| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
beta-adrenergic receptor
|
|---|---|
| ln Vivo |
Mean age and Acute Physiology and Chronic Health Evaluation II and Sequential Organ Failure Assessment scores were similar between the 2 groups. Paroxysmal atrial fibrillation/flutter (87%), paroxysmal atrial tachycardia (10%), and paroxysmal supraventricular tachycardia (3%) were observed. The initial landiolol dose administered was 6.3 ± 5.8 g/kg per minute. Rapid and substantial reduction of heart rate was observed in the landiolol group without any deterioration of hemodynamics. Landiolol significantly reduced heart rate (from 145 ± 14 bpm to 90 ± 20 bpm) compared to the control group (from 136 ± 21 bpm to 109 ± 18 bpm, P < 0.05). The conversion to sinus rhythm was observed more frequently in the landiolol group than in the control group at every point (P < 0.01 at 8 h; P < 0.05 at 1 and 24 h).
Conclusion: Landiolol safely reduced heart rate and, in part, converted to sinus rhythm in septic patients with supraventricular tachyarrhythmias.[2]
|
| Animal Protocol |
Objectives: To elucidate pharmacokinetics and pharmacodynamics of landiolol hydrochloride, newer developed ultra-short-acting beta-blocker, in patients with various cardiac tachyarrhythmias.
Background: The short duration of action and titratability of landiolol hydrochloride make it ideal for use in patients with a clinical need for beta-blockers. Methods: In a total of 31 examinations we infused the drug in 19 patients (mean age, 55 +/- 14 years). After the persistence of the tachyarrhythmias was confirmed, continuous infusion was started at rates of 0.005, 0.01, 0.02, 0.04, and 0.08 mg/kg/min for 5 minutes (for paroxysmal atrial fibrillation, paroxysmal supraventricular tachycardia, and ventricular tachycardia) or 15 minutes (for ventricular premature complex). We analyzed the pharmacokinetics of 16 examinations. A one-compartment model provided a close fit for each blood concentration-time curve. [1] Aim: To investigate whether landiolol, an ultra-short-acting β1-antagonist, can safely and effectively control heart rate in septic patients with supraventricular tachyarrhythmias. Methods: We reviewed all patients with sepsis who admitted to our intensive care unit between January 2006 and December 2011. Sixty one septic patients suffered from supraventricular tachyarrhythmias (heart rate ≥ 120 bpm for > 1 h). Among 61 patients, 39 patients were treated with landiolol (landiolol group) and 22 patients were not treated with landiolol (control group). Arterial pressure, heart rate, cardiac rhythm, pulmonary arterial pressure and cardiac output (if a pulmonary arterial catheter was inserted) were compared between the 2 groups at 1, 8 and 24 h after the initiation of tachyarrhythmias.[2] |
| ADME/Pharmacokinetics |
The maximum plasma concentrations obtained clearly showed dose dependence and revealed a very short half-life (ranging from 2.3 to 4.0 minutes). The area under the plasma concentration-time curve also increased accordingly, indicating that it was dose-dependent. In patients with paroxysmal atrial fibrillation, landiolol hydrochloride reduced the heart rate from 111 ± 20 beats/min to 90 ± 10 beats/min. In 3 out of 5 patients with paroxysmal supraventricular tachycardia and 1 patient with ventricular tachycardia, sinus rhythm was restored without any adverse reactions. No significant changes were observed in peripheral blood pressure. Conclusion: landiolol hydrochloride has a shorter elimination half-life than any other β-blocker and is safe for use in the treatment of patients with various arrhythmias. [1]
|
| Toxicity/Toxicokinetics |
164457 Canine LDLo, intravenously administered at 100 mg/kg: Behavioral effects: ataxia; Lung, pleural, or respiratory effects: dyspnea; Kidney, ureter, and bladder effects: other changes. Journal of Toxicological Science, 22(Supplement)
164457 Rat LDLo, intravenously administered at 150 mg/kg: Behavioral effects: altered sleep duration (including altered righting reflex); Behavioral effects: tremor; Lung, pleural, or respiratory effects: respiratory depression. Journal of Toxicological Science, 22(Supplement) |
| References |
|
| Additional Infomation |
Landiolol belongs to the morpholine class of drugs. Landiolol is a rapid-acting beta-blocker used to quickly control ventricular rate.
|
| Molecular Formula |
C25H39N3O8
|
|---|---|
| Molecular Weight |
509.59246
|
| Exact Mass |
509.273
|
| CAS # |
133242-30-5
|
| Related CAS # |
144481-98-1 (HCl);133242-30-5 (Free base);
|
| PubChem CID |
114905
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
727.5±60.0 °C at 760 mmHg
|
| Melting Point |
125.4ºC
|
| Flash Point |
393.8±32.9 °C
|
| Vapour Pressure |
0.0±2.5 mmHg at 25°C
|
| Index of Refraction |
1.531
|
| LogP |
0.8
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
36
|
| Complexity |
666
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CC1(C)OC(COC(CCC2C=CC(OCC(O)CNCCNC(N3CCOCC3)=O)=CC=2)=O)CO1
|
| InChi Key |
WMDSZGFJQKSLLH-RBBKRZOGSA-N
|
| InChi Code |
InChI=1S/C25H39N3O8/c1-25(2)35-18-22(36-25)17-34-23(30)8-5-19-3-6-21(7-4-19)33-16-20(29)15-26-9-10-27-24(31)28-11-13-32-14-12-28/h3-4,6-7,20,22,26,29H,5,8-18H2,1-2H3,(H,27,31)/t20-,22+/m0/s1
|
| Chemical Name |
[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl 3-[4-[(2S)-2-hydroxy-3-[2-(morpholine-4-carbonylamino)ethylamino]propoxy]phenyl]propanoate
|
| Synonyms |
Landiolol; 133242-30-5; ONO-1101; Ono 1101; [(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl 3-[4-[(2S)-2-hydroxy-3-[2-(morpholine-4-carbonylamino)ethylamino]propoxy]phenyl]propanoate;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9624 mL | 9.8118 mL | 19.6236 mL | |
| 5 mM | 0.3925 mL | 1.9624 mL | 3.9247 mL | |
| 10 mM | 0.1962 mL | 0.9812 mL | 1.9624 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Management of Rapid Heart Rate in Patients With Atrial Fibrillation/Flutter and Left Ventricular Dysfunction -Randomized Controlled Trial of Landiolol vs. Diltiazem-
CTID: UMIN000015053
Phase: Status: Complete: follow-up complete
Date: 2014-09-15
Products are for research use only; We do not sell to patients
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