Medications used in the treatment of insomnia include nonbenzodiazepine receptor agonists, benzodiazepine receptor agonists, the selective melatonin receptor agonist ramelteon, and sedating antidepressants.
All can be considered first-line agents for insomnia; agent choice is largely dictated by past trials, cost, side-effect profile, drug interactions, and patient preference.
Short-acting (eg, triazolam) and intermediate-acting (eg, estazolam, temazepam) benzodiazepine receptor agonists are useful for sleep-onset insomnia.
These agents have been the hypnotics of choice for many years because of their relative safety compared with the barbiturates, as well as their low cost.
The older sedative-hypnotics that have a prolonged half-life increase the risk for next-day sedation and daytime psychomotor impairment and pose an increased risk for abuse and dependence.
Other complications of benzodiazepine use include tolerance, withdrawal, abuse, and rebound insomnia.
Sedative-hypnotics include nonbenzodiazepine receptor agonists (zaleplon, zolpidem, eszopiclone); short-acting benzodiazepine receptor agonists (triazolam); intermediate-acting benzodiazepine receptor agonists (estazolam, temazepam); and selective melatonin agonists (ramelteon).
Both eszopiclone and sustained-release zolpidem are effective for both sleep-onset and sleep-maintenance insomnia, with a reduced abuse potential and long-term efficacy of up to 6 months as compared with nonselective benzodiazepine receptor agonists.
By binding to specific subunits of GABA Benzodiazepines are on the Beer’s List of potentially inappropriate medications for older patients.
They are not recommended in the elderly because of the risk of falls; if used, they should be given at the lowest effective dose for the shortest amount of time.
One approach is to isolate the neuronal uptake pump for serotonin by homogenizing brain regions rich in serotonin terminal fields.
The homogenization process lysises the neuronal membranes in such a way that the membrane can close back on itself to form synaptosome preparations which retain the functional integrity of the serotonin uptake pump.
For this reason, the medication trial should probably be initiated with a very low dose -- as little as 10 to 25 milligrams (mg) per day of imipramine, for example. Typically taken in one dose at bedtime, but can be divided. Use during pregnancy or breast-feeding only after approval from your physician. Headache, drowsiness, dizziness, nervousness, trouble sleeping, dry mouth, nausea, vomiting, blurred vision, altered taste, sweating, stomach upset, constipation, loss of appetite, anxiety, or yawning may occur.