antihypertensive drugs

Question 1

what kind of GPCR is a-receptor

Answer 1

when activated: IP3 and DAG formed, leading to increased intracellular Ca release from SR = vasoconstriction effects

Question 2

what is the use of a-blocker and names

Answer 2

hypertension treatment

prazosin, doxasozin

Question 3

what are the adverse effects of a-blocker

Answer 3

• first dose hypertension = sudden drop of blood pressure when lie down to stand up after 1st dose administration (due to great reduction in TPR)
• hypotension related effects
• becos of drop of TPR = reduction in BP = compensation
• BR reflex
• RAAS activation

Question 4

what are the mechanisms of B1 and B2-receptors and their location

Answer 4

B1: cAMP: PKA activation, P- L type and SR channel = intracellular Ca
- heart, brain

B2: MLCK no P = relaxation of smooth muscles
- airway SM, liver etc

Question 5

what could these b blocker do

Answer 5

1. heart effect:
   - reduce contractility = CO = Blood pressure
   - antiarrythmia at nodal tissue
   - TPR reduces (vascular smooth muscle): reduced NAd release at peripheral presynaptic neurones

• antihypertensives, antiarrythmia, angina, Heart failure durg, MI

ALSO HAS KIDNEY EFFECT (no RAAS )

Question 6

what are the adverse side effects - non selective B blocker

Answer 6

B2 effects:

• bronchoconstriction
• insulin induced hypoglycaemia NOT corrected - as tachycardia (warning sign)
• peripheral vascular effects

Question 7

what are the B1 specific effects and how to overcome

Answer 7

• B blocker - heart failure patient dangerous - Pindolol - sympathomimetic
• CNS effects: sedation/ depression
• reduce drug lipid solubility