Barbiturates: Uses, common brands, and safety info

Barbiturates have been used in clinical medicine for more than 100 years. Their use has become quite limited in recent decades due to concerns related to side effects and the potential for abuse. Currently, barbiturates are primarily prescribed for seizure disorders and tension headaches, often in cases when either medical problem has not been adequately controlled by safer options. This guide includes a list of the most prescribed barbiturates and information about their safety and costs. 

Other barbiturates

• Nembutal (pentobarbital) is used for seizure treatment and sedation in hospital settings.

• Brevital (methohexital) and Amytal (amobarbital) are used for sedation in the hospital.

• Seconal (secobarbital) is used to calm patients before surgery.

What are barbiturates?

Barbiturates are a class of drugs, based on the parent compound barbituric acid and used for a limited number of neurologic conditions. They are considered sedatives or depressants, and this property explains some of their typical uses as well as their adverse effects. These central nervous system (CNS) depressants were used for psychiatric conditions throughout much of the early and mid 20th century. This usage was curtailed when problems with patients becoming dependent on barbiturates became widely known. These drugs can be abused for their sedative-hypnotic effects, which has further reduced prescriptions for them.

How do barbiturates work?

Barbiturates work by quieting the activity of nerve cells in the brain by binding to the receptor for and increasing the action of the brain neurotransmitter GABA. Nerve cells function by sending electrical signals to one another, and barbiturates decrease the electrical functioning of these cells. Consequently, these drugs may be carefully used for conditions when nerve cells are overactive, such as epilepsy, and times when reduced brain activity is useful, such as during surgical sedation. While they can be very effective, the challenge with barbiturates is that the dosage that may have a beneficial effect is often close to the dosage that may have a dangerous effect, and depending on what other medications or health conditions an individual has, those dosages may be difficult to predict.

What are barbiturates used for?

• Epilepsy: Phenobarbital can serve as a long-acting anticonvulsant for both generalized and focal seizures. Pentobarbital can serve as a short-acting anticonvulsant in the hospital setting.

• Tension headache: Butalbital compounds can be used for this indication.

• Surgical anesthetic and critical care sedation: Pentobarbital and methohexital have been used in this way.

• Reducing drug withdrawal symptoms in the hospital setting: Phenobarbital is used uncommonly for this purpose.

Who can take barbiturates?

Adults: Adults can be prescribed these medications for short-term and long-term treatment of seizures and tension headaches.

Seniors: While older adults can be prescribed these medications as well, barbiturates are listed as one of the highest risk medicines for this age group. The concern centers around a heightened risk of side effects. The 2019 American Geriatric Society Beers Criteria for older adults cites greater concerns for physical dependence, tolerance of sleep effects, and overdosage. 

Children: Children with seizures can be prescribed barbiturates. Hyperactivity side effects are a particular concern for children. The use of these medications for children with tension headaches is typically avoided. Newborns withdrawing from opiates or other drugs may be given phenobarbital in the hospital.

Females of reproductive age: Women who have the potential for pregnancy are typically counseled regarding the need for contraception while taking barbiturates or prescribed an alternative medication.

Are barbiturates safe?

Barbiturates have an array of possible hazards with their use, including both short-term and long-term toxicity. Their safe utilization requires careful consideration of the person’s unique health characteristics including age, other health conditions, and other medication.

When phenobarbital is being taken, blood tests are monitored regularly. Phenobarbital levels in the blood are checked to determine if the dosing needs to be adjusted. Blood cell counts, liver tests, and kidney tests are checked to look for side effects and problematic coinciding health conditions. In some cases of butalbital usage, blood tests are also done to monitor for these side effects.

Misuse, withdrawal, and overdose

Barbiturates can be abused. Historically, barbiturate abuse has been widespread enough to gain Seconal (secobarbital) and Nembutal (pentobarbital) the street names “red devils” and “yellow jackets.” These depressant and hypnotic drugs are also known as “downers” and “goofballs.”

If barbiturates are taken regularly and then suddenly stopped, dangerous withdrawal symptoms such as seizures may occur. Healthcare providers might recommend a gradual taper off of the drug.

Barbiturate overdose can be deadly, based on its action as a depressant to the respiratory and cardiovascular systems.

Interactions

Barbiturates interact with a long list of other drugs due to their metabolism in the liver. In the setting of taking barbiturates and other drugs, some medication effects may be heightened while others are dampened. Any medicine that causes tiredness or sedation (e.g. benzodiazepines, opioids, and sleeping pills), as well as illicit drugs and alcohol, can be particularly dangerous if taken along with a barbiturate. The combined sedative effects could produce a life-threatening reduction in breathing.

Based on their tendency to reduce calcium and vitamin D levels, barbiturates can cause the weakening of bones when used for an extended time. In these situations, healthcare providers may recommend an increased intake of calcium and vitamin D.

Warnings

Butalbital is one of the numerous medications that are included in combination tablets with acetaminophen, a medicine that contains a black box warning from the FDA for the potential for liver failure with overdosage. Numerous common cough and cold medications are other examples of combination medicines that include acetaminophen. Tylenol (acetaminophen) accidental overdose can occur when an individual takes Tylenol along with other products that contain acetaminophen, such as the barbiturate butalbital combination tablets like Fioricet and Esgic.

Barbiturate recalls

• Animal and veterinary forms of phenobarbital and combination phenobarbital/amitriptyline (2/8/2018)

RELATED: How to treat seizures in dogs

Barbiturate restrictions

• These medications are not to be taken by individuals with a prior history of allergic reactions to barbiturates or other components of the pills. They are also to be avoided by anyone with severe liver disorders, difficulty breathing, and porphyria.

• Particular caution is needed in patients with any of the following conditions:

  • Liver problems

  • Kidney problems

  • Heart problems

  • Anemia

  • Overactive thyroid

  • Reduced mental alertness

  • Depression

  • Diabetes

  • Underactive adrenal glands

  • History of drug abuse

  • Heavy alcohol use

• Females with the potential for pregnancy as well as older adults are often warned against the use of barbiturates.

Can you take barbiturates when pregnant or breastfeeding?

In pregnancy, barbiturates can cause harm to the fetus. Accordingly, alternative medications are typically sought. In certain circumstances when no acceptable alternative exists and the risks are deemed acceptable by the healthcare provider and patient, the medical advice might be to continue the barbiturate drug.

Breastfeeding mothers should be aware that barbiturates can be found in the breast milk of mothers who take these medications. This may pose risks to the baby including sedation. A baby exposed long-term to barbiturates in breast milk could experience withdrawal symptoms if the mother suddenly stops taking the barbiturate medication.

Are barbiturates controlled substances?

Yes, most barbiturate formulations are controlled substances.

• Secobarbital and pentobarbital, and DEA Schedule II drugs.

• Butalbital is most often a DEA Schedule III drug, depending on the combination form.

• Phenobarbital and methohexital are DEA Schedule IV drugs. 

Common side effects of barbiturates

• Nausea, vomiting, or constipation

• Reduced bone density with chronic use

• Hyperactivity, particularly in children

• Rash or hives

• Pain

• Swelling

• Sleep disturbance

• Dizziness

• Headache

• Sun sensitivity

• Side effects of drugs that come in combination with barbiturates should be noted, including acetaminophen, caffeine, aspirin, and codeine

Serious side effects of barbiturates

• Drowsiness or lethargy

• Joint, tendon, or skin damage

• Respiratory depression (reduced breathing)

• Blood cell disorders

• Suicidal thoughts

• Depression

• Porphyria exacerbation

• Blood clot

• Liver damage

• Physical dependence on the medication

• Withdrawal if abruptly stopped after chronic use

• Reduced heart rate or blood pressure, particularly with intravenous use

• Allergic reactions, potentially severe such as Stevens-Johnson Syndrome

• Confusion or hallucination

• Fainting

How much do barbiturates cost?

Phenobarbital is currently available only as a generic drug, and its average cash price is typically about $56. Medicare Part D and Medicare Advantage cover this medicine. The cost will vary with insurance coverage. Coupons for phenobarbital are available from SingleCare. When using SingleCare, you may pay less than $20 for phenobarbital.

The various combinations containing butalbital are available in generic and brand-name forms and usually cost between $42 and $437. Some Medicare and health insurance drug plans may cover butalbital medications. SingleCare offers coupons for Fioricet, Esgic, Bac, Zebutal, Vtol LQ, and generic formulations of butalbital to assist in finding an affordable price. You can get a discount of up to 80% with SingleCare.  The free SingleCare prescription discount card can also assist with savings for thousands of other prescription drugs.