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Desloratadine
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DRUG INFO
Desloratadine
Drug Name:
Desloratadine
Indication: For the relief of symptoms of seasonal allergic rhinitis, pruritus, reduction in the number of hives in patients with chronic idiopathic urticaria.
Pharmacology: Desloratadine is a long-lasting antihistamine. Desloratadine is a second-generation H1-receptor antagonist which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, for example, swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be "activated," releasing other chemicals which produce the effects that we associate with allergy. Desloratadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Desloratadine does not enter the brain from the blood and, therefore, does not cause drowsiness.
Mechanism Of Action: Like other H1-blockers, Desloratadine competes with free histamine for binding at H1-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
Drug Category: Antihistamines; Antihistamines; ATC:R06AX27
Brand Names/Synonyms: Aerius; Alavert; Clarinex; Clarinex Reditabs; Claritin; Claritin Reditabs; Descarboethoxyloratadine; Descarboethoxyoratidine; Desloratadine; Desloratadine [Usan]; Desloratidine; Loratadine; Sch 34117
Dosage Forms: SYRUP; TABLET
Absorption: Not Available
Interactions:
DrugBank: Interactions for Desloratadine
Interactions for Desloratadine:
In two controlled crossover clinical pharmacology studies in healthy male (n=12 in each study) a nd
female (n=12 in each study) volunteers, desloratadine 7.5 mg (1.5 times the daily dose) once daily was coadministered
with erythromycin 500 mg every 8 hours or ketoconazole 200 mg every 12 hours for 10 days. In three separate
controlled, parallel group clinical pharmacology studies, desloratadine at the clinical dose of 5 mg has been
coadministered with azithromycin 500 mg followed by 250 mg once daily for 4 days (n=18) or with fluoxetine 20 mg once
daily for 7 days after a 23 day pretreatment period with fluoxetine (n=18) or with cimetidine 600 mg every 12 hours
for 14 days (n=18) under steady state conditions to normal healthy male and female volunteers. Although increased
plasma concentrations (C max and AUC 0-24 hrs) of desloratadine and 3-hydroxydesloratadine were observed ,
there were no clinically relevant changes in the safety profile of desloratadine, as assessed by electrocardiographic
parameters (including the corrected QT interval), clinical laboratory tests, vital signs, and adverse events.
Table 1
Changes in Desloratadine and 3-Hydroxydesloratadine Pharmacokinetics in Healthy Male and Female Volunteers |
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Desloratadine |
3-Hydroxydesloratadine |
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C max |
AUC
0-24 hrs |
C max |
AUC
0-24 hrs |
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Erythromycin
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(500 mg Q8h)
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+24% |
+14% |
+43% |
+40% |
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Ketoconazole
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(200 mg Q12h)
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+45% |
+39% |
+43% |
+72% |
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Azithromycin
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(500 mg day 1,
250 mg QD × 4 days)
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+15% |
+5% |
+15% |
+4% |
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Fluoxetine
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(20 mg QD)
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+15% |
+0% |
+17% |
+13% |
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Cimetidine
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(600 mg Q12h)
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+12% |
+19% |
-11% |
-3% |
Chemical IUPAC Name: Not Available
Chemical Formula: C19H19ClN2
Half Life: 50 hours
Drug Type: Approved Drug
# Accession No: APRD00324
CAS Registry Number: 100643-71-8
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Desloratadine News
(When available)
FDA Approves CLARINEX-D(R) 12 HOUR (desloratadine 2.5mg ... Feb 6, 2006
Schering-Plough Corporation (NYSE: SGP) today announced that the US Food and Drug Administration (FDA) has approved CLARINEX-D® 12 HOUR (desloratadine 2.5 mg ... - Medical News Today (press release),
FDA Approves Clarinex-D 12 Hour (Desloratadine/Pseudoephedrine) ... Feb 2, 2006
2, 2006 -- Schering-Plough Corporation today announced that the US Food and Drug Administration (FDA) has approved Clarinex-D® 12 hour (desloratadine 2.5 mg ... - DG News
FDA Approves CLARINEX-D(R) 12 HOUR (desloratadine 2.5mg ... Feb 1, 2006
Schering-Plough Corporation today announced that the US Food and Drug Administration (FDA) has approved CLARINEX-D(R) 12 HOUR (desloratadine 2.5 mg and ... - Finanzen.net,
FDA OKs Clarinex-D 12 Hour Feb 3, 2006
Clarinex (desloratadine) is a nonsedating antihistamine available by prescription for the treatment of seasonal allergy symptoms. ... - CBS News
Congestion for Use of Clarinex-D 12 Hour cleared – FDA Gives the ... Feb 4, 2006
Clarinex (desloratadine) , used for treatment of seasonal allergy symptoms, is a nonsedating antihistamine procured only by prescription . ... - MedIndia,
FDA approves CLARINEX-D 12 HOUR for seasonal allergic rhinitis Feb 6, 2006
...rhinitis. CLARINEX-D 12 HOUR is a drug containing a combination of desloratadine 2.5 mg and pseudoephedrine sulfate, USP 120 mg. ... - MedIndia,
Sepracor Announces Fourth Quarter and Full Year 2005 Results ... Jan 31, 2006
CLARINEX(R) brand desloratadine HCl - Marketed by Schering-Plough Corporation, Sepracor earns royalties on sales of all formulations of CLARINEX in the US ... - Genetic Engineering News,
Schering-Plough swings to profit in Q4 Jan 31, 2006
Global sales of the anti-allergy medicine Clarinex (desloratadine) dropped 14% to $139 million, as US revenues continued to feel the pinch of declining market ... - Pharma Times (subscription),
Lake Region news Dec 30, 2005
Bradford County Telegraph, ...are unopened over-the-counter medications such as cough syrups, ibuprofen, benedryl, Nyquil, Dayquil,arthritis patches and rubs, milk of magnesia and alavert. ...
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