How does alcohol affect hypnotics?

Thunderwolf, MSN, RN · Sep 1, 2005

Alcohol use, especially with alcoholics, can and does elevate liver enzymes. A classic marker in evaluating liver enzymes is that if the GGT is the only elevated enzyme, it suggests alcohol ingestion....something to keep in mind when evaluating lab values. Also, chronic alcoholics may tend to have lower Magnesium levels due to malabsorption in the gut. Another thing to keep in mind is that significant, chronic alcohol use just eats away at those liver cells and damages them, which elevate the enzymes in general...that is why you see elevated enzymes due to the damage. Now the purpose of the liver is to metabolize chemicals, such as medication. Most meds are not in their active form, but in their inactive form, until they are bioconverted by the liver into their active form to be useful (usually 4 times the half-life of the drug till a steady state of therapeutic effectiveness is present). The half life of medications are different for each medication. Some meds are 6 hours, some 8, some 12, etc. It may take longer to bioconvert meds into their useful form if the liver is damaged...therefore, circulating in the blood stream longer, taking longer to bioconvert into effectiveness. The liver also breaks down chemicals and meds as measured via a drug's half-life as well. If the liver is damaged, it may take longer for a medication to break down to sub-therapeutic levels till it is out of the system. The key thing about the liver is that it sees alcohol as a poison and will attempt to metabolize it first in order to get rid of it. This is why folks with liver damage may need smaller doses of a medication compared to persons with a more healthier liver. However, "elevated liver enzymes" have nothing to do with metabolizing the drug; elevated enzymes indicate damage. Now, let's get to answering your question as to why a sleeper may not be helpful in inducing sleep for the alcohol user. It is quite often the acute absence of alcohol or lower alcohol levels that cause excitment of the neurons which cause disruption of sleep, even with a sleeper on board. For the sake of example, let's use Restoril...a Benzodiazepine. Here comes physiology 101. Bare with me. Your neurons have many receptors on them which are influenced by chemicals in the body (neurotransmitters). These chemicals when they bind on these receptor sites can either excite or relax the neuron, depending on the chemical(s). One major receptor site is the GABA receptor, which when stimulated by GABA increases the inflow of calcium into the nerve...causing relaxation of that nerve(s). Here is the other part to remember about this. The nerve also has receptor sites for alcohol AND benzodiazepine which appear to boost the work of the already mentioned GABA site...therefore, increasing the GABA effect. Result is increased relaxation and sedation potential. This is why it is not a good idea to mix alcohol with downers/benzos/sleepers. The effect is called "synergic" because 1+1 does not equal 2, but 3. This is why alcohol and sedative overdoses occur...the extreme relaxation of nervous tissue...coma, respiratory failure. Combine this with an already damaged liver which keeps a medication in the blood stream longer also contributes. Now, to get to the answer as to why alcoholics have difficulty sleeping with a sleeper. It could be a couple of reasons. The sudden "absence of alcohol" from the alcohol receptor sites causes "an excitatory effect" on the nerves (less inflow of calcium into the nerves)...aka withdrawal, which can overshadow any positive effect from the sleeping pill inducing any relaxation to make sleep possible. Another reason is that "chronic use of benzodiazepines" causes the nerves to adapt to their effects...when this occurs, the benzo receptor of the nerve begins to produce a lessened effect on the GABA relaxation of the nerve(s). (Does your alcohol user chronically use benzos as well?) The sleeping medication just isn't effective like it used to be...adaptation. This is another reason why sleeping pills should not be taken any more than 10 days...they become less effective...the body adapts. Actually, chronic benzodiazepine use for sleep begins to disrupt sleep cycles by lessening the REM stages of sleep as well...less dreams. Not good. REM sleep is very important to healthy sleep. This is why the person may sleep, but not feel rested in the morning...less REM sleep. Just like chronic alcohol use can cause withdrawal when abruptly stopped, acute disruption in "chronic benzodiazepine" use can do the same...cause withdrawal...rebound REM sleep (nightmares), insomnia, disrupted thought processes, seizures, and heightened anxiety (nerve cell excitement due to lessened inflow of calcium into the nerve cells).. In fact, acute benzo withdrawal after chronic use can become quite nasty...just like alcohol withdrawal. This is also the reason why detox is quite often needed from BOTH chronic alcohol and/or benzo/sedative use...but, only under a doctor's care and supervision...NOT on one's own. This is also quite often the reason why doctors try to shy away from benzodiazepine prescription if they can. Docs may try other meds as sleep aids which bypass or have less of a GABA effect...such as Desyrel, an antidepressant which causes drowsiness from it's antihistamine properties...not by GABA. I hope this wasn't too complicated. But essentially, that's the nuts and bolts to answering your question. I hope I was helpful.

milenko · Sep 1, 2005

Mate, Thanks for the info, it seems that I wasnt very far off the beaten path but your answer really puts it into perspective. Thanks for taking the time to write all that down. Actually taught me more than what I could find in my pharmacology book.

Thanks again

Alcohol use, especially with alcoholics, can and does elevate liver enzymes. A classic marker in evaluating liver enzymes is that if the GGT is the only elevated enzyme, it suggests alcohol ingestion....something to keep in mind when evaluating lab values. Also, chronic alcoholics may tend to have lower Magnesium levels due to malabsorption in the gut. Another thing to keep in mind is that significant, chronic alcohol use just eats away at those liver cells and damages them, which elevate the enzymes in general...that is why you see elevated enzymes due to the damage. Now the purpose of the liver is to metabolize chemicals, such as medication. Most meds are not in their active form, but in their inactive form, until they are bioconverted by the liver into their active form to be useful (usually 4 times the half-life of the drug till a steady state of therapeutic effectiveness is present). The half life of medications are different for each medication. Some meds are 6 hours, some 8, some 12, etc. It may take longer to bioconvert meds into their useful form if the liver is damaged...therefore, circulating in the blood stream longer, taking longer to bioconvert into effectiveness. The liver also breaks down chemicals and meds as measured via a drug's half-life as well. If the liver is damaged, it may take longer for a medication to break down to sub-therapeutic levels till it is out of the system. The key thing about the liver is that it sees alcohol as a poison and will attempt to metabolize it first in order to get rid of it. This is why folks with liver damage may need smaller doses of a medication compared to persons with a more healthier liver. However, "elevated liver enzymes" have nothing to do with metabolizing the drug; elevated enzymes indicate damage. Now, let's get to answering your question as to why a sleeper may not be helpful in inducing sleep for the alcohol user. It is quite often the acute absence of alcohol or lower alcohol levels that cause excitment of the neurons which cause disruption of sleep, even with a sleeper on board. For the sake of example, let's use Restoril...a Benzodiazepine. Here comes physiology 101. Bare with me. Your neurons have many receptors on them which are influenced by chemicals in the body (neurotransmitters). These chemicals when they bind on these receptor sites can either excite or relax the neuron, depending on the chemical(s). One major receptor site is the GABA receptor, which when stimulated by GABA increases the inflow of calcium into the nerve...causing relaxation of that nerve(s). Here is the other part to remember about this. The nerve also has receptor sites for alcohol AND benzodiazepine which appear to boost the work of the already mentioned GABA site...therefore, increasing the GABA effect. Result is increased relaxation and sedation potential. This is why it is not a good idea to mix alcohol with downers/benzos/sleepers. The effect is called "synergic" because 1+1 does not equal 2, but 3. This is why alcohol and sedative overdoses occur...the extreme relaxation of nervous tissue...coma, respiratory failure. Combine this with an already damaged liver which keeps a medication in the blood stream longer also contributes. Now, to get to the answer as to why alcoholics have difficulty sleeping with a sleeper. It could be a couple of reasons. The sudden "absence of alcohol" from the alcohol receptor sites causes "an excitatory effect" on the nerves (less inflow of calcium into the nerves)...aka withdrawal, which can overshadow any positive effect from the sleeping pill inducing any relaxation to make sleep possible. Another reason is that "chronic use of benzodiazepines" causes the nerves to adapt to their effects...when this occurs, the benzo receptor of the nerve begins to produce a lessened effect on the GABA relaxation of the nerve(s). (Does your alcohol user chronically use benzos as well?) The sleeping medication just isn't effective like it used to be...adaptation. This is another reason why sleeping pills should not be taken any more than 10 days...they become less effective...the body adapts. Actually, chronic benzodiazepine use for sleep begins to disrupt sleep cycles by lessening the REM stages of sleep as well...less dreams. Not good. REM sleep is very important to healthy sleep. This is why the person may sleep, but not feel rested in the morning...less REM sleep. Just like chronic alcohol use can cause withdrawal when abruptly stopped, acute disruption in "chronic benzodiazepine" use can do the same...cause withdrawal...rebound REM sleep (nightmares), insomnia, disrupted thought processes, seizures, and heightened anxiety (nerve cell excitement due to lessened inflow of calcium into the nerve cells).. In fact, acute benzo withdrawal after chronic use can become quite nasty...just like alcohol withdrawal. This is also the reason why detox is quite often needed from BOTH chronic alcohol and/or benzo/sedative use...but, only under a doctor's care and supervision...NOT on one's own. This is also quite often the reason why doctors try to shy away from benzodiazepine prescription if they can. Docs may try other meds as sleep aids which bypass or have less of a GABA effect...such as Desyrel, an antidepressant which causes drowsiness from it's antihistamine properties...not by GABA. I hope this wasn't too complicated. But essentially, that's the nuts and bolts to answering your question. I hope I was helpful.

Editorial Team / Admin · Sep 1, 2005

Most excellent, Thunderwolf. I really enjoyed reading your explanation!!