Peringatan Keamanan

Acute oral LD50 is 810 mg/kg in rat and 230 mg/kg in mouse MSDS.

Pentoxyverine

DB11186

small molecule approved investigational withdrawn

Deskripsi

Pentoxyverine, also referred to as carbetapentane, is a non-opioid central acting antitussive with antimuscarinic, anticonvulsant ^A32717, and local anesthetic properties. It is an active ingredient in over-the-counter cough suppressants in combination with guaifenesin and H1-receptor antagonists ^A32160. Pentoxyverine acts on sigma-1 receptors, as well as kappa and mu-opioid receptors.

The FDA withdrew the use of all oral gel drug products containing pentoxyverine citrate.^L43942 Other forms of pentoxyverine citrate continue to be marketed.

Struktur Molekul 2D

Berat 333.472

Wujud solid

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life is 2.3 hours following oral dosing [A32160].

Volume Distribusi No pharmacokinetic data available.

Klirens (Clearance) No pharmacokinetic data available.

Absorpsi

In humans, maximum plasma concentrations are achieved 1.2 hours after oral dosing ^A32160.

Metabolisme

No pharmacokinetic data available.

Rute Eliminasi

No pharmacokinetic data available.

Interaksi Makanan

1 Data

1. Avoid alcohol. Concomitant use of pentoxyverine with alcohol may cause additive CNS depressant effects.

Interaksi Obat

0 Data

Tidak ada data.

Target Protein

Sigma non-opioid intracellular receptor 1 SIGMAR1

Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2

Voltage-gated sodium channel alpha subunit SCN1A

Kappa-type opioid receptor OPRK1

Mu-type opioid receptor OPRM1

Referensi & Sumber

Artikel (PubMed)

PMID: 24671376
Dicpinigaitis PV, Morice AH, Birring SS, McGarvey L, Smith JA, Canning BJ, Page CP: Antitussive drugs--past, present, and future. Pharmacol Rev. 2014 Mar 26;66(2):468-512. doi: 10.1124/pr.111.005116. Print 2014.
PMID: 14691051
Brown C, Fezoui M, Selig WM, Schwartz CE, Ellis JL: Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol. 2004 Jan;141(2):233-40. doi: 10.1038/sj.bjp.0705605. Epub 2003 Dec 22.
PMID: 19034038
Deisemann H, Ahrens N, Schlobohm I, Kirchhoff C, Netzer R, Moller C: Effects of common antitussive drugs on the hERG potassium channel current. J Cardiovasc Pharmacol. 2008 Dec;52(6):494-9. doi: 10.1097/FJC.0b013e31818eec8d.
PMID: 3768695
Tortella FC, Musacchio JM: Dextromethorphan and carbetapentane: centrally acting non-opioid antitussive agents with novel anticonvulsant properties. Brain Res. 1986 Sep 24;383(1-2):314-8.
PMID: 2666123
Leander JD: Evaluation of dextromethorphan and carbetapentane as anticonvulsants and N-methyl-D-aspartic acid antagonists in mice. Epilepsy Res. 1989 Jul-Aug;4(1):28-33.
PMID: 23872380
Leung YM, Tzeng JI, Kuo CS, Chen YW, Chu CC, Wang JJ: The use of carbetapentane for spinal anesthesia and use-dependent block of sodium currents. Eur J Pharmacol. 2013 Aug 15;714(1-3):366-72. doi: 10.1016/j.ejphar.2013.07.013. Epub 2013 Jul 16.

Link

Contoh Produk & Brand

Produk: 17 • International brands: 0

Produk

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Suspension • - • Oral • US
Carbatuss

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Corzall

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Corzall PE

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Corzall Plus

Liquid • - • Oral • US
Exall

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Exall D

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Menampilkan 8 dari 17 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.