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62 Cards in this Set
- Front
- Back
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Metyrosine |
preoperative Pheochromocytoma (benign tumor of adrenal medulla that causes inc prod. of NT)
MOA: dec. biosynthesis of Epi & NE by inhibiting tyrosine hydroxylase
SE: sedation, crystal urea |
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Reserpine |
Tx of severe Hypertension
Indole alkaloid from Rauwolfia serpentina
MOA: Inhibits transport of NE from cytoplasm into storage vesicles hydrolyzed by esterases
inc. NE exposure to MAO
SE: Severe Hypotension, sec Parkinsons |
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Guanethidine |
hypertension
contains guanidine grp (pka ~ 12)
MOA : enter the neuron by uptake-1 process stabilize storage vesicles to inhibit release of NE = dec. sympathetic outflow = dec. BP
Bio: 5%; half-life: 5 days |
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Guanadrel |
hypertension
contains guanidine grp (pka ~ 12)
MOA : enter the neuron by uptake-1 process stabilize storage vesicles to inhibit release of NE = dec. sympathetic outflow = dec. BP
Bio: 85%; half-life: 12 hrs |
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Norepinephrine |
used to ounteract hypotensive crisis
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Epinephrine |
treat hypotensive crisis nasal decongestant stimulate heart in cardiac arrest relax bronchial smooth muscle in asthma anaphylactic shock (chronic allergic rxns) open-angle glaucoma |
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Dipivefrin |
Tx of open-angle glaucoma
Prodrug
more lipophilic than epinephrine |
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Phenylephrine
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nasal decongestant Used topically to dilate pupil during surgery Treat severe hypotension from either shock or drug administration
selective alpha 1-receptor agonist
orally active
doa twice that of Epi |
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Midodrine |
treatment of orthostatic hypotension; vasoconstrictor
N-glycyl pro-drug of desglymidodrine |
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Xylometazoline |
Nasal Decongestant |
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Oxymetazoline |
Nasal Decongestant |
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Tetrahydrozoline |
Nasal Decongestant |
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Nephazoline |
Nasal Decongestant |
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Clonidine |
Tx of hypertension: initial inc. in BP (because of alpha1 receptors) but is followed by a longer-lasting hypotensive effect
potent vasodilator
alpha2:alpha1= 300:1 |
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Apraclonidine |
laser surgery on the eye
alpha2:alpha1= 30:1 |
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Brimonidine |
treatment of glaucoma
alpha2:alpha1= 1000:1 |
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Guanabenz |
treatment of hypertension
MOA: stimulates alpha2 adrenoceptors in the brain to dec. sympathetic outflow
half-life: 6 hrs |
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Guanfacine |
treatment of hypertension
MOA: stimulates alpha2 adrenoceptors in the brain to dec. sympathetic outflow
half-life: 17 hrs |
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Methyldopa
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Lowers BP
Biotransformation to Methyldopate that inc. aqueous solubility for parenteral preparation
alpha2-adrenergic selective |
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Isoproterenol |
asthma (Beta 2) treats heart block (Beta 1)
MOA: acts at both Beta-1 & Beta-2 (non-selective)
metabolized by COMT not MAO (b/c of steric hindrance) |
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Terbutaline |
Used as bronchodilator asthma tx
Resorcinol derivative
Beta-2 selective agonist
Not a substrate for COMT or MAO = longer doa
Orally active |
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Albuterol |
asthma |
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Salmeterol |
asthma |
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Bitolterol |
asthma |
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Ritodrine |
controls premature labor
MOA: relaxes uterine smooth muscle |
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Dobutamine |
treats congestive heart failure
potent inotropic effect but minimal chronotropic effect |
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p-Tyramine |
increase in BP |
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L-(+)-Pseudoephedrine |
nasal decongestant
(S,S)-diastereoisomer of ephedrine
MOA : indirect-acting mechanism (if OH were R then it would would be direct-acting)
use with caution in hypertensive individuals |
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Ephedrine |
Various allergic conditions Nasal decongestant Bronchodilator Cardiac stimulant Vasopressor Appetite suppressant |
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Phenylpropanolamine |
nasal decongestant appetite suppressant cough and cold
Discontinued in the U.S.: causes elevated BP increasing risk for stroke, intracranial bleeding in women
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Tolazoline |
treats symptoms of Raynaud’s syndrome
treats persistent pulmonary hypertension in newborns when other measures do not work
non-selective alpha-antagonist
stimulate GI smooth muscle (cholinergic act.) increases gastric secretion (histaminic act.)
contraindicated in patients with peptic ulcer |
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Phentolamine |
prevent or control hypertensive episodes in patients with pheochromocytoma
has been used for male erectile dysfunction
non-selective alpha-antagonist |
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Phenoxybenzamine |
used primarily to manage patients with preoperative pheochromocytoma also for patients whose tumors are not amenable to surgery
non-selective alpha-antagonist; irreversible
adverse effects effects: reflex tachycardia, increased cardiac output, postural hypotension |
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Prazosin |
used primarily to treat hypertension (produce peripheral dilation without increasing HR) used for treating BPH
S.E.: first dose phenomenon – postural hypotension |
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Terazosin |
used primarily to treat hypertension (produce peripheral dilation without increasing HR) used for treating BPH
S.E.: first dose phenomenon – postural hypotension |
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Doxazosin |
used primarily to treat hypertension (produce peripheral dilation without increasing HR) used for treating BPH
S.E.: first dose phenomenon – postural hypotension |
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Yohimbane |
not used therapeutically inc. heart rate, BP improves mood (serotonin antagonist) tx of male impotency and postural hypotension |
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Ergotamine |
inducers of uterine contraction – contract post-partum uterus used in the treatment of migraine
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Ergonovine |
inducers of uterine contraction – contract post-partum uterus |
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Methylergonovine |
inducers of uterine contraction – contract post-partum uterus |
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Methysergide |
used in the treatment of migraine Raynaud's Disease |
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Lysergic Acid |
prototype? |
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LSD (Lysergic Acid Diethyl Amide) |
hallucinogen |
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Propranolol |
prevention of hypertension cardiac arrhythmias angina pectoris migraine headache
Prototypical and non-selective beta-blocker
Contraindicated in asthma, bronchitis |
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Propanolol Metabolites |
Naphthoxylactic acid (primary) 4-Hydroxypropranolol: antagonistic activity
membrane stabilizing effect |
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Carteolol |
Hypertension Open-angle Glaucoma
Contraindicated in asthma, lung diseases & diabetes
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metipranolol |
Hypertension Open-angle Glaucoma
Contraindicated in asthma, lung diseases & diabetes |
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Penbutolol |
Hypertension
Contraindicated in asthma, lung diseases & diabetes |
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Timolol |
Open-angle glaucoma prev. of migraines Therapy affter MI
Contraindicated in asthma, lung diseases & diabetes |
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Levobunolol |
Hypertension Open-angle glaucoma
Contraindicated in asthma, lung diseases & diabetes
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Nadolol |
Hypertension Angina pectoris
Contraindicated in asthma, lung diseases & diabetes
(Angina pectoris is the medical term for chest pain or discomfort due to coronary heart disease. It occurs when the heart muscle doesn't get as much blood as it needs. This usually happens because one or more of the heart's arteries is narrowed or blocked, also called ischemia.) |
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Pindolol |
Membrane stabilizing activity
Contraindicated in asthma, lung diseases & diabetes |
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Sotalol |
Arrythmias
Contraindicated in asthma, lung diseases & diabetes |
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Acebutolol |
hypertension cardiac arrythmias
has weak agonist activity metabolite = Diacetolol that has selective beta-antagonist act. |
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Atenolol |
hypertension angina pectoris and therapy after MI Membrane stabilizing activity |
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Betaxolol |
hypertension glaucoma Membrane stabilizing activity |
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Bisoprolol |
hypertension |
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Bisoprolol |
hypertension |
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Esmolol |
cardiac arrythmias
rapidly hydrolyzed by esterases admin. by IV |
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Metoprolol |
hypertension angina pectoris and therapy after MI |
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Labetolol |
Antihypertensive with a-1, b1 and b2 blocking activity
mixture of the four isomers B-blocking activity vs a-blocking activity: 1.5 X |
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Carvedilol |
Treatment of congestive heart failure
Antihypertensive with a-1, b1 and b2 blocking activity (S) enantiomer -a-1 and B antagonist (R) enantiomer - a-1 antagonist
B-blocking activity vs a-blocking activity: 10-100 X |
