Term
|
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
|
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
|
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
|
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
|
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
|
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
|
|
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
|
|
Term
| Anticholinergics - Indications |
|
Definition
| -urinary incontinence (adults with overactive bladder) |
|
|
Term
|
Definition
-bladder needs functional sphincter & stable detrusor muscle
-incontinence = spasticity of detrusor muscle (parasympathetic)
-Anti-Ach decrease frequency and urgency to void |
|
|
Term
|
Definition
| -constipation, dry mouth, decreased lacrimation (mydriasis) |
|
|
Term
| Anti-gout agents - indications |
|
Definition
| gout - primarily affects great toe |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| Na+, K+, Ca++, Mg+, HCO3-, Cl-, PO4- |
|
|
Term
|
Definition
| glucose, amino acids, creatinine, drugs |
|
|
Term
| Ca inhibitors and osmotic diuretics |
|
Definition
| uncommonly used diuretics |
|
|
Term
|
Definition
| not a major target for diuretics |
|
|
Term
|
Definition
-majority of Na reabsorption occurs here (~35%)
-NaCl transport system is here
-Loops selectively block this system |
|
|
Term
|
Definition
-only 10% of NaCl reabsorbed here
-different NaCl cotransporter than in loop
- this cotransporter is inhibited by thiazide diuretics |
|
|
Term
|
Definition
-major site of action for aldosterone inhibitors
-exchange of Na drives K+ out
-K+ sparing diuretics work this way |
|
|
Term
|
Definition
-available oral or IV
-lasts 6 hours |
|
|
Term
|
Definition
hypokalmeia
dehydration
hyponatremia
renal toxicity with other agents (like ACE inhibitors) |
|
|
Term
| 75% of thiazide prescriptions |
|
Definition
HCTZ
(Chlothalidone ~20%, metolazone ~5%) |
|
|
Term
|
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
|
Definition
-hyperkalemia
-gynocomastia (5-10% of pts) |
|
|
Term
|
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
|
Definition
| major neurotransmitter for parasympathetic system (drugs that mimic this activate relaxation of bladder sphincter and contraction of detrusor) |
|
|
Term
|
Definition
oldest anticholinergic (2-3 x daily dose)
available as patch (2 x week) |
|
|
Term
|
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
|
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
|
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
|
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
|
Definition
peptide hormones
steroid hormones
glycoprotein hormones |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| conformational change; hours to days (testosterone & progesterone mechanism) |
|
|
Term
|
Definition
| gonadotropin releasing hormone (GnRH) |
|
|
Term
|
Definition
| stimulates release of FSH & LH |
|
|
Term
|
Definition
| stimulates follicular development in women, and spermatogenesis in men; stimulates conversion of androgen to estrogen |
|
|
Term
|
Definition
| leutinizing hormone: works with FH to stimulate ovulation |
|
|
Term
| corticotropin releasing hormone |
|
Definition
| CRH: stimulates release of ACTH |
|
|
Term
|
Definition
| adrenocorticotropin releasing hormone... |
|
|
Term
|
Definition
| thyroid-releasing hormone, stimulates release of TSH |
|
|
Term
|
Definition
| stimulates thyroid to synthesize & release T3 & T4 |
|
|
Term
|
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
|
Definition
|
|
Term
|
Definition
| unconjugated have high first pass effect; conjugated degrade slower and are usually lower dose |
|
|
Term
|
Definition
|
|
Term
|
Definition
-progesterone is primary
-often given with estrogens
-necessary for implantation and maintenance of embryo |
|
|
Term
|
Definition
| -comes from PREgnant MARe urINe |
|
|
Term
|
Definition
| higher bioavailability thru the skin than oral |
|
|
Term
|
Definition
-act locally as well as systemically
-can help with vaginal dryness and atrophy |
|
|
Term
|
Definition
-major therapy for HRT
-usually given 5-10 days on 16th or 21st day of cycle |
|
|
Term
|
Definition
| hormone replacement therapy |
|
|
Term
|
Definition
-selective estrogen receptor modulators
-designer drugs: bind to estrogen receptors activating certain pathways & inhibiting others
-used less frequently |
|
|
Term
|
Definition
| fixed dose of estrogen (& usually progesterone) for entire cycle |
|
|
Term
|
Definition
-same dose of estrogen for 1st 21 days
-progesterone increases in 2nd half of cycle |
|
|
Term
|
Definition
-estrogen constant thru cycle
-progesterone varies |
|
|
Term
|
Definition
-for women who can't tolerate estrogen
-must be taken every day, same time, continually |
|
|
Term
|
Definition
| transdermal patch: every week for 3 weeks (can be used continuously for 4 weeks & skip period) |
|
|
Term
|
Definition
| inserted for 3 weeks, removed for 1 week (can be used continuously for 4 weeks & skip period) |
|
|
Term
|
Definition
|
|
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
|
Definition
| 5mg/day, 35mg/week, 150mg/month |
|
|
Term
|
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
|
Definition
| increase insulin secretion |
|
|
Term
|
Definition
| pen needles with multiple doses |
|
|
Term
|
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
|
Definition
| have a short-acting and intermediate-actin insulin components |
|
|
Term
|
Definition
| two types: glucocorticoids and mineralcorticoids |
|
|
Term
|
Definition
| long-term high-dose use can induce DM or osteoporosis |
|
|
Term
|
Definition
|
|
Term
|
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
|
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
|
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
|
Definition
| thyroid hormone receptors found in pituitary, liver, skeletal muscle, heart, kidney, lung and intestine |
|
|
Term
|
Definition
prescribed 90% of time, because body can convert T4 to T3;
80% absorbed (in ileum and duodenum) |
|
|
Term
|
Definition
| responsible for a lot of functioning of body |
|
|
Term
|
Definition
|
|
Term
|
Definition
1/2 life 7 days;
8 weeks to see if there is TSH stablization |
|
|
Term
|
Definition
| can result in permanent narrowing of airways (remodeling) = hypertrophy and mucous hypersecretion |
|
|
Term
|
Definition
sympathetic = beta 2, bronchodilation
anticholinergic=minimal bronchodilation |
|
|
Term
|
Definition
| mast cells, alveolar macrophages, histamine, prostaglandins and leukotrines |
|
|
Term
|
Definition
| reduce asthma by blocking 5-lipoxygenase or LTE4 |
|
|
Term
|
Definition
most common treatment of asthma;
liquid is aerosolized and inhaled;
short-acting & long-acting |
|
|
Term
|
Definition
|
|
Term
|
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
|
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
|
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
|
Definition
| found in various tissues throughout body; |
|
|
Term
|
Definition
histamine receptors: located on endothelial and smooth muscle cells;
released during allergic reaction: edema, hives, bronchoconstriction |
|
|
Term
|
Definition
| histamine receptors: on paritel cells in t GI, stimulate acid secretion |
|
|
Term
|
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
|
|
Term
| Rx 2nd gen antihistamines |
|
Definition
| levocetirizine, Allegra, Clarinex |
|
|
Term
| combo 2nd gen antihistamines |
|
Definition
| Allegra-D, Zyrtec-D ("D" signifies pseudoephedrine) |
|
|
Term
|
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
|
Definition
|
|
Term
|
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
|
Definition
|
|
Term
|
Definition
| eye drop for seasonal allergies; histamine I antagonist for watery eyes |
|
|
Term
|
Definition
| low systemic absorption, dosed ~6 hours, |
|
|
Term
|
Definition
| block acid secretion, available OTC and prescription |
|
|
Term
|
Definition
| H ion secretion stimulated by ACh, histamine, or GI; block these, and less H released, so less HCl, higher pH |
|
|
Term
|
Definition
| 65-75% histamine secretion in GI |
|
|
Term
|
Definition
| block 90-99% of H secretions; BETTER DRUG FOR GI ISSUES |
|
|
Term
|
Definition
|
|
Term
|
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
|
|
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
|
Definition
| inhibit nausea and vomiting; block various neurotransmitters associated with nauseous stimuli |
|
|
Term
|
Definition
|
|
Term
|
Definition
| cheaper antiemetics ($0.50 per pill), available in many forms |
|
|
Term
|
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
|
Definition
| furosemide works on which part of nephron? which cotransporter? |
|
|
Term
|
Definition
|
|
Term
| alpha blockers specificity and side effects |
|
Definition
|
|
Term
|
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
|
Definition
|
|
