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179 Cards in this Set
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amitriptyline
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TCA
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imipramine
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archetypical TCA
MOA: blocks reuptake of NE and 5HT tertiary amines - 5HT selective; secondary - NE selective 2-3 weeks to work b/c autoreceptors must downregulate S/E (1 ergic per ring) 0. Q-like: heart blocks 1. anticholinergic: tachycardia, blurred vision, dry mouth, constipation 2. antihistaminergic: sedation and weight gain 3. antiadrenergic: orthostatic hypotension, dizziness, and drowsiness 4. may ppt a manic phase in bipolar patients 5. acute O/D = very dangerous = resp despression, delerium, hypertension, cardiac arrest! |
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DESIPRAMINE
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TCA
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nortriptyline
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TCA
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tranylcypromine
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MAO-A inhibitor (antidepressant)
selective for MAO A, so it inhibits the degredation of all 3 monoamines S/E: 1. MAOI + TCA = hypertensive crisis 2. MAOI + tyramine = hypertensive crisis 3. MAOI in slow acetylator = hepatotoxiicty 4. cardiovascular side effects 5. acute OD toxicity - agitation, delerium, mania -> sz, hyperthermia. give activated charcoal selegiline - mao b inhibitor for pd |
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fluoxetine
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SSRI
the first one. fewer anticholinergic and cardiovascular S/E than TCA S/E: 1. nausea, diarrhea, constipation 2. insomnia, nervousness 3. sexual dysfunction!!!! 4. MAOI + SSRI => serotonin syndrome = hyperthermia and muscle rigidity with wild swings in vitals and mental status, |
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paroxetine
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SSRI
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CITALOPRAM
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SSRI
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escitalopram
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SSRI
S enantiomer of citalopram, more potent, take less and begins working in 1-2 weeks |
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SERTRALINE
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SSRI
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CHLORPROMAZINE
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the archetypal first generation antipsychotic
blocks all 4 dopaminergic pathways: mesolimbic, mesocortical, tuberoinfundibular, and nigrostriatal treats only the positive symptoms S/E: D2 dopaminergic mesocortical: even more negative symptoms nigrostriatal: extrapyramidal side effects (pseudoparkinsonism, tardive dyskinesia, muscle spasms, motor restlessness) 3. tuberoinfundibular - hyperprolactinemia antihistaminergic: sedation and weight gain cholinergic: urinary retention, dry mouth, constipation, blurred vision, impaired cognition/memory adrenergic - orthostatic hypertension, reflex tachycardia, sexual dysfunction serotonin - orthostatic hypotension, sedation, and weight gain Neuroleptic Malignant Syndrome rigidity and hyperthermia with altered mental status treat with bromocriptine (DA agonist to reverse neuroleptic action) or dantrolene (RyR blocker) btw, chlorpromazine also tests pituitary function (prolactin should increase with a dose) |
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haloperidol
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first gen antipsychotic
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clozapine
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archetypal second gen antipsychotic
fewer S/E than first gen b/c only mesolimbic is blocked improve the negative symptoms (cognition, etc) as well as positive symptoms AGRANULOCYTOSIS is a side effect! |
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aripiprazole
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second gen antipsychotic
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cortisone
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not quite as potent as cortisol but doesnt agonize mineralocorticoid receptor
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hydrocortisone
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=cortisol (naturally occuring) short acting
least potent effects: 1. liver - increases glycogenolysis and gluconeogenesis 2. skel muscle - increases muscle catabolism to make precursors for gluconeogenesis 3. lymphocytes - decreases their proliferation and also blocks the phospholipase A step decreasing PG and LT production 4. skin atrophy and catabolism 5. adipocytes - lipolysis, redistribution to central adiposity 6. brain - CNS arousal - run from that bear!! 8. heart - increased blood pressure uses: 1. addison's syndrome 2. 11 beta hydroxylase deficiency given 2/3 in morning and 1/3 at night has an effect on mineralocorticoid receptor S/E 1. immune system suppression 2. cushing like body habitus 3. osteporosis (decreases osteoblast activity) 4. peptic ulcers (decreases PG secretion and therefore mucus production) 5. growth suppression in kids 6. motherfucking cataracts 7. behavior problems don't withdraw cold turkey - iatrogenic adrenocortical insufficiency also during surgery, either give a ton or wean them off of them. surgery should trigger a huge cortisol release from pain response. if they can't make enough cortisol, they may become hypotesnive and die! |
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hydrocortisone sodium phosphate
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water soluble glucocorticoid for IV use
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prednisone
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5x more potent than cortisol
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PREDNISOLONE
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active form of prednisone
give to people with liver problems who cant metabolize prednisone to its active form (ex alcoholic with chronic liver dz_ |
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triamcinolone hexacetonide
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long acting glucocorticoid b/c it has fluorine and an acetonide group
can be used topically or interarticularly b/c it is not freely diffusable |
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fludrocortisone acetate
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mineralocorticoid
1.mineralocorticoid deficiency 2. part of treatment for addison's |
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AMINOGLUTETHIMIDE
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inhibits aromatase and many enzymes in glucocorticoid synth
uses: 1. cushing's syndrome (reduces glucocorticoid prodn!!) 2. breast cancer (no longer used) chad uses it in his steroid cycles bad se/e? |
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BETAMETHASONE
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40x more potent than cortisol
can give lower dose and have no effect on mineralocorticoid |
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solumedrol
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water soluble glucocorticoid for IV use
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hydrocortisone sodium succinate
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water soluble glucocorticoid for IV use
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methylprednisolone sodium succinate
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water soluble glucocorticoid for IV use
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stanozolol
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anabolic steroid - inhibits catabolic actions of glucocorticoids
1. burn pt 2. short stature 3. anemia s/e:cardiotoxic, hepatotoxic, cause rage, androgenize women work as antiandrogens, feeding back on pituitary and blocking production of gonadotropins and eventually testosterone cause impotence and decrease secondary sex char if you take synthetic androgens with them, that's when you get boobies because they are converted to estrogen by aromatase |
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danazol
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steroid which feeds indirectly decreases estrogen production.
it feeds back on the pituitary to decrease FSH and LH production, eventually decreasing estrogen production use: endometriosis Dana dreadlock has endometriosis. |
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ETHINYL ESTRADIOL
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modified estrogen which can be given orally...
1. used with norethindrone in the combination pill 2. Aberrant growth. suppresses somatomedins. give progestin too to prevent bleeding 3. Delay of puberty (check to see if there is a gonadotropin deficiency first before using steroids as steroids can prematurely close epiphyseal plate) 3. Precocious puberty due to a tumor - use depot progestin (MPA) to suppress gonadotropin release 4. postmenopausal osteoporosis. give prog to reduce endometrail cancer risk 5. postmenopausal sx such as hot flashes. give progestin too 6. use in huge doses to treat cancer. down reg receptor? s/e: 1. breast cancer 2. cholestasis 3. feminization, gynecomastia 4. gall stones 5. breast tenderness |
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medroxyprogesterone
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=provera. methyl group added to progesterone increases its activity! acetate increases its t1/2
1. depoprovera for contraception 2. also precocious puberty |
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NORETHINDRONE
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synthetic progestin modified to decrease its metabolism
used alone in minipill and in combination pill and probably in norplant? similar to levonorgestrel |
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PROGESTERONE
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used in combination with estrogens in contraception
only active in presence of estrogen and primed estroen system the estrogen system turns on the progestin receptor 2 receptors, PRA and PRB. PRA is antagonist of the other 1. growth delay (if sufficient gonadotropins) 2. precocious puberty 3. excessive growth - large dose of estrogen + progesterone to prevent breakthrough bleeding) 4. dysfunctional uterine bleeding - prog supports endometrium 5. with hirsuitism therapy, use oral contraceptives for normal hormone function |
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TESTOSTERONE
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USE:
1. hypognadism 2. anemia (before epo) 3. anabolic agent (abused) 4. osteoporosis s/e: 1. edema/ fluid retention 2. increases plasma cholesterol and lowers HDL 3. liver disorders - cholestasis 4. sleep apnea 5. psychol disturb converted to 5DHT by 5alphaR to have effect in the genitalia and hair follicles methyltestosterone - orally active but hepatotoxic. also cardiotoxic. |
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CLOMIPHENE
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weak estrogen agonist / antiestrogen
opposes estrogen's inhibition on LH and FSH release. causes LH and FHS release. for some reason, LH builds up and is released when you stop giving them clomiphene. ?(mulitiple ova because estrogen receptor is blocked) |
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flutamide
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Flutamide is an oral nonsteroidal antiandrogen used as an antihormonal agent in the treatment of metastatic prostatic carcinoma.
used with gonadotropin agonists (chronic=decrease Gn effect) (Leuprolide) for 1. prostate cancer 2. hirsuitism 3. baldness (situations of too much androgens) Mark tidwell plays the skin flute. he is bald and hairy |
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finasteride
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5 alpha reductase inhibitor
1. prevention of prostate cancer 2. also for hair growth |
inhibits that final step of testosterone activation |
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RALOXIFENE
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SERM - its large side chain group prevents binding of certain helper proteins in the transcription apparatus
1. agonist in bone 2. antagonist in uterus use: prevention and treatment of osteoporosis! high aff for ERalpha and beta |
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TAMOXIFEN
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SERM - anti-estrogen used to prevent and treat breast cancer (estrogen receptor + tumors)
1. anagonist - breast 2. agonist - bone, liver, endometrium (this doesnt matter as much) mild therapy, effective, doesnt make pt sick receptor antagonist (antiestrogen) in breast *money* |
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mifepristone
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RU486 - antiprogestin
competitive inhibitor of the progesterone receptor blocks progesterin support of the endometrium and sensitizes it to prostaglandins. taken orally with vaginal suppository of progstaglandin E1. terminates preg in 1st 7 weeks |
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lorazepam
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benzodiazepine (shorter acting)
In order to prevent this state, you give them drugs to quiet the brain down and gradually withdraw the medication. One such drug is Librium [chlordiazepoxide], a long-acting benzodiazepine that self-tapers as you decrease the dose. If they have liver injury (liver function test 3x normal) you would give a shorter acting drug such as Ativan [lorazepam] (recommended) or Serax [oxazepam] (very short acting). |
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oxazepam
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benzodiazepine (very short acting)
good for etoh w/d. use instead of chlordiazepoxide if liver injury is present. |
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CHLORDIAZEPOXIDE
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benzodiazepine
gold standard for for etoh w/d. if pt has liver failure, use lorazepam or oxazepam |
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disulfiram
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blocks acetaldehyde DH
used to prevent alcoholics from drinking |
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naltrexone
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opioid receptor antagonist (oral)
used to treat opiate intoxication also used to reduce relapsing and craving in opiate and etoh addiction recovery |
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NALOXONE
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opioid receptor antagonist (IV - not active oral)
USES: 1. opiate intoxication (OD) 2. rehab (opiate and etoh) - reduces relapsing and craving 3. in buperorphine pills to keep addicts from injecting them to get high |
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chloral hydrate
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barbituate like drug
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zolpidem
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ambien. it's abusable
catch some zzz's motherfucker |
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gammahydroxybutyrate
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good anesthetic, no analgesic properties
1. binds GABA-B receptors and inhibits norepi release 2. inhibit dopamine release at low doses but increase dopamine release at high dose profound CNS depression with short term amnesia coma withdrawal is similar to alcohol but can last 2 wks unless you put them to sleep they will become psychotic |
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buprenorphine
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opiate partial agonist
can be used to treat opiate withdrawal |
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opiates
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affect mu receptors
suppress cough slow down the GI tract decrease urinary flow respiratory depression decreases HR and BP analgesic |
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METHADONE
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opiate agonist (loong acting - long half life)
use: 1. pain 2. opioid withdrawal / rehab for pain: long acting dose q6h adjust every 6-7 days excellent for NEUROPATHIC pain |
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ACETAZOLAMIDE
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CA inhibitor
azul - blue sky mountain sickness Uses: 1. urine alkalinization a. to increase clearance of acidic drugs b. to increase solubility of uric acid stones 2. prophylaxis for high altitude pulmonary edema 3. glaucoma (not used anymore) S/E: 1. hyperchloremic metabolic acidosis 2. calcium phosphate stones 3. K wasting 4. NH3 intoxication (esp in liver failure pt) |
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FUROSEMIDE
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loop diuretic - blocks the Na/K/2Cl transporter in the TAL
Uses: 1. acute volume overload (e.g. pulm edema) 2. hypercalcemia (give saline too because these pts have nephrogenic diabetes insipidus and are not responding to their ADH and are volume contracted) S/E: 1. K wasting with acidosis 2. ototoxicity (you forget this) 3. hypercalciuria and calcium oxalate stones |
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HYDROCHLOROTHIAZIDE
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works in DCT - blocks Na/Cl transporter
Uses: 1. HTN - hypertension, esp. in pts with poor kidney function 2. CHF - congestive heart failure. they are volume overloaded 3. hypercalciuria and calcium oxalate stones (will increase reabs of calcium. subseq dec in PTH and eventually dec in vitamin D will keep blood Ca from rising). limit salt intake b/c it will blunt effects of thiazide S/E: 1. K wasting and metabolic alkalosis 2. increase blood lipids, uric acid, and glucose levels *may work in PCT, too, if used in combination with loop diuretics to unmask PCT action |
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hydrochlorothiazide + triamterene
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combination of
DCT diuretic & ENac blocker (K sparing diuretic) |
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amiloride
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ENac blocker (K sparing diuretic)
Uses: 1. Primary and Secondary aldosteronism primary: conn's syndrome secondary: liver failure, kidney failure, heart failure S/E 1. hyperkalemia 2. metabolic acidosis 4. acute kidney injury and kidney stones (rare s/e) |
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TRIAMTERENE
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ENac blocker
(K sparing diuretic) Uses: 1. Primary and Secondary aldosteronism primary: conn's syndrome secondary: liver failure, kidney failure, heart failure S/E 1. hyperkalemia 2. metabolic acidosis 4. acute kidney injury and kidney stones (rare s/e) |
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aldoctone
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mineralocorticoid blocker(K sparing diuretic)
1. Primary and Secondary aldosteronism primary: conn's syndrome secondary: liver failure, kidney failure, heart failure S/E 1. hyperkalemia 2. metabolic acidosis 3. gynecomastia and BPH with aldoctone and alclarinone 4. acute kidney injury and kidney stones (rare s/e) |
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alclarinone
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mineralocorticoid blocker(K sparing diuretic)
Uses: 1. Primary and Secondary aldosteronism primary: conn's syndrome secondary: liver failure, kidney failure, heart failure S/E 1. hyperkalemia 2. metabolic acidosis 3. gynecomastia and BPH with aldoctone and alclarinone 4. acute kidney injury and kidney stones (rare s/e) |
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SPIRONOLACTONE
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mineralocorticoid blocker(K sparing diuretic)
1. Primary and Secondary aldosteronism primary: conn's syndrome secondary: liver failure, kidney failure, heart failure S/E 1. hyperkalemia 2. metabolic acidosis 3. gynecomastia and BPH with aldoctone and alclarinone 4. acute kidney injury and kidney stones (rare s/e) |
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CHLORTHALIDONE
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thiazide diuretic
works in DCT - blocks Na/Cl transporter Uses: 1. HTN - hypertension, esp. in pts with poor kidney function 2. CHF - congestive heart failure. they are volume overloaded 3. hypercalciuria and calcium oxalate stones (will increase reabs of calcium. subseq dec in PTH and eventually dec in vitamin D will keep blood Ca from rising). limit salt intake b/c it will blunt effects of thiazide S/E: 1. K wasting and metabolic alkalosis 2. increase blood lipids, uric acid, and glucose levels *may work in PCT, too, if used in combination with loop diuretics to unmask PCT action |
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hydrochlorothiazide + triamterene
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thiazide + K sparing diuretic (ENac blocker)
=diazide mismatch because triamterene is short acting hydrochlorothiazide + amiloride is a better drug b/c both are long acting |
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hydrochlorothiazide + amiloride
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hydrochlorothiazide + amiloride
thiazide + K sparing both are long acting |
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MANNITOL
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osmotic diuretic
1. intracellular volume expansion (cerebral edema) 2. intratubular blockage ( rhabdomyolysis, transfusion reaction -> cast nephropathy) S/E: 1. hypernatremia 2. volume depletion 3. acute kidney injury due (toxic!) 4. if the kidneys arent working this drug will make things worse! |
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TOLVAPAN
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V2 (ADH receptor) antagonist
tolVapan V V V V V V use: 1. SIADH (can occur in chronic bronchitis, pulmonary tuberculosis, or lung tumors) 2. heart failure - heart not pumping so body thinks it is volume depleted so ADH is too high S/E 1. hypernatremia tolvapan. don't get mixed up with tolcapone (which is a comt inhibitor) |
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lorazepam
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benzodiazepine
lorazepam can be given IM, but can cause tissue necrosis. |
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diazepam
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benzodiazepine
diazepam can be given IV or rectally (di). according to dr boyce, it is an older agent, not soluble in water and can cause phlebitis uses: 1. anticonvulsant 2. insomnia 3. anxiety 4. sedation and amnesia for procedures 5. etoh withdrawal and other sedative withdrawal 6. muscle spasm (these are from the brain not modulating the reflex arc) s/e of bzd not fatal - therapeutic index of 1000 1. respiratory depression 2. CVS depression notes: cross tolerance to ethanol. synergistic effects with alcohol, opiates, anti-histamines |
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midazolam
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benzodiazepine
can be given IM (Midazolam Muscle) |
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phenytoin
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anticonvulsant (Na blocker)
partial, generalized, and status epilepticus must monitor serum drug levels! Notes 1. P450 inducer -> 0 order kinetics, saturates it. additional drug will cause huge increase in conc. -> drug interactions e.g. halothane hepatotoxicity 2. precipitates in D5W, only give with normal saline! 3. can cause tissue necrosis when given peripherally!! (lose a limb! if poor circulation!!) dont give in peripheral IV if at all possible S/E 1. ataxia, nystagmus, and diplopia 2. Skin exfoliation 3. Stevens-Johnson's syndrome - autoimmune rash, skins sloughs off -> infection. stop taking phenytoin and call your dr. if you get a rash!!! 4. Hirsuitism, Gingival Hyperplasia, Folate depletion |
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phosphenytoin
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anticonvulsant (Na channel blocker)
salt form is better tolerated in the veins with less tissue necrosis |
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CARBAMEPAZINE
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anticonvulsant (Na blocker)
used for partial and generalized seizures Notes: 1. autoinducer of hepatic enzymes, so must increase dose S/E 1. diplopia and ataxia 2. leukopenia 3 . bone marrow suppression (rare) |
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lamotrigine
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anticonvulsant (Na blocker)
partial seizures S/E rash (lamers have a wash) somnolence (lamers sleep) lamer = sleepy person with a rash |
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topiramate
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anticonvulsant (Na blocker and enhances GABA - both classes - unique!)
used for partial and generalized * used to treat Lenox-Gastaut syndrome (the head banging seizure kids) mnemonic - so they will stop hitting the top of their heads!! S/E slowed speech kidney stones paresthesias glaucoma |
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ethosuximide
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anticonvulsant (Ca blocker)
good for absence sz S/E dose dep gastric distress hyperactivity, dizziness, headache |
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vigabatrin
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anticonvulsant
enhances inhibition by GABA |
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gabapentin
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anticonvulsant
enhances inhibition by GABA |
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tiagabine
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anticonvulsant
enhances inhibition by GABA |
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ethanol
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enhances GABA in VTA
inhibits Glu in VTA has effects on serotonin and opiate receptors too CNS depression |
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phenobarbital
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barbituate (increases length of GABA Cl ionophore opening)
good for generalized seizures prodrug is Primidone S/E sedation, depression, hyperactivity, cognitive problems |
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primidone
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prodrug of phenobarbital
barbituate |
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oxacarbazepine
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anticonvulsant (Na blocker)
used for partial and generalized like carbamepazine 1. hyponatremia |
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VALPROATE ACID
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anticonvulsant (Na and Ca blocker)
generalized (common!) and partial S/E: (Mrs. Val) 1. lethargy 2. tremor 3. alopecia 4. liver failure 5. weight gain |
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levetiractem
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partial sz - unknown MOA
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zonisamide
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reduces Ca channels
partial sz |
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trazadone
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atypical antidepressant
1. blocks 5HT reuptake 2. blocks postsynatpic 5HT2 receptors (thus increasing 5HT1 activity) |
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BUPROPION
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atypical antidepressant
blocks DA and NE reuptake used for smoking sessation lowers seizure threshold - dont give to anorexics or bulemics |
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venlafaxine
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atypical antidepressant
inhibits 5HT and NE reuptake (like TCA...) causes nausea via 5HT3 receptor i guess you can throw up while you're fucking sexual s/e go away |
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mirtazapine
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1. blocks alpha2 autoreceptors
2. blocks postsynaptic 5HT2 receptors a mirthful blocker no significant sexual dysfunction |
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duloxetine
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selective 5HT and NE reuptake inhibitor (like a TCA du=2)
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lithium carbonate
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treats bipolar affective disorder
inhibits phosphatase, blocking regeneration of inositol S/E - narrow therapeutic index 1. nausea, vomiting, diarrhea, weakness, tremor, polydipsea 2. nephrogenic diabetes insipidus, hypothyroidism, arrhythmia b/c lithium decreases effect of ADH, it can be used to treat SIADH |
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olanzepine + fluoxetine
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second gen antipsychotic + SSRI
treats bipolar affective disorder |
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AMANTANDINE
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antiviral agent, yet blocks Glutamate Receptors
treats Parkinson's disease treats dyskinesia caused by levodopa treats extrapyramidal side effects of first gen antipsychotics (pseudoparkinsonism and tardive dyskinesia) |
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BENZTROPINE
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anticholinergic (a PD drug)
1. treats Parkinson's disease good for young patients, not for elderly (thinking chemical->dementia) 2. treats extrapyramidal side effects of first gen antipsychotics (pseudoparkinsonism and tardive dyskinesia) |
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BROMOCRIPTINE
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dopamine agonist (ergot alkaloid)
1. Parkinson's Disease 2. acromegaly / gigantism (reduces GH secretion) 3. hyperprolactinemia ass'd with partuition, abortion, and prolactinomas. (decreases prolactin secretion) 4. treat neuroleptic malignant syndrome (caused by first gen antipsychotics) s/e:fibrosis s/e: sedation, hallucinations, compulsive behavior (gambling) |
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dantrolene
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ryanodine receptor blocker (a muscle relaxant)
used to treat neuroleptic malignant syndrome NMS hyperthermia and rigidity with altered level of consciousness think carlos dansby = muscle |
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HYDROMORPHONE
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opiate - 3rd tier
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CODEINE
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antitussive
opiate - second tier - often with acetaminophen |
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fentanyl
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opiate - 3rd tier
fentanyl patch dont reach Cmax for 24 hours, give them something in the meantime doesnt go away when patch is off lasts 24-72 hours less in skinny pt (fat abs) less in febrile sweaty pt |
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meperidine
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synthetic opiate. not recommended.
pain reliever. has its place: normal kidney and liver function and a clear source of pain such as trauma highly emitogenic (give phenergan with it) *SEIZURE!! - toxic metabolite normeperidine might build up in patient with renal failure and cause seizure. contraindication: renal failure or liver failure |
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oxycodone
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opiate - 2nd tier, longer acting oxycodone (like oxycontin) are 3rd tier
OPIATES conjugated in liver and excreted by kidney S/E CONSTIPATION (give a laxative!) - only S/E that wont go away w/o help nausea/vomitting (use dopamine blocking antiemtics) urinatry retention sedation dry mouth Resp. Depression is uncommon. |
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pentazocine
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NOT recomended.
mixed agonist. compete with agonists. ceiling effect not used much for pain management, but used with anesthesia to reverse opioid effects |
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PROPOXYPHENE
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NOT RECOMENDED opiod
not any better than placebo 3 P's for placebo. the placebo fiend. toxic metabolite at high doses |
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dextromethorphan
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opiate. antitussive. in cough syrup
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immediate acting opiates
Codeine, Hydrocodone, Morphine, Hydromorphone, Oxycodone (plain) |
last 3-5 hours given PO or PR
(much shorter when given by IV bolus) reach max concentration in: Cmax : 6 / 30 / 60 IV/ SC / PO give q4h and dose find mod pain inc 25-50% each day severe pain inc 50-100% each day |
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extended release opiates
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improve compliance, convenience, no bolus effect (roller coaster), less potential for abuse
if patient goes into renal failure, decrease dosage, switch from routine dosing to prn, change to short acting, and hydrate patient. for the love of god, dont use methadone. dose tid, bid, or qd adjust dose every 2-4 days give 10% as breakthrough dose |
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selegiline
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MAO-B inhibitor
parkinson's drug may be neuroprotective too if it keeps chemicals like MPTP from being activated dont eat wine or cheese! |
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tolcapone
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COMT inhibitor
bust a cap in comt!!!!! it takes a toll on your liver!! black box decreases LDOPA degredation in the periphery s/e of LIVER FAILURE! black box warning. must have liver function tests periodically |
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encaptone
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COMT inhibitor
decreases LDOPA degredation in the periphery safe drug |
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LEVODOPA
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L-DOPA
parkinson's drug relieves sx but may contribute to progression of the disease. usually reserved for people no longer responsive to dopamine agonists or anticholinergics |
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carbidopa
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Decarboxylase inhibitor
given in sinemit LDOPA is not converted to dopamine in the periphery by the decarboxylase where it causes nausea |
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pergolide
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dopamine agonist (ergo alkaloid)
use for parkinson's disease nonselective s/e: fibrosis s/e: sedation, hallucinations, compulsive behavior (g |
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pramipexole
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D2 selective agonist (not ergot)
Parkinson's disease drug good for young patients to delay having to use levodopa may be neuroprotective s/e: sedation, hallucinations, compulsive behavior (gambling) pex = good for young ppl with parkinsons - would have been good for Michael J |
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ropinrole
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D2 selective agonist (not ergot)
Parkinson's disease drug good for young patients to delay having to use levodopa may be neuroprotective s/e: sedation, hallucinations, compulsive behavior (gambling) |
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BENZOCAINE
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commonly used topical anesthetic because it diffuses across membranes easily
benzocaine and procaine are both esters s/e: methemoglobinemia |
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bupivicaine
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local anesthetic
highly protein bound, so long duration of action |
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COCAINE
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blocks reuptake of catecholamines (potentiates)
amide and ester linkage used as a local anesthetic long ago (Na channels) |
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lidocaine
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most common local anesthetic
local anesthetic MOA: 1. unprotonated neutral form diffuses into membrane and shifts the Na (and K) channels into unresponsive conformations 2. unprotonated form diffuses through membrane, is protonated, and then goes into the pore, binds to specific domain and blocks the pore O/D: into central 1. twitching 2. seizure 3. metallic taste 4. tinitis 5. hypotension 6. arrhythmia |
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EMLA CREAM
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Eutectic Mixture of Local Anesthetics (EMLA cream)
mix lidocaine and prilocaine, lowering their melting point and put it in an oily substance. can diffuse across skin and membranes easily. great to use to start IV's in children and superficial laser procedures |
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PROCAINE
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ester anesthetic (most are amides)
used in dentistry (novocaine) |
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chirocaine
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S enantiomer of bupivicaine.
hint: S is SAFE less cardiotoxic with longer duration than the racemic mixture |
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local anesthetic toxicity
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CNS excitation -> cardiovascular depression
tinnitis, metallic taste, quivering, lethargy, SEIZURE arrhythmia, hypotension |
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prilocaine
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local anesthetic (topical)
side effect of methemoglobinemia (along with benzocaine) |
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tetracaine
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long lasting local anesthetic used in spinal anesthesia (thru interspinous lig into subarachnoid)
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ropivicaine
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common local anesthetic. long duration of action, so used in epidurals.
bupivicaine and chirocaine have a long duration of action as well, and they are used in epidurals (epidural = more of a sectional block. bathes spinal nerves in area) |
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OCTREOTIDE
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synthetic somatostatin with a D amino acid
decreases pituitary secretion of the cousins (prolactin, GH, TSH) Uses: 1. acromegaly (DRUG OF CHOICE, better than bromocriptine) 2. hormone producing GI tumors, carcinoid syndrome, carcinoma 2. hyperprolactinemia? |
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leuprolide
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GnRH analog
1. acute usage: increases LH and FSH release. then increased sex hormone secretion induce ovulation 2. chronic usage: downregulates GnRH receptors and leads to decreased LH and FSH. then decreased sex hormone secretion. uses: (acts as antiestrogen) 1. endometriosis 2. prostate cancer 3. breast cancer 1. polycystic ovary syndrome 2. endometriosis 3. precocious puberty 4. prostate cancer 5. breeast cancer |
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pitocin
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synthetic oxytocin (has a D amino acid)
1. milk letdown in lactating women 2. uterine contractions uses 1. induce labor 2. induce milk letdown with nursing (contract myoepithelial cells) 3. abortifacient 4. stop postpartem bleeding |
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SOMATROPIN
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synthetic GH.
given every night, which is suboptimal (not pulsatile) uses: 1.growth hormone deficiency 2. sometimes wasting |
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METHYLERGONOVINE
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**
control postpartem bleeding, but NOT for labor induction because it can hurt the baby with too much uterine contraction stetler |
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desmopressin
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synthetic vasopressin with a D amino acid
V2 receptor agonist (selective for the ones on the kidney) 1. can be used in neurogenic diabetes insipidus to increase water reabsorption 2. nocturnal enuresis 3. obstructive sleep apnea (associated with diabetes insipidus, nocturnal enuresis, and obesity) |
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IGF1
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IGF1
USES: 1. pituitary dwarfism 2. growth problems due to GH resistance (GH receptor prob, bypasses it) remember that the IGF binding proteins arent there for regulation may be good for wasting patients, burn patients |
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prolactin
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prolactin stimulates milk production (NOT LETDOWN)
stimulation 1. suckling 2. cold 3. TRH 4. sleep 5. stress 6. pregnancy inhibition 1. dopamine MAY CAUSE INFERTILITY! hypoprolactinemia 1. chlorpromazine 2. haloperidol (DA blockers) hyperprolactinemia treated with dopamine agonists 1. bromocriptine (ergo hell yeah) 2. pergolide 3. cabergoline 4. quinagolide hypoprolactinemia |
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VASOPRESSIN
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triggers:
1. decreased volume 2. increased osmolarity functions: V1: vasoconstriction V2: increased expr of aquaporin 2 at cell membrane, increased water reabsorption lack of vasopressin causes neurogenic diabetes insipidus lack of response - nephrogenic diabetes insipidus |
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combination pill
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ethinyl estradiol + norethindrone or levonorgestrel
most effective birth control suppresses LH and FSH, therefore, ovulation never occurs days 25-5, hormones are withdrawn and endometrium is shed S/E: 1. breakthrough bleeding 2. weight gain, breast growth 3. post contraceptive infertility 4. cholestasis. watch out in people with liver disease. could become jaundiced. 5. migraines - indicate risk of stroke! 6. increase glucose tolerance - watch out in diabetics! 7. high doses of estrogen - thromboembolism, myocardial infarction, and stroke (coagulopathY!) 8. high doses - increases breaset cancer risk! |
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norplant
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levonorgestrel in silastic tube slow release
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mini-pill
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norethindrone only
changes mucus high failure rate, but no estrogen s/e used throughout cycle |
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androgens
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have androgenic and anabolic effects
are estrogen precursors and can lead to increased estrogen production |
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mestranol
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synthetic estrogen which is demethylated for a slow release. avoid bolus effect.
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gonadotropins
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uses:
1. delayed puberty due to gonadotropin deficiency. allows more physiologic than just giving sex hormones. if gonadotropins are low in a child with delayed puberty, use gonadotropins before sex hormones |
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DIETHYLSTILBESTROL
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stilbene estrogen that is no longer used, thank God
used to be used for birth control until it was realized that it caused uterine cancer and birth defects |
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SODIUM THIOPENTAL
(same as pentothione / thiopentone) not same as pentobarbital |
barbituate
uses: 1. sedative (not nighttime, bzd is better) 2. detox 3. anticonvulsant 4. good for C sections. wait for fetus to redistribute (3-5 min) bzds are better sleeping agents reduce dose in aged, HYPOVOLEMIC, INTOXICATED, anemic, hypothermic, or chf b/c you can kill them also, do not give with succinylcholine b/c it will precipitate in the IV S/E: (TI =4) 1. resp. depression. decreases response to hypoxia 2. hypotension (venodilator) 3. decreases sympathetic output contraindication: 1. upper respiratory obstruction 2. cardiac tamponade (lower blood pressure in a patient whose heart cant response is a BAD IDEA!) hypovolemic (pearl harbor) 3. ischemic heart disease congestive heart failure 4. porphyria |
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KETAMINE
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a sedative. similar to PCP. causes dissociative anesthesia, whatever that is
2. only sedative that has analgesic properties. causes analgesia by blocking the ASPARTATE receptor at the spinal cord. blocks wind-up 3. great because of its cardiovascular stability 4. used for pre-emptive analgesia - minimizes requirements for analgesia post op S/E: excitement, hallucinations, and flashbacks during onset |
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alprazolam
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bzd
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FLUMAZENIL
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competitive blocker of BZD
blocks the action of benzodiazepines binds to same site on the GABA Cl ionophore but has no action USES 1. reverse BZD effects after a procedure 2. BZD overdose |
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pentobarbital
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barbituate
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VDSS
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apparent volume of distribution in a steady state
after the alpha phase of distribution (drugs goes into tissues), beta phase should be a straight line when [] is graphed in a log scale because of first order kinetics if you draw the line back to time 0, you get the imaginary concentration at time 0 divide the weight of the drug by this concentration to get the VDSS |
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baclofen
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for muscle spasm. cuts back on the first half of the reflex arc in the spinal cord. the spinal cord is also in the back btw.
inhibits the release of excitatory transmitters in the spinal cord in the first half of the reflex arc. |
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etomidate
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sedative, neither a barb or a bzd
not smooth on induction, causes clonus which can make a procedure difficult and interfere w/ ecg reading in cardiac procedure etoh - etomidate induction isnt smooth. like a shot of cheap whiskey - clonus |
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sodium amytal
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barbituate
used for WADA test injected into carotid lateralizes cerebral speech dominance in neurosurgery |
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buspirone
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anxiolytic
used similarly to a bzd get anxious person out of that downward spiral |
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GLIPIZIDE
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sulfonylurea = secretagogue
MOA: block K channel Use: Type II DM S/E: hypoglycemia weight gain |
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GLYBURIDE
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sulfonylurea = secretagogue
starts with g and rhymes with wide MOA: block K channel Use: Type II DM S/E: hypoglycemia weight gain |
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REPAGLINIDE
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meglinitide = secretagogue
MOA: bind to a different site on the K channel and block it use: DM Type II S/E: hypoglycemia weight gain nate and repa |
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NATEGLINIDE
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meglinitide = secretagogue
MOA: bind to a different site on the K channel and block it use: DM Type II S/E: hypoglycemia weight gain nate and repa |
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METFORMIN
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biguanide - lowers blood glucose by
1. acting on liver to decrease glucose production 2. increasing glucose uptake (insulin sensitivity!!!) better than sulfonylureas and meglitinides b/c it is insulin-sparing drug (does not have their side effects of hypoglycemia or weight gain either) S/E 1. *lactic acidosis* - board question alert. the liver doesnt do its job of taking up lactate as well ** 2. diarrhea 3. abdominal discomfort |
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PIOGLITAZONE
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a thiazolidinedione (increases insulin sensitivity)
*must monitor liver function tests s/e: 0. LIVER FAILURE!!!! 1. weight gain 2. edema 3. hypoglycemia (esp. if taken with insulin / secretagogues because they work together) |
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ROSIGLITAZONE
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a thiazolidinedione
1. big one - (increases insulin sensitivity) 2. decreases liver release of glucose (same as biguanides, but reverse importance) *must monitor liver function tests s/e: 0. LIVER FAILURE!!!! 1. weight gain 2. edema 3. hypoglycemia (esp. if taken with insulin / secretagogues because they work together) |
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ACARBOSE
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alpha glucosidase inhibitor. delay carbohydrate absorption. this keeps glucose from peaking out so high postprandially (this may be the main cause of damage in DM)
s/E: flatulance and bloating (do bacteria eat the carbs?) |
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REGULAR INSULIN
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hexameric with zinc
(hexamer favored over monomer) must take 45 minutes before eating works for 4-8 hours. too long to optimally control postprandial hyperglycemia but too short for once/ day |
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LYSPRO INSULIN
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rapid acting insulin
AA rearrangement favors monomer over hexamer |
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insulin detemir
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long acting insulin (1/day)
effects for 24 hours has a fatty acyl group attached to it, so it associates with albumin. it also self associates well. bound to albumin, it is not filtered by kidney or broken down by proteases as fast few S/E from binding to albumin b/c there are 100 million albumin binding sites and much less detemir so the acyl group makes it long lasting |
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glulisine
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rapid acting insulin
AA rearrangement favors monomer over hexamer |
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ULTRALENTE INSULIN
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long acting. similar to NPH (int) but lasts even longer?
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insulin aspart
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rapid acting insulin
AA rearrangement favors monomer over hexamer |
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15 in 15
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15 g carbs and check in 15 min
used to treat hypoglycemia in conscious patients |
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glucagon injection
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to treat hypoglycemia in an unconscious patient
works for 15 min, long enough to get an IV in |
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NPH INSULIN
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neutral protamine hagedorn
intermediate acting insulin (2/day) insulin + salmon protamine to bind it and release it slowly cloudy. when mixing, draw up regular insulin first not to contaminate the regular insulin with the salmon protamine. twice / day dosage duration 12-16 hours |
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GLARGINE
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long acting insulin (1/day)
has 2 Arg residues kept in an acid buffer 98% precipitates in physiologic pH of 7.4 b/c it has an isolectric point (pKa) of around 7.4. normal insulin has a pKa of 5.5. the arginines raise this to 7.4 it releases slowly because of this pH effect probs: stings when injected (acid buffer) CANNOT be MIXED with regular insulin b/c it will precipitate |
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exubera
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inhaled insulin
rapid acting low bioavailability and $$, but increases compliance type 1 - should be used in conjunction with a longer acting insulin type 2 - can be monotherapy or with oral drugs contraindications: 1. smokers (last 6 mo) 2. lung dz. (asthma, COPD) 3. pregnant women - risk not yet ruled out |
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treatment for hyperglycemia and hypoglycemia
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hyperglycemia
1. IV glucose 2. IV saline *3* when glucose goes below 300 switch to IV 5% glucose to prevent cerebral edema (happens with rapid change in osmolarity and hypoglycemia (crash) hypoglycemic / KA 15 in 15 if conscious if unconscious and seizing 1. glucagon shot 2. start IV 3. IV glucose anticipate nausea/ vomitting |
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symlin
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synthetic amylin
uses: 1. DM type 1 and 2 2. weight loss?? Amylin - released by the pancreas along with insulin. 3 effects which slow glucose appearance in blood 1. signals brain to stop feeding (satiety center) 2. signals stomach to slow gastric emptying, 3. signals liver to decrease glucose secretion |
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exenatide
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synthetic glp-1
USES: 1. DM Type 1 and 2 2. weight loss! Glp-1 - 2 effects that decrease glucose appearance 1. increases amylin production 2. tells brain to stop feeding (satiety center) hint:execute your weight loss tide yourself over |
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TUBOCURARINE
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the prototypical non-depolarizing neuromuscular blocker (NDNMB)
effect on prejunctional recepors: causes fade (mobilization) MOA: binds the alpha subunit of the acetylcholine receptor yet has no agonist activity. it blocks the pore. S/E: 1. hypotension from autonomic ganglionic block |
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SUCCINYLCHOLINE
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the only depolarizing neuromuscular blocker
can act classically (Accom) or nonclassically (Phase II) 1. classical action - causes an accomodation block (phase 1 block), binds the alpha subunit of the acetylcholine receptor. is an agonist, however it stays bound for 5-7 minutes (5-10?) the time dependent gate closes, and the pore is now blocked used when rapid onset and rapid recovery are desired 2. non classical. prolonged SC (SC drip) can cause a phase II block (desensitization) effect on prejunctional receptors: causes fasciculation (curare causes fade) S/E MALIGNANT HYPERTHERMIA 1. potassium release** 2. intraocular pressure increase 3. gastric pressure increase 4. muscle pain All about second does effects SECOND dose effects, esp in infants-> bradycardia SC blocks nicotinic and muscarinic. muscarinics recover faster, and in infants, muscarinic system is more mature than their nicotinic system the second dose will stimulate only muscarinics on the heart, causing bradycardia infants, denervation patients, spinal chord injury, severe trauma, burns 1. receptors in immature form 2. receptors may be extrajunctinoal due to lack of MEP they open longer and let more K out. they are not in the junction, and it gets into blood HYPERKALEMIA!!!--> V tach! in newborns, burn patients, trauma, and denervation causes immature receptors (gamma rather than epsilon subunits) to stay open longer and release K+, which can cause cardiac arrhythmias). this is especially important in newborns (lots of imm) or denervation, burns, and severe trauma pts (receptors regress back to imm) contraindicated: BURNS NEWBORNS DENERVATION SEVERE TRAUMA CHRONIC RENAL FAILURE (high K already) |
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atracurium
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non-depolarizing neuromuscular blocker (NDNMB)
atra cur - curarine!!! effect on prejunctional recepors: causes fade (mobilization) MOA: binds the alpha subunit of the acetylcholine receptor yet has no agonist activity. it blocks the pore. S/E: 1. hypotension from autonomic ganglionic block S/E: atracurium is metabolized by the hoffman reaction. its metabolite, laudanosine crosses the BBB and causes seizures. hoffman means that it will eventually be eliminated even w/o enzymes |
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botulism toxin
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blocks release of Ach (Fusion blocker)
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agents which increase NM block and therefore interact with NM blockers
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1. inhalation anesthetics which increase NM block.
2. aminoglycoside antibiotics which increase NM block 3. magnesium (preeclamplasia rx) - also increases NM block |
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aminoglycosides
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antibiotics
block AchR, bad for MG patients! |
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dibucaine
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assess plasma cholinesterase activity before giving succinylcholine to make sure it will be broken down. normal is 80% inhibition.
abnormal might be only 20%?? |
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