butalbital/acetaminophen/caffeine

Action and Spectrum

Actions and Spectrum:  

Action: 

butalbital: a barbiturate that works by relaxing muscle contractions and reducing anxiety. 

acetaminophen: a pain reliever that works by blocking the production of certain chemicals in the body that cause pain and inflammation.  

Caffeine: a stimulant that constricts blood vessels in the brain and increases blood flow, which can help relieve headaches.  

Spectrum: 

butalbital/acetaminophen/caffeine is most effective for treating tension headaches and migraines that are moderate to severe in intensity.  

It is generally not recommended for treating mild headaches or headaches caused by other conditions.  

The medication is usually taken orally, and the dosage and frequency of use depend on the individual’s age, medical history, and other factors.  

Side effects may include dizziness, drowsiness, nausea, and vomiting.  

Before using butalbital/acetaminophen/caffeine, discussing the potential dangers and advantages with a healthcare professional is crucial. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Butalbital  

Shortness of breath 

Abdominal pain, nausea, vomiting 

 a feeling of intoxication, lightheadedness, sedation 

Dizziness, drowsiness  

Acetaminophen 

pancytopenia, thrombocytopenia 

Agranulocytosis, leukopenia, neutropenia, 

thrombocytopenic purpura 

Anaphylactoid reaction 

Hepatotoxicity 

Angioedema, laryngeal edema 

Pruritic maculopapular rash, urticaria  

Caffeine  

Diuresis 

Restlessness Tachycardia,  

Tremor 

Diarrhea, nausea, vomiting 

palpitations (dose dependent) 

Insomnia, irritability, nervousness, tinnitus 

Black Box Warning

Black Box Warning:  

Warning: severe and sometimes fatal hepatotoxicity may occur. 

butalbital, acetaminophen, and caffeine capsules contain acetaminophen, a component which cause severe and sometimes fatal liver injury. The risk of liver injury is higher in individuals who consume alcohol, have liver disease, or consume more than the recommended dose of acetaminophen.  

Patients should be advised not to exceed the maximum recommended dose and to avoid consuming other products containing acetaminophen while taking this medication.  

Patients should also be instructed to immediately stop taking the medication and seek medical attention if they experience symptoms such as nausea, vomiting, abdominal pain, or yellowing of the skin or eyes. 

butalbital, acetaminophen, and caffeine capsules should be used cautiously in patients with a history of liver disease or alcohol abuse.   

Additionally, people taking other drugs that may have an impact on the liver should use it cautiously. 

This drug may impair your mental and physical functioning or make you feel sleepy or dizzy. Prior to understanding how this drug affects them, patients shouldn’t drive or operate machinery. 

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: People who are allergic to any of the active ingredients in the medication should not take it. 

Liver disease: This medication contains acetaminophen, which can be harmful to people with liver disease.  

Alcohol use disorder: combining of butalbital and alcohol can increase the risk of liver damage and other side effects.  

Porphyria: This is a rare genetic disorder that affects the heme production in the body. butalbital/acetaminophen/caffeine can trigger an acute attack in people with this condition.  

Respiratory depression: This medication can cause respiratory depression, especially in people with a history of breathing problems or taking other medications that can depress breathing.  

Glaucoma: butalbital/acetaminophen/caffeine can increase intraocular pressure, which can be dangerous for people with glaucoma. 

Pregnancy: This medication can harm a developing fetus and should not be used during pregnancy, especially in the first and third trimesters. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology: 

butalbital/acetaminophen/caffeine is a combination medication used to relieve tension headaches. Each of the three active ingredients works differently to alleviate the symptoms of headaches. 

Pharmacodynamics: 

The combination of these three drugs provides a synergistic effect, where the soothing and muscle-relaxant effects of butalbital are combined with the analgesic and antipyretic effects of acetaminophen, and the stimulant effects of caffeine. This medication can provide quick relief of tension headaches and can be effective for short-term management of acute pain. 

MOA:  

butalbital is a medication classified as a barbiturate that functions by depressing the central nervous system. This action helps to reduce tension and promote muscle relaxation. It is believed to work by amplifying the effects of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter in the brain. This increase in GABA activity leads to a decrease in the release of neurotransmitters that are involved in pain signaling, such as substance P and glutamate. 

acetaminophen is an analgesic and antipyretic medication that functions by inhibiting the production of prostaglandins, which are chemicals that cause pain and inflammation in the body. Acetaminophen primarily operates in the central nervous system by obstructing pain signals that are transmitted to the brain. It also has a minor impact on the peripheral nervous system. 

caffeine is a central nervous system stimulant that functions by inhibiting the activity of adenosine, a neurotransmitter that promotes sleep and reduces arousal. By blocking adenosine, caffeine increases the activity of other neurotransmitters such as dopamine and norepinephrine, resulting in heightened alertness and reduced fatigue.  

Pharmacokinetics:  

absorption:  

butalbital/acetaminophen/caffeine is an oral medication that is absorbed from the gastrointestinal tract. Absorption of the individual components varies. butalbital is absorbed rapidly and peak plasma levels are achieved within 1 to 2 hours after oral administration. acetaminophen is also rapidly absorbed, and peak plasma levels are achieved within 30 to 60 minutes. caffeine is absorbed more slowly, and peak plasma levels are achieved within 15 to 120 minutes. 

Distribution: 

The three butalbital/acetaminophen/caffeine components are distributed widely throughout the body.butalbital and acetaminophen are highly protein-bound, with about 45% and 25% bound to plasma proteins, respectively. caffeine is less protein-bound, with about 35% bound to plasma proteins. Butalbital crosses the blood-brain barrier and placenta and is distributed into breast milk. acetaminophen crosses the placenta and is distributed into breast milk. caffeine crosses the blood-brain barrier and placenta but is not distributed into breast milk to a significant extent.  

Metabolism: 

 butalbital/acetaminophen/caffeine is metabolized primarily in the liver. butalbital is metabolized by the cytochrome P450 system to inactive metabolites. acetaminophen is metabolized mainly by glucuronidation and sulfation in the liver, and a small amount is metabolized by the cytochrome P450 system to a toxic metabolite that is normally detoxified by glutathione. caffeine is metabolized primarily by the cytochrome P450 system to paraxanthine and other metabolites. 

Excretion and elimination: 

The three components of butalbital/acetaminophen/caffeine are excreted mainly in the urine. butalbital and its metabolites are excreted by the kidney, with about 90% of a dose excreted within 72 hours. acetaminophen and its metabolites are excreted mainly in the urine, with about 85% of a dose excreted within 24 hours. caffeine and its metabolites are excreted mainly in the urine, with about 95% of a dose excreted within 24 hours. 

Adminstartion

Administration:  

Dosage: The dosage of butalbital/acetaminophen/caffeine may vary depending on the severity of the headache and the patient’s age and medical history. The usual adult dose is one or two tablets taken every four to six hours, as needed. The maximum daily dose should not exceed six tablets. 

Timing: The medication can be taken with or without food, but it is important to take it with a full glass of water to ensure proper absorption. It is best to take it as soon as the headache symptoms start to appear.  

Duration: Do not take butalbital/acetaminophen/caffeine for longer than prescribed by your doctor. If your headache persists or worsens, contact your doctor for further evaluation.  

Missed dose: If you miss a dose of butalbital/acetaminophen/caffeine, take it as soon as you remember. If it is close to your next scheduled dose, skip the missed dose and continue with your regular dosing schedule.  

Overdose: Do not take more than the prescribed amount of butalbital/acetaminophen/caffeine. Overdosing can cause serious harm to your health, including liver damage or even death 

Storage: Store butalbital/acetaminophen/caffeine tablets at room temperature, away from moisture and heat. Keep them out of reach of children and pets. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: Butalbital/acetaminophen/caffeine 

Why do we use Butalbital/acetaminophen/caffeine?  

butalbital/acetaminophen/caffeine is a medication that is used to treat tension headaches and migraine headaches. butalbital is a barbiturate that helps to relax the muscles in the head and neck, while acetaminophen is a pain reliever that helps to reduce the pain associated with headaches.

caffeine is also included in the medication to help enhance the effects of both butalbital and acetaminophen, as well as to constrict blood vessels in the brain, which can also help alleviate headache pain. 

The combination of these three drugs can be effective in treating headaches for some people, but it is important to note that it can also have side effects and may not be suitable for everyone. It is always recommended to consult with a healthcare professional before taking any medication to determine if it is safe and appropriate for you.