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Mod. 1-Physiochem

Module 1 Physiochemical properties of Drugs

Van der waals shifting electron density in areas of a molecule, or in a molecule as a whole, results in the generation of transient positive or negative charges.
Hydrogen atoms bound to nitrogen or oxygen become more positively polarized, allowing them to bond to more negatively polarized atoms such as oxygen, nitrogen, or sulfur – bond strength ++
Ionic atoms with an excess of electrons are attracted to atoms with a deficiency of electrons(imparting an overall positive charge on the
Covalent two bonding atoms share electrons – bond strength is the strongest
ED50 the dose at which 50% of patients will experience a therapeutic effect
TD50 the dose at which 50% of the patients will experience toxicity
LD50 the dose at which 50% of patients will die
Therapeutic Window the window between the therapeutic effect and the toxic effect at which the toxic effect is acceptable Efficacy without unacceptable toxicity – differs from drug to drug
Antagonists Inhibition of agonist activity. prevent agonist from binding to receptor and prevent DR*
Pharmacokinetics what the body does to the drug; how does the body move through the drug
Hydrophilic - “Water-loving”/water-soluble - Polar, usually ionized - Renal excretion -Requires transport mechanism to cross cell membranes & BBB -Forms H+ bonds
Hydrophobic -Lipophilic -“Fat-loving”/water insoluble -Passively diffuses across cell membranes and BBB -Non-polar, usually not ionized
Full Agonists -Causes maximal change in cellular activity of target -Stabilizes DR
Partial Agonists -Activates receptor without maximal efficacy -Stabilizes DR and DR*
Inverse Agonists -Inactivates free active receptors -Stabilizes DR in the case of R*
Competitive Antagonists -Reversible binding blocks agonist at active site -Stabilizes DR, prevents DR*
Noncompetitive Antagonists -Irreversible binding blocks agonist at active or allosteric site
Agonist ACTIVATES a receptor
Antagonist BLOCKS and INHIBITS function of agonist (prevents agonist activity)
Weak acids are best absorbed in the? stomach
Weak bases are best absorbed in the? small intestine
Volume of distribution (Vd) Volume of fluid required to contain the total amount of drug absorbed in the body at uniform concentrations equal to that in the plasma steady state
Potency takes lower dosage to produce same response of another
Type I hypersensitivity Can cause anaphylaxis
Type II hypersensitivity more cytotoxic; Mediated by IgG or IgM antibodies;• Can occur within minutes, can occur within hours; Can result in lysis or necrosis; Can result in reactions that are not always thought to be allergic reactions typically but can cause thrombocytopenia
Type III hypersensitivity Mediated by IgG or IgM; Can occur 3-8 hours of administration; Results in erythema, edema and necrosis; Antibody mediated
Type IV hypersensitivity Delayed reaction; Not mediated by antibodies but T cells; Cell mediated versus humoral; Response time delayed – 48-72 hours after offending agent; Results in erythema and induration
Created by: Hanika



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