Week 2 Flashcards
Drugs are biologic active substances that can modify
Cell function
Terms used to measure drug response or ACTION
Dose response curve
Potency
Efficacy
Describe dose effect curve
Dose of a drug (amount) given with a measured effect (response)
On a dose effect curve graph what does x axis represent and what does h axis represent
X axis - increasing dose
Y axis - increasing effect of the drug
Describe what the therapeutic effect looks like on a graph
As dose (x axis) increases the effect is 0 at first then a quick increase effect
What does EC50
Effective concentration of drug is needed to get half of maximum effect
What is potency
The amount of drug to provide an effect
Potency is shown by the location along the
Log dose axis (x axis )
10mg of morpheme has the same effect as 100mg of meperidine therefore which is more potent?
Morphine
More potent drugs can reach _____ levels at lower doses
Toxic
What is the maximum intensity of effect (response) that can be produced by a drug no matter the dose
Maximal effect
If drug dose is increased after maximal effect it may increase chance for an?
Adverse reaction
Efficacy indicates?
Drug action
What is the therapeutic index (TI)
Ratio of median lethal dose (LD50) to the median effective dose (ED50)
* TI = LD50/ED50
What is LD50
Death dose in 50% of test animals
What is ED50
Dose required to produce desirable effect on 50% of tested animals
The higher the therapeutic index (TI)
The safer the drug
Drugs do not perform a new function on the organism, either the drug produces the same ____ or ____
The same action as an endogenous agent or block the action of the endogenous agent
Endogenous agents are
Any chemicals produced in your body (ex hormones)
Drug must bind to a ____ on the cell membrane to exert an effect
Receptor
What are drug receptors
Many large molecules (proteins) either on the cell membrane or within the cell
Usually specific drug binds with a specific receptor, what action is happening?
Lock and key
Drug receptor interactions are
Weak chemical bonds
Different drugs compete for same receptor sites, stronger ____(more potent) binds with more receptors than weaker _____ (less potent) drugs
Affinity for both blanks
Describe agonist drugs
Naturally occurring neurotransmitters (NTs)
Describe process of agonist drugs
Affinity for a receptor
Combines with receptor
Produces an effect
Antagonist drugs do what?
Counteracts agonist drugs
What are the 3 types of antagonist drugs
Competitive antagonist
Non competitive antagonist
Physiologic antagonist
Describe the mechanism for competitive antagonist
Affinity for receptor
Combines with receptor
Produces no effect
Describe the mechanism of a noncompetitive antagonist
Binds to a different receptor site than antagonist
Reduces maximal response of agonist
Describe mechanism of physiologic antagonist
Affinity for a different receptor than agonist
Decreases maximal response of the agonist by producing an opposite effect via different receptors
Amount and rate of drug passing through cell membrane are important in what 2 things
Time course of action
Individual response
Membranes are composed of (3)
Lipids
Proteins
Carbohydrates
Lipid soluble substance moves across the lipoprotein membrane by passive transfer called
Simple diffusion using a concentration gradient (from high to low concentration)
Water soluble substances have difficulty passing through
A lipoprotein membrane
In active transport substances are transported
Against a concentration gradient
Blocked by metabolic inhibitors
Mediated by transport “carriers” with energy
Facilitated diffusion does not
Move against a concentration gradient
Factors that influence the movement of drugs are in 4 major steps (ADME)
Absorption
Distribution
Metabolism
Excretion
Absorption refers to the process where drug molecules are transferred from where to what?
From administration site to circulating blood, passing through biologic membranes
What 3 things influence rate of absorption
Physiochemical factors
Site of absorption
Solubility
Weak electrolyte drugs dissociate (separate) in solution (pKa) and break into?
Un-ionized and ionized forms
Describe un ionized
Uncharged non polar lipid soluble
EASILY crosses cell membrane
Describe ionized
Charged polarized less lipid soluble
DIFFICULT to cross cell membrane
What 2 things will determine the amount of drug present in ionized and un ionized states
pH of site of administration and dissociation characteristics
Weak acids are better absorbed when
pH is less than pKa
Weak bases are better absorbed when
The pH is greater than the pKa
Release of dose from a tablet or capsule follows what 4 steps in oral absorption
Disruption (of coating)
Disintegration
Dispersion
Dissolution (dissolved in GI fluid)
Drug in solution skips the oral absorption steps and usually a quicker
Onset of action
Absorption from injection site; if the drug has low solubility then it has a ____ duration
Longer
Drugs occur in 2 forms in the blood
Bound to plasma proteins (reservoir for the drug)
Free drug (pharmacological effect b/c it only passes through cell membrane)
Distribution is the passage of drugs into various body fluid compartments for an
Action
What are some factors of distribution
Size of the organ
Blood flow of the organ
Solubility of the drug
Plasma protein binding capacity
Barriers
Biologic activity of a drug is related to
Concentration of the free or unbound drug in the plasma
(This is the biologically active drug)
drug interaction happens when one drug is bounded and another highly bounded drug displaces the first drug from plasma protein binding sites increasing what?
The effect of the first drug
Blood brain barrier; to penetrate the CNS depends on the (2)
Drugs lipid solubility and degree of ionization
What is a highly lipid soluble un ionized drug easily penetrates the blood brain barrier to access CF and induce sleep seconds after IV
Thiopental
In what kind of circulation are metabolites secreted via bile into intestine and continue with some drug being excreted in the cycle
Enterohepatic circulation
Enterohepatic circulation allows for ?
Prolonged effect of the drug
Drugs get ____ if it goes to a non specific site
Terminated
Metabolism (bio transformation): produces compounds that are more
Polar and more easily excreted
(Mostly in the LIVER)
Metabolite is more ____ and ____ soluble therefore renal reabsorption with be _____ b/c reabsorption favours lipid soluble metabolites
Polar and lipid soluble
Reduced
Metabolism is what kind of process
Enzyme dependent process
What are the 3 ways drugs metabolize
Active to inactive
Inactive to active
Active to active