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YFRM 300 > Drugs affecting the CVS > Flashcards

Drugs affecting the CVS Flashcards

1
Q

What are some cardiovascular diseases
that can be treated with medication

A

Myocardial infarction
coronary atherosclerosis
Hyperlipidemia
peripheral artery disease.
hypertension

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2
Q

Cardiovascular disease

A

Heart & blood vessels
* Hypertension
* Atherosclerosis
* Ischaemic heart disease
* Heart failure
arryythmias

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3
Q

Classification of Cardiovascular Drug

A
  • Cardiac therapy
  • Antihypertensives
  • Diuretics
  • Beta-blocking agents
  • Calcium-channel blockers
  • Agents acting on renin-angiotensin system
  • Serum lipid modifying agent
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4
Q

Cardiac therapy

A

ncompasses a variety of medications used to treat cardiovascular diseases by targeting different aspects of heart function, blood pressure, and cholesterol levels. Here are the primary classes of medications involved

cting on the heart * Cardiac glycosides
* Antiarrhythmics
* Cardiac stimulants
* Vasodilators (cardiac disease) * Other

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5
Q

What are the different indications for B-blocking therapy?

A

ndications for Beta-Blocking Therapy
Beta-blockers are used to treat various cardiovascular and other conditions. Here are the common indications for beta-blocking therapy:

Hypertension (High Blood Pressure): Used to lower blood pressure by reducing heart rate and cardiac output.
Angina Pectoris (Chest Pain): Used to reduce the heart’s oxygen demand.
Heart Failure: Certain beta-blockers improve survival and reduce hospitalizations.
Arrhythmias (Irregular Heartbeats): Used to control heart rate and rhythm.
Myocardial Infarction (Heart Attack): Used to reduce mortality and prevent recurrence.
Migraine Prophylaxis: Used to prevent migraine headaches.
Anxiety: Used off-label to manage symptoms of anxiety.
Glaucoma: Used to reduce intraocular pressure.

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6
Q

Categories of Beta-Blockers and Examples

A

Beta-blockers can be categorized based on their selectivity and additional properties:

Non-Selective Beta-Blockers:

Examples:
Propranolol: Used for hypertension, angina, arrhythmias, migraine prophylaxis.
Nadolol: Used for hypertension and angina.

Selective Beta-Blockers (Beta-1 Selective):

Examples:
Atenolol: Used for hypertension and angina.
Metoprolol: Used for hypertension, angina, heart failure, and myocardial infarction.
Bisoprolol: Used for hypertension and heart failure.

Beta-Blockers with Additional Alpha-Blocking Activity:

Examples:
Carvedilol: Used for hypertension and heart failure.
Labetalol: Used for hypertension, including in pregnancy.

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7
Q

Beta-Blockers Listed in the Essential Medicines List (EML)

A

The World Health Organization (WHO) Essential Medicines List (EML) includes a selection of beta-blockers based on their clinical importance and effectiveness:

Atenolol: Listed for hypertension and angina.
Metoprolol: Listed for hypertension, angina, heart failure, and myocardial infarction.
Propranolol: Listed for hypertension, angina, arrhythmias, and migraine prophylaxis.

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8
Q

Beta-blocking agents: indications

A

Angina pectoris (β1
-selective)
Acute coronary syndrome / acute MI
Arrhythmias
Congestive cardiac failure (Vasodilatory non-β1
-selective)
(Hypertension (β1-selective) 5th line agent)

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9
Q

Other indications (Non-selective agents)

A

Essential tremor * Symptomatic anxiety
* Adjunct in thyrotoxicosis
* Migraine prophylaxis

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10
Q

Beta-blocking agents: pharmacokinetics

A
  • Lipid soluble: propranolol, metoprolol, labetalol
  • Least lipid soluble: atenolol, sotalol – fewer CNS adverse effects
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11
Q

Beta-blocking agents: side effects

A

Bradycardia
Bronchospasm
Masking hypoglycaemia
Fatigue
Cold extremities
Cholesterol dysregulation
* CNS effects: insomnia, depression
Lipid soluble: propranolol,
metoprolol, labetalol * Least lipid soluble: atenolol, sotalol
– fewer CNS adverse effect

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12
Q

The use of Atenolol and Thiazide diuretics.

A

can lead to an increase in risk of developing type 2 diabetes mellitus.
due to metabolic effects of both medications such as insulin resistance and alterations in glucose metabolism.

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13
Q

Less Protection from Stroke:

A

This might be due to the specific effects of atenolol on central blood pressure and the limited ability of thiazides to provide comprehensive cardiovascular protection.

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14
Q

Beta-blocking agents: contra-indications / cautions

A

Asthma & COPD
Heart block
Diabetes mellitus
Depression (non-selectives)

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15
Q

Alpha1-blocking agents

A
  • Doxazosin*
  • Prazosin
  • Terazosin
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16
Q

Alpha1-blocking agents: indications

A

Hypertension 4th line (NOT monotherapy) * Pheochromocytoma-associated hypertension
* Benign prostatic hypertrophy (BPH

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17
Q

Contraindication

A

Hypersensitivity, * For controlled-release tablets: history of GI obstruction, oesophageal
obstruction, decreased lumen diameter of GIT
* Caution hepatic impairment * Adverse effects: * First dose hypotension, hypotension, dizziness, vertigo, headache, fatigue
* Orthostatic hypotension, palpitations, nausea et

17
Q

How are Alpha blockers metabolized

A

They are metabolized in the liver and excreted mainly as metabolites in the feaces.

18
Q

Renin-AngiotensinAldosterone System
(RAAS)

A

Coordinate renal and
cardiovascular functions
* Homeostatic control of blood
volume
* Electrolyte balance
* Vascular resistance

19
Q

Proteolytic enzyme
* Stored in juxtaglomerular cells in
kidneys

A

Renin

20
Q

Renin

A

Released; response to sympathetic
activation of B1 receptors, systemic
hypotension, decreased tubular Na+ * ↓ arterial pressure = ↓ renal
perfusion + baroreflex mediated
sympathetic activation of renal β1
induce release of renin

21
Q

A mineralocorticoid that increases sodium reabsorption, promoting sodium retention.

A

Aldosterone

22
Q

Antidiuretic hormone

A

ADH (also known as vasopressin)
is a posterior pituitary peptide
hormone. * Antidiuretic action on the kidney
and powerful vasoconstrictor

23
Q

Angiotensin converting enzyme inhibitors ACE

A

have 3 classes

class 1: captopril

class 2: enalapril
perindopril
Quinapril
ramipril
trandolapril
class 3: water soluble- lisinopril.

24
Q

Angiotensin 2 receptor blockers. ARBS

A

Candesartan
Irbesartan
Losartan*
Telmisartan
Valsartan

25
Q

ACE inhibitors

A

Mechanism of action: * Inhibit ACE1

Act preferentially on angiotensinsensitive vascular beds including
kidney, heart and brain.

Antihypertensive effectiveness
increased by
* Low salt diet * Enhanced renin secretion (patients
on diuretics)
ACE inhibitors

26
Q

Preferred in patients with diabetes mellitus:

A
  • Lack negative effects on glucose tolerance and blood lipids
  • Reduce microalbuminuria
27
Q

Preferred in congestive heart failure.

A
  • Counteract overall metabolic-hormonal abnormalities
  • Indirect diuretic effect via inhibition of aldosterone production.
28
Q
A
29
Q

ACE Contraindications:

A
  • Pregnancy - teratogenic
  • History of angioedema and hyperkalaemia
  • Bilateral renal artery stenosis or stenosis of an artery to a dominant/single kidney
  • Aortic valve stenosis
  • Severe renal impairment (eGFR <30ml/min) – unless specialist dose-adjusted

General cautions: * Angioedema rare, but important adverse effect (caused by inhibition of
bradykinin degradation) – more common in Black patients and tho

30
Q

ACE Adverse effects:

A

Dry cough
* Angioedema
* Hyperkalaemia (due to reduced
aldosterone secretion) * Hypotension
* In patients with bilateral renal artery
stenosis: precipitate renal failure,
because AT2 usually constrict
efferent arterioles and maintains
pressure in the glomerulus for
filtration

31
Q

Pharmacokinetic

A

Administer orally (bioavailability ranges from 25%-75%) * Varying degrees of first pass hepatic metabolism, several has active
metabolites

32
Q

Enalapril

A

Pharmacokinetics:
Excreted predominantly in the urine as enalaprilat (active metabolite)
and unchanged drug

Adverse effects:
* Dry cough most common usually happen in early phase of tx (can
happen after many years on tx)
Angioedema (can happen after many years on tx) * Hyperkalaemia

33
Q

Enalapril

A

Contraindications:
Bilateral renal artery stenosis, hyperkalaemia, pregnancy.

Drug interactions: * Other antihypertensives (hypotension) * Potassium-sparing diuretics / potassium supplements
* ARBs
* High-dose aspirin & all NSAIDs
* Digoxin & lithium
* Trimethoprim

34
Q

Angiotensin-converting-enzyme (ACE) inhibitors (ACEIs: Contraindications

A
  • Pregnancy - teratogenic
  • History of angioedema and hyperkalaemia
  • Bilateral renal artery stenosis or stenosis of an artery to a dominant/single kidney
  • Aortic valve stenosis
  • Severe renal impairment (eGFR <30ml/min) – unless specialist dose-adjusted
    General cautions: * Angioedema rare, but important adverse effect (caused by inhibition of
    bradykinin degradation) – more common in Black patients and those with history
    of allergy
  • Combination with ARBs should be avoided
35
Q

Adverse effects:

A
  • Dry cough
  • Angioedema
  • Hyperkalaemia (due to reduced
    aldosterone secretion) * Hypotension
  • In patients with bilateral renal artery
    stenosis: precipitate renal failure,
    because AT2 usually constrict
    efferent arterioles and maintains
    pressure in the glomerulus for
    filtration.
36
Q

Angiotensin converting-enzyme (ACE) inhibitors (ACEIs): Pharmacokinetics

A

Pharmacokinetics: * Administer orally (bioavailability ranges from 25%-75%) * Varying degrees of first pass hepatic metabolism, several has active
metabolite

37
Q

Angiotensin receptor blockers (ARBs)

A

Safe to use in diabetes mellitus (do not affect serum glucose), gout (do not
increase serum uric acid levels), dyslipidaemias (do not increase
cholesterol levels), ACEI-mediated angioedema (only 8% cross-reactivity) * Adverse effects: hyperkalemia, neutropenia, increase hepatic
aminotransferase enzymes
* Contraindication: pregnancy – cause foetal injury and death
* Caution in patient with renal artery stenosis

38
Q

Losartan.

A
  • First pass metabolism to an active metabolite
  • Plasma protein binding 99%
  • Half-life (losartan): 1.5-2.5 hours
  • Half-life (active metabolite): 6-9 hours
  • Maximal antihypertensive effect: 3-6 weeks of tx
  • Uricosuri
39
Q

Losartan: Contraindications, Cautions:,Adverse effects.

A

Contraindications: * Bilateral renal artery stenosis, hyperkalaemia, pregnancy
Cautions: * Unilateral renal artery stenosis, pre-existing renal insufficiency,
hypersensitivity (angioedema) to ACEIs
Adverse effects: * Dizziness, dose-related orthostatic hypotension
* Hyperkalaemia, raised liver enzymes

40
Q
A

YFRM 300 (18 decks)

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