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GI M2 > Drugs I > Flashcards

Drugs I Flashcards

1
Q

3 agonists for gastric acid production

A

H, AcH, and gastrin

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2
Q
  • tidine drugs
  • clinical uses (3)
  • pronounced effect on…
  • adverse
A

H2 receptor complete antagonists (only H2 no H1 or H3)

2nd line GERD and most PUD, as effective as PPI for NSAID incued ulcers, OTC preps for dyspepsia

nocturnal acid secretion (H2 dependent)

-crosses placenta/breast milk

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3
Q

Cimetidine

Potency/SFX

A

H2 receptor competitive antagonists (only H2 no H1 or H3)

Weakest potency

slows hepatic metabolism

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4
Q

Ranitidine

Potency/SFX

A

H2 receptor complete antagonists (only H2 no H1 or H3)

Medium potency

slows hepatic metabolism less than cimetidine

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5
Q

Nazitidine

Potency/SFX

A

H2 receptor complete antagonists (only H2 no H1 or H3)

Medium potency

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6
Q

Fanotidine

Potency/SFX

A

H2 receptor complete antagonists (only H2 no H1 or H3)

Strongest potency

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7
Q

Best trx for frequent GERD

A

H2 antagonist 2x daily with PPI

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8
Q
  • prazoles
  • mechanism
  • when do they work

Bioavailability

T1/2

A

Irreversible Proton Pump inhibitors

Prodrugs

suppress fasting and meal acid stimulation=98% acid decrease

Decreased 50% by food-take before

2 hours but irreversible antagonist so works longer

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9
Q

-prazoles vs -tidines

A

better for PUD-heal ulcers faster (esp duo)

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10
Q
  • prazoles

- clincal uses

A

first line GERD and PUD-including H. pylori (triple therapy) and NSAID ulcers

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11
Q

Triple therapy components

Quad therapy components

A

H2 antagonist, PPI, metronidazole,/clarithomyocin

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12
Q
  • prazoles SFX

- 1 special and important association

A

Increase gastric bacterial contents>enteric infection

-worried about C. dif in hospital

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13
Q

when to take -tidines vs -prazoles

A

both before eating (1 hour ideally)

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14
Q

CaCO3, Mg (Oh2)+Al (OH3), Mg(OH)2+CaCO3

A

antacids

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15
Q

Antacids

  • mechanism
  • clinical use
  • SFX
A

Weak bases that react with HCl to reduce gastric acid/peptic activity (pepsin inactivated at pH>4)

primary trx for intermittent heart burn

Bloating depending on base

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16
Q

Dementia causing drugs

A

Bismuth compounds and -prazoles in 75+ yo

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17
Q

Sucralfate

  • Reaction
  • mechanism (2)
  • effects (2)
  • Clinical Use
  • SFX
  • Contraindication
A

Octasulfate+Al(OH)3

Selectively binds and coats necrotic ulcer but requires Acidic conditions in gut to be activated

Acts as barrier to acid, pepsin, and bile
Stimulates synthesis of PGE-stim mucos and HCO3 secretion

Preventing and healing duodenal ulcers

Constipation 2%

Should not be taken with H2 antagonists/PPI/antacids-need acidic environment to work

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18
Q

Colloidal Bismuth compounds

  • mech
  • effects 92)
  • CLinical use
  • SFX
A
  • selectively bind and coat necrotic ulcer
  • acts as barrier to acid/pepsin+direct antimicrobial activity vs H. pylori+binds ENTEROTOXINS
  • trx H. pylori ulcers when combined with Abx (2nd line)

Risk of enteric infection-supressed gastric acid barrier

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19
Q

Misoprostol

  • mech
  • effects (3)
  • CLincal Use
  • SFX (2)
A

PGE1 analog

mucosal protective effects via stim of mucus and HCO3 production+increase BF+reduces H2 induced cAMP production (less acid secretion)

Prevention of NSAID induced ulcers

Dose dependent D+Stimulant effect on uterus (don’t give to childbearing-age women)

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20
Q

Metoclopramide

  • mech
  • effects (4)
  • clincal use and primary use
  • SFX (4)
A

D2-R antagnoist

hasten eso clearance, raises LES, and accelerates gastric emptying+antiemtic properties

Gastric motor failure (post Surgery or DM)
Primarily Antiemetic agent

Extrapyramidal Sx (Parkinsonism/Tardive dyskinesia), anxiety, depression, drowsiness

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21
Q

Lubiprostone

  • mech
  • effects (3)
  • clincal use (2)
  • SFX
  • Contraindication
A

FA drives form PGE1 that activates type 2 Cl channel

Produces Cl rich fluid that softens stool, cinreases motility, and promotes spontaneous BM

Chornic idiopathic constipation and IBS with C

D

Children

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22
Q

Linaclotide

  • mech
  • effects (3)
  • clincal use (2)
  • 1 SFX
  • Contraindication
A

Peptide agonist of guanylate cyclase 2C that activates CFTR

Choloride rich fluid increases motility and promotes spontaneous BM
Reduces Pain via reducing activation of colonic sensory neurons

Chonirc idiopathic constipation and IBS w/ C

D-occasionally so severe need to stop

Children

23
Q

3 Bulk Forming Laxatives

  • Mech
  • effects (2)
  • clinical
  • SFX (2)
A

Psyllium, Methylcellulose, Polycorbophil (only synthetic)

Ingestible hydrophilic colloids that absorb water forming bulky gel in GI tract

Gel distends colon and promotes peristalsis

Intermittent consipation in its not responding to high fiber

bacterial digestion in colon->bloating and flatulence

24
Q

Stool softeners-3

  • 2 mechs
  • effect
  • 2 clinical
  • SFX
A

Docusate, Glycerin suppository, Mineral Oil

Enhance penetration of water/lipids into stool
Retard water absorption from stool

lubricate/soften stool->easier passage

Hospitals-Docusate-prevent constipation/straining
Mineral Oil-treat fecal impaction in child/debilitated

Long term use->impair absorption of ADEK

25
Q

Mg(OH2)

  • effect
  • use (2)
  • SFX
A

Soluble but non absorbable-alter osmolarity of fecal water in colon

Increase stool liquidity due to increase in fecal fluid

trx acute constipation or prevent chornic

@ renal insuf-hyperMg @ prolonged periods

26
Q

Sorbitol

  • effect
  • use (2)
  • SFX
A

Increase stool liquidity due to increase in fecal fluid

trx acute constipation or prevent chornic

Metabolized via bacteria in colon-cramps and farts

27
Q

Lactulose

  • effect
  • use (2)
  • SFX
A

Increase stool liquidity due to increase in fecal fluid

trx acute constipation or prevent chornic

Metabolized via bacteria in colon-cramps and farts

28
Q

Mg Citrate

  • effect
  • use
A

Increase stool liquidity due to increase in fecal fluid

Purgative agent for rapid bowel evacuation

29
Q

Polyethylene Glycol

  • mech
  • effect
  • use
A

Soluble but non absorbable-alter osmolarity of fecal water in colon

Increase stool liquidity due to increase in fecal fluid

Lavage solutions with PEG are used for pre colonoscopy

30
Q

Sodium Phosphate

  • mech
  • effect
  • use
  • SFX
  • contraindications (2)
A

Soluble but non absorbable-alter osmolarity of fecal water in colon

Increase stool liquidity due to increase in fecal fluid

Purgative agent for rapid bowel evacuation

Electrolyte abnLs

Renal insufficiency or cardiac disease

31
Q

Name all 6 osmotic laxatives and primary use and IMPORTANT

A

Mg(OH)2, sorbitol, lactulose, Mg Citrate, NaPO4, PEG

acute C or prevent chornic C

ensure adequate hydration to compensate for fecal fluid loss

32
Q 
Stimulant laxatives (4)
Mech-2
Effect-2
Use
SFX
A

Cathartics
-Bisacodyl, Aloe Vera, Sena, Cascara Sagrada

stimulate ENS and secretion of colonic electrolytes and fluid

Produce BM-O-6-12 hours, R-.5-2hrs

Its with ANS/ENS impairments

Acute and long term=safe,possible cramping

33
Q

Bisacodyl

-special uses (2)

A

stimulant laxative

Trx for acute and chronic C

used with PEG for pre-colonscopy

34
Q

Diphenoxylate

  • effect
  • 2 mechs
  • use
  • SFX 2
A

Agonists at mu opiod-R in ENS

Increased colonic transit time and fecal water abs

nonspecfic/noninfectious D

CNS opiod effects at high doses (x-BBB)
Potential for dependence with prolonged use

35
Q

Loperamide

  • effect
  • 2 mechs
  • use
  • SFX 2
A

Agonists at mu opiod-R in ENS

Increased colonic transit time and fecal water abs

nonspecfic/noninfectious D

Mild cramping, no cross BBB so no CNS toe

36
Q

Trx for IBS with predominant D (2)

A

Opioid agonists-Loperamide and Diphenoxylate

37
Q

Trx for IBS with predominant C (3,2,2)

A

Osmotic Laxatives-Mg(OH)2, sorbitol, PEG

Bulk forming laxatives-Psyllium and Methylcellulose

Cl Channel activators-Lubiprostone/Linaclotide

38
Q

Amitriptyline

  • type
  • 2 mech
  • 2 effects
  • use (2)
  • SFX-1 divided by 5
A

Tricyclic antidepressant
SNRI and weak anticholinergic properties

Alter central processing of visceral sensation
Anticholinergic effects-altered GI motility and secretion to reduce stool freq and liquidity

low dose-help IBS with CHRONIC PAIN without altering mode
Anticholinergic effects may help with D

Antichoinergic-Dry mouth, urinary retention, constipation, blurred vision, confused

39
Q

Desipramine

  • type
  • 2 mech
  • 2 effects
  • use (2)
  • SFX-1 divided by 5
A

Tricyclic antidepressant
SNRI and weak anticholinergic properties

Alter central processing of visceral sensation
Anticholinergic effects-altered GI motility and secretion to reduce stool freq and liquidity

low dose-help IBS with CHRONIC PAIN without altering mode
Anticholinergic effects may help with D

Antichoinergic-Dry mouth, urinary retention, constipation, blurred vision, confused

40
Q

3 drugs to trx IBS with pain

A

amitriptyline, desipramine, alosetron

41
Q

Alosetron

  • mech
  • effect (3)
  • use
  • 3SFX
A

Antagonists at 5-HT3-R

Inhibits unpleasant visceral afferent pain, bloating, and N

WOMEN-severe D predominant IBS who are refractory

1/3 constipation (severe enough to discontinue-10%)
Rare-severe constipation req hospitaliation
-possibly an progress to ischemic colitis

42
Q

5 aminosalicylates (4)

  • 2 mech
  • effect
  • 2use
  • SFX (3 important I think)
A

-sala-drugs-mesalamine, sulfasalazine, olsalazine, balsalazide

inhibit inflammation via COX and lipoxygenase paths

work topically in diseased GI mucosa

1st line for Mild/mod UC
1st line for mild to mod disease involving colon or distal ileum

sulfasalazine has higher incidence of systemic effects
GI, BM suppression, Arthylgias and Myalgias

43
Q

4 Glucocorts used to trx IBD

  • mech
  • effect
  • use (3)
  • SFX
A

Prednisone, Prednisolone, hydrocortisone, Budesonide

Act through GC receptors/DNA to regulate transcription of numerous genes

Generalized antiinflammatory

Mod to severe IBD

  • rectal administration preferred if rectum/sigmoid IBD
  • Not useful for maintaining disease remission

Protein catabolism (cushing), Fat resdistribtuon, hyperglycemia

44
Q

Prednisone+1

  • mech
  • effect
  • special
A

Prednisolone

Act through GC receptors/DNA to regulate transcription of numerous genes

Generalized antiinflammatory

Most common oral agents

45
Q

Hydrocortisone

  • mech
  • effect
  • special
A

Act through GC receptors/DNA to regulate transcription of numerous genes

Generalized antiinflammatory

enemas/foam/suppostories-maximize colonic and rectal effects while minimizing systemic absorption

46
Q

Budesonide

  • mech
  • effect
  • special
  • –special use
A

Act through GC receptors/DNA to regulate transcription of numerous genes

Generalized antiinflammatory

Entocort-controll-ed release oral version that hits only distal ileum and colon b/c 10% bioavailibity

Trx mild/mod CD involving ileum and prox colon

47
Q

Azathiopurine+1

  • mech
  • effect
  • use
  • SFX (5)
A

6MP

Inhibit purine biosyn

immunosup through inhibition of lymphoid cell prolferation

1st line-Inducation and maintenance of remission in CD

N,V,BM sup, mucositis
HEPATOTOX

48
Q

Methotrexate

  • mech
  • effect
  • use
  • SFX 4
A

Inhibit purine biosyn

immunosup through inhibition of lymphoid cell prolferation

2nd line-Inducation and maintenance of remission in CD

N,V,BM sup, mucositis (no hepatotoxic)

49
Q

Anti-TNF Agents-3

  • mech
  • 2 effects
  • 1 use and 1 special use
  • SFX
A

Inflaximab, adalimumab, certolizumab

monoclonal Ab vs TNF that when bound prevent infalmmatory cytokine binding to receptor

Suppress TH1 immune response and suppresses release of inflammatory cytokines

acute and chronic trx of mod/severe REFRACTORY CD
Inflaximab-refractory UC as well

opportunistic infection from TH1 suppression+many more

50
Q

Natalizumab

  • mech
  • effect
  • use
  • sfx + why
A

anti-integrin agent (alpha 4 subunit)

inhibits integrin fxn in circulating inflammatory cells which stops them from adhering to vascular endothelium

mod/severe CD that failed everything else

multifocal leukoencephaloapthy due to reactivate not latent Human polyoma virus

51
Q

-setron

  • mech
  • effect
  • use (3)
  • efficacy change
A

antagonists at 5-ht3-R

inhibit 5-ht3-R on vagal and spinal afferents and at vomiting center

  • restricted to emesis via vagal stim-post op/chemo
  • —not motion sickness

acute chemo/post op/post radiation related N and V

effiaacy enhanced with corticosteroid and NK1-R Ant

52
Q

-prepitant

  • mech2
  • effect
  • use
  • special
A

antagonists and NK1-R
-Fosaprepitant converted in aprepitant after 30 mins

Central blockade in area psotrema=anti V

used in combo with 5-HT3-R Ant and corticosteroids for prevention of acute and delayed N from highly emetogenic chemo

inhibits metabolism via CYP3A4

53
Q

H1 antihistamines (3)

  • mech
  • Effect-2
  • use
  • sfx (2)
A

Diphenhydramine, dimenhydrinate, Meclizine

antagnoists at H1-R

weakly antiemetic with anticholinergic properties

prevent/trx motion sickness

anticholinergic-Sedation, dry mouth, urinary retention
Meclizine (less anticholnergic prperties and less sedating)

GI M2 (2 decks)

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