Benzodiazepine Insomnia Drugs
The first benzodiazepine to appear on the market in the late 1950's was Librium ®, to be quickly followed by a series of similar drugs during the 1960's and 1970's.
Benzodiazepines (often referred to as benzodiazepine hypnotics) act in much the same way as barbiturates by assisting the natural brain chemical gamma-aminobutyric acid (GABA). GABA interacts with some 40% of the neurons all over the brain to produce a general calming effect, acting as the body's natural hypnotic and tranquillizer.
Benzodiazepines are often divided into three groups:
- Short-acting - effective for less than 6 hours.
- Medium-acting - effective for between 6 and 10 hours.
- Long-acting - effective in excess of 10 hours.
Some of the more commonly prescribed benzodiazepines include:
| Generic Name | Trade Name | Comments |
| Lorazepam | Ativan ® | Lorazepam is used to relieve anxiety. It is also used to treat irritable bowel syndrome, epilepsy, insomnia, and nausea and vomiting from cancer treatment and to control agitation caused by alcohol withdrawal.
Long-acting
Side effects from lorazepam are common and include:
-drowsiness
-dizziness
-tiredness
-weakness
-dry mouth
-diarrhea
-upset stomach
-changes in appetite |
| Flurazepam | Dalmane ® | Flurazepam is designed to be used on a short-term basis to help you fall asleep and stay asleep through the night.
Long-acting
Side effects from flurazepam are common and include:
-headache
-heartburn
-diarrhea
-hangover effect (grogginess)
-drowsiness
-dizziness or lightheadedness
-weakness
-dry mouth |
| Triazolam | Halcion ® | Triazolam is designed to be used on a short-term basis to help you fall asleep and stay asleep through the night.
short-acting
Side effects from triazolam are common and include:
-headache
-heartburn
-diarrhea
-hangover effect (grogginess)
-drowsiness
-dizziness or lightheadedness
-weakness
-dry mouth |
| Clonazepam | Klonopin ®
Rivotril ® | Clonazepam is used to control seizures. It is also used to relieve anxiety.
Long-acting
Side effects from clonazepam are common and include:
-drowsiness
-dizziness
-tiredness
-weakness
-dry mouth
-diarrhea
-upset stomach
-changes in appetite |
| Chlordiazepoxide | Librium ® | Chlordiazepoxide is used to relieve anxiety and to control agitation caused by alcohol withdrawal.
Long-acting
Side effects from clonazepam are common and include:
-drowsiness
-dizziness
-tiredness
-weakness
-dry mouth
-diarrhea
-upset stomach
-changes in appetite |
| Nitrazepam | Mogadon ®
Remnos ®
Somnite ® | Nitrazepam is used to induce sleep and cause relaxation.
long-acting
Side effects from nitrazepam are common and include:
-anxiety
-confusion
-fast, pounding, or irregular heartbeat
-loss of memory
-mental depression |
| Estazolam | ProSom ® | Estazolam is used on a short-term basis to help you fall asleep and stay asleep through the night.
Long-acting
Side effects from estazolam are common and include:
-headache
-heartburn
-diarrhea
-hangover effect (grogginess)
-drowsiness
-dizziness or lightheadedness
-weakness
-dry mouth |
| Temazepam | Restoril ® | Temazepam is used on a short-term basis to help you fall asleep and stay asleep through the night.
Long-acting
Side effects from temazepam are common and include:
-headache
-heartburn
-diarrhea
-hangover effect (grogginess)
-drowsiness
-dizziness or lightheadedness
-weakness
-dry mouth |
| Oxazepam | Serax ® | Oxazepam is used to relieve anxiety. It also is used to control agitation caused by alcohol withdrawal.
Medium-acting
Side effects from oxazepam are common and include:
-drowsiness
-dizziness
-tiredness
-weakness
-dry mouth
-diarrhea
-upset stomach
-changes in appetite |
| Clorazepate | Tranxene ® | Clorazepate is used to relieve anxiety. It also is used to control agitation caused by alcohol withdrawal as well as seizures.
Long-acting
Side effects from clorazepate are common and include:
-drowsiness
-dizziness
-tiredness
-weakness
-dry mouth
-diarrhea
-upset stomach
-changes in appetite |
| Alprazolam | Xanax ® | Xanax is used to relieve anxiety, nervousness, and tension associated with anxiety disorders. Xanax is also used to treat panic disorders.
Medium-acting
Common side effects include:
-drowsiness, dizziness, or clumsiness
-depression
-nausea, vomiting, diarrhea, or constipation
-difficulty urinating
-vivid dreams
-headache
-dry mouth
-decreased sex drive
-changes in behavior |
Like barbiturates, both addiction and dependence are commonly seen in people taking benzodiazepines for any length of time. Benzodiazepines also demonstrate a remarkably large range of side effects, many resulting directly from the manner in which the drug works.
By enhancing the effects of GABA, benzodiazepines not only inhibit the activity of those parts of your brain that the body wishes to shut down during sleep, but also act on many of the neurotransmitters that you need during the day. Normal alertness, memory function, muscle co-ordination, emotional responsiveness, heart rate and blood pressure control, to mention just a few, all depend upon messages that benzodiazepines suppress. As well as enhancing the effects of GABA, benzodiazepines also affect other areas of your body such as the kidneys, colon, blood cells and the adrenal cortex. It's not surprising therefore that we see a very long and varied list of side effects associated with this group of drugs.
One of the biggest problems however lies in the cumulative effect of a large number of benzodiazepines. Many of the commonly prescribed drugs are long-acting - that is to say that they remain in the body for periods well in excess of 10 hours. This means two things:
- Firstly, they continue to work long after you get up in the morning and need to be active and alert.
- Secondly, as you continue to take your daily dose night after night, you are simply adding to the remains of the drug still in your body and effectively overdosing.
The time taken for a drug to work its way out of your system is often referred to as the drug's half-life. In simple terms, the time it takes for the concentration of the drug within your blood to fall to half of its peak value.
For some benzodiazepines the half-life falls well within the normal 24 hour day/night cycle. Xanax ® with a half-life of 6 to 12 hours and Halcion ® with a half-life of 2 to 5 hours present a relatively low risk of accumulation. Klonopin ® and Rivotril ® with half-lives of 18 to 50 hours and Valium ® with a half-life of 36 to 200 hours, on the other hand, will show a marked build-up within just a matter of days.
As with barbiturates, benzodiazepines were designed for short-term use over a matter of days, and certainly for no longer than two or three weeks. Many people however quickly become both psychologically and physiologically dependent on these drugs and continue taking them for weeks, months or even years.
Within a matter of only days these drugs lose their effectiveness and you not only no longer enjoys the benefits originally given by the drug, but now have to suffer the numerous and on-going side effects.
Not surprisingly the benzodiazepines are following the fate of the barbiturates as a form of insomnia medication and now falling from favor. So where do we go next?
Next >>> Non-benzodiazepines
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The information contained here should NOT be used as a substitute for the advice of an appropriately qualified and licensed physician or other health care provider. The information provided here is for educational and informational purposes only and in no way should be considered as an offering of medical advice.
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