Primaquinbis(phosphat)

Bezeichnung:Primaquinbis(phosphat)

CAS-Nr63-45-6

Englisch Name:Primaquine diphosphate

CBNumberCB1116162

SummenformelC15H27N3O9P2

Molgewicht455.34

MOL-Datei63-45-6.mol

Synonyma

Primaquinbis(phosphat)

Primaquinbis(phosphat) physikalisch-chemischer Eigenschaften

Schmelzpunkt	205-206 °C (dec.)(lit.)
storage temp.	2-8°C
Löslichkeit	water: soluble50mg/mL, clear, orange to red
Wasserlöslichkeit	moderately soluble
Merck	13,7833
BRN	3812133
BCS Class	1 (CLogP), 3 (LogP)
Stabilität	Stable. Incompatible with strong oxidizing agents.
CAS Datenbank	63-45-6(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25
S-Sätze:	45
RIDADR	UN 2811 6.1/PG 3
WGK Germany	3
RTECS-Nr.	VA9660000
F	10
HazardClass	6.1(b)
PackingGroup	III
HS Code	29334900

Gefahreninformationscode (GHS)

Primaquine diphosphate Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R25:Giftig beim Verschlucken.
S-Sätze Betriebsanweisung:
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Chemische Eigenschaften
orange powder
Verwenden
acetylcholinesterase inhibitor
Verwenden
Primaquine diphosphate is an established antimalarial drug used in the treatment of persistent liver forms of P. vivax or P. ovale infection for its ability to kill late-stage gametocytes and hypnozoites. In historical terms, this aminoquinoline was the stimulus for the discovery of glucose-6-phosphate (G6P) dehydrogenase deficiency as it induced hemolytic anemia in patients lacking the G6P-metabolizing enzyme.
Verwenden
Antimalarial.
Trademarks
Primaquine (Sanofi Aventis).
Biologische Aktivität
primaquine, an 8-aminoquinoline, is introduced as a curative antimalarial agent in 1950. since then, the drug has been applied extensively to against the exoerythrocytic stage of malaria. it is demonstrated tthat primaquine, by binding to nucleic acids, could therefore block protein synthesis, alter lipid synthesis and interact with biological membranes. [1]
Clinical Use

Treatment of malaria (Plasmodium vivax and Plasmodium ovale), in combination with chloroquine
Treatment of Pneumocystis jiroveci pneumonia (PCP), in combination with clindamycin
in vitro
chicken embryo cells (cec) model were adopted to investigate the effect of primaquine on newcastle disease virus replication. it was found that virus-induced hemadsorption was inhibited by primaquine in a dose-dependent manner and was completely suppressed by primaquine 250 g/ml. viral ribonucleic acid (rna) synthesis was found to be suppressed when primaquine was added early in the virus replication cycle. whereas, when the drug was added late in the cycle, rna synthesis was stimulation. [1]
in vivo
primaquine liposomes were labelled by 99mtc and injected intravenously to swiss albino mice. after injection, the major accumulation organ of liposomes was liver followed by spleen, pancreas, lungs and the others. findings also suggested that primaquine could block the eradication of the parasites and prevent relapse by destruction of the exoerythrocytic liver stages. [2]
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Antimalarials: avoid concomitant use with artemether/lumefantrine.
Stoffwechsel
Rapidly metabolised in the liver. Its major metabolite carboxyprimaquine accumulates in the plasma on repeated dosage but possesses less antimalarial activity than the parent compound. Little unchanged drug is excreted in the urine.
läuterung methode
It forms yellow crystals from 90% aqueous EtOH and is moderately soluble in H2O. The oxalate salt has m 182.5-185o (from 80% aqueous EtOH), and the free base is a viscous liquid b 165-170o/0.002mm, 175-177o/2mm. [Elderfield et al. J Am Chem Soc 68 1526 1964, Elderfield et al. J Am Chem Soc 77 4817 1955, Beilstein 22 III/IV 5817.]
Einzelnachweise
[1]burdick jr and durand dp. primaquine diphosphate: inhibition of newcastle disease virus replication. antimicrob agents ch. 1974 oct 15; 6(4): 460-4.
[2]aricat b, ozert ay, ercans mt and hincalt aa. characterization, in vitro and in vivo studies on primaquine diphosphate liposomes. j. microencapsulation. 1995; 12(5): 469-85.
[3]soto j, toledo j, rodriquez m, sanchez j, herrera r, padilla j and berman j. double-blind, randomized, placebo-controlled assessment of chloroquine/primaquine prophylaxis for malaria in nonimmune colombian soldiers. clin infect dis. 1999 jul; 29: 199-201.

Primaquine diphosphate Upstream-Materialien And Downstream Produkte

Primaquinbis(phosphat) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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