Peringatan Keamanan

Toxicity after overdose may involve CNS effects like extreme drowsiness, lethargy, confusion, delirium, and coma in adults; paradoxical excitation, irritability, hyperactivity, insomnia, hallucinations, seizures, and respiratory depression or arrest in infants and young children, CNS adverse effects predominate o er cardiac adverse effects; death may occur within hours after ingestion of drug in untreated patients; rhabdomyolysis has also been reported A32705.

Phenyltoloxamine

DB11160

small molecule approved

Deskripsi

Phenyltoloxamine is an antihistamine drug with sedative and analgesic effects. It is a H1 receptor blocker and a member of the ethanolamine class of antihistaminergic drugs. It is available in combination products that also contain other analgesics and antitussives such as acetaminophen. Phenyltoloxamine citrate is the more common salt form that acts as an active ingredient in pharmaceutical products and promotes hay fever relief via reversing the effects of histamine. Phenyltoloxamine acts as an adjuvant analgesic, which augments the analgesic effect of acetaminophen. It also potentiates the effects of other drugs, such as codeine and codeine derivatives.

Although phenyltoloxamine's ability to potentiate the effects of analgesics may be explained in part by its chemical nature as a first-generation H1 antihistamine that is capable of crossing the blood-brain barrier and causing tranquilizing effects at CNS histamine receptors, many of the drug's specific pharmacokinetics are not readily available - perhaps also because many early (phenyltoloxamine was involved in studies as early as the 1950s) first-generation antihistamines were not optimally investigated A32705. Nevertheless, phenyltoloxamine is used to a fairly limited extent in contemporary medicine, with only very few products involving it as an active ingredient.

Struktur Molekul 2D

Berat 255.361
Wujud -

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Readily accessible data regarding the half-life of phenyltoloxamine is not available. In fact, many first-generation H1 antihistamines have never had their pharmacokinetics (ie. absorption, distribution, metabolism, and elimination) optimally investigated [A32705].
Volume Distribusi Readily accessible data regarding the volume of distribution of phenyltoloxamine is not available. In fact, many first-generation H1 antihistamines have never had their pharmacokinetics (ie. absorption, distribution, metabolism, and elimination) optimally investigated [A32705].
Klirens (Clearance) Readily accessible data regarding the clearance of phenyltoloxamine is not available. In fact, many first-generation H1 antihistamines have never had their pharmacokinetics (ie. absorption, distribution, metabolism, and elimination) optimally investigated [A32705].

Absorpsi

Readily accessible data regarding the absorption of phenyltoloxamine is not available. In fact, many first-generation H1 antihistamines have never had their pharmacokinetics (ie. absorption, distribution, metabolism, and elimination) optimally investigated A32705.

Metabolisme

Readily accessible data regarding the metabolism of phenyltoloxamine is not available. In fact, many first-generation H1 antihistamines have never had their pharmacokinetics (ie. absorption, distribution, metabolism, and elimination) optimally investigated A32705.

Rute Eliminasi

Readily accessible data regarding the primary route of elimination of phenyltoloxamine is not available. In fact, many first-generation H1 antihistamines have never had their pharmacokinetics (ie. absorption, distribution, metabolism, and elimination) optimally investigated A32705.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

D(2) dopamine receptor DRD2
D(1B) dopamine receptor DRD5
D(1A) dopamine receptor DRD1
D(4) dopamine receptor DRD4
Histamine H1 receptor Hrh1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23282578
    Simons FE, Simons KJ: H1 antihistamines: current status and future directions. World Allergy Organ J. 2008 Sep;1(9):145-55. doi: 10.1097/WOX.0b013e318186fb3a.
  • PMID: 5492933
  • PMID: 2569485
    Sunshine A, Zighelboim I, De Castro A, Sorrentino JV, Smith DS, Bartizek RD, Olson NZ: Augmentation of acetaminophen analgesia by the antihistamine phenyltoloxamine. J Clin Pharmacol. 1989 Jul;29(7):660-4.
  • PMID: 821705
    Gilbert MM, De Sola Pool N, Schecter C: Analgesic/calmative effects of acetaminophen and phenyltoloxamine in treatment of simple nervous tension accompanied by headache. Curr Ther Res Clin Exp. 1976 Jul;20(1):53-8.
  • PMID: 23282332
    Church DS, Church MK: Pharmacology of antihistamines. World Allergy Organ J. 2011 Mar;4(3 Suppl):S22-7. doi: 10.1097/WOX.0b013e3181f385d9.
  • PMID: 6483639
    Forbes JA, Barkaszi BA, Ragland RN, Hankle JJ: Analgesic effect of acetaminophen, phenyltoloxamine and their combination in postoperative oral surgery pain. Pharmacotherapy. 1984 Jul-Aug;4(4):221-6.
  • PMID: 13096396
    HOEKSTRA JB, TISCH DE, RAKIETEN N, DICKISON HL: Pharmacological properties of a new antihistaminic agent, phenyltoloxamine (Bristamin). J Am Pharm Assoc Am Pharm Assoc. 1953 Oct;42(10):587-93.

Contoh Produk & Brand

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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