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Pharm Exam 3 > 6 - Sympatholytic Pharmacology > Flashcards

6 - Sympatholytic Pharmacology Flashcards

1
Q

Receptor agonists for Sympathetic NS activate what signal transducton cascade (ex. a1 receptor)

A

Gq -> PLC –> IP3 and DAG

IP3–> Increase Ca++

DAG –> activate Protein Kinase C

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2
Q

Receptor antagonists block ______

A

agonist binding to the receptor

(antagonize the effect of agonist, not the receptor itself)

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3
Q

What effect would antagonist alone have on receptor activation?

A

None!

If no agonist, no action

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4
Q

nonselective alpha antagonists

A

Phenoxybenzamine

Phentolamine

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5
Q

a1 receptor antagonists

A

Prazosin

Terazosin

Doxazosin

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6
Q

AE’s of a1 antagonists

A
  1. Orthostatic HoTN**
  2. Inhibition of ejaculation
  3. Nasal congestion
  4. Reflex tachycardia
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7
Q

Clinical uses for a1/2 receptor antagonists

A
  • Pheo
  • Hypertensive crisis

(Phentolamine also used for male impotence)

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8
Q

a1 antagonists are all ____ adminstered except _____

A

orally

Phentolamine (parrenteral)

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9
Q

____ can be relieved with a1 blockers to cause __________

A

BPH

bladder base relaxation

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10
Q

Non-selective alpha receptor groups

A

B haloalkylamines (Phenoxybenzamine)

Imidazolines (phentolamine)

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11
Q

Phenoxybenzamine effects

A

Also blocks receptors for:

  • Ach
  • Histamine
  • Serotonin
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12
Q

Phenoxybenzamine PD

A

irreversible antagonist = covalent binding to receptor is permanent

***Therefore very LONG duration

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13
Q

Competitive (reversible) non-selective alpha receptor blocker

A

Phentolamine

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14
Q

Phentolamine is a _____ but induces ______

A

potent vasodilator

Induces pronounced reflex tachyardia

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15
Q

Phentolamine also blocks..

A

5HT receptors

and is a muscarinic and histamine receptor agonist

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16
Q

Phentolamine block of _____ may promote release of NE

A

presynaptic a2

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17
Q

Components of Quinazolines

A

Quinazoline ring

Piperazine ring

Acyl moiety

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18
Q

Quinazolines vary in

A

half life

Praz = 3h

Teraz = 12h

Doxaz = 20h

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19
Q

Quinazolines undergo extensive

A

metabolism, excreted in bile

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20
Q

Quinazoline effects

A

Vasodilation

relaxation of sm. muscle in enlarged prostate and in bladder base

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21
Q

Quinazolines exhibit _____

A

“first dose” effect

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22
Q

Quinazolines are all _______

A

a1 antagonists

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23
Q

Yohimbe MOA

A

blocks a2 receptors = increase symptathetic discharge

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24
Q

Aryloxypropanolamines structure

A

Aromatic ring attached to non-carbon atom in side chain

R group (bulky alkyl group…isopropy or tert-butyl) on a terminal NH group

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25
Q

Aryloxypropanolamines general function

A

B receptor antagonists

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26
Q

Nonselective B agonists

A
  • Propanolol
  • Nadolol
  • Timolol
  • Pindolol
  • Carteolol
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27
Q

Nonselective B antagonists - 2 properties

A

Lipophilic

Local anesthetic properties

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28
Q

B antagonist blockde is _________

A

activity-dependent

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29
Q

B antagonists (e.g. Propanolol) pharmacologial effects (6)

A
  1. Decreased CO (and HR)
  2. Decreased Renin release (imp. for HTN relief)
  3. Increase VLDL, Decrease HDL
  4. Inhibit lipolysis
  5. Inhibit compensatory glycogenolysis during Hypoglycemia
  6. Increase bronchial resistance
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30
Q

Positive effects of nonselectve B blockers on Heart Failure is largely due to _____

A

decreases in the RAAS

Ultimately lowers vasoconstruction (AT2) and fluid volume (aldosterone)

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31
Q

8 Therapeutic uses for nonselective B blockers (propanolol)

A
  1. HTN
  2. angina
  3. arrythmia
  4. CHF (types 1 and 2)
  5. glaucoma
  6. migraine
  7. stage fright
  8. thyrotoxicosis
32
Q

Non-selective B adrenergic receptor antagonists that are NOT propanolol

A

Nadolol

Timolol

Pindolol

33
Q

Nadolol is less ____

A

lipophilic than propanolol

34
Q

Nadolol PK

A

Long T1/2 (20h)

Mostly excreted unchanged in urine

35
Q

Nadolol use

A

HTN

Migraine

Angina

36
Q

Timolol structure

A

thiadiazole nucleus with morpholine ring

37
Q

Timolol uses

A

HTN

Angina

Migraine
GLAUCOMA

38
Q

How will B blockers affect pupil size

A

they wont!

Doesn’t have same effect as cholinergic

39
Q

Pindolol possesses ________

It is a _________

A

intrinsic sympathomimetic activity (ISA)

partial agonist

40
Q

Pindolol less likely to…

A

cause bradycardia and lipid abnormalities

41
Q

Pindolol use

A

HTN, angina, migraine

42
Q

(PIndolol) Dose response curves and partial agonists

A

****REVIEW SLIDE****

43
Q

Drugs that possess intrinsic sympathomimetic activity

A

ISA

44
Q

Nonselective B partial agonists

A

Pindolol and Carteolol

45
Q

Carteolol less likely to cause ______

A

bradycardia and lipid abnormalities

46
Q

Carteolol use

A

HTN and glaucoma

47
Q

Nonseletive B antagonists that are used in glaucoma

A

Timolol, Carteolol

48
Q

Selective B1 antagonists are considered ______

Examples?

A

Cardioselective

  1. Metoprolol
  2. Bisoprolol
  3. Atenolol
  4. Esmolol
  5. Nebivolol
49
Q

3rd gen B1 selective antagonists

A

Nebivolol

50
Q

Very short acting B1 selective antagonist

A

Esmolol

(half life 9 minutes)

51
Q

Moderate lipophilicity B1 selective antagonists

A

Metoprolol and bisoprolol

52
Q

Which B1 selective antagonist has significant first pass metabolism

A

Metoprolol, bisoprolol

53
Q

Esmolol metabolism

A

undergoes rapid metabolism by esterases in RBC’s

54
Q

Metoprolol and bisoprolol use

A

HTN

angina

CHF

antiarrhythmic

55
Q

Atenolol use

A

HTN, angina

56
Q

Esmolol use

A

SVT

Afib/Aflutter

Peri-op HTN

57
Q

Nebivolol causes…

Use?

A

vasodilaion due to nitric oxide production

**used for HTn

58
Q

Mechanisms underlying vasodilating actions of B blockers

A

Ca++ –X-> L-type VGCC –> Intracell. Ca++ –> Contraction

Vasodilation occurs via two pathways

  • B2 Agonist – functions via cAMP
  • NO – functions via cGMP
59
Q

Mixed adrenergic receptor antagonists

A

Labetalol

Carvedilol

60
Q

Labetalol is a _____ mixture

A

racemic

61
Q

Labetalol structure

A

Two asymmetric carbons

(1 and 1’)

62
Q

Isomers of labetalol

A

1S, 1’R = a1 block

both 1 + 1’ R = B block

63
Q

where does the ‘mixed’ effect come into play with labetalol

A

The blockade of B (nonselective) stops the reflex tachycardia you’d normally expect with an a1 blocker

64
Q

Labetalol use

A

HTN, hypertensive crisis

65
Q

Carvedilol isomers effects

A

Both enatomers block a1

Only S-enantiomer blocks B

66
Q

Mixed effect for carvedilol

A

Nonselective bet blocking prevents reflex tachycardia from a1 block

67
Q

Carvedilol use

A

HTN, CHF 1 and 2

68
Q

5 AE’s of beta blockers

A
  1. Bradycardia
  2. AV block
  3. sedation
  4. mask hypoglycemia Sx
  5. WIthdrawal
69
Q

Chronic B blockade results in …

A

pronounced withdrawal due to upregulation of the B receptors

70
Q

CI’s for beta blockers

A

Asthma, COPD, CHF type 4 (final stage)

71
Q

Catecholamine depleter

A

reserpine

72
Q

Reserpine MOA

A

block vesicular monoamine transporters (NET, DAT)

Depletes vesicular pool of NE!

73
Q

Reserpine PK

A

slow onset, sustained effect (weeks)

74
Q

Reserpine use

A

HTN treatment (refractory)

75
Q

Due to it’s slow onset of action, reserpine will _______

A

NOT activate the baroreceptor response

Pharm Exam 3 (11 decks)

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