UNIVERSITY OF SANTO TOMAS FACULTY OF PHARMACY | DEPARTMENT OF MEDICAL TECHNOLOGY THERAPEUTIC DRUG MONITORING 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 drugreceptor 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