Butalbital: Side Effects, High, Addiction, And Abuse

butalbital medication

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Butalbital is a pain reliever used in various prescription medications. However, many users do not really know what butalbital is. Before taking the medication, it is important that patients know as much as they can about the butalbital drug.

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Table of Contents

What Is Butalbital?

Butalbital technically is its own medication. For many years, it was sold on its own in pill form. It is barbiturate, and during the time it was available as a single agent, many observed problems with it and began to question how safe it was to use.

Now, the medication is no longer sold on its own in the United States. Without other drugs to rely on, it is seen as being too toxic. The FDA only approves its use as an ingredient in combination medications, not as a single agent.

Butalbital Brand Names

Because the drug is not sold on its own, its brand names refer to the combination drugs that include it. There is no generic butalbital.

Combination medications containing the drug include:

  • Butalbital and acetaminophen (paracetamol) (trade names: Axocet, Bucet, Bupap, Cephadyn, Dolgic, Phrenilin,Forte, Sedapap)
  • Butalbital, paracetamol (acetaminophen), and caffeine (trade names: Fioricet, Esgic, Esgic-Plus)
  • Butalbital and aspirin (trade name: Axotal)
  • Butalbital, aspirin, and caffeine (trade names: Fiorinal, Fiormor, Fiortal, Fortabs, Laniroif)
  • Butalbital, paracetamol (acetaminophen), caffeine, and codeine phosphate (trade name: Fioricet#3 with Codeine)
  • Butalbital, aspirin, caffeine, and codeine phosphate (trade name: Fiorinal#3 with Codeine)
  • Ergotamine tartrate, caffeine, butalbital, belladonna alkaloids (trade name: Cafergot-PB)
Any medication that contains the drug is a prescription medicine. Butalbital without a prescription cannot be accessed legally.

Butalbital Drug Class

Key to understanding what butalbital grounds in knowing its drug class. Most people only know the medication as a pain reliever and are unable to clarify its classification. However, knowing how the drug is classified reveals a lot about how it works and the dangers it carries.

Is Butalbital A Narcotic?

Narcotics are substances derived in some manner from the opium plant. They may be opium itself, derived from opium, or synthetic substances engineered to mimic opium. The medicine is not derived from opium in any manner, and this is not a narcotic.

Is Butalbital A Controlled Substance?

Butalbital is a controlled substance, according to the DEA. It is classified as a Schedule III drug. This means that it has therapeutic benefits, but also the potential for abuse and addiction. However, this potential for negative results is less than those in Schedule I and II. However, the butalbital schedule should be taken into consideration when prescribing a medication containing it.

butalbital drug class

Is Butalbital An Opiate?

Opiates are medications that produce effects in the body through their interaction with opiate receptors. This is not how medicine works. As such, it is not considered an opiate.

Is Butalbital A Barbiturate?

Barbiturate is a central nervous system depressant class of medications. These medicines have sedative, hypnotic, and anesthetic effects. These medications fall under this umbrella due to how the drug interacts with the central nervous system. This means that it is a barbiturate.

What Is Butalbital Used For?

Medications with the drug are used to address pain. Exact butalbital uses can vary depending on what medications iis combined with.

For example, with acetaminophen and caffeine, people may use butalbital for headaches, but when combined with codeine, it treats more severe pain.

The most common application is butalbital for migraines. For this, it is highly effective, but doctors prefer to avoid it due to potential toxicity. In some cases, it may also be used for reducing general muscle tension and for sedation, but given the availability of alternative medications, this is rare.

Butalbital Dosage

Given that the medication is no longer sold as a single agent, there are no standards for dosage. Combination medications will include varying amounts of the other active ingredients; however,  butalbital 50 mg is a standard dose of the medication in each combination. The prescribing doctor will determine how many pills the user should take.

Of course, there is a limit to how much of the medicine can be taken. The butalbital LD50 is 160 mg per kilo in rats. There are no human trials available.

Assuming the same is true for humans, an adult weighing 70 kilos would need to take 11,200 mg of the medication to overdose. However, this only accounts for the pure form of the medication. Given that the drug is always combined with other drugs, the LD50 is going to be significantly lower than 11,200 mg.

Butalbital Overdose

Butalbital overdose can occur if someone takes too much of a drug containing the medication or if they mix it with contraindicated substances. Anyone taking the medication needs to know what signs to look for that signal a problem.

Symptoms of overdose include:

  • confusion
  • poor judgment
  • slow speech
  • slurred speech
  • extreme drowsiness
  • sluggishness or hyporeflexia
  • struggles with movement
  • difficulty balancing
  • respiratory depression
  • high blood pressure
  • bradycardia
  • hypovolemic shock
  • hypothermia
  • limp muscles
  • apnea
  • coma
Anyone exhibiting these symptoms needs immediate medical attention. 911 should be called, and the people with the overdose victim should remain nearby in case they are needed.

Butalbital Side Effects

Even if someone takes the medication correctly, things can go wrong. The side effects of butalbital range from the minor to the severe. Users need to know what side effects are possible so they can look out for them.

Common Side Effects

The most commonly observed side effects range from minor to severe, including:

  • drowsiness
  • lightheadedness
  • dizziness
  • sedation
  • nausea
  • a sensation of being intoxicated
  • shortness of breath (severe)
  • vomiting (severe)
  • abdominal pain (severe)

butalbital side effects

Rare Side Effects

Less frequent but still concerning side effects include:

  • headaches
  • shakiness
  • tingling
  • agitation
  • fainting
  • fatigue
  • droopy eyelids
  • bursts of energy
  • hot flashes
  • numbness
  • seizure
  • confusion
  • excitement
  • depression
  • dry mouth
  • hyperhidrosis
  • difficulty swallowing
  • acid reflux
  • gas
  • constipation
  • tachycardia
  • leg pain
  • muscle fatigue
  • diuresis
  • pruritus
  • fever
  • earache
  • nasal congestion
  • tinnitus
  • euphoria
  • allergic reactions
  • dermatological reactions

Butalbital And Pregnancy

Pregnant women often experience headaches, and as such, many wonder about the possibility of using butalbital in pregnancy. It is important that women understand how the medication is classified for pregnancy.

The pregnancy category of the medication is C. This means that it has been found to cause adverse effects in studies on pregnant animals, but its effects in human pregnancies have either not been studied, or the studies are not comprehensive enough to be used to make a concrete ruling.

With that said, infants can be born dependent on barbiturates. This means that any mother taking the drug while pregnant is risking her child going through withdrawal after birth. This is bad enough on its own, but it is not the only risk. It has also been found to increase the risk of certain birth defects.

Additionally, the medications combined with butalbital can cause problems, too. Altogether, this means butalbital is not safe during pregnancy.

Butalbital Mechanism Of Action

What butalbital does comes down to its mechanism of action, or how it works on the body. The drug binds at the GABAA receptor binding site associated with a Cl- ionophore. This then creates the effects of the drug, both those that are therapeutic and those that are considered side effects.

How long it takes for butalbital to work varies, but in general, it will kick in within 30 minutes and last for about four hours. Users should never take the medication more frequently than directed.

butalbital mechanism of action

How Long Does It Stay In One’s System?

The question of how long butalbital works for is different than the question of how long it remains in the system. Drugs that work for just an hour or less can remain in the body in metabolite form for weeks. Users need to know how long the medication will remain in their system.

Butalbital Half-Life

The half-life of the butalbital drug is 35 hours—significantly longer than the four hours that most users will be able to feel its effects. At this point, the presence of the drug in the plasma is half its original concentration in the majority of patients. However, the drug will remain detectable for much longer.

Does Butalbital Show Up On A Drug Test?

Anyone undergoing a butalbital drug test will test positive if they have used the drug within a certain time period. The length of this detectable period will depend on the type of sample being tested. Urine, oral fluid, blood, and hair tests can reveal use.

Detectability on various drug tests:

  • How long butalbital stays in the urine is approximately seven days.
  • Saliva testing can detect it for 48 to 52 hours.
  • How long butalbital stays in the blood is generally about three days.
  • When testing hair, it can be detected for up to three months.

Is Butalbital Addictive?

Butalbital is an addictive medication. Additionally, many of the medications it is combined with are addictive as well. This comes together to make it easy for people using it for legitimate purposes to become dependent upon medicine.

The drug can be found sold on the street and used recreationally, but this is not the typical path to addiction. Most addicts come to their addiction through prescription use, finding their bodies withdrawing from it when it is not used and their minds desiring its effects.

Recreational use of a drug is illegal being determined as abuse. Also, buying butalbital in unauthorized sourses is unsafe, as well as legally prosecuted.

Signs that butalbital addiction is developing include: 

  • engaging in risky behavior to access the drug
  • changes in appearance after being on the drug for a while
  • less interest in activities they once enjoyed
  • performance at work or in hobbies may deteriorate
  • memory loss
  • confusion
  • hostility
  • aggression
  • lying to doctors to obtain the medicine
  • mixing their medication with other substances to increase the high felt
  • running out of their prescription early
  • isolating themselves
  • stealing money
  • stealing medications
Anyone exhibiting these signs or those who notice these changes in their friends, loved ones, or family members need to seek drug addiction treatment as soon as possible.

Butalbital Abuse

When people engage in butalbital abuse, there are generally two ways it is done. The first is to take the medication containing it in large doses.

The other way to abuse the medication is to take it in a relatively small dose but mix it with other substances. This can be done to increase the high experienced or to counteract other drugs taken—for example, bringing them down from a stimulant.

Both methods of abusing butalbital are very dangerous, given the toxicity of the drug.

butalbital high

Butalbital High

While the path that leads people to abuse can vary, the driving factor that keeps them abusing it is the butalbital high. When a user takes a butalbital recreational dose, they can experience a euphoria that is intense and not unlike that delivered by many street drugs.

Characteristics of this high include: 

  • A reduction in anxiety, possibly causing it to vanish completely.
  • Severe drowsiness that can leave the person feeling as though they are unable or unwilling to move.
  • Intense relaxation of the body and mind.
  • A sense of euphoria caused by the way the medication interacts with the GABAA receptors.
  •  Extreme lightheadedness that can leave the user feeling like they are floating.
  • A general sense of wellbeing.
  • Numbness, especially in the extremities.
  • Hallucinations.
  • Loss of motor control.
Ultimately, the drug can get one high, but the risks are not worth the perceived benefits.

Butalbital Withdrawal

When someone becomes physically addicted to the medication, they will go through butalbital withdrawal when they stop taking it. For some users, experiencing this may be the first sign they have that they are addicted, assuming they are not using the medication recreationally.

Withdrawal symptoms include:

  • fever
  • high blood pressure
  • changes in heart rate and rhythm
  • changes in respiration
  • delirium
  • vomiting
  • shaking
  • tinnitus
  • breathing struggles
  • drowsiness
  • a sense of increased awareness
  • anxiety
  • disorientation
  • severe headaches
  • seizures
  • disturbed vital signs

Users who are addicted can expect to begin experiencing symptoms within 36 hours of their last dose of butalbital. These symptoms tend to go away in about two weeks, but due to their risks, treatment at a rehabilitation center is required.

Butalbital Interactions

Part of what makes this medication so dangerous are the numerous butalbital drug interactions. On its own, there is a fine line between therapeutic and toxic doses. When combined with the wrong substances, butalbital interactions arise and can be deadly.

butalbital and alcohol

Butalbital And Alcohol

People taking the medication should not drink alcohol. The butalbital and alcohol interaction can be severe, even deadly. Both substances are depressants. This means they slow and reduce the function of the central nervous system. Since the CNS is responsible for things like keeping the heart beating and the lungs breathing, heavily depressing this system can cause severe complications, including death.

Butalbital And Hydrocodone

Much like with alcohol, mixing hydrocodone with the medication is risky since the medications both depress the CNS. Depressed breathing is the biggest risk of this combination. Users who take both medications may stop being able to breathe on their own and could fall into a coma or die as a result.

Butalbital And Tramadol

Many people believe that tramadol is a safe narcotic because it is synthetic. However, it remains a CNS depressant like other narcotics. This means that if mixed with butalbital, it could depress the CNS to the point that vital functions become impaired or cease, causing coma or death.

Other Drug Interactions

Major drug interactions include:

    • Alfentanil
    • Anisindione
    • Buprenorphine
    • Butorphanol
    • Codeine
    • Dezocine
    • Dicumarol
    • Ethanol
    • Fentanyl
    • Hemin

Moderate drug interactions include:

Minor drug interactions include:

  • Dolutegravir
  • Fenoprofen
  • Fluoxetine
  • Levobupivacaine
  • Lidocaine

Buying Butalbital

No pure form of the medicine is manufactured. This means that determining the cost of the medication depends on which combination the user needs. It is possible to buy butalbital online from reputable pharmacies. It is also sold illegally online and on the street.

One should not seek for butalbital on the streets as it is illegal and implies additional health risks.

buy butalbital online

The cheapest formulation offered is with acetaminophen. This can cost as little as 21 dollars for 30 pills from a legitimate pharmacy. When combined with aspirin alone, the butalbital price rises just a dollar. However, once combined with codeine, pills jump to 32 dollars for 30 tablets at the cheapest.

Butalbital value off-pharmacy varies widely. The most expensive version is with codeine as it combines two addictive substances. These can cost as much as $30 a pill. Combinations with just aspirin or acetaminophen can be as little as $5 a pill.

Ending Butalbital Addiction

Anyone who is abusing the drug needs to seek help. Due to the toxicity of the medication and its numerous interactions, the risk of death is high. Drug rehabilitation centers can help addicts detox and learn the skills needed to stay clean.

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View Sources
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  3. Browne M. L. et al. Maternal Butalbital Use and Selected Defects in the NationalBirth Defects Prevention Study. Headache. 2013. https://www.health.ny.gov/diseases/congenital_malformations/docs/meds2.pdf.
  4. The U.S. National Library of Medicine. Compound Summary: Butalbital. https://pubchem.ncbi.nlm.nih.gov/compound/Butalbital.
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