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Pharm Exam 1
| Term | Definition |
|---|---|
| Pharmacodynamics | What the drug does to the body |
| DR | Drug + Receptor; usually drug bound to a protein |
| ED50 | dose where 50% of the people would experience a therapeutic effect. Expected dose |
| TD50 | dose where 50% of people would experience toxicity. Toxic dose |
| LD50 | dose where 50% of patients would die. Lethal dose |
| Therapeutic Window (TI) | Efficacy without unacceptable toxicity. The window between the therapeutic effect and the toxic effect. |
| How to calculate TI | TD50/ED50 50% ppl with toxic/50% of ppl with therapeutic |
| High TI | wide therapeutic window (desirable because a higher dose is needed to reach toxicity and a lower dose is needed to reach efficacy) |
| Low TI | small therapeutic window (warfarin, lithium) |
| Agonists; DR* | drug is bound and is eliciting a change; conformational change is depicted by the asterisk |
| 3 types of Agonists | Full, partial or mixed agonist-antagonist, Inverse |
| Full Agonist | Elicits maximal response; stabilizes DR*, causing a full effect by activating an inactive receptor |
| Partial or mixed agonist-antagonist | stabilizes DR (antagonist, no change) and DR* (agonist, change) |
| Inverse | inactivates free active receptors (R*), stabilizes DR in the case of R* |
| Antagonists | inhibition of agonist activity. Stabilizes DR and prevents DR* |
| 3 types of antagonists | competitive, noncompetitive, nonreceptor |
| Competitive antagonists | reversible binding, active site. An agonist can bump off antagonist at the active site and cause DR* |
| Noncompetitive antagonists | irreversible active site or allosteric site; high affinity bond, no matter how many agonists it cannot bump off the agonists; Also it will bind to an alternate site and prevent the agonist from binding or prevent the agonist from causing change |
| Nonreceptor: 2 types | Chemical: agonist inactivation (protamine binds to heparin and inactivatess it) Physiologic: mediates opposite response of agonist (how a beta blocker acts in hyperthyroidism; the patient is tachycardic so you give a beta blocker that will counter it |
| Pharmacokinetics | What the body does to the drug |
| 4 topics of pharmacokinetics | absorption, distribution, metabolism, and excretion. |
| Is the lipid core hydrophilic or hydrophobic? | hydrophobic |
| Are the surfaces of the extracellular and intracellular membranes hydrophobic or hydrophilic? | hydrophilic |
| How do drugs pass through the membrane? | Passive diffusion (small and hydrophobic) Facilitated diffusion (hydrophilic; needs a transporter and does not use ATP) Active Transport (hydrophilic; needs a transporter and uses ATP. Endocytosis: drug is engulfed and released in the cell. |
| Nonionized molecules | lipid soluble |
| Ionized molecules | hydrophilic, charged, and has difficulty penetrating the membrane |
| pKa which equation is used to calculate it? | pH at which 50% of the drug is ionized Henderson-Hasselbach equation pH + log ([HA]/[A-]) |
| pH trapping | determined by pKa and pH across membrane weakly acidic drugs (ASA); they are protonated in the stomach (nonionized) and deprotonated in plasma (ionized) |
| BBB has tight junctions that prevent passive diffusion. So how do drugs penetrate the CNS? | They are small and hydrophobic Active transport Facilitated transport Intrathecal (bypass) this is the easiest |
| Absorption depends on..... | the rate at which and extent to which the drug leaves its site of administration |
| Bioavailability | extent to which the drug reaches systemic circulation; "fraction absorbed" |
| What is the assumption about bioavailability | the site of action is reached directly from the systemic circulation |
| Factors that modify absorption | concentration, circulation at the site of absorption, drug solubility, and surface area |
| 2 phases of distribution | Initial phase: once the drug reaches systemic circulation 2nd phase: once the drug reaches the tissues (distribution to tissues) |
| Volume of distribution Vd = Dose/ [Drug]plasma | 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. |
| Low Vd | retained in the vascular compartment so it does not distribute well |
| High Vd | highly distributed into non-vascular compartments; so it can pass through plasma to target organs. |
| what type of bond: shifting electron density in areas of a molecule, or in a molecule as a whole, results in the generation of transient (+) or (-) charges. These areas interact with transient areas of opposite charge on another molecule. | Van der Waals; weakest |
| What type of bond: two bonding atoms share electrons | covalent; strongest/irreversible |
| what type of bond: 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 | hydrogen |
| What type of bond: Atoms with an excess of electrons (imparting an overall negative charge on the atom) are attracted to atoms with a deficiency of electrons (imparting overall positive charge on the atom) | ionic |
| Hydrophilic or Hydrophobic: "water-loving"/water-soluble | hydrophilic |
| Hydrophilic or Hydrophobic: Polar, usually ionized (contains a charge) | hydrophilic |
| Hydrophilic or Hydrophobic: lipophilic | hydrophobic |
| Hydrophilic or Hydrophobic: "fat loving"/water soluble | hdrophobic |
| Hydrophilic or Hydrophobic: Renal excretion | hydrophilic |
| Hydrophilic or Hydrophobic: Requires transport to cross cell membrane and BBB | hydrophilic |
| Hydrophilic or Hydrophobic: Passively diffuses across the cell membranes and BBB | hydrophobic |
| Hydrophilic or Hydrophobic: Forms H+ bonds | hydrophilic |
| Hydrophilic or Hydrophobic: non-polar, usually not ionized (no charge) | hydrophobic |
Created by:
nab81
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