Pharmacology Flashcards

1
Q

What is familial hypercholesterolemia (FH)? How does it affect LDL cholesterol levels in the blood?

A

Answer: Familial hypercholesterolemia (FH) is an inherited defect in how the body recycles LDL (bad) cholesterol.
It results in very high LDL levels in the blood, with severe cases reaching above 190 mg/dL. People with FH are born with high LDL cholesterol.

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2
Q

Name two PCSK9 inhibitors commonly used for the treatment of hypercholesterolemia.

A

Answer:

  • alirocumab
  • evolocumab.
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3
Q

What are the main indications for using PCSK9 inhibitors?

A

Answer: is familial hypercholesterolemia, which can potentially lead to obesity and diabetes.

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4
Q

How do PCSK9 inhibitors lower cholesterol levels in the body? What is their mechanism of action?

A

Answer:

  • PCSK9 inhibitors lower cholesterol levels by inhibiting the binding of PCSK9 to LDL receptors.
  • This inhibition increases the number of LDL receptors available to clear LDL from the blood.
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5
Q

What are the potential adverse effects of PCSK9 inhibitors?

A

Answer: The potential adverse effects of PCSK9 inhibitors include
* flu-like symptoms and
* myalgia (muscle pain).

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6
Q

How is alirocumab or evolocumab typically administered?

A

Answer: intramuscular (IM) injection.

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7
Q

What is the role of inclisiran in the treatment of hyperlipidemia? How does it work?

A

Answer:
* Inclisiran is a small interfering RNA that limits PCSK9 production by silencing or turning off the gene PCSK9.
* This super activates the liver to remove harmful cholesterol from the body.

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8
Q

an statin therapy be used during pregnancy? Why or why not?

A

Answer: No, statin therapy is contraindicated during pregnancy.

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9
Q

What is the common side effect of statin therapy that is mentioned in the notes?

A

Answer:
Myalgia (muscle pain) is a very common side effect of statin therapy.

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10
Q

What are the possible ranges for systolic and diastolic blood pressure readings that indicate hypertension?

A

Answer: Possible hypertension is indicated by systolic blood pressure between 140 and 180 mmHg, and diastolic blood pressure between 90 and 110 mmHg.

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11
Q

What additional checks can be performed if hypertension is suspected?

A

Answer:
Include home monitoring, repeated checks, or ambulatory blood pressure monitoring (ABPM).

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12
Q

What are the blood pressure thresholds for severe hypertension?

A

Answer: Severe hypertension is defined as systolic blood pressure higher than 180 mmHg and diastolic blood pressure higher than 110 mmHg.

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13
Q

Fill in the blanks: Possible hypertension is defined as systolic blood pressure between _____ mmHg and _____ mmHg, and diastolic blood pressure between _____ mmHg and _____ mmHg.

A

Answer: Possible hypertension is defined as systolic blood pressure between 140 mmHg and 180 mmHg, and diastolic blood pressure between 90 mmHg and 110 mmHg.

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14
Q

Fill in the blanks: Severe hypertension is defined as systolic blood pressure higher than _____ mmHg, and diastolic blood pressure higher than _____ mmHg.

A

Answer: Severe hypertension is defined as systolic blood pressure higher than 180 mmHg, and diastolic blood pressure higher than 110 mmHg.

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15
Q

What are the main indications for thiazide diuretics and loop diuretics?

A

Answer:

  • Thiazide diuretics are used to treat hypertension, while
  • loop diuretics are used to treat heart failure and acute pulmonary edema.
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16
Q

Name two loop diuretics.

A

Answer: Furosemide and Bumetanide

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17
Q

What is the mechanism of action of loop diuretics?

A

Answer: Loop diuretics
1. inhibit the sodium-potassium-chloride (Na-K-Cl) cotransporters in the thick ascending limb of the loop of Henle.
2. By inhibiting these cotransporters, they reduce the absorption of sodium, potassium, and chloride ions,
3. leading to increased urine production and decreased blood pressure.

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18
Q

What are the common side effects of loop diuretics?

A

Answer:
* hypotension,
* electrolyte disturbances (hyponatremia, hypokalemia, hypomagnesemia, hypocalcemia),
* hypochloremic alkalosis,
* ototoxicity, and gout.

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19
Q

What are the main indications for β-blockers?

A

Answer:
β-blockers are used in
* angina,

  • acute coronary syndrome,
  • myocardial infarction,
  • hypertension, and
  • heart failure.
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20
Q

What is the mechanism of action of β-blockers?

A

Answer: β-blockers competitively
1. inhibit β1 adrenergic receptors,
2. which lowers the heart rate and blood pressure.

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21
Q

What is the main indication for dihydropyridine calcium channel blockers?

A

A

nswer: Dihydropyridine calcium channel blockers, such as Amlodipine,
* are used in hypertension and angina.

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22
Q

What is the mechanism of action of ACE inhibitors?

A

Answer:
**ACE inhibitors reduce the activity of the renin-angiotensin-aldosterone system (RAAS) **
by blocking the conversion of angiotensin I to angiotensin II, thereby preventing
1. vasoconstriction,
2. vascular smooth muscle hypertrophy,
3. ventricular remodeling, and
4. aldosterone release.

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23
Q

Name two examples of ACE inhibitors.

A

Answer: Ramipril and Lisinopril

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24
Q

What are the common side effects of ACE inhibitors?

A

Answer: The common side effects of ACE inhibitors can be remembered using the mnemonic CAPTOPRIL:
1. Cough, (dry cough )
2. Angioedema,
3. Proteinuria,
4. Taste disturbance,
5. Other (fatigue, headache),
6. Potassium increased,
7. Renal impairment,
8. Itch,
9. Low blood pressure (1st dose).

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25
Q

What are the main indications for angiotensin receptor blockers (ARBs)?

A

Answer:
ARBs are used in hypertension, post-myocardial infarction,
and heart failure when ACE inhibitors are not tolerated.

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26
Q

What is the main indication for mineralocorticoid antagonists?

A

Answer: Mineralocorticoid antagonists are used in resistant hypertension and heart failure.

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27
Q

What is the mechanism of action of α-blockers?

A

Answer: α-blockers
block α adrenoceptors,
causing vasodilation.

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28
Q

What is the main indication for α-blockers?

A

Answer: α-blockers are used in confirmed resistant hypertension.

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29
Q

What is Coronary Artery Disease (CAD)?

A

Answer: CAD is a condition where the major blood vessels supplying the heart are narrowed, leading to reduced blood flow, which can cause symptoms like chest pain (angina) and shortness of breath.

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30
Q

Name an example of a nitrate medication.

A

Answer: Isosorbide mononitrate

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31
Q

What are the main indications for nitrates?

A

Answer: angina (including glyceryl trinitrate or GTN) and acute heart failure.

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32
Q

What is the mechanism of action of nitrates?

A

Answer: Nitrates work by relaxing all types of smooth muscles through the metabolism to nitric oxide (NO).

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33
Q

What are the common adverse effects of nitrates?

A

Answer:
1. headache and
2. hypotension/collapse.

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34
Q

How is GTN (glyceryl trinitrate) administered?

A

Answer: GTN is typically administered as spray and could also be admitted asublingually (under the tongue) for immediate relief of angina symptoms.

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35
Q

What is the main indication for nicorandil?

A

Answer: Nicorandil is mainly indicated for the treatment of angina.

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36
Q

What is the mechanism of action of nicorandil?

A

Answer: Nicorandil works as an ATP-sensitive potassium (KATP) channel activator.

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37
Q

What are the contraindications and cautions for nicorandil?

A

Answer: Nicorandil is contraindicated in acute pulmonary edema, hypovolemia, left ventricular dysfunction, severe hypotension, and shock.

38
Q

What are the common adverse effects of nicorandil?

A

Answer: headache and mouth/GI ulcers.

39
Q

How is nicorandil administered?

A

Answer: orally (PO).

40
Q

What is the main indication for Ivabradine?

A

Answer: Ivabradine is mainly indicated for the treatment of angina.

41
Q

What is the mechanism of action of Ivabradine?

A

Answer:
* Ivabradine selectively blocks HCN channels, specifically the If channels, which slows down the heart rate.
* It only works in sinus rhythm and does not affect heart rate in atrial fibrillation (AF).

42
Q

What are the contraindications and cautions for Ivabradine?

A

Answer: Ivabradine is contraindicated in decompensated heart failure, blood pressure below 90/50, and conduction abnormalities.

43
Q

What is the common adverse effect associated with Ivabradine?

A

Answer: Visual disturbances are a common adverse effect of Ivabradine.

44
Q

How is Ivabradine administered?

A

Answer: orally (PO).

45
Q

What is the main indication for Ranolazine?

A

Answer: Ranolazine is indicated for
refractory angina, which is angina that is not controlled with other standard treatments.

46
Q

What is the mechanism of action of Ranolazine?

A

Answer: Ranolazine is a late sodium channel modulator that helps decrease the calcium load on the heart.

47
Q

What are the contraindications and cautions for Ranolazine?

A

Answer: Ranolazine is contraindicated in moderate-severe hepatic impairment and should be used with caution in patients with a body weight less than 60 kg, the elderly, moderate to severe congestive heart failure, QT interval prolongation, and mild renal/hepatic impairment.

48
Q

What are the common adverse effects of Ranolazine?

A

Answer: The common adverse effects of Ranolazine include
* asthenia (weakness/fatigue),
* constipation,
* headache, and
* vomiting.

49
Q

ow is Ranolazine administered?

A

Answer: orally (PO)

50
Q

What are the main indications for aspirin?

A

Answer:
* Aspirin is the main antiplatelet agent used for arterial thrombosis.
* It is indicated for acute coronary syndrome (ACS), ischemic stroke, and thromboprophylaxis in patients at high cardiovascular risk.

51
Q

What is the mechanism of action of aspirin?

A

Answer:
1. Aspirin irreversibly blocks cyclooxygenase (COX) in platelets,
2. inhibiting the synthesis of thromboxane A2 (TXA2) and also
3. inhibiting the production of antithrombotic prostaglandin I2 (PGI2).

52
Q

What are the contraindications and cautions for aspirin?

A

Answer: should be avoided in patients with
1. active peptic ulceration and
2. bleeding disorders.

53
Q

What are the common adverse effects of aspirin?

A

Answer:
include gastrointestinal (GI) bleeding and ulceration.

54
Q

How is aspirin administered?

A

Answer: orally (PO).

55
Q

What are the main indications for clopidogrel?

A

Answer: Clopidogrel is indicated for

  • thromboprophylaxis in patients intolerant to aspirin and for acute coronary syndrome (ACS).
  • When combined with aspirin, it has a synergistic action.
56
Q

What is the mechanism of action of clopidogrel?

A

Answer: Clopidogrel
1. ** inhibits P2Y12 receptors,**
2. preventing the binding of adenosine diphosphate (ADP) and
3. subsequent platelet activation.

57
Q

What are the contraindications and cautions for clopidogrel?

A

Answer:
Clopidogrel should be used with caution in patients at
increased risk of bleeding and peptic ulcer.

58
Q

What are the common adverse effects of clopidogrel?

A

Answer:
* gastrointestinal (GI) bleeding and
* ulceration.

59
Q

How is clopidogrel administered?

A

Answer: orally (PO).

60
Q

What are the main indications for direct oral anticoagulants (DOACs)?

A

Answer:
1. used for the prevention of venous thrombosis in patients undergoing hip and knee replacements, as well as in
2. the treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE).

61
Q

hat is the mechanism of action of DOACs?

A

Answer: DOACs act as direct inhibitors of thrombin (e.g., dabigatran) or
factor Xa (e.g., rivaroxaban), which are key components in the coagulation cascade.

62
Q

Are there specific contraindications or cautions for DOACs in terms of overdose or hemorrhage risk?

A

Answer:
* There is no specific agent available to reduce hemorrhage in DOAC overdose.
* However, DOACs have a predictable degree of anticoagulation, resulting in a minimal risk compared to other anticoagulants such as warfarin or heparin.

63
Q

What are the common adverse effects of DOACs?

A

Answer: is bleeding.
However, it is generally less common compared to warfarin or heparin.

64
Q

How are DOACs administered?

A

Answer: orally (PO).

65
Q

What are the main indications for streptokinase?

A

Answer:
Streptokinase is mainly indicated for** reducing mortality** in acute myocardial infarction (MI).

66
Q

What is the mechanism of action of streptokinase?

A

Answer:
* Streptokinase is a protein extracted from cultures of streptococci that promotes the conversion of plasminogen to plasmin,
* leading to fibrinolysis.

67
Q

Are there any contraindications or cautions for the use of streptokinase?

A

Answer: Streptokinase may cause allergic reactions and should not be given to patients with recent streptococcal infections.

68
Q

What is the main adverse effect of streptokinase, and how can it be controlled?

A

Answer: is hemorrhage.
Tranexamic acid, which inhibits plasminogen activation, can be used to control the bleeding.

69
Q

How is streptokinase administered, and when should further doses be withheld?

A

Answer:
* Streptokinase is administered intravenously (IV). Its action is blocked after four days by the generation of antibodies,
* so further doses should not be given after this time.

70
Q

What are the main indications for tPA (tissue plasminogen activator)?

A

Answer:
* tPA is principally used to open occluded arteries in ST-elevation myocardial infarction (STEMI) or stroke (if the percutaneous coronary intervention window is missed).
* It is less frequently used in life-threatening thrombosis or pulmonary embolism (PE).

71
Q

What is the mechanism of action of tPA?

A

Answer:
1. tPA converts plasminogen to plasmin,
2. which breaks down fibrin into fragments,
3. causing clot lysis.

72
Q

Are there any contraindications or cautions for the use of tPA?

A

Answer:
* tPA is contraindicated in trauma,
* peptic ulcer,
* bleeding tendencies, and
* other conditions associated with an increased risk of hemorrhage.

73
Q

What is the main adverse effect of tPA, and how can it be controlled?

A

Answer:
The main adverse effect of tPA is hemorrhage.
* Tranexamic acid, which inhibits plasminogen activation, can be used to control the bleeding.

74
Q

How is tPA administered?

A

Answer: intravenously (IV).

75
Q

What are alteplase and duteplase?

A

Answer:
* Alteplase and duteplase are recombinant tissue plasminogen activators (rt-PA), similar to tPA.

  • They are used for their thrombolytic effects.
76
Q

How do alteplase and duteplase differ from tPA?

A

Answer:
* Alteplase and duteplase are more effective on fibrin-bound plasminogen than plasma plasminogen,
* which means they have a higher specificity for breaking down clots.

77
Q

What are the main indications for the use of digoxin?

A

Answer: Digoxin is indicated for
* heart failure,
* arrhythmias, and
* hypertension (as a fourth-line option).

78
Q

What is the mechanism of action of digoxin?

A

Answer:
1. Digoxin inhibits the Na-K-ATPase membrane pump,
2. leading to an increase in intracellular sodium and calcium.
3. This results in increased contraction of muscles and reduced conduction of the AV node.

79
Q

What are the contraindications and cautions associated with digoxin?

A

Answer:
* Digoxin has a narrow therapeutic index.
* Excessive levels can cause AV delay leading to bradycardia and heart block.
* It can also increase ventricular irritability, resulting in ventricular arrhythmias.
* Overdose can lead to digoxin toxicity, characterized by symptoms such as nausea, vomiting, yellow vision, and headache.

80
Q

What are the side effects of digoxin?

A

Answer:
* heart block, arrhythmias, nausea, vomiting, diarrhea, and
* disturbances of color vision.

81
Q

How is digoxin administered?

A

Answer: intravenously (IV)

82
Q

What is the main indication for the use of neprilysin inhibitors such as sacubitril/valsartan?

A

Answer: Neprilysin inhibitors are mainly indicated for the treatment of heart failure.

83
Q

What is the mechanism of action of neprilysin inhibitors?

A

Answer:
1. Neprilysin inhibitors block the breakdown of natriuretic peptides by neprilysin.
2. This leads to increased levels of natriuretic peptides,
3. which cause vasodilation and
4. decrease sympathetic tone.

84
Q

What are the contraindications and cautions associated with neprilysin inhibitors?

A

Answer: Neprilysin inhibitors should not be used alongside an ACE inhibitor (ACEi) or angiotensin receptor blocker (ARB).

85
Q

What are the adverse effects of neprilysin inhibitors?

A

Answer: Adverse effects of neprilysin inhibitors include
* hypotension,
* renal impairment,
* hyperkalemia, and
* Angioedema.

86
Q

How are neprilysin inhibitors administered?

A

Answer: orally (PO).

87
Q

How do SGLT2 inhibitors lower blood glucose levels?

A

A:
1. SGLT2 inhibitors lower blood glucose levels by inhibiting the reabsorption of glucose in the kidneys,
2. leading to increased glucose excretion in the urine.

88
Q

Q: What additional effects do SGLT2 inhibitors have in patients with heart failure?

A

A:
1. SGLT2 inhibitors have been shown to promote diuresis (increased urine production) and
2. natriuresis (increased excretion of sodium) due to the osmotic diuresis caused by glucose excretion in the urine.
3. This can lead to a reduction in blood volume and blood pressure.

89
Q

Q: How is the reduction in blood pressure observed with SGLT2 inhibitors thought to occur?

A

A:
* The reduction in blood pressure with SGLT2 inhibitors is thought to be multifactorial and may involve mechanisms such as osmotic diuresis,
* reduction in arterial stiffness, and improvement in endothelial function.

90
Q

Q: What is the primary indication for SGLT2 inhibitors?

A

A: The primary indication for SGLT2 inhibitors is the treatment of type 2 diabetes mellitus.

91
Q

Q: In addition to diabetes, in what condition have SGLT2 inhibitors shown beneficial effects?

A

A: SGLT2 inhibitors have shown beneficial effects in patients with
heart failure with reduced ejection fraction, leading to their approval for this indication in some countries.