Pharmacodynamics Flashcards
What does it mean for a drug to be classified by its action?
Therapeutic use
What does it mean for a drug to be classified by its molecular target?
Based on receptors or enzymes
Beta blockers block what?
Beta adrenergic receptors
What does it mean for a drug to be classified by its source?
Natural source of the drug
What does it mean for a drug to be classified by its chemical nature?
Broad chemical class (e.g. steroid)
Pharmacokinetics or pharmacodynamics: absorption
Pharmacokinetics
Pharmacokinetics or pharmacodynamics: distribution
Pharmacokinetics
Pharmacokinetics or pharmacodynamics: metabolism
Pharmacokinetics
Pharmacokinetics or pharmacodynamics: targets
pharmacodynamics
Pharmacokinetics or pharmacodynamics: receptor effects
pharmacodynamics
Pharmacokinetics or pharmacodynamics: elimination
Pharmacokinetics
What are the three characteristics of a drug receptor?
- Recognize and bind other molecules
- Propagate regulatory signals
- Modulate ongoing cellular functions
Intracellular receptors bind what type of ligands (what type of chemicals)?
Lipophilic (e.g. steroids, thyroid hormones etc)
Intracellular receptors usually do what to change the cell?
Modulate gene expression
Receptors with enzymatic activity work how?
Extracellular bit binds to molecule, causes changes downstream
What type of receptor is the insulin receptor?
Tyrosine kinase (enzymatic)
Transforming growth factor beta receptors are what type of receptors?
Serine/theonine kinases (enzymatic)
CD45 receptor are what type of receptor?
Tyrosine phosphatases
ANP are what type of receptors?
Guanylyl cyclases (enzymatic)
What type of receptor are the nicotinic/Ach receptors?
ligand-gated ion channels
The ligand-gated channels commonly serve as receptors for what two types of molecules?
Hormones, neurotransmitters
7-membrane-spanning receptors’ N terminus is extracellular, or intracellular?
Extracellular
7-membrane-spanning receptors are coupled to what protein?
G-coupled
What is the MOA of receptors with intrinsic enzymatic activity?
Dimerization of receptor to create an enzyme
Interleukin 3 receptor is of what type?
Receptor that associates with intracellular enzymes
Erythropoietin receptor receptor is of what type?
Receptor that associates with intracellular enzymes
Leptin receptor is of what type?
Receptor that associates with intracellular enzymes
What are the G-coupled receptor?
AKA 7-transmembrane receptor
B adrenergic receptor is of what type?
7TMR
Rhodopsin receptors are of what type?
7TMRs
Frizzled receptors are of what type?
7TMRs
How are receptors regulated?
Number available to bind is either upregulated or downregulated
Why is it important to taper drugs?
Upregulated/down regulated receptors could have very different effect if drug is not there.
What is the equation for Kd?
Koff / Kon
[R][L]/[RL]
What is Bmax?
Maximum binding of drug to receptors
What does the Kd point represent?
Where half of receptors are bound, and half are free
Why do we log the hyperbolic curve generated by Bmax plots?
Easier to find Kd and to compare two drugs
What is the EC50?
Point where a drug is half of its maximal effectiveness
What is a drug’s Emax?
concentration of maximal effectiveness
What is potency?
a measurement of drug dose used to compare the relative affinity and effectiveness of two or more drugs.
What is the numerical value used to compare the potency of two different drugs?
EC50
What is efficacy?
the maximal effect a drug can induce (Emax)
What is the numerical value used to compare the efficacy of two drugs?
Emax
True or false: potency and efficacy are independent of one another.
True
