CVD Drugs - Chemistry Flashcards
What converts angiotensinogen in angiotensin I
~ antihypertensives
Renin
What converts angiotensin I to angiotensin II?
ACE (angiotensin converting enzyme)
What are the effects of angiotensin II?
• vasoconstriction
• activation of sympathetic nervous system
• ADH release from posterior pituitary to increase water absorption
• aldosterone secretion - promotes reaborbtion of Na and water. Promoting K secretion
Which drug classes target RAAS and give examples
ACEI - Ramipril
Renin inhibitors - Aliskiren
Angiotensin receptor blockers - Lostran
Aldosterone inhibitors - Spiractalone & Elerenone
Angiotensin promotes the release of aldosterone. Why does the release of aldosterone cause an increase in BP
Aldosterone promotes the reabsortbtion of fluid in kidneys, increasing blood volume, thus increasing BP
Which reaction occurs to convert angiotensin I to angiotensin II
ACE catalysis hydrolysis of the linkage peptide
ARBs bind to which receptors and which areas are they’re receptors located
They bind (block) to AT1 receptors found in the heart, kidneys and blood vessels
They are antagonist or inverse agonist
Prevent angiotensin II from binding to AT1
Lostran is a PRO drug, how it is metabolised?
Hydrolysis, reduction or oxidation
Oxidation
Regarding RAAS, which is a hormone potent in vasoconstriction
Angiotensin II
What are the main 2 target and enzymes (in RAAS) for antihypertensive agents
Renin and ACE
Which drug class inhibits angiotensin I synthesis
Renin inhibitors - aliskren
ACEI are products to decrease and increase what?
Decrease polarity
Increase absorption
Do antihypertensives block the action of endogenous or exdogenous hormones with vasoconstriction properties?
Endogenous hormones
Beta blockers
BB act on b1 adrenoreceptors, where are they main located
Heart
B1 adrenoreceptors are…
• found in the heart
• G-coupled protein receptors
What happens when b1 adrenoreceptors are activated
Cardiac muscle contraction
BB act on the heart to…
Reduce cardiac output
BB act on the CNS to….
Decrease activity of the sympathetic nervous system
BB act on the kidneys to…
Decrease renin release
Give an example of a 1st gen beta blocker and their selectivity?
Propranolol (aka aryloxypropanolamine)
Non selective - act on both b1 and b2
Give an example of a 2st gen beta blocker and their selectivity?
Bisporolol
B1 selective - cardio selective
Why should propranolol not be given in asthmatics
It blocks b2 adrenoreceptors in lungs, constricting airways
Vasodilators
What is cyclic GMP
Secondary messenger
cGMP is converted into GMP via
PDE5
What is an example of a PDE5 inhibitor
Slidinafil - vasodilator in the penis
Levels of cGMP can be increased by
PDE5 inhibitors - increases half life of cGMP and this action of vasodilation
CCBs
Which subunit do CCB bind to ?
a1 subunit
What are the 3 classes of CCB
• dihydropyradines
• benzothiazepines
• phenylalkylamines
All these classes of drug bind to different areas of the a1 subunit, but are very close - making them allosterically linked. What does allosterically linked mean?
When one drug bind, it will affect the bind of another near by drug
Are dihydropyradines hydrophilic or hydrophobic
Hydrophobic
Statins
What is the role of NDAP?
Reducing agent
Give an example of type 1 and type 2 statin
Type 1 - simvastatin
Type 2 - Atorvastatin, rosuvastatin, fluvastatin
From type 1 or type 2, which has the most ADRs
Type 1
Which type is harder to synthesis
Type 1 - due to the number of chiral circles
