CHEM-241-Principles of ChemistryDesloratadine (C19H19ClN2)Project done by:Mohammad Mansour Id: 201401973Submitted to: Prof. Ghassan YounesTABLE OF CONTENTSChapter 1. Introduction 11.1 Definition 11.2 History 1 1.3 List of excipients…………………………………………………………………………………………1 Chapter 2.
Physical and Chemical Properties 22.1 Table of Properties 22.2 Structure 22.
2 Naming 2Chapter 3. Method of Preperation 33.1 Synthesis 3Chapter 4. Application and Uses 34.1 Applications 34.2 How Does It Work 34.
3 Recommended Dose 44.4 Side Effects 44.5 Price…………… 4 References 5 1. Introduction:1.1. DefinitionDesloratadine is a tricyclic H1-antihistamine that used for treating allergies. It is an active metabolite of loratadine and named Clarinex in US and Aerius in Europe and Canada and can be found in many doses and forms.
1.2. Medical uses:Desloratadine is an antihistamine used to relieve allergy symptoms and it can be used to treat It is used to treat hives.1.
3. List of excipients • Microcrystalline cellulose • Starch, pregelatinised• Mannitol• Talc• Magnesium stearate• Tablet coating: • Hypromellose 6cP• Titanium dioxide (E171)• Macrogol 6000• Indigo carmine aluminum lake (E132) 2. Physical and chemical properties:Desloratadine is a Histamine-1 Receptor Antagonist. The mechanism of action of desloratadine is as a Histamine H1 Receptor Antagonist according to FDA Pharm Classes.
2.1. Table of properties:Molecular Formula C19H19ClN2Complexity 425Molecular Weight 310.
825 g/molFormal Charge 0Topological polar surface area 24.9 A^2Color blue solidHydrogen Bond Donor count 1Covalently-Bonded Unit Count 1Hydrogen Bond Acceptor count 22.2. Structure:2D Structure: 3D Structure: 2.3.
Iupac naming2.4. 8-chloro-11-piperidin-4-ylidene-5,6-dihydrobenzo1,2cyclohepta2,4-bpyridine3. Method of Preperation3.1. SynthesisIn this regard, a desirable process for preparing Desloratadine of formula (I) and its pharmaceutically acceptable salts comprises i. reacting 4-(8-Chloro-5,6-dihydro-11H-benzo5,6cyclohepta1,2-bpyridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester (Loratadine) with sodium hydroxide in a solvent mixture of toluene and polyethylene glycol (PEG 400) at reflux temperatureii.
adding a mixture of water and toluene to the reaction mixture, whereby two phases are obtained; iii. separating the organic phase; iv. concentrating the separated organic phasev. dissolving the obtained concentrate in a toluene: methyl isobutyl ketone (MIBK) mixture followed by the addition of isopropyl ether (IPE) at 60° C.; vi. cooling the slurry mass to 5° C. to 10° C.
; vii. isolating Desloratadine by filtration. 4.
Application and Uses:4.1. Applications Relieve allergy symptoms such as:watery eyesrunny nose itching eyes/nosesneezing/ hives/ itching.
4.2. How does it work:Desloratadine if from a medication group known as antihistamines, H1-receptor antagonists class .
During an allergic reaction, the body produces a chemical called histamine, which leads to allergy symptoms such as hives, sneezing, itchy throat, congestion, and itchy watery eyes. It works by stopping the action of histamine in the body.4.3.
Recommended dose:Usual Adult Dose for Allergic RhinitisInitial dose: 5 mg orally once a dayMaintenance dose: 5 mg orally once a dayUsual Adult Dose for UrticariaInitial dose: 5 mg orally once a dayMaintenance dose: 5 mg orally once a dayUsual Geriatric Dose for Allergic RhinitisInitial dose: 5 mg orally once a day.Maintenance dose: 5 mg orally once a day.Usual Geriatric Dose for UrticariaInitial dose: 5 mg orally once a day.Maintenance dose: 5 mg orally once a day.Renal Dose AdjustmentsInitial dose: 5 mg orally once every other day.Maintenance dose: 5 mg orally every other day.Liver Dose AdjustmentsInitial dose: 5 mg orally once every other day.
Maintenance dose: 5 mg orally every other day4.4. Side effectsThe most common side-effects are fatigue, dry mouth, and headache4.5. PriceThe lowest price of desloratadine is around $18.14 the 85% average retail price of $129.52.References:https://en.wikipedia.org/wiki/Desloratadine#Side_effectshttps://pubchem.ncbi.nlm.nih.gov/compound/Desloratadine#section=DrugBank-Interactionshttps://www.drugs.com/dosage/desloratadine.htmlhttps://chealth.canoe.com/drug/getdrug/desloratadine-allergy-controlhttps://www.google.com.lb/search?ei=GohPW4TIBYOTsgG_wYToDQ&q=Desloratadine+price+&oq=Desloratadine+price+&gs_l=psy-ab.3.o..3885.6346.0.7027.7.1.0.0.0.0.0.0..0.0….0…1c.1.64.psy-ab..7.0.0….0.YG559eSSEZc