Merck, Sharpe And Dohme Corp

1595 Words Dec 10th, 2014 7 Pages
Belsomra® (suvorexant)
Manufacturer: Merck, Sharpe & Dohme Corp.
FDA approval date: August 13, 2014
FDA rating: New Molecular Entity (NME) Standard drug approval (S)
Many current sleep aides target gamma-aminobutyric acid (GABA) receptors in the brain which can cause unwanted side effects like next day time sedation, rebound insomnia and physical or psychological dependence. Belsomra is being reviewed due to the unique mechanism of action focusing on efficacy and safety profile.
Pharmacology and Indications
Suvorexant is FDA indicated for insomnia (falling asleep and staying asleep) on as needed basis. Suvorexant alters the neurotransmitters in the brain involved in the sleep cycle.1When orexin receptors, which are involved in regulation of sleep/wake cycle are blocked, there is a reduction in the excitation of the arousal system.2

Table 1: Pharmacokinetics3, 4
Drug Dosage Range Absorption Distribution Metabolism Elimination Onset and Half Life suvorexant 5mg-20 mg decreased with higher doses Vd~49 L
Protein bound>99% hepatic urine (23%) feces (66%) Onset 30 mins , t ½ 12 hr. diphenhydramine 50 mg – 100 mg 42 % to 62% bioavailable Vd~ adult
17 L/kg
Elderly 14 L/kg
Protein bound 98.5% renal Urine (as metabolites and unchanged) Onset 1-3 hrs. t ½ 2-8 hrs. temazepam 7.5 mg – 30 mg well absorbed Vd 1.4 L/kg
Protein bound 96% hepatic urine(~80% to 90%) inactive metabolite Onset 30 mins, t ½ 3.5-18 hrs. eszopiclone 1-3 mg rapid-high fat meal delays absorption Protein…

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