Orphenadrindihydrogencitrat

Bezeichnung:Orphenadrindihydrogencitrat

CAS-Nr4682-36-4

Englisch Name:Orphenadrine citrate

CBNumberCB3401680

SummenformelC24H31NO8

Molgewicht461.5

MOL-Datei4682-36-4.mol

Synonyma

Orphenadrindihydrogencitrat

Orphenadrindihydrogencitrat physikalisch-chemischer Eigenschaften

Schmelzpunkt	132-1340C
storage temp.	Sealed in dry,2-8°C
Löslichkeit	Sparingly soluble in water, slightly soluble in ethanol (96 per cent).
Farbe	White to Pale Beige
InChIKey	ASDBZPGDZBFZAH-UHFFFAOYSA-N
CAS Datenbank	4682-36-4(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xn,Xi
R-Sätze:	22-40-20/21/22
S-Sätze:	22-36-62-38-36/37/39-28-26-24/25
RIDADR	3249
WGK Germany	3
HazardClass	6.1(b)
PackingGroup	III
HS Code	2922190900

Gefahreninformationscode (GHS)

Orphenadrine citrate Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R40:Verdacht auf krebserzeugende Wirkung.
S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Chemische Eigenschaften
White Solid
Originator
Norflex,Riker,US,1959
Verwenden
A histaminergic compound
Verwenden
skeletal muscle relaxant, antihistaminic agent
Verwenden
Muscle relaxant (skeletal); antihistaminic
Definition
ChEBI: A citrate salt which comprises equimolar amounts of orphenadrine and citric acid.
Manufacturing Process
As described in US Patent 2,567,351, o-methylbenzhydryl bromide is added slowly to β-dimethylaminoethanol at refluxing temperature. After the addition has been completed the mixture is refluxed and stirred for an additional 16 hours. The mixture is cooled and the bottom layer consisting of the crude hydrobromide salt of β-dimethylaminoethanol is drawn off. The excess amino alcohol is distilled from the upper layer in vacuo and the residue is reacted with citric acid.
Trademarks
Norflex (3M Pharmaceuticals).
Therapeutic Function
Muscle relaxant
Allgemeine Beschreibung
Orphenadrine citrate, N,Ndimethyl-2-(o-methyl-α-phenylbenzyloxy)ethylamine citrate(1:1) (Norflex), introduced in 1957, is closely related todiphenhydramine structurally but has much lower antihistaminicactivity and much higher anticholinergic action.Likewise, it lacks the sedative effects characteristic ofdiphenhydramine. Pharmacological testing indicates that itis not primarily a peripherally acting anticholinergic becauseit has only weak effects on smooth muscle, on the eye,and on secretory glands. It does reduce voluntary musclespasm, however, by a central inhibitory action on cerebralmotor areas, a central effect similar to that of atropine.
Clinical Use
Orphenadrine citrate is used for the symptomatic treatment ofParkinson disease. It relieves rigidity better than it doestremor, and in certain cases, it may accentuate the latter. Thedrug combats mental sluggishness, akinesia, adynamia, andlack of mobility, but this effect seems to diminish rather rapidlywith prolonged use. It is best used as an adjunct to theother agents, such as benztropine, procyclidine, cycrimine,and trihexyphenidyl, in the treatment of paralysis agitans.Orphenadrine citrate is also used as an adjunct to rest, physiotherapy,and other measures to relieve pain of local musclespasm (e.g., nocturnal leg cramps).
The drug has a low incidence of the usual side effectsfor this group, namely, dryness of mouth, nausea, and mildexcitation.

Orphenadrine citrate Upstream-Materialien And Downstream Produkte

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