Peringatan Keamanan

The most prevalent signs and symptoms associated with an overdose of guaifenesin have been nausea and vomiting L6100.

Although adequate and well-controlled studies in pregnant women have not been performed, the Collaborative Perinatal Project monitored 197 mother-child pairs exposed to guaifenesin during the first trimester L6100. An increased occurrence of inguinal hernias was found in the neonates L6100. However, congenital defects were not strongly associated with guaifenesin use during pregnancy in 2 large groups of mother-child pairs L6100.

Moreover, guaifenesin is excreted in breast milk in small quantities L6100. Subsequently, caution should be exercised by balancing the potential benefit of treatment against any possible risks L6100.

Additionally, an LD50 value of 1510 mg/kg (rat, oral) has been reported for guaifenesin MSDS.

Guaifenesin

DB00874

small molecule approved investigational vet_approved

Deskripsi

Guaifenesin possesses a storied history, having been originally formally approved by the US FDA in 1952 and continues to be one of very few - if not perhaps the only drug that is readily available and used as an expectorant F4525. Since that time the agent has been a combination component of various prescription and non-prescription over-the-counter cough and cold products and is currently a widely available over-the-counter generic medication F4525. Although it is principally believed that guaifenesin elicits an action to facilitate productive cough to manage chest congestion A177661, L6100, F4516, F4522, F4525, it is not known whether the agent can reliably mitigate coughing.

Regardless, on March 1, 2007, the FDA received a petition asking the FDA to notify the public that some antitussives, expectorants, decongestants, antihistamines, and cough/cold combinations are not known to be safe and effective in children under the age of 6 years F4525. After the negotiation between FDA and major manufacturers, a voluntary transition of labels for not using guaifenesin in children under the age of 4 years was endorsed by FDA in 2008 F4525.

Furthermore, there has also been contemporary 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 A177652.

Struktur Molekul 2D

Berat 198.2158
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life in plasma observed for guaifenesin is approximately one hour [A177676, L6079, L6100, F4522, F4525].
Volume Distribusi The geometric mean apparent volume of distribution of guaifenesin determined in healthy adult subjects is 116L (CV=45.7%) [F4525].
Klirens (Clearance) The mean clearance recorded for guaifenesin is about 94.8 L/hr (CV=51.4%) [F4525].

Absorpsi

Studies have shown that guaifenesin is well absorbed from and along the gastrointestinal tract after oral administration A177634, F4522, L6100.

Metabolisme

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 A177676, L6100. Moreover, it has been observed that guaifenesin also experiences both oxidation and demethylation A177676. In particular, the medication is quickly metabolized hepatically by way of oxidation to ?-(2-methoxyphenoxy)-lactic acid A177676. 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 A177676. 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 A177676.

Rute Eliminasi

After administration, guaifenesin is metabolized and then largely excreted in the urine A177676, L6079, L6100, F4522, F4525.

Interaksi Makanan

2 Data
  • 1. Take with a full glass of water.
  • 2. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

NMDA receptor GRIN1

Referensi & Sumber

Synthesis reference: Wilfred P. Shum, Harry Mazurek, Jian Chen, "Process for producing enantiomerically enriched guaifenesin." U.S. Patent US5495052, issued August, 1949.
Artikel (PubMed)
  • PMID: 26632082
    Thompson GA, Solomon G, Albrecht HH, Reitberg DP, Guenin E: Guaifenesin Pharmacokinetics Following Single-Dose Oral Administration in Children Aged 2 to 17 Years. J Clin Pharmacol. 2016 Jul;56(7):894-901. doi: 10.1002/jcph.682. Epub 2016 Jan 24.
  • PMID: 19166957
    Kagan L, Lavy E, Hoffman A: Effect of mode of administration on guaifenesin pharmacokinetics and expectorant action in the rat model. Pulm Pharmacol Ther. 2009 Jun;22(3):260-5. doi: 10.1016/j.pupt.2008.12.020. Epub 2009 Jan 6.
  • PMID: 23825891
    Keshavarz M, Showraki A, Emamghoreishi M: Anticonvulsant Effect of Guaifenesin against Pentylenetetrazol-Induced Seizure in Mice. Iran J Med Sci. 2013 Jun;38(2):116-21.
  • PMID: 15842963
    Yuta A, Baraniuk JN: Therapeutic approaches to mucus hypersecretion. Curr Allergy Asthma Rep. 2005 May;5(3):243-51.
  • PMID: 29238574
    Albrecht HH, Dicpinigaitis PV, Guenin EP: Role of guaifenesin in the management of chronic bronchitis and upper respiratory tract infections. Multidiscip Respir Med. 2017 Dec 11;12:31. doi: 10.1186/s40248-017-0113-4. eCollection 2017.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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