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91 Cards in this Set
- Front
- Back
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Pilocarpine
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Muscarinic Agonist
Tx of glaucoma and xerostomia Miotic; works on ciliary muscle |
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Neostigmine
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Acetylcholine Esterase Inhibitor
Quat. Amine = No CNS Tx Myasthenia Gravis |
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Atropine
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Competitive muscarinic antagonist
*Blocks Ach but can ↑Ach to overcome Tertiary amine – into CNS Effects depend on ‘tone’ -↑ HR if PNS Overdose – treat with AChEI (↑ Ach) |
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Scopolamine
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Muscarinic antagonist
Tertiary amine – in CNS Duration can be days - tx motion sickness due to CNS depressant effects - ↑ doses = excitation |
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Tolterodine
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Muscarinic antagonist
- tx incontinence & overactive bladder *Functional selectivity for urinary bladder |
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Mecamylamine
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Nicotinic Antagonist/Ganglionic Blocking Agent
Tertiary amine – into CNS Competative inhibitor with nicotine Blocks Nn – affects CNS and periphery **Orthostatic Hypotension → tone will not allow a change in BP |
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Succinylcholine
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Nicotinic Agonist/Skeletal Muscle Relaxant
Safe from AChE Causes hyperkalemia, increased IOP, releases histamine, and malignant hyperthermia |
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Tubocurarine
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NMJ Blocking Agent
Non-depolarizing Skeletal Muscle Relaxants Binds Nm reversibly for Ach @ NMJ end-plate Flaccid paralysis w/out preliminary contractions (no twitch) Doesn’t gain access to brain |
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Cyclobenzaprine
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Skeletal Muscle Relaxants
Spasmolytic (Analogue Tricyclic Antidepressants) Decrease NE reuptake (atropine like) - tx (acute, short-term) muscle spasm associated w/ muscoskeletal injury Works with Internuncial neuron |
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Tizanidine
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CNS-active muscle relaxant
Sympathomimetic Clonidine-like compound α2 agonist - tx muscle spasticity |
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Sildenafil
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Inhibits cGMP degredation
Inhibits phosphodiesterase ↑ cGMP relaxes smooth muscle → increase in blood flow = erection Arginine → NO (via NOS-regulated by Calcium/calmodulin) → Guanylyl Cyclase → cGMP |
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Ryanodine
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Mediates release of calcium from SR
Receptor on T-tubules ↑ calcium → Muscle contraction |
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Glucagon
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Antidote for β-blockers - ↑ cAMP
Released from pancreas when blood glucose levels are low Binds glucagon receptors on liver cells → release of glucose or synthesis |
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MAO Inhibitor
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Sympathomimetic
Drug interactions Tyramine in foods → dangerous increase in BP if w/ MAOI ↑ NE due to stopping metabolism **meperidine + MAOI → fever & convulsions |
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Bretylium
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Anti-Release of NE
Prevents NAP-induced NE release Used to terminate ventricular fibrillation Use IV only in emergency to raise BP Possible calcium interference Local anesthetic activity |
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Guanethidine/Guanadrel
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Anti-Release then Depletion of NE
Prevent NAP-induced NE release Chronic use → depletion Initial sympathomimetic effects – initial release of NE due to drug uptake into nerve (co-transporter) Peripheral effect |
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Reserpine
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Depletion of NE
Blocks vesicular NE and DA uptake → NE depletion Blocks VMAT (Vesicular Monoamine Transporter) Causes smooth ↓ in BP CNS effects: ↑ vagal outflow-bradycardia (↓ HR/CO/PR); psychic depression; sedation No initial sympathomimetic effects |
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Phentolamine
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Competitive Antagonist
Blocks α1 & 2 – nonselective α blocker Short half-life and fact acting Used to tx/diagnose catecholamine-secreting tumor |
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Phenoxybenzamine
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Covalent binding to α receptors
Blocks α1 & 2 – unselective α blocker Irreversible – alkylate Long acting tx shock |
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Prazosin
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Selective α1 antagonist
Prototype First dose – syncope (wait till PM for first dose due to orthostatic hypotension) - tx high BP |
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Tamsulosin
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Selective α1 antagonist
Selective for α1A (Subtype prominent in bladder sphincter smooth muscle) Blood vessels have tons of α1A When pts age - ↑ α1B which means less vessel wall effects (Younger pts have more vessel wall effects) - tx BPH (Benine Prostetic Hyperplasia) |
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Yohimbine
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α2 antagonist – can get into CNS
↑ SNS outflow from CNS →↑ BP - tx orthostatic hypotension |
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Carvedilol
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Mixed α & β blockers
- tx CHF Can cause orthostatic hypotension |
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Labetalol
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Mixed α & β blockers w/ some β2 agonist activity
- tx for high BP Can cause orthostatic hypotension |
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Propranolol
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Non-selective β blocker
Prototype Potentiates pressor effect of epinephrine by blocking β2 vasodilator activity Prevents hypokalemia “Local Anesthetic” effect (blocks Na+ channels) - tx angina, HTN, dysrhythmias, glaucoma |
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Esmolol
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Β1 selective blocker
IV – short half-life High doses can affect β2 activity (bronchioles effects – constriction) - tx acute arrhythmias |
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Metoprolol
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Β1 selective blocker
“Cardio selective” Used chronically in heart failure High doses – affect β2 (bronchioles effects – constriction) |
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Nebivolol
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Β1 selective blocker
Direct vasodilator effect by ↑ NO release - tx HTN |
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Metyrosine
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Tyrosine hydroxylase inhibitor
Decreases NE concentration Tx pheochromocytoma before surgery |
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Nadolol
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Nonselective beta blocker
Tx HTN Least lipophilic |
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Pindolol
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Nonselective beta blocker
Don’t use with asthma Tx HTN Less bradycardia b/c partial agonist activity Less lipophilic |
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Norepinephrine
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Endogenous catecholamine
sympathomimetic α1, α2, β1, β3 (no β2) vasoconstriction (↑PR ↓HR, ↓CO) made from tyrosine reuptake via Uptake I/NET (90%) metabolized by MAO and COMT |
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Dopamine
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Endogenous catecholamine
sympathomimetic D1, D2, α1, β1 Low doses = D1, β1 = vasodilatation No change PR, ↑HR, ↑CO High doses = α = vasoconstriction ↑PR, ↓HR, ↓CO (like NE) D1 receptors in kidney |
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Epinephrine
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Endogenous catecholamine sympathomimetic; ↓HIS release
α1, α2, β1, β2, β3 Low doses = β2 = vasodilatation ↓PR, ↑HR, ↑CO High doses = α = vasoconstriction ↑PR, ↓HR, ↓CO (like NE) Circulating NT |
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Isoproterenol
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Sympathomimetic
only β (no α) vasodilatation (↓PR ↑↑HR ↑↑CO) |
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Phenylephrine
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direct acting sympathomimetic at α1
nasal decongestant…local administration |
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Albuterol
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direct acting sympathomimetic at β2 dilate; tx acute asthma
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Amphetamine
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indirect acting sympathomimetic
facilitate NE release (displace NE via NET) |
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Cocaine
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indirect acting sympathomimetic
prevents uptake of NE (blocks NET) potent local anesthetic & vasoconstrictor b/c ↑[NE] in synapse α1 SE = ↓IOP, mydriasis |
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Prazosin
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Sympatholytic
α blocker (affinity but no efficacy) |
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Propranolol
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Sympatholytic
β blocker (affinity but no efficacy) |
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Metaraminol
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false transmitter of NE (α1 agonist)
less potent than NE depletes neuronal NE pressor some β1 effects initially (from NE) stopping infusion = huge ↓bp |
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Tyramine
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indirect acting sympathomimetic
facilitate NE release displace NE from cell via NET (↑[NE] in synapse)…longer t1/2 in cheese and wine |
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Ephedrine
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mixed sympathomimetic
direct activity on β2 displace NE can dilate bronchioles |
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Oxymetazolone
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sympathomimetic at α2 and α1
nasal decongestant |
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α-methyl DOPA
levonordefrin |
prodrug (cross BBB)
false transmitter (???effectiveness) α-methyl DOPA → α-methyl DA →α-methyl NE in CNS α2 causes ↓bp (more vagal) |
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Pseudoephedrine
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α1 agonist
tx incontinence (α1) constrict sphincter caution with BPH NOT α1 selective |
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Clonidine
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α2 agonist sympathomimetic in CNS
↓bp b/c enhance vagal and ↓SNS Tx pain (CNS) b/c enhance PNS |
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Salmeterol
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Sympathomimetic at β2 (dilate)
Long acting (not for acute attack) |
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Ritodrine
Terbutaline |
Sympathomimetic at β2
Relax to delay labor Systemic admin = relax bronch sm muscle; Also, ↓bp so ↑SNS which ↑renin…↑CO, tachycardia |
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Moxonidine
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I1 agonist
Tx HTN Not in USA |
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Fenoldopam
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sympathomimetic at D1
↓bp, retain renal blood flow |
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Dobutamine
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Sympathomimetic at β1
Pressor Functionally cardioselective ↑CO with little effect on TPR |
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Chronotropic
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changes HR
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Inotropic
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Changes force of contraction
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Tocolytic
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relaxes uterine smooth muscle to prevent premature labor
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Lusitropic
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myocardial relaxation
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Which organs ONLY receives SNS innervation?
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Most blood vessels
Sweat glands Spleen Piloerector Muscles |
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Which receive ONLY PNS innervation?
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ciliary muscle in eye
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Location of Nicotinic Receptors
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all ganglia
adrenal medullary cells skeletal muscle NMJ CNS |
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What happens when ACh is injected?
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Will bind to endothelial cell receptors, increasing Nitric Oxide and causing vasodilation
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Mimetic Effect at Nm receptors
(name drugs) |
ACh
Nicotine Succinylcholine |
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Mimetic Effects at Nn receptors
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ACh
Nicotine |
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Location, Signaling and Use of M1 receptors
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CNS neurons
ganglion cells near parietal cells of stomach Signalled via activation of PLC, increases IP3 and increases Ca2+ Used for Alzheimers, M1 block for ulcers |
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Location, Signaling and Use of M2 receptors
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Heart
Autoreceptors Soem smooth muscle Signalled via K+ channel activation, which inhibits adenylyl cyclase and decreases Ca2+ Used for cardiac slowing |
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Location, Signaling and Use of M3 receptors
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In exocrine glands,smooth muscle, and endothelium
Signalled via activation of PLC, increases IP3 which increases Ca2+ Can vasodilate via NO, secretion, smooth muscle contraction |
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What acts on radial muscle?
What acts on ciliary muscle? |
NE = radial muscle of eye
Pilocarpine = ciliary muscle |
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DUMBBELSS
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Diarrhea
Urination Miosis Bradycardia Bronchoconstriction Excitation of skeletal muscle and the CNS Lacrimation Salivation Sweating |
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Antidotes for AChEIs
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2-PAM
Atropine |
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Uses for Sympathomimetics
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Alleviate symptoms (decongestant)
Delay Labor Tx incontinence Tx Asthma Life Support by treating anaphylaxis Delay absorption of drugs at injection site Vasoconstriction to decrease bleeding Pressor |
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B1 Agonists
(via activation of AC) |
increase cardiac excitation
increase renin release from renal JG cells |
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B2 Agonists
(via activation of AC) |
Increase plasma glucose levels
Relaxes smooth muscle Also some receptor in heart (increases in heart failure) |
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B3 agonists
(via activation of AC) |
Increase plasma free fatty acids
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MOA of Sympathomimetics
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Act on GPCR to change activity of adenylyl cylase and PLC, as well as Calcium and Potassium channels
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D Agonists
(via activation of AC) |
vasodilatation
cardiac stimulation increases kidney blood flow |
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Alpha 2 agonists
(via inhibition of AC) |
inhibit NE release via autoreceptors
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Alpha 1 Agonists
(via activation of PLC) |
Contraction of smooth muscle of the radial muscle of the iris and bladder sphincter
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Alpha 2 agonists
(via activation of K+ channels, also inhibit Ca channel opening) |
Muscles relax (since decrease in Ca, harder to get action potential)
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B Agonists
(via activation of Ca channels) |
PKA, acts directly to open cardiac L type Ca channels
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Cardiovascular Alpha 1 & 2 Receptors
(What is the effect?) |
Vasoconstriction
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Cardiovascular B2 receptor
(What is the effect?) |
Vasodilatation of skeletal muscle
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Cardiovascular D1 Receptor
(What is the effect?) |
Vasodilation of vessels supplying kidney
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Cardiovascular B1 Receptor
(What is the effect?) |
Increase cardiac excitation
dysrhythmogenic increase renin secretion |
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Norepinephrine effects on Arterial Pressure
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Increase PR
Decrease HR (reflex) Decrease CO |
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Epinephrine effects on Arterial Pressure
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Decrease PR at low dose, Increase at high dose
Increase HR at low dose, decrease HR at high dose Increase CO at low dose, Decrease CO at high dose |
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Isoproteronol effects on Arterial Pressure
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Decrease PR
Increase HR x 2 Increase CO x 2 |
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Dopamine effects on Arterial Pressure
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no change in PR(no B2), increase PR at high dose
Increase HR at low dose, Decrease HR at high dose Increase CO at low dose, Decrease CO at high dose |
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-olol
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Beta blocker
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-ol
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Sympathomimetic
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-ilol
-alol |
Mixed alpha and beta blocker
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-osin
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Alpha 1 antagonists
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