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60 Cards in this Set
- Front
- Back
Cholinergic agonists (3)
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Carbachol - ganglion stimulating
Bethanechol, Pilocarpine - muscarinic agonists |
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Actions of cholinergic agonists
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Decrease HR, CO, and BP
Vasodilation GI, bronchiolar, salivary secretions GI motility GU detrussor muscle contraction Eye: Miosis |
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Acetylcholinesterase Inhibitors (Reversible, 4)
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Neostigmine
Physostigmine Pyridostigmine Edrophonium |
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Types of muscarinic receptors on target tissue
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M1: Gastric parietal cells
M2: Cardiac cells, smooth muscle M3: Exocrine glands, smooth muscle |
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Hexamethonium
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Nicotinic ACh receptor antagonist: ganglionic blocker. Blocks both SNS and PSNS.
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AchE toxicity (Organophosphate poisoning)
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DUMBBELSS:
diarrhea urination miosis bronchospasm bradycardia excitation of CNS, skeletal muscle lacrimation salivation sweating |
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Antidote for AchE toxicity
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Atropine (muscarinic antagonist)
Pralidoxime (chemical antagonist, regeneratives active cholinesterase) |
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Muscarinic antagonists (and uses)
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Atropine: mydriasis and cycloplegia
Benztropine: Parkinson's, decreases movement Scopolamine: motion sickness Ipratropium: Asthma, COPD |
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Atropine: Effects and side effects
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Effects: blocks SLUD
salivation lacrimation urination defecation Side effects: hot as a hare: increased body temperature dry as a bone: decreased secretions (saliva, sweat) mad as a hatter: SNS-type effects blind as a bat: pupil dilation red as a beet: flushed skin |
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Sympathomimetics: Catecholamines and main receptors
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Epinephrine: a1, a2, b1, b2
Norepinephrine: a1, a2, b1 Isoproterenol: b1=b2 Dopamine: D1 = D2 > b > a Dobutamine: b1 > b2 |
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Amphetamine
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Sympathomimetic, indirect general agonist, releases stored catecholamines.
Uses: narcolepsy, obesity, ADD |
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Ephedrine
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Sympathomimetic: indirect agonist, releases stored catecholamines.
Uses: nasal decongestion, urinary incontinence, hypotension |
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Phenylephrine
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Sympathomimetic: a1 > a2 agonist.
Uses: pupil dilator, vasoconstriction, nasal decongestion. |
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Albuterol, Terbutaline
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Sympathomimetic: B2 > B1.
Uses: short acting beta agonist in asthma, bronchodilation |
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Cocaine
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Sympathomimetic: Indirect general agonist, uptake inhibitor.
Uses: causes vasoconstriction and local anesthesia. |
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Clonidine, methyldopa
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Sympathomimetic: centrally-acting a-agonist. Decreases central adrenergic outflow.
Uses: hypertension, especially with renal disease. |
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Ganglionic cholinergic agonists (3)
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Nicotine
Trimethaphan Mecamyline - No therapeutic use; widespread effects |
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NMJ cholinergic drugs: agonists and antagonists
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Depolarizing drugs are agonists (nicotine, succinylcholine).
Non-depolarizing drugs are antagonists (tubocurarine). |
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Non selective alpha blocker
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Phenoxybenzamine (irreversible)
Phentolamine (reversible) Used for pheochromocytoma, can cause orthostatic hypotension, reflex tachycardia. |
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Alpha 1 blockers
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Prazosin
Terazosin Doxazosin Used for HTN, urinary retention in BPH. Can cause hypotension, dizziness, headache. |
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Alpha 2 blockers
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Mirtazapine
Used in depression Causes sedation, increased serum cholesterol, increased appetite. |
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Beta 1 blockers
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A BEAM:
acebutolol betaxolol esmolol atenolol metaprolol Uses: Cardioselective. Decreases CO, renin secretion in HTN. Decreases HR and contractility, O2 consumption in angina pectoris. Slows progression of CHF. Decrease mortality after MI. |
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Non selective beta blockers and toxicities
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Propanolol, timolol, pindolol, nadolol, labetalol.
Toxicities: impotence, exacerbation of asthma, cardiovascular side effects (bradycardia, AV block, CHF), CNS (sedation, sleep alterations) *Use with caution in diabetics - hides effects of hypoglycemia |
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Glaucoma drugs: approaches
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a agonists (epinephrine, brimonidine)
b blockers (timolol, betaxolol, carteolol) diuretics (acetazolamide) cholinomimetics (pilocarpine, physostigmine, echothiophate) prostaglandin (Latanoprost) |
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Goals of glaucoma treatment
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Constrict pupil (more PSNS, less SNS effect)
Increase fluid outflow (a agonist) Decrease fluid production (b blocker) |
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Treatment of Parkinson's
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Parkinsons: destruction of dopaminergic neurons in substantia nigra.
Dopamine agonists: l-dopa/carbidopa, bromocriptine, pramipexole, ropinirole, amantadine (enchances DA release) MAO inhibitors: selegiline (MAO-B selective) Antimuscarinics: Benztropine COMT inhibitors: entacapone, tolcapone BALSA bromocriptine amantadine levodopa (L-dopa/carbidopa) selegiline antimuscarinics |
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Levodopa/Carbidopa
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Parkinson's treatment.
L-dopa can cross BBB, is converted to DA by dopa decarboxylase in CNS. Carbidopa inhibits peripheral decarboxylase to prevent peripheral activation of DA. Peripheral DA effects: arrythmias. Other SE: dyskinesia. |
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MAO selectivity
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MAOa: breaks down 5HT, NE.
MAOb: breaks down DA. |
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Selegiline
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MAOb-selective inhibitor. Increases CNS DA, used in treatment of Parkinson's.
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Sumatriptan
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Serotonin agonist, used for acute migraines, cluster headache attacks. Causes chest discomfort, mild tingling (contraindicated in pts with CAD or Prinzmetal's angina). Strong anticholinergic side effects.
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Phenytoin: MOA
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Blocks the voltage-gated Na channel once it is open (activity dependent INACTIVATION).
Uses: simple & complex partial seizures, tonic-clonic seizures. |
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Carbamazepine: MOA
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Blocks the voltage-gated Na channel once it is open (activity dependent INACTIVATION).
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Lamotrigine: MOA
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Inhibits voltage-gated Na+ and Ca+2 channels.
Uses: Simple & complex partial seizures, tonic-clonic seizures. |
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Gabapentin: MOA
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Increase GABA release
Used for Simple & complex partial seizures, tonic-clonic seizures. |
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Epilepsy drugs (9)
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Phenytoin
Carbamazepine Lamotrigine Gabapentin Topiramate Phenobarbital Valproate Ethosuximide Benzodiazepines (Diazepam, lorazepam) |
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Topiramate: MOA
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Inhibits Na+ channels, potentiates GABAergic function.
Uses: partial seizures (simple & complex) |
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Phenobarbital: MOA
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Barbiturate. Bind to GABAa receptors and potentiate them by increasing the duration of their opening. Can work even if GABA is not bound (unlike BZD).
Uses: Simple & complex partial seizures, tonic-clonic seizures. |
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Treatment for absence seizures
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Valproate
Ethosuximide |
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Valproate: MOA
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Increases Na channel inactivation, increases GABA concentration - subtle effects on multiple channels.
Uses: all seizures, especially absence. |
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Ethosuximide: MOA
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Blocks thalamic T-type Ca++ channels, disrupting slow rhythmic firing of thalamic neurons.
First choice for absence seizures. *Hepatic toxicity |
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Benzodiazepines: MOA
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Potentiates GABAa receptor by increasing frequency with which it opens.
Uses: Status seizures. |
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Drugs for status epilepticus seizures
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Benzodiazepines, phenytoin
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Phenytoin: profile
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MOA: use-dependent blockade of Na+ channels.
Clinical use: grand-mal seizures, class IB anti-arrythmic. Toxicity: nystagmus, ataxia, diplopia, lethargy. Chronic use produces gingival hyperplasia in children, peripheral neuropathy, hirsutism, megaloblastic anemia (decrease vitamin B12), malignant hyperthermia (rare), teratenogenic (fetal hydantoin syndrome) |
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Psychiatric drugs: Classes (5)
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Benzodiazepines
Barbiturates Neuroleptics (work on DA) Atypicals (DA, 5HT) Lithium |
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Barbiturates: drugs, MOA
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Phenobarbital
Pentobarbital Thiopental Secobarbital MOA: facilitate GABAa action by increasing duration of Cl- channel opening, thus decreasing neuron firing. (BarbiDURATE = increased DURATion of Cl- channel opening) |
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Barbiturates: uses, side effects
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Use: sedative for anxiety, seizures, insomnia, induction of amnesia (thiopental).
Side effects: dependence, additive CNS depression with alcohol, respiratory or CV depression (can lead to death), induction of cytochrome P450. |
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Benzodiazepines: drugs, MOA
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Diazepam
Lorazepam Triazolam Temazepam Oxazepam Midazolam Chlordiazepoxide MOA: facility GABAa action by increasing frequency of Cl- channel opening (FREnzodiazepines have increased FREquency of Cl- channel opening) |
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Benzodiazepines: Clinical use, side effects
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Uses: anxiety, spasticity, status epilepticus (diazepam), detoxification (esp alcohol withdrawal with DT)
Side effects: dependence, additive CNS depression with alcohol. Less risk of respiratory depression & death than with barbiturates. Treat OD with flumazenil (competetive GABA antagonist). |
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Overdose antidotes:
Organophosphates Benzodiazepines Morphine |
Organophosphates: atropine
Benzodiazepines: flumazenil Morphine: naloxone (all antagonists) |
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Neuroleptics
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thioridazine, haloperidol, fluphenazine, chlorpromazine
MOA: most antipsychotics block D2 receptors (excess DA effects connected with schizophrenia) Use: schizophreniz, psychosis Toxicity: extrapyramidal effects, sedation, endocrine side effects, anti- muscarinic, a adrenergic, and histaminic effects (orthostatic hypotension). |
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Conditions associated with antipsychotics
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(antipsychotics block dopamine)
Neuroleptic malignant syndrome: rigidity, autonomic instability, hyperpyrexia - treat with dantrolene and DA agonists. Tardive dyskinesia: stereotypic oral-facial movements probably due to DA receptor sensitization; results of long-term antipsychotic use. |
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Atypical antipsychotics
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Clozapine, olanzapine, risperidone
MOA: block 5HT2 and DA receptors. Uses: schizophrenia, positive and negative sxs. Olanzapine is also used for OCD, anxiety disorder, and depression. SE's: fewer extrapyramidal, anticholinergic than other antipsychotics |
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Lithium
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Antipsychotic.
MOA not established - inhibition of IP3 cascade? Use: mood stabilizer for bipolar disorder, blocks relapse and acute manic events. Toxicity: tremor, hypothyroidism, polyuria (ADH antagonist --> nephrogenic DI), teratogen (cardiac). Narrow therapeutic index. |
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Antidepressants: Classes (4)
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SSRI's
TCA's Heterocyclics MAOI's |
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SSRI's
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Fluoxetine
Sertraline Paroxetine Citalopram MOA: blocks reuptake of serotonin into presynaptic cell. Use: endogenous depression. Toxicity: fewer than TCA's. CNS stimulation - anxiety, insomnia, tremor, anorexia, nausea, and vomiting. With MAOI's: Serotonin syndrome - hyperthermia, muscle rigidity, cardiovascular collapse. |
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Tricyclic antidepressants
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Imipramine
Amitriptyline Desipramine Nortriptyline Clomipramine Doxepin MOA: block reuptake of NE and serotonin Use: endogenous depression, bedwetting (imipramine decreases stage 4 sleep), OCD SE's: sedation, alpha-blocking, anticholinergic effects (tachycardia, urinary retention). Toxicity: Tri-C's - Convulsion, Coma, Cardiotoxicity. |
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Heterocyclics
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Used in major depressive disorders:
Tazodone - inhibits 5HT reuptake Buproprion - Smoking cessation. MOA unknown. Venlafaxine - Inhibits 5HT, DA, NE reuptake, used in GAD. Mirtazapine - a2 antagonist (increased release of Ne, 5HT), potent 5HT2 receptor antagonist Maprotiline - blocks NE reuptake. |
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MAO inhibitors
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Phenelzine
Tranylcypromine MOA: nonselective MAO inhibition (A > B, so NE and 5HT increased) Use: atypical depression (psychotic or phobic), anxiety, hypochondriasis Toxicity: hypertensive crisis with tyramine ingestion and meperidine; CNS stimulation. Contraindicated with SSRI's, B agonists (serotonin syndrome). |
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Opioid analgesics: drugs and MOA
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Morphine
Fentanyl Codeine Heroin Methadone Meperidine Dextromethorphan MOA: act as agonists at opioid receptors to modulate synaptic transmission. Mu = morphine Delta = enkephalin Kappa = dynorphin |
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Opioid analgesics: clinical uses, toxicities
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Dextromethorphan = pain, cough supression
Loperamide, diphenoxylate = diarrhea Methadone = maintenance programs for addicts. Toxicity: addiction, respiratory depression, constipation, miosis, additive CNS depression with other drugs. Tolerance does NOT develop to miosis and constipation. Treat OD with naloxone, naltrexone (opioid receptor antagonist). |