Baclofen Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R61:Kann das Kind im Mutterleib schädigen.
R25:Giftig beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R42/43:Sensibilisierung durch Einatmen und Hautkontakt möglich.
R20/21/22:Gesundheitsschädlich beim Einatmen,Verschlucken und Berührung mit der Haut.
S-Sätze Betriebsanweisung:
S53:Exposition vermeiden - vor Gebrauch besondere Anweisungen einholen.
S22:Staub nicht einatmen.
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).
S52:Nicht großflächig für Wohn- und Aufenthaltsräume zu verwenden.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Chemische Eigenschaften
Off-White Solid
Verwenden
Baclofen may be used as a pharmaceutical secondary reference standard for the determination of the analyte in plasma samples by liquid chromatography tandem mass spectrometry and tablet formulations by UV spectroscopy, respectively.
Definition
ChEBI: A monocarboxylic acid that is butanoic acid substituted by an amino group at position 4 and a 4-chlorophenyl group at position 3. It acts as a central nervous system depressant, GABA agonist and muscle relaxant.
Biologische Funktion
Baclofen (Lioresal) is the parachlorophenol analogue
of the naturally occurring neurotransmitter γ-aminobutyric
acid (GABA).
Allgemeine Beschreibung
Odorless or practically odorless white to off-white crystalline powder.
Air & Water Reaktionen
Insoluble in water.
Reaktivität anzeigen
Baclofen is an amine. Amines are chemical bases. They neutralize acids to form salts plus water. These acid-base reactions are exothermic. The amount of heat that is evolved per mole of amine in a neutralization is largely independent of the strength of the amine as a base. Amines may be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable gaseous hydrogen is generated by amines in combination with strong reducing agents, such as hydrides.
Brandgefahr
Flash point data for Baclofen are not available. Baclofen is probably combustible.
Biologische Aktivität
Selective GABA B receptor agonist. Skeletal muscle relaxant.
Mechanism of action
Baclofen appears to affect the neuromuscular axis by
acting directly on sensory afferents, γ-motor neurons,
and collateral neurons in the spinal cord to inhibit both
monosynaptic and polysynaptic reflexes. The principal
effect is to reduce the release of excitatory neurotransmitters
by activation of presynaptic GABAB receptors.
This seems to involve a G protein and second-messenger
link that either increases K
+ conductance or decreases
Ca
++ conductance.
Clinical Use
Baclofen is an agent of choice for treating spinal spasticity
and spasticity associated with multiple sclerosis. It is
not useful for treating spasticity of supraspinal origin.
Doses should be increased gradually to a maximum of
100 to 150 mg per day, divided into four doses.
Nebenwirkungen
Side effects are not a major problem, and they can be
minimized by graduated dosage increases.They include
lassitude, slight nausea, and mental disturbances (in including
confusion, euphoria, and depression). The
drowsiness is less pronounced than that produced by
diazepam—an important therapeutic advantage. Hypotension
has been noted, particularly following overdose.
Elderly patients and patients with multiple sclerosis
may require lower doses and may display increased sensitivity
to the central side effects. Baclofen may increase
the frequency of seizures in epileptics.
Sicherheitsprofil
Poison by ingestion,subcutaneous and intravenous routes. Human systemiceffects by ingestion: blood pressure lowering, coma,muscle weakness, pulse rate decrease, respiratorydepression. When heated to decomposition it emits toxicfumes of Cl
-
Stoffwechsel
Baclofen is rapidly and effectively absorbed after oral
administration. It is lipophilic and able to penetrate the
blood-brain barrier.Approximately 35% of the drug is
excreted unchanged in the urine and feces.
Baclofen Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
