Drugs Flashcards
How do organic nitrates work? Give two examples
Relax all types of smooth muscle
- Glyceryltrinitrate (short acting)
- Isosorbide mononitrate (long acting)
How is GTN given?
Sublingual - tablet or spray in stable angina
IV in unstable angina/MI
How is ISMN given?
Orally for prophylaxis of angina
- take in morning and at lunch in order to have ‘nitrate low period’ for rest of day to avoid tolerance
What are some side effects of nitrates?
Headaches Hypotension and fainting Reflex tachycardia (co-administer beta-blocker) Tolerance Formation of methaemoglobin (rare)
How do CCBs work?
Block Ca entry into cells, therefore reducing muscle contraction
Act on L-type Ca channels found in heart, smooth muscle and other locations
Which conditions are CCBs used in?
Hypertension
Stable angina
HR control in supra ventricular arrhythmias
Give 3 examples of CCBs and what is their selectivity for different channels?
Verapamil –> relatively selective for cardiac channels
Diltiazem –> intermediate selectivity
Amlodipine –> relatively selective for smooth muscle
Which CCBs are preferred for use in hypertension and angina, and why?
Drugs selective for smooth muscle
e.g. Amlodipine and nifedipine
To minimise unwanted cardiac effects
In which cardiac conditions should CCBs be avoided/stopped?
Heart failure
Heart block
Having which two conditions concurrently makes CCBs particularly useful?
Hypertension and angina
What are the side effects of CCBs?
hypotension
dizziness
flushing
ankle oedema
How do CCBs help in supraventricular arrhythmias? Which CCB is usually used?
Suppress conduction through the AV node
Verapamil
What is angiotensin converting enzyme (ACE) and what effects does it have?
Enzyme on surface on endothelial cells
- converts angiotensin I to angiotensin II –> vasoconstriction
- inactivates bradykinin (vasodilator)
What is the mode of action of ACE inhibitors?
Block conversion of angiotensin I to angiotensin II
What is the mode of action of angiotensin receptor blockers (ARBs)?
Block action of angiotensin II
What are some side effects of ACE inhibitors?
Initial hypotension (especially if taking diuretics) Dry cough (bradykinin in the lungs) Hyperkalaemia Angioedema Renal dysfunction
What are some side effects of ARBs?
Same as ACE inhibitors but
NO DRY COUGH
–> as no effect on bradykinin
Can ACE inhibitors or ARBs be given in pregnancy?
NO –> foetal toxicity
Can ACE inhibitors/ARBs be used in renal disease?
Should not be used in bilateral renal artery stenosis
BUT
ACE inhibitors good in diabetic nephropathy