Exam 1 -- Drug Dosage Regimens Flashcards
steady-state plasma concentration (Css)
the point at which the drug’s intake rate equals its elimination rate, resulting in a stable concentration of the drug in the blood stream during repeated dosing
ineffective range
refers to drug concentrations in the bloodstream that are too low to produce a therapeutic effect
therapeutic range
concentration range of a drug in the bloodstream that produces desired therapeutic effect without causing toxicity or adverse effects
What aer pharmacokinetic variables?
- bioavailability
- volume of distribution
- clearance
determine concentration-time relationships of drug in plasma
bioavailability (F)
the fraction of administered drug reaching the systemic circulation in itsactive form
Which route of administration has the highest bioavailability?
intravenous = 1
* all other routes are lower and somewhere between 0 to 1
minimum effective concentration
the line of plasma concentration that separates the ineffective range from the therapeutic range
apparent efficacy
the observed effectiveness of a drug in producing a desired therapeutic effect in clinical practice
* drugs may have a lower efficacy than seen lab when used in real-world conditions
onset of action
the point where the dose crosses into the therapeutic range from the ineffective range
duration of action
the amount of time spent in the therapeutic range during a dose
rate of availability
rate at which drug enters systemic circulation
* effects onset of action
* can affect apparent efficacy and duration of action
What factors affect the rate of availability?
- dissolution of drug into absorbable form
- blood flow
volume of distribution (Vd)
the apparent body volume in which a drug distributes
How is volume of distribution determined?
Vd = Amount of drug in body / plasma concentration
What factors affect Vd?
body weight and body composition
clearance (CL)
elimination of active drug from the plasma after its distribution
* CL includes elimination by excretion as well as metabolism
How is clearance determined?
CL = rate of elimination / plasma concentration
Factors the affect clearance?
body weight and blood flow to clearance organs
Clearance increases as plasma concentration…?
increases
Css occurs when amount fo drug coming into the body (dose x bioavailabilty) = …?
amount of drug going out of the body (clearance)
Maintenance dose (Dm)
maintains Css by replacing loss due to elimination
* Dm = ((Css * CL) / F) * dosing interval
* maintenance dose is dependent on clearance
Loading dose (DL)
quickly reaches Css by quickly filling Vd
* DL = (Css * Vd) / F
* loading dose is dependent on Vd
half-life
time for plasma concentration of drug to decrease by half
plateau effect
Css is achieved in about 4-5 * half-lifes
zero-order elimination
refers to a pharmacokinetic process in which a drug is eliminated from the body at a constant rate, regardless of it concentration
first-order elimination
refers to a pharmacokinetic process in which the rate of drug elimination from the body is proportional to its concentration