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PHAR 341 - Pharmacology > Adrenergic Pharmacology > Flashcards

Adrenergic Pharmacology Flashcards

1
Q

Effects of direct acting non-selective adrenergic agonist (epinephrine) on the CNS

A
  • doesn’t cross the blood brain barrier
  • fear, anxiety, restlessness, tremor, headache occur as an indirect effect
  • mydriasis (pupil dilation)
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2
Q

Effects of direct acting non-selective adrenergic agonist (epinephrine) on the Cardiovascular system

A
  • vasocontriction
  • increased intophy (muscular contraction) and chronotropy
  • vasodilates skeletal muscle blood vessels
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3
Q

Effects of direct acting non-selective adrenergic agonist (epinephrine) on the Respiratory System

A
  • brochodilation
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4
Q

Effects of direct acting non-selective adrenergic agonist (epinephrine) of GI tract

A
  • decrease motility and secretion
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5
Q

Effects of direct acting non-selective adrenergic agonist (epinephrine) on Urinary Tract

A
  • decrease voiding pressure
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6
Q

Effects of direct acting non-selective adrenergic agonist (epinephrine) on glands

A
  • sweating

- pallor (vasocontriction of blood vessels in the face = pale face)

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7
Q

Summary of ephinephrine effects:

A
  • positive inotrope and chronotrope (increases rate and force of the heart)
  • vasocontriction
  • less dilation of skeletal muscle blood vessels
  • bronchodilation
  • tends to increase both diastolic and systolic pressure
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8
Q

Adrenergic Receptor subtypes

A

alpha and beta

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9
Q

Alpha Adrenergic Receptor subtypes

A

alpha 1 and alpha 2

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10
Q

Beta Adrenergic Receptor subtypes

A

beta 1, 2, 3

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11
Q

Alpha 1 receptor Mechanism of Action

A
  • increase IP3 and DAG
  • IP3-promotes the release of Ca2+ from intracellular stores
  • DAG activates protein kinase C
  • results in excitation
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12
Q

Alpha 2 receptors Mechanism of Action

A
  • inhibit adenyl cyclase

- relsuts in inhibition

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13
Q

Beta Adrenergic Receptor subtypes Mechanism of Action

A
  • increase cAMP

- affects depend on the tissue

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14
Q

Location of alpha 1 receptors

A
  • vascular smooth muscle
  • pupillary dilator muscle
  • pilomotor muscle
  • prostate
  • bladder sphincter
  • heart
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15
Q

Location of alpha 2 receptors

A
  • vascular smooth muscle
  • GI smooth muscle
  • fat cells
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16
Q

Location of beta 1 receptors

A
  • heart
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17
Q

Location of beta 2 receptors

A
  • respiratory
  • uterine
  • vascular smooth muscle
  • skeletal muscle
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18
Q

Location of beta 3 receptors

A
  • fat cells
  • bladder
  • heart
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19
Q

Dopamine receptor subtypes

A

D1,2,3,4,5

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20
Q

D1 effects

A
  • stimulates adenylyl cyclase

similar to beta receptor

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21
Q

D2 effects

A
  • inhibits adenylyl cyclase activity
  • open potassium channels
  • decrease calcium influx
    (similar to alpha 2 receptors)
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22
Q

Location of D3,4,5

A

CNS

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23
Q

Location of D1 receptors

A
  • smooth muscle
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24
Q

Effects of alpha 1 receptor activation

A
  • contraction of vascular smooth muscle
  • contraction of pupillary dilator muscle (dilates pupil)
  • erects hair (pilomotor muscle)
  • contraction of prostate
  • contration of bladder sphincter
  • increase contraction force
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25
Q

Effects of alpha 2 receptors

A
  • inhibition adrenergic and cholinergic transmitter release nerve terminals
  • contraction of vascular smooth muscle
  • (indirect) relaxation of GI smooth muscle
  • inhibits lipolysis from fats
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26
Q

Effects of beta 1 receptors

A
  • positive chronotropy and inotropy
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27
Q

Effects of beta 2 receptors

A
  • relaxation of the respiratory system
  • relaxation of the uterine system
  • relaxation (dilate) of vascular smooth muscle
  • uptakes K+ in the skeletal muscle
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28
Q

Effects of D1 receptors

A
  • dilates renal vessels
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29
Q

Dopamine activates:

A

D1 and D2 and beta 1 receptors

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30
Q

Dopamine causes:

A
  • relaxes vascular smooth muscle
  • suppresses norepinephrine release
  • dilates renal blood vessels
  • increase in force and rate of heart contraction
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31
Q

Dobutamine activates:

A
  • alpha 1
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32
Q

Dobutamine uses:

A
  • hypotensive emergencies to preserve cerebral and coronary blood flow
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33
Q

Selective alpha Agonists

A
  • Phenylephrine

- Xylometrazoline/oxymetazoline

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34
Q

Phenylephrine

A
  • selective alpha Agonist
  • dilates pupils
  • decogestant
  • can be used to raise blood pressure
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35
Q

Xylometazoline/Oxymetazoline

A
  • topical decongestant
  • contricts the nasal mucosa
    oxymetazoline may cause hypotension due ti significant affinity for alpha 2 receptors
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36
Q

Selective alpha 2 agonists

A
  • Clonidine
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37
Q

Effects of selective alpha 2 agonists

A
  • decrease blood pressure through action in the CNS to decrease sympathetic output
    by decreasing chronotropy, inotropy, decrease vascular tone
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38
Q

Clonidine

A
  • alpha 2 agonist
  • antihypertensive
  • reduces symptoms of alcohol and nicotine withdrawl
  • analgesic as an epidural
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39
Q

Side effects of Clonidine

A

Dry mouth and constipation (should be able to answer why?)

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40
Q

Selective beta receptor Agonists

A
  • Isoproterenol
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41
Q

isoproterenol

A
  • activates beta receptors
  • positive chronotrophic and inotropic actions
  • potent vasodilator
  • increases cardiac output
  • decrease diastolic or slight increase systolic pressure
42
Q

Selective beta 2 receptor agonist

A
  • salbutamol
43
Q

Salbutamol

A
  • selective beta 2 receptor agonist

- bronchodilator

44
Q

Selective beta 3 receptor agents

A
  • Mirabegron
45
Q

Mirabegron

A
  • selective beta 3 receptor agonist
  • relaxes bladder detrusor muscle
  • effective for overactive bladde
46
Q

Adverse effects of Mirabegron

A
  • hypertension and tachycardia

- inhibits CYP2D6 (potential for drug interactions)

47
Q

Indirect acting Sympathomimetic Drugs

A
  • amphetamine and methamphetamine
  • tyramine
  • ephedrine
  • MOA inhibitors
  • Reserpine
  • Guanethidine and Bretylium
48
Q

Amphetamine and Methamphetamine

A
  • preipheral actions are mediated primarily through the release of catecholamines
  • central effects reflect release of several biogenic amines (Noradrenaline, dopamine, and serotonin)
49
Q

Tyramine

A
  • release stored catecholamines = norepinephrine

- by-product of tyrosine metabolism

50
Q

Ephedrine

A
  • direct mixed agonist (alpha and beta receptor)
  • enhances the release of norepinephrine
  • mild stimulant
51
Q

MAO Inhibitors (Selegiline)

A
  • two major subtypes -> A and B

- MAO-B inhibitor at low doses - allows MAO-A to continue functioning in the liver

52
Q

Reserpine

A
  • inactivates storage vessicle so that nerve terminals are unable to store catecholamines
  • causes catecholamine depletion (in CNS and peripherally)
  • very sedating
  • causes serious depression
53
Q

Guanethidine and Bretylium

A
  • prevent release of noradrenaline
  • used as antihypertensive
    (bretylium - used as antiarrythmic agent)
54
Q

non-selective competitive alpha antagonist

A
  • phentolamine
55
Q

Phentolamine therapeutic uses

A
  • pheochromocytoma
  • Male erectile disfunction
  • reverse severe local vasoconstriction caused by inadvertent infiltration of alpha agonists into subcutaneous tissue during intended intravenous administration
56
Q

Phentolamine adverse effects

A

severe tachycardia

57
Q

irreversible alpha 1 selective blocker

A
  • phenoxybenzamine
58
Q

Phenoxybezamine therapeutic uses

A
  • male erectile disfunction
59
Q

Phenoxybezamine adverse effects

A
  • postural hypotension and tachycardia (via baroreflex)
60
Q

Phentolamine pharmacology

A
  • inhibits response to serotonin

- may be an agongist at muscarinic and H1 and H2 histamine receptors

61
Q

Phentolamine pharmacology

A
  • inhibits reuptake of released norepinephrine
  • blocks histamine receptors
  • blocks acetylcholine receptors
  • blocks serotonin receptors
62
Q

Phenochromocytoma

A
  • tumor usually in the adrenal medulla

- releases a mixture of epinephrine and norepinephrine

63
Q

alpha 1 selective antagonists

A
  • Prazosin
64
Q

Prazosin Pharmacology

A
  • relaxes both arterial and venous smooth muscle

- extensively metabolized in humans

65
Q

Prazosin Adverse Effects

A
  • tachycardia (but less than other drugs)
  • postural hypotension
  • first dose effect (transient dizziness to syncope) more common in elderly patients
66
Q

Prazosin Uses:

A
  • hypertension (2nd or 3rd line)

- mild benigin prostatic hyperplasia

67
Q

Alpha 1 receptor subtypes

A

3 -> A,B,D

68
Q

alpha 1A receptor is on

A
  • peripheral arterial smoot muscle and veins

- predominate in the prostate and urethra

69
Q

alpha 1B receptor is on

A
  • CNS, spleen and lungs, and arteries and veins
70
Q

alpha 1D receptor is on

A
  • detrusor muscle of the the bladder
  • in the spinal cord
  • in the arteries and veins
    (relative proportion of B to A increases with age)
71
Q

Tamsulosin

A
  • competitive, selective for alpha 1 A and D over B

- therefore greater effect on prostate smooth muscle than vascular smooth muscle

72
Q

Tamsulosin Adverse Effects

A
  • little if any effect on BP

- causes a lot of dizzines

73
Q

Tamsulosin Uses

A
  • mild benign prostatic hyperplasia
74
Q

Effects of the beta blocker on the Heart

A
  • negative inotropic
  • negative chronotropic
  • slows atrioventricular conduction (AV node)
75
Q

Effects of the beta blocker on the Vasculature

A
  • opposes beta2-mediated vasodilation
76
Q

Effects of the beta blocker on Respiratory Tract

A
  • opposses beta2-mediated brochodilation
77
Q

Effects of the beta blocker on the Metabolic/Endrocrine

A
  • inhibit lipolysis and gylcogenolysis (type 1 diabetic beta2)
  • increased VLDL
  • decreased HDL
78
Q

Pharmacokinetic properties of specific beta blockers

A
  • ungergo first pass metabolism
  • first pass effect varies amoung individuals
  • variability in the plasma concentrations
  • dose requirements can vary greatly amoung individuals
79
Q

Propranolol

A
  • non-selective beta blocker

- extensive first pass metabolism

80
Q

Propranolol Adverse Effects

A
  • fatigue, dizziness, depression, nightmares, bradycardia

- increases triglyceride levels significantly

81
Q

Propranolol Uses

A
  • hypertension
  • angina
  • migraine (prophylaxis)
  • essential tremor
  • decrease sudden death after MI
  • severe hyperthyroidism
82
Q

Metoprolol

A
  • selective beta 1 blocker (no detectable partial agnost effect)
  • relative affinity for beta 1 and beta 2 receptors
83
Q

Metoprolol Adverse Effects

A
  • fatigue
  • dizziness
  • bradycardia
84
Q

Metoprolol Uses

A
  • hypertension
  • angina
  • after an MI
    (used preferably in patients with diabetes since beta 2 receptors in liver may play a role in recovery from hypoglycemia)
85
Q

Pure antagonsits vs partial agonists

A
  • partial agonists can weekly activate beta receptors
  • intrinsic sympathomimetic activity is desirable to prevent untoward effects like precipitation of asthma or excessive bradycardia
86
Q

Acebutolol

A
  • beta 1 selective antagonist with partial beta 1 agonist properties
  • low oral bioavailability
  • weak membrane stabilizing activity
87
Q

Acetbutolol Adverse Effects

A
  • fatigue and dizziness

- less likely to cause bradycardia and alter plasma lipids

88
Q

Acetbutolol Use

A
  • Hypertension

- Angina

89
Q

Local anesthetic membrane-stabilizing effect

A
  • typical local anesthtic blockade of sodium channels

- concentrations required, but not usually acheived

90
Q

Labetalol

A
  • racemic mixture of two pairs of chiral isomers
  • two isomers are elpha 1 selevtive blockers
  • one isomer is a non-selective beta blocker with some beta 2 agonist activity
91
Q

Labetalol Adverse Effects

A
  • hypotension (accompained by less tachycardia than occurs with a alpha blocker)
92
Q

Labetalol Use

A
  • hypertension (including hypertensive emergency and during pregnancy
93
Q

Uses for beta blockers

A
  • Hypertension
  • ischemic heart disease (angina)
  • cardiac arrhythmias
  • glaucoma
  • hyperthyroidism
  • neurologic diseases
  • beta 3 blockade
94
Q

How beta blockers work for hypertension

A
  • often used with either a diuretic or vasodilator
95
Q

How beta blockers work for ischemic heart disease (angina)

A
  • reduce the frequency of anginal episodes
  • improve exercise tolerance
  • act by decreasing cardiac work and oxygen demand
96
Q

How beta blockers work for cardiac arrhythmias

A
  • treatment of supraventricular and ventricular arrhythmias
  • increase atrioventricular nodal refractory period
  • slow ventricular response rates in atrial flutter and fibrilation
97
Q

How beta blockers work to treat glaucoma

A
  • decrease intraocular pressure (given locally in drop form)
98
Q

How beta blockers work to treat hyperthyroidism

A
  • block excessive catecholamine action
  • perhaps also inhibit conversion of thyroxine to triidothyronine (Propranolol used extensively for severe hyperthyroidism
99
Q

How beta blockers work to treat neurological diseases

A
  • reduce the frequency and intesity of migraine head aches (propranolol)
  • may reduce certain skeletal muscle tremors
  • low doses of propranolol may decrease symptoms of preformance anxiety
100
Q

Howo beta blockers are used to treat a alpha 3 receptor blockade

A
  • activate beta 3 receptor which may cause negative inotropihc effects in the hears
  • theoretically beta 3 might contribute to heart failure
  • there is no therapeutic use for selective beta 3 blockers

PHAR 341 - Pharmacology (7 decks)

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