Barbiturate (Oral, Parenteral, Rectal)

Derived from barbituric acid, Barbiturates work by enhancing the action of a neurotransmitter that obstructs the activity of nerve cells in the brain.

Overview

Barbiturates are a class of synthetic drugs that act as a sedative by depressing the nervous central system. Barbituric acid actually has no therapeutic action, but its by-products enhance the neurotransmitter, GABA (gamma-aminobutyric acid) and help to inhibit the activity of nerve cells in the brain.

Historically, Barbiturates were regularly prescribed to treat mental health disorders such as anxiety and depression. However, they have been almost entirely replaced for these purposes due to their tendency to cause a high percentage of both physical and psychological dependence. Their medical use goes back to 1903 when it was advertised as being safe and side-effect free. Used largely in the 1950's and 1960's as sleeping tablets, its harmful effects resulted in Barbituates being sold on streets for recreational and dangerous drug use.

Barbiturates also have a high risk of overdose, as there is a fine line between a lethal dose and normal dose. This risk is made greater if you have combined barbiturates with alcohol or other central nervous system suppressors. For the above-mentioned illnesses, doctors now tend to prescribe benzodiazepines, which are in the same drug's class.

Currently, barbiturates have less varied use. Certain barbiturates are used as anticonvulsants, contributing to the control of seizures in some disorders or diseases. Epilepsy is one of the most common diseases that doctors will prescribe barbiturates for. The medicine is also commonly used as a sedative for anxious or tense patients before and during surgery. Alongside this, barbiturates may also be used for other conditions such as migraines, increased pressure in the skull, insomnia, alcohol and benzodiazepine poisoning, or other illnesses as decided on a case-by-case basis by your doctor.

When taking barbiturates, it is advised that you remain under regular supervision with a healthcare professional. They can cause adverse side effects that are likely to affect many people who take them. Fortunately, the most common side effects are unlikely to cause much impact on a person's routine and often disappear once the body has become adjusted to the medicine. For patients who have been administering barbiturates regularly, withdrawal is likely and must be managed with the help of a healthcare professional. This can be an unpleasant experience that can affect users differently. For those who have been regular users of barbiturates for extended periods of time, sudden withdrawal can be fatal. You must discuss a care plan with your doctor before stopping or reducing any barbiturate medication.

Barbiturates are classified according to the speed that they are released into the system. Different administration methods and medications offer slow, intermediate, short and very short effects. They can be administered through the oral route, parenteral route, and rectal route. It has a number of dosage forms that include the oral routes of elixir, capsule, and tablet, the parenteral routes of suspension or solution, or the rectal routes of enema or suppository. The best route and dosage form for a patient will be decided by a doctor when discussed. Factors such as your illness, treatment plan, previous conditions and general health will all be taken into account when making this decision.

Barbiturates must only ever be prescribed by a doctor and purchased in a licensed pharmaceutical store.

Conditions treated

  • Seizure disorders such as epilepsy
  • Migraines
  • Sedatives for surgical procedures
  • Increased pressure in the skull
  • Alcohol poisoning
  • Benzodiazepine poisoning
  • Insomnia

Type of medicine

  • Central nervous system depressant

Side effects

A number of the side effects you may experience when taking Barbiturates can be mild and may not require medical attention. These are likely to be reactions that have occurred whilst your body adjusts to the medicine. The most common side effect that patients experience when taking barbiturates includes clumsiness, unsteadiness, dizziness, lightheadedness, drowsiness, and a groggy, hangover-like feeling. If you find that any these effects become too bothersome or you are concerned in any way, it is important that you discuss them with your doctor.

A number of less common side effects that are less harmful may also be experienced. These include anxiety or nervousness, constipation, feeling faint, headaches, irritability, vomiting, nausea, and nightmares or difficulty sleeping. Some of these reactions may disappear once you have become used to the medicine, however, if you are finding any of them difficult to manage or they are causing you worry, make an appointment with your healthcare professional. Before you begin your treatment, it is important to discuss side effects, their management, and how you might be able to alleviate them with your doctor. With many medications, changes can be made to your diet and lifestyle that may help to counteract some of the medicinal side effects.

If you notice any chest pain, hives, swelling of the cheeks, lips and eyes or difficulty in breathing whilst taking Barbiturates, it is essential that you inform your doctor immediately as it could be a sign of an allergic reaction. Other signs of an allergic reaction include wheezing and a tightness in the chest, red, rashy skin, painful sores, ulcers or white spots in the mouth and a fever.

Uncommon side effects of this medication include confusion, mental depression and a feeling of unusual excitement. These are all reactions that can impair your judgment and can become harmful or dangerous situations. If you experience any of these effects, it is important to consult your doctor right away.

In very rare cases, you may experience hallucinations. These can be extremely unpleasant and unsafe for you and the people around you. If you begin to see, hear or feel things that are not there, it is important that you inform a relative or close contact and see your doctor right away. Other rare reactions to barbiturates include unusual bleeding or bruising and an unusual tiredness or weakness. These are all rare side effects that can lead to more harmful medical issues and must all be reported to a healthcare professional immediately.

For patients who have long-term or chronic use of barbiturates, it can cause some harmful side effects that will require immediate medical attention. An unusual amount of weight loss, the loss of appetite, muscle weakness, bone pain and tenderness or yellow eyes or skin are all signs of harmful effects from long-term use of barbiturates. If you experience any of these symptoms, you must inform your doctor as soon as possible. Alongside this, if you notice slurred speech, decreased motor control, agitation, the inability to urinate and slowed brain function, it is important to make an appointment with your healthcare professional. These symptoms are all indicators of having a barbiturate dependency and must be dealt with immediately. In the circumstance that you do believe you are dependent on your medication, it is essential that you continue taking it as per usual. To suddenly stop can cause severe withdrawal symptoms which may result in hospitalization.

In severe cases, a patient may experience a barbiturate overdose. Due to there being a fine line between a normal and lethal dose, overdoses are more common with this medicine than most. In the event that you suspect you are having an overdose, call 911 and get to a hospital as soon as you can. Symptoms that indicate an overdose include severe confusion, a decrease or the loss of reflexes, severe drowsiness, a high temperature, severe and continuing irritability, poor judgment, a slow heartbeat, staggering and difficulty in walking, trouble in sleeping, weakness and unusual movements of the eyes.

As with all medication, it is important to attend regular doctor's appointments and communicate to track and manage any side effects that you may be experiencing. When taking barbiturates, it is especially important that you maintain this communication once you and your doctor have decided to stop taking the medication. This is because barbiturates are highly likely to cause withdrawal. Withdrawal can be an unpleasant experience which can result in anxiety, irritability, insomnia, faintness, sickness and in some cases, convulsions. For some patients who have been prescribed high doses and regular use, severe withdrawal symptoms can occur. This includes seizures, low blood pressure, becoming delirious and having hallucinations. Before discontinuing your barbiturate treatment, it is vital that your doctor is aware and has discussed its management with you. It is likely that your doctor will wean you off the medication with lower doses other a long period of time. Sudden withdrawal from high doses can be fatal.

Dosage

As there are a number of routes to administer barbiturates, the dosage varies. The way that barbiturates are administered and dosed is dependant on the speed that the medication is required to be released.

The most common ways to take barbiturates are by capsule or tablet, rectal suppository or injection. For patients who are taking capsules or tablets, it is vital that they are always swallowed whole. Breaking, crushing or chewing them before swallowing can have harmful effects.

For those who will be using rectal suppositories, it is important to have a good understanding of how to insert it. It is advised that you moisten the suppository with cold water before inserting. You should then lie down on your side and use your finger to insert the suppository up into the rectum.

You should only use this medicine as directed by your doctor and should never alter the dose yourself. If you feel that you dose is not strong enough, discuss it with your doctor. Some forms of barbiturates can be combined. In these cases, your doctor will determine the best dosage and administration route.

If you happen to miss a dose of your medicine, make sure to take it as soon as you can. However, if enough time has passed that it is almost time for your next dose, it is important that you do not double dose. Instead, skip the missed dose and go back to your regular dosing schedule.

Slow release barbiturates

Slow release barbiturates can last for up to 24 hours. These tend to be used in combination with other medications as part of a treatment plan for epilepsy and other seizure disorders. This is because of their extended depressant action which can help to prevent seizures and convulsions. Slow release barbiturates include barbital and phenobarbital.

Phenobarbital can be either taken in the form of an injection or orally. Its oral dosage forms are as an elixir, capsules or tablets. Dosages are dependant on the purpose of a patient's treatment, their ages, and their current health.

Taking phenobarbital orally for insomnia:

  • Adults are recommended to take 100 to 320 mg at bedtime.
  • A child's dose must be decided by a doctor.

Taking phenobarbital orally for daytime sedation:

  • Adults can take 30 to 120 mg a day. This must be taken in smaller doses two or three times during the day.
  • A child's dose must be determined by a doctor and is based on their body weight or size. A typical dose for children is 2 mg per kg of body weight, taken three times a day.

Taking phenobarbital orally for pre-surgery sedation:

  • Adults should take 100 mg before surgery.
  • The dose for children is based on their body weight. It must be decided by a doctor. The standard dose is 1 to 3 mg per kg of body weight.

Taking phenobarbital orally for control of seizures:

  • Adults should take 60 to 250 mg a day.
  • A child's dose is based on body weight and must be decided by a doctor. The standard daily dose is 1 to 6 mg per kg of body weight.

Taking phenobarbital by injection for insomnia:

  • Adults are advised to take 100 to 325 mg. This should be injected under the skin, or into a muscle or vein.
  • A child's dose must be decided by a doctor.

Taking phenobarbital by injection for daytime sedation:

  • The recommended dose for adults is 30 to 120 mg a day. This should be injected under the skin, or into a muscle or vein and given in smaller doses. The doses should be given two or three times throughout the day.
  • A child's dose must be determined by their doctor.

Taking phenobarbital by injection for pre-surgery sedation:

  • The adult dose is 130 to 200 mg. It will be injected into a muscle 60 to 90 minutes before the surgical procedure.
  • A child's dose is based on body weight and must be decided by a doctor. The standard daily dose is 1 to 3 mg per kg of body weight. This will be injected into a muscle or vein 60 to 90 minutes before the surgical procedure.

Taking phenobarbital by injection for control of seizures:

  • Adults should take 100 to 320 mg. This will be injected into a vein. If necessary, the dose may be repeated but it is usually no more than 600mg a day. However, in certain cases, higher doses may be required for some types of continuing seizures.
  • A child's dose is based on their body weight and it must be decided by a doctor. The initial dose is usually 10 to 20 mg per kg of body weight and must be injected into a vein. In some cases, higher doses may be necessary for prolonged types of seizures.

Intermediate release barbiturates

  • Barbiturates that offer intermediate release into the system include amobarbital and butabarbital sodium. These can last for up to 12 hours and are mainly used in treating insomnia.

Taking amobarbital orally for insomnia:

  • The adult dose is 65 to 200 mg at bedtime.
  • A child's dose must be determined and approved by a doctor.

Taking amobarbital orally for daytime sedation:

  • The adult dose is 50 to 300 mg, taken in smaller doses throughout the day.
  • A child's dose is dependant on body weight and must be decided by your doctor. The standard dose is 2 mg per kilogram of body weight taken. This should be taken three times a day.

Taking amobarbital orally for sedation before surgery:

  • Adults are advised to take 200 mg one to two hours before a surgical procedure.
  • A child's dose is dependant on body weight and must be decided by a doctor. The standard dose is 2 to 6 mg per kilogram of body weight but is usually no more than 100 mg. This dose should be taken before surgery.

Taking amobarbital orally for sedation during labor:

  • Adults can take 200 to 400 mg. The total dose should not be more than 1000 mg. This dose can be taken every one to three hours if needed.

Taking amobarbital by injection for insomnia:

  • Adults should take 65 to 200 mg. This will be injected into a muscle or vein.
  • A child's dose is based on their body weight and it must be decided by a doctor. For children up to six years old, the dose is 2 to 3 mg per kg of body weight and should be injected into a muscle. For children who are six years and older, the dose is 2 to 3 mg per kg of body weight when injected into a muscle. If the dose will be injected into a vein, the dose is 65 to 500 mg.

Taking amobarbital by injection for daytime sedation:

  • The recommended dose for adults is 30 to 50 mg a day. This should be injected into a muscle or vein two or three times a day.

Taking amobarbital by injection for pre-surgery sedation:

  • A child's dose is based on body weight and must be decided by a doctor. The standard daily dose is 3 to 5 mg per kg of body weight when injected into a muscle. If injecting into a vein, the dose is 65 to 500mg.

Taking amobarbital by injection for control of seizures:

  • Adults and children who are six years of age and over should take 65 to 500 mg. This will be injected into a vein.
  • For children who are six years old and younger, the dose is based on their body weight and it must be decided by a doctor. The standard dose is usually 3 to 5 mg per kg of body weight and must be injected into a muscle or vein.

Short release barbiturates

  • Barbiturates that are quickly released into the system include pentobarbital and secobarbital. These are commonly used to overcome insomnia, as a daytime sedative or as a pre-surgery sedation for children.

Taking pentobarbital orally for insomnia:

  • Adults are advised to take 100 mg at bedtime.
  • A child's dose will be decided by your doctor.

Taking pentobarbital orally for daytime sedation:

  • Adults can take 20mg three to four times each day.
  • A child's dose will be decided by your doctor and is dependant on body weight. The standard dose is 2 to 6 mg per kg of bodyweight each day.

Taking pentobarbital orally for pre-surgery sedation:

  • Adults are to take 100gm before surgery.
  • A child's dose must be decided by a doctor. It is dependant on body weight. The standard dose is 2 to 6 mg per kg and it will usually not exceed 100 mg.

Taking pentobarbital by injection for insomnia:

  • Adults can take 150 to 200 mg when it is injected into a muscle. If injecting into a vein, the dose is 100 mg. If needed, a patient can take additional small doses. However, the dose should not exceed 500 mg in a day.
  • The dose for children must be decided by a doctor. It is based on body weight. The standard dose is 2 to 6 mg per kg of body weight when injected into a muscle. If injected into a vein, this dose is 50 mg. Additional small doses can be given if necessary.

Taking pentobarbital by injection before surgery:

  • Adults can take 150 to 200 mg. This should be injected into a muscle.
  • The dose for children must be decided by a doctor. It is based on body weight. The standard dose is 2 to 6 mg per kg of body weight when injected into a muscle and should not be more than 100 mg.

Taking pentobarbital by injection to control seizures:

  • The initial dose for adults is 100 mg injected into a vein. Extra, small doses may be given if required but the dose should be no more than 500 mg.
  • Children should receive the first dose of 50 mg injected into a muscle or vein. Small doses may be additionally given if needed.

Taking pentobarbital by rectal dosage for insomnia:

  • Adults are advised to take 120 to 200 mg, inserted into the rectum at before bed.
  • Children of 12 to 14 years of age are advised to take 60 or 120 mg inserted into the rectum, before bed.
  • Children from five to 12 years of age are advised to take 60 mg inserted into the rectum, before bed.
  • Children one to four years of age should take 30 or 60 mg, inserted into the rectum before bed.
  • Infants of two months to one year of age are advised to take 30 mg inserted into the rectum before sleeping at night.
  • The dose for children under two months of age must be decided by your doctor.

Taking pentobarbital by rectal dosage for daytime sedation:

  • Adults are advised to take 30 mg inserted into the rectum. This should be taken two to four times each day.
  • A child's dose is dependant on body weight and it must be decided by a doctor. The standard dose for children is 2 mg per kg of body weight. This should be inserted into the rectum three times a day.

Taking pentobarbital by rectal dosage for pre-surgery sedation:

  • Children of 12 to 14 years old are advised to take 60 or 120 mg.
  • Children from five to 12 years old are advised to take 60 mg.
  • Children from one to four years of age are advised to take 30 or 60 mg.
  • Infants from two months to one year of age are advised to take 30 mg.
  • The dose for children under two months of age must be decided by your doctor.

Very short release barbiturates

These barbiturates are ultra-short acting and are used in the form of an injection as a way to rapidly induce unconsciousness in patients before a surgical procedure. This is followed by gaseous anesthetics which will maintain the patient's unconscious state. Immediate release barbiturates include thiopental sodium and thiamylal. They will only ever be administered by a doctor or professional healthcare team.

Interactions

Before starting your barbiturate treatment it's important that your doctor is aware of any other medications that you may be taking. For peace of mind, make sure to inform them of any herbal remedies, vitamins or over-the-counter medicines and supplements that you are also taking. The implications that other medications may have with barbiturates can vary from minor to severe, with the following medicines all causing extreme contradictions to your treatment.

Medicines that may seriously affect barbiturates include:

  • Artemether
  • Boceprevir
  • Cobicistat
  • Dasabuvir
  • Elvitegravir
  • Isavuconazonium Sulfate
  • Lopinavir
  • Maraviroc
  • Nisoldipine
  • Ombitasvir
  • Paritaprevir
  • Ranolazine
  • Telaprevir
  • Voriconazole

It is also vital that you communicate any prior illnesses, allergies or sensitivities to your doctor before taking barbiturates. Other medical problems can seriously affect the use of barbiturate medicines. It is of particular importance to make your doctor aware of any history of alcohol or drug abuse, mental expression or hyperactivity. Barbiturates can become an addictive drug and it is important that your doctor is clear as to whether you may become dependent. If you have asthma or any chronic lung disease, type 2 diabetes mellitus, overactive thyroid, anemia, porphyria or kidney disease, it is also important to discuss it with your doctor. In addition to these conditions, higher blood levels of barbiturates can affect interact with liver disease and increase a risk of side effects.

Your dietary and lifestyle factors should be also considered before starting your treatment. Alcohol, smoking and eating certain sugars and salts can exacerbate certain side effects or react with the medication. It is important to discuss the effects of food, alcohol, and tobacco on barbiturates with your healthcare professional, to ensure that your treatment will run as smoothly as possible.

Warnings

It is important that your barbiturate dosage is followed exactly as planned and directed by your doctor. Barbiturates have the potential to become habit-forming, which can result in mental and physical dependency. Signs of any mental or physical dependence to barbituates include mood swings, depression, slurred speech, sluggishness, a slowed heart pulse and dilated pupils. If you do suspect that you may be dependant on barbiturates, it is important that you make an appointment with your doctor but continue taking your medication as advised in the meantime. Never suddenly stop taking your medication as this can cause severe withdrawal symptoms that can be fatal.

Because of the potential to become dependent on barbiturates, your doctor will want to make sure that you are given the lowest dose possible that will result in the best effects on your condition. You should never take any more of your dose than needed, at more regular intervals than required. Once your treatment has ended, it is also important that you do not use it for any longer and it is advised that you throw away any remaining medication.

For patients who are taking barbiturates for epilepsy, the medication must be taken daily and in regularly spaced doses as decided by your doctor. This will ensure that it will control your seizures by maintaining a continual amount of barbiturates in your blood. This amount must be kept constant so it is important that you do not miss any doses.

Heavy users of this medication are much more prone to side effects and long-lasting damage from barbiturates. Amongst reactions that include weight loss, muscle weakness, and bone pain, heavy users have a greater chance of contracting bronchitis, pneumonia, and hypothermia. This is because barbiturates cause the cough reflex to become suppressed.

For pregnant women, barbiturates pose the threat of causing a newborn baby to have barbiturate withdrawal symptoms. This applies to regular users of barbiturates as well as patients undergoing new treatment. If you are expecting or pregnant, make sure to discuss the effects of barbiturate on an unborn child with your doctor. He may reduce your dose or suggest an alternative medication whilst you are pregnant.

Storage

As with all medication, it is important that you keep barbiturates in a safe, secure area that children and vulnerable adults cannot access. With the exception of suppositories, this medicine should always be kept in a closed container at room temperature, away from direct heat, moisture, sunlight and freezing conditions.

When storing the suppository form of barbiturates, make sure to keep it a closed container in the refrigerator.

You must always make sure that you dispose of barbiturates once they reach their expiry date. This can help to prevent dependency as well as any dangerous reactions that the out of date medication may cause. If you suspect that your tablets have been damaged or tampered with, dispose of them immediately and consult your doctor.

Summary

With successful use, barbiturates have the ability to give those with epilepsy or seizure disorders a seizure free or drastically reduced life. This can hugely affect a person, giving them the opportunity to work, exercise and experience activities that they were unable to partake in before. It can also give patients with insomnia or who require sedation effective, controlled treatment. When used correctly, it can be either a short or long-term treatment that can contribute to a happier and healthier life.

However, barbiturates can cause some unpleasant side effects that many long-term users are likely to experience. It is a drug that has a chance to become habitual for regular users, causing a mental and physical dependence. Alongside this, withdrawal symptoms such as anxiety, irritability, insomnia, faintness, and sickness are likely in those who have been taking barbiturates for an extended period of time. For this reason, patients who have previous a history of alcohol and drug abuse may need extra monitoring or an alternate medication to barbiturates. It is also important that patients who are self-administering the medication must maintain good communication and total transparency with your doctor. Be prepared to have regular visits and checkups as well as making changes to your lifestyle and diet. It is also essential that you follow your doctor's orders exactly, and never alter or suddenly stop a dose. This will all contribute to your treatment being the best that it can be and cause the least impact on your life.

Aside from its more long-term uses, it is an effective and rapid-acting sedative, commonly used before surgical procedures. When used in this circumstance, the chances of experiencing adverse or negative effects such as dependence or withdrawal are highly unlikely.

For those who have pre-existing conditions or diseases, or who are currently on other medications, it is vital that you discuss them with your healthcare professional. Barbiturates can have some severe interactions with other medications or illnesses and it in some circumstances, an alternative medicine may be recommended. For those with kidney or liver disease, type 2 diabetes, porphyria or an underactive adrenal gland, it is particularly important that you consult your doctor. It is likely that they will provide extra tests and appointments during your treatment, as these illnesses can all have severe implications.

To achieve the best results possible from barbiturates, they require lots of commitment and responsibility. You must be diligent with your dosage schedule and mindful of any side effects or feelings of dependency. A strong link to communication between your doctor and you is hugely important, as these side effects and reactions will need to be closely monitored.

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Last Reviewed:
December 24, 2017
Last Updated:
May 03, 2018
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