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120 Cards in this Set
- Front
- Back
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CYP3A is responsible for metabolism of:
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Most calcium channel blockers
Most benzodiazepines Most HIV protease inhibitors Most HMG-CoA-reductase inhibitors Cyclosporine Most non-sedating antihistamines Cisapride Present in GI tract and liver |
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CYP3A inhibitors
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Ketoconazole
Itraconazole Fluconazole Cimetidine Clarithromycin Erythromycin Troleandomycin Grapefruit juice |
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CYP3A inducers
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Carbamazepine
Rifampin Rifabutin Ritonavir St. John’s wort |
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CYP2D6 catalyzes metabolism of
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Codeine
Many -blockers Many tricyclic antidepressants |
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CYP2D6 inhibitors
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Fluoxetine
Haloperidol Paroxetine Quinidine |
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CYP2C9 metabolizes
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Most NSAIDs (including COX-2)
S-warfarin (the active form) Phenytoin |
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CYP2C9 inhibitor
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Fluconazole
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CYP2C19 metabolizes
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Diazepam
Phenytoin Omeprazole |
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CYP2C19 inhibitors
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Omeprazole
Isoniazid Ketoconazole |
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CYP1A2 induced by:
metabolizes: |
smoking tobacco
Theophylline Imipramine Propranolol Clozapine |
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CYP1A2 inhibitors
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Many fluoroquinolone antibiotics
Fluvoxamine Cimetidine |
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ventricular tachycardia, torse de pointes, is associated with:
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terfenadine
astemizole (Hismanal) cisapride (Propulsid) grepafloxacin (Raxar) mibefradil (Posicor) Ketoconazole assoc with one of these |
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Vd
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amt of drug in body/plasma drug conc
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CL
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elimination rate/plasma conc
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Half life
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0.7xVd/CL
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Loading dose
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Cp x Vd / F
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Maintenance dose
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Cp x CL / F
Cp is target conc |
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rate of elimination is constant regardless of C
constant amount of drug eliminated per unit time Cp decreases linearly with time |
zero order
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rate of elimination is proportional to the drug concentration
constant fraction of drug eliminated per unit time Cp decreases exponentially with time |
first order
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phase I metabolism
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reduction oxidation hydrolysis
yields polar water soluble metabolites cyp450 |
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phase II metabolism
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acetylation glucuronidation sulfation
yields polar inactive metabolites conjugation |
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maximal effect a drug can produce
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efficacy
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amount of drug needed for a given effect
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potency
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decreases potency
increases EC50 shifts curve right |
competitive antagonist
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decreases efficacy
shifts curve down same agonist dose |
noncompetitive antagonist
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lower maximal efficacy regardless of dose
may be more or less potent (independent factor) |
partial agonist
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LD50/ED50
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therapeutic index
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ACh ligand gated Na/K channels
always excitatory, faster |
nicotinic
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Nicotinic ACh receptor
activated by blocked by |
ACh, nicotine
tubocurarine |
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ACh receptors are G protein coupled, 2nd messengers
slower, excitatory or inhibitory |
Muscarinic
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Muscarinic ACh receptor
activated by blocked by |
ACh, muscarine
Atropine |
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a1
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Sympathetic
G protein Increases vascular smooth muscle contraction, increases pupillary dilator muscle contraction (mydriasis) |
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a2
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Sympathetic
G protein Decreases sympathetic outflow (negative feedback modulator on presynaptic, dec NE), decreases insulin release |
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b1
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Sympathetic
G protein Increases heart rate, increases contractility, increases renin, increases lipolysis |
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b2
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Sympathetic
G protein Smooth muscle relaxation, vasodilation, bronchodilation, inc HR, inc contractility, inc lipolysis, inc glucagon, dec uterine tone, relax ciliary muscles |
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M1
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parasympathetic
G protein CNS, enteric nervous system |
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M2
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parasympathetic
G protein dec HR and contractility of atria |
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M3
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parasympathetic
G protein inc exocrine gland secretions, inc gut peristalsis, inc bladder contraction (voiding), bronchoconstriction, inc pupillary sphincter muscle contraction (miosis), ciliary muscle contraction (accommodation) |
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blocks choline reuptake
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hemicholinium
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blocks VAChT
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Vesamicol
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blocks ACh exocytosis
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botulinum
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enhances ACh exocytosis
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black widow venom
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blocks tyrosine hydroxylase
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metyrosine
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blocks dopamine uptake into vesicles
for HTN, dec BV basal tone |
reserpine
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blocks NE exocytosis
for extreme HTN, but bad side effects |
guanethidine
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increases NE exocytosis
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amphetamine
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increases NE reuptake
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cocaine
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NE negative feedback receptor blocks exocytosis
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a2
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negative feedback on ACh exocytosis
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a2 and M
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positive feedback on ACh exocytosis
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N
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catecholamine metabolism
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COMT, MAO
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MAO inhibitor
COMT inhibitor effect |
Pargyline
Entacapone increase amounts of Epi/Norepi |
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cholinomimetic agents
direct indirect |
direct: bethanechol, carbachol, pilocarpine, methacholine
indirect: neostigmine, pyridostigmine, edrophonium, physostigmine, echothiophate |
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For post-op and neurogenic ileus and urinary retention
cholinomimetic direct agonist |
bethanechol
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glaucoma, pupillary contraction, release of intraocular pressure
cholinomimetic direct agonist |
carbachol
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potent stimulator of sweat, tears, saliva (xerostomia), contracts ciliary muscle of eye- opens trabeculae (open angle), pupillary sphincter (closed narrow angle), resistant to AChE
cholinomimetic direct agonist |
Pilocarpine
Pile on the sweat and tears |
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challenge test for dx of asthma
stimulates muscarinic receptors in airway cholinomimetic direct agonist |
methacholine
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postop and neurogenic ileus and urinary retention, myasthenia gravis tx, reversal of nmj blockade postop
inc ACh, no CNS cholinomimetic indirect agonist |
Neostigmine
Neo CNS = no cns |
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myasthenia gravis tx long acting, no cns
inc ACh, inc strength cholinomimetic indirect agonist |
pyridostigmine
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dx of myasthenia gravis, extremely short acting, noncovalent, reversible
inc endogenous ACh cholinomimetic indirect agonist |
Edrophonium
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glaucoma, crosses cns, atropine overdose tx
inc ACh |
Physostigmine
phys for eyes |
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glaucoma, strabismus
stable covalent irreversible bonds last days inc ACh crosses bbb cholinomimetic indirect agonist |
echothiophate
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diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal muscle and cns, lacrimation, sweating, salivation
DUMBBELSS |
cholinesterase inhibitor poisoning
(excess ACh) |
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treatment of cholinesterase inhibitor poisoning
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atropine (M antagonist) and pralidosime (antagonist used to regenerate active cholinesterase) and physostigmine (prophylactic)
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AChE inhibitors
Low level vs high level |
low: inc skeletal m activation
high: neuromuscular blockade (persistant depol phase 1) and subsequent desensitization of Nm (phase 2) |
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alzheimers tx
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AChE inhibitor
physostigmine, donepizil, rivastigmine |
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Muscarinic antagonists
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atropine, homatropine, tropicamide, benztropine, scopolamine, ipratropium, tiotropium, oxybutynin, glycopyrrolate, flavoxate, tolterodine, enablex (darifenacin), vesicare (solifenacin), methscopolamine, pirenzepine, propantheline, otenzepad
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M antagonist
produces mydriasis and cycloplegia caution: glaucoma |
atropine, homatropine, tropicamide
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M antagonist
parkinson's |
benztropine
park my benz |
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M antagonist
motion sickness |
scopolamine
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M antagonist
asthma, COPD |
ipratropium, tiotropium
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M antagonist
reduces urgency in mild cystitis and reduces bladder spasms |
oxybutynin, glycopyrrolate, flavoxate, tolterodine, enablex (darifenacin), vesicare (solifenacin),
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M antagonist
peptic ulcer treatment dec salivary secretion |
Methscopolamine, pirenzepine M1, propantheline
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M2 antagonist
for bradycardia, antiarrhythmic |
Otenzepad
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Atropine
heart eye airway stomach gut bladder application |
M antagonist- blocks parasymp
low- dec HR, high- inc HR dilation, cycloplegia dec secretions dec acid secretion dec motility dec urgency blocks DUMBBELSS |
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atropine toxicity
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hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter, constipation, urinary retention in men with BPH
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nicotine antagonists
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hexamethonium, trimethapham, mecamylamine HCl, d-Tubocurarine
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N antagonist
ganglionic blocker prevents vagal reflex responses to change in BP |
Hexamethonium
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Hexamethonium toxicity
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severe orthostatic hypotension, blurred vision, constipation, sexual dysfunction
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nicotinic antagonist
short acting ganglionic blocker cannot cross bbb, no cns effects treats extreme hypotension crisis, reduces sympathetic tone, reduces vasoconstriction |
trimethaphan
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uses of ganglionic blockers
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HTN crisis
controlled hypotension during sx autonomic hyperreflexion (pt with spinal cord injury) |
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M antagonist applications
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produce mydriasis and cycloplegia, parkinson's, motion sickness, asthma, COPD, reduce urgency and bladder spasms, peptic ulcer tx, dec resp tract secretions, hayfever/colds, dec sweat gland secretions, bradycardia, antiarrhythmic
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a1, a2, b1, b2
anaphylaxis, glaucoma (open angle), asthma, hypotension direct sympathomimetic |
epinephrine
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a1, a2, b1
hypotension, decreases renal perfusion direct sympathomimetic |
NE
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b1 = b2
AV block, bradycardia, asthma direct sympathomimetic |
isoproterenol
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a1 > a2
pupillary dilation, vasoconstriction, nasal decongestion direct sympathomimetic |
phenylephrine
oxymetazoline |
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b2 > b1
for acute asthma direct sympathomimetic |
albuterol
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b2 > b1
reduces premature uterine contractions direct sympathomimetic |
terbutaline
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b2
reduced premature uterine contractions direct sympathomimetic |
ritodrine
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indirect general agonist, releases stored catecholamines, central and peripheral
narcolepsy, obesity, add indirect sympathomimetic |
amphetamine
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indirect general agonist, releases stored catecholamines
nasal decongestion, urinary incontinence, hypotension (vasoconstriction), bronchodilator indirect sympathomimetic |
ephedrine
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indirect general agonist, uptake inhibitor
vasoconstriction, local anesthesia indirect sympathomimetic |
cocaine
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centrally actin a2 agonist
decreases central adrenergic flow (sympathetic tone) for hypertension, especially with renal disease because no decrease in blood flow to kidney |
Clonidine, a methyldopa
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a2 agonist
decreases aqueous humor synthesis, glaucoma tx |
apaclonidine
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b2 agonists
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metaproterenol, albuterol, salmeterol, terbutaline
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b2 agonist use
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smooth muscle relaxation, obstructive airway disease, acute bronchospasms, HTN
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a blockers
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phenoxybenzamine, phentolamine, prazosin, terazosin, doxazosin, tamsulasin, mirtazapine, yohimbine
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for pheochromocytoma, before sx for HTN, irreversible and reversible
severe HTN episode, bowel pseudo-obstruction |
phenoxybenzamine
phentolamine |
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phenoxybenzamine
phentolamine toxicity |
orthostatic hypotension (unopposed b2)
reflex tachycardia (block a2, inc symp, b1 activation) sexual dysfunction |
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a1 selective blocker
for HTN, urinary retention in BPH toxicity: first dose orthostatic HoTN, dizziness, headache |
Prazosin, terazosin, doxazosin, tamsulasin
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a2 selective blocker
for depression toxicity: sedation, inc cholesterol and appetite |
mirtazapine
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a2 selective blocker
for male sexual dysfunction |
yohimbine
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b blockers
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acebutolol, betaxolol, esmolol, atenolol, metoprolol, propranolol, timolol, pindolol, labetolol
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b blocker effect on HTN
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dec cardiac output, dec renin secretion- dec angiotensin II- dec vascular tone and PR
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b blocker effect on antina pectoris
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dec HR and contractility
dec in O2 consumption- dec arrhythmias and vasospastic episodes |
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b blocker effect on MI
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decrease mortality
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b blocker effect on SVT (propranolol, esmolol)
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dec AV conduction velocity (class II antiarrhythmic) block voltage dependent Na channels- stabilize arrhythmias
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b blocker effect on CHF
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slows progression of chronic failure
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b blocker effect on glaucoma (timolol)
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dec secretion of aqueous humor
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b blocker toxicity
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impotence, exacerbation of asthma, cardiovascular adverse (bradycardia, AV block, CHF) CNS (sedation, sleep alteration)
caution: diabetics, COPD bronchoconstriction |
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nonselective antagonists
b1 = b2 |
propranolol, timolol, nadolol, pindolol, labetalol
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b1 selective antagonists
b1 > b2 |
acebutolol, betaxolol, esmolol (short, ER) atenolol, metoprolol
A BEAM of b1 blockers |
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nonselective a and b antagonists
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carvedilol, labetalol
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partial b agonists
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pindolol, acebutolol
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neuromuscular blocking drugs
depolarizing |
succinylcholine
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used for muscle paralysis in sx or mechanical ventilation
selective for motor N receptor |
neuromuscular blocking drugs
|
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reversal of succinylcholine blockage
phase I Phase II |
phase I: no antidote, block potentiated by AChE inhibitors
low conc reverses in seconds phase II: antidote is AChE inhibs higher doses, longer lasting not reversed by inc in ACh not bypassed by stimuli downstream |
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nondepolarizing neuromuscular blocking drugs
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tubocurarine
|
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competetitive with ACh for Nm receptors
reversed by inc in ACh (neostigmine, edrophonium, AChE inhibs) during block m's can be activated by stimuli downstream |
tubocurarine
neuromuscular blocking nondepolarizing drug |
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used to treat malignant hyperthermia (inhaled anesthetics and succinylcholine inc Ca, mutant ryanodine receptor)
prevents release of Ca |
Dantrolene
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