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PDAT5 CV > 6 - Adrenergic Agonists & Antagonists > Flashcards

6 - Adrenergic Agonists & Antagonists Flashcards

1
Q

What drug class/categorization?

Tamsulosin
indoramin / urapidil

A

Alpha Adrenergic Receptor ANTAGONIST

A1-Selective

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2
Q

What is
EPINEPHRINE REVERSAL?

A

Since Epi stimulates Both a-NE & b-NE receptors…

but the dominant effect = ↑BP

  • *Alpha Effect (↑BP)**
  • *OVERWHELMS**
  • *B-NE effect** (Vasodilation -> ↓BP)

if EPI + a-NE ANTAGONIST are admin together –> lowered BP

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3
Q

What drug class/categorization?

EPINEPHRINE

A

ADRENERGIC AGONIST

Direct-Acting & A1/A2/B1/B2 non-selective

Catecholamine:
not orally, degraded by COMT & MAO

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4
Q

Beta Antagonist

Respiratory System Efects

A

Blockade of B2 Receptors in Bronchial Smooth Muscle:
↑Airway Resistance

Treatment of:
Angina / CHF following MI

Preferred are:
Selective B1 Antagonist = Metoprolol

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5
Q

What drug class/categorization?

Metoprolol** + **Esmolol

A

Beta Adrenergic Receptor ANTAGONIST

2st Gen = B1-Selective

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6
Q

What drug class/categorization?

Reserpine

A

NE ANTAGONIST

  • *Inhibit VMAT2**
  • depletes NT stores* –> ↓BP

not used often due to depression

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7
Q

What drug class/categorization?

Entacapone

A

ADRENERGIC AGONIST

Indirect Acting

COMT inhibitor

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8
Q

What Receptor?

Pancreatic Islets = INHIBITS Insulin Release

A

α2-Adrenoceptor Activation

found on BOTH :
PRE-synaptic neurons & POSTsynaptic cells

liver cells / plateles / smooth muscles of BV’s & CNS neurons

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9
Q

What Receptor?

Externam Bladder Sphincter = Urine Retention

Genitilia = Ejaculation

A

α1-Adrenoceptor Activation
alpha 1 = more CONTRACTION

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10
Q

What Receptor?

  • *GI Tract & Smooth Muscle Walls = RELAXES**
  • *(PRE-sympathetic Effect)**
A

α2-Adrenoceptor Activation

found on BOTH :
PRE-synaptic neurons & POSTsynaptic cells

liver cells / plateles / smooth muscles of BV’s & CNS neurons

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11
Q

What drug class/categorization?

Bisoprolol** + **Betaxolol
B-Olol

A

Beta Adrenergic Receptor ANTAGONIST

B1-Selective

Bisoprolol = 2nd gen

Betaxolol = 3rd Gen

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12
Q

What drug class/categorization?

Selegiline

A

ADRENERGIC AGONIST

Indirect Acting

MAO inhibitor

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13
Q

What drug class/categorization?

Cocaine

A

ADRENERGIC AGONIST

Indirect Acting

  • *Uptake Inhibitor**
  • Impair re-uptake of release catecholamines into sympathetic neurons*
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14
Q

What drug class/categorization?

EPHEDRINE

A

ADRENERGIC AGONIST

Mixed Acting

A1/A2/B1/B2 & Releasing Agent

Non-Catecholamine:
resist MAO oxidation

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15
Q

What Receptor?

Sympathetic Nerve Terminals = INHIBITS NorEpinephrine Release

A

α2-Adrenoceptor Activation

found on BOTH :
PRE-synaptic neurons & POSTsynaptic cells

liver cells / plateles / smooth muscles of BV’s & CNS neurons

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16
Q

What drug class/categorization?

-ZOSINS
Prazosin / Terazosin / Doxazosin
Alfuzosin / Bnazosin

A

Alpha Adrenergic Receptor ANTAGONIST

A1-Selective

Without A2-NE Blockade:
less TachyCardia & Palpitations

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17
Q

What Receptor?

  • *GI Tract**
  • *Relax Muscular Motility**
A

α1-Adrenoceptor Activation
alpha 1 = more CONTRACTION

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18
Q
  • *Adrenergic Agonist**
  • *Catecholamine Properties**
A

Metabolism:
inactive derivatives are formed
mainly metabolized by Hepatic COMT , some in BRAIN
MAO for some NT’s released from vesicles in nerve terminal

NOT GIVEN ORALLY
IV / IM / Topical / Sprays

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19
Q

What Receptor?

Skeletal Muscle Cells = Tremor / Glycogenolysis (HYPERglycemia)

A

β2-Adrenoceptor Activation​
B2 = more RELAXATION

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20
Q

What drug class/categorization?

Nadolol** / **Sotolol** / **Timolol“3-letter +olol, except for esmolol”
levobunolol / metipranolol

A

Beta Adrenergic Receptor ANTAGONIST

1st Gen = Non-Selective

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21
Q

What drug class/categorization?

Clonidine

A

ADRENERGIC AGONIST
Also Guanabenz

Direct-Acting & a2-Selective

↓BP
through central action ↓NE

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22
Q

What drug class/categorization?

Labetalol** + **Bucindolol

A

Beta Adrenergic Receptor ANTAGONIST

NON-Selective
3rd gen

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23
Q

What Receptor?

FAT CELLS = Lipolysis
TGs –> FFA’s

Fat Cells = THERMOGENESIS in skeletal muscle

A

β3-Adrenoceptor Activation​

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24
Q

What drug class/categorization?

Yohimbine

A

Alpha Adrenergic Receptor ANTAGONIST

A2-Selective

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25
Q

What Receptor?

Eye = ↓reduces production of aqueous formation
by decreasing CaMP

A

α2-Adrenoceptor Activation

found on BOTH :
PRE-synaptic neurons & POSTsynaptic cells

liver cells / plateles / smooth muscles of BV’s & CNS neurons

26
Q

What Receptor?

  • *Eye Pupil**
  • *Mydriasis (Dilation) / Raises Eyelid**
A

α1-Adrenoceptor Activation
alpha 1 = more CONTRACTION

27
Q
  • *Adrenergic Agonist**
  • *DIRECT ACTING**
A
  • *ONLY Ephedrine + NE** –> activate BOTH A+B receptors
  • NE has LOW affinity for b2 receptors*

PhenylEphrine –> A1

Clonidine –> A2

Dobutamine –> B1

Tertbutaline –> B2

28
Q

What Receptor?

Eye = Increased flow of AQUEOUS HUMOR
by increasing cAMP

A

β2-Adrenoceptor Activation​
B2 = more RELAXATION

29
Q

What drug class/categorization?

Atenolol** + **Acebutalol

“A - olol’s”

A

Beta Adrenergic Receptor ANTAGONIST

2st Gen = B1-Selective

30
Q

Denervation Supersensitivity
Adrenergic Nervous System = Receptor REGULATION

A

–motor nerve to effector organ is cut

–can be skeletal muscle or autonomic effector

–nerve allowed to degenerate

–no transmitter binding

–proliferation of receptors

–muscle gradually becomes extremely sensitive to neurotransmitter

–Example: restoring the secretion of acid from the stomach following vagotomy (severing the vagus nerve)

31
Q

Adrenergic Agonist
Non-Catecholamine Properties

A
  • not a catecholamine*
  • does NOT have 2 -OHs on Phenyl Ring*

Metabolism

  • *MAO** for ephedrine / phenylephrine
  • *Some RESIST Oxidation by MAO** = longer duration of action vs catecholamines

ORAL

32
Q

What drug class/categorization?

Celiprolol** + **Betaxolol** + **Nebivolol

A

Beta Adrenergic Receptor ANTAGONIST

B1-Selective

3rd Gen

33
Q

Beta Antagonist

w/ Alpha Antagonist Activity

A

Labetolol / Carvedilol

LESS TACHYCARDIA
useful in patients with:
Chronic Heart Failure

34
Q

What drug class/categorization?

IsoProterenol

A

ADRENERGIC AGONIST

Direct-Acting & B1/B2 non-selective

35
Q

What drug class/categorization?

NorEpinephrine

A

ADRENERGIC AGONIST

  • Direct-Acting &** A1/A2/B1 *non-selective
  • no B2 target like Epi*

Catecholamine:
not oral / COMT + MAO metabolism

36
Q

What Receptor?

Blood Vessels = Vasoconstriction
Arterioles & Veins

A

α1-Adrenoceptor Activation
alpha 1 = more CONTRACTION

37
Q

What Receptor?

Brain (medulla) = INHIBITS Sympathetic outflow

A

α2-Adrenoceptor Activation

found on BOTH :
PRE-synaptic neurons & POSTsynaptic cells

liver cells / plateles / smooth muscles of BV’s & CNS neurons

38
Q

Beta Antagonist

Ocular Effects

A

Blockade of B-receptors @ EYE
↓IntraOcular Pressure
reduction in aqueous humor production

Preferred:
Non-Selective Timolol & Levobunolol
&
Selective B1 Antagonist Betaxolol

39
Q

What Receptor?

Blood Platelets = Aggregation

A

α2-Adrenoceptor Activation

found on BOTH :
PRE-synaptic neurons & POSTsynaptic cells

liver cells / plateles / smooth muscles of BV’s & CNS neurons

40
Q

What Receptor?

Sweat = Apocrine Secretion

Skin (Pilomotor) = Goosebumps

A

α1-Adrenoceptor Activation
alpha 1 = more CONTRACTION

41
Q

What Receptor?

HEART

SA node = ↑Firing Rate

Ventricular Myocardium = ↑Force of Contraction

AV node = ↑conduction Velocity

A

β1-Adrenoceptor Activation​
responsible for HEART EFFECTS

b2 may contribute but are LESS important than B1

42
Q

What Receptor?

Spleen Capsule = Expels RBC

A

α1-Adrenoceptor Activation
alpha 1 = more CONTRACTION

43
Q
  • *Adrenergic Agonist**
  • *Mixed-Acting**
A

Indirectly Release NE & Directly Activate Receptors

Ephedrine
nasal decongestant / access CNS

Pseudoephedrine
less potent than ephedrine in producing: tachycardia / ↑BP / CNS stim

44
Q

What drug class/categorization?

OXYMETAZOLINE

A

ADRENERGIC AGONIST

Direct-Acting & A1/A2 non-selective

45
Q

Adrenergic Agonist
Indirect-Acting

A

↑NE or ↑Epi Availability
in the synapse to stim. adrenergic receptors

Amphetamine –> fascilitate NE release

Cocaine –> impair Re-uptake of catecholamines

Entacapone –/–> block COMT

Selegiline –/–> block MAO

46
Q

What drug class/categorization?

Phentolamine** / **Phenoxybenzamine

A

Alpha Adrenergic Receptor ANTAGONIST

NON-Selective

A1 Antagonist + A2-NE blockade:
stimulation of B1-NE receptors –> Tachycardia & Palpitations

47
Q

What drug class/categorization?

Amphetamine

A

ADRENERGIC AGONIST
also TYRAMINE

Indirect Acting

Releasing Agent
fascilitate NE release from sympathetic nerve endings

48
Q

What Receptor?

Kidney = RENIN RELEASE
(juxtaglomerular cells)

A

β1-Adrenoceptor Activation​
responsible for HEART EFFECTS

b2 may contribute but are LESS important than B1

49
Q

What Receptor?

  • *Detruser Muscle Bladder** = Relaxes
  • *INCREASES bladder capacity & prevents urination**
A

β3-Adrenoceptor Activation​

50
Q

What Receptor?

Uterine Smooth Muscle (Pregnant) = Relax

Bladder Wall = Relax

A

β2-Adrenoceptor Activation​
B2 = more RELAXATION

51
Q

What drug class/categorization?

PHENYLEPHRINE

A

ADRENERGIC AGONIST

Direct-Acting & a1-Selective

NON-catecholamine
resist MAO oxidation –> longer duration of action

52
Q

What Receptor?

Bronchial Muscles = Relaxes
receptors present but nerve innervation is SPARSE ~ indirect

A

β2-Adrenoceptor Activation​
B2 = more RELAXATION

53
Q

What drug class/categorization?

P - olol’s
All starting with P:
Penbutolol / Pindalol / Propranolol

A

Beta Adrenergic Receptor ANTAGONIST

1st Gen = Non-Selective

54
Q

What Receptor?

Liver = GlycoGenolysis
HYPERglycemia

A

BOTH

α1-Adrenoceptor Activation
alpha 1 = more CONTRACTION

β2-Adrenoceptor Activation​
B2 = more RELAXATION

55
Q

Beta Antagonist

w/ Partial AGONIST = ISA Activity

A

ISA = Intrinsic Sympathomimetic Activity

Useful in pts where:

  • *Bradycardia is undesirable** (HTN & ANGINA)
  • *Abnormalities in Plasma Lipids**

Ex.
PINDOLOL / ACEBUTOLOL / CARTEOLOL

56
Q

What drug class/categorization?

Carvedilol + Carteolol

A

Beta Adrenergic Receptor ANTAGONIST

NON-Selective
3rd gen

57
Q

What Receptor?

Skeletal Muscle Arterioles = VasoDILATION

Cardiac Muscle Arterioles = VasoDILATION

A

β2-Adrenoceptor Activation​
B2 = more RELAXATION

58
Q

What drug class/categorization?

Metyrosine

A

NE ANTAGONIST

  • *Inhibit Tyrosine Hydroxylase**
  • competitive inhibition* –> rate limiting step in catecholamine synth.

↓BP by reducing synthesis of:
↓dopamine ↓NE ↓Epi

59
Q

What drug class/categorization?

TERTBUTALINE

A

ADRENERGIC AGONIST

Direct-Acting & B2-Selective

relieves bronchoconstriction

60
Q

What drug class/categorization?

Dobutamine

A

ADRENERGIC AGONIST

Direct-Acting & B1-Selective

↑HR & ↑CO

61
Q

Beta Antagonist

CV System Effects

A

Chronically for ↓BP

  • *Heart (B1):**
  • *-NEG inotropic effect / chronotropic effect**
  • SLOWED* AV node conduction

Treatment of:
Angina / CHF following MI

62
Q

Beta Antagonist

Metabolic & Endocrine Effects

A

Chronic Use of B-Antagonist
associated with:
↑VLDL & ↓HDL
both UNFAVORABLE in CV disease

PDAT5 CV (30 decks)

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