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nibbs06's version from 2018-11-05 03:00

PGenetics

Question Answer
WARFARINCYP2C9
CLIPIDOGREL2C19 PD -> TO ACTIVE FORM
CODEINE2D6 PD -> TO ACTIVE FORM
POOR METABERS + PRO-DDecreased efficacy and ADR, and no active metabolite
ULTRA METABERS + PRO-DIncreased efficacy (toxicity) and ADR, and excess active metabolite
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FDA REQ GENETIC TESTING FOR …
Question Answer
ISONIAZIDE POOR ACETYLATORSHEPATOTOXICITY (NAT4 NOT ACTIVE)
3 consequences for a PM taking a Pro-DrugDecreased efficacy and ADR, and no active metabolite
3 consequences for a UM taking a Pro-DrugIncreased efficacy (toxicity) and ADR, and excess active metabolite
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MEMORY STUFF

Question Answer
Certain Toxic effects, especially those caused by immunological processesPhase 3
Monitoring of toxicity of a new treatment relative to the standard treatmentPhase 3
Estimating rates of adverse events/toxicityPhase 2
Using a positive control via an established active controlPhase 2
Filing an NDA for a new drugPhase 2
Using MTD as the lead dosePhase 2
Efficacy is the main goalPhase 2
Determines ADME of a drugPhase 1
AUC, Vd & half-life determinedPhase 1
MTD & DLT are determinedPhase 1
Starting dose is MRSDPhase 1
Determines the MTD & DLTPhase 1
Safe Dose range is determinedPhase 1
Has highest rate of drug failurePhase 2
Uses healthy subjectsPhase 1
Effectiveness is observedPhase 4
Non-Compliance is often observed inPhase 4
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PDYNAMICS

Question Answer
EC50 of a drug isEffective Concentration 50 is the concentration of the agonist that is necessary to produce a response that is 50% of the maximum response
EC50 value of a drug tells us about itsPharmacological Potency (Pharm Potency is measured by effectiveness, not mathematically) – inversely related
When comparing 2 agonist drugs of the same efficacy, high affinity(low Kd) predictshigh potency (low EC50)
In a concentration vs response relationship graph, an Antagonist produces a _________ shift, which depends on ___Rightward. Concentration and affinity of the antagonist
IC50 of a drug isthe concentration of an ANTagonist that lowers the max agonist response by 50%
IC50 reflectsKd(affinity) (Inversely)
Positive modulators cause a _________ shiftLeftward
What properties are changed by a modulator?Binding on Allosteric-site by modulator will increase/decrease the affinity at the Orthostatic-site
What values are changed by a modulator?REAL change of EC50 & Potency
The shift made by a modulator depends onmodulator concentration & affinity
Graphs of Antagonists & Modulator are similar in thatthey’re almost the same – the concentration vs response is similar to the concentration vs binding because binding reflects response.
ED50 of a drug isthe Effective Dose in 50% of the population that produces the desired therapeutic effect – a measure of POTENCY (inverse relationship)
Cumulative Quantal Drug Dose-Response Relationship graphs allow us toevaluate therapeutic or adverse effect of a drug in a population of people (ED1-ED99 and TD1-TD99 determined)
To compare the effects of drug effects in a population, we would use acumulative quantal drug dose-response graph
To compare drugs, we can determine therapeutic potency fromED50 or TD50 (Inverse)
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