Peringatan Keamanan

Barbiturates are associated with congenital heart malformations, facial clefts, and other malformations. 5
There is no available data on the use of barbexaclone in pregnancy. One case of a 36 year old women
who used barbexaclone 300mg/day and oxcarbezine 600mg/day for 2 years before the pregnancy and 10 weeks into
pregnancy resulted in an uncomplicated delivery and normal physical, motor, and mental development at 24 months of age.
5

Barbexaclone

DB09001

small molecule experimental

Deskripsi

Barbexaclone, a salt compound of propylhexedrine and phenobarbital, is a potent antiepileptic. By weight, barbexaclone is 40% propylhexedrine and 60% phenobarbital. While barbexaclone has sedative properties, propylhexedrine has psychostimulant properties intended to offset these sedative effects. Pharmacokinetic studies have demonstrated that the pharmacokinetics of phenobarbital given as barbexaclone are not affected by propylhexedrine. Several reports from Spanish and Italian literature suggest that barbexaclone is at least as effective as phenobarbital in adults and children, while being better tolerated and having less sedative properties. These reports were conducted in a small series of patients in the 1970s and 1980s, and have yet to be confirmed by larger controlled trials. Despite the lack of controlled trials, barbexaclone was used widely in Turkey until it was discontinued in 2009.

Barbexaclone exists in 25mg and 100mg tablets. 100mg of barbexaclone is equivalent to 60mg of phenobarbital. With this difference in potency in mind, other pharmacokinetic considerations such as dose titration, daily dosing, and optimal plasma concentration can be considered the same as for the equivalent amount of phenobarbital.

There has been a case of barbexaclone abuse due to the amphetamine like properties of propylhexedrine, although the comparative abuse potential is much lower than amphetamine.

Struktur Molekul 2D

Berat 387.524
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) After IV administration in mice, levels of phenobarbital declined exponentially with a half life of 7.5h. [3] For propylhexedrine t0.5a = 0.31h and t0.5b = 2.5h.
Volume Distribusi In mice, the volume of distribution was 0.78L/kg of phenobarbital, and 19.3L/kg for propylhexedrine, after i.v. administration. [3] High but unequal tissue accumulation of propylhexedrine was observed in mice: lung = kidney > liver = brain > spleen > heart > skeletal muscle. [3]
Klirens (Clearance) -

Absorpsi

After oral administration of barbexaclone in mice the maximum plasma levels of prophylhexedrine appeared after 4 minutes, and propylhexedrine was seen to penetrate the blood brain barrier rapidly. Bioavailability (AUC oral / AUC iv) = 0.37. 3 Phenobarbital was observed to reach the blood more slowly, and brain uptake was a slow process. Equilibrium concentrations with plasma reached after 30 minutes after i.v injection. 3

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

1139 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Barbexaclone.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Barbexaclone.
Buprenorphine Barbexaclone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Barbexaclone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Barbexaclone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Barbexaclone.
Hydrocodone Barbexaclone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Barbexaclone.
Magnesium sulfate The therapeutic efficacy of Barbexaclone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Barbexaclone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Barbexaclone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Barbexaclone.
Mirtazapine Barbexaclone may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Barbexaclone.
Orphenadrine Barbexaclone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Barbexaclone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Pramipexole Barbexaclone may increase the sedative activities of Pramipexole.
Ropinirole Barbexaclone may increase the sedative activities of Ropinirole.
Rotigotine Barbexaclone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Barbexaclone.
Sodium oxybate Barbexaclone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Barbexaclone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Barbexaclone.
Thalidomide Barbexaclone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Barbexaclone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Mefloquine The therapeutic efficacy of Barbexaclone can be decreased when used in combination with Mefloquine.
Orlistat Orlistat can cause a decrease in the absorption of Barbexaclone resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetaminophen The metabolism of Acetaminophen can be increased when combined with Barbexaclone.
Propacetamol The metabolism of Propacetamol can be increased when combined with Barbexaclone.
Chloramphenicol The metabolism of Barbexaclone can be decreased when combined with Chloramphenicol.
Doxycycline The serum concentration of Doxycycline can be decreased when it is combined with Barbexaclone.
Felbamate The serum concentration of Barbexaclone can be increased when it is combined with Felbamate.
Griseofulvin The serum concentration of Griseofulvin can be decreased when it is combined with Barbexaclone.
Lamotrigine The serum concentration of Lamotrigine can be decreased when it is combined with Barbexaclone.
Mianserin The therapeutic efficacy of Barbexaclone can be decreased when used in combination with Mianserin.
Primidone The risk or severity of adverse effects can be increased when Primidone is combined with Barbexaclone.
Methylphenobarbital The risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Barbexaclone.
Phenobarbital The risk or severity of adverse effects can be increased when Phenobarbital is combined with Barbexaclone.
Pyridoxine The metabolism of Barbexaclone can be increased when combined with Pyridoxine.
Teniposide The serum concentration of Teniposide can be decreased when it is combined with Barbexaclone.
Ulipristal The serum concentration of Ulipristal can be decreased when it is combined with Barbexaclone.
Voriconazole The serum concentration of Voriconazole can be decreased when it is combined with Barbexaclone.
Topotecan Barbexaclone may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Barbexaclone.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Barbexaclone.
Perampanel The metabolism of Perampanel can be increased when combined with Barbexaclone.
Warfarin The metabolism of Warfarin can be increased when combined with Barbexaclone.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Barbexaclone.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Barbexaclone.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Barbexaclone.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Barbexaclone.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Barbexaclone.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Barbexaclone.
Aminophylline The therapeutic efficacy of Barbexaclone can be decreased when used in combination with Aminophylline.
Meperidine Barbexaclone may increase the hypotensive and central nervous system depressant (CNS depressant) activities of Meperidine.
Somatostatin The risk or severity of adverse effects can be increased when Somatostatin is combined with Barbexaclone.
Ethanol Barbexaclone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Barbexaclone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Barbexaclone.
Fluvoxamine The risk or severity of adverse effects can be increased when Barbexaclone is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Barbexaclone is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Barbexaclone is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Barbexaclone is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Barbexaclone is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Barbexaclone is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Barbexaclone is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Barbexaclone is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Barbexaclone is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Barbexaclone is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Barbexaclone is combined with Dapoxetine.
Desvenlafaxine The risk or severity of adverse effects can be increased when Barbexaclone is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Barbexaclone is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Barbexaclone is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Barbexaclone is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Barbexaclone is combined with Alaproclate.
Cyclosporine The metabolism of Cyclosporine can be increased when combined with Barbexaclone.
Methyclothiazide The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Methyclothiazide.
Chlorthalidone The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Chlorthalidone.
Bendroflumethiazide The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Bendroflumethiazide.
Metolazone The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Metolazone.
Benzthiazide The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Benzthiazide.
Hydroflumethiazide The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Hydroflumethiazide.
Indapamide The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Indapamide.
Chlorothiazide The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Chlorothiazide.
Hydrochlorothiazide The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Hydrochlorothiazide.
Trichlormethiazide The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Trichlormethiazide.
Polythiazide The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Polythiazide.
Quinethazone The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Quinethazone.
Cyclopenthiazide The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Cyclopenthiazide.
Epitizide The risk or severity of hypotension and orthostatic hypotension can be increased when Barbexaclone is combined with Epitizide.
Protriptyline The metabolism of Protriptyline can be increased when combined with Barbexaclone.
Amoxapine The metabolism of Amoxapine can be increased when combined with Barbexaclone.
Desipramine The metabolism of Desipramine can be increased when combined with Barbexaclone.
Amineptine The metabolism of Amineptine can be increased when combined with Barbexaclone.
Dimetacrine The metabolism of Dimetacrine can be increased when combined with Barbexaclone.
Butriptyline The metabolism of Butriptyline can be increased when combined with Barbexaclone.
Dosulepin The metabolism of Dosulepin can be increased when combined with Barbexaclone.
Oxaprotiline The metabolism of Oxaprotiline can be increased when combined with Barbexaclone.
Opipramol The metabolism of Opipramol can be increased when combined with Barbexaclone.
Amitriptylinoxide The metabolism of Amitriptylinoxide can be increased when combined with Barbexaclone.

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23981808
    Bolukbasi F, Delil S, Bulus E, Senturk A, Yeni N, Karaagac N: End of the barbexaclone era: an experience of treatment withdrawal. Epileptic Disord. 2013 Sep;15(3):311-3. doi: 10.1684/epd.2013.0605.
  • PMID: 6139756
    Iven H, Feldbusch E: Pharmacokinetics of phenobarbital and propylhexedrine after administration of barbexaclone in the mouse. Naunyn Schmiedebergs Arch Pharmacol. 1983 Sep;324(2):153-9.
  • PMID: 14968233
    Yaris F, Kadioglu M, Kesim M, Ulku C, Yaris E, Kalyoncu NI: Barbexaclone use in pregnancy. Saudi Med J. 2004 Feb;25(2):245-6.
Textbook
  • ISBN: 0-632-06046-8
    Shorvon, Simon D.;Dodson, W. E.;Fish, David;Perucca, Emilio;Aminoff, Michael J. (2004). The Treatment of Epilepsy (2nd ed.). John Wiley & Sons.

Contoh Produk & Brand

Produk: 0 • International brands: 1
International Brands
  • Maliasin — Abbott

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