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問題一覧
1
Focuses on quality aspects of medicines and aims to ensure fitness for medicinal product
Pharmaceutical chemistry.
2
The study of drugs, and involves drug development.
Pharmaceutical chemistry.
3
Involves cures and remedies for disease, analytical techniques, pharmacology, metabolism, quality assurance, and drug chemistry
Pharmaceutical chemistry.
4
Relationship of how structural features of the molecule contribute to or take away from, the desired biological activity
Structure activity relationship.
5
Many compounds containing tertiary amine groups exhibited activity as muscle relaxants when converted to quaternary ammonium compounds. (T/F)
True.
6
Molecules with widely differing pharmacologic properties could be converted to muscle relaxants with properties similar to those of tubocurarine when methylated. (T/F)
True.
7
Natural neurotransmitter and activator of muscle contractio
Acetylcholine.
8
Discovered by Loewri and Navrati
Acetylcholine.
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Selectivity of drug action via the concept of a
Magic bullet by Ehrlich.
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Permitted eradication of disease states without significant harm coming to the organism being treated (patient)
Selective toxicity.
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Magic bullet Modified by Albert into “selective toxicity” (True/False)
True.
12
how one chemical group can produce two different biological effects (muscle relaxation and muscle contraction)
Acetylcholine.
13
Binding of two molecules to receptors on the α-β and δ-α subunits causes the opening of the channel, subsequent movement of potassium through the channel is associated with a graded depolarization causing muscle contraction
Acetylcholine.
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non-depolarizing competitive antagonist at nicotinic acetylcholine receptors, causing the relaxation of skeletal muscle.
D-Tubocurarine.
15
Have a direct effect on absorption, excretion, and compatibility with other drugs in solution
Acid and base properties.
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any substance capable of donating a proton
Acid.
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any substance capable of accepting a proton
Base.
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It indicates the relative strength of the acid or base
Ka- ionization.
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Negative log of the ionization constant
pka.
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A general rule for determining whether a chemical is strong or weak acid or base
Pka.
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strong acid; conjugate base has no meaningful basic properties in water
pka 2.
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weak acid; weak conjugate base
Pka 4 to 6.
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very weak acid; conjugate base getting stronger
Pka 8 to 10.
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essentially no acidic properties in water; strong conjugate bas
Pka 12.
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• pH = pKa + log(A/HA)
Weak acids.
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• pH = pKw–pKb +log(B/HB)
Weak bases.
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The solubility of a drug molecule in water greatly affects the routes of administration that are available, as well as its absorption, distribution, and elimination.
Solubility.
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Dipole-dipole interaction between a Hydrogen atom and a strongly electronegative atom (F, O, N, S, Se)
Hydrogen bond.
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Can also exist between alcohol molecules, carboxylic acids, aldehydes, esters, amines, amides, and polypeptides
Hydrogen bond.
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Weak electrolytes (acids/bases) exist in both an ionized form and a non-ionized form in a solution.
Ionization.
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The extent of ionization depends on the pKa of the weak electrolyte and the pH of the solution. The ionized form is Polar and therefore more water soluble than the non-ionized form.
Ionization.
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it is a relative measure of a drug's lipid and water solubility and is usually expressed in terms of a partition coefficient.
Drug Polarity.
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The presence of oxygen and nitrogen-containing functional groups usually enhances water solubility
Drug Polarity.
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defined as the ratio of the solubility of the compound in an organic solvent to the solubility of the same compound in an aqueous environment
Partition coefficient.
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the combination of an acid and a base.
Salt.
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Two classes based upon the chemical nature of the substance
Salt.
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are made by combining drug molecules with inorganic acids and bases
Inorganic salt.
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in comparison with the parent molecule
Increased water solubility.
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are made by combining two drug molecules, one acidic and one basic
Organic salt.
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generally used to make depot injections
Increased lipid solubility.
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Rule of thumb to evaluate drug-likeness or determine if a chemical compound with a certain pharmacological or biological activity has chemical properties and physical propertie
Lipinski rule of five.
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No more than 5 hydrogen bond donors (the total number of nitrogen–hydrogen
Lipinski rule of five.
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No more than 10 hydrogen bond acceptors (all nitrogen or oxygen atoms
Lipinski rule of five.
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A molecular mass of less than 500 Daltons
Lipinski rule or five.
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An octanol-water partition coefficient (log P) that does not exceed 5
Lipinski rule or five.