Pharmacology Flashcards
Selective HCN chanel blocker
Used in ____
Ivabradine
Angina - decreases HR and increases cardiac efficiency
β agonists eg.s
catecholamines - doputamine (β selective)
adrenaline
noradrenaline
In cardiac arrest adrenaline is given ____
Its effects are ___ (and give receptors)
IV
+ve chrono and iono (β1) peripheral vasoconstriction (α1) dilate coronary arteries (β2)
Dobutamine is given in ____ by ___ route
acute HF eg. post-op/shock
IV
β antagonists eg.s
propranolol (non-selective)
atenolol, bisoprolol, metoprolol (β1 selective)
Effect of β-blockers on HR, force, O2 requirement and exercise tolerance
decrease HR, force (therefore CO), O2 requirement (although non-selective cause coronary vessels to constrict) and exercise tolerance
Uses of β-blockers
AF and SVTs - delay at AVN
Angina - increase diastole = LV perfused
Post-MI
Compensated HF - low dose eg. carvedilol (also α1 antagonist)
adverse effects of β-blockers
bronchospasm
aggravate HF - if rely on sympathetic drive for CO
bradycardia/heart block
hypoglycaemia - glucose release in liver is β2 controlled
fatigue
cold extremities
non-selective competitive muscarinic ACh receptor antagonist eg. and effect
atropine
for bradycardia
increases HR
Drug that blocks NaKATPase on sarcolemma to increase influx of sodium and calcium => increased CICR and contractility
Digoxin
Use for HF with AF
digoxin
Indirectly increases vagal activity and slows SAN and AVN
digoxin
Digoxin toxicity may occur if ____
Unwanted effects=
hypokalaemic (competes w. K for space on NaKATPase) self-repeating tachycardia heart block GI yellow vision
Calcium sensitiser eg.
Mode of action
indication for use
levosimendan
sensitises troponin C for Ca2+ and vasodilation
IV for acute decompensated HF
Inodilator eg.s
Mode of action
Indication for use
milrinone amrinone
inhibit PDE => increase cAMP in cardiac and SM cells => increase contractility and decrease TPR
IV in acute HF
AT1 receptor blockers (ARBs) eg.
losartan, valsartan
ARB and ACEI indications for use
hbp, HF, post-MI, reduce oedema in HF
NOT IN PREGNANCY
Organic Nitrates benefits for angina __
decrease preload - mainly venodilators
decrease afterload (at high dose also = arteriodilators)
dilate coronary collaterals to supply ischaemic area
Organic Nitrates eg.s
Indications
isosorbide mononitrate - PO morning and lunch to stop tolerance
GTN spray / IV if ACS
stable angina, ACS and prinzmetal angina
antagonists of ETa receptor (for endothelin) eg.s
indicated for
bosentan, ambrisentan
pulmonary hypertension
renin inhibitors eg.
alsikiren
NOT WITH ACEI or ARB
ACEI eg.s
effects
side effects
lisinopril, ramipril
less vasoconstriction due to AT2 decrease
more vasodilation due to bradykinin increase
less blood vol due to aldosterone decrease
dry cough
CCB 3 eg.s
verapamil (mostly cardiac CaL channel selective)
amlodipine (mostly SM CaL channel selective)
diltiazem (intermediate selectivity)
effect and method of action of CCBs
block CaL channels => decreased rate and conduction through AVN and force of contraction
CCB preferred for hbp
amlodipine (less effects on heart)
causes arteriole and artery + coronary artery vasodilation
Side effects of CCBs
ankle swelling, hypotension, dizzy, flushing
DONT give verapamil with β-blockers.
DONT GIVE IN HF
K+ channel openers eg.s
mechanism of action
nicorandil - angina (also has NO activity)
minoxidil - last resort for severe hbp
open Katp channels in vascular SM by antagonising ATP that closes them => hyperpolarised + CaL inhibition => relaxation
α1 antagonists eg.
cause
indications for use
prazosin + doxazosin
vasodilation and decreased sympathetic transmission
for benign prostatic hyperplasia and if they also have hbp
Thiazide diuretic eg.
Inhibit ____ in ___
Indications
bendroflumethiazide
inhibit NaCl reabs by blocking NaCl co-transporter in distal tubule
mild HF, hbp, severe resistant oedema (along w. loop)
Loop diuretic eg.
Inhibit ___ in ___
indications
furosemide
NaCl reabs by NaKCl co-transporter blockage in thick ascending loop of Henle
acute pulmonary oedema (IV) chronic HF
Type I antiarrhythmics target-
Phase 0 - Na+ channels
Type I antiarr. classes
a-moderate ass/dis rate = longer refractory period disopyramide
b - rapid ass/dis = prevent prem beats lignocaine
c - slow dis/ass = depress conduction flecainide
Type 2 antiarrhythics
β-blockers - act on depol in SAN and AVN eg. metoprolol
Type 3 antiarrhythmics
K+ channel blockers -prolong AP and increase refractory period eg. amiodarone, sotalol
Type 4 antiarrhythmics
CCBs - slow SAN and AVN conduction and decrease force
eg. verapamil
Drugs that work on atria (rate control of SVT) =
Ic and III eg. flecainide and amiodarone
rate control antiarrhythmics =
β blockers and CCBs
rhythm control antiarrhythmics =
K+ and Na+ blockers
Drugs that work on AVN (rhythm control of SVT) =
adenosine, digoxin, II and IV ie. β-blockers and verapamil
Drugs that work on atria (rate control of SVT) =
Ic and III = flecainide, sotalol/amiodarone
Antiarrhythmics that work on the ventricles =
Ia+b + II
disopyramide, lignocaine, β-blockers
antiarrhythmics that work on atria and ventricles + AV accessory pathways
amiodarone, sotalol (III) and disopyramide (Ia) and flecainide (Ic)
Adenosine (IV) acts on ____ receptors in the ___
Used in ____
A-1 adenosine receptors in the AVN paroxysmal SVTs (atria=140-250bpm) caused by re-entry involving the SA/AVN/atrial tissue
Drug for termination of paroxysmal SVTs (atria=140-250bpm)
Adenosine IV
A-1 adenosine receptors are coupled to ___ > activates ____ > _____ AVN
Gi/o
GIRK
hyperpolarises AVN and so suppresses impulse transduction
Adenosine is used in acute/chronic SVT
acute - is quickly removed
Drug that stimulates vagal activity = slows conduction and increases refractory period in AVN and bundle of His
+ve ionotropic effect
digoxin (IV/PO)
Inhibits the NaKATPase
Treats acute/chronic AF
digoxin
Used for prophylaxis of AF and atrial flutter =
verapamil (PO)
adenosine/verapamil is better for acute AF/ atrial flutter
adenosine
don’t prescribe verapamil with ___
β-blockers (other -ve ionotropic drugs)
Used in ventricular arrythmias post-MI
Ib - lignocaine IV
Ia - procainamide IV
Used to prevent recurrent Ventricular arrhythmias
Ia - disopyramide PO
Prophylaxis for AF (a Na blocker)
Ic - Flecainide