Week 4 quiz Flashcards
Define pharmacodynamics
the effect of drugs on the body
What functions can be altered from the interaction of a drug and a receptor
change in cell function; alter rate or magnitude of cellular response
What is the most important class of drug receptors?
proteins
What are the four types of agonists
primary, allosteric, partial, inverse
What Is a primary agonist
agonist that binds to the same site as the endogenous ligand
What is an allosteric agonist
agonist that binds to a different site as the endogenous ligand but on the same receptor
What is a partial agonist
a drug that binds to and activates a given receptor but has only partial efficacy at the receptor relative to a full agonist
What is an inverse agonist
Bind to the same receptor as the endogenous ligand but generate a decrease in function
Name the two types of antangonists
Syntopic antagonism, Allosteric antagonism
What is an antagonist?
Drug that competively binds to receptor sites but does not illicit a cellular response
What is syntopic antagonism?
When an antagonist binds to the same receptor site as the endogneous ligand and blocks it from binding
What is allosteric antagonism
When an antagonist binds to a different receptor site on the same receptor and inhibits the endogenous ligand from binding to the primary site
How does the chemical structure of a drug affect its action in the body
If the drugs target receptors are located everywhere, the drug will be distributed everywhere. If the receptors are very specific to a certain site, the drug can target those specific receptors
What is the signature tetrameric ring called in most antibiotics
Beta-Lactam ring
What do racemic mixtures consist of?
Stereoisomers with potentially different pharamacodynamic effects.
Name a drug that would be more effective if it was delivered in only one of its stereoisomer forms
Solalol, Labetalol, Warfarin
How can dynamics change with time in regard to receptors?
down regulation or desensitization
What are orphan receptors?
Receptors discovered through the human genome project that have no known function or drugs that utilize them
What is the pharmacophore?
Chemical properties required for optimal action at receptors: size, shape, position, orientation of charged groups.
What is efficacy
Ability of a drug to activate a receptor and generate a response
Can DNA or pharmacogenetics affect pharmacokinetics or pharmacodynamics?
Yes
Examples of pharmacodynamic drug-drug interactions
Nitrates and Erectile dysfunction drugs
Warfarin sodium and vitamin K with NSAIDS
NSAIDS and hypertension
Are there many drugs that affect ion transport?
No
What are 2 sites of the body that can be affected by ion transport drugs
Kidney - Diuretics and sodium resorption
Gastrointestinal tract -Proton pump inhibitors and hydrogen
How can ion transport channels be acted upon by drugs?
Ligand binding sites - Beta receptor antagonists
Message propagation - Sulfonylurea diabetes agents, calcium channel blockers, etc.
Example of a Beta adrenergic receptor drug?
metroprolol and dobutamine
Typical location of Alpha1 receptors
Postsynaptic effector cells, especially smooth muscle
Typical location of Alpha2 receptors
Presynaptic adrenergic nerve terminals, platelets, lipocytes, smooth muscle
Typical location of Beta1 receptors
Postsynaptic effector cells, especially heart, lipocytes, brain; presynaptic adrenergic and cholinergic nerve terminals, juxtaglomerular apparatus of renal tubules, ciliary body epithelium
Typical location of Beta2 receptors
Postsynaptic effector cells, especially smooth muscle and cardiac muscle
Typical location of Beta3 receptors
Postsynaptic effector cells, especially lipocytes; heart
Parasympathetic neurotransmitter?
Acetylcholine
Sympathetic neurotransmitter?
Norepinephrine or Acetylcholine
Function of parasympathetic M2 receptors?
Slow down heart rate, reduce contraction, reduce conduction velocity
Function of sympathetic Alpha1 receptors?
Arterial and venous constriction
Function of sympathetic Alpha2 receptors?
vasoconstriction locally and vasodilation due to central effect
Function of sympathetic Beta1 receptors?
increase cardiac output, increased pacemaker activity, increased conduction velocity, intrinsic contractility increased
Function of sympathetic Beta2 receptors?
vasodilation
Function of respiratory muscarinic receptors?
bronchoconstriction
Function of respiratory Beta2 receptors?
bronchodilation
Function of urinary bladder muscarinic receptors?
bladder contraction
Function of urinary tract alpha receptors
promote urinary continence
Dopamine receptors are located mainly in the?
brain - some in the renal vascular bed and cardiovascular system
With drugs that have an immediate effect the effect is directly related to?
plasma concentrations
What are time lapse drugs
Drugs that can sometimes have an immediate release of high levels and still elicit a clinical effect when concentrations are low or gone.
Ex. Ace inhibitors
