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| 50mg |
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| 250mg |
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| 500mg |
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| 1g |
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Epinastine (also known as WAL-801CL HCl) is a potent antihistamine H1 without sedative activity and a mast cell stabilizer that is used in eye drops for the treatment of allergic conjunctivitis. The release of histamine from mast cells is inhibited by epinastine hydrochloride, which also blocks the histamine H1 receptor. This avoids the common allergic reactions that result from histamine activation on the skin, mucous membranes, and capillaries.
| ln Vitro |
Epinastine can displace specific [3H]NC-5Z binding at low concentrations in locust nervous tissue. Epinastine binds to the neuronal octopamine receptor in honey bees with Ki of 1.1 nM. Epinastine antagonises octopamine-induced cAMP formation in the insect brain[2].
Epinastine inhibits the release of histamine from peritoneal mast cells in rats that is brought on by compound 48/80 and the antigen-antibody reaction. Comparably, epinastine inhibits the release of histamine from isolated rat peritoneal mast cells as well as from rat mesenterial pieces when compound 48/80 is present. In actively sensitized guinea pigs, epinastine effectively inhibits both the release of Ca2+ from the intracellular Ca store of rat peritoneal mast cells exposed to compound 48/80 and substance P, as well as the uptake of Ca2+ into lung mast cells[3]. One of the chemokines released by eosinophils isolated from atopic diseases, IL-8, is suppressed by epinastine in a dose- and time-dependent manner[4].
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| ln Vivo |
Epinastine demonstrates a high affinity for H1-receptors in receptor binding studies in the guinea pig ileum. Epinastine prevents rats, dogs, and guinea pigs from experiencing histamine-induced reactions in their skin or lungs[1].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
The absolute bioavailability of epinastine is about 40%. Epinastine is mainly excreted unchanged. The renal elimination is mainly via active tubular secretion. 56 L/hr [patients with allergic conjunctivitis receiving one drop of ELESTAT® ophthalmic solution in each eye twice daily for seven days] Metabolism / Metabolites Mainly excreted unchanged, less than 10% metabolized. Biological Half-Life 12 hours |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Evidence from 7 individuals indicates that transfer of epinastine into breastmilk and the resulting infant serum levels are likely to be minimal and unlikely to cause adverse effects in breastfed infants. In the U.S., epinastine is only available as eye drops. Because absorption from the eye is limited, epinastine would not be expected to cause any adverse effects in breastfed infants. To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue. ◉ Effects in Breastfed Infants In a study of 7 nursing mothers who were taking oral epinastine 20 mg once daily. No adverse reactions in the infants were reported. ◉ Effects on Lactation and Breastmilk Antihistamines in relatively high doses given by injection can decrease basal serum prolactin in nonlactating women and in early postpartum women. However, suckling-induced prolactin secretion is not affected by antihistamine pretreatment of postpartum mothers. The prolactin level in a mother with established lactation may not affect her ability to breastfeed. Low ophthalmic doses of epinastine are unlikely to have the same effect on serum prolactin. Protein Binding 64% |
| References |
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| Additional Infomation |
Epinastine is a benzazepine that is 6,11-dihydro-5H-dibenzo[b,e]azepine in which the azepine ring is fused to the e side of 4,5-dihydro-1H-imidazol-2-amine. It has a role as an anti-allergic agent, a histamine antagonist, an ophthalmology drug and a H1-receptor antagonist. It is a member of guanidines and a benzazepine.
Epinastine is used for the prevention of itching associated with allergic conjunctivitis. It has a multi-action effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response. Epinastine is an Adrenergic Receptor Agonist and Histamine-1 Receptor Inhibitor. The mechanism of action of epinastine is as an Adrenergic Agonist and Histamine H1 Receptor Antagonist. The physiologic effect of epinastine is by means of Decreased Histamine Release. See also: Epinastine Hydrochloride (has salt form). Drug Indication For the prevention of itching associated with allergic conjunctivitis. FDA Label Mechanism of Action Epinastine has a multiaction effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response. |
| Molecular Formula |
C₁₆H₁₅N₃
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|---|---|
| Molecular Weight |
249.31
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| Exact Mass |
249.127
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| Elemental Analysis |
C, 77.08; H, 6.06; N, 16.85
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| CAS # |
80012-43-7
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| Related CAS # |
Epinastine hydrochloride; 108929-04-0; Epinastine-13C,d3 hydrobromide; 127786-29-2 (HBr)
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| PubChem CID |
3241
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| Appearance |
White to off-white solid powder
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| Density |
1.32 g/cm3
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| Boiling Point |
428ºC at 760 mmHg
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| Melting Point |
270ºC
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| Flash Point |
212.7ºC
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| Index of Refraction |
1.727
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| LogP |
2.667
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
19
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| Complexity |
378
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1CC2N(C3C(CC4C2=CC=CC=4)=CC=CC=3)C=1N
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| InChi Key |
WHWZLSFABNNENI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H15N3/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16/h1-8,15H,9-10H2,(H2,17,18)
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| Chemical Name |
2,4-diazatetracyclo[12.4.0.02,6.07,12]octadeca-1(18),3,7,9,11,14,16-heptaen-3-amine
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| Synonyms |
WAL801; WAL 801; WAL-801; Epinastine; brand names Alesion, Elestat, Purivist, Relestat
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 50 mg/mL (~200.6 mM)
H2O: < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0111 mL | 20.0554 mL | 40.1107 mL | |
| 5 mM | 0.8022 mL | 4.0111 mL | 8.0221 mL | |
| 10 mM | 0.4011 mL | 2.0055 mL | 4.0111 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02182518 | Completed | Drug: Epinastine Drug: Placebo |
Rhinitis, Allergic, Perennial | Boehringer Ingelheim | May 2000 | Phase 3 |
| NCT02260063 | Completed | Drug: Epinastine syrup Drug: Epinastine tablets |
Healthy | Boehringer Ingelheim | November 1998 | Phase 1 |
| NCT02182531 | Completed | Drug: Epinastine Drug: Pseudoephedrine |
Healthy | Boehringer Ingelheim | August 1999 | Phase 1 |
| NCT02260037 | Completed | Drug: Epinastine nasal Drug: Placebo |
Healthy | Boehringer Ingelheim | August 2001 | Phase 1 |
| NCT01382654 | Completed | Drug: epinastine 0.1% Drug: epinastine 0.2% |
Allergic Rhinitis | Merck Sharp & Dohme LLC | September 2006 | Phase 2 |
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