Peringatan Keamanan

Bioallethrin can produce hypersensitivity reactions in patients sensitive to ragweed or chrysanthemum L2609. Ingestion of bioallethrin can produce life-threatening convulsions or coma. Less serious toxic effects include sore throat, nausea, vomiting, abdominal pain, mouth ulceration, increased secretions and/or dysphagia. Systemic effects include dizziness, headache and fatigue are common, and palpitations, chest tightness and blurred vision and occur 4-48 h after exposure.

Bioallethrin is not carcinogenic or mutagenic L991. In rats doses over 58.7 mg/kg/day produce reproductive effects and doses over 125 mg/kg/day are embryotoxic.

### Observed LD50 for various routes in animal studies L991:

Rat

- Male Oral - 709 mg/kg
- Female Oral - 1040 mg/kg
- Inhalation - 2.51 mg/L

Rabbit

- Dermal - >3000 mg/kg

Bioallethrin

DB13746

small molecule approved experimental

Deskripsi

Bioallethrin refers to a mixture of two of the allethrin isomers (1R,trans;1R and 1R,trans;1S) in an approximate ratio of 1:1, where both isomers are active ingredients. A mixture of the two same stereoisomers, but in an approximate ratio of R:S in 1:3, is called esbiothrin. A mixture containing only S-forms of allethrin is referred to as esbioallethrin or S-bioallethrin. Bioallethrin is a synthetic pyrethroid used as a pesticide against household pest insects such as mosquitoes, houseflies and cockroaches. It is claimed to have low mammalian toxicity.

Struktur Molekul 2D

Berat 302.414
Wujud liquid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Metabolism of bioallethrin in both rats and humans is considered to be virtually 100% oxidative A32818,A32819. This is because bioallethrin is very resistant to hydrolysis of its ester group although a negligible amount of hydrolysis may occur. In humans bioallethrin is metabolized primarily by CYP2C19 with some metabolism by CYP2C8, CYP3A4, and CYP2C9*2 A32818. The metabolites produced include primary alcohols via allylic oxidation near the cyclopropane group and subsequent oxidation to carboxylic acid, formation of a primary alcohol via oxidation of a methyl group to located on the cyclopropane portion of the molecule, formation of a primary alcohol via allylic oxidation near the 5-membered ring or formation of an epoxide at this location and subsequent hydrolysis to a diol. In rats bioallethrin has been found to be metabolized mainly by CYP2C6, CYP2C11, and CYP3A1 with some contribution from CYP1A1, CYP2A1 and CYP3A2 A32818. Rats appear to metabolize bioallethrin at about 15 times the rate of humans.

Rute Eliminasi

Pyrethroids are excreted in both the feces and urine but values specific to bioallethrin are not available A32819.

Interaksi Obat

186 Data
Esmolol Esmolol may increase the arrhythmogenic activities of Bioallethrin.
Betaxolol Betaxolol may increase the arrhythmogenic activities of Bioallethrin.
Dofetilide Dofetilide may increase the arrhythmogenic activities of Bioallethrin.
Metoprolol Metoprolol may increase the arrhythmogenic activities of Bioallethrin.
Isradipine Isradipine may increase the arrhythmogenic activities of Bioallethrin.
Disopyramide Disopyramide may increase the arrhythmogenic activities of Bioallethrin.
Lidocaine Lidocaine may increase the arrhythmogenic activities of Bioallethrin.
Ibutilide Ibutilide may increase the arrhythmogenic activities of Bioallethrin.
Atenolol Atenolol may increase the arrhythmogenic activities of Bioallethrin.
Diltiazem Diltiazem may increase the arrhythmogenic activities of Bioallethrin.
Trimethadione Trimethadione may increase the arrhythmogenic activities of Bioallethrin.
Timolol Timolol may increase the arrhythmogenic activities of Bioallethrin.
Mexiletine Mexiletine may increase the arrhythmogenic activities of Bioallethrin.
Amlodipine Amlodipine may increase the arrhythmogenic activities of Bioallethrin.
Digoxin Digoxin may increase the arrhythmogenic activities of Bioallethrin.
Nimodipine Nimodipine may increase the arrhythmogenic activities of Bioallethrin.
Nisoldipine Nisoldipine may increase the arrhythmogenic activities of Bioallethrin.
Hyoscyamine Hyoscyamine may increase the arrhythmogenic activities of Bioallethrin.
Sotalol Sotalol may increase the arrhythmogenic activities of Bioallethrin.
Acetyldigitoxin Acetyldigitoxin may increase the arrhythmogenic activities of Bioallethrin.
Lercanidipine Lercanidipine may increase the arrhythmogenic activities of Bioallethrin.
Lamotrigine Lamotrigine may increase the arrhythmogenic activities of Bioallethrin.
Cinnarizine Cinnarizine may increase the arrhythmogenic activities of Bioallethrin.
Propranolol Propranolol may increase the arrhythmogenic activities of Bioallethrin.
Atropine Atropine may increase the arrhythmogenic activities of Bioallethrin.
Ethosuximide Ethosuximide may increase the arrhythmogenic activities of Bioallethrin.
Bisoprolol Bisoprolol may increase the arrhythmogenic activities of Bioallethrin.
Nicardipine Nicardipine may increase the arrhythmogenic activities of Bioallethrin.
Adenosine Adenosine may increase the arrhythmogenic activities of Bioallethrin.
Magnesium sulfate Magnesium sulfate may increase the arrhythmogenic activities of Bioallethrin.
Verapamil Verapamil may increase the arrhythmogenic activities of Bioallethrin.
Losartan Losartan may increase the arrhythmogenic activities of Bioallethrin.
Moricizine Moricizine may increase the arrhythmogenic activities of Bioallethrin.
Levomenthol Levomenthol may increase the arrhythmogenic activities of Bioallethrin.
Loperamide Loperamide may increase the arrhythmogenic activities of Bioallethrin.
Alprenolol Alprenolol may increase the arrhythmogenic activities of Bioallethrin.
Quinidine Quinidine may increase the arrhythmogenic activities of Bioallethrin.
Zonisamide Zonisamide may increase the arrhythmogenic activities of Bioallethrin.
Levosimendan Levosimendan may increase the arrhythmogenic activities of Bioallethrin.
Felodipine Felodipine may increase the arrhythmogenic activities of Bioallethrin.
Procainamide Procainamide may increase the arrhythmogenic activities of Bioallethrin.
Nitrendipine Nitrendipine may increase the arrhythmogenic activities of Bioallethrin.
Tocainide Tocainide may increase the arrhythmogenic activities of Bioallethrin.
Perhexiline Perhexiline may increase the arrhythmogenic activities of Bioallethrin.
Deslanoside Deslanoside may increase the arrhythmogenic activities of Bioallethrin.
Nifedipine Nifedipine may increase the arrhythmogenic activities of Bioallethrin.
Carvedilol Carvedilol may increase the arrhythmogenic activities of Bioallethrin.
Bretylium Bretylium may increase the arrhythmogenic activities of Bioallethrin.
Propafenone Propafenone may increase the arrhythmogenic activities of Bioallethrin.
Acebutolol Acebutolol may increase the arrhythmogenic activities of Bioallethrin.
Flecainide Flecainide may increase the arrhythmogenic activities of Bioallethrin.
Nadolol Nadolol may increase the arrhythmogenic activities of Bioallethrin.
Encainide Encainide may increase the arrhythmogenic activities of Bioallethrin.
Bepridil Bepridil may increase the arrhythmogenic activities of Bioallethrin.
Practolol Practolol may increase the arrhythmogenic activities of Bioallethrin.
Mibefradil Mibefradil may increase the arrhythmogenic activities of Bioallethrin.
Digitoxin Digitoxin may increase the arrhythmogenic activities of Bioallethrin.
Ajmaline Ajmaline may increase the arrhythmogenic activities of Bioallethrin.
Aprindine Aprindine may increase the arrhythmogenic activities of Bioallethrin.
Oxprenolol Oxprenolol may increase the arrhythmogenic activities of Bioallethrin.
Dexpropranolol Dexpropranolol may increase the arrhythmogenic activities of Bioallethrin.
Nimesulide Nimesulide may increase the arrhythmogenic activities of Bioallethrin.
Prenylamine Prenylamine may increase the arrhythmogenic activities of Bioallethrin.
Cyclandelate Cyclandelate may increase the arrhythmogenic activities of Bioallethrin.
Flunarizine Flunarizine may increase the arrhythmogenic activities of Bioallethrin.
Fluspirilene Fluspirilene may increase the arrhythmogenic activities of Bioallethrin.
Celiprolol Celiprolol may increase the arrhythmogenic activities of Bioallethrin.
Dronedarone Dronedarone may increase the arrhythmogenic activities of Bioallethrin.
Nebivolol Nebivolol may increase the arrhythmogenic activities of Bioallethrin.
Clevidipine Clevidipine may increase the arrhythmogenic activities of Bioallethrin.
Azimilide Azimilide may increase the arrhythmogenic activities of Bioallethrin.
Methsuximide Methsuximide may increase the arrhythmogenic activities of Bioallethrin.
Seletracetam Seletracetam may increase the arrhythmogenic activities of Bioallethrin.
Nylidrin Nylidrin may increase the arrhythmogenic activities of Bioallethrin.
Tedisamil Tedisamil may increase the arrhythmogenic activities of Bioallethrin.
Vernakalant Vernakalant may increase the arrhythmogenic activities of Bioallethrin.
Ziconotide Ziconotide may increase the arrhythmogenic activities of Bioallethrin.
Dotarizine Dotarizine may increase the arrhythmogenic activities of Bioallethrin.
Cariporide Cariporide may increase the arrhythmogenic activities of Bioallethrin.
Xylometazoline Xylometazoline may increase the arrhythmogenic activities of Bioallethrin.
Nilvadipine Nilvadipine may increase the arrhythmogenic activities of Bioallethrin.
Sparteine Sparteine may increase the arrhythmogenic activities of Bioallethrin.
Tranilast Tranilast may increase the arrhythmogenic activities of Bioallethrin.
Fasudil Fasudil may increase the arrhythmogenic activities of Bioallethrin.
Bupranolol Bupranolol may increase the arrhythmogenic activities of Bioallethrin.
Agmatine Agmatine may increase the arrhythmogenic activities of Bioallethrin.
Indenolol Indenolol may increase the arrhythmogenic activities of Bioallethrin.
Fendiline Fendiline may increase the arrhythmogenic activities of Bioallethrin.
Eperisone Eperisone may increase the arrhythmogenic activities of Bioallethrin.
Trimebutine Trimebutine may increase the arrhythmogenic activities of Bioallethrin.
Pinaverium Pinaverium may increase the arrhythmogenic activities of Bioallethrin.
Nicorandil Nicorandil may increase the arrhythmogenic activities of Bioallethrin.
Melperone Melperone may increase the arrhythmogenic activities of Bioallethrin.
Barnidipine Barnidipine may increase the arrhythmogenic activities of Bioallethrin.
Aranidipine Aranidipine may increase the arrhythmogenic activities of Bioallethrin.
Azelnidipine Azelnidipine may increase the arrhythmogenic activities of Bioallethrin.
Benidipine Benidipine may increase the arrhythmogenic activities of Bioallethrin.
Cilnidipine Cilnidipine may increase the arrhythmogenic activities of Bioallethrin.
Darodipine Darodipine may increase the arrhythmogenic activities of Bioallethrin.
Efonidipine Efonidipine may increase the arrhythmogenic activities of Bioallethrin.

Target Protein

Sodium channel protein
Voltage-gated sodium channel alpha subunit SCN1A
Voltage-dependent calcium channel CACNG1
Voltage-dependent T-type calcium channel CACNA1G
Voltage-dependent P/Q-type calcium channel CACNA1A
Voltage-dependent L-type calcium channel CACNA1C

Referensi & Sumber

Artikel (PubMed)
  • PMID: 8841090
    Narahashi T: Neuronal ion channels as the target sites of insecticides. Pharmacol Toxicol. 1996 Jul;79(1):1-14.
  • PMID: 20881019
    Cao Z, Shafer TJ, Murray TF: Mechanisms of pyrethroid insecticide-induced stimulation of calcium influx in neocortical neurons. J Pharmacol Exp Ther. 2011 Jan;336(1):197-205. doi: 10.1124/jpet.110.171850. Epub 2010 Sep 29.
  • PMID: 2881709
    Clark JM, Matsumura F: The action of two classes of pyrethroids on the inhibition of brain Na-Ca and Ca + Mg ATP hydrolyzing activities of the American cockroach. Comp Biochem Physiol C. 1987;86(1):135-45.
  • PMID: 2422664
    Gusovsky F, Hollingsworth EB, Daly JW: Regulation of phosphatidylinositol turnover in brain synaptoneurosomes: stimulatory effects of agents that enhance influx of sodium ions. Proc Natl Acad Sci U S A. 1986 May;83(9):3003-7.
  • PMID: 7135402
    Staatz CG, Bloom AS, Lech JJ: Effect of pyrethroids on 3Hkainic acid binding to mouse forebrain membranes. Toxicol Appl Pharmacol. 1982 Jul;64(3):566-9.
  • PMID: 14634047
    Hildebrand ME, McRory JE, Snutch TP, Stea A: Mammalian voltage-gated calcium channels are potently blocked by the pyrethroid insecticide allethrin. J Pharmacol Exp Ther. 2004 Mar;308(3):805-13. doi: 10.1124/jpet.103.058792. Epub 2003 Nov 21.
  • PMID: 18948380
    Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. doi: 10.1124/dmd.108.022343. Epub 2008 Oct 23.
  • PMID: 789062
    Miyamoto J: Degradation, metabolism and toxicity of synthetic pyrethroids. Environ Health Perspect. 1976 Apr;14:15-28.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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