L14: Drug effects on smooth muscle Flashcards

1
Q

Where is smooth muscle found?

A

Walls of the hollow organs of the body involved in the transport of gases, liquids & solids

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2
Q

What is smooth muscle controlled by?

A

Autonomic nervous system by hormones

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3
Q

What is contraction regulated by?

A

Myosin-light chain phosphorylation

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4
Q

What is smooth muscle cell composed of?

A

Actin+myosin filaments
Adherens junction
Gap Junction
Sarcoplasmic reticulum (release & reaccumulates Ca2+)

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5
Q

Regulation of smooth muscle contraction

A

1) Myosin light chain undergoes phosphorylation, detaching from actin filaments

2) Ca2+-calmodulin complex activates MLCK

3) Myosin binds to actin

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6
Q

How is smooth muscle contraction relaxed?

A

Myosin light chain phosphatase reverse phosphorylation which causes relaxation

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7
Q

What is the inhibition of MLCP called and what does it promote?

A

Calcium Sensitisation
- Promotes contraction

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8
Q

What is the activation of MLCP called and what does it promote?

A

Calcium Desensitisation
- Promote relaxation

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9
Q

What protein does Ca bind to in smooth muscle to initiate contraction?

A

Calmodulin

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10
Q

What enzyme removes the phosphate group?

A

Myosin phosphotase

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11
Q

What does vascular tone determine?

A

Contraction & releaxion of vascular smooth muscle

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12
Q

5 classes of hypertension drugs

A

1) alpha1-adrenoceptor antagonists
2) beta1-adrenoceptor antagonist
3) Ca2+ channel blockers
4) Diuretics
5) Drugs inhibiting RAAS

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13
Q

Function of RAAS

A

Maintenance of blood pressure via hormones in circulation

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14
Q

What is the endothelium derived relaxing factor?

A

Nitric Oxide

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15
Q

What is Nitric Oxide released by and in response to?

A

Released by endothelial cells in response to stimuli

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16
Q

What do endothelial cells lining blood vessels release?

A

Substance that relaxes neighbouring vascular smooth muscle cells- cause vasodilation

17
Q

2 drugs acting on the NO pathway

A

1) Nitrovasodilator drugs
2) PDE-5 inhibitors

18
Q

How do nitrovasodilator drugs mimic/enhance actions of NO?

A

Decompose in blood plasma to release NO
- Treat angina

19
Q

How does PDE-5 inhibitors mimic/enhance the actions of NO?

A

Stop breakdown of cGMP
- Used for erectile dysfunction & pulmonary hypertension

20
Q

What cells is NO released from in blood vessels?

A

Endothelial cells

21
Q

Name of enzyme activated by NO in smooth muscle cells & what is its product?

A

GC (Guanylyl Cyclase)
Product: GTP to cGMP

22
Q

What enzyme converts angiotensin I to angiotensin II?

A

Angiotensin-converting enzyme (ACE)

23
Q

What does RAAS do?

A

Regulates arterial pressure through angiotensin II & aldosterone

24
Q

Where is renin released from?

A

Juxtaglomerular cells of the kidney

25
Where is ACE found?
Surface of vascular endothelial cells, lungs
25
26
Where is aldosterone released from?
Adrenal cortex (cells in the outer layer of the adrenal gland)
27
28
Function of ACE
- Converts angiotensin I to angiotensin II - Inactivates vasodilator, bradykinin