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177 Cards in this Set

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Zileuton
5-LOX inhibitor (for ashtma)
zafirlukast
LTD4, LTE4 antag
methylxanthines
- for asthma (bronchodilator) by:
- block adenosine
- inhibit phosphodiesterase
- other effects like caffeine (since caffeine is one... incr. HR, incr. alert, incr. gastric acid + pepsin, conulsions and arrhythmia at high doses, etc.)
- removed by CYP 450 in liver; drug interactions bad because low therapeutic range
xanthine oxidase
- makes uric acid (gout)
diphenhydramine
- H1 antag (1st gen)
- dry mouth (anticholinergic)
phenothiazines
- H1 antag (1st gen)
- also block seretonin and Epinephrine
chlorpheniramine (like diphenhydramine))
- H1 antag (1st gen)
Loratidine
- H1 antag (2nd gen)
cetirizine
H1 antag (2nd gen)
dimenhydrinate
- gravol (h1 antag)
cimetidine
- H2 antag
- inhibits CYP P450
ranitidine
- H2 antag
famotidine
- H2 antag
serotonin is made from what aa?
tryptophan
NE and E made from which aa?
tyrosine
enterochromaffin-like cells hold what?
histamine
enterochromaffin cells hold what?
serotonin
sumatriptan
5HT1 agonist (for migrane)
Ondansetron
- 5HT3 antag (antiemetic)
cisapride
(hard)
- 5HT4 agonist (incr. GI motility)
tubocurarine
- displaces histamine from heparin binding sites in granules, along with morphine
- neuro muscular inhibitor
cromolyn
stop mast degranulation
urticaria
hives
bromocriptine
- stimulates dopamine / dopamine agonist
- inhibits prolactin
dopamine inhibits what hormone?
prolactin
ergot alkaloids are agonists for what receptors?
5HT, dopamine, alpha
SRS-A contains what?
- slow reacting substances of anaphylaxis
- LTC4, E4, D4
indomethacin
- indole derivative
- potent cyclooxygenase inhibitor
- lots toxicities to it (headache, nausea, psychoses, ulcers, thrombocytopenia, aplastic anemia, confusion, depression)
- (used to close ductus arteriosus)
misoprostol
- PGE analog
- stop stomach secretions (acid, etc.)
- give with arthritis drugs (when inhibit PG) so won't get ulcers
- causes diarrhea
leuteolytic effect
- regression of corpeus leutium (from PGF2a effects)
glucocorticoid
- stimulate synthesis lipocortin -> inhibit phospholipase
- decrease AA -> decrease eicosenoids
lipocortin
- stimulated by glucocorticoid
- inhibit phospholipase (therefore AA)
celecoxib
celebrex (cox II inhib)
rofecoxib
vioxx (cox II inhib)
ETYA
- like AA, but triple bonds (so inhibit lipooxygenase, maybe cyclo too?)
- lipid soluble, so sucked up into random places, doesn't work in vivo
FLAP
5-lipooxygenase activating protein
montelukast
(hard)
Leukotriene inhibitor
- tradename singulair
ASA is bad for people with what 3 conditions?
- ulcers (because incr. acid in stomach)
- asthma (bronchconstriction, etc.)
- renal failure (PG reliant)
aryl propionic acid derivatives
NSAIDs like ibuprofin, naproxin
naproxin
like ibuprofin, but t1/2 = 14h instead of 2-6
DMARDs
Disease Modifying Anti Rhumetic Drugs
(aka - SAARDs - slow acting...)
hydroxychloroquine
- a DMARD
- antimalarial
- ototoxicity and ocular toxicitity (retinopathy)
teratogenicity
- birth defects
stomatitis
swelling of oral mucosa
methotrexate
immunosuppressive drug (a DMARDs)
- causes stomatitis, teratogenicity, and GI defects
TNF-a
proinflammatory cytokine
IL-1
proinflammatory cytokine
infliximab
monoclonal antibody to TNFa
etanercept
- bind 2 TNFa
- increase chance Tb
sodium urate crystals are the problem in...
gout
colchicine
- stop migration of MTs in granulocytes, inhibiting migration
- for gout
allopurinol
- inhibit Xanthine Oxidase
- forms alloxanthine, which also inhibits
uricosuric drugs
- decrease urate reabsorption in proximal tuble (for gout)
probenecid
uricosuric drug
sulfinpyrazone
uricosuric drug
acute (stopping of asthma)
termination of attack
prophylactic (stopping of asthma)
prevention of attack
sodium cromoglycate (cromolyn sodium)
stops mast cell degranulation (asthma)
- with inhaler
beclomethasone
- a glucocorticoid (for asthma)
theophylline
- a methylxanthine (the prototype)
- others are caffeine and theobromine
treatment for infantile apnea
methylxanthines
PSNS predominates: (4 items)
- cilliary muscles
- heart
- salivary glands
- bronchiole smooth muscle
SNS predominates: (2 items)
- sweat glands
- veins and arterioles
sweat glands have what type of receptor?
muscarinic (even though SNS)
renal vascular smooth muscle has what type of receptor?
dopamine (even though SNS)
hemicholinium
stops uptake of choline (with Na)
choline acetyl transferase
makes ACh from choline and AcCoa
vesamicol
inhibits transport of ACh into vesicles
tyrosine hydroxylase
- tyrosine -> DOPA
- rate limiting step of NE formation
aromatic a.a. decarboxylase
DOPA -> dopamine
dopamine-B hydroxylase
- dopamine -> NE
- in vesicle
metyrosine
inhibit tyrosine hydroxylase
PNMT
NE -> E (in adrenal medulla)
reserpine
- stops transfer of dopamine into vesicles (for NE)
cocaine
- inhibit reputake of NE
COMT
- catechol-o-methyltransferase
- metabolise NE
MAO
monoamine oxidase
- metabolise NE
atropine
block muscarinic
adrenal medulla has what type of receptor?
Nn
M1 + M3 acts through what second messenger?
- incr. IP3, DAG
- incr. CA, activ. PKC
M2 acts through what second messenger?
- decr. adenylyl cyclase
- decr. CA, open K+
a1 acts through what second messenger?
- incr. IP3, DAG
- incr. CA, activ. PKC
a2 acts through what second messenger?
- decr. adenylyl cyclase
- decr. cAMP dependent PK
B1 + B2 act through what second messenger?
- incr. adenylyl cyclase
- incr. cAMP dependent PK
baroreceptor reflex originates in the...
carotid sinus (and aaortic arch)
phenelzine
MAO inhibitor
mydriasis
- pupil dilation
what SNS receptor controls pupil size?
a1 - contraction of radial pupillary dilatior
what SNS receptor controls ciliary muscle?
b2 - relaxes it
what SNS receptor controls the liver?
B2 - glyconeolysis, gluconeogenesis
what SNS receptor controls the pancreas?
a
what SNS receptor controls fat cells?
B1
ipratropium
- like atropine
- synthetic, quaternary
- muscarinc blocker
- used for asthma (inhibit bronchoconstrict and secretions)
salbutamol
B2 agonist (for asthma)
- with inhaler
- salmeterol (longer acting)
tocolytic
- stops premature labour
phenylephrine
- a1 + a2 agonist
clondine
- a2 agonist (for hypertension)
dobutamine
- b1 agonist (for failing heart)
terbutaline
- B2 agonist (prevent premature labour)
ephedrine
- like amphetamine (release NE)
- used in China
- weak base, excreted in urine
- crosses BBB easily
methylphenidate
- like amphetamine
- for ADHD
tyramine
- amphetamine like
- cheese reaction (with MAO inhibitor)
pheochromocytoma
- catecholeamine secreting tumour of chromaffin tissue (hypertension)
- treat with a and b blockers
phenoxybenzamine
- a1 + a2 antagonist (irreversable)
phentolamine
- a1 + a2 antagonist (competitive)
yohimbine
- a2 antag
- Benign prostatic hypertrophy (BPH)
- use a1 antag
prazosin
- a1 antag (to treat BPH)
tamusolin
- a1 antag
atenolol / metoprolol
- B1 antag
miosis
- contraction of pupils
bethanechol
- M3 (and little M2) agonist
- GI motility
- bladder emptying
pilocarpene
- M3 agonist
- lipid soluble (3o amine)
- for glaucoma
butyrylcholinesterase
- plasma cholinesterase (+ liver, non-neuronal cells)
- hydrolyzes ester containing drugs
myasthenia gravis
- loss of N receptors
- muscle weakness; drooping eyelids, etc.
edrophonium
- reversible, short acting anticholinesterase
- not well absorbed
- diagnose myasthenia gravis
neostigmine
- reversible, medium acting anticholinesterase
- not well absorbed
- treat myasthenia gravis
- anesthtists reverse NMJ blocking drugs
- incr. GI motility, empty bladder
physostigmine
- reversible, mid acting anticholinesterase
- well absorbed
- treat glaucoma topically
parathion
- permanent cholinesterase blocker
- insectiside
- toxic humans - can't remove
malathion
- permanent cholinesterase blocker
- insectiside
ecothiophate
- permanent cholinesterase blocker
- not well absorbed
- treat glaucoma topically
sarin
- permanent cholinesterase blocker
- used in war
alzheimer's is trying what as a drug?
cholinesterase inhibitors
pralidoxime
cholinesterase reactivator
cycloplegia
- no near vision (when you have muscarinic blockers)
muscarinic antag do what to HR?
- first decr. (because loss of negative feedback)
- then incr.
scopolamine
- muscarinic antagonist (lipid soluble)
lobeline
- like nicotine, less potent
- lipid soluble
- both are alkaloids (acidic urine makes excretion easier)
trimethaphan
- ganglionic blocking drug
- used for hypotension in certain anesthetic procedures
hexamethonium
- ganglionic blocking drug
- originally used for hypotension
pancuronium
- neuromuscular blocking agent (longest lasting)
vecuronium
- neuromuscular blocking agent (shortest and fastest)
decamethonium
depolarizing neuromuscular blocking agent
- not succeptable to cholinesterase
succinylcholine
- depolarizing neuromuscular blocking agent
Reyes syndrome
- neurological disorder
- happens when give ASA to kids with fever
tartazine
- yellow food colouring
- allergic to ASA of allergic to this
capsicum
- heat in heat rubs
- in hot peppers
pseudoephedrine
- a agonist (used in cold preparations as decongestant)
phenylpropanolamine
- a agonist (for decongestant)
- not used anymore because caused strokes in young women
dextromethorphan
- cough suppressent
- codeine also works
glyceryl guaiacolate
- an expectorant (in cold medication)
expectorant
- reduce viscosity of septum (supposed to...)
antiseptic
- kills bacteria
- in lozenges / mouthwash
- phenols, benzoic acid, cetylpyridinium chloride
hydrocortisone
- reduce inflammation
- for poison ivy, insect bites
calamine lotion
- for insect bites, poison ivy
- cooling, temporary relief
valerian
- contain valepotriates
- "sedative and hypnotic" (CNS depressant, so interaction with alcohol?)
- placebo
Devil's Claw
- for inflammation
- biotransformmed in gut -> not effective
comefrey
- stimulates cell proliferation
- wound healing
- should not be used internally -> liver injury (people use for ulcers though)
feverfew
- for migranes
- lots of toxicities
- antipyretic, antispasmodic, emmenogogue
-
sesquiterpene lactones (in what herbal?)
(hard)
- in feverfew
ginseng
- adaptogen
- aphrodesiac
- enhances memory, learning, physical stamina, health
- yeah right!
kava
- anti-anxiety
- mild sedative
- problems with alcohol, scaly skin... severe warnings from health canada
warfarin
- anticoagulant
thalidomide
- prevent morning sickness
- in first trimester, has teratogenicity on child
cabachol
- like Ach
- less succeptable to AchE
methacholine
- like Ach
- a bit less Nicotinic activity
- a bit less AchE activity
bromfenac
- NSAID taken off market because of serious hepatotoxicity
carbamazepine
- anticonvulsant
- serious hypersensitivity reactions
hapten
- drug that binds to protein, then can be sensitzed to it (allergic response)
clavulinic acid
- increases effects of penicillin
sulfonamides
- displace methotrexate, phenytoin, and warfarin from albumin (therefore, higher blood conc.)
ethanol, carbamazepine, phenytoin - worry about what when taking these drugs?
incr. effect CYP 450
tetracycline
- antibiotic used for acne
- can't absorb when complex with antacid or Ca
debrisoquine hydroxylase deficiency
CYP 450 2D6 deficiency
- 2D6 metabolizes ecstacy, codeine
S-mephenytoin hydroxylase deficiency
CYP 450 2C19 deficiency (Japanese and Chinese)
NAT (2 types)
N acetyl transferase (Phase 2 rxn)
- NAT1 - broad, in lots tissues
- NAT2 - in specific tissues
isoniazid
- acetylated by NAT
- VB6 deficency when not enough NAT (neuronal toxicity)
thymidylate synthase
dUMP -> dTMP for DNA
- polymorphic - people with 3 (instead of 2) less effective anti-cancer drug
malignant hyperthemia
- when give anesthetic and depolarizing muscle relaxant
- Ca channel problem (stays open to stimulation)
- RYR1 gene - problem in pigs, 50% problem in humans
dimercaprol (BAL)
- chelating agent for bismuth, arsenic, lead, polonium, mercury
- DMSA less toxic (since BAL also toxic)
EDTA
- binds calcium, but lead much better
- chelating agent
oral penicillamine (chealating agent for...)
for copper
deferoxamine
chealating agnet for iron
CN (binds with? to treat (2 ways))
ferric iron (Fe3+) - use nitrile
- thiosulfate acts as sulfur source to inactivate
fomepizole
- new alcohol dehydrogenaze inhibitor
to treat bromide poisoning...
give chlorine
methylene blue
- to treat methemoglobinemia
- intermediate electron acceptor from NADPH