Suvorexant
description Pharmacokinetics Mechanism of action side effects Dosage- Product Name
- Suvorexant
- CAS No.
- 1030377-33-3
- Chemical Name
- Suvorexant
- Synonyms
- Suvorexan;(R)-(4-(5-chlorobenzo[d]oxazol-2-yl)-7-Methyl-1,4-diazepan-1-yl)(5-Methyl-2-(2H-1,2,3-triazol-2-yl)phenyl)Methanone;5-Chloro-2-[(5R)-5-methyl-4-[5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoyl]-1,4-diazepan-1-yl]-1,3-benzoxazole Suvorexant (MK-4305);MK 4305;EOS-61934;SUVOREXABT;Suvorexant;CID24965990;MK-4305, >=98%;MK4305 MK-4305
- CBNumber
- CB62589660
- Molecular Formula
- C23H23ClN6O2
- Formula Weight
- 450.92
- MOL File
- 1030377-33-3.mol
Suvorexant Property
- Melting point:
- 153℃
- Boiling point:
- 669.8±65.0 °C(Predicted)
- Density
- 1.41
- storage temp.
- Room Temperature
- solubility
- Acetonitrile (Slightly), Chloroform (Slightly), DMSO (Slightly, Heated)
- form
- Solid
- pka
- 1.47±0.40(Predicted)
- color
- White to Pale Beige
- InChIKey
- JYTNQNCOQXFQPK-MRXNPFEDSA-N
- SMILES
- C(N1[C@H](C)CCN(C2=NC3=CC(Cl)=CC=C3O2)CC1)(C1=CC(C)=CC=C1N1N=CC=N1)=O
Safety
- DEA Controlled Substances
- CSCN: 2223
CAS SCH: IV
NARC: N
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H336May cause drowsiness or dizziness
H373May cause damage to organs through prolonged or repeated exposure
H400Very toxic to aquatic life
H410Very toxic to aquatic life with long lasting effects
- Precautionary statements
-
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P271Use only outdoors or in a well-ventilated area.
P273Avoid release to the environment.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P314Get medical advice/attention if you feel unwell.
P391Collect spillage. Hazardous to the aquatic environment
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 22911
- Product name
- Suvorexant
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $56
- Updated
- 2024/03/01
- Product number
- 22911
- Product name
- Suvorexant
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $124
- Updated
- 2024/03/01
- Product number
- 22911
- Product name
- Suvorexant
- Purity
- ≥98%
- Packaging
- 50 mg
- Price
- $689
- Updated
- 2024/03/01
- Product number
- 9002140
- Product name
- Suvorexant
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $39
- Updated
- 2022/04/27
- Product number
- 9002140
- Product name
- Suvorexant
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $86
- Updated
- 2022/04/27
Suvorexant Chemical Properties,Usage,Production
description
Suvorexant (Belsomra®) is a novel sedative hypnotic drug that is prescribed to promote sleep in patients with insomnia. It is the first of a new class of drugs classified as dual orexin receptor antagonists (DORAs) and is currently approved for the treatment of insomnia in the United States and Japan. It is a CNS depressant and blocks the binding of wake-promoting neuropeptides orexin A and orexin B to the two orexin receptors (OX1R and OX2R) thus, altering the signaling (action) of orexin in the brain and suppressing the sleep-wake drive.
Suvorexant is a central nervous system (CNS) depressant and can impair daytime wakefulness even when used as prescribed. Prescribers should monitor for somnolence and CNS depressant effects, but impairment can occur in the absence of symptoms, and may not be reliably detected by ordinary clinical exam. CNS depressant effects may persist in some patients for up to several days after discontinuing Suvorexant.
Belsomra (Suvorexant) can impair driving skills and may increase the risk of falling asleep while driving. Discontinue or decrease the dose in patients who drive if daytime somnolence develops. Caution patients taking Belsomra 20 mg against next-day driving and other activities requiring full mental alertness. Caution patients taking lower doses of Belsomra as well, because there is individual variation in sensitivity to Belsomra.
Pharmacokinetics
In fasting conditions, the median time to maximum plasma concentration of suvorexant is 2 h. For suvorexant 10 mg, the mean absolute bioavailability is 82 %. Administration of suvorexant with a high-fat meal had no clinically significant on systemic drug exposure, but delayed tmax by 1.5 h. Steady state is achieved within 3 days. The mean volume of distribution of suvorexant is 49 L. Suvorexant is extensively bound to plasma proteins, including albumin and a1-acid glycoprotein, and does not preferentially distribute into the red blood cells.
Suvorexant is primarily metabolized by CYP3A, with a minor contribution by CYP2C19. The main circulating compounds are the unchanged drug and a hydroxyl metabolite, which is not expected to be pharmacologically active. Suvorexant is primarily eliminated in the faeces.
Mechanism of action
Suvorexant is a dual antagonist of orexin receptors OX1R and OX2R. It exerts its pharmacological effect by inhibiting binding of neuropeptides orexin A and B, also known as hypocretin 1 and 2, that are produced by neurons in the lateral hypothalamus. These neurons control the wake-promoting centers of the brain and are active during wakefulness, especially during motor activities, and stop firing during sleep. By inhibiting the reinforcement of arousal systems, suvorexant use causes a decrease in arousal and wakefulness, rather than having a direct sleep-promoting effect.
www.drugbank.ca/drugs/DB09034
side effects
Suvorexant (BELSOMRA) has possible side effects. Before you begin treatment, it’s important to know what these side effects are and to discuss the risks and benefits of taking BELSOMRA with your doctor.
Below is a list of the most commonly reported adverse events that occurred in 3-month clinical trials:
placebo (n=767) BELSOMRA 15 mg or 20 mg (n=493)
- Diarrhea (placebo 1%, BELSOMRA 2%)
- Dry mouth (placebo 1%, BELSOMRA 2%)
- Upper respiratory tract infection (placebo 1%, BELSOMRA 2%)
- Headache (placebo 6%, BELSOMRA 7%)
- Next-day drowsiness (placebo 3%, BELSOMRA 7%)
- Dizziness (placebo 2%, BELSOMRA 3%)
- Abnormal dreams (placebo 1%, BELSOMRA 2%)
- Cough (placebo 1%, BELSOMRA 2%)
Side effects that you should report to your doctor or health care professional as soon as possible:
- allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
- confusion
- depressed mood
- feeling faint or lightheaded, falls
- hallucinations
- inability to move or speak for up to several minutes while you are going to sleep or waking up
- memory loss
- periods of leg weakness lasting from seconds to a few minutes
- problems with balance, speaking, walking
- restlessness, excitability, or feelings of agitation
- unusual activities while asleep like driving, eating, making phone calls
Side effects that usually do not require medical attention (Report these to your doctor or health care professional if they continue or are bothersome.):
- abnormal dreams
- daytime drowsiness
- diarrhea
- dizziness
- headache
Dosage
The recommended dosage is 10 mg, to be taken orally no more than once per night, within 30 min of going to bed and with at least 7 h remaining until the planned awaken time. If this dosage is well tolerated but not effective, the dosage can be increased up to a maximum of 20 mg once daily; the lowest effective dosage should be used. Patients taking concomitant moderate cytochrome P450 (CYP) 3A4 inhibitors should receive a reduced dose of 5 mg.
Description
Suvorexant, a dual orexin receptor antagonist marketed under the trade name Belsomra®, discovered and developed by Merck for the treatment of insomnia, was approved by the US FDA in August 2014 and became available in Japan in November of the same year. The drug’s mechanism of action operates through the competitive blockade of wake-promoting neuropeptides orexin A and orexin B toward receptors orexin receptor type 1 and orexin receptor type 2, which are believed to modulate sleep-wake cycles.
Uses
Suvorexant (MK-4305) is a dual (non-selective) orexin receptor antagonist in development by Merck & Co. for the treatment of insomnia. It works by turning off wakefulness rather than by inducing sleep. Users of higher doses had an increased rate of suicidal ideation.
Definition
ChEBI: Suvorexant is an aromatic amide obtained by formal condensation of the carboxy group of 5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid with the secondary amino group of 5-chloro-2-[(5R)-5-methyl-1,4-diazepan-1-yl]-1,3-benzoxazole. An orexin receptor antagonist used for the management of insomnia. It has a role as a central nervous system depressant and an orexin receptor antagonist. It is a member of 1,3-benzoxazoles, a member of triazoles, a diazepine, an aromatic amide and an organochlorine compound.
Biological Activity
Suvorexant is a dual orexin receptor (OXR) antagonist that blocks both OX1R and OX2R (Kis = 1.2 and 0.60 nM, respectively). It reduces locomotor activity and promotes sleep by inhibiting the binding of orexin A and B. In rats, suvorexant decreases self-administration of, and conditioned place preference for, cocaine ( | 16186 | ISO60176). It also decreases dopamine levels in the rat ventral striatum following a cocaine-induced increase. Formulations containing suvorexant are used in the treatment of insomnia. Suvorexant is regulated as a Schedule IV compound in the United States. This compound is also available as an analytical reference standard.
Synthesis
Commercially available acid 240 was first
subjected to a copper-assisted substitution reaction involving
1,2,3-triazole in DMF at elevated temperatures. Although these
conditions resulted in an excellent yield of a triazole-substituted
product, an approximate 4:1 ratio of the desired 2-arylated triazole
241 and the undesired 1-arylated triazole byproduct were recovered
from the reaction. The mixture was then treated with N,Ndimethylethylenediamine
in acid to sequester copper. Next, the
mixture of arylated triazoles was carefully subjected to sodium tbutoxide
in DMF and ethyl acetate to form the corresponding
sodium salts, and interestingly it was found that the desired
sodium salt of 241 could be isolated based on its solubility profile
under these conditions. Acidification of the desired carboxylate salt
using dilute HCl gave rise to acid 241 in 60% yield across the fourstep
sequence. Next, subjection of this acid to oxalyl chloride in
chilled DMF generated the acid chloride 242 in excellent yield. This
crude acid chloride was used immediately in the next step of the
synthetic sequence.
target
OX1 receptor
Metabolism
Suvorexant is primarily metabolized by cytochrome-P450 3A4 enzyme (CYP3A4) with a minor contribution from CYP2C19. Major circulating metabolites are suvorexant and a hydroxy-suvorexant metabolite, which is not expected to be pharmacologically active. There is potential for drug-drug interactions with drugs that inhibit or induce CYP3A4 activity.
Suvorexant Preparation Products And Raw materials
Raw materials
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View Lastest Price from Suvorexant manufacturers
- Product
- Suvorexant 1030377-33-3
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- 98% HPLC
- Supply Ability
- 100kg
- Release date
- 2023-08-14
- Product
- Suvorexant 1030377-33-3
- Price
- US $450.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 20tons
- Release date
- 2023-06-05
- Product
- suvorexant 1030377-33-3
- Price
- US $48.00-40.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 20tons
- Release date
- 2021-06-18