DRUGABSORPTION,DISTRIBUTIONANDELIMINATION;PHARMACOKINETICS.docVIP

DRUG ABSORPTION, DISTRIBUTION AND ELIMINATION; PHARMACOKINETICS I. DRUG ADMINISTRATION Often the goal is to attain a therapeutic drug concentration in plasma from which drug enters the tissue (therapeutic window between toxic concentration and minimal effective concentration). A. Enteral Routes 1. Sublingual (buccal) Certain drugs are best given beneath the tongue or retained in the cheek pouch and are absorbed from these regions into the local circulation. These vascular areas are ideal for lipid-soluble drugs that would be metabolized in the gut or liver, since the blood vessels in the mouth bypass the liver (do not undergo first pass liver metabolism), and drain directly into the systemic circulation. This route is usually reserved for nitrates and certain hormones. 2. Oral By far the most common route. The passage of drug from the gut into the blood is influenced by biologic and physicochemical factors (discussed in detail below), and by the dosage form. For most drugs, two- to five-fold differences in the rate or extent of gastrointestinal absorption can occur, depending on the dosage form. These two characteristics, rate and completeness of absorption, comprise bioavailability. Generally, the bioavailability of oral drugs follows the order: solution suspension capsule tablet coated tablet. 3. Rectal The administration of suppositories is usually reserved for situations in which oral administration is difficult. This route is more frequently used in small children. The rectum is devoid of villi, thus absorption is often slow. B. Parenteral Routes 1. Intravenous injection Used when a rapid clinical response is necessary, e.g., an acute asthmatic episode. This route allows one to achieve relatively precise drug concentrations in the plasma, since bioavailability is not a concern. Most drugs should be injected over 1-2 minutes in order to prevent the occurrence of very high drug concentrations in the injected vein, possibly causing