Shared Flashcard Set

Details

Pharm test 4
ISU PA
157
Pharmacology
Graduate
11/09/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
Diuretics - indications
Definition
1. reduce edema (esp. from hepatic failure --> albuminemia)
2. heart failure (have diluted electrolytes & increased edema)
3. electrolyte disturbances (like hyperkalemia)
4. renal failure (probs making urine)
5. HTN -
Term
diuretics - MOA
Definition
-inhibits reabsorption of K+, Na+, etc
-pts may need multiple diuretics that work on different parts on nephron
-any situation that decreases filtration will prevent them from reaching site of action
Term
diuretics - adverse reactions
Definition
Term
loop diuretics
Definition
-most potent diuretic class
-inhibit Na/K/2Cl transporter in thick ascending loop of Henle
-rapidly absorbed
-IV effects almost immediate
-eliminated by renal secretion (half-life dependent on renal function)
-act on luminal side of tubule
-1-2 times daily doses
-should be dosed in the morning (so they don't pee all night)
Term
thiazide diuretics
Definition
-work on Na-Cl cotransporter in distal convoluted tubule (luminal side)
-promote Na and Cl excretion
-enhances Ca reabsorption-
-
Term
potassium sparing diuretics
Definition
-antagonize aldosterone (more hyperkalemic with these agents)
-slow onset of action
-triamterene metabolized by liver & excreted by kidneys
-spironolactone metabolized by liver also
Term
Impotence agents - indications
Definition
-rapidly absorbed w/ bioavailability of ~40%
-maximum serum concentration @ ~2 hrs
-some significant drug interactions (Norvir)
-half life ~4 hours for sildenafil (once per day), but cialis is ~36 hours (once every couple days)
-off-label for ED, pulmonary hypertension, HAPE/HACE (high-altitude pulmonary/cerebral edema)
Term
impotence agents - MOA
Definition
-nitric oxide released into corpus cavernosum during sexual stimulation, promoting smooth muscle relaxtion & increased blood flow
-phosphodiesterase type 5 (PDE5) is responsible for breakdown of NO in corpus cavernosum
-these agents inhibit PDE5 and enhance effects of NO
-needs to be in conjunction with sexual arousal, so won't work for performance anxiety
Term
impotence agents - SA
Definition
-small effects on PDE3 (in eye - results in blurred vision)
-increase in NO can cause rapid drop in BP
Term
BPH agents (Alpha 1 receptor blockers) - indications
Definition
hypertenstion and BPH
Term
BPH agents (Alpha 1 receptor blockers) - MOA
Definition
-decreases prostatic pressure on urethra
-sympathetic innervation (NE) and hormonal control of prostate, bladder neck, and urethra (smooth muscle)
-pseudophedrine and anitcholinergics can increase effects of BPH
Term
BPH agents (Alpha 1 receptor blockers) - SA
Definition
"first dose effect"
Term
Anticholinergics - Indications
Definition
-urinary incontinence (adults with overactive bladder)
Term
Anticholinergics - MOA
Definition
-bladder needs functional sphincter & stable detrusor muscle
-incontinence = spasticity of detrusor muscle (parasympathetic)
-Anti-Ach decrease frequency and urgency to void
Term
Anticholinergics - SA
Definition
-constipation, dry mouth, decreased lacrimation (mydriasis)
Term
Anti-gout agents - indications
Definition
gout - primarily affects great toe
Term
Anti-gout agents - MOA
Definition
Term
Anti-gout agents - SA
Definition
Term
Lytes
Definition
Na+, K+, Ca++, Mg+, HCO3-, Cl-, PO4-
Term
non-lytes
Definition
glucose, amino acids, creatinine, drugs
Term
Ca inhibitors and osmotic diuretics
Definition
uncommonly used diuretics
Term
proximal tubules
Definition
not a major target for diuretics
Term
loop of henle
Definition
-majority of Na reabsorption occurs here (~35%)
-NaCl transport system is here
-Loops selectively block this system
Term
distal convoluted tubule
Definition
-only 10% of NaCl reabsorbed here
-different NaCl cotransporter than in loop
- this cotransporter is inhibited by thiazide diuretics
Term
collecting tubule
Definition
-major site of action for aldosterone inhibitors
-exchange of Na drives K+ out
-K+ sparing diuretics work this way
Term
Lasix
Definition
-available oral or IV
-lasts 6 hours
Term
loops SA
Definition
hypokalmeia
dehydration
hyponatremia
renal toxicity with other agents (like ACE inhibitors)
Term
75% of thiazide prescriptions
Definition
HCTZ
(Chlothalidone ~20%, metolazone ~5%)
Term
thiazide SA
Definition
hypokalemia and hyponatremia (neither of these are very common)
-often prescribed with ACEI or Angio II RBs, which can mess with electrolyte balances
Term
K+ sparing diuretics SA
Definition
-hyperkalemia
-gynocomastia (5-10% of pts)
Term
aldosterone
Definition
steroid hormone that acts on gene transcription and increases activity of various pumps, leading to increase in Na reabsorption and K excretion
Term
impotence agents - contraindications
Definition
not to be used with nitrates (causes potentially fatal fall in BP)
Term
1st generation BPH agents
Definition
prazosin, terazosin, doxazosin
Term
alpha subtype IA BPH agent
Definition
tamsulosin (70% of subtype IA are in the bladder, so there is less systemic hypotenion with this drug)
Term
acetylcholine
Definition
major neurotransmitter for parasympathetic system (drugs that mimic this activate relaxation of bladder sphincter and contraction of detrusor)
Term
oxybutynin
Definition
oldest anticholinergic (2-3 x daily dose)
available as patch (2 x week)
Term
tolteridine
Definition
also 1st generation
high first pass effect (given as long-acting to get around this)
Term
M3 specific anticholinergics
Definition
darifenacin
solifenacin
trospium
fesoteridine (prodrug)
** all newer, higher cost
Term
allopurinol
Definition
more for prevention
inhibits xanthene oxidase, which helps reduce production of uric acid; effects seen 2-3 days up to 2-3 weeks
-well absorbed
-1 x day dosing
Term
colchicine
Definition
-for acute care of gout
-exact mechanism not known
-reduces lactic acid, results in decreased uric acid
-decreased inflammatory response to crystals
-rapidly absorbed
-too high dose = emesis, diarrhea
-recently FDA pulled it from market because it was never studied officially
Term
what is a hormone?
Definition
chemical messenger carried by the blood
-responsible for reproduction, growth, & metabolism
Term
hormone agonists/antagonists
Definition
agonists mimic natural horomone, common
antagonists uncommon
Term
classes of hormones
Definition
peptide hormones
steroid hormones
glycoprotein hormones
Term
peptide hormones
Definition
Term
steroid hormones
Definition
Term
glycoprotein hormones
Definition
Term
extracellular binding
Definition
(insulin mechanism)
Term
intracellular binding
Definition
conformational change; hours to days (testosterone & progesterone mechanism)
Term
sex hormones
Definition
gonadotropin releasing hormone (GnRH)
Term
GnRH
Definition
stimulates release of FSH & LH
Term
FSH
Definition
stimulates follicular development in women, and spermatogenesis in men; stimulates conversion of androgen to estrogen
Term
LH
Definition
leutinizing hormone: works with FH to stimulate ovulation
Term
corticotropin releasing hormone
Definition
CRH: stimulates release of ACTH
Term
ACTH
Definition
adrenocorticotropin releasing hormone...
Term
TRH
Definition
thyroid-releasing hormone, stimulates release of TSH
Term
TSH
Definition
stimulates thyroid to synthesize & release T3 & T4
Term
estrogen indications
Definition
-maintain female reproductive system
-regulate menstrual cycle
-abnormal uterine bleeding
-endometriosis
-acne regulation
-sex changes
-contraceptive (oral)
-promote growth, development or vagina, uterus, fallopian tubes
-mediate physiologic changes of menopause
Term
plasma estrogen and progesterone levels
Definition
massive decrease in women ages 35-50 (precipitates menopause)
Term
estrogen MOA (as contraceptive)
Definition
-combine with progestins to thicken cervical mucus, inhibit sperm penetrations, lower mid-cycle FSH/LH levels
Term
estrogens A/D
Definition
Term
estrogens M/E
Definition
unconjugated have high first pass effect; conjugated degrade slower and are usually lower dose
Term
progestins indications
Definition
Term
progestins
Definition
-progesterone is primary
-often given with estrogens
-necessary for implantation and maintenance of embryo
Term
premarin
Definition
-comes from PREgnant MARe urINe
Term
transdermal estrogens
Definition
higher bioavailability thru the skin than oral
Term
vaginal estrogens
Definition
-act locally as well as systemically
-can help with vaginal dryness and atrophy
Term
Provera
Definition
-major therapy for HRT
-usually given 5-10 days on 16th or 21st day of cycle
Term
HRT
Definition
hormone replacement therapy
Term
SERMs
Definition
-selective estrogen receptor modulators
-designer drugs: bind to estrogen receptors activating certain pathways & inhibiting others
-used less frequently
Term
monophasic
Definition
fixed dose of estrogen (& usually progesterone) for entire cycle
Term
biphasic
Definition
-same dose of estrogen for 1st 21 days
-progesterone increases in 2nd half of cycle
Term
triphasic
Definition
-estrogen constant thru cycle
-progesterone varies
Term
progestin only
Definition
-for women who can't tolerate estrogen
-must be taken every day, same time, continually
Term
Orthoevra
Definition
transdermal patch: every week for 3 weeks (can be used continuously for 4 weeks & skip period)
Term
Nuvaring
Definition
inserted for 3 weeks, removed for 1 week (can be used continuously for 4 weeks & skip period)
Term
Depo injection
Definition
progestin only
Term
estrogens & progestins side effects
Definition
-nausea & headache are common
-smokers or over 35 yo at increased risk for clotting
Term
bisphosphonates A/D & M/E
Definition
-low % absorbed; should be taken on empty stomach w/ 8oz water
-1/2 life of 10 years; never really comes out of body
Term
bisphosphonates indications
Definition
inhibit bone resorption & increase bone mineral synthesis
-osteoporosis & Paget's disease
Term
bisphosphonates side effects
Definition
-nausea, reflux, lower GI
-osteonecrosis
-possibly cancer & fractures
-risks still need to be comprehensively studied
Term
Actonel dosing
Definition
5mg/day, 35mg/week, 150mg/month
Term
insulin MOA
Definition
-causes autophosphorylation of intrecellular proteins leading to glucose uptake by the cell
-this reduces blood glucose levels
-inhibit fatty acid oxidation
-promote macromolecule synthesis
Term
pancreatic spankers
Definition
increase insulin secretion
Term
insulin dosing
Definition
pen needles with multiple doses
Term
insulin pharmacokinetics
Definition
-different durations of action; rapid = take right when carbs are ingested, long-acting = keep blood sugar at controllable level all day (zinc, protamine, fat added to make long-acting)
-metabolized orally in the gut
Term
mixed insulins
Definition
have a short-acting and intermediate-actin insulin components
Term
Corticosteroids
Definition
two types: glucocorticoids and mineralcorticoids
Term
glucocorticoids
Definition
long-term high-dose use can induce DM or osteoporosis
Term
mineralcorticoids
Definition
Term
glucocorticoid receptors
Definition
throughout body; crosses membrane by passive diffusion (this is why they work topically, inhaled, rectal enemas)
-enter nucleus, causes increase production of mRNA
Term
glucocorticoids pharmacokinetics
Definition
rapid absorption;
oral and IV doses essentially equivalent
Term
corticosteriods misc
Definition
oral, creams, ointments, lotion, spray, enemas, available;
good for psoriasis, rashes, etc
ointemnts are more hydrating for irritated skin;
also IV (short acting) or IM (long acting); good for ulcerative colitis, crohns (for targeted treatment)
Term
prednisone
Definition
made by body, up to 7.5mg per day;
after 2 weeks of doses more than this, adrenals go to sleep (treatment should be stopped)
Term
chronic corticosteroid side effects
Definition
Term
thyroid agents
Definition
thyroid hormone receptors found in pituitary, liver, skeletal muscle, heart, kidney, lung and intestine
Term
T4
Definition
prescribed 90% of time, because body can convert T4 to T3;
80% absorbed (in ileum and duodenum)
Term
T3 and T4
Definition
responsible for a lot of functioning of body
Term
T3
Definition
95% absorbed
Term
synthetic T4
Definition
1/2 life 7 days;
8 weeks to see if there is TSH stablization
Term
asthma
Definition
can result in permanent narrowing of airways (remodeling) = hypertrophy and mucous hypersecretion
Term
asthma & nervous system
Definition
sympathetic = beta 2, bronchodilation
anticholinergic=minimal bronchodilation
Term
asthma & inflammation
Definition
mast cells, alveolar macrophages, histamine, prostaglandins and leukotrines
Term
arachidonic acid pathway
Definition
reduce asthma by blocking 5-lipoxygenase or LTE4
Term
beta 2 agonists
Definition
most common treatment of asthma;
liquid is aerosolized and inhaled;
short-acting & long-acting
Term
short-acting inhalers
Definition
AKA rescue inhalers
Term
long-acting inhalers
Definition
more lipophilic, hang out ~12 hours, usually taken twice a day;
systemic absorption can cause tachycardia and tremors
Term
beta 2 agonists indications
Definition
asthma, COPD, RAD, cystic fibrosis, pneumonia, exercise-induced asthma, hyperkalemia
Term
beta 2 agonists side effects
Definition
tachycardia and tremors
hypokalemia in high doses (drives Na into cells)
drug interactions
non-selective beta-blockers
*more than 1 canister/month = OVERUSE*
(1 canister = ~200 puffs)
Term
short-acting beta 2 agonists
Definition
alubuterol aerosol (dosed as needed)
Term
long-acting beta 2 agonists
Definition
salmeterol (dosed 2 x daily for long-term control or preventative; 30-60 mins prior to activity
Term
corticosteroids for asthma
Definition
inhibit inflammation by reducing certain cytokines production;
decrease inflammation & mucous production;
low dose, effect takes 3-4 days, maximal effect 3-4 weeks
Term
corticosteriods for asthma side effects
Definition
Headache, throat itching, wheezing, thrush (pts need to rinse mouth after)
Term
anticholinergics
Definition
inhibit acetylcholine; chronic maintenance therapy for COPD; 2nd line agent in control of lung disease
Term
short-acting anticholingergic
Definition
ipratropium (atrovent); several times a day
Term
long-acting anticholinergic
Definition
tioproprium (Spiriva); dosed 1 x per day
Term
nebulizers
Definition
delivers anticholinergics and beta 2 agonists in a mist form;
promotes slower breathing, which calms pt and makes for easier breathing;
delivers drug over 10-15 mins; comes in pre-packaged doses
Term
antihistamines
Definition
found in various tissues throughout body;
Term
h1 receptors
Definition
histamine receptors: located on endothelial and smooth muscle cells;
released during allergic reaction: edema, hives, bronchoconstriction
Term
h2 receptors
Definition
histamine receptors: on paritel cells in t GI, stimulate acid secretion
Term
h1 receptor anagonists
Definition
benadryl and claritine; for rhinitis, allergic, seasonal, perennial, urticaria
Term
H1 receptor physiologic antagonists
Definition
epinephrine (for life-threatening)
Term
1st generation antihistamines
Definition
benadryl, chlortrimitone (sp?):
sedation, dizziness, drowsiness, overall CNS depression;
dosed every 3-4 hours
Term
2nd generation antihistamines
Definition
equally effective, but longer 1/2 lives, fewer side effects (act more on peripheral receptors); used for daily (dosed 1-2 x per day)
Term
OTC 2nd gen antihistimines
Definition
Zyrtec, Claritin,
Term
Rx 2nd gen antihistamines
Definition
levocetirizine, Allegra, Clarinex
Term
combo 2nd gen antihistamines
Definition
Allegra-D, Zyrtec-D ("D" signifies pseudoephedrine)
Term
nasal steriods
Definition
pharmacology same as inhaled steroids;
onset of action usually a couple days;
metabolized in liver, excreted in feces and urine; used daily for max efficacy
Term
generic nasal steroids
Definition
Flonase is only one
Term
montelukast (Singulair)
Definition
oral leukotrine antagonist: selectively binds to LTD4 and LTE4 in arachidonic pathway, which reduces edema, inflammation, and constriction of airways
Term
montelukast pharmacokinetics
Definition
if no benefit in 1-2 days, then probably they won't work
Term
montelukast side effects
Definition
rare, minimal
Term
olopatadine
Definition
eye drop for seasonal allergies; histamine I antagonist for watery eyes
Term
olopatadine kinetics
Definition
low systemic absorption, dosed ~6 hours,
Term
gastrointestinal agents
Definition
block acid secretion, available OTC and prescription
Term
GI agents pharmacology
Definition
H ion secretion stimulated by ACh, histamine, or GI; block these, and less H released, so less HCl, higher pH
Term
histamine 2 receptors
Definition
65-75% histamine secretion in GI
Term
proton pump inhibitors
Definition
block 90-99% of H secretions; BETTER DRUG FOR GI ISSUES
Term
histamine 2 receptors
Definition
OTC and Rx
Term
proton pump inhibitors
Definition
prodrugs, maintain pH >4 (normal is 2); allows for healing of ulcers & other symptoms; short-term use for short-term problems; minimal side effects
Term
proton pump inhibitors side effects
Definition
minimal; some GI, may decrease b12 oral absorption
Term
OTC proton pump inhibitors
Definition
Prilosec, Pravacid
Term
Rx proton pump inhibitors
Definition
Nexium, Aciphex, Protonix
Term
proton pump inhibitors misc.
Definition
capsules can be opened and mixed with applesauce, etc; 3-4 days to see full effect; decreased acid may depress absorption of other oral drugs
Term
antiemetics
Definition
inhibit nausea and vomiting; block various neurotransmitters associated with nauseous stimuli
Term
Zofran
Definition
$20-40 per pill
Term
Compazine and Phenergan
Definition
cheaper antiemetics ($0.50 per pill), available in many forms
Term
sucralfate
Definition
once dissolved in acid, becomes negatively charged and forms viscous adherent complex; like a band-aid over ulcer; binds up to 6 hours
Term
diuretic MOA
Definition
furosemide works on which part of nephron? which cotransporter?
Term
differences between PDEs
Definition
Term
alpha blockers specificity and side effects
Definition
Term
MOA of contraceptives
Definition
Term
differences of insulin (length of action, oral vs. IM, etc)
Definition
Term
thryoid agents differences
Definition
Term
long vs. short acting beta agonists vs. anticholinergics
Definition
Term
MOA and side effects of inhaled steroids
Definition
Term
potency of different GI agents
Definition
proton pump inhibitors are better
Term
MOA of GI aagents
Definition
Supporting users have an ad free experience!