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PHARM block 3 without coagulation drugs Flashcards

1
Q

GI drugs uses

A

most common forms of: nausea/vomiting, diarrhea, constipation, gerd

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2
Q

drugs used to induce therapeutic emesis

A

ipecacuana; hypertonic saline; apomorphine

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3
Q

ipecacuana

A

ipecac syrup; obsolete

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4
Q

use of drugs to induce emesis

A

to empty stomach after poison ingestion; alternative to/combo with gastric lavage

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5
Q

contraindications of drug-induced emesis

A

ingestion of corrosives (cleaning fluids); ingest aliphatics (petroleum -> lipid pneumonia); somnolence, unconciousness

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6
Q

adverse effects of drug-induced emesis

A

aspiration, vagal syncope, hypochloremia, hypovolemia, absorption of emetic drug (NaCl, ipecac)

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7
Q

antiemetic drugs

A

antihistamines (inhibit dopamine); phenothiazines; dopamine antagonists; 5-HT-antagonists; corticosteroids; cannabinoids (effective, illegal in some states); neurokinin-1-receptor antagonist; adjunct medications

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8
Q

antiemetic antihistamines

A

diphenhydramine, hydroxizine

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9
Q

diphenhydramine, hydroxizine adverse effects

A

sedation

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10
Q

diphenhydramine, hydroxizine indications

A

pregnancy, motion sickness

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11
Q

phenothiazines

A

perchlorphenazine, proemthazine

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12
Q

perchlorphenazine, proemthazine adverse effects

A

epm disturbances, dyskinesias, sedation

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13
Q

perchlorphenazine, proemthazine indications

A

metabolic/endocrine, cns

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14
Q

dopamine antagonists

A

metoclopramide, (domperidon) - risk of arrhythmia -> used in compounds

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15
Q

metoclopramide, (domperidon) adverse effects

A

s.a., but less pronounced

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16
Q

metoclopramide indications

A

widely used to prevent/treat moderate nausea/emesis

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17
Q

5-HT-antagonists

A

ondansetron, granisetron, tropisetron, dolasetron

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18
Q

ondansetron, granisetron, tropisetron, dolasetron adverse effects

A

CONSTIPATION (contraindicated w/opiates), headache

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19
Q

ondansetron, granisetron, tropisetron, dolasetron indications

A

cytostatic-induced EARLY vomiting

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20
Q

antiemetic corticosteroids

A

dexamethasone

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21
Q

dexamethasone adverse effects

A

none

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22
Q

dexamethasone indications

A

intracranial pressure, cytostatic-induced LATE vomiting; given together w/5-HT-antagonists

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23
Q

cannabinoids

A

marijuana, THC (dronabinol), nabilone

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24
Q

marijuana, THC, nabilone adverse effects

A

drowsiness, confusion, amotivational syndrome (prolonged use)

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25
Q

cannabinoids indications

A

wasting related to AIDS, cancer

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26
Q

neurokinin-1-receptor antagonist

A

aprepitant

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27
Q

aprepitant adverse effects

A

fatigue, dizziness, diarrhea

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28
Q

aprepitant indications

A

cytostatic-induced; combo tx

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29
Q

adjunct antiemetic drugs

A

benzodiazepines, atropine, scopolamine, erythromycin (prokinetic)

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30
Q

benzodiazepines antiemetic indications

A

anticipatory vomiting

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31
Q

erythromycin moa

A

macrolide antibiotic, motilin agonist

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32
Q

erythromycin uses

A

diabetic gastroparesis, postoperative GI atony -> prokinetic

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33
Q

metoclopramide moa

A

central D2 antagonist (dopamine); peripheral M1 agonist

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34
Q

metoclopramide uses

A

antiemetic, gerd, diabetic gastroparesis -> prokinetic

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35
Q

metoclopramide pk

A

oral, im, iv, rectal

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36
Q

metoclopramide pd

A

antiemetic; prokinetic (GI)

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37
Q

metoclopramide adverse effects

A

extrapyramidal symptoms, esp in children; restlessness; drowsiness; with prolonged, high dose -> galactorrhea, gynaecomastia, parkinsonoid

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38
Q

most important therapy for diarrhea

A

drinking balanced fluid to maintain kidney fxn

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39
Q

diarrhea-causing drugs

A

adrenergic blockers ((reserpine)); antimicrobials (tetracyclines, sulfonamides, broad spectrum) - affect flora; bile acids, fatty acids, carcinoid tumor secretions; digestive enzyme blockers (acarbose, orlistat); dietary agents (OLESTRA, some sweeteners); cardiac glycosides - sign of overdose; cholinergic agonists; laxatives; prostaglandins

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40
Q

drugs for diarrhea treatment

A

peripheral opioid-receptor agonists (loperamide, diphenoxylate (combine w/atropine)); tinctura opii; somatostatin; alpha2 agonists (clonidine); adjunct meds - spasmolytic drugs; bile-acid induced diarrhea (colestyramine); clostridium-difficile associated enterocolitis (vancomycin; metronidazole)

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41
Q

loperamide moa

A

mainly peripheral; opioid receptor agonist; OTC drug

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42
Q

loperamide pk

A

oral

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43
Q

loperamide pd

A

inhibits intestinal fluid secretion; inc intestinal fluid absorption; inc tonic (non-propulsive) intestinal smooth muscle tone

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44
Q

loperamide adverse effects

A

constipation; kids, high dose - opioid-like adverse effects

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45
Q

loperamide contraindications

A

ileus, subileus, fever, antibiotics-associated diarrhea, megacolon, pregnancy, lactation

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46
Q

ineffective drugs used for diarrhea

A

activated charcoal tablets; pektin; kaolin -> placebo, irritable bowel syndrome, ‘stool freaks’; drugs w/serious adverse effects -> antibiotics/septics in OTC preps, tannin

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47
Q

constipation-causing drugs

A

ALL opioids - strong; anticholinergics (antidepressants, phenothiazines, antiparkinson drugs); ganglionic blockers; calcium channel antagonists; k-wasting diuretics; ‘irritant’-type laxatives (chronic abuse)

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48
Q

types of laxatives

A

bulk-forming agents (fiber) - bran, psyllium, methylcellulose -> distend bowel -> inc peristalsis; hyperosmolar agents - sorbitol, lactulose, polyethylenglycol (for surgery prep) -> retain water in gut; stool softening/lubricating agents - docusate sodium, glycerin, mineral oil (can cause lipid pneumonia); stimulants/irritants - bisacodyl, castor oil, phenolphtalein, anthrachinones; enema - containing any of others (helps pregnant women push)

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49
Q

peptic ulcer drugs

A

proton pump inhibitors; H2-antagonists; antimicrobial agents; antacids; others - (anticholinergics), prostaglandins, mucosal protective agents (rare)

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50
Q

H2 receptor antagonists

A

cimetidine, ranitidine, famotidine, nizatidine

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51
Q

cimetidine characteristics

A

prototype drug; many pk interactions (cyt p450 inhibition - warfarin, phenytoin, theophylline); antiandrogenic effects; GYNAECOMASTIA

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52
Q

ranitidine characteristics

A

more POTENT; longer duration; no antiandrogenic effects; no gynaecomastia

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53
Q

famotidine + nizatidine characteristics

A

further improved potency, duration; nizatidine - 100% bioavail

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54
Q

cimetidine, ranitidine, famotidine, nizatidine pk

A

oral, IV

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55
Q

cimetidine, ranitidine, famotidine, nizatidine adverse effects

A

mild; headache, diarrhea, muscular pain, confusion

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56
Q

proton pump inhibitors (PPI)

A

omeprazole, lansoprazole, pantoprazole

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57
Q

omeprazole, lansoprazole, pantoprazole pk

A

oral, iv, prodrugs -> activated after secretion from gastric mucosal cells into acid canaliculi

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58
Q

omeprazole, lansoprazole, pantoprazole pd

A

IRREVERSIBLE! binding of proton pump; dose-dependent, complete inhibition of basal and stimulated acid secretion; long duration (up to 3d)

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59
Q

omeprazole, lansoprazole, pantoprazole adverse effects

A

mostly secondary to anacidity (gastric bacterial flora, aspiration pneumonia w/assisted resp)

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60
Q

antacids characteristics

A

weak base + HCL = salt + water; immediate relief from hyperacidity

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61
Q

antacids categories

A

absorbable/poorly absorbable - best in combos; laxative/constipative

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62
Q

antacids pd

A

SHORT duration (~2h); need large qty’s - not suitable for ulcers; repeat at short intervals for lasting effect

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63
Q

antacids adverse effects

A

alkalosis (absorble antacids); interference w/absorption of other drugs (chelation, adsorption)

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64
Q

typical poorly-absorbable antacid combinations

A

aluminumhydroxide (promotes constipation); magnesiumhydroxide (promotes laxation)

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65
Q

simethicone

A

de-foaming agent; takes off surface tension -> defoam -> dec bloating

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66
Q

misoprostol moa

A

stable analogue of prostaglandin E1

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67
Q

misoprostol pd

A

cytoprotective; only clinically effective in doses that also inhibit acid secretion

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68
Q

misoprostol uses

A

prevention of ulcers induced by NSAIDs - protects mostly the stomach

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69
Q

misoprostol adverse effects

A

not well tolerated; all ae’s associated w/PGs seen - nausea, diarrhea, abdominal cramps, uterine contractions

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70
Q

misoprostol contraindications

A

PREGNANCY

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71
Q

sucralfate characteristics

A

coating agent; complex of aluminumhydroxide, sulfated sucrose

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72
Q

sucralfate pk

A

topical action; little systemic absorption

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73
Q

sucralfate pd

A

coats ulcer ground in acidic environment; stimulates PG synth; ineffective when combo w/antacids

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74
Q

sucralfate uses

A

longterm maintenance therapy to prevent ulcer recurrence

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75
Q

therapeutic issues: peptic ulcer disease

A

all tx include PPI or H2-antagonist and 2 or 3 antimicrobial agents; antimicrobials prevent recurrence (no healing); HP eradication mostly successful; antimicrobials ~10d, PPI ~6wks; symptom relief best w/PPI; healing rate same for PPI/H2-ant; no diet recs; smoking stops healing, promotes recurrence

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76
Q

aspirin clinical effects

A

anti-inflammatory (directly in tissue); analgesic (2ndary to anti-inflammatory); antipyretic (only if temp is inc); anti-platelet (slightly inhibit thromboxane)

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77
Q

anti-inflammatory effects of aspirin

A

non-selective COX inhibition - irreversible acetylation (unique), salicylate-induced reversible inhibition (like NSAIDs); interference w/kallikrein/bradykinin system (minor) - interfere w/granulocyte adherence, PMN leukos, macrophages

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78
Q

analgesic effects of aspirin

A

mild/moderate pain; site of pain - peripheral; 2ndary to anti-inflammation; minor 2ndary cns effect at subcortical sites; co-medication in moderate/severe pain

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79
Q

antipyretic effects of aspirin

A

dec high temp, normal temp unaffected; regulation at cns level (cox inhibition, IL-1 formation); vasodilation; profuse sweating

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80
Q

anti-platelet effects of aspirin

A

irreversible acetylation of thromboxane synthetase - low dose effect, specific for aspirin, pre-systemic effect on thrombosis in portal vein, 8-10d effect, effects add up, stop after surgery; inhibit thromboxane synthetase by salicylate - high dose effect, mild

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81
Q

aspirin combined effect on coagulation

A

irreversibly inhibits TXA2 for life of platelet -> inc BT; inhibits COX in endothelial cells, but can synth new COX

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82
Q

aspirin adverse effects

A

analgesic, short-term doses - upset GI, slight inc BT; prolonged tx - erosive gastritis, gastric/duodenal ulcers/complications -> MUST have protection; high dose (unusual) - cns syndrome - salicylism (vomiting, tinnitus, vertigo); low dose - inc urate levels -> gout -> inc dose -> dec gout; impaired renal fxn when combo w/2d nsaid; aspirin-asthma; reye syndrome -> NEVER give to kids w/fever/viral infection

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83
Q

aspirin intoxication

A

respiratory alkalosis, then metabolic acidosis, mixed imbalances of acid-base homeostasis

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84
Q

aspirin adverse effects on kidneys

A

dec renal blood flow; acute interstitial nephritis; analgesic nephropathy

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85
Q

aspirin adverse effects on kidney: dec renal blood flow

A

pt’s w/compromised renal perfusion -> kidney synth PGE2, PGI2 (vasodilators) to balance vasoconstriction; aspirin dec PGs -> dec PGE2 -> inc na/h2o & dec PGI2 -> hyperkalemia, acute renal failure

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86
Q

aspirin adverse effects on kidneys: acute interstitial nephritis

A

type I hypersensitivity -> acute renal failure; almost any drug can cause interstitial nephritis, most common -> antibiotics/nsaids

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87
Q

aspirin adverse effects on kidneys: analgesic nephropathy

A

chronic interstitial nephritis from prolonged analgesics use, esp combos of diff agents; renal papillary necrosis after yrs -> chronic interstitial nephritis -> progressive chronic renal failure

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88
Q

aspirin clinical uses: antiplatelet dose level

A

prevent coronary events, transient ischaemic attacks; reduce colon ca incidence

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89
Q

aspirin clinical uses: analgesic dose level

A

tx mild/moderate pain; fever (not kids); moderate pain when combo w/codein; adjunct tx of severe pain w/strong opioids

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90
Q

ibuprofen characteristics

A

commonly used minor analgesic, otc

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91
Q

ibuprofen pk

A

oral, 99% protein bound

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92
Q

ibuprofen pd

A

nsaid

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93
Q

ibuprofen adverse effects

A

GI (less than aspirin); RARE: rash, pruritius, aseptic meningitis, tinnitus, dizziness, headache, fluid retention, acute renal failure, interstitial nephritis, nephrotic syndrome, hepatitis

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94
Q

diclofenac moa

A

potent COX inhibitor, some selectivity for COX-2

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95
Q

diclofenac pk

A

t1/2~1h; accums in synovial fluid (t1/2~6h); enteric-coated, sustained release available - important for chronic joint pain

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96
Q

diclofenac uses

A

analgesic (in combo w/codeine); antirheumatic

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97
Q

diclofenac adverse effects

A

like other nsaids

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98
Q

indomethacin characteristics

A

the more potent -> more efficacious -> more side effects

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99
Q

indomethacin moa

A

more potent, unselective COX inhibitor; additional anti-inflammatory effects

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100
Q

indomethacin pk

101
Q

indomethacin adverse effects

A

severe nsaid-like; abdominal pain, diarrhea, GI bleeding, pancreatitis, hyperkalemia, renal failure, thrombocytopenia, APLASTIC anemia

102
Q

indomethacin uses

A

ONLY in rheumatic, arthritic complaints

103
Q

piroxicam moa

A

potent, unselective COX inhibitor; additional anti-inflammatory effects

104
Q

piroxicam pk

A

t1/2~55h -> once daily dosing, accumulation

105
Q

piroxicam adverse effects

A

severe nsaid-like; GI (~20%+); pancreatitis; hyperkalemia; renal failure; thrombocytopenia; aplastic anemia

106
Q

piroxicam uses

A

ONLY for rheumatologists or not at all

107
Q

acetaminophen characteristics

A

NOT an NSAID; frequently used as minor analgesic

108
Q

acetaminophen pk

A

oral; t1/2~2h

109
Q

acetaminophen pd

A

analgesic (like aspirin), antipyretic (like aspirin); NOT anti-inflammatory, NOT anti-platelet

110
Q

acetaminophen adverse effects

A

mild inc in hepatic enzymes; RARE: hepatic failure, renal failure, dizziness, excitement, disorientation

111
Q

acetaminophen intoxification

A

fatal hepatic failure, antidote - acetylcysteine

112
Q

risk for NSAID-induced GI bleeding

A

low: acetaminophen, ibuprofen; intermediate: aspirin, diclofenac; high: piroxicam, indomethacin, ketoprofen

113
Q

COX isoenzymes

A

COX-1 - constitutive - for homeostasis; COX-2 - induced by growth factors, tumor promoters, cytokines - major source of prostanoids in inflammation, ca

114
Q

glucocorticoid receptor subtypes

A

type 1 - mineralocorticoid (misnomer) - kidney, colon, salivary glands, sweat glands; type 2 - glucocorticoid - broad tissue distribution

115
Q

glucocorticoid response elements

A

effectuate all changes in gene expression - contained in ~10% of all human genes -> huge impact

116
Q

cortisol effects, ideally

A

keep humoral/local inflammatory response reasonable; protect glucose-dependent tissue from starvation; switch to catabolism -> preserve electrolytes/water; improve mood

117
Q

cortisol metabolic effects: protect glucose-dependent tissues from starvation

A

stimulate gluconeogenesis from AA, glycerol; stimulate liver glycogen; dec gluc use in periphery; stimulate insulin secretion - bring gluc to cells; stimulate lipolysis; NET EFFECT - inc plasma gluc

118
Q

cortisol metabolic effects: increase nutrient availability for the brain

A

stim gluconeogenesis from AA, glycerol; stimulate liver glycogen storage; dec gluc use peripherally; stim insulin secretion; stim lipolysis -> NET EFFECT - inc plasma gluc/TGs -> HYPERGLYCEMIC; protein CATABOLISM, mainly muscle -> inc plasma AA

119
Q

cortisol metabolic effects: electrolyte, water balance

A

aldosterone-like effects; NET EFFECTS - positive na-balance, ecv expansion, hypokalemia, alkalosis; dec body ca++ stores (dec intestinal absorption, inc renal excretion)

120
Q

adrenal crisis metabolic imbalances

A

caused by abrupt discontinuation of exogenous GC; hyponatremia, hypovolemia, hyperkalemia, acidosis (low bicarb), hypoglycemia, inc BUN

121
Q

adrenal crisis symptoms

A

dehydration, hypotension, abdominal complaints, “pseudo-peritonitis”, hypothermia -> dehydration-related fever, delirium, coma; tx w/cortisol, cortisone

122
Q

cortisol effects: immunosuppressive/anti-inflammatory

A

down-reg stress from injury; interfere w/peripheral leukocyte fxn; move leukocytes to lymphatics; suppress inflammation mediators; suppress mast cell degranulation; inhibit lipoxygenase; inhibit COX-2; inhibit complement effects (not activation); antibody production inhibited (high doses only)

123
Q

cortisol effects: cns

A

variable effects on mood, behavior, excitability, insomnia, euphoria -> depression; may inc icp (large doses); improve mood, appetite in terminally ill pt’s

124
Q

cortisol effects: fetal lung maturation

A

critically important b4 gestational wk 34; preterm: inject 2 doses -> mature lungs, stim pulmonary surfactant production

125
Q

corticosteroids used as aerosol inhalants

A

for asthma - beclomethasone, budesonide; high first pass metabolism

126
Q

glucocorticoids adverse effects

A

low dose inhalant/topical - local ae’s, none systemic; high dose inhalant/topical - local ae’s, minor systemic; prolonged systemic use - severe -> only use if not alternatives; single ultrahigh dose bolus - inc risk of pre-existing infection, aggravation of DM, inc risk of stress ulcers

127
Q

glucocorticoids adverse effects: prolonged systemic use

A

similar to cushing’s syndrome - affects skin, bone, sk muscle, eyes, GI, cv system, blood, electrolytes, endocrine sys, immunological status, mental status

128
Q

interactions during prolonged systemic tx: cardiac glycosides

A

inc toxicity due to hypokalemia

129
Q

interactions during prolonged systemic tx: loop diuretics, thiazides, irritant laxatives

A

inc potassium loss

130
Q

interactions during prolonged systemic tx: NSAIDs

A

inc peptic ulcers, GI bleeding

131
Q

interactions during prolonged systemic tx: antidiabetics

A

dec antidiabetic effects

132
Q

interactions during prolonged systemic tx: ACE-inhibitors

A

inc risk of blood dyscrasias (unspecified blood disorder)

133
Q

interactions during prolonged systemic tx: chloroquine, mefloquine

A

inc risk of myopathy, cardiomyopathy

134
Q

interactions during prolonged systemic tx: atropine, anticholinergics

A

inc rise in intraocular pressure

135
Q

how to minimize GC toxicity

A

use topical when possible; adapt systemic use to diurnal rhythm (8am); vary daily dose; taper dose asap; use other immunomodulator as sub or in combo

136
Q

glucocorticoids indications

A

allergic rxn (asthma, angioneurotic edema, drug rxns, envenomations); collagen disorders (rheumatoid arthritis, polymyosistis); ophthalmologic (allergic uveitis, conjunctivitis); GI (bowel inflammatory dz); hematologic (acute allergic purpura, leukemia); infections (gram- septic shock); joint, bone (arthritis, bursitis, tendosynovitis); neurologic (cerebral edema, MS); pulmonary (COPD, infant RDS); renal (nephrotic syndrome); dermatologic (atopic dermatitis); thyroid (subacute thyroiditis); surgery/EM (acute severe trauma)

137
Q

drugs used to minimize glucocorticoid use

A

leukotriene-receptor antagonist (asthma, allergy); lipoxygenase inhibitors; anti-IgE-antibodies; cyclosporin (bowel inflammatory dz); tacrolimus (rheumatism, dermatology); methotrexate; azathioprine; etanercept; remicade (BID); thalidomide; activated protein C (septic shock)

138
Q

gouty attack clinical features

A

sudden onset; nocturnal; precipitating factor; monoarticular; small, peripheral joint; fever

139
Q

gout differential diagnosis

A

critical: bacterial infection of joint; other: pseudogout, aseptic monoarthritis, trauma; plasma urate level unreliable predictor of gouty attack

140
Q

gout risk factors

A

OBESITY; high purine (PROTEIN) diet; metabolic factors; excessive alcohol; drug therapy; kidney failure;

141
Q

pathophysiology of gouty attacks

A

plasma urate - ONE determinant of gouty attack, but inc levels may persist for years w/o attack; slight rise could cause attack

142
Q

deposition of monosodium urate crystals depends on

A

‘solubilizers’ in plasma; plasma pH (alcoholics -> acidotic); tissue perfusion/temp

143
Q

summary of gout treatment

A

aspirin competes w/urate for secretion -> inc urate in predisposed ppl! inc fluid intake -> inc excretion; allopurinol - don’t give if prone to attack -> slight inc in purines at start

144
Q

colchicine characteristics

A

plant alkaloid w/cytostatic properties

145
Q

colchicine pk

146
Q

colchicine pd

A

binds to tubulin (inhibit microtubule assy) -> depolymerization -> cytostatic effect on leukocytes, inhibit inflammation -> pain relief; NO EFFECT on msu crystals or plasma urate levels

147
Q

colchicine uses

A

tx acute gouty attack

148
Q

colchicine adverse effects

A

related to cytostatic properties; acute: GI complaints, pain, DIARRHEA (frequent); chronic: no longterm tx -> alopecia, agranulocytosis, aplastic anemia, myopathy, neuropathy

149
Q

colchicine contraindications

150
Q

uricostatics: allopurinol pk

A

oral; converted to oxypurinol (alloxanthine) by xanthine oxidase

151
Q

allopurinol pd

A

competitively inhibit xanthine oxidase -> large dec urate, large inc hypo/xanthine -> more soluble than urate -> dec risk of urate precipitation, inc hypo/xanthine renal excretion

152
Q

allopurinol adverse effects

A

GI upset; may inc urate at onset; rare: erythema multiforme, stevens-johnson syndrome

153
Q

allopurinol uses

A

manage chronic gout; NOT in first 1-2 wks after acute episode

154
Q

uricosuric agents

A

probenecid, sulfinpyrazon, (benzbromarone)

155
Q

probenecid, sulfinpyrazon, (benzbromarone) pd

A

block tubular reabsorption of urate at therapeutic conc

156
Q

low doses of uricosuric agents…

A

BLOCK tubular secretion of urate! don’t use after first few weeks of attack

157
Q

probenecid, sulfinpyrazon, (benzbromarone) interactions

A

probenecid inhibits tubular secretion of penicillin, naproxen, ketoprofen, indomethacin (nsaids) -> can’t tolerate co-tx

158
Q

probenecid, sulfinpyrazon, (benzbromarone) adverse effects

A

mild; sulfinpyrazone - GI

159
Q

treatment of chronic hyperuricemia

A

dec of the body urate pool takes months/yrs; maybe lifelong therapy; ensure high fluid turnover; start in symptom-free interval; dec purine-rich food; tx w/uricosuric/static drug; can use nsaid/low dose colchicine at onset of therapy - prevent recurrence; weight loss; urine alkalinization may help -> if overdue -> calcium oxalate stones

160
Q

diagnosis of rheumatoid arthritis

A

at least 4 of these: morning stiffness for >1hr, arthritis of >=3 joints for >6wks, arthritis of hand joints, symmetric arthritis for >6wks, rheumatoid nodules, serum rh factor positive, radiographic changes typical of RA; FOGGY to diagnose

161
Q

treatment modalities for rheumatoid arthritis

A

rest, motion exercise, physiotherapy, diet, heat, cold; symptomatic tx w/nsaid; dz modifying drugs (dmard); immunosuppressant drugs (w/flair up); corticosteroids, surgery, novel/experimental

162
Q

NSAIDs clinical effects in rheumatoid arthritis

A

anti-inflammatory; analgesic

163
Q

risk for NSAID-induced GI bleeding

A

low: acetaminophen (not used in RA), ibuprofen; intermediate: aspirin, diclofenac, diflunisal; high: piroxicam, indomethacin, ketoprofen

164
Q

disease modifying anti-rheumatic drugs (DMARDs) uses

A

to reduce/prevent joint damage (nsaids relieve symptoms, no real effect on destruction)

165
Q

DMARDs features

A

poorly understood mech’s; none effective in >60% pt’s -> unpredictable efficacy; therapeutic effects take 2-4 mths; if ineffective in pt once, not considered in future for same pt

166
Q

important DMARDs

A

methotrexate (MTX), gold compounds, cytotoxic agents

167
Q

methotrexate characteristics

A

aminopterin analogue; cytostatic drug

168
Q

methotrexate pk

A

oral, subQ, im, iv

169
Q

methotrexate pd in rheumatoid arthritis

A

low doses DMARD -> module immune system; inhibit AICAR transformylase, thymidilate synthetase pathway (higher conc) -> dec PMN chemotaxis; inhibit DHFR -> dec lymphocyte, macrophage fxn

170
Q

methotrexate moa1

A

-> inc AICAR -> AICAR inhibits ADA, AMP deaminase -> AMP, adenosine inc, AMP -> adenosine -> inc inc adenosine -> act on A2b receptors -> suppress NF-kappaB activation induced by TNF, other inflammatory mediators

171
Q

methotrexate interactions

A

nsaid reduce Cl; combo w/sulfonamides potentiates bone marrow toxicity

172
Q

methotrexate adverse effects

A

GI, stomatitis, hair loss, mild inc liver enzymes; RARE: leukopenia, thrombopenia, severe inc liver enzymes, cns disturbances

173
Q

methotrexate contraindications

A

teratogen in pregnancy

174
Q

combine methotrexate with:

A

folic acid daily (stomatitis)

175
Q

methotrexate effects at (time)

176
Q

methotrexate advantages vs other DMARDs

A

best response rate; less ae’s; well-tolerated longterm; well tolerated in dmard combo tx

177
Q

gold compounds moa

A

taken up by macrophages -> suppress phagocytosis, enzyme activity -> slows bone/articular destruction in ra

178
Q

gold compounds effects at (time)

A

after 4-6mths of tx, with ae’s acting immediately

179
Q

gold compounds toxicity

A

dermatology, hematology, kidneys -> infrequently used

180
Q

cytotoxic agents

A

alkylating agents; antimetabolites; others

181
Q

alkylating agents

A

chlorambucil, cyclophosphamide

182
Q

chlorambucil, cyclosphosphamide moa

A

cross-link dna -> prevent replication

183
Q

chlorambucil, cyclophosphamide toxicities

A

bone marrow suppression; infertility; carcinogenic risk (most cytostatics); hemorrhagic cystitis (characteristic)

184
Q

chlorambucil, cyclophosphamide contraindications

A

teratogen - pregnancy

185
Q

antimetabolites

A

azathioprine (azt)

186
Q

azathioprine characteristics

A

purine metabolite; prodrug of 6-mercaptourine

187
Q

azathioprine pd

A

converted to 6-mercaptourine -> convert to additional metabolites -> inhibit de novo purine synth -> suppress B, T cell fxn, Ig synth, IL-2 secretion

188
Q

azathioprine interactions with allopurinol

A

xanthine oxidase metabolizes active material of azt b4 excretion in urine -> pt’s on allopurinol need to reduce azt dose

189
Q

azathioprine toxicities

A

bone marrow suppression; GI disturbances; inc infections/malignancies

190
Q

leflunomide pd

A

arrest cells in G1 phase -> inhibit autoimmune T cell prolif, autoantibody synth by B cells; other cells not affected -> use salvage pathway whereas activated lymphocytes need de novo since need is 8x

191
Q

biological response modifiers

A

anti-cytokine (anti-TNF); anti-IL1; others (abatacept, rituximab)

192
Q

anti-cytokines (anti-TNF)

A

adalimumab; etanercept; infliximab

193
Q

anti-IL1

194
Q

biological response modifiers uses

A

in combo with low dose mtx; in earlier tx

195
Q

biological response modifiers contraindications

A

when pt has history of immunosuppression i.e. TB

196
Q

asthma abnormality

A

insufficient expiration

197
Q

drugs used in asthma symptom relief

A

symptom relief: beta2 agonists (fast/long-acting), ipratropium, theophylline (less often)

198
Q

drugs used in asthma long term control

A

corticosteroids; cromolyn, nedocromil; leukotriene modifiers; anti-IgE antibody

199
Q

adjunct drugs used in asthma

A

antibiotics; mucolytics; oxygen (sedatives ci’d)

200
Q

asthma last resort drugs

A

general anesthesia; muscle relaxation; controlled respiration; bronchial lavage; ketamine

201
Q

short-acting beta2 agonists

A

albuterol, levalbuterol, pirbuterol, terbutaline, metaprotenerol - for acute episodes

202
Q

long-acting beta2 agonists

A

salmeterol, formoterol - for prophylaxis, long term therapy

203
Q

beta2 agonists adverse effects

A

selectivity is relative; beta2 - muscle tremor, diabetogenic; beta1 - tachy, arrhythmogenic; loss of responsiveness; high dose continuous use - hypokalemia;

204
Q

beta2 agonists uses

A

NOT anti-inflammatory; can be for preventative i.e. b4 going to gym

205
Q

beta2 agonists and theophylline moa

A

can have over-additive effect!

206
Q

theophylline characteristics

A

methylxanthine, related: caffeine, theobromine

207
Q

theophylline pk

A

oral, sustained release; iv; many drug interactions; low therapeutic margin

208
Q

theophylline adverse effects

A

cns - nervousness, tremor; cv - catecholamine release, +inotropy/chronotropy; arrhythmogenic; GI - hyperacidity, nausea

209
Q

theophylline toxicities

A

convulsions, coma

210
Q

theophylline uses

A

controversial -> dec in US (seizure risk - last choice); considered safe/useful in Europe esp in emergencies; more used for intermittent claudication

211
Q

theophylline molecular moa

A

induce histone deacetylase -> dec inflammatory gene expression -> promotes corticoid action (unrelated to phosphodiesterase) -> controller/preventer drug

212
Q

anticholinergics

A

ipratropium, thiotropium

213
Q

ipratropium characteristics

A

polar compound; mostly local effect when used as inhalant; ineffective in 30% of asthma pt’s

214
Q

ipratropium adverse effects

A

rare w/usual doses; dry mouth; NO tremor, tachy, dyskrinia (thickening mucous)

215
Q

ipratropium uses

A

esp COPD w/vagal components; asthma in kids/old; psychogenic exacerbations of asthma; combo with beta2 agonists

216
Q

thiotropium characteristics

A

much longer half-life; limited absorption from bronchial mucosa into system; some selectivity for M1, M3 receptors; labeled for COPD (combo tx)

217
Q

corticosteroids inhalants

A

beclomethasone, budesonide, flunisolide, fluticasone

218
Q

corticosteroids systemic

A

any e.g. prednisone, dexamethasone

219
Q

corticosteroids adverse effects

A

depends on dose/asthma severity; inhalant low dose - local ae’s, insig systemic ae’s; inhalant high dose - local ae’s, minor systemic (avoid in kids); oral/systemic - severe systemic ae’s; single high dose (emergencies) - no systemic except risk of infection, aggravate DM

220
Q

beclomethasone, budesonide, flunisolide, fluticasone pd

A

dec asthma symptoms; dec hyperreactivity; improve bronchial/pulmonary epithelial fxns

221
Q

beclomethasone, budesonide, flunisolide, fluticasone pk

A

10% inhaled deployed into bronchial tree

222
Q

beclomethasone, budesonide, flunisolide, fluticasone application

A

use application aids (e.g. spacer); in combo - apply 10 mins after b2 agonist inhaled

223
Q

beclomethasone, budesonide, flunisolide, fluticasone local adverse effects

A

oral/esophageal candidiasis, hoarseness -> apply b4 meals

224
Q

beclomethasone, budesonide, flunisolide, fluticasone systemic adverse effects

A

little bioavail -> minor ae’s compared to systemic corticosteroids

225
Q

cromolyn, nedocromil characteristics

A

mast cell stabilizers

226
Q

cromolyn, nedocromil pk

A

topical aerosol (for other indications - nasal spray, eye drops, oral)

227
Q

cromolyn, nedocromil pd

A

inhibit early/late response by stabilizing mast cells, eosinophils -> dec hyperreactivity

228
Q

cromolyn, nedocromil uses

A

preventative tx of antigen/exercise-induced asthma; INEFFECTIVE in acute exacerbation

229
Q

cromolyn, nedocromil adverse effects

A

cough, airway irritation; RARE: drug allergies, gastroenteritis

230
Q

leukotriene modifiers pd

A

effective in antigen/exercise-induced asthma, esp aspirin-asthma

231
Q

leukotriene modifiers adverse effects

A

inc LFT, headache, dyspepsia

232
Q

leukotriene modifiers

A

zileuton, montelukast, zafirlukast

233
Q

zileuton moa

A

5-lipoxygenase antagonist; rarely used

234
Q

montelukast, zafirlukast moa

A

LTD4 anatagonist, also blocks LTE4

235
Q

leukotriene modifiers characteristics

A

less effective than inhaled corticosteroids, but used to dec cort. dose; definite position in asthma therapy not established

236
Q

mucolytics pd

A

facilitate expectoration by dec viscosity of bronchial mucus

237
Q

mucolytics

A

water (most important); acetylcysteine

238
Q

acetylcysteine pd

A

disrupts S-S bonds in mucoproteins

239
Q

mucolytics application

A

nebulizer, oral, iv, endotracheal lavage; tastes, smells like rotten eggs -> oral is best

240
Q

mucolytics adverse effects

A

mechanical airway irritation, GI disturbances; allergic rxns; use w/CAUTION in severe acute asthma, gastric ulcer pt’s

241
Q

asthma absolute contraindications

A

ALL beta-blockers; cholinergic drugs; centrally-acting anticholinergic drugs; codeine, dextrometorphane; aspirin, other nsaids

242
Q

asthma relative contraindications

A

diuretics; ace-inhibitors; cns depressants; sedatives

243
Q

treatment of mild intermittent asthma

A

reliever - inhaled short-acting beta2 agonist as needed - less than 1x/day; controller - none or cromolyn b4 allergen exposure

244
Q

treatment of mild persistent asthma

A

reliever - inhaled short-acting beta2 agonist as needed, but less than 4x/day; controller - inhaled low dose corticosteroid or cromolyn, nedocromil

245
Q

treatment of moderate persistent asthma

A

reliever - inhaled long-acting beta2 agonist; controller - inhaled corticosteroid

246
Q

treatment of severe persistent asthma

A

reliever - (plus oral theophylline); controller - oral corticosteroid

247
Q

asthma prevention of acute exacerbation

A

short oral prednisolone ‘rescue’ at anytime

248
Q

emergency treatment of asthma

A
  1. oxygen, monitor
249
Q

NO-NO’S in asthma emergency treatment

A

nedocromil, cromolyn; uncritical sedation

Pharmacology (15 decks)

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