Drugs are Poisons Flashcards
(18 cards)
Atropine effect
Blocks muscarinic receptors in the brain
Physostigmine
ACh esterase inhibitor
Digitalis mode of action: 1) 2) 3) 4)
1) Inhibits Na+/K+ ATPase
2) Increases intracellular Na+
3) Decreases Ca2+ extrusion
4) Increases heart contractile force
Digitalis drug type
Cardiac glycoside
Digitalis overdose effects
Causes cardiac arrhythmias
Exacerbated by low K+
Digitalis overdose treatment
K+
Paracetamol effect
Analgesic
Paracetamol mode of action
Metabolite in brain might activate CB1 cannabinoid receptor
Paracetamol off-target effects
Depletes glutathione in liver
This leads to oxidative damage of liver cells, necrosis
Size of therapeutic window for paracetamol
Large.
Good/bad mechanisms different
Size of therapeutic window for digitalis
Small
Good/bad mechanisms are the same
Terfenadine
Precursor to fexofenadine
Enzyme that converts terfenadine to fexofenadine
CYP3A4
Source of dihydrobergamottin
Grapefruit
Compound in grapefruit that inhibits CYP3A4 action
Dihydrobergamottin
Effects of dihydrobergamottin on ingested terfenadine:
1)
2)
1) Terfenadine is not converted into fexofenadine in the liver by CYP3A4
2) Terfenadine becomes bioavailable, causes irregular heartbeat
Dihydrobergamottin
Irreversible inhibitor of CYP3A4 in liver
CYP3A4
Liver enzyme, converts terfenadine to fexofenadine (among other things)