China (Mainland)
Citalopram CAS NO.59729-33-8
- Min.Order: 1 Kilogram
- Payment Terms: L/C,T/T,MoneyGram,Other
- Product Details
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Quick Details
- ProName: Citalopram
- CasNo: 59729-33-8
- Molecular Formula: C20H21FN2O
- Appearance: White powder
- Application: Pharmaceutical intermediates
- DeliveryTime: within one week
- PackAge: packing 25kg/drum
- Port: Any prot in china
- ProductionCapacity: 100 Metric Ton/Year
- Purity: 99%
- Transportation: by air/sea/courier
- LimitNum: 1 Kilogram
- Residue on Ignition: ≤ 0.1%
- Heavy Metal: ≤ 10.0 ppm
- Valid Period: 2 years
- Type: Pharmaceutical Intermediates
- Specification: HIS
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Details
| Categories |
Antidepressants, Selective Serotonin Reuptake Inhibitors (SSRIs), Serotonin Uptake Inhibitors, Antidepressive Agents, Second-Generation |
| CAS number | 59729-33-8 |
| Weight |
Average: 324.3919 Monoisotopic: 324.163791509 |
| Chemical Formula | C20H21FN2O |
| InChI Key | InChIKey=WSEQXVZVJXJVFP-UHFFFAOYSA-N |
| Indication | For the treatment of depression. Unlabeled indications include: treatment of mild dementia-associated agitation in nonpsychotic patients, smoking cessation, ethanol abuse, obsessive-compulsive disorder (OCD) in children, and diabetic neuropathy. |
| Pharmacodynamics | Citalopram is one of a class of antidepressants known as selective serotonin reuptake inhibitors (SSRIs). It is used to treat the depression associated with mood disorders. It is also used on occassion in the treatment of body dysmorphic disorder and anxiety. The antidepressant, antiobsessive-compulsive, and antibulimic actions of citalopram are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. In vitro studies show that citalopram is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. Citalopram has no significant affinity for adrenergic (α1, α2, β), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. The chronic administration of citalopram was found to downregulate brain norepinephrine receptors, as has been observed with other drugs effective in the treatment of major depressive disorder. Citalopram does not inhibit monoamine oxidase. |
| Mechanism of action | The antidepressant, antiobsessive-compulsive, and antibulimic actions of citalopram are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. Citalopram blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors. SSRIs bind with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs. |
| Absorption | Rapidly and well absorbed from the GI tract. Peak plasma concentrations occur within 4 hours of a single orally administered dose. Bioavailability is 80% following oral administration. Food does not affect absorption. |
| Volume of distribution |
12 L/kg |
| Protein binding | Citalopram, dimethylcitalopram, and didemethylcitalopram is 80% bound to plasma proteins. |
| Metabolism |
Citalopram is metabolized mainly in the liver via N-demethylation to its principle metabolite, demethylcitalopram. Other metabolites include didemethylcitalopram, citalopram N-oxide, and a deaminated propionic acid derivative. However, the predominant entity in plasma is unchanged citalopram. Cytochrome P450 (CYP) 3A4 and 2C19 isozymes appear to be principally involved in producing demethylcitalopram. Demethylcitalopram appears to be further N-demethylated by CYP2D6 to didemethylcitalopram. Citalopram metabolites possess little pharmacologic activity in comparison to their parent compound and do not likely contribute to the clinical effect of the drug.
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| Route of elimination | 12-23% of an oral dose of citalopram is recovered unchanged in the urine, while 10% of the dose is recovered in the feces. |
| Half life | 35 hours |
| Clearance |
The systemic clearance of citalopram was 330 mL/min, with approximately 20% of that due to renal clearance. |
| Toxicity | Symptoms most often accompanying citalopram overdose, alone or in combination with other drugs and/or alcohol, included dizziness, sweating, nausea, vomiting, tremor, somnolence, and sinus tachycardia. In more rare cases, observed symptoms included amnesia, confusion, coma, convulsions, hyperventilation, cyanosis, rhabdomyolysis, and ECG changes (including QTc prolongation, nodal rhythm, ventricular arrhythmia, and very rare cases of torsade de pointes). Acute renal failure has been very rarely reported accompanying overdose. Withdrawal symptoms include flu-like symptoms, insomnia, nausea, imbalance, sensory changes and hyperactivity. |
| Affected organisms |
Humans and other mammals |
| State | solid | ||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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