Final Flashcards
____ are H2 receptor antagonists that competitively inhibit H+ secretion by _____ cells
- Tidines ; parietal
_____ irreversibly bind to proton pump and prevennt acid release
PPIs
_______ is a prosaglandin analogue that stimulates _____ cell receptors and ______ cell
misoprostol; parietal; mucus
_______ forms a viscous gel network by binding to broken parts of mucus lining
sucralfate
______ is an opioid that can help diminish propulsive activity to treat diarrhea
loperamide
the hypertension subtype _____ is associated with stiffnness of large arteries and adults > 50
isolated systolic (SBP only)
the hypertension subtype _____ is associated with narrowing or arterioles and adults < 40
isolated diastolic (DBP)
______ Hypertension has no known cause wherase _______ hypertension has an identifiable cause
primary (essential); secondary
(increase or decrease) in angiotensin, aldoseterone, renin is associated with hypertensionn
increase
increase aldosterone –> (increase or decrease) of Na+ and H20 –> (increase or decrease in BV
increase; increase
vasodilator deficiency in hypertension is associated with decreased ______ and _______
NO; prostacyclin
Catopril is an example of an _______that blocks angiotensin II production thus ______ secretion. It also prevents inactivation of bradykinin
ACE inhibitor; aldosterone
Losartan is an an example of an _______ that blocks ______ by blocking the AT1 receptors.
ARBs. ; action of angiotensin II
Hydrochlorothiazide is a thiazide-______ diuretic that prevents reabsorption of ___ and ____ in the ____ tubule by inhibiting the co-transporter
thiaside-type; Na+ and Cl- ; distal
Chlorthalidone and indapamide are thiazide- ______ diuretics that work to decrease ____, _____ and ________
thiazide-like, BV, CO, peripheral resistance
amlodipine is a ___________ that is most vascular selective and is associated with side effects such as headache, flushing and peripheral edema
dihydropyridine
verapamil is a _________ that is most cardiac selective and reduced the calcium influx into cardiac muscle cells.
phenulalkylamine
Dilitazem is a ________ that inhibits voltage gated L-type Ca2+ channels and is associated with bradycardia
benzothiazepine`
G protein coupled receptors for ______ hormones include ____, _____, _____ and are located on the cell surface
peptide; Oxytocin, TSH, FSH
Receptor Tyrosine Kinases include for _____ hormones include ______ and ______ and are located on the cell surface
peptide; insulin receptor, GH
Steroid hormone receptors include … bind to DNA and cause changes in gene expression
glucocorticoid, estrogen, thyroid hormone
What are the two ways to treat hypersecretion
- drug that interferes with synthesis or block the receptor
- remove/ablate with radiation or surgery 1
Short acting bolus insulin is insulin ______ and should be taken 30-60 minutes before meals
regular
fast acting bolus insulin is insulin ______, ________, ______ and should be taken at the start of meals
glulisine, lispro, aspart
Intermediate acting basal insulin is insulin _____ and should be taken at bedtime or twice a day
isphane
long acting basal insulin is insulin ____, _____ is newer and should be taken once or twice a day because it has no peak effect
glargine, detemir
Metformin is an antiglycemic __________ and works by
1. (increase/decrease) _____ gluconeogenesis
2. (increase/decrease) insulin _______
3. (increase/decrease)______ glucose uptake
4. (increase/decrease) _______ net glucose uptake
biguanide
1. decrease hepatic gluconeogenesis
2. increase insulin sensitivity
3. increase muscle glucose uptake
4. reduce net glucose uptake in intesttine
Glyburide is an antidiabetic ________ that works by (increase/decrease) insulin release from beta cells
sulfonylurea; increase
Acarbose is an oral antidiabetic _____________ that works by (increase/decrease) the breakdown of starches and carbohydrates at the brush border of the small intestine
alpha-glucosidase inhibitor; decrease
Rosiglitazone is an ____________ that is a selective agonist for PPAR and (activates or inhibits) the PPARy receptor to regulate transcription of insulin responsive genes
Thiazolidinedione (TZD); activates
Exenatide is an ___________ that binds to GLP-1 on pancreatic beta cells and (increase/decrease) cytosolic calcium –> (increase/decrease) release of insulin-containing granules
incretin mimetic; increase; increase
SABA and LABAs act as _______ receptor (agonist ot antagonist)
B2-adrenergic receptor; agonists
When _______ bind to receptors on smooth muscle,
–> release of ______
—> removal of _____ via channels
—-> ( activation/ inhibition) of myoslin light chain phosphatase
—-> uncouple cross bridge = _____
B2-adrenergic receptor agonists
–> release of cAMP
—> removal of Ca2+ via channels
—-> activation of myosin light chain phosphaase
–> uncouple cross bridge = relaxation
When _____ binds to the glucocorticoid receptor complex
trans-________ prevents translocation of inflammator TF from cytosol –> nucleus and decreases pro-inflammatory cytokines, proteases, ROS
trans-_______ up regulates antinflammatory proteins by binding to ______
Corticosterone
trans-repression prevents translocation of inflammator TF from cytosol –> nucleus and decreases pro-inflammatory cytokines, proteases, ROS
trans-activation up regulates antinflammatory proteins by binding to GRE
Classical psychedelics are 5HT 2A receptor _______
partial antagonists
______ signalinng is excitatory and Gq coupled and involves the Ca2+ regulation of voltage gated channels in the _____. It also has a role in drug tolerance
Canonical; mPFC
______ signalling involves ___ bound receptors for downstream cascades that control cell growth, proliferation and angiogenesis
non-canonical; arrestin
Psychedlics work as ______by blocking the action of _____ involved in the termination of _____ action in the synapse and inhibits reuptake from synapses and reverses flow by monoamine transporters ______ (MDMA)
MOA inhibitors; MOA; 5HT; SERT, DAT
Ketamine is an glutamate ______ antagonist and activates excitatory_______ signalling
NMDAR; AMPAR
MDMA releases ______ and _________ via transporters
serotonin and dopamine
the _______ pathway is also known as the dopamine pathway and goes from the ____ –> _____-
mesocorticolimbic ; VTA –> NAcc
Mu receptor ________ in the VTA (inhibits/stimulates) GABA release –> dopamine = reward
Antagonism; inhibits
respiratory depression occurs as a result of mu receptor _______ in the ________ that interferes with the breathing signal resulting in breathing
antagonism; brainstem
Buprenorphine/naloxone has a (High/low) binding affinity to MOR receptors as a _________
high; partial agonist
Methadone is a ________ at MOR receptors
full agonist
the mesolimbic pathway is associated with _____ symptoms such as delusions, halucinations, disorganized speech and behaviour and catatonic behaviour
positive
the mesocortical pathway is associated with _____ symptoms such as Alogia, anhedonia, affective flattenninng, avoilition, asociality
negative
the nigrostriatal pathway is asssociated with ______
motor movements
the Tuberoinfundibular pathway is associated with ________
prolactin secretion
FGA are D2 _________
antagonists
SGA are 5HT-2A and D2 ______ and _______ for 5HT-1A which increases dopamine release
antagonists; agonists
TGA are D2 _____ and 5HT-2A ________
partial agonists; antagonists
5HT-2A_______ and D2 ________ increase prolactin release
agonism; antagonism
5HT-2A_______ and D2 ________ decrease prolactin release
antagonism; agonism
Risperidone and Paliperidone are examples of _____
SGA
Chlorpromazine and Haloperiodl are examples of _____
FGA
Aripriprazole and Brexpriprazol are examples of _____
TGA
D2 antagonists (FGA and SGA)____-regulate D2 receptors whereas D2 partial agonnists do not
up
______ reduces mortality rate
clozapine
Clozapine is an _____
SGA
Prevalence of disease =
= (# with disease)/ (# with disease + # non-disease)
Ex. number eligible for trial / total screened
Odds =
= Proportion/ (1- proportion)
Proportion =
= Odds/ (1+Odds)
Incidence rate is the instantaneous risk for developping a disease at any point in time and =
= number of cases / # years per person of follow up
Incidence proportion is the proportion of the population that develops the disease during fixed period of follow up annd =
new cases of disease observed during a defined period of follow up)/ N(aka number at risk during the period)
Risk ratio =
= incidence proportion-r / incidence proportion-p
= incidence rate -r / incidence rate - p
Risk difference =
= incidence proportion-r – incidence proportion - p
= incidence rate-r – incidence rate-p
Disease odds ratio =
= [ incidence proportion-r/ (1-incidence proportion-r)] \ [incidence proportion-p\ (1-incidence proportion-p)]
number needed to treat =
NNT = (1/ |RD|)
Clinical research take _____ years and with accelerated approval can be. fastter by ____ years
9 ; 3
the median cost to bring a drug to market is ________
1.1 billion
The overall likelihood of approval from phase 1 onward is ____ %
8%
_____ is the study of rare human diseases with extreme traits. For pain it looks at ____ and ______ targets
extreme genetics; lipid targets, ion channel targets
____ mutatin shows extreme genetic pain phenotypes that include ___ functional channels, deficits in channel _____ (easier) and deficits in channel _____ (longer)
SCN9A ; no; opening; inactivation
A clinical trial is an expensive experiment to answer the question:__________
does the medicine (safely) work
4 reasons for potential clinical trial failure
- lack of clinical efficacy
- unmanageable toxicity
- poor drug-like properties
- lack of commercial need & poor strategic planning
In phase 1 it takes ___ for oncolgy studies ___ for CNS and ___ for ____ to approved
In phase 2 it takes ___ years for oncolgy studies ___ years for CNS and ___ years for ____ to be approved
In phase 1 it takes __3_ for oncolgy studies 15__ years for CNS and __33 for opthamolgy to approved
In phase 2 it takes 7__ for oncolgy studies __20 years for CNS and __34_ for opthamology to approved
