Pharm Topic 10: Adrenoceptor Agonists And Antagonists

Front 1

Epinephrine (class, actions)

Back 1

Class - Directly acting Non-selective agonist
Receptors - all alphas and betas:
1) Increase HR
2) " BP
3) " contractility
4) " Cardiac output
5) " Blood glucose and lactic acid
6) Decreases peripheral cascular resistance slightly
7) Vasoconstriction
8) Vasodialation of skel muscle

Front 2

Epinephrine (Clinical uses, untoward effects, additional comments/administration)

Back 2

Uses:
-Wide angle glaucoma (A)
-Prolongs local anesthesia and keeps local (A)
-Anaphylactic shock
-Heart block or cardiac arrest (B)
-Bronchodialator for asthma (B)
-Increases blood sugar and FFAs (B)
Untoward:
-Tachycardia
-Palpitation
-Cardiac arrhythmias
-Cerebral hemorrhage
-Headache
-Tremor
-Restlessness
Not given orally, critical in anaphylaxis and cardiac arrest

Front 3

Norepinephrine (class, actions)

Back 3

Class - Direct acting non selective agonist
Receptors - A1-2, B1:
1) Increase both sys and dia BP
2) Vasoconstriction
3) Increase peripheral vascular resistance
4) Direct increase in HR and contraction
5) Indirect decrease in HR

Front 4

Norepinephrine (Clinical uses, untoward effects, additional comments/administration)

Back 4

Uses:
-Hypotension
Untoward effects: (same as epi + hypertension)
-Palpitation
-Caridiac arrhythmiass
-Cerebral hemorrhage
-Headache
-Tremor
-Restlessness
-Hypertension

Front 5

Isoproterenol (class, actions)

Back 5

Class - Direct acting Beta 1-2 agonist:
-Decreases peripheral vascular resistance
-Increases cardiac output
-Tachycardia
-Bronchodilation

Front 6

Isoproterenol (Clinical uses, untoward effects, additional comments/administration)

Back 6

Uses:
-Bronchodialator for asthma
-Heart block or cardiac arrest
-Shock
Untoward:
-Palpitations
-Tachcardia
-Headache
-Flushed skin
-Cardiac ischemia patients with coronary disease
Administered IV or inhilation for asthma

Front 7

Dobutamine (class, actions)

Back 7

Class - Direct B1 agonist:
-Increase contractility
-Minor increase in HR
-Increase AV conduction

Front 8

Dobutamine (Clinical uses, untoward effects, additional comments/administration)

Back 8

Uses:
-Short term treatment of cardiac decompensation post surgery
-Congestive heart failure or MI
Untoward:
-Increase in BP and HR
-Arrhythmias
Administered via continuous IV

Front 9

Direct Beta 2 agonists (Names, actions)

Back 9

Intermedaite acting - Albuterol, Metaproterenol, terbutaline, ritodrine.
Long acting - Formoterol, Salmeterol
-Relaxation of bronchial SM
-Relaxation of uterine SM
-Activation of other B2 receptors after systemic administration

Front 10

Direct Beta 2 agonsits (Name em, Clinical uses, untoward effects, additional comments/administration)

Back 10

Terbutaline, Albuterol, Metaproterenol, Formoterol, Salmeterol
Uses:
-(intermediates) Bronchodilation for asthma and COPD
-(intermediates) Acute bronchospasms
-Formeoterol and salmeterol used for asthma prophylaxis
-Ritodrine used to stop premature labor

Front 11

Phenylephrine (class, actions)

Back 11

Class - Direct A1 agonist
Action - Vasoconstriction

Front 12

Phenylephrine (Clinical uses, untoward effects, additional comments/administration)

Back 12

Uses:
-Nasal and conjunctival congestion
-Postural hypotension
-Hypotension post shock
Untoward:
-Hypertension
-Reflex brachycardia
-Dry mouth
-Sedation
-Rebound hypertension upon abrupt withdrawl
Administered orally

Front 13

Clonidine (class, actions)

Back 13

Class - Direct acting A2 agonist
Actions:
-Decrease sympa outflow from brain to periphery leading to decreased peripheral vascular resistance and BP
-Decreased production of aqueous humor

Front 14

Clonidine (Clinical uses, untoward effects, additional comments/administration)

Back 14

Uses:
-Adjunctive therapy in shock
-Hypertension
-Reduce sympa response in withdrawl from narcotics, alcohol, tobacco
-Glaucoma
Administered parenternal, oral

Front 15

Amphetamine, methamphetamine, Methyphenidate (class, actions)

Back 15

Class - Indirect acting by causing NT release:
-CNS stimulation
-Increases BP
-Myocardial stim

Front 16

Amphetamine, methamphetamine, Methyphenidate (Clinical uses, untoward effects, additional comments/administration)

Back 16

Uses:
-ADHD
-Narcolepsy
-Obesity (get tolerance)
Untoward:
-Restlessness
-Tremor
-Insomnia
-Anxiety
-Tachycardia
-Hyoertension
-Cardiac Arrhythmias
-Can lead to hemorrhagic stroke in peeps with inderlying disease.
Can cause tolerance and dependence. Long term use causes schizophrenia. Schedule 2 drugs.

Front 17

Dopamine (class, actions)

Back 17

Mixed acting A1-2, B1, Dopamine receptor agonist and causes NE release:
-Vasodialation of coronary, renal, and mesentaric beds
-Increased glomeruler filtration rate and natriuresis
-Increases HR and contractility
-Increases systolic BP

Front 18

Dopamine (Clinical uses, untoward effects, additional comments/administration)

Back 18

Uses:
-Cardiogenic shock
-Congestive Heart failure
-Acute renal failure
Untoward:
-High doses lead to vasoconstriction
Administered IV. Important for ability to maintain renal blood flow.

Front 19

Ephedrine (class, actions)

Back 19

Mixed acting A1-2, B1-2 agonist and causes NE release.
Actions like a long lasting epinephrine + CNS stimulation.

Front 20

Ephedrine (Clinical uses, untoward effects, additional comments/administration)

Back 20

Uses:
-Bronchodilator for asthma
-Nasal congestion
-Hypotension and shock
Untoward:
-Restlessness
-Tremor
-Insomnia
-Anxiety
-Tachycardia
-Hypertension
Administered by all routes

Front 21

A1 receptors (location and action)

Back 21

1) Non-skel muscle arteries and veins - Contraction
2) Heart - Increased contraction force
3) Eye - Dilation
4) GH, salivary, sweat, pancreas exocrine glands - Secretion
5) Uterus, Sphincters - Contraction
6) pilomotor muscles - Erects hair

Front 22

A2 receptors (location and action)

Back 22

1) Inhibits nori release to all organs
2) Pancrease - Inhibits B cells
3) Fat cells - inhibits lypolysis
4) Platelets - Aggregation

Front 23

B1 receptors (location and action)

Back 23

1) Heart - Increases HR, force, conduction vel, glycogenolysis
2) JG cells - Increases renin release

Front 24

B2 receptors (location and action)

Back 24

1) Skel arteries and veins - Relaxation
2) Eye - Relaxes ciliary muscle
3) Bronchiole and GI SM - Relaxation
4) Bladder, Uterus - Relaxation
5) Pancrease B cells - Insulin release
6) Growth hormone and other secretions - Inhibits
7) Liver - Activates glycogenolysis
8) Mast cells - Inhibits histamine relsease

Front 25

B3 receptors (location and action)

Back 25

Fat cells - Activatedd lipolysis

Front 26

Why cant you give catecholamines orally?

Back 26

B/c they are charged.

Front 27

Differences between Ephedrine and Epi

Back 27

1) Ephedrine is orally effective
2) " has a longer duration of action
3) " has a lower potency
4) " has greater CNS activity

Front 28

Catecholamine vs noncatecholamine characteristics and examples

Back 28

Catecholamines: Epi, Nori, Dopamine, Dobutamine, Isoproterenol.
-Rapid onset of action
-Brief duration
-Not administered orally
-Do not cross BBB
Non Catecholamines: All others
-Longer duration of action
-Can be given orally

Front 29

Cocaine mechanism

Back 29

Blocks reuptake 1 of Nori

Front 30

Phenoxybenzamine (class, effect)

Back 30

Class - Covalent, irreversible Alpha 1,2 blocker.
Causes decreased vascular resistance and increased HR due to reflex tachy as well as blocking A2 inhibition on catecholamine stim of heart.

Front 31

Phenoxybenzamine (therapeutic uses and side effects)

Back 31

Treats catecholamine excess and peripheral vascular disease
Can cause hypotension, tachycardia ect.. failure of ejaculation.

Front 32

Phentolamine (class, effect)

Back 32

Same as Phenoxybenzamine except shorter duration of action and competitive reversible inhibition.

Front 33

Prazosin (class, effect)

Back 33

A1 antagonist.
Decreases peripheral resistance by causing vasodilation of arteries and veins. (Doxasozin and terazosin do same thing)

Front 34

Prazosin (therapeutic uses and side effects)

Back 34

Used to treat hypertension and prostate hypertrophy.
Can get hypotension on first dose.

Front 35

Tamsulosin (class, effect)

Back 35

Alpha 1 (a and d specifically) antagonist.
Useful in treating prostatic hyperplasia and lower urinary tract symptoms.

Front 36

Yohimbine (class effect)

Back 36

Alpha 2 antagonist.

Front 37

Nadolol (class, antiarrythmic, partial agonist, additional actions)

Back 37

Non selective BB
Not antiarrythmic
Not partial agonist
Does not cross BBB

Front 38

Pindolol (class, antiarrythmic, partial agonist, additional actions)

Back 38

Non selective BB
Is Antiarrythmic
Is Partial Agonist
Has some sympa stim activity

Front 39

Propranolol (class, antiarrythmic, partial agonist, additional actions)

Back 39

Non selective BB
Is antiarrythmic
Not partial agonist

Front 40

Timolol (class, antiarrythmic, partial agonist, additional actions)

Back 40

Non selective BB
Not antiarythmic
Not partial agonist

Front 41

Metoprolol (class, antiarrythmic, partial agonist, additional actions)

Back 41

2nd gen B1 blocker
Is Antiarrythmic (@ high doeses)
Not partial agonist

Front 42

Carvedilol (class, antiarrythmic, partial agonist, additional actions)

Back 42

Non selective BB + A1 blocker
Is antiarrythmic
Not partial agonist
Also an antioxidant for heart failure

Front 43

Labetalol (class, antiarrythmic, partial agonist, additional actions)

Back 43

Non selective BB + A1 blocker
Is antiarrythmic
Is partial agonist

Front 44

Therapeutic uses of BBs

Back 44

Hypertension
Congestive heart failure
Arrythmias
Angina
Glaucoma
Migraine
Hyperthyroidism

Front 45

Side effects of BB's

Back 45

1) Decreases HR
2) Bronchoconstriction (counterindicated in asthma, COPD)
3) Masks symptoms of hypoglycemia
4) Causes CNS effects like fatigue and nightmares
5) NVDF (nausea, vomiting diarrhea, flatulence)

Front 46

How do BBs mask hypoglycemia

Back 46

Normally during hypoglycemia, when blood sugar drops, there is a reflex epi release which, in addition to increasing blood glucose, causes palpitations. Diabetics use these palpitations as an indicator that they are hypoglycemic. The blocking of the B1 effect of epi masks this.

Front 47

Angina, Chronic Angina, unstable angina, and variant/prizmetals angina

Back 47

Angina in general is sensation of pressure in chest region caused by inadequate coronary blood supply.
Chronic - Caused by fixed coronary stenosis. Often triggered by excersize and stress. BBs can treat.
Unstable Angina - Platelets can rupture and break off, can occur at rest, is an emergency. BBs can treat.
Variant angina - Occurs at rest b/c of a coronary spasm. Not treated with BBs.

Front 48

Reserpine (class, effect)

Back 48

Anti-adrenergic. Blocks uptake of catecholamines into vessicles causing depletion of vessivles (works peripheral and CNS)

Front 49

Reserpine (therapeutic uses, side effects)

Back 49

Used to treat hypertension
SE - Drowsiness, severe depression, parkinsonism, diarrhea, possibly breast cancer.

Front 50

Guanethidine/Guanadrel (class, effect)

Back 50

Anti-adrenergc. Displaces catecholamines in vesicles, prevents release of cats, and depletes stores of cats. Does not enter CNS

Front 51

Guanethidine/Guanadrel (therapeutic uses, side effects)

Back 51

Treats hypertension.
SE - Orthostatic hypotension, para dominance, inhibited ejac, decreased heart tone.

Front 52

Metatyrisine (class, effect)

Back 52

Anti-cholinergic. Inhibits Tyrosine hydroxylas, the RLS in cat synth, depleting cats.

Front 53

Metatyrisine (therapeutic uses, side effects)

Back 53

Used for inoperable pheochromocytoma.
SE - sedation, diarrhea, anxiety, crystalluria

Front 54

Methyldopa (class, effect)

Back 54

A2 agonist which reduces sympa outflow. Is a prodrug. Works in CNS similar to clonidine.

Front 55

Methyldopa (therapeutic uses, side effects)

Back 55

Used to treat hypertension
SE - Sedation, GI probs, liver probs, impotence