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sympatholytics Flashcards

1
Q

side effects of alpha 1 receptor antagonist

A

Orthostatic hypotension, inhibition of ejaculation, nasal stuffiness, tachycardia

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2
Q

beta-haloalkylamines

A

-Non-selective a receptor
antagonist
-Also blocks acetylcholine,
histamine, and serotonin
receptors
-irreversible antagonist
resulting from covalent
modification of receptor

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3
Q

imidazolines

A

-Non-selective a receptor
antagonist
-Competitive (reversible)
blocker
-Potent vasodilator, but
induces pronounced reflex
tachycardia
-Block of presynaptic a2
receptors may promote
release of NE
-Also blocks 5-HT receptors,
and is a muscarinic and
histamine receptor agonist

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4
Q

action of phenoxybenzamine

A

-noncomptetive (irreversible) antagonist at a1 and a2 receptors
-new receptors must be synthesized in order to restore receptor function leading
to a long drug effect

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5
Q

action of phentolamine

A

competitive (reversible) antagonist at a1 and a2 receptors

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5
Q

clinical use of phenoxybenzamine and phentolamine

A

Perioperative management of patients with pheochromocytoma (tumor of
adrenal medulla that results in excessive epinephrine and norepinephrine
synthesis and release)

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5
Q

problems of phenoxybenzamine and phentolamine

A

Not useful in treatment of hypertension due to a2 effects

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6
Q

by blocking alpha 2 receptors, we get a greater release of _____ at the ______ and increased ___

A

NE, Heart, HR

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7
Q

alpha 1 antagonist

A
  • Vary in half-life:
    • Prazosin 3 hrs
    • Terazosin 12 hrs
    • Doxazosin 20 hrs
  • Undergo extensive metabolism, excreted
    mainly in the bile
  • Vasodilators
  • Relaxation of smooth muscle in enlarged
    prostate and in bladder base
  • Quinazolines produce peripheral
    vasodilation without causing reflex
    tachycardia or increased cardiac output
    (a presynaptic a 2 -antagonist effect)
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7
Q

prazosin

A

decrease TPR via a1 antagonism -> activate baroreceptor reflex -> increase NE release into myocardium -> increase heart rate via b1 receptors -> negative feedback via a2 receptors in myocardium mitigates NE release

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8
Q

phentolamine

A

decrease TPR via a1 antagonism -> activate baroreceptor reflex -> increase NE release into myocardium -> increase heart rate via b1 receptors -> antagonism of a2 receptors in myocardium blocks negative feedback -> cardiac overstimulation

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9
Q

tamsulosin (flomax)

A

-alpha 1 antagonist
-very selective to prostate urethra as this is rich in a1 a receptors
-less prone to induce fall in BP as compared to classical a1 blockers such as Prazosin
**Benign Prostatic Hyperplasia (BPH)
-BPH is problem with voiding may lead to overactive bladder.
-Stimulation of a1 a receptors in the trigone muscle of the bladder & urethra contract, contributing
to the resistance to outflow of urine. a1 blockers antagonize this effect

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10
Q

Beta 1 signal through Gs

A

-Activate adenylyl cyclase
-increase cAMP leading to protein kinase activation,
-Results in phosphorylation of ion channels and other proteins

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10
Q

yohimbine (yocon) alpha 2 adrenergic receptor antagonist

A

-Indole alkaloid
-Found in Rubaceae and
related trees. Also in
Rauwolfia Serpentina.
-Blockade of a2 receptors
increases sympathetic
discharge
-Folklore suggests use in
the treatment of male
impotence

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11
Q

beta blockers cardiovasular indications

A

angina, cardiac arrhythmia, post myocardial infraction, hypertension, congestive heart failure

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12
Q

cardiac arrhythmia

A

Slow AV nodal conduction

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12
Q

angina

A

Reduction in myocardial oxygen demand due to decreased heart rate and contractility

13
Q

post myocardial infarction

A

Reduction in myocardial oxygen demand
Slow AV nodal conduction

14
Q

hypertension

A

Decrease cardiac output
Inhibition of renin secretion

15
Q

congestive heart failure

A

Decreases chronic overstimulation/toxicity of compensatory catecholamines

16
Q

propranolol

A

-Non-selective beta antagonist
-Lipophilic
-Extensive hepatic metabolism, “first-pass”
-Local anesthetic properties
-Blockade is activity- dependent

17
Q

pindolol (visken)

A

-non selective beta antagonsit
-Possesses “Intrinsic sympathomimetic activity (ISA)
-Partial agonist
-Less likely to cause bradycardia and lipid abnormalities
-Good for patients who have severe bradycardia or little cardiac reserve
-Administered: Oral
-Uses: Hypertension, angina,
migraine

17
Q

propranolol pharmacologic effect

A

-Decreased cardiac output and heart rate
-Reduced renin release
-increase VLDL, Decrease HDL
-Inhibit lipolysis
-Inhibit compensatory glycogenolysis and glucose release in response to hypoglycemia
-Increase bronchial airway
resistance
-uses Hypertension, angina, cardiac arrhythmias, migraine, stage fright,
thyrotoxicosis, glaucoma, congestive heart failure (types II and III)

18
Q

nadolol (corgard)

A

-non-selective beta adrenergic antagonist
-Less lipophilic than propranolol
-Long half-life: ~20 hours
-Mostly excreted unchanged in
urine
-Administered: Oral
-Uses: Hypertension, angina,
migraine

19
Q

timolol (timoptic, blocadren)

A

-non selective beta antagonist
-Thiadiazole nucleus with
morpholine ring
-Administered: Oral, Ophthalmic
-Uses: glaucoma, hypertension,
angina, migraine,

20
Q

carteolol (cartrol, ocupress)

A

-nonselective beta antagonist
-Possesses “Intrinsic
sympathomimetic activity (ISA)
-Partial agonist
-Less likely to cause bradycardia
and lipid abnormalities
-Administered: Oral, Opththalmic
-Uses: Hypertension, glaucoma

21
Q

esmolol (brevibloc)

A

-selective beta 1 antagonist
-Very short acting
-Half-life: 9 minutes
-Rapid hydrolysis by esterases found in red blood cells
-Administered: Parenteral
Note: incompatible with sodium bicarbonate
-Uses: Supraventricular tachycardia, atrial
fibrillation/flutter, perioperative hypertension

21
Q

para-substituted phenyl derivatives

A

-selective beta 1 antagonist
-“Cardioselective”
-Less bronchconstriction
-Moderate lipophilicity
-Half-life: 3-4 hours
-Significant first-pass metabolism
-Administered: Oral, parenteral
-Uses: Hypertension, angina, antiarrhythmic, congestive heart failure

22
Q

atenolol (tenormin)

A

-selective beta 1 antagonist
-“Cardioselective”
-Less bronchconstriction
-Low lipophilicity, “Water-soluble Metoprolol”
-Half-life: 6-9 hours
-Administered: Oral, parenteral
-Uses: Hypertension, angina

23
Q

side effects of beta blockers

A

Bradycardia, AV block, sedation, mask symptoms
of hypoglycemia, withdrawal syndrome

23
Q

contraindications of beta blockers

A

Asthma, COPD, congestive heart failure (Type IV)

24
Q

lavetalol (normodyne, trandate)

A

-mixed adrenergic receptor antagonist
-Phenylethanolamine derivative
-Two asymmetric carbons (1 and 1’)
-Racemic mixture used clinically
-(1R, 1’R)-isomer Non-selective b
receptor antagonist
-(1S, 1’R)-isomer a1 antagonist
-(Administered: Oral, parenteral
-Uses: Hypertension, hypertensive
crisis
-b-blocking activity prevents reflex tachycardia normally associated with a1 receptor antagonists
-vasodilation via a1-blockade prevents bradycardia associated with b-blockade

25
Q

carvedilol (coreg)

A

-Non-selective b receptor antagonist
-a1 receptor antagonist
-Both enantiomers antagonize a1 receptors
-Only (S)-enantiomer possesses b-blocking activity
-b-blocking activity prevents reflex tachycardia normally associated with a1 receptor antagonists
-Administered: Oral
-Uses: Hypertension, congestive
heart failure

26
Q

actions of catecholamine synthetic path: inhibiting with metyrosine

A
  • Inhibits tyrosine hydroxylase
  • Depletes catecholamines everywhere
27
Q

clinical use of catecholamine synthetic path: inhibiting with metyrosine

A
  • Perioperative management of
    pheochromocytoma (tumor of adrenal
    medulla that results in excessive
    epinephrine and norepinephrine synthesis
    and release)
28
Q

problems of catecholamine synthetic path: inhibiting with metyrosine

A

Depletes catecholamines everywhere

29
Q

bretylium tosylate (bretylol)

A

-drugs that reduce storage or release of NE
-Aromatic quaternary ammonium
-Precise mechanism unknown
-Displace and release NE and prevent further release (depletion)
-Local anesthetic
-Administered: Parenteral
-Uses: Antiarrhythmic (ventricular fibrillation)

29
Q

reserpine (serpasil)

A

-catecholamine depleters
-Indole alkaloid obtained from the
root of Rauwolfia serpentina
-Block vesicular monoamine
transporters
-Deplete vesicular pool of NE
-Slow onset of action
-Sustained effect (weeks)
-Used in the treatment of hypertension (rarely because of adverse effects)
-May precipitate depression

30
Q

actions of VMAT inhibitor reserpine

A

-Nonselective, irreversible inhibitor of Vesicular
Monoamine Transporter (VMAT)
-Depletes stored NE

31
Q

clinical use of VMAT inhibitor reserpine

A

Hypertension but rarely used because of adverse effects

32
Q

problems of VMAT inhibitor reserpine

A

-Expected peripheral adverse effects (orthostatic hypotension, increased GI activity)
-CNS effects such as sedation, severe depression and suicide in susceptible individuals

pt (17 decks)

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