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Sleepdex - Resources for Better Sleep

Medicines for Insomnia

Anxiolytic and Sedative-Hypnotic Drugs

Sedatives and hypnotic drugs are prescribed to produce drowsiness and to promote sleep

  • Sedatives -- drugs that decrease activity and moderate excitement
  • Hypnotics -- drugs produce drowsiness and facilitate the onset and maintenance of sleep, from which one is easily aroused

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. If insomnia cannot be treated with non-drug therapies, the use of sleep medications may be helpful. These medicines are almost always prescribed only for short times. They tend to disrupt natural sleep patterns. Prolonged use of sleeping pills can result in tolerance and physical dependence.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).

Non-Benzodiazepines

These are the go-to medicines that most doctors prescribe for insomnia. They are sometimes referred to as "Z-drugs".

zolpidem tartrate (Ambien) classed as an imidazopyridine compound
zaleplon (Sonata) classed as a pyrazolopyrimidine compound
eszopiclone (Lunesta) classed as a cyclopyrrolone compound

 

Benzodiazepines

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.

diazepam (Valium)
temazepam (Restoril)
triazolam (Halcion)
clonazepam (Klonopin)
flurazepam (Dalmane)
clonazepam (Klonopin)
quazepam (Doral)
triazolam (Halcion)
lorazepam (Ativan)
alprazolam (Xanax)
estazolam (ProSom)
flunitrazepam (Rohypnol)
temazepam (Restoril)
oxazepam (Serax)
prazepam (Centrax)

Although doctors sometimes prescribe benzodiazepines for insomnia, newer drugs are usually preferred. Benzodiazepines are still widely used for anxiety.

Antipsychotics

Low doses of antipsychotic drugs are sometimes used for insomnia.

Orexin Antagonists

This is a new class of drugs under development.

Tricyclic antidepressants

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.)

doxepin (Sinequan)
amitriptyline (Elavil)
nortriptyline (Pamelor)

Chloral derivatives

chloral hydrate

Chloral hydrate is rarely used for sleep disorders any more.

Antihistamines

Over-the-counter sleeping pills use antihistamines as their active ingredient. Some widely used ones include:

diphenhydramine (Benadryl)
hydroxyzine (Vistaril, Atarax)
doxylamine
niaprazine
promethazine
triprolidine
pyribenzamine

Newly Developed Medicines

See our page on emerging drugs for insomnia.

Chronobiotics

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.

Ramelteon is a melatonin agonist that is currently marketed for insomnia. Tasimelteon is a melatonin agonist now under development and the manufacturer expects it to hit the market in 2012.

Ideally, a chronobiotic would be used to get people “back on track”-
especially when they have jet lag or shift-work sleep disorder. An abstract on chronobiotics. And another one.

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.

Do sleeping pills work?

Alcohol and Sleep

Sodium oxybate (gamma hydroxybutyric acid)

Concerns about long-term use of insomnia medicine

Sleep Aids for Seniors

 

 

 

 

 

Antihistimines

Benzodiazepines

The Z-Drugs

 

Other Drugs

Melatonin Agonists

Orexin Antagonists

Most Prescribed Sleeping Pills

Barbituates

Related

Taking Sleeping Pills

Z-Drug Zombies

Multiple Sleep Latency Test

Prescription Drugs and Their Effect on Sleep

Non-Drug Approaches

 

"Sleep hath seized me wholly"

(William Shakespeare – Cymebline)

 

 sleeper with head in hand