Tìm theo
Barbexaclone
Các tên gọi khác (4 ) :
  • Barbexaclon
  • Barbexaclona
  • Barbexaclone
  • Barbexaclonum
Thuốc Gốc
Small Molecule
CAS: 4388-82-3
Barbexaclone, a salt compound of propylhexedrine and phenobarbital, is a potent antiepileptic. [4] By weight, barbexaclone is 40% propylhexedrine and 60% phenobarbital. [2] 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. [4] Despite the lack of controlled trials, barbexaclone was used widely in Turkey until it was discontinued in 2009. [1] 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. [4] 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. [2]
Cơ Chế Tác Dụng : Barbexaclone, a salt compound of propylhexedrine and phenobarbital, is a potent antiepileptic. [4] By weight, barbexaclone is 40% propylhexedrine and 60% phenobarbital. [2] 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. [4] Despite the lack of controlled trials, barbexaclone was used widely in Turkey until it was discontinued in 2009. [1] 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. [4] 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. [2] Phenobarbitol targets GABA receptors in the CNS. Propylhexedrine is a TAAR1 agonist.
Dược Động Học :
▧ Absorption :
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]
▧ Volume of Distribution :
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]
▧ 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.
Độc Tính : 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]
Chỉ Định : Created for the treatment for epilepsy, with the intent of creating an antiepileptic with less sedative properties than phenobarbital.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Abbott
    Sản phẩm biệt dược : Maliasin
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB09001
Wikipedia
http://en.wikipedia.org/wiki/Barbexaclone
Drugs.com
http://www.drugs.com/international/barbexaclone.html
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