Desloratadine Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Desloratadine is a second generation of tricyclic antihistamine. It is a H1-receptor antagonist which has anti-inflammatory activity. Its affinity to the H1 receptor is higher than most other H1-receptor antagonists. Desloratadine works by blocking a certain natural substance (histamine) which is produced during an allergic reaction. Desloratidine has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system.
Desloratadine is used to treat nasal and non-nasal symptoms (watery eyes, runny nose, itching eyes/nose, sneezing, and itching) of seasonal allergic rhinitis. It is also used to relieve chronic itching caused by hives.
Chemische Eigenschaften
Beige Solid
Verwenden
Desloratadine has been used to test its effect on embryoid body development in in vitro gastrulation model of P19C5 stem cells. It has also been used as an antihistamine mimic in rats and to treat lung cancer (A549) and glioblastoma (U87) cells in various cellular studies.
Definition
ChEBI: Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis
nd chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness.
Indications
Desloratadine (Clarinex) is an active metabolite of loratadine. A 5 mg
daily dose has been shown to be effective. There is no evidence that it offers
any advantage over loratadine.
Fexofenadine (like its parent compound terfenadine) may rarely promote
cardiac arrhythmias (24). No significant difference in efficacy has been noted
in the nonsedating H1 blockers. Combinations of nonsedating antihistamines
in the morning and sedating antihistamines in the evening may be more cost
effective than increasing doses of the nonsedating agent.
Allgemeine Beschreibung
Desloratadine, 8-chloro-6,11-dihydro-11-(4-piperdinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine(Clarinex) is a white to off-white powder that is slightlysoluble in water, but very soluble in ethanol and propyleneglycol. It is the proposed active metabolite loratadine and hasa very similar receptor binding and safety profile. It is indicated for the symptomatic relief of pruritus andreduction in the number and size of hives in chronic idiopathicurticaria patients 6 months of age and older and for therelief of the nasal and nonnasal symptoms of perennial allergicrhinitis (in patients 6 months of age and older) and seasonalallergic rhinitis (in patients 2 years of age and older).
Desloratadine is extensively metabolized to 3-hydroxydesloratadine,also an active metabolite, which is subsequentlyglucuronidated . The cytochrome enzymesresponsible for the formation of 3-hydroxydesloratadinehave not been reported. Coadministration ofdesloratadine with CYP3A4 inhibitors results in marginalincreases in plasma concentrations of desloratadine and3-hydroxydesloratadine, but no significant changes in safetyor efficacy. The mean elimination half-life of desloratadineis about 6 hours, and the drug and its metabolites areeliminated in the urine and feces.
Einzelnachweise
[1] https://www.drugbank.ca
[2] Raif S. Geha, Eli O. Meltzer (2001) Desloratadine: A new, nonsedating, oral antihistamine, The Journal of Allergy and Clinical Immunology,107, 751-762
Desloratadine Upstream-Materialien And Downstream Produkte
Upstream-Materialien
N-Methyl Desloratadine
Natriumhydroxid
Ethyl-chlorformiat
2H-Pyrano[3,2-b]pyridine,3,4-dihydro-4-methylene-(9CI)
Loratadine ketone
N-T-BUTYL-3-METHYL PYRIDINE-2-CARBOXAMIDE
100643-73-0
1-Methylpiperdin-4-ylmagnesium chloride, 0.50 M in THF
Loratadine
8-Chloro-6,11-dihydro-11-(1-methyl-4-piperidinyl)-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ol
3-[2-(3-CHLORO-PHENYL)-ETHYL]-PYRIDINE-2-CARBOXYLIC ACID TERT-BUTYLAMIDE
3-[2-(3-Chlorophenyl)ethyl]-2-pyridinecarbonitrile
8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-one
Downstream Produkte
