Gabapentin Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R61:Kann das Kind im Mutterleib schädigen.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S53:Exposition vermeiden - vor Gebrauch besondere Anweisungen einholen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
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.
Chemische Eigenschaften
White Crystalline Solid
Verwenden
Gabapentin is an Amino acid structurally related to γ-Aminobutyric Acid (GABA), designed to cross the blood brain barrier. Used as an anticonvulsant.
Definition
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.
Biologische Funktion
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.
Allgemeine Beschreibung
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.
Biologische Aktivität
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.
Nebenwirkungen
Long-Term Side Effects of Gabapentin:
- Mood changes.
- Behavioral changes.
- Depression.
- Anxiety.
- Memory loss.
- Weakened muscles.
Nebenwirkungen
Dose-limiting adverse effects
include somnolence, dizziness, ataxia, peripheral edema, and infection (22).
Gabapentin Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
