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, |
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Definition
reduce urgency in cystitis reduce bladder spasm following urologic surgery urinary incontence |
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Term
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Definition
block Nn receptor on autonomic ganglia and adrenal medulla blocks dominant system (usually parasympathetic) |
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Term
ganglionic blocker drug and its use and MOA |
|
Definition
mecamylamine HTN back up drug decrease sympathetic tone and vasodilates |
|
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Term
structure of neuromuscular blockers |
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Definition
similar to ACh have 2 quatenary N, unable to get in CNS |
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Term
uses of neuromuscular blockers |
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Definition
surgical relaxation trachea intubation control ventilation control motor acrivity in seizure (not tx it) |
|
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Term
what category of drugs are best at helping with trachea intubation |
|
Definition
depolarizing neuromuscular blockers |
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Term
MOA non-depolarizing neuromuscular blockers |
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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) |
|
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Term
side effect of all non-depolarizing neuromuscular blockers |
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Definition
motor weakness: small muscles first then large, large first to recover diaphragm is last |
|
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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
|
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Term
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Definition
spontaneously inactivate to metabolite laudanosine (causes seizures, can be used in liver and kidney dysfynction) |
|
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Term
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Definition
same as articurium but when spontaneously inactivated does not produce as much laudanosine so less seizures occur |
|
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Term
mivacurium SE, duration, onset of action |
|
Definition
shortest DURATION short onset of action
causes histamine release > hypotension and reflex tachycardia |
|
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Term
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Definition
|
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Term
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Definition
blocks M receptors and causes tachycardia |
|
|
Term
what drug is a depolarizing neuromuscular blocker, what is its structure |
|
Definition
succinylcholine - 1 ACh together |
|
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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
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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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|