First Aid autonomic pharm
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alpha-1 | Gq; increaes vasculr smooth muscle contraction
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alpha-2 | Gi; decrease sym outflow; decrease insuline release
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beta-1 | Gs; heart- increase HR, contractility; increase renin release, increase lipolysis, maintains aqueous humor formation
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beta-2 | Gs; lungs- vasodilation, bronchodilation; heart- increase HR, contractility; increase lipolysis, increase glucagon release
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M1 | Gq; in brain; CNS, enteric nervous system
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M2 | Gi; decrease HR, contractility
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M3 | Gq; increase exocrinie gland secretions, increase gut peristalsis, increase bladder contraction
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D1 | Gs; relaxes renal vascular smooth muscle
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D2 | Gi; modulates transmitter release, especially in brain
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H1 | Gq; increase nasal and bronchial mucus production, contraction of bronchioles, pruritis, pain
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H2 | Gs; increase gastric acid secretion
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V1 | Gq; increase vascular smooth muscle contraction
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V2 | Gs; increase water permeability and reabsorption in the collecting tubles of kidney
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Gq receptors | H1, alpha-1, V1, M1, M3 (HAVe 1 M&M)
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Gs receptors | B1, B2, D1, H2, V2
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Gi receptors | M2, alpha-2, D2 (MAD 2's)
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Gq protein MOA | PLC --> PIP2 --> IP3 and DAG --> increase Ca++ in and PKC
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Gs protein MOA | adenylyl cyclase --> cAMP --> PKA
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Gi protein MOA | inhib adenylate cyclase -->decreased cAMP --> inhib PKA
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bethanechol | direct ACh agonist; activates bowel and bladder
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carbachol | direct ACh agonist; used in glaucoma, pupillary contraction, release of intraocular pressure
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pilocarpine | direct ACh agonist; stimulates sweat, tears, saliva
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methacholine | direct ACh agonist; challenge test for asthma diagnosis
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neostigmine | AChE inhibitor; reversal of neuromuscular jxn blockade, MG; NO CNS penetration
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pyridostigmine | AChE inhibitor; MG (long-acting)
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edorphonium | AChE inhibitor; tensilon test to diagnose MG
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physostigmine | AChE inhibitor; glaucoma
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used in glaucoma; crosses BBB; used to treat atropine OD | physostigmine
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AChE inhibitor poisoning | excess ACh; DUMBBELSS- diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal muscle and CNS, lacrimation, sweating, salivation
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AChE inhibitor OD antidote | atropine (anti-muscarinic), parlidoxime (regenerates active AChE)
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AChE inhibitor for Alzheimer's | donepezil, galantamine, rivastigmine
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muscarinic antag; produces mydriasis and cycloplegia | atropine
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muscarinic antag; use in Parkinson's | benztropine
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muscarinic antag; use for motion sickness | scopolamine
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muscarinic antag; used in asthma, COPD | ipratropium
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muscarinic antag; use to reduce urgency in mild cystitis and reduce bladder spasms | oxybutynin
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muscarinic antag; use for peptic ulcer treatment | propantheline, methoscopolamine, glycopyrrolate
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glaucoma drugs | alpha-agonists (epi, brimonidine), beta-blockers (timolol), cholinergics (pilocarpine), diuretics (acetazolamide, mannitol), PG (latanoprost)
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1st line for glaucoma | latanoprost (PG)
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glaucoma drug that increases outflow of aqueous humor | pilocarpine
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atropine contraindications | glaucoma, BPH, GI obstruction, dementia, infants with fever
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atropine | muscarinic antag; (blocks ACh effects); used to treat cholinesterase inhibitor poisoning (insecticides)
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parathion | AChE inhibitor in insecticides --> HIGH amounts of ACh; get DUMBBELS
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effects of atropine | muscarinic antag --> decreased ACh effects; increased temp, decrease secretions, peripheral vasodilation, mydriasis, agitation, urinary retention, constipation
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hexamethonium | nicotinic antag; blocks both sym and parasym; prevents reflex bradycardia caused by NE
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epi | alpha-1, alpha-2, beta-1, beta-2 sympathomimetic
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NE | alpha-1, alpha-2 > beta-1 sympathomimetic
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isoproterenol | beta-1 = beta-2 sympathomimetic
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dopamine | D1 = D2 > B > alpha sympathomimetic
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dobutamine | beta-1 > beta-2 sympathomimetic
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phenylephrine | alpha-1 > alpha-2 sympathomimetic
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albuterol | beta-2 > beta-1 sympathomimetic
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terbutaline | beta-2 > beta-1 sympathomimetic
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ritodrine | beta-2 sympathomimetic
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amphetamine | indirect general agonist; releases stored catecholamines
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ephedrine | indirect general agonist; release stored catecholamines
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cocaine | indirect general agonist; uptake inhibitor
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clonidine | central alpha-2 agonist
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methyldopa | central alpha-2 agonist
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treatment for anaphylaxis, open angle glaucoma | epi
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treatment for septic shock | NE
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treatment for shock, heart failure | dopamine
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treatment for cardiogenic shock | dobutamine
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treatement for acute asthma | albuterol
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treatement for reducing premature uterine contractions | terbutaline, ritodrine
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treatement for narcolepsy, obesity, ADD, MDD | amphetamine
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treatment for nasal congestion, urinary incontinence, hypoTN | ephedrine
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causes vasoconstriction and local anesthesia | cocaine
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treatment for HTN, especially in patients with renal disease | clonidine, methyldopa
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phenoxybenamine | irreversible alpha blocker
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phentolamine | reversible alpha blocker
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used to treat pheochromocytoma | phenoxybenzamine (irreversible alpha block), phentolamine (reversible alpha block)
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SE: 1st dose orthostatic hypoTN | prazosin (alpha-1 blocker)
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prazosin, terzosin, doxzosin | alpha-1 blocker
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use to treat HTN, urinary retention in BPH | prazosin (alpha-1 blocker)
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mirtazapine | alpha-2 blocker
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use for thin, elderly patient with depression | mirtazapine (anti-depressant, alpha-2 blocker)
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anpham26
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