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Barb and BDZ

TermDefinition
How do BDZ and Barbiturates act as depressants? By binding to GABA-A receptors
Toxicity of BDZ/Barb Behavioral - alcohol-like impaired judgment and coordination, increased risk of injury, additive effects if combined with alcohol! Physiological - respiratory depression, dangerous when combined w/ alcohol
BDZ Characteristics (Xanax, Valium) - safer and frequently prescribed - wider therapeutic index - act faster and shorter half-life - positive allosteric modulator (increase Cl-)
Flumazenil BDZ antagonist that will stop BDZ action and decrease CL- influx
GABA-A Receptors Have Multiple Binding Sites GABA alone = Cl- influx GABA + BDZ = Increased Cl- influx GABA + BDZ + BDZ antagonist (flumazenil) = Lower Cl- influx, because GABA still occurring GABA + BDZ + GABA antagonist = Very little Cl- influx = BDZ cannot do much on its own bc it is an all
BDZ as Therapeutics (Xanax, Ativan, Klonopin, Valium) Effective for: anxiety, insomnia, anticonvulsants (epilepsy), alcohol/barbiturate withdrawal Side effects: memory problems, altered REM, violence
BDZ Duration of Activity Low dose long acting → used for daytime relief of anxiety Higher dose short acting → used to induce sleep
Barbiturate Characteristics (phenobarbital) - higher toxicity - higher addiction potential - reserved for severe cases like seizures or anesthesia - Higher risk of fatal respiratory depression
Barbiturate Duration of Action Ultra short → acts fast and puts person to sleep (e.g, IV anesthesia) Short/intermediate → sleep induction Long → calming and anxiety relief
Barbiturates + BDZ via oral administration metabolized in the liver (CYP450) by liver enzymes and excreted in urine
Barbiturates and BDZ and other depressants (alcohol, opiates) all POTENTIATE EACH OTHER! Interfere with each other’s metabolism and produce synergistic effects on GABA receptor potentiation May result in blackout; coma, death Linked to accidenctal overdsoes, suicide, and respiratory depression
Psychological dependence of BDZ/Barb more likely with drugs that have a rapid onset of effects and have a shorter duration of action (especially w/ short acting barbiturates!)
Physical dependence of BDZ/Barb potential life threatening withdrawal syndrome linked to larger doses of sedative-hypnotics
Withdrawal from BDZ/Barb - Peripheral and cognitive effects (like alcohol) - Rebound insomnia and REM rebound Barbiturates: anxiety, insomnia, weakness, nausea, vomiting, seizure, disorientation, delusions, agitation, hallucinations BZD: less severe, anxiety, irritability,
Addiction for BDZ/Barb - Very high for barbiturates - Less for BZD and Z-drugs Probability of BDZ abuse is associated with polydrug use → individuals who have a history of drug/alcohol abuse are more likely to abuse BDZ
Created by: a1icat
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