Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

PHRM 825 > ANS - 9 > Flashcards

ANS - 9 Flashcards

(67 cards)

Start Studying
1
Q

What effect would an antagonist alone have on receptor activation?

A

no effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Side effects of a1 receptor antagonists:

A
  • orthostatic hypotension
  • inhibition of ejaculation
  • nasal stuffiness
  • tachycardia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

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

A

B-Haloalkylamines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

non-selective a receptor antagonists examples

A
  • Phenoxybenzamine
  • Phentolamine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Selective a1 receptor antagonists examples

A
  • Prazosin
  • Terazosin
  • Doxazosin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is this?

A

Phenoxybenzamine (Dibenzyline)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

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

A
  • Aziridinium
  • covalent
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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:

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is this?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What does a reversible receptor blockade graph look like?

A

slide to the right

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What does an irreversible receptor blockade graph look like?

A

decreasing

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

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

A

*competitive
* non-selective

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

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

A

pheochromocytoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What is this?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

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

A

Quinazoline, “-osin”

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

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

A
  • competitive
  • peripheral
  • vasodilation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Prazosin clinical use

A
  • Hypertension
  • Reynaud’s disease
  • Benign prostatic
  • hyperplasia (BPH) a1a
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Minor problem with Prazosin

A

fall in BP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
What is this?
Yohimbine (Yocon) | indole alkaloid = a2 antagonist
26
Beta Blockers: Therapeutic Indications
* angina * migraine * glaucoma * cardiac arrhythmia * post-myocardial infarction * hypertension * congestive heart failure (I and II)
27
What are the receptors for epinephrine?
B1, B2 > a1, a2
28
What are the receptors for norepinephrine?
a1, a2, B1
29
What is the base structure for Beta blockers?
Aryloxypropanolamines | note: non-carbon atom in side chain (O)
30
T or F: The S configuration of the beta blocker hydroxyl is much more active than the R configuration.
True | most B blockers are used clinically as racemic mixtures
31
T or F: The aromatic moiety is the primary determinant of B blocker activity (and B1 selectivity)
True
32
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
* lipophilic, double * hepatic (liver) * kidney
33
What is this?
Propanolol (Inderal)
34
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
* decrease * reduce * increase, decrease * inhibit * inhibit * increase
35
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
* lipophilic * 20 hours * urine * orally * migraine * liver
36
Non-selective Beta Blockers: Timolol (Timoptic, Blocadren) * ___ nucleus with morpholine ring * Administered: ___ and ___ * uses: glaucoma (ciliary epithelium), hypertension, angina, migraine
* thiadiazole * oral, opthalmic
37
What is this?
Timolol (Timoptic, Blocadren)
38
T or F: Beta blockers affect pupil size
False; only M3 (miosis) and a1 (mydrasis) control pupil size
39
Probelms with Beta Blockers: Propranolol and Timolol
* Use cautiously in asthmatics due to blockade of B2 receptors (prevents bronchodilation) * rebound hypertension if discontinued abruptly (must taper dose!)
40
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
* intrinsic sympathomimetic activity * partial * bradycardia (twice) * orally
41
T or F: Pindolol and Carteolol are partial agonists.
True
42
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 ___
* intrinsic sympathomimetic activity * partial * bradycardia (twice) * orally and ophthalmic * glaucoma
43
Selective B1-receptor antagonists: base structure
only one ring
44
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
* para, phenyl * cardioselective * less bronchoconstriction * first pass * orally and parenteral | used only for heart stuff
45
B1 selective antagonist - Metoprolol: Clinical use: ___, angina, cardiac arrhythmias, ischemic heart disease Problems: minor ___ hypertension if discontinued abruptly (___ dose)
* hypertension * rebound, taper
46
Selective B1 antagonists: Atenolol (Tenormin) * "cardio___" * Less bronch___ * ___ lipophilicity, "water-soluble metoprolol" * half life: 6-9 hours * Administered: ___ and ___ * Uses: ___ and angina
* cardioselective * bronchoconstriction * low * orally and parenteral * hypertension
47
What is this?
Atenolol (Tenormin) B1 selective antagonists
48
T or F: Bisoprolol is refered to as "water soluble metoprolol"
False; Atenolol is known as the "water-soluble metoprolol" | the terminal amide causes less lipophilicity (more h2o soluble)
49
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
* short acting * minutes * esterases * parenteral * sodium bicarbonate * tachycardia
50
What is this?
Esmolol B1-receptor antagonists
51
3rd generation B1-adrenergic receptors: Nebivolol (Bystolic) * ___ lipid solubility * Vaso___ due to nitric oxide * Hypertension * looks hella weird
* low * vasodilation
52
What is this?
Nebivolol (Bystolic) 3rd generation B1 antagonist
53
Side effects of B-blockers
* bradycardia * AV block * sedation * mask symptoms of hypoglycemia * withdrawal syndrome
54
T or F: Chronic use of beta blockers causes more beta receptors to grow.
True; this is when abruptly stopping therapy is bad (more receptors=worse effects)
55
Contraindications for beta blockers
* asthma * COPD * congestive heart failure (type IV)
56
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
* beta * a1 * asymmetric * 1R * 1S * reflex tachycardia * orally and parenteral
57
T or F: mixed adrenergic antagonists end in "lol" not "olol"
True
58
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
* Beta * a1 * a1 * Beta * reflex tachycardia * orally
59
What is this? Which side is beta? Which side is alpha?
Carvedilol (Coreg) mixed adrenergic agonist * beta = three ring side (left) * alpha = one ring side (right)
60
T or F: Carvedilol has a 1:10 ratio for alpha:beta antagonism
True
61
The clinical difference between Carvedilol and Labetalol
* Carvedilol: heart failure; hypertension * Labetalol: Hypertension particularly hypertensive emergencies * Problems: Minor but rebound hypertension if discontinued abruptly– taper dose
62
Indirect-acting Sympatholytics - Metyrosine (action): * inhibits ___ hydroxylase * Depletes ___ everywhere
* tyrosine hydroxylase * catecholamines
63
Indirect-acting Sympatholytics - Metyrosine (clinical use): * ___ management of ___ (tumor of adrenal medulla that results in excessive Epi and NE synthesis/release)
perioperative, pheochromocytoma
64
Indirect-acting Sympatholytics - Metyrosine (Problem)
depletes catecholamines everywhere
65
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)
* quaternary * parenteral * antiarrhythmic
66
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 ___
* indole * vesicular monoamine transporters (VMAT) * NE * slow * weeks * hypertension * depression
67
Problems with Reserpine
* orthostatic hypotension * increased GI activity * sedation (CNS) * severe depression/suicidal ideation (CNS)

PHRM 825 (49 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions