T4: just drogas Flashcards
hydrocortisone (cortisol) (cortaid)
short-to medium-acting glucocorticoid
anti-inflam: 1.0
mincort: 2+ (potent!)
initial tx of adrenalcortical insufficiency (also anti-inflam, UC)
prednisone (intensol)
short-to medium-acting glucocorticoid
anti-inflam: 4.0
mincort: 1+ (slight but signif)
anti-allergic, AIs, SLE, collagen, skin stuff, edema, endocrine, GI, blood, MS, Ca, eye, resp, rheum, tub. meningitis
methylprednisolone (medrol)
short-to medium-acting glucocorticoid
triamcinolone (nasocort)
Intermediate-acting glucocorticoid
anti-inflam: 5.0
mincort: 0 (none!)
intralesional, allergic rhinitis, eye, asthma, topical, adrcort insuff, endocrine, GI, blood, NS, kidney, rheum, allergic, SLE, resp
dexamethasone (baycadron)
long acting glucocorticoid
anti-inflam: 20-30!!
mincort: 0 (none!)
anti-inflamm., immunosuppr (lots) manage cerebral edema, sep. shock, swelling, dx agent (cushing’s), antiemetic, eye (conjunct), ear (OE)
metyrapone (metopirone)
Glucocorticoid synthesis inhibitor and antagonist
inhibits CYP11B1 (11 β-hydroxylase) which is the enzyme that converts 11-deoxycortisol to cortisol (both cortisol and ald. inhib)
ketoconazole (nizoral)
Glucocorticoid synthesis inhibitor and antagonist, antifungal
inhibits CYP17 (17 α-hydroxylase) and at higher concentrations CYP11A1 (cholesterol–>pregnenolone) effectively blocking all steroid biosynthesis
*most effective inhibitor for Cushing’s disease, acts quickly, can add metyrapone *synergism
fludrocortisone
synthetic mineralocorticoid agonist
both glucocorticoid and mineralocorticoid activity
- added if using prendnisone/prednisolone or reduced dose hydrocortisone for 1/2 adrenocortical insufficiency (1: Addison’s) (need mineralcort. activity)
- Na+ losing adrenogenital syndrome
spironolactone (aldactone)
glucocorticoid and mineralocorticoid antagonists
synthetic c 17- lactone- competes w. aldosterone (kidneys)
mineralcort. activitiy
edema, excessive aldosterone excretion? HTN, CHF etc. hypokalemia
normalize K+ before surgery (and low Na+ diet)
cosyntropin (cortrosyn)
glucocorticoid, mineralocorticoid, androgen, progesterone and estrogen agonist
synthetic derivative of ACTH
ddx prim. adrenal from secondary (pit) adrenocortical insuff.
aspirin
antiplatelet
irreversible*(for life of platelet) inactivation of COX 1 (endo. cells can resyn. enzyme)
suppr. syn of TXA2 (proaggr) and PGI2 (vadodil.)
(low dose sel. inhibs. TXA2 gen, preserves PGI2 prod.)
tx: prev. ME, ischemic attack, stroke, art. thrombi, vein graft occlusion (160-325 mg)
adverse: abd discomfers, epigastric pain, heartburn, nausea, GI bleeding, operative bleeding (w. warfarin), imp. hemostasis in mom/fetus
dipyridamole (persantine)
antiplatelet
blocks platelet adhesion to the vascular subendo. by inhibiting phosphodiesterase–>inc. cAMP (via inc. AC)
clopidogrel (plavix)
antiplatelet
inhibits ADP binding to receptor (P2Y12 component)–>prevents activation of GPIIb/IIIa, irreversible
tirofiban HCl (aggrastat)
antiplatelet
heparin (hep-lock)
anticoagulant
negatively charged, sulfated mucopolysacchs. (syn. in mast cells, abundant in lungs)
binds lys residues of protease inhib antithrombin III (neg moieties)
inactivates active factor Xa, thrombin (IIa), platelets
fast!
IV, subQ
enoxaparin sodium (lovenox)
anticoagulant (interfere w. fibrin formation, tx for venous thromboembolic disorders-stasis)
protamine sulfate
heparin antagonist used in OD-fast, last 2hrs (1: 100) anticoag. effects of its own (CI?) -arginine, strongly basic, electropositive (hep is neg) adverse: hypotension, anaphylaxis (fish)
warfarin sodium (coumadin)
anticoagulant
block vitamin K (epoxide reductase inhibition) (essential cofactor in the post-translational modification of clotting factors II, VII, IX and X and anticoag proteins C and S)–>unable to bind Ca2+, can’t form thrombin, can’t form clot
need to clear clotting factors for anticoag act. (typ. on heparin 1st), long-acting
lepirudin (refludan)
hirudins (leech)
anticoagulant
65 aa polypep, highly sp. inhib. of thrombin
used when heparin-induced thrombocytopenia
adverse: hypersn, bleeding, pregnancy, no antidote
alteplase (activase)
fibrinolytic
serine protease, sim. to tPA
infusion IV or into iccl. vessel
activates fibrin-bound plasminogen–>plasmin
reverse w/ aminocaproic acid/tranexamic acid
aminocaproic acid (amicar)
fibrinolytic
reverses fibrinolytics
factor VIII (hemofil M, koate)
hemostatics
for hemophilia A (factor VIII deficiency)
factor IX (bebuline)
hemostatic
for hemophilia B (factor IX deficiency)
phytonadione (mephyton)
synthetic vitamin K
tPA
fibrinolytic (from endothelial wall)
activates plasminogen–>plasmin (binds lysine res. of fibrin, which it cleaves and solubizes–>blood flow restored
protamine sulfate
antagonizes bleeding from heparin, positively charged (arginine), instantaneous
anticoag act of its own
vitamin K:
Phytonadione (MephytonR )
(cofactor) glutamic residues–>gamma-carboxyglutamic acid (2, 7, 9, 10)–>bind Ca2+ (PL surfaces) in clotting cascade
fat-soluble naphthoquinones
nutrient factors to tx anemia
Iron and combinations
Folic acid derivatives and combinations
Cyanocobalamin (Vitamin B12) and combinations
Calcium carbonate (Tums)
antacid
can cause “milk alkali”: renal damage
not for long term use
-drug interactions (dig. glyc, tetras, phentoin)-dec. bioavail.
Aluminum hydroxide and magnesium hydroxide (Maalox)
antacid
Al: constipation
MgCl: laxative
may accumulate in pts. with poor renal function
Al: hypophos., Alzheimer’s
-drug interactions (dig. glyc, tetras, phentoin)-dec. bioavail.
Cimetidine (Tagamet)
H2-Receptor Antagonist (parietal cells)
-in resp. to histamine, gastrin, and ACh (vagal stim)
-acute tx and ppc of PUD, also ZES and GERD
@night esp. effective
side effects: P450 (warf, theophy, pheynytoin) anti androgen effects, caution w. preggos
Ranitidine (Zantac)
H2-Receptor Antagonist
Omeprazole (Prilosec)
Proton Pump Inhibitor
irrev. inact. H+/K+ ATPase
GERD, PUD, ZES (suppr. basal and meal-stim gastric acid sec)
prodrug, absorb. in intestine
-reduces absorb. Ca, Mg, inc. inf., rebound acid hypersec., hyperplasia of ECL and parietal cells (lack of acid fdbk inhib of gastrin rel)
-alters bioavail., metab, interferes with clopidogrel
Pantoprazole (Protonix)
Proton Pump Inhibitor
Sucralfate (Carafate)
Mucosal Protective Agent
Al salt of sulf. sucrose
polymerizes–>sticky material that binds to exp. proteins in ulcer crater–>protective barrier
-SE: constip, drug interaxns, syst. effects w. imp. renal func
Misoprostal (Cytotec)
Mucosal Protective Agent analogue of PGE1 -inc. mucus prod, may reduce acid sec. -prev. NSAID ind. ulcer SE: not for preggos (ind. contractions) diarrhea, ha, aggrav. IBD
Bismuth subsalicylate (Pepto-Bismol)
Mucosal Protective Agent:
Colloidial bismuth compound, also for IBD
-coating action, antipepsin, *antibac activity (H. pylori)
Reye’s syndrome assoc. (avoid in kiddos)
Esomeprazole (Nexium)
Proton Pump Inhibitor
Lansoprazole (Prevacid)
Proton Pump Inhibitor
antimicrobials for PUD
no single drug v. effective, combo tx, incl. PPI/H2antag
raise pH–>inc. efficacy
“triple therapy”: metronidazole,colloidal bismuth (pepto), 1 of: amoxicillin, tetracycline, (not in kids: gray teeth), clarithromycin
probs: $, low pt compliance
Helidac therapy: dosage kit (bismuth subsalicylate, metronidazole, and tetracycline)
more combos
Dietary fiber [Bran, Psyllium (Metamucil)]
methylcellulose
polycarbophil
Bulk-Forming Laxative
take with simethicone: anti-flatulance/bloating
SE: fecal impaction/int. obstruct. (need to take w. water!)
-drug interaxns (cardiac glycosides)
Docusate sodium (Colace)
Stool Surfactant Agent (“fecal softener”)
detergent effect on stool, hospitalized pts
SE: affects solubility of drugs (more quickly)- space meds
Magnesium hydroxide (Milk of Magnesia)
Osmotic Laxative/Cathartic
can also neutralize stomach acid, acute use (1-6 hrs)
others: Mg sulfate, Mg citrate
risk: prol. usage in renal insuff. pt–>hypermag.
Polyethylene glycol
Miralax, Colyte, Go lytely
Osmotic Laxative/Cathartic
inert, nonabsorbable sugar, osmotic diuretic as well
(Na sulfate, NaCl, NaHCO3, KCl)
more long term use than Mg hydroxide, prep for dx/sx proc.
no bad SEs!
Bisacodyl (Dulcolax)
Stimulant Laxative/Cathartic
-inhibits abs. H2O, stim. peristaltic mvmnts
acute/some chronic constipation (2-8 hrs)
w/ polyeth. glycol for colon prep
Anthraquinone derivatives [Aloe, Senna (SennaKot)/sennosides, Cascara]
Stimulant Laxative/Cathartic
- poor absorb., hydrolyzed in colon
adverse: chronic use: melanosis coli (brown pig.), colorectal ca?
Metoclopramide (Reglan)
Prokinetic Agent
antiemetic, blocks dopamine receptors, 5HT
-also CRTZ
-gastroparesis, GERD, antiemetic
Erythromycin
Prokinetic Agent
stim. motilin, promotes gastric emptying
tx gastroparesis
Methylnaltrexone
Prokinetic Agent treat opioid-induced constipation in patients with advanced illness (acts on intestinal u-opioid rec) given parenterally (subQ) don't cross BBB, do not effect analgesic effects of opioids
Alvimopan (Entereg)
Prokinetic Agent (same as methylnaltrexone) treat postoperative/paralytic ileum, short term (oral) don't cross BBB, do not effect analgesic effects of opioids
Methylcellulose
synthetic cellulose derivative
Polycarbophil
acts like bulk forming agent
insoluble, hydrophilic, polyacrylic resin
Lubiprostone (Amitiza)~
tx for chronic idiopathic constipation and IBS (females)
act. Cl channels, intest. BB–>inc. fluid sec (PG?)
not absorbed well from GI, few syst. effects
SE: nausea, diarrhea, flatulence, bloating, GI distress, ha
not safe during pregnancy?
Linaclotide (Linzess)~
tx for chronic idiopathic constipation and IBS
activates guanyl cycles and inc. cGMP
not used in kiddos
SEs: diarrhea, cramp, dehyd. risk
Dietary fiber [Bran, Psyllium (Metamucil), pectin, polycarbophil, cellulose]
Antidiarrheal Agent
bind excess water, bulk-forming
Bismuth subsalicylate (Pepto-Bismol) (colloidal bismuth compound)
antidiarrheal agent, acute, non-specific
absorb excess water, antimicrobial activity
slower acting than opioids, anti-inflamm.
“traveler’s diarrhea” (w. cipro)
*don’t use in kiddos (Reye’s)
adverse: syst. effects
Loperamide (Imodium)
antidiarrheal agent, OTC, acute non-specific
dec. intestinal motility, constr. circular musc, relax long. musc, antimicrobial (unless in intestinal mucosa)
* opioid analog* (not into CNS, DOES cross BBB, pumped out)
* BUT drugs that inhibit P-gp (verapimil) then take loperamide can cause central opioid effects
- don’t use if infectious orgs.
adverse: toxic megacolon
Dicyclomine (Bentyl)
Irritable Bowel Syndrome
antispasmodic, anticholinergic act.
Hyoscyamine
Irritable Bowel Syndrome
antispasmodic, anticholinergic act.
Lubiprostone (Amitiza)
Irritable Bowel Syndrome
Sulfasalazine (Azulfidine)
Aminosalicylate (IBD)
salicylate-antiinflammatory (aspirin usually irritates upper GI), cleaved in bowel (sulfapyridine and amino salicylic acid)
antimicrobial
UC, Crohn’s
CI in sulfonamides, aspirin allergies (use *corticosteroids instead: short-term use)
Mesalamine
Aminosalicylate (IBD) aminosalicylic acid(-5-ASA) UC, antiinflammatory irritating to upper GI, enema or oral timed-rel, pH-sens
Budesonide (Entocort)
Glucocorticoid (IBD)
enteric prep, acute attacks, mod-sec.
(also prednisone, etc, hydrocortisone enema)
Azathioprine
Antimetabolite (IBD)
thiopurine
chronic sev. or steroid-resist. IBD
Methotrexate
Antimetabolite (IBD)
dihydrofolate reductase inhibitor
chronic sev. or steroid-resist. IBD
Inflixamib (Remicade)
Anti-Tumor Necrosis Factor Therapy (IBD)
MoAb, given IV
inactivates TNF-a, suppresses immune function
mod-sev Crohn’s
SE: hypersn, AI disorders, inf from IV, immsuppr
Natalizumab (Tysabri)
Anti-Integrin Therapy (IBD)
mod-sev. Crohn’s (last resort)
give IV
adverse: dev. of multifocal leukoencephalopathy due to reactivation of hum. polyomavirus (JC virus)
Simethicone (mylicon)
Anti-Flatulence Agent
atropine
anticholinergic, anti-diarrheal, IBS
propantheline
anticholinergic, anti-diarrheal, IBS
dicyclomine
anticholinergic, anti-diarrheal, IBS
Bethanechol (URECHOLINE, others)
Cholinergic agonist, inc. tone/motility GI
tx postop ileus, inc. lower esophageal sphincter tone
Chenodiol (Chenix)
Ursodiol (Actigall)
Monooctanoin (Moctanin)
dissolution of gallstones
analogs of bile salts that alter cholesterol/bile sate metab. and help dissolve small gallstones
lactase (Lact Aid)
alpha-D-galactosidase (Beano)
dig. enzymes, helps pts with enz. deficiencies, pancreatic disease
morphine
Strong Analgesic (μ agonist) 10mg subQ -good for sev. pain IV doses lower sedation/mental clouding (OD) anxiety relief euphoria nausea (stim. CRTZ) resp. depression *death* (can tx resp. distress in pulm. edema) pupil constriction anti-cough histamine rel. (use benadryl, naloxone) lower seizure threshold endocrine disturbs. sm. musc effects (constipa., reten, bronchoconstr., inc. biliary press.) CV effects (hypotension, cut. vasodilation, inc. CSF press.) skel musc. regidity immunosuppression
codeine
Strong Analgesic (μ agonist) weaker than morphine antitussive (lower dose) *but can rel. histamine-->aggrav. asthma, etc.
fentanyl
Strong Analgesic (μ agonist) patch or IV short-term, fx stronger than morphine-100 ug is typ. dose
heroin
Strong Analgesic (μ agonist) acetylated morphine
hydrocodone (Vicodin, Lortab, Norco, Zohydro ER, others)
Strong Analgesic (μ agonist) exs are hydrocodone + acetaminophen(inhib. PG prod) problem: can OD, tox. doses of acetomin. 1st -Zohydro ER: just hydrocodone, no acetomin. -antitussive (lower dose)
hydromorphone (Dilaudid)
Strong Analgesic (μ agonist)
like morphine, more potent
IV, oral
meperidine (demerol)
Strong Analgesic (μ agonist) -almost discarded, still around
methadone (dolophine)
Strong Analgesic (μ agonist) -tx of heroin addxn
oxycodone (Percodan, Percocet, OxyContin, Oxecta)
Strong Analgesic (μ agonist)
more powerful than hydrocodone
combo prod. w/ acetomin. (percocet)
Oxycontin: just opioid, used to get high “Billy heroin”: appalachia
oxymorphone (opana)
Strong Analgesic (μ agonist) -pulled in 70s (drug users) marked as having lower abuse potential-false
pentazocine (talwin)
Partial Agonist and Mixed Agonist/Antagonist Analgesic
buprenorphine (Buprenex, Sabutrex, Suboxone)
Partial Agonist and Mixed Agonist/Antagonist Analgesic
-replacement for methadone for opioid addxn, more readily available
butorphanol (Stadol)
Partial Agonist and Mixed Agonist/Antagonist Analgesic
tramadol (Ultram)
Partial Agonist and Mixed Agonist/Antagonist Analgesic
-weak u agonist, less intense “buzz”, dec. abuse pot.
apentadol (Nucynta)
Partial Agonist and Mixed Agonist/Antagonist Analgesic
naloxone (Narcan, Evzio)
opioid antagonist
-opioid OD, IV, inj.
naltrexone (ReVia, Vivitrol)
opioid antagonist
-longer acting, oral: 12-24 hrs
methylnaltrexone (Relistor)
opioid antagonist
alvimopan (Entereg)
opioid antagonist
naloxegol (Movantik)
opioid antagonist
-opioid-ind. constipation
warfarin sodium (coumadin) uses: ppx of thromboembolism: ??? adverse ???
nonvalvular a fib, valve HD, prosthetic heart valves, acute venous thrombosis, PE, MI, prevention of reocclusion of coronary artery bypass grafts, thrombosis prev. (CVCs), w/ chemo
hemorrhage, HTN (CVD), skin lesions (! switch to hep), GI, hypersn, alopecia, fever, leukopenia
pregnancy abnormalities (crosses placenta!)
heparin uses ???
adverse ???
interactions ???
venous thromboemoblism, art. thromboembolism, extracorporeal circ., preggos (NOT coumadin), maintain patency fo indwelling catheters
adverse: thrombocytopenia, bleeding, hypersn, alopecia, burning in feet, local cap rupture
- suppr. aldosterone, interacts with insulin rec.
warfarin sodium (coumadin) interactions and reversal w/ ??
may prolong oral anticoag respons: ASA, salicylates, etc
may diminish: corticosteroids, exc. vit K
-reversal w. vit K and FFP (2,7,9,10)
fibrinolytics (tPA, pro-urokinase) uses? 3 things? adverse? reverse?
ven/art TE, shunts/catheters, occlusion of prost. heart valves
3: timing, lytic state, min. bleeding
sev. bleeding, IC hemorrhage, allergic rxs (strepto)
- rev. w/ fibrinolysis inhibs (aminocaproic acid)
iron interactions ???
adverse ???
OD ???
absorption inhibited by: eggs, milk, coffee/tea, antacid, tetracyclines, FQs
enhanced by vit C
adverse: GI irritation, N/V, C/D, dark stools
lethal dose: 200-250 mg/kg (tox: 30-60)
tx w/ deferoxamine mesylate (desferal) when >300 -chelates iron, forms stable complex–>red urine
deferoxamine mesylate (desferal)
iron OD when >300
chelates iron, forms stable complex–>red urine
THF (metab. Folic acid) values
normal vs abnormal
Normal serum levels: 5-15 ng/ml;
normal CSF levels: 16- 21 ng/ml;
normal erythrocyte levels: 175-316 ng/ml.
megaloblastic anemia
folic acid toxicity
- giving to pts w/ undiagnosed anemia; may obscure the diagnosis of pernicious anemia by alleviating the hematologic manifestations of the disease while allowing the neurologic complications to progress
- prevented w/ vit B12
folic acid adverse
rare hypersn, anorexia, naseau abdom. distension, etc, CNS effects (confusion, depression, alt. sleep, conc.)
folic acid tx for
megaloblastic anemia (may be tropical) NOT for pernicious or other megaloblastic when vit B12 is deficient (rule out before >0.1 mg dose FA) -preggos: 0.4 mg/day
hydroxocobalamin
cyanocobalamin
vit. B12, use for pernicious anemia
erythropoietin (Epoetin Alfa, Epogen, Procrit)
natural: sec. by peritubular cells in kidney cortex in responses to hypoxia
stimulates prolif and maturation of committed erythroid progenitors to inc. red cell production
tx of anemia (chronic renal disease)
anemia of AIDS pts (zidovudine (AZT)
cancer chemo pts, autologous blood donation
erythropoeitin adverse
flu-like, skin runs, arthralgia, (albumin), HTN in renal disease pts, clotting, seizures, hyperkalemia
filgrastim (G-CSF) (Neupogen)
hum.granulo.-colony-stim factor
-regulates prod. of neutrophils in BM, enhances function of mature neutros, accel. recovery of neutro cell counts
BM transplant, chemo/HIV- neutropenia
sargramostim (GM-CSF) (Leukine)
hum. granulocyte-macrophage colony-stim. factor
- supports growth and diff. of stem cells into granulos and macros, enhances chemotactic, anti fungal and anti parasitic act. of granulos and monos, accelerates myeloid recovery in lymphoma, leukemia, BM transplant pts., ca pts
oprelvekin (IL-11) (Neumega)
IL-11: thrombopoietic CF, stim. prolif of megakaryocytic progenitor cells, maturation, and inc. platelet production
-prev. thrombocytopenia in ca. pts
mineral oil
LC HCs from petroleum, poorly absorbed- stool softener
- kids and debil. adults
risks: pneumonitis (aspiration), dec. absorb. vit. ADEK, fat-sol. drugs, oil can leak!
castor oil
hydrl. in sm. int–>ricinoleic acid–>inhib. fluid absorb, stim. peristalsis
v. intense!
bowel prep., but no longer recommended
warfarin
-assoc. w/ valves, stenosis
long-term tx ops ischemic stroke-outweighs bleeding risk
maintain INR, inc. w. amiodarone(dec. dose!)
acetomin. may inc. INR
newer anticoags for nonvalv. a fib, as good as warfarin in stroke prev.
dabigatran etexilate
rivaroxaban
apixaban
-less IC bleeding, no INR monitoring, fewer interaxns, no antidotes, not for ESRD
dabigatran
thrombin inhibitor risk of GI bleeding efflux transported of P-gp dec. w/ rifampin inc. w/ amiodarone (dec. dose)
propranolol
heart block, hypotnsn, brady, bronchospasm, depression
metoprolol
heart block, hypotnsn, brady, bronchospasm, depression
diltiazem
heart block, hypotension, heart fail, brady, edema
- amiodarone: both inc. (dec. dose)
- pref. for asthma/COPD pts*
verapamil
heart block, hypotnsn, heart fail, brady, dizzy, ha, fatigue, edema, nausea, constip.
- inc. serum conc. with amiodarone-which inc. as well! (dec. dose)
- pref. for asthma/COPD pts*
digoxin
brady, Av block, arrhythmias, anorexia, N/V/D, abd pn, ha, confusion, abn vision
-pos. digoxin toxicity w/ amiodarone!
