Cardiac DRUGS Flashcards
(48 cards)
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
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)
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
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
- Nausea ⇒ GI bleeds
- Any bleeding disorder contraindicate
*
5
Q
What is Aspirin resistance?
A
- 10% of pts
- Affects effectiveness of Aspirin
- Testing of platelet activity not common so rarely identified
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
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
8
Q
Give examples of thienopyridines
A
- Ticlopidine (first)
- Clopidogrel
- Prasugrel
- Ticagrelor
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
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
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
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)
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
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
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
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
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
18
Q
Outline the mechanism of action of Abiciximab
Outline its indiations
A
Intravenous antiplatelet agent: Monoclonal AB
Indications;
- Pre-PCI: prevents ischaemic complications
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;
- 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
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
Outline the mechanism of Angiotensin receptor blockers (ARBs)
aka AG2 receptor antagonists, AIIRAs
* 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
For ARBs, outline;
* Indications
* Contraindications & Cautions & Adverse affects
* Monitoring
* Drug interactions
Indications
* 2nd line to ACEi
Contraindications & Cautions & Adverse affects
* Same as ACEi
Monitoring
* Same as ACEi
Drug interactions
* Same as ACEi
27
Give examples of ARBs
Sartan's
* Candesartan
* Irbesartan
* Losartan
* Telmisartan
* Valsartan
28
Outline the mechanism of Aldosterone antagonists
Aldosterone functions
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
Give examples of Aldosterone antagonists
* Eplerenone
* Spironolactone
30
Outline the indications for aldosterone antagonists
* HF (25-50mg)
* Post-MI HF (EF \<40%, 3-14d of MI)
* Hypertension (step 4)
31
Outline the contraindications & cautions & adverse affects of Aldosterone antagonists
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
Outline drug interactions with aldosterone antagonists
* Hyperkalaemia
* ACEi & ARBs
* Potassium
* Ciclosporin
* Eplerenone plasma levels
* Antiarrhythmic's
* Antibacterial's
* Antidepressant's
* Antifungal's
* Antiviral's
* Lithium
33
Outline the mechanism of action of Beta-adrenoceptor blokers (B-blockers)
* 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
Give examples of B-blockers
* Atenolol
* Bisoprolol
* Metoprolol
* Nebivolol
* Carvedilol
35
Outline the indications for B-blockers
* **HF** (bisopro, carvedi, nebivo)
* **Post-MI 2º prevention**
* **Angina** (1st line, HR 50-60)
* **AF** (1st line)
36
Outline the contraindications & cautions & adverse effects of B-blockers
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
Outline the mechanism of action of calcium-channel blockers (CCBs)
* **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
Give examples of calcium channel blockers & their types
Dihydropyridine (DHP) CCBs
* Amlodipine
* Nifedipine
* Felodipine
* Lacidipine
Non-DHP CCBs
* Diltiazem
* Verapamil
39
Outline the indications for CCBs
* Angina
* 2nd to B-blockers or DHPs in conjunction
* Hypertension
* 2st line in black/ \>55yrs
* AF (2nd line, non-DHP: verapamil)
40
Outline the contraindications & cautions & adverse effects of CCBs
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
Outline the mechanism of Nitrates
* Vaso/ veno dilatory efects
* Inc coronary blood flow
* Reduce preload & afterload
* (Low workload = low oxygen demand)
* Prevent coronary spasm & vasoconstriction induced by exercise
42
Give examples of nitrates
* Glyceryl trinitrate (GTN)
* Isosorbide mononitrate
* Isosorbide dinitrate
43
Outline the indications for nitrates
* Angina
44
outline the contraindications & cautions & adverse effects of nitrates
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
Outline the mehanism of action of potassium-channel activators
Opening potassium channels leads to arterial vasodilation and reduced afterload
Nicorandil also has nitrate-like action: venous dilation & reduced preload
46
Give examples of potassium-channel activators
* Nicorandil
47
Outline the indications for potassium-channel activators
* Angina (adjunct or alternative)
48
Outline the contraindications & cautions & adverse effects of potassium-channel activators
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
