Desloratadine And Pseudoephedrine
Desloratadine And Pseudoephedrine Uses, Dosage, Side Effects, Food Interaction and all others data.
Desloratadine is a long-acting, tricyclic, non-sedating, selective peripheral histamine H1-receptor antagonist which inhibits the release of pro-inflammatory mediators from human mast cells and basophils.
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.
Pseudoephedrine is structurally related to ephedrine but exerts a weaker effect on the sympathetic nervous system. Both drugs naturally occur in in ephedra plant which have a history of use in traditional Eastern medicine and were first researched in the west in 1889. The decongestant effect of pseudoephedrine was described in dogs in 1927.
Pseudoephedrine causes vasoconstriction which leads to a decongestant effect. It has a short duration of action unless formulated as an extended release product. Patients should be counselled regarding the risk of central nervous system stimulation.
| Trade Name | Desloratadine And Pseudoephedrine |
| Generic | Desloratadine + Pseudoephedrine |
| Weight | 2.5mg + 120mg, 5mg + 240mg |
| Type | Oral tablet, extended release |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Allergic Rhinitis: Desloratadine is used for the relief of the nasal and non-nasal symptoms of allergic rhinitis (Both seasonal and perennial) in patients 2 years of age and older.
Chronic Idiopathic Urticaria: Desloratadine is also used for the symptomatic relief of pruritus, reduction in the number of hives, and size of hives, in patients with chronic idiopathic urticaria 2 years of age and older.
Pseudoephedrine is an alpha and beta adrenergic agonist used to treat nasal and sinus congestion, as well as allergic rhinitis.
Pseudoephedrine is a sympathomimetic amine used for its decongestant activity.
Desloratadine And Pseudoephedrine is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Asthma, Chronic Idiopathic Urticaria, Common Cold, Nasal Congestion, Perennial Allergic Rhinitis (PAR), Seasonal Allergic Rhinitis, Nasal symptoms, Non-nasal symptoms, AntihistamineAllergic Rhinitis (AR), Allergies, Common Cold, Common Cold Associated With Cough, Common Cold/Flu, Cough, Cough caused by Common Cold, Eye allergy, Fever, Flu caused by Influenza, Headache, Irritative cough, Nasal Allergies, Nasal Congestion, Nasal Congestion caused by Common Cold, Pain, Perennial Allergy, Priapism, Respiratory Allergy, Rhinorrhoea, Seasonal Allergic Rhinitis, Seasonal Allergies, Sinus Congestion, Sinusitis, Sneezing, Sore Throat, Symptoms of Acute Bronchitis Accompanied by Coughing, Throat irritation, Upper Respiratory Tract Infection, Upper respiratory tract congestion, Upper respiratory tract signs and symptoms, Dry cough, Minor aches and pains, Sinus pain, Watery itchy eyes, Airway secretion clearance therapy
How Desloratadine And Pseudoephedrine works
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.
Pseudoephedrine acts mainly as an agonist of alpha adrenergic receptors and less strongly as an agonist of beta adrenergic receptors.[A10896] This agonism of adrenergic receptors produces vasoconstriction which is used as a decongestant and as a treatment of priapism. Pseudoephedrine is also an inhibitor of norepinephrine, dopamine, and serotonin transporters.
The sympathomimetic effects of pseudoephedrine include an increase in mean arterial pressure, heart rate, and chronotropic response of the right atria. Pseudoephedrine is also a partial agonist of the anococcygeal muscle. Pseudoephedrine also inhibits NF-kappa-B, NFAT, and AP-1.
Dosage
Desloratadine And Pseudoephedrine dosage
Pediatric drops :
- Child 6 -11 months of age: 2 ml drops once daily
- Child 1 -2 years of age: 2.5 ml drops once daily
Syrup:
- Child 6-11 months of age: 2 ml once daily
- Child 1-5 years of age: 2.5 ml once daily
- Child 6-11 years of age: 5 ml once daily
- Adults & > 12 years of age: 10 ml once daily
Tablet:
- Adults and children 12 years of age and over: 5 mg daily
Side Effects
Desloratadine is generally well tolerated. However, dry mouth, fatigue, somnolence and myalgia are commonly reported side-effects. Less common side-effects may include dizziness, headache and nausea. Rarely rash, pruritus and urticaria may occur.
Toxicity
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.
The oral LD50 of pseudoephedrine is 2206mg/kg in rats and 726mg/kg in mice.
Patients experiencing an overdose of pseudoephedrine may present with giddiness, headache, nausea, vomiting, sweating, thirst, tachycardia, precordial pain, palpitations, difficulty urinating, muscle weakness, muscle tension, anxiety, restlessness, insomnia, toxic psychosis, cardiac arrhythmias, circulatory collapse, convulsions, coma, and respiratory failure. Treat overdose with symptomatic and supportive treatment including removal of unabsorbed drug.
Precaution
Hepatic and renal impairment. Pregnancy and lactation.
Interaction
Concomitant administration of Erythromycin, Ketoconazole, Azithromycin, Fluoxetine, and Cimetidine with Desloratadine increased the plasma concentration of Desloratadine. But there were no clinically relevant changes in the safety profile of Desloratadine.
Volume of Distribution
The apparent volume of distribution of pseudoephedrin is 2.6-3.3L/kg.
Elimination Route
Desloratadine administered orally for ten days to healthy volunteers as a 5 mg tablet once daily resulted in a mean Tmax of approximately 3 hours, a mean steady-state Cmax 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.
A 240mg oral dose of pseudoephedrine reaches a Cmax of 246.3±10.5ng/mL fed and 272.5±13.4ng/mL fasted, with a Tmax of 6.60±1.38h fed and 11.87±0.72h fasted, with an AUC of 6862.0±334.1ng*h/mL fed and 7535.1±333.0ng*h/mL fasted.
Half Life
Desloratadine has a mean plasma elimination half-life of approximately 27 hours.
The mean elimination half life of pseudoephedrine is 6.0h.
Clearance
A 60mg oral dose of pseudoephedrine has a clearance of 5.9±1.7mL/min/kg.
Elimination Route
Approximately 87% of a C-desloratadine dose was equally recovered in urine and feces as metabolic products.
55-75% of an oral dose is detected in the urine as unchanged pseudoephedrine.
Pregnancy & Breastfeeding use
Pregnancy: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, Desloratadine should be used in pregnancy only if clearly needed.
Lactation: Desloratadine passes into breast milk. Therefore, a decision should be made whether to discontinue nursing or to discontinue Desloratadine, taking into account the importance of the drug to the mother.
Contraindication
Desloratadine is contraindicated in patient having hypersensitivity to this medication or to any of its ingredients or Loratadine.
Special Warning
Paediatric Use: The safety and effectiveness of Desloratadine in pediatric patients under 2 years of age have not been established.
Geriatric Use: In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
In adult patients with liver or renal impairment: A starting dose of one 5 mg tablet every other day is recommended based on pharmacokinetic data.
Acute Overdose
No clinically relevant adverse events have been reported in case of overdosage. However, in the event of overdosage, symptomatic and supportive treatment is recommended.
Storage Condition
Store in a cool and dry place, protected from light.
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