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
|
|
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
|
|
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
|
|
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
|
Definition
patients are secretative, hard to diagnosed
often have eczema, chapped skin
compulsive hand washing or teeth brushing |
|
|
Term
|
Definition
|
|
Term
| what anxiety drug can be used in those with substance abuse problems |
|
Definition
|
|
Term
|
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
|
|
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
|
|
Term
|
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
|
Definition
|
|
Term
|
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
|
|
Term
| what are two SSRI are for anxiety |
|
Definition
|
|
Term
|
Definition
inhibit re-uptake of serotonin at transporter
blocking removal increases concentration at synaptic cleft |
|
|
Term
|
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
|
Definition
|
|
Term
| SSRI metabolizm and excretion |
|
Definition
metabolized in liver
excreted in feces and urine |
|
|
Term
|
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
|
Definition
venlafaxine
duloxetine
desvenlafaxine |
|
|
Term
|
Definition
| block serotonin and NE re-uptake transporters |
|
|
Term
|
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
|
Definition
| blocks pre-synaptic autoreceptors for NE and 5HT and increases NE and 5HT at synapse |
|
|
Term
| in who is depression most common |
|
Definition
|
|
Term
| define unipolar depression |
|
Definition
|
|
Term
| what is the most common form of depression |
|
Definition
|
|
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
|
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
|
|
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
|
|
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
|
Definition
depression
chronic anxiety
chronic panic
SAD
PTSD |
|
|
Term
| uses of piperazine derivatives |
|
Definition
|
|
Term
| side effects of Mirtazapine |
|
Definition
sedation
1% incidence of agranulocytosis |
|
|
Term
|
Definition
chronic anxiety
depression
PTSD |
|
|
Term
|
Definition
| inhibit serotonin reuptake (less than SSRI) |
|
|
Term
|
Definition
little anticholinergic, hypotension, and CV effects
more safe than TCA |
|
|
Term
|
Definition
|
|
Term
|
Definition
| inhibit dopamine and NE reuptake |
|
|
Term
|
Definition
| stimulating, dont take at bed time |
|
|
Term
|
Definition
|
|
Term
| what are the atypical anti-depressants |
|
Definition
bupropion
trazodone
mirtazapine |
|
|
Term
| 3 tricyclic antidepressants |
|
Definition
imipramine
amitripryline
clomipramine |
|
|
Term
|
Definition
| block NA and serotonin reuptake transporter on nerve |
|
|
Term
|
Definition
depression
chronic anxiety
bedwetting - imipramine
chronic panic
PTSD |
|
|
Term
|
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
|
Definition
tranylcypromine
phenelzine |
|
|
Term
|
Definition
| mitochondria enzymes that break down dopamine and serotonin in liver and brain |
|
|
Term
| what are the types of MAO, where are they |
|
Definition
|
|
Term
|
Definition
| suicide inhibiton of MAO increases NT in cleft |
|
|
Term
|
Definition
SSRI
trazodone
venlafaxine
warfarin
OTC decongestants
tryamine
cause serotonin syndrom |
|
|
Term
| signs of serotoniin syndrome |
|
Definition
|
|
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
|
Definition
|
|
Term
| 5 drugs used for manic depression |
|
Definition
lithium salts
carbamazepine - anticonvulsant
valproic acid - anticonvulsant
gabapentin - anticonvulsant, neurotic pain relief
risperidone |
|
|
Term
|
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
|
Definition
| idiopathic, shows in teens |
|
|
Term
| what are schizophrenia drugs called on the street, man |
|
Definition
neuroleptic agents
major tranquilizers |
|
|
Term
|
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
|
|
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
|
|
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
|
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
|
Definition
| not first line, last choice |
|
|
Term
|
Definition
clozapine analog
high affinity 5HT2
medium affinity D2 |
|
|
Term
|
Definition
stroke in elderly with dementia
hyperglycemia and diabetes
low extra-pyramid side effects
minimal sedation
increased QT (cannot use CVD) |
|
|
Term
|
Definition
tx negative symptoms of schizophrenia well
first line therapy |
|
|
Term
|
Definition
clozapine analog
high 5HT2 affinity
intermediate D2 affinity |
|
|
Term
|
Definition
stroke in elderly with dementia
hyperclycemia and diebetes
low extra-pyramid effects
minimal sedation |
|
|
Term
|
Definition
lessen symptoms of tardive dyskinesia
first line anti-psychotic
tx negative symptoms of schizophrenia well |
|
|
Term
|
Definition
clozapineanalog
high affinity 5HT2
intermediate D2 affinity |
|
|
Term
|
Definition
stroke in elderly with dementia
hyperglycemia and dementia
low extra-pyrmiad effect
minimal sedation |
|
|
Term
|
Definition
| tx negative symptoms of schizophrenia well |
|
|
Term
|
Definition
active metabolite od risperidone
high affinity 5HT2
intermediate D2 affinity |
|
|
Term
|
Definition
|
|
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
|
Definition
first line therapy
tx negative schizophrenia symptoms well |
|
|
Term
|
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
|
Definition
| stroke in elderly with dementia |
|
|
Term
|
Definition
anti-psychotic
bipolar disorder
major depression |
|
|
Term
|
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
|
Definition
| cannot initiate or maintain sleep (symptom not disease) |
|
|
Term
|
Definition
|
|
Term
| define circadian rhythm alteration |
|
Definition
| disturbance in sleep wake cycle (jet lag) |
|
|
Term
|
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
|
|
Term
|
Definition
| peanecthetic and intraoperative medication (anterograde amnesia) |
|
|
Term
|
Definition
reoccuring insomnia
initiating sleep |
|
|
Term
| use of intermediate BDZ for sleep |
|
Definition
|
|
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
|
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
|
Definition
binds to BDZ receptor at GABA-Cl channel causing hyperpolarization
does not affect different stages of sleep like BDZ or barbituiates |
|
|
Term
|
Definition
binds to BDZ receptor at GABA-Cl channel causing hyperpolarization
does not affect different stages of sleep like BDZ or barbituiates |
|
|
Term
|
Definition
melatonin receptor agonist
binds mT1 and MT2 receptors for melatonin |
|
|
Term
| what type of drug is chloral hydrate |
|
Definition
|
|
Term
|
Definition
| unknown activate metabolite trichloroethanol |
|
|
Term
|
Definition
minimal rebound insomnia and tolerance
sleep walking/activities, amnesia (increases with alcohol) |
|
|
Term
|
Definition
| minimal rebound insomnia and tolerance |
|
|
Term
|
Definition
|
|
Term
|
Definition
NO anoxiolytic, muscle relaxant, amnesic, or abuse potential
do not consume alcohol
decreased testosterone |
|
|
Term
|
Definition
sleep longer
jet lag
long term administration |
|
|
Term
|
Definition
sleep longer
long term use |
|
|
Term
|
Definition
difficulty initiating sleep
good for elderly |
|
|
Term
|
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
|
|
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
|
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
|
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
|
|
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
|
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
|
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
|
Definition
zidovudine
lamivudine
entricitabine |
|
|
Term
|
Definition
| host adds 3P then drug terminates DNA elongation |
|
|
Term
|
Definition
peripherial neuropathy
lactic acidosis
marrow supression - zidovudine |
|
|
Term
|
Definition
|
|
Term
|
Definition
| host adds 2P, drug terminates DNA elongation |
|
|
Term
|
Definition
|
|
Term
|
Definition
maculopapular rash
CNS effects - enfavirenz |
|
|
Term
|
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
|
Definition
| in combination with out PI because it is an extra good P450 inhibitor |
|
|
Term
| name an integrase inhibitor |
|
Definition
|
|
Term
|
Definition
| inhibits viral genetic integration into host chromosomes |
|
|
Term
| name three anti-herpes drugs |
|
Definition
acyclovir
gencyclovir
foscarnet |
|
|
Term
|
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
|
Definition
| TK adds 1P, host adds 2P, DNA chain termination |
|
|
Term
|
Definition
|
|
Term
|
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
|
|
Term
| name and influenza a and b drug |
|
Definition
|
|
Term
|
Definition
| neuroaminidase inhibitor that stopps viral budding |
|
|
Term
|
Definition
|
|
Term
|
Definition
| stops mycolic acid assembly |
|
|
Term
|
Definition
| peripherial neuritis (take B6 to fix) |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| rifampin side effects (5) |
|
Definition
P450 inhibitor
pseudomembrane colitis
renal failure
anemia
red/orange urine |
|
|
Term
|
Definition
|
|
Term
| which antibiotics should be adjusted with renal dysfunction |
|
Definition
|
|
Term
|
Definition
| inhibit transpeptidation in cross linking |
|
|
Term
| what are the side effects of B-lactams |
|
Definition
|
|
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
|
|
Term
| which cephalosporin is the most B-lactaminase resistant, which group is it in |
|
Definition
| cephtriaxone (3 and 4th generation) |
|
|
Term
|
Definition
| binds d-alanine terminal to inhibit peptidoglycan elongation |
|
|
Term
|
Definition
| red man syndrome (upper body flushing due to histamin release and infusion too fast) |
|
|
Term
|
Definition
| altering d-alanine terminal |
|
|
Term
| tetracyclines work on what subunit |
|
Definition
|
|
Term
| what are two tetracyclines |
|
Definition
| tetracycline + docycycline |
|
|
Term
|
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
|
|
Term
| what are two aminoglycosides |
|
Definition
| doxycycline and gentamycin |
|
|
Term
|
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
|
|
Term
| what are three macrolides |
|
Definition
| erythromycin, azithromycin, clathromycin |
|
|
Term
|
Definition
|
|
Term
|
Definition
| bind to motilin receptor increasing GI motility (used in gastroperosis in diabetics) |
|
|
Term
| what drug is an antifolate |
|
Definition
|
|
Term
|
Definition
pteridine + PABA use DHPS to make DHF
DNF uses DHFR to make THF |
|
|
Term
|
Definition
| inhibit DHPS (dihydrofolate synthase) |
|
|
Term
|
Definition
| inhibit dihydrofolate reductase (DHPR) |
|
|
Term
|
Definition
hypersensitivity, SJS
in G6PDH deficiency get hemolytic anemia
marrow supression because it stops THF causing anemia
phototoxicity |
|
|
Term
|
Definition
| ciproflaxcin and levoflaxcin |
|
|
Term
|
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
|
Definition
| cannot have O2 present (works on anaerobes only) |
|
|
Term
| side effects metronidazole |
|
Definition
|
|
Term
|
Definition
giardia
entomebia
trichomonas
bacterioides
clostridium
gardnerella |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| doxycyclin or azithromycin |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
pen G
if using a cephalosporin: cephalexin |
|
|
Term
|
Definition
| anti-steph penicillin (naficillin) |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| tetracycline or macrolide |
|
|
Term
| what microbes cause atypical pneumonia |
|
Definition
chalmydia
mycoplasma
legionella |
|
|
Term
|
Definition
| cephtriaxone (+ampicillin for listeria) |
|
|
Term
|
Definition
|
|
Term
|
Definition
| binds ergosterol opening pores killing fungi |
|
|
Term
|
Definition
| serious systemic infection, too toxic for regular use |
|
|
Term
| amphotericin B side effects |
|
Definition
|
|
Term
| fluconazole and voraconazole MOA |
|
Definition
| inhibit 14a-demythelase stopping lenosterol conversion to ergosterol |
|
|
Term
|
Definition
routine fungal infection
less serious fungal infection
anti-fungal (candidia) |
|
|
Term
|
Definition
|
|
Term
|
Definition
| stops squaline exopidase stopping squaline conversion to squaline epoxidase |
|
|
Term
|
Definition
| dermatophic infection (tinea), oncomycosis (nails) |
|
|
Term
| terbinafine administration |
|
Definition
|
|
Term
|
Definition
| prophylaxis and tx DOC for blood schizonticide (malaria in blood) |
|
|
Term
|
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
|
|
Term
|
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
|
|
Term
| where are m5 receptors, what type of receptor |
|
Definition
|
|
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
|
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
|
|
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
|
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
|
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
|
Definition
|
|
Term
|
Definition
| conduction at SA/AV nodes |
|
|
Term
|
Definition
|
|
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
|
Definition
stimulates Nn and Nm receptors
activates sympathetic and parasympathetc NS (mostly parasympathetic) |
|
|
Term
|
Definition
|
|
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
|
Definition
tropicaamide
scopolamide
bnstropine
atropine
tolterodine
oxybutynin |
|
|
Term
| physpstigmine distribution |
|
Definition
| tertiary amine: lipid soluble |
|
|
Term
|
Definition
antidote for muscarinic blockers (anticholinergic toxicity) like atropine
reversible acetylcholinesterase inhibitor |
|
|
Term
|
Definition
|
|
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
|
Definition
IV short acting 10-20min reversible acetylcholinesterase inhibitor to diagnose myasthemia gravis
if muscle activity returns then they have it |
|
|
Term
|
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
|
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
|
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
|
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
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
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
|
Definition
| blocks receptors in PNS and CNS |
|
|
Term
|
Definition
| tertiary amine: lipid soluble, enters CNS |
|
|
Term
|
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
|
Definition
dilate pupil (mydriasis) for eye exam
paralyze accomodation |
|
|
Term
|
Definition
| motion sickness - block receptors in vestibular apparatus that induce nausea and vomiting |
|
|
Term
|
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
|
|
Term
| what drug can be used for bronchodilation in asthma and COPD |
|
Definition
|
|
Term
| use of tolerodine, oxybutynin, |
|
Definition
reduce urgency in cystitis
reduce bladder spasm following urologic surgery
urinary incontence |
|
|
Term
|
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
|
|
Term
|
Definition
| spontaneously inactivate to metabolite laudanosine (causes seizures, can be used in liver and kidney dysfynction) |
|
|
Term
|
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
|
Definition
|
|
Term
|
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
|
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
|
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
|
Definition
|
|
Term
|
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
|
Definition
| activate GABAa which increases frequency of Ca channel opening decreasing neuron activity |
|
|
Term
|
Definition
|
|
Term
|
Definition
activate GABAb opening K channel causing hyperpolarization and inhibiting neuron activity
prevent post synaptic propogation of AP |
|
|
Term
|
Definition
| less sedating than diazepam |
|
|
Term
|
Definition
a2 agonist: prevents NT release
(glutamate presynaptic, AP post synaptic)
classif autoreceptor mecanism |
|
|
Term
|
Definition
fewer effects than clonidine and methyldopa (a2 agonist for HTN)
hypotension and drowsiness due to decreased NE release |
|
|
Term
|
Definition
|
|
Term
|
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
|
|
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
|
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
|
Definition
| ACh releasing NT binds to cholinergic receptor (Nm, Nn, M) |
|
|
Term
|
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
|
Definition
| travel in blood to effect broadly distributed target cells |
|
|
Term
|
Definition
| communication between neurons acts on specific cellular receptor |
|
|
Term
|
Definition
|
|
Term
|
Definition
cholinergic neurons in sympathetic, parasympathetic, and adrenal medulla
iin all NMJ |
|
|
Term
|
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
|
Definition
|
|
Term
| what drugs are used for insulin replacement therapy, how |
|
Definition
lispro: mealtime
glargine: basal |
|
|
Term
|
Definition
K channel blocker leads to increased insulin release from B cells
SE: hypoglycemia, weight gain |
|
|
Term
|
Definition
inhibit gluconeogenesis in liver
no hypoglycemia or weight gain
SE: rare lactic acidosis in pt with renal dysfunction because drug accumulates |
|
|
Term
|
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
|
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
|
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
|
Definition
adrenal insufficiency
congenital adrenal hypothyroid
after cushing surgery |
|
|
Term
|
Definition
aldosterone: Na/water retention, edema, increased BP
glucacorticoid: cushing like, ulcers |
|
|
Term
| use of conjugated equine estrogen |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
oral contracepitive
hormone replacement |
|
|
Term
|
Definition
progesterone receptor blocker
abortion (when added with prostaglandins) |
|
|
Term
|
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
|
Definition
androgen receptor blocker (used with GNRH agonist continous administration(
prostate cancer |
|
|
Term
|
Definition
PDE3 inhibitor increases cAMP: relaxes, vasodilates, increases blood flow
erectile dysfunction |
|
|
Term
|
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
|
Definition
| hypocalcemia (tetany, M spasms) |
|
|
Term
|
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
|
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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|
