What Is Butalbital-Acetaminophen-Caffeine Used For?
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Butalbital-Acetaminophen-Caffeine - Uses, Dosage, Side Effects, Drug Warnings, and Precautions

Published on Oct 13, 2022 and last reviewed on Jul 06, 2023   -  7 min read


Butalbital-Acetaminophen-Caffeine is a combination medication used to treat the symptoms of tension headaches. Read the article to know more.


Butalbital-Acetaminophen-Caffeine is a prescription drug available as an oral tablet, oral capsule, and oral solution. The drug is used to treat tension headaches. Acetaminophen acts as an analgesic (relieves pain), Caffeine strengthens Acetaminophen's pain-relieving effect, and Butalbital provides a sedative effect. Overall, all three drugs in this combination medication prevent the muscular muscle contractions in tension headaches and relieve the pain.

Avoid taking this medicine if on therapy with drugs that come under the monoamine oxidase (MAO) inhibitors, such as Isocarboxazid, Phenelzine, Tranylcypromine, Linezolid, etc. If any symptoms of hypersensitivity (extreme rash, breathing difficulty) or associated symptoms are experienced while on this medication, stop taking it and get emergency medical help.

Drug Group:

The drug group for each of the medications of this combination is as follows:

  • Butalbital- It comes under the class of barbiturates and acts on the central nervous system (brain and spinal cord).

  • Acetaminophen- It is an analgesic (pain-relieving) and antipyretic (brings down temperature).

  • Caffeine- Belongs to the class of drugs called methylxanthines.

What Is Butalbital-Acetaminophen-Caffeine Used For?

The combination of Butalbital-Acetaminophen-Caffeine is widely prescribed for muscular or tension-type headaches.

Tension-Type Headaches- These headaches are characterized by a moderate, aching pain which is commonly described as a sensation of a tight band tied around the head. Muscle contractions are caused by the scalp or the neck. It may be accompanied by photophobia (sensitivity towards light) or increased sensitivity to sound. The common causes include decreased sleep, stress, and psychological factors.

Tension-type headaches are commonly observed in older teens and the adult population. It is more commonly observed to be experienced by women than by men.

How Does Butalbital-Acetaminophen-Caffeine Work?

The exact mechanism by which the combination works is unknown. However, the action of the individual drugs is as follows:

  • Butalbital- It is a barbiturate that acts by mimicking and enhancing the effects of a chemical called gamma-aminobutyric acid (GABA) in the brain. This will result in the relaxing of the muscles, which causes headaches.

  • Acetaminophen- Acetaminophen relieves pain by inhibiting the synthesis of chemicals called prostaglandin in the body, which is associated with inflammation and feeling of pain.

  • Caffeine- Caffeine blocks pain signaling and restricts blood flow to the affected areas, thereby alleviating the pain sensation.

Onset of Action:

All three drugs of this combination are well-absorbed on oral administration, and about 80-90 % reach the blood circulation. The pain-relieving effect of Acetaminophen is reached within 30 minutes to one hour after taking the medication. The sedating effect of Butalbital starts within one to two hours. In short, the symptoms of the headache will be relieved within an hour after the drug is administered, and the effect lasts for about three to four hours.


Butalbital in this drug combination is known to be habit-forming when taken for a long period or in large doses. It can cause mental and physical dependence or addiction. Hence, only take the medication as instructed by your doctor, and do not share this drug with anyone else.

Expiry Date:

Avoid taking this medicine post its exposure date, which will be printed on the back of your drug pack.

What Is the Dosage of Butalbital-Acetaminophen-Caffeine?

For tension-type headaches, the doctor will prescribe the dose as required. Long-term use is not recommended due to the increased risk of dependence. The common dose and dosage forms of the drug are as follows:

  • Oral Capsule- (Acetaminophen- Butalbital- Caffeine) 300 mg-50 mg- 40 mg , 325 mg- 50mg-40 mg.

  • Oral Tablet- (Acetaminophen- Butalbital - Caffeine) 325 mg- 50 mg- 40 mg.

  • Oral Solution- (Acetaminophen - Butalbital - Caffeine) 325 mg/15 ml -50 mg/15 ml -40 mg/15 ml.

The common dosing is as follows:

Dosage of Butalbital-Acetaminophen-Caffeine

The physician will adjust the doses for the elderly and patients with liver and kidney diseases.

How to Use Butalbital-Acetaminophen-Caffeine?

  • Take this medication by mouth with or without food as directed by the doctor, usually every four hours as needed.

  • Abrupt stopping the medicine may result in withdrawal symptoms (such as nausea, vomiting, mood problems, and seizures). The doctor might gradually reduce the dose to help prevent withdrawal. If this medication is taken for a long period or in large doses, withdrawal is more likely to occur. If the withdrawal is experienced, inform the healthcare provider straight away.

  • Inform the physician if there is a worsening of headaches, an increase in the number of headaches, or a decrease in the effectiveness of the medication. Never take more than is advised. The doctor may need to adjust the prescription or add a different drug to stop the headaches.

Missed Dose:

There might not be a dosing regimen because this medication is taken as needed. Use the missed dose as soon as you remember if on a schedule. If it is almost time for the next scheduled dose, skip the missed dose. To make up for a missed dose, do not take double doses.


In case of overdose and usual symptoms arise, seek medical help or contact the nearest poison control center immediately.

What Are the Contraindications of Butalbital-Acetaminophen-Caffeine?

Butalbital-Acetaminophen-Caffeine is contraindicated (use strictly to be avoided) in the following conditions:

  • Allergy to the medication or its components.

  • Porphyria (rare genetic blood disorder).

What Are the Drug Warnings and Precautions?

Inform the physician if any of the following conditions are present:

  1. Allergies- Avoid taking the medication if there is a history of allergy to the drug or any of its components.

  2. Liver Diseases- Notify the doctor if there is a history of liver cirrhosis or drug addiction.

  3. Kidney Diseases- Monitoring of the therapy may be required.

  4. Ulcers or Gastric Bleeding- The medication may worsen the ulcers. Talk to the healthcare professional before using the drug.

  5. Psychiatric Illness- Avoid use in the case of mental illness or a history of mood changes like anxiety, depression, etc.

  6. Elderly- Dose adjustment may be required. Use as prescribed by the doctor.

  7. Alcoholism- Avoid the use of medication if there is a habit of consumption of more than three drinks per day.

  8. Drugs- Avoid use in case of administration of MAO inhibitors in the last two weeks due to serious interaction. Also, avoid using Riociguat and Viloxacine while on therapy with this drug.

  9. Using Birth-Control Pills- The drug may cause the contraceptive pills to be ineffective. Inform the healthcare professional before taking the medication.

  10. Pregnancy and Breastfeeding- If pregnant while taking this medication, the baby may develop dependence. The drug is also reported to pass through breast milk. Hence, inform the doctor if pregnant or breastfeeding.

What Are the Side Effects of Butalbital-Acetaminophen-Caffeine?

The common side effects of this medication include;

  • Nausea

  • Vomiting.

  • Abdominal pain.

  • Dizziness.

  • Lightheadedness.

  • Difficulty breathing.

These symptoms will go away on their own. However, if they become severe or become persistent, seek medical help.

Some of the severe side effects include;

  • Seizures.

  • Confusion.

  • Allergic symptoms such as blistering, peeling, or rash.

  • Dark urine.

  • Brown stools.

  • Yellowing of skin and white of the eyes.

Seek medical help immediately if the symptoms mentioned above are experienced.

What Are the Interactions of Butalbital-Acetaminophen-Caffeine?

It is quite common for medications to interact with other drugs, food, beverages, or supplements. These interactions may give rise to unwanted side effects. Some of the common interactions are listed below:

1. With Other Drugs:

  • Alfentanil.

  • Alprazolam.

  • Amobarbital.

  • Anisindione.

  • Aprobarbital.

  • Butabarbital.

  • Calcium oxybate.

  • Capmatinib.

  • Carisoprodol.

  • Chloral hydrate.

  • Chlordiazepoxide.

  • Chlorzoxazone.

  • Clarithromycin.

  • Clonazepam.

  • Clorazepate.

  • Dantrolene.

  • Darunavir.

  • Diazepam.

  • Dicumarol.

  • Doxorubicin.

  • Doxorubicin hydrochloride liposome.

  • Esketamine.

  • Estazolam.

  • Ethchlorvynol.

  • Etonogestrel.

  • Flunitrazepam.

  • Flurazepam.

  • Givosiran.

  • Halazepam.

  • Imatinib.

  • Isoniazid.

  • Ketazolam.

  • Lorazepam.

  • Lormetazepam.

  • Magnesium oxybate.

  • Medazepam.

  • Mephenesin.

  • Mephobarbital.

  • Meprobamate.

  • Metaxalone.

  • Methocarbamol.

  • Methohexital.

  • Midazolam.

  • Nifedipine.

  • Nitrazepam.

  • Oxazepam.

  • Pentobarbital.

  • Phenindione.

  • Phenobarbital.

  • Phenprocoumon.

  • Piperaquine.

  • Pixantrone.

  • Pneumococcal 13-valent vaccine, diphtheria conjugate.

  • Potassium oxybate.

  • Prazepam.

  • Primidone.

  • Quazepam.

  • Secobarbital.

  • Sodium oxybate.

  • Temazepam.

  • Thiopental.

  • Trazodone.

  • Triazolam.

  • Ulipristal.

2. With Alcohol- Drinking alcohol while on this medication can lead to dizziness, confusion, and tiredness. It can also result in liver damage. Hence, avoid using alcohol while on therapy with this medication.

3. With Food- Avoid caffeine-containing food and beverages or talk with the pharmacist or doctor before starting the therapy.

4. With Laboratory Tests- The drug may interfere with some lab tests. Hence, notify the professional before taking any medical tests.

Last reviewed at:
06 Jul 2023  -  7 min read




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