This prolonged effect in the elderly has been associated with increased auto accidents and falls with hip fractures. This characteristic results in an extraordinarily long active half-life, which can approach 11 days. Flurazepam, like diazepam and clorazepate, has active breakdown products. Rapid onset of action is characteristic of flurazepam and triazolam, indicating that both of these agents have excellent sleep-inducing effects. The many drugs in this class are best viewed therapeutically based on their pharmacodynamics ( Table 1). These drugs act at γ-aminobutyric acid (GABA) neuroreceptors and have far less overdose danger and abuse potential than previous medications used for sleep. In the 1970s benzodiazepines became available for the treatment of insomnia. These medications and similar barbiturate-like medications (methaqualone, glutethimide, ethchlorovynol, methyprylon) can still be prescribed, but should be used sparingly because of their potential for abuse and overdose. Marilyn Monroe, Elvis Presley, and Jim Morrison, among others, were celebrities who died during this era from overdoses of sleeping pills. Unfortunately, these medications can be drugs of abuse and have a significant danger of overdose. In the years leading up to the 1960s, barbiturates were commonly utilized for their sedative effects. Unfortunately, the median lethal dose (LD 50) for chloral hydrate is quite close to the therapeutic dose, and murders rather than robberies were often the result. Chloral hydrate was the original “Mickey Finn” slipped into the drinks of unsuspecting marks for the purposes of criminal activity. Historically, sedative/hypnotics have been some of the most commonly prescribed drugs. An understanding of the disorders of sleep and the effects of medications is required for the appropriate use of medications affecting sleep.ĭiagnoses Resulting in Chronic Insomnia a For example, restless legs syndrome and periodic limb movement disorder may be treated with dopamine agonists. Conversely, medications may be used therapeutically for specific sleep disorders. Many medications affect sleep stages and can thus cause sleep disorders or exacerbate the effect of chronic illnesses on sleep. Chronic medical illnesses can become symptomatic during specific sleep stages. Parasomnias include disorders of arousal and of REM sleep. Medications, including amphetamines, may be used to induce daytime alertness. Excessive daytime sleepiness is often associated with obstructive sleep apnea or depression. An understanding of the electrophysiologic and neurochemical correlates of the stages of sleep is useful in defining and understanding sleep disorders. Nonpharmacologic behavioral methods may also have therapeutic benefit. Other agents for insomnia include sedating antidepressants and over-the-counter sleep products (sedating antihistamines). Two newer benzodiazepine-like agents, zolpidem and zaleplon, have fewer side effects, yet good efficacy. Benzodiazepines are frequently used to treat insomnia however, there may be a withdrawal syndrome with rapid eye movement (REM) rebound. Chronic insomnia affects 15% of the population. Transient insomnia is extremely common, afflicting up to 80% of the population. Sleep disorders can be divided into those producing insomnia, those causing daytime sleepiness, and those disrupting sleep.
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