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Choi Pharm Flashcards

1
Q

Drugs for Acid-Peptic Dz

A

Agents that reduce intra-gastric acidity:
1. antacids-
NaHCO3, Ca carbonate, Mg hydroxide, Al hydroxide
2. H2 antagonists( -dine)-
cimetidine, ranitidine, nizatidine, famotidine
3. PPI (-zole)-
omeprazole, esomeprazole, lansoprazole, dexlansoprazole, rabeprazole, pantoprazole
Agents that promote mucosal defense:
sucralafate, misoprostol, bismuth compound

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2
Q

Sodium Bicarbonate (baking soda, alka seltzer)

A 
Antacid
Can cause: 
CO2 gas - distention, belching 
metabolic alkalosis
Na - fluid retention
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3
Q

Calcium carbonate (tums)

A 
Antacid
Can Cause:
-CO2 gas - distention, belching
-metabolic alkalosis
-Milk alkali syndrome when taken with milk              (hypercalcemia, renal insufficiency, metabolic alkalosis)
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4
Q

Magnesium hydroxide

A

Antacid
Can Cause:
-osmotic diarrheagiven in combo with aluminum hydroxide (maalox)

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5
Q

Aluminum Hydroxide

A

Antacid
Can Cause:
-constipation
-given in combo with magnesium hydroxide (maalox)

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6
Q

Complications of Antacids

A
  • pts with renal insufficiency should not take long term
  • affects absorption of other medications (should not be taken within 2 hours of tetracyclines, fluoroquinolone, itraconazole, and iron)
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7
Q

H2 antagonists

A

Cimetidine, Ranitidine, Nizatidine, Famotidine
-Best for nocturnal acid secretion

Adverse effects of cimetidine:

  • gynecomastia
  • inhibits CYP1A2, CYP2C9, CYP2D6, and CYP3A4 (negligible with nizatidine and famotidine)
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8
Q

PPI’s

A

Omeprazole, Esomeprazole, Lansoprazole, Dexlansoprazole, Rabeprazole, Pantoprazole

  • prodrugs
  • antagonize meal-stimulated and nocturnal acid secretion
  • very short half-life but long duration of action (covalently bind)
  • Should be taken 1 hour before meal and for a few days for full affect

Adverse effects:

  • decreased B12 levels with prolonged therapy
  • increased hip fractures
  • life threatening hypomagnesemia with secondary hypocalcemia (black box warning)
  • increased risk of both community-acquired respiratory infections and nosocomial pneumonia
  • increased risk of enteric infections
  • potential problems due to increased serum gastrin

*should not be given with clopidogrel

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9
Q

Triple Therapy

A

clarithromycin+metronidazole+PPI

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10
Q

Quadruple Therapy

A

PPI+metronidazole+bismuth cpmd+tetracycline

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11
Q

Sucralafate

A

Promote Mucosal Defense

  • physical barrier and stimulates mucosal PG and HCO3 secretion
  • prevention of stress
  • related bleeding in critically ill pts

Adverse effects:
-Constipation

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12
Q

Misoprostol

A

Promote Mucosal Defense

  • PGE1 analog
  • Reduces histamine-stimulated cAMP production
  • stimulates mucous and HCO3 secretion, enhances mucous blood flow

Clinical Uses:
-NSAID-induced ulcers

Adverse effects:
-diarrhea, cramping, abdominal pain, stimulate uterine contrations (C/I in pregnancy)

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13
Q

Bismuth Compunds (pepto bismol)

A
  • create protective layer, may stimulate PG, mucous, HCO3 secretion
  • direct antimicrobial effects and binds enterotoxins

Clinical:

  • dyspepsia, acute diarrhea, prevention of traveler’s diarrhea
  • quadruple therapy

AE:

  • black stool and darkening of tongue
  • short-term use only, avoid in renal insufficiency
  • prolonged usage may lead to bismuth toxicity resulting in ENCEPHALOPATHY (ataxia, HA, confusion, seizures)-salicylate toxicity
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14
Q

Prokinetic Dugs

A

Cholinomimetics, D2 antagonists, Macrolides

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15
Q

Bethanechol

A

Cholinomimetic

  • stimulates M3
  • used in past for tx of gastroparesis
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16
Q

Neostigmine

A

Cholinomimetic

  • AChE inh.
  • IV–> hosp. pts with acute large bowel distention (Ogilvie’s syndrome)

AE:
-excessive salivaiton, N/V, diarrhea, bradycardia

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17
Q

Metoclopramide (domperidone in other countries)

A

D2 antagonist

  • D2 receptor inhibits cholinergic stimulation
  • tx for diabetic gastroparesis, prevention of vomiting, postpartum lactation stimulation

AE:

  • restlessness, drowsiness, insomnia, anxiety, and agitation
  • EPS
  • Tardive dyskinesia
  • elevated prolactin
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18
Q

Erythromycin (as prokinetic)

A

Stimulates motilin receptors causing a MMC

-IV for gastroparesis, gastric emptying of blood in acute upper GI hemorrhage before endoscopy

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19
Q

Laxatives

A
  • bulk forming
  • stool softeners
  • osmotic laxatives
  • stimulant laxatives
  • Cl channel activator
  • opiod receptor antagonists
  • 5HT4 agonists
  • Guanylate cyclase C agents
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20
Q

Bulk forming laxatives

A

psyllium, methylcellulose, polycarbophil

21
Q

stool surfactant agents

A

ducosate and glycerin suppository

22
Q

osmotic laxatives

A

magnesium hydroxide, sorbitol, lactulose, magnesium citrate, sodium phosphate, balanced polyethylene glycol

23
Q

stimulant laxatives

A

aloe, senna, cascara, bisacodyl

24
Q

Cl channel activator (laxative)

A

lubiprostone

25
Q

opiod receptor antagonists

A
  • methylnaltrexone (tx for opioid induced constipation)

- alvimopan (short term use of postoperative ileus

26
Q

5HT4 agonists

A
  • tegaserod - removed form market
  • cisapride - Long QT
  • prucalopride - in europe
27
Q

Guanylate cyclase C agonists

A

Linaclotide - activates CFTR

28
Q

Anti-diarrheals

A
  • opiod agonists
  • colloidal bismuth compounds
  • bile salt-binding resins
  • octreotide
29
Q

Opioid agonists (anti diarrheal)

A
  • Loperamide - OTC

- Diphenoxylate - Rx (given w/ atropine to discourage abuse)

30
Q

bile salt-binding resins

A

cholestyramine, colestipol, colesevelam

-decrease diarrhea caused by excess fecal bile acids

31
Q

octreotide

A
  • synthetic somatostatin

- inh of endocrine tumor (carcinoid, VIPoma) effects

32
Q

Drugs for IBS

A
  1. Anticholinergics (w/ diarrhea)
    - antispasmodics, infrequently used
    - dicyclomine and hyoscyamine
  2. 5-HT3 antagonists (w/ diarrhea)
    - alosetron
  3. 5-HT4 agonists (w/ constipation)
    - tegaserod (removed from market)
  4. Cl channel activator
    - lubiprostone (w/ predominate constipation)
33
Q

Anti-Emetics

A
  • 5-HT3 antagonists
  • corticosteroids
  • neurokinin R antagonists
  • D2 antagonists
  • H1 antagonists
  • antimuscarinics
  • cannabinoids
34
Q

5-HT3 antagonists (anti emetics)

A

ondansetron, granisetron, dolasetron, palonosetron, tropisertron

Clinical use
-chemo induced N/V, postoperative and post-radiation N/V

AE
- HA, dizziness, constipation, prolongation of QT interval

35
Q

Corticosteroids (as anti-emetic)

A
  • enhances efficacy of 5-HT3 receptor antagonists (-tron’s)

- prevention of acute and delayed N/V in pts receiving moderately to highly emetogenic chemo regimens

36
Q

Aprepitant

A

neurokinin receptor antagonist (anti-emetic)

  • highly selective
  • in combo with 5-HT3 antagonists and coricosteroids for the prevention of acute and delayed N/V from highly emetogenic chem

AE

  • fatigue, dizziness, diarrhea
  • may inhibit the metabolism of other drugs metabolized by the CYP3A4 (docetaxel, paclitaxel, etoposide, ironotecan, imatinib, vinblastine, vincristine)
  • increased plasma level by ketoconazole, ciprofloxacin, clarithromycin, nefazodone, ritonavir, nelfinavir, verapamil, quinidine
  • DECREASES THE INR IN PTS TAKING WARFARIN*
37
Q

phenothiazines (anti emetics)

A

procholorperazine, promethazine, thiethylperazine

  • potent antiemtic and sedative properites
  • inhibition of DA and M receptors
  • antihistamine (sedation)
38
Q

butyrophenones

A

droperidol

  • central DA blockade
  • post-operative n/v, in conjunction with opiates an benzos for sedation for surgical and endoscopic procedures, for neuroleptanalgesia, for induction and maintenance of general anesthesia

AE
- EPS, hypotension, may prolong QT

39
Q

Metoclopramide, trimethobenzamide

A

substituted benzamides (anti emetics)

  • central dopaminergic blockade
  • n/v from highly emtogenic chemo regimen

AE
- EPS

40
Q

H1 antagonists

A
  • weak antiemetic activity
  • useful for prevention or tx of motion sickness

AE

  • sedation, dizziness, confusion, dry mouth, cycloplegia, urinary retention
  • Diphenhydramine, dimenhydrinate - used in conjunction with other antiemetics for tx of emesis due to chemo
  • meclizine- prevention of motion sickness and tx of vertigo
  • scopalamine - tx of motion sickness

C/I w/ glaucoma

41
Q

Benzos (anti emetics)

A

lorazepam, diazepam

-before the initiation of chemo to reduce anticipatory n/v caused by anxiety

42
Q

cannabinoids (anti emetics)

A
  • dronabinol
  • THC; appetite stimulant and antiemetic
  • nabilone
  • THC analog
43
Q

Tx for IBD

A

mild
- 5-aminosalicylates

moderate
- TNF antagonists, oral coricosteroids, Azathioprine, MTX

Severe
- TNF antagonists, IV corticosteriods

-5-ASA = First line for UC
-Mesalamine = first line for Crohn’s
-Corticosteroids
(Budesonide for Crohn’s)
-Immunosuppressive agents
- Azathioprine, mercaptopurine, cyclosporine, methotrexate-
Antimicrobials
- Metronidazole, ciprofloxacin
Biological agents
- Anti-TNF-a antibodies, natalizumab (adhesion/migration)

44
Q

Aminosalicylates

A
  • active component is 5-ASA; work topically not systemically; 80% absorbed in small intestine
  • azo compounds (work better in UC) = sulfasalazine, balsalazide, olsalazine
  • mesalamine compounds (work better in CD) = Pentasa, Asacol, Apriso, Lialda, Rowasa (enema formulations), Canasa (suppository)

AE:

  • slow acetylators have more frequent and more sever adverts effects
  • upset stomach, HA, arthralgias, myalgias, BM suppresion, malaise
  • Gives Jared a small penis
  • Hypersensitivity rxns
  • oligospermia
  • impairs folate absorption and processing
45
Q

Anti TNF Ab’s

A

used in tx of IBD

infliximab, adalimumab (100%), certolizumab

46
Q

Disulfram

A

inhibits ALDH

47
Q

Naltrexone

A

nonselective competitive antagonist of opioid receptors

48
Q

Acamprosate

A

NMDA antagonist and GABA(a) agonist

GI (2 decks)

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