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Barbiturate

Medical Uses: – Barbiturates are used as anxiolytics, hypnotics, anticonvulsants, and general anesthetics. – They can reduce time to fall asleep, increase total sleep time, […]

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Medical Uses:
– Barbiturates are used as anxiolytics, hypnotics, anticonvulsants, and general anesthetics.
– They can reduce time to fall asleep, increase total sleep time, and induce anesthesia.
– High doses are utilized in medical aid in dying, euthanasia, and as euthanizing agents in veterinary medicine.

Chemistry and Classification:
– Barbiturates bind to receptors via hydrogen bonds and have various applications in supramolecular chemistry.
– They are classified as ultra short-acting, short-acting, intermediate-acting, and long-acting based on their duration of action.
– Common barbiturates include thiopentone, pentobarbitone, amobarbitone, and phenobarbitone.

Mechanism of Action and Effects:
– Barbiturates act as positive allosteric modulators of GABA receptors, potentiating inhibitory effects and inhibiting excitatory receptors.
– They increase chloride ion channel opening at GABA receptors and bind to various ligand-gated ion channels.
– Overdose effects include incoordination, shallow breathing, and potential fatal outcomes, especially when combined with other CNS depressants.

Risks and Interactions:
– Barbiturates rank high in physical harm, social harm, and dependence, with risks for older adults and pregnant women.
– They can induce hepatic enzymes, affecting drug metabolism and potentially causing fatal overdoses with certain medications.
– Barbiturates interact with benzodiazepines, enhancing their effects and increasing the risk of overdose.

Society, Culture, and Legal Aspects:
– Barbiturates were historically used in military settings and faced reduced prescriptions due to overdoses and dependence in the past.
– They are classified as controlled substances in the US and regulated under different schedules internationally.
– Recreational use of barbiturates can lead to significant morbidity, addiction, and potential for suicide, and they are often consumed with alcohol or other substances.

Barbiturate (Wikipedia)

Barbiturates are a class of depressant drugs that are chemically derived from barbituric acid. They are effective when used medically as anxiolytics, hypnotics, and anticonvulsants, but have physical and psychological addiction potential as well as overdose potential among other possible adverse effects. They have been used recreationally for their anti-anxiety and sedative effects, and are thus controlled in most countries due to the risks associated with such use.

Barbituric acid, the parent structure of all barbiturates

Barbiturates have largely been replaced by benzodiazepines and nonbenzodiazepines ("Z-drugs") in routine medical practice, particularly in the treatment of anxiety disorders and insomnia, because of the significantly lower risk of overdose, and the lack of an antidote for barbiturate overdose. Despite this, barbiturates are still in use for various purposes: in general anesthesia, epilepsy, treatment of acute migraines or cluster headaches, acute tension headaches, euthanasia, capital punishment, and assisted suicide.


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