Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C13H20N2O2 |
Molecular Weight | 236.3101 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC[C@@H](O)CN1CCN(CC1)C2=CC=CC=C2
InChI
InChIKey=PTVWPYVOOKLBCG-ZDUSSCGKSA-N
InChI=1S/C13H20N2O2/c16-11-13(17)10-14-6-8-15(9-7-14)12-4-2-1-3-5-12/h1-5,13,16-17H,6-11H2/t13-/m0/s1
DescriptionSources: http://www.medscape.com/viewarticle/432995_1Curator's Comment: description was created based on several sources, including
https://www.rlsnet.ru/mnn_index_id_2804.htm | https://www.drugs.com/international/levodropropizine.html | https://www.ncbi.nlm.nih.gov/pubmed/26097707 | https://www.ncbi.nlm.nih.gov/pubmed/1611233
Sources: http://www.medscape.com/viewarticle/432995_1
Curator's Comment: description was created based on several sources, including
https://www.rlsnet.ru/mnn_index_id_2804.htm | https://www.drugs.com/international/levodropropizine.html | https://www.ncbi.nlm.nih.gov/pubmed/26097707 | https://www.ncbi.nlm.nih.gov/pubmed/1611233
Levodropropizine is a non-opioid cough suppressant whose peripheral antitussive action may result from its modulation of sensory neuropeptide levels within the respiratory tract. Levodropropizine exerts its antitussive effect through an inhibitory action at the level of the airway sensory nerves and it has been shown to be able to inhibit in vitro the release of neuropeptides from C-fibers. Levodropropizine is an effective antitussive drug both in children and adults, showing statistically significant better outcomes vs. central antitussive drugs in terms of overall efficacy in reducing cough intensity, frequency and night awakenings. After oral administration, Levodropropizine is absorbed from the intestine, undergoes the first-pass metabolism and reaches peak plasma concentrations approximately 90 to 120 minutes after administration. Levocloperastine undergoes extensive biotransformation and is widely distributed throughout the body. Levocloperastine can cross the placental barrier (although to a moderate extent), but there is no evidence of accumulation, and is eliminated in the form of metabolites mainly in the faeces and to a lesser degree in the urine. The pharmacological effects of Levodropropizine were confirmed in large-scale clinical trials, non-blind or comparative. In the 10 trials reported here, oral Levodropropizine caused a rapid remission (after the first day of treatment) in cough symptoms (intensity and frequency of a daytime cough and disturbed night-time sleep) in all groups of patients. In children, the improved sleep quality resulted in a significant reduction in irritability and an overall improvement in their quality of life. Importantly, in adult patients with COPD, Levodropropizine reduced the frequency and intensity of dry unproductive cough without adversely influencing the beneficial effects of underlying treatment. In clinical trials, Levodropropizine was generally well tolerated, with mild and transient nausea the only adverse event reported. There was no evidence of central adverse events with Levodropropizine.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: GO:0099539 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1611233 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Levotuss Approved UseIndication: Dry non-productive cough with pharyngitis, laryngitis, acute tracheitis and tracheobronchitis, influenza, bronchopneumonia, chronic obstructive bronchitis, bronchial asthma, emphysema, lung tumor, allergic and infectious-inflammatory diseases of the respiratory tract (symptomatic treatment). |
PubMed
Title | Date | PubMed |
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Important drugs for cough in advanced cancer. | 2001 Nov |
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Levodropropizine does not affect P0.1 and breathing pattern in healthy volunteers and patients with chronic respiratory impairment. | 2003 |
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Levocloperastine in the treatment of chronic nonproductive cough: comparative efficacy versus standard antitussive agents. | 2004 |
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[Determination of levodropropizine and its pharmacokinetics in human plasma using LC/MS/MS]. | 2004 Dec |
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Rapid and sensitive liquid chromatography-tandem mass spectrometry method for the quantitation of levodropropizine in human plasma. | 2005 May 5 |
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HPLC determination and steady-state bioavailability study of levodropropizine sustained-release tablets in dogs. | 2006 Jun |
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Currently available cough suppressants for chronic cough. | 2008 |
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Sensitive spectrophotometric method for quantitation of guaifenesin and dropropizine in their dosage forms. | 2010 |
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An anaphylactic reaction caused by levodropropizine. | 2010 Mar |
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Clinical expert guidelines for the management of cough in lung cancer: report of a UK task group on cough. | 2010 Oct 6 |
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Interventions for cough in cancer. | 2010 Sep 8 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.rlsnet.ru/tn_index_id_14657.htm
10 ml of syrup (60mg Levodropropizine) or 20 drops, preferably diluted in half a glass of water, 1-3 times a day at intervals of not less than 6 hours; Children from 2 to 12 years of age are given 1 mg / kg (syrup) 1-3 times a day until cessation ceases, but not more than a week
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3081798
In the experiments the quasidiploid V79 Chinese hamster cells were used. Cells attached on petri dishes were exposed to Dropropizine (8000 ug/ml) Then the drug solutions were removed by aspiration, the cells were rinsed with PBS buffer and the numbers of cells in each treated group as well as in control groups were counted at 24-h intervals. Cytostatic effects lasting 24 h were observed.
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QR05DB27
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R05DB27
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NCI_THESAURUS |
C66917
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LEVODROPROPIZINE
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ACTIVE MOIETY