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BMS60043
Drugs acting on chloride channels (GABA receptor)
| Question | Answer | Clinical Effects | Clinical Effects | Clinical Effects |
|---|---|---|---|---|
| Endogenous Antagonists | carbolines | |||
| Exogenous Agonists | benzodiazepines (BDZ); barbiturates, propofol, alcohol | |||
| Benzodiazepines (BDZ) | attach to the alpha subunit; work only when GABA is present | sedative, hypnotic, amnesic,muscle tone decrease, anti-epileptic; no analgesia | ||
| -zepam | BDZ | |||
| -zolam | BDZ | |||
| Short Acting BDZ | TOMB: Triazolam Oxazepam Midazolam Brotizolam | |||
| Intermediate Acting BDZ | LETAL: Lorazepam Estazolam Temazepam Alprazolam Loprazolam | |||
| Long Acting BDZ | Diazepam Flurazepam Clotiazepam Nitrazepam Flunitrazepam | |||
| Which BDZ don't do Phase I metabolism? | TOL: Temazepam Oxazepam Lorazepam | |||
| non-BDZ hyp | Zaleplon Zolpidem Zopiclone | |||
| BDZ antagonist | Flumazenil | |||
| Barbiturates and Profolol | beta subunit; work without GABA; no analgesia | |||
| Barbiturates | sedative-hypnotics (anesthesia) anti-epileptic | |||
| thiopental | sedative-hypnotic barbiturate | |||
| phenobarbital | anti-epileptic barbiturate | |||
| profolol | sedative hypnotic anesthesia | |||
| vigabatrin | inhibits GABA transaminase, decreases GABA metabolism, increases GABA | anti-epileptic | ||
| Tiagabin | GABA-reuptake inhibitor; increases GABA | anti-epileptic | ||
| Gabapentin | not a GABA agonist;alpha-2 delta ligand at PQRN-Ca channel; decreases transmitter release | |||
| Baclofen | ||||
| Endogenous Antagonists | carbolines | |||
| Exogenous Agonists | benzodiazepines (BDZ); barbiturates, propofol, alcohol | |||
| Benzodiazepines (BDZ) | attach to the alpha subunit; work only when GABA is present | sedative, hypnotic, amnesic,muscle tone decrease, anti-epileptic; no analgesia | sedative, hypnotic, amnesic,muscle tone decrease, anti-epileptic; no analgesia | |
| -zepam | BDZ | |||
| -zolam | BDZ | |||
| Short Acting BDZ | TOMB: Triazolam Oxazepam Midazolam Brotizolam | |||
| Intermediate Acting BDZ | LETAL: Lorazepam Estazolam Temazepam Alprazolam Loprazolam | |||
| Long Acting BDZ | Diazepam Flurazepam Clotiazepam Nitrazepam Flunitrazepam | |||
| Which BDZ don't do Phase I metabolism? | TOL: Temazepam Oxazepam Lorazepam | |||
| non-BDZ hyp | Zaleplon Zolpidem Zopiclone | |||
| BDZ antagonist | Flumazenil | |||
| Barbiturates and Profolol | beta subunit; work without GABA; no analgesia | |||
| Barbiturates | sedative-hypnotics (anesthesia) anti-epileptic | sedative-hypnotics (anesthesia) anti-epileptic | ||
| thiopental | sedative-hypnotic barbiturate | |||
| phenobarbital | anti-epileptic barbiturate | |||
| profolol | sedative hypnotic anesthesia | |||
| vigabatrin | inhibits GABA transaminase, decreases GABA metabolism, increases GABA | anti-epileptic | anti-epileptic | |
| Tiagabin | GABA-reuptake inhibitor; increases GABA | anti-epileptic | anti-epileptic | |
| Gabapentin | not a GABA agonist;alpha-2 delta ligand at PQRN-Ca channel; decreases transmitter release | |||
| Baclofen | GABA B agonists (presynaptic); decreases transmitter release | |||
| Endogenous Agonists | GABA, endozepines | |||
| Endogenous Agonists | GABA, endozepines | |||
| Endogenous Agonists | GABA, endozepines |