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Adrenergic Agonists and Antagonists
Dr. P adrenergics
60
Medical
Graduate
08/29/2012

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Cards

Term
receptors that epi acts on and affinities?
Definition
acts on ALL adrenergic receptors with greatest affinity for B2 >B1> A
Term
receptors that NE acts on and their affinities?
Definition
doesn't act on B2
affinities alpha's > beta-1
Term
receptors that isoprotenolol binds to?
Definition
only betas.
Term
what adrenergic receptors does dopamine bind to?
Definition
beta-1 and dopamine receptors D1 and D2
Term
what receptors does dobutamine bind to?
Definition
only one. Beta-1
Term
actions of alpha-1 activation? 5 things
Definition
1. vasoconstriction
2. increase TPR
3. increase BP
4. mydriasis
5. contract bladder sphincter and trigone
Term
actions of alpha-2 activation? 3 things
Definition
inhibit Ach release
inhibit NE release
inhibit insuling secretion
Term
actions of beta-1 activation? 3 things
Definition
tachycardia
increase myocardial contractility
increase renin release
Term
actions of beta-2 activation? 5 things
Definition
vasodilation
decreased TPR
bronchodilation
increase glycogenolysis
relax uterine smooth muscle
Term
vascular effects of NE and Epi on cutaneous vesels and skeletal muscles?
Definition
cutaneous: only has alpha receptors. NE has high affinity --> vasoconstriction. Primary response to both epi and NE is vasoconstriction.
skeletal muscle: NE --> vasoconstriction and Epi --> vasodilation (therapeutic response)
Term
side effect of NE mediated increase in BP?
Definition
reflex bradycardia from strong baroreflex
Term
Clinical uses for Epi
Definition
used only in emergency situations
1. bronchospasm relief
2. cardiac resuscitation
3. reduce IOP
Used with anesthetic to increase effective time of local effect via vasoconstriction to maintain drug in tissues.
Term
side effects of Epi
Definition
hypertension, direct tachycardia, reflex bradycardia, arrythmias, tremor, and HYPERGLYCEMIA (beta-2 modulated release of glucagon).
Term
contraindications for use of Epi
Definition
hyperthyroidism, diabetes, and pt on beta blockers (unapposed alpha increase in TPR)
Term

Dopamine cardiovascular effects?

Dopamine renal effects?

Definition
Beta-1 mediated increase in ionotropy Vascular D1 receptor mediated vasodilation Renal D1 receptor mediated inhibition of Na pump and Na/H exchanger in TAL.
Term
When is dopamine used clinically?
Definition
to improve cardiac and renal finction in pt with severe heart/renal failure. Only used after hypovolemia is treated.
Term
Dobutamine receptors and cardiovascular effects?
Definition
selective for beta-1 receptors
ionotropic>chronotropic CVS effect w/o change in TPR.
Term
Clinical uses of dobutamine?
Definition
short term managment of decreased CO from surgery, CHF or MI
Term
Name the non-selective alpha agonist.
Definition
oxymetazoline
Term
what are the clinical uses of oxymetazoline?
Definition
Used as nasal decongestants. As an alpha agonists, it causes vasoconstriction of mucosal blood vessels and decreases mucous secretion. Can become desensitized.
Term
name the alpha-1 selective agonist
Definition
phenylephrine
Term
Name 3 selective alpha-2 agonists.
Definition
Clonidine, apraclonidine, methyldopa
Term
clinical uses for phenylephrine?
Definition
topical nasal decongestant
mydriatic agent** (produces mydriasis w/o loss of accomadation b/c no PNS interaction unlike atropine)
phenylephrine is contraindicated in narrow/closed angle glaucoma.
maintain BP during spinal anesthesia.
Term

Uses of clonidine?

MOA?

Definition

treat HTN Preparation for addiction withdrawal

binds to alpha 2 receptor on presynaptic terminal and inhibits release of NE to treat HTN

Can cross BBB to decrease sympathetic outflow from brainstem for withdrawal treatment

 

Term
MOA for clonidine in HTN and withdrawal symptom relief
Definition
being a selective alpha-2 agonist, it binds to the presynaptic A2 receptor inhibiting release of NE
can cross BBB to act on lower brainstem to decrease sympathetic outflow.
Term
abruptly stopping clonidine treatment will cause ___?
Definition
rebound hypertension
Term
apraclonidine (iopidine) is used clinically for what?
Definition
mostly used for treatment of OPEN angle glaucoma. Since it is a alpha-2 specific agonist --> decreases aqueous humor production w/o mydriasis (a1 mediated)
Term
name 2 beta-1 selective agonists
Definition
dopamine and dobutamine
Term
name 3 beta-2 adrenergic receptor selective drugs
Definition
albuterol, salmeterol, ritodrine.
Term
Uses and MOA of salmeterol?
Definition
symptomatic relief of bronchospasm of COPD and nocturnal asthma. Has a long duration (12 hours) but with a slow onset so not used in acute attacks.
Term
clinical use of ritodrine and MOA?
Definition
specifically developed Beta-2 agonist to cause uterine relaxation to arrest premature labor
Term
beta-2 agonist side effects? 4 things
Definition
increase HR (???), tremor, decrease plasma K, increase blood glucose
Term
Name 2 non-selective alpha antagonists
Definition
phenoxybenzamine and phentolamine.
Term
name 2 alpha-1 selective antagonists
Definition
prazosin and tamsulosin
Term
Clinical use for non-selective alpha antagonists
Definition
phenoxybenzamine and phentolamine are used to treat pheochromocytoma via irreversible binding of alpha receptors --> decreased TPR and preload.
Term
side effects of phenoxybenzamine and phentolamine
Definition
reflex tachycardia, orthostatic hypertension, and tachycardia from increase NE due to presynaptic blockage of feedback A2 receptor.
Term
Clinical uses and MOA for prazosin
Definition
HTN, CHF, and BPH
MOA: blocks alpha-1 receptor in arteries and veins to decrease TPR and preload. Can cross BBB to suppress sympathetic outflow from lower brainstem.
Term
side effects of prazosin
Definition
orthostatic hypotension and syncope especially upon first treatment. Limit with low initial dose and titrate up to therapeutic dose.
Retention of Na and water thus use w/ diuretic.
Term
Clinical use of tamsulosin
Definition
symptomatic relief of urinary symptoms of BPH by relaxing smooth muscle. pretty specific for a1 in the sphincter and trigone
Term
Name 3 non-selective (first generation) beta antagonists
Definition
proponanolol, timolol, sotalol
Term
Name 3 beta-1 selective (2nd gen) beta antagonists
Definition
atenolol (tenormin), esmolol, metoprolol
Term
Name 3 3rd generation beta antagonists? what makes a drug a 3rd gen beta antagonists?
Definition
Non-selective: labetalol and carvedilol B1 selective: nebivolol There are additional protective effects in order to be a 3rd gen.
Term
beta blockers with high lipophilicity
Definition
propanolol, timolol and metoprolol
Term
name 4 membrane stabilizing beta blockers?
What does membrane stabilizing mean?
Definition
propanolol, carvedilol, pindolol and acebutolol.
membrane stabilizing means hyperpolarizaion of the membrane via reduced Ca entry and open K channels.
Term
clinical uses of propanolol
Definition
treat essential HTN, exercise angina, arrythmias, CHF, MI, thyrotoxicosis, migraine prophylaxis (because of it lipophillicity)
Term
propanolol moa?
Definition
non selective beta blocker. with long term effects of decreasing renin release and formation of ANG II.
Term
timolol clinical uses and MOA
Definition
used to treat open angle glaucoma via block of non specific beta receptors and resulting decrease in aqueous humor production and decrease in IOP
Term
Pt presents with long history of moderate controlled asthma and has HTN. If you had to choose a beta blocker, which would it be?
Definition
atenolol because it is Beta-1 specificand won't interfere with asthma treatments (in a perfect world)
Term
side effects of beta blockers
Definition
rebound effects, asthma exacerbation, 1st and 2nd gen mask hypoglycemic symptoms (except sweating), sexual dysfunctions.
Term
advantage with 3rd gen beta blockers?
Definition
vasodilatory effects via B2 agonists, A1 blockers and NO mediated vasodilation, antioxidant effects, anti-proliferative effect on cardiac tissue
Term
clinical uses of lebetolol and MOA
Definition
reduce HR and contractility (B1 block) and reduce TPR (A1 block) and vasodilation (via B2 agonist) thus this is a 3rd gen blocker.
Term
Carvedilol uses and MOA
Definition
uses: HTN, CHF
MOA: reduce HR and contractility (B1 block)
decreae TPR (A1 block)
anti-oxidant properties
Term
Nebivolol uses and MOA
Definition
TREAT UNCOMPLICATED HTN.
High b1 selectivity and increase NO availability.
Term
name 4 amphetamines and identify what drug class they belong to
Definition
they are indirect acting sympathomimetics
amphetamine
methamphetamine (desosxy)
dextroamphetamine (dexedrine)
methylphenidate (ritalin)
Term
MOA for amphetamines?
Definition
increase release of dopamine via inhibition of uptake of biogenic amine NT's, and inhibit MAO.
Term
clinical uses for amphetamines?
Definition
narcolepsy, ADHD, ADD, appetite suppressant
Term
name the mixed acting sympathomimetic and its actions
Definition
ephedrine
increases everything and can cross BBB.
Term
Indirect acting sympatholytics (2)?
its use?
Definition
1. methyldopa. used in pregnancy HTN.
2. Metyrosine. used in treatment of pheochromocytoma.
Term
use and 2 examples of monoamine oxidase inhibitors?
Definition
treats refractory depression. Phenelzine and Tranylcypromine and selegiline
Term
COMT inhibitors and use?
Definition
entacapone and tolcapone used in parkinsons.
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