Cardiovascular drugs

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  • Created by: Rscottqub
  • Created on: 10-03-20 14:52
2 main CV drugs
B adreno receptor blockers , Ca ion channel blockers
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what are these used to treat (3)
1. hypertension 2. Angina 3. Cardiac arrhythmias
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hypertension
normally due to decreased lumen of artery walls.
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BP is determined by (2)
1. vol of blood the heart pumps 2. resistance to flow in arteries
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the more blood pumping and the more resistance the
higher the BP
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are there noticeable symptoms with hypertension
NO, but if left untreated - increased risk of heart attacks and strokes
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Angina
Chest pain due to not enough O2 blood reaches the heart
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common cause of angina
CAD- coronary artery disease - which is caused by a build up of atherosclerotic plaque
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when does angina occur
when one or more coronary arteires becomes narrowed/blocked
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Arrhythmias
if electrical impulses dont work properly can lead to HR being too fast/too slow/ irregular - can be harmless but can also be very serious
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Adreno receptors
respond to NT adrenaline and Noradrenaline
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both A + NA control
BP, airways, HR
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2 types of adreno receptors
Alpha and Beta - then within each are subtypes - A1, B1/B2 - and then there is even subtype of subtypes - A1a A1b etc
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Generally activating Alpha receptors causes
smooth muscle contraction
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generally activating B1
causes cardiac muscle contraction
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activating B2
causes smooth muscle relaxation
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B1 found
in heart
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B2 are mainly in the
airways/lungs
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so if we block B1
then HR will decrease - cardiac muscle will relax
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if we block B2
smooth muscle with contract - causing constriction of airways
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for this reason we want CV drugs to be
B1 specific
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Catelchoamines
adrenaline and Noradrenaline -
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what is the structural difference between A+NA
Adrenaline has an extra methyl group - see diagram and learn structures
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B blocking drugs ....
prevent catelchoamines binding to B receptors
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If we remove any group from the catelchoamine
activity is greatly reduced
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OH in catelchoamine (not the phenol ones)
important but not essential - R>S enantiomer
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2 x OH in phenol
again important but not vital, can be replaced with other groups capable of forming H bonds
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aklyl link
links aromatic to amine - the longer this is the less activity
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Black CV development
In the 60s he wanted to acheive B selectivity over alpha-
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isoprenaline
discovered but still only a partial agonist - Cl groups replaced OH in the phenol
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the next step was
adding an extra aromatic ring - still only a partial agonist
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what did they want to do next?
extend the alkyl chain
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however what issue did they face
B napthol = out of stock , had to use Alpha napthol
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this lead to the discovery of
propranolol - pure Beta antagonist (but still binds to both B1 and B2) but did not bind to alpha
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All B blockers have the same
general scaffold - they vary in the groups attached to the scaffold
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1st generation B blockers have
heteroaromatic ring , short N substituent
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examples of 1st generation B blockers
propranolol , timolol
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1st generation selectivity
B selective over Alpha, NOT B1 and B2 selective
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do we want our drug to bind to both B1 and B2?
NO- we dont want binding to B2-> airway constriction and causes resp issues - cannot use if patient has asthma
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2nd generation B blockers
benzene ring para sub with amide , short N substituents
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does it have to be an amide group ?
no, can be any group capable of forming H bonds - but must be in PARA position
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2nd generation selectivity
B1 selective - therefore no respiratory issues
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2nd generation polarity
very polar - hydrophilic - therefore cannot pass BBB - less CNS side effects
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1st generation CNS
has CNS side effects since - very hydrophobic - lipophilic can pass BBB
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cold extremities
may be seen with 1st/2nd generation - due to decreased HR - decreased blood flow
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3rd generation
expansion via N substituent - doesnt matter if have para sub - if ever has expanded N chain - always 3rd - sicne 1/2 never have expanded N chain
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3rd generation selectivity
B1 selective , except for carvediol
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what else does 3rd gen have
extra vasodilating properties due to NO release.
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cold extremities in 3rd generation
No- due to extra vasodilating properties - counteracts the cold extremities caused by reduced HR
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Bisoprolol
2nd generation - so B1 selective
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Nebivolol
3rd generation - B1 selective
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Carvediol
3rd generation - but B1 and B2 (exception)
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CV action on hypertension
reduce HR and cardiac output
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CV action on angina
decrease HR and contractile force of contraction -> reduced demand for O2
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arrhythmia
inhibits sympathetic influences
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symptoms of B blockers
dizziness, tiredness, cold extremities ,
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Other cards in this set

Card 2

Front

what are these used to treat (3)

Back

1. hypertension 2. Angina 3. Cardiac arrhythmias

Card 3

Front

hypertension

Back

Preview of the front of card 3

Card 4

Front

BP is determined by (2)

Back

Preview of the front of card 4

Card 5

Front

the more blood pumping and the more resistance the

Back

Preview of the front of card 5
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