organic nitrates Nicorandil "Beta blockers"

Question 1

Organic itrates?

Answer 1

Nytroglycerin (glyceryl trinitrate)

Amyl nitrate

Isosorbide Dinitrate

Isosorbide Mononitrate

Question 2

Pharmacological action of trinitrates?

Question 3

nitric oxide pathway?

Answer 3

Question 4

excitation/contraction coupling?

Answer 4

For vascular smooth muscle to contract, a rise in
intracellular calcium concentration must occur
(Excitation/contraction coupling)

Question 5

isosorbide pathway?

Answer 5

Question 6

half lives?

Question 7

administration?

Answer 7

Question 8

side effects?

Answer 8

tachycardic, hypotensive, dizzy, headache

Question 9

nitrate tolerace?

Answer 9

Definition:
A decreased therapeutic response to a certain dose
Nitrate Tolerance
May develop in less than 48 hours after the initiation of treatment.
Usually develops following frequent oral dosing or continuous
administration
Can be avoided in most patients if there is a nitrate-free interval of
10-12 hours per day.
Can be reversed within 18 hours of stopping nitrates.

Question 10

proposed mechanism of tolerance?

Answer 10

Early counter-regulatory responses (pseudotolerance)
Neurohormonal activation of vasoconstrictor signals and
intravascular volume expansion

Long-term treatment (vascular tolerance)
Intrinsic vascular changes, eg, a loss of nitrovasodilatorresponsiveness caused by increased vascular superoxide
production (increased oxidative stress)

Question 11

nicorandil ation?

Answer 11

Question 12

actions of nicorandil?

Answer 12

Opens ATP-sensitive potassium channels
(dilates peripheral and coronary resistance arterioles)
Possesses a nitrate moiety
(dilates systemic veins and epicardial coronary arteries)

Question 13

combined effect of nicorandil?

Answer 13

Increases coronary blood flow reduces pre-load and
afterload

Question 14

common adr of nicorandil?

Question 15

less comon ADR;s of nicorandil?>

Answer 15

Risk of gastrointestinal ulceration, including perianal
ulceration. Healthcare professionals should consider
nicorandil treatment as a possible cause in patients who
present with symptoms of gastrointestinal-tract ulceration

Question 16

beta blockers?

Answer 16

Atenolol (Tenormin)

Bisoprolol fumarate ( Cardicor, Monocor)

Nebivolol (Nebilet)

Propranolol hydrochloride (Inderal)

Question 17

beta syntehsis

Answer 17

Question 18

beta receptors?

Answer 18

Question 19

tissue discributio?

Answer 19

alpha1
– Vascular/genitourinary/intestinal smooth muscle
liver, heart.
alpha2
– Pancreatic islets, platelets, nerve terminals, VSM
beta1
– Heart, juxtaglomerular cells.
beta2
– Vascular/bronchial/genitourinary/gastrointestinal
smooth muscle, skeletal muscle, liver.

beta3
– Adipose tissue

Question 20

agonist action on adrenoceptors?

Answer 20

β1 receptor stimulation induces:
a positive chronotropic and inotropic effect on the heart
renin release in the kidney
β2 receptor stimulation induces:
smooth muscle relaxation
tremor in skeletal muscle
increased glycogenolysis in the liver/skeletal muscle
β3 receptor stimulation induces:
lipolysis (free fatty acid release)

Question 21

antagonist action?

Question 22

use of beta blockers?

Answer 22

Arrhythmias
(inhibit aberrant pacemaker activity)
Angina
Hypertension
Hypertrophic Obstructive Cardiomyopathy
Phaeochromocytoma
Secondary Prevention

Question 23

guidelines?

Answer 23

Question 24

beta blockers still used in?

Answer 24

younger women who could gt pregnant

those who cannot take ace inhibi

those who had a heart attack or anigina or heart failure

Question 25

beta blockers effects?

Answer 25

cardiac?

decrease contraction (ionotropy)

decrease relaxation rate (neggative lusitropy)

decrease heart rate (negative chronotropy

Decrease conduction velocity (negative dromotropy)

Vascular?

Smooth muscle contraction (mild vasocontrction)

Question 26

heart filure?

Answer 26

Systolic dysfunction (↓ contractility or loss of inotropy)
 β-blockers treatment counterintuitive?
 Clinical studies report specific beta-blockers actually
 improve cardiac function and reduce mortality. Reduce
 deleterious cardiac remodelling in CHF.
 Pure β1 blockade (low-dose Bisoprolol)
 Exact mechanism(s)?
 Blockade of excessive, chronic sympathetic influences

Question 27

nebivolol?

Answer 27

β1 selective Nebivolol – dual vasodilator
Nitric oxide-potentiating vasodilatory effect
(via activation of endothelial NO synthase)
Lowers blood pressure by reducing peripheral
vascular resistance
Significantly increases stroke volume with
preservation of cardiac output

Question 28

metabolic effect of beta blockers?

Answer 28

Reduce free fatty acid levels
Reduce glycogenolysis with consequent
reduction of blood glucose
Inhibit β receptor-mediated renin release
Can mask “warning signs” of hypoglycemia

Question 29

lipid solubility?

Answer 29

low - bisoprolol atenalol

high - propranalol

Question 30

intrinsic sympathomimetic activity?

Answer 30

Oxprenolol
Such “partial agonists” may be useful in
individuals exhibiting excessive bradycardia
with sustained beta blocker therapy