5H-Dibenz(b,f)azepin-5-propanamin, 10,11-dihydro-N,N-dimethyl-monohydrochlorid Chemische Eigenschaften,Einsatz,Produktion Methoden
R-S?tze Betriebsanweisung:
R23/25:Giftig beim Einatmen und Verschlucken.
R36/38:Reizt die Augen und die Haut.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R22:Gesundheitssch?dlich beim Verschlucken.
S-S?tze Betriebsanweisung:
S7:Beh?lter dicht geschlossen halten.
S16:Von Zündquellen fernhalten - Nicht rauchen.
S24:Berührung mit der Haut vermeiden.
S33:Ma?nahmen gegen elektrostatische Aufladungen treffen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn m?glich, dieses Etikett vorzeigen).
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Chemische Eigenschaften
White Solid
Verwenden
Imipramine hydrochloride is used as a serotonin uptake inhibitor. It mainly used in the treatment of major depression and enuresis (inability to control urination). It has also been evaluated for use in panic disorder.
Allgemeine Beschreibung
Imipramine hydrochloride, 5-[3-(dimethylamino)propyl]-10,11-dihydro-5H-dibenz[b,f]azepine monohydrochloride(Tofranil), is the lead compound of the TCAs. It is also a closerelative of the antipsychotic phenothiazines (replace the10–11 bridge with sulfur, and the compound is the antipsychoticagent promazine). It has weaker D
2 postsynaptic blockingactivity than promazine and mainly affects amines (5-HT,NE, and DA) via the transporters. As is typical of dimethylaminocompounds, anticholinergic and sedative (central H
1block) effects tend to be marked. The compound per se has a tendency toward a high 5-HT-to-NE uptake block ratio andprobably can be called a serotonin transport inhibitor(SERTI). Metabolic inactivation proceeds mainly by oxidativehydroxylation in the 2-position, followed by conjugationwith glucuronic acid of the conjugate. Urinary excretion predominates(about 75%), but some biliary excretion (up to25%) can occur, probably because of the large nonpolargrouping. Oxidative hydroxylation is not as rapid or completeas that of the more nucleophilic ring phenothiazine antipsychotics;consequently, appreciable N-demethylation occurs,with a buildup of norimipramine (or desimipramine).
Clinical Use
The demethylated metabolite is less anticholinergic, lesssedative, and more stimulatory and is a SNERI.Consequently, a patient treated with imipramine has twocompounds that contribute to activity. Overall, the effect isnonselective 5-HT versus NE reuptake.
Sicherheitsprofil
Human poison by
ingestion. An experimental poison by
ingestion, intravenous, subcutaneous, and
intraperitoneal routes. An experimental
teratogen. Human systemic effects by
ingestion: sleep, somnolence, convulsions,
muscle contraction or spasticity, coma, blood pressure decrease, dyspnea (difficulty
in breathing), paresthesia (abnormal
sensations), and kidney changes.
Experimental reproductive effects. Mutation
data reported. Used in the treatment of
depression. When heated to decomposition
it emits very toxic fumes of NO, and HCl.
See also DIAZEPAM.
5H-Dibenz(b,f)azepin-5-propanamin, 10,11-dihydro-N,N-dimethyl-monohydrochlorid Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
