butobarbital

Action and Spectrum

Actions and Spectrum: 

Actions: 

Like other barbiturates, butobarbital works pharmacologically by amplifying the central nervous system neurotransmitter gamma-aminobutyric acid’s (GABA) inhibitory effects. The main inhibitory neurotransmitter, GABA, usually lowers neural excitability through its activities. 

Spectrum: 

As a medication in the barbiturate class, butobarbital’s range of action is attributed to its depressive effects on the central nervous system (CNS). Although barbiturates, such as butobarbital, have a wide range of effects, such as sedation, muscle relaxation, anticonvulsant effects, hypnotic (sleep-inducing) effects, and anesthetic properties, their use has decreased over time as a result of safety concerns and the availability of safer alternatives. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Exfoliative dermatitis 

Drowsiness 

Confusion 

Ataxia 

Erythema multiforme 

Hepatitis 

Headache 

Ataxia 

GI disorders 

Fever 

CNS depression 

Paradoxical excitement 

Respiratory depression 

Megaloblastic anemia 

Black Box Warning

Black Box Warning: 

Avoid using when possible as repeated doses are cumulative and can cause excessive sedation, respiratory illness, renal disease, and hepatic impairment. Dependency and tolerance can easily develop. Abrupt withdrawal can cause serious withdrawl syndrome, which includes rebound insomnia, anxiety, tremor, dizziness, nausea, convulsions, delirium, and death.

DRIVING: The effects of alcohol may intensify drowsiness, which may last into the next day and impair one’s ability to do skilled duties like driving. 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Geriatrics 
• Pediatrics 
• Severe hepatic impairment 
• History of CNS depression and coma, sleep apnea, or pulmonary insomnia 
• Alcohol addiction 
• Pregnancy and lactation 

Cautions 

• Heterozygous familial hypercholesterolemia 
• Porphyria 
• Central retinal venous/arterial thrombosis 
• Pregnancy 
• Hyperlipidaemias 
• Breast feeding 
• Renal impairment 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the administration of the drug during pregnancy. 

Breastfeeding warnings:  

No data is available regarding the excretion of drug in breast milk. 

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

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: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

Barbiturate butobarital is used as a hypnotic. While it is no longer advised because of the possibility of dependence, tolerance, and negative effects, patients who are already taking it may need to continue using it if they have severe, uncontrollable insomnia. 

Pharmacodynamics: 

The effects of butobarbital on the central nervous system (CNS) and its interactions with the gamma-aminobutyric acid (GABA) neurotransmitter system are part of its pharmacodynamics, just like those of other barbiturates. The primary inhibitory neurotransmitter in the central nervous system is GABA, and butobarbital amplifies its actions. 

Pharmacokinetics: 

Absorption 

Oral use of butobarbital results in good absorption. Food in the stomach and the drug’s formulation are two examples of variables that can affect the rate and degree of absorption. After oral administration, the effect starts to take effect really quickly. 

Distribution 

Protein-bound is 26% 

Butobarbital is one of the barbiturates that are lipophilic, which means they have a preference for fatty tissues. They are found in many different parts of the body, including the liver, brain, and other tissues. The medication can pass through the blood-brain barrier and distribute rather quickly. 

Metabolism 

Mostly by hydroxylation in the liver. 

Hepatic metabolism of butobarbital occurs mainly via the liver’s cytochrome P450 enzyme system. Hydroxybutobarbital is the primary metabolite of butobarbital. Hepatic enzymes may be stimulated by the metabolism of barbiturates, which could accelerate the metabolism of other medications. 

Elimination and Excretion 

The half-life is 40 hours 

The drug is excreted unchanged in small amounts via urine. 

Adminstartion

Administration: 

Oral administration of barbiturates often takes the form of pills or capsules. The prescribing healthcare provider would establish the precise dosage and frequency based on the patient’s condition, reaction to therapy, and other personal considerations. In specific medical circumstances, intravenous barbiturates may be used. This administration method, which is frequently employed in medical operations or emergency situations, enables a quicker start of action.

Barbiturates may occasionally be prepared as suppositories to be administered via the rectal canal. When it is not practical to administer orally, this method can be utilized. Individualized butobarbital dosages would be prescribed according on the patient’s age, weight, health, and reaction to therapy. To attain the intended therapeutic impact while lowering the risk of side effects, healthcare professionals carefully titrate the dose. 

Patients using butobarbital or any other barbiturate need to have their side effects and therapeutic response constantly watched. Assessments of the degree of sedation, breathing rate, and general health may be part of the monitoring. Long-term use of barbiturates is often not advised because of the possibility of tolerance, dependency, and other negative effects. Depending on the particular medical problem being treated, the healthcare provider would decide how long butobarbital treatment should last. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: butobarbital 

Pronounced: byoo-toh-BAR-bi-tal 

Why do we use butobarbital? 

Historically, barbiturates were frequently used as hypnotics or sedatives to promote sleep. They produce drowsiness and relaxation by depressing the central nervous system. Barbiturates were used to lessen anxiety because they had anxiolytic characteristics, such as butobarbital. However, the availability of safer alternatives has reduced their use for this purpose.  

Butobarbital is mostly recommended for hypnotic and sedative situations. It can also be used as an alternate medication of choice for supplementary therapy in cases of epilepsy and cerebrovascular illness.