CLEMASTINE FUMARATE

(2R)-2-(2-((1R)-1-(4-chlorophenyl)-1-phenylethoxy)ethyl)-1-methylpyrrolidine (E)-but-2-enedioic acid; (R-(R',R'))-2-(2-(1-(p-Chlorophenyl)-1-phenylethoxy)ethyl)-1-methylpyrrolidinium hydrogen fumarate; (+)-2-(2-((p-Chloro-alpha-methyl-alpha-phenylbenzyl)oxy)ethyl)-1-methyl pyrrolidine fumarate; (+)-(2R)-2-(2-(((R)-p-Chloro-alpha-methyl-alpha-phenylbenzyl)oxy)ethyl)-1-methylpyrrolidine fumarate; Clemastine hydrogen fumarate; Agasten; Aloginan; Alphamin; Anhistan; Clemanil; Fulumino; Inbestan; Kinotomin; Lacretin; Lecasol; Maikohis; Mallermin-F; Marsthine; Masletine; Meclastine hydrogen fumarate; Mecloprodine; Piloral; Reconin; Tavegil; Tavegyl; Tavist; Tavist-1; Telgin-G; Trabest; Xolamin;

CLEMASTINE

 

PRODUCT IDENTIFICATION

CAS RN

15686-51-8 (parent), 14976-57-9 (fumarate)

EINECS RN

239-055-2

FORMULA

C21H26ClNO·C4H4O4

MOLE WEIGHT

459.96

 

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE

white crystalline powder

MELTING POINT

 

BOILING POINT

 

DENSITY

 

SOLUBILITY IN WATER

slightly

pH

 

VAPOR DENSITY

 

REFRACTIVE INDEX

 

FLASH POINT

 

 

STABILITY AND REACTIVITY
STABILITY Stable under normal conditions.

INCOMPATIBLE MATERIALS

Strong oxidizing agents.

DECOMPOSITION PRODUCTS

Carbon monoxide, Carbon dioxide, Nitrogen oxides, Hydrogen chloride

POLYMERIZATION Has not been reported

NFPA RATINGS

Health: 1, Flammability: 0, Reactivity: 0

 

SAFETY

HAZARD NOTES

Avoid contact and inhalation. Target organs: Central nervous system.

EYE

May cause skin irritation.

SKIN

May be harmful if absorbed through the skin. Eye Contact: May cause eye irritation.

INGESTION

May be harmful if swallowed.

INHALATION

May be harmful if inhaled. Material may be irritating to mucous membranes and upper respiratory tract.

TARGET ORGANS

Central nervous system.

 

TRANSPORT & REGULATORY INFORMATION

UN NO.

 
HAZARD CLASS

 

PACKING GROUP

 

HAZARD SYMBOL

 

RISK PHRASES

 

SAFETY PHRASES

 

 

EXTERNAL LINKS & GENERAL INFORMATION
Histamine is a substance produced by the body as part of its defence mechanisms. It is stored in cells called mast cells, in almost all tissues of the body. When the body reacts to a foreign substance (known as an allergen, eg flower pollen, pet fur, dust mites), the mast cells are stimulated by the allergen and release their stores of histamine. The released histamine then binds to its receptors (H1 receptors), causing a chain reaction that results in allergic symptoms. It causes an increase in blood flow to the area of the allergy, and the release of other chemicals that add to the allergic response. All this results in the symptoms of an allergic reaction. In hayfever, this causes inflammation of the nose, eyes, skin or airways and results in itchy watery eyes, a runny nose, sneezing and nasal congestion. Histamine is also responsible for the symptoms of allergic and itchy rashes, and allergic reactions to foods, medicines or insect bites. It can also cause more severe allergic reactions such as angioneurotic oedema, which involves severe swelling of the eyes, lips, tongue or throat. Clemastine works by blocking histamine H1 receptors. It doesn't prevent the actual release of histamine from mast cells, but prevents it binding to its receptors. This in turn prevents the release of other allergy chemicals and increased blood supply to the area, and provides relief from the symptoms of allergies. Clemastine is called a sedating antihistamine because it enters the brain in significant quantities and causes drowsiness. (http://netdoctor.co.uk/)

Corticosteroids are the most effective medications for the systemic therapy of allergic dermatitis. They are, however, the most likely to result in unwanted side-effects. Oral prednisolone or prednisone can be administered at 1mg/kg daily in the morning until the symptoms are controlled and then only on alternate days at a reducing dose. Controlling concurrent precipitating and secondary skin disease (acariosis, pyoderma, Malassezia dermatitis, flea infestation) are essential. The use of antihistamines either on their own or with glucocorticoids is recommended – if only to lower the dose of the glucocorticoids. H1 blockers such as chlorpheniramine, clemastine, hydroxyzine, diphenhydramine and trimeprazine have been found to allow for a reduce corticosteroid dosage and may be effective on their own. ( http://www.vetpath.co.za/)

Antipruritics

 

Product

CAS RN.

Ammonium lactate 515-98-0

Bamipine

4945-47-5

Benzocaine

94-09-7
Camphor 76-22-2
Capsaicin 404-86-4

Chloropyramine

59-32-5
Chlorpheniramine 132-22-9

Chlorphenoxamine

77-38-3
Clemastine fumarate 14976-57-9

Clemastine

15686-51-8
Cyproheptadine hydrochloride 41354-29-4
Cyproheptadine 129-03-3
Dibucaine 85-79-0

Dimetindene

5636-83-9
Diphenhydramine hydrochloride 147-24-0

Diphenhydramine

58-73-1
Hydroxyzine 68-88-2

Isothipendyl

482-15-5
Ketotifen 34580-13-7
Lidocaine hydrochloride monohydrate 6108-05-0
Lidocaine hydrochloride 73-78-9

Lidocaine

137-58-6
Loratadine 79794-75-5
Menthol 1490-04-6

Mepyramine

91-84-9
Methdilazine hydrochloride 1229-35-2
Methdilazine 1982-37-2
Ondansetron 99614-02-5

Oxybuprocaine

99-43-4
Pheniramine 86-21-5

Pramocaine

140-65-8
Promethazine hydrochloride 58-33-3

Promethazine

60-87-7

Quinisocaine

86-80-6

Tetracaine

94-24-6

Thenalidine

86-12-4

Thonzylamine

91-85-0

Tolpropamine

5632-44-0
Trimeprazine hydrochloride 1936-51-2
Trimeprazine tartrate 4330-99-8
Trimeprazine 84-96-8

Tripelennamine

91-81-6

 

 

SALES SPECIFICATION

APPEARANCE

white crystalline powder

IDENTIFICATION

pass Test A (TLC), B (Infrared Absorption)

ASSAY

98.0 - 101.0%

OPTICAL ROTATION

+15° ~ +18 °

HEAVY METALS

20ppm max

LOS ON DRYING

0.5% max

RELATED SUBSTANCES

1.0% max (total), 0.3% max (individual)

 

PACKING

 

 

PRICE

U$6,900 (500g)