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119 Cards in this Set
- Front
- Back
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nAChR vs mAChR?
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nAChR - ligand gated Na/K channels (Nn - autnomic ganglia; Nm - NMJ)
mAChR - Gprtn coupled receptors; 5 subtypes |
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which autonomic receptors are coupled to which G-prtns with what intracellular action? (mneumonic)
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"QISS and QIQ till you're SIQ of SQS (sex)"
alpha1 - Gq alpha 2 - Gi beta 1 - Gs beta 2 - Gs M1 - Gq M2 - Gi M3 - Gq D1 - Gs D2 - Gi H1 - Gq H2 - Gs V1 - Gq V2 - Gs order: Sympathetic, Parasympathetic (M1-M3), Dopamine, Histamine, Vasopressin |
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what intracellular mechanism for Gq?
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Gq --> activates Phospholipase C --> PIP2 --> DAG which activates PKC & IP3 which increases Ca++ channel influx
(alpha 1, M1, M3, H1, V1) |
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what intracellular mechanism for Gi?
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Gi --| inhibits adenylyl cyclase, decreases cAMP, decreased PKA activity
-PKA then does NOT activate myosin light chain kinase (smooth mm) nor increase Ca++ influx (heart) (alpha2, M2, D2) |
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what intracellular mechanism for Gs?
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Gs --> stimulates adenylyl cyclase --> increases cAMP --> activates PKA:
-heart --> increased Ca++ influx -smooth mm --> increased myosin light chain kinase (increase mm activity) |
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what other receptors are coupled to Gs like the beta adrenergics?
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TSH
PTH Glucagon |
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what receptor mediates increased vascular smooth mm contraction?
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alpha-1; Gq
V1; Gq |
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what receptor mediates increased pupillary dilatory mm contraction (mydriasis)?
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alpha-1; Gq
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what receptor mediates intestinal & bladder sphincter contraction?
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alpha-1; Gq
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what parasympathetic receptor mediates the CNS & enteric nervous system?
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M1; Gq
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what receptor mediates decreased HR & contractility of the atria?
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M2; Gi
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what receptor mediates increased exocrine gland secretion?
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M3; Gq
(sweat, gastric acid) |
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what receptor mediates increased gut peristalsis?
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M3; Gq
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what receptor mediates increased bladder contraction?
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M3; Gq
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what receptor mediates bronchoconstriction?
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M3; Gq
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what receptor mediates increased pupillary sphincter mm contraction (miosis)?
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M3; Gq
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what receptor mediates ciliary mm contraction (accommodation)?
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M3; Gq
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what receptor mediates decreased sympathetic outflow?
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alpha-2; Gi
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what receptor mediates decreased insulin release?
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alpha-2; Gi
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what receptor mediates increased heart rate?
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beta-1 (beta2 - according to FA...); Gs
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what receptor mediates increased contractility?
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beta-1 (& beta2 - according to FA...?); Gs
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what receptor mediates increased renin release?
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beta1; Gs
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what receptor mediates increased lipolysis?
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beta1, beta2; Gs
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what receptor mediates vasodilation?
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beta2; Gs
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what receptor mediates bronchodilation?
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beta2; Gs
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what receptor mediates increased insulin release?
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beta2; Gs
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what receptor mediates decreased uterine tone?
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beta2; Gs
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what receptor mediates renal vascular smooth mm relaxation?
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D1; Gs
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what receptor mediates modulation of transmitter release, especially in the brain?
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D2 (among others....); Gi
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what receptor mediates increased nasal & bronchial mucus production?
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H1; Gq
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what receptor mediates contraction of bronchioles?
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H1; Gq
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what receptor mediates pruritis?
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H1; Gq
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what adrenergic receptor mediates pain?
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H1; Gq
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what receptor mediates increased gastric acid secretion?
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H2; Gs
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what receptor mediates increased H20 permeability & reabsorption in collecting tubules of kidney?
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V2; Gs
(V2 is found in the 2 kidneys) (V1 mediates vascular smooth mm contraction) |
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what inhibits the release of acetylcholine at the nerve termina?
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botulinum
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what inhibits the reuptake of choline into the nerve terminal?
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hemicholinium
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what inhibits ACh from being packaged into vesicles by ChAT?
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vesamicol
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what inhibits the conversion of tyrosine to DOPA?
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metyrosine
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what inhibits the packaging of dopamine & NE into vesicles?
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reserpine
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what inhibits the reuptake of NE at the nerve terminal?
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cocain
TCA amphetamine |
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what prevents release of NE filled vesicles at the nerve terminal?
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Guanethidine
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what increases release of NE by nerve?
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amphetamine
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on the cardiac NE nerve terminal what is the effect of
alpha2 receptor? AII receptor? M2 receptor? |
alpha2 - inhibits NE release (negative feedback)
AII - promotes NE release (angiotensin II) M2 - inhibits NE release |
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bethanechold?
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direct cholinomimetic
-activates bowel & bladder smooth mm -resistant to AChE |
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what direct cholinomimetic is resistant to AChE?
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bethanecol (activates bowel & bladder)
pilocarpine (used for emergency glaucoma) |
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carbachol?
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direct cholinomimetic agonist
(CARBon copy of AcetylCHOLine) -used for eyes |
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used for postoperative & neurogenic ileus & urinary retention?
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bethanechol
direct cholinomimetic agonist |
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used for glaucoma, pupillary contraction, & relief of intraocular pressure?
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Carbachol
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Pilocarpine?
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direct cholinomimetic
-contracts mm of eye (open angle) -contract pupillary sphincter (narrow angle) -resistant to AChE |
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use for emergency glaucoma?
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Pilocarpine
direct agonist cholinomimetic "cry, drool, sweat on PILOw" potent stim: sweat, tears, saliva |
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challenge test for diagnosis of asthma?
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Methacholine
direct agonist cholinomimetic -stimulate muscarinic receptors in airway when inhaled |
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Neostigmine?
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anticholinesterase (indirect agonist)
NeO = no CNS penetration used for postop neurogen ilues & urinary retention; myasthenia gravis, reversal of NMJ |
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Pyridostigmine?
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anticholinesterase
used for myasthenia gravis (long acting) does NOT penetrate CNS pyRIDostigmine gets RID of myasthenia gravis |
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use for dx of myasthenia gravis?
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Edrophonium
(anticholinesterase) extremely short acting |
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Edrophonium?
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anticholinesterase; extremely short acting
use for dx myasthenia gravis |
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Physostigmine?
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anticholinesterase
use for glaucoma (crosses BBB) use for atropine overdose |
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tx for atropine OD?
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physostigmine
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anticholinesterase useful in glauchoma?
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Physostigmine (crosses BBB)
Echothiophate |
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echothiophate?
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anticholinesterase
use for glaucoma |
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anticholinesterase for Alzheimer's?
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Donepezil
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Donepizil?
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anticholinesterase
used for Alzheimer's |
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what are potential complications of cholinomimetic agents?
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COPD exacerbation
asthma peptic ulcers |
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cholinesterase inhibitor poisoning? antidote?
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antidoe - atropine + pralidoxime (regenerates active AChE)
DUMBBELSS diarrhea urination miosis bronchospasm bradycardia Excitation - skeletal mm, CNS Lacrimation Sweating Salivation |
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atropine?
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muscarinic antagonist
used for eye |
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homatropine?
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muscarinic antagonist
used for eye |
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tropicamide?
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muscarinic antagonist
used for eye |
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benztropine?
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muscarinic antagonist
used for Parkinson's |
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scopolamine?
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muscarinic antagonist
used for motion sickness; side effects from tx of myasthenia gravis |
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ipratropium?
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muscarinic antagonist
used for asthma, COPD |
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muscarinic antagonist for asthma / COPD?
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Ipratropium
(I PRAy i can breathe soon) |
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oxybutinin?
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muscarinic antagonist
used for Genitourinary (reduce urgency in cystitis; reduce bladder spasms) |
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glycopyrrolate?
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muscarinic antagonist
used for Genitourinary (reduce urgency in cystitis; reduce bladder spasms) |
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methscopolamine?
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muscarinic antagonist
used for peptic ulcer treatment |
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pirenzepine?
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muscarinic antagonist
used for peptic ulcer tx |
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propantheline?
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muscarinic antagonist
used for peptic ulcer tx |
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increase temp, less sweating, rapid pulse, dry mouth, dry flushed skin, cycloplegia, constipation, disorientation?
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atropine toxicity; in elderly can cause acute angle-closure glaucoma, urinary retention (if have prostatic hyperplasia) & hyperthermia in infants
"Hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter" |
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indirect sympathomimetics?
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amphetamine - releases stored catecholamines
ephedrine - releases stored catecholamines cocaine - uptake inhibitor |
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epinephrine?
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alpha1-----3+
alpha2-----3+ beta1-------4+ beta 2------4+ D1-----------0 used for anaphylaxis, open angle glaucoma, asthma, hypotension |
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norepinephrine?
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alpha1-----4+
alpha2-----4+ beta1-------2+ beta 2------0 D1-----------0 used for Hypotension (but decreases renal perfusion) |
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isoproterenol?
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alpha1-----0
alpha2-----0 beta1-------4+ beta 2------4+ D1-----------0 used for AV block (rare) |
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dopamine?
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alpha1-----4+ (at high doses)
alpha2-----4+ (at high doses) beta1-------4+ (at medium doses) beta 2------2+ (at medium doses) D1-----------+ (at low dose) used for shock (renal perfusion), heart failure inotropic & chronotropic D1 > beta > alpha |
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dobutamine?
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alpha1-----1+
alpha2-----1+ beta1-------4+ beta 2------1+ D1-----------0 heart failure, cardiac stress testing inotropic and chronotropic |
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phenylephrine?
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alpha1-----++++
alpha2-----++ beta1-------0 beta 2------0 D1-----------0 used for pupillary dilation, to induce vasoconstriction, for nasal decongestion |
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metaproterenol, albuterol, salmeterol, terbutaline?
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albuterol, metaproterenol, terbutaline
alpha1-----0 alpha2-----0 beta1-------++ beta 2------++++ D1-----------0 MAST acute asthma - Metaproterenol and Albuterol long term tx - Salmeterol reduce premature uterine contractions - Terbutaline |
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what to use to reduce premature uterine contractions?
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terbutaline, ritodrine
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what to use for acute asthma? long term tx?
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acute - metaproterenol and albuterol
long term - salmeterol |
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indirect sympathomimetics?
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amphetamine - releases stored catecholamines
ephedrine - releases stored catecholamines cocaine - uptake inhibitor |
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epinephrine?
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alpha1-----3+
alpha2-----3+ beta1-------4+ beta 2------4+ D1-----------0 used for anaphylaxis, open angle glaucoma, asthma, hypotension |
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norepinephrine?
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alpha1-----4+
alpha2-----4+ beta1-------2+ beta 2------0 D1-----------0 used for Hypotension (but decreases renal perfusion) |
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isoproterenol?
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alpha1-----0
alpha2-----0 beta1-------4+ beta 2------4+ D1-----------0 used for AV block (rare) |
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dopamine?
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alpha1-----4+ (at high doses)
alpha2-----4+ (at high doses) beta1-------4+ (at medium doses) beta 2------2+ (at medium doses) D1-----------+ (at low dose) used for shock (renal perfusion), heart failure inotropic & chronotropic D1 > beta > alpha |
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dobutamine?
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alpha1-----1+
alpha2-----1+ beta1-------4+ beta 2------1+ D1-----------0 heart failure, cardiac stress testing inotropic and chronotropic |
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phenylephrine?
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alpha1-----++++
alpha2-----++ beta1-------0 beta 2------0 D1-----------0 used for pupillary dilation, to induce vasoconstriction, for nasal decongestion |
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metaproterenol, albuterol, salmeterol, terbutaline?
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albuterol, metaproterenol, terbutaline
alpha1-----0 alpha2-----0 beta1-------++ beta 2------++++ D1-----------0 MAST acute asthma - Metaproterenol and Albuterol long term tx - Salmeterol reduce premature uterine contractions - Terbutaline |
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what to use to reduce premature uterine contractions?
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terbutaline, ritodrine
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what to use for acute asthma? long term tx?
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acute - metaproterenol and albuterol
long term - salmeterol |
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ritodrine?
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alpha1-----0
alpha2-----0 beta1-------0 beta 2------4+ D1-----------0 reduces premature uterine contractions |
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what happens to HR w/NE? Isoproterenol?
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NE - reflex bradycardia (b/c casues increase in BP via vasoconstriction; alpha > beta)
Isoproterenol - reflex tachycardia; causes decreased BP from beta > alpha (vasodilation) |
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clonidine?
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central acting alpha-2 agonist
decrease central adrenergic outflow use to tx HTN, espeically w/renal dz - no decrease in blood flow to kidney |
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alpha-methyldopa?
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central acting alpha-2 agonist
decrease adrenergic outflow use for tx HTN especially w/renal dz (doesn't decrease blood flow to kidney) |
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good way to tx HTN in setting of renal dz?
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central alpha-2 agonists (clonididne, alpha-methyldopa)
doesn't decrease flow to kidneys |
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phenoxybenzamine?
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nonselective alpha adrenergic blocker
Irreversible use for pheochromocytoma before removal b/c high levels of catecholimens won't overcome irreversible block (also long t-half) |
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phentolamine?
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nonselective alpha blocker
used for pts on MAO inhibitors who eat tyramine containing foods |
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toxicity of nonselective alpha blockers?
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orthostatic hypotension
reflexive tachycardia |
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doxazosin, terazosin, prazosin?
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alpha-1 selective alpha blockers
tx HTN, urinary retention in BPH "1st dose orthostatic HTN, dizziness, headache" |
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mirtazapine?
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alpha-2 selective alpha blocker
use for tx of depression tox: sedation, increased cholesterol, increased appetite |
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Beta-blockers used for?
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HTN
Angina pectoris MI SVT CHF Glaucoma |
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use of beta-blockers in HTN?
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decrease CO
decrease renin secrection (receptors on JGA) |
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use of beta-blockers in Angina pectoris?
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decrease HR & contractility
decreases O2 consumption |
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use of beta-blockers in MI?
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decrease mortality
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use of beta-blockers in SVT? which ones?
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class II anti-arrythmics
decrease AV conduction velocity (region between P & QRS - PR interval) -propranolol, esmolol |
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use of beta-blockers in CHF?
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slow progression of chronic failure
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use of beta-blockers in Glaucoma? which one?
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decrease secretion of aqueous humor
Timolol |
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impotence, bradycardia, AV block, CHF, sedation, sleep alterations are toxicity of? use with caution in what populations?
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beta blocker toxicity
-also asthma exacerbation, "CV & CNS adverse effects" use w/caution in diabetics |
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Acebutol
Betaxolol Esmolol Atenolol Metoprolol |
A-BEAM of beta-1 selective blockers
-useful for comorbid pulmonary dz special characteristics -slow acting - esmolol -partial agonist - acebutol |
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Pindolol
Nadolol Timolol Propranolol |
Nonselective beta blockers
"Please Try Not being Picky" |
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Labetalol
Carvedilol |
nonselective alpha & beta agonists - vasodilatory
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Pindolol
Acebutol |
partial beta agonists
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