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177 Cards in this Set
- Front
- Back
Zileuton
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5-LOX inhibitor (for ashtma)
|
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zafirlukast
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LTD4, LTE4 antag
|
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methylxanthines
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- 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 |
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xanthine oxidase
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- makes uric acid (gout)
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diphenhydramine
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- H1 antag (1st gen)
- dry mouth (anticholinergic) |
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phenothiazines
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- H1 antag (1st gen)
- also block seretonin and Epinephrine |
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chlorpheniramine (like diphenhydramine))
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- H1 antag (1st gen)
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Loratidine
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- H1 antag (2nd gen)
|
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cetirizine
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H1 antag (2nd gen)
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dimenhydrinate
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- gravol (h1 antag)
|
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cimetidine
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- H2 antag
- inhibits CYP P450 |
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ranitidine
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- H2 antag
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famotidine
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- H2 antag
|
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serotonin is made from what aa?
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tryptophan
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NE and E made from which aa?
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tyrosine
|
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enterochromaffin-like cells hold what?
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histamine
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enterochromaffin cells hold what?
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serotonin
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sumatriptan
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5HT1 agonist (for migrane)
|
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Ondansetron
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- 5HT3 antag (antiemetic)
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cisapride
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(hard)
- 5HT4 agonist (incr. GI motility) |
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tubocurarine
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- displaces histamine from heparin binding sites in granules, along with morphine
- neuro muscular inhibitor |
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cromolyn
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stop mast degranulation
|
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urticaria
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hives
|
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bromocriptine
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- stimulates dopamine / dopamine agonist
- inhibits prolactin |
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dopamine inhibits what hormone?
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prolactin
|
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ergot alkaloids are agonists for what receptors?
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5HT, dopamine, alpha
|
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SRS-A contains what?
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- slow reacting substances of anaphylaxis
- LTC4, E4, D4 |
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indomethacin
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- indole derivative
- potent cyclooxygenase inhibitor - lots toxicities to it (headache, nausea, psychoses, ulcers, thrombocytopenia, aplastic anemia, confusion, depression) - (used to close ductus arteriosus) |
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misoprostol
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- PGE analog
- stop stomach secretions (acid, etc.) - give with arthritis drugs (when inhibit PG) so won't get ulcers - causes diarrhea |
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leuteolytic effect
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- regression of corpeus leutium (from PGF2a effects)
|
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glucocorticoid
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- stimulate synthesis lipocortin -> inhibit phospholipase
- decrease AA -> decrease eicosenoids |
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lipocortin
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- stimulated by glucocorticoid
- inhibit phospholipase (therefore AA) |
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celecoxib
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celebrex (cox II inhib)
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rofecoxib
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vioxx (cox II inhib)
|
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ETYA
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- like AA, but triple bonds (so inhibit lipooxygenase, maybe cyclo too?)
- lipid soluble, so sucked up into random places, doesn't work in vivo |
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FLAP
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5-lipooxygenase activating protein
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montelukast
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(hard)
Leukotriene inhibitor - tradename singulair |
|
ASA is bad for people with what 3 conditions?
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- ulcers (because incr. acid in stomach)
- asthma (bronchconstriction, etc.) - renal failure (PG reliant) |
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aryl propionic acid derivatives
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NSAIDs like ibuprofin, naproxin
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naproxin
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like ibuprofin, but t1/2 = 14h instead of 2-6
|
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DMARDs
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Disease Modifying Anti Rhumetic Drugs
(aka - SAARDs - slow acting...) |
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hydroxychloroquine
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- a DMARD
- antimalarial - ototoxicity and ocular toxicitity (retinopathy) |
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teratogenicity
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- birth defects
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stomatitis
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swelling of oral mucosa
|
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methotrexate
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immunosuppressive drug (a DMARDs)
- causes stomatitis, teratogenicity, and GI defects |
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TNF-a
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proinflammatory cytokine
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IL-1
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proinflammatory cytokine
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infliximab
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monoclonal antibody to TNFa
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etanercept
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- bind 2 TNFa
- increase chance Tb |
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sodium urate crystals are the problem in...
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gout
|
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colchicine
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- stop migration of MTs in granulocytes, inhibiting migration
- for gout |
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allopurinol
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- inhibit Xanthine Oxidase
- forms alloxanthine, which also inhibits |
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uricosuric drugs
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- decrease urate reabsorption in proximal tuble (for gout)
|
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probenecid
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uricosuric drug
|
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sulfinpyrazone
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uricosuric drug
|
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acute (stopping of asthma)
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termination of attack
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prophylactic (stopping of asthma)
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prevention of attack
|
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sodium cromoglycate (cromolyn sodium)
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stops mast cell degranulation (asthma)
- with inhaler |
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beclomethasone
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- a glucocorticoid (for asthma)
|
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theophylline
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- a methylxanthine (the prototype)
- others are caffeine and theobromine |
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treatment for infantile apnea
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methylxanthines
|
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PSNS predominates: (4 items)
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- cilliary muscles
- heart - salivary glands - bronchiole smooth muscle |
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SNS predominates: (2 items)
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- sweat glands
- veins and arterioles |
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sweat glands have what type of receptor?
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muscarinic (even though SNS)
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renal vascular smooth muscle has what type of receptor?
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dopamine (even though SNS)
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hemicholinium
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stops uptake of choline (with Na)
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choline acetyl transferase
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makes ACh from choline and AcCoa
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vesamicol
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inhibits transport of ACh into vesicles
|
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tyrosine hydroxylase
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- tyrosine -> DOPA
- rate limiting step of NE formation |
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aromatic a.a. decarboxylase
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DOPA -> dopamine
|
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dopamine-B hydroxylase
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- dopamine -> NE
- in vesicle |
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metyrosine
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inhibit tyrosine hydroxylase
|
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PNMT
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NE -> E (in adrenal medulla)
|
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reserpine
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- stops transfer of dopamine into vesicles (for NE)
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cocaine
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- inhibit reputake of NE
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COMT
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- catechol-o-methyltransferase
- metabolise NE |
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MAO
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monoamine oxidase
- metabolise NE |
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atropine
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block muscarinic
|
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adrenal medulla has what type of receptor?
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Nn
|
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M1 + M3 acts through what second messenger?
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- incr. IP3, DAG
- incr. CA, activ. PKC |
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M2 acts through what second messenger?
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- decr. adenylyl cyclase
- decr. CA, open K+ |
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a1 acts through what second messenger?
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- incr. IP3, DAG
- incr. CA, activ. PKC |
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a2 acts through what second messenger?
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- decr. adenylyl cyclase
- decr. cAMP dependent PK |
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B1 + B2 act through what second messenger?
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- incr. adenylyl cyclase
- incr. cAMP dependent PK |
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baroreceptor reflex originates in the...
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carotid sinus (and aaortic arch)
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phenelzine
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MAO inhibitor
|
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mydriasis
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- pupil dilation
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what SNS receptor controls pupil size?
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a1 - contraction of radial pupillary dilatior
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what SNS receptor controls ciliary muscle?
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b2 - relaxes it
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what SNS receptor controls the liver?
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B2 - glyconeolysis, gluconeogenesis
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what SNS receptor controls the pancreas?
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a
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what SNS receptor controls fat cells?
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B1
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ipratropium
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- like atropine
- synthetic, quaternary - muscarinc blocker - used for asthma (inhibit bronchoconstrict and secretions) |
|
salbutamol
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B2 agonist (for asthma)
- with inhaler - salmeterol (longer acting) |
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tocolytic
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- stops premature labour
|
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phenylephrine
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- a1 + a2 agonist
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clondine
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- a2 agonist (for hypertension)
|
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dobutamine
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- b1 agonist (for failing heart)
|
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terbutaline
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- B2 agonist (prevent premature labour)
|
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ephedrine
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- like amphetamine (release NE)
- used in China - weak base, excreted in urine - crosses BBB easily |
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methylphenidate
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- like amphetamine
- for ADHD |
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tyramine
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- amphetamine like
- cheese reaction (with MAO inhibitor) |
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pheochromocytoma
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- catecholeamine secreting tumour of chromaffin tissue (hypertension)
- treat with a and b blockers |
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phenoxybenzamine
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- a1 + a2 antagonist (irreversable)
|
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phentolamine
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- a1 + a2 antagonist (competitive)
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yohimbine
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- a2 antag
|
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- Benign prostatic hypertrophy (BPH)
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- use a1 antag
|
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prazosin
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- a1 antag (to treat BPH)
|
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tamusolin
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- a1 antag
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atenolol / metoprolol
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- B1 antag
|
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miosis
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- contraction of pupils
|
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bethanechol
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- M3 (and little M2) agonist
- GI motility - bladder emptying |
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pilocarpene
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- M3 agonist
- lipid soluble (3o amine) - for glaucoma |
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butyrylcholinesterase
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- plasma cholinesterase (+ liver, non-neuronal cells)
- hydrolyzes ester containing drugs |
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myasthenia gravis
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- loss of N receptors
- muscle weakness; drooping eyelids, etc. |
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edrophonium
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- reversible, short acting anticholinesterase
- not well absorbed - diagnose myasthenia gravis |
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neostigmine
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- reversible, medium acting anticholinesterase
- not well absorbed - treat myasthenia gravis - anesthtists reverse NMJ blocking drugs - incr. GI motility, empty bladder |
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physostigmine
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- reversible, mid acting anticholinesterase
- well absorbed - treat glaucoma topically |
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parathion
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- permanent cholinesterase blocker
- insectiside - toxic humans - can't remove |
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malathion
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- permanent cholinesterase blocker
- insectiside |
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ecothiophate
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- permanent cholinesterase blocker
- not well absorbed - treat glaucoma topically |
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sarin
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- permanent cholinesterase blocker
- used in war |
|
alzheimer's is trying what as a drug?
|
cholinesterase inhibitors
|
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pralidoxime
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cholinesterase reactivator
|
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cycloplegia
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- no near vision (when you have muscarinic blockers)
|
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muscarinic antag do what to HR?
|
- first decr. (because loss of negative feedback)
- then incr. |
|
scopolamine
|
- muscarinic antagonist (lipid soluble)
|
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lobeline
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- like nicotine, less potent
- lipid soluble - both are alkaloids (acidic urine makes excretion easier) |
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trimethaphan
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- ganglionic blocking drug
- used for hypotension in certain anesthetic procedures |
|
hexamethonium
|
- ganglionic blocking drug
- originally used for hypotension |
|
pancuronium
|
- neuromuscular blocking agent (longest lasting)
|
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vecuronium
|
- neuromuscular blocking agent (shortest and fastest)
|
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decamethonium
|
depolarizing neuromuscular blocking agent
- not succeptable to cholinesterase |
|
succinylcholine
|
- depolarizing neuromuscular blocking agent
|
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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)
|
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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)
|
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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 |