Term
Direct acting muscarinic agonists |
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Definition
- acetylcholine
- carbachol
- methacholine
- bethanechol
- pilocarpine (Salagen) - muscarine
- cevimiline (Evoxac) |
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Term
Reversible cholinesterase Inhibitors |
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Definition
- edrophonium
- physostigmine/eserine
-neostigmine
-pyridostigmine
- rivastigmine
- donepezil
- carbamate insecticides (e.g. Carbaryl) |
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Term
Irreversible cholinesterase inhibitors |
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Definition
- DFP/diisopropylfurophosphate/isofluorophate & echothisophate
- organophosphate insecticides (Parathion, Malathion)
- nerve gases (used in chemical warfare, e.g. Sarin) |
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Term
cGMP phosphodiesterase (PDE-5) inhibitors |
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Definition
- Sildenafil (Viagra) -onset 30 m; peak blood lvls 1 h; duration 4 h
-Vardenafil (Levitra) -onset 30 m; peak blood lvls 1 h; duration 4 h
-tadalafil (Cialis) - onset 45 m; duration 36 h because longer half-life
-MOA: inhibit PDE-5, which normally degrades the vasodilatory cGMP; vasodilation = erection
-side effects: may inhibit PDE-5 in peripheral tissues, leading to vasodilation, hypotension, and a subsequent reflex tachycardia (pts. must have CV function assessed before being given these drugs) |
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Term
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Definition
- atropine, homoscyamine, homoatropine
- scopolamine, methoscopolamine
-dicyclomine
-propantheline
-glycopyrrolate
-ipratropium
-tiatropium
-benzotropine
-trihexyphenidyl
-tolteridine
-oxybutynin
-solifenacin
-tropicamide |
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Term
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Definition
- muscarinic agonist
-NEVER administered via IV b/c rapidly degraded by plasma "pseudocholinesterase"
-used to tx. glaucoma |
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Term
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Definition
- muscarinic agonist; ACh analog
-resistant to hydrolysis by cholinesterases
-stimulates nicotinic + muscarinic receptors
-used to tx. glaucoma |
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Term
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Definition
-muscarinic agonist; ACh analog
-stimulates only muscarinic, not nicotinic, receptors
-used for pulmonary function testing in asthmatics |
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Term
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Definition
-muscarinic agonist; ACh analog
-resistant to rapid hydrolysis
-stimulates only muscarinic, not nicotinic, receptors
-used in the tx. of urinary retention; stim. GI motility |
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Term
Pilocarpine (Salagen, Ocusert Pilo) |
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Definition
-muscarinic agonist
-used to tx. glaucoma + xerostomia |
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Term
Toxic effects of acetylcholinesterase inhibitors (reversible OR irreversible) |
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Definition
- S.L.U.D.G.E
-S -salivation -L-lacrimation -U-urination -D-defecation -G-GI distress -E-emesis
-muscle fasciculations followed by paralysis due to desensitization of nicotinic receptors
-bradycardia, hypotension, shock |
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Term
Treatment of acute cholinesterase inhibitor poisoning |
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Definition
(1) high doses of atropine (2-4 mg IV) + 2 mg IM every 10 min to block muscarinic receptors
(2) if organophosphate (i.e. irreversible) poisoning, follow with pralidoxime to reactivate acetycholinesterase
(3) supportive treatment (i.e. diazepam for seizures) |
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Term
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Definition
-irreversible/slowly reversible acetylcholinesterase inhibitor
- used in tx. of glaucoma |
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Term
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Definition
-reversible acetycholinesterase inhibitor
- used in tx. of Alzheimer's disease
-Alzheimer's - loss of cholinergic neurons in nucleus basalis of Meynert
-used along with donepezil |
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Term
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Definition
-reversible acetylcholinesterase inhibitor
-used in the treatment of Alzheimer's, along with Rivastigmine |
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Term
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Definition
-reversible acetylcholinesterase inhibitor
-used to tx. atropine/muscarinic antagonist poisoning
-nonquaternary - CAN ENTER CNS |
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Term
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Definition
- used to tx. Myasthenia gravis
-used by military to protect personnel against nerve agents; "pre-exposure antidotal enhancement" |
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Term
Diagnosis and Treatment of Myasthenia Gravis |
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Definition
(1) diagnosis - Edrophonium (Tensilon)
(2) tx. - neostigmine, pyridotigmine
*Edrophonium, neostigmine, pyridostigmine quaternary ammonium compounds - DO NOT ENTER CNS |
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Term
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Definition
-acetycholinesterase reactivator
-not effective with carbamate insecticide poisoning |
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Term
Carbamate insecticides (carbaryl) |
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Definition
-reversible acetycholinesterase inhibitor
- tx. (1) atropine, but pralidoxime is NOT useful |
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Term
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Definition
-irreversible acetylcholinesterase inhibitor
-tx. poisoning with (1) atropine, (2) pralidoxime |
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Term
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Definition
- toxin prevents release of acetycholine from nerve endings - affects both autonomic nerve endings (classic anticholinergic effects) and NMJ (paralysis)
-death from diaphragmatic paralysis
-tx: symptomatic support + Ab against toxin |
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Term
S/S of anti-muscarinic agent poisoning: |
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Definition
- dry, hot skin -mydriasis, blurring of vision, photophobia -CNS stimulation: agitation, hallucinations, seizures -cessations of GI mobility (no bowel sounds) -weak, rapid pulse -tachycardia/tachyarrhythmia
-tx. with physostigmine + other cholinesterase inhibitor; benzodiazepines for seizures |
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Term
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Definition
-muscarinic antagonist
-natural
-racemix mixture of d,l-hyoscyamine; able to get into CNS (vs. homoatropine, which is not!!!)
-causes tachycardia, which may be preceded by a slight bradycardia
-used in the tx. of certain types of MIs where there is an increase in vagal tone (i.e. fall in BP + low cardiac output)
-CNS effects: low dose - sedative effects; mod doses - hallucinogenic effects; high doses - stimulant effects (agitation/seizures) |
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Term
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Definition
-muscarinic antagonist
-synthetic analog of atropine
-does not enter CNS |
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Term
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Definition
-muscarinic antagonist
-natural; structurally similar to atropine
-enters CNS!
-uses of scopolamine similar to atropine, but it has more of a CNS depressant effect (sedation/amnesia)
-used orally/patch form (Transderm Scop) for the prevention of motion sickness/vertigo |
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Term
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Definition
- muscarinic antagonist
-quaternary analog of scopolamine that does not enter CNS |
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Term
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Definition
-muscarinic antagonist
-non-quaternary
-antispasmodic used in the treatment of IBS |
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Term
Propantheline (Pro-bathine) |
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Definition
-muscarinic antagonist
-quaternary, so no CNS effects!
-antispasmodic used to treat IBS (same as dicyclomine) |
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Term
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Definition
-muscarinic antagonist
-quaternary, doesn't affect CNS
-used pre-op to dry respiratory secretions and inhibit vagal reflexes (i.e. bradycardia) |
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Term
Ipratropium (Atrovent) & Tiatropium (Spiriva) |
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Definition
- muscarinic antagonist
- quaternary
-used in treatment of asthma & COPD
-Tiatropium - newer drug, longer acting |
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Term
Benztropine (Cogentin) & Trihexyphenidyl (Artane) |
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Definition
- muscarinic antagonist
-centrally acting
-used in the treatment of idiopathic or drug-induced PD |
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Term
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Definition
-muscarinic antagonist
-used to treat urinary incontinence |
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Term
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Definition
-muscarinic antagonist
-used to tx. urinary incontinence |
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Term
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Definition
-muscarinic antagonist
-used to treat urinary incontinence |
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Term
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Definition
-muscarinic antagonist
-used to pupillary dilation for ophtho exam |
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Term
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Definition
-competitive ACh antagonists that act at the neuromuscular junction *because competitive, effects can be overcome by cholinesterase inhibitors
-blocks nicotinic receptors during surgery
-promote muscle relaxation |
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Term
Succinylcholine (Anectine) |
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Definition
-depolarizing neuromuscular blocking drug *b/c non-competitive, effects cannot be overcome by acetylcholinesterase inhibitors
-initially stimulates nicotinic receptors at the NMJ to cause weak contractions (fasciculations), then causes relaxation and paralysis |
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Term
non-selective adrenergic receptor agonists |
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Definition
-epinephrine -norepinephrine -isopreterenol -dopamine |
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Term
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Definition
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Term
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Definition
-albuterol -metaproterenol -pirbuterol -salmeterol -terbutaline
-used as "bronchodilators" (most often as "rescue" inhalers)
-terbutaline used to manage premature labor by causing B2-mediated uterine relaxation |
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Term
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Definition
-phenylephrine -midodrine (ProAmatine)
-phenylephrine: raises diastolic + mean BP, but with more reflex bradycardia than NE because NE also stimulates B1 in SA node
-uses of phenylephrine: (1) maintain diastolic BP during shock/spinal anesthesia, (2) hemorrhoids, (3) nasal congestion, (4) mydriatic agent (pupillary dilation mediated by a1 receptors), (5) tx. supraventricular tachycardia
-phenylephrine poor oral absorption
-uses of midodrine: (1) orthostatic hypotension (can be given orally), (2) tx. urinary incontinence (a1 constricts urinary sphincter) |
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Term
Indirect-acting sympathomimetics |
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Definition
-cocaine -pseudoephedrine (Sudafed) & ephedrine -amphetamine & methamphetamine - methylphenidate (Ritalin) |
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Term
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Definition
- selectivity: a1 = a2 = B1 = B2
- at low IV doses, stimulates a2 & B2 receptors --> causes: decrease in diastolic BP, increase in systolic, increase in pulse pressure, but no change in MAP
-at higher doses, a1 & B1 receptors also stimulation --> NOW, increase in diastolic BP, increase in systolic, increase in pulse pressure, increase in MAP
-uses: (1) tx. circulatory collapse during anaphylactic shock, (2) bronchospasm during circulatory shock/asthma, (3) cardiac arrest, (4) bradycardia due to A-V block/sinus, (5) mixed w/ local anesthetics to prolong action at local sites of injection and to minimize local bleeding |
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Term
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Definition
-adrenergic receptor agonist
-a1 = a2 = B1 >> B2
-both low & high rates of IV infusion increase systolic, diastolic, MAP, and pulse pressure (but to higher degree at high rates)
-CAUSE REFLEX DECREASE IN HEART RATE
-uses: used during spinal anesthesia to prevent drop in MAP |
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Term
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Definition
-adrenergic agonist
- B1 = B2 >> all others
- both low & high rates decrease diastolic + mean pressures while increasing pulse pressure + heart rate
-uses: "pharmacologic provocation" to assist tilt-table tests for diagnosis of unexplained syncopes (vasovagal syncope) |
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Term
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Definition
-adrenergic agonist
-D receptor > B1 > a1 >>all others
-D receptors in GI/renal smooth muscle at low doses --> cause vasodilation -B1 at intermediate doses -a1 at high doses
-uses: (1) cardiogenic + neurogenic shock |
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Term
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Definition
-selective B1 agonist
-mix of 2 stereoisomers: (1) a1 agonist, (2) potent B1 agonist + a1 antagonist
-B1 stimulation increases cardiac contractility, CO, pulse pressure; no change in diastolic at therapeutic doses
-uses: (1) CHF, (2) shock |
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Term
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Definition
-indirect acting sympathomimetic
-MOA: inhibits reuptake of NE
-good local anesthetic, exerts its own local vasoconstrictor action at site of local injection (slows its own loss from site)
-uses: (1) pain relief, (2) epistaxis while doing intubation of trachea through nose |
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Term
Pseudoephedrine (Sudafed)/Ephedrine |
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Definition
-indirect acting sympathomimetic agent
-stimulates release of NE from nerve endings + stimulates adrenergic receptors DIRECTLY
-uses: (1) treat nasal/bronchial congestions --> promotes nasal & sinus drainage |
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Term
Sympathomimetics that must be administered orally: |
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Definition
- a1 agonists: phenylephrine + midodrine
-B2 agonists: albuterol, metaproterenol, pirbuterol, salmeterol, terbutaline
-indirect-acting sympathomimetics (except cocaine) - pseudoephedrine + methamphetamine
-ACTION LASTS HOURS |
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Term
Sympathomimetics that must be administered parenterally: |
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Definition
-B1 agonists : dobutamine
-cocaine
-E, NE, isoproterenol, dopamine
-ACTION LASTS FEW MINUTES |
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Term
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Definition
Cardioselective B-blockers: -acebutelol (B1) -atenolol (B1) -esmolol (B1) - shortest duration (10 min) -metoprolo (B1)
Non-selective B-blockers: -nadolol (B1 + B2) -pindolol (B1 + B2) -propranolol (B1 + B2) -timolol (B1 + B2)
*Labetalol (B-blocker + a-blocker) |
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Term
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Definition
- acebutolol + pindolol
-preserve at least sm. amount of B-receptor function
-DO NOT INTERFERE WITH B2-MEDIATED BV RELAXATION --> CAN DECREASE TPR <--part of their anti-hypertensive mechanism!
-contain "intrinsic sympathetic/sympathomimetic activity (ISA)" |
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Term
Cell membrane stabilizing B-blockers |
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Definition
-acebutolol + propranolol
-"local anesthetic" action only at high concentrations of the drug; therefore, this property has greater implications during overdosage |
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Term
Lipid solubilities of B-blockers |
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Definition
-acebutolol - LOW LIPID SOLUBILITY -atenolol - LOW -esmolol - LOW -metoprolol - MEDIUM -nadolol - LOW -pindolol - MEDIUM -propranolol -HIGH -timolol- MEDIUM
-significance: poorly lipid soluble drugs do not enter the CNS and are excreted, unchanged, through the kidney*; highly lipid soluble drugs DO enter the CNS and are metabolized by the liver before they are excreted
*exception is esmolol, which has low lipid solubility, but is rapidly inactivated by circulating (plasma + red blood cell) esterases |
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Term
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Definition
-B- and a1-blocker
- uses: (1) tx. of mod->severe HTN, (2) emergency tx. of hypertensive crisis
-MOA: a1 blockage is the primary mechanism by which this drug exerts its effect( --> decrease in TPR, decrease in MAP (MAP = CO*TPR))
-side effects: a-blockade = orthostatic hypotension (due to decreased vasoconstriction) |
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Term
Non-selective a (a1 + a2) blockers |
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Definition
- phenoxybenzamine
-phentolamine |
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Term
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Definition
- prazosin -terazosin -doxazosin -tamsulosin -alfuzosin -silodosin |
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Term
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Definition
-nonselective a-blocker
-MOA: non-competitive inhibition (i.e. binding to a1 + a2 receptors irreversible); only synthesis of new receptors can restore a-adrenergic function
-uses: prevent severe catecholamine-induced HTN that occurs in pheochromocytoma patients during the pre-operative period prior to surgery; better than other drugs because catecholamines cannot over the irreversible blockade
Side effects: -may inhibit histamine, serotonin, and ACh receptors, too. -miosis, sedation, drowsiness, vomiting, lethargy (enters CNS) -shock/circulatory failure (drug increases vasodilation) |
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Term
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Definition
-nonspecific a-blocker
-competitive antagonist (unlike phenoxybenzamine); short acting
-uses: (1) diagnosis of pheochromocytoma-->"Phentolamine test": following admin, short term drop in BP (35/25 mmHg after 5 mg phentolamine) suggests prescence of pheochromocytoma (normally, 5 mg doesn't cause fall in people w/o pheo) (2) during surgical removal of pheo (prevents rise in BP due to catecholamines that are released during surgery) (3) tx. overdose of a-agonist (e.g. NE) (4) prevent local dermal tissue necrosis that may occur accidentally at sites of injection of a-agonists (due to local vasoconstriction) (5) New form (OraVerse) used to reverse oral soft-tissue anesthesia resulting from intraoral submucosal injectio of a local anesthetic preparation containg a vasoconstrictor (e.g. E) |
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Term
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Definition
-selective a1 blocker
-uses: (1) *long-term tx. of mild-mod primary hypertension, esp. when given with a diuretic to offset fluid retention* (2) relax urinary sphincter and prostatic urethra, which relieves the obstructive urinary symptoms of BPH (3) tx. of Reynaud's (4) under consideration for tx. of nightmares related to PTSD
Side effects: -orthostatic hypotension, but usually only sever during the first day of admin ("first dose phenomenon") -salt + water retention -some tachycardia |
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Term
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Definition
-selective a1 blockers
-newer drug; MOA + uses almost identical to prazosin, but half-life much longer so may be better for long-term control of conditions like chronic HTN because fewer doses need to be remember by the patient
-(remember: prazosin - used to treat mild-mod primary HTN) |
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Term
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Definition
-selective a1 blocker; more specifically, block a1A receptor (found ONLY in smooth muscle of bladder neck + prostate)
-uses: (1) tx. of BPH
-Tamulosin/Silodosin vs. Prazosin, which is also used to treat BPH -> Tamu/Silo have fewer systemic vascular actions because a1A receptors are found ONLY in neck of bladder/prostate |
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Term
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Definition
-selective a1 blocker
-uses: (1) tx. BPH --> not receptor sub-type selective like tamsulosin/silodosin, but exhibits "uroselectivity" (mechanism: uroselectivity thought to be due to the accumulation of alfuzosin in prostatic tissue, where it is 2x circulating plasma level) |
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Term
Peripherally-acting sympathetic neuronal blockers |
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Definition
- decrease availability of the NE to its receptors
- reserpine
-guanethidine (Ismelin) |
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Term
Centrally-acting sympathetic neuronal blockers |
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Definition
-stimulate a2 receptor sites in brain and indirectly reduce sympathetic neuronal traffic from central sympathetic vasomotor centers to peripheral CV organs via negative FB mechanism
-methyldopa -clonidine -guanabenz -guanfacine |
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Term
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Definition
-peripherally acting sympathetic neuronal blocker
-MOA: decreases uptake of intraneuronal DA + NE into storage vesicles --> eventually depletes stored level of NE --> reduces amount released with each subsequent nerve impulse
-in CV system, decreases CO + TPR
-uses: (1) primary HTN
-side effects: (1) sedation/mental depression (due to depletion in CNS) (2) postural hypotension (3) bradycardia (4) fluid retention (5) diarrhea (due to unopposed parasympathetic activity) |
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Term
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Definition
-peripherally acting sympathetic neuronal blocker
-MOA: blocks intraneuronal reuptake of DA + NE (like reserpine), but ALSO directly blocks NE release from nerve endings
-NOT USED TO TX. HTN (UNLIKE RESERPINE) IN US
-notable interaction- guanethidine + tricyclic antidepressants: in order for guanethidine to be effective, must be taken up by the reuptake pump; reuptake prevented by antidepressants
-side effects: (1) bradycardia (2) orthostatic hypotension (3) fluid retention (4) NO CNS effects b/c it cannot enter brain (unlike reserpine) (5) diarrhea (due to unopposed parasympathetic activity) |
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Term
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Definition
-centrally-acting adrenergic neuronal inhibitor
-pro-drug -> requires metabolism to its active form (methyldopa converted by DOPA decarboxylase to a-methylnorepinephrine) --> a-methylnorepi acts as a2 adrenergic agonist in central vasomotor centers
-causes decrease in renin release, HR, CO, and *TPR*
-use: tx. of HTN during pregnancy (drug does not harm fetus)
-side effects (common to all a2 agonists): (1) peripheral fluid retention (2) xerostomia (3) sedation
-*induces a # of "autoimmune" disorders - (+) Coombs test, although hemolytic anemia is rarely present; abnormal liver function tests during 1st weeks of taking drug* |
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Term
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Definition
- centrally acting sympathetic neuronal blocker
- sm. dose required for therapeutic effect; administered transdermally (via patch)
-uses: (1) tx. of primary HTN (2) ADHD (3) migraine (4) menopausal hot flashes (5) PTSD (6) nicotine/alcohol withdrawl
-side effects: (1) local skin reaction (contact dermatitis) (2) rebound hypertension if the drug stopped abruptly |
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Term
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Definition
-centrally acting sympathetic neuronal blockers
-similar to Clonidine
-uses: (1) tx. of primary hypertension
-side effects (beneficial): (1) lowers total serum cholesterol (may be high in hypertensives) (2) causes less fluid retention (3) less sedation and less rebound hypertension than with Clonodine
-Intuniv - Guanfacine for ADHD |
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Term
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Definition
-nicotine (at low doses*) - acts on nicotinic receptors in autonomic ganglia + in skeletal muscle + in CNS
*at very high doses, nicotine acts as depressant |
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Term
Ganglionic blocking agents |
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Definition
-mecamylamine
-blocks nicotinic receptors in autonomic ganglia, but not the nicotinic receptors in skeletal muscle (person can still move skeletal muscle) |
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Term
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Definition
-used in the treatment of Parkinson's disease
-amino-acid precursor that is transported to brain via active a.a. pump and converted to dopamine by the enzyme L-dopa decarboxylase
-in periphery, the portion of drug that does not cross the BBB, is metabolized by DOPA decarboxylase to form dopamine; peripheral dopamine converted to NE + E (some) & metabolites DOPAC + HVA (mostly)
-side effects: (1) nausea/vomiting due to stimulation of the chemoreceptor trigger zone (CRTZ) by dopamine in the periphery (2) tachycardia (3) arrhythmias (4) orthostatic hypotension (5) CNS disturbances: depression, psychosis, hallucinations, nightmares, euphoria (6) increased libido, release of inhibitions, compulsive behaviors (7)*choreiform movements - after long term therapy
-USUALLY USED IN CONJUNCTION WITH CARBIDOPA |
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Term
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Definition
-used in the treatment of Parkinson's in conjunction with L-dopa
-inhibits DOPA decarboxylase in the periphery, but does not cross BBB
-allows for reduction in the dosage of L-dopa given (b/c less is metabolized in the periphery) + its side effects |
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Term
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Definition
- used in the treatment of Parkinson's disease
-combination of L-dopa + Carbidopa
-2 formulations available: 10/100 (C/L), 25/100 (C/L)
-sustained release version: Sinemet CR |
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Term
Bromocryptine (Parlodel)
Pergolide (Permax) |
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Definition
-used in the treatment of Parkinson's disease
-ergot-derived non-specific dopamine receptor agonists
-not as effective as L-dopa, but used in patients that cannot tolerate L-dopa
-may decrease severity of "on-off phenomenon"
-*BROMOCRYPTINE HAS ALSO BEEN USED TO TREAT HYPERPROLACTINEMIA-INDUCED AMENNORHEA & GALACTORRHEA BECAUSE IT INHIBITS PROLACTIN SECRETION
-however, bromocryptine no longer recommended for new mothers who do not wish to breast feed because of the risk of psychosis & seizures; a new drug, carbergoline (Dostinex) recommended for hyperprolactinemia |
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Term
Ropinirole (Requip)
Pramipexole (Mirapex) |
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Definition
-used in the treatment of Parkinson's disease
-non-ergot derived dopaminergic receptor agonists (preferentially target D2 & D3 receptors)
-being used increasingly as first-line drugs
-side effects the same, but less severe than older dopamine receptor agonists (bromocryptine + pergolide): (1) choreiform, dyskinetic movements (2) nausea (3) dizziness, confusion, sedation, behavioral changes, hallucinations
-Pramipexole (Mirapex) may have antioxidant and neuroprotective effects which may be beneficial for SLOWING THE PROGRESSION of the disease
-both drugs also used in the treatment of "restless leg syndrome" |
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Term
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Definition
-used in the treatment of Parkinson's disease
-originally used as an anti-viral agent
-stimulates the release of dopamine from nerve endings and may also inhibit its reuptake
-less effective than L-dopa; usually used as a supplement to L-dopa
-side effects: (1) mental disturbances, hyperexcitability, ataxia, confusion, convulsions (2) choreiform movements
-excreted by the kidney, so it requires proper kidney function |
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Term
Selegiline/Deprenyl (Eldepryl) |
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Definition
-used in the treatment of Parkinson's disease
-inhibit MAO-B and consequently the degradation of dopamine by the enzyme in the CNS (MAO-B only present in CNS)*
*at high doses, inhibits MAO in non-specific manner
-used as a supplement for L-dopa; especially useful in the later stages because it can decrease the severity of the "on-off phenomenon"
-some reports that Selegiline may SLOW PROGRESSION of disease by inhibiting the conversion of MPTP to MPP and other toxic metabolites; however, not yet proven! |
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Term
Entacapone (Comtan)
Tolcopone (Tasmar) |
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Definition
-used in the treatment of Parkinson's disease
-inhibit the metabolism of L-dopa and dopamine by COMT
-approved for used with L-dopa + carbidopa
-side effects due to increased levels of dopamine + other catecholamines (hallucinations, nausea, hypertension) |
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Term
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Definition
-used in the treatment of Parkinson's disease -combination product of: L-dopa, carbidopa, entacapone |
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Term
Benztropine (Cogentin)
Trihexyphenidyl (Artane) |
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Definition
-used in the treatment of Parkinson's disease
-anticholinergic drugs that reverse the imbalance between ACh + DA that occurs in Parkinson's --> blocks muscarinic receptors AND inhibits synaptic uptake of dopamine
-used for mild Parkinson's; better at treating tremor than rigidity
-drug of choice for treating iatrogenic Parkinson's from DA antagonists |
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