Adrenergic Pharmacology Flashcards

Question 1

Q

Selected α1-adrenergic receptor roles

α_1A

α_1B

α_1D

Signal transduction mechanisms

Answer

A

Stimulation of PLC and calcium release

Question 2

Q

α_1A

Major roles

Answer

A

Cardiac hypertrophy

Prostate smooth muscle contraction

Urethral smooth muscle contraction

Question 3

Q

α_1B

Major roles

Answer

A

Contraction mesenteric arteries

Growth of adventitia after balloon-injury

Cardiac hypertrophy

Question 4

Q

α_1D

Major role

Answer

A

Contraction mesenteric arteries

Contraction of coronary/femoral arteries

Contraction of the bladder

Question 5

Q

α_2A

Signal Transduction Mechanism

Major effects

Answer

A

(Stimulates GIRK channel Inhibits L- and N-type VOCC)

(Inhibition of sympathetic outflow and NE release

Inhibition of insulin secretion

anesthetic-sparing effects )

Question 6

Q

α_{2A cont.}

Signal Transduction Mechanism

Major role

Answer

A

Inhibits adenylyl cyclase

Decreased lipolysis

Question 7

Q

α_2Acont.

Signal Transduction Mechanism

Major effects

Answer

A

Stimulates Na/H+ exchanger

Intestinal absorption of Na and water

Question 8

Q

α_2A

Signal Transduction Mechanism

(Major effects)

ALL

Answer

A

(Stimulates GIRK channel

Inhibits L- and N-type VOCC)

~~(Inhibition of sympathetic outflow and NE release. Inhibition of insulin secretion anesthetic-sparing effects )

Inhibits adenylyl cyclase (Decreased lipolysis)

Stimulates Na/H+ exchanger (Intestinal absorption of Na and water)

Question 9

Q

α_2B

Signal Transduction Mechanism

Major effects

Answer

A

Stimulates GIRK channel

Inhibits N-type VOCC

Analgesia, Sedation

Salt induced hypertension

Question 10

Q

α_{2B CONT}

Signal Transduction Mechanism

Major effects

Answer

A

Stimulates L-type VOCC

Contraction of some visceral arteries

Question 11

Q

α_2BCONT

Signal Transduction Mechanism

Major effects

Question 12

Q

**α_2B **

Signal Transduction Mechanism

Major effects

All

Answer

A

Stimulates GIRK channel

Inhibits N-type VOCC

(Analgesia, Sedation Salt induced hypertension)

Stimulates L-type VOCC

(Stimulates L-type VOCC)

Question 13

Q

α_2C

Signal Transduction Mechanism

Major effects

Answer

A

Stimulate GIRK channel.

Inhibit N-type calc channel

(CNS presynaptic inhibition

Inhibition of adrenal catecholamine release)

Question 14

Q

α_2C

Signal Transduction Mechanism

Major effects

Answer

A

Stimulates L-type VOCC

(Contraction of cutaneous, mesenteric, and sephanous veins)

Question 15

Q

α_2C

Signal Transduction Mechanism

Major effects

All

Answer

A

Stimulate GIRK channel

Inhibit N-type calc channel

(CNS presynaptic inhibition*
Inhibition of adrenal catecholamine release)*

Stimulates L-type VOCC

Contraction of cutaneous, mesenteric, and sephanous veins

Question 16

Q

β1

Signal transduction Mechanisms

Answer

A

Stimulates adenylyl cyclase

and L-type VOCC

Stimulates funny current

Stimulates SERCA

Question 17

Q

β1

Major roles

Answer

A

Stimulation of renin secretion

Reduction in heart cycle length

Stimulation of myocardial contraction

Hastens heart relaxation

Question 18

Q

β2

Signal transduction Mechanisms

Answer

A

Stimulates adenylyl cyclase and L-type VOCC

Question 19

Q

β2

Major roles

Answer

A

Relaxation of smooth muscles

Relaxation of bronchioles

Reduction in heart cycle length

Stimulation of myocardial contraction

Hastens myocardial relaxation

Lipolysis

Glycogenolysis

Stimulation of muscle anabolism

Question 20

Q

β3

Signal transduction Mechanisms

Answer

A

Stimulates adenylyl cyclase

Stimulates NO production

Question 21

Q

β3

Major roles

Answer

A

Relaxation of bladder

Relaxation of smooth muscles

Reduction of myocardial contraction

Question 22

Q

epinephrine (Adrenalin, Epipen)

Clinical uses

Pharmacologic effects

Answer

A

Clinical uses

hypersensitivity reaction, anaphylaxis, coupled with defibrillatory in cardiac arrest

hemostatic agent or with local anesthetics

peptic ulcer/gastrointestinal bleeding

nasal congestion, asthma

mydriasis for eye surgery

Pharmacologic effects

bronchodilation (β2)

vasoconstriction (α1) (α2)

cardiac stimulation (β1)

mydriasis (α1)

Question 23

Q

epinephrine (Adrenalin, Epipen)

Advantages

Precautions, adv reactions, interactions

Answer

A

Advantages

Act quick and for a short period of time

Precautions, adv reactions, interactions

no real contraindication in life-threatening situations

no Bronchodilatation in the presence of β-blockers

Cause hypertension in presence of β-blockers,

Avoid if patient takes MAO/COMT inhibitors

Question 24

Q

norepinephrine (Levophed)

Clinical uses

Pharmacologic effects

Answer

A

Clinical uses

neurogenic shock

sepsis

Pharmacologic effects

vasoconstriction (α1) (α2)

cardiac stimulation (β1)

Question 25

Q

norepinephrine (Levophed)

Advantages

Precautions, adv reactions, interactions

Answer

A

Advantages

acts quick and for a short period of time

Preferred to epinephrine, dobutamine, vasopressine, but any of those works.

However, dopamine which was traditionally used increase mortality rate significantly

Precautions, adv reactions, interactions

no real contraindication in life-threatening situations

Question 26

Q

phenylephrine

Clinical uses

Pharmacologic effects

Answer

A

Non-selective, yet favoring a1

Clinical uses

Nasal and eye congestion

Allergic conjunctivitis

Phenylephrine can be used for emergency hypotension

Pharmacologic effects

vasoconstriction (a1)

mydriasis (a1)

Question 27

Q

phenylephrine

Advantages

Precautions, adv reactions, interactions

Answer

A

Advantages

vasoconstriction is rapid and intense

Oxymetazoline has the highest efficacy

Phenylephrine has less central effects

Precautions, adv reactions, interactions

not for prolonged relief (<10 days)

rebound congestion (tachyphylaxis)

Question 28

Q

midodrine (Amatine, ProAmatine)

Clinical uses

Pharmacologic effects

Answer

A

Clinical uses

chronic orthostatic hypotension

hypotension due to autonomic neuropathy

Pharmacologic effects

Vasoconstriction (α1)

Question 29

Q

midodrine (Amatine, ProAmatine)

Advantages

Precautions, adv reactions, interactions

Answer

A

Advantages

Precautions, adv reactions, interactions

safety not established sufficiently!

efficacy not established sufficiently!

supine hypertension, pruritus, urinary retention in 10-20% of patients

Question 30

Q

Oxymetazoline

Answer

A

Selectivity

Non-selective, full a1 and partial a2A

High

Very low

Question 31

Q

clonidine (Catapres, Duraclon)

Clinical uses

Pharmacologic effects

Answer

A

Clinical uses

hypertension

cardiovascular symptoms of alcohol/narcotics/opioids withdrawal

adjunctive to relieve pain (reduce opioid requirement)

adjunctive in anesthesia (reduce anesthetic require)

diarrhea

Pharmacologic effects

Decrease sympathetic drive (a2)

Increase parasympathic outflow (a2)

Decrease norepinephrine release (a2)

Analgesia (a2)

Sedation (a2)

Stimulate intestin

Question 32

Q

clonidine (Catapres, Duraclon)

Advantages

Precautions, adv reactions, interactions

Answer

A

Advantages

dosing once a day

Precautions, adv reactions, interactions

may cause CNS depression

may reduce attentional performance

may cause sexual dysfunction in men

prone to rebound hypertension at withdrawal

Embryotoxic!

Question 33

Q

guanfacin (Intuniv,Tenex)

and ganabenz (Wytensin)

Clinical uses

Pharmacologic effects

Answer

A

Clinical uses

Hypertension

ADHD (in children only, is not a stimulant

Pharmacologic effects

Decrease sympathetic drive (a2)

Increase parasympathic outflow (a2)

Decrease norepinephrine release (a2)

Question 34

Q

guanfacin (Intuniv,Tenex)

and ganabenz (Wytensin)

Advantages

Precautions, adv reactions, interactions

Answer

A

Advantages

The a2A selectivity of Guanfacine does not impair attentional performance: clonidine and guanabenz do

Precautions, adv reactions, interactions

Caution in hypotention, cardiovascular and cerebrovascular disease, liver and renal impairement

Avoid use in elderly

may cause hypotension (<10 %), bradycardia (<2%), and sedation (5-45%)

Subject to rebound hypertension

Avoid combination with CYP inhibitors, sedatives, hypnotics, antidepressants, benzodiazepines

Question 35

Q

methyl-dopa (Aldomet, Aldoril, Dopamet)

Clinical uses

Pharmacologic effects

Answer

A

Clinical uses

Moderate to severe hypertention

Pregnancy-induced hypertension

Severe pre-eclampsia

hypertension during pregnancy

Pharmacologic effects

decrease sympathetic drive (a2)

increase parasympathetic outflow (a2)

decrease norepinephrine release (a2)

Question 36

Q

methyl-dopa (Aldomet, Aldoril, Dopamet)

Advantages

Precautions, adv reactions, interactions

Answer

A

Advantages

Not embryotoxic: clonidine, ganfacine and guanabenz are!

Precautions, adv reactions, interactions

avoid with liver and kidney diseases

Avoid in elderly because of CNS and cardiovascular effects

may cause liver and kidney toxicity

CNS depression

Hypotension and bradycardia

Question 37

Q

apraclonidine (Iopidine)

and brimonidine (Alphagan)

Clinical uses

Pharmacologic effects

Answer

A

Clinical uses

Reduction of intraocular pressure in open-angle glaucoma or ocular hypertension

Pharmacologic effects

Reduction of aqueous humor (a2)

Question 38

Q

apraclonidine (Iopidine)

and brimonidine (Alphagan)

Advantages

Precautions, adv reactions, interactions

Answer

A

Advantages

Apraclonidine don’t cross blood-brain

Precautions, adv reactions, interactions

CNS depression (5%), especially children (25-85%)

allergic conjunctivitis (>10%), visual disturbance (5-10%), Burning sensation (5-10%)

Dry mouth (5-10%)

Question 39

Q

Isoproterenol (Isuprel)

Clinical uses

Pharmacologic effects

Answer

A

Isoproterenol Low Low High High high Non-selective b

Clinical uses

cardiac resuscitation

Acute heart failure

Pharmacologic effects

Cardiac stimulation (b1)

Bronchodilation (b2)

Vasodilatation (b2) (b3)

Question 40

Q

Isoproterenol (Isuprel)

Advantages

Precautions, adv reactions, interactions

Answer

A

Advantages

Efficacy better than Dobutamine, but does it worth the risks!

Precautions, adv reactions, interactions

Avoid with preexisting angina, tachyarrhythmias, coronary artery disease, diabetes, distributive shocks

May cause angina, hyper/hypotension, tachyarrhythmias, hypokalemia, hyperglycemia, dypnea, pulmonary edema ….

Cardiac ischemia may occur

Question 41

Q

Dobutamine (Dobutrex)

Clinical uses

Pharmacologic effects

Answer

A

Clinical uses

Acute heart failure

Cardiogenic shock

Pharmacologic effects

Cardiac stimulation (α1, b1)

Vasoconstriction (α1)

Advantages

Increase cardiac output with little vasoconstriction compared to NEPI

Precautions, adv reactions, interactions

Similar to isoproterenol, but with a much lower incidence

Question 42

Q

albuterol (Ventolin, Proventil, AccuNeb, Vospire) and

Terbutaline (Brethine, Bricanyl)

B2

Answer

A

Clinical uses

asthma

Pharmacologic effects

Bronchodilatation (b2)

Advantages

Act quick

Precautions, adv reactions, interactions

tremors, restlessness

hypotension, tachycardia

hyperglycemia, hyperlipidemia

decreases concentration of K

Question 43

Q

Salmeterol (Serevent, Seretide*, Advair**) and

Formoterol (Foradil,Symbicort*)

Answer

A

Clinical uses

adjunctive treatment of asthma

Prevention/not treatment of exertion-induced bronchospasm

Pharmacologic effects

Bronchodilatation (b2)

Advantages

Only for uncontrolled asthma

Salmeterol is 10000X more lipophilic than Albuterol

Formoterol has low efficacy toward internalization of the receptor

Precautions, adv reactions, interactions

Same as Albuterol

May increase asthma-related death!

Question 44

Q

Phenoxybenzamine (Irreversible a antagonist) and

Phentolamine (Non-selective a antagonist)

Answer

A

Clinical uses

Preoperative in pheochromocytoma (both)

Adjunctive treatment if pheochromocytoma is inoperable

Prevention of necrosis in case of extravasation of sympathomimetics

Pharmacologic effects

hypotension (α1)

vasodilatation of arteries and veins (α1)

depression baroreflex (α1)

Advantages

phentolamine is reversible

Disadvantages

effects of phenoxybenzamine last more than 24 hrs

hypotension, tachycardia

extreame nasal stuffiness

Question 45

Q

Prazosin a1

Doxazosin a1

**Antagonist **

Answer

A

Clinical uses

benign prostate hyperplasia

alternative treatment of hypertension

Pharmacologic effects

hypotension (α1)

relaxation of smooth muscle (α1)

depression baroreflex (α1)

Advantages

Terazosine and Doxazosin are taken once daily

Disadvantages

Prazosin needs to be taken several times/day

very strong first dose effect! dizziness 50%, even syncope

Nasal stuffiness

Hypotension, tachycardia

Question 46

Q

Alfuzosin

Silodosin

**a1 antagonist **

Answer

A

Clinical uses

benign prostate hyperplasia

Pharmacologic effects

relaxation of prostate smooth muscle (α1)

Advantages

Selective for prostate

lesser first dose effects

Alfuzosin also induce apoptosis of prostate smooth muscle

Disadvantages

Same side effects as prazosin,

but in less patients and to a lesser degree

Question 47

Q

propranolol (Na channel blockade)

timolol (No)

Selective for b1, b2

Answer

A

Clinical uses

Adjunctive or alternative treatment of hypertension

Angina pectoris

tachycardia

Myocardial infarction

Timolol is used for intraocular hypertention

Propranolol is used for situational anxiety

Pharmacologic effects

Reduction of heart rate (β1)

Reduction of ventricular contraction (β1)

Reduction of renin release (β1)

*Reduce aqueous humor (?)

Reduce anxiety (β1 and others)

Advantages

They “work” !!! Especially propranolol

Timolol may be less prone to side effects

Precautions, adv reactions, interactions

Cross BBB and cause dizziness (<10%), insomnia (<5%), depression (<5%)

May cause Bradycardia, Heart failure, Bronchospasms

May potentiate, and mask, signs of hypoglycemia in diabetic

May prevent effect of epinephrine in anaphylaxis

These effects are more prevalent for propranolol

Question 48

Q

pindolol

Selective for b1, b2

**Antagonsit **

Partial β1 agonist

Partial β3 agonist

Na channel blockade

NO production

Answer

A

Clinical uses

Adjunctive abd alternative treatment of hypertension

Alternative treatment of hypertension

Tachycardia

Situational anxiety

Pharmacologic effects

Reduction of heart rate (partial β1 agonist)

Reduction of ventricular contraction (partial β1 agonist)

Reduction of renin release (partial β1 agonist)

Vasodilatation ( partial β3 agonist)

Advantages

Maintains partial receptor functions

Marginally affects basal, but prevents the consequence of elevated sympathetic drive

Less subject to rebound tachycardia & hypertension

Precautions, adv reactions, interactions

“Lesser efficacy” than propranolol,

>>> yet slightly higher prevalence of side effects

Insomnia (> 10%), dizziness (<10%), fatigue (<10%) and depression (up to 8%)

Question 49

Q

bisoprolol no

metoprolol (Na channel blockade +/-)

Selective for b1 Antagonist

Answer

A

Clinical use

Adjunctive or alternative treatment of hypertension

Angina pectoris

Metoprolol is used in hemodynamically stable, acute myocardial infarction (iv)

reduces mortality/hospitalization in patients with heart failure in patient already receiving ACE inhibitors, diuretics, and/or digoxin

Pharmacologic effect (Receptor)

Reduction of heart rate (β1)

Reduction of ventricular contraction (β1)

Reduction of renin release (β1)

Side effects and drug interactions

Metabolism and kinetic

Hypotension, Bradychardia

Dizziness or Fatigue

More with Metroprolol

Metoprolol cross BBB

Question 50

Q

Esmolol no

Selective for b

Answer

A

Clinical use

Intraoperative tachycardia

Supraventricular tachycardia

Atrial fibrillation/flutter

SVT and post-operative hypertension in children

Pharmacologic effect (Receptor)

Reduction of heart rate (β1)

Reduction of ventricular contraction (β1)

Side effects and drug interactions

None that will last

Hypotension (less than 10%)

Question 51

Q

Nebivolol

Best b1 over b2 selectivity

Moderate β3

Partial β3 agonist

NO production

Answer

A

Clinical uses

Adjunctive treatment of hypertension

Alternative treatment of hypertension

stable Heart failure

Pharmacologic effects

Reduction of heart rate (β1)

Reduction of ventricular contraction (β1)

Vasodilatation (partial β3 agonist, which activate nitric oxide synthase)

Antioxidant (NADPH oxidase inhibitor)

Advantages

Well tolerated

Marginally more potent than the first generation

Promotes NO release (an advantage in elderly)

Precautions, adv reactions, interactions

headache (< 10%), dizziness (<5%), fatigue (<5%)

Question 52

Q

labetolol

Weakest selectivity, but favors b1, b2

Partial β2 agonist

Partial β3 agonist*

a1 antagonist

Na channel blockade

NO production

Answer

A

Clinical use

Adjunctive treatment of hypertension

Alternative treatment of hypertension

Hypertensive emergency

Pediatric hypertension

hypertension of pregnancy

Pharmacologic effect (Receptor)

Reduction of heart rate (β1)

Reduction of ventricular contraction (β1)

Not as much as propranolol

Vasodilatation (α1) (β2) (β3)

Side effects and drug interactions

Hypotension (up to 58%)

dizziness (up to 20%)

Nausea (up to 19%)

Fatigue (up to 11%)

Metabolism and kinetic

Negligible amount cross BBB

Question 53

Q

Carvedilol

Weakest selectivity, but favors b1, b2

a1 antagonist

Na channel blockade

Ca channel blockade

Answer

A

Clinical use

Adjunctive treatment of hypertension

Alternative treatment of hypertension

Mild to severe heart failure

Left ventricular dysfunction following myocardial infarction

Angina pectoris

Pharmacologic effect (Receptor)

Reduction of heart rate (β1)

Reduction of ventricular contraction (β1)

Vasodilatation (α1)

Antioxidant

Anti-proliferative

Side effects and drug interactions

Dizziness (up to 30%)

Fatigue (up to 24%)

Hypotension (up to 20%)

Weight gain and diarrhea (up to 12%)

Weakness, bradychardia (up to 10%)

Metabolism and kinetic

Cross BBB

Question 54

Q

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Adrenergic Pharmacology Flashcards

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