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Drug treatment for CVD Flashcards

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1
Q

What is the molecular action of beta-receptors?

A

Gs-protein-dependent activation of Adenylate Cyclase

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2
Q

What is the result of beta-receptor activation in terms of cyclic AMP?

A

: It increases cyclic AMP levels.

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3
Q

What does the activation of beta-receptors lead to?

A

It activates Protein Kinase A.

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4
Q

What are the effects of beta-receptor activation on intracellular Ca2+ levels?

A

It can either increase or decrease intracellular Ca2+ levels.

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5
Q

In which type of muscle does beta-receptor activation increase contractility?

A

Cardiac Muscle

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6
Q

In which types of muscles does beta-receptor activation decrease contractility?

A

Arterial smooth muscle and Bronchial smooth muscle.

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7
Q

What is the name of the non-selective beta-blocker that was developed?

A

Propranolol

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8
Q

What conditions are beta-blockers effective for?

A

Angina, hypertension, arrhythmias, migraine, tremor, anxiety, and thyrotoxicosis.

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9
Q

What are the effects of beta-blockers on the heart?

A

They decrease force and rate of contraction, as well as blood pressure.

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10
Q

What effect do beta-blockers have on the lungs (specifically b2 receptors)?

A

They cause bronchoconstriction.

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11
Q

What are the effects of beta-blockers on arterioles (specifically b2 receptors)?

A

They decrease blood supply to muscles, skin, and penis.

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12
Q

What are some side effects of beta-blockers on the heart?

A

Fatigue and bradycardia.

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13
Q

What are some side effects of beta-blockers on the lungs?

A

Breathlessness and increased asthma symptoms.

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14
Q

What are some side effects of beta-blockers on arterioles?

A

Fatigue, claudication, cold hands/feet, and erectile dysfunction.

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15
Q

What is the purpose of developing b1 selective beta-blockers?

A

To reduce side-effects.

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16
Q

Why is hypoglycemia dangerous in relation to beta blockers?

A

It activates the release of adrenaline, which can cause symptoms like tremor, palpitations, and sweats. These symptoms are blocked by beta-blockers.

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17
Q

What should patients be able to do in relation to hypoglycemia while taking beta blockers?

A

They need to be able to recognize hypoglycemia.

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18
Q

Are beta-blockers contraindicated in diabetic patients with recurrent hypoglycemia?

A

Yes, beta-blockers are contraindicated in diabetic patients with recurrent hypoglycemia.

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19
Q

What is the molecular action of thiazide diuretics?

A

They block the Na/Cl symporter in the Distal Convoluted Tubule, leading to diuretic action.

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20
Q

What is the core drug in the thiazide class?

A

Bendroflumethiazide

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21
Q

What is another term for “thiazide-like drug”?

A

Indapamide

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22
Q

What are the effects of thiazides on the kidney (Na/Cl symporter)?

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A

They increase sodium (Na+) loss and water loss, leading to a decrease in blood pressure (BP).

23
Q

What are the effects of thiazides on arterioles (K-ATP)?

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A

They decrease blood pressure (BP).

24
Q

What are some side effects of thiazides on the kidney?

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A

Hyponatremia (decreased sodium), hypokalemia (decreased potassium), alkalosis (decreased hydrogen ions), hypercalcemia (increased calcium), hypomagnesemia (decreased magnesium), and an increase in urate (gout).

25
What is the effect of thiazides on insulin resistance?
They increase insulin resistance, leading to an increase in glucose levels (diabetes).
26
What is the potential effect of thiazides on the liver?
There may be an increase in lipids, which can contribute to arterial disease.
27
What are some other uses of thiazides?
They can be used for treating edema, urinary tract stones, and nephrogenic diabetes insipidus.
28
What is the role of the adrenergic system?
The adrenergic system regulates various physiological responses in the body.
29
How does the alpha-1 receptor act and what is its effect?
The alpha-1 receptor acts via Gq protein to increase inositol triphosphate (IP3) levels, which leads to an increase in intracellular calcium (Ca2+) release from the sarcoplasmic reticulum.
30
What are some commonly used alpha blockers?
Doxazosin is the most common alpha blocker in the UK. It reduces intracellular Ca2+ release in arteriolar smooth muscle and is also used in prostatic hypertrophy to relax the bladder outflow sphincter.
31
What are some side effects of alpha blockers?
Palpitations (reflex tachycardia) and postural hypotension.
32
Name three examples of calcium channel blockers.
Amlodipine, diltiazem, and verapamil.
33
What is the molecular mechanism of calcium channel blockers?
They block the L-type voltage-gated Ca2+ channel, leading to a decrease in intracellular Ca2+ levels. This results in smooth muscle relaxation in arterioles, a decrease in force of contraction in cardiac muscle, and a decrease in heart rate in the SA and AV nodes.
34
What are some other uses of calcium channel blockers?
Calcium channel blockers are also used for angina, Raynaud's syndrome, and arrhythmias.
35
What is the cause of ankle swelling as a side effect of calcium channel blockers?
Calcium channel blockers preferentially dilate pre-capillary arterioles, impair the function of the pre-capillary sphincter, increase hydrostatic pressure, and result in net filtration, leading to ankle swelling.
36
What are some other side effects of calcium channel blockers?
Palpitations (reflex tachycardia), constipation, flushing, headache, and exacerbation of heart failure can occur as side effects.
37
What is the role of ACE (Angiotensin-Converting Enzyme) in the body?
ACE converts angiotensin I (AT-I) to angiotensin II (AT-II) and breaks down bradykinin, a vasoactive peptide.
38
What are the physiological effects of ACE inhibitors (ACE-I's)?
ACE inhibitors decrease the levels of AT-II and increase the levels of bradykinin.
39
Which ACE inhibitor is mentioned in the provided information?
Ramipril
40
What are some side effects of ACE inhibitors?
ACE inhibitors can cause a dry cough (due to bradykinin accumulation in the lungs), renal impairment (especially with renal artery stenosis), hyperkalemia, and are commonly given with a diuretic. They are also used for heart failure.
41
What is the molecular action of aldosterone antagonists?
Aldosterone antagonists block the upregulation of Epithelial sodium channels (ENaC) in the Distal Convoluted Tubule (DCT) by aldosterone.
42
Name a drug that is an aldosterone antagonist.
Spironolactone is an aldosterone antagonist. It is used as an 'add-on' in resistant hypertension and is a first-line treatment in hyperaldosteronism.
43
What is the role of angiotensin II receptor antagonists (AR-11 blockers)?
Angiotensin II receptor antagonists block the action of AT-II on the AT1 receptor, resulting in similar physiological effects to ACE inhibitors.
44
Name an angiotensin II receptor antagonist drug mentioned in the provided information.
Losartan is mentioned as an angiotensin II receptor antagonist.
45
What are some side effects of spironolactone?
Spironolactone can cause impaired renal function, hyperkalemia, and gynecomastia (due to its structural similarity to estrogen).
46
What are some specific causes of hypertension (HT)?
Specific causes of HT include chronic kidney (renal) disease, structural causes such as renal artery stenosis and aortic coarctation, and endocrine (hormonal) causes such as high aldosterone levels (Conn's syndrome), high catecholamine levels (pheochromocytoma), high cortisol levels (Cushing's syndrome), and high growth hormone levels (acromegaly).
47
What is a specific cause of hypertension related to pregnancy?
Pregnancy/pre-eclampsia can cause hypertension.
48
Describe the basic principles of managing hypertension according to national guidelines.
The management of hypertension typically involves lifestyle modifications, such as maintaining a healthy diet, engaging in regular physical activity, reducing sodium intake, and avoiding excessive alcohol consumption. Medication may be prescribed based on the patient's blood pressure level and risk factors. The choice of medication may include diuretics, beta-blockers, ACE inhibitors, angiotensin II receptor blockers (ARBs), calcium channel blockers (CCBs), or other classes of antihypertensive drugs, depending on individual patient characteristics and comorbidities.
49
According to NICE guidance, at what blood pressure (BP) level should Stage 3 hypertension be treated immediately?
Stage 3 hypertension should be treated immediately when systolic blood pressure (SBP) is above 180 mmHg.
50
According to NICE guidance, at what blood pressure (BP) level should Stage 2 hypertension be treated?
Stage 2 hypertension should be treated once confirmed on 24-hour BP monitoring when BP is above 160/100 mmHg.
51
According to NICE guidance, at what blood pressure (BP) level should Stage 1 hypertension be treated?
Stage 1 hypertension should be treated if there is evidence of end-organ damage or if the patient is diabetic when BP is above 140/90 mmHg.
52
What are the target blood pressure (BP) levels according to NICE guidance for individuals under the age of 80 years?
The target BP for individuals under the age of 80 years is below 140/90 mmHg.
53
What are the target blood pressure (BP) levels according to NICE guidance for individuals over the age of 80 years?
The target BP for individuals over the age of 80 years is below 150/90 mmHg.
54
What are the target blood pressure (BP) levels according to NICE guidance for individuals with diabetes?
The target BP for individuals with diabetes is below 135/85 mmHg.

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