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| list the various areas of study that comprimise the pharmaceutical sciences. |
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Definition
| pharmacology, phamracodynamics, pharmaceutical toxicology, pharmacokinetics, medicinial chemistry, pharmaceutics, pharmacogenomics. |
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| the study and design of drug formulation for optimum delivery, stability, pharmacokinetics and patient acceptance |
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| the study of drug design to optimize pharamcokinetics and pharmacodynamics and synthesis of new drug candidates |
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| the study of biochemical and physciological effecst of drugs on organisms |
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| the study of adverse effects of drugs |
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| the study of the factors that control the concentration of drug at various sites in the body. |
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| the study of the cellular and molecular interactions of drugs with their receptors. Also defined as a description of interactions that occur between a drug and its receptor, and succeeding events that lead to pharmacological action of the drug. |
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| a drug must do the following |
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Definition
| has a desirable pharmacological action, has few or not side effects, reaches its intended location in the right concentration at the right time, remains at the site of action for the necessary period of time, is rapidly and completely removed from the body when it is no longer needed. |
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| concerned with the design and dosage forms that will deliver the drug in the right amount at the right time to a patient. Depends on formulation, stability, pharmacokinetics, and patient compliance. |
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| categorization of therapuetic agents |
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Definition
| reasons include: safe delivery of accurate drug dosage, convenience, protection from environment, protection from GIT, and conceal drug taste or odor. Other reasons: liquid preparations, extend drug action, provide rate controlled drug action, place at the optimal site of action, place drug into blood tissue or lungs, and identification. |
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| absorption, distribution, metabolism, and excretion = the steps of a drug while in the body. |
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| describe atomic structure and define atomic number and atomic mass |
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Definition
| Atom is composed of proton, neutron and electron. Atomic number Z: the number of protons. Atomic mass A: the number of protons plus neutrons |
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| Group: a vertical column in the periodic table. Same electron configuration in their valence shell, and share similar properties. Trend from top to bottom: atomic radius increases, ionization energy decreases, electronegativity decreases. |
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| Period: a horizontal row in the periodic table. Same number of atomic orbital’s. Trend from left to right: a progressive filling of valence shell, a progression from metals to non-metals, atomic radius decreases, ionization energy increases, and electron affinity increases. |
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| Two atoms with the same number of protons but different number of neutrons are isotopes. Their chemical and electrical properties are the same. The only thing that changes are the nuclear properties. |
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| Radioisotope is an isotope with an unstable nucleus. Decays by emitting alpha, beta or gamma rays. |
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| Alpha Beta and Gamma rays of radioisotopes |
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Definition
| Alpha: emit alpha particles with 2 protons and 2 neutrons. Beta: emit electron, antineutrinos or positrons. Gamma: emit electromagnetic rays. |
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| Chemical bonds are electrostatic forces holding atoms together to form molecules. Usually involves the valence electrons. |
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| 3 types of chemical bonds and definitions |
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Definition
| 3 types of chemical bonds: Ionic, Covalent, and Metallic. Ionic: the attraction between oppositely charged ions. The electrostatic attractions between positive and negative ion hold the compound together. Covalent: results from the sharing of electrons between atoms. The sharing electrons are attracted to both nuclei involved in the bond. You have single (one pair), double (two pairs) or triple (three pairs) bonding. Triple > double > single bond in order of strength. Nonpolar covalent bonds have electrons that are shared equally. Polar bonds have unequal sharing. |
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| Electronegativity is the power of an atom to attract electrons. If you have high electronegativity then you have increased polarity, which leads to a dipole moment. Dipole: an object whose centers of positive and negative charges do not coincide. |
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Definition
| Dipole Moment: measurement of a dipole. µ = δ x l |
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Definition
| between molecules, hold molecules together, electrical force, much weaker than chemical bonding force |
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Definition
| between 2 molecules within a certain distance can develop electrostatic force, not necessarily a force because of distance. |
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Term
| ionic dipole and dipole dipole |
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Definition
| ionic-dipole interaction – cation develops interaction forming a dipole. dipole-dipole interaction – two dipoles interact, the electrostatic force will interact between the positive and negative. This is true for most organic solvents. |
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Term
| hydrogen bond and van der waals |
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Definition
| hydrogen bond (special type of dipole dipole), Van der Waals force- between nonpolar molecules, result from temporary fluctuations. |
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| rank types of intermolecular forces in order of strength |
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Definition
| ionic > h bond > dipole dipole > van der waals |
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Term
| simple v complex molecule |
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Definition
| Simple molecule: structure determined by chemical bond. Complex: structure determined by chemical bond and intermolecular forces. In proteins, intermolecular forces are used to create the quarternary structure from tertiary. |
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Definition
| A special dipole dipole interaction. Special because of unique position, the strongest dipole dipole interaction. The sharing electrons of H (viewed as proton because of its strong positive charge) are drawn to O or N, hence the dipole interactions. Only occurs when said H is already bonded to O or N and finds itself attracted to a different O or N. |
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| Determines electric force of each objective, and if they are charged they will have electric force between them. F = (K*Q1*Q2) / d^2 where Q1: the charge on object 1 (in Coulombs) Q2: the charge on object 2 (in Coulombs) d: the distance between the two objects (in meters) k: the Coulomb's law constant. (dependent upon the medium). |
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| what does coulumbs law mean? |
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Definition
| if Ke (dielectric constant) decreases then F increases. Alcohol, ethanols, isopropanols decrease the Ke of their solution. The permeability of a given medium is proportional to the Ke of a medium. Permittivity is proportional to its Ke. So Ke is the capacity of the medium to reduce electric force of the charged particles of the objectives, it’s a physical property. If it has a strong Ke, it has strong capacity to reduce electric forces within the medium. Thus electrical force is inversely proportional to the Ke of a medium. |
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| Coulombs and DA Precipitation: anion and cation form an ion pair resulting in precipitation of DNA. Must add salt to make it work apparently to get the anion cation pairing. Need alcohol because it has a smaller Ke so it decreases the overall medium. This in turn increases electric forces between DNA cation and salts anion. Probably a question on this because she said she wants us to be able to use the principles. |
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| medicinal chemistry definition and 3 major aspects |
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Definition
| Medicinal Chemistry- the intersection of chemistry and pharmacology. Invention, discovery, design, identification, and preparation of pharmaceutical drugs. 3 major aspects: 1. Identification, synthesis and development of new chemical entities suitable for therapeutic use. 2. The study of existing drugs of their biological properties. 3. Structure – activity relations (SAR). |
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| Target validation, HT (hithroughput) screening, lead optimization, preclinical, clinical phase 1 (safety), clinical phase 2 (efficacy), clinical phase 3 (2-4 years), lastly in therapy. |
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Heterocycles- a ring structure, containing hetero atoms in addition to carbon: S N O.
Look these up if you want but I think we just need to know the names: Tetrahydrofuran THF, pyridine, triazole, thiazole, pyrrole, pryoline, furan, tetrazole, quinaline, phthalan. |
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| drug receptor interactions |
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Definition
| Receptor: or enzyme. A protein, on the cell membrane, or within the cytoplasm or cell nucleus, bind to ligand (anything that can bond with receptor), result in biological changes. |
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Definition
| Normally, hormones and transmitters fit with their receptors. Agonist: hormone or transmitter fits but doesn’t work. Antagonist: hormone or transmitter doesn’t really fit, example is caffeine. |
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| reversible and irreversible drug-receptor interactions |
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Definition
Most drug-receptor interactions are reversible and contain weak chemical bonds. Irreversible interactions are not common, use covalent bonds.
Covalent bonds between 2 atoms, one from drug and one from receptor. The strongest of all drug-receptor interactions. Are irreversible, generally prolonged duration, have side effects. There are also ionic bonds ( drug cation or drug as anion), hydrogen bonds, hydrophobic interactions (between nonpolar segments, weak interactions). KNOW: Covalent > ionic > h bond > hydrophobic in strength. Usually multiple interactions are involved. |
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| Chemical Name – CAS Index naming system, official name. Code designation. Acronym (not encouraged with professionals). Trivial Name. Trademark. And USAN or nonproprietary/generic name (single, simple, informative. Available for unrestricted public use. Selected by USAN council. Useful because suitability in routine process of prescribing, ordering, dispensing, and administrating. Suitability for use in educational programs. And suitability for international use. |
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| structure activity relationship |
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Definition
| Relationship between chemical structure and biological activity. Chemical structure may affect drug-receptor interactions (bind affinity) and physiochemical properties. |
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Definition
| set of structural features responsible for binding event/site. A set of structural features, be recognized at the receptor site, responsible for the drugs biological activity, generally a small portion of the molecule, more than one functional group, and arranged with a specific geometry. The longer the alkyl chain, the more lipophilic it is. Even numbered chains are very weak as an opioid analgesic. Linear alkyl chain is more lipophilic than branched chain. |
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| functional group modification |
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Definition
| Functional group modification cane reduce or eliminate undesired side effects, improve bioavailability, modify undesired metabolic or excretion properties, and enhance potency. (note: cancer cells use more folic acid compared to normal tissue). Modification can offer oral bioavailability. Androgynous groups and naturally found in the body. You can also replace functional groups/atoms that are monovalent and similar in size (ex: H can be replaced with F). You can also change the stereochemistry to your benefit. |
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Definition
Kinetic: the energy possessed by the motion of an object
Potential: store energy possessed by the position of an object (ex: she held a stapler and it had higher energy the higher it was). Examples- energy stored in chemical bonds, in concentration gradients, in nuclei of atoms, or as electrical potential (separation of charges).
Rest: the energy equivalent of the rest mass of the body. E=mc2 mass converts to energy and vice verse. |
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Definition
| E’= PE + KE. This is bernoulli’s equation. For non-viscous incompressible fluid in steady flow, the sum of pressures, potential and kinetic energies per unit volume is constant at any point. |
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| macroscopic v. microscopic energies |
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Definition
Macro- measurable and observable
Micro- occur at molecular or atomic scale. Molecular kinetic energy is phase change energy. Microscopic potential energy is chemical bond and intermolecular forces. Microscopic rest energy is nuclear energy. |
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| role of microscopic potential energy in the interactin of atoms and molecules |
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Definition
| 2 basic types of interactions of atoms and molecules: attraction and repulsion. It is important in substrate enzyme, ligand receptor, and biosynthetic reactions. SE: transition state due to microscopic energy, optimal distance between substrate and enzyme. Ligand receptor- most drugs exert their actions through ligand receptory interactions. Biosynthetic reactions closely related to Potential energy plot. |
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| importance of ATP in bioenergetics |
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Definition
| Cells store energy in a molecule called ATP. The main source of energy for living organisms is a sugar called glucose. In breaking down glucose (glycolysis), the energy in the glucose molecule’s chemical bonds is released and can be harnessed by the cell to form ATP molecules. ATP hydrolysis provides most of the free energy required for living processes. When O-P bonds are cleaved by hydrolysis it immediately and directly provides the free energy to drive an immense variety of endergonic biochemical reactions. |
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| describe energy diagram in relations to molecular interactions |
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Definition
| you have a PE plot. Repulsion is the dotted line in the positive y-axis part. Attraction is the dotted line in the negative y-axis plot. The smaller the x, or the smaller the distance between atoms, the higher the attraction and repulsion. Makes sense cause they are close together. The most stable point is found on the solid line at the lowest y value. |
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| There are also liquid crystals that are the intermediate between liquid and crystal. Hence the name. they observe flow like liquid but retain properties of crystalline solids. There are 2 types: nematic or threadlike: no positional order but point in the same direction aka packing order. and smectic or soaplike: maintain positional order and align themselves in layers/planes. |
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| lipids as liquid crystals |
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Definition
| Lipid cell membrane is a good example of a liquid crystal. Phospholipids are used as storage, absorption, transport and excretion. The cell membrane is a liquid crystal. Diseases include: 1. Atherosclerosis- laying down of lipid in the liquid crystal state of the walls of blood vessels. As a deposit it is atherosclerosis. 2. Gall stones- formation of liquid crystal of bile. H20, cholesterol, and bile acid in right ratio can form liquid crystal intermediate therefore leading to gallstones. |
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| water as an excellent solvent |
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Definition
| Hydrogen bonding (OH’s, ketones, amines), High dielectric constant (salts), dipole dipole (polar organic molecules), dipole ionic (ionic organic), amphiprotic solvent (strong electrolytes) |
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