      Document 0087
 DOCN  DRG0087
 UNIQUE IDENTIFIER        DRG-0160
 NAME OF SUBSTANCE        Guaifenesin [USAN 1996]
 REGISTRY NUMBER          93-14-1
 STANDARD CHEMICAL NAME   1,2-Propanediol, 3-(2-methoxyphenoxy)- [USAN
                          1996]
 SYNONYMS                 Glyceryl guaiacolate [USAN 1996]
 SYNONYMS                 Guaiacol glyceryl ether [Merck Index 1989]
 SYNONYMS                 Guaiphenesin [USAN 1996]
 SYNONYMS                 Deconsal II [PDR 1995]
 SYNONYMS                 Dimacol [USAN 1996]
 SYNONYMS                 Actifed-C [Merck Index 1989]
 SYNONYMS                 Myocaine [Merck Index 1989]
 SYNONYMS                 Contac Cough Formula [USAN 1996]
 SYNONYMS                 Relaxil G [Merck Index 1989]
 SYNONYMS                 Robitussin [USAN 1996]
 SYNONYMS                 Sirotol [Merck Index 1989]
 SYNONYMS                 Brexin EX [USAN 1996]
 SYNONYMS                 Cremacoat 2 [CHEMLINE]
 SYNONYMS                 Aeronesin [CHEMLINE]
 SYNONYMS                 Amonidrin [USAN 1996]
 SYNONYMS                 Congestac [USAN 1996]
 SYNONYMS                 alpha-Glyceryl guaiacol ether [Merck Index
                          1989]
 SYNONYMS                 Aresol [CHEMLINE]
 SYNONYMS                 Calmipan [Merck Index 1989]
 SYNONYMS                 Guaiacyl glyceryl ether [Merck Index 1989]
 SYNONYMS                 Glyceryl guaiacyl ether [Merck Index 1989]
 SYNONYMS                 XL-90 [Merck Index 1989]
 SYNONYMS                 Colrex Expectorant [Merck Index 1989]
 SYNONYMS                 Equicol [Merck Index 1989]
 SYNONYMS                 Gecolate [Merck Index 1989]
 SYNONYMS                 Glycodex [Merck Index 1989]
 SYNONYMS                 Oresol [Merck Index 1989]
 SYNONYMS                 Neuroton [Merck Index 1989]
 PROTOCOL ID NUMBERS      NIAID ACTG 186
 SECONDARY SOURCE ID      AI3-24947 [CHEMLINE]
 SECONDARY SOURCE ID      My 301 [Merck Index 1989]
 PHARMACOLOGICAL ACTION   Increases sputum and bronchial secretions by
                          reducing adhesiveness and surface tension. By
                          reducing the viscosity of secretions,
                          guaifenesin increases the efficiency of the
                          cough reflex and ciliary action in removing
                          accumulated secretions from the trachea and
                          bronchi. The drug is readily absorbed from
                          the gastrointestinal tract and readily
                          metabolized and excreted in the urine. It has
                          a plasma half-life of 1 hour. The major
                          urinary metabolite is beta-(2-methoxyphenoxy)
                          lactic acid. [PDR 1995]
 DISEASES STUDIED/TREATED Prevention of recurrent HIV-associated
                          sinusitis [NIAID ACTG 186]
 CLASSIFICATION CODE      Expectorant [USAN 1996]
 OTHER MAJOR USES         Used as expectorant in pharyngitis,
                          bronchitis, and asthma [PDR 1995]
 SUBSTANCE INTERACTIONS   May interfere with laboratory test for
                          diagnosis of carcinoid syndrome; may falsely
                          elevate the VMA test for catechols. [PDR
                          1995]
 ADVERSE EFFECTS          No serious adverse effects have been reported
                          with the use of guaifenesin. [PDR 1995]
 CONTRAINDICATIONS        Contraindicated in patients with
                          hypersensitivity to guaifenesin. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Centrally acting muscle
                          relaxant with expectorant properties [Merck
                          Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: White to slightly gray,
                          crystalline powder, having a bitter taste;
                          may have a slight characteristic odor [AHFS
                          Drug Information 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C10H14O4 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 198.22 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MELTING POINT: 78.5-79 C [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   BOILING POINT: 215 C [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   ELEMENTAL COMPOSITION: C60.59%, H7.12%,
                          O32.29% [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Soluble in water, ethanol,
                          chloroform, glycerol, propylene glycol, DMF;
                          moderately soluble in benzene; practically
                          insoluble in ether [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   STABILITY: Powder tends to become lumpy on
                          storage [AHFS Drug Information 1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Tablets, solution. [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.
                          [NIAID ACTG 186]
 MANUFACTURERS            Adams Laboratories
 REFERENCES               Sisson JH, Yonkers AJ, Waldman RH. Effects of
                          guaifenesin on nasal mucociliary clearance
                          and ciliary beat frequency in healthy
                          volunteers. Chest 1995 Mar;107(3):747-51.
 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               Brock MH, Dansereau RJ, Patel VS. Use of in
                          vitro and in vivo data in the design,
                          development, and quality control of
                          sustained-release decongestant dosage forms.
                          Pharmacotherapy 1994 Jul-Aug;14(4):430-7.
 REFERENCES               Croughan-Minihane MS, Petitti DB, Rodnick JE,
                          Eliaser G. Clinical trial examining
                          effectiveness of three cough syrups [see
                          comments]. J Am Board Fam Pract 1993
                          Mar-Apr;6(2):109-15.
 REFERENCES               Wawrose SF, Tami TA, Amoils CP. The role of
                          guaifenesin in the treatment of sinonasal
                          disease in patients infected with the human
                          immunodeficiency virus (HIV). Laryngoscope.
                          1992 Nov;102(11):1225-8.
 ENTRY MONTH              9301
 LAST REVISION DATE       960308
 

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