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74 Cards in this Set
- Front
- Back
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Medical pharmacology
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the science of substances used to prevent, diagnose and treat diseases
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toxicology
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branch of pharmacology used to deal with undesirable effects of chemicals on living systems
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materia medica
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the science of drug prep and the medical use of drugs
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What advent allowed accurate evaluation of theraputic claims
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controlled clinical trial
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Biologic substrate of drug action
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drug receptor
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receptors for which no known ligand is known and whose function is also unknown
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orphan receptors
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Funfact: Receptors and effectors do not function in isolation, they are influenced by regulatory proteins
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That shit cray
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The relation of ones individual genetic make up to his or her response to a specific drug
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Pharmacogenomics
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General principle of drugs 1
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All substances under certain circumstances are toxic and that the only difference between herbs and manufactured drugs are the amount of impurities
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General principle of drugs 2
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All dietary supplements should be held to the same standards as medical drugs in order to not develop a separation between alternative medicine and conventional
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Insertion of the appropriate healthy gene into a pathologic somatic cell
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Gene therapy
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Homozygous knockout
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gene for the receptor or its endogenous ligand has been eliminated, allowed to see what happens in its absence
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Heterozygous knockout
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similar to homozygous, though instead of a complete suppression of gene expression, it is only partial
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Purpose of knockout mice
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visualizes the role of the missing gene product very clearly
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Knockdown mice
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when even partial expression is fatal, these mice can be bread that have a very limited supression of function
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Knockin mice
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overexpression of proteins of interest
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agonist
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activator
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antagonist
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inactivator
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chemical antagonists
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drug that counteracts the effects of another drug by binding to it and not to the receptor in question
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drugs that interact exclusively with water molecules
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osmotic agents
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drugs synthesized in the body
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hormones
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drugs synthesized outside of the body
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xenobiotics
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poisons
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drugs that have exclusively harmful effects
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toxins
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poisons of biologic origin (eg synthesized by plants or animals)
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drug chemical conditions
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electrical charge, shape, atomic size and composition
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Many organic drugs are...
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weak acids or bases
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most drugs have a MW of what
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between 100 and 1000
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why 100
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drugs must have a sufficient size to be able to have a charge, shape, size and composition that fits with the specific receptor, this is the minimum size for those conditions
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why 1000
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drugs larger than 1000MW cannot easily diffuse through the different compartments of the body
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how are large MW drugs delivered
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directly to the compartment of action - clot dissolving alteplase directly into vasculature
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strongest form of drug to receptor binding
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Covalent bond
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covalentbond morphology
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not reversible under biological conditions, usually overcome by either the synethesis of new enzymes (new platelets) also DNA alkylating agents for chemotherapy
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Most common drug receptor binding
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electrostatic binding
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Weakest form of receptor drug binding
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Hydrophobic bonds - important for interactions of lipid soluble drugs with lipid cell membranes
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If you wanted a highly selective drug, which type of receptor would you want?
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You would want a weaker bond because since the bond is weaker, a more precise fit is needed in order to bind
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Funfact: Inert compounds in the chemical sense can have significant pharmacological functions - xenon gas as an anesthetic
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That shit cray
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phenomenon by which drugs exist as two different enantiomers
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chirality
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carvediol
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more potent S form than R form as a B blocker, however equipotent as an A blocker
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Ketamine
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more potent and less toxic as a + enantiomer, still made as a racemic mixture
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Active enantiomer
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as a result of some drugs working in one confirmation only, mixed drugs have only about 50% effectiveness as an active ingredient
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Pharmacodynamic
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Drugs on the body
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Pharmacokinetics
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Body on Drugs
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The final change in function is carried out by what
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effector molecule
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Pharmacologic antagonist
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binds near to a receptor without activating it limiting binding of ligands
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full agonist
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saturates the receptor pool to its full extent
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Partial agonist
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bind to the same receptors as a full agonist but does not evoke as strong as of a response
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when a partial agonist does not stabilize the Ra configuration as well as a full agonist
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low intrinsic efficiency
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presence of antagonist at the agonist binding site will prevent the usual agonist effect
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neutral antagonism
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inverse agonist
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where the drug has a higher affinity for the Ri receptor confirmation, also shuts down constitutive activity (GABA A)
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neutral antagonist (drug)
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flumezenil
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methods to control drug duration
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as long as drug is bound to receptor, sometimes also longer as receptor complex must be destroyed in order to stop expression
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2 conditions for endogenous molecules to act as receptors
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selective in choosing ligands, and change its function upon binding of a drug
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binding with no detectable biological change
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inert binding site
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inactive precursor chemical that must be converted by biological processes to an actual drug
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prodrug
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pathway for drug absorption
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absorbed from site of administration, distributed to site of action, and permeating through barriers between compartments, elimination by metabolism
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type of diffusion that occurs within large aqueous compartments of the body
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aqueous diffusion
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what drives aqueous diffusion
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concentration gradients, described by fick's law
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what specifically does not diffuse through aqueous diffusion
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plasma protein bound drugs (albumin)
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limiting factor for drug absorption
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lipid diffusion because of large amount of lipid barriers in body
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function of special carriers
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molecules that are important for cell function and are too large or too insoluble in lipids to passively diffuse through membranes
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ABC family
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ATP Binding cassette family
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function of ABC pump
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excretion and metabolism of drugs into urine and resistance of tumors to chemotherapy
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types of ABC pumps
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MDR1 transporter, multi drug resistance associated protein(MRP)
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ficks law of diffusion
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the thicker or less surface area a surface has, the slower the diffusion of molecules through it
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ionization of a drug makes it lipid insoluble or soluble
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insoluble
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ionization of drugs
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makes it difficult to permeate lipid compartments
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weak acid drug definition
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neutral molecule that dissasociates into an anion and a proton
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weak base drug
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neutral molecule that can combine with a proton to form a cation
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protonated weak acid is more or less lipid soluble
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more soluble than unprotonated
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if want to prevent filtering of a drug, what to do
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adjust Ph of blood to make sure it is lipid insoluble so it cannot diffuse into the glomerulus
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weak acids excreted faster in what
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alkaline urine
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weak bases excreted faster in what
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acidic urine
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types of amines that can undergo reversible proton binding
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primary, secondary, tertiary
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prototype drugs
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type of drug in a family that best identifies the important characteristics of the group
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