Benzodiazepines for treating Insomnia
Posted 04-24-2008 at 08:37 PM by ladypam
Some people have a problem of staying awake so take stimulants. But there are some people who just cannot fall asleep. And so they take sleeping pills. Having a good sleep, especially at night is essential to having a healthy body and lifestyle. Getting a restful sleep, even for just a few hours can energize the body to perform their daily activities with much gusto and therefore creating a work output that leaves no room for mistake. However insomnia affects more than 40% of the entire population, occurring mainly in older people, in people undergoing a lot of stress, and in people who has done too much travel that may affect their circadian rhythm. But how does one with the problem of insomnia fall asleep quickly? The answer is Benzodiazepines.
How does it work?
Benzodiazepines are known to have several effects on the body and causing hypnosis and sedation is one of them. This substance is known to enhance the action of gamma-aminobutyric acid or GABA which is known to be a neurotransmitter that inhibits or suppresses the action of other substances. Benzodiazepines attach itself to a GABA receptor and make it more attractive for GABA to bind. Because of this, there is an increase in the uptake of GABA in the receptors, leading to an inhibition of excitatory feelings, thus giving a feeling of calmness and quiet on the brain. This sedative effect is what causes the person suffering from insomnia to sleep.
Common Benzodiazepines for Insomnia
There are several Benzodiazepines that are found to have a sedative and hypnotic effect on patients, therefore having the ability to treat their insomnia. These are the following:
Flurazepam is the most common benzodiazepine used to treat insomnia. Even at a low and short dose of 30 mg, improvement is already seen in the quality of sleep of the patients, as well as the ability to fall asleep. Its full capacity is usually felt when taken during the 2nd and 3rd evenings. This medication can be taken for at least two weeks consecutively to feel its effectiveness over other benzodiazepines. It does not produce a tolerance over this long period of time. Rebound insomnia is not seen during the withdrawal of flurazepam, except for delayed and mild disturbances to sleep. Adverse effects with flurazepam are low although the incidence of sedation during the day is higher. A common flurazepam in the market is Dalmane.
Quazepam (Doral) is one of the newer benzodiazepines created, which is quite similar to flurazepam since it produces the same metabolite, therefore basically having the same effects as flurazepam.
Temazepam or commonly known as Euhypnos, Restoril, and Normison, is found to have moderate effects in the production of sleep. It produces rebound insomnia as a withdrawal symptom, with a delayed and moderate intensity.
Another familiar benzodiazepine prescribed for the treatment of insomnia is triazolam. It is more known to be Halcion. This benzodiazepine triazolam is the medication frequently given for hypnosis to occur. It is found to be absorbed easily by the body through the bloodstream. Even after a sublingual treatment, it still acts fast. Triazolam is also seen to inactivate without any difficulty, with a low incidence of having daytime sedation. Triazolam is often given to treat jetlag since it has the ability to induce sleep and maintain it. Just a small amount of this medication, around .125 mg to .25 mg can already cause an effect to occur. But there is no documented evidence yet to prove its effectiveness when taken during the evenings for a longer period of time.
Several disadvantages are associated with Triazolam, which has made it quite unpopular to use, especially for those who already have other ailments and underlying health problems. It can cause impairment in memory. It can also produce anterograde amnesia. Tolerance can be developed to triazolam, with an increase in anxiety during the day time. It is also known to cause a strong rebound insomnia while under medication. It also has symptoms that are found to be probably due to withdrawal such as hallucinations, severe anxiety, delirium and confusion.
These benzodiazepine medications earlier mentioned are the most popular and well known of all benzodiazepines. But there are still several benzodiazepine medications in the market that are directed on the treatment of insomnia, each with their own brand name and structure. Examples of this benzodiazepines are Nitrazepam, with brand name Mogadon; Loprozolam with brand name Dormonoct; Lormetazepam, with brand name Noctamid; Estrazolam, with brand name Prosom; Flunitrazepam with brand name Rohypnol.
Non-benzodiazepines for Insomnia
There are also a few medications that are also indicated for the treatment of insomnia, with the same action and effects of benzodiazepines, and yet, are not considered to be benzodiazepines. These include Zopiclone, Zolpidem, and Zelplon. Zopiclone, more commonly known with the brand names Zimovane and Imovane , is actually a derivative of cyclopyrrolone, a hypnotic agent. Pharmacologically, it has the same effect as with benzodiazepines and even has as a withdrawal symptom, the possibility of a rebound amnesia. Zolpidem is more known as Ambien, Myslee, Nimadorm, Hypnogen, Stilnoct, Zolfresh, Zolt, and Sanval while zaleplon is Sonata.
Flumazenil is known to be a benzodiazepine receptor antagonist, often used to treat an overdose on benzodiazepines. It is also effective in reversing the effect of Zopiclone, Zelplon, and Zolpiderm.
Insomnia is not only a problem of not being able to sleep but produces more problems due to the lack of sleep of the person. Less sleep means a lowered response time to stress as well as lowered resistance and immunity. Therefore, treatment of benzodiazepines is not actually limited to the inability to fall asleep but on other health problems that may arise from the lack of sleep. Benzodiazepines is the not the ultimate in treating sleep disorders. It is just the most popularly prescribed by doctors. But, just in case allergic reactions have been found with benzodiazepines, there are other alternatives such as barbiturates and non-benzodiazepine, non-barbiturate medications. With the multitude of choices, it is often hard to choose what is right for you. The right one to use is what gives you the best effect, what the body can tolerate, and what can effectively treat insomnia.
How does it work?
Benzodiazepines are known to have several effects on the body and causing hypnosis and sedation is one of them. This substance is known to enhance the action of gamma-aminobutyric acid or GABA which is known to be a neurotransmitter that inhibits or suppresses the action of other substances. Benzodiazepines attach itself to a GABA receptor and make it more attractive for GABA to bind. Because of this, there is an increase in the uptake of GABA in the receptors, leading to an inhibition of excitatory feelings, thus giving a feeling of calmness and quiet on the brain. This sedative effect is what causes the person suffering from insomnia to sleep.
Common Benzodiazepines for Insomnia
There are several Benzodiazepines that are found to have a sedative and hypnotic effect on patients, therefore having the ability to treat their insomnia. These are the following:
Flurazepam is the most common benzodiazepine used to treat insomnia. Even at a low and short dose of 30 mg, improvement is already seen in the quality of sleep of the patients, as well as the ability to fall asleep. Its full capacity is usually felt when taken during the 2nd and 3rd evenings. This medication can be taken for at least two weeks consecutively to feel its effectiveness over other benzodiazepines. It does not produce a tolerance over this long period of time. Rebound insomnia is not seen during the withdrawal of flurazepam, except for delayed and mild disturbances to sleep. Adverse effects with flurazepam are low although the incidence of sedation during the day is higher. A common flurazepam in the market is Dalmane.
Quazepam (Doral) is one of the newer benzodiazepines created, which is quite similar to flurazepam since it produces the same metabolite, therefore basically having the same effects as flurazepam.
Temazepam or commonly known as Euhypnos, Restoril, and Normison, is found to have moderate effects in the production of sleep. It produces rebound insomnia as a withdrawal symptom, with a delayed and moderate intensity.
Another familiar benzodiazepine prescribed for the treatment of insomnia is triazolam. It is more known to be Halcion. This benzodiazepine triazolam is the medication frequently given for hypnosis to occur. It is found to be absorbed easily by the body through the bloodstream. Even after a sublingual treatment, it still acts fast. Triazolam is also seen to inactivate without any difficulty, with a low incidence of having daytime sedation. Triazolam is often given to treat jetlag since it has the ability to induce sleep and maintain it. Just a small amount of this medication, around .125 mg to .25 mg can already cause an effect to occur. But there is no documented evidence yet to prove its effectiveness when taken during the evenings for a longer period of time.
Several disadvantages are associated with Triazolam, which has made it quite unpopular to use, especially for those who already have other ailments and underlying health problems. It can cause impairment in memory. It can also produce anterograde amnesia. Tolerance can be developed to triazolam, with an increase in anxiety during the day time. It is also known to cause a strong rebound insomnia while under medication. It also has symptoms that are found to be probably due to withdrawal such as hallucinations, severe anxiety, delirium and confusion.
These benzodiazepine medications earlier mentioned are the most popular and well known of all benzodiazepines. But there are still several benzodiazepine medications in the market that are directed on the treatment of insomnia, each with their own brand name and structure. Examples of this benzodiazepines are Nitrazepam, with brand name Mogadon; Loprozolam with brand name Dormonoct; Lormetazepam, with brand name Noctamid; Estrazolam, with brand name Prosom; Flunitrazepam with brand name Rohypnol.
Non-benzodiazepines for Insomnia
There are also a few medications that are also indicated for the treatment of insomnia, with the same action and effects of benzodiazepines, and yet, are not considered to be benzodiazepines. These include Zopiclone, Zolpidem, and Zelplon. Zopiclone, more commonly known with the brand names Zimovane and Imovane , is actually a derivative of cyclopyrrolone, a hypnotic agent. Pharmacologically, it has the same effect as with benzodiazepines and even has as a withdrawal symptom, the possibility of a rebound amnesia. Zolpidem is more known as Ambien, Myslee, Nimadorm, Hypnogen, Stilnoct, Zolfresh, Zolt, and Sanval while zaleplon is Sonata.
Flumazenil is known to be a benzodiazepine receptor antagonist, often used to treat an overdose on benzodiazepines. It is also effective in reversing the effect of Zopiclone, Zelplon, and Zolpiderm.
Insomnia is not only a problem of not being able to sleep but produces more problems due to the lack of sleep of the person. Less sleep means a lowered response time to stress as well as lowered resistance and immunity. Therefore, treatment of benzodiazepines is not actually limited to the inability to fall asleep but on other health problems that may arise from the lack of sleep. Benzodiazepines is the not the ultimate in treating sleep disorders. It is just the most popularly prescribed by doctors. But, just in case allergic reactions have been found with benzodiazepines, there are other alternatives such as barbiturates and non-benzodiazepine, non-barbiturate medications. With the multitude of choices, it is often hard to choose what is right for you. The right one to use is what gives you the best effect, what the body can tolerate, and what can effectively treat insomnia.
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