ガバペンチン 化学特性,用途語,生産方法
外観
白色〜わずかにうすい褐色, 結晶〜粉末
溶解性
水溶状：試験適合
用途
脳中の GABA を上昇させます。 抗けいれん作用を示します。
用途
GABA 脳中の GABA を上昇させます。 抗けいれん作用を示します。
効能
抗けいれん薬, 抗てんかん薬
商品名
ガバペン (ファイザー); ガバペン (ファイザー)
説明
Gabapentin was introduced in 1993 in the UK and early 1994 in the USA as an
adjunctive therapy in the treatment of refractory partial seizures and secondarily generalized
tonic-clonic seizures. Although being a lipophilic analog of the neurotransmitter GABA,
gabapentin appears to exert its anticonvulsive function by a GABA receptor independent
mechanism, possibly involving the L-system amino acid transporter protein. Gabapentin
easily crosses the blood brain barrier and exhibits a favorable pharmacokinetic profile with
high tolerability. It does not interfere with the metabolism of other concomitant administered
antiepileptic drugs, thus having a low potential for drug interactions. Studies are currently
underway for the use of gabapentin as mono-therapy for the treatment of various seizures.
化学的特性
White Crystalline Solid
使用
Gabapentin is an Amino acid structurally related to γ-Aminobutyric Acid (GABA), designed to cross the blood brain barrier. Used as an anticonvulsant.
定義
ChEBI: A gamma-amino acid that is cyclohexane substituted at position 1 by aminomethyl and carboxymethyl groups. Used for treatment of neuropathic pain and restless legs syndrome.
適応症
Gabapentin (Neurontin) significantly decreases pain scores and sleep interference
associated with PHN. An initial dose of 300 mg/day is increased
over 4 weeks (900, 1,800, 2,400, 3,600 mg/day divided t.i.d.) until efficacy
is obtained or side effects become intolerable.
生物学の機能
Gabapentin (Neurotonin) was initially designed to be a
rigid analogue of GABA. When it was discovered to
have antiepileptic properties, it was assumed that this
activity was related to a GABAergic mechanism.
However, subsequent studies have failed to show any
GABAergic activity of gabapentin. Although it has not
yet been possible to ascribe any definite mechanism to
its antiepileptic activity, there is recent evidence that it
may function as an agonist at GABAB receptors in the
brain.
Gabapentin is recommended as adjunctive therapy
in the treatment of partial seizures in adults.When used
with other drugs, it appears to be an effective AED; it is
usually not effective when employed alone for patients
with severe seizures.
Gabapentin is generally well tolerated, with somnolence,
dizziness, and ataxia the most commonly reported
adverse effects. A low incidence of potentially serious side effects and no significant allergic reactions have
been reported.
一般的な説明
Gabapentin and its closely related analog pregabalin,(S)-3-isobutyl-GABA, are broad-spectrum anticonvulsantswith multiple mechanisms of action.24,51 Inaddition to modulating calcium influx and stimulateGABA biosynthesis as discussed earlier, they also competefor the biosynthesis of L-glutamic acid because oftheir structural similarity to L-leucine.51 Gabapentin andpregabalin have very little liability for causing metabolicbaseddrug–drug interactions, particularly when used incombination with other AEDs because they are not metabolizedin humans. More than 95% of the drug is excretedunchanged through the kidneys. However, there are somedifferences in their bioavailability. Unlike gabapentin,which exhibits 60% bioavailability when given in lowdoses because of intestinal uptake by a saturable smallneutral L-amino acid transporter, the absorption of pregabalinis almost complete (98%) and exhibits an ideal linear pharmacokinetic profile.24 This high bioavailability of pregabalincan be attributed to its closer structure similarity tothe essential amino acid, L-leucine.
生物活性
Anticonvulsant with several possible mechanisms of action. Increases GABA in the brain and binds to a novel site associated with voltage-sensitive Ca 2+ channels. Prevents neuronal death and is antinociceptive and anxiolytic.
副作用
Long-Term Side Effects of Gabapentin:
- Mood changes.
- Behavioral changes.
- Depression.
- Anxiety.
- Memory loss.
- Weakened muscles.
副作用
Dose-limiting adverse effects
include somnolence, dizziness, ataxia, peripheral edema, and infection (22).
ガバペンチン 上流と下流の製品情報
原材料
準備製品