Category Archives: Insomnia

Treatment of Insomnia

Several classes of medications are used in the treatment of insomnia. They include the benzodiazepines, non-benzodiazepine hypnotics, antidepressants, and over-the-counter medications. There are six benzodiazepines that are specifically marketed as hypnotics in the United States or in Canada: flurazepam, temazepam, triazolam, estazolam, quazepam, and (in Canada only) nitrazepam. Several other benzodiazepines (e.g., lorazepam, clonazepam, oxazepam),… Read More »

Current Therapies for Insomnia

Most individuals who suffer from insomnia either self-treat with nonprescription sleep aids (e.g., antihistamines, herbal remedies), use alcohol as a sedative, or take no drug therapy at all. For those who do seek professional help (approximately one-third of insomniacs), the majority receive physician-prescribed benzodiazepine or non-benzodiazepine sedative hypnotics to treat their insomnia. Such hypnotic agents… Read More »

Sedating Antidepressants

Given the high comorbidity of insomnia and depression and / or anxiety, sedating antidepressants have considerable relevance for treating insomnia. (Note: Sedating antidepressants can effectively treat both depressive and anxious symptoms.) The sleep-promoting properties of the sedating antidepressants, as well as their lack of abuse potential or propensity to induce tolerance, make these agents viable… Read More »

Benzodiazepine Hypnotics

Benzodiazepine hypnotics can be categorized into three groups based on their pharmacokinetic characteristics: short-acting, intermediate-acting, and long-acting. Short-acting benzodiazepines such as triazolam (Pfizer’s Halcion, generics) generally have elimination half-lives of 6 hours or less; intermediate-acting benzodiazepines such as temazepam (Mallinckrodf s Restoril, generics), oxazepam (Wyeth’s Serax / Serepax, Boehringer-Ingelheim’s Adumbran, generics), and lormetazepam (Wyeth’s Loramet,… Read More »

Nonbenzodiazepine Hypnotics

Non-benzodiazepine hypnotics were introduced in most markets in the early 1990s. To date, three non-benzodiazepine hypnotics have been launched for insomnia — zolpidem, zopiclone, and zaleplon (Wyeth and King Pharmaceuticals’ Sonata). Characteristics that distinguish these drugs from traditional benzodiazepines (discussed later) are their increased receptor-binding specificity, favorable pharmacokinetics, and overall broader range of safety. More… Read More »

Emerging Therapies for Insomnia

Most of the late-stage compounds in clinical development for insomnia are non-benzodiazepine gamma-aminobutyric acid -acting agents. These drugs’ developers are hoping that their new compounds, once approved, will achieve less restrictive labeling from regulatory authorities than the currently marketed benzodiazepine and non-benzodiazepine hypnotics — most of which have short-term prescribing limits and all of which… Read More »

Melatonin Agonists / Analogues

The role of melatonin in circadian biology is well described, although a clear demonstration of melatonin’s sleep-promoting activities remains to be demonstrated. To date, several companies have undertaken development of melatonin agonists and / or analogues that may offer clinical advantages over the widely available nonprescription, synthetic versions of melatonin. This section discusses two clinical… Read More »

Nonbenzodiazepine GABA-A Agonists

As mentioned, non-benzodiazepine gamma aminobutyric acid-A agonists in clinical development are very similar in terms of mechanism of action, safety, and efficacy to the currently marketed non-benzodiazepine hypnotics zolpidem, zopiclone, and zaleplon (which are sometimes referred to as the “Z” drugs). Consequently, none of these clinical-stage compounds is likely to offer major benefits in terms… Read More »

Nonprescription Pharmacotherapies: Alcohol, Over-the-Counter, and Complementary and Alternative Medicines

A large percentage of individuals with insomnia self-medicate with alcohol, over-the-counter (OTC) antihistamines, or complementary and alternative preparations. In the United States, the formulation and manufacture of OTC products are regulated by the U.S. Food and Drug Administration (FDA). Other products not requiring a prescription, such as dietary supplements, are unregulated. The National Center for… Read More »

Herbal Preparations And Dietary Supplments

Herbal products used as CAM are prepared from roots, stems, flowers, buds, or leaves of plants. These plant products can be used whole, dried, crushed, and steeped as tea; other preparations contain extracts. While some herbal preparations have shown some efficacy in improving some sleep parameters in a few studies, most studies are small and… Read More »