Pharmacokinetics Flashcards
Window of therapeutic index?
Safer is window is as big as possible
If above window then TOXIC
If lower doesn’t meet effective concentration
ADME
- Absorption
- Distribution
- Metabolism
- Excretion
Compliance
Patients willingness to take drugs
Routes of drug administration
- Enteral (oral rectal)
- Parenteral (subcutaneous/ intramuscular/ intravenous)
- Percutaneous (inhalation/ Sublingual/ topical)
Absorption depends on:
Route of administration
Blood flow at site of administration
Drug solubility
Active vs passive diffusion
Dose of drug
What is bioavailability
Fraction of the total dose administered that reaches the plasma
Does drug diffuse directly to target organs?
No. Drug randomly diffuses.
Chemical properties of a drug:
Chemical nature
Molecular weight
Solubility
Partition coefficient
What affects the absorption of drugs from gastrointestinal tract :
- formulation of drug
- stability of drug (digestive enzymes)
- time available for absorption (tansit time, diarrhoea)
- lipid solubility
- interaction with food
- conc of drug
- blood flow
Pharmaceutical interventions influencing absorption:
- particle size (dry powder inhaler)
- coating of tablets
What is enteric coating of tablets?
Slow-release
Solid core around it and water diffuses in and releases drug
Factors affecting transdermal (through skin) absorption:
- lipid solubility
- formulation
- skin thickness
- hydration
- blood flow
Pinocytosis?
Facilitated diffusion and active transport
Lipophilicity?
Strongly decides whether a compound an pass through membrane
Distribution depends on:
- lipid solubility
- diffusion barriers
- tissue binding
- plasma protein binding (albumin)
One compartment model?
Assume the body is one whole compartment
Pharmacokinetics view of the body (specific properties):
- how many membranes
- pH value
- circulation
- size of surface area
- any diffusion barriers
- any inactivating enzymes
Special highly regulated diffusion barriers?
- Blood brain barrier
- Placenta
AVD
Apparent volume of distribution
The notional volume of fluid required to dilute
the absorbed dose to the concentration found in plasma
How extensively a drug is distributed in the body
What is the AVD of drug that is heavily plasma protein bound?
Low ~ 6 litres