaminophen, metyrapone may shift the metabolism towards the oxidative route that produces a hepatotoxic metabolite. Risk C: Monitor therapy

Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates. Risk C: Monitor therapy

Probenecid: May increase the serum concentration of Acetaminophen. Probenecid may also limit the formation of at least one major non-toxic metabolite, possibly increasing the potential for formation of the toxic NAPQI metabolite. Risk D: Consider therapy modification

SORAfenib: Acetaminophen may enhance the hepatotoxic effect of SORAfenib. SORAfenib may increase the serum concentration of Acetaminophen. Risk D: Consider therapy modification

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

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy

Tricyclic Antidepressants: May enhance the vasopressor effect of Alpha1-Agonists. Risk D: Consider therapy modification

Vitamin K Antagonists (eg, warfarin): Acetaminophen may enhance the anticoagulant effect of Vitamin K Antagonists. Most likely with daily acetaminophen doses >1.3 g for >1 week. Risk C: Monitor therapy

Ethanol/Nutrition/Herb InteractionsSee individual agents.

Dietary ConsiderationsSome propducts may contain phenylalanine and/or sodium.

Mechanism of ActionAcetaminophen inhibits the synthesis of prostaglandins in the central nervous system and peripherally blocks pain impulse generation. Phenylephrine causes vasoconstriction of the arterioles of the nasal mucosa.

Pharmacodynamics/KineticsSee individual agents.

REFERENCES

  1. Antlitz AM, Mead JA Jr, and Tolentino MA, “Potentiation of Oral Anticoagulant Therapy by Acetaminophen,” Curr Ther Res Clin Exp, 1968, 10(10):501-7. [PubMed 4971464]
  2. Bagheri H, Bernhard NB, and Montastruc JL, “Potentiation of the Acenocoumarol Anticoagulant Effect by Acetaminophen,” Ann Pharmacother, 1999, 33(4):506. [PubMed 10332548]
  3. Bartle WR and Blakely JA, “Potentiation of Warfarin Anticoagulation by Acetaminophen,” JAMA, 1991, 265(10):1260. [PubMed 1995971]
  4. Boeijinga JJ, Boerstra EE, Ris P, et al, “Interaction Between Paracetamol and Coumarin Anticoagulants,” Lancet, 1982, 1(8270):506. [PubMed 6121161]
  5. Gadisseur AP, Van Der Meer FJ, and Rosendaal FR, “Sustained Intake of Paracetamol (Acetaminophen) During Oral Anticoagulant Therapy With Coumarins Does Not Cause Clinically Important INR Changes: A Randomized Double-Blind Clinical Trial,” J Thromb Haemost, 2003, 1(4):714-7. [PubMed 12871405]
  6. Gebauer MG, Nyfort-Hansen K, Henschke PJ, et al, “Warfarin and Acetaminophen Interaction,” Pharmacotherapy, 2003, 23(1):109-12. [PubMed 12523469]
  7. Hylek EM, Heiman H, Skates SJ, et al, “Acetaminophen and Other Risk Factors for Excessive Warfarin Anticoagulation,” JAMA, 1998, 279(9):657-62. [PubMed 9496982]
  8. Kwan D, Bartle WR, and Walker SE, “The Effects of Acute and Chronic Acetaminophen Dosing on the Pharmacodynamics and Pharmacokinetics of (R)- and (S)-Warfarin,” Clin Pharmacol Ther, 1995, 57:212.
  9. Rubin RN, Mentzer RL, and Budzynski AZ, “Potentiation of Anticoagulant Effect of Warfarin by Acetaminophen (Tylenol®),” Clin Res, 1984, 32:698a.
  10. van den Bemt PM, Geven LM, Kuitert NA, et al, “The Potential Interaction Between Oral Anticoagulants and Acetaminophen in Everyday Practice,” Pharm World Sci, 2002, 24(5):201-4. [PubMed 12426965]
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