PHARMACOLOGY PRINCIPLES
PHARMACODYNAMICS
processes of interaction of pharmacologically active substances with target sites, and the biochemical
and physiologic consequences leading to therapeutic or adverse effects.
Drug Receptors
determine the quantitative relations between dose or concentration of drug and pharmacologic
effects. The affinity determines concentration of drug required to form significant drug-
receptor complexex
limit the maxiimal effect a drug may produce
responsible for selectivity of action
mediate actions of pharmacologic agonists and antagonists
Dose-Response
response is concentration dependent until a maximal effect is reached which then marks the
plateau where there is saturation at the receptor or overload of a transport process
PHARMACOKINETICS
Processes of uptake of drugs by the body, distribution into the tissue, biotransformations/metabolisms
they undergo, and elimination of the drug and its metabolites from the body
Absorption
Depends on drug’s dissociating from its dosing form, dissolving in gastrintestinal fluids, then
diffusing across the biological membrane barriers into the bloodstream.
Bioavailability – fraction of the drug absorbed in the systemic circulation
- Bioavailability > 70% is most desirable for drugs to be orally useful
Distribution
Metabolism
Biontransformation
Occurs at the liver
Phase I
Phase II
Clearance
THEREPAUETIC-DRUG MONITORING
PEAK
TROUGH
ANTI-EPILEPTIC DRUGS
PHENYTOIN | DILANTIN
o Diphenylhydantoin
o Primary or secondary generalized tonic-clonic seizures, partial or complex-partial seizures, and status
epilepticus
o Principal Metabolite : 5-(p-hydroxyphenyl)-5-phenyldantoin
o Therapeutic Range : 10 – 20 ug/mL (40-79 umol/L)
o Side Effect independent of plasma concentration: Gingival Hyperplasia
o Toxic Effect Manifestations
> 20 ug/mL : Seizure Control not enhanced; Nystagmus and Ataxia
> 35 ug/mL : precipitate seizure activity
o Specimen Collection
Peak : if px displays signs of intoxication; 4-5 hrs after the dose (up to 8 hrs)
Trough :monitor adequacy of therapy
Carbamazepine | Tegretol
o Same use with phenytoin with the addition of treating pain associated with trigeminal neuralgia and as
a mood-stabilizing drug in bipolar disorder
o
Endocrinology/wynlor| 1