7 Medicines and Pharmacology Flashcards
Requirements for skin absorption
Based on lipid solubility through the epidermis
Requirements for CSF absorption
Non-ionized, lipid-soluble drugs
Why can you not use sulfonamides in newborns?
Displaces unconugated bilirubin from albumin in newborns
Where are tetracycline and heavy metals stored?
Bone
0 order kinetics?
Constant amount of drug is eliminated regardless of dose
1st order kinetics?
Drug eliminated proportional to dose
How long does it take for a drug to reach a steady state?
5 half-lives
Volume of distribution?
Amount of drug in the body divided by the amount of drug in plasma or blood
Drugs with high VOD have higher concentrations in extravascular compartment (i.e. fat tissue) compared to intravascular concentrations
Bioavailability
Fraction of unchanged drug reaching the systemic circulation IV drugs - 100% PO drugs (less)
ED50
Drug level at which desired effect occurs in 50% of patients
LD50
Drug level at which death occurs in 50% of patients
Hyperactive
Effect at an unusually low dose
Tachyphylaxis
Tolerance after only a few doses
Potency
Dose required for effect
Efficacy
Ability to achieve results without untoward effect
Phase I drug metabolism
Hepatocyte smooth endoplasmic reticulum
Demethylation, oxidation, reduction,hydrolysis reactions
Mixed function oxidases
Requires NADPH/oxygen
Phase II drug metabolism
Hepatocyte smooth endoplasmic reticulum
Glucuronic acid and sulfates attached
Forms water-soluble metabolite - usually inactive and ready for excretion
Biliary excreted drugs may become deconjugated in intestines with reabsorption, sometimes in active form
Inhibitors of P450
Cimetidine Isoniazid Ketoconazole Erythromycin Cipro Flagyl Allopurinol Verapamil Amiodarone MAOIs Disulfiram
Inducers of P450
Cruciform vegetables ETOH Insecticides Cigarette smoke Phenobarbital (barbiturates) Dilantin Theophylline Warfarin
Polar drugs
Ionized
Water soluble
More likely to be eliminated in unaltered form