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Cardiovascular > Cardiac DRUGS > Flashcards

Cardiac DRUGS Flashcards

1
Q

Outline the process of platelet plug formation & inhibition

A
  • Platelets (1a,1b,2b,3a) adhere to damaged subendothelium
    • 1a - Collagen 1,2&3
    • 1b - vWF & microfibrils
    • 2b/3a - vWF & fibrinogen
  • Form monolayer, spheres & release a & b granules
    • ⇒ ADP, thromboxane A2 & 5HT
    • ⇒ Aggregation & vasoconstriction
  • Inhibited by PGI2 & NO
    • Inhibits vasoconstriction
    • Inhibits ADP, TcA2 & 5HT release
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2
Q

Outline the class & mechanism of Aspirin

A

Antiplatelet drug

  • Blocks thromboxane A2 pathway of platelet activation by irreversibly acetylating cyclo-oxygenase
  • Effects exist for lifespan of platelet (8-9d)
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3
Q

What are the indications for Aspirin

A
  • Primary prevention - less clear due to bleeding risk, only in high risk pts
  • Secondary prevention - ALL CV disease
  • AF: 75-300mg
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4
Q

Outline the adverse affects/ risk factors/ contraindications of Aspirin

A
  • Bronchospasm in up to 20% asthmatic adults [caution]
  • Gastric side-effects
    • Nausea ⇒ GI bleeds
      • Bleeding from Duodenal > Gastric ulcers
    • [Active/recent ulcer/ bleeding contraindicate]
    • Prophylaxis with PPIs should be considered if Hx
  • Any bleeding disorder contraindicate
    *
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5
Q

What is Aspirin resistance?

A
  • 10% of pts
  • Affects effectiveness of Aspirin
  • Testing of platelet activity not common so rarely identified
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6
Q

What drug interactions occur with Aspirin

A
  • Analgesics: concomitant use
  • Anticoagulands: bleeding risk
  • Antidepressents: bleeding with
    • SSRIs
    • Venlafaxine
  • Cytotoxics: aspirin reduces excretion of methotrexate
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7
Q

Outline the mechanism of Thienopyridines

A

Thienopyridines mechanism;

  • Irreversibly block the binding of ADP to platelet reception
  • ⇒ Prevent expression of the active glycoprotein IIb/IIa receptor
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8
Q

Give examples of thienopyridines

A
  • Ticlopidine (first)
  • Clopidogrel
  • Prasugrel
  • Ticagrelor
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9
Q

Outline the class & mechanims of Clopidogrel

A

Thienopyridine, mechanism;

  • Irreversibly block the binding of ADP to platelet reception
  • ⇒ Prevent expression of the active glycoprotein IIb/IIa receptor
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10
Q

What are the indications for Clopidogrel?

A

Indications;

  • 2º prevention of CV events
    • post-MI/ post-stroke/ **PVD **(75mg)
    • post-PCI + stent insertion (+ Aspirin, 300-600mg loading dose, 75mg)
  • ACS
    • +Aspirin
    • 300-600mg loading dose, 75mg
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11
Q

Outline contraindications & cautions & adverse effects for Clopedigrel

A

Contraindications

  • Hypersensitivity
  • Bleeding problems
  • Severe hepatic impairment

Cautions

  • Bleeding risk
  • Renal impairment

Adverse effects

  • **Skin rash **(distinguish from self-limiting X-ray contrast-media-induced skin rash which occurs 1wk post PCI)
  • GI side effects
  • Bleeding & bruising
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12
Q

Outline the class & mechanism of Prasugrel

Compare to Clopidogrel

A

Thienopyridine, mechanism;

  • Irreversibly block the binding of ADP to platelet reception
  • ⇒ Prevent expression of the active glycoprotein IIb/IIa receptor

Compared to Cloppidogrel;

  • **Earlier onset of anti-aggregatory effects **(<½hr) & less inter-patient varibility
  • P is better in ACS & diabetics
  • P is worse in stroke/ TIA (contraindication)
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13
Q

What are the indications for Prasugrel?

Outling dosing

A
  • **1º or delayed PCI **for ACS
  • Stent thrombosis during clopidogrel therapy
  • Diabetes

Dosing;

  • ​60mg loading, 10mg
  • 5mg in <60kg >75yrs
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14
Q

Outline contraindications & cautions & adverse effects of Prasugrel

A

Contraindications;

  • Hx of CVA/ TIA
  • Hypersensitivity
  • Bleeding problems
  • Severe hepatic impairment

Cautions

  • Bleeding risk
  • Renal impairment
  • Pregnancy & lactation

Adverse effects

  • Skin rash (distinguish from self-limiting X-ray contrast-media-induced skin rash which occurs 1wk post PCI)
  • GI side effects
  • Bleeding & bruising
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15
Q

Outline examples and mechanism of actions of Glycoprotein IIb/IIIa receptor inhibitors

A
  • Abcliximab
    • Monoclonal AB
  • Eptifibatise/ tirofiban
    • Small-molecule GPIIb/IIIa inhibitors
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16
Q

Outline the mechanism of action of Eptifibatise

Outline its indiations

A

IV antiplatelet agent: Small-molecule GPIIb/IIIa receptor inhibitor

Indication:

  • Prevention of early MI in patients presenting with ACS
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17
Q

Outline the mechanism of action of Tirofiban

Outline its indiations

A

IV antiplatelet agent: Small-molecule GPIIb/IIIa receptor inhibitor

Indication:

  • Prevention of early MI in patients presenting with ACS
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18
Q

Outline the mechanism of action of Abiciximab

Outline its indiations

A

Intravenous antiplatelet agent: Monoclonal AB

Indications;

  • Pre-PCI: prevents ischaemic complications
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19
Q

Outline the mechanism of action of angiotensin-converting enzyme inhibitors

Outline AG2 function

A

ACEi block conversion of Angiotensin 1 to Angiotensin 2.

Angiotensin 2 functions;

  1. Massive vasoconstriction
  2. ADH secretion from posterior pituitary
  3. Aldosterone secretion from adrenal gland cortex
  4. Sympathetic activity increase
  5. Renal
    • Na+Cl- reabsorption in proximal tubule (and hence H2O)
    • K+ exretion
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20
Q

Give examples of ACEi

A
  • Captopril
  • Analapril
  • Lisinoprl
  • Ramipril
  • Perindopril
21
Q

Outline the indications for ACEi’s

A
  • Hypertension [all non-black <55yrs]
  • HF [all LVF]
  • Post-MI 2º prevention [all post-MI]
  • CV risk reduction [all CVD]
22
Q

Outline the contraindications & cautions & adverse effects of ACEi’s

A

Contraindications

  • Valvular stenosis
  • Angioedema
  • Hypersensitivity
  • Bilateral renal artery stenosis
  • Pregnancy

Cautions

  • Hypotension (systolic <90mmHg)
  • Patients on high-dose diuretics (ie furosemide >80mg daily)
  • Breast feeding
  • Moderate to severe renal impairment

Adverse effects

  • First-dose hypotension [use long-acting, 1st dose at night, avoid diuresis]
  • Dry cough [may resolve, switch]
  • Angioedema [stop]
  • Rash [switch, stop]
23
Q

Outline the key drug interactions with ACEi’s

A
  • Ciclosporin & potassium: inc risk of hyperkalaemia [low K+ diet]
  • Diuretics: enhances hypotensive effect
  • Lithium: increases lithium levels
24
Q

What monitoring is important for patients on ACEi’s

A
  • Baseline BP & U&Es
    • 2wks then annually
  • Serum creatinine >20% |or| eGFR drops >15%
25
Q

Outline the mechanism of Angiotensin receptor blockers (ARBs)

aka AG2 receptor antagonists, AIIRAs

A
  • Bind to angiotensin 2 receptors and block action of angiotensin 2

Angiotensin 2 function

  • Angiotensin 2 functions;
  • Massive vasoconstriction
  • ADH secretion from posterior pituitary
  • Aldosterone secretion from adrenal gland cortex
  • Sympathetic activity increase
  • Renal
    • Na+Cl- reabsorption in proximal tubule (and hence H2O)
    • K+ exretion
26
Q

For ARBs, outline;

  • Indications
  • Contraindications & Cautions & Adverse affects
  • Monitoring
  • Drug interactions
A

Indications

  • 2nd line to ACEi

Contraindications & Cautions & Adverse affects

  • Same as ACEi

Monitoring

  • Same as ACEi

Drug interactions

  • Same as ACEi
27
Q

Give examples of ARBs

A

Sartan’s

  • Candesartan
  • Irbesartan
  • Losartan
  • Telmisartan
  • Valsartan
28
Q

Outline the mechanism of Aldosterone antagonists

Aldosterone functions

A

Structurally similar to aldosterone & competitively binds to mineralocorticoid receptor

Aldosterone function;

  1. Upregulates and activates basolateral Na+/K+ pumps
  2. Upregulates epithelial sodium channels
  3. Secretes K+
  4. Secretes H+ for Na+ (regulating plasma bicarbonate HCO3-)

Normal mechanism;

  • Stimulated by angiotensin 2
  • Released from adrenal gland cortex
29
Q

Give examples of Aldosterone antagonists

A
  • Eplerenone
  • Spironolactone
30
Q

Outline the indications for aldosterone antagonists

A
  • HF (25-50mg)
  • Post-MI HF (EF <40%, 3-14d of MI)
  • Hypertension (step 4)
31
Q

Outline the contraindications & cautions & adverse affects of Aldosterone antagonists

A

Contraindications

  • Hypersensitivity
  • Serum K+ >5mmol/L
  • Renal/ hepatic failure (severe, mod=caution)
  • Anuria

Adverse affects

  • Hyperkalaemia [common, diet]
  • Renal dysfunction [common, withdrawal]
  • Gynaecomastia [eplerenone has no progesterone effects]
  • GI…
  • Menstral irregularities
  • Rash
32
Q

Outline drug interactions with aldosterone antagonists

A
  • Hyperkalaemia
    • ACEi & ARBs
    • Potassium
    • Ciclosporin
  • Eplerenone plasma levels
    • Antiarrhythmic’s
    • Antibacterial’s
    • Antidepressant’s
    • Antifungal’s
    • Antiviral’s
  • Lithium
33
Q

Outline the mechanism of action of Beta-adrenoceptor blokers (B-blockers)

A
  • Block action of noradrenaline at B-adrenoceptors
  • Located in;
    • Myocardium
    • Throughout circulatory system
  1. Inhibit sympathetic stimulation of HR & myocardial contractility
    • -ve chronotropic [speed]: slow SA node firing
    • -ve inotropi [contractility]
    • Anti-arrhythmic & anti-ischaemic
  2. Lower BP (unclear, lowers renin/ sympathetic tone?)
34
Q

Give examples of B-blockers

A
  • Atenolol
  • Bisoprolol
  • Metoprolol
  • Nebivolol
  • Carvedilol
35
Q

Outline the indications for B-blockers

A
  • HF (bisopro, carvedi, nebivo)
  • Post-MI 2º prevention
  • Angina (1st line, HR 50-60)
  • AF (1st line)
36
Q

Outline the contraindications & cautions & adverse effects of B-blockers

A

Contraindications

  • Asthma/ bronchospasm
  • 2nd/ 3rd degree heart BLOCK
  • PVD
  • Patients on Verapamil

Cautions

  • COPD
  • uncontrolled HF, sick sinus syndrome, hypotension, bradycardia
  • Prenancy/ breast feeding

Adverse effects

  • Bradycardia (HR <50bpm)
  • Symptomatic hypotension
  • Bronchospasm (swap + supervise)
  • Fatigue
  • Cold-extremities (gloves/ socks)
  • Sleep disturbances (water-soluble agent)
37
Q

Outline the mechanism of action of calcium-channel blockers (CCBs)

A
  • Inhibit inward movement of calcium ions through slow channels in myocardial cells
  • Dihydropyridine (DHP): Affinity for vascular smooth muscle
    • peripheral vasodilation
    • Reduced BP
    • Reduced afterload
  • non-DHP: Affinity for myocardial cells & conduction system
    • Negative inotropy
    • Myopcardial depression
    • AV conduction delay
38
Q

Give examples of calcium channel blockers & their types

A

Dihydropyridine (DHP) CCBs

  • Amlodipine
  • Nifedipine
  • Felodipine
  • Lacidipine

Non-DHP CCBs

  • Diltiazem
  • Verapamil
39
Q

Outline the indications for CCBs

A
  • Angina
    • 2nd to B-blockers or DHPs in conjunction
  • Hypertension
    • 2st line in black/ >55yrs
  • AF (2nd line, non-DHP: verapamil)
40
Q

Outline the contraindications & cautions & adverse effects of CCBs

A

Contraindications

  • Cardiogenic shock/ aortic stenosis/ post-acute MI/ ACS
  • non-DHPs: dangeous arrhythmias/ LVF

Cautions

  • Worsening HF

Adverse effects

  • non-DHP: Bradycardia (reduce)
  • Symptomatic hypotension (reduce)
  • Flushing (dissipates/ time)
  • GI disturbances
  • Ankle oedema (reduce/ +ACEi/ ARB)
  • Gingival hypeplasia (change)
41
Q

Outline the mechanism of Nitrates

A
  • Vaso/ veno dilatory efects
    • Inc coronary blood flow
    • Reduce preload & afterload
    • (Low workload = low oxygen demand)
  • Prevent coronary spasm & vasoconstriction induced by exercise
42
Q

Give examples of nitrates

A
  • Glyceryl trinitrate (GTN)
  • Isosorbide mononitrate
  • Isosorbide dinitrate
43
Q

Outline the indications for nitrates

A
  • Angina
44
Q

outline the contraindications & cautions & adverse effects of nitrates

A

Contraindications

  • Hypersensitivity
  • Any hypovolaemic/ tensive condition
  • Any containing heart disease (restrictive/ constrictive/ stenosed)
  • Cerebral haemorrhage

Cautions

  • Hypothyroidism
  • Closed-angle glaucoma

Adverse effects

  • Hypotension
  • Headache (cerebral vasodilation)
45
Q

Outline the mehanism of action of potassium-channel activators

A

Opening potassium channels leads to arterial vasodilation and reduced afterload

Nicorandil also has nitrate-like action: venous dilation & reduced preload

46
Q

Give examples of potassium-channel activators

A
  • Nicorandil
47
Q

Outline the indications for potassium-channel activators

A
  • Angina (adjunct or alternative)
48
Q

Outline the contraindications & cautions & adverse effects of potassium-channel activators

A

Contraindications

  • Cardiogenic shock
  • LVF/ hypotension
  • Hypertensitivity
  • Pregnancy & breast feeding

Cautions

  • Haemodynamically unstable/ MI/ failure/ low pressure
  • No driving/ machinary until sure not affects

Adverse effects

  • Headache
  • Dizziness & hypotension
  • Peripheral vasodilation
  • Ulceration (GI/ skin/ mucosa, change)
  • Angiodema

Cardiovascular (18 decks)

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