Desloratadine

310.82

310.82

1308068-626-2

FVF865388R

759824|675447

DTXSID1044196

C47474

R06AX27|R01BA52|R - Respiratory system

2933399090

24.9

4.5

Beige Solid

1'+-.0.06 g/cm3(Predicted)

154-154.5 °C @ Solvent: Ethyl acetate

467.9±45.0 °C(Predicted)

236.8±28.7 °C

1.626

DMSO: >10mg/mL

2-8°C

6.25E-09mmHg at 25°C

175.5 Ų [M+H]+ [CCS Type: TW, Method: Major Mix IMS/Tof Calibration Kit (Waters)]

1993

3

R11:Highly Flammable.

S16-S23-S36/37/39

DE8011000

P201, P202, P261, P264, P270, P272, P273, P280, P281, P301+P312, P302+P352, P305+P351+P338, P308+P313, P310, P321, P330, P333+P313, P363, P391, P405, P501

H302

|Danger|H302 (88.52%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P261, P264, P270, P272, P273, P280, P281, P301+P312, P302+P352, P305+P351+P338, P308+P313, P310, P321, P330, P333+P313, P363, P391, P405, and P501|Aggregated GHS information provided by 122 companies from 16 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Information regarding desloratadine overdose is limited, although somnolence has been reported. In case of overdose, symptomatic and supportive treatment, including removing the unabsorbed drug, is recommended; note, however, that desloratadine and its active metabolite 3-hydroxydesloratadine cannot be eliminated by hemodialysis. In animal studies, lethality was observed at or above doses of 250 mg/kg in rats and of 353 mg/kg in mice (oral LD50), doses that represent 120 and 290 times the human exposure based on the recommended daily oral dose. In monkey, no deaths occurred at doses up to 250 mg/kg, representing an exposure roughly 810 times that of the recommended dose in humans.

Loratadine and desloratadine use are associated with a low rate of liver enzyme elevations which are usually asymptomatic, mild and self-limited even without modification of the dose. In addition, rare instances of clinically apparent liver injury attributed to loratadine and desloratadine use have been reported as isolated case reports. The time to onset of liver injury varied but was typically within 2 to 4 weeks of starting the medication. Most cases were associated with a hepatocellular pattern of enzyme elevations resembling acute viral hepatitis. Immunoallergic and autoimmune features were not described and most cases were self-limited in course. However, at least one fatal instance of acute hepatitis attributed to loratadine has been reported. In none of the cases, was there a clear link to loratadine and all had other possible or probable non-drug causes. Thus, loratadine and desloratadine have been convincingly implicated in cases of clinically apparent liver injury in the literature and the association is suspect only.

Desloratadine is bound approximately 82 to 87% to plasma proteins, while its active metabolite, 3-hydroxydesloratadine, is bound approximately 85 to 89%.

For the relief of symptoms of seasonal allergic rhinitis, perennial (non-seasonal) allergic rhinitis. Desloratidine is also used for the sympomatic treatment of pruritus and urticaria (hives) associated with chronic idiopathic urticaria.|FDA Label|Azomyr is indicated for the relief of symptoms associated with:allergic rhinitis (see section 5.1)urticaria (see section 5.1)|Aerius is indicated for the relief of symptoms associated with:allergic rhinitis;urticaria.|Neoclarityn is indicated for the relief of symptoms associated with:allergic rhinitisurticaria|Symptomatic treatment of seasonal allergic rhinitis when accompanied by nasal congestion.|Treatment of allergic rhinitis and urticaria.|Desloratadine Teva is indicated for the relief of symptoms associated with:allergic rhinitis;urticaria.|Dasselta is indicated for the relief of symptoms associated with:allergic rhinitis;urticaria.|Desloratadine ratiopharm is indicated in adults for the relief of symptoms associated with:allergic rhinitischronic idiopathic urticaria as initially diagnosed by a physician|Aerius is indicated for the relief of symptoms associated with:- allergic rhinitis (see section 5.1)- urticaria (see section 5.1)|Opulis is indicated for the relief of symptoms associated with:- allergic rhinitis (see section 5.1)- urticaria (see section 5.1)

Loratadine and its metabolic derivative desloratadine are second generation antihistamines that are used for the treatment of allergic rhinitis, angioedema and chronic urticaria. Loratadine and desloratadine have been linked to rare, isolated instances of clinically apparent acute liver injury.

Antihistamines

Desloratadine is a long-acting 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, such as the 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 allergies. 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.

A class of non-sedating drugs that bind to but do not activate histamine receptors (DRUG INVERSE AGONISM), thereby blocking the actions of histamine or histamine agonists. These antihistamines represent a heterogenous group of compounds with differing chemical structures, adverse effects, distribution, and metabolism. Compared to the early (first generation) antihistamines, these non-sedating antihistamines have greater receptor specificity, lower penetration of BLOOD-BRAIN BARRIER, and are less likely to cause drowsiness or psychomotor impairment. (See all compounds classified as Histamine H1 Antagonists, Non-Sedating.)|Drugs that bind to but do not activate CHOLINERGIC RECEPTORS, thereby blocking the actions of ACETYLCHOLINE or cholinergic agonists. (See all compounds classified as Cholinergic Antagonists.)

Desloratadine administered orally for ten days to healthy volunteers as a 5 mg tablet once daily resulted in a mean T_max of approximately 3 hours, a mean steady-state C_max of 4 ng/ml, and a mean steady-state AUC of 56.9 ng\*hr/ml. A similar profile was observed using 10 ml of an oral solution containing 5 mg of desloratadine. Food was found not to affect desloratadine absorption.|Approximately 87% of a ¹⁴C-desloratadine dose was equally recovered in urine and feces as metabolic products.

Desloratadine is metabolized to the active metabolite 3-hydroxydesloratadine, which is subsequently glucuronidated.|Desloratadine is a known human metabolite of Rupatadine and loratadine.

Desloratadine has a mean plasma elimination half-life of approximately 27 hours.

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 (eg. nasal congestion, watery eyes) brought on by histamine.

Aerius

Human drugs -> Azomyr -> EMA Drug Category|Antihistamines for systemic use -> Human pharmacotherapeutic group|Human drugs -> Aerius -> EMA Drug Category|Human drugs -> Neoclarityn -> EMA Drug Category|Human drugs -> Aerinaze -> EMA Drug Category|Nasal preparations -> Human pharmacotherapeutic group|Human drugs -> Desloratadine Actavis -> EMA Drug Category|Human drugs -> Desloratadine Teva -> EMA Drug Category|Human drugs -> Dasselta -> EMA Drug Category|Human drugs -> Desloratadine ratiopharm -> EMA Drug Category|Human drugs -> Allex -> EMA Drug Category|Human drugs -> Opulis -> EMA Drug Category|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients