Basic Principles Flashcards
Actions of body on drug
Pharmacokinetics
Actions of drug on body
Pharmacodynamics
Passive movement of non protein bound drugs between blood and extravascular space through small water filled pores
Affected by DRUG CONCENTRATION and CHARGE
Aqueous diffusion
Permeation
Pharmacokinetics
Exceptions to aqueous diffusion
Brain
Testes
Eye
Placenta
Most important limiting factor for permeation in the BBB and placenta
CONCENTRATION
Lipid Diffusion
Pharmacokinetics
Transport NOT GOVERNED BY FICK’s LAW is limited by
CAPACITY
Transport by special carriers
Pharmacokinetics
Endocytosis is limited by
CAPACITY
Fick’s Law of Diffusion
C1-C2 x surface area x (permeability coefficient/thickness)
Implications of Fick’s Law
Absorption is faster in
LARGER SA SI>stomach
THINNER MEMBRANES lungs>skin
Partial avoidance of first pass effect
Rectal
SRV: IMV to PV
MRV: IIV to IVC
IRV: IPV to IIV to IVC
Slowest route of administration
Topical
More evaporation
Less evaporation
Tinctures
Ointments
Acidic drugs are bound to
Basic drugs are bound to
Albumin
Orosomucoid
Reversible
Shift to R - inc potency - add more S
Examples
Competitive antagonist
Propanolol B blocker and Isoproterenol B agonist
Irreversible
Downward shift - Emax lowered
Examples?
Norepinephrine and phenoxybenzamine
Binds to a different receptor causing the opposite effect
Examples?
Physiologic antagonists
Histamine and epinephrine
Propanolol and thyroid hormone
Inverse agonist
Reduces constitutive activity
Binds with the same receptor to produce opposite effect
Interacts directly with drug
Chemical antagonists
Dimercaprol for lead poisoning
Pralidoxime for organophosphate poisoning