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40 Cards in this Set
- Front
- Back
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How do we distinguish drugs that bind between bases and those that bind on the surface of DNA? (what are the terms we use?)
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Intercalating and non-intercalating.
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What is the mechanism of action of Doxorubicin?
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It intercalates between DNA base pairs and prevents the action of TopoisomeraseII, leaving DNA in separate strands.
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What does vincristine bind to prevent polymerization?
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Tubulin
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How is imatinib excreted?
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Feces
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What are three of the four different types of MAb therapy?
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Naked, Antibody conjugate, ADEPT, ADAPT
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How does cisplatin work?
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It crosslinks DNA, usually guanines, causes destacking and DNA cannot be repaired.
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How is cisplatin administered?
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IV
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A mutation to what type of gene can lead to cancer? Why?
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The RAS of p53
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What is one of the two ways bacteria become resistant to drugs?
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Mutation, genetic transfer
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In what phase of clinical trials do most drugs fail?
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Phase II
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Why are intercalating agents not used systemically?
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Reacts with host cell DNA as well as exogenous cell DNA
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Why don't sulfa drugs target humans?
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humans synthesize pyrimidines via different pathway than prokaryotes
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If a bacterium is penicillin resistant, what enzyme does that bacterium likely have
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β-lactamase
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penicillin disrupts the synthesis of what necessary structure in bacterial
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cross-linkage of cell wall
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what's the different between a topoisomerase poison and an intercalating agent?
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topo poison stabilizes topoisomerase-DNA structure to halt transcription and replication. intercalating stabilizes DNA and does not bind topoisomerase
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you can add what types of groups to ampicillins to make them orally active
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esters
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in the active site what group on sulfonomides can be modified
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the amide group attached to the sulfur
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why are most penicillin drugs not given orally
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not absorbed well and acid sensitive
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how is vancomycin metabolized in the body
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it isn't
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sulfonimides are mostly given by what route
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oral
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what makes a drug a good anesthetic
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it causes quick induction and quick recovery
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what receptors do most anesthetics bind to
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GABA receptors
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what common characteristic of anesthetics allows them to cross the blood brain barrier
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hydrophobicity
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what is the difference between an analgesic and an anesthetic
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analgesic = loss of pain
anesthetic + loss of sensation or general feeling |
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opioid receptors are what kind of receptor
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g-protein linked receptors
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endogenous (naturally occurring) opioids exist in the body. what type of molecule are these?
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peptides (oligopeptides)
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what kind of liver metabolism is morphine involved with/why
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phase II conjugation
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the following is an important medicine, what is the structure called?
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diamorphine, MORPHINE, thebaine, codiene
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the following structure is used as an analgesic, which of the following statements is false
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the structure is a weaker analgesic than morphine, the structure acts as a prodrug, THE STRUCTURE IS CONVERTED TO MORPHINE IN THE BRAIN, the colored methyl group masks an important binding group
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what is the source of this analgesic structure
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opium, frog, AN ENDOGENOUS COMPOUND PRESENT IN THE BODY, snake venom
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what makes the orvinal opiates so potent in relation to morphine derivatives
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orvinol opiates demonstrate greater rigidity, steropspecificity as well as increased substituent binding interaction and are more hydrophobic (cross blood brain barrier)
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which reaction during the modification of thebaine was paramount in the discovery of orvinol opiates
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Diels-Alder cycloaddition
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when designing opiates to induce the highest levels of analgesia, which of the TM g-protein binding sites (μ,κ, or δ) is best to agonize?
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μ receptor induces the largest analgesia effects but also the most side effects
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What receptor does methadone bind to help with detox
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NMDA - acts as an agonist
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How is methadone effective for detox
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it lessens the symptoms of withdrawal without having the euphoria and the doses can be decreased
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why is methadone effective
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stays in the body for long periods and is easily administered
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what is the ratio of men to women with parkinson's disease and what is the gene that is hypothesized to be the reason it is more common in men than in women
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3:2, SRY gene
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What type of reaction does an MAO-B enxyme catalyze
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oxidation of monoamines
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what is the pharaceutical advantage of taking an MAO-B inhibitor along with L'DOPA
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increases the concentration of dopamine in the brain, delaying the need for L'DOPA therapy and/or increasing the amount of L"DOPA administered
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why should parkinson patients avoid taking L'DOPA with food high in protein
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L"DOPA is a hijacking drug which hijacks the transport proten for amino acids
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