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PRESCRIPTION SLEEP AIDS
OVERVIEW

Prescription Sleep Aids
Basics:

Prescription sleep aids are controlled substances which must be taken under the supervision of a physician, and usually for limited periods of time. This class of drugs carries certain risks as far as addiction, impaired task performance, overdosing, etc. Driving may constitute a risk until the organism adjusts to the medication. Similarly, the performance of any task requiring a high degree of concentration or precision may be impaired. Adverse effects may be exacerbated in older people, leading to confusion, loss of memory, excessive daytime drowsiness, and occasionally depressed mood.

Based on their chemical structure, prescription sleep medications can be classified into 2 broad categories: Benzodiazepines and Non-Benzodiazepines.

Among the benzodiazepine group, the most notorious agent is probably Valium, which is quite likely the most commonly prescribed sleep aid in the US. Multiple other benzodiazepine agents are available, the main differences being the time of onset, duration of action, and side-effect profile.

Non-benzodiazepines are a heterogeneous chemical group, generally considered to be less addictive than the benzodiazepine group. As we shall see below, certain agents in this group are even approved by the FDA for long-term use. This being said, please keep in mind that these drugs pose risks similar to benzodiazepines with regards to impaired concentration and task-performance.

Below is an overview of the most commonly used prescription sleep aids, covering the quintessential facts pertaining to each individual agent (onset and duration of action, dosage, side effects and adverse reactions, etc)


Prescription Sleep Aids
Overview:

  1. Benzodiazepines:
    These are tranquilizers with sedative, anti-anxiety, muscle relaxant and hypnotic action. They act in the brain on a specific groups of receptors called GABA receptors, with inhibitory effects on the central nervous system.
    Below is a list of commonly prescribed benzodiazepine drugs:
    • Ativan (Lorazepam): Ativan is a benzodiazepine agent with short to medium duration of action. It provides good anxiety relief and insomnia relief, but has relatively high addictive potential. ...Read more
    • Versed (Midazolam): Versed is a fast acting benzodiazepine agent, with relatively short duration of action. It has powerful sedative, hypnotic, anxiolytic and muscle relaxant effects. ...Read more
    • Diazepam (Valium): Valium is a fast-acting benzodiazepine agent with intermediate duration of action. It is quite likely the most commonly prescribed sleep medication in the US. ...Read more
    • Restoril (Temazepam): Restoril is a powerful sedative, hypnotic, anxiolytic and muscle relaxant agent. It is fast acting and has an intermediate duration of action. ...Read more
    • Alprazolam (Xanax, Niravam): Alprazolam is a short acting benzodiazepine agent, used mainly for the treatment of severe anxiety disorder ...Read more


  2. Non-Benzodiazepines:
    • Ambien and Ambien CR: Zolpidem Tartrate (marketed under the brand name of Ambien) is a non-benzodiazepine agent which acts on the same brain receptors as benzodiazepines (GABA receptors), inhibiting the function of the central nervous system. ...Read more
    • Lunesta (Eszopiclone): Contrary to most other prescription sleep aids, Lunesta is approved by the FDA for long-term use in the treatment of insomnia. ...Read more
    • Rozerem (Ramelteon): Rozerem is an entirely new type of sleep agent which acts on the melatonin receptors in the brain, inhibiting central nervous system activity. It is considered the safest prescription sleep agent on the market at this time (and perhaps the funniest, too... yes, it's the TV promotional featuring Abe Lincoln and the beaver!) ...Read more

Prescription Sleep Aids
Ativan (Lorazepam):

Lorazepam is a benzodiazepine agent with short to medium duration of action. It provides good anxiety relief and insomnia relief, but has relatively high addictive potential.

The effects of Lorazepam can be felt about 30 minutes after taking an oral dose, are maximal at 2 hours after the dose, and last 6-12 hours.

Lorazepam comes in tablets of 0.5 mg, 1 mg, and 2 mg. The starting dose is usually between 0.5 and 2 mg per day, which can be increased later on as needed to achieve proper symptom control (under a physician's supervision).

Please note:
  • Lorazepam can cause respiratory suppression by depressing the central nervous system respiratory drive. As such, it's contraindicated in people with severe respiratory disease, including those with severe asthma.
  • By the same token, Lorazepam can worsen sleep apnea and should not be taken by persons suffering from this condition.
  • Lorazepam can compound the effects of alcohol or other narcotic agents, resulting in profound sedation and possibly coma. It should therefore not be taken concomitantly with such agents.
  • Lorazepam can aggravate narrow-angle glaucoma, and is contraindicated in such cases.
  • Lorazepam can cause ataxia (clumsy, unsteady gait and motor incoordination)
  • Lorazepam is contraindicated during pregnancy and breast feeding, as it can cause significant harm to the fetus or infant.
  • Elderly persons may experience increased confusion and cognitive problems with the use of Lorazepam.
  • With regular use of Lorazepam, tolerance will develop – which means that larger doses are required to achieve the same effects.
  • Withdrawal symptoms (anxiety, insomnia, headache, tension, restlessness, sweating, dizziness, nausea, vomiting, hyperthermia, tremors and even seizures) may develop after as little as 1 week of Lorazepam usage.
  • Amnesia symptoms (memory lapses) are a common problem with Lorazepam. This can occur especially at the beginning of the treatment. To minimize such symptoms, the initial dose of Lorazepam should not exceed 2 mg per day

Disclaimer: The information above is correct to the best of our knowledge, but please note that it is not exhaustive and its accuracy is not guaranteed. For complete information on Lorazepam, please consult a pharmacology monograph.


Prescription Sleep Aids
Versed (Midazolam):

Midazolam is a fast acting benzodiazepine agent, with relatively short duration of action. It has powerful sedative, hypnotic, anxiolytic and muscle relaxant effects. Onset of action is 10-20 minutes after oral administration, with peak effects 1-2 hours after the dose. Effects last for 6-8 hours.

Midazolam comes in tablets of 7.5 mg. The recommended dose for insomnia is 1-2 tablets (7.5- 15 mg). Due to its rapid onset of action, Midazolam should be taken immediately prior to bedtime.

Please note:
  • Like all benzodiazepines, Midazolam can cause next-day drowsiness, concentration difficulties, memory lapses and impaired task performance. This may be more pronounced in the elderly and in those suffering from liver failure.
  • Midazolam should not be used in combination with alcohol or other narcotic drugs, since this could lead to excessive sedation and possibly coma.
  • Midazolam is contraindicated in pregnant and breast-feeding women, due to its harmful effects on the fetus or infant.
  • Midazolam is contraindicated in people suffering from severe respiratory disease (including severe asthma), severe liver disease, sleep apnea, and narrow angle glaucoma.
  • As with all benzodiazepines, regular use of Midazolam will lead to the development of tolerance – which means that larger doses are required to achieve the same effects.
  • Discontinuing Midazolam abruptly, especially after prolonged usage and/or higher doses, may result in withdrawal symptoms such as anxiety, insomnia, headache, tension, restlessness, sweating, dizziness, nausea, vomiting, hyperthermia, tremors and even seizures.
  • Medications such as Tagamet, birth control pills, certain antibiotics, etc., may interfere with the hepatic metabolism of Midazolam, resulting in increased Midazolam blood levels.

Disclaimer: The information above is correct to the best of our knowledge, but please note that it is not exhaustive and its accuracy is not guaranteed. For complete information on Midazolam, please consult a pharmacology monograph.


Prescription Sleep Aids
Valium (Diazepam):

Diazepam is a fast-acting benzodiazepine agent with intermediate duration of action. It is quite likely the most commonly prescribed sleep medication in the US. As far as its pharmacological action is concerned, Diazepam is a potent sedative-hypnotic agent, with marked anti-anxiety and muscle relaxant effects.

Onset of action is 15-30 minutes after oral administration, with peak effects at 1-2 hours after the dose. Effects last 8-12 hours.

Diazepam comes in tablets of 2 mg, 5 mg, and 10 mg. The recommended dose for insomnia is 5-10 mg for adults, and 2-5 mg for seniors (which may be increased gradually to achieve the desired effects).

Please note:
  • Like all benzodiazepines, Diazepam can cause next-day drowsiness, concentration difficulties, memory lapses and impaired task performance. This may be more pronounced in the elderly and in those suffering from liver failure.
  • Diazepam should not be used in combination with alcohol or other narcotic drugs, since this could lead to excessive sedation and possibly coma.
  • Diazepam is contraindicated in pregnant and breast-feeding women, due to its harmful effects on the fetus or infant.
  • Diazepam is contraindicated in people suffering from severe respiratory disease (including severe asthma), severe liver disease, sleep apnea, and narrow angle glaucoma.
  • As with all benzodiazepines, regular use of Diazepam will lead to the development of tolerance - which means that larger doses are required to achieve the same effects.
  • Discontinuing Diazepam abruptly, especially after prolonged usage and/or higher doses, may result in withdrawal symptoms such as anxiety, insomnia, headache, tension, restlessness, sweating, dizziness, nausea, vomiting, hyperthermia, tremors and even seizures.
  • Medications such as Tagamet, birth control pills, certain antibiotics, etc., may interfere with the hepatic metabolism of Diazepam, resulting in increased Diazepam blood levels.

Disclaimer: The information above is correct to the best of our knowledge, but please note that it is not exhaustive and its accuracy is not guaranteed. For complete information on Diazepam, please consult a pharmacology monograph.


Prescription Sleep Aids
Restoril (Temazepam):

Temazepam is a powerful sedative, hypnotic, anxiolytic and muscle relaxant agent. It is fast acting and has an intermediate duration of action. It is mainly used for the short-term treatment of severe insomnia.

Onset of action is 10-20 minutes after oral administration, with peak effects at 1.5 hours after the dose. Effects last for 8-12 hours.

Temazepam comes in tablets of 7.5 mg, 15 mg, 22.5 mg, and 30 mg. The usual dose for insomnia is 7.5-15 mg, which can be increased up to 30 mg if necessary. Due to its rapid onset of action, Temazepam should be taken immediately prior to bedtime.

Please note:
  • If taken for more than 2-4 weeks, Temazepam may cause a strong physical dependence syndrome, resulting in withdrawal symptoms upon discontinuation of treatment.
  • Temazepam may cause respiratory suppression by inhibiting the central nervous system respiratory drive. As such, it is contraindicated in people with severe respiratory disease, including those with severe asthma.
  • By the same token, Temazepam can worsen sleep apnea and should not be taken by persons suffering from this condition. Temazepam can compound the effects of alcohol or other narcotic agents, resulting in profound sedation and possibly coma. It should therefore not be taken concomitantly with such agents.
  • Temazepam can aggravate narrow-angle glaucoma, and is contraindicated in such cases.
  • Temazepam can cause ataxia (clumsy, unsteady gait and motor incoordination).
  • Temazepam is contraindicated during pregnancy and breast feeding, as it can cause significant harm to the fetus or infant.
  • Elderly persons may experience increased confusion and cognitive problems with the use of Temazepam.
  • Tolerance to Temazepam develops quickly, usually in less than 1 week – which means that larger doses are required to achieve the same effects.
  • Withdrawal symptoms (anxiety, rebound insomnia, headache, tension, restlessness, sweating, dizziness, nausea, vomiting, hyperthermia, tremors and even seizures) may develop after as little as 1 week of Temazepam usage. Therefore, Temazepam treatment shouldn't be discontinued abruptly, but rather tapered down gradually.
  • Amnesia symptoms (memory lapses) may occur with Temazepam, especially at the beginning of the treatment.

Disclaimer: The information above is correct to the best of our knowledge, but please note that it is not exhaustive and its accuracy is not guaranteed. For complete information on Temazepam, please consult a pharmacology monograph.


Prescription Sleep Aids
Alprazolam (Xanax, Niravam):

Alprazolam is a short acting benzodiazepine agent, used mainly for the treatment of severe anxiety disorder, panic disorder and anxiety symptoms associated with clinical depression. In case a person's insomnia is secondary to such disorders, Alprazolam is a good treatment option.

Onset of action is 10-20 minutes after oral administration, with peak effects at 1-2 hours after the dose. Effects last for 6-8 hours.

The initial recommended dose of Alprazolam is 0.25 mg 2-3 times a day. This may be increased gradually as needed to control symptoms, but not to exceed 2-3 mg per day. The elderly are more susceptible to develop adverse reactions to Alprazolam, and should be started on a lower initial dose (0.125 mg 2-3 times a day).

Please note:
  • Alprazolam should be used short-term, usually no longer than 2-4 weeks, since the body quickly develops tolerance to it (which means that higher doses are required to achieve the desired effects).
  • Withdrawal effects (agitation, rebound anxiety, tremors, nausea, vomiting, seizures, etc) can be very marked after stopping Alprazolam abruptly, especially if taking higher doses. Therefore, Alprazolam treatment needs to be tapered down gradually.
  • Occasionally, Alprazolam can aggravate depression and unmask suicidal ideation.
  • Alprazolam can cause drowsiness, confusion, decreased performance of daily task, concentration deficits and memory lapses. Effects may be exacerbated in the elderly, or in those suffering from liver disease.
  • Alprazolam should not be taken with alcohol, since the two have cumulative effects which may result in deep sedation and possibly coma.
  • Alprazolam is contraindicated in severe respiratory insufficiency (including severe asthma), sleep apnea, severe liver disease, and narrow-angle glaucoma.
  • Alprazolam should not be taken during pregnancy and breast feeding, as it may cause serious harm to the fetus or infant.
  • Many drugs, including Tagamet and oral contraceptives, interfere with the metabolism of Alprazolam, resulting in increased Alprazolam blood levels and hence increased effects.
  • Eating grapefruit or drinking grapefruit juice inhibits the intestinal metabolism of Alprazolam, resulting in increased blood levels and hence increased effects.

Disclaimer: The information above is correct to the best of our knowledge, but please note that it is not exhaustive and its accuracy is not guaranteed. For complete information on Alprazolam, please consult a pharmacology monograph.


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