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Mod. 1-Physiochem
Module 1 Physiochemical properties of Drugs
| Question | Answer |
|---|---|
| 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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