CHEM-241-Principles of Chemistry Desloratadine

CHEM-241-Principles of Chemistry

Desloratadine
(C19H19ClN2)

We Will Write a Custom Essay Specifically
For You For Only $13.90/page!


order now

Project done by:
Mohammad Mansour
Id: 201401973

Submitted to: Prof. Ghassan Younes

TABLE OF CONTENTS

Chapter 1. Introduction 1
1.1 Definition 1
1.2 History 1
1.3 List of excipients…………………………………………………………………………………………1
Chapter 2. Physical and Chemical Properties 2
2.1 Table of Properties 2
2.2 Structure 2
2.2 Naming 2
Chapter 3. Method of Preperation 3
3.1 Synthesis 3
Chapter 4. Application and Uses 3
4.1 Applications 3
4.2 How Does It Work 3
4.3 Recommended Dose 4
4.4 Side Effects 4
4.5 Price…………… 4
References 5

1. Introduction:
1.1. Definition
Desloratadine 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 C19H19ClN2
Complexity 425
Molecular Weight 310.825 g/mol
Formal Charge 0
Topological polar surface area 24.9 A^2
Color blue solid
Hydrogen Bond Donor count 1
Covalently-Bonded Unit Count 1
Hydrogen Bond Acceptor count 2

2.2. Structure:
2D Structure: 3D Structure:

2.3. Iupac naming
2.4.
8-chloro-11-piperidin-4-ylidene-5,6-dihydrobenzo1,2cyclohepta2,4-bpyridine
3. Method of Preperation

3.1. Synthesis
In 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 temperature
ii. 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 phase
v. 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 eyes
runny nose
itching eyes/nose
sneezing/ 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 Rhinitis
Initial dose: 5 mg orally once a day
Maintenance dose: 5 mg orally once a day
Usual Adult Dose for Urticaria
Initial dose: 5 mg orally once a day
Maintenance dose: 5 mg orally once a day
Usual Geriatric Dose for Allergic Rhinitis
Initial dose: 5 mg orally once a day.
Maintenance dose: 5 mg orally once a day.
Usual Geriatric Dose for Urticaria
Initial dose: 5 mg orally once a day.
Maintenance dose: 5 mg orally once a day.
Renal Dose Adjustments
Initial dose: 5 mg orally once every other day.
Maintenance dose: 5 mg orally every other day.
Liver Dose Adjustments
Initial dose: 5 mg orally once every other day.
Maintenance dose: 5 mg orally every other day
4.4. Side effects
The most common side-effects are fatigue, dry mouth, and headache
4.5. Price
The lowest price of desloratadine is around $18.14 the 85% average retail price of $129.52.

References:
https://en.wikipedia.org/wiki/Desloratadine#Side_effects
https://pubchem.ncbi.nlm.nih.gov/compound/Desloratadine#section=DrugBank-Interactions
https://www.drugs.com/dosage/desloratadine.html
https://chealth.canoe.com/drug/getdrug/desloratadine-allergy-control
https://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