Cardiovascular Drugs Flashcards
What are some examples of cardioselective beta-blockers?
Bisoprolol
Atenolol
What is the mechanism of action for cardioselective beta-blockers?
- Cardioselective beta-1-adrenoceptor antagonist.
- Preferentially blocks beta-1 receptors in cardiac and renal tissue.
- Inhibits sympathetic stimulation of the heart and renal vasculature.
- Blockade of SAN reduces HR(negative chronotropic effect) and blockade of receptors in the myocardium depresses cardiac contractility (negative inotropic effect).
- blockade of beta-1 adrenoceptors in renal tissue inhibits release of renin, depressing vasoconstrictive effects of the RAAS.
What are the indications of cardioselective beta-blockers
- Hypertension
- Angina
- Rate-control in atrial fibrillation
- Carvedilol or Bisoprolol may be used as part of supportive therapy for mild / moderate heart failure.
List the side effects of cardioselective beta-blockers
- Bradycardia
- Hypotension
- Bronchospasm
- Fatigue (Can affect up to 10% of patients)
- Cold extremities
- Sleep disturbances
- Loss of hypoglycaemic awareness
What is important clinically regarding Pharmacokinetics/dynamics for cardioselective beta-blockers?
- Avoid higher doses & use with caution in patients with Asthma COPD – risk of bronchospasm.
- Avoid in patients with Hx of frequent hypoglycaemia.
- Do not combine Beta-Blockers with rate-limiting Ca2+-Channel-Blockers (Verapamil / Diltiazem) in anti-hypertensive therapy, - risk of heart-block.
What information should you tell the patient before starting on a cardioselective beta blocker
- Compliance is important – hypertension is asymptomatic but nonetheless a dangerous risk factor that needs controlled.
- Fatigue and cold extremities are common side-effects.
What are some examples of non-cardioselective beta-blockers?
Propranolol
Carvedilol
What is the mechanism of action for non-cardioselective beta-blockers?
- Propanolol: Non-cardioselective beta-1-adrenoceptor antagonist.
- Carvedilol: Non-selective beta-1, beta-2 and alpha-1-adrenergic receptor antagonistic effects.
- Inhibits sympathetic stimulation in the heart and vascular smooth muscle.
What are the indications of non-cardioselective beta-blockers?
- Hypertension
- Angina
- Anxiety
- Migraine prophylaxis
- Post-MI prophylaxis
- Carvedilol or Bisoprolol may be used as part of supportive therapy for mild / moderate heart failure.
List the side effects of non-cardioselective beta-blockers
- Bradycardia
- Hypotension
- Bronchospasm
- Fatigue (Can affect up to 10% of patients)
- Cold extremities
- Sleep disturbances
- Loss of hypoglycaemic awareness
What is important clinically regarding Pharmacokinetics/dynamics for non-cardioselective beta-blockers?
Caution in diabetic patients – risk of deranged CHO metabolism
Avoid in patients with Asthma & COPD – risk of bronchospasm
Do not combine Beta-Blockers with rate-limiting Ca2+-Channel-Blockers (Verapamil / Diltiazem) in anti-hypertensive therapy.
Propanolol is lipid-soluble and is mostly cleared by the liver. Avoid in liver impairment. Avoid abrupt withdrawal – risk of liver impairment.
What information should you tell the patient before starting on a non-cardioselective beta blocker
- Nightmares and sleep disturbances may occur.
- Compliance is important – hypertension is asymptomatic but nonetheless a dangerous risk factor that needs controlled.
- Fatigue and cold extremities are common side-effects.
What are some examples of ACE Inhibitors?
Ramipril
Enalapril
Lisinopril
Perindopril
What is the MoA for ACE Inhibitors?
- Inhibits conversion of Angiotensin I to Angiotensin II (a more potent systemic vasoconstrictor).
- This inhibits Aldosterone release from the adrenal cortex, depressing renal sodium and fluid retention, thereby decreasing blood volume.
What are the indications for ACE Inhibitors?
- Hypertension
- Heart Failure
- Nephropathy
- Prevention of Cardiovascular events in high risk patients
List some side effects of ACE Inhibitors:
- Dry cough (10% of Patients, causing cessation of treatment in 5%)
- Hypotension
- Hyperkalaemia
- Renal Impairment
- Angioedema
What is important clinically regarding Pharmacokinetics/dynamics for ACE Inhibitors?
Adverse drug reactions are higher in patients with:
High-dose diuretic therapy / Hypovolaemia / Hyponatraemia / Hypotension / Unstable Heart Failure / Renovascular disease
What information should you tell the patient before starting on an ACE Inhibitor
- Blood test required at 1-2 weeks to check electrolyte balance.
- Dry cough is a common side-effect.
What are some examples of Nitrates?
Isosorbide Mononitrate Glyceryl Trinitrate (GTN)
What is the MoA for Nitrates?
• Converted to Nitric Oxide, a potent vasodilator.
Cardioselective, acting predominantly on coronary blood vessels, enhancing flow of blood to ischaemic areas of the myocardium.
• reduces myocardial oxygen consumption by reducing cardiac preload and afterload.
What are the indications for Nitrates?
- Treatment of Angina
* Severe hypertension (intravenous GTN is sometimes used in this setting)