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190 Cards in this Set
- Front
- Back
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alpha1 and alpha2 receptor substrate preferences
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epi>norepi>dopamine>isoproterenol
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beta receptor substrate preferences
(B1, B2, B3) |
isoproterenol, epinephrine, norepi, dopamine
B1: epi=norepi B2: epi>>>norepi B3: norepi>>>epi |
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B1 receptor locations and function
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heart- increases contractility, heart rate, cardiac output, stroke volume
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B2 receptor locations and function
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in skeletal muscles and blood vessels- decreases diastolic pressure, decreases TPR, vasodilation, bonchodilation
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Alpha receptor locations and function
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in skeletal muscles and blood vessels- increases TPR, vasoconstriction, bonchoconstriction, increases diastolic pressure, increases blood pressure
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effect of low dose epinephrine
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prefers B receptors- increase in heart rate, function, CO, vasodilation, no change in TPR, dilates bronchioles
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effect of high dose epinephrine
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prefers alpha receptors and B1- increases heart contractility, increase in TPR-> increase in blood pressure-> vagal reflex bradycardia
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effect of norepinephrine
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prefers B1 and alpha receptors- increase TPR-> increase BP-> vagal reflex bradycardia
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effect of isoproterenol
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mostly B effects- increase Hr and CO, vasodilation, bronchodilation, no change in BP
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effect of low dose dopamine
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mostly B1 effects- increase heart function, no effect on TPR and BP
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effect of high dose dopamine
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mostly alpha and B1 effects- increase in CO, increase in TPR->vagal reflex bradycardia
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phenylephrine
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synthetic alpha 1 agonist- vasoconstriction, used as a nasal decongestant
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oxymetazoline
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synthetic alpha 1 agonist- vasoconstriction, used as a nasal decongestant
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tetrahydrozoline
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synthetic alpha 1 agonist- vasoconstriction, used as red eye reducer (visine)
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methoxamine
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synthetic alpha 1 agonist- vasoconstriction
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xylazine
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synthetic alpha 2 agonist- CNS mediated effect, negative feedback to reduce catecholamine synthesis and therefore reduce sympathetic outflow to periphery. rebound hypertension. analgesia and sedation, decrease in BP, bradycardia, reverse with yohimbine
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clonidine
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synthetic alpha 2 agonist- CNS mediated effect, negative feedback to reduce catecholamine synthesis and therefore reduce sympathetic outflow to periphery. rebound hypertension. used for ADHD, insomnia, high BP, counter stimulants
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dobutamine
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synthetic B1 agonist- increases heart contractility and CO without requiring high O2 demand. used to temporarily treat heart failure.
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isoproterenol
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synthetic B1/2 agonist- used to treat congestive heart failure due to cardiac stimulatory effects
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albuterol
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synthetic B2 agonist- treat asthma with bronchodilation and smooth muscle relaxation. no cardiac effects
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metapoterenol
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synthetic B2 agonist- bronchodilation and smooth muscle relaxation. no cardiac effects
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terbutaline
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sythetic B2 agonist- used to relax uterus from premature labor
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BRL37344
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synthetic B3 agonist- increase lipolysis
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tyramine
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indirectly acting sympathomimetic- acts to increase norepi in synaptic cleft, powerful CNS stimulant. found in cheese and wine, increases TPR, vagal reflex bradycardia
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amphetamines
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indirectly acting sympathomimetic- acts to increase norepi in synaptic cleft, powerful CNS stimulant, meth and extasy, arousal, psychosis
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cocaine
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indirectly acting sympathomimetic- acts to increase norepi in synaptic cleft, powerful CNS stimulant, vasoconstiction
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imipramine
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indirectly acting sympathomimetic- acts to increase norepi in synaptic cleft, powerful CNS stimulant. tricylcic antidepressant, modulates serotonin and norepi release in CNS
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amitryptyline
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indirectly acting sympathomimetic- acts to increase norepi in synaptic cleft, powerful CNS stimulant. tricylcic antidepressant, modulates serotonin and norepi release in CNS
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ephedrine
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mixed acting sympathomimetic- causes release of endogenous catecholamines and binds adrenergic receptors directly. in Ma Huang herb, not degraded, long duration of action, mild CNS effects, increase BP, increase bronchodilation, increase bladder sphincter tone (treat incontinence)
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pseudoephedrine
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mixed acting sympathomimetic- causes release of endogenous catecholamines and binds adrenergic receptors directly. sudafed, used as a nasal decongestant- low CNS and CV effects
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guanethidine
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adrenergic neuron blockade- inhibits release of norepi from postganglionic neurons. causes initial transient hypertension then decreases BP and decrease CO, used to treat high BP, does not cross BBB
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bretylium
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adrenergic neuron blockade- inhibits release of norepi from postganglionic neurons. does not cross BBB
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clonidine
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adrenergic neuron blockade- inhibits release of norepi from postganglionic neurons. alpha 2 agonist- inhibits norepi release, antihypertensive
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reserpine
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adrenergic neuron blockade- inhibits release of norepi from postganglionic neurons. antihypertensive
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alpha-methyl-DOPA
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adrenergic neuron blockade- inhibits release of norepi from postganglionic neurons. weak alpha1, alpha2 agonist to decrease symp outflow, antihypertensive
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alpha-CH3-p-tyrosine
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adrenergic neuron blockade- inhibits release of norepi from postganglionic neurons.
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disulfiram
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adrenergic neuron blockade- inhibits release of norepi from postganglionic neurons. blocks dopamine conversion to norepi
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pargyline
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catecholamine metabolism blocker- MAO inhibitor, blocks catecholamine degradation, used as an antidepressant. do not mix antidepressants with wine and cheese-> hypertensive crisis
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moclobemide
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catecholamine metabolism blocker- MAO inhibitor, blocks catecholamine degradation, used as an antidepressant. do not mix antidepressants with wine and cheese-> hypertensive crisis
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tolcapone
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catecholamine metabolism blocker- COMT inhibitor
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dibenamine
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alpha receptor antagonist- used to treat hypertension, heart failure, peripheral vascular ischemia, prostatic hyperplasia, shock. alpha1 and 2 antagonist, irreversible, slow onset, long lasting, decreases TPR. used to treat hypertension
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phenoxybenzamine
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alpha receptor antagonist- used to treat hypertension, heart failure, peripheral vascular ischemia, prostatic hyperplasia, shock. alpha1 and 2 antagonist, irreversible, slow onset, long lasting, decreases TPR. used to treat hypertension
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phentolamine
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alpha receptor antagonist- used to treat hypertension, heart failure, peripheral vascular ischemia, prostatic hyperplasia, shock. alpha1 and 2 antagonist, reversible, short acting, decrease TPR, treat hypertension. adverse tachycardia (increase in norepi on B1) and increases norepi release (block presynaptic alpha 2)
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prazosin
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alpha receptor antagonist- used to treat hypertension, heart failure, peripheral vascular ischemia, prostatic hyperplasia, shock. alpha1 antagonist, reversible, does not increase norepi release bc no effect on alpha2 at presynapse. decrease BP with no reflex tachycardia (norepi on B1)
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Tamsulosin
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alpha receptor antagonist- used to treat hypertension, heart failure, peripheral vascular ischemia, prostatic hyperplasia, shock. alpha1 selective antagonist for urinary tract. relaxes muscles in bladder for men with prostatic hyperplasia
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yohimbine
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alpha 2 antagonist- reverses xylazine, reversible, increase norepi release
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tolazoline
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alpha receptor antagonist- used to treat hypertension, heart failure, peripheral vascular ischemia, prostatic hyperplasia, shock.
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antipamezole
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alpha receptor antagonist- used to treat hypertension, heart failure, peripheral vascular ischemia, prostatic hyperplasia, shock.
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alpha antagonist adverse reactions
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hypotension, syncope on standing, reflex tachycardia, nasal stuffiness, increase GI motility
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propranolol
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beta antagonist- used for cardiac arrythmias, hypertension (due to high CO), decrease symp muscle tremors due to stress and anxiety, decrease intraoculat pressure for glaucoma. nonselective b antagonist, decreases HR, contractility and CO, hypersensitivity with withdrawal due to receptor upregulation.
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pindolol
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beta antagonist- used for cardiac arrythmias, hypertension (due to high CO), decrease symp muscle tremors due to stress and anxiety, decrease intraoculat pressure for glaucoma. b1 and b2 antagonist and partial agonist. less severe withdrawal, high doses act like agonist- increase HR, BP, bronchodilation
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timolol
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beta antagonist- used for cardiac arrythmias, hypertension (due to high CO), decrease symp muscle tremors due to stress and anxiety, decrease intraoculat pressure for glaucoma. b1 and b2 blocker for glaucoma treatment
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metoprolol
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beta antagonist- used for cardiac arrythmias, hypertension (due to high CO), decrease symp muscle tremors due to stress and anxiety, decrease intraoculat pressure for glaucoma. selective b1 blocker, cardio selective (lopressor)
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butoxamine
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beta antagonist- used for cardiac arrythmias, hypertension (due to high CO), decrease symp muscle tremors due to stress and anxiety, decrease intraoculat pressure for glaucoma. selective b2 antagonist, black smooth muscle dilation, no cardiac effects
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beta blocker adverse effects
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cardiac failure, bradycardia, dont use with asthma, hypoglycemia shock in diabetics
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GABA
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inhibitory-hyperpolarizes, distributed throughout CNS.
A- Cl- in B- K+ out |
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barbituates
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work on GABA A. sedation, anesthesia, seizure control
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benzodiazepines (valium, xanax)
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work on GABA A. anxiolytics, muscle relaxants, anticonvulsants
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glycine
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inhibitory
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strychnine
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competitive antagonist for glycine
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What gender is a spontaneous pneumothorax common in? Why?
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females on birth control- because estrogen is a muscle relaxant
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domoic acid
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NMDA agonist- neurotoxicity
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opiate receptors
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u-analgesia
k-analgesia delta-euphoria act to inhibit release of NT signaling pain. activates dopamine release in brain. |
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hemicholinium
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synthetic blocker of choline reuptake into the NT
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vesamicol
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blocks storage of Ach in vesicles
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botulism toxin
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prevents synaptobrevin from fusing with NT and releasing Ach -> flaccid paralysis
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nicotinic locations
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ligand gated ion channels- all autonomic ganglia (ps and symp), neuromuscular junctions of skeletal muscle, in adrenal medulla triggering release of epi and norepi, CNS
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muscarinic locations
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parasympathetic actions cells. SLUD. glands (sweat, lacrimal, mucous, salivary), smooth muscle contraction (airways, GI, bladder, gallbladder), pupillary constriction in iris, relaxation of sphincters, slowing Hr
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dominant tone in heart
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parasymp
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dominant tone in eye
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parasymp
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dominant tone in lungs
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symp
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dominant tone in GI
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parasymp
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dominant tone in salivary gland
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parasymp
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dominant tone in blood vessels
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symp
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Ach (as a drug)
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no theraeutic applications, is metabolized too rapidly
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methacholine
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parasympathomimetic drug- selective muscarinic activity, somewhat resistant to AchE, used for urinary and GI, can get cardio effects- bradycardia, hypotension
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carbachol
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parasympathomimetic drug- resistant to AchE, M and N activity, stimulates urinary and GI, induces miosis, increases aqueous humor outflow
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bethanecol
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parasympathomimetic drug- resistant to AchE, selectively muscarinic, used to test pancreatic function bc it increases secretions, stimulates bladder contraction
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pilocarpine
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parasympathomimetic drug- 100X more potent that Ach, mostly muscarinic actions, used to treat dry mouth bc it increases secretions. also used to treat glaucoma. can cause small degree of increased HR and BP
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arecoline
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parasympathomimetic drug- from the betel nut, M and N activity, CNS stimulant like nicotine, increases GI peristalsis
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muscarine
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parasympathomimetic drug- not therapeutic, from mushroom toxicity, SLUD, counter it with atropine
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atropine
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antimuscarinic drug- used as a preanesthetic to decrease resp secretions, induces long lasting miadriasis (weeks), antiasthmatic, OTC cold, decreases nasal and lacrimal secretions, muscarinic specific, tachycardia, decreased GI motility, drying of airways, tremor, CNS delusions, excitement
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homoatropine
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antimuscarinic- less potent than atropine, rapid onset, short duration
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scopolamine
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antimuscarinic- OTC for motion sickness, sedative and euphoria, similar to atropine
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propantheline
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antimuscarinic- can't cross the BBB, decrease GI spasms and diarrhea, decrease spasms in esophagus for horses with choke
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tropicamide
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antimuscarinic- miadriasis, short duration
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nicotine
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nicotinic receptor stimulants- in CNS, can affects symp and ps, stimulates epi and norepi release, can affect NM in skeletal muscle, desensitization
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lobeline
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nicotinic stimulant
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DMPP
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nicotinic stimulant, 3x more potent than nicotine
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hexamethonium
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nicotinic receptor blocker- blocks ps and symp, CNS only
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trimethaphan
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nicotinic receptor blocker- has been used to lower BP during sx
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edrophonium (tensilon)
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AchE inhibitor- irreversible, used to diagnose myasthenia gravis (antibodies against Ach receptors)
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physostigmine (eserine)
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AchE inhibitor- slowly reversible, absorbed via GI tract, can cross BBB, treat MG, treat glaucoma, treat atropine poisoning (increases Ach counteracts muscarinic antagonist)
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neostigmine
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AchE inhibitor- cant cross BBB, treats MG
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pyridostigmine
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AchE inhibitor- longer half life, used by army prophylactically for nerve gas
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demecarium
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AchE inhibitor
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carbaril
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AchE inhibitor- insecticide
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diisopropyl fluorophosphoric acid
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AchE inhibitor- irreversible, very dangerous
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organophosphate poisoning
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AchE inhibitor- treat with PAM immediately to bind some phosphate, treat with atropine
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AchE inhibitor therapeutic uses
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glaucoma->miosis and increased drainage, anesthesia-> reverse nondepolarizing NM blockage, MG-> increase Ach at NM junction, atropine poisoning-> use physostigmine
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4 elements of anesthestic state
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1. unconsciousness
2. amnesia 3. analgesia (not the same as antinocioception) 4. immobility |
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stages of anesthesia
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1. analgesia
2. excitement 3. surgical anesthesia 4. medullary paralysis |
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rank lipid solubility: thiopental, barbital, phenobarbital
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barbital<phenobarbital<thiopental (most immediate effect)
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barbituate MOA
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allosteric binding to GABA A, increases binding of benzodiazepines and GABA also, keeps Cl- channels open longer- less sensitive to incoming excitatory impulses
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barbituates in CNS and PNS
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CNS- directly activates GABA Cl-, depresses autonomic ganglia, gradual CNS depression
PNS-blocks Ach at nicotinic synapses |
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barbituates lack.....
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antinocioceptive properties!!! pain just doesnt register in cortex. combine with strong analgesic like opiate.
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barbituates good for....
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anesthesia, anticonvulsant, decrease intracranial pressure
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barbituate adverse effects
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1. central respiratory depression
2. cardiovascular depression (slow rate, more venous pooling, decrease in sympathetic tone, tachyarrythmias) 3. decrease in renal blood flow 4. splenic sequestration of RBCs 5.very alkaline ph at IV injection (thrombophlebitis) 6. induction of CYP450, will metabolize other drugs |
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barbituate dose
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high protein binding, depends on patient
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barbituate breed caution
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greyhound- far smaller Vd, enzyme saturation
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propofol (class and MOA)
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phenol, sedative-hypnotic, intralipid need to use within a day, allosteric modulation of GABA A, synergism with benzodiazepines
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propofol actions and adverse
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depression of CNS, used for general anesthesia, rapid recovery (minimal drug accumulation), decrease blood flow and intracranial pressure. adverse: resp depression, decrease laryngeal function, hypotension, vasodilation, 10% dogs and cats have a hyperexcited phase (transient, looks like a seizure)
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imidazoles (etomidate) MOA
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very short acting, minimal CV and resp effects, good for high risk patients, binds GABA A, no antinocioception, can inhibit steroid genesis
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cyclohexamine (ketamine and tiletamine)
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dissociative anesthetic, dysphoria, analgesia and anesthesia, violent recovery
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cyclohexamine MOA
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blocks the NMDA nicotinic receptor (glutamate excitatory), can still have skeletal movement- doesnt necessarily need more drugs
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cyclohexamine adverse effects
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shallow irregular breathing, increased HR, arrythmias, increased salivation (give with atropine), muscle rigidity, longer duration in cats
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tiletamine
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like ketamine, longer lasting in cats, usually partenered with a benzodiazepine->zolazepam aka telazol
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fentanyl
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potent opiod
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sufentanil
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potent opiod
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alfentanil
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potent opiod
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remifentanil
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potent opiod
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opiod advantages
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mild CV effects, rapidly metabolized so no hangovers, usually given with benzos, decreases other drugs dosages
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2 most popular inhalant anesthetics
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isoflurane, sevoflurane
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vapor pressure
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pressure that vapor molecules exert when liquid and vapor phases are in equilibrium
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low boiling point means what for vapor pressure?
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high vapor pressure
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lipid solubility =?
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potency, more soluble, more potent
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partial pressure
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individual pressure of each gas/vapor in a mixture of gases
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speed of uptake vs blood solubility and CO
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faster speed of uptake with less CO
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MAC
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minimum alveolar concentration- prevents motor response to a supramaximal noxious stimulus in 50% animals, want 1.3-1.4 MAC for ED95
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MAC for iso, sevo, deso, N2O (%)
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iso (1.3)< sevo (2.1)< deso (7.2)< N2O (200)
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factors that decrease MAC
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old age, pregnancy, hypothermia, hypotension, hypoxemia, hyponatremia, CNS depressant drugs or analgesics
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factors that increase MAC
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hyperthermia, hypernatremia, CNS stimulants (coffee)
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inhalant anesthetic potency rank
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iso>sevo>deso>>>N2O
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inhalant central respiratory depression
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deso>iso>sevo
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inhalant CO depression
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sevo>iso>deso, all can increase HR
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inhalant anesthetic effect on drug metabolism
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decreases blood flow to liver, decreased drug metabolism by 50-70%, decrease drug dosage mornign of sx
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speed of induction of anesthetic inhalants
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N2O>deso>sevo>iso
same for recovery speed |
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sevo advantages over iso
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faster induction and recovery, more rapid adjustment of anesthetic level, slightly less hypotensive, less respiratory depressant
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sevo major disadvantage
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metabolized to compound A, nephrotoxic in some species, not much known about it. used NaOH or KOH instead of soda lime to decrease the risk
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desoflurane clinical highlights
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requires a special vaporizor, fast induction and recovery, quick adjustments
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chlorpromazine and acetylpromazine
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major tranquilizers
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diazepam
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minor tranquilizer
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pentobarbital
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sedative at low doses, hypnotic at higher doses
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sedative
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1. decreased motor activity
2. CNS depression 3. could lead to sleep 4. potentially annesthetic |
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hypnotic
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causing sleep, potentially anesthetic
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nociception
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neurophysiological term denotes activity in the nerve pathways that transmit the signals associated with tissue damage or inflamation
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analgesic
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relieve pain, nsaids, opiods
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NSAIDs
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reduce fever, inflammations, relieve pain
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acetaminophen, ibuprofen, naproxen
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NSAIDS
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Opiods (narcotics)
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interact with opiod receptors, physical dependence, relieves pain
ex: morphine, fentanyl |
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neuroleptanalgesic
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mental detachment, marked analgesia, usually due to a combo of opiod and tranquilizer
ex: morphine and promazine or fentanyl and dropiderol |
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opiod antagonist
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competes for receptor sites with opiods
ex: naloxone |
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opiod agonist/antagonist
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agonists for some receptors and antagonists for others
ex: butorphanol |
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amnesic
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ex: benzodiazepines
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dissociative anesthetic
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ketamine
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local anesthetic actions
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1. increase threshold for excitation
2. slow impulse conduction 3. decrease rate of rise of AP 4. decrease amplitude of AP 5.abolishes ability to generate AP |
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local anesthetic AMIDES
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lidocaine, bupivicaine
metabolized by liver enzymes |
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local anesthetics ESTERS
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procain, tetracaine
metabolized byt psuedocholinesterases in the plasma and liver |
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local anesthetic site of action
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Na channels
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some alpha 2 agonists may act like LA
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xylazine
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fiber size susceptibility to LA neural blockade
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small (sympathetic)>intermediate (sensory)> large (motor)
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can be given with local anesthetics?
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alpha agonists like epinephrine or phenylephrine (not IV) to help increase duration of action but vasoconstriction
also could give sodium bicarbonate |
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lidocaine vs bupivicaine
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lidocaine- much safer- used to treat ventricular arrythmias
bupivicaine- longer lasting effects, can cause Vfib, decrease BP, death |
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onset and duration of local anesthetics
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procaine (30 min) <lidocaine<mepivicaine<bupivicaine (3- 6 hours)
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cetacaine
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tetracaine plus benzocaine, not very safe for cat intubation. causes methemoglobin
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morphine on opiod receptors
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mu and kappa- analgesia
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butorphanol on opiod receptors
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mu antagonist and kappa agonist
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naloxone on opiod receptors
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antagonist for all
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opiod effect on mice, camels, giraffe
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mice- straub tail
camel and giraffe- star gazing |
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opiod effects on CV and Resp, GI
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depresses respiration, vagal bradycardia except horses and cats-tachycardia and hypertension
dogs- vomit if given morphine subQ or IM |
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loperimide
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immodium, mu agonist- decreased motility to treat diarrhea
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opiods and histamine
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some opiods cause the release of histamine (morphine)
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morphine
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mu agonist, depression unless given IV then you get transient excitement, vagal bradycardia, hoptension, vomiting, defecation, histamine release, analgesia
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meperidine (demerol)
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mu agonist, severe hypotension if given IV (not im), histamine release, short lasting
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oxymorphone
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mu agonist, no CV effect, $
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hydormorphone
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mu agonist, little CV effect, use in sick animals
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fentanyl
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mu agonist, causes severe bradycardia,
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etorphine and carfentanil
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mu agonist, used for restraint of large exotic herbivores, very dangerous and potent, have an antagonist handy
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opiod HR effects in dogs
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bradycardia:
fentanyl> morphine> oxymorphine=hydromorphine> meperidine |
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opiod BP effects in dogs
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hypotension:
oxymorphone= hydromorphone> fentanyl> morphine> meperidine |
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tramadol
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can act as opiod agonist
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opiod antagonists
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naloxone, naltrexone, nalorphone, diprenorphine
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mu antagonists and alpha agonists
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butophanol, pentazocaine, nalbuphine
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buprenorphine
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some analgesia with mu binding btu not as much as a mu agonist. long lasting
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apomorphine
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yawn, stretch, erection, vomit
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acepromazine (acetylpromazine)
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phenothiazine tranquilizer, decreases body temp, decreases muscle rigidity, can prevent or treat drug induced seizures, blocks alpha 1-> vasodilation
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benzodiazepine tranquilizers
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diazepam, midazolam, zolazepan, lorazepam, clonazepam, date rape drug
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flumazenil
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benzodiazepine antagonist, $$$
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gabapentin, pregabalin, vigabatrin,progabide
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gaba analogue, anticonvulsant, analgesic, anxiolytic
|
|
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butyrophenone tranquilizers
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dopamine antagonist, droperidol and azaperone
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