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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
Q

Characteristics of adrenergic agonists- catecholamines

A

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

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26
Q

Characteristics of adrenergic agonists- non-catecholamines

A

Lack catechol OH group, have linger half lives and have higher lipid affinity- CH3

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27
Q

Characteristics of adrenergic agonists- substitution on amine nitrogen

A

Increase affinity for Beta-receptors

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28
Q

Adrenergic agonist- direct effect

A

Epinephrine, NE, albuterol, pirbuterol, terbutaline, dobutamine, dopamine, isoproteranol, phenylephrine, clonidine, salmeterol, and formoterol

29
Q

Adrenergic agonist- indirect

A

Amphetimine and tyramine

30
Q

Adrenergic agonist- mixed

A

ephedrine

31
Q

Epinephrine

A

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
Q

Epinephrine therapeutic uses

A

Emergent tx of asthma, glaucoma, anaphylaxis, w/local anesthetics to prolong DOA through vasoconstriction

33
Q

Epinephrine Pharmacokinetics

A

Rapid onset w/ IV, given sub-Q, inhalation, endotrancheal, and topically

34
Q

Epinephrine ADRs

A

CNS- anxiety, fear, tension, HA, tremor, hemorrahage, increased BP, cerebral hemorrhage
CV-arrhythmias
Pulmonary edema

35
Q

Epinephrine Interaction

A

Hyperthyroidism- exaggerated CV effects due to increased production of receptors
Cocaine- exaggerated CV effects due prevention of re-uptake.

36
Q

Norepinephrine

A

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
Q

Dopamine

A

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
Q

alpha1 selective agonists

A

Methoxamine, phenyleprhine, oxymetazoline,

39
Q

Methoxamine

A

Alpha 1 selective agonist

Not used often but used to tx shock

40
Q

Phenylephrine

A

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
Q

Oxymetazoline

A

Alpha 1 selective agonist

Topical, constrict vascular smooth muscle in relief of opthamic hyperemia.

42
Q

Adreneric agonist- Alpha 2 selective agonists

A

Feedback, decrease E and increase NE

Clonidine, a-methyldopa, and guanfacine

43
Q

Chlonidine

A

Alpha 2 selective agonist
Lowers BP by suppressing sympathetic outflow
ADR dry mouth and sedation

44
Q

a-methyldopa

A

alpha 2 selective agonist

Metabolized to a-methylnorepinephrine which is an a agonist in CNS to decrease sympathetic outflow

45
Q

Gaunfacine

A

a-2 agonist in CNS to decrease sympathetic outflow

ADR dry mouth and sedation

46
Q

Adrenergic agonist- B nonselective agonists

A

Isoproterenol and dobutamine

47
Q

Isoproterenol

A

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
Q

Dobutamine

A

B1 selective

Increases cardiac rate and output, usted to increased CO in CHF, racemic mixture cancers out alpha

49
Q

Adrenergic Agonist- B2 selective agents

A

Albuterol. pirbuterol, terbutaline, salmeterol, and formoterol
Predominately in the lung and vasculature

50
Q

Albuterol, pirbuterol, terbutaline

A

Adrenergic Agonist- B2 selective

Short acting bronchodilators (less cardiac stimulation)

51
Q

Salmeterol and formoterol

A

B2 selective agents

B2 long acting bronchodilator

52
Q

Indirect Adrenergic Agosist

A

Cause body to release more neurotransmitters. Cause NE and Serotonin release from presynaptic terminals

53
Q

Amphetamine

A

Indirect adrenergic agonist

CNS stimulant, increases BP by alpha effect of vasculature, beta effect on heart

54
Q

Mixed action adrenergic agonists

A

Cause NE release and stimulates receptros

55
Q

Ephedrine

A

Mixed action
Alpha, beta, and CNS stimulant
Use- nasal sprays due to local vasoconstrictor activity; urinary incontinence
Long DOA

56
Q

Therapeutic uses of agonists

A

Shock, hypotension, cardiac arrest, and local vasoconstriction, narcolepsy, weight reduction, ADHD

57
Q

Adrenergic Antagonists- alpha blockers

A

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
Q

Phenoxybenzamine

A

Adrenergic antagonist Alpha blocker
Irreversible, nonselective and noncompetitive block, tx of pheochromocytoma to preclude HTN crisis that can result from manipulating tissue.

59
Q

Phentolamine

A

Adrenergic antagonist Alpha blocker

Competitive, nonselective block (alpha 1 and 2 response is more E being created and alpha 1 decreased vasoconstriction)

60
Q

Prazosin, doxazosin, terazosin

A

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
Q

Tamsulosin

A

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
Q

Adrenergic antagonists- beta blockers

A

Work by blocking beta

Ex- prpranolol (prototype), timolol, nadolol, acebutolol, atenolol, metoprolol, and esmolol

63
Q

Propranolol (prototype)

A

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
Q

Timolol and nadolol

A

Adrenergic antagonist beta blocker
Nonspecific beta blocker
Uses- glaucoma and HTN

65
Q

Acebutolol, atenolol, metoprolol, esmolol

A

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
Q

Adverse effects of beta-receptor antagonists

A

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
Q

Adrenergic Antagonists w/ partial activity

A

Pindolol and acebutal

Weakly stimulate B1 and B2. Used for HTN

68
Q

Adrenergic antagonists- labetolol and carvediol

A

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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