Medicines for Insomnia
Anxiolytic and Sedative-Hypnotic Drugs
Sedatives and hypnotic drugs are prescribed to produce drowsiness and to promote sleep
Drugs that are anxiolytic and sedative-hypnotic alter the continuum of excitability in the brain. At low doses, many patients have a greater sense of well-being and decreased arousal. At higher doses, people become sleepy and their cognitive physical performance deteriorates.
An anxiolytic is any drug or therapy used in the treatment
of anxiety disorders that works on the central nervous system to relieve
the symptoms of anxiety. Anxiolytics are not "minor tranquilizers".
Insomnia as a Medical Problem
Insomnia is one of the most common complaints people present to their doctors, but from a medical standpoint, it can be difficult to address. When sleep disturbances are not resolved with other measures, the use of sleep medications may be helpful. These medicines are almost always prescribed only for short times. Prolonged use of sleep medications for persistent insomnia can impair natural sleep patterns (i.e., rapid eye movement deprivation) and alter physiologic functions. Prolonged use (more than 1 to 2 weeks) of these medications can result in tolerance, psychological and physical dependence, drug intoxication, and drug hangover.There may be an increased risk of cancer from long-term use, although this connection is not clear. More tips on taking sleeping aids.
Insomnia is a problem for many people, and there are many different ways to attack it, such as through exercise and changing the patient’s sleeping patterns. Another option for management is via pharmaceuticals, both over-the-counter (OTC) and prescription. OTC medications tend to be used for infrequent and/or mild cases of insomnia, whereas prescription drugs are usually used for chronic and moderate-to-severe situations. Physicians have the freedom to prescribe all sorts of different medicinces, including those that are "off-label" for sleep disorders.
Prescription drugs for insomnia sell at the rate of $1.85 billion per year in the United States (2011 numbers per Wall St. Journal.). Although there are branded drugs such as Lunesta and Ambien, which tend to be expensive, most patients are given lower priced generic medications.
The action of sleep medication in the brain
The challenge for the drug developers is always to maximize sleep, minimize side effects and residual effects that produce sleep inertia, and improve (or at least not degrade) sleep architecture. Researchers today are excited about drugs that address different neurotransmitter systems – not just the old benzodiazepine system. The hope is that the new drugs will have less addiction potential and improve sleep quality by increasing the amount of time the person spends in deep sleep every night.
Almost all sleep aids exert effects on neurotransmitters, either by affecting the breakdown, reuptake, or binding to a cell receptor (antagonists). Drugs can also mimic neurotrasmitters (agonists). Antihistimines block the effects of a neurotransmitter on the postsynaptic receptor. Benzodiazepines are agonists and stimulate the postsynaptic receptor.
The effects can be complex, but the neurotransmitters either make the postsynaptic neuron more likes to fire (excitatory) or less likely to fire (inhibitory).
These are the go-to medicines that most doctors prescribe for insomnia. They are sometimes referred to as "Z-drugs".
Benzodiazepines were developed as anti-anxiety drugs. The main beznodiazepine in the 60’s was Valium, which was the top selling prescription drug in the country for several years. These medicines enhance the activity of the inhibitory neurotransmitter GABA. Because they effectively permit people who take them to get to sleep, they found use as sleeping pills. Benzodiazepines with short half-lives were developed to produce sleeping pills that did not leave the user with a sedated hang-over the next morning.
Although doctors sometimes prescribe benzodiazepines for insomnia, newer drugs are usually preferred. Benzodiazepines are still widely used for anxiety.
Low doses of antipsychotic drugs are sometimes used for insomnia.
This is a new class of drugs under development.
At one time, tricyclic antidepressants were the go-to prescription for doctors when patients complained about insomnia. The off-label, first-line use of antidepressants for treating insomnia in the absence of depression is now considered debatable. (Nonbenzondiazepone drugs are now the most common.)
Chloral hydrate is rarely used for sleep disorders any more.
Over-the-counter sleeping pills use antihistamines as their active ingredient. Some widely used ones include:
Newly Developed Medicines
Chronobiotics is a catch-all term that has been around for a while for drugs that affect the circadian pacemaker. Melatonin is the most well-known chronobiotic, but a bunch of other drugs – approved and experimental – could be classified in this category. These drugs include other indoleamines, cholinergic agents, peptides, and benzodiazepines.
Related: Concerns about overprescription
Sleep experts recognize that both primary and secondary sleep disorders
often result in people using
prescription and non-prescription drug use that may as a side
effect exacerbate disturbances in sleep.
Morphine and similar opioid drugs cause selective decreases in rapid-eye-movement (REM) sleep through actions on brainstem cholinergic neurons, neurons known to participate in the initiation of this sleep state.
Mysteries remain, but brain scients are making progress into understading the, neurotransmitters and neuromodulatory substances involved in falling and staying asleep. We're also learning more about the biochemical underpinnings involved in the circadian rhythm. Already we have seen the arrival of melatonin agonists on the market and the advancement of orexin antagonists through the development process It is an exciting time for insomnia medication.
"Sleep hath seized me wholly"
(William Shakespeare – Cymebline)