Butalbital is a barbiturate that exerts its effect by mimicking the inhibitory effect of gamma-aminobutyric acid (GABA) by binding to a site, distinct from the benzodiazepine binding site, on the GABA receptor. This leads to an increase in the duration of GABA-mediated opening of chloride channels and enhances the inhibitory effect of GABA. Consequently, its physiologic effects include sedation, hypnosis, reduction of anxiety, and respiratory depression and the drug causes tolerance and dependence.
Butalbital is a barbiturate with an intermediate duration of action. Butalbital is often combined with other medications, such as acetaminophen (paracetamol) or aspirin, and is commonly prescribed for the treatment of pain and headache. Butalbital, 5-allyl-5-isobutyl barbituric acid, is a barbiturate with an intermediate duration of action. It has the same chemical formula as talbutal but a different structure. Butalbital is often combined with other medications, such as acetaminophen or aspirin, and is commonly prescribed for the treatment of pain and headache.
Mechanism of Action of Butalbital
Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. Insufficiently high therapeutic doses, barbiturates induce anesthesia. Butalbital binds at a distinct binding site associated with a Cl– ionopore at the GABAA receptor, increasing the duration of time for which the Cl– ionophore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
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The effects of butalbital (30, 100, and 1000 ug/kg) on the number of cells expressing c-fos-like immunoreactivity (c-for-LI), a marker of neuronal activation, within lamina I, IIo of the trigeminal nucleus caudal is and the nucleus of the solitary tract 2 hours after the intracisternal injection of capsaicin (0.1 mL; 15.25 mg/mL) or vehicle in urethane-anesthetized guinea pigs (N = 45) /was examined/. Robust c-fos-LI was observed within nuclei of cells in the trigeminal nucleus caudalis after capsaicin (329 +/- 35). Butalbitaldose-dependently reduced the number of labeled cells to a maximum of 66% (1000 micrograms/kg intraperitoneally [i.p.], P < .01) in lamina I, IIo but not within area postrema, medial reticular nucleus, or the nucleus of the solitary tract. Pretreatment with bicuculline (30 micrograms/kg i.p.) blocked the effect of butalbital, thereby suggesting the importance of the GABAA receptor to activation involved in the transmission of nociceptive information. Our studies suggest the possibility that GABAA receptors might provide an important therapeutic target in a migraine and related headache disorders.
Indications of Butalbital
- A headache
- A tension Headache
- Used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain.
MA a migraine
Contra Indications of Butalbital
- Porphyria
- High blood pressure
- Heart hisease
- Abnormally low blood pressure
- Pneumonia
- Lung failure causing loss of breath
- Decreased lung function
- Liver problems
- Periods of Not breathing
- Pregnancy
- Chronic obstructive lung disease
Dosage of Butalbital
- Strengths: 325 mg-50 mg; 650 mg-50 mg; 300 mg-50 mg; 325 mg-25 mg
Headache
Butalbital 50 mg/acetaminophen 300 or 325 mg
- 1 or 2 tablets orally every 4 hours as needed not to exceed 6 tablets per day
Butalbital 25 mg/acetaminophen 325 mg
- 2 tablets orally every 4 hours as needed not to exceed 12 tablets per day
Pediatric Dose for Headache
12 years or older
Butalbital 50 mg/acetaminophen 300 or 325 mg
- 1 or 2 tablets orally every 4 hours as needed not to exceed 6 tablets per day
Butalbital 25 mg/acetaminophen 325 mg
- 2 tablets orally every 4 hours as needed not to exceed 12 tablets per day
Side Effects of Butalbital
The most common
- Memory or concentration problems
- Excitement, irritability, aggression, or confusion
- Dizziness
- constipation
- muscle aches
- Nausea and vomiting
- Severe stomach ache
- diarrhoea,
- anorexia,
- flatulence,
- headache,
- dizziness,
- heartburn
- joint pain
Common
- Memory loss.
- Impaired attention span.
- Agitation.
- Depression.
- Nausea and vomiting
- Severe stomach ache
- Severe diarrhea
- Mouth sores
- Vaginal thrush
- Skin rash
- Headache
Rare/Less common
- Confusion
- Fever or sore throat
- Rash
- Slowed breathing or breathing difficulties
- Sores in the mouth
- Broken blood vessels under the skin
- Easy bruising or bleeding
- Swelling of the eyes, lips, or cheeks
- Blistering or peeling of the skin
- Restless muscle movements in the eyes, tongue, jaw, or neck
Drug Interactions of Butalbital
Butabital may interact with following drugs, supplements & may change the efficacy of the drug
- albendazole
- alcohol
- allopurinol
- alpha blockers (e.g., alfuzosin, doxazosin, silodosin, tamsulosin)
- amphetamines (e.g., dextroamphetamine, lisdexamphetamine)
- anti-cancer medications (e.g., cabazitaxel, docetaxel; doxorubicin; etoposide, ifosfamide, irinotecan, vincristine)
- antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- baclofen
- barbiturates (e.g., butalbital, pentobarbital phenobarbital)
- benzodiazepines (e.g., chlordiazepoxide, clonazepam, diazepam, lorazepam)
- beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
- bupropion
- calcitriol
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- carbamazepine
- carvedilol
- celecoxib
- ciprofloxacin
- clobazam
- oral corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
- cyclosporine
- doxycycline
- estrogens (e.g., conjugated estrogen, estradiol, ethinyl estradiol)
- folic acid
- gabapentin
- “gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
- lansoprazole
- loperamide
- losartan
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- multivitamins
- montelukast
- nitrates (e.g., isosorbide dinitrate, isosorbide mononitrate)
- ondansetron
- phenytoin
- progestins (e.g., dienogest, levonorgestrel, medroxyprogesterone, norethindrone)
- proton pump inhibitors (e.g., lansoprazole, omeprazole)
- ranitidine
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine,paroxetine, sertraline)
- sildenafil
- “statin” anti-cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
- theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
- thiazide diuretics (e.g., chlorothiazide, hydrochlorothiazide)
- tramadol
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- valproic acid
- warfarin
- zafirlukast
Pregnancy & Lactation
FDA Pregnancy Category C
Pregnancy
Medications used to prevent major seizures should not be stopped. The use of this medication is not recommended during pregnancy. However, the decision about whether or not to stop the medication must weigh the potential benefits against the potential risks. If you become pregnant while taking this medication, contact your doctor immediately.
Lactation
This medication passes into breast milk. If you are a breastfeeding mother and are taking phenobarbital, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding.
References
