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Pharmacology > Exam III > Flashcards

Exam III Flashcards

1
Q

Sodium Bicarbonate

A
  • aka Alka Seltzer
  • antacid = neutralizes gastric acid.
  • fast acting, short duration
  • CO2 ⇒ belching, flatulence
  • only used short term, not very effective
  • use: heart burn
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2
Q

Calcium Carbonate

A
  • aka Tums
  • antacid = neutralizes gastric acid
  • fast acting, short duration.
  • CO2 ⇒ belching, flatulence
  • only used short term, not very effective
  • causes rebound ↑ H+ secretion
  • use: heart burn
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3
Q

Magnesium Hydroxide

A
  • antacid
  • given in combo with Aluminum Hydroxide
  • alone causes diarrhea (saline laxative)
  • toxicity in pts with renal insufficiency
  • use: heart burn, acute constpipation
  • side effects: hypermagnesemia in pts with renal insufficiency
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4
Q

Aluminum Hydroxide

A
  • antacid
  • given in combo with magnesium hydroxide
  • alone causes constipation
  • toxicity in pts with renal insufficiency
  • use: heart burn
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5
Q

Antacids

A
  • neutralizes gastric acid
  • fast acting, short duration
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6
Q

PPI

A
  • inhibits H+K+ ATPase
  • reduce gastric acid secretion
  • long acting, take 1x a day
  • prodrug, take 1 hr before eating (take on empty stomach, is weak base)
  • t1/2 = <2hr, hepatic elimination
  • 3-4 days for max effect
  • converted to active form in stomach
  • use: GERD, peptic/duodenal ulcers, prevent NSAID ulcers, prevent stomach bleeding.
    • H. pylori: use PPI with 2 antibiotics
  • side effects: ↑ risk GI infection
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7
Q

H2 Blockers

A
  • reduce gastric acid secretion
  • faster onset than PPI but less effective
  • use: GERD, peptic/duodenal ulcers, prevent NSAID ulcers, prevent stomach bleeding in the critically ill (stress gastritis)
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8
Q

Gastrin

A
  • acts on parietal cells, enterochromaffin-like cells (ECL)
  • parietal cells: stimulates H+K+ ATPase (proton pump) via CCK2 receptor ⇒ gastric acid release
  • ECL: stimulates release of histamine ⇒ parietal cell activation
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9
Q

Histamine

A
  • acts on parietal cells
  • via H2 receptor, stimulates H+K+ ATPase ⇒ gastric acid release.
  • causes: bronchoconstriction, ↑ GI motility, ↑ gastric acid, ↑ HR, vasodilation, pain and itching, triple response (reddening, wheal, flare)
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10
Q

ACh (GI)

A
  • acts on parietal cell and enterochromaffin like cell (ECL)
  • parietal: thru M3 stimulates H+K+ ATPase ⇒ gastric acid release
  • ECL: release histamine ⇒ parietal cell activation
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11
Q

Omeprazole

A
  • inhibits H+K+ ATPase
  • reduce gastric acid secretion
  • long acting, take 1x a day
  • prodrug, take 1 hr before eating (take on empty stomach, is weak base)
  • t1/2 = <2hr, hepatic elimination
  • 3-4 days for max effect
  • converted to active form in stomach
  • use: GERD, peptic/duodenal ulcers, prevent NSAID ulcers, prevent stomach bleeding.
    • H. pylori: use PPI with 2 antibiotics
  • side effects: ↑ risk GI infection
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12
Q

Esomeprazole

A
  • inhibits H+K+ ATPase
  • reduce gastric acid secretion
  • long acting, take 1x a day
  • prodrug, take 1 hr before eating (take on empty stomach, is weak base)
  • t1/2 = <2hr, hepatic elimination
  • 3-4 days for max effect
  • converted to active form in stomach
  • use: GERD, peptic/duodenal ulcers, prevent NSAID ulcers, prevent stomach bleeding.
  • H. pylori: use PPI with 2 antibiotics
  • side effects: ↑ risk GI infection
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13
Q

Lansoprazole

A
  • inhibits H+K+ ATPase
  • reduce gastric acid secretion
  • long acting, take 1x a day
  • prodrug, take 1 hr before eating (take on empty stomach, is weak base)
  • t1/2 = <2hr, hepatic elimination
  • 3-4 days for max effect
  • converted to active form in stomach
  • use: GERD, peptic/duodenal ulcers, prevent NSAID ulcers, prevent stomach bleeding.
    • H. pylori: use PPI with 2 antibiotics
  • side effects: ↑ risk GI infection
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14
Q

Cimetidine

A
  • H2 blocker
  • faster onset than PPI but less effective
  • use: heart burn (dydpepsia), GERD, peptic/duodenal ulcers, prevent NSAID ulcers, prevent stomach bleeding in critically ill (stress gastritis)
  • side effects: drug interactions (inhibits CYP)
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15
Q

Ranitidine

A
  • H2 blocker
  • faster onset than PPI, less effective
  • reduces gastric acid secretion
  • use: heart burn, GERD, peptic/duodenal ulcers, prevent NSAID ulcers, stress gastritis in critically ill
  • side effects: well tolerated
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16
Q

Famotidine

A
  • H2 blocker
  • reduces gastric acid secretion
  • faster onset than PPI but less effective
  • use: heart burn, GERD, peptic/duodenal ulcers, prevent NSAID ulcers, stress gastritis in critically ill
  • side effects: well tolerated
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17
Q

Sucralfate

A
  • mucosal protective agent
  • slurry dose, use QID via NG tube
  • use: stress-related gastritis
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18
Q

Misoprostol

A
  • mucosal protective agent
  • PGE1 analog
  • QID orally
  • use: prevent NSAID ulcers
    • use with antipregestin to expel aborted fetus
  • side effects: diarrhea, abd cramps/pain
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19
Q

Bismuth-Salicylate

A
  • aka Peptobismol
  • use: dyspepsia, diarrhea, in 2nd line therapy for H pylori
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20
Q

Metoclopramide

A
  • D2 blockade, 5-HT4 agonism, 5-HT3 antagonism
  • suppresses DA effects on ACh release from myenteric plexus ⇒ ↑ stomach emptying, ↑ upper GI motility
  • D2 block ⇒ ↓ nausea/vomiting from chemo trigger zone
  • use: ↑ stomach emptying in diabetic/post surg gastric stasis, GERD resistant to PPI/H2 blockers, anti-emetic, CINV**
  • side effects: sedation, restlessness, anxiety, agitation in elderly, extra-pyramidal symptoms, irreversible tardive dyskinesia
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21
Q

Erythromycin

A
  • macrolide antibiotic
  • stimulates GI motility via motilin
  • use: gastric stasis
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22
Q

Methylnatrexone

A
  • opioid antagonist
  • doesn’t cross BBB
  • use: prevent opioid induced constipation without blocking analgesia
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23
Q

Alvimopan

A
  • opioid antagonist
  • can’t cross BBB
  • use: prevent opioid induced constipation without blocking analgesia
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24
Q

Stimulant Laxatives

A
  • act on enteric nerves to ↑ colon contractions and secretions
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25
Q

Bisacodyl

A
  • stimulant laxative
  • acts on enteric nerve to ↑ colon contractions and secretions
  • 6-10 hr onset after oral, 30-60 min rectal onset
  • use: with stool softeners to prevent/treat opioid constipation, with osmotic laxative before bowel surgery/exam
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26
Q

Anthraquinones

A
  • stimulant laxatives
  • 6-12 hr onset orally, 2 hr rectally
  • not safe
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27
Q

Osmotic Laxatives

A
  • poorly absorbed
  • retain water in GI tract via osmotic activity
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28
Q

Balanced Polyethylene Glycol Solution

A
  • osmotic laxative
  • retain water in GI tract via osmotic activity
  • use: bowel cleansing before exams**, prevent/treat constipation
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29
Q

Saline Laxatives

A
  • magnesium or phosphate salts
  • fast acting
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30
Q

Sodium Phosphate

A
  • saline laxative
  • fast acting 1-3 hr
  • use: two dose regiment for bowel cleansing before exams
  • dont’ use in pts with renal/cardiac disease, electrolyte abnormalities
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31
Q

Magnesium Citrate

A
  • saline laxative
  • use: acute constipation
  • side effect: hypermagnesemia in pt with renal insufficiency
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32
Q

Lactulose

A
  • indigestible sugar
  • converted to fatty acids by colonic bacteria ⇒ acid trap ⇒ ↓ blood ammonia in hepatic encephalopathy
  • slow acting 24-48 hr
  • side effect: flatulence, cramps
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33
Q

Sorbitol

A
  • indigestible sugar
  • slow acting 24-48 hr
  • induces diarrhea
  • side effect: flatulence, cramps
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34
Q

Mannitol

A
  • indigestible sugar/alcohol
  • slow acting 24-48 hr
  • induces diarrhea
  • side effect: flatulence, cramps
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35
Q

Bulk Forming Laxatives

A
  • slow acting 1-3 days
  • absorbs water, distends colon, promotes peristalsis.
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36
Q

Bran

A
  • bulk-forming laxative
  • slow acting 1-3 days
  • absorbs water, promotes peristalsis
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37
Q

Psyllium

A
  • bulk-forming laxative
  • slow acting 1-3 days
  • absorbs water, promotes peristalsis
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38
Q

Methylcellulose

A
  • bulk-forming laxative
  • short acting 1-3 days
  • absorbs water, promotes peristalsis
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39
Q

Polycarbophil

A
  • bulk-forming laxative
  • slow acting 1-3 days
  • absorb water, promote peristalsis
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40
Q

Stool Softeners

A
  • slow acting 1-3 days
  • increase water and lipid content in stool
  • give oral or rectal
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41
Q

Docusate

A
  • stool softener
  • slow acting 1-3 day
  • increases water and lipid in stool
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42
Q

Lubiprostone

A
  • chloride channel activator
  • prostanoic acid analog
  • increases intestinal secretions
  • use: chronic constipation, IBS with constipation
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43
Q

Loperamide

A
  • meperidine analog
  • use: OTC for diarrhea
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44
Q

Simethicone

A
  • anti-foaming agent
  • use: reduce esophageal reflux when with antacids
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45
Q

Ocreotide

A
  • somatostatin analog
  • inhibits secretion of GI/pancreatic hormones and 5-HT
  • use: dumping syndrome/diarrhea after gastric surgery; watery diarrhea and flushing etc from carcinoid tumors and VIPomas; ↓ portal pressure and variceal bleeding from chronic liver disease
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46
Q

Alosetran

A
  • long acting 5-HT3 antagonist
  • use: IBS with diarrhea
  • side effects: constipation, fatal ischemic colitis
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47
Q

Vomiting Center Stimulants

A
  • from chemoreceptor trigger zone: D2, opioid, NK1, 5-HT3
  • vestribular system: M1, H1
  • vagal and spinal afferents: 5-HT3
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48
Q

-setron

A
  • 5-HT3 antagonists
  • no drug interactions
  • use: nausea and vomiting; with dexamethosome for acute CINV; with NK1 antagonist for delayed CINV
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49
Q

Odansetron

A
  • 5-HT3 antagonist
  • no drug interactions
  • use: nausea and vomiting; with dexamethosome for acute CINV; with NK1 antagonist for delayed CINV
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50
Q

Granisetron

A
  • 5-HT3 antagonist
  • no drug interactions
  • use: nausea and vomiting; with dexamethosome for acute CINV; with NK1 antagonist for delayed CINV
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51
Q

Dolasetron

A
  • 5-HT3 antagonist
  • no drug interactions
  • use: nausea and vomiting; with dexamethosome for acute CINV; with NK1 antagonist for delayed CINV
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52
Q

Palosetron

A
  • 5-HT3 antagonist
  • longest t1/2
  • no drug interactions
  • use: nausea and vomiting; with dexamethosome for acute CINV; with NK1 antagonist for delayed CINV
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53
Q

Dexamethosone

A
  • corticosteroid
  • oral or IV
  • enhances effects of 5-HT3 antagonists
  • use: with 5-HT3 antagonists for CINV
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54
Q

NK1 Antagonist

A
  • antagonizes substance P in periphery and CNS
  • enhances effects of 5-HT3 antagonists
  • may inhibit drug metabolism by CYP3A4
  • use: with 5-HT3 and dexamethosone for delayed CINV
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55
Q

Aprepitant

A
  • NK1 antagonist
  • antagonizes substance P in periphery and CNS
  • enhances effects of 5-HT3 antagonists
  • may **inhibit **drug metabolism by CYP3A4
  • use: with 5-HT3 and dexamethosone for delayed CINV
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56
Q

Fosaprepitant

A
  • NK1 antagonist
  • antagonizes substance P in periphery and CNS
  • enhances effects of 5-HT3 antagonists
  • may **inhibit **drug metabolism by CYP3A4
  • use: with 5-HT3 and dexamethosone for delayed CINV
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57
Q

Droperidol

A
  • cannabinoid
  • strong D2 blocking effects
  • use: CINV
  • side effect: QT prolongation and sudden death
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58
Q

Cyclizine

A
  • H1 antagonist
  • use: motion sickness
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59
Q

Scopolamine

A
  • antimuscarinic
  • use: motion sickness
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60
Q

Benzos

A
  • anxiolytic
  • use: reduce anticipatory nausea and vomiting with chemo
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61
Q

Pancrelipase

A
  • pancreatic extract containing lipase, amylase, proteolytic activity
  • take before meals
  • use: pancreatic enzyme deficiency from cystic fibrosis, pancreatitis
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62
Q

Ursodiol

A
  • natural bile acid
  • use: dissolve small cholesterol gallstones, prevent gall stones during rapid weight loss, treat cholesterol gallstones as last resort
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63
Q

5-ASA

A
  • 5-amilosalicylic acid
  • anti-inflammatory on diseased GI mucosa.
  • use: induce/maintain remission in mild-mod UC, Crohn’s
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64
Q

Basalazide

A
  • 5-ASA analog with azo linkage
  • converted in gut to 5-ASA
  • use: IBD
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65
Q

Olsalazine

A
  • 5-ASA analog with azo linkage
  • converted in gut to 5-ASA
  • use: IBD
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66
Q

Sulfasalazine

A
  • 5-ASA analog with azo linkage
  • converted in gut to 5-ASA
  • use: IBD
  • not well tolerated
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67
Q

Mesalamine

A
  • 5-ASA delayed release tablets, enemas, and suppositories
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68
Q

Budesonide

A
  • glucocorticoid
  • use: IBD
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69
Q

Azothioprine

A
  • antimetabolite
  • anti-cancer drug interferes with nucleotide synthesis.
  • inhibits cell proliferation, immunosuppressive effect
  • use: low dose for IBD, induce/maintain remission of UC and Crohn’s
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70
Q

6-Mercaptopurine

A
  • antimetabolite
  • anti-cancer drug interferes with nucleotide synthesis.
  • inhibits cell proliferation, immunosuppressive effect
  • use: low dose for IBD, induce/maintain remission in UC and Crohn’s
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71
Q

Inflixumab

A
  • TNFalpha Ab
  • immunosuppressive
  • use: mod-severe IBD that doesn’t respond to others
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72
Q

Adalimumab

A
  • TNFalpha Ab
  • immunosuppressive
  • use: mod-severe IBD that doesn’t respond to others
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73
Q

Certolizumab

A
  • TNFalpha Ab
  • immunosuppressive
  • use: mod-severe IBD that doesn’t respond to others
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74
Q

Natalizumab

A
  • anti-integrin Ab
  • against alpha4 subunit of integrins
  • interferes with leukocyte adherence and migration thru vascular endothelium to GI mucosa target cells
  • use: severe Crohn’s resistant to others
  • side effect: fatal leukoencephalopathy with latent JC virus
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75
Q

Delayed CINV

A
  • >24 hr after cancer therapy
  • due to GI mucosal damage triggering mociceptive input and release of 5-HT and mediators
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76
Q

Acute CINV

A
  • <2 hr after cancer therapy
  • from chemoreceptor trigger zone stimulation
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77
Q

H1

A
  • causes ↑ Ca via Gq
  • in endothelial cells and smooth muscle
  • in lungs, GI, uterus, small blood vessels
  • constricts smooth muscle
  • dilates endothelial cells
  • ⇒ bronchoconstriction, ↑ GI motility, ↑ uterine contraction, arterial vasodilation, venous vasoconstriction
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78
Q

H2

A
  • causes ↑ cAMP via Gs
  • in heart, stomach, mast cells, brain
  • causes ↑ HR
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79
Q

H3

A
  • causes ↓ cAMP, activated ERK
  • on presynatpic membrane
  • causes negative feedback
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80
Q

H4

A
  • causes ↓ cAMP, ↑ Ca
  • on leukocytes
  • in immune system, regulates cytokine production
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81
Q

H1 antagonists

A
  • 1st gen cause sedation, can cross BBB
  • 2nd gen don’t cause sedation
  • use: allergic rxn, motion sickness, Meniere’s disease, sedation
  • has antiparkinson effects, anticholinergic effects, antiserotinergic effects, local anesthesia via inhibited voltage gated Na channels, orthostatic hypotension
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82
Q

Chlorpheniramine

A
  • 1st gen H1 antagonist
  • causes sedation
  • use: allergic rxn, motion sickness, Meniere’s disease, sedation.
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83
Q

Diphenhydramine

A
  • 1st gen H1 antagonist
  • causes sedation
  • use: allergic rxn, motion sickness, Meniere’s disease, sedation.
84
Q

Pyrilamine

A
  • 1st gen H1 antagonist
  • causes sedation
  • use: allergic rxn, motion sickness, Meniere’s disease, sedation.
85
Q

Promethazine

A
  • 1st gen H1 antagonist
  • causes sedation
  • use: allergic rxn, motion sickness, Meniere’s disease, sedation.
86
Q

Cyproheptadine

A
  • 1st gen H1 antagonist, 5-HT2 antagonist
  • causes sedation
  • use: allergic rxn, motion sickness, Meniere’s disease, sedation, post gastrectomy dump syndrome
87
Q

Fexofenadine

A
  • 2nd gen H1 antagonist
  • use: allergic rxn, motion sickness, Meniere’s disease
88
Q

Loratadine

A
  • 2nd gen H1 antagonist
  • use: allergic rxn, motion sickness, Meniere’s disease
89
Q

Cetirizine

A
  • 2nd gen H1 antagonist
  • use: allergic rxn, motion sickness, Meniere’s disease
90
Q

Acrivastine

A
  • 2nd gen H1 antagonist
  • use: allergic rxn, motion sickness, Meniere’s disease
91
Q

5-HTR1

A
  • causes ↓ cAMP via Gs
92
Q

5-HTR2

A
  • causes ↑ Ca via Gq
  • in periphery
93
Q

5-HTR3

A
  • works on ligand gated Na channel
  • not G protein coupled
94
Q

5-HTR4

A
  • causes ↑ cAMP via Gs
95
Q

5-HTR6

A
  • causes ↑ cAMP via Gs
96
Q

5-HTR7

A
  • ↑ cAMP via Gs
97
Q

Buspirone

A
  • anxiolytic
  • 5-HT1a agonist
98
Q

Sumatriptan

A
  • 5-HT1d/1b agonist
  • use: migraines
99
Q

-triptan

A
  • 5-HT agonists
100
Q

Cisapride

A
  • 5-HT4 agonist
  • use: gastroesophageal reflux
101
Q

Ritaserine

A
  • 5-HT2R antagonist
  • reduces thromboxane formation
  • blocks DA reputake, improves mood in schizo
102
Q

Ketaserin

A
  • inhibits 5-HT2
103
Q

5-HT

A
  • acts as NT on H4 causing ↑ HR
  • stimulates coronary bed
  • pos chronotropic and inotropic effects
  • triple response of BP: ↓ BP at outflow, ↑ BP in pulm and renal, ↓ BP in skeletal muscle
  • causes platelet aggregation
  • constricts smooth muscle in GI tract (cause diarrhea and malnutrition)
104
Q

‘DONT’ in Poisoning

A
  • Dextrose: when altered mental status
    • from OD with insulin, insulin-secretagogues, slicylates, starvation
  • Oxygen: for hypoxia
  • Naloxone: for opioid overdose
  • Thiamine: for Wernike-Korsakoff syndrome, reduce ketoacidosis from starvation
105
Q

Elevated Anion Gap in Poisoning

A
  • causes metabolic acidosis
  • from toxic organic acid metabolites: methanol, ethylene glycol
  • from lactic acidosis: salicylates in kids, cyanide in firefighters, CO
106
Q

Elevated Osmolar Gap in Poisoning

A
  • with alcohols: ethanol, methanol, ethylene glycol
107
Q

Hemodialysis in Poisoning

A
  • for salicylates, acetamiophen, methanol, ethylene glycol
  • not for lipophilic drugs with low aqueous solubility or drugs with high Vd
108
Q

Urinary Alkalinization in Poisoning

A
  • to eliminate salicylates
  • not useful with rhabdomyolysis
109
Q

Acetaminophen Antidote

A
  • n-acetyl-l-cysteine
110
Q

Toxic Alcohol Antidote

A
  • ethanlol + fomepizole
111
Q

CO Antidote

A
  • oxygen
112
Q

Cyanide Antidote

A
  • hydroxocobalamin or nitrite + thiosulfate
113
Q

Heroin Antidote

A
  • naloxone
114
Q

Iron Toxicity Antidote

A
  • deferoxamine (chelates)
115
Q

Inorganic Lead Antidote

A
  • dimercaptrol, succimer, EDTA (chelators)
116
Q

Mercury and Arsenic Antidote

A
  • dimercaptrol, succimer
117
Q

Anticholinesterase Antidote

A
  • atropine, pralidoxime (for organophosphate ACHEI)
118
Q

Salicylate Antidote

A
  • bicarbonate
119
Q

Cardiotoxic Drug Antidote

A
  • bicarbonate
120
Q

CO Poisoning

A
  • causes hypoxia, headaches going to coma, death.
  • tx: oxygen
121
Q

Salicylate Poisoning

A
  • mild CNS: hyperventilation, tinnitus, resp alkalosis ⇒ bicarb loss.
  • sweating, nausea, vomiting ⇒ dehydration
  • severe poisoning (kids): uncouples oxidative phosphorylation.
    • hyperthermia, metabolic acidosis, hypoglycemia, restlessness, delirium, seizures, depression, coma, resp and CV collapse, death.
  • tx: manage ABC, cool, give bicarb, give fluids, hemodialyze if severe.
122
Q

Acetaminophen OD

A
  • causes liver failure
  • tx: gastric lavage, activated charcoal, N-acetylcysteine (NAC) to replenish glutathione and detoxify NAPQI
123
Q

Serotonin Syndrome

A
  • from SSRI, MAOI, amphetamines, meperidine, methadone, dextromethorphan
  • mild symptoms: anxiety, akathisia, tremors, tachycardia, sweating, diarrhea, mydriasis
  • serotonin syndrome: clonus, hyper-vigilance, hyperthermia, HTN, hyperreflexia
  • severe: rigidity, hyperthermia >40C, seizures, coma
  • tx: discontinue drugs, give benzo anticonvulsants propranolol
124
Q

Teratogens

A
  • cytotoxic drugs
  • hormones
  • warfarin
  • methotrexate
  • ACEI, ARB
125
Q

Isotretinoin

A
  • synthetic retinoid
  • use: severe cystic acne
  • side effects: teratogen
126
Q

Aciretin

A
  • synthetic retinoid
  • use: psoriasis
  • side effect: teratogen (don’t get pregnant for 3 yrs after stopping)
127
Q

Mesolimbin DA Pathway

A
  • mediates pleasure, euphoria, wanting, craving
  • causes withdrawal
  • to frontal cortex ⇒ learn cues for drug craving
  • to nucleus accumbens ⇒ wanting/craving
128
Q

Acts on VTA

A
  • VTA = ventral tegmental area in midbrain
  • acted on by ethanol, nicotine, opioids
129
Q

Acts on Acc

A
  • Acc = nucleus accumbens
  • acted on by cocaine, amphetamines, cannabinoids, opioids
130
Q

Methadone

A
  • maintenance of heroin addicts, opioids
  • reduces cravings, induces tolerance
131
Q

Benzo (Drugs)

A
  • for alcohol withdrawal and sedative hypnotics
132
Q

Varenicline

A
  • nicotinic receptor partial agonist
  • smoking cessation
133
Q

Clonidine

A
  • alpha 2 agonist
  • reduces SNS overactivity in opiate withdrawal
134
Q

Disulfiram

A
  • aversive conditioning for alcoholics
  • causes acute physical distress from alcohol use
135
Q

Naltrexone

A
  • opioid receptor antagonist
  • reduces rewarding effects of drug use
  • for opioid addicts and alcoholics
136
Q

Acamprostate

A
  • NMDA receptor antagonism
  • reduces reinforcing effects of drug
  • for alcohol
137
Q

Amphetamine/Methamphetamine

A
  • evoke release of catecholamines in periphery and CNS
  • symptoms: ↑ HR, ↑ or ↓ BP, ↑RR, hyperthermia, mydriasis, euphoria, ↑ speech.
  • overdose: anxiety, agitation, paranoia, seizures, arrhytmias, MI, cerebral hemorrhage, rhabdomyolysis
138
Q

Cocaine/Methylphenidate

A
  • CNS effects from blocked DA reuptake
  • sympthoms: ↑ HR, ↑ or ↓ BP, ↑ RR, hyperthermia, mydriasis, euphoria, ↑ speech
  • overdose: anxiety, agitation, paranoia, seizures, arrhythmias, MI, cerebral hemorrhage, rhabdomyolysis
139
Q

MDMA/Ecstasy

A
  • **release 5-HT **
  • have mild hallucinogenic effects
  • similar to amphetamines
140
Q

LSD/Mescaline

A
  • 5-HT2A partial agonist
  • symptoms: ↑HR, ↑or↓ BP, ↑RR, mydriasis, nausea, altered perceptions with panic/anxiety
  • OD not life threatening
141
Q

Phencyclidine/Ketamine

A
  • NMDA receptor antagonist
  • symptoms: euphoria, hallucinations, agiation/violent behavior, psychosis, catatonia, anxiety/panic, ↑HR, ↑BP, ↑RR, miosis, nystagmus, rhabdomyolysis
  • overdose: go to coma, seizures, renal failure, death
142
Q

Cannabinoids

A
  • THC
  • use: anorexia from AIDs, prevent nausea/vomiting during chemo
  • symtpoms: euphoria, conjunctivitis, ptosis, ↑HR, appetite
143
Q

Anandamide

A
  • aka AEA
  • endocannabinoid
  • activates CB2 and CB1 receptors
  • released from Ca influx that N-acyl transferase
144
Q

2-AG

A
  • endocannabinoid
  • activates CB1 and CB2 receptors
  • released with Ca influx activating phospholipase C
145
Q

Rimonobant

A
  • CB1 antagonist
  • use: obesity (↓ appetite)
  • side effects: depression, off the market
146
Q

Nicotine Withdrawal

A
  • irritability, impatience, hostility
  • anxiety
  • depressed mood
  • difficulty concentrating
  • restless
  • ↓ HR
  • ↑ appetite or weight gain
147
Q

Acute Opioid Withdrawal

A
  • peaks in 36-72hr
    • drive for drug
  • begins 8-12 hr, peaks in 48-72 hr
    • tearing, runny nose, yawning, sweating
  • begins 12-14hr, peaks in 48-72hr
    • ​restless sleep
  • begins in 12hr, peaks 48-72 hr
    • dilated pupils, anorexia, goosebumps, irritability, tremor
  • at peak
    • insomnia, violent yawning, weakness, GI upset, chills, flushing, muscle spasm, ejaculation, abd pain
148
Q

Blood Ethanol Concentration

15-50

50-100

100-200

200-300

300-400

>500

A
  • 15-50 = 0.015-0.05:
    • modest impairment to drive
  • 50-100 = 0.05-0.1:
    • impaired motor function, sedation, euphoria
  • 100-200 = 0.1-0.2:
    • emotional instability, slurred speech, ataxia, analgesia
  • 200-300 = 0.2-0.3:
    • emesis, stupor
  • 300-400 = 0.3-0.4
    • coma
  • >500 = >0.5
    • respiratory depression, death
149
Q

Moderate Alcohol Dose

High Dose

A
  • moderate = cutaneous vasodilation, ↑ HDL levels, ↓ risk atherosclerosis and CV mortality
  • high = toxic effects, ↓ CO and muscle strength. contributes to cardiomyopathy, muscle weakness, nutritional deficiencies.
150
Q

Alcohol and GI Fnct

A
  • >40% irritates gastric mucosa
  • cause inflammation, erosive gastritis with chronicity
  • potentiates ulcerogenic effects of other drugs
151
Q

Alcohol and Liver

A
  • causes ↑ acetyl-CoA, ↓ NAD+
  • leads to fatty liver, alcoholic hepatitis, cirrhosis
152
Q

Alcohol and Kidney

A
  • inhibits ADH release, ↑ output of dilute urine
153
Q

Alcohol and Sexual Fnct

A
  • ↑ desire but ↓ physio response and performance
154
Q

Cytosolic Alcohol Dehydrogenase

A
  • converts ethanol to acetaldehyde
  • rate limiting step for ethanol, methanol, ethylene glycol
  • zero order kinetics
  • plateaus at 7-10g/hr (1 drink per hour)
155
Q

Microsomal Ethanol Oxidixing System (MEOS)

A
  • hepatic P450 enzyme
  • chronic alcohol use causes drug interactions
156
Q

Mitochondrial Acetaldehyde Dehydrogenase

A
  • converts acetaldehyde to acetate
157
Q

Ethanol Clinical Uses

A
  • nerve lysis for intractable pain
  • methanol or ethylene glycol poisoning
158
Q

Chronic Alcoholism

A
  • tolerance
  • cross-tolerance with benzo, barbiturates, sedatives
  • physical and psychological dependence
  • can have: peripheral neuropathy (weakness, tingling, numbness) or Wernike encephalopathy, liver toxicity, GI toxicity
  • withdrawal: severe = delirium tremens - tremor, delirium, hallucinations, fever, autonomic instability, seizures
159
Q

Wernike Encephalopathy

A
  • aka wet brain
  • oculomotor paralysis, ataxia, confusion
  • go to coma and death
  • from thiamine deficiency
  • goes to Korsakoff’s psychosis = irreversible memory impairment and loss of contact with reality
160
Q

Fetal Alcohol Syndrome

A
  • from chronic alcohol abuse during pregnancy
  • causes: narrow forehead
    • short paplebral fissures,
    • small nose,
    • small midface,
    • long upper lip with deficient philtrum,
    • microcephaly
    • attentional and intellectual deficits,
    • mental retardation.
161
Q

17beta-estradiol

A
  • most important physio estrogen
  • has aromatic as part of ring
  • eliminated by liver, poor oral availability
  • transdermal patches avoid 1st pass
  • use: post menopausal therapy
162
Q

Estrogen

A
  • works through E2 to stimulate growth and induces P receptors.
  • important for female reproductive tract and breast
  • with P, helps regulate LH and FSH
  • E2 ⇒ ↓LDL, ↑HDL, ↑ triglycerides
  • premenopause side effects: altered skin pigmentation, ↑ risk gallbladder disease, nausea, breast tenderness, headache, ↑ risk VTE, ↑ risk MI and stroke, ↑ risk uterine cancer
  • post menopause additional side effects: ↑ risk breast cancer
163
Q

Progestin

A
  • works thru P to direct functional differentiation during luteal phase and pregnancy
  • prevents development of uterine cancer from unopposed estrogen
  • side effect: acne, ↑ body hair, weight gain, ↑ risk infertility, ↑ risk breast cancer
164
Q

Estrone Sulfate

A
  • conjugated estrogen
  • absorbed in lower GI tract
  • forms estrone after enzymatic hydrolysis
  • use: oral hormone replacement in post-menopausal women
165
Q

Equiline Sulfate

A
  • conjugated estrogen
  • absorbed in lower GI tract
  • forms equiline from enzymatic hydrolysis
  • use: oral hormone replacement in post-menopausal women
166
Q

Estradiol Valerate

A
  • esterified estrogen
  • parenteral injection in oil
  • slowly released, prolonged delivery of 17beta-estradiol (2-4wks)
  • ↓ hepatic effects of estrogens
  • use: hypogonadism
167
Q

Estradiol Cypionate

A
  • esterified estrogen
  • parenteral injection
  • slowly released, prolonged delivery 17beta-estradiol (2-4wks)
  • ↓ hepatic effects estrogen
  • use: hypogonadism
168
Q

Ethinyl Estradiol

A
  • synthetic steroidal estrogen
  • 17-ethinyl substitution ⇒ ↓ 1st pass effect
  • t1/2= 13-27hr
  • use: combo oral contraceptives, hypogonadism
169
Q

Mestranol

A
  • synthetic steroidal estrogen
  • 17-ethinyl substitution ⇒ ↓ 1st pass effect
  • t1/2 = 13-27hr
  • use: combo oral contraceptives
170
Q

Diethylstilbesterol (DES)

A
  • synthetic non-steroidal estrogen
  • potent, prolonged effects
  • relieves bone pain, improves quality of life
  • use: palliative tx of advanced prostate or breast cancer
  • side effect: cardiovascular toxicity (thromboembolism, stroke, fluid retention)
171
Q

Medroxyprogesterone Acetate

A
  • 21-carbon analog of progesterone
  • in DepoProvera
  • anti-aldosterone effects, inhibits LH and FSH release
  • use: hormone replacement in post-menopausal women
172
Q

Megestrol Acetate

A
  • 21-carbon analog of progesterone
  • has anti-aldosterone effects
  • inhibits LH and FSH release
  • use: stimulate appetite and weight gain in AIDS pts
173
Q

Norethindrone

A
  • 19-norestosterone derivative
  • has 17-ethinyl group, good bioavailability
  • makes decidual change in endometrium
  • weak androgen and antiestrogen effects
  • strong inhibitor of LH and FSH release
  • use: combo oral contraceptive, progestin mini-pill, contraceptive patch, emergency post-coital contraceptive
174
Q

Levonorgestrel

A
  • 19-norestosterone derivative
  • has 17-ethinyl group, good bioavailability
  • makes decidual change in endometrium
  • weak androgen and antiestrogen effects
  • strong inhibitor of LH and FSH release
  • use: combo oral contraceptive, progestin mini-pill, contraceptive patch, emergency post-coital contraceptive
175
Q

Norethynodrel

A
  • 19-norestosterone derivative
  • has 17-ethinyl group, good bioavailability
  • makes decidual change in endometrium
  • estrogenic effects
  • strong inhibitor of LH and FSH release
  • use: combo oral contraceptive, progestin mini-pill, contraceptive patch, emergency post-coital contraceptive
176
Q

Desogestrel

A
  • 19-norestosterone derivative
  • has 17-ethinyl group, good bioavailability
  • makes decidual change in endometrium
  • minimal androgenic or estrogenic effects
  • strong inhibitor of LH and FSH release
  • use: combo oral contraceptive, progestin mini-pill, contraceptive patch, emergency post-coital contraceptive
177
Q

Norgestimate

A
  • 19-norestosterone derivative
  • has 17-ethinyl group, good bioavailability
  • makes decidual change in endometrium
  • minimal androgenic or estrogenic effects
  • strong inhibitor of LH and FSH release
  • use: combo oral contraceptive, progestin mini-pill, contraceptive patch, emergency post-coital contraceptive
178
Q

Dienogest

A
  • 19-norestosterone derivative
  • has 17-ethinyl group, good bioavailability
  • makes decidual change in endometrium
  • **antiandrogenic **
  • strong inhibitor of LH and FSH release
  • use: combo oral contraceptive, progestin mini-pill, contraceptive patch, emergency post-coital contraceptive
179
Q

Ulipristal Acetate

A
  • selective progesterone receptor modulator (SPRM)
  • agonist and antagonist effects
  • prevents ovulation and impairs implantation
  • 60% effective when started within 120hr of intercourse
  • use: emergency contraception
  • side effect: headache, nausea, dysmennorhea
180
Q

Testosterone

A
  • poor bioavailability
  • rapid hepatic metabolism
  • T gels and patches for slow transdermal delivery
181
Q

Testosterone Ethanate

A
  • parenteral esterified testosterone
  • converted to testosterone
  • no hepatotoxicity
  • inject every 2-4wks
  • use: induce purbertal changes in hypogonadal boys
182
Q

Testosterone Cypionate

A
  • parenteral esterified testosterone
  • converted to testosterone
  • inject every 2-4wks
  • use: induce pubertal changes in hypogonadal boys
183
Q

Methyl Testosterone

A
  • orally active androgen, anabolic steroid
  • has 17-alkyl substitution
  • dose related hepatotoxicity
184
Q

Fluoxymesterone

A
  • orally active androgen, anabolic steroid
  • has 17-alkyl substitution
  • dose related hepatotoxicity
185
Q

Oxandrolone

A
  • orally active androgen, anabolic steroid
  • has 17-alkyl substitution
  • dose related hepatotoxicity
186
Q

Danazol

A
  • **synthetic steroid derivative **
  • 17-ethinyl group
  • mix of weak androgen, antiestrogen, progestin, glucocorticoid activity
  • inhibits ovarian function, ↓ LH and FSH
  • use: endometriosis, prevent episodes of hereditary angioneurotic edema in pts with complement C1 inhibitor deficiency
187
Q

Combo Oral Contraceptive

A
  • mix of estrogen and 19-nortesterosterone/progestin analog
  • estrogen inhibits ovulation and ↓ fertility
  • progestin enhances estrogen actions and provides normal cycling with estrogen withdrawal
  • use: dysmenorrhea, acne, hirsutism
188
Q

Monphasic Combination Contraceptive

A
  • fixed dose estrogen and progestin
  • 99-100% effective
  • use: dysmenorrhea, acne, hirsutism
189
Q

Biphasic or Triphasic Combo Contraceptive

A
  • varied dose progestin and/or estrogen
  • reduces spotting
  • use: dysmenorrhea, acne, hirsutism
190
Q

Progestin Only Contraceptive

A
  • daily mini pills of progestin (19-nortestosterone derivative)
  • use: when estrogen contraindicated, dysmenorrhea, endometriosis
  • side effect: weight gain, abnormal bleeding, delayed onset fertility, ↑ risk osteoporosis
191
Q

Plan B = Levonorgestrel

A
  • 2-4 oral combo contraceptive pills or progestin alone contraceptive pills
  • 80% effective when begun within 72hrs
  • use: emergency contraception
  • side effect: nausea
192
Q

Preven = Levonorgestrel + EE

A
  • 2-4 oral combo contraceptive pills or progestin alone pills.
  • 80% effective when started within 72 hr
  • use: emergency contraceptive
  • side effect: nausea
193
Q

Flutamide

A
  • androgen receptor (AR) antagonist, non-steroidal
  • markedly ↑ plasma testosterone levels
  • use: prostate cancer therapy with GnRH super-agonist, prevent flare-up of tumor
  • side effect: gynecomastia
194
Q

Bicalutamide

A
  • potent non-steroidal androgen receptor antagonist
  • markedly ↑ plasma testosterone levels
  • less hepatotoxic than flutamide
  • use: prostate cancer therapy with GnRH super-agonist, prevent tumor flare
  • side effect: gynecomastia
195
Q

Spironolactone

A
  • weaker androgen receptor antagonist
  • use: hirsutism
  • side effect: gynecomastia
196
Q

Finasteride

A
  • 5alpha-reductase inhibitor, prevents dihydrotestosterone synthesis
  • use: benign prostatic hypertrophy, male pattern baldness
  • side effect: 2% sexual dysfunction
197
Q

Dihydrotestosterone (DHT)

A
  • androgen derivative
198
Q

Tamoxifen

A
  • non-steroidal estrogen receptor antagonist
  • aka selective estrogen receptor modulators
  • estrogen antagonist on breast
  • estrogen agonist on bone
  • partial estrogen agonist on uterus
  • use: ER-pos breast cancer, prevention of breast cancer in high risk, tx/prevention of osteoporosis, infertility
  • side effect: ↑ risk uterine cancer, ↑ risk VTE
199
Q

Clomiphene

A
  • non-steroidal receptor antagonist
  • aka selective estrogen receptor modulator (SERM)
  • leads to loss of estrogen feedback inhibition on hypothalamic pituitary axis ⇒ ↑ LH and FSH
  • use: infertility in women with impaired release of LH and FSH
  • side effect: ↑ risk VTE
200
Q

Raloxifene

A
  • non-steroidal estrogen receptor antagonist
  • aka selective estrogen receptor modulator (SERM)
  • estrogen antagonist on breast
    • not as strong as tamoxifen
  • estrogen agonist on bone
  • use: tx/prevention breast cancer, osteoporosis, infertility
  • side effect: ↑risk VTE, risk uterine cancer
201
Q

Anastrazole

A
  • aromatase inhibitor (CYP19), non-steroidal
  • don’t convert androgen to estrogen
  • use: breast cancer resistant to tamoxifen
  • side effect: ↑ risk osteoporosis
202
Q

Fluvestrant

A
  • steroidal anti-estrogen = estrogen receptor antagonist
  • impairs estrogen receptor dimerization and retention in nucleus, promote receptor degradation.
  • use: advanced breast cancer resistant to therapy
  • side effect: ↑ risk osteoporosis
203
Q

Mifepristone

A
  • progesterone receptor antagonist
  • blocks glucocorticoid receptors
  • use during 1st 7 wks conception
  • 95% effective in terminating pregnancy
  • use with misprostol to promote expulsion of aborted fetus
  • use: 1st trimester abortion
  • side effect: nausea, vomiting, diarrhea, vaginal bleeding
204
Q

Drospirenone

A
  • anti-mineralcorticoid
  • no androgenic activity
  • less bloating and breast tenderness than 1-nortesterone related progestins
205
Q

Androgen

A
  • such as testosterone
  • stimulates spermatogenesis
  • use: ↑ sperm counts in infertile men, hypogonadism, endometriosis, hereditary angioneurotic edema, cancer therapy
  • side effects: ↑ muscle mass, linear growth, virilizing effects (sex organs, body hair, larynx), closure of epiphyses of long bones, hepatotoxicity, jaundice, acne, ↑ aggression
206
Q

Exemestane

A
  • non-steroidal aromatase inhibitor (CYP19)
  • don’t convert androgens to estrogens
  • use: breast cancer resistant to tamoxifen
  • side effect: ↑ risk VTE

Pharmacology (6 decks)

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