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NURS 216A
September 12
| Question | Answer |
|---|---|
| What affects molecular kinetics? | 1. Molecular characteristics 2. Membrane transport |
| How do we avoid a toxic range or a toxic dose? | - ED50: median therapeutic dose - TD50: median toxicity dose The ratio between TD50 : ED50 = TI (therapeutic index) |
| What are the three categories of pharmacotherapeutics? | 1. Drug or medication: chemical agent 2. Biologics: naturally produced in animal cells 3. Natural health product: naturally occurring (vitamins, minerals, dietary supplements) |
| What are the four factors affecting administration route of medication? | 1. Drug to target tissues 2. Clinical setting 3. Medical situation 4. Drug dynamics |
| What is the intranasal route of administration? | - Into the nasal cavity, capillary absorption - Localized or systemic effect (preparation dependent) - Direct CNS effect (diffusion across mucosa and distribution along CNS nerve network) |
| What is the rectal route of administration? | - Inserted into the lower GI, rectum - Local and systemic effect (portal circulation sweeps 25% into the body, 75% stays localized) - Low first pass metabolism |
| What is the parenteral route of administration? | 1. Intravenous (IC) 2. Intramuscular (IM) 3. Subcutaneous (SC) |
| What is the IC route of administration? | Needle catheter into a vein - IMMEDIATE absorption - fastest onset of action - Dose given = dose circulating to receptors - Systemic effect |
| What is the IM route of administration? | - Needle injection into muscle - Aqueous (faster effect) or depot preparation (slower effect) - Capillary bed absorption into the bloodstream - Systemic effect, epinephrine for allergic reactions |
| What is the SC route of administration? | - Injection into adipose tissue of hypodermis, absorption via capillary bed - Systemic effect (slow or fast dependent on preparation) |
| Define pharmacokinetics | Pharma = medicines Kinetics = motion - Movement across cell membranes via lipid bilayer - 4 phases: ADME |
| What are the features of membrane transport? | 1. Passive - diffusion, osmosis, facilitated diffusion 2. Active |
| Easily absorbed and distributed molecules are: | 1. Lipophilic 2. Non ionized 3. Small |
| Easily excreted molecules are: | 1. Hydrophilic 2. Ionized |
| What is absorption? | The time it takes for the drug to reach systemic circulation |
| What is bioavailability? | - Systemic circulation's drug concentration - Measurable in blood test - Known for most standard doses - Can adjust dose to achieve desired patient effect: titrating to effect |
| What is therapeutic range? | Concentration of drug in the blood serum that produces the desired effect without causing toxicity |
| What is a loading dose? | Initial higher dose of a drug that may be given at the beginning of treatment to RAPIDLY achieve a therapeutic level |
| What is a recommended dose? | - A dose that elicits a therapeutic effect - ED50: median therapeutic dose, elicits a therapeutic response in 50% of patients |
| What is distribution? | - Transport through the body to target tissues - Can be calculated for relative comparison of distribution to tissues = Vd |
| What is plasma protein binding? | - Cohesion with plasma protein molecules - Drugs have varying "affinity" for plasma carrier proteins - Binding DECREASES distribution rates - Competitive, reversible, saturable |
| What is the rule of unbound vs bound drugs? | Unbound drugs = effective Bound drugs = NOT effective |
| What is metabolism? | - Chemical conversion to prepare the drug for excretion - Termination of drug action |
| What is biotransformation? | - Metabolism by the liver - Active drug to inactive metabolite - Inactive drug to active metabolite (prodrug) - PO drugs: portion is first pass metabolized - the bioactive drug metabolized as above - Hydrophilic drugs are excreted |
| What is excretion? | - Elimination of a drug - Inactive substances and metabolites are eliminated - Kidneys are the primary organ of excretion |
| What are the factors affecting renal excretion? | 1. Molecular characteristics - ionization, hydrophilicity, size 2. Cardiac output (renal blood flow) 3. Renal function - Elderly, neonates, young infants - Integrity of glomerulus (renal disease) 4. Overdose |
| What are first order elimination kinetics? | - The more you take, the faster the body will work to eliminate it (homeostasis) - Elimination proportionate to the drug serum concentration - Drug plasma concentration in mg/dL or L - Clearance (Cl) = elimination/peak plasma concentration |
| What are zero order elimination kinetics? | - Rate of elimination or "clearance" is constant - Difficult drugs to clear |
| What are the nine routes of administration? | 1. Oral (PO) 2. Sublingual (SL) 3. Intranasal 4. Inhalation 5. Endotracheal 6. Topical 7. Transdermal 8. Rectal 9. Parenteral |
| What is the oral route of administration? | - Called enteral (passes through lower GI tract) - Most common and most challenging d/t kinetics (acidic enviornment, peristalsis dependent) - Goes through first pass metabolism - Systemic effect - Causes issues if patient vomits |
| What is the sublingual route of administration? | - Under the tongue, capillary absorption into the blood stream - Bypasses GI system and first pass metabolism, faster acting than PO - Systemic effect |
| What is the inhalation route of administration? | - Breathed into lungs, pulmonary capillary network - rapid effects - Localized or systemic effect (preparation dependent) - Local: asthma drugs - Systemic: general anesthesia |
| What is the endotracheal route of administration? | - Used in ER or ICU situation - Epinephrine |
| What is the topical route of administration? | - Applied directly to a surface - Local effect, minimal systemic presence (systemic presence % can be contraindicated) - Daltons (molecular weight); many molecules are too large to penetrate all skin layers |
| What is the transdermal route of administration? | - Patch, dermal capillary absorption (molecules must be small enough to penetrate skin layers) - Systemic effect desired - Long acting - slow, sustained release and absorption |
| What are the features of molecular characteristics? | 1. Charge (ionization) - Neutral molecules converted to electrically charged ones = ionized 2. Neutral (90% of the time so it can be easily absorbed and travel through the body, favours non-charged molecules) 3. Lipophilicity vs hydrophilicity 4. Size |
| What are the factors affecting absorption? | 1. Administration route 2. Molecular characteristics |
| What does a small number mean of a TI? | Small number = higher risk TI = 10; means we have to give the drug 10 times before it is toxic |
| What are the factors affecting distribution? | 1. Blood flow to the tissue (BBB) 2. Size of the tissue 3. Molecular characteristics (size, charge) 4. Plasma Protein Binding |
| What are the two phases of metabolism? | 1. Phase 1 - Hydrolysis, reduction, and oxidation - Removal of hydrogen proton and addition of oxygen) - Cytochrome P450 enzyme group 2. Phase 2 - Only some drugs require this phase - Conjugation and polarization - 5 main enzymes used |
| What is the main CYP450 enzyme group? | - Saturable - Dynamic - Drugs can increase (more active, metabolize faster) or inhibit (less active, metabolize slower) certain enzyme functions |
| What is Rhinocort spray? | A corticosteroid based localized drug that is sprayed into the nasal cavity (intranasal route) and absorbed by capillaries |
| How do antacids work? | Increase the stomach pH, useful if there is an aspirin overdose |
| How does aspirin work? | NSAID, Taken PO, travels to the stomach and is absorbed in the stomach (pH=2) instead of the more alkaline environment of the small intestine. Travels through the stomach mucosa into portal circulation, zero order kinetics |
| What is dilantin? | Anticonvulsant drug, prevents the spread of seizure activity in the brain, zero order kinetics |
| How does ibuprofen work? | NSAID, reduce inflammation, analgesic, and antipyretic |
| How does acetaminophen work? | Analgesic and antipyretic, reduce fever and pain (NOT inflammation) |
Created by:
aschelle
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