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Seds/hyps/anxys/EtoH
UVa med pharmacology block 2
| Question | Answer |
|---|---|
| Flurazepam (Dalmane) | Benzo - allosteric modulator of GABA gated Cl- channels potentiates GABA med'd IPSP->synaptic inhib (reqs GABA) T1/2 long (>1day) Fx: sedation, decr motor performance, lethal w/EtOH, disinhib rxns, dependence |
| Temazepam (Restoril) | Benzo - allosteric modulator of GABA gated Cl- channels potentiates GABA med'd IPSP->synaptic inhib (reqs GABA) T1/2 intermed (6-24hrs) Fx: sedation, decr motor performance, lethal w/EtOH, disinhib rxns, dependence |
| Triazolam (Halcyon) | Benzo - allosteric modulator of GABA gated Cl- channels potentiates GABA med'd IPSP->synaptic inhib (reqs GABA) T1/2 short (2-3hrs) Fx: sedation, decr motor performance, lethal w/EtOH, disinhib rxns, dependence |
| Chlordiazepoxide (Librium) | Benzo - allosteric modulator of GABA gated Cl- channels potentiates GABA med'd IPSP->synaptic inhibition (reqs GABA) - tx Preanesthesia, anxiety, absence seizures, muscle spasticity T1/2 long>1day |
| Chlorazepate (Tranxene) | Benzo - allosteric modulator of GABA gated Cl- channels potentiates GABA med'd IPSP->synaptic inhibition (reqs GABA) - tx anxiety, absence seizures T1/2 long>1day |
| Diazepam (valium) | Benzo - allosteric modulator of GABA gated Cl- channels potentiates GABA med'd IPSP->synaptic inhibition (reqs GABA) - tx Preanesthesia, anxiety, muscle spasticity T1/2 long>1day |
| Midazolam (Versed) | Benzo - allosteric modulator of GABA gated Cl- channels potentiates GABA med'd IPSP->synaptic inhibition (reqs GABA) - tx Preanesthesia, anxiety, absence seizures, muscle spasticity T1/2 short (3hrs) |
| Lorazepam (Ativan) | Benzo - mech same as others tx severe anxiety, preanesthesia, emesis, status epilepticus T1/2 intermed 12-16hrs high potency |
| Alprazolam (Xanax) | Benzo - mech same as others tx severe anxiety, preanesthesia, emesis High potency |
| Clonazepam (Klonopin) | Benzo - mech same as others tx severe anxiety, preanesthesia, emesis High potency |
| Oxazepam | benzo - tx anxiety disorder, acute alcohol withdrawal T1/2 intermediate |
| Zolpidem (Ambine) | Benzo related agent - positive alpha1-subunit selective modulator of GABA cl channels - Tx insomnia T1/2 short 1-2hrs |
| Flumazenil | competitive benzo receptor antag - tx reversal of Benzo toxicity/sedation T1/2 short 1hr fx: may precipitate w/drawal, risk of seizures |
| Buspirone (buspar) | Atypical anxiolytic - partial agonist at 5-HT1a - pre/postsynaptic inhib - nonsedative - tx anxiety fx req 1-2wks lack benzo sidefx |
| Phenobarbital | barbiturate sed/hypnotic - potent's GABAergic transmission, high dose GABA indy Cl- influx->hypnotic, high dose->anesthetic T1/2 very long severe sidefx |
| Secobarbital | barbiturate sed/hypnotic - potent's GABAergic transmission, high dose GABA indy Cl- influx->hypnotic, high dose->anesthetic tx preanesthesia, insomnia severe sidefx @ high dose |
| Thiopental | barbiturate sed/hypnotic - potent's GABAergic transmission, high dose GABA indy Cl- influx->hypnotic, high dose->anesthetic tx ultra-fast induction of anesthesia t1/2 short acting |
| Ethanol | methanol/ethylene glycol poisoning incr GABAa receptor/Cl- fx, severe dependance, tolerance to sedative fx + cross tolerance to other seds Dose dependent clearance |
| Methanol/Ethylene glycol | Converted to formaldehyde by Alc-dehydrogenase (Toxic)-> blindness, liver degen, CNS toxicity tx'd w/ethanol |
| Disulfiram | Anti-alcoholic - inhibs aldehyde dehydrog-> acetaldehyde-> aversive sidefx non-compliance is problem, CI exposure to heavy metals |
| Acamprosate | anti-alcoholic - unclear mech - modestly decr relapse rate post detox, well tolerated |
| Naltrexone | anti-alcholic - opiate receptor antag, decr relapse to heavy drinking, attens rewarding fx of alcohol useless as sole tx, helpful when combined w/rehab |
| What are the uses of Lorazepam? | severe anxiety pre-anesthetic status epilepticus anti-emetic |
| Drugs that have insomia usefulness should have what common features? | - fast onset - half life shouldn't be too short so it lasts through the night, but not too long so that there is excessive morning sedation - should produce refreshing sleep |
| What is the therapeutic use of Temazepam? What are it's advantages? | - Insomnia - Intermediate half-life, little hangover, refreshing sleep |
| What is the therapeutic use of Flurazepam? What are it's advantanges? | - Used for insomnia - Long half life, produces little hangover (redistribution) |
| Name four long half life BDZ's? | flurazepam, chlordiazepoxide, clorazepate, diazepam |
| What are the uses of Alprazolam? | severe anxiety |
| What are the uses of Clonazepam? | Severe anxiety, absence (petit mal) seizures |
| What is required for a BDZ to be a useful anxiolytic? | Long lasting, low levels of drug **since anxiolytic effects require the lowest doses |
| What are the three high potency BDZ? What is their use? | Lorazepam, Clonazepam, Alporazolam Severe anxiety |
| What are the uses Midazolam? | Pre-anesthetic |
| What is the therapeutic use of Zolpidem? What is special about it and what is its advantage? | - Insomnia - BDZ-like compound, purely a1 subunit action, short T1/2, minize morning sedation and tolerance |
| Name two intermediate half life BDZs" | Temazepam, Estazolam |
| Name two short half-lfe BDZs? | Zolpidem, Triazolam |
Created by:
sam.mrosenfeld
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