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Pharm Block 15
KYCOM Block 15
600
Pharmacology
Graduate
04/06/2014

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Term
synthesis of histamines
Definition
decarboxylation of AA L-histadine via pyridoxal phosphate dependent enzyme and L-histadine decarboxylase
Term
degradation of histamines
Definition
rapidly converted to inactive metabolite
Periphery: oxidative deamination: catalized by diamine oxidase making imidazole acetic acid
CNS and periphery: methylation of tele-nitrogen in imidazole ring catalized by histamine-N-methyltransferase making t-N-methylhistamine
Term
3 sites of histamine storage
Definition
found in almost all tissies: low in plasma and body fluids
mast cells: major site of storage and release, activated by IgE
basophils: similar to mase cells, high IgE binding affinity, store and secrete histamine
Term
mast cells: locations 3, how is histamine stored
Definition
high in skin, mucosa of bronchial tree and intestinal mucosa

histamine stored as granules with proteoglycan and chondroitin sulfate E
Term
basophils: location of high concentration, how does is histamine stored
Definition
high in neurons of CNS

histamine stored in granules with proteogltcan chondroitin monosulfate
Term
3 causes of histamine release
Definition
allergic disorders, drugs, endogenous peptides (bradykinin, substance P)
Term
explain the 2 processes of histamine release
Definition
cytolytic: plasma membrane is damaged and contents leak out

non-cytolytic: ligand binds receptor on mast cell, ATP dependent change in Ca causes leaking of cytoplasm and exocytosis of granules
Term
what are the MOA of the 3 types of histamine receptors
Definition
H1, H2, H3: G protein coupled receptors

H1: Gi receptor coupled to phospholipase C forms IP3 which releases Ca from ER and DAG which activates Ca via calmodulin dependent protein kinase and phospholipase A2 in target cell
Term
functions of the H1 and H2 receptors 3
Definition
1. histamine stimulates pain and hitch in nerve endings

2. histamine shock: large dose decreases BP and small vessels trap blood decreasing BV and CO

3. endothelium: increases Ca > phospholipase A2 > NO > diffusion to smooth muscle > guanylyl cyclase >>

> H1 receptor cGMP activates protein kinase and causes fast capillary dilation, increased permeability, lymph flow, and edema

> H2 receptor cAMP activates protein kinase and causes slow sustained capillary dilation
Term
functions of only the H1 receptr
Definition
bronchoconstriction
Term
Tx of autocoid bronchoconstriction
Definition
epinepherine
Term
MOA and distribution of 1st gen antihistamine
Definition
competitive reversible H1 inhibitor
crosses BBB
anticholinergic
Term
interactions of 1st gen antihistamine 3
Definition
EtOH, CNS depressants, MAOI
Term
effects of only 1st gen antihistamine 8
Definition
CNS: restless, nervous, insomnia
OD: excitation, convulsion, coma, respiratory collapse
anticholinergic: increased SANS, inhibit M receptor / ACh, atropine like
Term
MOA and distribution of 2nd gen antihistamine
Definition
competitive reversible H1 inhibitor
does not cross BBB
no anticholinergic effects
Term
effects of both 1st and 2nd gen antihistamine 7
Definition
inhibit histamine on smooth muscle, vasoconstriction, permeability, edema, wheals, flare,itch
Term
what do antihistamines never effect 2
Definition
anaphylactic bronchoconstriction
H2 vasodilation
Term
what is the story for the 8 1st gen antihisamines
Definition
dying phrends and dying men hydrated cyclically like pros with purel with chlori and my bro's phrend ramine who used pro meth from a magazine
Term
what are the 8 1st gen antihistamines
Definition
diphenhydramine
dimenhydrinate
hydroxyzine
cyproheptadine
purilamine
chlorpheniramine/brompheniramine
promethazine
meclizine
Term
diphrenhydramine: use 3, SE 2
Definition
allergies, OTC sleep med, extrapyrmidal SE

SE: sedation, lots of anti-M
Term
dimenhydrinate: use 1, SE 1
Definition
motion sickness
SE: anti-M
Term
hydroxyzine HCl: use 2, SE 1
Definition
long acting, skin allergies
SE: CNS depression, lots
Term
cyproheptadine: use 2, SE 3
Definition
drowsy, increased weight
mild anticholinergic
Term
purilamine: 2 SE
Definition
sedation, GI SE
Term
chlorpheniramine/brompheniramine: use 1, SE 1
Definition
allergy
SE: CNS stimulation (daytime med)
Term
promethazine: use 1, SE 2
Definition
nausea and vomiting
SE: anticholinergic, sleep
Term
meclizing: use 1
Definition
motion sickness, less effective
Term
what is the story for 2nd gen antihistamines
Definition
des and lora dined on citrsy flex or grenadine
Term
what are the 4 2nd gen antihistamines
Definition
desloratadine
loratadine
cetrizine
fexofenadine
Term
SE of the 2 2nd gen antihistamines (1 each)
Definition
desloratadine: renal/hepatic damage (less)
loratadine: renal/hepatic damage
cetrizine: renal/hepatic damage
fexofenadine: renal damage (use 1/3 dose)
Term
define asthma
Definition
hyperactivity of airway releases leukotrienes and histamine which cause smooth muscle proliferation, mucous gland hypertrophy, hypersecretion, inflammatory cells, edema, and loss of epithelium
Term
what are the 3 effector cells in asthma, at what point to they come into play
Definition
mast cells - immediate response
eosinophils - late response
T cells - chronic response
Term
mast cell: location, 6 things they release
Definition
3-5x more in respiratory tract of asthmatic

histamine, PGE, PAF, LTD, LTC, LTE
Term
eosinophils: effect, 1 thing they release
Definition
primary airway effector
number in bronchial lavage fluid is related to bronchial hyperreactivity

major basic protein- damages airway epithelium
Term
T cells: effect, 2 thing they release
Definition
number is proportional to bronchial hyperreactivity

releases interleukins
Term
symptoms of asthma
Definition
intrmittent
wheeze, cough, dyspnea, chest tightness
Term
5 qualifications for intermittent asthma
Definition
<2d/w
<2d/mo nocturnal symptoms
FEV >80%
FEV:FEC normal
SABA use <2d/wk
Term
5 qualifications for persistant mild asthma
Definition
>2d/wk
3-4d/mo nocturnal asthma
FEV >80%
FEV:FEC normal
SABA use >2d/wk
Term
5 qualifications for persistant moderate asthma
Definition
>2d/wk
>2d/mo nocturnal asthma
FEV >60% <80%
FEV:FEC <5% reduction
SABA use daily
Term
5 qualifications of persistant severe asthma
Definition
continous symptoms
frequent nocturnal symptoms
FEV <60%
FEV:FEC >5% reduction
hospitlized in last year for asthma
Term
4 ways asthma is diagnosed
Definition
reversible airway obstruction
history of symptoms
spirometric pulmonary function tests
methocholine challenge test
Term
5 goals of asthma therapy
Definition
normal activity and exercise levels
near normal pulmonary function tests
prevent chronic symptoms
prevent recurrent exacerbations
avoid medication SE
Term
2 types of B2 agonists and their 8 drugs
Definition
SABA: albuterol, levabuterol, terbutaline, pirbutrol, bitolerol, metaproterenol

LABA: salmeterol, formoterol
Term
SABA: onset, duration, usage
Definition
rapid onset 5-15min inhaled
4-6h duration
DOC mild asthma, rescue inhaler (not anti-inflammatory
Term
LABA onset, duration
Definition
onset 1h
duration 12h
Term
MOA B2 agonist 2
Definition
relax bronchial smooth muscle (adenylyl cyclase > cAMP > PKA > MLCK > smooth muscle relaxation)

stabilizes mast cell membranes
Term
SE of B2 agonist 3
Definition
more in oral/suryp (often used in kids)
tremor, tachyarrhythmia, muscle cramps
Term
2 types of corticosteroids used in asthma and their 6 drugs
Definition
inhaled: trimacinolone, flutocasone, budesonide

systemic- methylprednisone, prednisone, prednisolone
Term
how are steroids used in asthma, time of onset
Definition
used in moderate to severe asthma with SABA PRN
continous prevention
onset in 4-12h
Term
MOA steroids in asthma 4
Definition
stimulate glucocorticoid receptors
inhibit inflammation
reduce mucous production
increase B2 receptors (increases SABA effectiveness)
Term
why is a spacer used
Definition
only 10% of steroid reaches lung, 90% is metabolized by first pass if oral

increases deposition in lung by decreasing particle velocity and zise
Term
3 techniques for inhaling and exhaling corticosteroids and their benifits
Definition
open mouth: decreases particle size but also aim

closed mouth: increases aim but increases particle size

nose exhaling: helps with coating of mucosa in allergies
Term
what are 2 propellents used in inhalers
Definition
chlorofluorocarbon (CFC)
hydrofluroalkaline (HFA)
Term
explain how to use an inhaler
Definition
shake and remove cap
exhale slow with pursed lips
close/open mouth technique
press once
slowly inhale over 5 sec
hold breath 10 sec
exhale slowly
wait 1 min before next puff
Term
what is the story for the other drugs (non steroid or B2 agonist) used in asthma
Definition
the old man and liz needed chrome from chrome mountain, i prayed they throw the line to tio but monte leukast was za first leukast to salute on this
Term
what are the 9 other drugs used in asthma
Definition
omalizumab
nedcromil
chromolyn
ipratropium
throphylline
tiotropium
monteleukast
zafirleukast
zileuton
Term
MOA omalizumab
Definition
monoclonal anti-IgE antibody
Term
MOA nedcromil and chromolyn
Definition
inhibit mast degranulation and thus release of histamine and leukotrienes
Term
MOA impratopium
Definition
short acting muscarinic antagonist decreases PANS decreasing smooth muscle contraction
Term
MOA throphylline 3
Definition
blocks adenosine (a bronchoconstrictor)
decreases PDE III in smooth muscle of bronchi
decreases PDE IV in inflammatory cells thus decreasing cytokines
Term
MOA tiotropium
Definition
long acting muscarinic antagonist (with no M2 action) decreases PANS decreasing smooth muscle contraction
Term
MOA monteleukast and zafirleukast
Definition
block leukotriene receptors (cys-LT)
anti-inflammatory
causes bronchodilation
Term
MOA zileuton
Definition
block 5-lipooxygenase
Term
SE omalizumab 2
Definition
cancer
anaphylaxis
Term
SE nedcromil, chromolyn 4
Definition
anaphylaxis
laryngeal edema
headache
rash
Term
SE ipratopium
Definition
atropine like in high dose
Term
SE throphylline 5
Definition
CNS, CV, increase HR, GI, diuretic like
Term
SE tiotropium
Definition
atropine like in high dose
Term
SE monteleukast, zafirleukast, zileuton
Definition
headache in 13%
Term
use of omalizumab
Definition
severe allergen induced asthma
Term
use nedcromil, chromolyn 3
Definition
adjunct in mild-moderate asthma
exercise asthma
allergen asthma
Term
use ipratopium and tiotropium 2
Definition
in combination with B2 agonist (combivent, dunoeb) for COPD
pt with B2 intolerance
never acute use
Term
use monteleukast, zafirleukast, zileuton 2
Definition
alternate to steroid in mild asthma

adjunct to steroid in severe asthma
Term
age ok for use in monteleukast, zafirleukast, zileuton and administration
Definition
monteleukast 1yo+ oral
zafirleukast 5yo+ oral
zileuton 10yo + oral
Term
ipratopium and tiotropium: onset, dosing timing, administration
Definition
inhaled
slow onset
4x/d
Term
throphylline: administration 3, pharmacokinetic quality
Definition
P450 inhibitor
oral, rectal, parentrail
Term
nedcromil, chromolyn: administration, age ok to use, benifits based on age
Definition
inhaled
ok in kids - better than steroid but has not anti-inflammatory effect so steroid is still DOC
Term
omalizumab: age for ok use, administration, dosing timing
Definition
>12yo
intradermal
q2-4wk
Term
explain the six stages of asthma treatment
Definition
1. SABA PRN
2. LABA daily, SABA PRN
3. steroid daily, SABA PRN
4. LABA med dose daily, SABA PRN
5. LABA lg dose daily, SABA PRN
6. systemic steroid daily, steroid daily, SABA PRN
treat for 3mo, if stable step down a level
Term
what is the DOC for childhood asthma, what are 2 alternates
Definition
steroid inhaled daily
monteleukast, cromolyn
Term
define and what is cause of exercise asthma
Definition
pulmonary function decline (maybe only symptom or seen in 80% asthmatics)
caused by hyperventilation of cold air, respiratory heat, and water loss
Term
TX exercise induced asthma
Definition
<3h exercise: albuterol or terbutaline, chromolyn alternate

>3h exercise mild asthma: LABA
>3h exercise mod asthma: corticosteroid
Term
define and hat is cause of nocturnal astham, 3 signs
Definition
asthma in sleep or upon waking
worse 2-6am due to increased PANS, decreased epinepherine, increased inflammatory mediators, and GERD

morning cough, bronchospasm, esp in expiration (carcadian association)
Term
TX nocturnal asthma
Definition
LABA
corticosteroids if moderate to severe
Term
signs of aspirn induced asthma 3, when would you use aspirin anyways
Definition
rhinorrhea, wheeze, SOB
desensitize for post MI arthritis
Term
what drug should you avoid in asthmatics
Definition
non-specific BB (even timolol opthalamic)
be careful with B1 specific too
Term
causes or associations with COPD 8
Definition
asthma
cardiac disease
renal disease
smoking
grain
coal
asbestos
pollution
Term
pathological changes in chronic bronchitis
Definition
increased mucous and glands lead to obstruction, inflammation, edema, infection, bronchial hyperplasia of smooth muscle
Term
pathological changes in emphysema
Definition
increased proteases cause inflammation, fibrosis, destruction of alveolar wall and tissue which enlarge air space distal to terminal bronchioles, decrease elastic recoil and support leading to airway collapse without accessory muscle support to increase expiration
Term
5 avenules of tx for COPD
Definition
primary intervention - stop smoking
primary therapy - bronchodilators
corticosteroids
long term O2 treatment
immunizations - pneumococcus q6mo
Term
2 drugs that help stop smoking, their MOA and SE
Definition
buproprion: sustained release tablet antidepressant (SE suicide)

varenicline: nicotinic partial agonist decreases dopamine in mesolimbic tract and thus decreases reinforcement for smoking
SE: N/V, suicide
Term
what are the indications for long term O2 therapy, what is the timeframe
Definition
15-20 h/d reduces mortality

PaO2 <55
right heart failure
polycythemia
impaired neuropsychological function with PaO2 <60
Term
what is the drug combination used for bronchodilation in COPD
Definition
ipratoripum or tiotropium + SABA PRN

add throphylline if unable to control
Term
explain how steroids are used in COPD
Definition
really only benifit asthmatics
if not asthmatic, give 20-30mg prednisone for 2-3wks and if successful switch to inhaled steroid
Term
explain the physiology of a cough
Definition
involves CNS, PNS, bronchial smooth muscle
physiological, normal response that helps clear debris
Term
what are the 4 antitussives
Definition
codiene
hydrocodone
dextromethorphan
bensonate
Term
what is an expectorant and its MOA
Definition
guaifensin: increases respiratory fluid output by decreasing viscosity and surface tension
Term
MOA dextromethorphan
Definition
isomere of codine levorphanol (L isomere is addicting) acts on medulla to increase threshold
equal in effectiveness to codiene
Term
SE dextromethorphan 3
Definition
GI
high dose causes CNS depression
Term
causes of acute rhinitis 6
Definition
virus
bacteria
foreign body
hypothyroid
pregnancy
drug induced - medicamentosa
Term
9 causes of chronic rhinitis
Definition
allergy - hay fever, perennial
vasomotor rhinitis
tumor
polyp nasal septal deviation
enlarged adenoids
sinusitis
CSF rinorrhea
Term
5 modes of tx for rhinitis
Definition
avoid allergen
reversible H1 antagonist
decongestant
corticosteroid - inhaled
cromolyn - inhaled
Term
when should you use reversible H1 antagonist in rhinitis 3
Definition
perennial
allergic rhinits or conjunctivitis
Term
what are 4 decongestants used in rhinitis
Definition
pseudophredrine
phenhyleephrine
naphazoline
oxymetazoline
Term
MOA decongestant
Definition
stimulate a1 (symphathomimetrics)
often in combo with H1 antagonist
Term
SE decongestant
Definition
rebound congestion upon DC
Term
nitroglycerine MOA
Definition
venodilator decreases preload which decreases work on heart
Term
nitroglycerine use
Definition
angina SL for acute attack
not great preventitive
Term
drugs good vo vasospasm angina
Definition
never BB
CCB vascular specific - amlodipine
Term
drugs good for stable angina prevention
Definition
#1 is BB
any CCB will work (amlodipine, ditilzaim, verapmil)
Term
furosemide: MOA
Definition
work on ascending loop of henle targeting Na/K/2Cl diuretic
Term
furosemide: SE 4
Definition
loops loose Ca
ototoxic
K loss and thus H loss so metabolic acidosis
Term
furosemide: use
Definition
DOC acute pulmonary edema
Term
hydrochlorothiazide: MOA
Definition
works on DCT NaCl channels
Term
hydrochlorothiazide: SE 4
Definition
K loss and thus H loss so metabolic acidosis
thiazides save Ca
hyperglycemia
Term
hydrochlorothiazide: use 2
Definition
DOC daily fluid balance duiretic (long half life)
DI NOT caused by lithium
Term
what is used to tx DI caused by lithium, why
Definition
amularide: becaue lithium and Na are similar in size and charge. comes into CD through Na channels
Term
amiloride: MOA
Definition
works in CD as direct Na channel blocker
K sparing
Term
eplerone and spironolactone: MOA
Definition
works in CD as ALD receptor blocker decreasing number of Na chennals, thus indirect CD blocker
K sparing
Term
SE K sparing diuretics
Definition
if you save K you save H causing metabolic acidosis
Term
niacin MOA 3
Definition
lowers VLDL, TG
raises HDL
Term
niacin SE 2
Definition
flushing
itching
Term
cholestyramine: MOA
Definition
bile acid sequesterant (ie cholesterol)
complexes with bile so you cannot recycle them and you loose them from the body and liver needs to make more bile acids and thus need to pull cholesterol from the blood to do it
Term
cholestyramine: contrindications, why
Definition
hyperTG patients: further increases TG because when liver starts making more bile acids it starts making other lipids too
Term
statins: MOA
Definition
HMG CoA reductase (rate limiting step in cholesterol synthesis) inhibitor
benifit all aspects of lipid profile
Term
which statin is most likley to raise HDL, which is least
Definition
atrivostatin > simvastatin
Term
Statin: SE
Definition
muscle toxicity (myalgia, myositis, rhabdomyalgia)
Term
statin interactions
Definition
take with P450 inhibitor increases statin levels and risk of muscle toxicity (never drink grapefruit juice!)
Term
fenofibrate MOA
Definition
increases gene expression of PPARy which increases lipoprotein lipase which lowers TG
Term
what two NT and change in parkinsons disease
Definition
decreased dopamine
increased ACh (Relative)
Term
levadopa: MOA
Definition
taken into CNS and turned into dopamine
use carbadopa to avoid DOPA decarboxylase break down in periphery
Term
ropinerole: MOA
Definition
dopamine agonist directly stimulates D2 receptors
Term
selegiline: MOA
Definition
stops metabolism of dopamine by MAOB blocking it
Term
entacapone: MOA
Definition
in periphery and CNS levodopa is converted to 3-o-methyodopa by COMT
drug blocks COMT to increases levadopa conversion to dopamine
Term
benzotropine: MOA 3
Definition
targets ACh, muscarinic blocker
lowers effect of ACh in parkinsons
Term
benzotropine: SE
Definition
atropine like
Term
drugs used for parkinsons
Definition
levodopa/carbadopa
ropinerole
selegiline
entacapone
benzotropine
Term
explain the break down process of ethanol and the SE 3
Definition
ethanol > alcohol DH > acetaaldehyde > aldehyde DH > acid aldehyde > acidosis, N/V, headache
Term
explain break down process of methanol and the SE 2
Definition
methanol > alcohol DH > formeldahyde > aldehyde DH > formic acid > acidosis, eye damage
Term
explain break down process of ethylene glycol and the SE 2
Definition
ethylene glycol > alcohol DH > aldehyde > aldehyde DH > acid aldehyde > acidosis, kidney damage
Term
MOA disulfram
Definition
blocks aldehyde DH causing aldehyde buildup which causes toxic effects deturing from alcohol use
Term
2 stimulants
Definition
methylphenidate
dextroamphetamine
Term
MOA stimulants 2
Definition
promote release of NE and dopamine
Term
USE stimulants 2
Definition
ADHD
narcolepsy
Term
SE stimulants 3
Definition
tachycardia
sweating
increased BP
Term
heparin MOA
Definition
uses antithombin III to cleave IIa, IXa, XIa, XIIa
works on activated factors so works rapidly
Term
heparin antidote and MOA
Definition
protamine: directly complexes with heparin stopping its action
rapid onset
Term
SE heparin
Definition
heparin induced thrombocytopenia (stop all drugs working through antithrombin III if induced, not just heparin)
Term
how can heparin be monitered
Definition
PTT
Term
enoxaprin: MOA
Definition
low molecular weight heparin
Term
warfarin MOA
Definition
takes time, decreased synthesis of II, IV, IX, X by stopping vitamin K
Term
warfarin antidote and MOA
Definition
Vit K: never going to be fast
fresh frozen plasma: fast, replenishes clotting factors
Term
how is warfarin monitered
Definition
INR
Term
rivaroxban: MOA, how monitored
Definition
blocks factor Xa
no need to monitor
Term
dabigatran: MOA, how monitored
Definition
direct thrombin inhibitor
no need to monitor
Term
clopidogrel: MOA, use
Definition
ADP receptor blocker
cannot activate platelets
good back up to aspirin
Term
abciximab: MOA
Definition
glycoprotein IIb/IIIa inhibitor blocks fibrinogen receptors prevents cross linking in platelet aggregation
Term
abciximab: use 3
Definition
angioplasty
acute coronary syndromes
unstable angina
Term
alteplace: MOA
Definition
tPA
fibrinolytic
breaks down clots
Term
alteplace: antidote
Definition
aminocaproic acid
Term
causes of nausea and vomiting in adults 10
Definition
metabolic
neuro
CV disorder
GI disorder
infection
pregnancy
operations
drugs
chemo
emotions
Term
causes of nausea and vomiting in kids 14
Definition
pyloric stenosis
duodenal ulcer
stress ulcer
adrenal insufficiency
septicemia
disease of pancreas, liver, biliary tree
GI obstruction
increased ICP
overfeeding
rapid feeding
inadequate burping
laying down too soon after feeding
Term
define nausea
Definition
immediate need to vomit, gastric stasis
Term
define retching
Definition
rhythmic action of respiratory muscles (abdominal, inercostal, diaphragmatic) against closed glottis
Term
define vomiting
Definition
forceful expulsion of gastric contentents caused by GI retroperistalsis, salivation, shivering, vasomotor changes
Term
afferent sensory nerves send receptors for nausea and vomiting to 3
Definition
chemoreceptor trigger zone (CTZ)
cerebral cortex
visceral afferents from pharynx and GI
Term
afferent signals are intergrated by vomiting center in medulla and efferent impulses go to 5
Definition
salivation center
respiratory center
pharyngeal, GI, abdominal muscles
Term
NT involved in vomiting center, CTZ, GI tract 4
Definition
ACH (M), histamine (H1), dopamine (D2), serotonin (5-HT3), opiate receptors
Term
categories of drugs that help with nausea and vomiting 5
Definition
5-HT3 antagonist
dopamine antagonist
antihistamine
anticholinergics
cannabis
Term
2 5-HT3 antagonists used in nausea and vomitin
Definition
odansetron
palonostron
Term
5 dopamine antagonist used in nausea and vomiting
Definition
chlori was a pro, a pro at doing meth, a pro chlori was, she drop it like it hot on the metro, chlori pride
chelrpromazine
promethazine
prochlorperazine
deoperidol
metoclopramide
Term
2 antihistamines used in nausea and vomiting and their administrations
Definition
meclizine (oral)
diphenhydramine (oral, IM, IV)
Term
1 anticholinergic used in nausea and vomiting
Definition
scopolamide
Term
cannabis aka
Definition
dronabinol
Term
odansetron: MOA
Definition
antagonist of central/peripheral 5-HT3 on vagal afferents, NTS, postremia
Term
what is the cause of post chemo nausea
Definition
serotonin released by enterochromaffin cells in SI in response to chemo may stimulate vagal afferents to vomiting reflex
Term
odansetron administration 4
Definition
tablets
oral
solutions
IV
Term
odansetron: use 4
Definition
most effective for chemo and upper abdominal irridation nausea
effective against hyperemesis of pregnacy
somewhat effective for post-op nausea
Term
how is palonostron different than odansetron
Definition
has t1/2 40h, longest of serotonins
Term
prochlorperazine, chlorpromazine, promethazine: MOA 3
Definition
D2 antagonist at CTZ
antihistamine
anticholinergic
Term
prochlorperazine, chlorpromazine, promethazine: use 2
Definition
most common general antinausea and antiemetic
NOT effective for nausea associated with chemo
Term
prochlorperazine, chlorpromazine, promethazine: SE
Definition
most common drug to cause drowsiness
Term
droperidol: MOA
Definition
D2 antagonist at CTZ
Term
droperidol: administration 2
Definition
IV, IM
Term
droperidol: use 2
Definition
surgical antiemetic
preop med when other tx not effective
Term
droperidol: SE 2
Definition
alters cardiac conduction
sedation
acute dystonia
Term
metoclopramide: MOA 5
Definition
stimulate ACh release from enteric neurons increasing GI motility and LES pressure (prokinetic)

Blocks D3 receptors at CTZ

supresses inhibitor interneurons by antagonizing 5-HT3 receptor

stimulates 5-HT4 receptor

agonist of D2 receptors that inhibit cholinergic neurons
Term
metoclopramide: administration 3
Definition
oral, IM, IV
Term
metoclopramide: use 4
Definition
adjunct to PPI and H2 blocker for GERD

gastroparesis (increases gastric emptying)

antinausea

antiemetic
Term
metoclopramide: SE
Definition
chronic use >12wk: tarditive dyskinesia

acute use: acute dystonia (reversible tarditive dyskinesia) or pseudoparkinsonism EPS symptoms
Term
MOA antihistamines for nausea and vomiting
Definition
H1 antagonist on vestibular afferents in brain stem
Term
use of antihistamines for nausea and vomiting
Definition
motion sickness
Term
MOA of scopolamide
Definition
anticholinergic
Term
scopolamide: administration 2
Definition
injectable bromide
transdermal patch
Term
scopolamide use
Definition
prevent and tx motion sickness
NO role in chemo nausea
Term
MOA dronabinol
Definition
stimulate CB1 cannaboid receptors on neurons in vomiting center
Term
use dronabinol 2
Definition
prophylactic for nausea in chrmo when other antiemetic uneffective

stimulate appetite in AIDS patients
Term
SE dronabinol 3
Definition
central sympathomimetic activity
tachycardia
high
Term
antiemetics used in pregnancy 3
Definition
antihistamines
odanzatron
promethazine considered
Term
antiemetic used in severe nausea in chemo 3
Definition
metoclopramide
odanzetron
cannibis
Term
antiemetic used in moderate emesis in chemo 3
Definition
prochlorperazine
odanzetron
dronabinol
Term
antinausea and antiemetic used in severe chemo
Definition
combinations of ones for mild and moderate symptoms
Term
cause of IBS
Definition
visceral hypersensitvity from alterations to neuroreceptor in afferent spinal neuron function

CNS odulation of afferent input in way that results in long term sensitization of pathways involved in visceral sensation

no structural or biochemical factors
Term
IBS associated diseases 5
Definition
depression
anxiety
chronic fatigue syndrome
functional dyspepsia
fibromyalgia
Term
symptoms of IBS 4
Definition
lower abdominal pain
constipation
diarrhea
bloating
Term
tx of constipation predominate IBS 2
Definition
dietary fiber
psyllium if unable to tolerate dietary fiber
Term
DC tx of constipation predominate IBS and why, MOA, dosing
Definition
tagsarod
heart attacks, severe diarrhea
12wk short term tx
5-HT4 agonist
Term
tx of diarrhea predominate IBS 3
Definition
psyllium
ipoeramide
avoid triggers
Term
triggers of diarrhea predominate IBS 7
Definition
caffiene
alcohol
sweeteners: sorbitol, fructose, mannitol
herbal medicines
tea (senna is laxative)
Term
tx of IBS with abdominal pain and bloating 2 and MOA
Definition
antispasmotics:
dicylomide
atropine-hyoscyamide-phenobarbitol-scopolamide: anticholinergic DOC for IBS effectiveness not proven
Term
adjnct tx for IBS 2, 2 effects
Definition
TCA, SSRI
help with analgesia with eating
relieve depression
Term
components of bile acids 3
Definition
cholic acid
chenodeoxycholic acid
deoxycholic acid
Term
functions of bile acids 4
Definition
induce flow of bile
feedback inhibition of cholesterol synthesis
eliminate cholesterol (promote excretion)
disperase and absorb lipids and fat soluble vitamins
Term
drug used for gallbadder
Definition
ursodeoxycholic acid
Term
ursodeoxycholic acid: MOA
Definition
cytoprotective on hepaticytes
functional gallbladder needed: modified by bile
degrades cholesterol monohydrate crystals in 40%
Term
ursodeoxycholic acid: use 2
Definition
cannot be used for bile acid therapy alone due to unfavorable surface area to size ratio

gall bladder dissolution

cholestatic liver disease
Term
define pancreatitis
Definition
loss of gland function (Exocrine and endocrine), inflammation, and pain
Term
function of pancreatic enzymes
Definition
protein and fat digestion
Term
how are pancreatic enzymes released
Definition
CCK releasing monitor peptide from duodenum triggers CCK then is degraded by trypsin

CCK stimulates release of pancreatic enzymes
Term
effects of chronic pancreatitis on physiology
Definition
trypsin insufficiency increases CCK and causes pain due to continous stimulation of enzymes and increased intraductal pressure

decreased digestive enzymes cases protein maldigestion and seatorrhea when >90% pancreas lost leading to malabsorption and diarrhea
Term
goals of tx of chronic pancreatitis 2
Definition
prevention of malabsorption
pain relief
Term
2 drugs used in chronic pancreatitis
Definition
lipase, protease
Term
lipase MOA
Definition
delivered to duodenum during 4h period with and after a meal
Term
use of lipase
Definition
decrease diarrhea and malabsorption due to pancreatitis
Term
protease MOA
Definition
delivered to duodenum and interrupts CCK mediated pain loop
Term
why would lipase and protease be coated or uncoated
Definition
coated: treat malabsorption
uncoated: treat malabsorption and pain
Term
explain how the two main categories of prostaglandins are made
Definition
phospholipid membrane (phosphitadil inositol) is broken by phospholipase A2 into arachidonic acid

arachidonic acid is converted to either 5-lipooxygenase, COX1, or COX2

to be converted to COX2 it needs to be induced by inflammation (unless in brain and kidney where it is constitutive)
Term
what type of receptors do prostaglandins use
Definition
G protein receptors that activate or inhibit adenylyl cyclase and phospholipase C
Term
explain the 5-lipooxygenase pathway and the 3 effects
Definition
5, 12, 15 - HPETE > 5-HETES > leukotriene >>

phagocyte mobilization, change in vascular permeability, inflammation
Term
what are the 3 products of the COX pathway
Definition
prostacyclin (PGI)
prostaglandin (PGE)
thromboxane A2 (TXA2)
Term
3 effects of prostacyclin
Definition
gastric acid secretion
decreased platelet aggregation
maintain renal flow despite vasoconstrictors
Term
6 effects of prostaglandins
Definition
maintain renal flow despite vasoconstrictors
sensitize nerve endings to bradykinin and histamine causing pain
increase thermoregulatory center in hypothalamus
stimulate stomach mucous
keep PDA open
Term
1 effect of thromboxane A2
Definition
platelet aggregation
Term
where do corticosteroids dysrupt the prostaglandin pathway
Definition
stop phospholipase A2 from breaking phosphitadil inositol from phospholipid membrane into arachidonic acid
Term
where do salycylates dysrupt the prostaglanding pathway
Definition
stop COX2 from inducing PGI, PGE, TXA2
Term
what are the 4 salicylates
Definition
acetylsalicylate (aspirin)
choline Mg trisalicylate
sulfasalazine
diflundail
Term
MOA of the 4 salicylates
Definition
acetylsalicylate - irreversible COX2 blocker
choline Mg trisalicylate - reversible COX2 blocker
sulfasalazine - reversible COX2 blocker
diflundail - reversible COX2 blocker
Term
which salicylate is differet, why
Definition
diflundail: does NOT cross BBB (NO antipyretic), does NOT affect uric acid secretion, 3-4x more potent
Term
10 non-respiratory effects of salicylates
Definition
anti-inflammation (PGE)
decrease pain (PGE)
anti-pyretic (no effect on normal body temp, PGE)
decrease gastric acid (PGI)
decrease stmach mucous (PGE) causes ulcers and hemorrhage
blood thinning (TXA2, PGI) (irreversible lasts life of platelet in aspirin)
closes PDA
vasoconstriction, Na/water retention, and kyperkalemia in renal vessels
Term
respiratory effects of normal, high, and toxic doses of salicylates
Definition
normal: stimulates resporatory medulla, uncouples ETC increasing CO2 stimulating respiratory medilla too, leads to hyperventilation and respiratory alkalosis

toxic: supresses respiratory center causing respiratory acidosis and metabolic acidosis (drug is acid)
Term
uses of salicylates 17
Definition
gout
RA
rheumatic fever
headache
arthralgia
myalgia
corns, callus, wart (topical)
blood thinner
angina
close PDA (dec PGE)
decrease colon cancer
ulcerative collitis
anti pyretic
analgesic
antiinflammatory
Term
how does the dose of salicylates effect the function
Definition
low dose t1/2 3-5h: blood thinner

med dose t1/2 3-5h: anti inflamm

high dose t1/2 15h: zero order kinetics
Term
side effects of salicylates 7
Definition
epigastric distress
N/V
bleeding
metabolic depression
15% have intolerance/hypersensitivity
rye syndrome: aspirin in viral infection in kids causes hepatitis and cerebral edema
Term
interactions with salicylates 4
Definition
antacids: decrease absorption
heparin: hemorrhage
probenecid: decrease excretion (contraindicatedin grot)

prolonged t1/2, effects, toxicity of many drugs
Term
5 signs of mild salicycate toxicity
Definition
N/V
hyperventilation
headache
confusion
tinnitus
Term
9 signs of severe salicylate toxicity
Definition
restlessness
delirium
hallucinations
convulsions
dizziness
coma
death
respiratory acidosis
metabolic acidosis
Term
TX or salicylate toxicity 3
Definition
increase urine pH to help elimination
IV dialysis
fluids
Term
proprionic acid derivatives MOA
Definition
COX 1 and 2 inhibitors
Term
story of proprionic acid derivatives
Definition
I bought a flurb producing napping oxen for ketoz profound ox fender
Term
6 proprionic acid derivatives and their half lives
Definition
ibprofen 2-4h (dose q4-6h)
flubiprofen 2-4h
naproxen 12-24h (dose q12h)
ketoprofen 2-4h
oxaprozin 58h (dose 1x/d)
fenoprofen 2-4h
Term
5 SE ibprofen
Definition
GI irritation (bleed is rare)
renal failure
nephritis
nephrotic syndrome
less anti-coagulation effects means less interactions
Term
SE naproxen
Definition
same as ibprofen plys CV effects
Term
SE ketoprofen
Definition
some lipooxygenase inhibition (no greater antiinflammatory effect)
Term
SE fenoprofen
Definition
interstitial nephritis
Term
story of COX2 inhibitors
Definition
val selectively rolfed on his cox
Term
3 COX2 inhibitors and their SE
Definition
celecoxib - sulfa hypersensitivity, don't anticoagulate (COX2 only), GI bleeds
rofecoxib - DC due to CV events
valdecoxib - DC due to SJS
Term
use of COX2 inhibitors 2
Definition
RA
osteoarthritis
COX2 depressed in colon cancer and alzheimers disease
Term
story of COX1/2 inhibitors
Definition
so in the back the key tore Dic's fence so now theres a total lack in da mesh
Term
5 COX1/2 inhibitors
Definition
sulindac
ketorolac
diclofenac
etodolac
indomethacin
Term
MOA sulindac
Definition
related to indomethican
less SE
converted to sulfide
Term
MOA and use ketorolac
Definition
potent analgesic
moderate anti inflammatory
chronic/post-op pain, seasonal allergic conjunctivits
Term
diclofenac MOA
Definition
formula with misoprostol (PGE-E1) to decrease GI SE, accumulates in synovium
Term
MOA etodolac
Definition
large difference between anti-inflamm dose and GI issue dose
Term
indomethacin MOA and uses 7
Definition
potent anti inflammatory used in gout, arthritis, anylosing spondylitis, acute shoulder

tocolytic: supresses contraction in preterm labor

closes PDA
Term
SE diclofenac 2
Definition
GI upset
hepatic disease (increases amniotransferases)
Term
etodolac SE
Definition
only 5% get GI issues
Term
indomethacin SE 5
Definition
GI upset, frontal headaches, neutropenia, thrombocytopenia, aplastic anemia
Term
MOA acetaminophen
Definition
analgsic, antipyretic, NO anti inflammatory effect
inhibit PGE synthesis in CNS
Term
pharmacokinetics of acetaminophen: normal and OD
Definition
significant first pass: conjugated via glucorindation/sulfination

hydroxylated to NAPQI which at normal dose reacts with glutathione but at toxic dose builds up and depletes glutathione and reacts to hepatic sulhydryl and causes necrosis
Term
acetaminophen antidote
Definition
n-acetyl cysteine sulfhydryl binds NAPQI as antidote
Term
SE acetaminophen
Definition
well tolerated at normal doses, no effect on platelets or uric acid
Term
use of acetaminophen 4
Definition
analgesic
antipyretic
DOC reye syndrome prevention (fever in kids with viruses, VZV)
DOC gout pt (not reaction with probenicid)
Term
what is a peptic ulcer
Definition
lesion in gastric/duodenal mucosa at site where mucosal epithelium is exposed to acid and pepsin
normal mucosa is protected by mucous and can withstand acid and pepsin attack but excess acid, intrinsic defect of barrier allows ulcers to form
Term
8 causes of PUD
Definition
H. pylori
NSAID
stress related mucosa damage
zollinger ellison (inc gastric acid)
viral: CMV
cocaine: vascular insufficiency
radiation
chemo: hepatic artery insufficiency
Term
explain how acid is releaed in the stomach
Definition
neuron releases ACh which stimulates gastrin release from duodenal G cells.

gastrin stimulates parietal cell in the fundus release of HCl and intrinsic factor

histamine is released from mucosa mast cells via paracrine pathway and stimulates acid release

H/K ATPase on Chief cells secrete pepsinogen against gradient. acid converts pepsinogen to pepsin which digests
Term
3 things that protect us from acid
Definition
mucous: secreted from epithelial and mucous cells in stomach, contains bicarbonate
continous cell removal
prostaglandin F2 inhibits acid secretion
Term
how does H. pylori cause damage
Definition
colonizes acidic mucosa causing inflammatory gastritis, peptic ulcer, gastric lymphoma, adenocarcinoma

increases HCl secretion
decreases mucosa defenses
Term
clinical signs of gastric or duodenal ulcer
Definition
epigastric pain: burning, gnawing, aching
Term
what persent of population is infected and what percent develops ulcers from H. pylori
Definition
50% infected
15% get ulcers
Term
what is GERD
Definition
symptomatic clinical or histological alteration due to gastroesophageal refluc (retrograde acid into esophagus) due to decreased LES pressure

due to acid spending too much time in esophagus not too much acid

causes inflammation and erosive esophagitis
Term
food causes of decreased LES pressure 10
Definition
carminatives (mints)
chocolate
fat
coffee
cola
tea
citris
tomato
onion
garlic
Term
hormone causes of decreased LES pressure 8
Definition
CCK
estrogen
gastric acid
gucagon progesterone
PGE
secretin
VIP
Term
drug causes of decreased LES pressure 15
Definition
anticholinergic
barbituates
BDZ
caffiene
CCB
dopamine
estrogen
EtOH
narcotics
nicotine
progesterone
throphylline
phentolamine
nitrates
isoproterenol
Term
causes of increased LES pressure 10
Definition
protein meal
gastric alkalinization
gastrin
PGE F2
prokinetics
endorphonium
methacoline
NE
pentagastrin
phenylperine
Term
what are the anatomical changes caused by all the things that change LES pressure allowing GERD 3
Definition
lower GE sphincter pressure due to...
spontaneous LES relaxations
transient increases in intra-abdominal pressure
atonic LES
Term
what are the 4 aggregating factors causing inflammation and erosive esophagitis
Definition
gastric acid
pepsin
bile
pancreatic enzymes
Term
4 complications of GERD
Definition
esophagitis
strictures
barretts esophagus
anemia
Term
typical signs of GERD 4
Definition
heartburn, may radiate to neck
hypersalivation
belching
regurgitation worse after fatty food, laying down, bending over
Term
atypical signs of GERD 5
Definition
nonallergic asthma
chronic cough
horseness
pharyngitis
CP like angina
Term
4 staps in PUD treatment
Definition
1. remove stress, smoking, NSAIDS
2. remove H. pylori
3. NSAID ulcer treatment
4. relief of symptoms
Term
how do we kill H. pylori
Definition
1 PPI + 2 of theses (clathriomycin, amoxicillin, metronidazole, tetracycline)

3 antibiotics may cause better compliance, effectiveness, less resistance
Term
how do we treat NSAID ulcers
Definition
H2 antagonist, PPI, or sucralfate
NSAID discontinuation
PPI causes better ulcer healing
Term
what can be used for PUD symptom relief 3
Definition
OTC H2 antagonist and antacids
RX PPI
Term
5 steps in GERD treatment
Definition
1. elevate head when sleeping, protein rich meals, stop smoking and drinking
2. OTC meds
3. perscription H2 antagonist
4. perscription PPI or high dose H2 antagonist
5. surery
Term
what OTC meds can be used for GERD 3
Definition
antacids
alginic acid
H2 antagonists
Term
how can GERD be prevented 2
Definition
PPI
ranitidine (only H2 antagonist for erosive esophagitis)
Term
which categories of drugs can be used for both PUD and GERD 3
Definition
H2 antagonists
PPI
Antacids
Term
which categories of drugs can be used only for PUD 2
Definition
prostaglandins
antimuscarinic
Term
which categories of drugs can be used olny for GERD 2
Definition
mucosal protective agents
promotility (prokinetic agents)
Term
3 H2 receptor antagonists
Definition
it rained on the cement as they family dined
raitidine
cimetidine
famotidine
Term
5 PPI drugs
Definition
ome es just being ome; lancing raspberries in a pan
omeprazole
esomeprazole
lansoprazole
rabeprazole
pantoprazole
Term
which antipsychotic isnt a PPI
Definition
apapriazole
Term
what drug is a prostaglandin
Definition
i missed the prostate and it released prostaglandins
misoprostol
Term
which drug is a antimuscarinic that can be used in PUD
Definition
that dic collected my acid
dicyclomine
Term
5 antacid drugs
Definition
a glince of Al, Mg, Ca, Na, can fix the acid
aglinic acid
aluminum hydroxides
Magnesium hydroxides
calcium carbonates
sodium bicarbonates
Term
2 mucosal protective agents
Definition
collin bismith sure cared about the fate of his mucous
colloidal bismuth
sucralfate
Term
1 promotility/prokinetic agent
Definition
i got on the metro and the clomping made my GI turn
metoclopramine
Term
DOC for peptic ulcer and GERD
Definition
H2 antagonist
Term
which PUD/GERD drug promotes healing
Definition
H2 antagonist, antacids
Term
DOC for long term hypersecretion conditions (zollinger ellison)
Definition
PPI
Term
which PUD/GERD drug works on reflux esophagitis
Definition
PPI
Term
which PUD/GERD drug is also antimicrobial
Definition
colloidal bismuth
Term
which PUD/GERD drug used for NSAID ulcer prevention
Definition
misoprostol
Term
which PUD/GERD drug used for NSAID ulcer treatment
Definition
PPI
Term
which PUD/GERD drug cannot be taken with antacids
Definition
sucralfate
Term
which PUD/GERD drug is also used in gastroparesis and as antiemetic
Definition
metoclopramine
Term
MOA H2 receptor antagonist 4
Definition
blocking H2 in stomach inhibits acid, histamine (and thus HCl), and gastrin secretion

indirectly blocks M receptor and gastrin receptor due to role of histamine in their production
Term
H2 antagonist: administration and excretion
Definition
oral
renal, excreted unchanged
Term
H2 antagonist: potency
Definition
famotidine > ranitidine > cimetidine
Term
H2 antagonist: use 3
Definition
DOC GERD and PUD
promote ulcer healing (need H. pylori tx or will reoccur)
Term
H2 antagonist: SE 4
Definition
limited H2 function in other tissues causes headache, dizziness, nausea

cimetidine is antiandrogenic (decreases production and blocks receptor) causing glyecomastia
Term
H2 antagonist: interactions 1
Definition
cimetidine: P450 inhibitor which potentiates warfarin, diazepam, phenytoin, quinidine, carbamazepine, throphylline, imipramine
Term
MOA PPI
Definition
H/K ATPase inhibitor inhibits gastri acid secretion by irreversibly inhibiting proton pump
Term
PPI: duration, administration
Definition
oral delayed relase capsule: destoried by gastric acid without gelatin coated capsule which prevents release of drug until intestines which it is rapidly absorbed

actions are long lasting because their irreversible so once daily dosing
Term
PPI uses 4
Definition
active ulcers
NSAID ulcers
reflux esophagatis
DOC zollinger ellison / hypersecretion
Term
PPI SE and interactions 5
Definition
omeprazole: P450 inhibitor increases warfarin, phenytoin, diazepam

3% get nausea, diarrhea, abdominal cholic

colpidogrel decreases drug effect
Term
misoprostol: MOA 3
Definition
PGE E2 and I2 receptor agonist decreases cAMP and inhbits acid secretion
stimulates mucous and bicarb production
Term
misoprostol: use 2
Definition
prevent NSAID (most selective, not most effective thats PPI)
peptic ulcer (less effective)
Term
misoprostol: pharmacokinetics
Definition
available in combo with diclofenac (NSAID)
Term
misoprostol: SE 5
Definition
diarrhea
abdominal cramps
abortion
premature birth
category X teratogenic birth defect
Term
dicyclomine: use
Definition
adjunct to peptic ulcer treatment
Term
dicyclomine: MOA
Definition
M blocker inhibits ACh stimulation of gastric acid secretion
Term
dicyclomine: SE
Definition
atropine like (Tachycardia, dry mouth, constipation, urine retention)
Term
antacids: MOA 3
Definition
react with gastric acid to make water and salt
reduce pepsin activity by increasing pH
alginic acid: not as effective at neutralizing acid but protects esophageal mucosa
Term
antacids: use 5
Definition
heal gastric ulcers
relieve GERD symptoms
AlOH slow relief
MgOH moderate relief
CaCO and NaHCO3 fast relief
Term
SE AlOH
Definition
binds phosphate causing constipation
Term
SE MgOH
Definition
diarrhea
Term
SE bicarbonates 3
Definition
systemic alkalosis - alkalinizes urine
liberate CO2 causing burps and farts
Term
SE all antacids
Definition
all have Na so important in HTN and CHF

affect absorption od drugs because they raise pH of stomach and bicarb alkalinizes urine
dont take other drugs +/-2h from antacid
Term
sucaralfate: MOA 5
Definition
requires acid for activation
complex of AlOH and sulfated sucrose binds positive charges in mucosa proteins
creates barrier impairing HCl diffusion and pepsin degradation
stimulates prostaglanding and bicarb release
Term
sucaralfate: SE
Definition
dont take with antacid, needs acid to activate
Term
colloidal bismuth: MOA 5
Definition
neutralize gastric acid
bind surface of stomach and create barrier
stimulate mucous and bicarb production
antibacterial on H. pylori
Term
colloidal bismuth: SE 3
Definition
black tongue
black stool
increased bleeding time with bismuth subsalicylate (NSAID)
Term
metoclopramine: MOA 3
Definition
stimulate ACh release from enteric neurons increasing GI motility and LES pressure
blocks D2 receptors
Term
metoclopramine: use 3
Definition
adjunct to PPI and H2 block in GERD
gastroparesis
antiemetic
Term
metoclopramine: SE 2
Definition
chronic use >12wk: tarditive dyskinesia
acute use: EPS/pseudo parkinsons
Term
name 2 ACEI
Definition
catopril
lsinopril
Term
use of ACEI 3
Definition
HTN
CHF
in diabetic renal benifit
Term
SE of ACEI 2
Definition
cough
angioedema: rapid sewlling of face after 1st dose
Term
contraindications of ACEI 1
Definition
pregnancy
Term
4 BB and their MOA
Definition
propranolol - no selective
desmolol, atenolol, metoprolol - B1 selective
Term
which BB are prefered in cardiac conditions
Definition
B1 selective
Term
contraindications to BB 3
Definition
asthma
diabetes
peripherial vascular disease: vasospastic angina
Term
SE BB 4
Definition
slows heart down
decreased CO
fatigue
never abruptly DC
Term
Use BB 4
Definition
HTN
CHF
anti-arrhythmic SVT class 2
angina
Term
use esmolol, why
Definition
BB only used in arrhythmia
short t1/2 10 min
Term
name one ARB and it MOA
Definition
losartin
block ANG II receptor, benifits similar to ACEI
Term
use of ARB 3
Definition
HTN
CHF
renal benifit in diabetes
Term
SE of ARB
Definition
no cough
Term
contraindications of ARB 2
Definition
pregnancy
hyperkalemia
Term
1 vasodilator
Definition
hydralazine
Term
MOA hydralazine
Definition
vasodilates using NO with specificity for arterioles
Term
MOA nitrates
Definition
work through NO with sepcificity to VEINS
Term
use hydralazine 2
Definition
HTN
CHF - back up if unable to use ACEI/ARB
Term
SE hydralazine
Definition
drug most likley to cause drug induced lupus in slow acetylators
Term
central A2 agonist 1
Definition
methyldopa
Term
MOA methyldopa
Definition
main effect inside CNS
stimulates A2 inhibitory recetors decreasing sympathetic output
Term
SE methyldopa 2
Definition
fatigue
hemolytic anemia
Term
use methyldopa
Definition
HTN, esp in pregnancy
Term
MOA carvedilol
Definition
A and B blocker
Term
use carvedilol 2
Definition
HTN
CHF
Term
MOA slidenafil
Definition
block PDE5 increasing cGMP and NO which causes vasodilation
Term
use slidenafil 2
Definition
pulmonary HTN
erectile dysfunction
Term
contraindications slidenafil
Definition
never use with nitrates, both work in same pathway too much dilation occurs
Term
3 CCB
Definition
verapamil
diltaziam
amidopine
Term
MOA verapamil
Definition
cardiodepressant
blocks L type Ca channels on heart
Term
MOA ditilaziam
Definition
cardiodepressant
blocks L type Ca channels on heart mostly
Term
MOA amlodipine
Definition
vasodilates, drops BP
blocks L type Ca channels on vessels
Term
use of verapamil 3
Definition
HTN
angina
arrhythmia SVT class 4
Term
SE cerapamil
Definition
constipation
Term
use ditilaziam 3
Definition
HTN
angina
arrhythmia SVT class 4
Term
use of amlodipine 3
Definition
HTN
angina
Term
SE amlodipine 2
Definition
reflex tachycardia
gingival hyperplasia
Term
MOA digoxin
Definition
positive inotrope
inhibits Na/K ATPase on cardiac myosites
when Na goes up Ca does too and gets stored in sarcoplasmic reticulum so not it releases more causing positive inotropic effect
Term
use digoxin
Definition
arrhythmia SVT
Term
SE digoxin 2
Definition
low theraputic index
arrhythmia
blurry yellow vision
Term
contraindications of digoxin
Definition
hypokalemia can enhance digoxin toxicity
digoxin and K bind same site on Na/K ATPase
Term
4 drugs used for ventricular tachycardia
Definition
procanamide
lodicaine
sotalol
amiodarone
Term
4 types of drugs used for SVT
Definition
CCB
BB
adenosine
digoxin
Term
2 drugs used to ventricular tachycardia and SVT
Definition
satolol
amiodarone
Term
2 drug only used for SVT
Definition
adenosine
Term
Procanamide: type, MOA, use
Definition
1A
block Na and K
ventricular arrhythmia
Term
lidocainel type, moa, use
Definition
1B
BB
ventricular arrhythmia
Term
satolol: type, MOA, use
Definition
3
block K and BB
any arrhythmia
Term
amioderone: type, MOA, use
Definition
3
block Na, K, Ca, BB
any arrhythmia
Term
SE procanamide 2
Definition
lupus in slow acetylators
torsades
Term
SE of sotalol
Definition
torsades
Term
SE amiodarone4
Definition
torsades - low risk
liver damage
pulmonary fibrosis
thyroid problems - due to iodine
Term
MOA adenosine
Definition
stimulate adenosine receptors (Gi coupled so still inhibitory(
short half life 8s
Term
2 Na channel blocker anti convulsants
Definition
phenytoin
carbamazepine
Term
MOA lamotrigine
Definition
Na channel blocker
glutamate inhibitor
Term
MOA ethosuxamide
Definition
block T type Ca channels
Term
MOA lerazepam
Definition
status epilepticus
Term
SE phenytoin 4
Definition
teratogenic
gingival hyperplasia
p450 inducer
zero order kinetucs
Term
SE carvamazepine 2
Definition
teratogenic
p450 inducer
Term
SE valproic acid 3
Definition
liver problems
hyperammonemia
teratogenic
Term
use ethosuxamide
Definition
absence seizure
Term
use lorazepam
Definition
status epilepticus
Term
use lamotrigine
Definition
most seizures
Term
SE lamotrigine
Definition
DC if any sign of rash could be SJS
Term
3 opioids
Definition
morphine
meperidine
buprenorphine
Term
MOA morphine
Definition
mu agonist
Term
MOA merperidine
Definition
mu agonist
Term
MOA burenophine
Definition
Mu partial agonist
Term
signs of morphine OD 4
Definition
meiosis
depressed respiratory - fatal
decreased GI/GU
gall bladder spasms
Term
SE meperidine 2
Definition
decreased respiration
serotonin syndrome
Term
SE buprenorphine
Definition
when you put it with a full Mu agonist it causes withdrawl
Term
MOA naloxone
Definition
mu antagonist
IV antidote to quickly reverse opioid action
Term
MOS sumatriptan
Definition
5HT1D agonist
vasoconstriction
Term
use sumatriptan
Definition
acute migraine
Term
how much of poo is warer
Definition
70-85%
Term
how many liters can the colon absorb max, how much on averate
Definition
50L max, average 100mL
Term
how many liters can the SI absorb
Definition
16
Term
what is the explain on why diarrhea and constipation occur
Definition
when there is not enough fluid (<100mL) reabsorption takes it all up causing constipation

when there is too much fluid >50L then the colon can't take it up causing diarrhea
Term
define diarrhea
Definition
excess fluid weight of stool >200g/d
Term
causes of diarrhea 5
Definition
retention of water in lumen
excessive secretion of electrolytes and water into lumen
exudation of protein and fluid from mucosa
altered intestinal motility
rapid transit
Term
sudden onset diarrhea complications 2 and prognosis
Definition
dehydration
electrolyte imbalance esp in kids and elderly
benign and self limiting
Term
what is the general treatment for sudden onset diarrhea
Definition
solution with K, Na, Cl, glucose
Term
when should pharmacotherapy be used in diarrhea 5
Definition
when symptoms persistant
nonspecific antidiarrheal agents do not adress cause
symptomatic relief in mild diarrhea
need to decrease intestinal motility
avoided in acute diarrhea caused by invasive organisms (could delay clearance)
Term
what are the intraluminal antidiarrheals 5
Definition
Kal Lin does meth on cellulose paper in many cars. he chose to try, its his business
kaolin
methycellulose
polycarbophil
cholestyramine
bismuth subsalicylate
Term
what are the opioid antidiarrheals
Definition
he lopped a dop of pares then gourged
loperamide
dophenoxylate
paregoric
Term
what is the somatostatin analalog antidiarrhea
Definition
it too 8 tides for his diarrhea to stop
octreotide
Term
MOA kaolin
Definition
clay that binds water and some enterotxins
Term
USE kaolin
Definition
symptomatic relief of mild diarrhea
Term
MOA methylcellulose/polycarbophil
Definition
absorb water and increase stool bulk, poorly fermented
effect takes 1-3d
Term
USE and contrindications of methylcellulose/polycarbophil 2
Definition
constipation, chronic diarrhea IBS
contraindicated in patients with obstructive symptoms
Term
cholestyramine MOA
Definition
anion exchange resin that binds bile acids and some bacterial toxins
Term
cholestyramine use 3
Definition
resection of distal ileum <100cm salt induced diarrhea
diarrhea caused by clindamycin
clostridium difficile colitis
Term
why cant cholestyramine be used for ieal resection salt induced diarrhea >100cm
Definition
drug aggrevates diarrhea because of evuntal bile salt deplation causing setaorrhea
Term
how does cholestyramine help with resection of distal ileum <100cm salt induced diarrhea
Definition
interrupts enterohepatic circulation of bile salts increasing concentrations and stimulating water and eletrolyte secretion
Term
bismuth subsalicylate composition 3
Definition
trivalent bismuth
salicylate
MgAl salicate clay
Term
bismuth subsalicylate MOA
Definition
reacts with HCl in stomach to make bismuth oxychloride and salicylic acid (which is absorbed in stomach)
bismuth oxychloride passes unaltered into feces and stops inflammation, microbes, secretion, nausea, cramps
Term
bismuth subsalicylate use 4
Definition
non syndromic episodic diarrhea
TX and prevention of travelers diarrhea
H. pylori infection
Term
bismuth subsalicylate SE
Definition
dark black stool and tongue due to reaction of drug and sulfides made by bacteria in mouth
Term
how do opioids affect diarrhea
Definition
Mu receptor induces intestinal motility
delta receptor induces intestinal secretion
Mu and delta receptors both induce absorption
diarrhea is most affected by Mu receptors
Term
loperamide potency and distribution
Definition
antidiarrheal 50x more potent that morphine
does not penetrate CNS (some does in kids) preventing abuse
Term
loperamide use 3
Definition
chronic diarrhea diseases
travelers diarrhea
occasional bout of diarrhea
Term
dophenoxylate potency and related drug
Definition
slightly more potent antidiarrheal than morphine
drug and metabolite structurly related to meperidine
Term
dophenoxylate SE
Definition
CNS effects potential for abuse and addiction
atropine added to discourage abuse and deliberate OD
Term
paregoric: composition and use
Definition
camphorated tincture of opium
rarley used due to addiction potential
Term
octerotide use
Definition
inhibit secretory diarrhea caused by hormone secreting tumors (usually VIP in carcinoid syndrome) of pancreas and GI
Term
4 functions of the colon
Definition
solidify, store, and evacuate stool
absorb water
Term
what determines the eficiency of the colon 4
Definition
luminal contents
integrity of colon
absorption
neuromuscular action
Term
define constipation 4
Definition
stool <3x/wk, difficulty initiating poo, small poo, incomplete pooing
Term
define chronic constipation
Definition
defect in common motility (NMJ at rectoanal region)
Term
5 reversible or secondary causes of constipation
Definition
lack of dietary fiber, drugs, hormone disturbances, neurogenic disorders, systemic illness
Term
what are the two sources of fiber and their effects
Definition
wheat and branL high lignin, most effective at increasing stool weight

fruits/veggies: pectins/hemicellyloses, more fermentable, adds less weight
Term
MOA of fiber
Definition
affects bulk, softness, and hydration of feces
resistant to enzyme digestion (fermentation)
enters colon unchanged
attracts water and increases stool bulk
Term
fiber drugs
Definition
psh your silly doing meth on cellulose paper in many cars
psyllium
methylcellulose
Term
psyllium husk MOA
Definition
hydrophillic mucilloid that is fermented in colon increasing colonic bacterial mass
Term
3 stool wetting agents and emollients
Definition
the document stated, the document stated use mineral oil, Na, Ca
docusate sodium
docusate calcium
mineral oil
Term
MOA docusate Na and docusate Ca
Definition
stool softener
anionic surfactant that lowers surface tension of stool allowing mixing of aquous and fat softening stool
Term
use docusate Na and docusate Ca
Definition
marginal effects on constipation
Term
mineral oil MOA and administration
Definition
penetrates and softens stool, take for 2-3d
Term
mineral oil SE 4
Definition
may interfere with absorption of water and fat soluble substances
foreign body reaction in mucosa
leakage of oil
Term
what are the osmotically active laxatives 3
Definition
saline laxatives: Mg sulfate, Mg citrate, Na phosphate
Term
MOA saline laxatives, administration
Definition
cathartic action due to osmotically mediated water retention which stimulates peristalsis
effective in 1-3h
Term
saline laxatives: use 3
Definition
evacuation of bowel
before exams
eliminate parasites
Term
saline laxatives 5 contraindications
Definition
avoid in renal damage, CV disease, electrolute imbalance, with diuretics
Term
what are the nondigestable sugar alcohols 2
Definition
glycerin
lactulose
Term
glycerin: MOA
Definition
trihydeoxy alcohol absorbed orally and acts as hygroscopic agent and libricant when given rectally
water retention stimulates peristalsis and cause bowel movement in <1h
Term
define inflammatory bowel disease
Definition
diseases affecting SI and LI caused by chronic inflammation without a cause
thought to be caused by putative antigen in genetically susceptible patient
inflammatory response mediated by cytokines, ROS, leukotrienes
Term
ulcerative colitis: location, depth
Definition
continous, in colon
superificial
Term
chrons disease: location, depth, complications 2
Definition
small and large bowel, segmental
all wayers
abscess, fistulae
Term
signs of inflammatory bowel disease 6
Definition
diarrhea
ulceration
exudate
protein loss enteropathy
bleeding
malabsorption
Term
treatment of complex inflammatory bowel disease
Definition
unknown inciting agent
chronic variable nature of inflammation
needs to incorporate variations in pharmacokinetics of drugs related to patient (genetic composition, age, severity of disease)
Term
goals of IBD treatment 5
Definition
relieve symptoms
induce remission of active disease
prevent relapse with maintenance therapy
heal fistulae
avoid emergency surgery
Term
categories of drugs that treat IBD 4
Definition
5-aminosalicylates
glucacorticoids
immune supression
biological response modifers
Term
5-aminosalicylates 2
Definition
(jamie) was messy and lame and took sulfa
mesalamine
sulfasalazine
Term
2 glucacorticoids
Definition
(pH)
prednisone
hydrocortisone
Term
3 immune supressors
Definition
i was doing meth while trecking on my cycle at the prince (concert)
methotrexate
cyclosporine
asathioprine
Term
1 biological response modifier
Definition
in the flick i got mad b/c my BF wouldnt stop binding me
infliximab
Term
mesalamine: MOA 2
Definition
inhibits COX
stops ROS
Term
mesalamine: use 2
Definition
mild to moderate UC
chronic UC prophylaxis
Term
mesalamine: SE 4
Definition
minor: headache, GI, rash
serious: nephrotoxicity (rare)
Term
sulfasalazine: MOA
Definition
conjugate of mesalamine diazo bonded to sulfapyridine
bacterial azoreductases in colon split into components
MOA is of masalamine, sulfapryridine has minor role
AZO bond prevents early absorption of aminosalicylate in SI
Term
sulfasalazine: use
Definition
acute to moderate UC
UC prophlyaxis
Term
sulfasalazine: SE 7
Definition
sulfapyridine causes fever, malaise, GI, megaloblastic anemia (give folate) agranulocytosis, SLE, SJS

additional SE of mesalamine
Term
use of prednisone in IBD 2
Definition
UC remission 90%
chrons remission 60-90%
Term
hydrocortizone use and administration in IBD
Definition
severe IBD
enema or rectal
Term
cyclosporine: MOA 2
Definition
inhibit calcineurin
supress proinflammatory TF
Term
cyclosporine: use
Definition
when glucacortioids dont work for remission of UC or chrons episode (80% effective, no prophylaxis)
Term
azathioprine: MOA
Definition
converted to 6-mercaptopurine, supresses lymphocytes
Term
azathioprine: onset time
Definition
slow 3-6mo
Term
azathioprine: use 2
Definition
reduce need for steroids
maintain serious UC and chrons
Term
infliximab: MOA
Definition
Ig binds TNF and neutralizes it
Term
infliximab: use 2
Definition
severe chrons tx
heal fistula in chrons
Term
where are H1 and H2 receptors located
Definition
H1 everywhere
H2 on parietal cells
Term
what kind of receptor are H1 receptors on endothelium
Definition
Gq pathway with cGMP and NO
Term
how come the histamine causes vasodilation and vasoconstriction
Definition
on endothelium histamine releases NO which vasodilates. histamine has a higher affinity for endothelium

on vessel smooth muscle histamine causes constriction but because there is a high affinity for the endothelial cells this does not play a part
Term
what is the difference between the first and second generation histamine antagonists
Definition
1. crosses BBB, anticholinergic, more useful in nausea and motion sickness, atropine like SE

2. does not cross BBB, no anticholinergic activity, expensive
Term
what are the 4 2nd gen histamine antagonists
Definition
loratadine
desloratadine
cetirizine
fexofenadine
Term
what are the steps for asthma treatment
Definition
1. SABA PRN
2. ICS + SABA PRN
3. LABA + ICS + SABA PRN
4. increase LABA dose
5. systemic steroid + SABA PRN
Term
throphylline MOA
Definition
inhibits PGE III in lung smooth muscle to relax bronchi
inhibits PDEIV in inflammatory cells preventing cytokine release
blocks adenosine (bronchoconstrictor)
Term
throphylline SE and why
Definition
PGE III stops break down of cAMP. inhibition increases cAMP in heart causing arrhythmia

increase with P450 inhibitors

low theraputic index
Term
TX exercise induced asthma
Definition
SABA prophylaxis
Term
COPD treatment steps
Definition
1. SABA + long acting M blocker (tiotropium)
2. other bronchodilator (theophylline)
3. ICS (not main strategy)
Term
2 drugs used for smoking cessation and their MOA
Definition
buproprion
verenicilne: N partial agonist prevents binding and blocks release of dopamine in mesolimbic tract stopping reinforcement of dopamine (SE: nausea, suicide)
Term
4 things only aspirin does (or is more likley to do)
Definition
more likley to cause hyperuricemia or gout than other NSAID

decreased platelet aggregation

cause 1st OD signs of tinnutis and hearting loss

respiratory and metabolic acidosis more likley
Term
how does aspirin cause antiplatelet activity
Definition
TXA2 is on platelet and increases aggregation. PGI2 is on endothelium and decreases aggregation. Both are released by COX

aspirin stops COX which decreases both but PGI2 just regenerates because endothelium has nuclei, plateles dont
Term
what are 2 things that all NSAIDS cause that people mistake fore being only aspirin
Definition
increase gastric acid and decrease mucous causing ulcers and hemorrhage

hypersensitivity and asthma
Term
indomethecan: uses
Definition
antiinflammatory: gout, arthritis, ankylosing spondylitis, osteoarthritis, acute shoulder
tocolytic agent to supress uterine contraction
CLOSE PDA
OK WITH GERD!!
Term
indomethecan: SE
Definition
GI complaints
severe frontal headaches
SERIOUS MARROW SUPRESSION: NEUTROPENIA, THROMBOCYTOPENIA, APLASTIC ANEMIA
Term
what drug is a COX2 inhibitor, how is it different than the COX1
Definition
celecoxib
specific to anti inflammatory
less GI issues
do not inhibitor platelet aggregation
Term
MOA acetaminophen
Definition
analgesic and antipyretic (NOT ANTIINFLAMMATORY SO NOT NSAID)

inhibits COX in CNS ONLY NO PERIPHERAL SO NO AFFECT ON PLATELETS, BLEEDING TIME, ASTHMA, EXCRETION OF URIC ACID
Term
MOA acetaminophen OD
Definition
INCREASED NAPQI DEPLETES HEPATIC GLUTATHIONE AND IT IS NOT DEGRATED BY SULFHYDRYL GROUP OF GLUTATHIONE LEADING TO HEPATIC NECROSIS
Term
acetaminophen OD antidote MOA
Definition
N-acetylcystine
HAS SULFHYDRYL LIKE GLUTATHIONE AND BINDS NAPQI AND DEGRADES IT (give within 10h)
Term
what receptors do we want to block 4 and stimulate 1 to help with nausea and vomiting
Definition
block: 5HT3, D2, M1/H1 (because the antihistamine gen 1 do both)

stimulate: CB1
Term
loperamide distribution
Definition
does not penetrate CNS (some does in kids) so it is OTC and has no abuse potential
Term
dophenoxylate distribution
Definition
CNS effects, potential for abuse and addiction
atropine is added to discourage abuse and deliberate OD
Term
what drugs are used to tx complex or severe IBD
Definition
immune supressors
cyclosporine
azothoromine
methotrexate
infliximab
Term
mesalamine: MOA, where does it effect
Definition
inhibits COX, stops ROS
effects ENTIRE GI
Term
sulfalazine: MOA, where does it effect
Definition
conjugate of mesalamine diazo bonded to sulfapyridine

bacterial azoreductases in colon split it into components

then mazalamine does it normal thing

ONLY WORKS IN THE COLON
Term
3 immune supressing agents and thier MOA
Definition
cyclosporine: inhibit calcineurin, supress inflammatory TF

azathioprine: converted to 6-mercaptopurine, supresses lymphocytes

methotrexate: cytotoxic, immune supression, antiinflammatory
Term
Infiximab MOA
Definition
Ig binds TnF and neutralizes it
Term
SE cimetadine
Definition
P450 inhibitor: potentiates effects of wararin, diazepam, phenytoin, quinidine, carbamazepine, throphylline, imipramine

antiandeogenic: decreases production and blocks receptor causing glyecomaztia
Term
antibiotics that tx H. pylori
Definition
metronixazole
clathromycin
amoxicillin
tetracycline
Term
why cant you take meds within 2h of antacids
Definition
affect absorption of other drugs because they raise pH of stomach, bicarb alkalinizes urine
Term
what does general anesthesia supres
Definition
reversible loss of sensation and consciousness: analgesia, amnesia, LOS, relax skeletal muscle, somatic, autonomic, endocrine reflexes, hemodynamic stability
Term
what are three things that affect transfer of drug from machine to alveoli
Definition
inspired PP
alveolar ventilation
characteristics of the breathing system
Term
what are three things that effect the transfer of drug from alveoli to arteriole
Definition
blood bas partition coefficient
cardiac output
alveolar to venous PP difference
Term
what are three things that affect transfer of drug from arterial blood to brain
Definition
brain blood partition coefficient
cerebral blood flow
arterial to venous PP difference
Term
how does the PP of a anesthetic change its effect in a person
Definition
it is proportional to fractional concentration of the mixture

increased amount dissolved (solibility) decreases partial pressure in solution

driving force that moves gas from machine to lung, lung to blood, blood to brain

at equlribium PP are equal in all body tissues, alveoli, inspired mixture
Term
how does solubility of a anesthetic change its effect in a person
Definition
blood gas partition coefficient: relationship between arterial PP and solubility

higher solubility means more dissolved and less PP of gas

more dissolved (water soluble) means faster distribution but slower induction

lipid soluble means slow distribution but fast induction into tissue
Term
how is alveolar ventilation of anesthetic calculated
Definition
= RR x (TV - dead space) x rate of drug induction
Term
why do we care about alveolar ventilation of anesthetic
Definition
more dead space means that same drug gets to lung less in some people

it is adjusted in respiratory depressants (opioids, barbs), pulmonary disease, emphysema, COPD
Term
what is the law of mass action
Definition
initially at alveoli PP of anesthetic is higher than alveolar blood so gas move sinto PP and PP in blood increases and as gradient lessens it slows
Term
how does changes in cardiac output effect inhaled anesthetics
Definition
CO determines pulmonary flow, increased pulmonary flow decreases induction of anesthetic

same volume of gas from alveoli diffuse into larger volume of blood per time

initially reduced concentration in blood and PP is proportional to its concentration

any increase in CO means more perfusion to tissues other than the brain
Term
what does increase in anesthetic concentration, alveolar ventilation, solubility of anesthetic, and CO do to rate of induction
Definition
concentration: increases
ventilation: increases
solubility: decreases
CO: decreases
Term
what actions of the drug in the body determine potency of general anesthetic
Definition
concentration in the brain
correlates with lipid solubility
Term
what is the minimum alveolar concentration
Definition
expression of potency of inhaled anesthetic
concentration that prevents 50% from responding to painful stimuli like incision

range for surgery 1-2
MAC 1.3 gives ED99
Term
what is the volume of expansion theory
Definition
molecules of drug dissolve in lipid bilayer causing neuronal membrane to expand stopping ion channels and propagation of AP

specific receptor binding on GABAa

NO effect on Cl channel like BDZ and barbs
Term
6 inhaled general anesthetics
Definition
no one deserves seven isolated halos en florance
nitrOUS oxide
desflurane
sevoflurane
isoflurane
halothane
enflurane
Term
inhaled general anesthetic most commonly used
Definition
isoflurane
Term
inhaled general anesthetic not able to be used alone in surgery
Definition
nitrous oxide
Term
inhaled general anesthetic often delivered with opioids or volitale anesthetics
Definition
nitrous oxide
Term
nitrous oxide: potency and why
Definition
low lotency, poor blood solubility
allows rapid achievement of alveolar to brain PP of lung
Term
nitrous oxide SE 3
Definition
not flamable but can support combustion
minimal skeletal muscle relaxation
inhaled anesthetics are addictive
considered safest
Term
halothane SE 8
Definition
low incidence of toxic effects, not flammable

rapid awakening

low margin of safety: circulatory depression, decreased CO, hypotension, bradycardua

halothane hepatitis: hepatic failure and death due to metabolism of immunologic biproducts

releases bromide

malignant hypothermia with succinylcholine (TX dantrolene)
Term
isoflurane SE 3
Definition
decreased BP due to decreased vascular tone

no renal of hepatic metabolism

irritating to airway
Term
enflurane SE 3
Definition
significant release of fluoride with prolonged use and high doses

seizure with high doses

less proability of arrhythmia
Term
sevoflurane SE 3
Definition
less irritating to airway

no tachycardia (preferred in pt prone to MI)

potential nephrotoxicity due to compound A: degradation made by sevofluraine, CO2, and sodalime
Term
desflurane SE 1
Definition
laryngeal spasm: not indicated for inhalation induction

special delivery system to make liquid at room temp
Term
why use IV anesthetic over inhaled
Definition
add flexability and permit administration of lower concentrations of inhaled agents
Term
drugs used as IV anesthetics 7
Definition
barbituates
benzos

kit, amy, e tom dated droned pairs of dolls on fentanyl and propfol
ketamine
etomidate
doperidol
fetanyl
propfol
Term
barbs used in IV anesthetics 2
Definition
thios penpal sent him meth in a hexagon envelope
thiopental
methohexital
Term
benzos used for IV anesthetics 1
Definition
mydalzing lamb had no pain
midazoloam
Term
barb as IV anesthetic: 1 good 1 bad
Definition
sedation
poor analgesia, may increase response to pain
Term
benzos as IV anesthetic: use, effects
Definition
midazoloam is only one used in anesthesia
other benzos provide anesthesia without analgesia and can only be used in procedures with little pain or adjunct to inhaled anesthetic
Term
doperidol and fentanul: use, SE
Definition
neuroleptic anesthesia
slow induction
may need ventilation
Term
ketamine MOA 2
Definition
opioid sigma agonist
NMSA antagonist
Term
ketamine SE
Definition
dissociative amnesia: dissociation from enivornment (eyes open, unresponsive to pain)

analgesia
amnesia
hallucinations
bad dreams
delirium: days to weeks later

increased ICP: do not use in cerebral ischemia risk pt

potent bronchodilator: good for patients with bronchospasm risk
Term
propofol: MOA, use, SE 2
Definition
interacts with GABAa receptors

rapid redistribution and elimination for short procedures and out patient surgery

low nausea and vomiting
pain on ijection
Term
etomidate: MIA, SE 2
Definition
interacts with GABAa receptors
high incidence of myclonus
pain on injection
Term
what does general anesthesia supres
Definition
reversible loss of sensation and consciousness: analgesia, amnesia, LOS, relax skeletal muscle, somatic, autonomic, endocrine reflexes, hemodynamic stability
Term
what are three things that affect transfer of drug from machine to alveoli
Definition
inspired PP
alveolar ventilation
characteristics of the breathing system
Term
what are three things that effect the transfer of drug from alveoli to arteriole
Definition
blood bas partition coefficient
cardiac output
alveolar to venous PP difference
Term
what are three things that affect transfer of drug from arterial blood to brain
Definition
brain blood partition coefficient
cerebral blood flow
arterial to venous PP difference
Term
how does the PP of a anesthetic change its effect in a person
Definition
it is proportional to fractional concentration of the mixture

increased amount dissolved (solibility) decreases partial pressure in solution

driving force that moves gas from machine to lung, lung to blood, blood to brain

at equlribium PP are equal in all body tissues, alveoli, inspired mixture
Term
how does solubility of a anesthetic change its effect in a person
Definition
blood gas partition coefficient: relationship between arterial PP and solubility

higher solubility means more dissolved and less PP of gas

more dissolved (water soluble) means faster distribution but slower induction

lipid soluble means slow distribution but fast induction into tissue
Term
how is alveolar ventilation of anesthetic calculated
Definition
= RR x (TV - dead space) x rate of drug induction
Term
why do we care about alveolar ventilation of anesthetic
Definition
more dead space means that same drug gets to lung less in some people

it is adjusted in respiratory depressants (opioids, barbs), pulmonary disease, emphysema, COPD
Term
what is the law of mass action
Definition
initially at alveoli PP of anesthetic is higher than alveolar blood so gas move sinto PP and PP in blood increases and as gradient lessens it slows
Term
how does changes in cardiac output effect inhaled anesthetics
Definition
CO determines pulmonary flow, increased pulmonary flow decreases induction of anesthetic

same volume of gas from alveoli diffuse into larger volume of blood per time

initially reduced concentration in blood and PP is proportional to its concentration

any increase in CO means more perfusion to tissues other than the brain
Term
what does increase in anesthetic concentration, alveolar ventilation, solubility of anesthetic, and CO do to rate of induction
Definition
concentration: increases
ventilation: increases
solubility: decreases
CO: decreases
Term
what actions of the drug in the body determine potency of general anesthetic
Definition
concentration in the brain
correlates with lipid solubility
Term
what is the minimum alveolar concentration
Definition
expression of potency of inhaled anesthetic
concentration that prevents 50% from responding to painful stimuli like incision

range for surgery 1-2
MAC 1.3 gives ED99
Term
what is the volume of expansion theory
Definition
molecules of drug dissolve in lipid bilayer causing neuronal membrane to expand stopping ion channels and propagation of AP

specific receptor binding on GABAa

NO effect on Cl channel like BDZ and barbs
Term
6 inhaled general anesthetics
Definition
no one deserves seven isolated halos en florance
nitrOUS oxide
desflurane
sevoflurane
isoflurane
halothane
enflurane
Term
inhaled general anesthetic most commonly used
Definition
isoflurane
Term
inhaled general anesthetic not able to be used alone in surgery
Definition
nitrous oxide
Term
inhaled general anesthetic often delivered with opioids or volitale anesthetics
Definition
nitrous oxide
Term
nitrous oxide: potency and why
Definition
low lotency, poor blood solubility
allows rapid achievement of alveolar to brain PP of lung
Term
nitrous oxide SE 3
Definition
not flamable but can support combustion
minimal skeletal muscle relaxation
inhaled anesthetics are addictive
considered safest
Term
halothane SE 8
Definition
low incidence of toxic effects, not flammable

rapid awakening

low margin of safety: circulatory depression, decreased CO, hypotension, bradycardua

halothane hepatitis: hepatic failure and death due to metabolism of immunologic biproducts

releases bromide

malignant hypothermia with succinylcholine (TX dantrolene)
Term
isoflurane SE 3
Definition
decreased BP due to decreased vascular tone

no renal of hepatic metabolism

irritating to airway
Term
enflurane SE 3
Definition
significant release of fluoride with prolonged use and high doses

seizure with high doses

less proability of arrhythmia
Term
sevoflurane SE 3
Definition
less irritating to airway

no tachycardia (preferred in pt prone to MI)

potential nephrotoxicity due to compound A: degradation made by sevofluraine, CO2, and sodalime
Term
desflurane SE 1
Definition
laryngeal spasm: not indicated for inhalation induction

special delivery system to make liquid at room temp
Term
why use IV anesthetic over inhaled
Definition
add flexability and permit administration of lower concentrations of inhaled agents
Term
drugs used as IV anesthetics 7
Definition
barbituates
benzos

kit, amy, e tom dated droned pairs of dolls on fentanyl and propfol
ketamine
etomidate
doperidol
fetanyl
propfol
Term
barbs used in IV anesthetics 2
Definition
thios penpal sent him meth in a hexagon envelope
thiopental
methohexital
Term
benzos used for IV anesthetics 1
Definition
mydalzing lamb had no pain
midazoloam
Term
barb as IV anesthetic: 1 good 1 bad
Definition
sedation
poor analgesia, may increase response to pain
Term
benzos as IV anesthetic: use, effects
Definition
midazoloam is only one used in anesthesia
other benzos provide anesthesia without analgesia and can only be used in procedures with little pain or adjunct to inhaled anesthetic
Term
doperidol and fentanul: use, SE
Definition
neuroleptic anesthesia
slow induction
may need ventilation
Term
ketamine MOA 2
Definition
opioid sigma agonist
NMSA antagonist
Term
ketamine SE
Definition
dissociative amnesia: dissociation from enivornment (eyes open, unresponsive to pain)

analgesia
amnesia
hallucinations
bad dreams
delirium: days to weeks later

increased ICP: do not use in cerebral ischemia risk pt

potent bronchodilator: good for patients with bronchospasm risk
Term
propofol: MOA, use, SE 2
Definition
interacts with GABAa receptors

rapid redistribution and elimination for short procedures and out patient surgery

low nausea and vomiting
pain on ijection
Term
etomidate: MIA, SE 2
Definition
interacts with GABAa receptors
high incidence of myclonus
pain on injection
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