Drug MoA Flashcards
Clopidogrel
P2Y12 inhibitor - prevents ADP binding and activating GPIIb and IIIa complex
Aspirin
COX-1 inhibitor - inhibits TXA2 preventing thrombosis
Apixaban, rivaroxaban
Direct Xa inhibitor. Prevents prothrombin conversion to thrombin. Thrombin catalyses fibrinogen to fibrin clot
Dabigatran
Direct thrombin inhibitor. Thrombin catalyses fibrinogen to fibrin clot
Fondaparinux, LMWH
Indirect Xa inhibitor
Abciximab
GPIIb/IIIa inhibitor. Prevents platelet aggregation - binding of fibrinogen, vWf
Trimethoprim
Dihydrofolate reductase inhibitor (prevents production of tetrahydrofolic acid). Essential in thymidine pathway inhibiting DNA synthesis
Methotrexate
Competitively inhibits dihydrofolate reductase - DNA, RNA synthesis inhibited
Sulfasalazine
Unclear - immunosuppressive, antibacterial, anti-inflammatory. Appears to inhibit the cystine-glutamate antiporter
Lithium
Decrease NE release
Inhibit dopamine and /NMDA (glutamate)
Increase serotonin synthesis
Increase GABA (inhibitory neurotransmitter)
Trazodone
blockade 5-HT2A receptor. Increasing dose antagonises H1 and Alpha-1-receptors
Olanzapine
Combination of dopamine and 5-HT2 antagonism
Donepezil, galantamine, rivastigmine
Cholinesterase Inhibitors - enhance cholinergic transmission
Memantine
NMDA antagonist (reduce glutamate reducing destruction of brain cells)
Cetirizine
metabolite of hydroxyzine
H1 inhibitor
Cinacalcet
reduce PTH decreasing serum calcium
Cinnarizine
inhibits contraction of vascular smooth muscle through blockade of L-type and T-type Ca channels.
D2, H1 and mACH receptors
Ropinirole
non-ergot-derived dopamine receptor antagonist
parkinsons
allopurinol
purine analogue. Xanthine oxidase inhibitor.
Reducing uric acid formation in gout
(also possibly purine synthesis)
colchicine
binds to tubulins preventing microtubule formation.
Anti-mitotic.
In gout, binds to neutrophils preventing migration to uric acid crystals
Sodium Valproate, lamotrigine, carrbamazepine
blocking voltage-dependent sodium-channel conductance. It has been found to inhibit depolarization of the glutaminergic presynaptic membrane, thus inhibiting release of glutamate
ethosuximide
Bock LVA Ca channels
phenobarbital
GABA increases flow of chloride ions into neuron decreasing excitability of post-synaptic neuron
BZD
enhance GABA action
mechanism of epileptic seizures
Excitatory effect inward Na and Ca currents
Inhibition effect inward Cl outward K and GABA
Flecanide and class
Class IC
Blocks sodium channel, slowing the upstroke of the cardiac action potential.
The greatest effect is on the His-Purkinje system and ventricular myocardium.
Amiodarone and class
class III Blocks potassium channel Prolongs phase 3 of the cardiac action potential, the repolarization phase where there is normally decreased calcium permeability and increased potassium permeability.
lidocaine
class IB Slowing activation of action potential through Na channel
Disopyramide
Increase sodium permeability of cardiac myocyte
Where are pacemaker cells found
Sino-atrial node within wall of right atrium.
SA nodal pacemaker activity normally governs the rhythm of the atria and ventricles
B-Blockers
1, cardiac B1 blockade - decrease HR, CF and CO
- Suppress reflex tachycardia caused by vasodilators
- B1 JGA blockade - decrease renin release - decrease RAAS mediated vasoconstriction
- long term - decreased peripheral vascular resistance
ACE
- Block ACE preventing Angiotensin II which reduces afterload on heart
- Reduces intra-glomerular pressure
- Reduces aldosterone promoting Na and H20 excretion. Reduce preload - beneficial in HF.
ARB
Block AT1 receptor (Ang II)
- Inhibit ANS and kidney
- Reduces CO and TPvR
- Kidney TPvR and fluid volume
Methylphenidate
Binds the DA transporter preventing the reuptake of DA
Theophylline
Methylxanthine - PDE4 inhibitor
Adenosine blocker
histone deacetylase inhibitor
LAMA SAMA
block muscarinic effects of acetylcholine action