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Barb and BDZ
| Term | Definition |
|---|---|
| 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 |