chapter 2 flashcards 115

Cellular Physiology

  • Cells are dynamic factories; they take in raw materials, manufacture and deliver products, and differ by tissue.

  • Common cellular characteristics: exchange materials with environment, obtain energy from nutrients, synthesize complex molecules, reproduce, communicate via biologic chemicals.

Cell Membrane

  • Essential for drugs to affect cellular function.

  • Lipid-soluble drugs dissolve in the lipid layer and diffuse.

  • Gated channels regulate ion movement.

  • Carrier proteins move drug molecules across.

Pharmacokinetics

  • Absorption: Process from drug entry into body to bloodstream entry.

    • Onsets drug action.

    • Affected by: dosage form, route, administration site blood flow, GI function, food, other drugs.

  • Distribution: Transport of drug molecules by blood and tissue fluids to action, metabolism, and excretion sites.

    • Dependent on blood circulation adequacy.

    • Affected by: protein binding, blood–brain barrier, pregnancy, lactation.

  • Metabolism (Biotransformation): Inactivation or chemical alteration of drugs.

    • Drugs change to inactive/active metabolites or prodrugs.

    • Enzymes are in kidneys, liver, RBCs, plasma, lungs, GI mucosa.

    • Affected by enzyme induction and inhibition.

  • Excretion: Elimination of medication from the body.

    • Requires adequate function of circulatory system, kidneys, bowel, lungs, skin.

Serum Drug Level

  • Laboratory measurement of drug amount in blood at a specific time.

  • Reflects dosage, absorption, bioavailability, half-life, metabolism, excretion rates.

  • Minimum Effective Concentration (MEC): Must be present for efficacy.

  • Toxic Concentration: Excessive drug level causing adverse effects, due to large single dose, repeated doses, or slow metabolism.

Receptor Theory of Drug Action

  • Drugs bind chemically with receptor cells, leading to:

    • Activation, inactivation, or alteration of intracellular enzymes.

    • Changes in cell membrane permeability.

    • Modification of neurohormone synthesis, release, or inactivation.

    • Involves agonists and antagonist drugs.

Nonreceptor Drug Actions

  • Few drugs act without receptor sites; examples include antacids, osmotic diuretics, some anticancer drugs, metal chelating agents.

Drug-Related Variables

  • Factors: Dosage (frequency, size, number), route of administration, drug–diet and drug–drug interactions.

  • Increased Effects: Additive effects, synergism, interference, displacement.

  • Decreased Effects: Antidote medication, decreased intestinal absorption, increased metabolism rate.

Patient-Related Variables

  • Age, body weight, pharmacogenomics, genetics, ethnicity, gender, pharmacogenetics, preexisting conditions, psychological considerations, tolerance, cross-tolerance.

Adverse Effects of Drugs

  • Any undesired responses to medication administration.

  • Can occur with usual therapeutic dosing, more likely with high dosing, specific drugs, and in older adults on multiple drugs.

Toxicology: Drug Overdose

  • Results from excessive medication, potentially damaging tissues.

  • Causes: single large dose, prolonged ingestion of smaller doses, involving various drug types.

  • Treatment Goals: Prompt treatment, supporting/stabilizing vital functions, preventing further damage (reducing absorption, increasing elimination, administering antidotes).