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Pharma > G.I. Drugs > Flashcards

G.I. Drugs Flashcards

1
Q

Esomeprazole

A

Proton Pump Inhibitor

Covalently modify the active site of H/K ATPase (IRREVERSIBLE)

Relies on slow turnover of ATPase at apical surface

First line treatment for hyperacidity (80-95% reduction)

Prodrug that requires acid activation to react with proton pump

Acid Labile

Must be absorbed into the blood and can only do so at higher pH so must be administered as:
- Gelatin Capsule

Lowers acid secretions by 90%

  • Used for GERD
  • Used for erosive esophagitis
  • Used for peptic ulcers
  • Zollinger- Ellison syndrome (secretion of gastrin from tumors in pancreas and intestine)
  • NSAID induced gastric ulcers
  • H. pylori treatment

NOT ALL Proton Pumps active at one time, so treatment requires 2-5 DAYS

Clearance through liver

Adverse Reaction

  • Hepatic Failure reduces clearance
  • Nausea, Abd pain, constipation, flatulence, diarrhea
  • Rare: Myopathy arthralgia, headache, skin rashes
  • Drug interactions through CYP activity
    • Increase serum warfarin concentration
    • Decrease activation of clopidogrel

Rebound hypergastrinemia and gastritis can occur (excessive gastrin secretion)

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2
Q

lansoprazole

A

Proton Pump Inhibitor

Covalently modify the active site of H/K ATPase (IRREVERSIBLE)

Relies on slow turnover of ATPase at apical surface

First line treatment for hyperacidity (80-95% reduction)

Prodrug that requires acid activation to react with proton pump

Acid Labile

Must be absorbed into the blood and can only do so at higher pH so must be administered as:
- Gelatin Capsule

Lowers acid secretions by 90%

  • Used for GERD
  • Used for erosive esophagitis
  • Used for peptic ulcers
  • Zollinger- Ellison syndrome (secretion of gastrin from tumors in pancreas and intestine)
  • NSAID induced gastric ulcers
  • H. pylori treatment

NOT ALL Proton Pumps active at one time, so treatment requires 2-5 DAYS

Clearance through liver

Adverse Reaction

  • Hepatic Failure reduces clearance
  • Nausea, Abd pain, constipation, flatulence, diarrhea
  • Rare: Myopathy arthralgia, headache, skin rashes
  • Drug interactions through CYP activity
    • Increase serum warfarin concentration
    • Decrease activation of clopidogrel

Rebound hypergastrinemia and gastritis can occur (excessive gastrin secretion)

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3
Q

Omeprazole

A

Proton Pump Inhibitor

Covalently modify the active site of H/K ATPase (IRREVERSIBLE)

Relies on slow turnover of ATPase at apical surface

First line treatment for hyperacidity (80-95% reduction)

Prodrug that requires acid activation to react with proton pump

Acid Labile

Must be absorbed into the blood and can only do so at higher pH so must be administered as:

  • Gelatin Capsule
  • Enteric coated capsule
  • Mixed with bicarbonate

Lowers acid secretions by 90%

  • Used for GERD
  • Used for erosive esophagitis
  • Used for peptic ulcers
  • Zollinger- Ellison syndrome (secretion of gastrin from tumors in pancreas and intestine)
  • NSAID induced gastric ulcers
  • H. pylori treatment

NOT ALL Proton Pumps active at one time, so treatment requires 2-5 DAYS

Clearance through liver

Adverse Reaction

  • Hepatic Failure reduces clearance
  • Nausea, Abd pain, constipation, flatulence, diarrhea
  • Rare: Myopathy arthralgia, headache, skin rashes
  • Drug interactions through CYP activity
    • Increase serum warfarin concentration
    • Decrease activation of clopidogrel

Rebound hypergastrinemia and gastritis can occur (excessive gastrin secretion)

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4
Q

cimetidine

A

H2 Receptor Antagonist

4-5hr duration

Adverse Reaction:

  • <3% incidence of effect overall
  • Minor effect: diarrhea, headache, drowsiness, fatigue, muscle pain
  • Parenteral administration in the elderly (hallucinations, delirium, confusion, slurred speech, and headaches)

Long term effect decrease testosterone binding to androgen receptor and hydroxylation

Decrease pepsin and intrinsic factor output

Tolerance can develop in 3 days

Rebound is a problem if discontinued suddenly

Block base level of acid secretion from ECL cells

Useful for nocturnal acid secretion, important for duodenal ulcers (4-8wk)

Use for Zollinger-Ellison syndrome (excessive gastrin secretion)

Not as effective as proton pump inhibitor but decreases acid secretion by 70% for 24 hours with daily dosing

Excretion is renal via organic cation system

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5
Q

famotidine

A

H2 Receptor Antagonist

10-12hr duration

Adverse Reaction:

  • <3% incidence of effect overall
  • Minor effect: diarrhea, headache, drowsiness, fatigue, muscle pain
  • Parenteral administration in the elderly (hallucinations, delirium, confusion, slurred speech, and headaches)

Long term effect decrease testosterone binding to androgen receptor and hydroxylation

Decrease pepsin and intrinsic factor output

Tolerance can develop in 3 days

Rebound is a problem if discontinued suddenly

Block base level of acid secretion from ECL cells

Useful for nocturnal acid secretion, important for duodenal ulcers (4-8wk)

Use for Zollinger-Ellison syndrome (excessive gastrin secretion)

Not as effective as proton pump inhibitor but decreases acid secretion by 70% for 24 hours with daily dosing

Excretion is renal via organic cation system

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6
Q

ranitidine

A

H2 Receptor Antagonist

6-8hr duration

Adverse Reaction:

  • <3% incidence of effect overall
  • Minor effect: diarrhea, headache, drowsiness, fatigue, muscle pain
  • Parenteral administration in the elderly (hallucinations, delirium, confusion, slurred speech, and headaches)

Long term effect decrease testosterone binding to androgen receptor and hydroxylation

Decrease pepsin and intrinsic factor output

Tolerance can develop in 3 days

Rebound is a problem if discontinued suddenly

Block base level of acid secretion from ECL cells

Useful for nocturnal acid secretion, important for duodenal ulcers (4-8wk)

Use for Zollinger-Ellison syndrome (excessive gastrin secretion)

Not as effective as proton pump inhibitor but decreases acid secretion by 70% for 24 hours with daily dosing

Excretion is renal via organic cation system

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7
Q

sucralfate

A

Misc. Drug

Octasulfate of sucrose with Al(OH)3

Forms sticky neutral pH polymer coating that swells and covers the epithelium

Used for STRESS ULCERS (sticks better to duodenal)

Acid activated, take before food and avoid antacids/PPIs

Common Side Effect is constipation (2%)

Block absorption of other drugs through the stomach

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8
Q

aluminum hydroxide

A

Neutralizing Antacids

Neutralizes pH of gastric contents

Largely supplanted by proton pump inhibitors

Used over the counter

Al is slower than Mg

Adverse effect:

  • Rebound acid secretion
  • AlOH- Constipation, nausea, possible phosphate loss, binds tetracyclines

Use in combo for H. Pylori Treatment

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9
Q

calcium carbonate

A

Neutralizing Antacids

Neutralize pH of gastric contents

Largely supplanted by PPIs

Widely used over the counter

Largely supplanted by proton pump inhibitors

Used over the counter

Adverse effect:
- Rebound acid secretion

Use in combo for H. Pylori Treatment

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10
Q

magnesium hydroxide

A

Antacids

Neutralize pH of gastric contents

Fast Acting

Stimulates gastric emptying and motility while

Largely supplanted by PPIs

Widely used over the counter

Largely supplanted by proton pump inhibitors

Used over the counter

Adverse effect:
- Rebound acid secretion

Use in combo for H. Pylori Treatment

ALSO A LAXATIVE

  • Mg stimulates CCK receptors and increases motility
  • Avoid in individuals with
  • Cardiac Disease
  • Renal Insufficiency
  • Diuretic Use
  • Electrolyte abnormalities
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11
Q

magnesium trisilicate

A

Antacids

Neutralize pH of gastric contents

Fast Acting

Stimulates gastric emptying and motility while

Largely supplanted by PPIs

Widely used over the counter

Largely supplanted by proton pump inhibitors

Used over the counter

Adverse effect:
- Rebound acid secretion

Use in combo for H. Pylori Treatment

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12
Q

misoprostol

A

Prostaglandin Analogs

Synthetic analogue of PGE1

Reduce 80-90% of basal or food-induced acid production

Short acting, up to 3 hr

Used to prevent NSAID-induced injury (but PPIs and H2-antagonists more commonly used for this purpose)

Adverse Effect:

  • Diarrhea (30%)
  • Exacerbate inflammatory bowel disease
  • Increase Uterine Contractions during Pregnancy
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13
Q

pirenzepine

A

Muscarinic Antagonist

Selective for M1 receptor

Blocks neurotransmission in Intramural Ganglia resulting in less stimulation of parietal cells and ECL cells

Reduce basal acid (40-50%)

Significant anticholinergic side effects

Rarely Used

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14
Q

bethanechol

A

Prokinetic Agent

Activating M receptors do not activate coordinated motility

Selectively activate M2 and M3 receptors

Side Effects:

  • Bradycardia
  • Flushing
  • Diarrhea
  • Cramps
  • Salivation
  • Blurred vision
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15
Q

cisapride

A

Prokinetic Agent

5-HT4 receptor agonist and adenylate cyclase stimulant

Used for GERD

Stimulate intrinsic sensory neurons

Adverse reaction:
- Fatal Cardiac arrythmia

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16
Q

erythromycin

A

Imitates Motilin

Increases motility

Macrolide Antibiotic

Cause gastric dumping, moves bezoars and improves gastric emptying with ILEUS, SCLERODERMA, and PSEUDOOBSTRUCTIONS

Fast dumps can be painful so not recommended for chronic use

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17
Q

metoclopramide

A

Prokinetic Agent

Dopamine receptor antagonist
- DA decreases ACh release so drugs enhance normal ACh response

Long used, increases lower esophageal sphincter tone and upper GI motility

Relieves GERD symptoms but does not promote healing

Used for nausea and vomiting in dysmotility syndromes

Used as AntiEMETIC also
- PREFERRED AGENT IN CHEMOTHERAPY INDUCED NAUSEA

Also a laxative

Adverse effect:
- Extrapyramidal side effects, dystonias, Parkinson’s like symptoms, Tardive dyskenesia with chronic use

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18
Q

neostigmine

A

Prokinetic Agent

AChE inhibitor (not insecticide)
- Commonly used to counter ILEUS
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19
Q

Tegaserod

A

Prokinetic Agent

Partial 5-HT agonist in gut for FEMALES with Irritable bowel syndrome

Can improve lower bowel motility in cases with chronic constipation and bloating

Adverse Reaction:
- Fatal Cardiac Arrhythmias

USED FOR CONSTIPATION PREDOMINANT IBS

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20
Q

magnesium citrate

A

Laxative

Osmotic Laxative

  • Non absorbable agent
  • Cause water retention

Techically a cathartic causing bowel emptying with watery stool, but act as laxative at lower dosages

Mg Stimulates CCK receptors and Increases motility

Avoid in individuals with renal insufficiency
Cardiac Disease
Electrolyte abnormalities
Diuretic Use

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21
Q

magnesium sulfate

A

Laxative

Osmotic Laxative

  • Non absorbable agent
  • Cause water retention

Techically a cathartic causing bowel emptying with watery stool, but act as laxative at lower dosages

Mg Stimulates CCK receptors and Increases motility

Avoid in individuals with renal insufficiency
Cardiac Disease
Electrolyte abnormalities
Diuretic Use

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22
Q

polyethylene glycol

A

Laxative

Osmotic Laxative

Non-absorbable agent

Cause water retention

Cathartics that cause bowel emptying with watery stool, but act as laxatives at lower dosages

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23
Q

lactulose

A

Laxative

Osmotic Laxative

Sugar

Used for constipation associated with opioid use and vincristine

Bacterial fermentation of lactulose also drops luminal pH and traps NH4 (increased in colons of patients suffering from hepatic disease)

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24
Q

mannitol

A

Osmotic Laxative

Sugar

Used for constipation associated with opioid use and vincristine

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25
Q

sorbitol

A

Osmotic Laxative

Sugar

Used for constipation associated with opioid use and vincristine

26
Q

docusate

A

Stool wetting agent

Surfactants that allow mixing of fatty substances and water in stool.

Effective as stool softeners

Do not increase frequency of defecation

27
Q

bisacodyl

A

Irritant laxative

Used orally or rectally

Generally safe but overdose causes catharsis

Warn patients not to chew tablets or mix with milk or antacids to ensure that the tablet reaches the site of action in the small intestine and avoid gastric irritation

28
Q

castor oil

A

Irritant laxative

Smooth muscle stimulant

Used as cathartic

  • laxative
  • induce labor
  • Purge
  • Neolid

Made from castor bean

4 ml will produce laxative effect in 4 hours

16 ml for cathartic effect

29
Q

glycerin

A

Irritant glycerin

Suppository that acts as hydroscopic agent and lubricant

Increased water retention
Stimulates peristalsis and produces an evacuation reflex

Rectal admin can produce a bowel movement in a hour

30
Q

methylcellulose

A

Bulk-forming laxative

Fiber based

Great for regular soft stools

May exacerbate intestinal obstructions

May absorb other drugs

31
Q

polycarbophil

A

ulk-forming laxative

Fiber based

Great for regular soft stools

May exacerbate intestinal obstructions

May absorb other drugs

32
Q

Psyllium

A

ulk-forming laxative

Fiber based

Great for regular soft stools

May exacerbate intestinal obstructions

May absorb other drugs

33
Q

bismuth subsalicylate

A

Antidiarrheal

Also used in H. pylori treatment

Suspended in magnesium aluminum silicate and oil of wintergreen

Naturally pink

Salicylate is released in stomach and absorbed systemically

34
Q

diphenoxylate

A

Antidiarrheal

Opioid

Piperidine derivative

Can have CNS effects

Packaged with atropine to discourage abuse

35
Q

loperamide

A

Antidiarrheal

Opioid

mu opioid receptor agonist that stops bowel motility

40-50X more potent than morphine

Does not enter CNS

36
Q

octreotide

A

Antidiarrheal Agent

Same as Somatostatin

Parenteral octapeptide

Used to combat secretory diarrhea of hormone secreting tumors

Used for post-surgical gastric dumping syndrome

Diarrhea associated with chemotherapy

Used to rest the pancreas in pancreatitis

Adverse reactions:

  • Nausea
  • Bloating
  • injection site pain

Long term therapy may result in gallstones

37
Q

chlorpromazine

A

Antiemetic Agent

Dopamine Receptor Antagonist

Phenothiazines

Originally used as antipsychotics

Preferred use is anti-nauseants and anti-emetic

Mechanism targets D2 receptors in CTZ and H1 receptors

Good for motion sickness

Can be useful in chemotherapy induced nausea

38
Q

cyclizine

A

Antiemetic

Antihistamine

Also has anticholinergic effects used in patients with abdominal cancer

H1 receptor antagonist

Used for post-operative emesis

Act primarily on brainstem and vestibular apparatus

39
Q

diphenhydramine

A

Antiemetic

Antihistamine

Also has anticholinergic effects used in patients with abdominal cancer

H1 receptor antagonist

Used for post-operative emesis

Act primarily on brainstem and vestibular apparatus

40
Q

dimenhydrinate

A

Antiemetic

Antihistamine

Dosed from of diphenhydramine

Also has anticholinergic effects used in patients with abdominal cancer

H1 receptor antagonist

Used for post-operative emesis

Act primarily on brainstem and vestibular apparatus

41
Q

dolasetron

A

Antiemetic

5-HT3 antagonist

Used in chemotherapy and antiemesis

Oral or parenteral

Excretion through liver

42
Q

hydroxyzine

A

Antiemetic

Antihistamine

Also has anticholinergic effects used in patients with abdominal cancer

H1 receptor antagonist

Used for post-operative emesis

Act primarily on brainstem and vestibular apparatus

43
Q

granisetron

A

Antiemetic agent

44
Q

metoclopramide

A

Prokinetic agent

Also a Antiemetic agent and Laxative

Dopamine receptor antagonist

Increases forward motility

Stops emesis, promotes defecation

Preferred agent for chemotherapy induced nausea

45
Q

ondansetron

A

Antiemetic

5HT3 antagonis

5HT3 promotes gut motility

Act centrally at the CTZ and the STN

Act peripherally in small intestine

Most widely used for chemotherapy induced emesis and nausea

3.9 hours

46
Q

palonosetron

A

Antiemetic

Given parenterally only

5HT3 antagonis

5HT3 promotes gut motility

Act centrally at the CTZ and the STN

Act peripherally in small intestine

Most widely used for chemotherapy induced emesis and nausea

Excretion via kidney

40 hours

47
Q

prochlorperazine

A

Antiemetic Agent

Dopamine Receptor Antagonist

Phenothiazines

Originally used as antipsychotics

Preferred use is anti-nauseants and anti-emetic

Mechanism targets D2 receptors in CTZ and H1 receptors

Good for motion sickness

Can be useful in chemotherapy induced nausea

48
Q

promethazine

A

Antiemetic

Antihistamine

Also has anticholinergic effects used in patients with abdominal cancer

H1 receptor antagonist

Used for post-operative emesis

Act primarily on brainstem and vestibular apparatus

49
Q

scopolamine

A

Antiemetic

Anticholinergic

Muscarinc ACh receptor antagonist

Used parenterally but most commonly used as trans-dermal patch

Effective for short or long-term prevention of motion sickness

Used for post-operative emesis

Acts on vestibular apparatus

Not effective for chemotherapy induced nausea, minimal CTZ effects

Adverse effects:

  • Blurred Vision
  • Outburst of uncontrolled behavior when used in presence of pain or anxiety
50
Q

apomorphine

A

Emetic

Acts on CTZ

Given Sub-Q

Largely superceded by activated charcoal

51
Q

ipecac

A

Emetic

Acts on CTZ

Given Sub-Q

Largely superceded by activated charcoal

52
Q

6-mercaptopurine

A

Irritable bowel disease therapy

Thiopurine

Derivative of chemotherapy

Prodrug

Converted to 6-thioguanine to inhibit DNA synthesis

Rapidly proliferating immune cells targetd

Used to maintain remission in both UC and Crohns disease

May help treat fistulas

Effective in 66% of patients but may require weeks/months

Adverse reactions:

  • Pancreatitis
  • Fever
  • Rash
  • Arthralgia
  • N/V are common
53
Q

adalimumab

A

IBD immune modulation

Fully human antibody

used to maintain remission

May gain use in acute UC must be given parenterally

Used for both Crohn’s and UC

Adverse effects:

  • Increased respiratory infections
  • Lack of effective response to TB
54
Q

alosetron

A

IBS treatment

Used for diarrheal predominant IBS

Focuses on motility of gut

55
Q

azathioprine

A

IBD treatment

Thiopurine

Protypical drug

Converted to 6-mercaptopurine which is converted to 6-thioguanine

Inhibits DNA synthesis

Rapidly proliferating immune cells targeted

Maintain remission in UC and Crohn’s disease

May help treat fistulas in Crohns disease

Effective in 66% of patients but may require weeks/months for clinical response

Adverse effects:

  • Pancreatitis
  • Fever
  • Rash
  • Arthralgias

Nausea and vomiting are common

Bone marrow suppression

56
Q

budesonide

A

IBD treatment

Glucocorticoids

Target immune and inflammatory response

Indicated for acute exacerbations and severe disease

200 more potent that hydrocortisone but is only 10% bioavailable and most of that is removed in hepatic first pass

Topical treatment inside the bowel (enema)

Adverse reaction:

  • Immunosuppresion
  • Endocrine disruption
  • Steroid psychoses
  • Other effects typical of steroid treatments
57
Q

infliximab

A

IBD treatment

Anti-TNF antibody

Humanized mouse antibody to TNF-a, interferes with inflammatory response

Used in maintaining remission

May gaine use in UC.

Must be used parenterally

Used for both Crohn’s and UC

Adverse effect:

  • Increased respiratory infections
  • Lack of effective response to TB
58
Q

mesalamine

A

IBD treatment

5-ASA based therapy

5-aminosilicyclic acid

DO not act through COX inhibition

Act though inhibition of TNF-a

Delivered as pro-drug or as enteric coated tablet

Delayed release in the jejunum

UC: treatment for acute flare-ups

Crohns: useful for flare-ups, must select dosage to target part of colon involved

59
Q

olsalazine

A

IBD treatment

5-ASA based therapy

5-aminosilicyclic acid

DO not act through COX inhibition

Act though inhibition of TNF-a

Delivered as pro-drug or as enteric coated tablet

Activated in the colon

UC: treatment for acute flare-ups

Crohns: useful for flare-ups, must select dosage to target part of colon involved

60
Q

prednisone

A

IBD glucocorticoid

Oral is prototype

Target immune and inflammatory response

Indicated for acute exacerbations and severe disease

61
Q

sulfasalazine

A

IBD treatment

5-ASA based therapy

5-aminosilicyclic acid

DO not act through COX inhibition

Act though inhibition of TNF-a

Delivered as pro-drug or as enteric coated tablet

Activated in the colon

UC: treatment for acute flare-ups

Crohns: useful for flare-ups, must select dosage to target part of colon involved

Has most side effect due to sulfa group

Headache
Nausea
Fatigue
Allergic reactions
Contraindicated in pregnancy

Pharma (39 decks)

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