Unit 3 Pharm

Front 1

Dimenhydrinate or Diphenhydramine

Back 1

Antihistamine/Antimuscarinic block H1 receptor in nucleus tractus solitarius where histaminergic synapses relay muscarinic impulses from the vestibular pathway to the emetic center.

Effective for motion sickness, vestibular component of opioid-induced NV.

Drowsiness, dry mouth, blurred vision

Front 2

Scopolamine

Back 2

Antimuscarinic blocks M1 receptors centrally and M1&3 peripherally.

Prevents (not treats) motion sickness.

Dry mouth, blurred vision, tachycardia.

Front 3

Lorazepam, Diazepam

Back 3

Benzodiazepines reduce NV from central cortical regions.

Prevents anticipatory nausea.

Sedation, enhances CNS depression of alcohol.

Front 4

Metoclopramide, Prochlorperazine, Domperidone

Back 4

Dopamine antagonists act at chemoreceptor trigger zone.

Treats chemotherapy, estrogen-induced NV.

Front 5

Odansetron

Back 5

5-HT3 antagonists block serotonergic receptors involved in initiation of vomiting reflex.

Controls chemo-induced NV, visceral inflammatory NV. No effect on D2-mediated pathways or late chemo-induced NV. Flat dose response.

Front 6

Dexamethasone

Back 6

Cortiosteroids inhibit gut 5HT release.

Treat inflammatory GI NV, reduce ICP in closed head injury, altitude sickness, enhance responses to other antiemetrics.

Front 7

Casopitant

Back 7

NK-1 antagonist treats late-phase chemo induced NV

Front 8

Nabilone, Dronabinol

Back 8

CB1 agonists used in refractory cancer/HIV drug induced NV

Intoxication and hallucination

Front 9

Antacids (Aluminum Hydroxide, Sodium Bicarbonate, Magnesium Hydroxide)

Back 9

Neutralizes acids (weak bases that buffer acids). Quick acting, quick relief, cheap, but blocks activation of PPIs.

Front 10

Ranitidine

Back 10

H2 receptor antagonist, reduces gastric acid secretion.

Front 11

Omeprazole

Back 11

PPI. Reduces acid by irreversibly inactivating H+/K+ ATPase, only activated at very low pH (thus don't use antacids).

Impairs B12 absorption and can lead to C. difficile or pneumonia.

Front 12

Pirenzepine

Back 12

M1 selective muscarinic antagonists. Leads to reduced gastric acid. Side effect of diarrhea.

Front 13

Sucralfate

Back 13

Enhance mucosal defense by coating (adheres well to gastric/duodenal ulcers). Requires acidic pH for activation so don't give with antacid/PPI/H2 antagonist.

Front 14

PPI + clarithromycin + metronidazole

Back 14

Kills H. pylori. Amoxicillin normally, metronidazole for penecillin allergic pts.

Front 15

Diphenoxylate & Loperamide

Back 15

Opioid agonists. Agonist at mu receptors in myenteric plexuses opens K+ channels hyperpolarizing cholinergic neurons involved in motility and δ receptors in epithelium to inhibit secretion. Loperamide does not cross BBB so minimum abuse potential or CNS effects.

Front 16

Absorbants (hydrophilic bulking agents) psyllium [Metamucil]

Back 16

Treat diarrhea by absorbing water. Treats constipation by absorbing water and swelling into a gel in large intestine. Instestinal dimension leads to increased peristalsis.

Treat with sufficient fluid, treats mild diarrhea.

Front 17

Adsorbants (bile binding resins: cholestyramine)

Back 17

Treats bile-acid-induced diarrhea due to bile malabsorption. Binds bile acids and some C. diff/E. coli enterotoxins so can be used as adjunct to antibacterials.

In ileal resected patients, will cause steatorrhea.

Front 18

Bismuth Subsalicylate [Pepto-Bismol]

Back 18

For acute diarrhea/traveler's diarrhea.

Front 19

Empiric Antimicrobials

Back 19

Rifaximin or fluoroquinolone treats febrile traveler's diarrhea.

Front 20

Odansetron, granesetron, etc.

Back 20

5-HT3 blockers. Blocks 5-HT3 receptors (serotonergic receptors in the vomiting reflex) in periphery (visceral vagal afferent) and in brain (chemo trigger zone). Long duration and effective against all grades of emesis.

Front 21

Metoclopramide

Back 21

Substrituded benzamides. D2 antagonists. Highly effective against cisplatin. Antidopaminergic side effects (sedation, diarrhea, extrapyramidal simptoms).

Front 22

Droperidol, haloperiodol

Back 22

Butyrophenones. Blocks dopamine receptors. Sedates and used in combo with other medications.

Front 23

Lorazepam, diazepam

Back 23

Benzodiazepines. Reduces NV originating from central cortical regions (emotional) due to GABA antagonism. Prevents anticipatory nausea but side effects include sedation, enhanced CNS depression by drugs.

Front 24

Dexamethasone

Back 24

Corticosteroid. Inhibits 5-HT release. Enhanced response to other antiemetics, treats inflammatory NV, altitude sickness. Side effects are immunosuppression, hyperglycemia, fat redistribution.

Front 25

Nabilone, Dronabilnol

Back 25

Cannabinoids. CB1 agonists used in refractory cases or moderate chemotherapy. Side effects are dysphoria, hallucinations, sedation, orientation.

Front 26

Aprepitant

Back 26

Substance P/Neurokinin-1 Receptor blocker. Targets neurokinin receptor in the brain and blocks the actions of natural substance.

Front 27

Ferrous (Fe2+) Sulfate

Back 27

Corrects defieciency of iron stores (ferritin). Absorbed in duodenum & proximal jejunum (must be 2+ form). Side effects are GI irritation: epigastric pain, NV, constipation/diarrhea.

Front 28

Iron (Fe3+) dextran

Back 28

Parenteral (injection) if oral efficacy reduced or GI side effects too much. Only use when oral therapy is not an option.

Front 29

Deferoxamine / Defirasirox (2nd line)

Back 29

Acute iron overdose due to iron absorption continuing even in excess iron. CP: GI irritation/cardiovascular collapse, then later bleeding/clotting irregularities + acidosis/edema, then liver/kidney injury, then GI fibrosis.

Deferoxamine = parenteral iron chelator that is excreted later in urine.

Front 30

Hydroxocobalamin

Back 30

Decrease of folate/Vit B causes decreased production/abnormal maturation of RBC precursors. Also decreased B12 leads to methylmalonyl-coA buildup leading to subacute combined degeneration (demyelination). Caused by pernicious anemia mostly.

Front 31

Folic acid

Back 31

Deficiency due to increased demand (pregnancy), poor absorption, alcoholism, dihydrofolate reductase inhibitors (methotrexate). Causes megaloblastic anemia b/c cannot make DNA and proliferate. Give folic acid only if sure it's not Vitamin B12 deficiency.

Front 32

Erythropoietin and Darbepoetin

Back 32

EPO released by kidneys to activate RBC precursors. EPO treatment effective in end-stage renal disease and HIV and anemia of chronic disease.

Darbepoetin is long-acting and not used for acute cases.

Side effects may be cardiovascular events, tumor progression.

Front 33

azathioprine

Back 33

Active form is a nucleoside analog so incorporated into growing DNA but lacks 3' OH. Blocks clonal prolif of T/B lymphocytes.

Used for AID and organ transplant.

Front 34

cyclophosphamide

Back 34

Alkylating agent. Biotransformed to phosphoramide mustard by P450 in liver. Reaction of phosphoramide with DNA is cytotoxic.

Front 35

cyclosporine (tacrolimus same mechanism)

Back 35

Act at clonal prolif stage and differentiation. Inhibits transcription of IL-2 reducing T cell prolif not B cell.Nephrotoxic.

Front 36

filgrastim (G-CSF)

Back 36

Recombinant G-CSF to treat neutropenia, stimulating BM.

Front 37

imatinib (Gleevec)

Back 37

Blocks tyrosine kinase active sites. Especially used in CML (philadelphia chromosome with active TyrK bcr-abl).

Front 38

methotrexate

Back 38

Structually related to folic acid and acts as antagonist of folic acid by inhibiting dihydrofolate reductase (converts folate to THF). Thus inhibits DNA synthesis (esp thymidine).

Front 39

mycophenolate

Back 39

Inhibits IMP dehydrogenase, enzyme that controls GMP synthesis in purine synthesis in B/T lymphocytes.

Used for organ transplant.

Front 40

prednisone

Back 40

Reduces lymphoid content in spleen/LNs, enhances destruction of lymphocytes (esp T), interferes with lymphoid cell cycles, inhibits Ab formation, inhibits macrophage phagocytosis. Works at clonal prolif, differentiation, and immune effect levels. For AID and transplant.

Front 41

Senna (anthraquinone glycoside)

Back 41

Irritant/Stimulant of colon mucosa leading to more peristalsis = laxative.

Front 42

Castor Oil

Back 42

Broken down to ricinoleic acid, which is very irritating to gut, leading to explosive diarrhea sometimes.

Front 43

Bisacodyl

Back 43

Long onset to effect 6-10 hrs. Contact laxative: Increases fluid/NaCl secretion.

Front 44

Methylcellulose, psyllium seeds

Back 44

Bulk laxatives that form gels in large intestine causing water retention and intestinal distention -> increasing peristalsis.

Front 45

Magnesium sulfate, Magnesium citrate, sodium phosphate, madnesium hydroxide, lactulose

Back 45

Nonabsorbable salts that hold water in intestine by osmosis and cause distention.

Front 46

Docusate

Back 46

Stool softeners. Become emulsified with stool producing softer feces.

Front 47

Mineral oil

Back 47

Lubricants. Facilitate passage of hard stools.

Front 48

clopidogrel

Back 48

Platelet aggregation blockers. Irreversibly inhibit binding of ADP to its receptors on platelets, thus inhibiting GPIIb/IIIa recetpros to bind fibrinogen.

Used to prevent thrombotic events with heart congestion. May cause TTP.

Front 49

eptifibatide

Back 49

Antiplatelet drug that blocks GP IIb/IIIa receptor so that receptor cannot interact with fibrinogen.

Decreases incidence of thrombotic copmlications of cornonary syndromes. Adverse effect is bleeding.

Front 50

warfarin

Back 50

Vitamin K antagonist. Inhibits Vitamin K epoxide reductase which converts K back to active form. Thus prevents activation of 10, 9, 7, 2 factors. 8-12 hrs till effect.

Used to prevent DVTs or pumonary embolism. Also for infarction patients, Afib and prosthetic heart valves. Bleeding is #1 side effect.

Front 51

heparin

Back 51

Thrombin inhibitor. Binds to antithrombin III (which normally inhibits thrombin and Factor 10) and increases activity 1000x. Allows antithrombin to rapidly inhibit circulating thrombin and Xa.

Used to prevent DVT, pulmonary embolism, surgery, infarction. Can lead to bleeding (treat with protamine sulfate), hypersensitivity, later thrombosis, and thrombocytopenia/thombosis in HIT.

Front 52

tissue plasminogen activators: tenecteplase

Back 52

Rapidly activates plasminogen that is bound to fibrin in a thrombus plug. Selectively lyses fibrin.

Used for myocardial infarction, pulmonary embolism, ischemic stroke. Can leed ro hemorrhage.