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| A prodrug is a medication or compound that, after administration, is metabolized into a pharmacologically active drug. Inactive prodrugs are pharmacologically inactive medications that are metabolized into an active form within the body |
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| is a guideline for healthcare professionals to help improve the safety of prescribing medications for older adults. It emphasizes deprescribing medication that is unnecessary health care, which reduces the problems of high risk–benefit ratio, polypharmacy, drug interactions, and adverse drug reactions. |
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| subcategory of absorption and is the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. By definition, when a medication is administered intravenously, its bioavailability is 100%. |
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| the situation where the overall intake of a drug is fairly in dynamic equilibrium with its elimination. In practice, it is generally considered that steady state is reached when a time of 4 to 5 times the half-life for a drug after regular dosing is started. |
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| Cmax is a term used in pharmacokinetics refers to the maximum (or peak) serum concentration that a drug achieves in a specified compartment or test area of the body after the drug has been administrated and prior to the administration of a second dose. Cmax is the opposite of Cmin, which is the minimum (or trough) concentration that a drug achieves after dosing.[1] |
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| is a term in pharmacokinetics used to assess the expected in vivo biological equivalence of two proprietary preparations of a drug. If two products are said to be bioequivalent it means that they would be expected to be, for all intents and purposes, the same |
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Definition
At its most basic level, a formulary is a list of medicines.[1] Traditionally, a formulary contained a collection of formulas for the compounding and testing of medication (a resource closer to what would be referred to as a pharmacopoeia today). Today, the main function of a prescription formulary is to specify particular medications that are approved to be prescribed under a particular insurance policy. The development of prescription formularies is based on evaluations of efficacy, safety, and cost-effectiveness of drugs.
Depending on the individual formulary, it may also contain additional clinical information, such as side effects, contraindications, and doses. |
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| a drug or chemical whose manufacture, possession, or use is regulated by a government, such as illicitly used drugs or prescription medications that are designated a Controlled Drug. |
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| The duration of action of a drug is known as its half life. This is the period of time required for the concentration or amount of drug in the body to be reduced by one-half. We usually consider the half life of a drug in relation to the amount of the drug in plasma. |
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| A drug that binds to and activates a receptor. Can be full, partial or inverse. A full agonist has high efficacy, producing a full response while occupying a relatively low proportion of receptors. A partial agonist has lower efficacy than a full agonist. It produces sub-maximal activation even when occupying the total receptor population, |
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| A drug that attenuates the effect of an agonist. Can be competitive or non-competitive, each of which can be reversible or irreversible. A competitive antagonist binds to the same site as the agonist but does not activate it, thus blocks the agonist’s action. A non-competitive antagonist binds to an allosteric (non-agonist) site on the receptor to prevent activation of the receptor. A reversible antagonist binds non-covalently to the receptor, therefore can be “washed out”. An irreversible antagonist binds covalently to the receptor and cannot be displaced by either competing ligands or washing. |
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| Adipex-P, Suprenza, Ionamin |
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| Creatinine is a waste product that is produced continuously during normal muscle breakdown. The kidneys filter creatinine from the blood into the urine, and reabsorb almost none of it. The amount of blood the kidneys can make creatinine-free each minute is called the creatinine clearance. |
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| essential for the production of numerous agents including cholesterol and steroids. Additionally, these enzymes are necessary for the detoxification of foreign chemicals and the metabolism of drugs. |
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| essential for the production of numerous agents including cholesterol and steroids. Additionally, these enzymes are necessary for the detoxification of foreign chemicals and the metabolism of drugs. |
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| An inducing agent can increase the rate of another drug's metabolism by as much as two- to threefold that develops over a period of a week. When an inducing agent is prescribed with another medication, the dosage of the other medication may need to be adjusted since the rate of metabolism is increased and the effect of the medication reduced. |
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Definition
| medication is taken with an agent that inhibits its metabolism, then the drug level can rise and possibly result in a harmful or adverse effect. |
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| Cytochrome P450 3A4 CYP3A4 |
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Definition
| CYP3A4 also is sensitive to enzyme induction, and a number of drugs are known to be CYP3A4 inducers. CYP3A4 inducers tend to lower plasma concentrations of CYP3A4 substrates |
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Definition
| Drugs metabolized by an enzyme |
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| Increase the activity of an enzyme |
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| Decrease the activity of an enzyme |
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| CYP3A4 Substrates Producing Potentially Serious Toxicity When Combined with CYP3A4 Inhibitors |
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Definition
Alprazolam (Xanax)
Carbamazepine (Tegretol)
Cyclosporine (eg, Neoral)
Disopyramide (Norpace)
Sildenafil (Viagra)
Methylprednisolone |
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| Schedule I Controlled Substances |
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| Substances in this schedule have no currently accepted medical use in the United States |
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| potential for abuse less than substances in Schedules I or II and abuse may lead to moderate or low physical dependence or high psychological dependence. |
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| Substances in this schedule have a low potential for abuse |
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| low potential for abuse relative to substances listed in Schedule IV and consist primarily of preparations containing limited quantities of certain narcotics. |
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| A drug's efficiency may be affected by the degree to which it binds to the proteins within blood plasma. The less bound a drug is, the more efficiently it can traverse cell membranes or diffuse. Common blood proteins that drugs bind to are human serum albumin, lipoprotein, glycoprotein, and α, β‚ and γ globulins. |
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