By Terje Simonsen; et al
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Refer to the text for a more detailed explanation. 3 Absorption, distribution and elimination. These processes occur simultaneously in the organism, but at different rates within a dosage interval. When the concentration is at its peak, the absorption is balanced (to the blood) by distribution and elimination. When all of the drug has been absorbed, absorption stops. When the concentration in the blood is lower than in peripheral tissue, redistribution will be greater than distribution. The illustration depicts the pharmacokinetics of a single dose of drug, eliminated via the kidneys.
A target protein is a part of a larger, more complicated physiological system that adapts itself to what occurs on a molecular level. Such an adaptation can sometimes occur gradually, so that it takes a long time before the full effect of the drug is achieved. This situation is seen in the treatment of high blood pressure (hypertension). When treating hypertension, the full effect will not be evident until 2–4 weeks after drug treatment has commenced. This is because it takes time for the blood pressure-regulating mechanisms to adapt to the new lowered pressure.
Full and partial agonists may compete for the same receptor in a tissue. By simultaneously administering a full and a partial agonist to a patient, the partial agonist will occupy some of the target proteins otherwise occupied by the full agonist. Morphine and buprenorphine both bind to opioid receptors and are used as analgesics. Morphine is a full agonist, while buprenorphine is a partial agonist. If morphine is administered first to reduce strong pains, and a short time later buprenorphine is administered to achieve a ‘supplementary effect’, the buprenorphine will reduce the analgesic effect of morphine by occupying a part of the receptors that the morphine could otherwise have acted upon.