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Flashcards in T4: just drogas Deck (120):
1

hydrocortisone (cortisol) (cortaid)

short-to medium-acting glucocorticoid
anti-inflam: 1.0
mincort: 2+ (potent!)
initial tx of adrenalcortical insufficiency (also anti-inflam, UC)

2

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

3

methylprednisolone (medrol)

short-to medium-acting glucocorticoid

4

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

5

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)

6

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)

7

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

8

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

9

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)

10

cosyntropin (cortrosyn)

glucocorticoid, mineralocorticoid, androgen, progesterone and estrogen agonist
*synthetic derivative of ACTH*
ddx prim. adrenal from secondary (pit) adrenocortical insuff.

11

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

12

dipyridamole (persantine)

antiplatelet
blocks platelet adhesion to the vascular subendo. by inhibiting phosphodiesterase-->inc. cAMP (via inc. AC)

13

clopidogrel (plavix)

antiplatelet
inhibits ADP binding to receptor (P2Y12 component)-->prevents activation of GPIIb/IIIa, irreversible

14

tirofiban HCl (aggrastat)

antiplatelet

15

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

16

enoxaparin sodium (lovenox)

anticoagulant (interfere w. fibrin formation, tx for venous thromboembolic disorders-stasis)

17

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)

18

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

19

lepirudin (refludan)
hirudins (leech)

anticoagulant
65 aa polypep, highly sp. inhib. of thrombin
used when heparin-induced thrombocytopenia
adverse: hypersn, bleeding, pregnancy, *no antidote*

20

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

21

aminocaproic acid (amicar)

fibrinolytic
*reverses fibrinolytics*

22

factor VIII (hemofil M, koate)

hemostatics
for hemophilia A (factor VIII deficiency)

23

factor IX (bebuline)

hemostatic
for hemophilia B (factor IX deficiency)

24

phytonadione (mephyton)

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!