Term
| unionized drug preferentially enters epineurium and cell membrane, but ionized drug binds channel; better block occurs if cytoplasm is acidic |
|
Definition
| importance of charge and pH on local anesthetics |
|
|
Term
| pain/autonomic fibers, cold, warmth, touch, deep pressure, motor |
|
Definition
| order of functional block in LAs |
|
|
Term
| two "Is" in names: lidocaine, etidocaine, bupivacaine, mepivacaine; metabolized in several steps by liver enzymes (severe problems for hepatic insufficiency!) |
|
Definition
|
|
Term
| one "I" in name; degraded by plasma esterases; include: procaine, tetracaine, cocaine, benzocaine |
|
Definition
|
|
Term
| duration of action proportional to time contact w/ nerve; absorption dependent on location of injection and dosage; distribution dependent on blood flow; some amides are highly bound to plasma proteins; add vasoconstrictor to reduce systemic toxicity and prolong duration |
|
Definition
| pharmacokinetics of local anesthetics |
|
|
Term
| CNS effects can be either excitatory or depressive; CV effects: decreased conduction, force of contraction, BP, and excitability, CV collapse; decreased contractions of bowel and uterine smooth muscle; hypersensitivity reactions; nausea |
|
Definition
|
|
Term
| potential side effect from benzocaine or prilocaine use; ferrous iron is oxidized to ferric iron in hemoglobin; lower O2 transport |
|
Definition
|
|
Term
| benzocaine is most common; also available are tetracaine 2%, lidocaine 2-10%, and cocaine 1-4% w/ vasoconstrictor; eutectic mixture of lidocaine and prilocaine allow action to 5mm depth after administration; lidoderm patch used for postherpetic neuralgia and neuropathic pain; phenylephrine is agent added for vasoconstriction; bupivacaine and ropivacaine are not used for this purpose |
|
Definition
|
|
Term
| intradermal or subQ injection; does not disrupt bodily functions; epinephrine prolongs duration of action (but DO NOT use in tissues supplied by end arteries); pts may experience pain post-injection; useful for minor surgery; agents commonly used are procaine (short duration), lidocaine (moderate), and bupivacaine (long) |
|
Definition
|
|
Term
| IV admin into torniquet-occluded limb; use is limited by potential risk; CV collapse reported after bupivacaine use in this type; lidocaine w/o epinephrine most commonly used; method used primarily for hand/forearm surgeries |
|
Definition
| intravenous regional anesthesia |
|
|
Term
| used to produce greater areas of anesthesia than infiltration; determinants of onset include: proximity of injection to nerve, concentration/volume injected, and degree of ionization; drugs used w/ epinephrine: lidocaine, prilocaine, bupivacaine, tetracaine |
|
Definition
| peripheral nerve blockade |
|
|
Term
| either epidural or spinal; can block ANS; epidural associated w/ greater toxicity b/c more drugs used for longer periods; baricity of solution can determine direction of migration; complications: infection, hematoma, cord trauma, and postural HA |
|
Definition
|
|
Term
| agents used are: lidocaine, prilocaine, ropivacaine, and bupivacaine (order shortest-longest duration); etidocaine not used due to motor block; primary site of action on spinal roots |
|
Definition
|
|
Term
| valuable during surgery on lower abdomen, LEs, and perineum; requires much smaller volume; lidocaine, tetracaine, and bupivacaine used (short-long duration in order); causes sympathetic block, vasodilation, blood pooling, and reduced cardiac output |
|
Definition
|
|
Term
| can be injected intrathecally or epidurally to produce segmental analgesia; useful for post-op or chronic pain; zinconotide (N-type calcium channel blocker) recently approved for severe chronic pain |
|
Definition
| opioids and pumps in epidural/spinal anesthesia |
|
|
Term
| most popular amide-type LA; wide variety of uses; fast onset and short/intermediate duration; has CV toxicity (usually depressant) at dose causing CNS toxicity |
|
Definition
|
|
Term
| amide type LA; slower onset w/ intermediate duration; more toxic in neonates so avoid use! |
|
Definition
|
|
Term
| amide type LA; more cardiotoxic than lidocaine so avoid high doses or intravascular injection; used in long duration infiltration anesthesia, major nerve blocks, epidurals, and spinal anesthesia; has S-enantiomer that is also active |
|
Definition
|
|
Term
| amide type LA; less cardiotoxic than bupivacaine and long-lasting; useful in epidurals |
|
Definition
|
|
Term
| amide type LA; known to cause methemoglobinemia; used for short duration peripheral nerve blocks and epidurals |
|
Definition
|
|
Term
| ester type LA; slow onset w/ short duration; metabolized to paraaminobenzoic acid which inhibits sulfonamides; used in infiltration anesthesia |
|
Definition
|
|
Term
| ester type LA; has slower metabolism and potentially more systemic toxicity; long-lasting for topical use and peripheral nerve blocks; has intermediate duration for spinal anesthesia |
|
Definition
|
|
Term
| ester type LA; blocks NE uptake; vasoconstrictor; used topically in ENT surgery ONLY; abuse potential |
|
Definition
|
|
Term
| ester type LA; low solubility; popular topical agent; known to cause methemoglobinemia |
|
Definition
|
|
Term
| disruption of H-P-G axis (infertility, PCOS), inappropriate growth of hormone-dependent tissue (breast/prostate CA, endometriosis), and decreased secretion of products (hypogonadism, menopause) |
|
Definition
| pathophysiologic processes of reproductive tract |
|
|
Term
| pituitary gonadotroph; stimulates seminiferous tubules in males and follicular growth/estrogen production in females |
|
Definition
|
|
Term
| pituitary gonadotroph; stimulates androgen secretion in males and triggers ovulation and luteinization in females |
|
Definition
|
|
Term
| from hypothalamus; stimulates release of FSH and LH |
|
Definition
|
|
Term
| anti-estrogen used to treat ovarian failure ("fertility drug"); blocks estrogen-mediated inhibition of FSH/LH release; potential overstimulation of ovaries can cause multiple pregnancies |
|
Definition
|
|
Term
| combinations of FSH and LH recovered from urine of menopausal women; produce follicular stimulation |
|
Definition
|
|
Term
| collected from the urine of pregnant women; action similar to LH; used after priming w/ menotropins to induce ovulation |
|
Definition
|
|
Term
| synthetic androgen used to inhibit output of FSH/LH in endometriosis in females (removes hormonal stimulation) |
|
Definition
|
|
Term
| GnRH super agonist; reduces androgenic stimulation by over-stimulating and desensitizing GnRH-Rs in pituitary; prevents release of FSH/LH and reduces circulating testosterone levels; treatment for prostate CA |
|
Definition
|
|
Term
| differ from leuprolide by one amino acid; more potent and longer-acting; typically given parenterally; same MOA |
|
Definition
|
|
Term
| synthetic estrogen; used in treatment of prostate CA; MOA unknown; has many unpleasant side effects and not frequently used |
|
Definition
|
|
Term
| pure GnRH antagonists; inhibit FSH/LH release without initial increase; used in management of infertility/IVF; prevents premature LH surge; under consideration for endometriosis tx |
|
Definition
|
|
Term
| menotropin class; purified FSH; produces follicular stimulation |
|
Definition
|
|
Term
| menotropin class; recombinant product; produces follicular stimulation |
|
Definition
|
|
Term
| premenopausal hypogonadism, suppression of symptoms of menopause (HRT), tx of breast/prostate/endometrial CAs, and combo oral contraceptives |
|
Definition
| uses of estrogens/anti-estrogens/estrogenic drugs |
|
|
Term
| highly lipophilic, well-absorbed from GI tract; extensively bound (>90%) to plasma proteins; hepatic metabolism |
|
Definition
| pharmacokinetics of steroidal estrogens |
|
|
Term
| positive effects on bone mass/density, positive effects on serum lipids, fluid retention, altered biliary function, facilitation of clot formation |
|
Definition
| metabolic effects of estrogens |
|
|
Term
| increased risk of endometrial CA w/o progestin; increased risk to clear-cell vaginal/cervical adenocarcinoma after exposure of females in utero; thromboembolic disorders; increased gallbladder dx; migraines at high doses; N/V at high doses; birth defects (questionable) |
|
Definition
| adverse effects of estrogens |
|
|
Term
| for post-menopausal women; treats osteoporosis, vasomotor disturbances, vaginal/vulvar atrophy; usually combined estrogen + progestin; may increase risk of CVD |
|
Definition
|
|
Term
| non-steroidal compounds from plants w/ weak estrogenic/anti-estrogenic activity; not regulated as drugs; risks and benefits not yet clear |
|
Definition
|
|
Term
| functional competitive estrogen R antagonist that decreases estrogenic stimulation of tumor cells; orally effective, half-life 5-7 days due to plasma binding; lowers circulating cholesterol and increases bone density (post-menopausal women); adverse effects: N/V, hot flashes, increased risk of endometrial CA |
|
Definition
|
|
Term
| water soluble salts of estrogen-sulfate esters; sulfate group is hydrolyzed by enzymes in lower gut, allowing absorption of estrogens; ex: Premarin |
|
Definition
|
|
Term
| synthetic estrogen, conjugated |
|
Definition
|
|
Term
| type 1 ER antagonist (partial agonist); prototype agent w/ no uterotrophic effect; increased thromboembolic risk early in tx |
|
Definition
|
|
Term
| steroidal aromatase inhibitor; selectively inhibits final step in estrogen synthesis; adjuvant therapy of breast CA w/ tamoxifen |
|
Definition
|
|
Term
| non-steroidal aromatase inhibitors; used in adjuvant therapy w/ tamoxifen; improve outcome among postmenopausal women w/ breast CA |
|
Definition
| anastrozole and letrozole |
|
|
Term
| hormone important in luteal phase of menstrual cycle; maintains thickened endometrium and transforms it into secretory endometrium |
|
Definition
|
|
Term
| principal endogenous estrogen in humans; produced by follicle; acts on endometrium to cause proliferation and thickening |
|
Definition
|
|
Term
| synthetic estrogen; orally effective prodrug; quickly demethylated to ethinyl estradiol |
|
Definition
|
|
Term
| synthetic estrogen; slower metabolism; half-life 12-24 hours; orally effective |
|
Definition
|
|
Term
| synthetic analog of progesterone; has selective activity; main component of DepoProvera |
|
Definition
|
|
Term
| anti-androgenic and anti-mineralocorticoid activity; available in combination-type OCPs |
|
Definition
|
|
Term
| synthetic progestin; has progestational and androgenic activity |
|
Definition
|
|
Term
| in gonane class of synthetic progestins; have least androgenic activity of progestins; one used in Norplant (effective for 5 years); other used in emergency contraception |
|
Definition
| levonogestrel and norgestrel |
|
|
Term
| highly lipophilic; extensively bound to plasma proteins; hepatic metabolism (progesterone half-life ~5min, 19-nor = 6-24hrs) |
|
Definition
| pharmacokinetics of progestins |
|
|
Term
| post-menopausal HRT w/ estrogen, OCP combos |
|
Definition
| therapeutic uses of progestins |
|
|
Term
| CV disorders (DVT, cerebral vascular dx, MI, CAD, hyperlipidemia), hormone-dependent neoplasia, liver tumors/dysfunction, and pregnancy |
|
Definition
| contraindications of OCPs |
|
|
Term
| inhibit ovulation and produce direct effects on reproductive tract; given as "minipills," depot preps, or IUDs; 99% efficacy (theoretical); problems: irregular/breakthrough bleeding, edema, weight gain, depression, HA, and impaired fertility upon withdrawal; DO NOT INTERFERE W/ LACTATION |
|
Definition
| progestin-only contraceptives |
|
|
Term
| RU486, abortion pill; competitive antagonist at progesterone and glucocorticoid Rs; orally active, half-life 20-40 hrs; effects: termination of pregnancy, disruption of normal ovulation, blockade of progesterone-mediated stimulation, and increased plasma levels of ACTH and adrenal steroids; uses are for medical abortion in first trimester (NOT FOR ECTOPIC!!) and possibly hormonal control tx (endometriosis, breast CA, others) |
|
Definition
|
|
Term
| biphosphonate; increases bone density by selective inhibition of function of osteoclasts responsible for bone resorption; orally effective but only 10% absorbed, rapidly cleared and bound in bone; adverse effects: diarrhea, nausea, abdominal pain, avascular necrosis of jaw (very rare) |
|
Definition
|
|
Term
| immediate precursor of estradiol; produced in testes and adrenal cortex; highly lipophilic |
|
Definition
|
|
Term
| alkylated androgenic steroid; orally effective; used as adjunctive therapy for weight gain following extensive surgery, chronic infections, or severe trauma; also treats alcoholic hepatitis, Turner's syndrome, and HIV wasting; not readily aromatized to estrogen; prolonged use causes liver toxicity; causes hypercholesterolemia |
|
Definition
|
|
Term
| synthetic androgenic steroid; may be used in hypogonadism, breast CA, stimulation of erythropoiesis, hereditary angioedema, and AIDS wasting; orally effective |
|
Definition
|
|
Term
| weak partial agonist for androgen receptor; may inhibit spermatogenesis and libido; minimal use, prostate CA? |
|
Definition
|
|
Term
| non-steroidal anti-androgenic agent; used in tx of prostate CA; survival similar to castration; adverse effects: impotence, gynecomastia (counteracted by leuprolide), and hepatotoxicity |
|
Definition
|
|
Term
| non-steroidal anti-androgen; has less hepatotoxicity and can be given once daily |
|
Definition
|
|
Term
| inhibitor of 5a reductase (type 2); oral bioavailability is 80%, plasma half-life is 5-7 hrs; used in BPH and male pattern baldness; side effect is impotence; contraindications: women who are or may become pregnant, liver impairment |
|
Definition
|
|
Term
| increase activity of GABA-Rs and K channels and decrease activity of AchR/glutamateRs |
|
Definition
| MOA of general anesthetics |
|
|
Term
| induction of a state of unconsciousness with the absence of pain sensation over the entire body |
|
Definition
|
|
Term
| produced by safe doses of two or more agents or methods, each of which contributes to total desired effect; goal: summate desired actions and minimize undesired |
|
Definition
|
|
Term
| include thiopental, thiamylal, and methohexital; rapid onset; terminated by redistribution; good for initiating anesthesia; terminal half-lives longer w/ continued infusion; neonates and infants require higher induction dose; have antiseizure activity; contraindicated in porphyria; provide poor analgesia and little muscle relaxation |
|
Definition
|
|
Term
| barbiturate GA; has long context-based half-life; do not use for continual infusion due to longer time to wake up post-op; IV admin; fairly lipophilic; difficult to get due to use as element in lethal injection cocktail |
|
Definition
|
|
Term
| barbiturate class of GA; not commercially available |
|
Definition
|
|
Term
| barbiturate class of GA; has relatively rapid clearance due to redistribution; IV admin |
|
Definition
|
|
Term
| onset and duration similar to barbiturates; has high degree of clearance so rapid recovery; can be used for maintenance and induction; poor analgesia; toxicity: decreased cerebral metabolism, decreased cerebral blood flow, decreased BP, depressed resp, pain on injection; infamous pop star-killing drug |
|
Definition
|
|
Term
| IV admin GA; cardiostable (used in hypotension risk); used for induction; poor analgesia; causes significant N/V and can suppress adrenocortical stress response; fentanyl prolongs elimination half-life |
|
Definition
|
|
Term
| can be used as IV GA; for short procedures but can be used for maintenance and/or induction; blocks glutamate Rs (not GABAergic); metabolized in liver; used w/ risk of hypotension or bronchospasm; analgesic; useful in children undergoing short, painful procedures; can cause amnesia/dissociative state; toxicity: emergence delirium, cataleptic state, increased cerebral blood flow; analog of PCP and known as "Special K" on the streets |
|
Definition
|
|
Term
| resp depression, lower response to CO2 or hypoxia, depressed CV drive, muscular rigidity (opioids, ketamine), hallucinations and emergence delirium (ketamine), steroidogenesis inhibition (etomidate), and reduced pain threshold (thiopental) |
|
Definition
|
|
Term
| ratio of concentrations of anesthetic in two tissues when partial pressure is the same in the tissues and is based on Henry's Law; higher blood/gas partition coefficient = longer induction time and longer duration of action |
|
Definition
| partition coefficient of gaseous anesthetic |
|
|
Term
| compares potency of inhalation anesthetics and useful when combining agents; defined as concentration of gas in alveolar compartment that results in lack of response to noxious stimulus in 50% of subjects |
|
Definition
| minimum alveolar concentration (MAC) |
|
|
Term
| high blood/gas partition coefficient; slow induction; largely used for maintenance; effective bronchodilator and some relaxation of skeletal muscle; weak analgesic; significant metabolism; toxicity: conc. dependent reduction in arterial BP, potent myocardial depressant, increased incidence of arrhythmias/bradycardia, potential to increase intracranial P, inhibits ventilatory response to CO2 or hypoxemia, hepatotoxicity, and MALIGNANT HYPERTHERMIA; mostly discontinued in US |
|
Definition
|
|
Term
| relatively high blood/gas partition coefficient; slow induction; used for maintenance; similar to halothane in bronchodilation and toxicity; additionally increases seizure activity!! limited use in US |
|
Definition
|
|
Term
| replacement for halothane in US; inhaled GA; lower blood/gas partition coefficient; induction in 10 mins; pungent odor may cause gagging; eliminated unchanged through expired air; side effects: tachycardia, peripheral vasodilation and hypotension, DILATES CORONARY ARTERIES, concentration-dependent depression of ventilation, malignant hyperthermia; most commonly used anesthetic in US |
|
Definition
|
|
Term
| lowest blood/gas partition coefficient in class; low fat solubility; very rapid onset and allows for rapid changes and emergence; minimal drug metabolism; useful for outpatient surgeries; unique side effects: transient tachycardia, depressed ventilation, coughing/salivation/bronchospasm in awake pts, airway irritant (not for induction), may produce CO if recycled |
|
Definition
|
|
Term
| low blood/gas partition coefficient; rapid onset and recovery but slower recovery than desflurane; can be used for induction; widely used in outpatient and peds surg; small percentage metabolized w/ organic fluoride as one by-product; potent bronchodilator; direct relaxation of skeletal muscle; no significant tachycardia; unique side effects: decreases cardiac output, reduces ventilation, nephrotoxic substance produced when recycled |
|
Definition
|
|
Term
| insoluble agent in blood so rapid induction/emergence; weak anesthetic but significant analgesic; used as adjunct; cannot be used at conc. above 80%; 99.9% elimination by lungs; second gas effect; side effects: accumulation in gas-filled spaces and "bends"-like effects, need to give 100% O2 at end of anesthesia to avoid diffusional hypoxia, contraindicated in pulmonary hypertension |
|
Definition
|
|
Term
| inhalation anesthetic withdrawn due to detrimental effects on kidneys; relatively good analgesic w/ slow onset; may be used in foreign ambulance services |
|
Definition
|
|
Term
| prototype is d-tubcurarine; function as competitive antagonists of nicotinic Rs at NMJ; all contain at least one quaternary nitrogen; two main classes: benzylisoquinolines and ammoniosteroids |
|
Definition
| non-depolarizing NM blockers |
|
|
Term
| have complex ring structures similar to d-tubocurarine; include: atracurium and mivacurium |
|
Definition
|
|
Term
| structures contain steroid nucleus; includes: rocuronium and pancuronium |
|
Definition
|
|
Term
| 1) muscles of fine mvmt (eyes, fingers, etc.), 2) limbs 3) trunk 4) intercostals 5) diaphragm |
|
Definition
| order of paralysis of NM blockers |
|
|
Term
| ammoniosteroid NM blocker; non-depolarizing; has primarily renal elimination; has intermediate duration of action; side effects: decreased BP, muscarinic R blockade causing tachycardia; use caution in pts w/ renal failure |
|
Definition
|
|
Term
| prototype of all NM blockers; competitive antagonist at nicotinic R; in benzylisoquinoline class; has longer half-life than most in class; renal elimination; side effects: decreased BP, bronchospasm, increased secretions |
|
Definition
|
|
Term
| NM blocker; unique for hepatic metabolism and intermediate duration of action; significant side effect is tachycardia |
|
Definition
|
|
Term
| NM blocker in ammoniosteroid class; unique w/ hepatic metabolism and low potency giving rapid onset |
|
Definition
|
|
Term
| in benzylisoquinoline class of NM blockers; eliminated by spontaneous breakdown and plasma esterases; has short to intermediate duration of action; less likely to produce anti-muscarinic side effects than others in class; |
|
Definition
|
|
Term
| in benzylisoquinoline class of NM blockers; has shortest duration of all; undergoes metabolism by plasma esterases; pulled from market in 2005 |
|
Definition
|
|
Term
| aminoglycoside abx, calcium channel blockers, and certain inhalation anesthetics |
|
Definition
| drugs enhancing curare-type NM blockade |
|
|
Term
| depolarizing NM blocker; has shortest time to onset and short duration of action; hydrolyzed by plasma esterases; problems: myalgia (from initial fasciculations), hyperkalemia and arrhythmias, atypical pseudocholinesterase causing prolonged paralysis, and malignant hyperthermia (very rare) |
|
Definition
|
|
Term
| occurs when long-acting exogenous agonist of nicotinic Rs do not dissociate from the R, thereby preventing fast-acting Na channels to repolarize and reset; blocks AP |
|
Definition
|
|
Term
| GABAb R agonist; thought to act in spinal cord to prevent presynaptic excitation of motor neurons and possibly at supraspinal CNS; treatment for spasticity associated w/ MS, spinal cord injury/dx, or trigeminal neuralgia; given orally and renally eliminateds but also used intrathecally; adverse effects: drowsiness, dizziness, lightheadedness, confusion, and muscle weakness |
|
Definition
|
|
Term
| inhibits Ca release in sarcoplasmic reticulum in skeletal muscle; used to treat malignant hyperthermia from anesthesia; given orally or IV and metabolized hepatically; adverse effect is muscle weakness |
|
Definition
|
|
Term
| a-glucosidase inhibitor in small intestine; slows carb digestion; gives rise to smaller postprandial spike and smaller risk of hyperglycemia/lactic acidosis/weight gain; used as adjunct to diet/exercise for glycemic control of DM2; given orally tid w/ meals; metabolized within GI tract by enzymes and bacteria; contraindicated in: diabetic ketoacidosis, IBD, colonic ulceration, intestinal obstruction, chronic intestinal dxs, and breastfeeding; adverse effects: hypoglycemia, GI disturbances, skin rash, and low serum iron |
|
Definition
|
|
Term
| first generation sulfonylureas; induce insulin release by inhibiting K conductance through K/ATP channels; used as adjunct to diet/exercise; orally administered once daily and metabolized in liver; not for use in Type 1 or w/ bosentan; adverse effects: hypoglycemia, pruritis, N/V/D, anorexia, hunger, leukopenia, agranulocytosis, etc.; most appropriate for non-obese DM2 pts |
|
Definition
| chlorpropramide and tolbutamide |
|
|
Term
| second generation sulfonylureas; induce release of insulin by inhibiting K conductance through K/ATP channels; same pharmacokinetics, etc as first generation |
|
Definition
|
|
Term
| meglatinides; insulin secretagogues; act similarly to sulfonylureas but bind to distinct SUR1 region of channel; used as adjunct to diet/exercise; control postprandial hyperglycemia w/o risk of long-lasting hypoglycemia; oral administration 30 mins prior to meal; RAPID distribution; metabolized in liver; contraindications similar to sulfonylureas except: gemfibrozil and NPH insulin for one agent; unique adverse effects: CV events, back pain, chest pain |
|
Definition
| repaglinide and nateglinide |
|
|
Term
| biguanide; activates AMPK which suppresses glucose production in liver (decreases transcription necessary for hepatic gluconeogenesis); inhibits ATP-dependent protein, fatty acid, and cholesterol biosynthesis; increases glucose uptake in skeletal muscle; adjunct tx in DM2; oral admin 1-2x/d, often in combo w/ another tx; excreted unchanged in urine; contraindicated: renal dx, acute/chronic met acidosis, DKA, temporarily w/ certain radiologic studies; adverse effects: GI upset, URI, hypoglycemia, and lactic acidosis (last 2 extremely rare) |
|
Definition
|
|
Term
| acts at SUR1 to increase K/ATP channel activity in beta cells; inhibits secretion of insulin; used orally to manage hypoglycemia; adverse effects: fluid retention, reaction w/ thiazide diuretics, ketoacidosis/nonketotic hyperosmolar coma |
|
Definition
|
|
Term
| thiazolidinediones; activate PPARg, which alters rate of expression of genes incoding proteins involved in regulating lipid metabolism; ultimately increase insulin sensitivity at target tissues; adjunct to diet/exercise in DM2; oral admin 1-2x/d; excreted unchanged in urine; adverse effects: increase in MI and angina, dose-related weight gain, edema, anemia, macular edema, increased bone fracture (first agent), tooth dx (second agent), URI, and HA |
|
Definition
| rosiglitazone and pioglitazone |
|
|
Term
| incretin; GLP-1 analog; controls hyperglycemia by potentiating glucose-mediated insulin secretion and suppressing postprandial glucagon release; adjunct to diet/exercise in DM2; subQ 60 mins before first and last meals daily; contraindicated: DM1, pancreatitis, renal impairment, severe GI dx, breastfeeding; adverse effects: hypoglycemia, GI disturbances, dizziness, HA, increased INR w/ warfarin |
|
Definition
|
|
Term
| incretin; inhibitor of DPP4; increases concentration of GLP-1; adjunct to diet/exercise in DM2; oral admin 4x/d; same contraindications and adverse effects as other incretins |
|
Definition
|
|
Term
| endogenous pancreatic hormone; acts to raise blood glucose levels; increases rate of glycogen breakdown and gluconeogenesis in liver; active during fasting state; treatment of acute hypoglycemia |
|
Definition
|
|
Term
| product dimerizes then associates into hexamers in solution; once injected, the rate-limiting step in absorption is dissociation; considered short-acting |
|
Definition
|
|
Term
| suspension of crystalline zinc compound combined w/ protamine; less soluble; has smaller peak and is more sustained long-term; considered intermediate-acting (peaks at 4 hrs) |
|
Definition
|
|
Term
| ultra-fast-acting analogs; alterations minimize the formation of dimers and hexamers and speed up absorption; peak at 30min-2hr; last for 3-4 |
|
Definition
|
|
Term
| C14 fatty acid added to B chain; induces reversible binding to fatty acid binding sites on albumin in plasma and interstitial tissue, which creates depots in blood; onset 1-3 hours, peak 9-?, duration 14-24 |
|
Definition
|
|
Term
| modification of B chain makes it soluble at acidic pH, but precipitates upon injection; slow absorption, 1-3 hrs to onset, no peak, long duration; good for use as basal insulin |
|
Definition
|
|
Term
| synthetic T4; oral bioavailability variable; half-life 7 days; used as replacement for hypothyroidism and as pituitary TSH suppressant; may exacerbate MI, angina, DM, DI, cortical insufficiency |
|
Definition
|
|
Term
| T3 hormone only; more potent than levothyroxine w/ 95% oral bioavailability; shorter half-life, does not increase plasma T4 levels; same considerations as levothyroxine |
|
Definition
|
|
Term
| drug commonly used in bipolar dx; actively concentrates in thyroid and inhibits hormone release from follicular cells to cause hypothyroidism |
|
Definition
|
|
Term
| thioamide; inhibits thyroid peroxidase; tx for Graves', hyperthyroidism, and toxic multinodular goiter; oral admin; preferred treatment for hyperthyroidism in males and non-pregnant females; adverse effects: increased risk of bleeding w/ oral anticoagulants |
|
Definition
|
|
Term
| thioamide; inhibits thyroid peroxidase and deiodinase (prevent peripheral T4 to T3 conversion); preferred tx for hyperthyroidism in pregnant females; adverse effects: severe injury and acute liver failure |
|
Definition
|
|
Term
| b blocker that inhibits deiodinase; useful for treating sxs of hyperthyroidism b/c they mimic nonspecific beta-adrenergic stimulation |
|
Definition
|
|
Term
| inhibits iodine uptake, iodination, organification, and thyroid hormone release; used for emergency tx of thyroid storm, protection during medical tx, and protection during radioactive emergencies; oral admin as solution; rapid onset of action but effects are reversible and transient; contraindicated w/ known hypersensitivities and adverse effect is hypothyroidism |
|
Definition
|
|
Term
| destroys follicular cells by ionizing radiation; tx for Graves', overactive/enlarged thyroid, and thyroid CA; oral admin as solution or capsule; delayed onset of action w/ observable decrease in weeks; tx is permanent; contraindicated in pregnancy; adverse effects: permanent hypothyroidism, induction of thyroiditis, worsening ophthalmopathy in Graves' |
|
Definition
|
|
Term
| radiocontrast agent used for biliary duct visualization; inhibits deiodinase; not approved for tx of hyperthyroidism |
|
Definition
|
|
Term
| produced in chief cells of parathyroid gland; secreted when plasma Ca is low; acts directly on bone to increase Ca and phosphate resorption; acts on kidney tubules to increase plasma Ca, decrease phosphate, and increase Vit. D3 in kidney |
|
Definition
|
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Term
| synthesized in kidney under positive regulation from PT gland; inhibits 25(D) 1a-hydroxylase to prevent further synthesis of self; increases absorption of dietary calcium in small intestine; induces expression of Ca uptake pump, calbindin, and ATP-dependent Ca pump in enterocytes |
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Definition
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Term
| produced by parafollicular cells and secreted when plasma Ca is high; binds to receptors in bone to inhibit osteoclast activity |
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Definition
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Term
| bisphosphonates; inhibit osteoclast function; interfere w/ malevonate pathway of cholesterol synthesis; decrease serum Ca levels; tx for: postmenopausal osteoporosis, osteoporosis in men, glucocorticoid-induced osteoporosis, Paget's dx; oral admin; contraindications: esophageal abnormalities, hypocalcemia, and severe renal failure; adverse effects: osteonecrosis of jaw, esophageal CA, back pain, arthralgia, abdominal pain, and dyspepsia |
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Definition
| alendronate and risedronate |
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Term
| bisphosphonate; inhibits osteoclasts and decreases serum Ca; used additionally for: heterotopic ossification following total hip replacement and hypercalcemia secondary to malignancy; oral or IV admin; contraindications: same plus clinically overt osteomalacia |
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Definition
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Term
| acts on Ca-sensing receptor on surface of chief cell and increases sensitivity for Ca; also decreases PTH secretion and plasma Ca levels; considered calcimimetic agent; tx: secondary hyperparathyroidism w/ chronic kidney dx, hypercalcemia w/ PT CA, and hypercalcemia in other CAs; oral admin; contraindicated in hypocalcemia; adverse effects: paresthesias, myalgias, cramping, tetany, and convulsions |
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Definition
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Term
| loop diuretic; inhibits Ca reabsorption in ascending limb in properly hydrated pts; sometimes used to treat hypercalcemia in CA pts; IV admin; contraindication: anuria; adverse effects: dehydration, postural hypotension |
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Definition
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Term
| mitogen for osteoblasts at excessive concentrations; causes increased bone formation, leads to skeletal fluorosis |
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Definition
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Term
| glucocorticoid that decreases plasma Ca in short term and induces osteoporosis long-term |
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Definition
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Term
| administration increases plasma Ca levels and decreases PTH secretion; tx for: hypocalcemia secondary to hypoparathyroidism, hypocalcemia secondary to rapid growth or pregnancy, adjunct tx of rickets/osteomalacia, and dietary deficiencies; IV admin of gluconate solution or oral admin of citrate supplements; contraindicated in V-fib or hypercalcemia; adverse effects: nausea, constipation, upset stomach |
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Definition
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