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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
Effects of alpha 2 receptors
- inhibition adrenergic and cholinergic transmitter release nerve terminals - contraction of vascular smooth muscle - (indirect) relaxation of GI smooth muscle - inhibits lipolysis from fats
26
Effects of beta 1 receptors
- positive chronotropy and inotropy
27
Effects of beta 2 receptors
- relaxation of the respiratory system - relaxation of the uterine system - relaxation (dilate) of vascular smooth muscle - uptakes K+ in the skeletal muscle
28
Effects of D1 receptors
- dilates renal vessels
29
Dopamine activates:
D1 and D2 and beta 1 receptors
30
Dopamine causes:
- relaxes vascular smooth muscle - suppresses norepinephrine release - dilates renal blood vessels - increase in force and rate of heart contraction
31
Dobutamine activates:
- alpha 1
32
Dobutamine uses:
- hypotensive emergencies to preserve cerebral and coronary blood flow
33
Selective alpha Agonists
- Phenylephrine | - Xylometrazoline/oxymetazoline
34
Phenylephrine
- selective alpha Agonist - dilates pupils - decogestant - can be used to raise blood pressure
35
Xylometazoline/Oxymetazoline
- topical decongestant - contricts the nasal mucosa oxymetazoline may cause hypotension due ti significant affinity for alpha 2 receptors
36
Selective alpha 2 agonists
- Clonidine
37
Effects of selective alpha 2 agonists
- decrease blood pressure through action in the CNS to decrease sympathetic output by decreasing chronotropy, inotropy, decrease vascular tone
38
Clonidine
- alpha 2 agonist - antihypertensive - reduces symptoms of alcohol and nicotine withdrawl - analgesic as an epidural
39
Side effects of Clonidine
Dry mouth and constipation (should be able to answer why?)
40
Selective beta receptor Agonists
- Isoproterenol
41
isoproterenol
- activates beta receptors - positive chronotrophic and inotropic actions - potent vasodilator - increases cardiac output - decrease diastolic or slight increase systolic pressure
42
Selective beta 2 receptor agonist
- salbutamol
43
Salbutamol
- selective beta 2 receptor agonist | - bronchodilator
44
Selective beta 3 receptor agents
- Mirabegron
45
Mirabegron
- selective beta 3 receptor agonist - relaxes bladder detrusor muscle - effective for overactive bladde
46
Adverse effects of Mirabegron
- hypertension and tachycardia | - inhibits CYP2D6 (potential for drug interactions)
47
Indirect acting Sympathomimetic Drugs
- amphetamine and methamphetamine - tyramine - ephedrine - MOA inhibitors - Reserpine - Guanethidine and Bretylium
48
Amphetamine and Methamphetamine
- preipheral actions are mediated primarily through the release of catecholamines - central effects reflect release of several biogenic amines (Noradrenaline, dopamine, and serotonin)
49
Tyramine
- release stored catecholamines = norepinephrine | - by-product of tyrosine metabolism
50
Ephedrine
- direct mixed agonist (alpha and beta receptor) - enhances the release of norepinephrine - mild stimulant
51
MAO Inhibitors (Selegiline)
- two major subtypes -> A and B | - MAO-B inhibitor at low doses - allows MAO-A to continue functioning in the liver
52
Reserpine
- 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
Guanethidine and Bretylium
- prevent release of noradrenaline - used as antihypertensive (bretylium - used as antiarrythmic agent)
54
non-selective competitive alpha antagonist
- phentolamine
55
Phentolamine therapeutic uses
- pheochromocytoma - Male erectile disfunction - reverse severe local vasoconstriction caused by inadvertent infiltration of alpha agonists into subcutaneous tissue during intended intravenous administration
56
Phentolamine adverse effects
severe tachycardia
57
irreversible alpha 1 selective blocker
- phenoxybenzamine
58
Phenoxybezamine therapeutic uses
- male erectile disfunction
59
Phenoxybezamine adverse effects
- postural hypotension and tachycardia (via baroreflex)
60
Phentolamine pharmacology
- inhibits response to serotonin | - may be an agongist at muscarinic and H1 and H2 histamine receptors
61
Phentolamine pharmacology
- inhibits reuptake of released norepinephrine - blocks histamine receptors - blocks acetylcholine receptors - blocks serotonin receptors
62
Phenochromocytoma
- tumor usually in the adrenal medulla | - releases a mixture of epinephrine and norepinephrine
63
alpha 1 selective antagonists
- Prazosin
64
Prazosin Pharmacology
- relaxes both arterial and venous smooth muscle | - extensively metabolized in humans
65
Prazosin Adverse Effects
- tachycardia (but less than other drugs) - postural hypotension - first dose effect (transient dizziness to syncope) more common in elderly patients
66
Prazosin Uses:
- hypertension (2nd or 3rd line) | - mild benigin prostatic hyperplasia
67
Alpha 1 receptor subtypes
3 -> A,B,D
68
alpha 1A receptor is on
- peripheral arterial smoot muscle and veins | - predominate in the prostate and urethra
69
alpha 1B receptor is on
- CNS, spleen and lungs, and arteries and veins
70
alpha 1D receptor is on
- 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
Tamsulosin
- competitive, selective for alpha 1 A and D over B | - therefore greater effect on prostate smooth muscle than vascular smooth muscle
72
Tamsulosin Adverse Effects
- little if any effect on BP | - causes a lot of dizzines
73
Tamsulosin Uses
- mild benign prostatic hyperplasia
74
Effects of the beta blocker on the Heart
- negative inotropic - negative chronotropic - slows atrioventricular conduction (AV node)
75
Effects of the beta blocker on the Vasculature
- opposes beta2-mediated vasodilation
76
Effects of the beta blocker on Respiratory Tract
- opposses beta2-mediated brochodilation
77
Effects of the beta blocker on the Metabolic/Endrocrine
- inhibit lipolysis and gylcogenolysis (type 1 diabetic beta2) - increased VLDL - decreased HDL
78
Pharmacokinetic properties of specific beta blockers
- ungergo first pass metabolism - first pass effect varies amoung individuals - variability in the plasma concentrations - dose requirements can vary greatly amoung individuals
79
Propranolol
- non-selective beta blocker | - extensive first pass metabolism
80
Propranolol Adverse Effects
- fatigue, dizziness, depression, nightmares, bradycardia | - increases triglyceride levels significantly
81
Propranolol Uses
- hypertension - angina - migraine (prophylaxis) - essential tremor - decrease sudden death after MI - severe hyperthyroidism
82
Metoprolol
- selective beta 1 blocker (no detectable partial agnost effect) - relative affinity for beta 1 and beta 2 receptors
83
Metoprolol Adverse Effects
- fatigue - dizziness - bradycardia
84
Metoprolol Uses
- 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
Pure antagonsits vs partial agonists
- partial agonists can weekly activate beta receptors - intrinsic sympathomimetic activity is desirable to prevent untoward effects like precipitation of asthma or excessive bradycardia
86
Acebutolol
- beta 1 selective antagonist with partial beta 1 agonist properties - low oral bioavailability - weak membrane stabilizing activity
87
Acetbutolol Adverse Effects
- fatigue and dizziness | - less likely to cause bradycardia and alter plasma lipids
88
Acetbutolol Use
- Hypertension | - Angina
89
Local anesthetic membrane-stabilizing effect
- typical local anesthtic blockade of sodium channels | - concentrations required, but not usually acheived
90
Labetalol
- 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
Labetalol Adverse Effects
- hypotension (accompained by less tachycardia than occurs with a alpha blocker)
92
Labetalol Use
- hypertension (including hypertensive emergency and during pregnancy
93
Uses for beta blockers
- Hypertension - ischemic heart disease (angina) - cardiac arrhythmias - glaucoma - hyperthyroidism - neurologic diseases - beta 3 blockade
94
How beta blockers work for hypertension
- often used with either a diuretic or vasodilator
95
How beta blockers work for ischemic heart disease (angina)
- reduce the frequency of anginal episodes - improve exercise tolerance - act by decreasing cardiac work and oxygen demand
96
How beta blockers work for cardiac arrhythmias
- treatment of supraventricular and ventricular arrhythmias - increase atrioventricular nodal refractory period - slow ventricular response rates in atrial flutter and fibrilation
97
How beta blockers work to treat glaucoma
- decrease intraocular pressure (given locally in drop form)
98
How beta blockers work to treat hyperthyroidism
- block excessive catecholamine action - perhaps also inhibit conversion of thyroxine to triidothyronine (Propranolol used extensively for severe hyperthyroidism
99
How beta blockers work to treat neurological diseases
- 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
Howo beta blockers are used to treat a alpha 3 receptor blockade
- 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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