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PHRM 825 > ANS - 9 > Flashcards

ANS - 9 Flashcards

1
Q

What effect would an antagonist alone have on receptor activation?

A

no effect

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2
Q

Side effects of a1 receptor antagonists:

A
  • orthostatic hypotension
  • inhibition of ejaculation
  • nasal stuffiness
  • tachycardia
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3
Q

Non-selective a-adrenergic receptor antagonists: What is this base structure?

A

B-Haloalkylamines

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4
Q

non-selective a receptor antagonists examples

A
  • Phenoxybenzamine
  • Phentolamine
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5
Q

Selective a1 receptor antagonists examples

A
  • Prazosin
  • Terazosin
  • Doxazosin
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6
Q

Non-selective a adrenergic receptor antagonists: Phenoxybenzamine (Dibenzyline)
* Also blocks ___, histamine, and ___ receptors
* ___ antagonist resulting from covalent modification of receptor

A
  • ACh, serotonin
  • irreversible
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7
Q

What is this?

A

Phenoxybenzamine (Dibenzyline)

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8
Q

B-Haloalkylamines: Mechanism of receptor inactivation -
* The ___ ion is highly reactive and forms a ___ bond

A
  • Aziridinium
  • covalent
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9
Q

Non-selective a-adrenergic receptor antagonists:
Imidazolines
* competitive (___) blocker
* potent vaso___, but induces pronounced reflex ___cardia
* block of presynaptic a2 receptors may promote release of ___
* Also blocks 5-HT receptors, and is a ___ and histamine receptor agonist.

A
  • reversible
  • vasodilator, tachycardia
  • NE
  • muscarinic

Example:

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10
Q

What is this?

A

Non-selective a receptor antagonist - Imidazoline
* Phentolamine (Regitine)

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11
Q

What does a reversible receptor blockade graph look like?

A

slide to the right

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12
Q

What does an irreversible receptor blockade graph look like?

A

decreasing

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13
Q

Phenoxybenzamine action:
* non-competitive (___) antagonist
* non selective (__ and ___ receptors)
* new receptors must be synthesized in order to restore receptor function leading to a long drug effect

A
  • irreversible
  • a1 and a2
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14
Q

Phentolamine action:
* ___ (reversible) antagonist
* ___ (a1 and a2 receptors)

A

*competitive
* non-selective

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15
Q

Phenoxybenzamine and Phentolamine: Clinical Use - ___ (tumor of adrenal medulla that results in excessive epinephrine and norepinephrine synthesis and release)

A

pheochromocytoma

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16
Q

Problems with Phenoxybenzamine and Phentolamine:
* Not useful in treatment of hypertension due to __ effects
* By blocking __ receptors, we get greater release of NE at the heart and increased HR

A

a2

a2 is responsible for prejunctional inhibition of NE release

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17
Q

a1 -adrenergic receptor antagonists: Quinazolines
* extensive metabolism, excreted mainly in the ___.
* Vaso___
* ___ of smooth muscle in enlargesd prostate and bladder base
* Vary in half life (Prazosin 3 hrs, Terazosin 12 hrs, and Doxazosin 20 hrs)
* “___-dose” effect

A
  • bile
  • vasodilation
  • relaxation
  • first dose effect
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18
Q

What is this?

A

a1 receptor antagonist
* Quinazoline
Examples
* Prazosin (Minipres)
* Terazosin (Hytrin)
* Doxazosin (Cardura)

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19
Q

It is an a1 receptor antagonist if it has a ___ ring and ends in ___

A

Quinazoline, “-osin”

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20
Q

Selective a1 antagonists: Prazosin - Action:
* Selective ___ a1 antagonists
* Decrease total ___ resistance
* vaso___

A
  • competitive
  • peripheral
  • vasodilation
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21
Q

Prazosin clinical use

A
  • Hypertension
  • Reynaud’s disease
  • Benign prostatic
  • hyperplasia (BPH) a1a
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22
Q

Minor problem with Prazosin

A

fall in BP

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23
Q

a1a Antagonist: Tamsulosin (Flomax)
* very selective to prostate urethra as this is rich in ___ receptors
* less prone to induce fall in ___ as compared to classical a1 blockers such as ___
* Used for BPH (an a1a antagonist prevent the contraction the ____ muscle which contributes to the resistance to outflow of urine).

A
  • a1a
  • BP, Prazosin
  • trigone
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24
Q

a2 - receptor antagonists
Example: Yohimbine (Yocon)
* ___ alkaloid
* Blockade of a2 receptors ___ sympathetic discharge
* Folklore suggests use in treatment of ____

A
  • indole
  • increases
  • male impotence
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25
Q

What is this?

A

Yohimbine (Yocon)

indole alkaloid = a2 antagonist

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26
Q

Beta Blockers: Therapeutic Indications

A
  • angina
  • migraine
  • glaucoma
  • cardiac arrhythmia
  • post-myocardial infarction
  • hypertension
  • congestive heart failure (I and II)
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27
Q

What are the receptors for epinephrine?

A

B1, B2 > a1, a2

28
Q

What are the receptors for norepinephrine?

A

a1, a2, B1

29
Q

What is the base structure for Beta blockers?

A

Aryloxypropanolamines

note: non-carbon atom in side chain (O)

30
Q

T or F: The S configuration of the beta blocker hydroxyl is much more active than the R configuration.

A

True

most B blockers are used clinically as racemic mixtures

31
Q

T or F: The aromatic moiety is the primary determinant of B blocker activity (and B1 selectivity)

A

True

32
Q

Non-selective Beta blockers:
Propranolol
* ___philic (determined by bulky __ ring)
* Extensive ___ metabolism, “first pass”
* Local anesthetic properties
* Blockade is activity dependent
* good for patients with ___ failure

A
  • lipophilic, double
  • hepatic (liver)
  • kidney
33
Q

What is this?

A

Propanolol (Inderal)

34
Q

Pharmacological effects of Propanolol:
* ___ cardiac output and HR
* ___ renin release
* ___ VLDL and ___ HDL
* ___ lipolysis
* ___ glycogenolysis and glucose release in response to hypoglycemia
* ___ bronchial airway resistance

A
  • decrease
  • reduce
  • increase, decrease
  • inhibit
  • inhibit
  • increase
35
Q

Non-selective Beta Blockers: Nadolol (Corgard)
* less ___ than propranolol
* long half life (___), More hydrophilic = longer half life
* mostly excreted unchanged in the ___
* administered ___
* uses: hypertension, angina, ___
* good for patients with ___ issues

A
  • lipophilic
  • 20 hours
  • urine
  • orally
  • migraine
  • liver
36
Q

Non-selective Beta Blockers: Timolol (Timoptic, Blocadren)
* ___ nucleus with morpholine ring
* Administered: ___ and ___
* uses: glaucoma (ciliary epithelium), hypertension, angina, migraine

A
  • thiadiazole
  • oral, opthalmic
37
Q

What is this?

A

Timolol (Timoptic, Blocadren)

38
Q

T or F: Beta blockers affect pupil size

A

False; only M3 (miosis) and a1 (mydrasis) control pupil size

39
Q

Probelms with Beta Blockers: Propranolol and Timolol

A
  • Use cautiously in asthmatics due to blockade of B2 receptors (prevents bronchodilation)
  • rebound hypertension if discontinued abruptly (must taper dose!)
40
Q

Non-selective Beta Blockers: Pindolol (Visken)
* possesses ____ (ISA)
* ___ agonist
* less likely to cause ___cardia and lipid abnormalities. (Good for patients with severe ___cardia or little cardiac reserve)
* Administered ___
* Uses: hypertension, angina, migraine

A
  • intrinsic sympathomimetic activity
  • partial
  • bradycardia (twice)
  • orally
41
Q

T or F: Pindolol and Carteolol are partial agonists.

A

True

42
Q

Non-Selective Beta antagonist: Carteolol
*possesses ____ (ISA)
* ___ agonist
* less likely to cause ___cardia and lipid abnormalities. (Good for patients with severe ___cardia or little cardiac reserve)
* Administered: ___ and ___
* Uses: hypertension and ___

A
  • intrinsic sympathomimetic activity
  • partial
  • bradycardia (twice)
  • orally and ophthalmic
  • glaucoma
43
Q

Selective B1-receptor antagonists: base structure

A

only one ring

44
Q

Selective B1-receptor antagonists: (Metoprolol, Bisoprolol)
* ___-substituted ___ derivatives
* “cardio___”
* Less bronch___
* moderate lipophilicity
* half life: 3-4 hours
* Significant ___ metabolism
* Administered: ___ and ___
* Uses: hypertension, angina, antiarrhythmic, congestive heart failure

A
  • para, phenyl
  • cardioselective
  • less bronchoconstriction
  • first pass
  • orally and parenteral

used only for heart stuff

45
Q

B1 selective antagonist - Metoprolol:
Clinical use: ___, angina, cardiac arrhythmias, ischemic heart disease
Problems: minor ___ hypertension if discontinued abruptly (___ dose)

A
  • hypertension
  • rebound, taper
46
Q

Selective B1 antagonists: Atenolol (Tenormin)
* “cardio___”
* Less bronch___
* ___ lipophilicity, “water-soluble metoprolol”
* half life: 6-9 hours
* Administered: ___ and ___
* Uses: ___ and angina

A
  • cardioselective
  • bronchoconstriction
  • low
  • orally and parenteral
  • hypertension
47
Q

What is this?

A

Atenolol (Tenormin)
B1 selective antagonists

48
Q

T or F: Bisoprolol is refered to as “water soluble metoprolol”

A

False; Atenolol is known as the “water-soluble metoprolol”

the terminal amide causes less lipophilicity (more h2o soluble)

49
Q

Selective B1 receptor antagonists: Esmolol (Brevibloc)
* Very __ acting
* half life: 9 ___
* rapid hydrolysis by ___ found in RBCs
* Administed: ___
* Incompatible with ___
* Uses: supraventricular ___, atrial fibrillation/flutter, perioperative hypertension

A
  • short acting
  • minutes
  • esterases
  • parenteral
  • sodium bicarbonate
  • tachycardia
50
Q

What is this?

A

Esmolol
B1-receptor antagonists

51
Q

3rd generation B1-adrenergic receptors: Nebivolol (Bystolic)
* ___ lipid solubility
* Vaso___ due to nitric oxide
* Hypertension
* looks hella weird

A
  • low
  • vasodilation
52
Q

What is this?

A

Nebivolol (Bystolic)
3rd generation B1 antagonist

53
Q

Side effects of B-blockers

A
  • bradycardia
  • AV block
  • sedation
  • mask symptoms of hypoglycemia
  • withdrawal syndrome
54
Q

T or F: Chronic use of beta blockers causes more beta receptors to grow.

A

True; this is when abruptly stopping therapy is bad (more receptors=worse effects)

55
Q

Contraindications for beta blockers

A
  • asthma
  • COPD
  • congestive heart failure (type IV)
56
Q

Mixed (a and B) adrenergic receptor antagonists: Labetalol -
* non-selective __ receptor antagonist
* __ selective receptor antagonist
* two ___ carbons
* (1__,1’R)-isomer possesses B-blocking activity
* (1__,1’R)-isomer possesses greatest a1 receptor blocking activity
* B blocking activity prevents ____ normally associated with a1 receptor antagonist
* Administered: ___ and ___
* use: hypertension, hypertensive crisis

A
  • beta
  • a1
  • asymmetric
  • 1R
  • 1S
  • reflex tachycardia
  • orally and parenteral
57
Q

T or F: mixed adrenergic antagonists end in “lol” not “olol”

A

True

58
Q

Mixed (a and B) adrenergic receptor antagonists: Carvedilol (Coreg)
* non-selective __ receptor antagonist
* __ selective receptor antagonist
* both enantiomers antagonize ___ receptors
* only (S)-enantiomer possesses ___ blocking activity
* B blocking activity prevents ____ normally associated with a1 receptor antagonist
* administered ___
* uses: hypertension, congestive heart failure

A
  • Beta
  • a1
  • a1
  • Beta
  • reflex tachycardia
  • orally
59
Q

What is this? Which side is beta? Which side is alpha?

A

Carvedilol (Coreg)
mixed adrenergic agonist
* beta = three ring side (left)
* alpha = one ring side (right)

60
Q

T or F: Carvedilol has a 1:10 ratio for alpha:beta antagonism

A

True

61
Q

The clinical difference between Carvedilol and Labetalol

A
  • Carvedilol: heart failure; hypertension
  • Labetalol: Hypertension particularly hypertensive emergencies
  • Problems: Minor but rebound hypertension if discontinued abruptly– taper dose
62
Q

Indirect-acting Sympatholytics - Metyrosine (action):
* inhibits ___ hydroxylase
* Depletes ___ everywhere

A
  • tyrosine hydroxylase
  • catecholamines
63
Q

Indirect-acting Sympatholytics - Metyrosine (clinical use):
* ___ management of ___ (tumor of adrenal medulla that results in excessive Epi and NE synthesis/release)

A

perioperative, pheochromocytoma

64
Q

Indirect-acting Sympatholytics - Metyrosine (Problem)

A

depletes catecholamines everywhere

65
Q

Drugs that reduce storage or release of NE - Bretylium tosylate (Bretylol):
* aromatic ___ ammonium
* mechanism not really known
* displaces NE and prevents further release (depletion)
* local anesthetic
* adminstered: ___
* uses: ___ (ventricular fibrillation)
* Guanethidine also does this (random note at bottom of slide)

A
  • quaternary
  • parenteral
  • antiarrhythmic
66
Q

Catecholamine depleters: Reserpine (Serpasil)
* ___ alkaloid obtained from Rauwolfia serpentina root
* irreversibly blocks ___
* deplete vesicular pool of __
* ___ onset of action
* sustained effect (___)
* used for ___ (rarely due to adverse effects)
* may cause ___

A
  • indole
  • vesicular monoamine transporters (VMAT)
  • NE
  • slow
  • weeks
  • hypertension
  • depression
67
Q

Problems with Reserpine

A
  • orthostatic hypotension
  • increased GI activity
  • sedation (CNS)
  • severe depression/suicidal ideation (CNS)

PHRM 825 (49 decks)

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