Loratadine
- CAS No.
- 79794-75-5
- Chemical Name:
- Loratadine
- Synonyms
- LORATIDINE;CLARITIN;Ethyl 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)piperidine-1-carboxylate;CLARATYNE;1-Piperidinecarboxylic acid;ethyl 4-(8-chloro-5,6-dihydro-11h-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylate;Tadine;Lisino;Loranox;Civeran
- CBNumber:
- CB5283770
- Molecular Formula:
- C22H23ClN2O2
- Molecular Weight:
- 382.88
- MOL File:
- 79794-75-5.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/4/17 18:50:11
| Melting point | 134-136°C |
|---|---|
| Boiling point | 531.3±50.0 °C(Predicted) |
| Density | 1.261±0.06 g/cm3(Predicted) |
| RTECS | TM6129200 |
| storage temp. | 2-8°C |
| solubility | DMSO: 26 mg/mL, soluble |
| form | powder |
| pka | 4.27±0.20(Predicted) |
| color | white |
| Water Solubility | It is soluble in DMSO (50 mg/ml), ethanol (77 mg/ml at 25°C), water (<1 mg/ml at 25°C), chloroform, and methanol. |
| Merck | 14,5578 |
| BCS Class | 2 |
| Stability | Stable, but may be heat sensitive - refrigerate. Incompatible with strong oxidizing agents. |
| InChIKey | JCCNYMKQOSZNPW-UHFFFAOYSA-N |
| CAS DataBase Reference | 79794-75-5(CAS DataBase Reference) |
| EPA Substance Registry System | 1-Piperidinecarboxylic acid, 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-, ethyl ester (79794-75-5) |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H319-H335-H315 | |||||||||
| Precautionary statements | P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P | |||||||||
| Hazard Codes | Xi | |||||||||
| Risk Statements | 36/37/38 | |||||||||
| Safety Statements | 22-24/25-36-26 | |||||||||
| RIDADR | 3077 | |||||||||
| WGK Germany | 2 | |||||||||
| HS Code | 29333990 | |||||||||
| NFPA 704 |
|
Loratadine price More Price(5)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich(India) | PHR1376 | Loratadine Pharmaceutical Secondary Standard; Certified Reference Material | 79794-75-5 | 1G | ₹11160.58 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | L9664 | Loratadine ≥98% (HPLC), powder | 79794-75-5 | 10MG | ₹16183.38 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | L9664 | Loratadine ≥98% (HPLC), powder | 79794-75-5 | 50MG | ₹64679.38 | 2022-06-14 | Buy |
| TCI Chemicals (India) | L0223 | Loratadine | 79794-75-5 | 100MG | ₹3600 | 2022-05-26 | Buy |
| TCI Chemicals (India) | L0223 | Loratadine | 79794-75-5 | 1G | ₹8600 | 2022-05-26 | Buy |
Loratadine Chemical Properties,Uses,Production
Description
Loratadine is a non-sedating antihistamine indicated for use in allergic rhinitis and chronic urticaria. Its major advantage over other non-sedating antihistamines such as astemizole and terfenadine is its very fast onset of action. Loratadine is claimed not to cross the blood-brain barrier.
Chemical Properties
White Crystalline Solid
Uses
Loratadine, is used as a peripheral histamine H1 receptor agonist. It is also used as an orally active antiallergic agent. It is an important raw material and intermediate used in Organic Synthesis, Pharmaceuticals, Agrochemicals and Dyestuff.
Indications
Loratadine (Claritin) is a long-acting, potent peripheral H1 blocker with minimal sedative effects. It does not appear to have the same adverse cardiac effects as the other nonsedating H1 antihistamines. It is indicated for allergic rhinitis and chronic urticaria.
General Description
Loratadine, 4-(8-chloro-5,6-dihydro-11Hbenzo[5,6]-cyclohepta[1,2-b]pyridin-l 1-ylidene-1-carboxylic acid ethyl ester, is a white to off-white powder insoluble in water but very soluble in acetone, alcohols, and chloroform. Loratadine is structurally related to the antihistamines azatadine and cyproheptadine, and to some tricyclic antidepressants. It differs from azatadine, in that a neutral carbamate group has replaced the basic tertiary amino moiety, and a phenyl ring has been substituted with a chlorine atom. Loratadine is a selective peripheral H1-antihistamine with a receptor-binding profile like that of the other members of this series, except that it has more antiserotonergic activity. Thus, it produces no substantial CNS or autonomic side effects or cardiac toxicity.
Loratadine displays potency comparable with that of astemizole and greater than that of terfenadine. Loratadine is indicated for the relief of nasal and nonnasal symptoms of seasonal allergic rhinitis. In the presence of a CYP3A4 inhibitor ketoconazole, loratadine is metabolized to descarboethoxyloratadine predominantly by CYP2D6.
Biological Activity
Peripheral histamine H 1 receptor antagonist (K i = 35 nM); devoid of central effects. Orally active antiallergic agent.
Clinical Use
Loratadine is related to the first-generation tricyclic antihistamines and to antidepressants. It is nonsedating, and neither it nor its major metabolite, desloratadine (descarboethoxyloratadine), is associated with the potentially cardiotoxic effects reported for terfenadine and astemizole. On chronic dosing, the AUC (plasma concentration–time curve) for the metabolite is greater than that for the parent drug, and its half-life is longer.
Drug interactions
Potentially hazardous interactions with other drugs
Antibacterials: concentration possibly increased by
erythromycin.
Antifungals: concentration of loratadine possibly
increased by ketoconazole – avoid concomitant use.
Antivirals: concentration possibly increased by
ritonavir.
Metabolism
Loratadine undergoes an extensive first pass metabolism, mainly by CYP3A4 and CYP2D6. The major metabolite-desloratadine is pharmacologically active and responsible for a large part of the clinical effect. Approximately 40% of the dose is excreted in the urine and 42% in the faeces over a 10 day period and mainly in the form of conjugated metabolites. Approximately 27% of the dose is eliminated in the urine during the first 24 hours. Less than 1% of the active substance is excreted unchanged in the active form, as loratadine or desloratadine.
Loratadine Preparation Products And Raw materials
Raw materials
1of2
chevron_rightPreparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| TAGOOR LABORATORIES PVT LTD | +919700187008 | AndhraPradesh, India | 93 | 58 | Inquiry |
| Cadila Pharmaceuticals Ltd | +91-7069076657 +91-7069076657 | Ahmedabad, India | 54 | 58 | Inquiry |
| GLP Pharma Standards | +91 9866074638 | Hyderabad, India | 1644 | 58 | Inquiry |
| Chemicea Pharmaceuticals Pvt Ltd | +91-918482849343 +91-8482849343 | Mumbai, India | 461 | 58 | Inquiry |
| Veer Pharmachem | +91-02645661117 +91-9879471589 | Gujarat, India | 39 | 58 | Inquiry |
| KARPSCHEM LABORATORIES | +91-7249203006 +91-7249203006 | Maharashtra, India | 786 | 58 | Inquiry |
| Glenmark Pharmaceuticals Limited | +912240189999 | Maharashtra, India | 93 | 58 | Inquiry |
| Ions Pharma | +912266707500 | Maharashtra, India | 89 | 58 | Inquiry |
| Hetero Drugs Limited | +91-4023704923 +91-4023704923 | Telangana, India | 296 | 58 | Inquiry |
| Sam Fine O Chem Limited | +91-9987622299 +91-9987622299 | Maharashtra, India | 94 | 58 | Inquiry |
| Supplier | Advantage |
|---|---|
| TAGOOR LABORATORIES PVT LTD | 58 |
| Cadila Pharmaceuticals Ltd | 58 |
| GLP Pharma Standards | 58 |
| Chemicea Pharmaceuticals Pvt Ltd | 58 |
| Veer Pharmachem | 58 |
| KARPSCHEM LABORATORIES | 58 |
| Glenmark Pharmaceuticals Limited | 58 |
| Ions Pharma | 58 |
| Hetero Drugs Limited | 58 |
| Sam Fine O Chem Limited | 58 |
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