| 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
| Molecular Formula | C13H20N2O2 |
| Molecular Weight | 236.3101 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
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
Doses
PubMed
Patents
Sample Use Guides
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 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.
