Term
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Definition
| Used to replace hepatic cysteine in acetaminophen OD (Lecture 2) |
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Term
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Definition
| Analgesic, antipyretic, metabolized by liver |
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Term
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Definition
| Barbiturate, sedative/hypnotic. Important now bc at pH 6 - poor renal excretion. At pH 8, excretion increased (Lecture 2) |
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Term
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Definition
| Blocks dopamine transport into vesicle at noradrenergic synapse (Lecture 5) |
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Term
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Definition
| Block release of NE, ATP, DBH. Initial ^BP, then long-term decrease (indirect sympathomimetic) (Lecture 5) |
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Term
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Definition
| Block reuptake of NE, 5HT, DA into varicosity (Lecture 5) |
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Term
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Definition
| Similar to DOPA, acts on CNS to decrease SNS outflow. Becomes alpha-methyl-NE which stimulates inhibitory areas in the medulla -> decreased BP |
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Term
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Definition
| Converts to octopamine (false transmitter). Releases nonvesicular NE - indirectly acting adrenergic agonist. Wine and cheese syndrome (Lecture 6) |
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Term
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Definition
| Alpha, Beta-1, Beta-2 agonist. Best stimulator of Alpha (vasoconstriction -> ^TPR -> ^BP). Used for hypersensitivity, cardiac arrest, adjuncts to local anesth |
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Term
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Definition
| Stimulates only Beta-1 and Alpha. Alpha dominates so NE administration causes ^TPR with decreased HR (vagal dominance). Used for shock (not often) |
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Term
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Definition
| Renal vasodilation at low [], Beta-1 at higher, Alpha at even higher. Used to treat shock by increasing dose to stimulate appropriate receptors. |
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Term
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Definition
| Only Beta-1 and Beta-2 receptors stimulated. Stimulates Beta best of Iso/NE/Epi. Not useful, but may be used for asthma |
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Term
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Definition
| Pure Alpha agonist. Not a catecholamine (lost –OH at position 4 of benzene ring) |
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Term
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Definition
| Pure Alpha agonist. Not a catecholamine (lost –OH at position 4 of benzene ring) |
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Term
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Definition
| Pure Alpha agonist. Not a catecholamine (lost –OH at position 4 of benzene ring) |
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Term
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Definition
| Indirect sympathomimetic. Displaces NE in CNS. Has CNS activity bc lacks –OH at position 3 AND 4 on benzene ring |
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Term
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Definition
| Selective Beta-2 agonist/bronchodilator. Avoids ^HR that comes with Beta-1/Beta-2 agonists. Ring hydroxyl shifted so COMT inactive -> increased t ½ |
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Term
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Definition
| Selective Beta-2 agonist/bronchodilator. Avoids ^HR that comes with Beta-1/Beta-2 agonists. Ring hydroxyl shifted so COMT inactive -> increased t ½ |
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Term
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Definition
| Selective Beta-2 agonist/bronchodilator. Avoids ^HR that comes with Beta-1/Beta-2 agonists. Ring hydroxyl shifted so COMT inactive -> increased t ½ |
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Term
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Definition
| Beta-1 selective agonist. ^CO with less reflex tachycardia (such as with Isoproterenol). Used for CHF |
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Term
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Definition
| Stimulates Alpha-2 (feedback inhibitor) receptors in CNS that decrease BP. Used to relieve HTN. Can be used to relieve symptoms of narcotic withdrawal |
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Term
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Definition
| Irreversible Alpha antagonist (covalent). Receptor can no longer be used. Maximum effect of agonist is decreased |
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Term
| -zosins (Prazosin, Terazosin, Doxazosin) |
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Definition
| Competitive Alpha antagonist/blocker. Alpha-1 selective |
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Term
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Definition
| Nonselective (Alpha-1 and Alpha-2) competitive antagonist |
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Term
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Definition
| Prototype of Beta blockers. Beta-1 and Beta-2 |
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Term
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Definition
| Beta blocker. Cardioselective (Beta-1 only). Excreted only by kidney so t ½ ^^ (high lipophilicity) |
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Term
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Definition
| Beta blocker. Not cardioselective. Excreted only by kidney so t ½ ^^ (high lipophilicity) |
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Term
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Definition
| Beta blocker. Cardioselective (Beta-1 only) |
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Term
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Definition
| Beta blocker. Partial agonist activity. At rest some ^HR, but w exercise, decreased max HR (~130). Supposedly good for asthmatics but not in reality |
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Term
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Definition
| Beta and Alpha blocker. No more effective at decreasing BP than regular Beta-blockers |
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Term
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Definition
| Beta blocker with short t ½ (5-10 mins), so used as IV drip to determine efficacy of Beta-blocker in MI patients |
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Term
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Definition
| PSNS neurotransmitter. Dose for CV< glands/SMC < Ganglia < NMJ (muscarinic). Ganglia< NMJ < CV < glands/SMC (nicotinic) |
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Term
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Definition
| Stimulates muscarinic receptors. Use of muscarinics is rare |
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Term
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Definition
| Stimulates nicotinic receptors at low doses. Blocks at higher doses (“depolarizing blockade”). Not degraded by AChE. Stimulation then blockade in SNS and PSNS. Only blockade in NMJ (-> resp paralysis) |
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Term
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Definition
| Muscarinic of choice. Used for GI stimulation in hypomotility, treat urinary retention |
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Term
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Definition
| Anti-muscarinic. Blocks PSNS, used for preanesthetic (dry secretions and constrict airways). Dilates pupils, contraindicated with glaucoma. Mad as hatter, dry as bone, red as beet, blind as stone. |
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Term
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Definition
| Antihistamine. Can block muscarinic receptors (classical H1 blockers also block muscarinic receptors) |
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Term
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Definition
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Term
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Definition
| Antimuscarinic. Oxygen bridge ^CNS penetration. Used for motion sickness. |
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Term
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Definition
| Antimuscarinic. Reduced CNS effects (quaternary amine) make it more desirable than atropine as preanesthetic |
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Term
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Definition
| Antimuscarinic. Reduced CNS effects (quaternary amine) make it more desirable than atropine as preanesthetic |
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Term
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Definition
| Ganglionic (SNS and PSNS) blocker (nicotinic) |
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Term
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Definition
| Ganglionic (SNS and PSNS) blocker (nicotinic) |
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Term
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Definition
| Competitive antagonist of AChE. Short duration (10 minutes), so used to test for myasthenia gravis |
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Term
| -stigmines (Neostigmine, Physostigmine, Pyridostigmine) |
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Definition
| Carbamates. Mimic ACh but slow hydrolysis (2-8 hrs). AChE inhibitor used for myasthenia gravis |
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Term
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Definition
| Organophosphate. Prodrug (-> Paraoxon). AChE inhibitor for mammals and insects. Muscarinic (bronchoconstriction and secretions), nicotinic (paralyze respiratory muscles), CNS (decreased resp drive) |
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Term
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Definition
| Organophosphate. Prodrug (-> Malaoxon). AChE inhibitor selective for insects, so used as insecticide |
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Term
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Definition
| Organophosphate. Muscarinic (bronchoconstriction and secretions), nicotinic (paralyze respiratory muscles), CNS (decreased resp drive) |
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Term
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Definition
| Antidote to organophosphates. Potentiated with atropine (anti-muscarinic) |
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Term
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Definition
| Blocks T-type calcium channel. Drug of choice for petit mal seizures. |
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Term
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Definition
| Used for petit mal, absence, and tonic-clonic seizures. Hepatotoxic, so do LFTs. Divalproex Na is enteric mixture of valproic acid and sodium valproate to reduce GI upset (GI “seizures”) |
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Term
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Definition
| Benzodiazepine (GABA channel potentiator). Long acting with good efficacy against petit mal seizures. Tolerance will occur |
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Term
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Definition
| GABA channel potentiator (?). Designed as GABA agonist but found to not mimic GABA. Renal excretion. No known significant interactions. Used in combo with other anti-Sz drugs, chronic pain of neural origin |
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Term
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Definition
| Prolongs inactivation state of Na+ channels. When neuron is firing fast, inactivation is more prominent. Related to tricyclic antidepressants. Drug of choice for partial seizures |
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Term
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Definition
| Hydantoin. Limits spread of Sz in brain. Effective against grand mal and partial seizures. Nonlinear effect and variable between patients. Gingival hyperplasia |
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Term
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Definition
| Sodium channel inhibitor. Anti-epileptic drug |
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Term
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Definition
| “New” anti-epileptic drug, has replaced Phenytoin |
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Term
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Definition
| Barbiturate. Enhances GABA. Used for grand mal and simple partial Sz. OK for complex partial. May exacerbate petit mal. Tolerance forms to sedative effects but not to anticonvulsive effect (beneficial) |
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Term
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Definition
| “New” anti-epileptic drug, has replaced Phenytoin |
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Term
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Definition
| Deoxy barbiturate. Similar to Phenobarbital in uses for epilepsy. Metabolized to Phenobarbital and Phenyethylmalonamide (used for complex partial seizures) |
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Term
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Definition
| Benzodiazepine (enhance GABA). Used to treat status epilepticus. Chosen over phenobarbital bc quick onset and decreased effect on respiration |
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Term
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Definition
| Benzodiazepine (enhance GABA). Used to treat status epilepticus. Chosen over phenobarbital bc quick onset and decreased effect on respiration |
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Term
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Definition
| Antagonist to Glutamate’s NMDA receptor. Used for Alzheimer. Excessive glutamate (-> Ca++) in CNS can lead to neuronal damage |
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Term
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Definition
| Cholinesterase inhibitor used for Alzheimer. Keeps patient out of nursing home for several more months |
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Term
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Definition
| Narcotic. Abused for euphoria and sedative action. OD -> respiratory depression (use Naloxone). Physical and psychological dependence |
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Term
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Definition
| Indirect-acting sympathomimetic. Displaces NE in CNS. Same effects as cocaine. |
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Term
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Definition
| Indirect-acting sympathomimetic. Displaces NE in CNS. Same effects as cocaine. |
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Term
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Definition
| Indirect-acting sympathomimetic. Current use for narcolepsy and ADHD. Increases BP, HR, arrhythmias, mydriasis. Tolerance occurs to anorexia, euphoria, lethal effects |
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Term
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Definition
| Hallucinogen. No medicinal use, strong psychological dependence, little physical dependence. Small doses produce frank hallucinations. Autonomic effects same as SNS stimulation |
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Term
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Definition
| Hallucinations at high doses (not like LSD – milder). Strong psychological dependence. Metabolites in urine for at least 2-3 weeks. |
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Term
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Definition
| Stimulant and psychedelic effects. Produces degeneration of 5HT in nerve cells and axons in rats. CSF of abusers is low in 5HT metabolites. Abusers get very depressed when they withdraw |
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Term
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Definition
| Stimulant and psychedelic effects. Produces degeneration of 5HT in nerve cells and axons in rats. CSF of abusers is low in 5HT metabolites. Abusers get very depressed when they withdraw |
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Term
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Definition
| PCP. Produces numbness, slurred speech at low doses. Analgesia, hallucinations, psychotic states and coma at high doses (bad combo) . Neuroleptics and hospitalization often required. |
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Term
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Definition
| Narcotic with long t ½. Smaller sedative effect (less reinforcing). Less withdrawal. |
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Term
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Definition
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Term
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Definition
| Crosses the BBB easily. Acts as extra precursor to allow surviving dopamine neurons to increase their output of dopamine. Converted by AAADC/VitB6 to Dopamine. Side effects: psychosis, N/V, arrhythmias |
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Term
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Definition
| Blocks peripheral AAADC. Allows L-Dopa dose to dramatically decrease -> less N/V, fewer arrhythmias, no concerns about VitB6 |
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Term
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Definition
| Cofactor for AAADC. Allows peripheral conversion of L-Dopa to Dopamine. Not preferable, bc L-Dopa is only useful for Parkinson in the CNS |
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Term
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Definition
| Antiviral agent that works by increasing dopamine output of nigrostriatal neurons. Parkinson |
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Term
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Definition
| Specific MAO-B inhibitor. Does not cause wine and cheese syndrome. Prevents dopamine degradation -> ^levels |
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Term
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Definition
| Dopamine agonist that can easily cross BBB. Parkinson |
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Term
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Definition
| Dopamine-2 agonist. Can cross BBB. Parkinson |
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Term
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Definition
| Dopamine-2 agonist. Can cross BBB. Parkinson |
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Term
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Definition
| COMT inhibitor. Prevents formation of O-Methyl-Dopa (inactive), so more L-Dopa reaches CNS |
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Term
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Definition
| Antipsychotic. Phenothiazine derivative. Strong hypotensive and sedative. Strong anti-muscarinic effects. These prevent EPS but give blurred vision, constipation, etc. Low tendency to produce acute dystonia |
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Term
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Definition
| Antipsychotic. Minimal sedation and only mildly antimuscarinic. Associated with high incidence of acute dystonia |
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Term
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Definition
| “Old” antipsychotic. Dopamine blocker. Not antimuscarinic so no ability to decrease movement difficulties (EPS) |
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Term
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Definition
| Antimuscarinic used to treat Parkinson Syndrome (not Disease). Use with Dopamine blockers |
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Term
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Definition
| Antimuscarinic used to treat Parkinson Syndrome (not Disease). Use with Dopamine blockers |
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Term
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Definition
| New/atypical antipsychotic. Blocks 5HT and all Dopamine receptors. Only mild blockade at D2 so no EPS. Antimuscarinic, hypotensive. Be careful of agranulocytosis |
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Term
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Definition
| New/atypical antipsychotic. Blocks 5HT and all Dopamine receptors. Only mild blockade at D2 so no EPS. Sedative, hypotensive. No agranulocytosis |
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Term
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Definition
| New/atypical antipsychotic. Blocks 5HT and all Dopamine receptors. Only mild blockade at D2 so no EPS. Sedative, hypotensive. No agranulocytosis |
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Term
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Definition
| New/atypical antipsychotic. Blocks 5HT and all Dopamine receptors. Only mild blockade at D2 so no EPS. Sedative, hypotensive. No agranulocytosis |
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Term
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Definition
| New/atypical antipsychotic. Blocks 5HT and all Dopamine receptors. Only mild blockade at D2 so no EPS. Sedative, hypotensive. No agranulocytosis |
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Term
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Definition
| D2 partial agonist with minimal sedative and hypotensive effects. “Dopamine stabilizer” |
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Term
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Definition
| GABA agonist. Spasmolytic. Hyperpolarizes cells and inhibits release of excitatory transmitters. Similar to Diezapam. Sedation a problem |
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Term
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Definition
| Blocks release of Ca++ from sarcoplasmic reticulum. Spasmolytic. Acts peripherally. Major side effect is generalized muscle weakness. Used to treat malignant hyperthermia |
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Term
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Definition
| Decreases muscle spindle afferent activity (peripheral action) by blocking interneurons. Spasmolytic |
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Term
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Definition
| Acts in the CNS to decrease repetitive motor activity. Spasmolytic |
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