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PDAT5 CV > 6 - Adrenergic Agonists & Antagonists > Flashcards

6 - Adrenergic Agonists & Antagonists Flashcards

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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
What Receptor? **Eye = *↓******reduces* production of aqueous formation** by ***decreasing CaMP***
**_α2-Adrenoceptor Activation_** found on **BOTH : PRE-synaptic neurons & POSTsynaptic cells** liver cells / plateles / smooth muscles of BV's & CNS neurons
26
What Receptor? * *Eye Pupil** * *Mydriasis (Dilation) / Raises Eyelid**
**_α1-Adrenoceptor Activation_** alpha 1 = more CONTRACTION
27
* *_Adrenergic Agonist_** * *DIRECT ACTING**
* *ONLY Ephedrine + NE** --\> activate **BOTH A+B receptors** * NE has LOW affinity for b2 receptors* ## Footnote **PhenylEphrine --\> A1** **Clonidine --\> A2** **Dobutamine --\> B1** **Tertbutaline --\> B2**
28
What Receptor? **Eye = Increased flow of AQUEOUS HUMOR** by increasing cAMP
**_β2-Adrenoceptor Activation​_** B2 = more RELAXATION
29
**What drug class/categorization?** **_Atenolol**_ + _**Acebutalol_** "A - olol's"
**_Beta Adrenergic Receptor *ANTAGONIST*_** **2st Gen = B1-Selective**
30
**Denervation Supersensitivity** Adrenergic Nervous System = Receptor REGULATION
–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
**_Adrenergic Agonist_ Non-Catecholamine Properties**
* 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
**What drug class/categorization?** **_Celiprolol**_ + _**Betaxolol**_ + _**Nebivolol_**
**_Beta Adrenergic Receptor *ANTAGONIST*_** **B1-Selective** 3rd Gen
33
**_Beta Antagonist_** ## Footnote **w/ Alpha Antagonist Activity**
**Labetolol / Carvedilol** ***LESS TACHYCARDIA*** useful in patients with: **_Chronic Heart Failure_**
34
**What drug class/categorization?** **_IsoProterenol_**
**_ADRENERGIC AGONIST_** **Direct-Acting &** **B1/B2 *non-selective***
35
**What drug class/categorization?** **_NorEpinephrine_**
**_ADRENERGIC AGONIST_** * *Direct-Acting &** **A1/A2/B1 *non-selective*** * no B2 target like Epi* Catecholamine: *not oral / COMT + MAO metabolism*
36
What Receptor? **Blood Vessels** = **Vasoconstriction** Arterioles & Veins
**_α1-Adrenoceptor Activation_** alpha 1 = more CONTRACTION
37
What Receptor? **Brain (medulla) = *INHIBITS* Sympathetic outflow**
**_α2-Adrenoceptor Activation_** found on **BOTH : PRE-synaptic neurons & POSTsynaptic cells** liver cells / plateles / smooth muscles of BV's & CNS neurons
38
**_Beta Antagonist_** ## Footnote **Ocular Effects**
**Blockade of B-receptors** @ **EYE** ↓**IntraOcular Pressure** *reduction in **aqueous humor production*** Preferred: **Non-Selective _Timolol & Levobunolol_** & **Selective B1 Antagonist _Betaxolol_**
39
What Receptor? **Blood Platelets** = **Aggregation**
**_α2-Adrenoceptor Activation_** found on **BOTH : PRE-synaptic neurons & POSTsynaptic cells** liver cells / plateles / smooth muscles of BV's & CNS neurons
40
What Receptor? **Sweat = Apocrine Secretion** **Skin (Pilomotor) = Goosebumps**
**_α1-Adrenoceptor Activation_** alpha 1 = more CONTRACTION
41
What Receptor? **HEART** **SA node = ↑Firing Rate** **Ventricular Myocardium = ↑Force of Contraction** **AV node = ↑conduction Velocity**
**_β1-Adrenoceptor Activation​_** responsible for HEART EFFECTS *b2 may contribute but are LESS important than B1*
42
What Receptor? **Spleen Capsule = Expels RBC**
**_α1-Adrenoceptor Activation_** alpha 1 = more CONTRACTION
43
* *_Adrenergic Agonist_** * *Mixed-Acting**
***Indirectly* Release NE** & **Directly Activate Receptors** **_Ephedrine_** nasal decongestant / access CNS **_Pseudoephedrine_** less potent than ephedrine in producing: tachycardia / ↑BP / CNS stim
44
**What drug class/categorization?** **_OXYMETAZOLINE_**
**_ADRENERGIC AGONIST_** **Direct-Acting &** **A1/A2 *non-selective***
45
**_Adrenergic Agonist_ Indirect-Acting**
**_↑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
**What drug class/categorization?** **_Phentolamine**_ / _**Phenoxybenzamine_**
**_Alpha Adrenergic Receptor *ANTAGONIST*_** **NON-Selective** **A1 Antagonist** **+ A2-NE blockade**: stimulation of **B1-NE receptors** --\> **Tachycardia & Palpitations**
47
**What drug class/categorization?** **_Amphetamine_**
**_ADRENERGIC AGONIST_** also **TYRAMINE** ***Indirect Acting*** **Releasing Agent** fascilitate **NE** release from sympathetic nerve endings
48
What Receptor? **Kidney = RENIN RELEASE** (juxtaglomerular cells)
**_β1-Adrenoceptor Activation​_** responsible for HEART EFFECTS *b2 may contribute but are LESS important than B1*
49
What Receptor? * *_Detruser Muscle Bladder_** = **Relaxes** * *INCREASES bladder capacity & prevents urination**
**_β3-Adrenoceptor Activation​_**
50
What Receptor? **Uterine Smooth Muscle (Pregnant) = Relax** **Bladder Wall = Relax**
**_β2-Adrenoceptor Activation​_** B2 = more RELAXATION
51
**What drug class/categorization?** **_PHENYLEPHRINE_**
**_ADRENERGIC AGONIST_** **Direct-Acting &** **a1-Selective** **NON-catecholamine** resist MAO oxidation --\> longer duration of action
52
What Receptor? **Bronchial Muscles = Relaxes** receptors present but nerve innervation is SPARSE ~ indirect
**_β2-Adrenoceptor Activation​_** B2 = more RELAXATION
53
**What drug class/categorization?** **_P - olol's_** All starting with P: Penbutolol / Pindalol / Propranolol
**_Beta Adrenergic Receptor *ANTAGONIST*_** **1st Gen = Non-Selective**
54
What Receptor? **Liver = GlycoGenolysis** HYPERglycemia
**BOTH** **_α1-Adrenoceptor Activation_** alpha 1 = more CONTRACTION **_β2-Adrenoceptor Activation​_** B2 = more RELAXATION
55
**_Beta Antagonist_** **w/ Partial _AGONIST_** = **ISA Activity**
**ISA = Intrinsic Sympathomimetic Activity** Useful in pts where: * *Bradycardia is undesirable** (HTN & ANGINA) * *Abnormalities in Plasma Lipids** Ex. **PINDOLOL / ACEBUTOLOL / CARTEOLOL**
56
**What drug class/categorization?** **_Carvedilol_** + **_Carteolol_**
**_Beta Adrenergic Receptor *ANTAGONIST*_** **NON-Selective** 3rd gen
57
What Receptor? **Skeletal Muscle Arterioles = VasoDILATION** **Cardiac Muscle Arterioles = VasoDILATION**
**_β2-Adrenoceptor Activation​_** B2 = more RELAXATION
58
**What drug class/categorization?** **_Metyrosine_**
**_NE *ANTAGONIST*_** * *_*Inhibit* Tyrosine Hydroxylase_** * competitive inhibition* --\> **rate limiting step in catecholamine synth.** ↓**BP** by reducing synthesis of: ↓dopamine ↓NE ↓Epi
59
**What drug class/categorization?** **_TERTBUTALINE_**
**_ADRENERGIC AGONIST_** **Direct-Acting & B2****-Selective** *relieves bronchoconstriction*
60
**What drug class/categorization?** **_Dobutamine_**
**_ADRENERGIC AGONIST_** **Direct-Acting & B****1-Selective** ↑HR & ↑CO
61
**_Beta Antagonist_** ## Footnote **CV System Effects**
Chronically for ↓**BP** * *Heart (B1):** * *-NEG inotropic effect / chronotropic effect** * **SLOWED* AV node conduction** Treatment of: **Angina / CHF following MI**
62
**_Beta Antagonist_** ## Footnote **Metabolic & Endocrine Effects**
**Chronic Use of B-Antagonist** associated with: ↑**VLDL** & ↓**HDL** *both UNFAVORABLE in CV disease*

PDAT5 CV (30 decks)

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