PRODUCT IDENTIFICATION

TOXICITY

H.S. CODE

CLASSIFICATION

EXTRA NOTES

PHYSICAL AND CHEMICAL PROPERTIES

white to off-white crystalline powder

Sparingly soluble

Soluble methanol

REFRACTIVE INDEX

NFPA RATINGS

Health hazard: 2, Fire: 0, Reactivity Hazard: 0

AUTOIGNITION

FLASH POINT

EXTERNAL LINKS & GENERAL DESCRIPTION

Wikipedia Linking

Google Scholar Search

Drug Information Portal (U.S. National Library of Medicine) - Olopatadine

PubChem Compound Summary - Olopatadine

http://www.drugbank.ca/
Olopatadine is a selective histamine H1 antagonist that binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Olopatadine is devoid of effects on alpha-adrenergic, dopamine and muscarinic type 1 and 2 receptors.

http://dmd.aspetjournals.org/
Effects of Olopatadine, a New Antiallergic Agent, on Human Liver Microsomal Cytochrome P450 Activities - Olopatadine, a new histamine H₁ receptor-selective antagonist, is a tricyclic drug containing an alkylamino moiety. Some compounds containing a similar alkylamino group form a cytochrome P450 (P450) -iron (II)-nitrosoalkane metabolite complex [metabolic intermediate complex (MIC)], thereby causing quasi-irreversible inhibition of the P450. There was concern that olopatadine might also form MICs, therefore, the present investigation was undertaken to explore this possibility. We identified the enzymes catalyzing olopatadine metabolism and investigated the effect of olopatadine on human P450 activities. During incubation with human liver microsomes in the presence of a NADPH-generating system, olopatadine was metabolized to two metabolites, M1 (N-monodemethylolopatadine) and M3 (olopatadine N-oxide) at rates of 0.330 and 2.50 pmol/min/mg protein, respectively. Troleandomycin and ketoconazole, which are both selective inhibitors of CYP3A, significantly reduced M1 formation but specific inhibitors of other P450 isozymes did not decrease M1 formation. Incubation of olopatadine with cDNA-expressed human P450 isozymes confirmed that M1 formation was almost exclusively catalyzed by CYP3A4. The formation of M3 was enhanced byN-octylamine and was inhibited by thiourea. High specific activity of M3 formation was exhibited by cDNA-expressed flavin-containing monooxygenase (FMO)1 and FMO3. Olopatadine did not inhibit P450 activities when it was simultaneously incubated with substrates for different P450 isozymes. Also, P450 activities in human liver microsomes were unaffected by pretreatment with olopatadine or M1. Furthermore, spectral analysis revealed that neither olopatadine nor M1 formed an MIC. Therefore, it is unlikely that olopatadine will cause drug-drug interactions involving P450 isozymes.

http://jnm.snmjournals.org/
Cerebral Histamine H1 Receptor Binding Potential Measured with PET Under a Test Dose of Olopatadine, an Antihistamine, Is Reduced After Repeated Administration of Olopatadine

APPEARANCE

white to off-white crystalline powder

IDENTIFICATION

passes Test

PURITY

98.5% min

SOLUTION CLARITY

0.1 Au max

RELATED SUBSTANCES

E-Isomer 0.5% max, Individual Impurity 0.05% max, Sum Impurity 1.0% max

LOSS ON DRYING

0.5% max

HEAVY METALS

10ppm max

RESIDUE ON IGNITION

0.1% max

6.1 (Packing group: III)

GHS

OSHA Hazards: Toxic by ingestion

Danger

PICTOGRAMS

HAZARD STATEMENTS

H301 Toxic if swallowed.
H400 Very toxic to aquatic life.

PRECAUTIONARY STATEMENTS

P273 Avoid release to the environment.
P301 + P310 IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

T ToxicN Dangerous for the environment

RISK PHRASES

25 Toxic if swallowed
50 Very Toxic to aquatic organisms

SAFETY PHRASES

45 In case of accident or if you feel unwell, seek medical advice immediately (show label where possible)
61 Avoid release to the environment. Refer to special instructions safety data sheet