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95 Cards in this Set
- Front
- Back
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Nicotinic and Muscarinic Receptors are what types of receptors?
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Nicotinic: ligand gated Na/K channels
Muscarinic: G-protein coupled |
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who are the Sympathetic Receptors and what types of receptors are they?
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Alpha1 : Gq coupled
Alpha2: Gi coupled Beta1: Gs coupled Beta2: Gs coupled |
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Major Fxns of Alpha1-adrenergic receptors?
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Inc Vascular Smooth Muscle Contraction
Inc Pupillary Dilator Muscle contraction (mydriasis) |
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Major Fxns of Alpha2 receptors?
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Dec sympathetic outflow
Dec insulin release |
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Major Fxns of Beta1 receptors?
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Inc Heart Rate
Inc Contractility Inc Renin Release Inc Lipolysis |
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Major Fxns of Beta2 receptors?
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Vasodilation
Bronchodilation Inc Heart Rate Inc Contractility Inc Lipolysis Inc Glucagaon release Dec uterine tone |
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Types of Parasympathetic receptors and what they're coupled to?
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M1 (Gq)
M2 (Gi) M3 (Gq) |
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Where are M1 receptors located?
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CNS
Enteric Nervous System |
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Major Fxns of M2 receptors?
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Dec HR and contractility of atria
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Major Fxns of M3 receptors?
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Inc exocrine gland secretions
Inc gut peristalsis Inc bladder contraction Bronchoconstriction Inc Pupillary Sphincter Muscle contraction (miosis-small) Ciliary Muscle Contraction (accomodation) |
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Types of Dopamine Receptors and their Major Fxns
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D1: relaxes renal vascular smooth muscle
D2: Modulates transmitter release, esp in brain |
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Types of Histamine Receptors and their Major Fxns?
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H1:
inc nasal, bronchial mucus production contraction of bronchioles pruritis pain H2 Inc Gastric acid secretion |
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Types of Vasopressin receptors and their Major Fxns?
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V1
Inc vascular smooth muscle contraction V2 Inc H20 perm and reabsorption in collecting tubules |
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To memorize the G-protein that each of the aforementioned receptors is coupled to, what is the order of receptors?
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alpha1
alpha2 beta1 beta2 M1 M2 M3 D1 D2 H1 H2 V1 V1 |
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To memorize the G-protein that each of the aforementioned receptors is coupled to, what is the mnenomic?
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QISS (kiss) and QIQ (kick) till you're SIQ (sick) of SQS (sex)
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what happens when you activate a Gq receptor/
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Activates Phospholipase C
Lipids--->PIP2 PIP2 ---> IP3 and DAG IP3 ---> Inc Ca influx DAG ---> Protein Kinase C activation |
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what happens when you activate a Gs receptor?
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Activates Adenylyl Cyclase
AC---> inc cAMP inc cAMP----> Protein Kinase A activation |
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what happens when you activate a Gi receptor?
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blocks adenylyl cyclase
Dec cAMP Dec PKA |
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How do you make Acetylcholine?
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Acetyl-CoA
+ Choline with choline acyltransferase |
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Precursors to Norepinephrine?
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Tyrosine-->DOPA--->dopamine
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Three drugs and where they inhibit the process that eventually leads to Ach release at synaptic terminal?
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Hemicholinum blocks uptake of choline into presynaptic cell
Vesamicol blocks the uptake of Ach into storage granules Botulinum blocks the release of ACh from storage granules |
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Mechanism for Metyrosine?
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stops conversion of tyrosine into DOPA
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Mech of Reserpine at nerve terminals?
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Blocks the uptake of Dopamine into secretory vesicles where dopamine is normally converted to Nor
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Effect of Guanethidine on adrenergic nerve terminals?
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blocks release of NE from presynaptic terminal
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Effect of Amphetamines on adrenergic nerve terminals?
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Stimulates relaese of NE
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Effect of Cocaine and TCA at Adrenergic nerve terminal?
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Block the reuptake of NE
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How does negative feedback work for Noradrenergic nerve terminals?
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NE feeds back onto alpha2 receptors on presynaptic terminals that in turn inhibit release of more NE
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who are 4 Direct Cholinergic Agonists?
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Bethanechol
Carbachol Pilocarpine Methacholine |
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actions of Bethanechol?
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Activates Bowel and Bladder smooth muscle (used postop)
Resistant to AChE |
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Uses of Carbachol
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Glaucoma (relesae intraocular pressure)
Pupillary Contraction |
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Effects of Pilocarpine?
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Potent stimulator of Sweat, Tears, Saliva
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Effects of Methacholine?
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Stimulates Musc. receptors in airway when inhaled
Used as a challenge test for Dx of asthma |
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Who are 5 Indirect Agonists of Cholinergic receptors (i.e. anticholinesterases)?
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Neostigmine
Pyridostigmine Edrophonium Physostigmine Echothiophate |
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Uses for Neostigmine?
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Postop and neurogenic ileus and urinary retention
Myasthenia Gravis Reverse NMJ blockade (postop) doesn't penetrate CNS! |
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Uses for Pyridostigmine?
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Myasthenia Gravis (long acting)
doesn't penetrate CNS |
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Uses for Edrophonium?
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Dx of Myasthenia Gravis (very short acting)
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Uses for Physostigmine?
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Glaucoma (crosses BBB)
Atropine Overdose |
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Uses for Echothiophate?
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Glaucoma
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Sx's of AntiCholinesterase poisoning?
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Diarrhea
Urination Miosis Bronchospasm Bradycardia Excitation of skeletal muscle and CNS Lacrimation Sweating Salivation |
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Who causes anticholinesterase poisoning?
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Parathion and other organophosphates
Irreversible inhibitors |
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Who are 6 major (and 5 similar...geez) Muscarinic Antagonists?
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Atropine (homatropine, tropicamide)
Benztropine Scopolamine Ipratropium Oxybutynin (glycopyrrolate) Methscopolamine (pirenzepine, propantheline) |
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Organ System used for and application for Atropine (homatropine, tropicamide)?
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Eye
Produces mydriasis and cycloplegia |
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What is mydriasis?
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super dilated
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What is cycloplegia?
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loss of accomodation
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Organ System used for and application for Benztropine?
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CNS
Rx for Parkinson's |
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Organ System used for and application for Scopolamine?
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CNS
Rx for Motion Sickness |
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Organ System used for and application for Ipratropium?
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Respiratory
Rx's asthma, COPD |
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Organ System used for and application for Oxybutynin (glycopyrrolate)?
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GU
Reduces urgency in mild cystitis Reduces bladder spasms |
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Organ System used for and application for Methscopolamine (pirenzepine, propantheline)?
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GI
Rx's peptic ulcers |
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Who is the Antidote of Cholinesterase Inhibitor Poisoning?
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Atropine plus pralidoxime (regenerates active cholinesterase)
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Besides the eyes, what can Atropine do?
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Decrease airway secretions
Decrease gastric acid secretions Dec gut motility Dec bladder urgency w/ cystitis |
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Toxicity Sx's of Atropine?
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Inc Body Temp
Rapid Pulse Dry Mouth Dry, flushed skin Cycloplegia Constipation Disorientation |
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Adverse Effects of Atropine for specific types of patients?
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Elderly: acute angle-closure glaucoma
BPH: urinary retention Infants: Hyperthermia |
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MOA for Hexamethonium?
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Nicotinic Antagonist
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Clinical Uses for Hexamethonium?
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Ganglionic Blocker
Experimentally to prevent vagal reflex responses to changes in BP (e.g. prevent reflex bradycardia caused by NE) |
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Adverse Effects of Hexamethonium?
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Severe Orthostatic Hypotension
Blurred Vision Constipation Sexual Dysfxn |
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Who are 9 Direct Sympathomimetics?
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Epinephrine
Norepinephrine Isoproterenol Dopamine Dobutamine Phenylephrine Albuterol and Terbutaline Ritodrine |
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Selectivity of Epi, NE, and Isoproterenol?
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Epi hits all 4, but a low dose is selective for Beta1
NE is more for alpha1 and alpha 2 > Beta1 Isoproterenol is ISOlated to Betas (beta 1=beta 2) |
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Selectivity of Dopamine and Dobutamine?
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Dopamine
D1=D2>beta>alpha Dobutamine B1>B2 |
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Selectivity of Phenylephrine, Albuterol/Terbutaline, and Ritodrine?
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Phenylephrine
a1>a2 Albuterol/Terbutaline B2>B1 Ritodrine B2 |
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Main Clinical uses of Epi?
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Anaphylaxis
Glaucoma (open angle) Asthma Hypotension |
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Main Clinical uses of NE?
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Hypotension (but it decreases renal perfusion)
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Main Clinical uses of Isoproterenol?
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AV block (rare)
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Main Clinical uses of Dopamine?
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Shock (inc renal perfusion)
Heart Failure |
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Main Clinical uses of Dobutamine?
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Shock
Heart Failure Cardiac Stress Testing |
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What is the difference between Dopamine's and Dobutamine's effects on the heart?
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Dopamine: inc inotropy and chronotropy
Dobutamine: inc just inotropy |
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Who are the Indirect Sympathomimetics?
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Amphetamine
Ephedrine Cocaine |
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How do the Indirect Sympathomimetics work?
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Amphetamine: releases stored catecholamines
Ephedrine: releases stored catacholamines Cocaine: uptake inhibitor |
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Uses for Amphetamine?
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Narcolepsy
Obesity ADD |
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Uses for Ephedrine?
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Nasal Decongestion
Urinary incontinence Hypotension |
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Uses for Cocaine?
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It causes vasoconstriction and local anesthesia
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What and who are the Sympathoplegics?
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They're central acting drugs
Clonidine alpha-Methyldopa |
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Uses for Clonidine and alpha-Methyldopa?
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They're central alpha2-agonists
They decrease central adrenergic outflow Used for HTN, esp w/ RF b/c they don't decrease blood flow to kidneys |
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Effects of NE, Epi, and Isoproterenol on BP and HR?
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NE
increases BP--->reflex brachycardia EPI effects on BP cancel each other out (no effect) Beta1's lead to inc HR ISO hitting on just Beta's-->drop in BP--->reflex tachycardia + effect on beta1's increase HR |
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Who are the Selective B2-agonists? (mnemonic)
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MAST
Metaproterenol Albuterol Salmeterol Terbutaline |
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Who are the Non-Selective Alpha-Blockers? difference between them?
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Phenoxybenzamine (irreversible)
Phentolamine (reversible) |
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uses of Phenoxybenzamine/Phentolamine? SE's?
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Used when removing Pheochromocytoma
Can cause orthostatic hypotension and reflex tachycardia |
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Who are the Alpha-1 Selective Blockers?
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Prazosin
Terazosin Doxazosin the -zosins! |
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Uses of the Alpha1 blockers and their SE's?
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USES
hypertension urinary retention in BPH SE's 1st dose orthostatic hypotension Dizziness HA |
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Who are the Alpha2 Selective Blockers?
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Mirtazapine
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Uses of Mirtazapine and SE's?
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USE: depression
SE's: Sedation, Inc serum cholesterol, Inc Appetite |
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How does the addition of an Alpha Blocker effect BP in a patient on Epi vs Phenyephrine?
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The BP in the Epi pt will go from high to low b/c of loss of Epi's effects on alpha receptors coupled with Epi's continued stimulus of Beta2's
The BP in the Phenylephrine pt will decrease, but just back to "normal" b/c of alpha blocking w/ no stimulus of betas |
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Who are the Non-Selective Beta Blockers?
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Propranolol*
Timolol Nadolol Pindolol Labetolol* |
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Who are teh B1-Blockers?
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Acebutolol (partial agonist)
Betaxolol Esmolol (short acting) Atenolol Metoprolol A BEAM |
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Who are the Non Selective Alpha and Beta Blockers?
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Carvedilol
Labetalol |
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Who are the partial Beta-Agonists...who are somehow beta blockers too?
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Pindolol
Acetabulol |
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6 Main uses for Beta-Blockers?
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HTN
Angina Pectoris MI Supreventricular Tachycardia (SVT) CHF Glaucoma |
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Specifically, which beta-blockers do you use for SVT? Glaucoma?
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SVT
propranolol esmolol Glaucoma timolol |
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effects on HTN of Beta Blockers?
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Dec CO
Dec Renin secretion |
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Effects on Angina of Beta Blocekrs
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Dec HR and Contractility--->dec O2 consumption
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Effects on MI of Beta blockers?
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Dec mortality
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Effects on SVT of Propranolol/esmolol?
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Dec AV conduction velocity (class II antiarrhythmic)
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Efffects on CHF of beta blockers?
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slows progression to chronic failure
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Effects on glaucoma of timolol?
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Dec secretion of aqueous humor
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Adverse Effects of beta blockers?
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Impotence
Exacerbation of asthma CV: bradycardia, AV block, CHF CNS: sedation, sleep alteration cautioned us w/ diabetics |
