Pharmacology Flashcards
HCN/funny current blocker and what disease it is used for?
Ivabradine
Used for angina
Name a beta 1 agonist used sometimes in heart failure?
Dobutamine
Propranolol is a …. and atenolol and bisoprolol are ….?
Non-selective beta antagonist and selective beta 1 antagonist
Give some adverse effects of beta blockers?
Worsen asthma
Worsen heart failure (at high doses)
Cold extremities
Which class of drug is atropine + main use?
Muscarinic antagonist + bradycardia
Digoxin mechanism?
Blocks the Na/K ATPase which increases intraceullar Na which blocks Na/Ca exchange
Increased Ca causes increased contraction
Digoxin is toxic when used in people with…. and can also induce ….?
Hypokalaemia and arrhythmias
What does Levosimendan (used in heart failure) do?
Binds to troponin C to increase its affinity for Ca
What do nitrates combine with to liberate NO + what molecule do they activate to produce cGMP?
SH groups + guanyl cyclase
Give an example of a short-acting and long-acting nitrate + 2 main side effects?
GTN and isosorbide mononitrate + headache and hypotension
ACEi name ending + 2 CIs + 2 side effects?
Pril + renal artery stenosis and pregnancy + cough and hyperkalaemia
ARB name ending + 2 CIs + side effect?
Artan + renal artery stenosis and pregnancy + hyperkalaemia
CCBs are selective for which type of calcium channel?
L-type channels
CCB (dihydropyridines) name ending + 2 key side effects?
Pine + periperipheral oedema and flushes
Name a K+ channel agonist + what disease is it used for?
Nicorandil + angina
Name an alpha 1 blocker + key side effect?
Doxazosin + postural hypotension
Give an example of a thiazide, loop and potassium sparing diuretic?
Bendrofluazide, furosemide, spironolactone
3 side effects of thiazide and loop diuretics?
Hypokalaemia, hyperglycaemia and gout (increased uric acid)
2 side effects of spironolactone?
Gynecomastia (breast swelling) and hyperkalaemia
Name 2 oral antiplatelets + their mechanism + key side effect?
Aspirin (blocks COX)
Clopidogrel (blocks P2Y12) + GI bleeds
Warfarin route + mechanism + side effect + CI?
Oral + inhibits vitamin K + haemorrhage + pregnancy
Heparin route + mechanism (+ exception) + CI?
IV/SC + increases AT III affinity for serine proteases IIa and Xa (LMWH only blocks Xa) + renal disease
Fibrinolytic route + mechanism + examples?
IV + activates plasmin which breaks down fibrin + strptokinase, duteplase and alteplase
What makes up the hydrophobic core of a lipoprotein?
Cholsterol esters
Triglycerides
Key molecule on the surface of lipoproteins?
Apoproteins
What apo does VLDL contain?
apoB100
What apo do chylomicrons contain?
apoB48
Place of formation + role of chylomicrons and VLDL?
Chylomicrons made in enterocytes and transport dietary triglycerides + VLDL made in the liver and transport liver triglycerides
Chylomicron to remnant summary?
MTP lipidates apoB48 to allow more triglycerides to enter
ApoA1 allows chylomicron to leave
ApoCII from HDL allows LPL to bind and break down triglycerides
How cholesterol esters + triglycerides are formed?
Esterification of cholsterol and monoglyceride + fatty acid
Lipoproteins travel by the lymphatics then venous system. True or False?
True
What are chylomicron and VLDL remnants?
Particles with no triglycerides but still containing cholesterol ester
ApoCII is returned to HDL in exchange for which apoprotein? How does this facilitate clearance of apoB lipoprotein + key enzyme in the liver?
ApoCII is returned to HDL in exchange for apoE
High affinity ligand for receptor-mediated clearance + heapatic lipase
What percent of apoB48 and apoB100 chylomicrons are removed by receptor mediated clearance?
100% of apoB48
Only 50% of apoB100
What happens to the remaining apoB100 remnants?
Become enriched in cholesterol esters and become LDL via IDL
Which receptor is vital for LDL clearance + where is it?
LDL receptor in liver
LDL clearance summary?
LDL undergoes hydrolysis and releases cholesterol
Normal 2 effects of HMG-CoA reductase?
Increase cholesterol synthesis and decrease LDL liver receptors
LDL role in athersclerosis?
Macrophages oxidise it to OXLDL to form foam cells
Athersclerosis summary?
Damaged endothelial express ICAM and VCAM
Macrophage and T lymphs migrate into cell wall
Macrophage oxidises LDL to OXLDL to form foam cell/plaque
Smooth muscle cells accumulate and cause hypertrophy
3 drugs to lower cholesterol?
Statins, fibrates and PCSK 9 inhibitors
How do statins work + 2 side effects + better taken at what time?
Inhibit HMG CoA reducatase + rhabdomylosis and myalgia + at night
Drug for hypertriglyceridaemia + mechanism?
Fibrates + lower VLDL production in the liver
Drug for familial hypercholesterolaemia + mechanism + example?
PCSK 9 inhibitor + blocks PCSK 9 from binding LDL receptors so more are available + alirocumab
What are the 3 components of Virchow’s triad?
Hypercoaguability, venous stasis and endothelial dysfunction
Colour + treatment for venous and arterial thrombus and which is more common?
Venous is red and treated with anticoagulants (more common)
Arterial is white and treated with antiplatelets
Soft clots are coated with … and hard clots are coated with …?
Fibrinogen and fibrin
Soft clot formation summary?
Damaged site exposes collagen Platelets bind and form TXA2 via COX TXA2 causes ADP serotonin/5-HT release 5-HT causes vasoconstiction ADP binds P2Y12 to activate more platelets TXA2 and GP receptors bind fibrinogen
Hard clot formation?
VII (tenase) converts X to Xa (prothrombinase)
Xa converts II (prothrombin) to X (thrombin)
Thrombin converts fibrinogen to firbrin
Name the 4 inactive precursors of the main clotting factors involved in coagulation that are blocked by warfarin?
II, VII, IX, X
Inactive precursors are … and have to undergo …. to form …?
Glycoproteins and gamma-carboxylation and serine proteases
What does the enzyme which carries out gamma-carboxylation of clotting factor precursors require?
Vitamin K (in its reduced, hydroquinone form)
What are the two forms of Vitamin K that exist?
K1 from diet
K2 from bacteria in intestine
Where are clotting factors released from?
The liver
How might a warfarin overdose be treated?
Vitamin K/clotting factor infusion
What does Antithrombin III (ATIII) do?
Inhibits serine proteases (IIa and Xa)
Give 2 examples of LMWHs?
Enoxaparin
Dalteparin
Dabigatran route + mechanism?
Oral + blocks thrombin
Rivaroxiban route + mechanism?
Oral + blocks Xa
Which enzyme aids platelet synthesis of TXA2?
COX
Tirofiban route + mechanism?
IV + blocks GPIIb/IIIa receptors
Class I anti arrhythmic examples + mechanism + phase they affect?
Lignocaine, lidocaine, quinidine, flecainide, propafenone + block Na channels + phase 0
Class 2 anti arrhythmic examples + mechanism + phase they affect?
Propanolol + beta blocker + phase 4
Class 3 anti arrhythmic examples + mechanism + phase they affect?
Amiodarone and sotalol + blocks K channels + phase 3
Class 4 anti arrhythmic examples + mechanism + phase they affect?
Verapamil and diltiazem + blocks Ca channel + phase 2
Adenosine mechanism?
Blocks AVN
Magnesium sulphate mechanism + used in?
Blocks Ca and Na channels + Torsades des Pointes
Ivabradine mechanism + used in?
Blocks the funny current (HCN channel) + angina
Atropine mechanism + used in?
Decreases vagal innervation on SAN + bradycardia
Thiazide vs loop diuretics vs spironolactone block what transporter + where?
Thiazide = Na/Cl in the distal tubule Loop = Na/K/Cl in the ascending Loop of Henle Spironolactone = Na ENaC channel in the nephron