Intracellular Enzymes Note

Tyrosine sine attaches to intracellular enzymes makes intracellular changes Insulin cell membrane receptors = stimulate transmembrane enzyme) that follow zero order Kinetics. Drugs thed JAspirin (ASA) Phenytoin (Dilantin) Ethanol (Alcohol) Tyrosine Kinase Activates Cellular Glucose Channel ( ↓ Glucose can now enter cell uptake Prodrugs: Drug is inactive until metabolized into active form Prodrugs: Drug (by liver) Vd=Drug drug plasma concentration dose measured Extensively Bound drugs (>90%) Warfarin NSAID Naproxen Furosemide (treats escra) Digitoxin Ibuprofen Side Effects? Drugs binding to receptors that they were not intended for! Agonist twillingly binds does no Produces very good effects ✓ What do they mimic Endogenous Substances naturally occured Substances in the the body Ex. Morphine Mimics Endorphins in CNS like... Serotonin, Dopamine Antagonizes Endogenous substances Partial Agonist HATFWAY Drug that turns a receptor on but only By itself... Will activate the receptor a little With a full Agonist... Will block the full Agonist even when all receptors are occupied. Overall... Produces weaker effect Ex. Buprenorphine Inverse Agonist Ex. Caffeine Binds to a receptor and decreases its activity below normal baseline High Affinty to Alpha & Beta receptors of sympathetic NS Primary Receptory Adenosine receptors of CNS 5 Major Receptor sites. G-protein Receptor (GPCR) Ion Channels "Nuclear Receptors • Non-enzymeT Transmembrane Enzyme Binding (JAK-STAT receptors Drugs that go through extensive "First Pass" Metabolism Morphine Meperidine (Demerol) Diazepam (Valium) Midazolam Lidocaine Nitroglycerine? THC? Narrow TI meds: TI TD50: ED5 Digoxin (Lanoxin) Warfarin (Coumadin) Phenytoin (Dilantin) Tacrolimus (Progref, Astagret)