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Sleepdex - Resources for Better Sleep

Prescription Sleep Medication

Doctors’ choice of hypnotic drugs depends on overall patient health and other medication use and other conditions. This is one reason why these drugs are prescription only – as a society we want a doctor to make these judgments, not the patient. Good doctors take into account the nature and type of insomnia, how fast the drug will work and last, and whether the sleeplessness happens early in the night or later. The patient’s age, sleep disorders, and a prescence of pain are also factored in.

For those with chronic insomnia drug holidays are useful. Until recently, the FDA had not approved any insomnia drug for extended use. Until the introduction of eszopiclone (Lunesta) all prescription hypnotics on the market were “labeled” for under a month of use. Of course, many patients and doctors continued to use prescription sleeping pills for longer times. Eszopiclone has been shown to be non-addictive even after extended use. However, it, and other medications, may be psychologically addictive even if they are not physically addictive. Many doctors advise their patients to “taper off” insomnia medications when the insomnia has abated or after a period of time just to get off the drug.

 

Generic Name U.S. Brand Name Dosages Company Abuse Potential Patent
Zaleplon Sonata 5, 10 mg Capsules King Yes No (disputed)
Zolpidem Ambien 5, 10 mg
Tablets
Sanofi Aventis Yes Generic Available
  Ambien CR 6.25, 12.5 mg Tablets Sanofi Aventis Yes Yes
Triazolam Halcion 0.125 and 0.25 mg Tablets Pharmacia and Upjohn Yes No
Ramelteon Rozerem 8 mg Tablets Takeda No Yes
Eszopiclone Lunesta 1, 2, 3 mg Tablets Sepracor Yes Yes


(A brief history of insomnia medications.)

Zaleplon

Zaleplon is a hypnotic which is drug that has the ability to cause sleep. It is indicated for use in patients that have difficulty falling asleep and is not indented to treat those who have difficulty staying asleep or who wake too early. It is different in chemical structure from benzodiazepines but acts at the same receptors in the brain as benzodiazepines. While benzodiazepines are used primarily in the treatment of anxiety, zaleplon and similar drugs are used almost exclusively for the treatment of insomnia.

In the United States and many other countries, Zaleplon is marketed as Sonata by King Pharmaceuticals. In Canada, zaleplon was sold under the brand name Starnoc however it was taken from the market; the reasons for this discontinuation are not clear. Zaleplon is available in some countries as Hegon, Zalep, Zaplon, or Zerene. The patent on Sonata began to expire on June 6, 2008 and King Pharmaceuticals does not have exclusivity as listed in the FDA’s Orange Book. More on zaleplon.

Sonata is available in 5 mg and 10 mg dosages; however, physicians sometimes prescribe a 20 mg treatment (two 10 mg capsules). Clinical safety studies were conducted using doses as high as 60 mg. Zaleplon is indicated for short term treatment of insomnia, that is, insomnia that is corrected by seven to ten days of treatment. The FDA has approved use of zaleplon for up to 30 days. Zaleplon is known to cause CNS depression and its affects are relatively rapid. Zaleplon causes sedation and sleep within one hour of administration therefore it should only be taken before bed and never before any activity that requires alertness. Like benzodiazepines, alcohol use can potentiate the CNS depressant effects and alcohol should not be consumed while taking zaleplon. Of note, zaleplon is potentially habit forming and dependency may occur. Once the drug is discontinued, one may experience rebound insomnia simply because the medicine has been taken away. Because of its sedative and euphoric effects, zaleplon may be abused i.e. used for non-medical, illegal reasons. NIH Information on Zaleplon

Zolpidem

Zolpidem is sedative-hypnotic medicine that is used to treat short-term insomnia. Its chemical structure is different than benzodiazepines but exerts its sedative affect by acting on so-called benzodiazepine receptors in the brain. Zolpidem does not have the same disruptive effects on sleep as benzodiazepines.

Zolpidem is marketed in the United States as Ambien but is known commercially by many other names worldwide. (The Guardian reports that 5.3 million people in England alone take zolpidem.) Ambien is available as 5 mg and 10 mg tablets and the maximum and usual treatment dose is 10 mg. This medication should not be taken with alcohol as excessive CNS depression can occur. There is also a potential for dependence and abuse with zolpidem. The most common side effects were headache, sleepiness and dizziness. A less common side effect is the "zombie" effect - unusual behavior while asleep.

Ambien is sold by Sanofi Aventis although at least 13 companies manufacture and sell a generic version of the rapid-acting form of zolpidem. Sanofi Aventis has extended the commercial viability of this drug by patenting and selling a CR or Controlled Release formulation. The CR formulation combines both a rapid-acting form and a slow-release form in a layered pill. According to the manufacturers, this allows a person suffering from insomnia to achieve sleep, from the rapid-acting component, and stay asleep, from the slow-acting component. Importantly, the chemical structure of the drug is the same in both the fast and slow layers, however the slow release layer contains a proprietary mixture of inactive ingredients that delays absorption and prolongs the hypnotic effect. Ambien CR is available in 6.25 and 12.5 mg strengths. NIH Information on Zolpidem.

Triazolam

Triazolam is related in structure to benzodiazepines but is of a slightly different class than classic benzodiazepines such as Ativan and Valium. Despite this subtle structural difference, triazolam achieves its biological effect by acting at benzodiazepine receptors in various regions of brain. Triazolam is indicated for the short term treatment of insomnia and should not be used for longer than three consecutive weeks. In clinical studies, triazolam was able to decrease sleep latency (you get to sleep faster), increase the duration of sleep and decrease the number of times people with insomnia wake during the night.
Triazolam was originally branded as Halcion; however there is no longer patent protection or exclusivity on this brand. It is still manufactured and sold as Halcion by Pharmacia and Upjohn yet generic versions exist. Triazolam is available in 0.125 and 0.25 mg tablets and a single dose of either strength is usually sufficient for uncomplicated insomnia. The maximum dose per day should not exceed 0.5 mg. Caution should be taken in elderly patients and they should receive lower doses. The most common side effects were drowsiness, headache, dizziness/lightheadedness, difficulty with coordination and nausea/vomiting.

Ramelteon

Ramelteon was introduced as Rozerem by Takeda Pharmaceuticals North America. Rozerem is indicated for treatment of the type of insomnia that is interferes with sleep onset. Ramelteon is rather unique among commonly prescribed sleep aids in that it is unrelated to benzodiazepines in both its chemical structure and its mechanism of action. Rozerem binds with high affinity (strongly) to two of the three main melatonin receptors in the brain. Melatonin is a hormone that is present naturally in humans. Melatonin is also available without a prescription as an OTC sleep aid. According to Takeda, Rozerem’s affinity and selectivity for specific melatonin receptors make it a more effective sleep aid and less likely to cause side effects than non-prescription melatonin. Because it does not interact with benzodiazepine receptors, ramelteon is essentially without risk of abuse and is therefore not a controlled substance. Clinical studies have shown that ramelteon does not cause physical dependence or rebound insomnia. Ramelteon is available in 8 mg tablets though it occasionally prescribed as two 8 mg tablets to be taken 30 thirty minutes prior to the desired onset of sleep. The most common side effects are drowsiness and dizziness. More on ramelteon.

Ramelteon is under patent to Takeda until March 6, 2017.

Eszopiclone

Eszopiclone is marketed as Lunesta by Sepracor Inc. for the treatment of insomnia. Lunesta is under patent until 2012 with exclusivity until December 15, 2009. Eszopiclone is available in 1, 2 and 3 mg film-coated tablets. The precise mechanism of action of eszopiclone as a hypnotic is unknown, but it most likely interacts with benzodiazepine receptors. Because of this interaction, eszopiclone is a controlled substance and there is potential for abuse of the drug. Unlike zaleplon, zolpidem and triazolam which are only prescribed for up to three to four weeks, Lunesta has been approved by the FDA for long term use (greater than six months). Long-term trials showed that Lunesta did not cause tolerance meaning that patients did not need larger doses to obtain the same effect. Lunesta is touted as superior to competing medications since it not only initiates sleep but also prevents nighttime waking.

The most common side effects of Lunesta include an unpleasant taste or dry mouth, dizziness, headache, cold symptoms and drowsiness. Serious side effects of eszopiclone, while rare, include sleep walking/driving, abnormal thoughts, memory loss, anxiety and allergic reactions. These rare and serious side effects.

Mixing Drugs

Mixing drugs without the knowledge and OK of a doctor is unwise and can result in serious health risks.  This includes taking more than one prescription drug at a time or a prescription drug and an over-the-counter drug that does something similar.  If your doctor is not available, consult a pharmacist – a real pharmacist, not just someone who works at the drug store.

Sedatives and hypnotics prescribed for sleep problems are especially noteworthy because they reduce metabolic activity – and too much reduction results in coma or death.  Don’t be too alarmed – the risk profile of today’s prescription drugs is much better than the barbiturates given to induce sleep decades ago.  People rarely accidently overdose on sleeping pills anymore, and if you follow the label you should have no problems.  But be careful to actually follow those instructions.  Using more than one of these drugs at the same time, however, is a bad idea.  For instance, if you take Ambien or Lunesta, you don’t need to also take an over-the-counter antihistamine sleep aid.  If your prescription medication isn’t working, talk to the doctor.  Don’t increase the dose or add another pill, even if the other pill is over-the-counter.

Alcohol should be mentioned because it, too, is a depressant and tends to lower respiration.  The National Institute of Health has a special publication and website about mixing alcohol and medicines: http://pubs.niaaa.nih.gov/publications/Medicine/medicine.htm

The FDA runs a telephone hotline to report adverse reactions: Medwatch: 1–800–FDA–1088

The National Poison Control Center also runs a hotline if you think you’ve been poisoned: 1-800-222-1222.  They can also help with drug overdoses.

Disposing of old sleeping medications

Overprescription?

Pharmacokinetics of Insomnia Medication

"Enjoy the honey-heavy dew of slumber" – William Shakespeare, Julius Caesar

Benzodiazepines are prescribed to relieve anxiety. They include such well known medicines as Xanax, Valium, Lorazepam, and Triazolam (Halcion). They belong to the group of medicines called central nervous system (CNS) depressants (medicines that slow down the nervous system).

Antihistimines - The three antihistimines you will see in over-the-counter sleep medications are diphenhydramine, doxylamine, and hydroxyzine.

There are other antihistimines used for other purposes including allergies and motion sickness, although drowsiness is a common side effect of many antihistimines..

Barbituates are a class of drugs that are sometimes called "downers". They were once presrcibed for insomnia, but have generally been replaced by safer medicines.

Chart of neurotransmitters and drug actions

What are "narcotics"?

Antipsychotics for Insomnia

The effectiveness of hypnotic drugs

 

 

 

 

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