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Olopatadine hydrochloride

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Olopatadine hydrochloride Basic information
Olopatadine hydrochloride Chemical Properties
  • Melting point:242-245?C
  • storage temp. Refrigerator
  • solubility H2O: ≥20mg/mL
  • form solid
  • Merck 14,6840
  • CAS DataBase Reference140462-76-6(CAS DataBase Reference)
Safety Information
  • Hazard Codes T,N
  • Risk Statements 25-50
  • Safety Statements 45-61
  • RIDADR UN 2811 6.1 / PGIII
  • WGK Germany 3
  • RTECS HQ4135060
  • HS Code 29329990
Olopatadine hydrochloride Usage And Synthesis
  • DescriptionPatanol was launched in the US for use in allergic conjunctivitis. It can be prepared in five steps from the sodium salt of phydroxyphenylacetic acid methyl ester with phthalide. It has a fast onset of action with a long duration of action (due to slow dissociation kinetics) that combines the ability to prevent human conjunctival mast cell mediator release with selective H1-receptor antangonistic activity (greater H3:H1 selectivity than H2:H1 selectivity). In addition, Patanol had no inhibition of 5- lipoxygenase, PAF acetyltransferase and thromboxane synthase while interfering with phospholipase A2. It has a presynaptic inhibition of tachykinin release and inhibits bronchial sensory nerves through activation of small conductance calcium activated potassium channels. It was more potent than ketotifen and terfenadine and was effective at inhibition of PAF, LTC4 induced conjunctivitis and TXB2 production. It does not accumulate in the CNS, has a low affinity for H1-receptors in the brain, and significantly inhibits allergen induce sneezing. Patanol was more effective in conjuctival than in corneal or the trabecuiar meshwork cells.
  • Chemical PropertiesWhite Solid
  • OriginatorKyowa Hakko (Japan)
  • UsesDual acting histamine H1-receptor antagonist and mast cell stabilizer. Antiallergic; antihistaminic.
  • Usesantiallergic, antihistaminic;histamine H1 antagonist
  • Usesurinary antispasmodic
  • UsesOlopatadine hydrochloride is a potent, selective antagonist of the H1 histamine receptor (Ki = 16-41.1 nM), with much lower affinities for the H2 and H3 receptors (Ki = 43.4 and 172 μM, respectively). It blocks histamine-induced phosphoinositide turnover in isolated cells (IC50 = 9.5-39.9 nM) and prevents passive cutaneous anaphylaxis in rats (ED50 = 49 μg/kg) and anaphylactic bronchoconstriction in guinea pigs (ID50 = 30 μg/kg). Olopatadine is effective in treating allergic rhinitis and conjunctivitis. It also suppresses itch in patients with well-controlled chronic urticaria. In humans, this antihistamine does not cause cognitive or psychomotor impairment at therapeutic doses.[Cayman Chemical]
  • brand namePatanol (Alcon).
  • Veterinary Drugs and TreatmentsOlopatadine HCl is a selective H1 receptor antagonist and inhibitor of histamine release from mast cells. It is marketed for topical use to alleviate symptoms of allergic conjunctivitis in humans and is thought to be safe for use in children three years of age and older. Olopatadine, upon topical application in humans, was shown to have very limited systemic absorption. It was detectable in the milk of nursing rats, after topical application, and like most medications should be avoided in pregnant or nursing animals.
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