week 18 p2 Flashcards
What does bioavailability mean
- Reflects the fraction of drug absorbed in the systemic circulation when the drug is given orally
- Total Available of drug that reaches the systemic circulation
- Neglects absorption
- Measures by comparing area-under0the curve (AUC) of the drug when measurement of the plasma are made from orally
- Reduction in total drug delivered to the systemic circulations first pass effect
- Reason why its known as that it losses the drug via first through GI tissues and liver before the systemic circulation
What is the equation for Bioavaiblity
• BA=AUCo/AUCiv x100
• AUOo= oral
AUCiv= intravenous
What happens after the drug is in system circulation
drug distribution in tissues
- What is distribution and modulation factors mean
• The process of transferring drug/chemical from the bloodstream to tissues- known as Distribution
What is distribution effected by
ionisation state and pH of the environment: ions trapping, non ionised drugs and chemical can cross cell membrane by passive diffusion
. Lipophilicity: Lipophilicity drugs that can cross cells membrane and blood and brain stream ( as its more preamble) and lipophilicity drugs accumulate in the fattest fat tissue e.g. breast
How is disruption of drugs effected
- Through binding of drugs to proteins
- In the blood drugs are transported in free unbound drug and reversable bond to blood components
- E.g. albumin, alpha-1 and lipoprotein
- Acidic drugs usually bound to albumin
- Basic drugs usually bound to apha-1 and lipoprotein or both
Another way that distribution is affected
• Binding of tissues
• Accumulation of drugs in tissues can prolong drug action
• Due to the tissues this releases accumulated drug as the plasma drug decreases
Lead to toxicity
What is the threptic effects of binding of tissues
• Bisphonate compound bine to bone matric cells
• Rifanmoin and accumulated in the brain
Digitoxin accumulation in heart muscle
- How is the distributions of drugs get into the tissues effected
• Rate of of blood flow to tissues- perfusion
• Tissue mass
Characteristics between blood and tissue
- What does distribution equilibrium mean
• Enter and exit rate are the same between blood and tissue
Is reached more in rich vascularised areas
What does distribution after equilibrium mean
• Drug concentrate and in extracellular fluid are reflected by plasma concentration
What does it mean by volume of distribution
• Volume fluid into the total drug administrated would have to be diluted to produce the concnetration in plasma
Why is plasma concentration important in this
• Retention of a drug in the plasma reflect binding to plasma protein
Equation of volume of distribution
• Concentration= amount of drug/volume
Volume= concentration x amount of drug
Eg of VOD
• if I five you 100mg of drug after that I take a blood sample and measure the plasma concentration is 10mg/l
100mg / 10mg/l = 100l