Ramelteon pill info

Ramelteon pill info - ROZEREMTM (ramelteon) Tablets...

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ROZEREM TM (ramelteon) Tablets DESCRIPTION ROZEREM™ (ramelteon) is an orally active hypnotic chemically designated as ( S )- N -[2-(1,6,7,8-tetrahydro-2 H -indeno-[5,4- b ]furan-8-yl)ethyl]propionamide and containing one chiral center. The compound is produced as the ( )-enan- tiomer, with an empirical formula of C 16 H 21 NO 2 , molecular weight of 259.34, and the following chemical structure: Ramelteon is freely soluble in organic solvents, such as methanol, ethanol, and dimethyl sulfoxide; soluble in 1-octanol and acetonitrile; and very slightly soluble in water and in aqueous buffers from pH 3 to pH 11. Each ROZEREM tablet includes the following inactive ingredients: lactose monohydrate, starch, hydroxypropyl cellulose, magnesium stearate, hypromellose, copovidone, titanium dioxide, yellow ferric oxide, polyethylene glycol 8000, and ink containing shellac and synthetic iron oxide black. CLINICAL PHARMACOLOGY Pharmacodynamics and Mechanism of Action ROZEREM (ramelteon) is a melatonin receptor agonist with both high affinity for melatonin MT 1 and MT 2 receptors and selectivity over the MT 3 receptor. Ramelteon demonstrates full agonist activity in vitro in cells expressing human MT 1 or MT 2 receptors, and high selectivity for human MT 1 and MT 2 receptors compared to the MT 3 receptor. The activity of ramelteon at the MT 1 and MT 2 receptors is believed to contribute to its sleep-promoting properties, as these receptors, acted upon by endogenous melatonin, are thought to be involved in the maintenance of the circadian rhythm underlying the normal sleep-wake cycle. Ramelteon has no appreciable affinity for the GABA receptor complex or for receptors that bind neuropeptides, cytokines, serotonin, dopamine, noradren- aline, acetylcholine, and opiates. Ramelteon also does not interfere with the activity of a number of selected enzymes in a standard panel. The major metabolite of ramelteon, M-II, is active and has approximately one tenth and one fifth the binding affinity of the parent molecule for the human MT 1 and MT 2 receptors, respectively, and is 17 – 25-fold less potent than ramelteon in functional assays. Although the potency of M-II at MT 1 and MT 2 receptors is lower than the parent drug, M-II circulates at higher concentrations than the parent producing 20 – 100-fold greater mean systemic exposure when compared to ramelteon. M-II has weak affinity for the serotonin 5-HT 2B receptor, but no appreciable affinity for other receptors or enzymes. Similar to ramelteon, M-II does not interfere with the activity of a number of endogenous enzymes. All other known metabolites of ramelteon are inactive. Pharmacokinetics The pharmacokinetic profile of ROZEREM has been evaluated in healthy subjects as well as in subjects with hepatic or renal impairment. When administered orally to humans in doses ranging from 4 to 64 mg, ramelteon undergoes rapid, high first-pass metabolism, and exhibits linear pharmacokinetics. Maximal serum concentration (C
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Ramelteon pill info - ROZEREMTM (ramelteon) Tablets...

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