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Barbiturate; Types, Indications/Uses, Contra Indications, Side Effects, Interactions

Barbiturate is a drug that acts as a central nervous system depressant, and can, therefore, produce a wide spectrum of effects, from mild sedation to total anesthesia. They are also effective as anxiolytics, hypnotics, and anticonvulsants. Barbiturates have addiction potential, both physical and psychological. They have largely been replaced by benzodiazepines in routine medical practice, particularly in the treatment of anxiety and insomnia, due to the significantly lower risk of addiction and overdose and the lack of an antidote for barbiturate overdose.

Types/ Classification of Barbiturate

Barbiturates	Allobarbital Amobarbital Aprobarbital Barbital Butabarbital Butobarbital Cyclobarbital Ethallobarbital Hexobarbital Mephobarbital Methohexital Narcobarbital Pentobarbital Phenallymal Phenobarbital Propylbarbital Proxibarbal Reposal Secobarbital Talbutal Thiamylal Thiopental Thiotetrabarbital Vinbarbital Vinylbital

Mechanism of action of Barbiturate

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. Barbiturates bind at a distinct binding site associated with a Cl^– ionopore at the GABA_A receptor, increasing the duration of time for which the Cl^– ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.

The effects of barbiturates 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 caudalis 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). Barbiturates dose-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 barbiturates, 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.

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Indications of Barbiturate

Typical applications for barbiturate are sedative, hypnotic for short-term, preanesthetic and control of convulsions in emergencies
Status Epilepticus
Sedation
Insomnia
Sleeplessness
Severe Convulsion
Withdrawal Symptoms
Generalized seizure
Partial onset seizure Epilepsy
Barbituratealso has an application in reducing intracranial pressure in Reye’s syndrome, traumatic brain injury and induction of coma in cerebral ischemia patients.
For the short-term treatment of insomnia.
A headache
A migraine
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.