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Isolated from the skin of poisonous frog Centrally-acting nicotinic agonist with analgesic activity Studied in animal models of pain |
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| increases GABA release from nerve terminals. Used asn an anticonvulsant and in the Tx of chronic pain syndromes. |
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Ketamine Phencyclidine (PCP) |
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Definition
| antagonists at the NMDA receptor that cause Dissociatinve anesthesia |
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| antagonist at NMDA receptor that is used to Tx Parkinsons disease |
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| Antagonist at the NMDA receptor that is used to Ts advanced Alzheimer disease |
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| dopamine receptors are found throughout the CNS but are especailly prevalent in (3)... |
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Basal ganglia Nucleus accumbens amygdala |
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| agonists at the α2-adrenoceptor that are antihypertensives that rarely cause hypotension. ALso are profoundly sedating w/o resp depression. |
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5-hydroxytryptamine (serotonin) |
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Definition
| 5-HT1 has 5 subtypes (1A-1E), all are GPCRs linked to adenyl cyclase inhibition, or K+ or Ca+ channels. Associated with regulation of mood, and migraines. Agonists used to tx migraines and as anxiolytic agents. 5-HT2 has 3 subtypes, all GPCR's linked to phospholipase C. Agonists cause hallucinations, antagonists have antipsychotic activity. 5-HT3 receptors are ligand gated ion channels. Antagonists are antiemetics, used for chemo and post-anesthesia. |
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| Muscarinic agonist. Antagonists of the muscarinic receptor are used to tx Parkinson's and extrapyramidal AE caused by dopaminergic antagonists, commonly seen in tx of psychoses. Cholinergic neuron loss seen in Alzheimer's. Some muscarinic antagonists cause amnesia, antiemetic effect, and sedation. Irreversible AChE used in warefare --> convulsions, coma, and death. |
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| tx: panic disorders and agraphobia |
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weak antagonist at NMDA receptor, used for early Parkinson influenza A tx |
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| inhibits reuptake of both norepinephrine and serotonin, has both central and peripheral anticholinergic effects. AE: sedation (tolerance develops), difficulty concentrating, dry mouth, blurred vision, incr HR, incr intracardiac conduction times, flattening or inversion of T waves, orthostatic hypotension due to alpha adrenergic blockade, can cause mania (most often in bipolar pt), weight gain. Given to normal pt --> no increased happiness/mood elevation. facilitates falling asleep and staying asleep. fatal does = 1-2 wk supply. |
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NK1 antagonist antiemetic with very few AE. |
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partial agonist at dopaminergic D2 and 5-HT1A receptors Antipsychotic |
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GABA(B) receptor agonist centrally acting muscle relaxant commonly used to treat muscle spasms associated with spinal cord injuries and neurodegenerative diseases. Baclofen pumps can be implanted to put small doses directly into CSF, used with MS, spinal lesions, etc |
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ester, local anesthestic used topically, often as mouth and throat spray. |
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muscarinic antagonist Parkinson treatment, centrally active. AE: dry mouth, sedation, urinary retention (spec w/men with prostate enlargement) |
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Parkinson tx dopaminergic agonist - no need for enzymatic conversion, selective for subtypes of dopamine receptors, longer duration of action, no conversion to ROS. |
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amine, local anesthestic LONG acting, slow onset, and HIGH toxicity (cardio). Very slow dissociation from binding site in Na channel --> long acting, does not need epinephrine to prolong duration. Used for local infiltration, nerve blocks, spinal and epidural anesthesia. Do NOT inject IV |
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mu partial agonist suboxone. acts selectively at mu receptors. Similar effect to morphine = competes with the full agonist and causes a reduction in opioid effect. Given IM, PO, SL, IN, IV… |
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Definition
atypical antidepressant inhibits reuptake of both norepinephrine and dopamine, but not serotonin. lack of sedation, anticholinergic, orthostatic hypotension, and cardiac conduction effects. Lowers seizure threshold. Useful for nicotine withdrawal tx. |
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Definition
5-HT1A partial agonist tx: anxiety. Good option for people who have abused or are at risk of abusing benzodiazepines. little activity aty dopamine or GABA receptors, does not cause sedation or have anticonvulsant effect. Tolerance doesn't develop, no cross-tolerance with benzodiazepines or other CNS depressants. |
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Definition
Competitive antagonist to Morphine produces analgesic and sedative effects by interacting as a partial agonist with kappa opioid receptors, but no efficacy at mu receptors and therefore competitive antagonist to morphine. AE: drowsiness, apathetic sedation. |
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