Gabapentin

Gabapentin 속성

Gabapentin MSDS

1-(Aminomethyl)cyclohexaneacetic acid

Gabapentin C화학적 특성, 용도, 생산

개요

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.

화학적 성질

White Crystalline Solid

용도

Gabapentin is an Amino acid structurally related to γ-Aminobutyric Acid (GABA), designed to cross the blood brain barrier. Used as an anticonvulsant.

정의

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.

Indications

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.

Biological Functions

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.

일반 설명

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.

생물학적 활성

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.

부작용

Long-Term Side Effects of Gabapentin:

• Mood changes.
• Behavioral changes.
• Depression.
• Anxiety.
• Memory loss.
• Weakened muscles.

부작용

Dose-limiting adverse effects include somnolence, dizziness, ataxia, peripheral edema, and infection (22).

Gabapentin 준비 용품 및 원자재

원자재

준비 용품

Gabapentin 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Sigma Audley	+86-18336680971 +86-18126314766	nova@sh-teruiop.com	China	515	58
Baoji Guokang Bio-Technology Co., Ltd.	0917-3909592 13892490616	gksales1@gk-bio.com	China	9327	58
Hong Kong Excellence Biotechnology Co., Ltd.	+86-86-18838029171 +8618126314766	ada@sh-teruiop.com	China	887	58
Guangzhou TongYi biochemistry technology Co.,LTD	+8613073028829	mack@tongyon.com	China	2996	58
Jinan Jianfeng Chemical Co., Ltd	0531-88110457; +8615562555968	info@pharmachemm.com	China	225	58
Shaanxi TNJONE Pharmaceutical Co., Ltd	+8618740459177	sarah@tnjone.com	China	1142	58
Dorne Chemical Technology co. LTD	+86-86-13583358881 +8618560316533	Ethan@dornechem.com	China	3149	58
hebei hongtan Biotechnology Co., Ltd	+86-86-1913198-3935 +8617331935328	sales03@chemcn.cn	China	973	58
Sinoway Industrial co., ltd.	0592-5800732; +8613806035118	xie@china-sinoway.com	China	992	58
Changzhou Rokechem Technology Co., Ltd.	18758118018	sales001@rokechem.com	China	255	58

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