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Prescription Sleep Medication
| 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 |
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. An Israeli generic
company, Teva Pharmaceutical Industries, is in the midst of patent
litigation in New Jersey District Court regarding King’s patent. Teva
has received tentative approval to manufacture an AB-rated generic
version of 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 . 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.
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.
Rozerem is under patent to Takeda until March 6, 2017 and they have
exclusivity until July 22, 2010.
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 are common to all of the medications
listed in this document and are not unique not eszopiclone. More
on eszopiclone.
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"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.
Pramipexole for Restless Legs Syndrome
What are "narcotics"?
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