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402 Cards in this Set
- Front
- Back
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What is the therapeutic class of acetylcholine?
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vasodilator, pupil constriction
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What is the pharmacologic class of acetylcholine?
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choline ester
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What is the MOA of acetylcholine?
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binds and directly activiates cholinergic receptors (specific for muscarinic and nicotinic)
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What is the clinical use of acetylcholine?
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miosis during ophthalmic surgery, coronary angiography
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What are the special considerations for acetylcholine?
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short duration due to being rapidly hydrolyzed by cholinesterase
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What is the pharmacologic class of bethanechol (urecholine)?
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choline ester
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What is the MOA of bethanechol (urecholine)?
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binds and directly activates cholinergic receptors (specific for muscarinic)
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What is the clinical use of bethanechol (urecholine)?
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postoperative or postpartum urinary retention
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What is the route of admin of acetylcholine?
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intraocular or intracoronary
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What is the route of admin of bethanechol (urecholine)?
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oral or sub Q
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What are special considerations for bethanechol (urecholine)?
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resistant to hyrolysis by cholinesterase but has relatively short duration of action
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What are adverse effects of bethanechol (urecholine)?
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should never be admin IV b/c it could cause hypotension and bradycardia
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What is the pharmacologic class of carbachol?
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choline ester
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What is the MOA of carbachol?
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binds and directly activates cholinergic receptors (specific for muscarinic and nicotinic)
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What is the clinical use of carbachol?
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glaucoma and miosis during ophthalmic surgery
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When is carbachol used?
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in cases in which a pt does not respond adquately to pilocarpine
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What is the pharmacologic class of muscarine?
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plant alkaloids
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What is the MOA of muscarine?
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direct-acting cholinergic receptor agonist (specific for muscarinic)
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What is the clinical use of muscarine?
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none
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What can consumption of the mushrooms containing muscarine cause?
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diarrhea, sweating, salivation, and lacrimation
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Is muscarine hydrolyzed by cholinesterase?
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no
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What is the route of admin of muscarine?
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none
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What is the pharmacologic class of nicotine?
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plant alkaloids
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Is nicotine hydrolyzed by cholinesterase?
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no
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What is the route of admin of nicotine?
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oral or transdermal
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What is the clinical use of nicotine?
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smoking cessation programs
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What is the MOA of nicotine?
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direct-acting cholinergic receptor agonist (specific for nicotinic)
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What is the therapeutic class of pilocarpine?
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antiglaucoma agent, sialagogue
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What is the pharmacologic class of pilocarpine?
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muscarinic receptor agonist
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What is the MOA of pilocarpine?
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actiavates muscarinic receptors in ciliary muscle, increasing aqueous humor outflow, activates muscarinic receptros in salivary gland, increasing salivation
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What is the clinical use of pilocarpine (salagen)
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treatment of glaucoma and dry mouth (xerostomia)
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Is pilocarpine (salagen) hydrolyzed by cholinesterase?
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no
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How is pilocarpine (salagen) admin?
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topical ocular or oral
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What are special considerations for pilocarpine (salagen)?
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useful in pts w/ xerostomia due to radiation of head and neck and Sjogren's syndrome
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What are adverse effects of pilocarpine (salagen)?
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miosis, blurred vision (accommodative spasms)
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What are interactions of pilocarpine (salagen)?
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additive effects w/ other cholinergic drugs, effects dec by atropine and otehr anticholinergic drugs
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What is the MOA of cevimeline (evoxac)?
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synthetic direct-acting muscarinic receptor agonist
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Is cevimeline (evoxac) hydrolyzed by cholinesterase?
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no
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What is the route of admin of cevimeline (evoxac)?
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oral
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What is the clinical use of cevimeline (evoxac)?
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xerostomia (ivestigating tx of dry eyes)
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What are adverse effects of cevimeline (evoxac)?
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inc sweating, nausea, visual disturbances caused by drug-induced miosis
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Who should cevimeline (evoxac) be used cautiously in?
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pts w/ asthma or cardiac arrhythmias
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What is the pharmacologic class of donepezil (aricept)?
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cholinesterase inhibitor
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What is the MOA of donepezil (aricept)>?
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reversibly binds and inhibits cholinesterase
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What is the duration of action of donepezil (aricept)?
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24 hours
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How is donepezil (aricept) admin?
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orally
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What is the clinical use of donepezil (aricept) and why?
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Alzheimer's b/c it readily crosses the BBB and inc the conc of ACh at central cholinergic synapses
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What is the therapeutic class of edrophonium (tensilon)?
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diagnostic agent
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What is the pharmacologic class of edrophonium (tensilon)?
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cholinesterase inhibitor
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What is the MOA of edrophonium (tensilon)?
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reversibly binds and inhibits cholinesterase
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What is the clinical use of edrophonium (tensilon)?
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diagnosis of myasthenia gravis, differential diagnosis of myasthenic crisis and cholinergic crisis
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What are special considerations of edrophonium (tensilon)?
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very short-acting after intravenous admin
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What are adverse effects of edrophonium (tensilon)?
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muscarinic effects (miosis, salivation)
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What are interactions of edrophonium (tensilon)?
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none significant
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What is the duration of action of edrophonium (tensilon)?
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10 minutes
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What is teh route of admin of edrophonium (tensilon)?
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IV
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What is the pharmacologic class of neostigmine?
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cholinesterase inhibitor (carbamate)
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What is the MOA of neostigmine?
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reversibly binds and inhibits cholinesterase
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What is the duration of action of neostigmine?
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2-4 hours
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What is the route of admin of neostigmine?
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oral, sub Q, IM
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What is the clinical use of neostigmine?
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myasthenia gravis, postoperative urinary retention, and postop abdominal distention
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What is the pharmacologic class of physostigmine?
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cholinesterase inhibitor
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What is the duration of action of physostigmine?
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1-5 hours
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How is physostigmine admin?
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IV, topical ocular, and IM
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What is the clinical use of physostigmine?
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antidote for curariform drug toxicity, glaucoma, reversal of CNS effects of antimuscarinic drugs such as atropine
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What is the MOA of physostigmine?
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reversibly inhibits cholinesterase
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What is the therapeutic class of pyridostigmine (mestinon)?
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antimyasthenic
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What is the pharmacologic class of pyridostigmine (mestinon)?
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cholinesterase inhibitor, cholinergic agonist
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What is the MOA of pyridostigmine (mestinon)?
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reversibly inhibits cholinesterase
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What is the clinical use of pyridostigmine (mestinon)?
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treatment of myasthenia gravis, reversal of nondepolarizing neuromuscular blockers (curariform drugs)
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What are special considerations of pyridostigmine (mestinon)?
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muscarinic effects blocked by atropine
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What are adverse effects of pyridostigmine (mestinon)?
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muscarinic effects (miosis, salavation)
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What are interactions of pyridostigmine (mestinon)?
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prolongs effects of succinylcholine, effects reduced by atropine, antidepressants, phenothiazine drugs, quinidine, and other drugs w/ anticholinergic effects
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What is the duration of action of pyridostigmine (mestinon)?
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3-6 hours
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What is the rougteof admin for pyridostigmine (mestinon)?
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oral, IM, IV
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What is the pharmacologic class of echothiophate (phospholine)?
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indirect-acting cholinergic receptor agonist (organophosphate)
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What is the MOA of echothiophate (phospholine)?
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irreversibly inhibits cholinesterase
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What is the duration of action of echothiophate (phospholine)?
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1 week or more
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What is the route of admin of echothiophate (phospholine)?
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topical ocular
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What is the clinical use of echothiophate (phospholine)?
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glaucoma and accommodative esotropia
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What are adverse effects of organophosphates?
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salivation, lacrimation, miosis, accommodative spasm, bronchoconstriction, bradycardia, intestinal cramps, and urinary incontinence
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What is the pharmacologic class of isoflurophate (floropryl)?
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indirect-acting cholinergic receptor agonist (organophosphate)
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What is the duration of action of isoflurophate (floropryl)?
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1 week or more
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What is the route of admin of isofluorphate (floropryl)?
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topical ocular
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What is the clinical use of isoflurophate (floropryl)?
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glaucoma and accommodative esotropia
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What is the MOA of isoflurophate (floropryl)?
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irreversibly inhibits cholinesterase
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What is the pharmacologic class of malathion (ovide)?
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indirect-acting cholinergic receptor agonist (organophosphate)
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What is the MOA of malathion (ovide)?
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irreversibly inhibits cholinesterase
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What is the duration of action of malathion (ovide)?
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1 week or more
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What is the route of admin of malathion (ovide)?
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topical
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What is the clinical use of malathion (ovide)?
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pediculosis (lice)
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What is the therapeutic class of sildenafil (viagra)?
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vasodilator
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What is the pharmacologic class of sildenafil (viagra)?
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phosphodiesterase inhibitor
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What is the MOA of sildenafil (viagra)?
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inhibits type 5 phosphodiesterase and degredation of cyclic guanosine monophosphate, therby inc vasodilation in corpus cavernosum evoked by acetylcholine released from sacral parasymp neurons
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What is the clinical use of sildenafil (viagra)?
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tx of erectile dysfunction
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What are special considerations of sildenafil (viagra)?
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concurrent use w/ organic nitrates can cause reflex tachycardia, angina, and death from myocardial ischemia
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What are adverse effects of sildenafil (viagra)?
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headache, nasal congestion, back pain, visual disturbances
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What are interactions of sildenafil (viagra)?
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ptotentiates vasodilation produced by organic nitrates, serum levels inc by CYP3A4 inhibitors
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What is the oral bioavailability of sildenafil (viagra)?
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40%
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What is the duration of action of sildenafil (viagra)?
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4-6 hours
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What is the pharmocologic class of tadalafil (cialis)?
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phosphodiesterase inhibitor
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What is the duration of action of tadalafil (cialis)?
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36 hours
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Which of the phosphodiesterase inhibitors' absorption is reduced with a high fat meal?
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sildenafil (viagra)
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What is the pharmacologic class of vardenafil (levitra)?
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phosphodiesterase inhibitor
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What is the duration of action of vardenafil (levitra)?
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4-6 hours
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What is the therapeutic class of atropine?
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anticholinergic agent
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What is the pharmacologic class of atropine?
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muscarinic receptor antagonist (belladonna alkaloid)
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What is the MOA of atropine?
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competitively blocks all muscarinic receptors
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What is the clinical use of atropine?
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bradycardia and AV block, irritable bowel symptoms, anticholinesterase poisoning, antisecretory agent
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What are special considerations of atropine?
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can slow heart rate when first admin
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What are adverse effects of atropine?
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tachycardia, mydriasis and cycloplegia, warm/dry/flushed skin, delirium and hallucinations
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What are interactions of atropine?
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additive anticholinergic effects w/ antihistamines and tricyclic antidepressents, slows absorption of other drugs by delaying gastric emptying
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What is the pharmacologic class of scopolamine?
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muscarinic receptor antagonist (belladonna alkaloid)
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What is used as an adjunct in anesthesia b/c it is more sedating than atropine?
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scopolamine
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What is the pharmacologic class of hyoscyamine (levsin)?
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muscarinic receptor antagonist (belladonna alkaloid)
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What is the clinical use of hyoscyamine (levsin)?
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to treat intestinal spasms and other GI disorders
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How is hyoscyamine (levsin) admin?
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oral or sublingual
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What is the therapeutic class of dicyclomine (bentyl)?
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antispasmodic
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What is the pharmacologic class of dicyclomine (bentyl)?
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muscarineic receptor antagonist (synthetic)
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What is the MOA of dicyclomine (bentyl)?
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blocks parasymp stimulation of intrinsic nervous system and reduces GI tone and motility, directly relaxes GI smooth muscle
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What is the clinical use of dicyclomine (bentyl)?
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irritable bowel symptoms (cramping and pain)
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What are special considerations of dicyclomine (bentyl)?
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none significant
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What are adverse effects of dicyclomine (bentyl)?
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constipation, dyspepsia, dry mouth, urinary retention, blurred vision, dec sweating
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What are interactions of dicyclomine (bentyl)?
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additive anticholinergic effects w/ antihistamines and other drugs
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What is the pharmacologic class of glycopyrrolate?
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muscarinic receptor antagonist (
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What is the clinical use of glycopyrrolate?
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used preop to inhibit excessive salivary and respiratory tract secretions, used during surgery to inhibit secretory and vagal effects of cholinesterase inhibitors
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What is the therapeutic class of ipratropium (atrovent)?
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bronchodilator
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What is the pharmacologic class of ipratropium (atrovent)?
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muscarinic receptor antagonist
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What is the MOA of ipratropium (atrovent)?
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blocks muscarinic receptors in bronchial smooth muscle and nasal mucosa, prevents vagal-stimulated bronchoconstriction
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What is the clinical use of ipratropium (atrovent)?
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COPD, rhinitis, asthma
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What are special considerations of ipratropium (atrovent)?
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admin by inhalation, tiotropium given once daily
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What are adverse effects of ipratropium (atrovent)?
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cough, nasal dryness and irritation
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What are interactions of ipratropium (atrovent)?
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none significant
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What is the pharmacologic class of oxybutynin (ditropan)?
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muscarinic receptor antagonist
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What is the clinical use of oxybutynin (ditropan)?
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reduce 4 symptoms of hyperactive bladder (daytime urinary freq, nocturia, urgency, and incontinence)
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What is the pharmacologic class of solifenacin (vesicare)?
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muscarinic receptor antagonist
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What is the clinical use of solifenacin (vesicare)?
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reduce 4 symptoms of hyperactive bladder
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What is the pharmacologic class of tolterodine (detrol)?
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muscarinic receptor antagonist
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What is the clinical use of tolterodine (detrol)?
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to reduce the 4 symptoms of hyperactive bladder
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What is the pharmacologic class of tropicamide (mydriacyl)?
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muscarinic receptor antagonist
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What is the clinical use of tropicamide (mydriacyl)?
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mydriasis to facilitate exam of teh peripheral retina
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What is the duration of action of tropicamide (mydriacyl)?
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about 1 hour
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What is the pharmacologic class of trimethaphan?
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nicotinic receptor antagonist (ganglionic blocking agent)
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What is the effect of trimethaphan?
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hypotension at symp blockade and dry mouth, blurred vision, and urinary retention at parasymp blockade
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What is the clinical use of trimethaphan?
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hypertensive emergencies
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What is the pharmacologic class of mivacurium?
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nicotinic receptor antagonist (nondepolarizing neuromuscular blocking agent)
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What is the duration of action of mivacurium?
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10-20 minutes
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What is the clinical use of mivacurium?
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induce muscle relaxation during surgery and intubation
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What is the pharmacologic class of pancuronium?
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nondepolarizing neruomuscular blocking nicotinic receptor antagonist
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What is the duration of action of pancuronium?
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120-180 minutes
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What is the pharmacologic class of tubocurarine?
|
nondepolarizing neuromuscular blocking nicotinic receptor antagonist
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What is the duration of action of tubocurarine?
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60-120 minutes
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What is the pharmacologic class of succinylcholine (anectine)?
|
depolarizing neuromuscular blocking nicotinic receptor antagonist
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What is the therapeutic class of succinylcholine (anectine)?
|
paralytic agent
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What is the MOA of succinylcholine (anectine)?
|
binds to nicotinic receptors causing prolonged depolarization of skeletal muscle and paralysis
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What is the clinical use of succinylcholine (anectine)?
|
short-term (DOA of 5-10 minutes) skeletal muscle relaxation for intubation and surgery
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What are special considerations of succinylcholine (anectine)?
|
causes transient muscle fasciculations, effects are not reversed by neostigmine or edrophonium
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What are adverse effects of succinylcholine (anectine)?
|
repiratory muscle paralysis and apnea, especially in persons w/ rare atypical cholinesterase, hyperkalemia sufficient to cause cardiac arrest in persons w/ unhealed skeletal muscle injury
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What are interactions of succinylcholine (anectine)?
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neuromuscular blockade enhanced by aminoglycoside antibiotics, clindamycin, amohtericin B, quinidine, and cholinesterase inhibitors
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What is the thearpeutic class of dobutamine (dobutrex)?
|
sympathomimetic, cardiac stimulant
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What is the pharmacologic class of dobutamine (dobutrex)?
|
selective B1 adrenergic receptor agonist (catecholamine)
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What is the MOA of dobutamine (dobutrex)?
|
activates B1 more than B2 and much more than A1 receptors, inc cardiac contractility and cardiac output > HR
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What is the clinical use of dobutamine (dobutrex)?
|
acute HF and cardiogenic shock
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What are special considerations of dobutamine (dobutrex)?
|
admin by intravenous infusino, should correct hypovolemia before initiating therapy
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What are adverse effects of dobutamine (dobutrex)?
|
tachycardia and arrhythmia
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What are interactions of dobutamine (dobutrex)?
|
synergistic effect on CO w/ nitroprusside
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What is the pharmacologic class of dopamine?
|
direct-acting adrenergic receptor agonist (catecholamine)
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What are the effects of dopamine?
|
renal vasodilation, cardiac stimulation, and inc BP
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What are the clinical uses of dopamine?
|
cardiogenic shock, septic shock, HF, and adjunct to fluid admin in hypovolemic shock
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What is the therapeutic class of epinephrine (adrenalin)?
|
sympathomimetic, bronchodilator, vasopresor
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What is the pharmacologic class of epinephrine (adrenalin)?
|
nonselective adrenergic agonist (catecholamine)
|
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What is the MOA of epinephrine (adrenalin)?
|
activates A and B receptors, inc inositol triphosphate and cyclic adenosine monophosphate
A1: vasoconstriction and inc BP B1: inc HR, conduction and contractility B2: vasodilation and dec DBP, bronchodilation |
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What is the clinical use of epinephrine (adrenalin)?
|
cardiac arrest, v-fib, anaphylactic shock, asthma, COPD
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What are adverse effects of epinephrine (adrenalin)?
|
HTN, tachycardia, ischemia, hyperglycemia
|
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What are interactions of epinephrine (adrenalin)?
|
none significant
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What is the pharmacologic class of isoproterenol?
|
direct-acting adrenergic receptor agonist (catecholamine)
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What are the effects of isoproterenol?
|
cardiac stimulation and bronchodilation
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What is the clinical use of isoproterenol?
|
asthma, refractory AV block, and refractory bradycardia
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What is the pharmacologic class of norepinephrine?
|
direct-acting adrenergic receptor agonist (catecholamine)
|
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What is the effect of norepinephrine?
|
vasoconstriction and inc BP
|
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What is the clinical use of norepinephrine?
|
hypotension and shock
|
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What is the therapeutic class of albuterol (proventil, ventolin)?
|
bronchodilator
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What is the pharmacologic class of albuterol (proventil, ventolin)?
|
adrenergic B2 receptor agonist (noncatecholamine)
|
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What is the MOA of albuterol (proventil, ventolin)?
|
activates B2 receptors in bronchial smooth muscle, in cyclic adenosine monophosphate, activating kinases, inhibitin myosin phosphorylation, and causing muscle relaxation
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What is the clinical use of albuterol (proventil, ventolin)?
|
asthma, acute bronchospasm, preventionof exercise-induced asthma, chronic bronchitis and emphysema: reversible airway obstruction
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What are special considerations of albuterol (proventil, ventolin)?
|
rapid onset after inhalationn, slower onset after oral admin
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What are adverse effects of albuterol (proventil, ventolin)?
|
tachycardia, muscle tremor, nervousness, restlessness
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What are interactions of albuterol (proventil, ventolin)?
|
use w/ monoamine oxidase inhibitors can cause HTN crisis, additive effects w/ other adrenergic agents and CNS stimulants
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What is the pharmacologic class of apraclonidine?
|
direct-acting adrenergic receptor agonist (noncatecholamine)
|
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What is the effect of apraclonidine?
|
dec aqueous humor formation
|
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What is the clinical use of apraclonidine?
|
chronic HTN
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What is the therapeutic class of clonidine (catapres)?
|
antihypertensive drug
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What is the pharmacologic class of clonidine (catapres)?
|
adrenergic A2 receptor agonist
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What is the MOA of clonidine (catapres)?
|
activates central A2 receptors, dec symp outflow from vasomotor center, inhibits pain neurotransmission in spinal cord
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What is the clinical use of clonidine (catapres)?
|
HTN, cancer pain unresponsive to opioids, opioid withdrawal
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What are special considerations of clonidine (catapres)?
|
7-day transdermal system available, abrupt w/drawal may cause severe rebound HTN
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What are adverse effects of clonidine (catapres)?
|
sedation and dry mouth
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What are interactions of clonidine (catapres)?
|
additive sedation w/ CNS depressants, additive hypotension w/ nitrates and antiHTn drugs, antiHTN effect dec by tricyclic antidepressants and adrenergic receptor antagonists
|
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What is the pharmacologic class of midodrine (proamatine)?
|
direct-acting adrenergic receptor agonist (noncatecholamine)
|
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What is the effect of midodrine (proamatine)?
|
vasoconstriction
|
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What is the clinical use of midodrine (proamatine)?
|
orthostatic hypotension
|
|
|
What is the pharmacologic class of oxymetazoline?
|
direct-acting adrenergic receptor agonist (noncatecholamine)
|
|
|
What is the effect of oxymetazoline?
|
vasoconstriction
|
|
|
What is the clinical use of oxymetazoline?
|
nasal and ocular decongestion
|
|
|
What is the therapeutic class of phenylephrine (neo-synephrine)?
|
vasoconstrictor and decongestant
|
|
|
What is the pharmacologic class of phenylephrine (neo-synephrine)?
|
selective adrenergic A1 receptor agonist (noncatecholamine)
|
|
|
What is the MOA of phenylephrine (neo-synephrine)?
|
activates A1 receptors, inc inositol triphosphate and causing contraction of vascular smooth muscle
|
|
|
What is the clinical use of phenylephrine (neo-synephrine)?
|
nasal and ocular decongestant, tx of drug-induced hypotension and spinal shock, dilation of pupil for opthalmoscopy
|
|
|
What are special considerations for phenylephrine (neo-synephrine)?
|
occular admin causes mydriasis w/out cycolplegia
|
|
|
What are adverse effects of phenylephrine (neo-synephrine)?
|
rebound nasal congestion, HTN
|
|
|
What are interactions of phenylephrine (neo-synephrine)?
|
may cuase HTN if given w/ monoamine oxidase inhibitors, vasopressor effect inc by tricyclic antidepressants
|
|
|
What is the pharmacologic class of ritodrine?
|
direct-acting adrenergic receptor agonist (noncatecholamine)
|
|
|
What is the effect of ritodrine?
|
bronchodilation and uterine relaxation
|
|
|
What is the clinical use of ritodrine?
|
asthma and premature labor
|
|
|
What is the pharmacologic class of terbutaline (brethine)?
|
direct-acting adrenergic receptor agonist (noncatecholamine)?
|
|
|
What is the effect of terbutaline (brethine)?
|
bronchodilation and uterine relaxation
|
|
|
What is the clinical use of terbutaline (brethine)?
|
asthma and premature labor
|
|
|
What is the therapeutic class of amphetamine (aderall)?
|
CNS stimulants
|
|
|
What is the pharmacologic class of amphetamine (aderall)?
|
sympathomimetic amines (indirect-acting adrenergic receptor agonist)
|
|
|
What is the MOA of amphetamine (aderall)?
|
inc neuronal release of NE
|
|
|
What is the clinical use of amphetamine (aderall)?
|
ADHD, narcolepsy
|
|
|
What are special considerations for amphetamine (aderall)?
|
in ADHD: inc attention span, dec motor restlessness, in narcolepsy: inc mental alertness, dec drowsiness and fatigue, schedule II controlled drug
|
|
|
What are adverse effects of amphetamine (aderall)?
|
tachycardia, HTN, anorexia, irritabiliyt, insomnia, tremor, growth inhibition, drug dependence
|
|
|
What are interactions of amphetamine (aderall)?
|
HTN crisi w/ monoamine oxidase inhibitors, HTN and bradycardia w/ B-blockers, inc or dec excretion w/ drugs that acidify or alkalinize urine
|
|
|
What is the pharmacologic class of cocaine?
|
indirect-acting adrenergic receptor agonist
|
|
|
What is the effect of cocaine?
|
inhibition of NE uptake, vasoconstriction
|
|
|
What is the clinical use of cocaine?
|
local anesthesia
|
|
|
What is the pharmacologic class of ephedrine?
|
mixed-acting adrenergic receptor agonists
|
|
|
What is the effect of ephedrine?
|
vasoconstriction
|
|
|
What is the clinical use of ephedrine?
|
nasal decongestion in viral and allergic rhinitis
|
|
|
What is the therapeutic class of pseudoephedrine (sudafed)?
|
decongestant
|
|
|
What is the pharmacologic class of pseudoephedrine (sudafed)?
|
indirect and direct acting adrenergic receptor agonist
|
|
|
What is the MOA of pseudoephedrine (sudafed)?
|
inc release of NE and directly activates adrenergic receptors causing vasocostriction and cardiac stimulation
|
|
|
What is the clinical use of pseudoephedrine (sudafed)?
|
nasal decongestant for allergic and viral rhinitis
|
|
|
What are special considerations of pseudoephedrine (sudafed)?
|
urine acidification or alkalinization may inc or dec excretion, respectively
|
|
|
What are adverse effects of pseudoephedrine (sudafed)?
|
tachycardia, inc BP, CNS stimulation
|
|
|
What are interactions of pseudoephedrine (sudafed)?
|
concurrent use w/ monamine oxidase inhibitors may cause sever HTN
|
|
|
What is the therapeutic class of phenoxybenzamine (dibenzyline)?
|
vasodilator
|
|
|
What is the pharmacologic class of phenoxybenzamine (dibenzyline)?
|
irreversible adrenergic A receptor antagonist
|
|
|
What is the MOA of phenoxybenzamine (dibenzyline)?
|
blocks A1 > A2 receptors
|
|
|
What is the clinical use of phenoxybenzamine (dibenzyline)?
|
presurgical tx of HTn caused by pheochromocytoma
|
|
|
What are special considerations of phenoxybenzamine (dibenzyline)?
|
forms covalent bond w/ A receptor, effects last several days
|
|
|
What are adverse effects of phenoxybenzamine (dibenzyline)?
|
postural hypotension
|
|
|
What are interactions of phenoxybenzamine (dibenzyline)?
|
hypotensive effect in by b-adrenergic blockers and CCB
|
|
|
What is the therapeutic class of phentolamine (regitine)?
|
vasodilator
|
|
|
What is the pharmacologic class of phentolamine (regitine)?
|
adrenergic A receptor antagonist
|
|
|
What is the MOA of phentolamine (regitine)?
|
competitively blocks A1 and A2 receptors
|
|
|
What is the clinical use of phentolamine (regitine)?
|
counteract vasoconstriction caused by accidental injection or extravasation of vasoconstrictors, control BP during surgical removal of a pheochromocytoma
|
|
|
What are special considerations of phentolamine (regitine)?
|
parenteral admin only
|
|
|
What are adverse effects of phentolamine (regitine)?
|
hypotension
|
|
|
What are interactions of phentolamine (regitine)?
|
severe hypotension if given w/ epi, blocks effects of A-adrenergic agonists
|
|
|
What is the pharmacologic class of doxazosin (cardura)?
|
selective (competitive) A1 blocker
|
|
|
What is the effect of doxazosin (cardura)?
|
vasodilation, dec vascular resistance and BP, and relax bladder neck and prostate
|
|
|
What is the clinical use of doxazosin (cardura)?
|
HTN, urinary retention due to BPH
|
|
|
What is the therapeutic class of tamsulosin (flomax)?
|
urologic agent
|
|
|
What is the pharmacologic class of tamsulosin (flomax)?
|
uroselective adrenergic A1-receptor antagonist
|
|
|
What is the MOA of tamsulosin (flomax)?
|
competitively blocks A1a receptors in prostate
|
|
|
What is the clinical use of tamsulosin (flomax)?
|
tx of urinary outflow obstruction in men w/ prostatic hyperplasia
|
|
|
What are special considerations of tamsulosin (flomax)?
|
not indicated for tx of HTN
|
|
|
What are adverse effects of tamsulosin (flomax)?
|
dizziness, headache, postural hypotension
|
|
|
What are interactions of tamsulosin (flomax)?
|
cimetidine may inc blood levels and effects
|
|
|
What is the pharmacologic class of alfuzosin (uroxatral)?
|
selective A1 blocker
|
|
|
What is the effect of alfuzosin (uroxatral)?
|
relax bladder neck and prostate
|
|
|
What is the clinical use of alfuzosin (uroxatral)?
|
urinary retention due to BPH
|
|
|
What is the therapeutic class of propranolol (inderal)?
|
sympatholytic, antiHTN
|
|
|
What is the pharmacologic class of propranolol (inderal)?
|
nonselective adrenergic B receptor antagonist
|
|
|
What is the MOA of propranolol (inderal)?
|
competitively blocks B1 and B2 receptors
|
|
|
What is the clinical use of propranolol (inderal)?
|
angina, HTN, post-MI, cardiomyopathy, benign tremor, migraine prophylaxis, thyrotoxicosis
|
|
|
What are special considerations for propranolol (inderal)?
|
highly lipophilic (CNS effects), has local anesthetic activity
|
|
|
What are adverse effects of propranolol (inderal)?
|
bronchoconstriction, inhibits glycogenolysis, nightmares and mood depression
|
|
|
What are interactions of propranolol (interal)?
|
additive hypotensive effect w/ nitrates and antiHTN drugs, additive bradycardia w/ digoxin, dec effects of dopamine and dobutamine, unopposed A-adrenergic receptor stimulation w/ epi and related drugs
|
|
|
What pharmacologic class is timolol (timoptic)?
|
nonselective b-blocker
|
|
|
What is the effect of timolol (timoptic)?
|
dec cardiac rate, otuput, AV node conduction, and O2 demand, dec BP, dec intraocular pressure
|
|
|
What is the clinical use of timolol (timoptic)?
|
HTN, AMI, migraine headache, glaucoma
|
|
|
What is the pharmacologic class of pindolol?
|
nonselective b-blocker
|
|
|
What is the effect of pindolol?
|
dec cardiac rate, output, AV node conduction, and O2 demand, dec BP
|
|
|
What is the clinical use of pindolol?
|
HTN
|
|
|
What is the pharmacologic class of atenolol (tenormin)?
|
selective adrenergic B1 receptor antagonist
|
|
|
What is the therapeutic class of atenolol (tenormin)?
|
sympatholytic, antiHTN
|
|
|
What is the MOA of atenolol (tenormin)?
|
competitively blocks B1 receptors
|
|
|
What is the clinical use of atenolol (tenormin)?
|
angina, HTn, post-MI cardioprotection
|
|
|
What are special considerations of atenolol (tenormin)?
|
less lipophilic, fewer CNS side effects, lacks local anesthetic or partial agonist activity
|
|
|
What are adverse effects of atenolol (tenormin)?
|
bronchoconstriction w/ higher doses b/c of B2 receptor blockade
|
|
|
What are interactions of atenolol (tenormin)?
|
additive hypotensive effect w/ nitrates and antiHTN drugs, additive bradycardia w/ digoxin, dec effects of dopamine and dobutamine, unopposed A-adrenergic receptor stimulation w/ epi and related drugs
|
|
|
What is the pharmacologic class of metoprolol (lopressor)?
|
selective B1 blocker
|
|
|
What are the effects of metoprolol?
|
dec cardiac rate, O2 demand, AV node conduction, otuput, and BP
|
|
|
What is the clinical use of metoprolol?
|
HTN, angina pectoris, AMI
|
|
|
What is the therapeutic class of carvedilol (coreg)?
|
antiHTN and HF tx
|
|
|
What is the pharmacologic class of carvedilol (coreg)?
|
non-selective adrenergic receptor antagonist
|
|
|
What is the MOA of carvedilol (coreg)?
|
blocks B1, B2, and A1 receptors, exerts antioxidant and antiapoptotic effects, causes vasodilation
|
|
|
What is the clinical use of carvedilol (coreg)?
|
HF, dec cardiac remodeling, disease progression, and mortality while improving symptoms, tx of HTN
|
|
|
What are special considerations of carvedilol (coreg)?
|
begin w/ low doses in HF and gradually inc
|
|
|
What are adverse effects of carvedilol (coreg)?
|
orthostatic hypotension, dizziness, fatigue, bradycardia, worsening of HF if dose too high
|
|
|
What are interactions of carvedilol (coreg)?
|
effects inc by antiHTN drugs, digoxin, monoamine oxidase inhibitors, effects dec by rifampin, thyroid hormones, NSAIDs, dec cardiovascular effects of dopamine or dobutamine
|
|
|
What is the therapeutic class of labetalol (normodyne, trandate)?
|
antiHTN
|
|
|
What is the pharmacologic class of labetalol (normodyne, trandate)?
|
adrenergic A and B receptor antagonist
|
|
|
What is the MOA of labetalol (normodyne, trandate)?
|
selective A1 and nonselective B1 and B2 blocker
|
|
|
What is the clinical use of labetalol (normodyne, trandate)?
|
HTN
|
|
|
What are special considerations of labetalol (normodyne, trandate)?
|
abrupt w/drawal may cause life-threatening HTN, arrhythmias, myocardial ischemia
|
|
|
What are adverse effects of labetalol (normodyne, trandate)?
|
postural hypotension
|
|
|
What are interactions of labetalol (normodyne, trandate)?
|
additive hypotensive effect w/ nitrates and antiHTN drugs, additive bradycardia w/ digoxin, dec effects of dopamine and dobutamine, unopposed A-adrenergic receptor stimulation w/ epi and related drugs
|
|
|
What is the therapeutic class of hydrochlorothiazide (HydroDiuril)?
|
antiHTN agent
|
|
|
What is the pharmacologic class of HCTZ (hydrodiuril)?
|
thiazide diuretic
|
|
|
What is the MOA of HCTZ (hydrodiuril)?
|
inhibits NaCl transporter in distal tubule, inc excretion of Na, K, Cl, dec Ca excretion
|
|
|
What is the clinical use of HCTZ (hydrodiuril)?
|
HTN, nephrogenic diabetes insipidus, nephrolithiasis
|
|
|
What are special considerations for HCTZ (hydrodiuril)?
|
prevents cardiovascular complications of HTN, including stroke and CAD
|
|
|
What are adverse effects of HCTZ (hydrodiuril)?
|
hypokalemia, metabolic alkalosis, hyperuricemia and gout, inc insulin requirement
|
|
|
What are interactions of HCTZ (hydrodiuril)?
|
dec excretion of Li, additive hypotension w/ anti HTN drugs and nitrates, additive hypokalemia w/ corticosteroids, amphotericin B, and loop diuretics
|
|
|
What is the therapeutic class of amiloride (midamor)?
|
K-sparing diuretic
|
|
|
What is the pharmacologic class of amiloride (midamor)?
|
epithelial Na channel blocker
|
|
|
What is the MOA of amiloride (midamor)?
|
blocks Na channels in distal tubule and collecting duct, inhibits Na reabsorption and K excretion
|
|
|
What is the clinical use of amiloride (midamor)?
|
prevention and tx of hypokalemia
|
|
|
What are special considerations of amiloride (midamor)?
|
often combined w/ thiazide or loop-acting diuretic
|
|
|
What are adverse effects of amiloride (midamor)?
|
hyperkalemia
|
|
|
What are interactions of amiloride (midamor)?
|
additive effects on K w/ ACE-I, ARBs, and K supplements
|
|
|
What is the therapeutic class of enalapril (vasotec)?
|
antiHTN agent
|
|
|
What is the pharmacologic class of enalapril (vasotec)?
|
ACE-I
|
|
|
What is the MOA of enalapril (vasotec)?
|
inhibits ACE and formation of angiotensin II, causes vasodilation, dec aldosterone secretion, inc CO, slows ventricular remodeling, and inc survival of HF
|
|
|
What is the clinical use of enalapril (vasotec)?
|
HTn, HF, post-MI, dec progression of diabetic nephropathy
|
|
|
What are special considerations of enalapril (vasotec)?
|
inhibits bradykinin degradation, causing cough and angioedema
|
|
|
What are adverse effects of enalapril (vasotec)?
|
hypotension, taste disturbances, dry cough
|
|
|
What are interactions of enalapril (vasotec)?
|
hyperkalemia if used w/ K-sparing diuretics and K supplements
|
|
|
What is the pharmacologic class of losartan (cozaar)?
|
angiotensin receptor antagonist
|
|
|
What is a common adverse effect of losartan (cozaar)?
|
hyperkalemia
|
|
|
What are common interactions of losartan (cozaar)?
|
serum levels of drug inc by cimetidine and dec by phenobarbital
|
|
|
What is the oral bioavailability of losartan (cozaar)?
|
33%
|
|
|
What is the therapeutic class of amlodipine (norvasc)?
|
antiHTN and antianginal agent
|
|
|
What is the pharmacologic class of amlodipine (norvasc)?
|
dihydropyridine CCB
|
|
|
What is the MOA of amlodipine (norvasc)?
|
blocks Ca channels in vascular smooth muscle, causing arteriolar vasodilattion and inc coronary blood flow
|
|
|
What is the clinical use of amlodipine (norvasc)?
|
HTN, angina pectoris
|
|
|
What are special considerations of amlodipine (norvasc)?
|
long half-life (30-50 hours)
|
|
|
What are adverse effects of amlodipine (norvasc)?
|
headache, edema, hypotension
|
|
|
What are interactions of amlodipine (norvasc)?
|
levels and effects inc by concurrent ingestion of grapefruit juice
|
|
|
What is the therapeutic class of hydralazine (apresoline)?
|
antiHTN, HF
|
|
|
What is the pharmacologic class of hydralazine (apresoline)?
|
vasodilator
|
|
|
What is the MOA of hydralazine (apresoline)?
|
alters intracellular Ca metabolism, relaxes arteriolar smooth muscle, causing vasodilation, dec cardiac afterload
|
|
|
What is the clincal use of hydralazine (apresoline)?
|
moderate to severe HTN, HF in combo w/ isosorbide dinitrate
|
|
|
What are special considerations of hydralazine (apresoline)?
|
hydralazine-isosorbide dinitrate is more effective than angiotensin inhibitors in black pts
|
|
|
What are adverse effects of hydralazine (apresoline)?
|
edema, reflex tachycardia and myocardial ischemia, lupus syndrome
|
|
|
What are interactions of hydralazine (apresoline)?
|
combined w/ B-blockers and diuretic to prevent tachycardia and fluid retention
|
|
|
What is the therapeutic class of fenoldopam (corlopam)?
|
antiHTN
|
|
|
What is the pharmacologic class of fenoldopam (corlopam)?
|
agonist at dopamine d1-like receptors
|
|
|
What is the MOA of fenoldopam (corlopam)?
|
causes arteriolar vasodilation, including afferent and efferent renal arterioles, inc renal blood flow
|
|
|
What is the clinical use of fenoldopam (corlopam)?
|
HTN emergencies
|
|
|
What are special considerations for fenoldopam (corlopam)?
|
rapid acting, short half-life of about 5min
|
|
|
What are adverse effects of fenoldopam (corlopam)?
|
can reduce serum K levels, which should be monitored
|
|
|
What are interactions with fenoldopam (corlopam)?
|
concurrent use w/ adrenergic B blockers may cause excessive hypotension and should be avoided
|
|
|
What is the pharmacologic class of indapamide (lozol)?
|
thiazide diuretic
|
|
|
What are adverse effects of indapamide (lozol)?
|
electrolyte imbalances and inc blood chol, glucose, or uric acid levels
|
|
|
What are interactions of indapamide (lozol)?
|
potentiates diuretic effects of loop diuretics
|
|
|
What is the oral bioavailability of indapamide (lozol)?
|
90%
|
|
|
What is the pharmacologic class of metolazone?
|
thiazide diuretic
|
|
|
What is the oral bioavailability of metolazone?
|
65%
|
|
|
What are adverse effects of metolazone?
|
blood cell deficiencies, electrolyte imbalances, inc blood chol and glucose levels
|
|
|
What are interactions of metolazone?
|
potentiates diuretic effect of loop diuretics
|
|
|
What is the pharmacologic class of bumetanide (bumex)?
|
loop diuretics
|
|
|
What is the oral bioavailability of bumetanide (bumex)?
|
85%
|
|
|
What are adverse effects of bumetanide (bumex)?
|
blood cell deficiencies, electrolyte imbalances, hearing impairment, and hypersensitivity reactions
|
|
|
What are interactions of bumetanide (bumex)?
|
diuretic effect dec by NSAIDs, admin with ACE-I may cause excessive hypotension
|
|
|
What is the pharmacologic class of ethacrynic acid?
|
loop diuretics
|
|
|
What is the oral bioavailability of ethacrynic acid?
|
100%
|
|
|
What are adverse effects of ethacrynic acid?
|
blood cell deficiencies, electrolyte imbalances, hearing impairment and rash
|
|
|
What are interactions of ethacrynic acid?
|
diuretic effect dec by NSAIDs
|
|
|
What is the therapeutic class of furosemide (lasix)?
|
loop-acting (high-ceiling) diuretic
|
|
|
What is the pharmacologic class of furosemide (lasix)?
|
membrane ion transport inhibitor
|
|
|
What is the MOA of furosemide (lasix)?
|
inhibits Na/K/2Cl cotransporter in ascending limb of loop of Henle, blocks NaCl reabsorption
|
|
|
What is the clinical use of furosemide (lasix)?
|
edema, HF, HTN, hypercalcemia
|
|
|
What are special considerations of furosemdie (lasix)?
|
inc Na/K exchange in collecting duct, leading to hypokalemia, inc Ca excretion
|
|
|
What are adverse effects of furosemide (lasix)?
|
hypokalemia, metabolic alkalosis, hyperuricemia, hypomagnesemia
|
|
|
What are interactions of furosemide (lasix)?
|
additive hypotension w/ antiHTN drugs and nitrates, additive hypokalemia w/ corticosteroids, amphotericin B, and thiazide diuretics, dec Li excretion, inc ototoxicity of aminoglycoside antibiotics
|
|
|
What is the therapeutic class of spironolactone (aldactone)?
|
K-sparing diuretic
|
|
|
What is the pharmacologic class of spironolactone (aldactone)?
|
aldosterone antagonist
|
|
|
What is the MOA of spironolactone (aldactone)?
|
blocks aldosterone receptors, inc Na excretion and dec K excretion
|
|
|
What are clinical uses of spironolactone (aldactone)?
|
primary hyperaldosteronism, hypokalemia, HF, HTN
|
|
|
What are special considerations of spironolactone (aldactone)?
|
eplerenone causes fewer anti-androgenic effects such as gynecomastia
|
|
|
What are adverse effets of spironolactone (aldactone)?
|
gynecomastia and impotence, hyperkalemia
|
|
|
What are interactions of spironolactone (aldactone)?
|
hyperkalemia if combined w/ angiotensin inhibitor and K supplements
|
|
|
What is the pharmacologic class of glycerol?
|
osmotic diuretics
|
|
|
What is the oral bioavailabiltiy of glycerol?
|
95%
|
|
|
What are adverse effects of glycerol?
|
HF, N/V, pulm congestion, and edema
|
|
|
What are interactions of glycerol?
|
potentiates effects of other diuretics
|
|
|
What pharmacologic class is triamterene (dyrenium)?
|
K-sparing diuretic
|
|
|
What is the oral bioavailability of triamterene (dyrenium)?
|
50%
|
|
|
What are adverse effects of triamterene (dyrenium)?
|
blood cell deficiencies, GI distress, hyperkalemia
|
|
|
What are interactions of triamterene (dyrenium)?
|
admin w/ ACE-I or K supplements may cause hyperkalemia, admin w/ NSAIDs may cause renal failure
|
|
|
What is the therapeutic class of mannitol (osmitrol)?
|
diuretic
|
|
|
What is the pharmacologic class of mannitol (osmitrol)?
|
osmotic agent
|
|
|
What is the MOA of mannitol (osmitrol)?
|
osmotic attraction of edematous and ocular fluid, filtered at glomerulus but not reabsorbed, inc electrolyte excretion
|
|
|
What is the clinical use of mannitol (osmitrol)?
|
oliguric renal failure, inc intracranial pressure, acute glaucoma, toxic overdose
|
|
|
What are special considerations for mannitol (osmitrol)?
|
transient volume expansion after IV admin
|
|
|
What are adverse effects of mannitol (osmitrol)?
|
transient volume expansion, occasionally leading to pulmonary edema or HF, serum electrolyte imbalances
|
|
|
What are interactions of mannitol (osmitrol)?
|
none significant
|
|
|
What is the therapeutic class of acetazolamide (diamox)?
|
diuretic
|
|
|
What is the pharmacologic class of acetazolamide (diamox)?
|
carbonic anhydrase inhibitor (CAI)
|
|
|
What is the MOA of acetazolamide (diamox)?
|
inhibits interconversion of carbonic acid and bicarb, inc renal NaHCO3 excretion, inhibits aqueous humor formation, causes metabolic acidosis (hyperchloremic)
|
|
|
What is the clinical use of acetazolamide (diamox)?
|
tx of open-angle glaucoma, mountain sickness, metabolic alkalosis, alkalinization of urine
|
|
|
What are special considerations of acetazolamide (diamox)?
|
tolerance to diuretic effect develops rapidly
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What are adverse effects of acetazolamide (diamox)?
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paresthesia, urinary calculus formation
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What are interactions of acetazolamides (diamox)?
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dec urinary excretion of weak bases
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What is the pharmacologic class of dorzolamide (trusopt)?
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carbonic anhydrase inhibitor
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What are adverse effects of dorzolamide (trusopt)?
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bitter taste, blurred vision, and ocular discomfort and allergic reactions
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What are interactions of dorzolamide (trusopt)?
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unknown
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