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Pharmacotherapeutics I > Adrenergic Pharmacology > Flashcards

Adrenergic Pharmacology Flashcards

1
Q

Synthesis and Storage of Dopamine (DA), norepinephrine (NE, and epinephrine

A

Tyrosine transported from plasma into nerve cell via Na+ dependent carrier. Oxidation to DOPA by tyrosine hydroxylase (rate limiting step). DOPA decarboxylated to form DA. DA transported into synaptic vesicles for protection via amine transporter system. DA hydroxylated to norepinephrine by dopamine B-hydroxylase within vesicle. NE is transported back to cytoplasm and methylated to epinephrine in adrenal medulla and stored in chromaffin cells.

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2
Q

Release of NE

A

Action potential triggers calcium influx, causing release of vesicles through exocytosis

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3
Q

Binding to Receptor

A

Postsynaptic (alpha and beta that work w/ g protein secondary messenger system) receptor activated by binding of NE –> intracellular response via 2nd messenger

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4
Q

Drugs that affect synthesis/uptake/release

A

Alpha methyltyrosine, reserpine, tyramine. guanethidine, amphetimine, cocaine, imipramine, fluoxetine, tricyclic antidepressents, phenelzine, selegiline

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5
Q

Alpha-methyltyrosine

A

Inhibits tyrosine hydroxylase

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6
Q

Reserpine

A

Blocks VMAT, transport of bioamines from cytoplasm into vesicles.

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7
Q

Tyramine

A

Dietary amines usually metabolized by MAO in GI and liver. In pt with MAO inhibitors tyramine is absorbed, large amounts cause displacement of vesicular NE and non vesicular release resulting in HTN crisis.

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8
Q

Guanethidine

A

Displaces NE in storage vesicles, leading to gradual depletion of NE

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9
Q

Amphetamine

A

Displaces endogenous NE, blocks reuptake by NET and DAT

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10
Q

Cocaine

A

Potent inhibitor of NET, eliminated catecholamine transport

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11
Q

Imipramine, fluoxetine

A

Inhibitors of NET

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12
Q

Tricyclic antidepressents

A

Blocks Na+/K+ ATPase, blocks NET, prevents uptake of epinephrine and NE and increases DOA

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13
Q

Phenelzine

A

Inhibits MAO-A, increasing NE and 5-HT serotonin content. Inhibits metabolism of NE and seratonin

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14
Q

Selegiline

A

Inhibits MAO, increasing DA.

Low doses for tx of Parkinson Disease

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15
Q

Adrenergic Receptors

A

Alpha and beta based on affinity to adrenergic agonists

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16
Q

Alpha affinity

A

Epinephrine binds the best, then NE, and lastly isoproteranol

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17
Q

Beta affinity

A

Isoproteranol > epinephrine > norepinephrine

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18
Q

Activity of Agonists- Alpha 1

A

Vasoconstriction

Increases PVR, BP, mydriasis, and increased closure of the sphincter of bladder

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19
Q

Activity of Agonists- Alpha 2

A

Central feedback receptor

Inhibit NE release (auto receptors) resulting in lowered BP, inhibit insulin release

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20
Q

Activity of Agonists- Beta 1

A

Primary receptor located in the heart
Tachycardia, increased myocardial contractility, resulting in increased cardiac output, increased release of renin (controls BP), and increased lipolysis

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21
Q

Activity of Agonists- Beta 2

A

Primarily located in the vasculature and lungs
Vasodilation, decreased PVR, decreased DBP, bronchodilation, increased muscle and liver glycogenolysis, increased glucagon release, relax uterine smooth muscle.

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22
Q

Desensitization of receptors

A

Make receptors unavailable for interaction through sequestion. Down regulate receptors, and unable to couple G-proteins.

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23
Q

Symapthyomimetic

A

Adrenergic drug which acts directl on adrenergic receptors activating them. Aka adrenergic agonists.

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24
Q

Endogenous catecholamines

A

Epinephrine, NE, and DA

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25
Characteristics of adrenergic agonists- catecholamines
OH group in the 3,4 position of the benzene ring Rapid inactivation because of enzymes scattered through various tissues OH groups prevent penetration to the CNS
26
Characteristics of adrenergic agonists- non-catecholamines
Lack catechol OH group, have linger half lives and have higher lipid affinity- CH3
27
Characteristics of adrenergic agonists- substitution on amine nitrogen
Increase affinity for Beta-receptors
28
Adrenergic agonist- direct effect
Epinephrine, NE, albuterol, pirbuterol, terbutaline, dobutamine, dopamine, isoproteranol, phenylephrine, clonidine, salmeterol, and formoterol
29
Adrenergic agonist- indirect
Amphetimine and tyramine
30
Adrenergic agonist- mixed
ephedrine
31
Epinephrine
Interacts with both alpha and beta Low dose- mainly beta effects (vasodilation); high dose- alpha effects (vasoconstriction CV: + inotropic, + chronotropic- increased CO Alpha effects- vasoconstricts arterioles B2- vasodilates vessels to liver and skeletal muscle Net result- increased SBP w/ slight decrease in DBP Respiratory- bronchodilation of smooth muscle (B2) Hyperglycemia-decreased insulin release (alpha2) increased glycogenesis, increased release of glucagon (B2) Lypolysis B1
32
Epinephrine therapeutic uses
Emergent tx of asthma, glaucoma, anaphylaxis, w/local anesthetics to prolong DOA through vasoconstriction
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Epinephrine Pharmacokinetics
Rapid onset w/ IV, given sub-Q, inhalation, endotrancheal, and topically
34
Epinephrine ADRs
CNS- anxiety, fear, tension, HA, tremor, hemorrahage, increased BP, cerebral hemorrhage CV-arrhythmias Pulmonary edema
35
Epinephrine Interaction
Hyperthyroidism- exaggerated CV effects due to increased production of receptors Cocaine- exaggerated CV effects due prevention of re-uptake.
36
Norepinephrine
At therapeutic doses alpha 1 and beta 1 receptors are afected CV- vasoconstriction in periphery (including kidney) reulting in elevated BP, baroreceptor reflex: increase BP -> increased vagal activity stimulation baroreceptors causing bradycardia. Tx use shock through vascular resistance, increase BP
37
Dopamine
Low doses act predominately on D1 receptors in renal, mesenteric, and coronary vascular beds (vasodilation). Higher doses a positive inotrope (action at beta1) High doses- vasoconstriction via alpha 1 receptors DOC for shock, at appropriate doses is useful in management of low CO associated with compromised renal function such as in severe CHF.
38
alpha1 selective agonists
Methoxamine, phenyleprhine, oxymetazoline,
39
Methoxamine
Alpha 1 selective agonist | Not used often but used to tx shock
40
Phenylephrine
Alpha 1 selective agonist Used like psuedofedrin, Topical constrict vascular smooth muscle in relief or nasal congestion Not catechol derivative so substrate for COMT Induces reflex bradycardia when given parenterally, raises BP due to vasoconstriction.
41
Oxymetazoline
Alpha 1 selective agonist | Topical, constrict vascular smooth muscle in relief of opthamic hyperemia.
42
Adreneric agonist- Alpha 2 selective agonists
Feedback, decrease E and increase NE | Clonidine, a-methyldopa, and guanfacine
43
Chlonidine
Alpha 2 selective agonist Lowers BP by suppressing sympathetic outflow ADR dry mouth and sedation
44
a-methyldopa
alpha 2 selective agonist | Metabolized to a-methylnorepinephrine which is an a agonist in CNS to decrease sympathetic outflow
45
Gaunfacine
a-2 agonist in CNS to decrease sympathetic outflow | ADR dry mouth and sedation
46
Adrenergic agonist- B nonselective agonists
Isoproterenol and dobutamine
47
Isoproterenol
Nonspecific B agonist (acts at B1 and B2) CV: + inotropic and chronotropic effects (B1); vasodilation of arterioles of skeletal muscle (B2) Pulmonary- bronchodilation (B2) Uses- stimulates heart in emergencies
48
Dobutamine
B1 selective | Increases cardiac rate and output, usted to increased CO in CHF, racemic mixture cancers out alpha
49
Adrenergic Agonist- B2 selective agents
Albuterol. pirbuterol, terbutaline, salmeterol, and formoterol Predominately in the lung and vasculature
50
Albuterol, pirbuterol, terbutaline
Adrenergic Agonist- B2 selective | Short acting bronchodilators (less cardiac stimulation)
51
Salmeterol and formoterol
B2 selective agents | B2 long acting bronchodilator
52
Indirect Adrenergic Agosist
Cause body to release more neurotransmitters. Cause NE and Serotonin release from presynaptic terminals
53
Amphetamine
Indirect adrenergic agonist | CNS stimulant, increases BP by alpha effect of vasculature, beta effect on heart
54
Mixed action adrenergic agonists
Cause NE release and stimulates receptros
55
Ephedrine
Mixed action Alpha, beta, and CNS stimulant Use- nasal sprays due to local vasoconstrictor activity; urinary incontinence Long DOA
56
Therapeutic uses of agonists
Shock, hypotension, cardiac arrest, and local vasoconstriction, narcolepsy, weight reduction, ADHD
57
Adrenergic Antagonists- alpha blockers
Reverse vasoconstrictive action of epinephrine, side effects commonly observed with nonselective alpha blockers- orthostatic hypotension, reflex tachycardia, vertigo, and sexual dysfunction Ex- phenoxybenzamine, phetolamine, prazosin, doxazosin, and , tamulosin
58
Phenoxybenzamine
Adrenergic antagonist Alpha blocker Irreversible, nonselective and noncompetitive block, tx of pheochromocytoma to preclude HTN crisis that can result from manipulating tissue.
59
Phentolamine
Adrenergic antagonist Alpha blocker | Competitive, nonselective block (alpha 1 and 2 response is more E being created and alpha 1 decreased vasoconstriction)
60
Prazosin, doxazosin, terazosin
Adrenergic antagonist Alpha blocker Selective alpha1 blocker- used for vasodilation Tx- hypertension, BPH, CHF by relaxing the arterial and venous smooth muscle and decreased PVR.
61
Tamsulosin
Adrenergic antagonist Alpha blocker Tx of BPH (benign prostate hyperplasia) Inhibitor of Alpha 1 receptor on smooth muscle of prostate (decreases tone of bladder neck and prostate and improves urine flow.)
62
Adrenergic antagonists- beta blockers
Work by blocking beta | Ex- prpranolol (prototype), timolol, nadolol, acebutolol, atenolol, metoprolol, and esmolol
63
Propranolol (prototype)
Adrenergic antagonist beta blocker Nonselective Uses- lowers BP, used to tx angina, cardiac arrhythmias, MI, glaucoma, prophylaxis for migraines Effects- lowers cardiac output (rate and force), prevents vasodilation, bronchoconstriction, increased Na retention, decreased glycogenolysis, and glucagon secretion
64
Timolol and nadolol
Adrenergic antagonist beta blocker Nonspecific beta blocker Uses- glaucoma and HTN
65
Acebutolol, atenolol, metoprolol, esmolol
Adrenergic antagonist beta blocker Preferentially blocks beta 1 receptors- cardioselective Eliminates unwanted bronchoconstriction, little effect of CHO- metabolims, or PVR Useful in hypertensive DM pt on insulin or oral hypoglycemics
66
Adverse effects of beta-receptor antagonists
Cause of exacerbate HF, life threatening bradycardia in pt w/ AV conduction defects, withdrawl syndrome, life threatening increase in airway resistance in patients w/ COPD and asthma, and blunts recognition of hypoglycemia in patients w/ type 1 DM.
67
Adrenergic Antagonists w/ partial activity
Pindolol and acebutal | Weakly stimulate B1 and B2. Used for HTN
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Adrenergic antagonists- labetolol and carvediol
Antagonists of alpha1 and beta 1&2 receptors. Peripheral vasodilation, dont alter lipid of glucose levels. Carvediol decreased lipid peroxidation and vascular wall thickening to benefit CHF Uses of labetolol- HTN, CHF, PIH, HTN emergenies -> rapidly lowers BP

Pharmacotherapeutics I (23 decks)

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