blueprint test 1 advanced pharm Flashcards
A___is a compound that is pharmacologically inactive as administered and then undergoes conversion to its active form via metabolism.
prodrug
The term ____ refers to the rapid hepatic inactivation of certain ORAL drugs.
first-pass effect
If the capacity of the liver to metabolize a drug is extremely____, that drug can be completely inactivated on its first pass thru the liver. As a result ___ therapeutic effect can occur
high
no
to circumvent the first pass effect a drug that goes thru rapid hepatic metabolism is often administered___
parenterally
____is defined as the movement of a drug from its site of administration into the blood
absorption
____is enhanced by rapid drug dissolution, high lipid solubility of the drug, a large surface area of absorption and high blood flow at the site of administration
absorption
__consists of 4 basic processes…absorption, distribution, metabolism and excretion
pharmacokinetics
___ processes determine the concentration of a drug at its sites of action, and thereby determine the intensity and time course of responses.
pharmacokinetic
____ is defined as the movement of drugs thru out the body
distribution
____is defined as the enzymatic alteration of drug structure
drug metabolism (biotransformation)
The most importance consequence of ___ ___ is promotion of renal drug excretion by converting lipid soluable drugs into more hydrophillic forms
drug metabolism
___ excretion has 3 steps glomerular filtration, passive tubular reabsorption, and active tubular secretion
renal
Most drug metabolism takes place in the ___ and is catlyzed by the cytochrome P450 system of enzymes
liver
Most drugs are excreted by the ____
kidneys
____is the study of the biochemical and physiological effects of drugs and the molecular mechanisms by which those effects are produced.
phamacodynamics
In 1906 the first american law to regulate drugs was the_______
federal pure food and drug act
The ___ regulates the safety of drugs prior to approving for use and their authority was expanded in 2007 to include rigorous oversight after a drug has been approved.
FDA
The ___ is responsible for protecting public health, effectiveness and quality of drugs, vaccines,medical devices, food supply, cosmetics, dietary supplements and products that give off radiation, tobacco, labeling, help speed products to market
FDA
_____is the study of drug movement thru out the body
pharmacokinetics
____is the study of what drugs do to the body and how they do it.
pharmacodynamics
_____are molecules that activate receptors.
agonists
When drugs act as _____ they simply bind to receptors and mimic the actions of the body’s own regulatory molecules
agonists
An ________is a drug that has high affinity and intrinsic activity
agonist
_____produce their effects by preventing receptor activation by endogenous regulatory molecules and drugs.
Antagonists
An ______ is a drug with an affinity for a receptor but with no intrinsic activity.
antagonist
____ produce their effects by preventing the activation of receptors by ______
antagonists
agonists
Because ____ act by preventing receptor activation if their is no ____ present the administration of an ____ will have no observable effect.
antagonist
agonist
antagonist
____have only a partial a moderate intrinsic activity. so their maximal efficacy is lower than a full agonist.
partial agonists
____can act as agonists(if there is NO full agonist present) and as antagonists( if a full agonist IS present.)
partial agonists
____is what the drug does to the body
pharmacodynamics
A___ is the components of a celll that interact with a drug.
receptor
drug + receptor is termed _____
coupling
Safer drugs have a ____ therapeutic index value.
higher
_______is any unintended and undesired effect that occurs at normal drug doses.
ADR adverse drug reaction
What population are ADR’s most common in____
elderly adults
A____as a nearly unavoidable secondary drug effect produced at therapeutic doses
side effect
_____is the degree of detrimental physiologic effects caused by excessive drug dosing.
toxicity
_____ is a decreased responsiveness to a drug as a result of repeated drug administration.
Tolerance
______ occurs due to chronic receptor occupation by a drug.
Tolerance
Which FDA pregnancy risk category” proven risk of fetal harm” with WARNINGS on drug label?
D
Which FDA pregnancy risk category “ remote risk of fetal harm”
A
Which FDA pregnancy risk category” proven risk of fetal harm” with CONTRAINDICATED on drug label?
X
Which FDA pregnancy risk category “slightly more risk”?
B
Which FDA pregnancy risk category “greater risk than?
C
Drug sensitivity in the very young results from______
organ system immaturity
How are drugs usually prescribed for pediatric patients (dosage) by ______
body surface area BSA x adult dosage divided 1.73 =dose
By what age ____ are most pharmacokinetic parameters similar to those in adults.
1
what population___ is the following from
drug responses may be prolonged and intense
absorption of IM drugs is more rapid than ____
limited protien binding capacity
blood brain barrier in not fully developed
drug metabolism and excretion is low
infants
adults
children 1 to 12 metabolize drugs ___ than adults
faster
_____have a decline in organ function
older adults
In older adults the proper index of renal function is
creatinine clearance
______ identifies drugs with a high likelihood of causing adverse effects in older adults.
Beers list
Drugs on Beers list to be avoided in older adults
some analgesics,TCA, antihistamines, antihypertensives_ alpha adrenergic blocking agents, sedative-hypnotics, drugs for urge incontinence and some muscle relaxants
what side effects from meds of beers list put elderly pts at risk?
gi bleeding
confusion,falls anticholinergic effects low bp and HR,
3 functions of the autonomic nervous system
regulation of heart, secretory glands and smooth muscle
the autonomic nervous system is divided into 2 parts
sympathetic and parasympathetic
functions of which nervous system?? slowing of HR increased gastric secretion emptying bowel/bladder focusing eye for near vision constricting the pupil contracting bronchial smooth muscle
parasympathetic
functions of which nervous system??
regulating the CV system/body temperature
implementing the fight or flight response
sympathetic
_____to spinal cord then brain
brain to spinal cord to ______
entire process called_________
sensor
effector
feedback loop of the autonomic system
the most important feedback loop of the autonomic nervous system ______
it helps to regulate BP
baroreceptor reflex
In both the sympathetic and parasympathetic nervous system there are 2 places where drugs can act________— ________
the synapses between pre and post ganglionic neurons
the junctions between post-ganglionic neurons and their effector organs
the adrenal gland is part of which nervous system?
autonomic/sympathetic
the adrenal gland releases____ into the bloodstream
epinephrine
the somatic motor system has only ___ neuron in the pathway from the spinal cord to the muscles innervated by somatic motor nerves
1
the somatic motor system has only 1 pathway and 1 site of action which is at _____
neuromuscular junction
the peripheral nervous system employs 3 neurotransmitters___ ___ ____
acetylcholine, norepinephrine and epinephrine
____ is the neurotransmitter used at most junctions of the PNS
acetylcholine
______is the transmitter released by practically all post ganglionic neurons of the syspathetic system
norepinephrine
_____is the major transmitter released by the adrenal medulla.
epinephrine
what are the primary receptor types of the PNS?
cholinergic and adrenergic
____receptors are defined as receptors that mediate responses to acetylcholine
cholinergic
_____receptors are defined as receptors that mediate responses to epinephrine(adrenaline) and norepinephrine
adrenergic
what are the 3 subtypes of cholinergic receptors??
nicotinic(n)
nicotinic(m)
muscarinic
what are the 4 subtypes of adrenergic receptors?
alpha 1, alpha 2, beta 1 , beta 2
dopamine receptors are classified as ___receptors, dopamine receptors only respond to dopamine
adrenergic
which receptor type are located behind eyes, blood vessels, male sex organs, prostatic capsule and bladder?
alpha 1
____receptors are located on the cell bodies of all postganglionic neurons of the parasympathetic and sympathetic nervous systems. ___are also located on the cells of the adrenal medulla.
nicotinic (n)
___receptors are located on all organs regulated by the PNS and also on sweat glands
muscurinic
___ receptors are located on skeletal muscle and causes ____ of skeletal muscle
nicotinic (m)
contraction
activation of ____ receptors in blood vessels produces vasoconstriction
alpha 1
activation of ____ receptors in the sexual apparatus of men causes ejaculation,in smooth muscle of bladder /and prostatic capsule causes contraction
alpha 1
____receptors of the PNS are located on nerve terminals which one of the 4 adrenergic receptors
alpha 2
____ receptors are referred to as presynaptic or prejunctional and there function is to inhibit transmitter release.
alpha 2
___receptors are located in the heart and the kidney.
beta 1
Activation of what receptors cause increase in HR and force of contraction, and velocity of impulse conduction thru the atrioventricular node and promotes renin release in the kidneys
beta 1
activation of what receptor causes the kidneys to release renin into blood which promotes synthesis of angiotensin a powerful vasoconstrictor can help elevate BP
beta 1
which receptors activate the lungs to bronchiodilate
uterine relaxation, vasodilation, increases blood glucose for energy and contraction in skeletal muscle
beta 2
____ receptors are located in the kidney and dilates renal blood vessels, enhancing renal perfusion
dopamine
____ can activate all alpha and beta recptors except for dopamine
epinephrine
____ can activate alpha 1 and 2 and beta 1 but not beta 2 or dopamine receptors
norepinephrine
___ can activate alpha 1 and beta 1 and dopamine receptors only
dopamine
the neurotransmitter ____ degrades into ___ and ___ acetate eliminated and choline taken back up for reuse.
acetylcholine
termination of the life cycle process for ____ is done reuptake for use or inactivation by MAO
norepinephrine
termination for the life cycle process for ___is accomplished by hepatic metabolism and Not by uptake.
epinephrine
activation of _____ receptors increase glandular secretion, contracts smooth muscle in bronchi and gi tract, slows HR, contract the iris sphincter/ciliary muscle, dilates blood vessels,promotes bladder voiding by contracting detrusor and relaxing trigone and sphincter
muscurinic
Bethanechol is an example of a ____ ____
muscurinic agonist