Basic Principles Flashcards
Action of the body on the drug
Pharmacokinetics
Action of the drug on the body
Pharmacodynamics
Physiologic mechanisms by which a drug produces its adverse effects
Pharmacotoxicology
______________ provides the link between pharmacokinetics and pharmacodynamics and is the focus of the target concentration approach to rational dosing
Concentration
The 3 primary processes of pharmacokinetics are _________, __________ and _________.
input
distribution
elimination
Drugs that produce an effect similar to the natural effect of hormones, neurotransmitters, and other substances
Agonists
Drugs that block the natural effects of hormones, neurotransmitters or other drugs
Antagonists
What type of agonist:
Shift the majority of available receptors into action
Full agonist
What type of agonist:
DO NOT evoke as great a response no matter how high the concentration
Partial agonist
What type of agonist:
Drug will reduce any constitutive activity, thus resulting in effects that are the opposite of the effects produced by conventional agonists at that receptor
Inverse agonist
(T/F) Sufficiently high concentrations of agonists can exceed the effect of a given antagonist
True
Can an antagonist reduce constitutive activity?
No, will only bring receptor effects down to constitutive (basal) activity. Cannot decrease effects lower than this constitutive (basal) level.
What is constitutive activity? Explain in depth to help with understanding.
Within a normal receptor pool, there are innactive forms of the receptor (Ri) and activated forms of the receptor (Ra). This means that there is some level of baseline receptor activity formed by the Ra receptors. This baseline level/effect is called constitutive, or basal, activity.
*antagonist cannot lower effects below this constitutive/basal activity level
Progressively inhibits a response in the presence of a fixed concentration of Agonist
Competitive Antagonists
Forms a covalent bond and the receptor is unavailable to bind with an agonist
Irreversible Antagonists
A drug that creates an ionic bond with another drug
Chemical Antagonists
Use of a drug to interrupt endogenous regulatory pathways mediated by different receptors
Physiologic Antagonists
Inverse agonists have a much higher affinity for the R__ form of receptors
Ri (inactivated form)
Conventional full agonist drugs have a much higher affinity for the R__ form of receptors
Ra (activated)
Partial agonists have an __________ affinity for both Ra and Ri forms
intermediate
(T/F) Conventional antagonist have an equal affinity to both Ra and Ri receptor forms
True
(t/f) allosteric activators/inhibitors act at the same site on the receptor as the drug
False
Allosteric activators/inhibitors act a different site on the receptor
Which drug-receptor bond is the weakest
Hydrophobic
Most common drug-receptor bond
electrostatic
Strogest drug-receptor bond. Often irreversible
Covalent
A signal triggering molecule on a target protein
Ligand
Mediate actions of endogenous chemical signals
Regulatory Proteins
Inhibited or activated by binding to a drug
Enzymes
Available receptors after the max effect of a drug is achieved
Spare receptors
Measured by the concentration of drug that is needed for DR binding
Affinity
The ability of the DR complex to activate ST (signal transduction)
Efficacy
The measure of the magnitude/intensity of a BR produced by the EC100 relative to the maximal attainable response produced in a target tissue
Intrinsic activity
Effective Concentration or Effective Dose required to produce 50% of that drug’s maximal response
EC50 or ED50
