      Document 0088
 DOCN  DRG0088
 UNIQUE IDENTIFIER        DRG-0159
 NAME OF SUBSTANCE        Pseudoephedrine hydrochloride [USAN 1996]
 REGISTRY NUMBER          345-78-8
 RELATED REGISTRY NUMBER  90-82-4
 STANDARD CHEMICAL NAME   Benzenemethanol,
                          alpha-(1-(methylamino)ethyl)-, [S-(R*,R*)]-,
                          hydrochloride [USAN 1996]
 SYNONYMS                 Deconsal II [PDR 1995]
 SYNONYMS                 Novafed [AHFS Drug Information 1995]
 SYNONYMS                 Sudafed [USAN 1996]
 SYNONYMS                 Actifed [PDR 1995]
 SYNONYMS                 Alleract Decongestant [PDR 1993]
 SYNONYMS                 CoAdvil [USAN 1996]
 SYNONYMS                 Congestac [USAN 1996]
 SYNONYMS                 Contac Nighttime Cold Medicine [USAN 1996]
 SYNONYMS                 Dimacol [USAN 1996]
 SYNONYMS                 Maximum Strength Dristan [USAN 1996]
 SYNONYMS                 Robitussin PE [USAN 1996]
 SYNONYMS                 Sine-Off [USAN 1996]
 SYNONYMS                 Tylenol Allergy Sinus [USAN 1996]
 SYNONYMS                 Tylenol Cold Medication [USAN 1996]
 SYNONYMS                 d-Pseudoephedrine hydrochloride [Merck Index
                          1989]
 SYNONYMS                 Maximum Strength Sine-Aid [USAN 1996]
 SYNONYMS                 Naldegesic [USAN 1996]
 SYNONYMS                 Sinarest No-Drowsiness Tablets [USAN 1993]
 SYNONYMS                 Histalet [USAN 1996]
 SYNONYMS                 Rondec [USAN 1996]
 SYNONYMS                 Isoephedrine hydrochloride [AHFS Drug
                          Information 1995]
 PROTOCOL ID NUMBERS      NIAID ACTG 186
 PROTOCOL ID NUMBERS      FDA 243A
 SECONDARY SOURCE ID      DRG
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Acts primarily on the alpha
                          adrenergic receptors of the respiratory
                          mucosa producing vasoconstriction, which
                          results in reduction of tissue hyperemia,
                          edema, and nasal congestion, and an increase
                          in nasal airway patency. The vasoconstriction
                          action of pseudoephedrine is similar to that
                          of ephedrine. Pseudoephedrine is rapidly and
                          almost completely absorbed from the
                          gastrointestinal tract. It has a plasma
                          half-life of 6-8 hours. The drug is
                          distributed to body tissues and fluids,
                          including fetal tissue, breast milk, and the
                          CNS. Approximately 50-75 percent of the
                          administered dose is excreted unchanged in
                          the urine; the remainder is apparently
                          metabolized in the liver to inactive
                          compounds by N-demethylation,
                          parahydroxylation, and oxidative deamination.
                          [PDR 1995]
 DISEASES STUDIED/TREATED Prevention of recurrent HIV-associated
                          sinusitis [NIAID ACTG 186]
 CLASSIFICATION CODE      Decongestant [PDR 1995]
 CLASSIFICATION CODE      Sympathomimetic [AHFS Drug Information 1995]
 OTHER MAJOR USES         Relief of nasal congestion in pharyngitis,
                          bronchitis, and asthma [PDR 1995]
 SUBSTANCE INTERACTIONS   May interact with beta-adrenergic blockers
                          and monoamine oxidase (MAO) inhibitors;
                          digitalis glycosides; guanethidine,
                          mecamylamine, methyldopa, reserpine, and
                          veratrum alkaloids; and tricyclic
                          antidepressants. [PDR 1995]
 ADVERSE EFFECTS          Adverse effects include tachycardia,
                          palpitations, headache, dizziness, nausea,
                          anxiety, nervousness, restlessness, tremor,
                          weakness, pallor, respiratory difficulty,
                          burning on urination, insomnia,
                          hallucinations, convulsions, depression,
                          abnormal heart rhythms, and low blood
                          pressure. [PDR 1995] [NIAID ACTG 186]
 CONTRAINDICATIONS        Contraindicated in patients with
                          hypersensitivity or idiosyncrasy to
                          sympathomimetic amines, severe hypertension,
                          or severe coronary artery disease, and in
                          those on monoamine oxidase (MAO) inhibitor
                          therapy. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Sympathomimetic amine;
                          adrenergic (vasoconstrictor) [AHFS Drug
                          Information 1995]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Fine, white to
                          off-white crystals or powder having a faint,
                          characteristic odor [AHFS Drug Information
                          1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C10H15NO.HCl [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 201.70 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MELTING POINT: 181-182 C [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Soluble in water, alcohol, and
                          chloroform [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL COMMENT: pKa 9.22 [Merck Index 1989]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Tablets. [AHFS Drug Information
                          1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral. [AHFS Drug
                          Information 1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Store at temperatures no greater
                          than 30 C (86 F). Protect from freezing and
                          light. [NIAID ACTG 186] [AHFS Drug
                          Information 1995]
 MANUFACTURERS            Adams Laboratories
 REFERENCES               Bronsky E, Boggs P, Findlay S, Gawchik S,
                          Georgitis J, Mansmann H, Sholler L, Wolfe J,
                          Meltzer E, Morris R, et al. Comparative
                          efficacy and safety of a once-daily
                          loratadine-pseudoephedrine combination versus
                          its components alone and placebo in the
                          management of seasonal allergic rhinitis. J
                          Allergy Clin Immunol 1995 Aug;96(2):139-47.
 REFERENCES               Wagner DL, Patel VS. Steady-state human
                          pharmacokinetics and bioavailability of
                          guaifenesin and pseudoephedrine in a
                          sustained-release tablet relative to
                          immediate-release liquids. Int J Pharm; VOL
                          114 ISS Feb 14 1995, P171-176, (REF 6).
 REFERENCES               Pade V, Aluri J, Manning L, Stavchansky S.
                          Bioavailability of pseudoephedrine from
                          controlled release formulations in the
                          presence of guaifenesin in human volunteers.
                          Biopharm Drug Dispos 1995 Jul;16(5):381-91.
 REFERENCES               Krivda SJ, Benson PM. Nonpigmenting fixed
                          drug eruption. J Am Acad Dermatol 1994
                          Aug;31(2 Pt 1):291-2.
 REFERENCES               Martinez Gallardo F, Lopez Fiesco A, Zamora
                          G. Symptomatic treatment of common cold in
                          children with a new combination of naproxen
                          sodium plus pseudoephedrine hydrochloride: a
                          comparative trial against pseudoephedrine
                          syrup. Proc West Pharmacol Soc 1994;37:157-8.
 REFERENCES               Pratter MR, Bartter T, Akers S, DuBois J. An
                          algorithmic approach to chronic cough. Ann
                          Intern Med 1993 Nov 15;119(10):977-83.
 REFERENCES               Segal AT, Falliers CJ, Grant JA, Podleski WK,
                          Woehler TR, Huster WJ, McNutt B. Safety and
                          efficacy of terfenadine/pseudoephedrine
                          versus clemastine/phenylpropanolamine in the
                          treatment of seasonal allergic rhinitis. Ann
                          Allergy 1993 May;70(5):389-94.
 REFERENCES               Cavanah DK, Ballas ZK. Pseudoephedrine
                          reaction presenting as recurrent toxic shock
                          syndome. Ann Intern Med 1993 Aug
                          15;119(4):302-3.
 REFERENCES               Wilson BE, Hobbs WN. Case report:
                          pseudoephedrine-associated thyroid storm:
                          thyroid hormone-catecholamine interactions.
                          Am J Med Sci 1993 Nov;306(5):317-9.
 ENTRY MONTH              9301
 LAST REVISION DATE       960308
 

SOURCE: National Library of Medicine, Bethesda, MD.  Distributed by AEGIS.
