Adrenergic Drugs-Konorev Flashcards
Norepinephrine and epinephrine are examples of these drugs
Direct adrenomimetics-Mixed alpha and beta agonists
Dobutamine, isoproterenol, terbutaline, and albuterol are examples of these drugs
Direct adrenomimetics-Beta agonists
Dopamine and fenoldopam are examples of these drugs
Direct adrenomimetics-Dopamine agonists
Phenylephrine and methoxamine are alpha agonists that have a higher affinity for this receptor:
a1>a2»_space;»»»B
Clonidine is an alpha agonist that has a higher affinity for this receptor
a2 > a1»_space;»> B
Norepinephrine and epinephrine are mixed alpha and beta agonists have higher affinity for these receptors
a1=a2; B1 > B2 for norepi
a1=a2; B1=B2 for epi
Dobutamine is a beta agonist that has highest affinity for this receptor
B1
Isoproterenol is a beta agonist with highest affinity for this receptor
B1=B2
Albuterol, terbutaline are beta agonists that have highest affinity for this receptor
B2
Dopamine has highest affinity for these receptors
D1=D2
Fenoldopam is a dopamine agonist with highest affinity for this receptor
D1»_space; D2
Epinephrine has its effects on cardiac function by binding these receptors
B1
Epinephrine has its effects on vascular tone by binding to this receptor
B2 and a1
Epinephrine has its effects on relaxing bronchial smooth muscle by binding to this receptor: ___ and decreases bronchial secretion and congestion within bronchial mucosa by binding to this receptor: ___
Relax bronchial smooth m: B2
Decrease secretion: a1
Epinephrine has its effects on causing muscle tremor and increases K uptake by skeletal muscle by binding these receptors
B2
Epinephrine has its effects on blood glucose levels by enhancing liver glycogenolysis by binding to this receptor ___ and inhibits insulin release by binding to this receptor ___
Glycogenolysis: B2
Inhibit insulin: a2
Dopamine stimulation by binding to ___ causes vasodilation –> high density of these receptors in renal, cerebral, mesenteric, and coronary vessels
D1
This alpha adrenergic agonist binds a1 > a2»_space;»> B; it is an effective mydriatic and decongestant, causes severe vasoconstriction and BP elevation, and is not a catechol
Phenylephrine
This drug is a selective a2 agonist has a central effect on a2 receptors in the lower brainstem area which decreases sympathetic outflow, reduction in BP, and bradycardia. Its local application produces vasoconstriction
Clonidine
___ activates a2 receptors in the vasomotor center of the brain, reduces sympathetic activity in the body, and reduces peripheral vascular resistant, decreases heart rate and CO
Clonidine
Isoproterenol is a non-selective beta agonist. Name the receptor associated with the following actions of isoproterenol:
- Positive inotropic and chronotropic action, increases CO: ___
- Vasodilator, decreases arterial pressure: ___
- Causes bronchodilation: ___
B1
B2
B2
This drug is a selective B1 agonist with potent inotropic action. It has less prominent chronotropic action as compared to isoproterenol
Dobutamine
These drugs are selective B2 agonists that cause bronchodilation and relaxation of the uterus
Terbutaline and albuterol
This indirect sympathomimetic drug inhibits the re-uptake of DA and NE
Cocaine
This indirect sympathomimetic drug inhibits MAO
Selegiline and phenelzine
These indirect sympathomimetic drugs reverse NE and DA uptake mechanism and increase their relese
Amphetamines, Methylphenidate, and Tyramine
This indirect sympathomimetic drug is a releasing agent AND direct adrenergic receptor agonist
Ephedrine
___ agonists usually are more lipophilic and easily penetrate the BBB - have significant central effects –> CNS stimulants
Indirect adrenergic agonists
Amphetamine, methamphetamine, and methyphenidate are this type of agonist
Indirect adrenergic agonists –> mild alerting affects, improved attention
This indirect adrenergic agonist inhibits transmitter reuptake at adrenergic synapses, has peripheral and intense central adrenomimetic action, and local anesthetic properties
Cocaine
This indirect adrenergic agonist releases stored catecholamine with some direct adrenomimetic action; is a plant constituent, non-catechol (long DOA and effective after PO); Non selective; Mild stimulant (enters CNS)
Ephedrine
This indirect adrenergic agonist accumulates in protein rich food during fermentation. It is readily metabolized by MAO in the liver (very high 1st pass effect) and if administered parenterally, affords indirect sympathomimetic action caused by release of stored catecholamines
Tyramine
These adrenergic agonists can be administered during hypotensive emergencies (hemorrhagic shock, OD of antihypertensives, CNS depressants)
Norepi, phenylephrine, and methoxamine
This adrenergic agonist can be used for treating chronic hypotension
Ephedrine
These adrenergic agonists can be administered to treat cardiogenic shock due to massive acute MI
Dopamine and dobutamine
For CV conditions, namely heart failure:
Short term use of ___ is used in acute HF while ___ is used in congestive severe HF with reduced renal perfusion
Dobutamine
Dopamine
For HTN tx with adrenergic agonists:
___ for long-term tx of HTN
___ for hypertensive emergencies
Alpha-2 agonists
Fenoldopam
For emergency therapy for complete AV block and cardiac arrest, these adrenergic drugs may be used
Epi and isoproterenol
Phenylephrine, methoxamine, and clonidine are examples of these drugs:
Direct adrenomimetics-Alpha agonists
Tx of bronchial asthma can be done with these B2 selective agonists
Albuterol and terbutaline
This adrenergic agonist is effective at treating the respiratory component (bronchospasm and upper airway congestion) and the CV component (severe hypotension, cardiac depression) of anaphylaxis
Epinephrine
This adrenergic agonist has ophthalmic applications like examination of the retina –> induction of mydriasis
Phenylephrine
These alpha2 selective agonists can be used for glaucoma
Apraclonidine and brimonidine
This B2 agonist can suppress premature labor
Terbutaline
This adrenergic agonist can be used for stress urinary incontinence
Ephedrine
These adrenergic agonists can be used for narcolepsy
Amphetamines and methylphenidate
These adrenergic agonists can be used for tx of ADHD
Methylphenidate
These adrenergic agonists can be used to tx obesity
Phentermine, ephedrine, and amphetamines
List some non-selective (a1 and a2) receptor antagonists
Phentolamine and phenoxybenzamine
List some a1 receptor SELECTIVE anatagonists
Prazosin, terazosin, tamsulosin, doxazosin, alfuzosin, silodosin
-All end in the suffix -osin!!!
___ is a competitive a antagonist
___ is a non-competitive irreversible a antagonist
Phentolamine
Phenoxybenzamine
List alpha antagonist drugs for the tx of pheochromocytoma
Phentolamine and phenoxybenzamine
These a1 selective antagonists can be used for tx of chronic (essential) HTN. They work well in moderate HTN and generally well tolerated
Prazosin, Terazosin, and Doxazosin
This combo of alpha anagonists can be used to treat ED
Combo of phentolamine and non-specific vasodilator papaverine (injected into penis)
These alpha antagonists can be used to tx BPH for chronic urinary obstruction
Tamsulosin and Silodosin
Silodosin–> greater selectivity for a1A than a1B
Prazosin, doxazosin, and terazosin are also effective
What are adverse effects associated with clinical use of alpha antagonists?
- Most significant effects are on the CV system
- seen less with a1 selective antagonists
- postural hypotension
- tachycardia
- retention of fluid and salt
- impaired ejaculation
- nasal stuffiness
Labetalol and Carvedilol are examples of this type of adrenergic drug
Mixed antagonists
B and a1 antagonists for both
Propanolol, Pindolol, Nadolol, and Penbutolol are examples of this adrenoceptor antagonist
B1 and B2
Metoprolol, Betaxolol, Acebutolol, and Atenolol are examples of this type of adrenoceptor antagonist
B1 selective
Atenolol, nadolol, propanolol, and betaxolol have what intrinsic activity as a beta-blocker at the receptors?
Anatagonist
Acebutolol, Labetalol, penbutolol, and pindolol have what intrinsic activity as a beta-blocker at the receptors?
Partial agonists
Carvedilol and metoprolol have what intrinsic activity as a beta-blocker at the receptors?
Inverse agonists
These beta blockers are used for long-term use in post-infarction period after an MI
Timolol, propanolol, and metoprolol
These beta blockers can be used for tx of glaucoma
Timolol and betaxolol
This beta blocker can be used to treat hyperthyroidism
Propanolol
This indirect acting antiadrenergic drug is a norepinephrine release inhibitor. It is taken up by the reuptake mechanism, replaces NE in vesicles, causes a gradual depletion of NE stores, and inhibits NE release via local anesthetic properties
Guanethidine
This indirect acting antiadrenergic drug is an inhibitor of tyrosine hydroxylase
Metyrosine
This indirect acting antiadrenergic drug can be used for tx of chronic HTN: ___
This indirect acting antiadrenergic drug can be used for tx of pheochromocytoma: ___
Guanethidine
Metyrosine
