BARBITURATES

Barbiturates are a kind of depressant or sedative drug. They are an old class of drug used to relax the
body and help people sleep. They can produce effects similar to those of alcohol, ranging from mild
relaxation to an inability to feel pain and loss of consciousness. As a medication, they reduce muscle
spasms, relieve anxiety, prevent seizures, and induce sleep. They can be classified as ultra-short-, short-,
intermediate-, and long-acting. When people take barbiturates by mouth, their effects begin within 30
minutes of swallowing and last from 4 to 16 hours.

USES:

Sedation – these agents have largely been replaced by more modern and safer agents like
benzodiazepines in this area.

Sleep induction or hypnosis – in short term insomnia, barbiturates may be effective. This is because
they tend to lose their effectiveness in sleep induction and maintenance after 2 weeks of use.

Before surgery as a preanesthetic agent – sedation is given prior to surgery to allay anxiety and to
ease the process of induction of general anesthesia. This is also an area where benzodiazepines have
replaced barbiturates.

Treatment of seizures - treatment of partial and generalized tonic-clonic and cortical focal seizures
could still utilize barbiturates including mephobarbital, Phenobarbital.

Acute convulsions – acute onset convulsions including status epilepticus, eclapmsia during pregnancy,
meningitis, tetanus and toxic reactions to strychnine or local anesthetics, convulsions during cholera
etc. are indications for use of barbiturates.

WHAT IS A NEUROTRANSMITTERS?

- It is chemical agent that is produced by a neuron that transmits messages to a specific structure
that was designed to target. And many times the target is another neuron so it can send a
message that is inhibitory message or an excitatory message.
- We have here a neuron you can see it is releasing a neurotransmitter, and these
neurotransmitter is going down and it’s going to find its special receptor that it binds with. Once
it binds and locks down on that receptor it’s going to either send an inhibitory message or
excitatory message. Depending on what type of neurotransmitter we’re dealing.
- If it is excitatory message means it is going to excite, it will increase the firing potential of that
neuron so we’re going to get a response, however if it is inhibitory neurotransmitter it’s going to
inhibit the message from being sent, it will decrease firing potential. Because of that we are
going to get the calm things down effect and depress the central nervous system.

ACTION:

The primary mechanism of action of barbiturates is inhibition of the central nervous system. It causes
central nervous system depression. So how they do this? Is that they amplify the effects of a specific
neurotransmitter called the [gamma]-aminobutyric acid (GABA) system and this is actually an inhibitory
neurotransmitter. Over the years Barbiturates have been slowly replaced by benzodiazepines especially
to the treatment of insomnia and anxiety, well because barbiturates have a very low therapeutic index
means there is a small threshold between the therapeutic dose and toxic dose so there is a higher
incidence of overdose with this drug compared to benzodiazepines.

- Both of them target the same receptors in the body but they do it differently. And how they
cause the ion channel to open up and hyperpolarize the cell

The GABA (inhibitory) channel is a Chloride channel that has five cells at its gate. When barbiturates bind
to the GABA channel they lead to prolonged opening of the channel letting in Chloride ions into the cells
in the brain. This leads to increased negative charge and alters the voltage in the brain cells. (It increase
the duration of how long the channel stays open so we have more chloride flowing through).

WHICH DRUGS ARE BARBITURATES? These are the drugs that most end with barbital or ital.

MOST COMMON BARBITURATES INCLUDE:

Amobarbital. This can treat insomnia, but it’s only effective in the short term. It can also help with
certain neurological (brain function) tests.

Butalbital. This medication is part of many combination medications, including aspirin,

acetaminophen, caffeine and codeine. Depending on the combination, it can treat migraines and
tension headaches.

Methohexital. This medication is useful for anesthesia in short diagnostic and treatment procedures.
It’s very helpful in procedures like electroconvulsive therapy.

Pentobarbital. This medication is useful for pre-anesthesia. It can also stop seizures as they’re
happening.

Phenobarbital. This medication is also useful for preventing seizures or stopping them when they’re
happening.

Secobarbital. This medication treats insomnia, but this is less common, and many healthcare
providers avoid prescribing it

LET’S TALK ABOUT NURSING RESPONSIBILITIES, SIDE EFFECTS AND PATIENT EDUCATION

‘REMEMBER THE WORD BARBITS”

B- “BARBS AND BENZOS DIFFERENCES

ARE BARBITURATES THE SAME AS BENZODIAZEPINES?

- Bind in different location on a gaba receptor for benzodiazepines it binds between the alpha
and the gama sub unit with barbiturates it tends to be found either the alpha sub unit or the
beta sun unit
- High doses of barbs can influence receptor without GABA – with barbiturates high doses can
influence the gaba a receptor without the help of the gaba neurotransmitter while benzos
cannot do that.
- - Low therapeutic index – barbiturates have a very low therapeutic index which makes the risk
of overdose.
- No antidote
Benzos are most commonly prescribed for insomnia and anxiety rather than barbiturates due to that
high risk of overdose, plus the high risk of dependency Dependence is when your body is so used to a
drug that you develop unpleasant or dangerous symptoms if you go too long without taking the drug.
And addiction is a mental health condition where dependence disrupts your life, where you are
compulsively seeking and using the drug despite adverse consequences.

AND NOW LEADS TO “A”

The addiction, dependence is high risk with barbiturates

- So as a nurse we need to look for the risk factors that can increase your patients risk
So if they are using this for a LONG TERM that can increase it and also check for their history if
they have a history of SUBSTANCE ABUSE in the past or if they are experiencing an any
SUICIDAL THOUGHTS because those factors can actually increase the risk along with over
dose.

WHICH NOW LEADS US INTO “R”

RECOGNIZE OVERDOSE signs and symptoms

- If and overdose does occur with a barbiturate as I said a while ago that there is no antidote so
they will be now supported on how severe it is.
Supported with mechanical ventilation- because respiratory failure is definitely a main thing that
presents. They may need dialysis to help remove some of those drug levels from the blood or
activated charcoal you want to educate who is taking a barbiturates that they want to avoid
other medications that can increase the risk of toxicity like alcohol can and other cns depressant
like they would not want to take barbiturates and benzos together.

The signs and symptoms that an overdose may be presenting in your patients you will just need to
remember the mnemonic LETHAL

L – LOST OF CONCIOUSNESS – to the point of coma

E- EYE PUPILS PINPOINT AND THEN PROGRESS TO DILATION AND FIXED AS IT PROGRESSES AND
BODY SHUT DOWN

T- TACHYCARDIA body will become weak

H- HAVE COLD AND SWEATY SKIN

A-

NEXT IS “B”

BE AWARE OF PATIENT SAFETY

- So in patient taking barbiturates it is normal to have side effects that they are going to feel very
relaxed, feel drowsy some can feel euphoric and their senses are going to be extremely dull and
they are not going to think clearly. So because of that because the drugs doing what it’s
supposed do there can be danger to themselves and to others.
 - So as a nurse make sure that the patient does not get up without assistance (AMBULATION)
because they are definitely RISK FOR FALLS. You need also to watch the BED POSITION because
they can get up and fall and hurt themselves, so adjust it in a lowest position with the side rails
up. And also IMPORTANT DESCISIONS to be made at this time whenever they are under the
influence of this. And if they are going home they don’t need to be DRIVING or doing anything
that requires concentration that can hurt themselves or the others
- And let the patient be aware that there is a risk of ACCIDENTAL OVERDOSE they need to take
this drugs exactly as prescribed, there’s a risk of addiction, withdrawal signs and symptoms and
tolerance that can develop especially if they are using these for long term.

THEN FOR “I” index low

- Specifically the therapeutic index, means there is a fine line between that therapeutic dose and
toxic dose so as a nurse you need to monitor those serum drug levels
- For example the familiar drugs in barbiturates is the phenobarbital, its serum level is anywhere
between 15-40 mcg/ml (micrograms/ milliliter) so anything greater than that it means our
patient is toxic.

“T” FOR TOLERANCE CAN DEVELOP

- So what is tolerance? Well tolerance can develop when patient can no longer get the same
effect from that drug, so in order to get the effects they were getting before they have to
increase their doses, but we’ve learned that with barbiturates there’s fine line between that
therapeutic and toxicity dose. So this can lead to accidental overdose and even death. And this
tends to happen to the patients who are taking these long term or who are abusing the drug.

AND LASTLY WE HAVE “S” STOPPING THE DRUGS ABRUPTLY CAN LEAD TO WITHDRAWAL SIGNS AND
SYMPTOMS.

- Can be anywhere from mild to severe, which tends to happen with patients who are using them
long term and it can happen as soon as 24 hours from when they last had that dose of that
drug. As a nurse we need to be familiar with those signs and symptoms that a patient is
withdrawing from a barbiturate because the patients going to need treatment to prevent shock
or eventually death.
- SO WHAT ARE THOSE SIGNS AND SYMPTOMS
Let’s remember the mnemonic CRAVES
C- CONVULSIONS
R- RESTLESSNESS
A- AGITATION
E- ELEVATED TEMPERATURE
S-SLEEP PROBLEMS
- This can actually be very severe and can progress to shock and eventually death