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Pharmacology
Pharmacokinetics
| Question | Answer |
|---|---|
| Process by which a drug enters the body | Absorption |
| Extent of absorption determines | Magnitude of response to drug and time of onset of action |
| Forms in which drugs can be administered | Tablets, enteric-coated preparations, sustained release preparations, topical preparations, injectable liquids |
| Routes of administration | Oral, intravenous, inhalation, epithelial, sublingual, rectal |
| Once absorbed, the drug must be transfered betwen one location ad another in the body | Drug distribution |
| Rate which drug enters compartments depends on... | Permeability of capillaries for drug, and perfusion |
| Volume of distribution | Volume of fluid in which the amount of drug in the body would need to be uniformly distributed to produce observed concentration in blood |
| Volume of distribution is determined by... | Strength of binding of drug to tissue components compared with plasma proteins |
| Vd = | Total amount of drug in body / Plasma drug concentration |
| Two processes of elimination | Metabolism and Excretion |
| How do lipophilic properties of drugs affect their metabolism | Hinders elimination from the body |
| Group of hepatic enzymes which catalyse Phase I reactions | CYP450 (cytochrome P450 mono-oxygenase) |
| Phase I reactions are | Functionalisation reactions in which a functional group is added or exposed |
| Phase II reactions involve | A covalent linkage made between a functional group on a drug or Phase I metabolite |
| How do the interactions between drugs affect drug metabolism? | Creates competition for metabolic pathways and drug induced alteration in liver enzymes |
| How does first-pass presystemic metabolism affect bioavailability? | Reduces bioavailability because drugs are extracted so efficiently by liver or gut wall that the amount reaching systemic circulation is considerably less than the amount absorbed |
| How do genetic factors affect drug metabolism? | Genetic polymorphisms result in different expression of enzymes |
| What's CYP2D6? | Catalyses metabolism of beta-blockers, tricyclics and antidepressant, codeine |
| t^(1/2)= | (0.693 x VD)/ CL |
| Bioavailability= | fraction absorbed x fraction escaping first pass clearance |
| Clearance | The ability of an individual organ or the body to eliminate a drug |
| Half-life is a major determinant of | Duration of action of a drug after a single dose AND dosing frequency required |
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