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CNS Drugs Exam 1
Pharmacology 2 Exam #1
| Drug Name | Use |
|---|---|
| Tiagabine | inhibits GABA reuptake by inhibiting GABA transporter GAT-1 (anticonvulsant) |
| Vigabatrine | Blocks GABA transaminase (GABA-T) and the conversion of GABA back to glutamate. This Promotes GABA activity (anticonvulsant) |
| Tetanus Toxin | inhibits GABA and glycine release (convulsant) |
| Muscimol | GABA-A receptor agonist (mimics psychosis) |
| Bicuculine | GABA-A receptor competitive antagonist (convulsant) |
| Picrotoxin | GABA-A receptor non-competitive antagonist (convulsant) - cannot overcome by adding more GABA |
| Baclofen | GABA-B receptor agonist (muscle relaxant). only drug that acts on GABA-B |
| Benzodiazpines | GABA-A modulators (enhance GABA-A receptor activation) - higher potency (get response faster), lower efficacy (not as large response) than barbiturates; drug of choice for general anxiety |
| Barbiturates | GABA-A modulators (enhance GABA-A receptor activation, also a weak agonist= can activate receptors w/o GABA [dangerous]) - lower potency (longer to get response), higher efficacy (greater max response), can also inhibit glutamate signalling |
| Chlordiazepoxide [Librium] | Benzodiazepine. Potentiate GABA-A receptor. Uses: General Anxiety disorder, Drug withdrawal; was the 1st benzo |
| Diazepam [Valium] | Benzodiazepine. Potentiate GABA-A receptor. Uses: General Anxiety disorder, muscle spasm, seizures, drug withdrawal, induction of anesthesia |
| Midazolam [Versed] | benzodiazepine. Potentiate GABA-A receptor. Used for induction of anesthesia, produces conscious sedation when used with opioid; produces anterograde amnesia |
| Flumazenil [Romazicon] | benzodiazepine competitive antagonist - can block benzos pretty well (shorter half life) but not very good at reversing respiratory depression |
| Benzodiazepine-Like drugs | mostly hypnotic agents(to treat insomnia); seletice for the allosteric site on alpha-1 subunit on GABA-A (BDZ receptor subtype) |
| Zolpidem [Ambien] | Benzodiazepine-like drug. Use Short term. DFA and DSA. Short acting (t1/2 ~ 2.5 h) |
| Zaleplon [Sonata] | Benzodiazepine-like drug. Use short term. DFA only. Very short acting (t1/2 ~1 h) |
| Eszopiclone [Lunesta] | Benzodiazepine-like drug. Approved for long term use. DFA and DSA. Intermediate acting (t1/2 6 hours) |
| Buspirone (Buspar) | Atypical antidepressant. Anti-Anxiety drug. Non-benzo. 5-HT1A partial agonist. Take 1 week+ to work. No benzo side effects (less CNS depression, not potentiated w/ alcohol, no anti-convulsant, no withdrawal, less abuse potential) not an anti-hypnotic |
| Barbiturate action classifications | Ultra-short (thiopental), Short/intermediate (secobarbital, pentobarbital), Long (phenobarbital) |
| Flunitrazepam [Rohypnol] | benzodiazepine used as a date rape drug |
| GHB (Gamma-hydroxybutyrate) | GABA-ergic drug used as a date rape drug. Dangerous because it does not have the benzodiazepine ceiling effect (can cause respiratory depression) |
| Propofol | Anesthetic inductive agent. GABA-A receptor enhancer |
| Ethanol | CNS depressant by enhancing GABA-A receptor activity and inhibiting glutamate receptor activity |
| Name the NMDA receptor antagonists | Riluzole, Memantine, Amantadine |
| Lithium | inhibit depolarizaation and DA and NE release but not 5-HT. inhibit the IP3 pathway's increase in Ca caused by D2 receptor activation. tx bipolar depression. blocks receptor mediated actions of some hormones, also alter ion distribution. |
| cocaine | inhibits monoamine transporters (NET, DAT, SerT). This blocks reuptake and increased time of action for NE, DA, and 5-HT |
| Serotonergic reuptake inhibitors | TCAs, SSRIs, SNRIs |
| Serotonin storage inhibitiors | amphetamine-like drugs, reserpine(if serotonin cannot be stored it cannot be released, will cause depression = why taken off market for anti-HTN) |
| Serotonin degradation inhibitors | MAO-Is |
| Sumatriptan | 5-HT1D receptor agonist. used to treat migraines |
| Ketanserin | 5-HT2A/C receptor antagonist. Used to treat glaucoma |
| Clozapine | 5-HT2A receptor antagonist. Used to treat schizophrenia |
| Odansetron | 5-HT3 receptor antagonist. anti-emetic. especially for chemotherapy |
| Alosetron | 5-HT3 receptor antagonist. Used for irritable bowel syndrome and excessive GI activity |
| Entacapone | Parkinson's Treatment. Selective, reversible inhibitor of COMT. Inhibits metabolism of l-dopa in the periphery but not CNS. Increase l-dopa action in the brain by decreasing metabolites in periphery and competetion with metabolites to get into the brain |
| Selegiline | Parkinson's Treatment. Selective irreversible inhibition of MAO-B (lose selectivity at higher doses). suppress dopamine destruction. Monotherapy or combo w/ l-dopa(can reduce wearing off effect). Esp used for Early diagnosed pts |
| Rasagiline | Parkinson's Treatment. More selective inhibition of MAO-B than Selegiline. suppresses dopamine destruction. Esp used for Early diagnosed pts |
| Pramipexole | non ergot dopamine agonist (D2 & D3 R) (parkinson's tx). Can be used mono or combo w/ l-dopa (reduce wearing off effect). Rare reversible gambling compulsions seen. |
| Apomorphine | non-ergot dopamine agonist. Used SubQ for parkinson's freezing episodes for rapid reversal of akinesia. transient action - 5-10 min (only use is for this) |
| Benztropine | Anti-cholinergic used for Parkinson's Tx. suppresses cholinergic interneuron action in the striatum. Reduces tremor and rigidity(rigidity ****). affect neurons of the indirect pathway. Not as effective as dopaminergic drugs. atropine-like side effects |
| Amantadine | NMDA receptor antagonist. promotes dopamine release and may decrease the onset of drug-induced dyskinesias |
| neuroleptics definition | dopaminergic based antipsychotics that suppress motor activity and emotionality |
| haloperidol | prototype of the typical antipsychotics. Affinity for the D2 receptor. Treats primarily positive symptoms |
| clozapine | atypical antipsychotic |
| risperidone | atypical antipsychotic |
| Name examples of Tricyclic antidepressant drugs (TCAs) | Imipramine (Tofranil), Amitryptiline (Elavil), Chlorimipramine (Anafranil), Doxepine (sinequan), Despramine (Norpramin) |
| Mechanism of Action for Tricyclic antidepressants (TCAs) | bind to reuptake transporters and block (SERT, NET) increasing 5-HT and NE in the synapse. Sloppy affinity accounts for adrenergic, cholinergic, and histamine related side effects |
| name examples of Monoamine oxidase inhibitors (MAO-Is) | Phenelzine (Nardil), Isocarboxazine (Marplan), Pargyline (Eutonyl), Deprenyl (Selegeline - reversible MAO-B inhibitor), Moclobemide (Aurorix - reversible MAO-A inhibitor) |
| Mechanism of Action for MAO-Is | inhibiting MAO metabolism increases 5-HT and NE concentrations in the synapses and stores/. (release more!). most are irreversible* |
| Name examples of selective serotonin reuptake inhibitors (SSRIs) | Fluoxetine(Prozac), Sertraline (Zoloft), Paroxetine (Paxil), Citalopram (Celexa, Lexapro) |
| Name the mechanism of selective serotonin reuptake inhibitors (SSRIs) | Block the SERT traansporter, increasing 5-HT concentrations in the synapse. very specific in blocking only serotonin transporter. show discontinuation syndrome when suddenly stopped |
| name examples of selective serotonin/norepinephrine reuptake inhibitors (SNRIs) | Venlafaxine (Effexor), Duloxetine (Cymbalta), some newer TCAs |
| Name the mechanism of selective serotonin/norepinephrine reuptake inhibitors | block SERT and NET selectively to increase 5-HT and NE concentrations in the synapse. dont have much activity at other receptors so there are less side effects |
| Imipramine (Tofranil) | tricyclic antidepressant |
| Lamotrigine (Lamictal) | anticonvulsant used in bipolar. more effective at preventing depressive episodes and mania than treating acute episodes |
| levodopa | can cross BBB and be metabolized into Dopamine, increasing dopamine in the CNS (Parkinsons treatment). When combined with carbidopa which inhibits l-dopa metabolism in the periphery l dopa is more bioavailable |
| carbidopa | inhibits AADC, a decarboxylase that metabolizes l-dopa in the periphery. combo with l-dopa to increases its bioavailability . MAO in the periphery doesnt really affect l-dopa levels |
| Bupropion (Wellbutrin) | atypical antidepressant - used for smoking cessation |
| Trazodone (Desyrel) | atypical antidepressant - used for sleep disturbances |
| Mirtazepine (Remeron) | atypical antidepressant |
| name 4 atypical antidepressants | Bupropion (Wellbutrin), Trazodone (Desyrel), Mirtazepine (Remeron), Buspirone (Buspar) |
| Amitryptiline (Elavil) | TCA |
| Chlorimipramine (Anafranil) | TCA |
| Doxepine (sinequan) | TCA |
| Despramine (Norpramin) | TCA |
| Phenelzine (Nardil) | MAO-I |
| Isocarboxazine (Marplan) | MAO-I |
| Pargyline (Eutonyl) | MAO-I |
| Deprenyl (Selegeline) | MAO-I - reversible MAO-B inhibitor) |
| Moclobemide (Aurorix) | MAO-I - reversible MAO-A inhibitor) |
| Fluoxetine(Prozac) | SSRI |
| Sertraline (Zoloft) | SSRI |
| Paroxetine (Paxil) | SSRI |
| Citalopram (Celexa, Lexapro) | SSRI |
| Venlafaxine (Effexor) | SSNRI |
| Duloxetine (Cymbalta) | SSNRI |
| Valproate (Valproic Acid, Depakote) | promotes synthesis of GABA at Glutamic Acid Decarboxylase. Also block recylcing of GABA at GABA-T-->SSA-DH step. Anticonvulsant used in bipolar. As effective as Li and often combined |
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HugsAndKisses
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