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61 Cards in this Set
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- Back
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Define Pharmacodynamics
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it is the study of the physiological effects of drugs on the body, the MOA, and the relationship between drug concentration and effect
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Define Pharmacokinetics
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branch of pharmacology dedicated to the determiniation of the fate of substances administered externally to a living organism
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Methods of Drug Administration
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Oral, Sublingual, Rectal, Topical (Skin and eye), Inhalation (anesthesia, and anti-ashmatics), Injections (IV, IM, SC, IT), Implants (BC)
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Define
ADME |
Absorption
Distribution Metabolilsm Excretion |
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Orally taken drugs must cross the ___________ to reach the blood supply
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gut wall
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Most orally (active, deactive) drugs pass through the cells ________________ wall
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active, lining the gut
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Thus in the gut, the drugs are required to cross ____ fatty membranes
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two
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Orally active drugs usually obey _________ rule.
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Lipinski's
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____________ drugs can be administered via injection
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Polar
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Define Lipinski's Rule of Five
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MW < 500
No More than 5 HBD groups No more than 10 HBA groups log P < +5 |
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Drug Absorption exception is that small _______ molecules less than ______mw, can cross the gut wall through small pores between cells
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polar, 200
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Drug Absorption exception;
Name the three transport protiens that can carry polar molecules across |
dugs (lisinpril), amino acids, nucleic acid bases
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Drug Absorption Exception:
Define Pinocytosis |
a process allowing the passage of large polar drugs into a cell without actually crossing the cell membrane
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Distribution
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Once across the gut wall, drugs enter the blood stream rapidly as their are no cell membranes to cross , only pores in the walls of the vessels
-Drugs absorbed orally, are first taken in to the liver where drug modification through metabolism occurs -A certain portion is absorbed while the other is deactivated -drug is distributed within 1 minute evenly after absorption |
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Drug Metabolism
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Foreign chemicals are modified by enzymes in the liver
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Metabolic reactions also occur in the ________, ________, and ___________.
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blood, gut wall, other organs
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____________are formed from drug metabolism.
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drug metabolites
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Drug Metabolites are usualy less active, except for ________.
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prodrugs
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Define First Pass Effect
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the phenomenom of a drug metabolism whereas a drug enters the system through the digestive system, taken into the hepatic portal system and is greatly reduced before it reaches systemic circulation
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Name the 4 potential biotransformations:
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Active Drug to Inactive Metabolite
Active drug to Active Metabolite Inactive Drug to Active Metabolite (Prodrug) Active Drug to Toxin (biotoxification) |
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Two pathways of metabolism:
Phase I, and Phase II |
Phase I reaction
Includes Oxidative, Reductive, and Hydrolytic reactions Phase II conjugation method |
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In a Phase I reaction, a polar drug is introduced or unmasked in order to make the drug more ___________ so that it is alle to be ___________
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water-soluble, excreted
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The majority of Phase I metabolites are generated through the __________ enzyme system known as the Cytochrome _________
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hydroxylating, P450
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Phase II reactions involve _________ attachement of small polar molecules to form _______________ compounds
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covalent, water soluble
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name 3 examples of endogenous molecules used in Phase II reactions
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glucoronic acid, gycine, sulfate
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What r the CYTP450 enzymes?
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heme protiens, heme portion is an iron containing porphyrin called protoporphyrin IX, and the protien portion is called an apoprotien
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Where is the CYP450 found?
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high concentrations in the liver, lungs, kidney, intestines, skin, placenta, adrenal cortex.....main one is liver for metabolic action
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Why is it called CYP450
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due to the iron being reduced and binding with carbon monoxide to form a complex that is visible through spectroscopy at 450nm.
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CYP450 is located in the __________________ reticulum of the liver and other cells
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endoplasmic
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Metabolic Transformations
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-
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Oxidative Processes:
Common oxidative processes include? |
the addition of oxygen to various functional groups
Changing the hybridization of groups from sp3 to sp2, etc...by removal of hydrogen |
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Common Oxidative metabolisms include
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Aromatic and aliphatic Hydroxylations, Epoxidation of alkenes, Oxidation of Alcohols to Aldehydes, and sulfide to sulfoxides to sulfones, Oxidation of imines to imine oxides, Dealkylation of heteroatoms
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Aromatic Hydroxilation:
Many drugs posses aromatic rings were this is a major route of drug metabolism. Hydroxylation occurs on these rings that are _____________, those that have electron donating groups, such as _______, ______, ________, ________. |
electron rich
OH, OCH3, NH2. Alkyl Groups |
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The presence of electron _______________ groups usually inhibits hydroxylation of that ring. Name the examples of said groups.
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withdrawing, i.e (F, Cl, Br, I) nitro, nitriles, carbonyls, sulfoxides, and sulfones
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Aromatic Hydroxylation
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-
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Aromatic Hydroxylation most often occurs at the ____________ position to the substituent.
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para
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Ortho substituents are also electron rich, however _________________ usually inhibits hydroxylation at these points
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steric crowding
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if more than one substituent is attached to the ring, then hydroxylation occurs at the ______________________
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para position to the most electron donating substituent
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What are MFO's and what do they do?
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mixed function oxidases, they are responsible for metabolizing the aromatic ring by epoxidation of the electron rich pi bond, resulting in an arene oxide intermediate.
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For a ring to be aromatic it must __________, ___________, __________.
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be flat, have a p-orbital in each atom of the ring, and the pi electrons should equal 2, 6, or 10
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Aromatic Hydroxylation example:
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-
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Epoxides can be acted upon by what enzyme to open the arene oxide with water? What is the product?
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Epoxide hydrolase
trans-dihydrodiols |
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Example of formation of trans-dihydrodiols is:
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-
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Epoxides are electrophiles that can react with other nucleophiles than water, such as _____________, and _____________, and _______________. Such a reaction creates a covalently bound cellular macromolecule which can lead to mutations.
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DNA, RNA, and proteins
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Example of Arene Oxide binding with DNA
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-
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If an arene oxide is formed on the terminal ring of a polycyclic structure and undergoes hydrolysis to a dihydrodiol, this will further undergo epoxidation to form a diol epoxide
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-
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Oxidation of aliphatic carbons adjacent to the functional group results in an alcohol. (the carbon undergoing oxidation must have at least one hydrogen)
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-
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The carbon adjacent to the functional group is called the __________ carbon
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alpha
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The result of alpha carbon oxidation through MFO is that an ....
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oxygen is inserted inbetween the C--H to give a C--O--H
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Alcohol dehydrogenase catylizes the oxidation of alcohols to give you ....
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carbonyl compounds
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Primary alcohols are oxidized to___________.
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aldehydes
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Aldehydes are highly reactive and undergo rapid metabolic oxidation to _________.
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carboxylic acids
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Secondary Alcohols are oxidized to _____________.
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ketones
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Tertiary alcohols and ketones____________ be further oxidized.
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cannot
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Sulfides can be metabolically oxidized by MFO to __________, ___________.
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sulfoxides, sulfones
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Sulfoxides can be oxidized to ______________.
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sulfones
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Sulfones are already in its highest oxidation state, therefore it cannot be further oxidized! (True or False)
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True
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Example of Sulfide Oxidation.....
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-
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Metabolic oxidation of an sp2 Nitrogen produces products called __________ ___________.
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imine oxides.
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These imine oxides exist as zwitter ions? (true or false)
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true
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Example of SP2 oxidation......
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-
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