Butalbital Withdrawal, Side Effects, Overdose, And Addiction Risks

Last Updated: May 5, 2021

Authored by Sharon Levy, MD, MPH

Reviewed by Michael Espelin APRN

What Is Butalbital?

Butalbital is synonymous with Itobarbital and Allylbarbital. Remedies with the combination acetaminophen, Butalbital, and mixtures of caffeine are often used to relieve muscular tension and pains; however, the habit-forming characteristics, risks of Butalbital overdose abuse put this drug on the controlled substances list.

So, what is Butalbital? The Butalbital drug belongs to a class of drugs known as barbiturates. It is also a sedative/ hypnotics and functions as a tension relaxer, used to treat severe headaches and pains. Butalbital as a single medication has been discontinued due to its withdrawal effects. It is used in combination with acetaminophen as Fioricet and with acetylsalicylic acid as Fiorinal.

The medication is no longer sold on its own in the United States. Without other medicine to rely on, it was considered too toxic.

Butalbital Preparations

Because the medicine is not sold on its own, its brand names refer to the combination that includes it. There are no generic versions available.

Combination Medications Containing Itobarbital Include:

 

Butalbital Preparations

Combinations Trade Names
Butalbital, Acetaminophen (Paracetamol) Axocet, Bucet, Bupap, Cephadyn, Dolgic,
Phrenilin, Forte, Sedapap.
Butalbital, Paracetamol (acetaminophen, and caffeine) Fioricet, Esgic, Esgic plus
Butalbital and aspirin Axotal
Butalbital, aspirin, and caffeine Fiorinal, Fiormor, Fiortal, Fortabs, Laniroif)
Butalbital, paracetamol  (acetaminophen),
caffeine, and codeine phosphate
Fioricet#3 with Codeine
Butalbital, aspirin, caffeine, and codeine phosphate  Fiorinal#3 with Codeine
Ergotamine tartrate, caffeine, butalbital,
belladonna alkaloids
Cafergot-PB

Butalbital Drug Class

Key to understanding what Itobarbital grounds are 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 medicine is classified reveals how it works and the dangers it carries.

Is Butalbital A Barbiturate?

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

Is Butalbital A Controlled Substance?

Itobarbital 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. Itobarbital schedule should be taken into consideration when prescribing a combination containing it.

What Is Butalbital Used For?

Medicines containing Itobarbital are used for the treatment of pain. Exact Itobarbital uses can vary depending on what meds it is combined with. For example, butalbital-acetaminophen-caffeine may be used for headaches, but when combined with codeine, it treats severe pain.

The most common application is Itobarbital for migraines. It is highly effective, but at the same time, doctors prefer to avoid it due to potential toxicity. It may also be used to reduce general muscle tension and sedation, but given the availability of alternative meds, this is rare.

Studies have shown that compounds containing Itobarbital have been effective in placebo-controlled trials in patients suffering from tension-related headaches. As a barbiturate, butalbital drug can produce intoxicating effects similar to alcohol consumption, including hangover, toxicity, and dependency.

Using butalbital-containing medicine for treatment in higher dosages can cause Butalbital withdrawal symptoms; hence the meds should only be used as a last resort when other medications are seen to be ineffective.

Young man calling for Butalbital overdose help.

Butalbital Overdose

Butalbital overdose can occur if someone takes too much of the meds or if they mix it with contraindicated substances. Anyone taking this medicine needs to know what signs to look for to signal the problem.
Symptoms of Butalbital 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. The first line of action is to dial an immediate response medical emergency unit or 911. Further information from individuals who were present at the scene may go a long way in saving the patient’s life.

Butalbital Side Effects

It is imperative to note that there may be a few health-impairing Butalbital side effects. While the medicine exists in combination with other meds such as acetaminophen, and others the possibilities of both common and rare side effects are significant due to different factors.

Butalbital drug often presents with health problems that impair the functions of the central nervous system (CNS). This is a problem as it affects every system controlled by the CNS, such as cognitive abilities, poor motor coordination, speech problem, and other deficiencies that can lead to loss of lives and properties. Here are some common butalbital side effects.

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)

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

Allergy to Butalbital

Severe allergic reaction to Itobarbital is quite rare, but some forms of an allergic reaction may occur due to physiological differences. Possible symptoms of allergic reactions may include itching, rashes, trouble breathing, swelling of body parts such as tongue, face, or throat, as well as dizziness.

Allergies may present themselves in many order ways, so adequate attention should be paid when using the medicament. One must seek immediate medical help once an allergic symptom is noticed to avoid deterioration.

Butalbital And Pregnancy

Various scientific research has been conducted over the years to determine the possible health defects of the medicine on pregnant women as well as their children in the long run. Of the mothers who admitted to periconceptional use of the medicine, a significant number experienced congenital heart problems, pulmonary valve stenosis, as well as atrial septal defects. There were close relationships between maternal use of the barbiturate and congenital heart defects. Even though the number of cases is not so much, further research is ongoing to concretize these findings. If these cases are found to be consistent in each study, then they can be treated as certified risks that must be averted during the administration of medicine.

Pregnant woman asks her doctor. about butalbital

Butalbital Mechanism Of Action

After oral ingestion of the barbiturate, it undergoes complete metabolism leading to renal excretion. The oxidation and hydroxylation processes yield two different forms of barbituric acids. The barbiturate effects mirror the inhibitory effects of GABA (gamma-aminobutyric acid). It does this by binding to a different site from the typical benzodiazepine site located on the GABA receptor. Consequently, this improves GABA inhibitory effects leading to certain physiological reactions such as sedation, respiratory depression, lowered anxiety, hypnosis, and increased risk of dependency.

The period of how long it takes for Itobarbital to work varies, but in general, and it will kick in within 30 minutes and last for about 4 hours.

How Long Does Butalbital Stay In Your System?

It is important to understand how long the substance remains detectable in one’s system for various reasons. Asides from the possibility of reaction with other medicines, there are other scenarios such as drug tests and the likes. Since various barbiturates have different detection windows, a closer look at the detection window for Itobarbital medicine is necessary.

Butalbital Half-Life

The half-life of Itobarbital is 35 hours. At this point, the presence of the barbiturate in plasma is half its original concentration in the majority of patients. However, the medicine will remain detectable for much longer.

Does Butalbital Show Up On A Drug Test?

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

Detectability on Various Tests:

  • Itobarbital stays in the urine for approximately seven days.
  • Saliva testing can detect it for 48 to 52 hours.
  • How long Itobarbital stays in the blood is generally about three days.
  • It can be detected for up to three months with a hair test.

Is Butalbital Addictive?

Itobarbital is an addictive medicine. Additionally, many of the meds 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 on this medicine.

Recreational use of the medicine is prohibited from being determined as abuse. Also, buying Itobarbital from unauthorized sources is unsafe, as well as legally prosecutable.

American Headache Society states that at least 2% of the U.S population is suffering from some form of chronic migraine. One-third of them abuses migraine meds, especially those that contain codeine.

The critical dose of exposure for opioids is about eight days in a month, after which the risk of dependency and addiction due to continued exposure becomes extremely high.

Butalbital Addiction Signs

Signs that Itobarbital addiction is developing include:

  • engaging in risky behavior to access the medicine
  • changes in appearance after being on the meds 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 meds with other substances to increase the high felt
  • running out of their prescription early
  • isolating themselves
  • stealing money
  • stealing meds

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 Withdrawal

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

Individuals who engage with frequent butalbital use, as much as 4 to 6 weeks or even longer, are almost sure to develop Butalbital withdrawal symptoms to the medicine. The longer one uses this medicine, the more severe withdrawal symptoms they’d experience.

Butalbital Withdrawal Symptoms

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.

Itobarbital 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 headache
  • seizures
  • disturbed vital signs
  • hallucinations

Butalbital Withdrawal Timeline

The acute phase may begin within an hour of discontinuation and last for up to 2 or 3 days. The timeline is largely dependent on the level of abuse of the individual involved. The addict would experience cravings and would seek the medicine to reduce the effects of withdrawal. Seizures, hallucinations, and disorientation are signs of complications and extreme danger, which could be fatal.

Some withdrawal phases may last up to 7 days and then become less intense. Cravings may continue even after this phase. Possible long-term issues may include stress sensitivity, lack of motivation, depression, anxiety, and desire to use the meds.

Butalbital Interactions

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

Butalbital And Alcohol

Butalbital and alcohol mixture is quite harmful. People taking this medicine should not drink alcohol. Both substances are depressants. This means they slow and reduces the function of the central nervous system. Since the CNS is responsible for keeping the heart beating and the lungs breathing, heavily depressing, this system can cause severe complications, including death.

Reports have shown that the medicine presents with hangover effects and produces a feeling of intoxication similar to that of alcohol. When used together with alcohol, the feeling of intoxication is extremely and dangerously heightened. The result is complete disorientation, inability to function, and even possible death.

Butalbital And Tobacco

Using the medicine with nicotine may be accidental and unintended in many cases, so it is advised to use with caution as interactions between both substances can increase the risk of Butalbital side effects. Tobacco may react with acetaminophen in the medicine, reducing its effectiveness and putting a strain on the liver. There is a potential risk of generating acetaminophen’s hepato-toxic metabolite known as NAPQI. The metabolite may lead to liver failure, acetaminophen overdose, and possibly death.

Butalbital And Hydrocodone

Much like with alcohol, mixing hydrocodone with this medicine is risky since both meds depress the CNS. Depressed breathing is the biggest risk of this combination. Users who take both may have breathing difficulties 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 medicine interactions include:

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

Moderate medicine interactions include:

Minor medicine interactions include:

  • Dolutegravir
  • Fenoprofen
  • Fluoxetine
  • Levobupivacaine
  • Lidocaine

Ending Butalbital Addiction

Itobarbital is a schedule III medicine with a high potential of dependency. Its withdrawal symptoms are very unpleasant. Hence it is medically inadvisable to stop using it abruptly if you have been on the medicine. Typically, a medical center would only recommend this medicine if other medications such as benzodiazepine have been unable to bring relief to the patient. However, caution must be taken while using this medicine. One must adhere strictly to the recommended dose and report to the doctor if one notices butalbital side effects or experiences withdrawal symptoms. Ensure to avoid the medicine when pregnant, and do not use it concomitantly with any other medicament or substance that may affect the CNS. Contact a medical facility for more recovery information.

Treatment and recovery options are available for both inpatient and outpatient rehab centers. An inpatient program may take 28 to 90 days, depending on the severity of the case. There are extended programs for exceptional cases as well.

Rehab Care Programs Consist of the Following:

After rehab care, one can enroll in a support group such as Narcotics Anonymous (NA) to help deal with the challenges that come with cravings and triggers over time.

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Page Sources

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Published on: July 4th, 2019

Updated on: May 5th, 2021

About Author

Sharon Levy, MD, MPH

After successful graduation from Boston University, MA, Sharon gained a Master’s degree in Public Health. Since then, Sharon devoted herself entirely to the medical niche. Sharon Levy is also a certified addiction recovery coach.

Medically Reviewed by

Michael Espelin APRN

8 years of nursing experience in wide variety of behavioral and addition settings that include adult inpatient and outpatient mental health services with substance use disorders, and geriatric long-term care and hospice care.  He has a particular interest in psychopharmacology, nutritional psychiatry, and alternative treatment options involving particular vitamins, dietary supplements, and administering auricular acupuncture.