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    Chemistry

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    Also known as: 93-14-1, Guaiphenesin, Guaiacol glyceryl ether, Glycerol guaiacolate, Glyceryl guaiacolate, 3-(2-methoxyphenoxy)propane-1,2-diol
    Molecular Formula
    C10H14O4
    Molecular Weight
    198.22  g/mol
    InChI Key
    HSRJKNPTNIJEKV-UHFFFAOYSA-N
    FDA UNII
    495W7451VQ
    Guaifenesin
    An expectorant that also has some muscle relaxing action. It is used in many cough preparations.
    Guaifenesin is an Expectorant. The physiologic effect of guaifenesin is by means of Decreased Respiratory Secretion Viscosity, and Increased Respiratory Secretions.
    1 2D Structure

    Guaifenesin

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    3-(2-methoxyphenoxy)propane-1,2-diol
    2.1.2 InChI
    InChI=1S/C10H14O4/c1-13-9-4-2-3-5-10(9)14-7-8(12)6-11/h2-5,8,11-12H,6-7H2,1H3
    2.1.3 InChI Key
    HSRJKNPTNIJEKV-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    COC1=CC=CC=C1OCC(CO)O
    2.2 Other Identifiers
    2.2.1 UNII
    495W7451VQ
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Breonesin

    2. Ether, Guaiacol Glyceryl

    3. Glycerol Guaiacolate

    4. Glyceryl Ether, Guaiacol

    5. Guaiacol Glyceryl Ether

    6. Guaiacolate, Glycerol

    7. Guaiphenesin

    8. Guaiphenezine

    9. Guiatuss

    10. Humibid

    11. Hytuss

    12. My 301

    13. My-301

    14. My301

    15. Scott Tussin

    16. Scott-tussin

    17. Scotttussin

    2.3.2 Depositor-Supplied Synonyms

    1. 93-14-1

    2. Guaiphenesin

    3. Guaiacol Glyceryl Ether

    4. Glycerol Guaiacolate

    5. Glyceryl Guaiacolate

    6. 3-(2-methoxyphenoxy)propane-1,2-diol

    7. Guaiphenesine

    8. Methphenoxydiol

    9. Aeronesin

    10. Breonesin

    11. Robitussin

    12. Bronchol

    13. Mucinex

    14. Aresol

    15. Propanosedyl

    16. Calmipan

    17. Cortussin

    18. Dorassin

    19. Flartussin

    20. Guaiacuran

    21. Guaiacurane

    22. Guaiamar

    23. Guaianesin

    24. Guaiphesin

    25. Hustosil

    26. Myocaine

    27. Myoscain

    28. Creson

    29. Gaiamar

    30. Hytuss

    31. Myocain

    32. Reduton

    33. Dilyn

    34. Resyl

    35. Glycerin Guaiacolate

    36. Glyceryl Guaiacol

    37. Methoxypropanediol

    38. Metossipropandiolo

    39. Metfenossidiolo

    40. Amonidrin

    41. Glycotuss

    42. Guajacuran

    43. Guajamar

    44. Guayanesin

    45. Guiaphenesin

    46. Hustodil

    47. Mintosyl

    48. Miocaina

    49. Miocurin

    50. Miorelax

    51. Mucostop

    52. Muskurelax

    53. Myorelax

    54. Myoscaine

    55. Neuroton

    56. Neurotone

    57. Reorganin

    58. Respenyl

    59. Ritussin

    60. Tenntuss

    61. Glyceryl Guaicolate

    62. Glyceryl Guiacolate

    63. Guanar

    64. Oresol

    65. Oreson

    66. Respil

    67. Sirotol

    68. Gvaja

    69. Resil

    70. Tolyn

    71. Tulyl

    72. Tulyn

    73. 3-(o-methoxyphenoxy)-1,2-propanediol

    74. Guaiacol Glycerol Ether

    75. Guaiacolglicerinetere

    76. Guaia-rom

    77. Relaxil G

    78. Relaxyl-g

    79. Guaicol Glyceryl Ether

    80. Gnaifenesin

    81. Guaifenesine

    82. Glyceryl Guaiacyl Ether

    83. Guaiacyl Glyceryl Ether

    84. Guaicol Glycerine Ether

    85. 3-(2-methoxyphenoxy)-1,2-propanediol

    86. Organidin Nr

    87. O-methoxyphenyl Glyceryl Ether

    88. Glycero-guaiacol Ether

    89. Guaiacol Glycerin Ether

    90. Guaifenesinum

    91. Amonidren

    92. Pneumomist

    93. 1,2-propanediol, 3-(2-methoxyphenoxy)-

    94. Trecid

    95. Glycerylguaiacol

    96. Glycerin Monoguaiacol Ether

    97. Guajacol-glycerinaether

    98. Glyceryl Guaiacol Ether

    99. 3-o-methoxyphenoxypropane 1:2-diol

    100. Glyceryl Guaiacolate Ether

    101. Glycerol Mono(2-methoxyphenyl) Ether

    102. Actifed C

    103. Guaiacolic Acid, Ester With Glycerol

    104. My 301

    105. Sl-90

    106. Xl-90

    107. Alpha-glyceryl Guaiacol Ether

    108. 1,2-dihydroxy-3-(2-methoxyphenoxy)propane

    109. Guaifensin

    110. Alpha-glyceryl Guaiacolate Ether

    111. Rac Guaifenesin

    112. G 87

    113. 1,2-propanediol, 3-(o-methoxyphenoxy)-

    114. Glycerol-alpha-guajakolether

    115. Component Of Quibron

    116. 3-(o-methoxyphenoxy)-propanediol-1,2

    117. Component Of Hycotuss

    118. Glycerol .alpha.-guiacyl Ether

    119. .alpha.-glyceryl Guaiacol Ether

    120. Glycerol .alpha.-guaiacyl Ether

    121. Guajacol-.alpha.-glycerin-ether

    122. Component Of Brondecon

    123. .alpha.-glyceryl Guaiacolate Ether

    124. Glycerol .alpha.-monoguaiacol Ether

    125. Component Of Quibron Plus

    126. Nsc-62112

    127. 1,2,3-propanetriol, Ether With 2-methoxyphenol

    128. Guaifenesin (guaiphenesin)

    129. Glycerol .alpha.-(o-methoxyphenyl)ether

    130. Glycerol .alpha.-(2-methoxyphenyl) Ether

    131. Component Of Colrex Expectorant

    132. 2-g

    133. 2/g

    134. Cvt-2534

    135. Nsc62112

    136. 495w7451vq

    137. Equicol

    138. Glycodex

    139. Dsstox_cid_3114

    140. Colrex Expectorant

    141. Dsstox_rid_76881

    142. Dsstox_gsid_23114

    143. Guaifenesina

    144. Tenntus

    145. Tussin

    146. Glycerinmonoguaiacol Ether

    147. Benylin-e

    148. Lufyllin-gg

    149. Aether Glycerinoguaiacolicus

    150. Guaifenesine [inn-french]

    151. Guaifenesinum [inn-latin]

    152. Guajacol-alpha-glycerinether

    153. Tedral Expectorant

    154. (component Of) Deconsal Ii

    155. Glycerol Alpha-guiacyl Ether

    156. Guaifenesina [inn-spanish]

    157. Glycerol Alpha-guaiacyl Ether

    158. My-301

    159. Glycerol Alpha-monoguaiacol Ether

    160. Glycerol-alpha-monoguaiacol Ether

    161. Guajacol-glycerinaether [german]

    162. Hsdb 3089

    163. Sr-01000737186

    164. Glycerol Mono(2-methoxyphenyl)ether

    165. Einecs 202-222-5

    166. Glycerol-alpha-guajakolether [czech]

    167. Nsc 62112

    168. Glycerol Alpha-(o-methoxyphenyl)ether

    169. Glycerol Alpha-(o-methoxyphenyl) Ether

    170. Glycerol Alpha-(2-methoxyphenyl) Ether

    171. Brn 2049375

    172. Glycerin Ether

    173. Glyc

    174. Ai3-24947

    175. Unii-495w7451vq

    176. Q-tussin

    177. Guaifenesin,(s)

    178. Cas-93-14-1

    179. Ncgc00016350-01

    180. Hustosil (tn)

    181. Prestwick_231

    182. Entex (salt/mix)

    183. Mfcd00016873

    184. Humabid

    185. Dimacol (salt/mix)

    186. Kwelcof (salt/mix)

    187. Guaifenesin Dc 95%

    188. Hycotuss (salt/mix)

    189. Guaifenesin [usan:usp:inn:ban:jan]

    190. Brondecon (salt/mix)

    191. Congestac (salt/mix)

    192. Triaminic (salt/mix)

    193. Dilor G (salt/mix)

    194. Guaifenesin-[13c3]

    195. Spectrum_000835

    196. Pneumomist (salt/mix)

    197. Q-tussin (salt/mix)

    198. Glycerol-a-guajakolether

    199. 3-(2-methoxy-phenoxy)-propane-1,2-diol

    200. Mucinex D (salt/mix)

    201. Robitussin (tn)

    202. Glycerol A-guiacyl Ether

    203. Tussar-2 (salt/mix)

    204. Brexin Ex (salt/mix)

    205. Tussar Sf (salt/mix)

    206. Guaifenesin [mi]

    207. Guaifenesin(guaiphenesin)

    208. A-glyceryl Guaiacol Ether

    209. Glycerol A-guaiacyl Ether

    210. Mucinex Dm (salt/mix)

    211. Prestwick0_000776

    212. Prestwick1_000776

    213. Prestwick2_000776

    214. Prestwick3_000776

    215. Spectrum2_001104

    216. Spectrum3_000444

    217. Spectrum4_000566

    218. Spectrum5_000758

    219. Guaifenesin [inn]

    220. Guaifenesin [jan]

    221. Lufyllin-gg (salt/mix)

    222. Naldecon-ex (salt/mix)

    223. (+-)-3-(o-methoxyphenoxy)-1,2-propanediol

    224. Guaifenesin [hsdb]

    225. Guaifenesin [usan]

    226. Chembl980

    227. Theolair Plus (salt/mix)

    228. Guaifenesin [vandf]

    229. Robitussin Cf (salt/mix)

    230. Schembl4321

    231. A-glyceryl Guaiacolate Ether

    232. Neothylline-gg (salt/mix)

    233. Guaifenesin [mart.]

    234. Oprea1_193170

    235. Pneumotussin Hc (salt/mix)

    236. Wln: Q1yq1or Bo1

    237. 1, 3-(o-methoxyphenoxy)-

    238. Bronkaid Caplets (salt/mix)

    239. Bspbio_000852

    240. Bspbio_002088

    241. Glycerol A-monoguaiacol Ether

    242. Guaifenesin [usp-rs]

    243. Guaifenesin [who-dd]

    244. Kbiogr_000972

    245. Kbioss_001315

    246. Slo-phyllin Gg (salt/mix)

    247. 1,2-propanediol, 3-(2-methoxyphenoxy)- (+-)-

    248. 4-06-00-05576 (beilstein Handbook Reference)

    249. Mls000028402

    250. 1, 3-(2-methoxyphenoxy)-

    251. Divk1c_000248

    252. Spectrum1500321

    253. Glycerol-.alpha.-guajakolether

    254. Spbio_001208

    255. Spbio_002791

    256. Pv Tussin Tablet (salt/mix)

    257. Tedral Expectorant (salt/mix)

    258. Bpbio1_000938

    259. Chebi:5551

    260. Gtpl7617

    261. Guaifenesin (jp17/usp/inn)

    262. Dtxsid5023114

    263. Guaifenesin [green Book]

    264. Tussi-organidin Nr (salt/mix)

    265. Hms500m10

    266. Kbio1_000248

    267. Kbio2_001315

    268. Kbio2_003883

    269. Kbio2_006451

    270. Kbio3_001308

    271. Contac Cough Formula (salt/mix)

    272. Guaifenesin [orange Book]

    273. Ru-tuss De Tablets (salt/mix)

    274. Glycerol A-(o-methoxyphenyl)ether

    275. Ninds_000248

    276. Guaifenesin [ep Monograph]

    277. Hms1570k14

    278. Hms1920b15

    279. Hms2090k20

    280. Hms2091h21

    281. Hms2097k14

    282. Hms2231m20

    283. Hms3369e03

    284. Hms3369n15

    285. Hms3651i17

    286. Hms3714k14

    287. Isoclor Expectorant C (salt/mix)

    288. Pharmakon1600-01500321

    289. Polaramine Expectorant (salt/mix)

    290. Guaifenesin [usp Monograph]

    291. Glycerol A-(2-methoxyphenyl) Ether

    292. Hy-b0264

    293. Obredon Component Guaifenesin

    294. Tox21_110389

    295. Tox21_302094

    296. Bbl009981

    297. Ccg-39687

    298. Flowtuss Component Guaifenesin

    299. Nsc757052

    300. S1740

    301. Stk365152

    302. Glycerol, 1-(2-methoxyphenyl) Ether

    303. Akos005435152

    304. Mucinex D Component Guaifenesin

    305. Tox21_110389_1

    306. Db00874

    307. Guaifenesin Component Of Obredon

    308. Ks-5306

    309. Mucinex Dm Component Guaifenesin

    310. Nsc-757052

    311. Guaiacol Glyceryl Ether, >=98% (gc)

    312. Guaifenesin Component Of Flowtuss

    313. Idi1_000248

    314. 3-(2-methoxyphenoxy)-1, 2-propanediol

    315. Guaifenesin Component Of Hycofenix

    316. Hycofenix Component Of Guaifenesin

    317. Ncgc00094689-01

    318. Ncgc00094689-02

    319. Ncgc00094689-03

    320. Ncgc00094689-04

    321. Ncgc00094689-06

    322. Ncgc00255343-01

    323. Ac-26819

    324. Guaifenesin Component Of Mucinex D

    325. Smr000058387

    326. Guaifenesin Component Of Mucinex Dm

    327. Sbi-0051397.p003

    328. Ab00052006

    329. Ft-0613565

    330. Ft-0669064

    331. G0159

    332. Sw196538-3

    333. (2s)-3-(2-methoxyphenoxy)propane-1,2-diol

    334. 1,3-propanetriol, Ether With 2-methoxyphenol

    335. D00337

    336. D70850

    337. 3-(2-methoxyphenoxy)-1,2-propanediol, 99+%

    338. 3-{[2-(methyloxy)phenyl]oxy}propane-1,2-diol

    339. Ab00052006-10

    340. Ab00052006-11

    341. Ab00052006_12

    342. Ab00052006_13

    343. A844457

    344. Q420682

    345. 3 - (2 - Methoxyphenoxy) - 1, 2 - Propanediol

    346. Sr-01000737186-2

    347. Sr-01000737186-3

    348. W-100252

    349. (+/-)-3-(o-methoxyphenoxy)-1,2-propanediol

    350. Brd-a90515964-001-05-8

    351. Brd-a90515964-001-09-0

    352. 1,2-propanediol, 3-(2-methoxyphenoxy)- (+/-)-

    353. Guaifenesin, European Pharmacopoeia (ep) Reference Standard

    354. ( Inverted Exclamation Marka)-3-(o-methoxyphenoxy)-1,2-propanediol

    355. Guaifenesin, United States Pharmacopeia (usp) Reference Standard

    356. Guaifenesin, Pharmaceutical Secondary Standard; Certified Reference Material

    357. Guaifenesin For Peak Identification, European Pharmacopoeia (ep) Reference Standard

    2.4 Create Date
    2005-03-25
    3 Chemical and Physical Properties
    Molecular Weight 198.22 g/mol
    Molecular Formula C10H14O4
    XLogP31.4
    Hydrogen Bond Donor Count2
    Hydrogen Bond Acceptor Count4
    Rotatable Bond Count5
    Exact Mass198.08920892 g/mol
    Monoisotopic Mass198.08920892 g/mol
    Topological Polar Surface Area58.9 Ų
    Heavy Atom Count14
    Formal Charge0
    Complexity151
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count1
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Information
    1 of 4  
    Drug NameGuaifenesin
    PubMed HealthGuaifenesin (By mouth)
    Drug ClassesExpectorant
    Drug LabelGuaifenesin (glyceryl guaiacolate) has the chemical name 3-(2-methoxyphenoxy)-1,2-propanediol. Its molecular formula is C10H14O4 with a molecular weight of 198.21. It is a white or slightly gray crystalline substance with a slightly bitter aromatic t...
    Active IngredientGuaifenesin
    Dosage FormTablet, extended release
    RouteOral
    Strength600mg
    Market StatusOver the Counter
    CompanyPerrigo R And D

    2 of 4  
    Drug NameMucinex
    PubMed HealthGuaifenesin (By mouth)
    Drug ClassesExpectorant
    Active IngredientGuaifenesin
    Dosage FormTablet, extended release
    RouteOral
    Strength600mg; 1.2gm
    Market StatusOver the Counter
    CompanyReckitt Benckiser

    3 of 4  
    Drug NameGuaifenesin
    PubMed HealthGuaifenesin (By mouth)
    Drug ClassesExpectorant
    Drug LabelGuaifenesin (glyceryl guaiacolate) has the chemical name 3-(2-methoxyphenoxy)-1,2-propanediol. Its molecular formula is C10H14O4 with a molecular weight of 198.21. It is a white or slightly gray crystalline substance with a slightly bitter aromatic t...
    Active IngredientGuaifenesin
    Dosage FormTablet, extended release
    RouteOral
    Strength600mg
    Market StatusOver the Counter
    CompanyPerrigo R And D

    4 of 4  
    Drug NameMucinex
    PubMed HealthGuaifenesin (By mouth)
    Drug ClassesExpectorant
    Active IngredientGuaifenesin
    Dosage FormTablet, extended release
    RouteOral
    Strength600mg; 1.2gm
    Market StatusOver the Counter
    CompanyReckitt Benckiser

    4.2 Therapeutic Uses

    Expectorants

    National Library of Medicine's Medical Subject Headings online file (MeSH, 1999)

    Guaifenesin is indicated as an expectorant in the temporary symptomatic management of cough due to minor upper respiratory infections and related conditions, such as sinusitis, pharyngitis, and bronchitis, when these conditions are complicated by viscous mucus and congestion. However, because supporting data are very limited, there is some controversy about its effectiveness. /Included in US product label/

    Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1537

    VET: Guaifenesin (glyceryl guaiacolate) is a centrally acting muscle relaxant that is believed to depress or block nerve impulse transmission at the internuncial neuron level of the subcortical areas of the brain, brain stem, and spinal cord. It also has mild analgesic and sedative actions. Guaifenesin is given IV to induce muscle relaxation as an adjunct to anesthesia for short procedures. It relaxes both laryngeal and pharyngeal muscles, allowing easier intubation, but has little effect on diaphragm and respiratory function. It may cause transient increases in cardiac rate and decreases in blood pressure. It is also used in treatment of horses with exertional rhabdomyolysis and in dogs with strychnine intoxication.

    Kahn, C.M. (Ed.); The Merck Veterinary Manual 9th ed. Merck & Co. Whitehouse Station, NJ. 2005, p. 2018

    VET: The drug is used intravenously as a skeletal muscle relaxant in horses. /Gecolate, Glycodex Injection/

    US FDA; Database of Approved Animal Drug Products, FDA Center for Veterinary Medicine, VMRCVM Drug Information Lab, CFR Product Abstract for: 030-434, Available from, as of October 24, 2007: https://dil.vetmed.vt.edu/

    4.3 Drug Warning

    The Centers for Disease Control and Prevention (CDC) issued a Morbidity and Mortality Weekly Report (MMWR) article describing three deaths in U.S. infants aged less than 12 months associated with cough and cold medications /including guaifenesen/. These medications were determined by medical examiners or coroners to be the underlying cause of death. The cases described in this report underscore the need for clinicians to use caution when prescribing and caregivers to use caution when administering cough and cold medications to children aged less than 2 years.

    McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007.

    Doses of guaifenesin larger than those required for expectorant action may produce emesis, but GI upset at ordinary dosage levels is rare.

    McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007.

    For self-medication, unless directed by a physician, guaifenesin should not be used for persistent or chronic cough such as that occurring with smoking, asthma, chronic bronchitis, or emphysema, or for cough accompanied by excessive phlegm. A persistent cough may be indicative of a serious condition. If cough persists for more than one week, is recurrent, or is accompanied by fever, rash, or persistent headache, a physician should be consulted.

    McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007.

    Adverse effects ... indicating need for medical attention only if they continue or are bothersome ... occurring at an incidence less frequent or rare /include/: diarrhea; dizziness; headache; nausea or vomiting; skin rash; stomach pain; urticaria (hives).

    Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1537

    For more Drug Warnings (Complete) data for GUAIFENESIN (7 total), please visit the HSDB record page.

    4.4 Minimum/Potential Fatal Human Dose

    2(?). 2= SLIGHTLY TOXIC: PROBABLE ORAL LETHAL DOSE (HUMAN) 5-15 G/KG, BETWEEN 1 PINT & 1 QT FOR 70 KG PERSON (150 LB).

    Gosselin, R.E., H.C. Hodge, R.P. Smith, and M.N. Gleason. Clinical Toxicology of Commercial Products. 4th ed. Baltimore: Williams and Wilkins, 1976., p. II-240

    4.5 Drug Indication

    Guaifenesin is an expectorant that is indicated for providing temporary symptomatic relief from congested chests and coughs which may be due to a cold, bronchitis, and/or other breathing illnesses.

    FDA Label

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Guaifenesin is categorized as an expectorant that acts by enhancing the output of phlegm (sputum) and bronchial secretions via decreasing the adhesiveness and surface tension of such material. Furthermore, guaifenesin elicits an increased flow of less viscous gastric secretions that subsequently promote ciliary action - all actions that ultimately change dry, unproductive coughing to coughs that are more productive and less frequent. Essentially, by decreasing the viscosity and adhesiveness of such secretions, guaifenesin enhances the efficacy of mucociliary activity in removing accumulated secretions from the upper and lower airway.

    5.2 MeSH Pharmacological Classification

    Expectorants

    Agents that increase mucous excretion. Mucolytic agents, that is drugs that liquefy mucous secretions, are also included here. (See all compounds classified as Expectorants.)

    5.3 FDA Pharmacological Classification
    5.3.1 Active Moiety
    GUAIFENESIN
    5.3.2 FDA UNII
    495W7451VQ
    5.3.3 Pharmacological Classes
    Expectorant [EPC]; Increased Respiratory Secretions [PE]; Sigma-1 Receptor Agonists [MoA]; Uncompetitive N-methyl-D-aspartate Receptor Antagonist [EPC]; Uncompetitive NMDA Receptor Antagonists [MoA]; Decreased Respiratory Secretion Viscosity [PE]; Sigma-1 Agonist [EPC]
    5.4 ATC Code

    R05CA03

    S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

    R - Respiratory system

    R05 - Cough and cold preparations

    R05C - Expectorants, excl. combinations with cough suppressants

    R05CA - Expectorants

    R05CA03 - Guaifenesin

    5.5 Absorption, Distribution and Excretion

    Absorption

    Studies have shown that guaifenesin is well absorbed from and along the gastrointestinal tract after oral administration.

    Route of Elimination

    After administration, guaifenesin is metabolized and then largely excreted in the urine.

    Volume of Distribution

    The geometric mean apparent volume of distribution of guaifenesin determined in healthy adult subjects is 116L (CV=45.7%).

    Clearance

    The mean clearance recorded for guaifenesin is about 94.8 L/hr (CV=51.4%).

    Readily absorbed from the gastrointestinal tract.

    Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1537

    It is not known whether guaifenesin is distributed into breast milk.

    Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1537

    Elimination /is/ renal, as inactive metabolites.

    Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1537

    Five donkeys and three horses were given guaifenesin, intravenously, by gravity administration, until recumbency was produced. The time and dose required to produce recumbency, recovery time to sternal and standing were recorded. Blood samples were collected for guaifenesin assay at 10, 20, 30, 40, 50, 60 min, and 2, 3, 4 and 6 hr after guaifenesin administration. Serum was analysed for guaifenesin using HPLC and pharmacokinetic values were calculated using a computer software package. In donkeys, heart and respiratory rates and blood pressures were recorded before and at 5-min intervals during recumbency. Arterial blood samples were collected before and at 5 and 15 min intervals during recumbency for analysis of pH, CO2, and O2. ANOVA was used to evaluate dynamic data, while t-tests were used for kinetic values. Respiratory rate was decreased significantly during recumbency, but no other significant changes from baseline occurred. The mean (+/- SD) recumbency dose of guaifenesin was 131 mg/kg (27) for donkeys and 211 mg/kg (8) for horses. Recovery time to sternal (min) was 15 (SD, 11) for donkeys and 34 (SD, 1.4) for horses. Time to standing was 32 min for donkeys and 36 min for horses. Calculation of AUC (area under the concentration-time curve) microgram/mL) (dose-dependent variable) was 231 (SD, 33) for donkeys and 688 (SD, 110) for horses. The clearance (CL) (mL/hr.kg) was 546 (SD, 73) for donkeys, which was significantly different from 313 (SD, 62) for horses. Mean residence time (MRT) (hr) was 1.2 (SD, 0.1) for donkeys and 2.6 (SD, 0.5) for horses. Volume of distribution Vd(area) (mL/kg) was 678 (SD, 92) for donkeys and 794 (SD, 25) for horses. At the rate of administration used in this study, donkeys required less guaifenesin than horses to produce recumbency, but cleared it more rapidly.

    PMID:9430767 Matthews N, Peck K et al; J Vet Pharmacol Ther 20 (6): 442-6 (1997)

    5.6 Metabolism/Metabolites

    After the oral administration of 400 mg guaifenesin, the agent experiences rapid hydrolysis (more than 60% of the dose hydrolyzed over a range of seven hours) with -(2-methoxyphenoxy)-lactic acid found as the major urinary metabolite but no parent drug detectable in the urine. Moreover, it has been observed that guaifenesin also experiences both oxidation and demethylation. In particular, the medication is quickly metabolized hepatically by way of oxidation to -(2-methoxyphenoxy)-lactic acid. Furthermore, guaifenesin is also demethylated by O-demethylase in liver microsomes to the point where about 40% of an administered dose is excreted as this metabolite in the urine within 3 hours. In fact, O-demethylase appears to be the primary enzyme for the metabolism of guaifenesin and the primary metabolites of the substance are -(2-methoxyphenoxy)-lactic acid and the demethylated hydroxyguaifenesin, both of which are themselves inactive moieties.

    The major urinary metabolite is beta-(2-methoxyphenoxy) lactic acid.

    Medical Economics Co; Physicians Desk Reference: Generics 2nd ed p.1474 (1996)

    It is excreted in urine principally as glucuronates & sulfates.

    Gosselin, R.E., H.C. Hodge, R.P. Smith, and M.N. Gleason. Clinical Toxicology of Commercial Products. 4th ed. Baltimore: Williams and Wilkins, 1976., p. II-240

    Oxidative o-demethylation of glyceryl guaiacolate ether occurred much more rapidly in ip injected male rats than in females. This sex difference in metabolism was paralleled by corresponding difference in o-demethylase activity between male & female animals.

    The Chemical Society. Foreign Compound Metabolism in Mammals Volume 3. London: The Chemical Society, 1975., p. 272

    5.7 Biological Half-Life

    The half-life in plasma observed for guaifenesin is approximately one hour.

    Guaifenesin has a plasma half-life of one hour.

    Medical Economics Co; Physicians Desk Reference: Generics 2nd ed p.1474 (1996)

    Centrally acting muscle relaxant glyceryl guaiacolate ether was found to have t/2 of 56.5 min in male rats and 88.5 min in female rats following ip administration.

    The Chemical Society. Foreign Compound Metabolism in Mammals Volume 3. London: The Chemical Society, 1975., p. 588

    5.8 Mechanism of Action

    Although the exact mechanism of action of guaifenesin may not yet be formally or totally elucidated, it is believed that expectorants like guaifenesin function by increasing mucus secretion. Moreover, it is also further proposed that such expectorants may also act as an irritant to gastric vagal receptors, and recruit efferent parasympathetic reflexes that can elicit glandular exocytosis that is comprised of a less viscous mucus mixture. Subsequently, these actions may provoke coughing that can ultimately flush difficult to access, congealed mucopurulent material from obstructed small airways to facilitate a temporary improvement for the individual. Consequently, while it is generally proposed that guaifenesin functions as an expectorant by helping to loosen phlegm (mucus) and thin bronchial secretions to rid the bronchial passageways of bothersome mucus and make coughs more productive, there has also been research to suggest that guaifenesin possesses and is capable of demonstrating anticonvulsant and muscle relaxant effects to some degree possibly by acting as an NMDA receptor antagonist.

    Guaifenesin is thought to act as an expectorant by increasing the volume and reducing the viscosity of secretions in the trachea and bronchi. Thus it may increase the efficiency of the cough reflex and facilitate removal of the secretions; however, objective evidence for this is limited and conflicting.

    Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1537

    By increasing respiratory tract fluid, guaifenesin reduces the viscosity of tenacious secretions and acts as an expectorant.

    McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007.

    Guaifenesin, a commonly used agent for the treatment of cough, is termed an expectorant since it is believed to alleviate cough discomfort by increasing sputum volume and decreasing its viscosity, thereby promoting effective cough. Despite its common usage, relatively few studies, yielding contrasting results, have been performed to investigate the action and efficacy of guaifenesin. To evaluate the effect of guaifenesin on cough reflex sensitivity. Randomized, double-blind, placebo-controlled trial. Fourteen subjects with acute viral upper respiratory tract infection (URI) and 14 healthy volunteers. On 2 separate days, subjects underwent capsaicin cough challenge 1 to 2 hr after receiving a single, 400-mg dose (capsules) of guaifenesin or matched placebo. Measurements and results: The concentration of capsaicin inducing five or more coughs (C(5)) was determined. Among subjects with URI, mean (+/- SEM) log C(5) after guaifenesin and placebo were 0.92 +/- 0.17 and 0.66 +/- 0.14, respectively (p = 0.028). No effect on cough sensitivity was observed in healthy volunteers. /The/ results demonstrate that guaifenesin inhibits cough reflex sensitivity in subjects with URI, whose cough receptors are transiently hypersensitive, but not in healthy volunteers. Possible mechanisms include a central antitussive effect, or a peripheral effect by increased sputum volume serving as a barrier shielding cough receptors within the respiratory epithelium from the tussive stimulus.

    PMID:14665498 Dicpinigaitis P, Gayle Y; Chest 124 (6): 2178-81(2003)

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    Guaifenesin

    About the Company : DKSH, founded with the goal of improving people's lives, assists businesses with market expansion and business growth in both existing and emerging markets. It has been fostering g...

    DKSH, founded with the goal of improving people's lives, assists businesses with market expansion and business growth in both existing and emerging markets. It has been fostering growth for businesses in Asia and beyond for over 155 years. DKSH operates in 36 markets, is listed on the SIX Swiss Exchange, employs 33,100 specialists, and generated net sales of CHF 11.1 billion in 2021. It is the leading global distributor of innovative pharma ingredients for pharmaceutical synthesis and formulation. It offers a range of products, ranging from animal care products to packaging materials, intermediates to nutraceuticals, and APIs to excipients.
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    09

    Jai Radhe Sales

    India
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    Virtual BoothJai Radhe Sales is your partner for all your sourcing needs.

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    Guaifenesin

    About the Company : Jai Radhe Sales was founded in 1999 as an out-of-the-box distribution firm specializing in the global supply of high-quality pharmaceutical ingredients. The firm provides complete ...

    Jai Radhe Sales was founded in 1999 as an out-of-the-box distribution firm specializing in the global supply of high-quality pharmaceutical ingredients. The firm provides complete sourcing solutions for pharmaceutical products from India, including technical and regulatory assistance. It believes in providing its customers with high-quality products at reasonable prices. It has always endeavored to achieve global standards in the field of pharmaceuticals and has carved out a niche for itself through new methods based on current market needs. Today, it has established itself as a truly global company, with exports to almost every continent.
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    10

    Synthokem Labs

    India
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    Virtual BoothSynthokem Labs specializes in producing APIs and intermediates for the global pharma industry.

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    Guaifenesin

    About the Company : Synthokem Labs Pvt Ltd is a privately owned company established in 1978, specializing in the production of Active Pharmaceutical Ingredients and Drug Intermediates. Operating acros...

    Synthokem Labs Pvt Ltd is a privately owned company established in 1978, specializing in the production of Active Pharmaceutical Ingredients and Drug Intermediates. Operating across two states, Telangana and Andhra Pradesh, in India, the company has earned global recognition for its expertise in manufacturing and distributing a diverse range of products. With a strong focus on research and development, Synthokem Labs is dedicated to offering accessible and affordable pharmaceutical solutions to those in need.
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    18-Jan-2021
    29-Nov-2024
    KGS
    overview
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    Average Price (USD/KGS)

    Number of Transactions

    Total Quantity (KGS)

    Total Value (USD)

    Quantity (KGS) & Unit rate (USD/KGS) over time

    API Imports and Exports

    Importing Country Total Quantity
    (KGS)    		 Average Price
    (USD/KGS)    		 Number of Transactions

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    DRUG PRODUCT COMPOSITIONS

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    DOSAGE - SOLUTION;ORAL - 200MG/5ML;2.5MG/5ML

    USFDA APPLICATION NUMBER - 205474

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    DOSAGE - TABLET, EXTENDED RELEASE;ORAL - 1.2G...DOSAGE - TABLET, EXTENDED RELEASE;ORAL - 1.2GM

    USFDA APPLICATION NUMBER - 21282

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    DOSAGE - TABLET, EXTENDED RELEASE;ORAL - 600M...DOSAGE - TABLET, EXTENDED RELEASE;ORAL - 600MG

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