Cardiac and renal phamacology Flashcards
Tetracaine
Anaesthetic blocking NaV
More anaesthetic at higher pH as more drug in unprotonated form
Lidocaine
Anaesthetic blocking NaV
Use dependent
Benzocaine
Anaesthetic not affect by pH as neutral
Tetrodotoxin
Mainly acts on nerve NaV
L type channels
Node and heart tissue
Sensitive to dihydropyridines
Slowly inactivating
Needs large depolarisation
T type channels
Mainly found in node
Insensitive to dihydropyridines
Phenylalkylamines (Verapamil)
Blocks L type Ca channels from inside
Dihydropyridines (Amlodipine)
Blocks L type channels from inside
Benzothiapines
Block Ca channels from outside and alter dihydropyridine binding
Sulfonurea drugs (Glibenclamide)
Mimics ATP to close kATP channel, depolarise and cause insulin release
Long QT1 and 2
Kv mutations
Long QT3
Nav mutations
Isoprenaline
Beta agonst
Raises cAMP to act on HCN
Used for bradycardia
ACh on nodes
Acts via M2
Causes decreased cAMP so less HCN
betagamma coupled to GIRK1 to hyperpolarise
Adr on heart
Via beta1
Increases cAMP so stimulates HCN
+ PKA opens Ca2+ channels
Quinidine
Blocks NaV
Class 1a antidysrhythmic
Use dependent (higher affinity for activated channels)
Lidocaine
Blocks NaV
Class 1b antidysrhythmic
Use dependent
Propenalol and Atenolol
Beta1 selective blockers (anti-dysrhythmic)
Class II
Amiodarone
Class 3 antidysrhythmic
Prolongs AP
Blocks Ina or Ik depending
Verapamil
Cardioselective Ca2+ channel blocker
Class IV antidysrhthmic
Digoxin
Binds K+ site of Na/K+ ATPase to raise Na intracellularly by 1.5mmol/l
So less Na+ gradient for Ca2+ removal
For heart failure
Dobutamine
Beta 1 agonists for circulatory shock or during heart surgery
Bisoprolol/Carvedillol
Beta blockers to stop damaging effect of chronic stimulation in heart failure
Pimobendam
Ca2+ sensitiser
Can cause long QT syndrome
Milrinone
PDE3 inhibitors for heart failure
Can cause dysrhythmias
Methyxanthanes
Non specific PDE inhibitor and A1/2 antagonist
Streptokinase
Binds plasminogen activator to activate
Alteplase
Tissue plasminogen activator that acts preferentially in clots
Clobidogrel
Inhibits platelet aggregation via inhibiting ADP binding
Eptifibatide/Abciximab/Tirofiban
Inhibitor of IIb/IIIa complex to stop cross linking
Heparin
Activates antithrombin III which inactive thrombin and X
Warfarin
Inhibits vit K epoxide reductase so can’t make clotting factors
Dabigatran
Inhibits thrombin
Loop diuretic; Furosemide
Blocks Na+/K+/2Cl- on TAL
Rapid venodilation
Gout, hypokalaemia
Thiazide diuretics; Hydrochlorothazide, Bendroflumethiaziole
Blocks Na+/Cl- on TAL/distal tubule
hypokalaemia, gout
Amiloride
Blocks epithelial Na+ channels on apical side
K+ sparing diuretic
Spironolactone
Aldosterone antagonist to increase expression of Na+ channels
Acetazolamine
Carbonic anhydrase inhibitor Blocks H+ provision for Na+ reabsoption For glaucoma Less effective Alkaline urine
Enalapril, Ramipril
ACE inhibitor
For heart failure and hypertension
Losartan
AT1 blocker
Salarsan
AT1 partial agonist