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how much and how fast the drug leaves its site of administration. The movement of a drug from its site of administration into the blood. The absorption rate determines how soon the effects of the drug will begin. The amount of absorption then helps determine how intense the effects of the drug will be. This is influenced by the chemical and physical properties of the drug.
Additive effect
the effects of one drug are added to the effects of another drug (1 + 1 = 2); this is different from synergism, where the sum is greater than additive (1 + 1 = 3)
absorption, distribution, metabolism, excretion
Adverse Drug Reaction
drugs can adversely affect all body systems and in varying degrees of intensity. among the more mild are drowsiness, nausea, itching and rash. Severe reactions include respiratory depression, neutropenia, hepatocellular injury, anaphylaxis, and hemorrhage - all of which can result in death. Broadly defined, an adverse drug reaction is an undesired response to a drug.
Adverse effect
an unwanted effect from a drug; it could be a side effect, toxic effect, or allergic reaction, or idiosyncratic reaction.
the degree or strength to which a drug attaches to a receptor. Drugs with high affinity are strongly attracted to their receptors. Conversely, drugs with low affinity are weakly attracted.
a molecule that activates a receptor. When drugs act as agonists, they simply bind to receptors and mimic the action of the body's own regulatory molecules.
an allergic reaction, which means drug acts as an antigen and produces antibodies, resulting in a true allergic reaction (hives/wheezing, etc).Estimates suggest that less than 10% of adverse drug reactions are of the allergic type.
produce their effects by preventing receptor activation by endogenous regulatory molecules and drugs. antagonists have virtually no effects of their own on receptor function.
Binding Sites
sites where the drug receptor macromolecule can bind to and become effective. The receptor sites allow specific molecules to find it by imposing specific requirements on the molecules in which they will interact. Like a lock and key analogy.
the ability of a drug to reach the systemic circulation from its site of administration. Different preparations of the same drug can vary in their bioavailability. Differences occur primarily with oral administration and not with parenteral administration. Factors that influence absorption are: a. solubility of the drug in the contents of the stomach b. dietary patterns c. tablet size d. quality control in manufacturing and formulation
how the body processes a drug; usually what the liver does to the drug to metabolize it. Also known as metabolism.
the lipid membrane that separates materials from getting into the CNS, unless it possesses the lipid characteristics that allow it to pass through the membrane
Clinical Pharmacology
Study of drugs in humans
cooperative and accurate participation in one's own drug therapy. Multiple drug factors and influence compliance. These include manual dexterity, visual acuity, intellectual capacity, psychologic state, attitude toward drugs, and ability to pay for medications.
the movement of drugs throughout the body. This is determined by blood flow to the tissues, the ability of a drug to exit the vascular system, and to a lesser extent, the ability of a drug to enter cells.
Dosage regimen
the dosage or administration schedule. How the drug is to be taken: how often, how long, what time of day, and what dosage amount is indicated.
Drug interaction
the effects of one drug's pharmacological effect on the presence of another drug in the body; could as be drug-food or drug-lab test interaction, in addition to drug-drug
Drug receptors
a functional macromolecule in a cell to which a drug binds to produce its effects. Special "chemicals" in the body that drugs interact with to produce their effects. The term receptor is generally reserved for what is arguably the most important group of macromolecules through which drugs act: the body's own receptors for hormone, neurotransmitters, and other regulatory molecules.
the abbreviation of the median effective dose. ED = effective dose. The dose that is required to produce a defined therapeutic response in 50% of the population. It can be considered a "standard" dose and is frequently selected for initial treatment.
the removal of drugs and their metabolites from the body. Drugs and their metabolites can exit the body in urine, bile, sweat, saliva, breast milk, and expired air. The most important organ for drug excretion is the kidney.
First pass
this refers to the rapid hepatic inactivation of certain oral drugs. When drugs are administered orally, they are absorbed from the GI tract and carried directly to the liver by way of the hepatic portal circulation. The drug can be completely inactivated on its first pass through the liver so that no therapeutic effect will occur. Passage through the liver may be avoided by administering drugs sublingually or parenterally. This permits the drug to temporarily bypass the liver, thereby allowing it to reach therapeutic levels in the systemic blood.
the half-life of a drug is the index of just how rapidly that decline will occur. This is the time required for the amount of drug in the body to decrease by 50%. The actual amount of drug that is lost during one half-life will depend upon just how much of the drug is present: the more drug that is in the body, the larger the amount lost during half-life.
Intrinsic activity
the ability of a drug to activate the receptor following binding.
LD 50
the dose that is lethal to 50% of animals treated.
Loading dose
a large initial dose that is administered to achieve a plateau or target concentration more quickly.
Maximal efficacy
the largest effect that a drug can produce. It is indicated by the height of the dose-response curve. Despite what intuition might tell us, a drug with a very high maximal efficacy is not always more desirable than a drug with lower efficacy.
also known as biotransformation, is the enzymatic alteration of drug structure.. Most drug metabolism takes place in the liver and is performed by the hepatic microsomal enzyme system (Cytochrome P-450)
Minimum theraputic concentration
the minimum blood level need for the drug to have a therapeutic effect (not just the minimum level to have any effect, but a therapeutic effect)
a dose that is toxic, but not necessarily fatal
Peak and trough concentrations
the peak is the highest blood (or serum) level a drug has, usually after several min when given IV, or longer if given by other routes; the trough is the lowest blood level just before another dose is given
the study of the biochemical and physiologic effects of drugs and the molecular mechanisms by which those effects are produced. The study of what drugs do to the body and how they do it.
what the body does to the drug; absorption, distributes, metabolizes, excretes the drug. Drug movement through the body.
the effects of the drug on the body (clinical pharmacology usually implies the patient/clinical-related effects)
what effect a non-pharmacologic or non-active chemical has on the body or what effect the patient reports. A preparation that is devoid of intrinsic pharmacologic activity. The primary use of a placebo is as a control during the testing of new medications.
how effective (strong/weak) a drug is; the effectiveness of a drug in relation to the concentration
the intensity of the effects of taking two drugs together. Potentiative interactions may be beneficial or detrimental. A potentiative interaction that enhances therapeutic effects is clearly beneficial. Conversely, a potentiative interaction that intensifies adverse effects is clearly detrimental.
Relative potency
potency refers to the amount of drug that must be given to elicit an effect. Potency is indicated by the relative position of the dose-response curve. Potency is rarely an important characteristic of a drug. Although potency is usually of no clinical concern, it can be important if a drug is so lacking in potency that doses become inconveniently large. It is important to note that the potency of a drug implies nothing about its maximal efficacy.
Side effect
a normal, but unwanted effect. (E.g. drowsiness is an expected or usual effect of antihistamines. Nausea from narcotics is an expected but unwanted effect.)
Steady state
administering repeated doses of a drug will cause that drug to build up in the body until a plateau (desired plasma level) has been achieved. The drug will continue to accumulate until a state has been achieved in which the amount of drug eliminated between doses equals the amount administered. Average drug levels will remain constant and plateau will have been reached. This plateau is known as steady-state concentration.
Therapeutic index
the measure of drug's safety. It is determined using laboratory animals and is defined as the ratio of a drug's LD50 to its ED50. A large therapeutic index indicates that a drug is relatively safe. Conversely, a small therapeutic index indicates that a drug is relatively unsafe or requires very close monitoring. May also be called the therapeutic window.
the positive or beneficial effect provided by use of drugs
a decreased responsiveness to a drug as a result of repeated drug administration. Patients who are tolerant to a drug require higher doses to produce the same effects that could be achieved with smaller doses before the tolerance developed.
an adverse drug reaction caused by excessive dosing or improper administration. Effects that damage or harm (i.e. renal or ototoxicity). May occur even at normal dose ranges (e.g. aplastic anemia from chloramphenical can occur when the drug is used in the proper dose range).Although the formal definition of toxicity includes only severe reactions that occur when dosage is excessive, the term toxicity has come to mean any severe adverse reaction, regardless of the dose that caused it.
the study of toxins or poisons. Find out what the cause and how much it takes to produce toxins. It is the aspect of pharmacology that deals with the adverse effects of drugs. It is concerned not only with drugs used in therapy, but also with the many other chemicals that may be responsible for household, environmental, or industrial intoxication.
Volume of distribution
the amount of space into which a drug can be distributed. The hypothetical volume of fluid into which the drug is disseminated. The volume of distribution is equal to the amount of drug in the body divided by the concentration in the blood.
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