Description

Simple

A medication used to treat congestion and a runny nose.

Clinical

An alpha and beta adrenergic agonist used to treat nasal and sinus congestion, as well as allergic rhinitis.

Overview

Pseudoephedrine is structurally related to [ephedrine] but exerts a weaker effect on the sympathetic nervous system.[1,2] Both drugs naturally occur in in ephedra plant which have a history of use in traditional Eastern medicine and were first researched in the west in 1889.[2] The decongestant effect of pseudoephedrine was described in dogs in 1927.[2]

Pharmacology

Indication

Pseudoephedrine is a sympathomimetic amine used for its decongestant activity.[11, Read more

Pharmacodynamic

Pseudoephedrine causes vasoconstriction which leads to a decongestant effect.[2, Read more

Mechanism of action

Pseudoephedrine acts mainly as an agonist of alpha adrenergic receptors[6] and less stro... Read more

Absorption

A 240mg oral dose of pseudoephedrine reaches a Cmax of 246.3±10.5ng/mL fed and 272.5±13.4ng/mL fasted, with a Tmax of 6.60±1.38h fed and 11.87±0.72h fasted, with an AUC of 6862.0±334.1ng\*h/mL fed and 7535.1±333.0ng\*h/mL fasted.[ Read more

Protein binding

-pseudoephedrine is 6.6±0.4% bound to human serum albumin and 22.5±3.2% protein bound in serum.[ Read more

Volume of distribution

The apparent volume of distribution of pseudoephedrin is 2.6-3.3L/kg.[11]

Clearance

A 60mg oral dose of pseudoephedrine has a clearance of 5.9±1.7mL/min/kg.[13]

Half life

The mean elimination half life of pseudoephedrine is 6.0h.[11]

Route of elimination

55-75% of an oral dose is detected in the urine as unchanged pseudoephedrine.[13]

Toxicity

The oral LD50 of pseudoephedrine is 2206mg/kg in rats and 726mg/kg in mice.[13]

Patients experiencing an overdose of pseudoephedrine may prese... Read more

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Severe Hypertension
      • Drugbank Id: DBCOND0058109
      • Modification Of:
        • Base:
          • Name: Hypertension
          • Drugbank Id: DBCOND0020037
        • Severity:
          • Includes:
            • severe
  • Regions: US
  • Patient Conditions:
      • Name: Urinary Retention
      • Drugbank Id: DBCOND0001412
  • Regions: US
  • Patient Conditions:
      • Name: Narrow-angle glaucoma
      • Drugbank Id: DBCOND0095646
  • Regions: US
  • Patient Conditions:
      • Name: Severe Coronary Artery Disease
      • Drugbank Id: DBCOND0037446
      • Modification Of:
        • Base:
          • Name: Coronary Artery Disease
          • Drugbank Id: DBCOND0000554
        • Severity:
          • Includes:
            • severe
  • Regions: US
  • With Categories Coadmin:
      • Name: Monoamine Oxidase Inhibitors
      • Drugbank Id: DBCAT001004
      • Mesh Id: D008996
  • Hypersensitivity:
    • true
  • Regions: US

Food Interactions

  • Take with or without food. The absorption is unaffected by food.

Interactions

Type in a drug name to check for interaction with Pseudoephedrine
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-benzylimidazole
The therapeutic efficacy of 1-benzylimidazole can be decreased when used in combination with Pseudoephedrine.
2,4-thiazolidinedione
The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Pseudoephedrine.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of serotonin syndrome can be increased when Pseudoephedrine is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of serotonin syndrome can be increased when Pseudoephedrine is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthine
The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with 3-isobutyl-1-methyl-7H-xanthine.
3,5-diiodothyropropionic acid
The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with 3,5-diiodothyropropionic acid.
3,5-Diiodotyrosine
The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with 3,5-Diiodotyrosine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of serotonin syndrome can be increased when Pseudoephedrine is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-Methoxyamphetamine
The risk or severity of hypertension can be increased when Pseudoephedrine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of serotonin syndrome can be increased when Pseudoephedrine is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanine
The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with 6-O-benzylguanine.
7-Deazaguanine
The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with 7-Deazaguanine.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypertensive activities of Pseudoephedrine.
7,9-Dimethylguanine
The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with 7,9-Dimethylguanine.
8-azaguanine
The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with 8-azaguanine.
8-chlorotheophylline
The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with 8-chlorotheophylline.
9-Deazaguanine
The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with 9-Deazaguanine.
9-Methylguanine
The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with 9-Methylguanine.
Abaloparatide
The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with Abaloparatide.
Abediterol
The risk or severity of hypertension can be increased when Pseudoephedrine is combined with Abediterol.
17 References
  1. 1 . AVIADO DM Jr, WNUCK AL, DE BEER EJ: Cardiovascular effects of sympathomimetic bronchodilators; epinephrine, ephedrine, pseudoephedrine, isoproterenol, methoxyphenamine and isoprophenamine. J Pharmacol Exp Ther. 1958 Mar;122(3):406-17.PubMed: 13539766
  2. 2 . Chen K, Schmidt C: Ephedrine and Related Substances Medicine. 1930 Feb;9(1):1-117.PubMed:
  3. 3 . Volpp M, Holzgrabe U: Determination of plasma protein binding for sympathomimetic drugs by means of ultrafiltration. Eur J Pharm Sci. 2019 Jan 15;127:175-184. doi: 10.1016/j.ejps.2018.10.027. Epub 2018 Oct 31.PubMed: 30391401
  4. 4 . Chao ST, Prather D, Pinson D, Coen P, Pruitt B, Knowles M, Place V: Effect of food on bioavailability of pseudoephedrine and brompheniramine administered from a gastrointestinal therapeutic system. J Pharm Sci. 1991 May;80(5):432-5. doi: 10.1002/jps.2600800507.PubMed: 1880721
  5. 5 . Kobayashi S, Endou M, Sakuraya F, Matsuda N, Zhang XH, Azuma M, Echigo N, Kemmotsu O, Hattori Y, Gando S: The sympathomimetic actions of l-ephedrine and d-pseudoephedrine: direct receptor activation or norepinephrine release? Anesth Analg. 2003 Nov;97(5):1239-45.PubMed: 14570629
  6. 6 . Johnson DA, Hricik JG: The pharmacology of alpha-adrenergic decongestants. Pharmacotherapy. 1993 Nov-Dec;13(6 Pt 2):110S-115S; discussion 143S-146S.PubMed: 7507588
  7. 7 . Thippaiah SM, Nagaraja S, Birur B, Pandurangi A: Successful Management of Psychotropics Induced Stuttering Priapism with Pseudoephedrine in a Patient with Schizophrenia. Psychopharmacol Bull. 2018 Feb 5;48(2):29-33.PubMed: 29713098
  8. 8 . Wee S, Ordway GA, Woolverton WL: Reinforcing effect of pseudoephedrine isomers and the mechanism of action. Eur J Pharmacol. 2004 Jun 16;493(1-3):117-25.PubMed: 15189772
  9. 9 . Foley KF, Van Dort ME, Sievert MK, Ruoho AE, Cozzi NV: Stereospecific inhibition of monoamine uptake transporters by meta-hydroxyephedrine isomers. J Neural Transm (Vienna). 2002 Oct;109(10):1229-40.PubMed: 12373557
  10. 10 . Fiebich BL, Collado JA, Stratz C, Valina C, Hochholzer W, Munoz E, Bellido LM: Pseudoephedrine inhibits T-cell activation by targeting NF-kappaB, NFAT and AP-1 signaling pathways. Immunopharmacol Immunotoxicol. 2012 Feb;34(1):98-106. doi: 10.3109/08923973.2011.582118. Epub 2011 Jun 2.PubMed: 21631396
  11. 11 . FDA Approved Drug Products: Zyrtec Cetirizine and Pseudoephedrine Oral Tablets (OTC) Link
  12. 12 . FDA Approved Drug Products: Motrin Cold and Sinus Ibuprofen and Pseudoephedrine Oral Caplets (OTC) Link
  13. 13 . FDA Approved Drug Products: Semprex Avacristine and Pseudoephedrine Oral Capsules Link
  14. 14 . FDA Approved Drug Products: Mucinex Guaifenesin and Pseudoephedrine Oral Extended Release Tablets (OTC) Link
  15. 15 . FDA Approved Drug Products: Loratadine and Pseudoephedrine Oral Extended Release Tablets (OTC) Link
  16. 16 . FDA Approved Drug Products: Clarinex 12 Hour Desloratadine and Pseudoephedrine Oral Tablets Link
  17. 17 . FDA Approved Drug Products: Clarinex 24 Hour Desloratadine and Pseudoephedrine Oral Tablets Link