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68 Cards in this Set
- Front
- Back
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Parasympathetic innervation of cardiac and smooth muscle, glands, nerve terminals
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1st synapse: nicotinic, ACh 2nd synapse: muscarinic, ACh |
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Innervation of sweat glands |
sympathetic 1st synapse: nicotinic, ACh 2nd synapse: muscarinic, ACh |
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Sympathetic innervation of cardiac and smooth muscle, glands, nerve terminals |
1st synapse: nicotinic, ACh 2nd synapse: alpha/beta, NE |
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Innervation of renal vasculature |
sympathetic 1st synapse: nicotinic, ACh 2nd synapse: dopamine receptor, dopamine |
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Innervation of adrenal medulla |
Sympathetic 1 neuron pathway nicotinic, ACh |
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Innervation of skeletal muscle |
Somatic 1 neuron pathway nicotinic (neuromuscular junction), ACh |
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alpha1 receptors |
Gq mechanism Eyes: mydriasis (pupillary dilator contraction) BVs: vasoconstriction Sphincters: intestinal and bladder sphincter contraction |
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alpha2 receptors |
Gi mechanism Insulin: decreases release (diabetogenic) Sympathetic outflow: decreases (negative feedback) Lipolysis: decreases Platelet aggregation: increases |
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beta1 receptors |
Gs mechanism Heart: increases HR and contractility Kidney: increases renin release Lipolysis: increases Glucagon: increases release |
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beta2 receptors |
Gs mechanism BVs: vasodilation Airways: bronchodilation Uterus: decreases uterine tone (tocolysis) Ciliary epithelium: increases aqueous humor production Increases insulin release |
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M1 receptors |
Gq mechanism CNS |
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M2 receptors |
Gi mechanism Heart: decreases HR and contractility |
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M3 receptors |
Gq mechanism "Everything else" Smooth muscle: increases gut peristalsis, bladder contraction Glands: increases secretions (lacrimal, salivary, gastric) Eyes: miosis (pupillary sphincter contraction), accommodation (ciliary muscle contraction) |
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D1 receptors |
Gs mechanism Kidney: relaxes renal vascular smooth muscle |
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D2 receptors |
Gi mechanism Modulates transmitter release, esp. in brain |
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H1 receptors |
Gq mechanism "Allergic response" Increases mucus production (nasal and bronchial) Increases vascular permeability Bronchiole constriction Pruritis (ex. itchy eyes) Pain Edema Wheals (hives) |
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H2 receptors |
Gs mechanism Increases gastric acid secretion |
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V1 receptors |
Gq mechanism Vasopressin (ADH) receptor Increases vascular smooth muscle contraction |
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V2 receptors |
Gs mechanism Vasopressin (ADH) receptor Increases H2O permeability and reabsorption in the renal collecting duct |
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Bethanechol
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Cholinomimetic Action: activates bowel and bladder smooth muscle; resistant to AChE Clinical uses: ileus, urinary retention |
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Carbachol |
Cholinomimetic Clinical uses: glaucoma, pupillary constriction |
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Pilocarpine |
Cholinomimetic "Pilocholpine" Action: contracts ciliary muscle and pupillary sphincter ;resistant to AChE Clinical uses: production of sweat (cystic fibrosis test), tears, and saliva; glaucoma (urgent tx) |
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Methacholine |
Cholinomimetic Action: stimulates muscarinic receptors in airway Clinical uses: challenge test for diagnosis of asthma |
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Neostigmine |
Anticholinesterase No CNS penetration Clinical uses: ileus, urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative) |
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Pyridostigmine |
Anticholinesterase No CNS penetration Clinical uses: myasthenia gravis (long-acting) |
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Physostigmine |
Anticholinesterase Penetrates CNS Clinical uses: anticholinergic toxicity (ex. atropine overdose) |
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Donepezil |
Anticholinesterase Clinical uses: Alzheimer disease |
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Rivastigmine |
Anticholinesterase Clinical uses: Alzheimer disease |
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Galantamine |
Anticholinesterase Clinical uses: Alzheimer disease |
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Edrophonium |
Anticholinesterase Clinical uses: diagnosis of myasthenia gravis (if pt's symptoms improve, pt has myasthenia gravis; if not, pt has Lambert-Eaton syndrome) |
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Cholinesterase inhibitor poisoning |
Often due to organophosphates (ex. parathion) that irreversibly inhibit AChE Organophosphates are components of insectisides, so poisoning is usually seen in farmers Causes DUMBBELSS: diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal muscle and CNS, lacrimation, sweating, salivation Tx with atropine and pralidoxime (regenerates AChE) |
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Atropine |
Muscarinic antagonist Competitive inhibitor Clinical uses: bradycardia, ophthalmic conditions, cholinesterase inhibitor poisoning (give with pralidoxime) S/E: increased body temperature (due to decreased sweating); rapid pulse; dry mouth; dry, flushed skin; cycloplegia; constipation; disorientation |
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Homatropine |
Muscarinic antagonist Produces mydriasis and cycloplegia |
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Tropicamide |
Muscarinic antagonist Produces mydriasis and cycloplegia |
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Benztropine |
Muscarinic antagonist Clinical uses: Parkinson disease |
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Scopolamine |
Muscarinic antagonist Clinical uses: motion sickness |
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Ipratropium |
Muscarinic antagonist "I pray I can breathe" Clinical uses: COPD, asthma |
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Tiotropium |
Muscarinic antagonist Clinical uses: COPD, asthma |
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Oxybutynin |
Muscarinic antagonist Clinical uses: reduce urgency in mild cystitis; reduce bladder spasms |
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Darifenacin |
Muscarinic antagonist Clinical uses: reduce urgency in mild cystitis; reduce bladder spasms |
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Solifenacin |
Muscarinic antagonist Clinical uses: reduce urgency in mild cystitis; reduce bladder spasms |
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Glycopyrrolate |
Muscarinic antagonist Clinical uses: GI (decrease drooling; peptic ulcers); respiratory (preoperative reduction of airway secretions) |
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Epinephrine |
Sympathomimetic beta>alpha (alpha effects predominate at high doses) Clinical uses: anaphylaxis (epi causes vasoconstriction, bronchodilation), open angle glaucoma; (DON'T USE IN CLOSED ANGLE GLAUCOMA); asthma; hypotension |
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Norepinephrine |
Sympathomimetic alpha1>alpha2>beta1 Clinical uses: hypotension (but decreases renal perfusion) |
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Isoproterenol |
Sympathomimetic
beta1=beta2 (iso means equal) Clinical uses: electrophysiologic evaluation of arrhythmias |
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Dopamine |
Sympathomimetic
D1=D2>beta>alpha Clinical uses: unstable bradycardia, acute heart failure, shock Inotropic and chronotropic alpha effects predominate at high doses |
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Dobutamine |
Sympathomimetic
beta1>beta2=alpha So unlike dopamine, there is no renal vasodilating effect Clinical uses: acute heart failure (inotropic>chronotropic) |
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Phenylephrine |
Sympathomimetic alpha1>alpha2 Clinical uses: hypotension, produces mydriasis for ocular procedures, rhinitis (decongestant) |
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Albuterol |
Sympathomimetic beta2>beta1 Clinical uses: acute asthma |
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Salmeterol |
Sympathomimetic beta2>beta1 clinical uses: long term asthma or COPD control |
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Terbutaline |
Sympathomimetic beta1>beta2 Clinical uses: reduce premature uterine contractions |
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Amphetamine, cocaine |
Indirect sympathomimetics
Inhibit reuptake of NE Cocaine causes vasoconstriction and local anesthesia; never give beta-blockers if cocaine intoxication is suspected (can lead to unopposed alpha1 activation and extreme hypertension) |
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Clonidine |
sympatholytic (alpha2-agonist) Clinical uses: hypertensive urgency; does not decrease renal blood flow; ADHD, severe pain S/E: CNS depression, bradycardia, hypotension, respiratory depression, miosis |
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alpha-methyldopa |
sympatholytic (alpha2-agonist) Clinical uses: hypertension in pregnancy (doesn't cross placenta) S/E: direct Coombs positive hemolytic anemia, SLE-like syndrome |
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phenoxybenzamine |
alpha blocker -- non-selective, irreversible clinical uses: pheochromocytoma (used preoperatively) to prevent catecholamine (hypertensive) crisis S/E: orthostatic hypotension, reflex tachycardia |
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phentolamine |
alpha blocker -- non-selective, reversible clinical uses: give to pts on MAO inhibitors who eat tyramine-containing foods |
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Prazosin |
alpha blocker -- alpha1 selective clinical uses: urinary symptoms of BPH; hypertension; PTSD S/E: first-dose orthostatic hypotension, dizziness, headache |
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Terazosin |
alpha blocker -- alpha1 selective clinical uses: urinary symptoms of BPH; hypertension S/E: first-dose orthostatic hypotension, dizziness, headache |
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Doxazosin |
alpha blocker -- alpha1 selective clinical uses: urinary symptoms of BPH; hypertension S/E: first-dose orthostatic hypotension, dizziness, headache |
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Tamsulosin (Flomax) |
alpha blocker -- alpha1 selective clinical uses: urinary symptoms of BPH; NOT used for hypertension S/E: least S/E of the alpha1-selective alpha blockers; first-dose orthostatic hypotension, dizziness, headache |
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Mirtazapine |
alpha blocker -- alpha2 selective clinical uses: depression S/E: sedation, increased serum cholesterol, increased appetite |
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Metoprolol, acebutolol, betaxolol, propanolol, carvedilol, esmolol, atenolol, nadolol, timolol, pindolol, labetalol |
Beta-blockers (end in "-lol") Clinical uses: angina pectoris (decrease O2 consumption), MI (decrease mortality), SVT (metoprolol, esmolol; class II antiarrhythmic), hypertension (decrease CO, renin secretion), CHF (keeps heart responsive to sympathetic stimulation), glaucoma (timolol; decrease secretion of aqueous humor), essential tremor (propranolol) |
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Beta-blocker toxicity |
Impotence, CV effects (bradycardia, AV block, CHF), CNS effects (seizures, sedation, sleep issues), decreased HDL, increased TGs, bronchospasm/bronchoconstriction, abrupt withdrawal can cause myocardial ischemia in CAD pts Avoid beta-blockers in cocaine users due to risk of unopposed alpha-adrenergic receptor agonist activity |
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Beta1-selective antagonists (beta1>beta2) |
Beta-blockers starting with letters A to M acebutolol, atenolol, betaxolol, esmolol, metoprolol |
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Non-selective antagonists (beta1=beta2) |
Beta-blockers starting with letters N to Z nadolol, pindolol, propranolol, timolol |
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Non-selective alpha and beta antagonists |
Have modified suffixes (instead of "-olol") carvedilol, labetalol |
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Longest-acting beta-blocker |
Propranolol |
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Shortest-acting beta-blocker |
Esmolol |
