Term
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Definition
Cholinoceptor Agonist
Mech – acts directly
Use – limited; miosis for eye surgery
SFx – too much activation; short t1/2 |
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Term
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Definition
Cholinoceptor Agonist
Mech – similar to Ach, but longer t1/2
Use – dx of bronchiolar hypersensitivity; dx belladonna poisoning |
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Term
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Definition
Cholinoceptor Agonist
Mech – activates M and N receptors
Use – topically in glaucoma to decrease intraocular pressure
SFx – high doses = over-activation of M receptors on heart = cardiac arrest |
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Term
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Definition
Cholinoceptor Agonist
Mech – 100X potency of Ach; not destroyed by AchE, no N activity
Use – pretty much just to poison people |
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Term
| Pilocarpine (isoptocarpine, salagen) |
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Definition
Cholinoceptor Agonist
Mech – primarily ophthalmic M3 effects; from leaves of S.American plant
Use – topical for glaucoma and oral for xerostomia; opens canal of schlemm (narrow angle glaucoma); enhances tone of trabec. network (wide angle glau.); can also stimulate cortical neurons |
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Term
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Definition
Cholinoceptor Agonist
Mech – NM = muscle contractions; NN = ↑HR, vasoconstriction, ↑ gut motility, ↑ carotid body firing (↑ resp. rate), nausea and vomiting
Use – smoking cessation
SFx – contraindications = ulcers, GI disorders, asthma; drug interactions = antiarrhythmics, antidepressants |
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Term
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Definition
Cholinoceptor Agonist
Mech – short acting
Use – dx myasthenia gravis from cholinergic crisis |
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Term
| Neostigmine / Pyridostigmine |
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Definition
Cholinoceptor Agonist
Mech – no CNS entry (quatranary amine)
Use – Rx of ileus, urinary retention, reversal of NM blockers |
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Term
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Definition
Cholinoceptor Agonist
Mech – long-term; enters CNS
Use – Rx for glaucoma, atropine overdose |
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Term
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Definition
Cholinoceptor Agonist
Mech – CNS entry
Use – Rx for Alzheimer’s |
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Term
| Organophosphates (echothiophate, malathion, parathion, sarin) |
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Definition
Cholinoceptor Agonist
Mech – irreversible inhibitors of AchE; lipid soluble, long acting
Use – echo = Rx for glaucoma; mala/para = insecticides; sarin = nerve gas |
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Term
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Definition
Cholinoceptor Agonist
Mech – predominately M3; not destroyed by AchE; no N action
Use – reduce reflux; gastric emptying abnormalities; help in urine voidance |
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Term
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Definition
Cholinoceptor Antagonist
Mech – M antagonist; competes with Ach for binding on M receptors (M1, M2, and M3)
Use – antispasmodic, antisecretory, AchE inhibitor overdose, antidiarrheal, ophthalmology; counteracts peripheral vasodilation from M agonists; does not affect BP; does not enter CNS; at high doses it ↓secretions, mydriasis, hyperthermia, tachycardia, sedation, urinary retention |
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Term
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Definition
Cholinoceptor Antagonist
Mech – nonselective M antagonist; mostly on bronchial M3; reduce bronchial secretions
Use – COPD and asthma (decreases bronchiole constrictions and secretions) |
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Term
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Definition
Cholinoceptor Antagonist
Mech – M receptors in brain; re-estanlish dopaminergic-cholinergic balance; parasymp effector sites; ↓GI motility/secretions, ↑HR
Use – Parkinson’s disease |
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Term
| Hexamethonium / Mecamylamine |
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Definition
Cholinoceptor Antagonist
Mech – block N receptors (NN and NM) |
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Term
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Definition
Cholinoceptor Antagonist
Mech – non-depolarizing NM blocker; small doses = block Na+ channels; high doses = they enter pores
Use – ↓neuromuscular action during anesthesia; tracheal intubation; control of ventilation; tx of convulsions
SFx – hypotension due to systemic histamine release; hyperkalemia; ↑interocular pressure; ↑intragastric pressure; muscle pain |
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Term
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Definition
Cholinoceptor Antagonist
Mech – depolarizing NM blocker; phase 1 = persistent depolarization, eventual paralysis (augmented by ACEIs); phase 2 = endplate repolarizes, but subsequent depolarizations are difficult
Use – ↓neuromuscular action during anesthesia; tracheal intubation; control of ventilation; tx of convulsions
SFx – hyperkalemia; ↑interocular pressure; ↑intragastric pressure; muscle pain
nist |
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Term
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Definition
Cholinoceptor Antagonist
Mech – block Ach synth; block CHT (choline transporter) |
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Term
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Definition
Cholinoceptor Antagonist
Mech – block Ach synth; block VAT |
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Term
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Definition
Cholinoceptor Antagonist
Mech – block Ach synth; block Ach vesicle release |
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Term
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Definition
Cholinoceptor Antagonist
Mech – block Ach breakdown; AchE inhibitor |
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Term
| Phenyleprine (neo-synephrine) / Methoxamine |
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Definition
Adrenergic agonist
Mech – α1 selective agonist (vascular smooth muscle… ↑HR and TPR); α1 > α2 >>>>> β
Use – antihypotensive, paroxysmal tachycardia, nasal decongestant |
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Term
| Clonidine (catapres) / α-Methyldopa (aldomet) |
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Definition
Adrenergic agonist
Mech – α2 selective agonist; ↓symp tone = ↓BP; α2 > α1 >>>>> β
Use – for HTN
SFx – dry mouth, sedation, hypotension |
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Term
| Apraclonidine (lodipine) / Brimonidine (alphagan) |
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Definition
Adrenergic agonist
Mech – α2 selective agonist; ↓symp tone = ↓aqueous humor
Use – for glaucoma
SFx – dry mouth, sedation |
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Term
| Metaproterenol (metaprel) |
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Definition
Adrenergic agonist
Mech – β2 selective agonist; relax bronchial smooth m., suppress leukotriene and histamine release in lungs, enhance mucociliary fxn, ↓microvascular permeability, inhibit phospholipase A2; COMT resistant
Use – long-term COPD, acute bronchospasm
SFx – tremor, restlessness, tachycardia, ↑plasma glucose/lactate/FFAs, ↓plasma K+ |
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Term
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Definition
Adrenergic agonist
Mech – β2 selective agonist; relax bronchial smooth m., suppress leukotriene and histamine release in lungs, enhance mucociliary fxn, ↓microvascular permeability, inhibit phospholipase A2; COMT resistant
Use – long-term COPD, acute bronchospasm, emergency tx for asthma
SFx – tremor, restlessness, tachycardia, ↑plasma glucose/lactate/FFAs, ↓plasma K+ |
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Term
| Albuterol (ventolin, salbutamol) |
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Definition
Adrenergic agonist
Mech – β2 selective agonist; relax bronchial smooth m., suppress leukotriene and histamine release in lungs, enhance mucociliary fxn, ↓microvascular permeability, inhibit phospholipase A2
Use – acute bronchospasm, delay pre-term delivery
SFx – tremor, restlessness, tachycardia, ↑plasma glucose/lactate/FFAs, ↓plasma K+ |
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Term
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Definition
Adrenergic agonist
Mech – β2 selective agonist; designed specifically as uterine relaxant; relax bronchial smooth m., suppress leukotriene and histamine release in lungs, enhance mucociliary fxn, ↓microvascular permeability, inhibit phospholipase A2
Use – prolong pregnancy
SFx – tremor, restlessness, tachycardia, ↑plasma glucose/lactate/FFAs, ↓plasma K+ |
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Term
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Definition
Adrenergic agonist
Mech – D1 selective agonist; some stimulation of α2 (inhibit NE release); renal/mesenteric/peripheral vasodilation
Use – hypertensive crisis
SFx – hypotension |
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Term
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Definition
Adrenergic agonist
Mech – β1 and β2 agonist; no α activation; ↓TPR, ↑HR
Use – bradycardia, complete heart block; CHF; ionotropic agent for MI |
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Term
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Definition
Adrenergic agonist
Mech – primarily β1; directly acts on α1, β1, and β2; does not interfere with NE or dopamine release; +ionotrope (β1), +chronotrope, TPR unchanged (α1-β2 balance)
Use – short-term cardiac failure; for stress tests
SFx – excessive ↑BP and ↑HR; ventricular ectopic activity; may increase MI size; tolerance may develop |
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Term
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Definition
Adrenergic agonist
Mech – potent α and β agonist; low dose= β1(↑PP/HR/SV/CO) β2(↓TPR, vasodilation, reflex tachycardia); moderate dose = same plus α1(↑TPR/BP); high dose = α1 predominates (↑HR/TPR, reflex bradycardia) lesser β effects
Use – given subcutaneously with local anesthetics to limit diffusion (causes vasoconstriction); powerful cardiac stimulant (β1); relieve hypersensitivity rxns; restore heart rhythm; manage post-intubation and infectious croup; topical agent for ulcers
SFx – in presence of β-blocker α1 effect is unopposed leading to ↑↑MAP (epi reversal phenomenon); restlessness, headaches, tremor, palpitations; cerebral hemorrhage; arrhythmias; angina in patients with CAD |
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Term
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Definition
Adrenergic agonist
Mech – α1>>β1>>>>>β2; ↑BP/PP; ↑coronary flow; unchanged CO
Use – limited |
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Term
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Definition
Adrenergic agonist
Mech – acts on D1, D2, β1, α1; dopamine is especially important in regulation of movement; susceptible to MAO and COMT (can’t be given orally); low dose = D1(diuretic, renal vasodilation and ↓Na+ reasbsorption) D2(↓NE release); moderate dose = β1 predominates(↑HR/systolicBP/contractility, release of NE); high doses = α1 predominates(vasoconstriction)
Use – for severe congestive heart failure, cardiogenic and septic shock
SFx – hypovolemia should be corrected before use; tachycardia, angina, headache, HTN; don’t use with MAOIs or tricyclic antidepressants |
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Term
| Ephedrine (ephedrine, ephedra) |
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Definition
Adrenergic agonist
Mech – mixed-acting adrenoceptor agonist (indirectly release NE and directly activate adrenoceptors) mild CNS stimulant
Use – pseudophedrine (decongestant) |
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Term
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Definition
Adrenergic agonist
Mech – indirect-acting adrenoceptor agonist; biogenic amine release, respiratory center stimulation, stimulates cortex (reduced need for rest); ↓food intake; activates peripheral α and β, ↑BP/HR; ↑urinary retention
SFx – arrhythmias |
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Term
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Definition
Adrenergic agonist
Mech – indirect-acting adrenoceptor agonist; can be used to make epi/NE; destroyed by MAO (tyramine-rich foods (fermented cheeses) and MAOIs cause ↓↓BP) |
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Term
| Prazosin / Terazosin / Doxazosin |
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Definition
Adrenergic Antagonists
Mech – α1>>>α2; ↓BP
Use – HTN, BPH
SFx – may cause orthostatic hypotension |
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Term
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Definition
Adrenergic Antagonists
Mech – α1>α2; irreversibly blocks α; indirect baroreflex; ↓BP and ↑HR(baroreflex)
Use – pheochromocytoma; high catecholamine states
SFx – orthostatic hypotension; tachycardia; myocardial ischemia |
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Term
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Definition
Adrenergic Antagonists
Mech – α1=α2 |
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Term
| Yohimbine / Rauwoscine / Torazoline |
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Definition
Adrenergic Antagonists
Mech – α2>α1; ↑sympathetic activity; ↑NE release; ↓BP with limited HR increase
Uses – HTN |
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Term
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Definition
Adrenergic Antagonists
Mech – slightly selective for α1A; may relax prostatic smooth muscle
Use – BPH
SFx – may cause orthostatic hypotension |
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Term
| Propranolol / Nadolol / Timolol |
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Definition
Adrenergic Antagonists
Mech – blocks β1 and β2 (β1=β2); ↓HR/BP/rennin
Use – HTN, angina, arrhythmias, migraine, hyperthyroidism
SFx – bradycardia, worsened asthma, fatigue, cold hands, vivid dreams |
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Term
| Metoprolol / Atenolol / Aloprenolol / Betaxolol / Nebivolol (AMEBA) |
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Definition
Adrenergic Antagonists
Mech – block β1 > β2; ↓HR/BP/rennin
Use – angina, HTN, arrhythmias
SFx – bradycardia, fatigue, vivid dreams, cold hands (may avoid asthma) |
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Term
| Pindolol / Acebutolol / Carteolol / Penbutolol |
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Definition
Adrenergic Antagonists
Mech – block β1 and β2 with ISA (intrinsic symp. activity); ↓BP and modestly ↓HR
Use – HTN, arrhythmias, migraine
SFx – fatigue, vivid dreams, cold hands (avoid bradycardia) |
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Term
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Definition
Adrenergic Antagonists
Mech – block β > α1
Use – heart failure
SFx – fatigue |
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