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DRUGS Flashcards

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1
Q

Thiazide Diuretics: Examples

A

Bendroflumethiazide, Indapamide, Chlortalidone

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2
Q

Thiazide Diuretics: Mechanism of Action

A

Blocks Na+/Cl- co-trasnporter of DISTAL convoluted tubule of kidney. Stops Na from being reabsorbed so water stays in DCT.

Also have vasodilating effects

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3
Q

Thiazide Diuretics: Indications

A

First-line treatment for HTN when CCBs are contraindicated (e.g. in oedema)
Also add on to ACEis and CCBs

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4
Q

Thiazide Diuretics: Dose, prescribing and route

A

PO, 2.5mg OD

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5
Q

Calcium Channel Blockers: Examples

A

Amlodipine, Nifedipine, Verapamil, Diltiazem

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6
Q

Calcium Channel Blockers: Mechanism of Action

A

Block entry of Ca to muscle cells (myocytes or arterial SMCs) to prevent contraction. They hence vasodilator and slowing of heart rate.

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7
Q

Calcium Channel Blockers: Types

A

DIHYDROPYRIDINES: Selective to vessels: help to vasodilator and reduce blood pressure (AMLODIPINE, NIFEDIPINE)
NON-DIHYDROPYRIDINES: Selective for cardiac tissue help to reduce contractility and heart rate (verapamil and diltiazem)

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8
Q

Calcium Channel Blockers: Indications

A
  • First or second line for HTN
  • First line for stable angina (reducing rate and contractility reduces mycote requirement)
  • Verapamil and diltiazem are cardiac specific and so can be used for arrhythmias (AF)
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9
Q

Calcium Channel Blockers: Adverse effects

A

Leg swelling, flushing, headache and palpitations

Verapamil can cause constipation and worsen heart failure

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10
Q

Angiotensin Receptor Blockers: Examples

A

Losartan, Candesartan, Irbesartan

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11
Q

Angiotensin Receptor Blockers: Mechanism of Action

A

Produced in RAAS system. Angiotensin II acts on SMCs or arteries to cause vasoconstriction.
ARBs block the AT1 angiotensin receptor on SMCs
- Dilates efferent nephron arteries reducing pressure in kidney and limiting damage here
- Reducing aldosterone levels and hence increasing sodium and water excretion

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12
Q

Angiotensin Receptor Blockers: Adverse Effects

A

Hypotension, Hypokalaemia (due to aldosterone drop)

Renal failure

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13
Q

Angiotensin Receptor Blockers: Prescribing, Dose and Route

A

PO 50mg OD (12.5mg if for heart failure). Titrate up.

Second line HTN treatment (with ACEi or CCB), third line is to add a TZD.

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14
Q

ACEis: Examples

A

Ramipril, Lisonopril, Perindopril

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15
Q

ACEis: Mechanism of Action

A

Inhibits Angiotensin covering enzyme and so stops angiotensin II from being produced. Prevents vasoconstriction and so PVR drops. No aldosterone secretion and so water and salt are excreted more.
- Dilates efferent nephron arteriole limiting kidney damage

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16
Q

ACEis: Indications

A
  • First line for HTN <55yo
  • Useful in chronic heart failure
  • Reduced risk of cardiac events in IHD
  • Useful in diabetic nephropathy
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17
Q

ACEis: Prescribing, Dose and Route

A

PO 2.5mg OD (lower dose for heart failure)

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18
Q

Loop Diuretics: Examples

A

Furosemide and Butenamide

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19
Q

Potassium Sparing Diuretics: Examples

A

Spironolactone, Amiloride, Eplenerone

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20
Q

Potassium Sparing Diuretic: Mechanism of Action

A

Blocks aldosterone receptors in the kidney to decrease reabsorption of sodium and water in the kidney tubule. MAINTAINS REABSORPTION OF POTASSIUM (Spironolactone)

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21
Q

Potassium Sparing Diuretic: Indications

A

Rarely used as first line diuretics but used consequentially when the patient develops hypokalaemia
Spironolactone can also be used to treat excessive hair growth and acne in women and early puberty in boys
- HTN due to hyperaldosteronaemia (CONN’S SYNDROME)

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22
Q

Potassium Sparing Diuretic: Adverse Effects

A

Spironolactone: hyperkalaemia, nausea, vomiting, headache, rashes, dizziness, decreased libido and gynecomastia in men

Amiloride: GI upset, dizziness, hypotension and urinary symptoms

Be wary of effect of lithium and digoxin clearance

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23
Q

Potassium Sparing Diuretic: Route, Prescribing and Dose

A

Spironolactone is PO 25-50mg. Best to take in morning.
Amiloride is most often given as CO-AMILOFRUSE (contain amiloride and furosemide). Usually contain 2.5mg of amiloride and 20mg of furosemide

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24
Q

Warfarin: Mechanism of Action

A

Clotting factors 2, 7, 9 and 10 require vit K to be present, in its reduced form, to be synthesised by liver. Warfarin blocks the enzyme that reduces vitamin K (vitamin K epoxide reductase)

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25
Warfarin: Indications
AF Heart valve replacement Someone at high risk of blood clots
26
Warfarin: Adverse effects
Easy bruising and bleeding | Always stop 4 days prior to surgery (replace with heparin in hospital)
27
Warfarin: Dosage Control
Dose extremely variable. Decided by monitoring their International Normalised Ratio (INR). INR = Patients PT/ Standard PT Aim for INR 2.0-3.0 (3.5 if valve replacement)
28
Anti-Platelets: Examples
Aspirin and Clopidogrel
29
Anti-Platelets (Aspirin): Mechanism of Action
Aspirin is a COX inhibitor that is weakly more selective for COX-1. Inhibiting COX reduces production of prostaglandins which cause vasoconstriction and platelet aggregation
30
Anti-Platelets (Clopidogrel): Mechanism of Action
Binds to ADP receptors on platelets stopping them from aggregating
31
Anti-Platelets: Indications
ACS to help inhibit platelet aggregation and limits arterial thrombosis - Long term preventing in pro-thrombotic disorders (high risk of MI) - Reduce risk of thrombus in AF when warfarin or NOAC is contraindicated - Clopidogrel used to prevent occlusion of stents - Aspirin can be used for mild to moderate pain
32
Anti-Platelets: Adverse Effects & interactions
ASPIRIN: - GI upset and gastric ulceration, haemorrhage. High dose can cause tinnitus, hearing problems, hyperventilation due to bronchospasm and metabolic acidosis CLOPIDOGREL: mostly to do with bleeding (can be serious if GI or intra-cranial). Dyspepsia and diarrhoea also common
33
Anti-Platelets: Route, Prescribing and Dose
PO (aspirin can be given per rectum if high dose needed) ACS: loading dose of 300mg and follow-uo of 75mg - Consider PPI with aspirin, encourage to take with food
34
Thrombolytics: Examples
Tissue Plasminogen Activator (TPA), Streptokinase
35
Thrombolytics: Mechanism of action
Drugs that break down blood clots that have already formed. Helps turn plasminogen into plasmin which lyses fibrin meshes. tPA is direct copy of endogenous enzyme
36
Thrombolytics: Indications
PE MI Stroke
37
Thrombolytics: Adverse effects
Streptokinase has a very short half life. Over-bleeding and haemorrhage is risk People can have hypersensitivity to streptokinase (sourced from bacteria). tPA doesn't have many AEs and so is used preferentially
38
Thrombolytics: Route, Prescribing and Dose
IV infusion, 100mg over 3 hours | Time window for prescribing is small (Usually within 3-4 hours but trust dependent)
39
Heparin: Examples
Fondaparinux, Tinzaparin, Enoxaparin, Dalteparin
40
Heparin: Types
Most common is LMWH: inhibits factor Xa and thrombin (common pathway) Also Unfractioned Heparin: activates antithrombin that then, in turn, inhibits factor Xa and thrombin
41
Heparin: Indications
LMWH given prophylactically and widely in hospital as part of VTE prevention pathways LMWH and fondaparinux are commonly given in ACS care as well
42
Heparin: Route
Sc injection ideally in abdo wall
43
Heparin: Prescribing and Dose
VTE control: 40mg tinza or enoxaparin | - Higher doses used when in treatment pathway for ACS
44
NOACs: Examples
Rivaroxaban, Apixaban
45
NOACs: Mechanism of action
Work in a similar way to heparin then directly inhibit factor Xa in the coag cascade
46
NOACs: Indications
Prophylaxis for VTE (esp in patients with joint replacement) Treatment of DVT and PE Prophylaxis of stroke Prophylaxis of clot in NON-VALVULAR AF
47
NOACs: Adverse effects
Bleeding is main AE Hypotension, nausea and vomiting Avoid in those with active bleeding, malignant neoplasms, oesophageal varices or anyone who's had surgery recently Avoid in pregnancy NOT LICENSED for use in people with prosthetic valves
48
NOACs: Route, Prescribing and Dose
PO, 2.5mg BD usually elevated to 10mg BD and then back down to 5mg BD maintenance dose
49
Amiodarone: Mechanism of Action
Blocks sodium, potassium and calcium channels and antagonises alpha AND beta adrenergic receptors. Reduces spontaneous depolarisation, slow conduction velocity (conductivity) and increases cells' resistance to depolarisation (refractoriness). Does this throughout myocardium and at AV node hence reducing ventricular contraction rate in AF
50
Amiodarone: Indications
Management of arrhythmias Management of AF Management of SVT, VT and VF
51
Amiodarone: Adverse effects
Can cause hypotension (if IV infusion). If used chronically can cause: - Pneumonitis - Bradycardia and AV block - Hepatitis - Photosensitivity and grey coloration of skin - Thyroid abnormalities (Contains iodine) * *very long half life. * **lots of interactions: increase conc. of digoxin, diltiazem and verapamil
52
Amiodarone: Prescribing
Should not be offered long term due to adverse effects
53
Beta-Blockers: Mechanism of action
BETA RECEPTORS: Beta-2 in tubes and Beta 1 found in heart. When beta-1 are stimulated they increase rate and contractility of heart. BBs block this
54
Beta-Blockers: Examples
Atenolol, Propanolol, Bisoprolol, Metoprolol
55
Beta-Blockers: Indications
1. First line for IHD (angina and ACS): improve sx and prog. 2. First line for AF: stabilise heart beat and regain sinus 3. Chronic heart failure: decrease contractility and stop heart enlarging 4. First line for SVT: restore sinus rhythm 5. HTN: second line. Control renin secretion in kidney as well as vasodilator
56
Beta-Blockers: Adverse effects and interactions
Headaches, cold extremities, Fatigue, GI upset, Sleep disturbances, Impotence in men DO NOT USE IN ASTHMATICS: bronchoconstriction can cause asthma attack (usually okay in COPD - use atenolol: good B1 selectivity) DO NOT USE WITH NON-DIHYDROPYRIDINE CCBs: verapamil and diltiazem
57
Beta-Blockers: Route, Dose and prescribing
PO, 12.5mg TD then titrate up
58
Cardiac Glycoside: Examples
Digoxin
59
Cardiac Glycoside: Mechanism of action
Reduce contractility of the heart by blocking Na+/K+ pumps meaning Na+ accumulates in myocyte, therefore Ca can't move out of the cell (exchanged). High Ca means contractility increases. Glycosides also increase parasympathetic tone and decrease conduction at AVN and hence decrease rate
60
Cardiac Glycoside: Indications
1. AF (increase parasympathetic tone and blocking at AVN sinus rhythm is established (BB better) 2. Heart failure (usually 3rd line after ACEi, BB and aldosterone agonist)
61
Cardiac Glycoside: Adverse effects and interactions
- Bradycardia - Dizziness - GI upset - Rash - Visual disturbances * Narrow TPI. At too high dose can cause arrhythmias * *Dont give in heart block or arrhythmia patients * **reduce dose in renal failure * ***be wary in electrolyte balance * ****be wary with loop and TZDs
62
Cardiac Glycoside: Route, prescribing and dose
PO (effect within 2 hours) IV (effect within 30 mins) Large volume of distribution: LOADING DOSE: 500micrograms followed by 250micrograms 6 hours later then 125-250microgram OD maintenance dose
63
Nitrates: Examples
Glyceryl Trinitrate (GTN), Isosorbide mononitrate
64
Nitrates: Mechanism of Action
Vasodilators which help to relieve sx of ischaemia. Converted to NO in body which is endogenous vasodilator: Increase production of cGMP reducing intracellular Ca which reduces contraction. Venous dilation reduces preload reducing cardiac work and myocardial O2 demand helping to relieve angina and cardiac failure.
65
Nitrates: Indications
1. GTN is short acting for treatment of acute angina and ACS 2. Isosorbide mononitrate is long action and used prophylactically for angina where BB or CCB not tolerated 3. IV nitrate used for pulmonary oedema +furosemide ++oxygen
66
Nitrates: Adverse Effects and Interactions
Vasodilatory effects: - Flushing - Headaches - Dizziness - Hypotension * can build up a tolerance to them * *do not give in patients with severe aortic stenosis, might cause cardiovascular collapse. Avoid in hypotensive patients.
67
Nitrates: Route, Prescribing and Dose
Sublingual spray or tablet. GTN half life <5min | GTN can also be given IV (50mg/50mL)
68
Statins: Examples
Simvastatin, Atorvastatin, Pravastatin, Rosuvastatin
69
Statins: Mechanism of Action
Inhibit HMG CoA Reductase which is en enzyme involved in making cholesterol. Encourage clearance of LDL and slightly increase HDL
70
Statins: Indications
1. 1ry prevention of cardiovascular disease. Always given in people >40yo with >20% risk of CVD in next 10 years 2. 2ry prevention of CVD (those that have already had an event) 3. Primary hyperlipidaemia and hypercholesterolaemia
71
Statins: Adverse Effects and Interactions
RARE Headaches, GI upset Myalgia: in severe cases can cause rhabdomyolysis Can cause raise in liver enzymes *use in caution in hepatic or renal impairment patients **metabolised by CYP450 so drugs that act on this system (amiodarone, diltiazme and macrocodes will have an effect on serum levels)
72
Statins: Route, Prescribing and Dose
PO, 40mg OD (50mg for atorva). Higher doses are used for 2ry prevention
73
What is an Ionotrope? | Give some examples
A drug which changes the force of contraction. | Digoxin, Amiodarone, BBs
74
What is a Chronotrope? | Give some examples
A drug that changes the rate of contraction. | Beta-Blockers, Amiodarone, Digoxin

CARDIOVASCULAR (2 decks)

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