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21 Cards in this Set

  • Front
  • Back
Endogenous, non-selective agonist
a. limited therapeutic value, short duration
b. shock
Endogenous, non-selective agonist (D receptors, alpha and beta receptors)
a. catecholamine by structure
b. activates the b1-AR in the heart (used in patient with heart failure)
c. useful in the treatment of shock
d. vasodilate renal vasculature!
Non-selective beta-AR agonist
a.extremely potent b-AR
b.potent vasodilator
c.positive chronotropy
d.adverse reactions: tachycardia, BP, arrhythmias
Indirect-acting agonist
a.alkaloid obtained from plant
b.increase NE release, direct agonism
c.prolonged action duration, potent CNS stimulant
d.nasal decongestant, treatment hypotension
e.adverse reactions; HT, insomnia, tachyphylaxis
Indirect-acting agonist
a.release of biogenic amines from storage
b.byproduct of tyrosine metabolism
c.high concentration in fermented food
d.metabolized by liver MAO (monoamine oxidase)
e.caution MAO inhibitors, severe hypertension
Indirect-acting agonist
a.Inhibition of NE and dopamine reuptake,
b.local anesthetic effect also potent CNS stimulant
c.shorter lasting than amphetamine, more intense
d. smoked, snorted or injected for rapid effect
e.hypertension, AMI, arrhythmias, seizures
Beta-AR non selective blocker
2. Timolol (Blocadren)
a. no intrinsic sympathomimetic activity
b. no membrane stabilizing
c. low lipophilicity
d. open-angle glaucoma
Adverse reaction: bronchoconstriction
Beta-AR non selective blocker
a. has intrinsic sympathomimetic activity
b. partial agonist activity
c. low degree of membrane stabilization
Adverse reaction: bronchoconstriction, bradycardia
. has intrinsic sympathomimetic activity (partial agonist activity)
i. maintain some degree of b1-AR activation while blunting the cardiac response to increased SANS
ii. produce smaller reductions in resting heart rate
iii. useful in patients dependent on sympathetic drive because of poor cardiac reserve
iv. preferred in patients subject to bradycardia
Beta-AR selective blocker
a. no ISA
b. hepatic biotransformation
c. hypertension, ischemic heart disease
Adverse reaction: bronchoconstriction, bradycardia
Muscarinic agonist resistant to ChE
a. Dx in asthma: cause bronchoconstriction at low level is hyperreactive airway
b. short-acting
Muscarinic agonist resistant to ChE
a. relieve GI dismotility (post-op)
b. Replaced by Metoclopramide
Direct-acting nicotinic agonists
a. (1) initial depolarization results in fasciculation of muscles (2) Receptor repolarization as [Ach] increases (3) Receptors refractory to depolarization (depolarization-desensitization)
b Clinical use: smoking cessation
c. Paradoxical flaccid paralysis, nicotine poisoning
Carbamate ChE inhibitor
a. Covalently bond to ChE
b. Tx of muscarinic block in CNS (rare)
c. Lipophilic --> cross BBB
Carbamate ChE inhibitor
a. Has quaternary ammonium; charged --> no BBB crossing
b. Tx of myasthenia gravis
c. Be careful with dosage
too little: myasthenia crisis
too much: cholinergic crisis
Organophophate ChE inhibitor
a. used for narrow angle glaucoma in old days
Prazosin (minipress)
Alpha1 selective antagonist
a. antihypertensive
b. alone or in combination
Adverse reaction: ‘first dose’ effect postural hypotension
Ca2+ channel blocker
ARB (Angiotensin II receptor Type I blocker)
a. Reduce vasoconstriction
b. Reduce aldosterone stimulation
c. Diuretic, anti-hypertenxive, Tx of CHF
Adverse effect: diziness, orthostatic hypotension, worsening of renal failure, Pregnancy C/D
a. Beneficial for diabetic's HTN control
b. Not metabolized
c. Tx for CHF
d. Preserve renal fn
e. Preserve LV fn after MI (acute management of MI)
f. Decrease myocardium remodeling
Ganglionic blocker
a. Hypertensive crisis in surgery
b. Aortic aneurysm surgery
c. reduction in parasympathetic and sympathetic
d. Veno- and veso-dilation
e. Cleared by liver
f. Never clinically given
g. IV only
Indirect NE and serotonin antagonist
a. Binds to vesicles that contain NE or serotonin
b. prevent their uptake and deplete the neuron of NE (takes 2~3wks)
c. Anti-hypertensive
Adverse effect: dizziness, orthostatic hypotension, DEPRESSION