Pharmacology Exam 1

In the equation: 
D+R <-- (K1/K2)--> DR --(K3)--> Effect

what does K1/K2 and K3 stand for?

the ____ of a drug for a receptor is the propensity of the DR complex to form (K1) divided by the propensity of it to dissociate (K2)

____ possess both affinity and efficacy

___ ____ possess affinity, but a lower efficacy than a full agonist that binds to the same receptor

partial agonists have a ___ Emax than a full agonist

____ possess affinity but lack efficacy

aspirin is an example of an _____ because it elicits no response (inhibits the formation of prostaglandins

morphine is an example of a ___ ___ because it elicits a full response

propranolol decreases HR and blood pressure but blocking NE receptors in the heart making it an

valium binds to benzodiazepine receptors in the brain on the GABA complex to produced sedation and decrease anxiety making it an

the intensity of a drug response is related to the number of ?

the range of a blood pressure decrease someone experiences when given a drug is example of a

whether or not a person's BP decreases when given a drug (yes or no) is an example of an

the lower the ED50 is,

binds to target and complex and elicits full response

binding elicits only a portion of response, Emax is lower vs a full agonist

binds with high affinity to a receptor and no response is elicited

binding elicits a response that is in the opposite direction of an agonist

effects of drugs on the body (drug-receptor interactions; dose-response curves)

effects of the body on drugs (absorption, distribution, metabolism, excretion)

relationship which describes both drug potency and efficacy; usually either hyperbolic (linear) or sigmoidal (log) in shape

describes the maximum effect, or how efficacious a drug is with respect to the target response

the dose at which 50% effect is elicited; describes potency of a drug

dose at which 50% of the lethal effect is elicited

competitive inhibitors do what to E50 and Emax?

if a drug has a high therapeutic index that means it is a

an ideal drug is _____ soluble

If a drug is dosed ___ and ____ it does NOT have to be absorbed it is immediately in the blood stream

in acidic conditions, a weak acid is ____ and a weak base is ____

In basic conditions, a weak acid is ____ and a weak base is _____

what are the two main plasma proteins that free drugs bind to?

what types of reactions are phase 1 reactions

the products of phase 1 reactions are more ___ and ___, ___, or _____

what occurs in phase 2 reactions

the products of phase 2 reactions are 3 things

T/F: distribution is the same between the different body compartments
True False

T/F: phase 2 always phase 1
True False

what is most common phase 2 conjugation in humans? Followed by?

where are CYP450's located

the oxidation of a drug involves

accelerates metabolism of other drugs metabolized by the same CYP because it works with DNA to increase the amount of CYP present

increases the amount of enzyme but not the enzyme activity

if this occurs metabolism of drugs by this CYP will decrease and blood levels may rise (bc less is being metabolized ad this may result in increased therapeutic effect of toxicity)

5 organs of excretion

if alkalinize urine:

weak acids, such as phenobarbital), are

if alkalinize urine:

weak bases , such as amphetamine, are

what increases filtration fraction and why

first order elimination is described as what?

zero order elimination is described as what?

with an arithemetic scale, if the elimination is a straight line it is ___

with a log scale, if the elimination is a straight line it is ____

what is faster, first or zero order?

for most drugs, the elimination phase is ____ except for some drugs such as ____ which is zero order

the half life of a zero order processes depends on

drug elimination, since it is essential a first order process can be defined for a given drug by its

the minimum effective drug level to the toxic drug level is known as the

Because of first order drug elimination, doubling the dose of a drug

if the daily dose replaces an identical amount of drug lost through metabolism or excretion each day, the average daily blood concentration and the resulting effect will be constant

states that it takes about four to five half-lives for the average blood concentration and related intensity of response to reach a steady level

5 organs of biotransformation

during chronic drug administration at a fixed dose and dosing interval, the mean steady state level reached is primarily determined by

during chronic drug administration at a fixed dose and dosing interval, the time until a steady state is reached is primarily determined by

during chronic drug administration at a fixed dose and dosing interval, the difference between peak and trough levels is primarily determined by

T/F: if a drug is more lipid soluble,the likelihood of it crossing the blood brain barrier increases
True False