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Foundations of Biomedical Science > Cardiovascular Drugs > Flashcards

Cardiovascular Drugs Flashcards

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1
Q

What class of drug is Atenolol (Tenormin)?

A

β-blocker

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2
Q

What class of drug is Captopril (Capoten)?

A

ACE inhibitor

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3
Q

What class of drug is Irbesartan (Karvea, Avapro)?

A

Angiotensin-II receptor blocker

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4
Q

What class of drug is Hydrochlorothiazide (Dithiazide)?

A

Thiazide diuretic

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5
Q

What class of drug is Frusemide (Lasix)?

A

Loop diuretic

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6
Q

What class of drug is Amiloride (Midamor)?

A

Potassium-sparing diuretic

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7
Q

What class of drug is Amlodipine (Norvasc)?

A

Calcium-channel blocker

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8
Q

What class of drug is Verapamil (Isoptin)?

A

Calcium-channel blocker

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9
Q

What class of drug is Tenecteplase (Metalyse)?

A

Recombinant tissue plasminogen activator (tPA)

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10
Q

What class of drug is Atorvastatin (Lipitor)?

A

Dyslipidaemia drug – statin

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11
Q

What class of drug is Rosuvastatin (Crestor)?

A

Dyslipidaemia drug – statin

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12
Q

What class of drug is Ezetimibe (Ezetrol)?

A

Dyslipidaemia drug

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13
Q

What class of drug is Digoxin (Lanoxin)?

A

Cardiac glycoside

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14
Q

What class of drug is Dobutamine (Dobutrex)?

A

Selective β1 adrenoceptor agonist (sympathomimetic)

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15
Q

What class of drug is Lignocaine?

A

Class 1b antiarrhythmic - (mild) Na+ channel blocker

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16
Q

What class of drug is Flecainide (Tambocor)?

A

Class 1c antiarrhythmic - (strong) Na+ channel blocker

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17
Q

What class of drug is Isoprenaline?

A

Non-selective β-agonist

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18
Q

What class of drug is Amiodarone (Cordarone)?

A

Antidysrrhythmic (Class 3) - K+ channel inhibitor

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19
Q

What class of drug is Propanolol?

A

Non-selective β-adrenoceptor antagonist

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20
Q

What class of drug is Pindolol?

A
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21
Q

What class of drug is Diltiazem?

A

Non-dihydropyridine (non-DHP) calcium channel blocker

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22
Q

What class of drug is Nifedipine?

A

Dihydropyridine (DHP) calcium channel blocker

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23
Q

What class of drug is Icatibant?

A

Selective β2-adrenoceptor antagonist

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24
Q

What class of drug is Botulinum toxin A?

A

Neurotoxin

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25
Q

What class of drug is Neostigmine?

A

Anticholinesterase

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26
Q

What class of drug is Donepezil?

A

Anticholinesterase

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27
Q

What class of drug is Phenelzine?

A

MAO inhibitor

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28
Q

What class of drug is Phentolamine?

A

Non-selective α-adrenoceptor blocker

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29
Q

What class of drug is Phenylephrine?

A

Selective α1-adrenoceptor agonist

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30
Q

What class of drug is Prazosin?

A

Selective α1-adrenoceptor antagonist

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31
Q

What class of drug is Quinidine?

A

Class 1a antiarrhythmic - (moderate) Na+ channel blocker

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32
Q

What class of drug is Vitamin K?

A

Vitamin

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33
Q

What class of drug is Heparin?

A

Injectable anticoagulant

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34
Q

What class of drug is Enoxaparin (Clexane)?

A

Injectable anticoagulant (low-MW heparin)

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35
Q

What class of drug is Warfarin?

A

Oral anticoagulant

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36
Q

What class of drug is Clopidogrel?

A

ADP receptor antagonist

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37
Q

What class of drug is Abciximab?

A

Glycoprotein IIb/IIIa antagonist (monoclonal antibody)

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38
Q

What class of drug is Amrinone?

A

Phosphodiesterase inhibitor

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39
Q

What class of drug is Glyceryl trinitrate (GTN)?

A

Venodilator

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40
Q

What class of drug is Carvedilol?

A

α1- and β1-adrenoceptor blocker

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41
Q

What class of drug is Spironolactone?

A

Aldosterone receptor antagonist

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42
Q

What class of drug is Mannitol?

A

Osmotic diuretic (hyperosmotic agent)

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43
Q

What class of drug is Cholestyramine?

A

Bile acid sequestrant

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44
Q

What class of drug is Niacin?

A

Vitamin

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45
Q

What class of drug is Gemfibrozil?

A

Fibrate

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46
Q

What is the mechanism of action of Atenolol (Tenormin)?

A

Competitively blocks β-receptors in heart, peripheral vasculature, bronchi, pancreas, uterus, kidney, brain and liver

Specifically in relevance to treatment of hypertension, atenolol slows down the heart rate and reduces workload of the heart by antagonism of β-receptors

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47
Q

What is the mechanism of action of Captopril (Capoten)?

A

Blocks conversion of angiotensin I to angiotensin II and also inhibits the breakdown of bradykinin

They reduce the effects of angiotensin II-induced sympathetic stimulation, vasoconstriction, sodium retention and aldosterone release

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48
Q

What is the mechanism of action of Irbesartan (Karvea, Avapro)?

A

Competitively blocks binding of angiotensin II to type 1 angiotensin (AT1) receptors, blocking effects of angiotensin more selectively than ACE inhibitor

Reduces angiotensin-induced vasoconstriction, sodium reabsorption and aldosterone release

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49
Q

What is the mechanism of action of Hydrochlorothiazide (Dithiazide)?

A

Moderately potent diuretic; inhibits reabsorption of sodium and chloride in the proximal (diluting) segment of the distal convoluted tubule and produces a corresponding increase in potassium excretion

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50
Q

What is the mechanism of action of Frusemide (Lasix)?

A

Inhibits reabsorption of sodium and chloride in the ascending limb of the loop of Henle. This site accounts for retention of approximately 20% of filtered sodium; therefore, it is a potent diuretic

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51
Q

What is the mechanism of action of Amiloride (Midamor)?

A

Inhibits sodium reabsorption in the distal tubule by blocking sodium channels. This promotes the loss of sodium and water from the body, but without depleting potassium.

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52
Q

What is the mechanism of action of Amlodipine (Norvasc)?

A

Blocks inward current of calcium into cells in vascular smooth muscle, myocardium and cardiac conducting system via L-type calcium channels

Dihydropyridine calcium channel blocker (CaCB)

Acts mainly on arteriolar SM to reduce peripheral vascular resistance and BP

Minimal effect on myocardial cells

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53
Q

What is the mechanism of action of Verapamil (Isoptin)?

A

Blocks inward current of calcium into cells in vascular smooth muscle, myocardium and cardiac conducting system via L-type calcium channels

Non-dihydropyridine calcium channel blocker (CaCB)

Verapamil has greater cardiac effects, reducing contractility, heart rate and conduction with less effect on vascular smooth muscle

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54
Q

What is the mechanism of action of Tenecteplase (Metalyse)?

A

Converts plasminogen to plasmin, which catalyses the breakdown of fibrin

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55
Q

What is the mechanism of action of Atorvastatin (Lipitor)?

A

Competitively inhibits HMG-CoA reductase, a rate-limiting enzyme in cholesterol synthesis Increases hepatic cholesterol uptake from blood, reduces concentrations of total cholesterol, LDL and triglyceride (modest), and produces a small increase in HDL concentrations.

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56
Q

What is the mechanism of action of Rosuvastatin (Crestor)?

A

Competitively inhibits HMG-CoA reductase, a rate-limiting enzyme in cholesterol synthesis. Increases hepatic cholesterol uptake from blood, reduces concentrations of total cholesterol, LDL and triglyceride (modest), and produces a small increase in HDL concentrations.

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57
Q

What is the mechanism of action of Ezetimibe (Ezetrol)?

A

Reduces absorption of dietary and biliary cholesterol by inhibiting its transport across the intestinal wall. This leads to an increased demand for cholesterol, an increase in LDL uptake and its removal from the plasma.

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58
Q

What is the mechanism of action of Digoxin (Lanoxin)?

A

Inhibits Na+/K+-ATPase on cardiac myocytes → increased Na+ in cell → decreased Na+/Ca2+ exchange → decreased Ca2+ efflux → increased Ca2+ stored in sarcoplasmic reticulum → more Ca2+ released by each action potential → increased contractility. Inhibition of Na+/K+-ATPase pump also thought to increase vagal tone → slower AV conduction time → increased diastolic filling time

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59
Q

What is the mechanism of action of Dobutamine (Dobutrex)?

A

Binding of agonist to β1 adrenoceptor (GPCR) → activation of adenyl cyclase → increased cAMP in cell → conversion of inactive protein kinase into active protein kinase → phosphorylation of calcium channel → increased Ca2+ entry → increased contractility

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60
Q

What is the mechanism of action of Lignocaine?

A

Reduces automaticity of myocardial tissue with little effect on cardiac conduction

It has a mild negative inotropic effect and weak neuromuscular blocking activity

Also opens up K+ channels, shortening repolarisation

Decreases the ERP

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61
Q

What is the mechanism of action of Flecainide (Tambocor)?

A

Slows cardiac conduction and to a lesser extent, increases refractory period in all myocardial tissues (including bypass tracts) but particularly in the His-Purkinje (ventricular conduction) system

Also has negative inotropic activity

Has no effect on K+ (so repolarisation and ERP remain unchanged)

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62
Q

What is the mechanism of action of Isoprenaline?

A

Increases cardiac output by its positive chronotropic and inotropic actions. It tends to maintain or increase systolic BP, and decreases diastolic BP by lowering peripheral vascular resistance. It increases automaticity and AV nodal conduction, and usually improves coronary blood flow

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63
Q

What is the mechanism of action of Amiodarone (Cordarone)?

A

Decreases sinus node and junctional automaticity, slows atrioventricular (AV) and bypass tract conduction and prolongs refractory period of myocardial tissues (atria, ventricles, AV node and bypass tract); also has weak beta-blocker activity.

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64
Q

What are the side effects of Atenolol (Tenormin)?

A

Hypotension Heart failure Nausea Diarrhoea Bronchospasm Dyspnoea Fatigue Dizziness Abnormal vision Hypoglycaemia

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65
Q

What are the side effects of Captopril (Capoten)?

A

Hypotension Cough Hyperkalaemia Headache Dizziness Fatigue Nausea Renal impairment

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66
Q

What are the side effects of Irbesartan (Karvea, Avapro)?

A

Dizziness Headache Hyperkalaemia First dose orthostatic hypotension

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67
Q

What are the side effects of Hydrochlorothiazide (Dithiazide)?

A

Dizziness Weakness Muscle cramps Polyuria Orthostatic hypotension Hyponatraemia Hypokalaemia Hyperuricaemia Hypochloraemic alkalosis Hypomagnesaemia

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68
Q

What are the side effects of Frusemide (Lasix)?

A

Hyponatraemia Hypokalaemia Hypomagnesaemia Dehydration Hyperuricaemia Gout Dizziness Orthostatic hypotension Syncope

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69
Q

What are the side effects of Amiloride (Midamor)?

A

Hyperkalaemia Hyponatraemia and hypochloraemia (especially when combined with thiazide diuretics) Weakness Headache Nausea Vomiting Constipation Impotence Dizziness Muscle cramps

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70
Q

What are the side effects of Amlodipine (Norvasc)?

A

Peripheral oedema Rash Headache Fatigue Dizziness Flushing Nausea Abdominal pain Bradycardia

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71
Q

What are the side effects of Verapamil (Isoptin)?

A

Bradycardia Constipation Peripheral oedema Rash Headache Fatigue Dizziness Flushing Nausea Abdominal pain

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72
Q

What are the side effects of Tenecteplase (Metalyse)?

A

Bleeding, including bleeding at injection sites Intra-cerebral bleeding Internal bleeding (eg. GI, genitourinary)

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73
Q

What are the side effects of Atorvastatin (Lipitor)?

A

Myalgia Mild transient GI symptoms Headache Insomnia Dizziness Myopathy Rhabdomyolysis

74
Q

What are the side effects of Rosuvastatin (Crestor)?

A

Myalgia Mild transient GI symptoms Headache Insomnia Dizziness Proteinuria

75
Q

What are the side effects of Ezetimibe (Ezetrol)?

A

Headache Diarrhoea Myalgia Raised ALT/AST

76
Q

What are the side effects of Digoxin (Lanoxin)?

A

Worsened arrhythmias Anorexia Nausea Vomiting Diarrhoea Blurred vision Visual disturbances Confusion Drowsiness Dizziness Nightmares Agitation Depression

77
Q

What are the side effects of Dobutamine (Dobutrex)?

A

Tachycardia Excessive increase in BP Ventricular ectopic activity Nausea Headache Angina Palpitations Shortness of breath Rash Fever

78
Q

What are the side effects of Lignocaine?

A

Worsened arrhythmia Lip and tongue numbness Headache Dizziness Drowsiness Confusion Visual disturbances Tinnitus Tremor Paraesthesia

79
Q

What are the side effects of Flecainide (Tambocor)?

A

Nausea Vomiting Diarrhoea Constipation Headache Dizziness Tinnitus CNS disturbances Angina Worsened arrhythmias Dyspnoea Flushing

80
Q

What are the side effects of Isoprenaline?

A

Palpitations Tachycardia Hypotension Flushing Headache Nervousness Restlessness Fine tremor

81
Q

What are the side effects of Amiodarone (Cordarone)?

A

Worsened arrhythmia Nausea and vomiting GIT symptoms Photosensitisation Skin discolouration Hypothyroidism Pulmonary fibrosis from long-term use

82
Q

What are the indications for use of Atenolol (Tenormin)?

A

Administration: oral tablet

  • Hypertension
  • Angina
  • Tachyarrhythmias
  • MI
  • Prevention of migraine

Contraindications: Renal failure, Atenolol recommended only in combination with other antihypertensive classes (monotherapy associated with higher CV mortality and stroke)

83
Q

What are the indications for use of Captopril (Capoten)?

A

Administration: oral tablet or liquid

  • Hypertension
  • Heart failure
  • Post-MI in patients with left ventricular dysfunction
  • Diabetic nephropathy (type 1 diabetes)

Contraindications: Collagen vascular disorders (e.g. SLE), Severe renal impairment - may predispose to neutropenia or agranulocytosis

84
Q

What are the indications for use of Irbesartan (Karvea, Avapro)?

A

Administration: oral tablet

  • Hypertension (includes combination with hydrochlorothiazide
  • Reduction of renal disease progression in patients with type 2 diabetes, hypertension and microalbuminuria (>30mg/24hours) or proteinuria (>900mg/24hours)

Contraindications: Peripheral vascular disease, Volume or sodium depletion, Aortic stenosis, Renal impairment, Pregnancy

85
Q

What are the indications for use of Hydrochlorothiazide (Dithiazide)?

A

Administration: oral table

  • Hypertension, in conjunction with diuretics, ACE-inhibitors, AT-II antagonist
  • Oedema associated with heart failure, hepatic cirrhosis or nephrotic syndrome
86
Q

What are the indications for use of Frusemide (Lasix)?

A

Produces a rapid and intense diuresis and have a short duration of action (4-6 hours)

Administration: oral tablet or liquid, IV (a trial of IV frusemide may be more effective than increasing oral doses in refractory heart failure)

  • Oedema associated with heart failure (combine with ACE inhibitor), hepatic cirrhosis, renal impairment and nephrotic syndrome
  • Severe hypercalcaemia

Contraindications: Severe sodium and fluid depletion

87
Q

What are the indications for use of Amiloride (Midamor)?

A

Administration: oral table

  • Prevention of diuretic-induced hypokalaemia
  • Oedema due to heart failure, hepatic cirrhosis or nephrotic syndrome, as an adjunct to thiazide or loop diuretic
  • Hypertension, in combination with hydrochlorothiazide
  • Oedema due to heart failure or hepatic cirrhosis, in combination with hydrochlorothiazide

Contraindications: Hyperkalaemia, Renal failure, Cirrhosis, Pregnancy

88
Q

What are the indications for use of Amlodipine (Norvasc)?

A

Administration: oral tablet

  • Hypertension
  • Angina
89
Q

What are the indications for use of Verapamil (Isoptin)?

A

Administration: oral tablet, IV (for SVT, AF or atrial flutter)

  • Hypertension
  • Angina
  • Supraventricular tachycardia
  • AF or atrial flutter

Contraindications: Severe bradycardia, 2nd or 3rd degree AV block, Hypotension, Various arrhythmias

90
Q

What are the indications for use of Tenecteplase (Metalyse)?

A

Administration: IV, used in conjunction with weight-adjusted heparin

  • Acute MI
91
Q

What are the indications for use of Atorvastatin (Lipitor)?

A

Administration: oral tablet

  • Hypercholesterolaemia
  • Hypertensive patients with additional risk factors for heart disease
  • Mixed hyperlipidaemia

Contraindications: Chronic liver disease, Severe intercurrent illness, Renal impairment, Pregnancy

92
Q

What are the indications for use of Rosuvastatin (Crestor)?

A

Administration: oral tablet

  • Hypercholesterolaemia
  • High risk of CVD

Contraindications: Chronic liver disease, Severe intercurrent illness, Renal impairment, Pregnancy, Hepatic impairment

93
Q

What are the indications for use of Ezetimibe (Ezetrol)?

A

Administration: oral tablet

  • Hypercholesterolaemia
94
Q

What are the indications for use of Digoxin (Lanoxin)?

A

Administration: Oral or IV

  • AF or atrial flutter
  • SVT with nodal re-entry
  • Heart failure

Contraindications: Hyperthyroidism, Hypothyroidism, 2nd or 3rd degree AV block, Various arrhythmias

High doses of digoxin disturb sinus rhythm and cause ectopic beats (after-depolarisations) due to increased intracellular calcium levels.

95
Q

What are the indications for use of Dobutamine (Dobutrex)?

A

Administration: IV

  • Inotropic support in acute heart failure and cardiogenic shock
  • Pharmacological stress testing of myocardial function

Contraindications: Ventricular arrhythmias, AF, Hypovolaemia

Use is restricted to settings where there is close monitoring of arterial and venous pressure, and continuous ECG

96
Q

What are the indications for use of Lignocaine?

A

Administration: IV injection

  • Serious ventricular arrhythmias
  • Neuropathic pain

Contraindications: Severe adverse reaction/allergy to lignocaine, Treatment with flecanide, Hypovolaemia, Electrolyte disturbances, 2nd or 3rd degree AV block, Heart failure

Adverse effects are dose-related.

97
Q

What are the indications for use of Flecainide (Tambocor)?

A

Administration: IV injection

  • SVT
  • Paroxysmal AF or atrial flutter
  • Maintenance of sinus rhythm following cardioversion

Contraindications: Hypovolaemia, Electrolyte disturbances, Structural heart disease, 2nd or 3rd degree AV block, Heart failure

98
Q

What are the indications for use of Isoprenaline?

A

Administration: IV infusion

  • Heart block
  • Bradycardia with haemodynamic compromise

Contraindications: Hypovolaemia, Tachycardia, Hyperthyroidism, Recent MI, Ischaemic heart disease

99
Q

What are the indications for use of Amiodarone (Cordarone)?

A

Administration: IV infusion, oral

  • Treatment and prophylaxis of serious tachyarrhythmias including VT, AF and SVT

Contraindications:, Allergy to amiodarone, Thyroid dysfunction, Lung disease, Electrolyte disturbances, 2nd or 3rd degree AV block, Pregnancy

100
Q

What is the mechanism of action of Propanolol?

A

Competitively block beta receptors in heart, peripheral vasculature, bronchi, pancreas, uterus, kidney, brain and liver

Beta-blockers reduce heart rate, BP and cardiac contractility; also depress sinus node rate and slow conduction through the atrioventricular (AV) node, and prolong atrial refractory periods

101
Q

What is the mechanism of action of Pindolol?

A

Competitively block beta receptors in heart, peripheral vasculature, bronchi, pancreas, uterus, kidney, brain and liver

Beta-blockers reduce heart rate, BP and cardiac contractility; also depress sinus node rate and slow conduction through the atrioventricular (AV) node, and prolong atrial refractory periods

102
Q

What is the mechanism of action of Diltiazem?

A

Block inward current of calcium into cells in vascular smooth muscle, myocardium and cardiac conducting system via L-type calcium channels

Act on coronary arteriolar smooth muscle to reduce vascular resistance and myocardial oxygen requirements, relieving angina symptoms

Diltiazem has a greater effect on arteriolar smooth muscle than verapamil

103
Q

What is the mechanism of action of Nifedipine?

A

Block inward current of calcium into cells in vascular smooth muscle, myocardium and cardiac conducting system via L-type calcium channels

Act on coronary arteriolar smooth muscle to reduce vascular resistance and myocardial oxygen requirements, relieving angina symptoms

Dihydropyridines act mainly on arteriolar smooth muscle to reduce peripheral vascular resistance and BP. They have minimal effect on myocardial cells

104
Q

What is the mechanism of action of Icatibant?

A

Inhibits bradykinin release, which prevents its involvement in the deeper tissue swelling associated with hereditary angioedema

105
Q

What is the mechanism of action of Botulinum toxin A?

A

Acts as a protease to cleave specific SNARE proteins (that normally form a complex that facilitates membrane fusion between the synaptic vesicle and the pre-synaptic neuronal membrane), preventing acetylcholine (ACh) release at the synapse

106
Q

What is the mechanism of action of Neostigmine?

A

Reduce breakdown of neuronally released acetylcholine by inhibiting cholinesterase

Enhance neuromuscular transmission in skeletal and smooth muscles

107
Q

What is the mechanism of action of Donepezil?

A

Decrease breakdown of acetylcholine reducing the apparent deficiency of cholinergic neurotransmitter activity in Alzheimer’s disease (due to its good entry into the CNS)

108
Q

What is the mechanism of action of Phenelzine?

A

Non-selective MAOIs irreversibly inhibit monoamine oxidases A and B (MAO-A and MAO‑B), blocking neurotransmitter reuptake, increasing the synaptic concentrations of adrenaline, noradrenaline, dopamine and serotonin

109
Q

What is the mechanism of action of Phentolamine?

A

Block the effects of adrenaline and noradrenaline at α1 and α2 receptors

Arterial and venous vasodilation is due to blockade of postsynaptic α1 receptors and inhibition of catecholamine-mediated vasoconstriction

Blockade of presynaptic α2 receptors results in increased noradrenaline release and enhances reflex tachycardia

110
Q

What is the mechanism of action of Phenylephrine?

A

Act on alpha adrenoreceptors on vascular smooth muscle in the respiratory tract, producing vasoconstriction of dilated nasal vessels, reducing tissue swelling and nasal congestion

111
Q

What is the mechanism of action of Prazosin?

A

Competitively binds to the α1-adrenoceptor and prevents binding by noradrenaline or adrenaline, inhibiting the sympathetic-mediated vasoconstriction

112
Q

What is the mechanism of action of Quinidine?

A

Acts primarily on Ifunny channels, providing a moderate Na+ block (but also providing a moderate K+ block)

Prolongs repolarisation (due to effects on K+)

Increases the effective/absolute refractory period (ERP)

113
Q

What is the mechanism of action of Vitamin K?

A

Essential cofactor in the synthesis of blood clotting factors II, VII, IX and X, and proteins C and S

Reverses effect of vitamin K antagonists

114
Q

What is the mechanism of action of Heparin?

A

Binds to antithrombin III, exposing the active site of thrombin, such that it can bind to it and Inactivate clotting factors IIa (thrombin) and Xa

Anti-coagulative effect is quantified by the use of the activated partial thromboplastin time (APTT), a measure of the instrinic pathway of the clotting cascade

115
Q

What is the mechanism of action of Enoxaparin (Clexane)?

A

Inactivate clotting factors IIa (thrombin) and Xa by binding to antithrombin III

LMWHs have a much greater effect on factor Xa than on thrombin

116
Q

What is the mechanism of action of Warfarin?

A

Inhibits the reduction of vitamin K by inhibiting vitamin K reductase, inhibiting the gamma-carboxylation reaction necessary for synthesis of vitamin K-dependent clotting factors (II, VII, IX, X) and the antithrombotic factors protein C and protein S

117
Q

What is the mechanism of action of Clopidogrel?

A

The active metabolite irreversibly binds to the platelet P2Y12 receptor and inhibits platelet aggregation for the life of the platelet

118
Q

What is the mechanism of action of Abciximab?

A

Occupies the glycoprotein IIb/IIIa receptor, thereby blocking platelet aggregation

119
Q

What is the mechanism of action of Amrinone?

A

Inhibits phosphodiesterase inhibitor activity, thereby preventing the breakdown of cAMP, whose increased levels activate protein kinase A (PKA), increasing Ca2+ entry into the cell

Increases cardiac contractility

120
Q

What is the mechanism of action of Glyceryl trinitrate (GTN)?

A

Provide exogenous source of nitric oxide (which mediates vasodilator effects)

Predominantly venodilators; reduce venous return and preload to the heart, reducing myocardial oxygen requirement

121
Q

What is the mechanism of action of Carvedilol?

A

Competitively block beta receptors in heart, peripheral vasculature, bronchi, pancreas, uterus, kidney, brain and liver

Beta-blockers reduce heart rate, BP and cardiac contractility; also depress sinus node rate and slow conduction through the atrioventricular (AV) node, and prolong atrial refractory periods

Also competitively blocks α1-adrenoceptors, effecting vasodilatation (thereby reducing afterload)

122
Q

What is the mechanism of action of Spironolactone?

A

Inhibit sodium absorption in the distal tubule by antagonising aldosterone, increasing sodium and water excretion and reducing potassium excretion; they are weak (potassium-sparing) diuretics

Aldosterone may contribute to the pathophysiology of heart failure; by reducing aldosterone activity, aldosterone antagonists improve outcome

123
Q

What is the mechanism of action of Mannitol?

A

Pharmacologically inert substance that is filtered but not absorbed, so it increases the plasma osmolality, reducing passive water absorption

Mainly affects the water-permeable parts of the nephron:

  • Proximal tubule
  • Descending limb of the Loop of Henle
  • Collecting tubules

Produces a rapid (30 minutes) but temporary (6 hours) drop in intraocular pressure.

124
Q

What is the mechanism of action of Cholestyramine?

A

Bind bile acids in intestinal lumen, preventing reabsorption, and increasing bile acid excretion in the faeces

Increased demand for cholesterol for bile acid synthesis results in an increase in LDL uptake and removal from plasma.

125
Q

What is the mechanism of action of Niacin?

A

Unclear

Decreases the secretion of VLDL particles from the liver

Reduces plasma LDLs and TAGs

Increases HDLs

Lowers Lipoprotein (a)

(Lp(a) is normally formed from LDL and is found in plaques, inhibiting thrombolysis)

126
Q

What is the mechanism of action of Gemfibrozil?

A

Activate peroxisome proliferator-activated nuclear receptors and modulate lipoprotein synthesis and catabolism

  • Activation of PPARα leads to increased synthesis of lipoprotein lipase (LPL)
  • Increased LPL activity results in increased lipolysis of lipoprotein triglycerides
    • moderate reduction in plasma TAGs
    • moderate increase in HDL
    • Variable effects on LDL (so would not be indicated in patients with hypercholesterolaemia)
127
Q

What are the side effects of Propanolol?

A

Common:

  • Hypotension
  • Heart failure
  • Nausea
  • Diarrhoea
  • Bronchospasm
  • Dyspnoea
  • Fatigue
  • Dizziness
  • Abnormal vision
  • Hypoglycaemia
128
Q

What are the side effects of Pindolol?

A

Common:

  • Hypotension
  • Heart failure
  • Nausea
  • Diarrhoea
  • Bronchospasm
  • Dyspnoea
  • Fatigue
  • Dizziness
  • Abnormal vision
  • Hypoglycaemia
129
Q

What are the side effects of Diltiazem?

A

Common (>1%)

  • Bradycardia

Infrequent (0.1–1%)

  • Atrioventricular block
  • Development or worsening of heart failure
130
Q

What are the side effects of Nifedipine?

A

Common (>1%)

  • Nausea
  • vasodilatory effects
    • headache
    • flushing
    • dizziness
    • hypotension
    • peripheral oedema
131
Q

What are the side effects of Icatibant?

A

As yet unknown

132
Q

What are the side effects of Botulinum toxin A?

A
  • Dysphagia
  • Dyspnoea
  • Muscle weakness
  • Paralysis
133
Q

What are the side effects of Neostigmine?

Common (>1%):

Increased salivation

Nausea

Vomiting

Diarrhoea

Abdominal cramps

May lead to a cholinergic crisis with increased cholinergic effects (eg excessive sweating, involuntary defecation and urination, miosis, nystagmus, bradycardia, hypotension, increased muscle weakness leading to fasciculation and paralysis), CNS effects (eg ataxia, seizures, agitation, coma) and death due to respiratory failure or cardiac arrest

A

x

134
Q

What are the side effects of Donepezil?

A

Common (>1%)

  • Nausea
  • Vomiting
  • Diarrhoea
  • Anorexia
  • Abdominal pain
  • Dyspepsia
  • Headache
  • Insomnia
  • Vivid dreams
  • Depression
  • Fatigue
  • Drowsiness
  • Dizziness
  • Tremor
  • Weight loss
  • Muscle cramps
  • Urinary incontinence
  • Increased sweating
  • Hypertension
  • Fainting

Rare (<0.1%):

Neuroleptic malignant syndrome

135
Q

What are the side effects of Phenelzine?

A

Common (>1%)

  • Orthostatic hypotension
  • Sleep disturbances (including insomnia and less commonly hypersomnia)
  • Headache
  • Drowsiness
  • Fatigue
  • Weakness
  • Agitation
  • Tremors
  • Twitching
  • Myoclonus
  • Hyperreflexia
  • Constipation
  • Dry mouth
  • Weight gain
  • Impotence
  • Loss of libido
  • Elevated serum aminotransferases

Infrequent (0.1–1%)

  • Itch
  • Rash
  • Sweating
  • Blurred vision
  • Peripheral oedema
  • Mania

Rare (<0.1%)

  • Hypertensive crisis
136
Q

What are the side effects of Phentolamine?

A

Common (>1%)

Orthostatic hypotension

Reflex tachycardia

Dizziness

Drowsiness

Fatigue

Nasal congestion

Infrequent (0.1–1%)

  • Miosis
  • Inhibition of ejaculation
  • GI irritation
  • Confusion
  • Headache
  • Urinary urgency
  • Dry mouth
  • Intracavernosal:
    • penile pain
    • haematoma

Rare (<0.1%)

  • Intracavernosal:
    • dizziness
    • fibrosis
    • priapism
137
Q

What are the side effects of Phenylephrine?

A

Common (>1%)

  • CNS stimulation
  • nervousness
  • excitability
  • dizziness
  • insomnia
  • tremor

Infrequent (0.1–1%)

  • tachycardia
  • palpitations

Rare (<0.1%)

  • hallucinations (particularly in children)
  • arrhythmias
  • hypertension
  • seizures
  • ischaemic colitis
138
Q

What are the side effects of Prazosin?

A
  • First-dose hypotension
  • Headache
  • Drowsiness
  • Tiredness
  • Weakness
  • Blurred vision
  • Nausea
  • Vomiting
  • Lightheadedness or dizziness upon standing
139
Q

What are the side effects of Quinidine?

A
  • Diarrhoea
  • Nausea
  • Vomiting
  • Loss of appetite
  • Stomach pain/cramps
140
Q

What are the side effects of Vitamin K?

A

Common (>1%)

  • Pain, tenderness and erythema (IM injection)

Infrequent (0.1–1%)

  • Allergic reactions including anaphylaxis (especially with rapid IV injection)

Rare (<0.1%)

  • Haemolytic anaemia
  • Hyperbilirubinaemia
  • Kernicterus (in neonates, especially if preterm)
141
Q

What are the side effects of Heparin?

A
  • Haemorrhage
  • Thrombocytopaenia (platelet deficiency)
  • Osteoporosis
142
Q

What are the side effects of Enoxaparin (Clexane)?

A
  • Haemorrhage
  • Thrombocytopaenia (platelet deficiency)
  • Osteoporosis
143
Q

What are the side effects of Warfarin?

A
  • Haemorrhage (so it is important to titrate the dose, determined by the INR)
144
Q

What are the side effects of Clopidogrel?

A

Common (>1%)

  • Diarrhoea

Infrequent (0.1–1%)

  • GI ulcer

Rare (<0.1%)

  • Thrombotic thrombocytopenic purpura
  • Aplastic anaemia
  • Thrombocytopenia
  • Neutropenia
145
Q

What are the side effects of Abciximab?

A

Development of antibodies (increased risk of thrombocytopenia), Bleeding, Allergic reactions, Thrombocytopenic purpura

146
Q

What are the side effects of Amrinone?

A
  • Increased cardiac work (O2 demand)
  • Increased risk of arrhythmias
  • Thrombocytopaenia
147
Q

What are the side effects of Glycerol trinitrate (GTN)?

A

Most are due to vasodilator effects

Common (>1%)

  • Headache
  • Flushing
  • Palpitations
  • Orthostatic hypotension
  • Fainting
  • Peripheral oedema

Infrequent (0.1–1%)

  • Contact dermatitis (topical)
  • Rebound angina
148
Q

What are the side effects of Carvedilol?

A

Common:

  • Hypotension
  • Heart failure
  • Nausea
  • Diarrhoea
  • Bronchospasm
  • Dyspnoea
  • Fatigue
  • Dizziness
  • Abnormal vision
  • Hypoglycaemia
149
Q

What are the side effects of Spironolactone?

A

Common (>1%)

  • hyperkalaemia
  • hyponatraemia
  • hypochloraemia (especially when combined with thiazide diuretics)
  • weakness
  • headache
  • nausea
  • vomiting
  • mastalgia

Infrequent (0.1–1%)

  • GI cramps
  • diarrhoea
  • ataxia
  • drowsiness
  • confusion
  • impotence
  • gynaecomastia
  • menstrual irregularities
  • mild acidosis
  • renal impairment
150
Q

What are the side effects of Mannitol?

A

No clear side effects attributable to mannitol

151
Q

What are the side effects of Cholestyramine?

A

Adverse effects are dose-related; minimise by starting with low dose and increasing gradually.

Common (>1%)

  • Constipation
  • Abdominal pain
  • Dyspepsia
  • Flatulence
  • Nausea
  • Vomiting
  • Diarrhoea
  • Anorexia

Infrequent (0.1–1%)

  • Increased triglycerides

Rare (<0.1%)

  • Faecal impaction
  • Aggravation of haemorrhoids
  • Steatorrhoea
  • Decreased absorption of fat-soluble vitamins
  • Increased bleeding tendency
  • Hyperchloraemic acidosis
152
Q

What are the side effects of Niacin?

A

Common (>1%)

  • vasodilation
  • face and neck flushing
  • hypotension
  • dyspepsia
  • diarrhoea
  • nausea
  • vomiting
  • hyperpigmentation

Infrequent (0.1–1%)

  • itching
  • rash
  • blurred vision
  • abdominal pain
  • jaundice
  • impaired liver function
  • hyperglycaemia
  • hyperuricaemia
  • nervousness

Rare (<0.1%)

  • hepatic failure
  • myopathy
  • increased creatine kinase
  • gout
  • macular oedema causing visual loss (reversible)
153
Q

What are the side effects of Gemfibrozil?

A

Common (>1%)

  • dry mouth
  • headache
  • myalgia

Infrequent (0.1–1%)

  • AF

Rare (<0.1%)

  • increased aminotransferase concentrations
  • impotence
  • reduced libido
  • depression
  • paraesthesia
  • peripheral neuritis
  • dizziness
  • taste disturbance
  • urticaria
154
Q

What are the indications for use of Propanolol?

A

Administration: Oral (tablet)

  • Hypertension
  • Angina
  • Tachyarrhythmias
  • Tetralogy of Fallot
  • MI
  • Prevention of migraine
  • Essential tremor
  • Phaeochromocytoma (with an alpha-blocker)

Contraindications:

Shock (cardiogenic and hypovolaemic)

Bradycardia (45–50 beats/minute)

Second‑ or third-degree AV block

Severe hypotension

Uncontrolled heart failure

155
Q

What are the indications for use of Pindolol?

A

Administration: Oral (tablet)

  • Hypertension
  • Angina
  • Tachyarrhythmias
  • MI
  • Chronic systolic heart failure as part of standard treatment (eg with ACE inhibitor, diuretics)
  • Prevention of migraine
156
Q

What are the indications for use of Diltiazem?

A

Administration: Oral (tablet or capsule)

  • Angina
  • Hypertension (controlled release)
157
Q

What are the indications for use of Nifedipine?

A

Administration: Oral (tablet)

  • Hypertension
  • Angina
158
Q

What are the indications for use of Icatibant?

A

Administration: Injection

  • Hereditary angioedema
159
Q

What are the indications for use of Botulinum toxin A?

A

Administration: Injection

  • Focal spasticity
  • Cervical dystonia (spasmodic torticollis)
  • Blepharospasm
160
Q

What are the indications for use of Neostigmine?

A

Administration: Injection (subcutaneous or intramuscular)

  • Myasthenia gravis
  • Reversal of neuromuscular blockade induced by non-depolarising neuromuscular blockers
    • Give simultaneously with anticholinergic agent, such as atropine (antidote) or glycopyrronium (anaesthesia) to prevent muscarinic effects (eg. bradycardia)
161
Q

What are the indications for use of Donepezil?

A

Administration: Oral (tablet)

  • Alzheimer’s disease

Contraindications:

GI or ureteric obstruction

Active peptic ulcer

Treatment with drugs with anticholinergic effects

Treatment with drugs that can cause bradycardia

162
Q

What are the indications for use of (MAO inhibitor)?

A

Administration: Oral (tablet)

  • Major depression (second line)
  • Panic disorder (second line)
163
Q

What are the indications for use of Phentolamine?

A

Administration: Injection (IV, IM or intracavernosal)

  • Phaeochromocytoma
  • Erectile dysfunction, with papaverine and/or alprostadil

Contraindications: Peptic ulcers

164
Q

What are the indications for use of Phenylephrine?

A

Administration: Oral (tablet, capsule or liquid), intranasal (spray), intraocular (eyedrops), injection

  • Relief of nasal congestion associated with acute and chronic rhinitis
  • Mild ocular congestion
  • Hypotension due to shock, anaesthesia or drugs, paroxysmal SVT, adjunct to spinal anaesthesia and regional analgesia

Contraindications:

Use within 14 days of MAOI treatment (risk of severe hypertension)

Severe coronary artery disease; the risk of arrhythmias increases in heart disease

Severe or uncontrolled hypertension

165
Q

What are the indications for use of Prazosin?

A

Administration: Oral (tablet)

  • Hypertension

Contraindications:

Heart failure due to mechanical obstruction, eg aortic stenosis

Volume depletion

Treatment with diuretics, beta-blockers, calcium channel blockers

166
Q

What are the indications for use of Quinidine?

A

Administration: Oral (tablet)

  • Atrial fibrillation
167
Q

What are the indications for use of Vitamin K?

A

Administration: Injection (oral, IV or IM)

  • Haemorrhage or threatened haemorrhage due to severe hypoprothrombinaemia
    • eg. from excessive dose of warfarin, hypovitaminosis K
  • Prevention and treatment of haemorrhagic disease of the newborn
168
Q

What are the indications for use of Heparin?

A

Administration: Injection (IV)

  • Prevention of VTE in surgical and high-risk medical patients
  • Treatment of VTE
  • Treatment of ACS
  • Treatment of peripheral arterial occlusion
  • Prevention of arterial thrombosis during coronary angioplasty
  • Prevention of extracorporeal thrombosis during haemodialysis
  • Prevention of extracorporeal thrombosis during cardiopulmonary bypass
  • Treatment of disseminated intravascular coagulation

Contraindications:

  • Severe thrombocytopenia from heparin or LMWH
  • Active bleeding or disease states with an increased risk of bleeding
    • eg. bleeding disorders
169
Q

What are the indications for use of Enoxaparin (Clexane)?

A

Administration: Injection (IV)

  • Prevention of VTE in surgical patients and in medical patients bedridden due to acute illness
  • Treatment of venous thrombosis
  • Prevention of extracorporeal thrombosis during haemodialysis
  • Treatment of acute STEMI, non-STEMI and unstable angina

Contraindications:

  • Severe thrombocytopenia from heparin or LMWH
  • Active bleeding or disease states with an increased risk of bleeding
    • eg. bleeding disorders
170
Q

What are the indications for use of Warfarin?

A

Administration: Oral (tablet)

  • Prevention and treatment of VTE
  • Prevention of thromboembolism in patients with prosthetic heart valves
  • Prevention of stroke in patients with previous MI and increased embolic risk
  • AF and a high risk of stroke or systemic embolism

Contraindications:

Alcoholism

Severe active bleeding or disease states with an increased risk of severe bleeding

eg. severe uncontrolled hypertension, severe hepatic disease, severe thrombocytopenia

Pregnancy (potential teratogenic effects)

171
Q

What are the indications for use of Clopidogrel?

A

Administration: Oral (tablet)

  • Prevention of vascular ischaemic events in patients with symptomatic atherosclerosis (recent ischaemic stroke, recent MI or peripheral arterial disease with intermittent claudication)
  • Non-ST-segment elevation acute coronary syndrome (with aspirin)
  • Adjuvant to reperfusion for STEMI (with aspirin), unless acute CABG is likely

Contraindications:

Severe active bleeding or disease states with an increased risk of severe bleeding

eg. bleeding disorders, severe hepatic disease

Hypersensitivity to a thienopyridine

172
Q

What are the indications for use of Abciximab?

A

Administration: IV

  • Unstable angina and non-STEMI in high-risk patients
  • PCI

Administered with heparin or low-MW heparins and low dose aspirin

173
Q

What are the indications for use of Amrinone?

A

Administration: Injection (IV)

  • Short-term management of severe congestive heart failure (CHF)

Contraindications:

Aortic stenosis

Hypertrophic cardiomyopathy

174
Q

What are the indications for use of Glyceryl trinitrate (GTN)?

A

Administration: Sublingual (spray or tablet), injection (IV) or transdermal (patch)

  • Prevention and treatment of stable angina
  • Heart failure associated with acute MI (infusion)

Contraindications:

Hypovolaemia

Raised intracranial pressure

Treatment with sildenafil, tadalafil or vardenafil (PDE5 inhibitors)

Anaemia

Hypotension

Hypertrophic obstructive cardiomyopathy

Cardiac tamponade

Aortic or mitral stenosis

Cor pulmonale

175
Q

What are the indications for use of Carvedilol?

A

Administration: Oral (tablet)

  • Hypertension
  • Chronic systolic heart failure, as part of standard treatment (eg with ACE inhibitors and diuretics)

Contraindications:

Shock (cardiogenic and hypovolaemic)

Bradycardia (45–50 beats/minute)

Second‑ or third-degree AV block

Severe hypotension

Uncontrolled heart failure

176
Q

What are the indications for use of Spironolactone?

A

Administration: Oral (tablet)

  • Primary hyperaldosteronism
  • Refractory oedema associated with secondary hyperaldosteronism, eg cirrhosis of the liver
  • Hirsutism in females
  • Heart failure

Contraindications: Renal failure

177
Q

What are the indications for use of Mannitol?

A

Administration: Injection (IV)

  • Acute angle-closure crisis unresponsive to conventional treatment
  • Intraocular pressure reduction before intraocular surgery (prevents prolapse of intraocular contents)
  • Prevention of acute renal failure
178
Q

What are the indications for use of Cholestyramine?

A

Administration: Oral (liquid)

  • Hypercholesterolaemia
  • Mixed hyperlipidaemia
  • Itch associated with partial biliary tract obstruction
  • Diarrhoea following ileal resection or disease
179
Q

What are the indications for use of Niacin?

A

Administration: Oral (tablet)

  • Hypercholesterolaemia, mixed hyperlipidaemia or severe hypertriglyceridaemia
  • Pellagra (niacin deficiency - characterised by diarrhoea, dermatitis and dementia)

Contraindications:

Symptomatic hypotension

After recent MI

180
Q

What are the indications for use of Gemfibrozil?

A

Administration: Oral (tablet)

  • Severe hypertriglyceridaemia with risk of pancreatitis
  • Mixed hyperlipidaemia and dyslipidaemia associated with diabetes (second line)

Contraindications:

Treatment with simvastatin

Severe renal impairment

Hepatic impairment

Foundations of Biomedical Science (9 decks)

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