T4: just drogas Flashcards
(120 cards)
1
Q
hydrocortisone (cortisol) (cortaid)
A
short-to medium-acting glucocorticoid
anti-inflam: 1.0
mincort: 2+ (potent!)
initial tx of adrenalcortical insufficiency (also anti-inflam, UC)
2
Q
prednisone (intensol)
A
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
3
Q
methylprednisolone (medrol)
A
short-to medium-acting glucocorticoid
4
Q
triamcinolone (nasocort)
A
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
5
Q
dexamethasone (baycadron)
A
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)
6
Q
metyrapone (metopirone)
A
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)
7
Q
ketoconazole (nizoral)
A
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
8
Q
fludrocortisone
A
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
9
Q
spironolactone (aldactone)
A
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)
10
Q
cosyntropin (cortrosyn)
A
glucocorticoid, mineralocorticoid, androgen, progesterone and estrogen agonist
synthetic derivative of ACTH
ddx prim. adrenal from secondary (pit) adrenocortical insuff.
11
Q
aspirin
A
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
12
Q
dipyridamole (persantine)
A
antiplatelet
blocks platelet adhesion to the vascular subendo. by inhibiting phosphodiesterase–>inc. cAMP (via inc. AC)
13
Q
clopidogrel (plavix)
A
antiplatelet
inhibits ADP binding to receptor (P2Y12 component)–>prevents activation of GPIIb/IIIa, irreversible
14
Q
tirofiban HCl (aggrastat)
A
antiplatelet
15
Q
heparin (hep-lock)
A
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
16
Q
enoxaparin sodium (lovenox)
A
anticoagulant (interfere w. fibrin formation, tx for venous thromboembolic disorders-stasis)
17
Q
protamine sulfate
A
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)
18
Q
warfarin sodium (coumadin)
A
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
19
Q
lepirudin (refludan)
hirudins (leech)
A
anticoagulant
65 aa polypep, highly sp. inhib. of thrombin
used when heparin-induced thrombocytopenia
adverse: hypersn, bleeding, pregnancy, no antidote
20
Q
alteplase (activase)
A
fibrinolytic
serine protease, sim. to tPA
infusion IV or into iccl. vessel
activates fibrin-bound plasminogen–>plasmin
reverse w/ aminocaproic acid/tranexamic acid
21
Q
aminocaproic acid (amicar)
A
fibrinolytic
reverses fibrinolytics
22
Q
factor VIII (hemofil M, koate)
A
hemostatics
for hemophilia A (factor VIII deficiency)
23
Q
factor IX (bebuline)
A
hemostatic
for hemophilia B (factor IX deficiency)
24
Q
phytonadione (mephyton)
A
synthetic vitamin K
25
tPA
fibrinolytic (from endothelial wall)
| activates plasminogen-->plasmin (binds lysine res. of fibrin, which it cleaves and solubizes-->blood flow restored
26
protamine sulfate
antagonizes bleeding from heparin, positively charged (arginine), instantaneous
anticoag act of its own
27
vitamin K:
| Phytonadione (MephytonR )
(cofactor) glutamic residues-->gamma-carboxyglutamic acid (2, 7, 9, 10)-->bind Ca2+ (PL surfaces) in clotting cascade
fat-soluble naphthoquinones
28
nutrient factors to tx anemia
Iron and combinations
Folic acid derivatives and combinations
Cyanocobalamin (Vitamin B12) and combinations
29
Calcium carbonate (Tums)
antacid
can cause "milk alkali": renal damage
not for long term use
-drug interactions (dig. glyc, tetras, phentoin)-dec. bioavail.
30
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.
31
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
32
Ranitidine (Zantac)
H2-Receptor Antagonist
33
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
34
Pantoprazole (Protonix)
Proton Pump Inhibitor
35
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
36
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
```
37
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)
38
Esomeprazole (Nexium)
Proton Pump Inhibitor
39
Lansoprazole (Prevacid)
Proton Pump Inhibitor
40
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
41
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)
42
Docusate sodium (Colace)
Stool Surfactant Agent ("fecal softener")
detergent effect on stool, hospitalized pts
SE: affects solubility of drugs (more quickly)- space meds
43
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.
44
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!
45
Bisacodyl (Dulcolax)
Stimulant Laxative/Cathartic
-inhibits abs. H2O, stim. peristaltic mvmnts
acute/some chronic constipation (*2-8 hrs*)
w/ polyeth. glycol for colon prep
46
Anthraquinone derivatives [Aloe, Senna (SennaKot)/sennosides, Cascara]
Stimulant Laxative/Cathartic
- poor absorb., hydrolyzed in colon
adverse: chronic use: melanosis coli (brown pig.), colorectal ca?
47
Metoclopramide (Reglan)
Prokinetic Agent
antiemetic, blocks dopamine receptors, 5HT
-also CRTZ
-gastroparesis, GERD, antiemetic
48
Erythromycin
Prokinetic Agent
stim. motilin, promotes gastric emptying
tx gastroparesis
49
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
```
50
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
```
51
Methylcellulose
synthetic cellulose derivative
52
Polycarbophil
acts like bulk forming agent
| insoluble, hydrophilic, polyacrylic resin
53
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?
54
Linaclotide (Linzess)~
tx for chronic idiopathic constipation and IBS
activates guanyl cycles and inc. cGMP
not used in kiddos
SEs: diarrhea, cramp, dehyd. risk
55
Dietary fiber [Bran, Psyllium (Metamucil), pectin, polycarbophil, cellulose]
Antidiarrheal Agent
| bind excess water, bulk-forming
56
```
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
57
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
58
Dicyclomine (Bentyl)
Irritable Bowel Syndrome
| antispasmodic, anticholinergic act.
59
Hyoscyamine
Irritable Bowel Syndrome
| antispasmodic, anticholinergic act.
60
Lubiprostone (Amitiza)
Irritable Bowel Syndrome
61
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)
62
Mesalamine
```
Aminosalicylate (IBD)
aminosalicylic acid(-5-ASA)
UC, antiinflammatory
irritating to upper GI, enema or oral
timed-rel, pH-sens
```
63
Budesonide (Entocort)
Glucocorticoid (IBD)
enteric prep, acute attacks, mod-sec.
(also prednisone, etc, hydrocortisone enema)
64
Azathioprine
Antimetabolite (IBD)
thiopurine
chronic sev. or steroid-resist. IBD
65
Methotrexate
Antimetabolite (IBD)
dihydrofolate reductase inhibitor
chronic sev. or steroid-resist. IBD
66
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
67
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)
68
Simethicone (mylicon)
Anti-Flatulence Agent
69
atropine
anticholinergic, anti-diarrheal, IBS
70
propantheline
anticholinergic, anti-diarrheal, IBS
71
dicyclomine
anticholinergic, anti-diarrheal, IBS
72
Bethanechol (URECHOLINE, others)
Cholinergic agonist, inc. tone/motility GI
| tx postop ileus, inc. lower esophageal sphincter tone
73
Chenodiol (Chenix)
Ursodiol (Actigall)
Monooctanoin (Moctanin)
dissolution of gallstones
| analogs of bile salts that alter cholesterol/bile sate metab. and help dissolve small gallstones
74
lactase (Lact Aid)
| alpha-D-galactosidase (Beano)
dig. enzymes, helps pts with enz. deficiencies, pancreatic disease
75
*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
```
76
codeine
```
Strong Analgesic (μ agonist)
weaker than morphine
antitussive (lower dose) *but can rel. histamine-->aggrav. asthma, etc.
```
77
fentanyl
```
Strong Analgesic (μ agonist)
patch or IV
short-term, fx
stronger than morphine-100 ug is typ. dose
```
78
heroin
```
Strong Analgesic (μ agonist)
acetylated morphine
```
79
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)
```
80
hydromorphone (Dilaudid)
Strong Analgesic (μ agonist)
like morphine, more potent
IV, oral
81
meperidine (demerol)
```
Strong Analgesic (μ agonist)
-almost discarded, still around
```
82
methadone (dolophine)
```
Strong Analgesic (μ agonist)
-tx of heroin addxn
```
83
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
84
oxymorphone (opana)
```
Strong Analgesic (μ agonist)
-pulled in 70s (drug users)
marked as having lower abuse potential-false
```
85
pentazocine (talwin)
Partial Agonist and Mixed Agonist/Antagonist Analgesic
86
buprenorphine (Buprenex, Sabutrex, Suboxone)
Partial Agonist and Mixed Agonist/Antagonist Analgesic
| -replacement for methadone for opioid addxn, more readily available
87
butorphanol (Stadol)
Partial Agonist and Mixed Agonist/Antagonist Analgesic
88
tramadol (Ultram)
Partial Agonist and Mixed Agonist/Antagonist Analgesic
| -weak u agonist, less intense "buzz", dec. abuse pot.
89
apentadol (Nucynta)
Partial Agonist and Mixed Agonist/Antagonist Analgesic
90
naloxone (Narcan, Evzio)
opioid antagonist
| -opioid OD, IV, inj.
91
naltrexone (ReVia, Vivitrol)
opioid antagonist
| -longer acting, oral: 12-24 hrs
92
methylnaltrexone (Relistor)
opioid antagonist
93
alvimopan (Entereg)
opioid antagonist
94
naloxegol (Movantik)
opioid antagonist
| -opioid-ind. constipation
95
```
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!)
96
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.
97
```
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)
98
```
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)
99
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
100
deferoxamine mesylate (desferal)
iron OD when >300
| chelates iron, forms stable complex-->red urine
101
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
102
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
103
folic acid adverse
rare hypersn, anorexia, naseau abdom. distension, etc, CNS effects (confusion, depression, alt. sleep, conc.)
104
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
```
105
hydroxocobalamin
| cyanocobalamin
vit. B12, use for pernicious anemia
106
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
107
erythropoeitin adverse
flu-like, skin runs, arthralgia, (albumin), HTN in renal disease pts, clotting, seizures, hyperkalemia
108
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
109
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
110
oprelvekin (IL-11) (Neumega)
IL-11: thrombopoietic CF, stim. prolif of megakaryocytic progenitor cells, maturation, and inc. platelet production
-prev. thrombocytopenia in ca. pts
111
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!
112
castor oil
hydrl. in sm. int-->ricinoleic acid-->inhib. fluid absorb, stim. peristalsis
v. intense!
bowel prep., but *no longer recommended*
113
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
114
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
115
dabigatran
```
thrombin inhibitor
risk of GI bleeding
efflux transported of P-gp
dec. w/ rifampin
inc. w/ amiodarone (dec. dose)
```
116
propranolol
heart block, hypotnsn, brady, bronchospasm, depression
117
metoprolol
heart block, hypotnsn, brady, bronchospasm, depression
118
diltiazem
heart block, hypotension, heart fail, brady, edema
- amiodarone: both inc. (dec. dose)
* pref. for asthma/COPD pts*
119
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*
120
digoxin
brady, Av block, arrhythmias, anorexia, N/V/D, abd pn, ha, confusion, abn vision
-pos. digoxin toxicity w/ amiodarone!
