Pharmacokinetics Lecture 2 Flashcards
Pharmacokinetics phase
The study of the movement of drugs into, within and out of the body that is necessary to achieve drug action
Phases
Absorption
Distribution
Metabolism
Excretion
Absorption
Movement of drugs into the bloodstream after administration
Pharmaceutic phase
When a drug is in solid form and disintegrates into smaller particles and combine with liquid form a solution
Excipients
Fillers and inert substances
What environments so drugs disintegrate and absorb faster in?
Acidic fluids with a pH of 1 or 2 rather than alkaline fluids
Small intestines form
Covered with villi which increase the surface area available for absorption
Enteric coated drugs disintegrate where?
Resist disintegration in gastric acid of the stomach
Only occurs until drug reaches alkaline environment in small intestine
Passive absorption
Diffusion
Active absorption
Requires carrier (enzyme) and energy is required
Pinocytosis
Cells carry drag across membrane by engulfing particles
What is the GI membrane composed of
Mostly lipid (fat) and protein (Drugs that are lipid soluble pass rapidly through)
What needs a carrier to pass through the membrane?
Water soluble drugs need an enzyme or protein and can’t cross blood brain barrier
How do large particles pass through cell membrane?
Nonionized
What drugs absorb the fastest
Drugs that are lipid soluble and nonionized
Where do drugs absorb faster?
Drugs given IM= more more blood vessels
Where do drugs absorb slower
Subcutaneous tissue because there is fewer blood vessels
First pass effect
Some drugs don’t got to systemic circulation but pay to the intestinal lumen to the liver
What happens in the liver?
Some drugs me metabolize in inactive form than excreted (reducing amount Of active drug)
Bioavailability
% of drug available for use
PO<100%
IV=100%
Desired drug effect= oral does is 3-5x larger than dose for IV
Factors effecting bioavailability
Drug form Route GI mucosa and motility Presence of food and other drugs Changes in liver metabolism or function
Effect rapid absorption on bioavailability
Increased bioavailability and can increase drug concentration which Amy lead to drug toxicity
Effect of Slow absorption on bioavailability
Limit the bioavailability of drug causing decrease drug concentration
Distribution
Process by which drug becomes available to the body fluids and tissues
What effects distribution
Protein binding
Blood flow
Blood tissue affinity
Inactive drug vs active drug
Inactive= bound to drug not available to interact with tissue receptor
Active: unbound free and can cause pharmacological response
What happens if 2 highly protein bound drugs are given concurrently
Compete for protein binding sites cause more free drugs to be released
What crosses the blood brain barrier
Highly lipid soluble and low molecular weight drugs and not water soluble drugs
Metabolism
Or bio transformation
Process by which body chemicals changes grubs into form that can be excreted
Where does metabolism occur
GI tract but mostly in liver (most drugs inactive due by enzymes$
Half life
Time it takes for one half of the drug concentration to be eliminated
Steady state
Amount of drug administered=drug eliminated
Necessary for optimal therapeutic benefit
Loading dose
Large initial dose to achieve rapid MEC
Excretion
Main route is kidneys
What can’t be filtered through kidneys
Protein bound drugs
Creatinine clearance
Between 86-135 mal/min
Metabolic Byproduct of kidneys and compares amount of creatine in blood and urine
Blood Urea Nitrogen (BUN)
Metabolic breakdown products between 7-20
Pharmacodynamic phase
Study of drug effect and mechanisms of action
Primary effect
Desired effect
Secondary effect
Desirable or undesirable
Onset of action
Time it takes to reach minimum minimum effective concentration after drug is administered
Peak action
Reach it’s highest blood concentration
Duration of action
Length of time drug exerts a therapeutic effect
Dose response relationship
Bodies psychologic response to changes in drug concentration at side of action
Potency
Amount of drug needed to elicit a specific psychological response to a drug
High=significant therapeutic response
Low= minimal therapeutic response
Therapeutic range
Between minimum effective concentration and minimum toxic concentration
Therapeutic index
Difference between therapeutic index and toxic affect
Closer to 1 equals greater toxicity
Peak levels
Highest concentration and Blood sample drawn at peak time
Indicate rate of absorption
Trough levels
Lower plasma concentration and drawn
Immediately before the next dose of drug given
Indicate rate of elimination
Agonist
Drugs that activate receptors and produce desired response
Antagonist
Drugs that prevent receptor activation and block a response
Side effects
Physiological effects not related to desired drug affects and all drugs have side effects
Adverse reactions
More severe side effects unintentional and undesirable
Tolerance
Decrease responsiveness over the course of therapy requires higher dosage of drug