GI DRUGS & Disorders Flashcards
Goal of tx for N/V :
Treat cause but often have to treat symptoms
For N/V, HX is critical. What are 5 essentials in getting a good HX?
- Onset
- PMH
- LMP(females)
- Appearance of emesis (coffee grounds or undigested food)
- recent bowel habits
N/V diagnostics :
X-ray
KUB
Ultrasound
labs: LFT’s
3 types of med can choose for N/V:
- Serotonin 5-HT Receptor antagonists (Zofran, Aloxi)
- Antidopaminergics
- Pepto
Causes of N/V:
- GI DISORDER: GERD, gastritis, constipation, pancreatitis, hepatitis
- Intracerebral / CNS / ⬆️ ICP
- Illness: microbial; H. Pylori
- Medications: Oc’s, antidepressants (like Celexa), antibiotics, chemo
How do the Serotonin 5 HT 3 receptor antagonists work (method of action/MOA)?
Selective 5-Ht3receptor antagonist, binds in both periphery and CNS, Reducing intestinal vagus nerve stimulation.
Not clear if result of CNS or peripheral antagonism.
blocks different NT than Compazine and Phenergan
Pharmacokinetics of 5ht receptor antagonists:
Well absorbed po Enhanced with food SL And IV preps available Metab via liver 70% protein bound Excreted via urine
Name 2 5Ht receptor antagonists:
Zofran and Aloxi
Adverse effects of 5ht receptor antagonists:
Headache Diarrhea Dizziness Constipation ** QTprolongation **
5ht receptor antagonists
Contraindicated in:
Congenital Long QT syndrome
Allergy
Who might not tolerate Zofran due to the side effect of constipation?
A pregnant pt with morning sickness
Pepto bismol (Bismuth Subsalicylate): MOA
= a derivative of salicylic acid, related to aspirin
- works to ⬇️ GI irritation»_space; ⬇ ️nausea
- also antidiarrheal properties / reduces bowel irritation (weak bacteriocidal activities for infectious diarrhea )
- also antacid properties
Pharmacokinetics Pepto Bismol:
Bismuth poorly absorbed but coats ulcers well
Subsalicylate hydrolyzed in stomach to salicylate
Bismuth is excreted in stool ** Can CAUSE BLACK STOOLS!**
Sub salicylate excreted in urine as salicylate
Side effects of PeptoBismol
Nausea
Constipation
Discolored tongue
Black stools
Contraindications for Pepto Bismol
Pediatrics (risk of Reye Syndrome)
Allergy
Phenothiazines: Phenergan, Compazine
MOA
- antidopaminergic / blocks dopamine receptors in brain thus blocking vagus nerve in GI tract
- Phenergan also has antihistamine effect on H 1 receptors
Phenothiazine
Pharmacokinetics / pharmacodynamics
Metabolized by liver
Excreted in stool
Side effects of phenothiazine
Sedation, dizziness, mood changes,constipation
Contraindications of Phenothiazines
Allergy
Severe HTN
BPH
PTS
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Reglan: adverse effects
EPS secondary to dopamine blockade; Elevated prolactin; Galactorrhea; GYNECOMASTIA 😜 Irreversible tardiness dyskinesia
Contraindications in Reglan
Allergy
Concurrent use of drugs capable of causing EPS/TD
Reglan in pregnancy and breastfeeding?
Safe in pregnancy; off-label use in peds; not safe in breast feeding
Other thoughts about Reglan and drug / drug interactions:
Do not use Reglan and Compazine together related to both act on dopamine receptors
Constipation fun facts
= decreased passage of stool, straining, pellet-like stools,unable to pass
Causes can be related to MEDS, MEALS, Or METS (side effects, diet, tumors)
**MIRAlax= first line of TX
Even funner diarrhea facts
= loose liquid stools / defined as 3 + / day Causes: Infections Meds Inflammatory bowel diseases
Antidiarrheals: opioid agonists
(Loperamide /Immodium)
MOA?
Slows intestinal motility through opioid receptor activation, also reduces fecal volume and increases viscosity
Antidiarrheal
Pharmacokinetics
- little po absorption
- significant first pass metab**
- excreted in stool
Adverse effects of antidiarrheals:
Fatigue, dizziness, constipation, nausea
Contraindications for antidiarrheals:
High fever
Bloody diarrhea
Acute UC flare
Age les than 2 yo
Pregnancy and antidiarrheals?
Safe in pregnancy unknown if distributed in breastmilk
Irritable Bowel Syndrome Basics
= functional GI DISORDER; no identifiable causes
»Dx of exclusion, once other GI problems ruled out
3 types:
1. Diarrhea -predominant
2. Constipation-predominant
3. Mixed
Tx» often lifestyle modifications, but some meds available
Meds for Irritable Bowel Syndrome
- Antispasmodics
2. 5HT3 antagonists
Antispasmodics for Irritable Bowel Syndrome:
MOA?
Dicyclomine, hyoscyamine
“Levsin”* can be used in all 3 presentations of IBS!*
-inhibits cholinergic receptors on smooth muscle
-not specific to GI smooth muscle so at high doses have significant anti cholinergic side effects (dry mouth, dry mucous, urinary retention…it is NON selective)
5HT3 antagonist (Alosetron/ Lotronex) MOA?
Modulates enteric nervous system slows GI activity
for diarrhea-predominant IBS ONLY
Inflammatory Bowel Disease:
What two diseases make up this category?
- Crohn’s Disease “TOP TO BOTTOM” can affect any portion of GI TRACT
- Ulcerative Colitis (COLON ONLY)
What is the first line of TX For Inflammatory Bowel Disease?
Steroid
For inflammatory bowel disease, remission maintenance meds =
First line is Aminosalicylates;
immunomodulators becoming popular because may allow pt to avoid a steroid
For Inflammatory Bowel- acute phase med & MOA
GLUCOCORTICOIDS FOR ACUTE FLARE
MOA= anti-inflammatory corticosteroids, reduces inflammation by suppressing migration of polymorphonuclear leukocyte so, decreases prostaglandin synthesis
Glucocorticoid-
Pharmacokinetics
- not well absorbed, Enterocort has max 21% bioavailability
- metabolized extensively in liver
- excreted in urine
Glucocorticoid
Adverse effects
H/A, N/V
Contraindications
Glucocorticoid
Allergy
Glucocorticoids in Irritable Bowel Syndrome:
What phase again?
ACUTE PHASE NOT FOR DISEASE REMISSION
Enterocort- 2 facts:
- High fat meal will delay Enterocort absorption
2. Rectal preparations are the first line for UC FLARE
Inflammatory Bowel Disease:
Maintenance meds are called- and MOA-
sulfasalazine (Azulfidine), mesalamine (ASACOL! ☎️! Your ass is calling!), balsalazide (Cozaal)
MOA is uncertain with these meds but thought to block prostaglandin synthesis,may also inhibit cellular functions of NK Cells, mucosal lymphocytes and macrophages
Aminosalicylates
Pharmacokinetics
Well absorbed in small intestine but not much colonic absorption
Up to 78% protein bound
Metab via liver
Excreted via stool
Aminosalicylates
Adverse effects
nausea, GI upset, H/A, bone marrow suppression ( leukopenia, anemia, thrombocytopenia)
Given that Aminosalicylates can cause bone marrow suppression, how can a provider determine if this is a med-related adverse event?
Establish a timeline- when started drug RX vs. when abnormal labs began
Inflammatory Bowel Disease: meds,MOA
Azathioprine (imuran), 6-MP (purinethol)
MOA: leads to immunocompromise, reduces immune response. Does this by blocking synthesis of purine, which then hinders DNA, RNA, and protein synthesis in fast growing cells like lymphocytes
Purine Analogs: pharmacokinetics
Imuran better absorbed than 6 MP
APPROX 30% protein bound
Metab via liver
Excreted via urine
Purine Analogs: adverse effects
PANCYTOPENIA, infection, hepatotoxicity, pancreatitis
Purine Analogs: contraindications
Pregnancy, breastfeeding;
Active malignancy
Long term use of purine analogs can lead to
Malignancies, especially lymphoma
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness
Contraindications of bulk laxatives:
Bowel obstruction, under age of 6
Pregnancy Category bulk laxatives
B; safe in pregnancy and breastfeeding
Gastric motility agent (Metoclopramide/ Reglan) MOA
Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism
Reglan: pharmacokinetics
Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency
Acid Reflux/ Gastritis:
prevalence, probable causes?
Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses
Descriptions and symptoms of gastritis
Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis
Other contributing factors to gastritis?
Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess
4 Types acid reflux/ gastritis meds
- Antacids
- Carafate
- H2 receptor antagonists
- PPI’s
Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?
These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity
Pharmokinetics/ dynamics of antacids
- Some po absorption; 25-35 % availability
- bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
- carbonate excreted via stool
- aluminum and mag excreted via urine
Pregnancy category of antacids
B, safe for breastfeeding as well
Antacids: adverse effects
N/V, constipation, dependence
Contraindications for taking antacids:
Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones
Carafate: MOA
Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts
Carafate: pharmacokinetics
- very little absorption, so not metabolized
- excreted in stool
Carafate: adverse effects
CONSTIPATION! Gotta love it!
Contraindications for use of Carafate-
Allergy; may use with caution with other meds… Can affect absorption
Carafate pregnancy category:
B ( off label for peds)
H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?
Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).
H2 receptor antagonists: pharmacokinetics
- good po absorption
- metabolized via liver
- excreted in urine
H2 receptor antagonists
Adverse Effects
H/A, dizziness, confusion in elderly,
…..GYNECOMASTIA (for real!?!?!)
H2 receptor antagonists- contraindications
Potent P450 inhibitor!
Use Tagamet with caution in elderly
Pregnancy category for H2 receptor antagonists
B - also safe in peds
Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?
Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion
PPI’s: pharmacokinetics/ dynamics
- PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
- all have fairly good bioavailability, decreased with po intake
- metab in liver / inhibits CYP2C19
- excreted in stool; dose-adjust for hepatic disease
- little renal excretion
PPI’s: adverse effects
H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use
PPI’s: contraindications
Allergy
Types of laxatives:
- Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)
Osmotic laxatives MOA:
Causes water retention in stool; soluble but no absorbable compounds
Pharmacokinetics of osmotic laxatives
NO PO absorption/ excreted in stool unchanged
Adverse effects of osmotic laxatives:
Diarrhea
abdominal complaints
Contraindications of osmotic laxatives:
- Existing electrolyte abnormality
- Age under 2 yo
Osmotic laxatives: great option for long or short term relief?
No adverse effects shown up to 12 months of daily use
Bulk laxatives - MOA?
Pharmacokinetics
Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug
Adverse effects of bulk laxatives:
N/V, abdominal fullness