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58 Cards in this Set
- Front
- Back
G protein Gs
(a) receptors (b) Effector (c) Second Messenger response |
(a) beta1, beta2, D1, H2, V2
(b) Adenylyl cyclase (c) increased cAMP |
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G protein Gi
(a) receptors (b) effector (c) second messenger response |
(a) alpha2, M2, D2
(b) adenylyl cyclase (c) decreased cAMP |
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G protein Gq
(a) receptors (b) effector (c) second messenger response |
(a) alpha, M1, M3, H1,V1
(b) phospholipase (c) increased IP3, increased IC Ca2+, DAG |
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Bethanechol
(a) classification (b) clinical application (c) action |
(a) direct cholinergic agonist
(b) postop and neurogenic ileus and urinary retention (c) activates bowel and bladder SM; resistant to AchE |
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Carbachol
(a) classification (b) clinical application |
(a) direct cholinergic agonist
(b) glaucoma, pupillary contraction, and release of intraocular pressure |
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Pilocarpine
(a) classification (b) clinical application (c) action |
(a) direct cholinergic agonist
(b) potenti stimulator of sweat, tears, saliva (c) contracts ciliary muscle of eye (open angle), pupillary sphincter (narrow angle); resistant to AChE |
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Methacholine
(a) classification (b) clinical application (c) action |
(a) direct cholinergic agonist
(b) challenge test for diagnosis of asthma (c) stimulates muscarinic receptors in airway when inhaled |
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Neostigmine
(a) classification (b) clinical application (c) action |
(a) anticholinesterase
(b) postop and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular jct blockage (postop) (c) increase endogenous Ach; no CNS penetration. |
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Pyridostigmine
(a) classification (b) clinical application (c) action |
(a) anticholinesterase
(b) myasthenia gravis (long acting) (c) increase enogenous Ach; increase strength; does not penetrate CNS |
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Edrophonium
(a) classification (b) clinical application (c) action |
(a) anticholinesterase
(b) diagnosis of myasthenia gravis (extremely short acting) (c) increase endogenous Ach |
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Physostigmine
(a) classification (b) clinical application (c) action |
(a) anticholinesterase
(b) glaucoma (crosses BBB into CNS) and atropine overdose (c) increase endogeous Ach |
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Echothiophate
(a) classification (b) clinical application (c) action |
(a) anticholinesterase
(b) glaucoma (c) increase endogenous Ach |
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Describe treatment for the following toxicity:
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, and Salivation (also abdominal cramp) |
Cholinesterase inhibitor poisoning
Antidote: atropine (muscarinic antagonist) plus pralidoxine (chemical antagonist used to regenerate active cholinesterase). |
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Classification and Application of atropine in the eye
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Muscarinig antagonist
Produce mydriasis and cycloplegia |
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Classification and Application of benzotropine
|
Muscarinig antagonist
Parkinson's disease |
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Classification and Application of Scopolopine
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Muscarinig antagonist
Motion sickness |
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Classification and Application of oxybutynin, glycopyrrolate
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Muscarinig antagonist
Reduce urgency in mild cystitis and reduce bladder spasms |
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Classification and Application of ipratropium
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Muscarinig antagonist
Asthma, COPD |
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Classification and Application of Methscopolamine (also pirenzepine, propantheline)
|
Muscarinig antagonist
Peptic ulcer treatment |
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Atropine classification and effect
|
Muscularinic antagonist
Increase pupil dilation (cycloplegia) Decrease airway secretions Decrease stomach acid secretions Decrease GI motility |
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Atropine toxicity
|
Increase body temperature, rapid pulse
Dry mouth Flushed skin Cycloplegia Constipation Disorientation Can cause acute angle glaucoma in elderly, urinary retention in men with BPH, and hyperthermia in infants |
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Hexamethonium
(a) classification (b) clinical use (c) toxicity |
(a) nicotinic antagonist
(b) ganglionic blocker. Used in lab models to prevent vagal reflex response to changes in BP (prevents reflex bradycardia by NE) (c) severe orthostatic hypotension, blurred vision, constipation, sexual dysfct |
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Epinephrine
(a) classification (b) mechanism/selectivity (c) applications |
(a)drug direct sympathomimetic
(b) alpha1,2 and beta 1,2 (low dose selective for beta 1) (c) anaphylaxis, glaucoma (open angle), asthma, hypotension |
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Norepinephrine
(a) classification (b) mechanism/selectivity (c) applications |
(a)drug direct sympathomimetic
(b) alpha1, alpha2>beta 1 (c) hypotension, (but decreased renal perfusion) |
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Isoprotenerenol
(a) classification (b) mechanism/selectivity (c) applications |
(a) direct sympathomimetics
(b) beta1=beta2 (c) AV block (rare) |
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Dopamine
(a) classification (b) mechanism/selectivity (c) applications |
(a) direct sympathomimetics
(b) D1=D2>beta>alpha, inotropic and chronotropic (c) shock (increased renal perfusion), heart failure |
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Dobutamine
(a) classification (b) mechanism/selectivity (c) applications |
(a) direct sympathomimetics
(b) beta1>beta2 inotropic but not chronotropic (c) shock, heart failure, cardiac stress testing |
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Albuterol/Terbutaline
(a) classification (b) mechanism/selectivity (c) applications |
(a) direct sympathomimetics
(b) alpha1>alpha2 (c) albuterol for acute asthma; terbulatine reduces premature uterine contractions |
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Ritodrine
(a) classification (b) mechanism/selectivity (c) applications |
(a) direct sympathomimetics
(b) beta 2 (c) reduces premature uterine contractions |
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Amphetamine
(a) classification (b) mechanism/selectivity (c) applications |
(a) indirect sypmathomimetics
(b) indirect general agonist, released stored catecholamines (c) narcolepsy, obesity, ADD |
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Ephedrine
(a) classification (b) mechanism/selectivity (c) applications |
(a) indirect sympathomimetics
(b) indirect general agonist, releases stored catecholamines (c) nasal decongestion, urinary incontinence, hypotension |
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Cocaine
(a) classification (b) mechanism/selectivity (c) applications |
(a) indirect sympathomimetics
(b) indirect general agonist, uptake inhibitor (c) causes vasoconstriction and local anesthesia |
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Clonidine, alpha methyldopa
(a) classification (b) mechanism/selectivity (c) applications |
(a) sympathoplegics
(b) centrally acting alpha 2 agonist, decreased central adrenergic outflow (c) HTN, esp w/renal disease (no decr in blood flow to kidney) |
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Phenoxybenzamine
(a) classification (b) applications (c) toxicity |
(a) non selective alpha blocker
(b) pheochromocytoma (use phenoxybenzamine before removing tumor since high levels of released catecholamines will not be able to overcome blockage) (c) orthostatic hypotension, reflex tachycardia |
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Alpha 1 selective blockers
|
Prazosin, terazosin, doxazosin
|
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Prazosin, terazosin, doxazosin
(a) classification (b) applications (c) toxicity |
(a) alpha 1 selective blocker
(b) HTN, urinary retention in BPH (c) 1st dose orthostatic hypotension, dizziness, headache |
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Mirtazapine
(a) classification (b) application (c) toxicity |
(a) alpha 2 selective blocker
(b) depression (c) sedation, increased serum cholesterol, increased appetite |
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Beta blocker: clinical applications
|
HTN (decr CO and renin)
Angina pectoris (decrease HR, contractility, resulting in decr O2 consumption) MI (beta blockers decrease mortality) SVT-propranolol, esmolol (decr AV conduction velocity) CHF (slows prgoression of chronic failure) Glaucoma-timolol-decreases secretion of aqueous humor |
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Nonselective antagonists
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Propranolol, timolol, nadolol, pindolol, and labetalol
|
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Beta 1 selective antagonists
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Acebutolol (partial agonist), betaxolol, esmolol (short acting), atenolol, metoprolol
|
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Non selective alpha and beta antagonists
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Carvediolol, labetalol
|
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Partial beta agonists
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Pindolol, acebutolol
|
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Toxicity of beta blockers
|
Impotence, exacerbation of asthma, CV adverse effects (bradycardia, AV block, CHF), CNS adverse effects (sedation, sleep alterations); use with caution in diabetics.
|
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Synthesis of histamine
|
Histidine converted to histamine by histadine decarboxylase
|
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Location of histamine
|
Circulating basophils and mast cells
|
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H1 antagonists
(a) list common (b) clinical use (c) sedation, dry mucosa |
(a) diphenydramine, promethazine, chlorpheniramine, hydroxyzine, fexofenadine*, loratadine*, cetirizine *
*indicates no CNS entry (b) allergic rxns, motion sickness, OTC (sleep aids and cold meds) (c) sedation, dry mucosa |
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H2 antagonists
(a) list common (b) clinical use (c) notes/toxicity |
(a) cimetidine, ranitidine, famotidine, nizatidine
(b) peptic ulcer disease, GERD, zollinger ellison syndrome (c) cimetidine: P450 inhibition, antiandrogen effect |
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Synthesis and degradation of serotonin
|
Tryptophan converted to 5HT by tryptophan hydroxylase. MAO degrades serotonin into 5H1AA
|
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5HT1 (A-F)
(a) second messenger (b) action |
(a) Gi, decr cAMP
(b) CNS, behavioral effects (sleep, feeding, thermoreg, anxiety), vasoconstriction |
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5HT2(A-C)
(a) second messenger (b) action |
(a) Gq; increase IP3, DAG
(b) CNS, behavioral effects, smooth muscle contraction, platelet aggregation |
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5HT3
(a)second messenger (b) action |
(a) ion channel
(b) CNS (area postrema), PNS, emesis, anxiety |
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5HT4
(a) second messenger (b) action |
(a) Gs; increase cAMP
(b) CNS: neuronal excitation, GI motility |
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Sumatriptan, naratriptan
(a) mechanism of action (b) clinical use (c) notes/toxicity |
(a) 5HT1D agonist
(b) migraines (c) n/a |
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Buspirone
(a) mechanism of action (b) clinical use (c) notes/toxicity |
(a) 5HT1A partial agonist
(b) anxiety disorders (c) lower addition potential than other drugs like benzos |
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Ondasetron
(a) mechanism of action (b) clinical use (c) notes/toxicity |
(a) 5HT3 antagonist
(b) emesis (c) mainly for postop or chemo induced n/v |
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SSRI's
(a) mechanism (b) clinical use (c) notes/toxicity |
(a) selectively block 5HT reuptake
(b) anxiety disorders, depression (c) sexual dysfct, interaction w/MAOI's can lead to serotonin syndrome |
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Ergot alkyloids (ergonovine, ergotamine, methysergide, bromocriptin, pergolide, LSD)
(a) mechanism of action (b) clinical use (c) notes/toxicity |
(a) agonists, partial agonists, and antagonists at 5HT and alpha receptors; some are agonists or partial agonists at DA receptors
(b) postpartum hemorrhage (ergonavine, ergotamine) -migraines (ergotamine for acute, methysergide for prophylaxis) -parkinson's disease, hyperprolactinemia (bromo, pergolide) -abuse (LSD) (c) Ergotism (St. Anthony's fire) -mental disorientation, convulsions, muscle cramps, hallucinations, dry gangrene of extremities |
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MAOI's
(a) mechanism of action (b) clinical use (c) notes/tox |
(a) inhibit metabolism of 5HT, NE, and DA by MAO
(b) depression (c) non selective MAO inhibitors -tyramine ingestions can lead to hypertensive crisis |