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🫀Pharmacology > Alpha Blockers/Beta Blockers/ Calcium Channel Blockers > Flashcards

Alpha Blockers/Beta Blockers/ Calcium Channel Blockers Flashcards

1
Q

Atropine

A

An anatagonist at all muscarinic receptors - causes heart rate to increase

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2
Q

Alpha 1 receptors

A

Vascular smooth muscle - VASOCONSTRICTION
GPCR- Gq = activates PLC
Higher affinitey to NE>E

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3
Q

Beta 1 receptors

A

Increase heart rate + force
GPCR - Gs = stimulate adenyl cyclase
Higher affinity to epinephrine

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4
Q

Mechanism of alpha 1 receptors

A

1) agonists lead to formation of IP3
2) IP3 formed by PLC activates IP3R = releases calcium from the sarcoplasmic reticulum
3) free Ca in the cytosol activates RYR - releases more Ca in the CDCR = Ca spark

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5
Q

Smooth muscle contraction mechanism

A

1)Ca spark = binding of 4 Ca ions to calmodulin
2)Ca - CaM complex activates myosin light chain kinase - phosphorylates regulatory light chain = associated with each neck of the dimeric myosin 2 heavy chain
3) Phosphorylation causes a conformational change in myosin head = increases angle in head/neck domain of myosin - increases ATPase activity - interact efficiently with action = molecular motor
CROSS BRIDGE CYCLING AND SMOOTH MUSCLE CONTRACTION

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6
Q

Mechanism of B1 receptor

A

1) cAMP formed by AC = PKA - phosphorylates a number or receptors (more likely to open)
2)IP3R and RYR2 are phosphorylated = more Ca released from sarcoplasmic reticulum into the cytosol
3) free Ca in the cytosol activates RYR2 = more Ca in CDCR
INCREASED FORCE OF CONTRACTION

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7
Q

Increased chrontropy

A

High [Ca2+] at SAN&AVN = increases depolarisation rate

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8
Q

Increased inotropy

A

High [Ca2+] in cardiac myocytes = increases force of contraction

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9
Q

M2 receptor mechanism to decrease heart rate

A

1) PNS send AP from medulla oblongata via vagus nerve to the heart = control heart rate
2) Vagus nerve releases ACh - acts on M2 receptors of SAN/AVN - reduce pacemaker activity
3) M2 receptors - inhibitory Gi - agonist = decrease in cAMP/PKA = decrease heart rate
4) Reduction in pace maker = reduction in heart rate = decrease in cardiac output

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10
Q

Atropine is an antagonist at muscarinic receptors. At M2 will it increase heart rate or decrease heart rate?

A

INCREASE HEART RATE
M2 = Gi - inhibitory
Antagonist - increase cAMP and PKA = increase heart rate

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11
Q

The a1 agonist phenylephrine is added to cold medications will it cause vasoconstriction or vasodilation?

A

VASOCONSTRICTION

a1 - Gq - increase in IP3 and Ca2+

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12
Q

Phenylephrine

A

reduce nasal congestion

a1 agonist

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13
Q

Clonidine

A

resistant hypertension - causes vasodilation

a2 agonist

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14
Q

Dobutamine

A

Cardiogenic shock
B1 agonist
increased heart rate + force of contraction

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15
Q

Salbutamol

A

Bronchodilation

B2 agonist

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16
Q

Epinephrine

A

anaphylaxis and MI
agonist of a1/a2/B1/B2
increased heart rate + force of contration and central shunting of blood

17
Q

Norepinephrine

A

Agonist of a1/a2/B1

18
Q

Doxazosin

A

resitant hypertension - vasodilation

a1 antagonist

19
Q

Prazosin

A

resistant hypertension and benign prostatic hyperplasia

a1 antagonist

20
Q

Atenolol/Bisoprolol/Metaprolol

A

primarily hypertension + heart failure after MI

cardio selective - B1 antagonist ONLY

21
Q

Phenoxybenzamnine

A

phaeochromocytoma

non selective a1/a2 antagonist - causes irreversible blockade of all a adrenoreceptors

22
Q

Propranolol

A

hypertension/angina

non selective B1/B2 antagonist (same as timolol)

23
Q

A 45 year old Caucasian man presents clammy + crushing pain. Has a blue inhaler. Which beta adrenergic agonist should be administered?

A

Epinephrine

- heart attack

24
Q

A man with asthma had MI now has heart failure. Which beta adrenergic antagonist should not be administered?

A

Propranolol
- non selective beta blocker = cause bronchoconstriction - asthma
NEED CARDIO SELECTIVE

25
Q

Clinical indication of Ca blockers

A

decrease blood pressure
treat atrial tachyarrhythmias
treat ischemic heart disease

VASODILATION
slow vetricular response
decrease workload of heart by slowing heart rate + decrease oxygen demand

🫀Pharmacology (3 decks)

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