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Pharm Block 12
KYCOM Block 12
495
Pharmacology
Graduate
12/04/2013

Additional Pharmacology Flashcards

 


 

Cards

Term
what are the constraints that make anxiety normal
Definition
brief
event related
unconcious, no control
Term
what are symptoms of anxiety
Definition
muscle tone
sweating
tachycardia
tachypenia
weakness
irritability
fatigue
Term
what are the two rules of diagnozing generalized anxiety disorder
Definition
symptoms >6 mo
3+ symptoms from the list
Term
what are the symptoms of generalize anxiety disorder
Definition
excessive anxiety
worry that is difficult to control
feeling on edge
poor concentration/ mind blanking
restlessness, fatigue, sleep disturbance
muscle tension, irrtability
social, occupation, functional impairment
poor coping abilities
Term
what is the non-medication tx for generalized anxiety disorder
Definition
psycho-education
short term councling
stress management
psycho-therapy
exercise
Term
what medications are used to tx acute anxiety, why, what redigmen
Definition
BZD for 2 weeks
most effective, safe, rapid
Term
what medications are used to treat chronic anxiety (4)
Definition
SSRI, SNRI, TCA, buspirone
Term
what medication is used to tx anxiety in kids under 12 (1)
Definition
anti-histamines
Term
what medications are used to treat anxiety in elderly (3)
Definition
burpirone
lorazepam
osazepam
Term
what medications are used to tx anxiety in hepatic failure (2)
Definition
lorazepam
osezepam
Term
what is the map of tx for chronic anxiety
Definition
venlafaxine or SSRI
no effect: switch
no effect: imipramine, busprione, hydroxyzine, pregalbalin, duloxetine
no effect: BZD 2-4 weeks
Term
what are syptoms of panic disorder
Definition
depersonalization
de-realization
fear of loosing control
fear of going crazy
fear of dying
abdominal distress, chest pain, chills, dizzy, choking, hot flashes, palpitations, nausea, paresthesias, SOB, sweating, tachycardia, trembling
Term
what is the non-medication tx for panic disorder
Definition
avoid percipitating substances (caffiene, stimulants)
cognative behavorial therapy
self help books
exercise
Term
what medicine is used for acute/urgent panic dosorder
Definition
BDZ
Term
what is the map of tx for chronic panic disorder
Definition
SSRI or venlafaxine
no effect: switch or try imipramine
no effect: BZD, pindolol, anti-depressant
Term
what are the signs of SAD
Definition
intense irrational persistant fear of being negativley evaluated, scrutinized, or embarrased
fear of adressing group, eating with others, interacting with authority, talking to strangers, using public toiles

blushing, butterflies, diarrhea, sweating, tachycardia, trembling
Term
what are the two types of SAD, describe them
Definition
generalized: avoids wide range of social stituations

non-generalized: fear limited to specific situations
Term
what is the non-medicine tx for SAD
Definition
cognative behavorial therapy for several months in a group
Term
what medicines are used to tx SAD
Definition
antidepressants: SSRI (paroxetine), SNRI
BZD (clonazepam)
GABA analog: gabapentin, pregabaline
B-blocker for "performance" one hour prior
Term
what are the conditions for diagnosis of PTSD
Definition
exposure to traumatic event (witness, experienced, confronted with sutation possible harm) with response of fear, helplessness, horror
Term
what is the map of tx for PTSD
Definition
SSRI (sertaline) for 12 mo
no response: different SSRI, venlafaxine XR
no response: TCA, mirtazapine
Term
signs of OCD
Definition
patients are secretative, hard to diagnosed
often have eczema, chapped skin
compulsive hand washing or teeth brushing
Term
OCD tx
Definition
therapy, SSRI
Term
what anxiety drug can be used in those with substance abuse problems
Definition
busprione
Term
benzodiazapine MOA
Definition
y-aminobutyric acid (GABA) opens Cl channel causing hyperpolarization at post-synapse inhibiting action potential

drug binds to receptors next to GABA receptors increasing GABA affinity (allosteric modulation) causing more Cl channel opening and further inhibition
Term
what are the two types of BDZ and what are they involved with
Definition
BZ1: deals with sleep
BX2: deals with memory, cognative function, muscles, anti-convulsant, ataxia, emotion, anxiolytic
Term
which BDZ has a different MOA, why
Definition
chlorazepate: prodrug that turns into active metabolite
Term
what are the short acting BDZ, how long
Definition
3-8h
osazepam
Term
what and the intermediate acting BDZ, how long
Definition
Lorazepam
alprazolam
10-20h
Term
what are the long acting BDZ, how long
Definition
chlordiazepoxide
diazepam
chlorazepate
1-3d
Term
can you use BDZ in pregnancy, why
Definition
no, crosses placenta and breast milk
Term
what are the main side effects ob BDZ
Definition
drowsiness
confusion
ataxia and fine motor loss
congative impairment (long term recall, new learning)
potentiate alcohol (CNS depressant)
tolerance with time
withdwarl
Term
what occurs in BDZ withdrawl
Definition
anxiety
insomnia
irritability
weakness

severity is drug and dose dependant
avoid with titration
Term
where does BDZ distribute to
Definition
lipid soluble: goes to brain and perused organs first
Term
where and when and how is BDZ metabolized
Definition
metabolized to water soluble in liver before elimination

oxidation, hydroxylation, conjugation with glucuronic acid
Term
where and when is BDZ excreted
Definition
after metabolized in urine
Term
what BDZ have different metabolism, why
Definition
lorazepan and oxazepam bipass liver oxidation and have shorter half life
Term
what substances can reduce oxidation of BDZ in liver
Definition
liver disease
cimetidine
contraceptives
Term
what drug is a benzodiazepine antagonist
Definition
fulmazenil
Term
how does fulmazenil work
Definition
binds to sites to competitavly antagonize allosteric effect of BDZ
Term
why would you use fulamazenil
Definition
BDZ over dose or side effects
Term
what drug is a azapirone
Definition
buspirone
Term
MOA buspirone
Definition
partial agonist to 5HT receptors in limibc which activate G receptors and open K channel hyperpolarizing and decreasing firing
Term
side effects of buspirone
Definition
little CNS depression, motor effect, muscle relaxing, anti-convulsant

no physical dependance or withdrawl

headache, dizziness
Term
which anxiety drugs have slowest onset
Definition
buspirone, SSRI
2 weeks
Term
what are two SSRI are for anxiety
Definition
paroxentine
sertaline
Term
SSRI MOA
Definition
inhibit re-uptake of serotonin at transporter
blocking removal increases concentration at synaptic cleft
Term
SSRI side effects
Definition
no dependance, withdrawl, CNS depression alcohol potentiation

insomnia, tremor, palpitations, vasldilation, NVD, loss of lobido

paroxetine: postural hypotension

anorexia, nausea, vomiting, diarrhea

loss of libido, sexual dysfunction
Term
SSRI distribution
Definition
protein bound
Term
SSRI metabolizm and excretion
Definition
metabolized in liver
excreted in feces and urine
Term
what drugs alter SSRI
Definition
cimetidine increase half life
MAOI can be fatal (wait 14 d for switch)

TCA inhibits metabolism

tryptophan increases serotonin effect

warfarin increases bleeding risk
Term
what drug is a SNRI (3)
Definition
venlafaxine
duloxetine
desvenlafaxine
Term
MOA SNRI
Definition
block serotonin and NE re-uptake transporters
Term
side effects SNRI
Definition
simillar to SSRI

hypertension

do not abruptly DC, slowly titrate due to BP effects
Term
what are the anti-histamine anxiety drugs
Definition
Piperazine Deratives...
Hydroxyzine HCl
Kydroxyzine Pamoate
Term
MOA anti-histamine anxiety drugs
Definition
antagonizes H1 receptor (excitatory) located in hippocampus and cortex
Term
side effects of anti-histamine anxiety drugs
Definition
sedation
do not combine with alcohol
Term
MOA mirtazapine
Definition
blocks pre-synaptic autoreceptors for NE and 5HT and increases NE and 5HT at synapse
Term
in who is depression most common
Definition
women
Term
define unipolar depression
Definition
no family history
Term
what is the most common form of depression
Definition
unipolar
Term
what are signs of depression
Definition
affective, cognative, motor, somatic
prominent and persistent symptoms
anhedonia
insomnia
fatigue
worthlessness andguild
inability to concentrate
thoughts of death or suicide
Term
define anhedonia
Definition
loss of interest in activities
Term
what is the prognosis of depression
Definition
usually does not reoccur once subsides
10-15% suicide
40-50% improve with tx
Term
what do you do if someone has reoccuring depression
Definition
prophlyactic tx
Term
signs of manic depression
Definition
eophoric mooods
pressured speech
psychomotor aggitation
distractability
insomnia
severe depression spells
Term
why shouldnt you use paroxetine in eldery
Definition
postural hypotension
Term
which SSRI are for depression
Definition
citalopram
escitalopram
paroxetine
sertaline
fluxetine
Term
which SSRI are for SAD, PTSD, OCD, which is PTSD DOC
Definition
paroxetine
sertaline - PTSD DOC
Term
uses of SNRI
Definition
depression
chronic anxiety
chronic panic
SAD
PTSD
Term
uses of piperazine derivatives
Definition
chronic anxiety
Term
side effects of Mirtazapine
Definition
sedation
1% incidence of agranulocytosis
Term
use of mirtazapine
Definition
chronic anxiety
depression
PTSD
Term
MOA trazodone
Definition
inhibit serotonin reuptake (less than SSRI)
Term
trazodone side effects
Definition
little anticholinergic, hypotension, and CV effects

more safe than TCA
Term
trazodone use
Definition
depression
Term
bupropion MOA
Definition
inhibit dopamine and NE reuptake
Term
buproion side effects
Definition
stimulating, dont take at bed time
Term
use buproion
Definition
depression
Term
what are the atypical anti-depressants
Definition
bupropion
trazodone
mirtazapine
Term
3 tricyclic antidepressants
Definition
imipramine
amitripryline
clomipramine
Term
MOA TCA
Definition
block NA and serotonin reuptake transporter on nerve
Term
uses TCA
Definition
depression
chronic anxiety
bedwetting - imipramine
chronic panic
PTSD
Term
side effects of TCA
Definition
no mood elevation in normal pt
unmasks manic behavior in bipolar - watch out

narrow theraputic index (5-6x is lethal)

sedation, light headed, hypotension, weight gain

anticholinergic: dry mouth, blurred vision

amine inhibit and anticholinergic: postural hypotension, tachycardia, flat T wave, supress depolarization
Term
what drugs interact with TCA, what happens
Definition
quinidine class I antiarrhytmic: dangerous with flat T wave side effect

MAOI: HTN, convulsion, coma

adrenergics: potentiate, stop amine removal

ethanol: toxic sedation (CNS depression)
Term
what drugs are MOI
Definition
tranylcypromine
phenelzine
Term
normal function of MAO
Definition
mitochondria enzymes that break down dopamine and serotonin in liver and brain
Term
what are the types of MAO, where are they
Definition
A: everywhere
B: stratum
Term
MOA MAOI
Definition
suicide inhibiton of MAO increases NT in cleft
Term
interactions with MAOI
Definition
SSRI
trazodone
venlafaxine
warfarin
OTC decongestants
tryamine

cause serotonin syndrom
Term
signs of serotoniin syndrome
Definition
seizure, coma, death
Term
where is tryamine found, what does it normally do in body
Definition
cheese, liver, beer, wine

inactivated by MAO in gut
Term
why is tryamine bad with MAOI
Definition
MAO normally breaks it down so now it builds up in nerves causing headache, nausea, HTN, arrhytmia, stroke
Term
use of MAOI
Definition
depression
Term
5 drugs used for manic depression
Definition
lithium salts
carbamazepine - anticonvulsant
valproic acid - anticonvulsant
gabapentin - anticonvulsant, neurotic pain relief
risperidone
Term
MOA lithium salts
Definition
membrane stabilization
can replace Na in AP but isnt enough to run the pumps

Alters IP3
Term
side effects of lithium salts
Definition
no sedation, euphoria, depression

low theraputc index need to monitor blood levels

nephrgenic diabetes insipidus
contraindicated in sick sinus syndrome
reversable hypothyroidism and goiter
tremor
Term
signs of lithium salt overdose
Definition
seizure, circulatory collapse
Term
interactions with lithium salts and their side effect
Definition
thiazide diruetics
MAOI- MALIGNANT HTN
Term
define psychosis, what are signs
Definition
disturbance of reality and perception
impaired cognative functioning
inappropirate or bad affect
Term
what are causes of psychosis
Definition
drug abuse
dementia
alzheimers
schizophrenia
Term
prognosis of schizophrenia
Definition
life long, no cure
need drugs all life
usually bad compliance
Term
cause of schizophrenia
Definition
idiopathic, shows in teens
Term
what are schizophrenia drugs called on the street, man
Definition
neuroleptic agents
major tranquilizers
Term
MOA schizophrenia
Definition
over action of biogenic amines as NT
Term
positive symptoms of schizophrenia
Definition
exaggerated distorted function
hallucinations, delusions
disorganized behavior
Term
negative symptoms of schizophrenia
Definition
loss of normal function
diminished speech
blunted emotions
loss of energy
inability to experience pleasure
Term
7 typical anti-psychotic drugs
Definition
pheothiazines
aliphatic - chlorpromazine
piperazine - trifluoperazine
fluphenazine
pierdine - thioridazine
butyrophenones
thioxanthenes
Term
what are the three most potent anti-psychotics, which is most of all
Definition
piperazine - trifluoperazine
butyrophenones
fluphenazine - MOST
Term
which anti-psychotic drugs come in depot form
Definition
butyrophenones
fluphenazine - MOST
Term
in general how to typical anti-psychotics work
Definition
interact with many NT systems and bind to many receptors antagonizing them
Term
MOA typical anti-psychotic
Definition
mostly antagonize dopamine D2 receptor (which is main one in brain)

physiological depolarization inactivation: initially increases firing at presynaptic neuron and later decreases release

post-synaptic neuron is antagonized entire time
Term
where are typical anti-psychotics acting
Definition
mesocortical mesolimbic tract
Term
how long does it take for typical anti-psychotics to work
Definition
weeks
Term
reason for extra pyrmidal side effects of anti-psychotics
Definition
D2 activity on motor systems
Term
reversible neurological extra pyrmidal side effects of anti-psychotics
Definition
acute dystonia: spasm in face, neck, back early in tx

akathisia: motor restlessness later in tx

parkinsonism

neuroleptic malignant syndrome
Term
what is neuroleptic malignant sndrome
Definition
severe parkinsons
fever
unstable BP
Term
tx neuroleptic malignant sndrome
Definition
DC anti-psychotic
dantrolene
Term
irreversible neurological extra pyrmidal side effects of anti-psychotics
Definition
tarditive dyskinesia: repetitive tick like movement of face, trunk extremities
Term
what agents most often cause irreversible neurological extra pyrmidal side effects of anti-psychotics
Definition
piperazine
heloperidol
Term
autonomic side effects of anti-psychotics cause
Definition
a-adrenergic blocking (develop tolerance over time to it tho)
Term
autonomic side effects of anti-psychotics
Definition
hypotension
sedation
stroke in elderly
Term
which antipsychotic most often causes a-adrenergic side effects, which least does
Definition
thioridazine - most
heloperidol - least
Term
endocrine side effects of anti-psychotics cause
Definition
block tuberoinfundibular dopamine pathway so it cannot regulate prolactin
Term
endocrine side effects of anti-psychotics
Definition
hyperprolactinemia
weight gain
gynecomastia
amenorrhea galactorrhea
Term
side effects specific to thioridazine
Definition
retinal deposits cause visual impairment
Term
signs of overdose of anti-psychotics
Definition
conduction defects that cause ventricular arrhytmia

probablly taking thioridazine others dont cause it much
Term
general MOA of atypical anti-psychotics
Definition
more specific to dopamine receptors causing less extra-pyrmidal side effects
Term
6 atypical anti-psychotics
Definition
clozapine
risperidone
olanzapine
quetiapine
paliperidone
airiprazole
Term
MOA clozapine
Definition
high affinity D4
low affinity D2, 5HT2, muscuranic, H1
Term
side effects of clozapine
Definition
stroke in elderly with dementia
intermediate autonomic effects
severe agranulocytosis so monitor WBC
Term
use of clozapine
Definition
not first line, last choice
Term
risperidone MOA
Definition
clozapine analog
high affinity 5HT2
medium affinity D2
Term
risperidone side effects
Definition
stroke in elderly with dementia
hyperglycemia and diabetes
low extra-pyramid side effects
minimal sedation
increased QT (cannot use CVD)
Term
use risperidone
Definition
tx negative symptoms of schizophrenia well
first line therapy
Term
olanzpine MOA
Definition
clozapine analog
high 5HT2 affinity
intermediate D2 affinity
Term
olanzapine side effect
Definition
stroke in elderly with dementia
hyperclycemia and diebetes
low extra-pyramid effects
minimal sedation
Term
olanzapine use
Definition
lessen symptoms of tardive dyskinesia
first line anti-psychotic
tx negative symptoms of schizophrenia well
Term
quetiapine MOA
Definition
clozapineanalog
high affinity 5HT2
intermediate D2 affinity
Term
quetiapine side effects
Definition
stroke in elderly with dementia
hyperglycemia and dementia
low extra-pyrmiad effect
minimal sedation
Term
quetiapine use
Definition
tx negative symptoms of schizophrenia well
Term
paliperidone MOA
Definition
active metabolite od risperidone
high affinity 5HT2
intermediate D2 affinity
Term
paliperidone metabolizm
Definition
no hepatic
renal only
Term
paliperidone side effects
Definition
stroke in elderly with dementia
hyperglycemia and diabetes
low extra-pyramid effect
increased QI wave(no use un CVD)
minimal sedation
Term
paliperidone use
Definition
first line therapy
tx negative schizophrenia symptoms well
Term
airiprazole MOA
Definition
partial D2, 5HT2, 5HT1A agonist (kicks out full agonist lesseing effect)

antagonist 5HT2A, 5HT7

affinity for H1, a-adrenergic, D4

no affinity for cholinergic receptors
Term
airiprazole side effects
Definition
stroke in elderly with dementia
Term
airiprazole use
Definition
anti-psychotic
bipolar disorder
major depression
Term
MOA benzodiazepines
Definition
receptors on GABA-Cl channel receptor complex increasing frequency of channel opening causing hyperpolarization
Term
side effects of all sleep BDZ
Definition
tolerance develops fast

increase effect of alcohol

avoid in sleep apenea because it relaxes muscles of upper airway
Term
define insomnia
Definition
cannot initiate or maintain sleep (symptom not disease)
Term
define hypersomnia
Definition
excessive sleep
Term
define circadian rhythm alteration
Definition
disturbance in sleep wake cycle (jet lag)
Term
define parasomnia
Definition
dysfunction of sleep like partial arousal
Term
what are the stages of the sleep cycle, how long, how many
Definition
stages 1-4: NREM
stage 5: REM
95 min each
4-5 per night
Term
what are the short acting sleep BDZ, how long
Definition
3-8 hours
midazolam
triazolam
Term
what are the intermediate acting sleep BDZ, how long
Definition
10-20 hours
temazepam
estazolam
Term
what are the long acting sleep BDZ, how long
Definition
1-3 days
quazepam
fulrazepam
Term
side effects of short acting BDZ for sleep
Definition
Triazolam only: tolerance in days, withdrawl causes rebound
Term
side effects of long acting BDZ for sleep
Definition
daytime sedation
hang over effect
Term
administration of midazolam
Definition
oral suryp, IV, IM
Term
use of midazolam
Definition
peanecthetic and intraoperative medication (anterograde amnesia)
Term
user of triazolam
Definition
reoccuring insomnia
initiating sleep
Term
use of intermediate BDZ for sleep
Definition
frequent waking
Term
use of long BDZ for sleep
Definition
reduce sleep
induration
decreasing waking
increase duration
Term
what type of drug is zolpidem
Definition
imidazopyridine derivative
Term
MOA zolpidem
Definition
binds to BDZ receptor at GABA-Cl channel causing hyperpolarization

does not affect different stages of sleep like BDZ or barbituiates
Term
what type od drug is zaleplon
Definition
pyrazolopurimidine derivative
Term
MOA zaleplon
Definition
binds to BDZ receptor at GABA-Cl channel causing hyperpolarization

does not affect different stages of sleep like BDZ or barbituiates
Term
ecozpiclone MOA
Definition
binds to BDZ receptor at GABA-Cl channel causing hyperpolarization

does not affect different stages of sleep like BDZ or barbituiates
Term
ramelton MOA
Definition
melatonin receptor agonist
binds mT1 and MT2 receptors for melatonin
Term
what type of drug is chloral hydrate
Definition
halogenated alcohol
Term
MOA chloral hydrate
Definition
unknown activate metabolite trichloroethanol
Term
zolpidem side effects
Definition
minimal rebound insomnia and tolerance

sleep walking/activities, amnesia (increases with alcohol)
Term
zaleplon side effects
Definition
minimal rebound insomnia and tolerance
Term
eszoipclone side effects
Definition
minimal rebound insomnia
Term
ramelton side effects
Definition
NO anoxiolytic, muscle relaxant, amnesic, or abuse potential

do not consume alcohol

decreased testosterone
Term
zolpidem use
Definition
sleep longer
jet lag
long term administration
Term
eczopiclone use
Definition
sleep longer
long term use
Term
ramelton use
Definition
difficulty initiating sleep
good for elderly
Term
chloral hydrate use
Definition
sedation in kids (dental)
Term
which sleep medicine is not a controlled substance, why
Definition
ramelteon: no CNS depressiing
Term
which sleep medicine is affected by P450 inducers and inhibitors
Definition
ramelton
Term
which sleep medicine has a continous release capsule, explain how it works
Definition
releases 5-10 mg immediatly and the rest over 3 h
Term
define agonist
Definition
drug that binds to the same site as the ligand and makes the same signal
Term
define allosteric agonist
Definition
drug that binds to different site than drug making no signal but causing drug to be more effective
Term
define partial agonist
Definition
drug produces lesser response than the ligand and competes for ligand site
Term
define competitive agonist
Definition
drug binds reversibly to receptor but increase in ligand can overcome it
Term
define non-competitive agonist, what are the two types
Definition
binds to receptor and prevents agonist from producing max effect

irreversible: more common, same receptor
allosteric: different receptor
Term
how can you tell if something on a graph is more potent or effective
Definition
moving left on the X axis is more potent
moving up on the Y axis is more effective
Term
what does a partial agonist graph look like compared to agonist
Definition
less effective
shorter, less high on the Y axis
Term
what does a allosteric agonist graph look like compared to agonist
Definition
same effectiveness (height on Y axis)
increased potency (more left on X axis)
Term
what does a non-competitive agonist graph look like compared to agonist
Definition
very short, sinking
less effective (height on Y axis)
less potent (more right on X axis)
Term
what does a antagonist graph look like compared to agonist
Definition
same effectiveness (height on Y axis)
less potency (more right on X axis)
Term
how does a Gs protein work
Definition
activates cAMP which increases PKA
Term
how does a Gi protein work
Definition
decreases cAMP which decreases PKA
Term
how does a Gq protein work
Definition
releases IP3 and DAG
IP3 releases Ca
DAG and Ca activate PKC
Term
what is the point of equal ionization
Definition
pKa
Term
what happens to an acid and base if you put it in stuff that is lower (more basic) than the pKa
Definition
acid will ionize
base will not ionize
Term
what happens to an acid and base if you put it in stuff that is higher (more acidic) than the pKa
Definition
acid will not ionize
base will ionize
Term
what form of a drug is best excreted
Definition
WA will be excreted beter in a basic enivornment

WB will be excreted better in an acidic enivornment
Term
what form of a drug is best distributed in the body
Definition
the same form

WA likes acid
WB likes base
Term
what is used to fix and WB or WB drug OD
Definition
NaHCO3 is used to alkalize urine and fix WA OD

NH3CL is used to acidify urine and fix WB OD
Term
define inducer
Definition
increases gene expression of P450 metabolizing enzymes which decreases the plasma level of the drug making it less effective and decreasing presence of symptoms
Term
what are 5 examples of inducers
Definition
rifampin, bensopyrine, chronic ethanol, phenytoin, barbituates
Term
define inhibitor
Definition
decrease gene expression for metabolizing P450 enzymes increasing plasma concentration of the drug which increases symptoms
Term
what are 4 examples of inhibitors
Definition
cimetidine, erythromycin, ketonazole, grapefruit
Term
define first order metabolism
Definition
rate of drug metabolism is proportional to concentration of the free drug
constant fraction of drug is metabolized per unit time
Term
define zero order metabolism
Definition
drugs with large doses saturate metabolizing enzymes
constant amount of drug is metabolized per unit time
Term
what are 3 examples of drugs with zero order kinetics
Definition
aspirin, ethanol, phenytoin
Term
what is a maintience dose for, how is it calculated
Definition
adjust rate so input equals rate of loss to keep a steady plasma level

(Cs)(Cl)/(F)
Term
what is loading dose for, how is it calculated
Definition
load initial volume of drug needed

(Cp)(Vd)/(F)
Term
how long does it take to get to steady state, what is it dependent on(2)
Definition
4-5 half lives
depends on half life and steady state is determined by first order kinetics
Term
NRTI: name 3 drugs
Definition
zidovudine
lamivudine
entricitabine
Term
NRTI MOA
Definition
host adds 3P then drug terminates DNA elongation
Term
NRTI side effects (3)
Definition
peripherial neuropathy
lactic acidosis
marrow supression - zidovudine
Term
NTRTI drug name
Definition
tenofovir
Term
NTRTI MOA
Definition
host adds 2P, drug terminates DNA elongation
Term
NNRTI drug name
Definition
enfavirenz
Term
NNRTI side effects
Definition
maculopapular rash
CNS effects - enfavirenz
Term
NNRTI MOA
Definition
binds reverse transcriptase causing inactivation
Term
name a protease inhibitor, what is the MOA
Definition
ritonavir
inhibits protease stopping viral replication
Term
protease inhibitor side effects (5)
Definition
central fat deposition
insulin release
hyperglycemia
P450 inhibitor - increased in infants
Term
how is ritonavir used
Definition
in combination with out PI because it is an extra good P450 inhibitor
Term
name an integrase inhibitor
Definition
raltegravir
Term
integrase inhibitor MOA
Definition
inhibits viral genetic integration into host chromosomes
Term
name three anti-herpes drugs
Definition
acyclovir
gencyclovir
foscarnet
Term
acyclovir MOA
Definition
TK adds 1P, host adds 2P, DNA chain termination
Term
acyclovir side effects (4)
Definition
delerium
tremor
seizure
nephrotoxicity (crystal urea, drink water)
Term
gencyclovir MOA
Definition
TK adds 1P, host adds 2P, DNA chain termination
Term
gencyclovir side effects
Definition
marrow supression
Term
foscarnet MOA
Definition
stops reverse transcriptase and DNA polumerase
Term
fascarnet side effects (2)
Definition
nephrotoxicity
altered Ca and P balance
Term
what two herpes drugs treat CMV
Definition
foscarnet, gencyclovir
Term
name and influenza a and b drug
Definition
oseltamivir
Term
oseltamivir MOA
Definition
neuroaminidase inhibitor that stopps viral budding
Term
name two TB drugs
Definition
isoniazid
rifampin
Term
isoniazid MOA
Definition
stops mycolic acid assembly
Term
isoniazid side effects
Definition
peripherial neuritis (take B6 to fix)
Term
isoniazid clinical use
Definition
only TB
Term
rifampin MOA
Definition
stops RNA polymerase
Term
rifampin side effects (5)
Definition
P450 inhibitor
pseudomembrane colitis
renal failure
anemia
red/orange urine
Term
rifampin clinical use
Definition
broad
Term
which antibiotics should be adjusted with renal dysfunction
Definition
most of them
Term
MOA B-lactams
Definition
inhibit transpeptidation in cross linking
Term
what are the side effects of B-lactams
Definition
hypersensitivity
Term
what are the side effects of imipenem
Definition
seizures with renal dysfunction
Term
how can something become resistant to B-lactams
Definition
alter PBP, product B-lactaminase
Term
how can you avoid B-lactaminase
Definition
clavulamic acid: B lactaminase inhibitor
Term
which penicillin is the most B-lactaminase resistant, what group is it in
Definition
nacifillin (anti-staph)
Term
which cephalosporin is the most B-lactaminase resistant, which group is it in
Definition
cephtriaxone (3 and 4th generation)
Term
vancomycin MOA
Definition
binds d-alanine terminal to inhibit peptidoglycan elongation
Term
vancomycin side effects
Definition
red man syndrome (upper body flushing due to histamin release and infusion too fast)
Term
vancomycin resistance
Definition
altering d-alanine terminal
Term
tetracyclines work on what subunit
Definition
30S
Term
what are two tetracyclines
Definition
tetracycline + docycycline
Term
tetracycline resistance
Definition
unable to bind receptor site
Term
tetracycline side effects
Definition
metals (antacids) cause chelation
concentrations in bone and teeth
phototoxicity
Term
aminoglycosides work on what subunit
Definition
30S
Term
what are two aminoglycosides
Definition
doxycycline and gentamycin
Term
MOA aminoglycosides
Definition
need O2 to get into bacteria (will never work on anaerobes)
Term
aminoglycocide side effects
Definition
nephrotoxicity
ototoxiticy
muscle weakness due to decreased ACh release
Term
macrolides work on what subunit
Definition
50S
Term
what are three macrolides
Definition
erythromycin, azithromycin, clathromycin
Term
MOA macrolides
Definition
inhibit translocation
Term
MOA erythromycin
Definition
bind to motilin receptor increasing GI motility (used in gastroperosis in diabetics)
Term
what drug is an antifolate
Definition
TMP/SMX
Term
normal folate metabolism
Definition
pteridine + PABA use DHPS to make DHF

DNF uses DHFR to make THF
Term
MOA SMX
Definition
inhibit DHPS (dihydrofolate synthase)
Term
MOA TMP
Definition
inhibit dihydrofolate reductase (DHPR)
Term
side effects of SMX
Definition
hypersensitivity, SJS
in G6PDH deficiency get hemolytic anemia
marrow supression because it stops THF causing anemia
phototoxicity
Term
name two folroquinolones
Definition
ciproflaxcin and levoflaxcin
Term
MOA flouroquinolones
Definition
inhibit topoisomerae 2 (DNA gyrase) stopping positive supercoils
Term
flouroquinolone side effects
Definition
tendon and cartiladge: tendinitis, tears

phototoxicity
Term
function of flouroquinolones
Definition
kill all geam negatives
levoflaxcin kills gram positive too (good for atypical pneumonia)
Term
MOA metronidazole
Definition
cannot have O2 present (works on anaerobes only)
Term
side effects metronidazole
Definition
metal taste, disulfram
Term
metronidazole functions
Definition
giardia
entomebia
trichomonas
bacterioides
clostridium
gardnerella
Term
syphilis tx
Definition
pen G
Term
gonorrhea tx
Definition
cephtriaxone
Term
chalmydia tx
Definition
doxycyclin or azithromycin
Term
trichomonas tx
Definition
metronidazole
Term
gradnerella tx
Definition
metronidazole
Term
strep tx
Definition
pen G
if using a cephalosporin: cephalexin
Term
staph tx
Definition
anti-steph penicillin (naficillin)
Term
HA-MRSA tx
Definition
vancomycin
Term
CA-MRSA tx
Definition
TMP/SMX
Term
typical pneumonia tx
Definition
pen G or cephalexin
Term
atypical pneumonia tx
Definition
tetracycline or macrolide
Term
what microbes cause atypical pneumonia
Definition
chalmydia
mycoplasma
legionella
Term
meningitis tx
Definition
cephtriaxone (+ampicillin for listeria)
Term
PJP tx
Definition
TMP/SMX
Term
amphotericin B MOA
Definition
binds ergosterol opening pores killing fungi
Term
amphotericin B use
Definition
serious systemic infection, too toxic for regular use
Term
amphotericin B side effects
Definition
nephrotoxicity
Term
fluconazole and voraconazole MOA
Definition
inhibit 14a-demythelase stopping lenosterol conversion to ergosterol
Term
fluconazole use
Definition
routine fungal infection
less serious fungal infection
anti-fungal (candidia)
Term
voriconazole use
Definition
aspergillus
Term
terbinafine MOA
Definition
stops squaline exopidase stopping squaline conversion to squaline epoxidase
Term
terbinafine use
Definition
dermatophic infection (tinea), oncomycosis (nails)
Term
terbinafine administration
Definition
topical or oral
Term
chloroquine use
Definition
prophylaxis and tx DOC for blood schizonticide (malaria in blood)
Term
primaquine use
Definition
add to chloroquine for p. vivax and p. ovale because they chill in liver (tissue schizonicide)
Term
side effects of primaquine
Definition
in people with G6PDH deficiency causes hemolytic anemia
Term
explain the process of cholinergic activation up until NT release
Definition
1. Uptake of choline via Na cotransport RATE LIMITING
2. Choline acetyl transferase (CAT) and acetylCoA synthesizes acetylcholine
3. Storage of acetylcholine inside vesicle and H+ is effluxed
4. Depolarization: Ca channels open and lets Ca in
5. Ca mediated vesicle fusion: vesicles migrate and fuse to release contents
Term
what are the fates of ACh after release from neuron
Definition
a. Diffuse across synapse and bind to post-synaptic receptor (N or M) or pre-synaptic receptor (M)
b. Bind to pre-synaptic auto receptor for negative feedback
c. Rapidly metabolized by acetylcholinesterase into acetate and choline which is taken back into nerve (Causes short half-life)
Term
explain how the pre-synaptic autoreceptor works
Definition
i. M2 receptor on original nerve
ii. Inhibitory Gi protein causes cAMP to go down and Ca channels close
iii. Stopping release of neurotransmitter
Term
botox: where does it come from, what does it do
Definition
Produced by clostrum botulinium

Gets inside nerve and inhibits vesicles from fusing with membrane

Blocks release of ACh
Term
latrotoxin: where does it come from, what does it do
Definition
Spider venom

Causes flood of ACh to be released
Term
muscarinic receptors: innervated by, NT is
Definition
Cholinergic receptor on end organ

Affinity for ACh and agents that mimic ACh (cholinomimetics)
Term
what does a muscarinic receptor have the highest affinity for
Definition
Highest affinity for muscarine (in poisonous mushrooms)
Term
in one sentence describe the purpose of muscarinic receptors
Definition
Innervate parasympathetic nervous system effects onHeart, smooth muscle, endocrine glands
Term
where is m1 located, what type of receptor
Definition
Gq
brain
Term
how do Gq receptors work
Definition
phospholipase C > PIP2 > IP3 + DAG
Term
where is m2 receptor located
Definition
heart

Auto receptors on pre/post-ganglionic or pre-synaptic cholinergic nerves
Term
what type of receptor is m2, how does it work
Definition
Gi receptor

Heart: decrease K+ conductance

Presynaptic: decreases cAMP
Term
in general, what do M2 receptors do
Definition
Decreases HR and force of contraction (due to decreased K conductance)

Decreases ACh release
Term
where are m3 receptors located, what type of receptor, what do they do
Definition
everywhere but heart and brain

Gq receptor

constrict smooth muscle
Term
where are m4 receptors, what type of receptor
Definition
donno
Gi
Term
where are m5 receptors, what type of receptor
Definition
donno
Gq
Term
what does a muscarinic agonist do
Definition
stimulate muscarinic receptor by mimicing ACh but with longer half life
Term
why do muscarinic receptor agonists have a longer half life
Definition
no acetylcholinesterase issue
they only do M receptor (not n) so fewer side effects and uptake issues
Term
what are the 4 muscarinic agonists and their relative nicotinic effects
Definition
bethanechol - little
carbachol - lots causes SE
methacholine - little
pilocarpine
Term
what does benthanecol work on
Definition
stimulates GI and urinary tract
Term
how is bethanecol administered, why
Definition
oral, because it isnt absorbed well and limits SE
Term
uses of bethanecol
Definition
postop and post partum non-obstructive urinary retention

neurogenic atony of bladder with retention

gastric atony

urinary retention; caused by diabetic lack of GI tone, decreased bladder tone due to drugs (ANTI-PSYCHOTICS) ith anti-muscarinic effects
Term
what is carbachol used for
Definition
not much
Term
what is methacholine used for
Definition
bronchoconstriction - diagnostic for subclinical asthma

methacholine challenge test; asthma pt is more sensitive to methacholine induced bronchoconstriction
Term
what does pilocarpine do
Definition
stimulate salivary secretion
Term
what are the ways pilocarpine is administered, why for each (3)
Definition
IV/IV: it isnt, this increases toxicity
topical: reduce side effects (eye drops)
oral: xerostomia (increased SE)
Term
uses of pilocarpine
Definition
openangle and closed angle glaucoma: increases aq humor drainage and decreased production

xerostoma
Term
what causes xerostomia, what is it
Definition
difficulty swallowing due to head and neck radiation or sjogerns
Term
what is sjogerns and what are the symptoms
Definition
autoimmune disease
decreased secretions: lacrimation, saliva, vaginal
Term
effects of muscarinic agonist on GI tract
Definition
increase tone, constraction, peristalsis, secretions

nausea, belching vomiting, intestinal cramps, defecation
Term
effects of muscarinic agonist on urinary tract
Definition
increase urethral peristalsis
contract detrusor
relax trigone and sphincter
increase voiding pressure
decrease capacity of bladder
Term
effects of muscarinic agonist on cardiovascular system
Definition
decrease HR - neg chronotrophic
decrease conduction at SA/AV - negative domotrophic
decrease contraction force (neg inotrophic)
vasodilation
Term
what is chronotrophic
Definition
HR
Term
what is domotrophic
Definition
conduction at SA/AV nodes
Term
what is iontrophic
Definition
force of contraction
Term
explain how muscarinic agonist cause vasodilation
Definition
Vessels have M3 receptors on endothelial cells WITHOUT nerve attached (no physiological purpose!)

if you could activate them they release NO causing vasodilation (because the receptor is on endothelial cells DIFFERENT CELL TYPE = DIFFERENT RESPONSE)
Term
what is the overall cardiovascular response to the changes muscarinic agonist make
Definition
decreased HR, conduction, force, vasodilation causes decreased BP

sympathetic responds to this increasing BP
Term
what is the effect of muscairinic agonist on secretions, sweat, lungs, eyes
Definition
increase secretions: salivary, lacrimal, digestive, exocrine, tracheobronchial

sweat glands: (sympathetic but have non innervated M3)

bronchoconstriction

miosis and accommodation for near vision

stimulate chemoreceptors on carotid and aortic bodies
Term
side effects of muscarinic agonist
Definition
miosis, bradycardia, bronchoconstriction (avoid in asthma), increased gastric acid (avoid in ulcers), diarrhea, urination

flushing: due to vasodilation increasing blood flow

salivation, lacrimation, sweating (sympathetic!!)
Term
what are the antidotes to musarinic OD
Definition
atropine sulfate - muscarinic antagonist

epinepherine
Term
atrophine sulfate: admninistration, use
Definition
IV/SC
treat toxic reaction of muscarinic agonist
Term
how does epinepherine work
Definition
physiologic antagonist works on different receptor
overcomes cardiovascular and bronchoconstrictor receptors
Term
reversible acetylcholinesterase inhibitor
Definition
breaks down acetylcholinesterase and increases M and N receptor action all over body in parasympathetic, sympathetic, and somatic NS
Term
reversible acetylcholinesterase inhibitor drugs (8)
Definition
physpstigmine
pyridostigmine
neostigmine
edrophonium
ambenomium
donpezil
rivastigmine
galatamine
Term
irreversible acetylcholinesterase inhibitor drugs (6)
Definition
military nerve agents: sarlin nerve gas, soman, tabun

insecticides: parathion, malathion (organophosphates)

lice topical: malathion
Term
acetylcholinesterase inhibitor antidotes (2)
Definition
pralidoxime (PAM)
atropine
Term
cholinergic agonist MOA
Definition
stimulates Nn and Nm receptors
activates sympathetic and parasympathetc NS (mostly parasympathetic)
Term
cholinergic agonist drug
Definition
nicotine
Term
cholinergic antagonist MOA
Definition
binds to cholinergic receptors and stops ACh
stops parasympathetic and muscarinic transmission
Term
what are the two types of cholinergic antagonists and their general function
Definition
ganglionic blockers: show preference for blocking nicotonic of sympathetic and parasympathetic GANGLIA

NMJ blockers: block different impulses to SKELETAL MUSCLE

antimuscarinic and antinicotinic
Term
MOA of antimuscarinic agents
Definition
block M receptors blocking parasympathetic and sympathetic NS mediated by ACh (thats sweating for sympathetic)

no nicotinic receptor activation

competitive agonist - can be out competed

target organ depends on lipid solubility
Term
what are competitive muscarinic agonists / muscarinic antagonist antidotes
Definition
thiostigmine, ACh inhibitor, muscarinic agonist
Term
what strucure of antimuscarinic agents makes it more lipid soluble, what diseases is this required for
Definition
qaternary N is more polar and less likley to penetrate BBB or cornea so needs to have tertiary amine

parkinsons and opthalmology needs lipid soluble (gut and bronchi dont)
Term
6 antimuscarinic drugs
Definition
tropicaamide
scopolamide
bnstropine
atropine
tolterodine
oxybutynin
Term
physpstigmine distribution
Definition
tertiary amine: lipid soluble
Term
physpstigmine use
Definition
antidote for muscarinic blockers (anticholinergic toxicity) like atropine

reversible acetylcholinesterase inhibitor
Term
physpstigmine SE
Definition
seizure
Term
pyridostigmine/neostigmine MOA
Definition
quarinary amine (positive) water soluble

only used for Nm at NMJ

reversible acetylcholinesterase inhibitor increases ACh can outcompete binding of antibodies in myasthenia gravis
Term
use pyridostigmine/neostigmine
Definition
myasthenia gravis: autoimmune disease with antibodies to Nm causes weakness mostly in facial region, the more they excert the weaker they get, symptoms improve with rest

reversal of non-depolarizing blocking agents like tubocurarine
Term
edrophonium use
Definition
IV short acting 10-20min reversible acetylcholinesterase inhibitor to diagnose myasthemia gravis
if muscle activity returns then they have it
Term
ambenomium use
Definition
back up drug for myasthenia gravis if they cannot tolerate bromides
Term
donepezil/rivastigmine/galantamine distribution
Definition
tertiary amines: enter CNS
Term
donepezil/rivastigmine/galantamine use
Definition
alzheimers (mostly doneprezil)

neurodegenerative disorder with loss of memory and cognative function
pt looses cholinergic neurons in cortex (mynert's nuclei)

increasing ACh is many strategy for tx
Term
parathion/malathion: MOA, SE, use
Definition
insecticides, malathion is for lice

prodrugs, activated by P450

active form is hydrolyzed by plasma carbxylesterases which causes death in insects but sucks in us only in high doses
Term
SE acetylcholinesterase inhibitors and the receptor involved
Definition
diarrhea - M3
urination - M3
miosis - M3
bronchoconstriction - M3
bradycardia - M2
excitation of skeletal M - Nm
excitation of CNS - M1, Nn
lacrimation - M3
salivation - M3
sweating - M3 - sympathetic!
Term
what SE of acetylcholinesterase inhibitors are deatly
Definition
excitation of skeletal muscle / CNS

causes paralysis of diaphragm
Term
pralidoxime MOA
Definition
breaks bone between irreversible acetylcholinesterase inhibitor and ACh, regenerating the enzyme so it can work again
Term
what is chemical aging, why is it a problem
Definition
change in structure of irreversible acetylcholinesterase inhibitor makes it so pralodoxime can no longer remove the drug

due to hydrolysis reaction pulling alkyl grop off

rate depends on agent - can be minutes

releases enzyme so it breaks down ACh and stops effects at skeletal M
Term
atropine MOA
Definition
inhibits everything in acetylcholinesterase SE except excitation of heart
Term
nicotinic receptors: MOA, locations, types
Definition
binds ACh and nicotine
nitotine initially stimulates then blocks receptor

locations: CNS, adrenal medulla, autonomic ganglia, NMJ

types: autonomic ganglia Nn, skeletal muscle Nm
Term
cholinergic agonist
Definition
stimulates Nn and Nm receptors
stimulating parasympathetic and sympathetic (vessels, and sweating)
Term
SE/MOA high doses of nicotine
Definition
desensitization of receptors at organs leads to inability to cause parasympathetic response and thus causes sympathetic response
Term
what causes problems in cigarette smoke, why
Definition
benzopyrine P450 inducer
Term
nicotine distribution
Definition
crosses placenta
Term
uses of nicotine drug
Definition
smokinig cesation
Term
MOA cholinergic antagonist
Definition
blinds to cholinergic receptor stopping ACh stopping parasympathetic and muscarinic transmission
Term
types of cholinergic antagonists
Definition
ganglionic blockers
NMJ blockers
Term
where does atropine come from
Definition
belladone aklaloid, gymsin weed
Term
MOA atropine
Definition
blocks receptors in PNS and CNS
Term
distribution atropine
Definition
tertiary amine: lipid soluble, enters CNS
Term
half life atropine
Definition
short 4-8h
unless in eye 3-5d
Term
CNS effects of antimuscarinic
Definition
sedation, anti-motion sickness, anti-parkinsons, amnesia, delirium
Term
M1 effecs of antimuscarinic
Definition
GI relaxation, slow peristalsis

exocrine: reduced salivation, lacrimation, sweating, gastric secetion
Term
M2 effects of antimuscarinic
Definition
heart: initial bradycardia then tachycardia decreases in AV conduction

inhibit presynaptic M2 (inhibit inhibitory) and pathway becomes stimulate releasing more ACh -> initial bradycardia

M2 acts on heart a little more slowly and blocks it -> tachycardia
Term
effects of antimuscarinic on M3
Definition
eye: cycloplegia
bronchi: dilation
GI: relaxation, slow peristalsis
GU: relax bladder wall, urinary retention
vessesl: block muscarinic causing vasodilation (only when muscarinic agonist present or else does nothing)
exocrine: reduced salivation, lacrimation, sweating, gastric secretion
Term
SE of antimuscarinic - hot as a pistol
Definition
atropine fever: blocks thermoregulatory mechanisms causing hyperthermia (lethal in infants)
Term
SE of antimuscarinic - dry as a bone
Definition
decreased sweating, lacrimation, salivation, urination, pooing
Term
SE of antimuscarinic - blind as a bat
Definition
blurred bision, acute angle closure glaucome (esp elderly)
Term
SE of antimuscarinic - mad as a hatter
Definition
sedation, amnesia, delirium, hallucinations
Term
SE of antimuscarinic - red as a beet
Definition
atropine flush: dilation of cutaneous vessels in arms, head, neck, trunk

diagnostic for OD
Term
use of tropicaamide
Definition
dilate pupil (mydriasis) for eye exam
paralyze accomodation
Term
use of scopolamide
Definition
motion sickness - block receptors in vestibular apparatus that induce nausea and vomiting
Term
use benztropine
Definition
adjunct to L DOPA for parkinsonism (loss of dopaminergic neurons decreases dopamine and increases ACh)
Term
what drug can help with peptic ulcer disease
Definition
antimuscarinic
Term
what drug can be used for bronchodilation in asthma and COPD
Definition
antimuscarinic
Term
use of tolerodine, oxybutynin,
Definition
reduce urgency in cystitis
reduce bladder spasm following urologic surgery
urinary incontence
Term
MOA ganglionic blocker
Definition
block Nn receptor on autonomic ganglia and adrenal medulla
blocks dominant system (usually parasympathetic)
Term
ganglionic blocker drug and its use and MOA
Definition
mecamylamine
HTN back up drug
decrease sympathetic tone and vasodilates
Term
structure of neuromuscular blockers
Definition
similar to ACh
have 2 quatenary N, unable to get in CNS
Term
uses of neuromuscular blockers
Definition
surgical relaxation
trachea intubation
control ventilation
control motor acrivity in seizure (not tx it)
Term
what category of drugs are best at helping with trachea intubation
Definition
depolarizing neuromuscular blockers
Term
MOA non-depolarizing neuromuscular blockers
Definition
competitive blocker of ACh and Nm receptor at a subunit

can be outcompeted by acetylcholinesterase inhibitors
Term
what is the antidote to non-depolarizing neuromuscular blocker
Definition
acetylcholinesterase inhibitors neostigmine and pyridostigmine (because they work in peripherary)
Term
side effect of all non-depolarizing neuromuscular blockers
Definition
motor weakness: small muscles first then large, large first to recover
diaphragm is last
Term
what are the short duration neuromuscular blockers, how long
Definition
10 min
articurium
mivacurium
Term
what are the intermediate duration neuromuscular blockers, how long
Definition
25 min
cisatracurium
rochuronium
Term
what are the long duration neuromuscular blockers, how lonw
Definition
30 min
pancuronium
Term
MOA articurium
Definition
spontaneously inactivate to metabolite laudanosine (causes seizures, can be used in liver and kidney dysfynction)
Term
MOA cisatracurium
Definition
same as articurium but when spontaneously inactivated does not produce as much laudanosine so less seizures occur
Term
mivacurium SE, duration, onset of action
Definition
shortest DURATION
short onset of action

causes histamine release > hypotension and reflex tachycardia
Term
rocuronium onset time
Definition
shortest ONSET 1-2 min
Term
pancuronium SE, why
Definition
blocks M receptors and causes tachycardia
Term
what drug is a depolarizing neuromuscular blocker, what is its structure
Definition
succinylcholine - 1 ACh together
Term
MOA succinylcholine
Definition
phase one: simulates ACh and causes muscle contraction

phase two: overstimulation causes de-sensitization of the receptor so membrane repolarizes but it cannot easily repolarize
Term
what is the antidote for succinylcholine
Definition
there isnt one. acetylcholinesterase innhibitor dosent work.

it increases ACh in the phase one which just further mimics the drug

it increases ACh in phase two but at that point it dosent matter how much ACh there is, the receptor dosent work
Term
kinetics and distribution succinylcholine
Definition
short acting, works fast
less lipid soluble, cannot get into CNS
Term
succinylcholine: how long does it take to work, wat are the next two stages of timing, how long does it take to stop, why does it stop
Definition
30s- general anasthesia
90s- arm, back, leg muscle flaccid
more sec- repsiratory muscle flaccid
10 min- hydrolyzed in plasma and liver cholinesterase
Term
side effects of depolarizing neuromuscular blockers, why
Definition
can stimulate M and Nn too causing bradycardia

hyperkalemia in burn pt, head injury, trauma bc Na rushes in and K out at nicotinic receptors which are being fired

muscle pain due to initial contraction

increased risk if inhaled anasthetic
Term
interactions with depolarizing neuromuscular blockers, effect, tx
Definition
inhaled anasthetics: malignant hyperthermia (rare, fatal). due to abnormal release of Ca from skeletal M

tx dantrolene
Term
MOA dantrolene
Definition
blocks ryanoide receptor (RyR1) on SER blocking Ca release decreasing ability for contraction

decreased muscle contraction decreases body temo
Term
what tx malignant hyperthermia, how is the condition started
Definition
dantrolene
genetic alteration in RyR1 gene + succinylcholine or anesthetics --> prolonged Ca release --> muscle contraction, lactic acid, increased body temp
Term
MOA botulinium toxin
Definition
blocks release of ACh
Term
uses of botulinium toxin
Definition
local facial injection
spasticity - cerebral palsy
strabismus
blepharospasm
hyperhidrosis
migraines
Term
use of CNS skeletal relaxants
Definition
spasticity: increase in tonic stretch reflexes. caused by spinal injury, cerebral palsy, MS, stroke

often involves abnormal function of bladder and bowel
Term
how are BDZ dosed for their usages
Definition
low: anxiety
med: slwwp
high: anasthetic
Term
MOA diazepam
Definition
activate GABAa which increases frequency of Ca channel opening decreasing neuron activity
Term
SE diazepam
Definition
sedating
Term
MOA baclofen
Definition
activate GABAb opening K channel causing hyperpolarization and inhibiting neuron activity

prevent post synaptic propogation of AP
Term
SE baclofen
Definition
less sedating than diazepam
Term
MOA tyranidine
Definition
a2 agonist: prevents NT release
(glutamate presynaptic, AP post synaptic)

classif autoreceptor mecanism
Term
SE tryanidine
Definition
fewer effects than clonidine and methyldopa (a2 agonist for HTN)

hypotension and drowsiness due to decreased NE release
Term
rulusole MOA
Definition
Na channel blocker
Term
rulesole use
Definition
slow progression of amytrophic lateral sclerosis (ALS) / Lou Gherig's
Term
what are the CNS muscle relaxants
Definition
riluzole
tyanadine
baclofen
diazepam
Term
what does the CNS include
Definition
brain and spinal cord
Term
what are the components of the peripherial nervous system
Definition
afferent: nerves going to CNS
efferent: nerves leaving CNS
Term
what is the function of afferent nerves
Definition
carry information to CNS for processing
autonomic nervous system reflexes: baroreceptor, emotional
Term
compare preganglionic and poste ganglinic neuron cell bodies and axons
Definition
pre: cell body in CNS, non myelinated

post: cell body in ganglia, non-myelinated, terminates in effector organ
Term
function and nerve lay out of somatic NS
Definition
vountary control of sksletal muscle
one neuron, no ganglia
Term
autonomic NS function
Definition
involuntary control of heart, vessels visceral organs, glands
Term
what are the three types of input into the autonomic NS, explain where each comes from or is processed
Definition
afferent sign: travels to integrating center in hpothalamus, medulla, spinal cord

reflexes: dont involve processing (baroreceptor increases symp and decreases para to heart)

emotions; stimulate sympathetic and parasympathetic
Term
where do sympathetic preganglionic fibers come from, where do they go
Definition
T1-2, L1-5 synapse in sympathetic chain, post ganglionic extend to viscera
Term
explain the wiring of the adrenal medulla
Definition
recieves sympathetic preganglionic fiber that does not synapse in sympathetic chain and has no postganglionic fiber

instead releases hormones (N/NE) into the blood
Term
general function of sympathetic NS
Definition
continously active to maintain tone
functions as a unit
not essential for life
fight or flight
Term
sympathetic effect on: heart, energy, blood, pupil, lungs, bladder, GU, salivation, GI, muscle
Definition
increases HR, BP
energy mobilization
blood to skin and organs decreased
dilation of skeletal muscle vessels
dilation of pupil
bronchi constriction
bronchiole dilation
detrusor relaxation
construction of trigone and sphinctor
thick salivation
decrease in gastric motility
uterus relaxation
ejaculation
Term
where do parasympathetic NS fibers come from, where do they go
Definition
CN III, VII, IX, X, S2-4
synapse at ganglia near effector organ
Term
general functions of parasympathetic NS
Definition
essential for life
effects specific effector organ
rest and digest
Term
effect of parasympathetic on: eye, lung, bladder, GU, salivation, heart, GI
Definition
constrict iris constricts pupil
constriction of ciliary m. for near vision
constriction of bronchioles
contraction of detrusor
relaxing trigone and sphinctor
erection
watery salivation
decreased HR, CO
GI motility
Term
what are the effects when an organ has parasympathetic and sympathetic innervation
Definition
parasympathetic predominates
sympathetic only predominates if it is the only innervator
Term
where is sympathetic the only innervator
Definition
blood vessels, adrenal medulla, pilomotor muscles, sweat glands
Term
define cholinergic
Definition
ACh releasing NT binds to cholinergic receptor (Nm, Nn, M)
Term
define adrenergic
Definition
NE releasing and NT binds to adrenergic receptor (a and B)
Term
what are the two types of parasympathetic receptor/NT combinations, where are they located
Definition
preganglionic/postganglionic synapse: ACh/Nn

postganglionic/cardiac, smooth muscle, glands synapse: ACh/M
Term
what are the 4 types of sympathetic receptor/NT combinations, where are they located
Definition
preganglionic/postganglionic: ACh/Nn

postganglionic/sweat gland synapse: ACh/M

postganglionic/cardiac M, smooth M, gland synapse: NE/a or B

postganglionic / renal vascular smooth muscle synapse: D/D1 (dopamine is precursor for NE, D1 is main periphery dopamine receptor)
Term
what is the neuromumoral receptor/NT combination, where is it located
Definition
preganglionic/adrenal medulla synapse: ACh/Nm causes release of E and NE into blood
Term
what is the somatic receptor/NT synapse, where is it located
Definition
somatic/skeletal muscle synapse: ACh/Nm
Term
what are the three categories of chemical signalers
Definition
local
hormones
neurotransmitters
Term
local signalers: 2 examples, down side
Definition
rapidly destoried or removad
histamine, prostaglandin
Term
defne hormone
Definition
travel in blood to effect broadly distributed target cells
Term
define neurotransmitter
Definition
communication between neurons acts on specific cellular receptor
Term
3 examples of NT
Definition
ACh, NE, E
Term
where is ACh released
Definition
cholinergic neurons in sympathetic, parasympathetic, and adrenal medulla
iin all NMJ
Term
where is NE/E released
Definition
adrenergic neurons, nerve transmission
E from adrenal medulla into blood and activates non-adrenergic receptors
Term
octerotide: duration, type of drug, function, use
Definition
long acting
somatostatin analog
inhibits GH, glucagon, insulin, gastrin

acromeagly, carcinoid
Term
desmopressin: type of drug, MOA, use
Definition
ADH analog
V2 agonist

central diabetes insipidus (ADH replacement)
Term
tolvaptam: MOA, use
Definition
V2 blocker in CD

SIADH
Term
what drugs are used for insulin replacement therapy, how
Definition
lispro: mealtime
glargine: basal
Term
glipizide: MOA, SE
Definition
K channel blocker leads to increased insulin release from B cells

SE: hypoglycemia, weight gain
Term
metformin: MOA, SE
Definition
inhibit gluconeogenesis in liver

no hypoglycemia or weight gain
SE: rare lactic acidosis in pt with renal dysfunction because drug accumulates
Term
pioglutazone: MOA, SE
Definition
insulin sensitizer: stimulate PPARy receptors which increase number of insulin receptors on many organs (like skeletal M)

edema, weight gain
Term
what diabetes drugs target pancreas, MOA
Definition
GLP-1 is an incretin that causes insulin release
exenatide is a GLP-1 analog
incretins are metabolized to inactive by DPP-4
sitaglipdin is a DPP-4 antagonist
Term
levothyroxine: MOA, use
Definition
T4 agonist needs to be converted to T3

hypothyroid
Term
methinizaole: MOA, SE, use
Definition
blocks all the steps in thyroid hormone synthesis

iodide conversion to iodine via thyroid peroxidase
peroxidase conversion to MIT/DIT making T3/4

SE: agranulocytosis

TX: hyperthyroid
Term
I131: MOA, use, SE
Definition
thyroid sucks it up and B radiation destories thyroid

TX hyperthyroid

not for pregnant and kids
Term
explain the glucocordicoud/mineral corticoid activity of the three steroids
Definition
hydrocortizone: 1:1
dexamethasone: 1:0
flucortizone: 10:250
Term
use of hydrocortizone
Definition
adrenal insufficiency
congenital adrenal hypothyroid
after cushing surgery
Term
steroid SE
Definition
aldosterone: Na/water retention, edema, increased BP

glucacorticoid: cushing like, ulcers
Term
use of conjugated equine estrogen
Definition
hormone replacement
Term
use of ethadol estradiol
Definition
oral contraceptive
Term
use hydroxy progesterone
Definition
IM contraceptive
Term
use nerethindrome
Definition
oral contracepitive
hormone replacement
Term
mifperistone: MOA, use
Definition
progesterone receptor blocker
abortion (when added with prostaglandins)
Term
finastride: MOA, use
Definition
5a reductase inhibitor stops testosterone conversion to DHT

BPH, balding
Term
when can't you use finastride
Definition
a1 blocker and a1A blocker both treat BPH
if pt needs to lower BP then don;t choose finasteride
Term
flutamide: MOA, use
Definition
androgen receptor blocker (used with GNRH agonist continous administration(

prostate cancer
Term
slidenafil: MOA, use
Definition
PDE3 inhibitor increases cAMP: relaxes, vasodilates, increases blood flow

erectile dysfunction
Term
SE slidenafil
Definition
dont take with nitrates or a blockers (which are also vasodilators and cause orthostatic hypotension)

hypotension

PDE6 inhibition causes blue green color blidness
Term
Ca gluconate: use
Definition
hypocalcemia (tetany, M spasms)
Term
calcitrol: MOA, use
Definition
1,25-dihydroxy vitamin D in active form

rickets, osteomalacia, osteoperosis
Term
alendronate: MOA, use, SE
Definition
decrease bone reabsorption

TX: osteoperosis DOC, pagets disease

SE: esophageal irritation (stay upright after taking)
Term
raloxifene: MOA, SE, TX
Definition
selective estrogen receptor modulator, agonist on bone, antagonist on breast and uterus

antagonist at uterus DOES NOT give increased risk of endometrial cancer (like tamoxifin)

TX: osteoperosis, breast cancer
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