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
____ is a direct acting muscurinic agonist. it binds reversibly to muscurinic cholinergic receptors to cause activation.
bethanechol
____ is approved for urinary retention.
bethanechol
____ is the best known muscurinic antagonist
( anticholinergic drug)
atropine
___ produces its effects by complete blockade of receptor activation by acetylcholine or drugs that produce those effects.
atropine
_____ is used as a preanethetic med, eye disorders/eye surgery, bradycardia(sometimes), hypermotility/intestinal hypertonicity and muscurinic agonist poisoning.
Atropine
the most effective antidote to antimuscurinic poisoning is____
physostigmine
Cholinergic drugs are agents that influence the activity of _____ receptors
cholinergic
____ drugs act directly at the receptors where they mimic or block the actions of acetylcholine.
cholinergic
cholinergic inhibitors influence cholinergic receptors indirectly by preventing the breakdown of ____
acetylcholine
____ inhibitors are drugs that prevent the degradation of acetylcholine by acetylcholinesterase.
cholinesterase
The major use of reversible cholinesterase inhibitors is in the tx of _____
myasthenia gravis
secondary uses for reversible cholinesterase inhibitors are reversal of competitive (nondepolarizing) neuromuscular blockade and tx of _____
glaucoma
alzheimers, parkinsons dementia and poisoning muscurinic antagonists
____ cause stimulation of parasympathetetic/sympathetic nerves and release of epinephrine from the adrenal medulla
nicotinic (n)
the muscurinic receptors produce effect on their target organ: eye heart lung bladder gi tract sweat glands sex organs blood vessels
contraction
decreased rate
constrict bronchi
contraction of detrusor muscle and relaxation of trigone causes voiding
increased secretions, increased tone and motility
defecation
sweating
erection
vasodilation
muscurinic agonist drug example___
bethanechol
muscurinic antagonists drug example_____
atropine
ganglionic stimulating agents example_____
ganglionic blocking agents example _____
nicotine
mecamylamine
neuromuscular blocking agents example_____
d-Tubocurarine, succinylcholine
cholinesterase inhibitors example______
neostigmine, physostigmine
name 5 catecholamine drugs ____
epinephrine norepinephrine isoproterenol dobutamine dopamine
name 3 non catecholamines drugs_____
ephedrine
phenylephrine
albuterol
what are 3 therapeutic applications of beta blockers____
blocking these receptors will
- reduce HR
- reduce force of heart contraction
- reduced velocity of impulse conduction thru av node.
what is the difference between a selective and non-selective beta blocker?______
1st generation- non selective/ propranolol
2nd generation cardio selective /metaprolol
3rd generation which are both
propranolol is an example of what type/generation beta blocker_____
non -selective /1st gen
metaprolol is an example of what type/generation beta blocker??_____
cardio-selective/2nd gen
if you activate beta receptors what happens ?
increase HR,force of contaction,and av conduction velocity
release renin
dilation of arterioles-heart,lung, skeletal muscle,bronchi, relax uterus, liver glycogenolysis
beta blockers are given to tx (4)______
hypertension,angina, heart failure and svt
beta blockers produce most of their effects by blocking beta ____
1
most beneficial effects from tx with alpha blockers are ____
reduction in bp
_____reduce symptoms of bph by blocking ___ receptors in the bladder neck and prostatic capsule which causes the smooth muscle to relax
alpha blockers
alpha 1
the major adverse effect in tx with alpha blockers is ___
orthostatic hypotension
what does the term alpha adrenergic blockade mean?
drugs that produce selective blockade to alpha adrenergic agents
2 types of adrenergic antagonists______
alpha adrenergic blockers
beta adrenergic blockers
what does the term alpha 1 adrenergic blockade mean?____. what does the prescriber need to know about it____
cause direct blockade,usually reversible
to instruct pts about possible orthostatic hypotension*
reflex tachycardia,nasal congestion, inhibition of ejaculation
what is a alpha antagonist?___
examples of medications that fall into this category___
produces a blocking effect on alpha receptors
prazosin, phentolamine, phenoxybenzamine
what is anticholinergic activity?
what are the symptoms?
blocks the activity of acetylcholine atropine increases HR reduces secretions relaxes intestinal/bronchial smooth muscle, causes urinary retention, cns excitation, eyes-mydriasis
what are alpha agonists used for?
used for hemostatsis,nasal decongestion, elevation of bp.adjuncts to local anesthetics
what are beta agonists?
indications?
adverse effects?
activate beta receptors(clinically relavent only beta 1)
increase HR.
force of contraction
and av node impulse conduction velocity
tachycardia, dysrrhythmias, and angina
adrenergic agonists fall into 2 chemical categories___
catecholamines and non catecholamines
major adverse effects from alpha activation?
hypertension and local necrosis
____ is defined as the ability of a drug to injure a target cell or organisms that are in intimate contact with the target.
selective toxicity
_____ is a chemical that is produced by one microbe and has the ability to harm other microbes
antibiotic/antimicrobial
______ is defined as any agent , natural, or synthetic, that has the ability to kill or suppress microrganisms
antimicrobial/antibiotic
_____ are toxic to their taget by disruption of the bacterial cell wall, inhibition of an enzyme unique to bacteria, and /or disruption of bacterial synthesis
antibiotics/antimicrobial
____drugs are directly lethal to bacteria at clinically acheivable concentrations. ____ drugs can slow bacterial growth but do not cause cell death
bactericidal
bacterial-static
which ____ spectrum of antibiotics promote the emergence of resistance
Broad
A____is a new infection that emerges while being treated during the primary infection
superinfection
the first rule of antimicrobial therapy is to match the bug with the ___
drug
pregnant women are at risk if they use antibiotics, fetal risk of hearing loss to fetus, shouldnt use if breastfeeding either.
PCN is ok in 2nd and 3 rd trimester category b
.
____weaken the cell wall, causing bacteria to take up excessive amounts of water and rupture.
PCN(so they are bacterialcidal)
____ has a beta lactam ring and is known as beta lactam antibiotics
PCN
Since mammilian cells lack a cell wall and since ____ act specifically on enzymes that affect cell wall integrity, the ___ HAVE VIRTUALLY NO DIRECT AFFECT ON CELLS OF THE HOST. SO ____ ARE ONE OF ARE SAFEST DRUGS
PCN
PCN
PCN
___ are enzymes that cleave the beta lactam ring and there by render pcns antibiotics inactive
beta lactamases
and other beta lactam antibiotics (cephalosporins)
beta lactamases that act selectively on PCN are known as ______
penicillinases
Gram ____ bacteria are resistant to pcn’s that cannot penetrate the the cell envelope
negative
____ are the safest antibiotics available
pcn
PCN’s shouldnt be combined with_____ in the same IV solution
aminogylcosides
____are beta lactam antibiotics
cephalosporins
in ____ antibiotics the nucleus contains a beta lactam ring fused to a second ring
cephalosporins
_____ are bacterialcidal drugs that bind to PBPs which damages cell wall and causes cell death similar to pcns
cephalosporins
most __ generation cephalosporins are destroyed by beta lactamases
1st highly active against gram positive
___generation cephalosporins are less sensitive to destruction
2nd
____generation cephalosporins are highly resistant
3rd, 4th, 5th(5th active against msra)
The organism that most ofter causes a UTI ?
E coli
what drug is the treatment of choice for a UTI?
trimethoprim/sulfamethoxazole
____, a urinary tract antiseptic, is a drug of choice for uncomplicated cystitis
nitrofurantoin
_____and _____ act by inhibing bacterial synthesis of folic acid
trimethoprim sulfonamides both broad spectrum
____ and ____are used primarily for UTI
sulfamides and trimethoprim
sulfamides most serious adverse effects are ___and ___
stevens-johnson syndrome and kernicterus(infants)***
The principal adverse effects of trimethoprim are ___and _____
hyperkalemia and birth defects
aminogycosides are _____spectrum antibiotics used primarily against aerobic gram ____bacilli
narrow
negative
____are polar do not absorb in gi tract, can cause damage to vestibular and hearing injury. it happens when trough levels are elevated
aminoglycosides
_____ disrupt protein synthesis and are bactericidal
pregnancy d category
aminogylcosides
____are broad spectrum, bacteriostatic and inhibit bacterial protein synthesis
tetracyclines
____ 1st choice drug for chlamydia ,rickettsia, peptic ulcer disease, anthrax, lyme disease
tetracycline
____ cannot be taken with milk, antacids etc, binds to ca
tetracycline
adverse effect- satain teeth, cant give to pregnant women harm fetal teeth
tetracycline
tetracycline can cause ____ infection
c. diff, candidas
erythromycin is a a ___ antibiotic
macrolide
____is a macrolide antibiotic, bacteriostatic, inhibits bacterial protein synthesis
erythromycin
Clindamycin causes a high incident of _____
c.diff
____ is a macrolide and should be reserved for severe infections , can cause c diff in pts
clindamycin***
_____ a urinary tract antiseptic is a drug of choice in uncomplicated cystitis
nitrofurantoin
The principal cause of drug resistance in ___ is inadequate drug therapy, which kills sensitive bacteria while allowing resistant mutants to flourish.
TB
must treat with 2 to 4 drugs for at least 6 months to 2 years_____ and use DOT
TB
direct observation therapy
3 methods to evaluate tb therapy
sputum. cxr, clinical eval
1st line drugs 4 for tx of TB
isoniazid. rifampin, pyrazinamide, ethambutol
____ act by inhibiting bacterial dna gyrase, can cause tendon rupture (BLACK BOX), pt should be instructed to stop medication at the first sign of tendon pain
fluoroquinolones
fluoroquinolones can exacerbate muscle weakeness in pts with _____. also cause photosensitivity, don’t take with milk (ca products)
myasthenia gravis
_____ drugs have 4 classes
polyene antibiotics, azoles, echincandins, pyrimidine analogs
antifungals
amphotericin B, nystatin are a type of ______
antifungal, polyene antibiotic
1st drug of choice is ____ for mycoses, highly toxic only used in severe, infections, has to be IV
amphotericin B
____ are broad spectrum antifungals, have a lower toxicity can give po
azoles– itraconazole
_____are the newest class of antifungal drugs they disrupt the cell wall
echinocandins- caspofundin
pyrimidine analog - flucytosine is usually always combined with ____ because resistance is common. narrow spectrum used for candidias and cryptococcosis
amphotericin b
superficial mycoses either candidias or dermatophytes class used for this \_\_\_\_
azole such as fluconazole, ( oral _diflucan)//// clotrimazole( used for skin mouth and vaginal fungus), nystatin is used for gi tract infections-fungal
____is the first drug of choice for infections caused by HSV or VZV
acyclovir
__ inhibits viral replication by suppressing synthesis of viral dna( name of drug)
acyclovir- SAFE DURING PREGNNCY
cmv is the cause of ____
drug to tx is ganciclovir in the immunosuppressed host or for prevention in the same. serious side effects
mono
chronic hepatitis is usually caused by___ or___
B C
____ is treated with interferon alfa, ribavirin, and protease inhibitors (boceprevir and telaprevir)
Hep C
Ribavirin always is used in combination with ___ for tx of HCV
interferon alfa
Prinicipal adverse effects of _____ are flu like syndrome and severe depression
interferon alfa
___ cause FETAL *** death/malformation and hemolytic anemia when used in tx of HCV
ribavirin
____ can be treated with interferon alfa and lamivudine( nucleoside analog)
Hep B
flu shot can be given to people age ___ an older
6 months
oseltamivir is used to treat ____
flu
___ is a retrovirus that has RNA as its genetic material.
HIV
Principal targets of HIV are ____
CD4 T cells
____ has 3 phases, initial ( flue like symptoms), middle ( asymptomatic ( can last for 10 yrs), late ( t cells under 200cells/ml) AIDS rendering pt at risk to all kinds of opportunistic infections
HIV
5 classes of meds for tx of ______
NRTI- zidovudine
NNRTI-efavirenz
PI- lopinavir
HIV fusion inhibitors Work outside cell to block entry
CCR5 antagonists “ “
HIV
ART stands for antiretroviral therapy
principal labs in HIV evaluation ____
viral load and t cell count, plasma RNA
______ is the most common STD
preferred tx _____
chlamydia
doxycycline and azithromycin
2nd most common STD______________
caused by______
treated with_____
gonorrhea
Neisseria gonorrhea
gram -
ceftriaxone…. combined with either doxycycline or azithromycin
Syphyllis is treated with _____
penicillin G
genital herpes is treated with _____
acyclovir, famiclovir, or valacyclovir
____is effective as anvirucide but wont kill c diff
ethanol
_____ is lethal to all bacteria/spores/ viruses/fingi
aldehydes
what is the bacteria that most often cause sinusitis? 2
streptococcus pnemoniae
haemophilus influenza
drug tx of choice for sinusitis?
amoxillin- clavulanate _(augmentin)
which type/area is the most dangerous type of sinusitis? requiring iv therapy
sphenoidal—- too close to important structures
What are the 3 most common organisms of otitis media?
dx made by
streptococcus pneumonia
haemophilis influenza
Moraxella catarrhalis
presence of fluid behind tympanic membrane and inflammation of membrane too
drug tx of otitis media____
amoxicillin to start… follow with amoxicillin with clavulanate or cefuroxime if no response in 72 hrs
clinical manifestations of sinusitis 4
persistent symptoms lasting 10 days without improvement, fever, purulent nasal discharge, facial pain or sudden worsening of a viral infection that was getting better
____ is an infection of the skin with some extension to subq tissues
cellulitis
predisposing factors of cellulitis 5
dm, alcoholism, eczema, wounds, venous/lymphatic insufficiency
___ caused by 2 bacteria usually_____ menustration lets bacteria thru cervical canal, most at hisk, young women, sexally active multiple partners, past hx of ___
PID
chlamydia/gonnohrrea
PID
Most common bacteria that cause UTI ____
E. coli
drug for cystitis____
trimethoprim-sulfamethoxazole
drug for uncomplicated pyelonephritis not vomiting oral med _____
with fever vomiting____
fluoroquinolones
ceftriaxone iv
S/S of PCN allergic reaction?
rash, itching, swelling, SOB, anaphylaxsis
____is a joint action between 2 structures or drugs
synergism
____ is the cumulative action or effect
summation
an _____ enzyme is one that catalyses ___ reaction
oxidative
oxidation
____ antibiotics you dont use in common infections or pregnancy
tetracycline
Betalactamase inhibitor, such as_____ are combined with pcn’s to increase activity against beta lactamase producing bacteria
clavulonic acid
others sublactum, tazobactum
if pneumonia is suspected a ____ should always be preformed
cxr
key points on hx of pneumonia cough chest pain, sputum travels/animal exposure, occupational exposure
.
rusty colored sputum is a sign of which organism in pneumonia
tx with what drug____
streptococcus pneumoniae-
outpatient- macrolide- azithromycin or clarithromycin
inpatient- ceftriaxone
most common form of acquired community pneumonia is by what organism?
streptococcus pneumoniae
sinusitis drug of choice for tx?
amoxicillin and clavulanate
for community acquired mrsa drug tx of choice?
trimethoprim and sulfamethoxazoles or doxycycline
for hospitial acquired mrsa drug of choice?
vancomycin, daptomycin
____ means that 2 different preparations of a product are suppose to be the same
bioequivalent
