Efestad
Efestad Uses, Dosage, Side Effects, Food Interaction and all others data.
Efestad 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.
Efestad 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. Efestad blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Efestad does not enter the brain from the blood and, therefore, does not cause drowsiness.
| Trade Name | Efestad |
| 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 | Bulgaria |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Allergic Rhinitis: Efestad 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: Efestad 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.
Efestad 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 Efestad works
Like other H1-blockers, Efestad 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
Efestad 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
Efestad 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 Efestad increased the plasma concentration of Efestad. But there were no clinically relevant changes in the safety profile of Efestad.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Efestad Disease Interaction
Elimination Route
Efestad 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
Efestad 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, Efestad should be used in pregnancy only if clearly needed.
Lactation: Efestad passes into breast milk. Therefore, a decision should be made whether to discontinue nursing or to discontinue Efestad, taking into account the importance of the drug to the mother.
Contraindication
Efestad 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 Efestad 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 Efestad
Efestad contains Desloratadine see full prescribing information from innovator Efestad Monograph, Efestad MSDS, Efestad FDA label
FAQ
What is Efestad used for?
Efestad is an antihistamine used to relieve allergy symptoms such as watery eyes, runny nose, itching eyes/nose, sneezing, hives, and itching. Efestad 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 Efestad?
Efestad is a safe and effective treatment for allergic diseases.
How does Efestad work?
Efestad works by blocking histamine, a substance in the body that causes allergic symptoms.
What are the common side effects of Efestad?
Common side effects of Efestad are include:
- headache.
- nausea.
- diarrhea.
- dizziness.
- sore throat.
- dry mouth.
- muscle pain.
- extreme tiredness
Is Efestad safe during pregnancy?
As such these findings provide reassurance by indicating that the fetal safety of Efestad is similar to the currently recommended antihistamines during pregnancy and thus Efestad can be considered to be another option for use during pregnancy.
Is Efestad safe during breastfeeding?
Considering the minimal exposure of a nursing infant to the drugs through breast milk, maternal use of Efestad dose is unlikely to result in adverse effects in nursing infants and is considered to be compatible with breastfeeding.
Can I drink alcohol with Efestad?
Efestad alone or in combination with alcohol was safe and well tolerated.
Can I drive after taking Efestad?
Do not drive and do not use tools or machines.
When should be taken of Efestad?
You can take Efestad before or after meals.
Can I take Efestad every day?
The recommended dose of Efestad tablets is one 5 mg tablet once daily.
How long does Efestad take to work?
Efestad is also use to relieve the symptoms of allergic skin conditions such as skin itch and hives. Efestad usually starts to work within 75 minutes and lasts for 24 hours.
What is the half-life of Efestad ?
The 27-hour half-life of Efestad permits once daily administration.
How long can I take Efestad for?
You can limit treatment to 14 days.
Can I take Efestad for a long time?
Efestad 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 Efestad, as it can make you feel sleepy.
Who should not take Efestad?
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 Efestad?
tiredness. sleepiness. menstrual pain. Increased sleepiness or tiredness can happen if you take more Efestad than your doctor prescribed to you.
Can Efestad cause infertility?
Efestad is not expected to cause other pregnancy problems.
Does Efestad increase blood pressure?
The decongestant in Efestad and pseudoephedrine may cause blood pressure to increase and may also speed up the heart rate.
Can Efestad affects my kidney?
Older patients are more likely to have kidney or liver problems which may make them more sensitive to the effects of Efestad. Your doctor may give you a different Efestad dose if you have kidney or liver problems.
