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VetMed Pharmacology
VetMed Pharmacology - Absorption
| Question | Answer |
|---|---|
| External Tissue and Organ Barriers Limiting Absorption | cutaneous/dermal structures GI mucosal epithelium Pulmonary epithelium Mucosal membranes Corneal epithelium |
| Internal Tissue and Organ Barriers Limiting Absorption | SQ tissues Musculature Capillary basement membrane Vascular endothelium |
| Advantages of PO Route of Administration | Safest Large V and doses can be absorbed Convenient, Economical SA of SI allows adequate absorption of weak-acid or weak-base compounds |
| Disadvantages of PO Route of Administration | Variable rate of absorption Lower bioavailability Can be affected by diet GI irritation possible Caustic environment may inactivate some pharmaceuticals "First pass" removal by liver (Lidocaine) |
| Advantages of IV Route of Administration | Rapid onset 100% bioavailability |
| Disadvantages of IV Route of Administration | Least safe form of delivery |
| Advantages of IM Route of Administration | Timed release Safer than IV |
| Disadvantages of IM Route of Administration | Slow absorption with dehydration Abscess formation |
| Advantages of SQ Route of Administration | Low risk Timed release |
| Disadvantages of SQ Route of Administration | Slowed absorption with dehydration |
| Advantages of IP Route of Administration | Potentially can give large volume |
| Disadvantages of IP Route of Administration | Technically difficult Organ damage possible |
| Advantages of IO Route of Administration | Accessible route even with severe dehydration |
| Disadvantages of IO Route of Administration | Technically difficult Painful |
| Advantages of ID Route of Administration | Relatively safe |
| Disadvantages of ID Route of Administration | Relatively slow absorption rate Administration volume is limited |
| Nebulization | a technique for physically converting a liquid preparation into fine "mist" with droplets of small enough size to pass to the level of the alveolus |
| Biological Variables that Influence Pharmaceutical Absorption | surface area available biological mechanisms (passive vs. active transport) environmental pH differences vascular density biological barrier composition (muscle vs. skin) tissue binding |
| Pharmaceutical Variables that Influence Absorption | concentrations molecular size lipid solubility molecular shape ionic charge |
| Mechanisms of Pharmaceutical Biotransport | membrane pores active transport facilitated diffusion ionic or electrochemical diffusion pinocytosis/phagocytosis passive diffusion |
| Active Transport | energy-dependent transferred from low to high concentration can become saturated |
| Membrane Pores | movement between cells dependent on hydrostatic pressure |
| Facilitated Diffusion | carrier-dependent no energy needed transferred from high to low concentration can be saturated can be inhibited by metabolic poisoning agents (glucose entry) |
| Ionic or Electrochemical Diffusion | dependent on electrochemical gradient across membrane driven by difference in ionic charge depolarization costs energy to maintain high to low gradient |
| Pinocytosis and Phagocytosis | active process requiring energy engulfing of a volume of fluid or of particulate matter minor transport processes |
| Simple Passive Diffusion | no energy required transferred from high to low concentration most common and most important in-vivo transport process cannot be saturated rate and transport dependent on concentration of pharmaceutical |
| The rate at which a compound traverses the distance from point A to point B... | ...is a function of the square of that distance. |
| Anatomical Variables of Absorption into IV Compartment | degree of capillary density tissue mass portion of the total cardiac output received |
| Calculating Bioavailability | AUC (IM) / AUC (IV) X 100 |
| Fick's First Law of Diffusion | a substance will diffuse through an area at a rate that is dependent upon the differences in concentration for a given substances between two given points |
| Anatomical Structures with Membranes of Greater Thickness | blood brain barrier blood-CSF barrier blood-milk (mammary) barrier placental barrier |
| Relationship of Diffusion and Molecular Size | rate of diffusion is inversely proportional to square root of molecular weight, and for large compounds is inversely proportional to third square root of molecular weight |
| How to Increase Aqueous Solubility | addition or formulation with salts (Na+, K+) incorporate a charged "solvent" decrease overall size (mass) change the crystalline shape |
| Oil:Water Coefficient | a measure or indicator for estimating how well a pharmaceutical will diffuse across an intact phospholipid bilayer of cell membranes |
| How to Increase Lipid Solubility | increase pharmaceutical alkylation increase level of phenyl group addition or substitution replacement of oxygen groups with sulfur groups increase halogen group substitutions or additions decrease or minimize +/- of ionized charged groups |
| Variables Influencing Diffusion of Pharm Preparations in the form of a Suspension | depot surface area depot drug concentration particle surface area dissolution rate injection volume viscosity |
| Donnan Effect | charged molecules on one sie of a semi-permeable membrane will alter concentrations of "permeable" ionized particles |
| Ways to Manipulate Pharmaceutical Absorption | manipulation of size, shape, and ionic charge encapsulation use of suspending agents use of vasoconstrictive agents dispersion or "spreading" agents |
| Pharmocokinetic Definition of Absorption | transport or diffusion of a pharmaceutical or toxin from the anatomical site of administration into the central (intravascular) compartment |
| Definition of Bioavailability | percent of the original dose administered that enters the central (intravascular) compartment |
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