Esparflin
Esparflin Uses, Dosage, Side Effects, Food Interaction and all others data.
Esparflin 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.
Esparflin 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. Esparflin blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Esparflin does not enter the brain from the blood and, therefore, does not cause drowsiness.
| Trade Name | Esparflin |
| Availability | Prescription only |
| Generic | Desloratadine |
| Desloratadine Other Names | Descarboethoxyloratadine, Desloratadina, Desloratadine |
| Related Drugs | prednisone, cetirizine, loratadine, fluticasone nasal, promethazine, diphenhydramine, Zyrtec, Xolair |
| Type | |
| Formula | C19H19ClN2 |
| Weight | Average: 310.821 Monoisotopic: 310.123676325 |
| Protein binding | Desloratadine is bound approximately 82 to 87% to plasma proteins, while its active metabolite, 3-hydroxydesloratadine, is bound approximately 85 to 89%. |
| Groups | Approved, Investigational |
| Therapeutic Class | Non-sedating antihistamines |
| Manufacturer | |
| Available Country | Venezuela |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Allergic Rhinitis: Esparflin 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: Esparflin 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.
Esparflin 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, Antihistamine
How Esparflin works
Like other H1-blockers, Esparflin 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.
Dosage
Esparflin 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
Esparflin 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.
Precaution
Hepatic and renal impairment. Pregnancy and lactation.
Interaction
Concomitant administration of Erythromycin, Ketoconazole, Azithromycin, Fluoxetine, and Cimetidine with Esparflin increased the plasma concentration of Esparflin. But there were no clinically relevant changes in the safety profile of Esparflin.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Esparflin Disease Interaction
Elimination Route
Esparflin 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.
Half Life
Esparflin has a mean plasma elimination half-life of approximately 27 hours.
Elimination Route
Approximately 87% of a C-desloratadine dose was equally recovered in urine and feces as metabolic products.
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, Esparflin should be used in pregnancy only if clearly needed.
Lactation: Esparflin passes into breast milk. Therefore, a decision should be made whether to discontinue nursing or to discontinue Esparflin, taking into account the importance of the drug to the mother.
Contraindication
Esparflin 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 Esparflin 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.
Innovators Monograph
You find simplified version here Esparflin
Esparflin contains Desloratadine see full prescribing information from innovator Esparflin Monograph, Esparflin MSDS, Esparflin FDA label
FAQ
What is Esparflin used for?
Esparflin is an antihistamine used to relieve allergy symptoms such as watery eyes, runny nose, itching eyes/nose, sneezing, hives, and itching. Esparflin is used to treat allergies. It is an active metabolite of loratadine. It is used to relieve the symptoms of hay fever and hives of the skin.
How safe is Esparflin?
Esparflin is a safe and effective treatment for allergic diseases.
How does Esparflin work?
Esparflin works by blocking histamine, a substance in the body that causes allergic symptoms.
What are the common side effects of Esparflin?
Common side effects of Esparflin are include:
- headache.
- nausea.
- diarrhea.
- dizziness.
- sore throat.
- dry mouth.
- muscle pain.
- extreme tiredness
Is Esparflin safe during pregnancy?
As such these findings provide reassurance by indicating that the fetal safety of Esparflin is similar to the currently recommended antihistamines during pregnancy and thus Esparflin can be considered to be another option for use during pregnancy.
Is Esparflin safe during breastfeeding?
Considering the minimal exposure of a nursing infant to the drugs through breast milk, maternal use of Esparflin dose is unlikely to result in adverse effects in nursing infants and is considered to be compatible with breastfeeding.
Can I drink alcohol with Esparflin?
Esparflin alone or in combination with alcohol was safe and well tolerated.
Can I drive after taking Esparflin?
Do not drive and do not use tools or machines.
When should be taken of Esparflin?
You can take Esparflin before or after meals.
Can I take Esparflin every day?
The recommended dose of Esparflin tablets is one 5 mg tablet once daily.
How long does Esparflin take to work?
Esparflin is also use to relieve the symptoms of allergic skin conditions such as skin itch and hives. Esparflin usually starts to work within 75 minutes and lasts for 24 hours.
What is the half-life of Esparflin ?
The 27-hour half-life of Esparflin permits once daily administration.
How long can I take Esparflin for?
You can limit treatment to 14 days.
Can I take Esparflin for a long time?
Esparflin is unlikely to do you any harm if you take it for a long time. However, it's best to take it only for as long as you need to. It's best not to drink alcohol while you're taking Esparflin, as it can make you feel sleepy.
Who should not take Esparflin?
Follow all directions on your medicine label and package. Tell each of your healthcare providers about all your medical conditions, allergies, and all medicines you use.
What happens if I miss a dose?
Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.
What happen if I overdose of Esparflin?
tiredness. sleepiness. menstrual pain. Increased sleepiness or tiredness can happen if you take more Esparflin than your doctor prescribed to you.
Can Esparflin cause infertility?
Esparflin is not expected to cause other pregnancy problems.
Does Esparflin increase blood pressure?
The decongestant in Esparflin and pseudoephedrine may cause blood pressure to increase and may also speed up the heart rate.
Can Esparflin affects my kidney?
Older patients are more likely to have kidney or liver problems which may make them more sensitive to the effects of Esparflin. Your doctor may give you a different Esparflin dose if you have kidney or liver problems.
