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91 Cards in this Set
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- Back
- 3rd side (hint)
EPI
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-alpha 1, alpha 2, beta 1, beta 2
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-Rapid- alpha-1, only small ↑ in HR b/c of vagal reflex, ↑BP, ↑PP, ↑ TPR
-Slow- beta-2, large ↑ in HR, small ↓ in BP, ↓ TPR, ino=chrono -prolongs effects of local anesthetics, interacts w/halogenated (↑cardiac effects of CAs) -anaphylactic/cardiac arrest, redistribution of blood flow |
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NE
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- alpha1, alpha 2, beta1 NO beta 2 agonist
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no axn at beta-2 receptors, large reflex ↓ in HR, ↑ BP, ↑ TPR (NO redistribution of blood)
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Isoproterenol
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- beta 1= beta 2 agonist
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large ↑ in HR, small ↑ in BP, ↓ TPR
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Dobutamine
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Beta 1 agonist
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I.V, ino>chrono, cardiac decompensation, ↑ CO w/o ↑ TPR
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Beta-2 Agonists
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Albuterol
Terbuterol Metaproterenol |
all are more resistant to MAO/COMT, ↓leukotrienes/histamine
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Albuterol
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Beta 2 agonist
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asthma, more selective for beta 2 than other beta 2's
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Terbuterol
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Beta 2 agonist
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status asmaticus (IV)
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Metaproterenol
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Beta 2 agonist
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bronchospasm (less selective)
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Alpha 1 agonists
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Phenylephrine
Methoxamine |
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Phenylephrine
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Alpha 1 agonist
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mydriatic and nasal decongestant, dx of horner’s
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Methoxamine
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Alpha 1 agonist
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I.V. for hypotension, or to indirectly ↓HR in PAT
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Alpha 2 agonists
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Clonidine
Apraclonidine Methyldopa Guanfacine |
Side Effects: dry mouth & sedation (50%)
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Clonidine
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Alpha 2 agonist
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hypertension, ADHD/Tourette’s (+Ritalin), withdrawal htn
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Apraclonidine
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Alpha 2 agonist
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Glaucoma ↓ production of aqueous humor
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Methyldopa
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Alpha 2 agonist
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metabolized centrally to α-methylnorepinephrine, activates α2 receptors to ↓
sympathetic outflow |
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Guanfacine
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Alpha 2 agonist
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similar to clonidine
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Indirect Acting Sympathomimetics
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1) Methamphetamine
2) Methylphenidate 3) Atomoxetine 4) Ephedrine 5) Tyramine 6) Cocaine |
Side Effects: restlessness, tremor, irritability, headache, “psychosis”, psychological dependence
Uses: obesity, narcolepsy, enuresis, ADHD |
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Methamphetamine
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Indirect Acting Sympathomimetic
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-more pronounced CNS effects, less prominent peripheral effects
–Block reuptake of monoamines –Induces euphoria, increase alertness, decrease fatigue –Effects last 6-8 hours, initial “rush” assoc. with smoking or injection |
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Methylphenidate
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Indirect Acting Sympathomimetic
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more prominent effects on mental activities than motor activities
–Used for ADHD--ADHD etiology is unknown, may be assoc. with DA transmission dysfunction in striatum and prefrontal ctx and an increase in DAT activity – methylphenidate may decrease/block DAT binding sites--improves focus and inhibitory control |
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Atomoxetine
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Indirect Acting Sympathomimetic
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selective NE reuptake inhibitor in prefrontal ctx--non-stimulant, for ADHD (no effect on DA in striatum or nucleus accumbens)
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Ephedrine
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Indirect Acting Sympathomimetic
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•Has direct actions on α and β receptors and acts indirectly to increase NE release--amphetamine-like actions
•Similar effects to EPI and NE, with longer duration. Increases HR, CO, TPR (variably) and usually increases BP. Orally effective. Associated with tachyphylaxis •CNS stimulant, used for bronchodilation, nasal decongestant. Also used to enhance athletic performance, as an energy enhancer, and for weight loss |
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Tyramine
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Indirect Acting Sympathomimetic
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taken up into presynaptic nerve terminals and causes release of catecholamines
•Normal by-product of tyrosine metabolism, and found in many fermented foods (red wine, pickled herring, nuts, aged cheeses, soy and teriyaki sauce) •Normally metabolized by MAO in the liver without reaching significant blood concentration •Can ppt. a hypertensive crisis when patients on MAO inhibitors (particularly MAO-A inhibitors) ingest tyramine-containing foods |
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Cocaine
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Indirect Acting Sympathomimetic
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block DAT reuptake mechanism--less potent at NE and 5HT reuptake. Also has local anesthetic action, by blocking sodium channels
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Alpha Adrenergic Receptor Blockers
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Yohimbine
Prazosin Phentolamine Phenoxybenzamine |
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Phenoxybenzamine
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Nonselective Alpha Blocker-irreversible
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–Decreases PVR, increases CO (symp. reflex)
–α2 blockade increases NE release--reflex tachycardia –Decreases BP in upright position (dep. on existing tone) –Uses: pheochromocytoma –Side Effects: orthostatic hypotension, reflex tachycardia • Uses: treatment of pheochromocytoma |
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Phentolamine
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Nonselective Alpha Blocker-reversible
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Similar actions to phenoxybenzamine
–Uses: •short term control of BP in patients with pheochromocytoma •Treatment of hypertensive crisis following clonidine withdrawal or tyramine-MAOI interaction –Toxicity: hypotension, reflex tachycardia, myocardial ischemia |
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Prazosin
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Alpha1 Selective Blocker
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•Major action: arteriolar and venous dilation
•No significant change in HR or reflex tachycardia (no α2 autoreceptor block) –Also no significant increase in CO May be beneficial in patients with benign prostatic hyperplasia that are not good surgical candidates •Adverse effects: first dose phenomenon--marked postural hypotension and syncope, also dizziness, headache, drowsiness •Uses: hypertension, refractory CHF |
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Yohimbine
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Alpha2 Receptor Blocker
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competitive selective α2 receptor antagonist
–Can increase sympathetic outflow centrally and increase release of NE peripherally by blocking autoreceptors –Increase α1 and β1 activities, increase BP •Nonselective alpha blockers do not increase BP –Limited use for treatment of male sexual dysfunction (limited clinical evidence to support this) |
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Ergot Alkaloids
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•Have a variety of effects at α-adrenergic, 5HT and DA receptors
•CNS active •Used for the treatment of migraine (probably other receptor systems are responsible) and to prevent postpartum hemorrhage |
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Nonselective Beta Blockers
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Propranolol:
Nadolol Timolol Pindolol |
Inhibit the chronotropic, inotropic, and vasodilating response to β-adrenergic stimulation--have little effect on normal heart at rest (effects depends on existing tone)
Metabolic Effects: block glucose utilization in response to hypoglycemia –Block peripheral signals of hypoglycemia –Use with caution in patients with labile diabetes |
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Propranolol
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Nonselective Beta Blocker
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highly lipophilic, extensive first pass metabolism, highly protein bound, also used for migraine, stage fright
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Nadolol
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Nonselective Beta Blocker
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long duration of action
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Timolol
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Nonselective Beta Blocker
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short-acting, used for glaucoma
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Pindolol
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Nonselective Beta Blocker
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prototype for ISA
best for patients with obstructive airway disorders |
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Non-selective beta+alpha 1 blockers
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Carvedilol
Labetolol |
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Carvedilol
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Non-selective beta+alpha 1 blocker
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nonselective beta blocker, also blocks α1 receptors. Higher β1 : α1 blocking ratio, longer duration of β1 blocking activity
all patients with CHF respond favorably to beta blockers |
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Labetolol
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Non-selective beta+alpha 1 blocker
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also blocks α1 receptors, can inhibit Uptake-1, decreases BP with no reflex tachycardia
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Sotalol
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Nonselective Beta Blocker
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antiarrhythmic agent
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β1-Selective Antagonists
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Atenolol
Esmolol Acebutolol Metoprolol |
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Atenolol
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β1-Selective Antagonists
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limited CNS penetration, no ISA
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Esmolol
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β1-Selective Antagonists
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short duration, given IV, no ISA or membrane stabilization
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Acebutolol
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β1-Selective Antagonists
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actions similar to metoprolol, has ISA, membrane stabilizing activity
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Metoprolol
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β1-Selective Antagonists
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no ISA, do not use in patients with acute MI associated with bradycardia or heart block
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Sympatholytic Agents
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Metyrosine
Reserpine Guanethidine Bretylium |
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Metyrosine
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Sympatholytic Agents
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inhibits catecholamine synthesis. Decreases biosynthesis by inhibitng tyrosine hydroxylase. Used for treatment of pheochromocytoma. Not effective for treatment of hypertension.
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Reserpine
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Sympatholytic Agents
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Reduces cardiac output and PVR. Side effects include sedation, psychotic depression. Irreversibly blocks VMAT, making catecholamines stuck in the nerve terminal where they're eaten up. Depletes the catecholamines.
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Guanethidine
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Sympatholytic Agents
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Interferes with excitation-release coupling to inhibit NE release in peripheral adrenergic nerve terminals. Can also interfere with vesicular storage and act as a false transmitter. Uses: hypertension
Competes for Norepinephrine transporter (NET) |
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Bretylium
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Sympatholytic Agents
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prevents invasion of action potentials into nerve terminals—interferes with normal excitation-release coupling. Used for treatment of arrhythmias
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Choline Esters
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Carbachol
Bethanechol |
Indications
•CV (ACh infusion)--to test patency of the endothelium of coronary vessels •GI disorders (postoperative abdominal distension, gastric atony, adynamic ileus) •UR bladder disorders (urinary retention, hypotonic, myogenic or neurogenic bladder) •Ophthalmology: cataract extractions (ACh), wide angle glaucoma (local application--contraction of the ciliary body facilitates outflow of aqueous humor to decrease intraocular pressure) |
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Adverse Effects of Cholinomimetics
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DUMBELS: Diarrhea, Urination, Miosis, Bronchoconstriction, Excitation (of skeletal muscle and in CNS-convulsions), Lacrimation, Salivation and Sweating
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Tissue Sensitivity to ACh
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Cardiovascular effects >
Smooth Muscle and Glands> Autonomic Ganglia> Neuromuscular Junction |
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Carbachol
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Mixed nicotinic and muscarinic agonist
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May be used locally in eye to produce miosis
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Bethanechol
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Mostly muscarinic agonist
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GI/Urinary retention
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Pilocarpine
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Alkaloid muscarinic agonist
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-predominantly muscarinic actions; sweat glands very sensitive.
-used as a miotic agent in the treatment of glaucoma (open angle). -better tolerated than anticholinesterases. |
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Alcohol Anticholinesterases
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edrophonium
donepezil |
reversible, non-covalent, short duration
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Carbamate Anticholinesterases
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Neostigmine
Physostigmine |
reversible, covalent, moderate duration
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Organophosphates
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echothiophate
Malathion Soman Sarin DFP |
Irreversible covalent long duration
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Edrophonium
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Alcohol anitcholinesterase
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diagnostic test and to assess the adequacy of dosing of anti-ChE agents in the treatment of myasthenia gravis.
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Donepezil
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Alcohol anitcholinesterase
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Mild to moderate Alzheimer's Disease
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Neostigmine
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Carbamate anitcholinesterase
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Myasthenia Gravis:
Postoperative ileus, atony of smooth muscle of the GI or urinary bladder Termination of the effects of neuromuscular blockers |
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physostigmine
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Carbamate anitcholinesterase
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short acting glaucoma
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pyridostigmine
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Carbamate anitcholinesterase
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intermediate myasthenia gravis
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ambenonium
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carbamate anticholinesterase
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intermediate-long acting myasthenia gravis
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Echothiophate
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organophosphate
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long acting glaucoma, NOT lipid soluble tho
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Malathion
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organophosphate
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insecticide, metabolized well by humans tho
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Sarin, Soman, DFP
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Organophosphates
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lipophilic with excessive muscarinic action
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pralidoxime
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aka 2-pam
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Treatment of organophosphate posioning:
Within 1-2 days: Atropine + 2-PAM –2-PAM (pralidoxime) exerts a nucleophilic attack on phosporylated enzyme, causing a splitting off of the oxime-phosphonate to regenerate the AChE enzyme •Primarily affects skeletal muscle; no effect in CNS •Most effective if given before the “aging” process |
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Glaucoma Treatment with Anticholinesterases
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physostigmine (short-acting), demarcarium (intermediate), echothiophate (long-lasting).
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Myasthenia Gravis Treatment with Anticholinesterases
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neostigmine (short-acting), pyridostigmine (intermediate), ambenonium (intermediate-long acting).
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More lipid soluble agents (e.g., physostigmine) are well absorbed orally and have effects at both peripheral and central sites.
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Termination of the effects of neuromuscular blockers
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neostigmine, edrophonium
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Agents containing quaternary ammonium groups (i.e. edrophonium, neostigmine,) do not penetrate cell membranes easily, they are poorly absorbed from the GI tract or across the skin or into the CNS. These compounds seem to work more selectively at the neuromuscular junction.
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Antimuscarinic Agent
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Atropine
Scopolamine Cyclopentolate Pirenzepine Tolterodine Ipratropium |
COMPETITIVE blockade
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Sensitivity of different effector organs to Atropine
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↓salivation > ↓ bronchial secretions, sweating >
pupillary dilation, spasm of lens accommodation > tachycardia > ↓ micturition, ↓ gut tone/motility > ↓ gastric secretion and motility > CNS excitation, delirium, coma |
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Contraindications for anticholinergics
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Contraindications:
–Narrow angle glaucoma (may ppt. closure) –Prostatic hypertrophy –Gastric ulcer (slows emptying) |
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Atropine
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Antimuscarinic Agent
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Produce mydriasis and
cycloplegia minimal CNS effects at clinical doses Atropine is usually the preferred drug unless depressant action is wanted (i.e. preanesthetic medication) Antitremor activity, useful in treatment of Parkinson's Disease |
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Scopolamine
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Antimuscarinic Agent
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motion sickness
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Ipratropium
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Muscarinic Anticholinergic
Quaternary ammonium. blocks M2 and M3 receptors |
-used as an inhalational drug for treatment of asthma.
-poorly absorbed. -produces bronchodilation. -effects limited to mouth and airways—blocks M2 and M, receptors in airways. |
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Cyclopentolate
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Muscarinic Anticholinergic
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-Mydriatic.
-shorter duration. -preferred over atropine or scopolamine |
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Pirenzepine
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Muscarinic Anticholinergic
-selective M1 receptor antagonist. |
-used for peptic ulcer; greater GI selectivity, no CNS effects.
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Tolterodine
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Muscarinic Anticholinergic
Selective for M2 and M3 receptors |
-Targets the bladder, fewer side effects
-Urinary incontinence |
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Nondepolarizing (Competitive) Neuromuscular Blocks
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Tubocurarine, Pancuronium, Vecuronium
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Depolarizing-Desensitizing Blocks
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Succinylcholine
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Tubocurarine
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Prototype nondepolarizing (competitive, stabilizing) neuromuscular block
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-competitively blocks ACh transmitter action
-does not interfere with the contractile capabilities of the muscle -muscle does not respond to motor-nerve impulses or applied ACh -histamine release |
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Succinylcholine
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Prototype depolarizing (depolarizing-desensitizing) neuromuscular blocker
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-Characteristics of Paralysis: transient muscle fasciculations all over chest and abdomen.
-Neck, arms and legs before facial, lingual, laryngeal and pharyngeal. -I.V. administration. -Very short duration; rapidly hydrolyzed by butyrylcholinesterases. -No significant effect at autonomic ganglia. -Malignant Hyperthermia |
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dantrolene
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depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor
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treatment for malignant hyperthermia
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Anticholinesterases + competitive neuromuscular blockers
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reverse or decrease neuromuscular block.
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Anticholinesterases + depolarizing blockers
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do not reverse, and can enhance the neuromuscular block.
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Inhalation anesthetics + competitive neuromuscular blockers
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can act synergistically with competitive blockers.
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Aminoglycosides + competitive neuromuscular blockers
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can act synergistically with competitive blockers.
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Ganglionic Blocking Agents
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Hexamethonium, Trimethaphan.
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-still used for initial control of blood pressure in patients with acute dissecting aortic aneurysm.
-also used in the production of controlled hypotension to minimize hemorrhage in the operative field. |
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Site
Arterioles Veins Heart Iris Ciliary Muscle GI Tract Urinary Bladder Salivary Glands Sweat Glands |
PREDOMINANT TONE AT VARIOUS AUTONOMIC EFFECTOR SITES
Site Predominant Tone Arterioles Sympathetic Veins Sympathetic Heart Parasympathetic Iris Parasympathetic Ciliary Muscle Parasympathetic GI Tract Parasympathetic Urinary Bladder Parasympathetic Salivary Glands Parasympathetic Sweat Glands Sympathetic (cholinergic) |
PREDOMINANT TONE AT VARIOUS AUTONOMIC EFFECTOR SITES
Site Predominant Tone Effect of Ganglionic Blockade Arterioles Sympathetic Vasodilation Veins Sympathetic Vasodilation Heart Parasympathetic Tachycardia Iris Parasympathetic Mydriasis Ciliary Muscle Parasympathetic Cycloplegia GI Tract Parasympathetic Depressed tone and motility Urinary Bladder Parasympathetic Urinary retention Salivary Glands Parasympathetic Xerostomia Sweat Glands Sympathetic (cholinergic) Anhidrosis |