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