Loperamide hydrochloride
- CAS No.
- 34552-83-5
- Chemical Name:
- Loperamide hydrochloride
- Synonyms
- LOPERAMIDE HCL;suprasec;imodium;blox;pj185;imosec;Imosse;r18553;Clalet;Imossel
- CBNumber:
- CB8758181
- Molecular Formula:
- C29H34Cl2N2O2
- Molecular Weight:
- 513.5
- MOL File:
- 34552-83-5.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/7/2 8:55:37
| Melting point | 223-225°C |
|---|---|
| Density | 1.1905 (rough estimate) |
| refractive index | 1.6100 (estimate) |
| storage temp. | 2-8°C |
| solubility | Slightly soluble in water, freely soluble in ethanol (96 per cent) and in methanol. |
| pka | 8.66(at 25℃) |
| form | Solid |
| color | White to Almost white |
| Merck | 14,5571 |
| CAS DataBase Reference | 34552-83-5(CAS DataBase Reference) |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS06 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Danger | |||||||||
| Hazard statements | H301 | |||||||||
| Precautionary statements | P301+P330+P331+P310 | |||||||||
| Hazard Codes | T | |||||||||
| Risk Statements | 25 | |||||||||
| Safety Statements | 45 | |||||||||
| RIDADR | UN 2811 6.1/PG 3 | |||||||||
| WGK Germany | 3 | |||||||||
| RTECS | TM4960000 | |||||||||
| HazardClass | 6.1(b) | |||||||||
| PackingGroup | III | |||||||||
| HS Code | 29333990 | |||||||||
| Toxicity | LD50 in mice (mg/kg): 75 s.c.; 28 i.p.; 105 orally; in rats (mg/kg): 185 orally (Niemegeers) | |||||||||
| NFPA 704 |
|
Loperamide hydrochloride price More Price(8)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich(India) | PHR1162 | Loperamide hydrochloride Pharmaceutical Secondary Standard; Certified Reference Material | 34552-83-5 | 1G | ₹9753.33 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | L4762 | Loperamide hydrochloride | 34552-83-5 | 5G | ₹14570.45 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | L4762 | Loperamide hydrochloride | 34552-83-5 | 25G | ₹58065.3 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | 5.08162 | Loperamide Hydrochloride - CAS 34552-83-5 - Calbiochem | 34552-83-5 | 1G | ₹10550.01 | 2022-06-14 | Buy |
| Sigma-Aldrich | 34014 | Loperamide hydrochloride VETRANAL?, analytical standard | 34552-83-5 | 100MG | ₹5564.05 | 2022-06-14 | Buy |
Loperamide hydrochloride Chemical Properties,Uses,Production
Chemical Properties
White Solid
Uses
Loperamide hydrochloride is a Ca2+ channel protein inhibitor and MOR activator.
Definition
ChEBI: A hydrochloride obtained by combining loperamide with one equivalent of hydrochloric acid. Used for treatment of diarrhoea resulting from gastroenteritis or inflammatory bowel disease.
Indications
Loperamide hydrochloride (Imodium) structurally resembles both haloperidol and meperidine. In equal doses, loperamide protects against diarrhea longer than does diphenoxylate. It reduces the daily fecal volume and decreases intestinal fluid and electrolyte loss. Loperamide produces rapid and sustained inhibition of the peristaltic reflex through depression of longitudinal and circular muscle activity.The drug also possesses antisecretory activity, presumably through an effect on intestinal opioid receptors.
General Description
Loperamide is an antidiarrheal agent used in controlling acute nonspecific diarrhea and chronic diarrhea associated with inflammatory bowel diseases.
Biological Activity
High affinity μ -opioid receptor agonist with peripheral selectivity (K i values are 2, 48 and 1156 nM for μ -, δ - and κ -opioid receptors respectively). Antidiarrhoeal and antihyperalgesic agent. Also a Ca 2+ channel blocker; at low micromolar concentrations it blocks broad spectrum neuronal HVA Ca 2+ channels and at higher concentrations it reduces Ca 2+ flux through NMDA receptor operated channels.
Mechanism of action
Loperamide also is a potent inhibitor of intestinal CYP3A4, increasing the intestinal absorption of other CYP3A4 substrates. The clinically significant drug interactions of loperamide with coadministered CYP3A4 and CYP2C8 substrates or inhibitors would be limited, however, because of its two metabolic pathways.
Pharmacokinetics
Loperamide is marketed as capsules (2 mg) and liquid (1 mg/5 mL) preparations. The recommended dose is 4 mg initially and an additional 2 mg following each diarrheal stool. The dose should not exceed 16 mg/day. It is too lipophilic to dissolve in water for an intravenous dosage form, a property that limits its abuse potential. The compound is highly lipophilic and undergoes slow dissolution, thus limiting the bioavailability of the agent to approximately 40% of the dose. Its low oral bioavailability also can be attributed to first-pass metabolism by both CYP2C8 and CYP3A4 to its primary N-demethyl metabolite. Peak plasma levels are reached in approximately 5 hours, with an elimination half-life of approximately 11 hours. Approximately 1% of the dose is excreted into the urine unchanged.
Clinical Use
Loperamide is effective against a wide range of secretory stimuli and can be used in the control and symptomatic relief of acute diarrhea that is not secondary to bacterial infection.
Side effects
Adverse effects associated with its use include abdominal pain and distention, constipation, dry mouth, hypersensitivity, and nausea and vomiting.
Loperamide hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| TAGOOR LABORATORIES PVT LTD | +919700187008 | AndhraPradesh, India | 93 | 58 | Inquiry |
| Jigs Chemical ltd | +919099003427 | Gujarat, India | 239 | 58 | Inquiry |
| ANWITA APIS | +919000311012 | Hyderabad, India | 198 | 58 | Inquiry |
| MOLECRAFT LIFE SCIENCES PVT LTD | +91 9581188881 | Telangana, India | 189 | 58 | Inquiry |
| Vamsi Labs Ltd | +91-2172357274 +91-9891966300 | Maharashtra, India | 43 | 58 | Inquiry |
| Ralington Pharma | +91-7948911722 +91-9687771722 | Gujarat, India | 1350 | 58 | Inquiry |
| Lanz Labs Pvt Ltd | +91-2226205525 +91-2226205525 | Maharashtra, India | 5 | 58 | Inquiry |
| Fleming Laboratories Ltd | +91-9666407333 +91-9666022445 | Hyderabad, India | 22 | 58 | Inquiry |
| Besil Chem LLP | +91-7760252666 +91-9880731835 | Bangalore, India | 163 | 58 | Inquiry |
| Lake Chemicals Pvt Ltd | 91-80-22868600 | Karnataka, India | 9 | 58 | Inquiry |
| Supplier | Advantage |
|---|---|
| TAGOOR LABORATORIES PVT LTD | 58 |
| Jigs Chemical ltd | 58 |
| ANWITA APIS | 58 |
| MOLECRAFT LIFE SCIENCES PVT LTD | 58 |
| Vamsi Labs Ltd | 58 |
| Ralington Pharma | 58 |
| Lanz Labs Pvt Ltd | 58 |
| Fleming Laboratories Ltd | 58 |
| Besil Chem LLP | 58 |
| Lake Chemicals Pvt Ltd | 58 |
34552-83-5(Loperamide hydrochloride)Related Search:
1of4
chevron_right