H2, PPI, Prokinetics, Anti (emetics, diarrhea's, constipation), IBS Flashcards
GERD stepwise approach ?
Sleep head bed elevated 6-8 inches
Avoid lying down within 3 hours eating
No exercise within 3 hours after eating
No excessive squatting or bending within 3 hours after eating
Body weight
Avoid foods acidic, spicy, excessive fat
Avoid chocolate, peppermint, citric acids
Avoid alcohol, coffee, tea
Overeating
Stop smoking
H2 receptor antagonist Blockers MOA?
Inhibit acid secretion by gastric parietal cells through reverse blockade of histamine at the H2 receptor
H2 examples?
cimetidine (Tagament)
ranitidine (Zantac)
famotidine (Pepcid)
nizatidine (Axid)
H2 pharmacokinetics?
Metabolized Cytochrome P450 enzymes liver
Half-life 3-4 hours
Indications for H2?
GERD
Duodenal and PUD
H2 interactions?
May increase blood alcohol levels
Antacids and anticholinergics may decrease absorption of cimetidine
H2 contraindications?
-
Adverse reactions H2?
Arrhythmias, rash, nausea, vomiting, diarrhea, pancreatitis, granulocyte leukemia, thrombocytopenia, confusion, agitation, depression
H2 education for patients?
Taken after meals and before bed
Avoid drugs that interact or lowered pH affects activity
Smoking affects absorption of histamine blockers
PPI MOA?
Inhibition of the H+/K+/ATPase enzyme at the surface of the parietal cell
PPI examples?
Omeprazole (Prilosec)
Lansoprazole (Prevacid)
Esomeprazole (Nexium)
Pantoprazole (Protonix)
Rabeprazole (Aciphex)
PPI pharmacokinetics?
Metabolizeed by liver
Half-life 2 hours
Rapid absorption
PPI Indications?
GERD Erosive gastritis Hyper-secretory states Zollinger-Ellison syndrome Short term treatment of PUD caused by H.pylori
PPI interactions?
Drugs cytochrome P450 enzymes
Drugs that require higher pH (digoxin, ketoconazole, ampicillin)
PPI adverse reactions?
Long term use may result in increased fracture risk (believed to be result of calcium absorption decrease)
Rash
Abd. pain, N/V diarrhea,
constipation
Flatulence
PPI patient education?
Taken before meals / AM
Avoid taking with antacids
Contraindications for PPIs?
Older adults - cause osteopuritic, and renal disease
Liver and renal disease
PPI Tx for moderate to severe disease: step 1?
Lifestyle modifications and PPIs are used initially
PPI Tx for moderate to severe disease: step 2?
If sxs. do not improve, increase the dose of PPIs
PPI Tx for moderate to severe disease: step 3?
Add H2 blockers or pro kinetic agent
PPI Tx for moderate to severe disease: step 4?
Step down the proton pump inhibitor dose once the initial symptoms have resolved
In addition, the patient may be stepped down to an H2 blocker
Failure of results within a 3-month span requires a gastroenterologist referral
Prokinetic Agents/Gastrointestinal Stimulants MOA?
Stimulate the motility
Does not stimulate gastric, biliary, or pancreatic secretions
Sensitizes tissues to the action of ACH
Metoclopramide (Reglan) pharmokinetics?
Increases resting tone of the LES
Increases tone and amplitude of gastric secretions
Increases peristalsis of the duodenum and jejunum
Accelerated gastric emptying
**settles down nausea, they get a little less GERD; adjunct to GERD , it increases resting tone of the LES*
Indications for Metoclopramide?
Acute and recurrent diabetic gastroparesis
Antiemetic properties
Adjunct therapy migraines
Short term therapy GERD with failure H2 and PPI
Adverse reactions and indications with Metoclopramide?
Restless, drowsiness, mental depression which may include SI
Extrapyramidal symptoms 1 in 500 patients, especially pediatric and older patients
Include Tardive dyskinesia
Hypotension, hypertension, tachycardia
Bowel disturbance, diarrhea
Neutropenia, leukopenia
**if on SSRi’s make sure to use caution with this medication cause it can cause dyskinesia especially if they have had it before with same type of medication or ar eat high risk of getting this side effect then just avoid this drug*
Contraindications to Metoclopramide?
GI hemorrhage, obstruction, perforation
Pheochromocytoma (HTN crisis)
Renal disease
Patients with epilepsy or history of medication induced extrapyramidal
Metoclopramide patient education?
Impair / sedate ( not great for GERD but can be used if failure of H2’s)
Take 30 min before meals
Watch for extrapyramidal symptoms
is Metoclopramide pregnancy safe?
this medicine is safe in pregnancy ( once of the few that is indicated in pregnancy especially for hyperemesis)
Antiemetics facts?
Nausea and vomiting common in the primary care setting
Treatment is often nonpharmacological
Antiemetics MOA?
Provide symptom relief - to get fluids in them - so they stop puking etc.
Prevent fluid and electrolyte disturbances
Consider treatment of cancer patients
Antiemetics: Seritonin blocker agents?
Palonosetron (Aloxi)
Dolasetron (Anzamet)
Antiemetics: Phenoththiazines?
Prochlorperazine (Compazine)
Promethazine (Phenergan)
Antiemetics: 5-HT3 receptor antagnist ?
Ondansetron (Zofran)
- 5HT3’s - was used for hyperemesis in pregnancy until we started seeing birth defects **
Antiemetics pharmacokinetics?
Rapid absorbed (Zofran 100% IV or IM, 50% oral)
Crosses blood brain barrier and placenta
Metabolized liver
Half life:
Promethazine 9-16 hr - longer HF
Prochlorperazine 3-5 hr
Ondansetron 3-6 hr
Adverse reactions with Antiemetics?
Arrhythmias ( Zofran prolonged QT)
Rash
Watch ANC / WBC Compazine
Aplastic anemia
Agitation extrapyramidal systems -
BBW-Dementia related psychosis Compazine - ( watch for it if they are taking serotonin)
Current concern pregnancy Zofran
Phenothiazine’s - Watch small children and older adults - more extrapyramidal sxs in our elderly
Meclizine ( Antivert) subclass?
Subclass: Antihistamines, 1st generation; Nausea/Vomiting; Vertigo/Motion Sickness
Meclizine ( antivert) MOA?
non-selectively antagonizes central and peripheral histamine H1 receptors; antagonizes cholinergic receptors, producing antiemetic effects
Dose of Antivert?
non selectie H1 like benadryl
25 mg PO to start
12.5 mg for PEDS dosing
**only PO , may need to start with another antiemetic if they are N/V, maybe zofran first to relax them and chill them out so the can take the anti vert *
Practical Pharmacology of Antidiarrheal’s are used?
acute versus chronic
Using Antidiarrheal’s pay attention in children and the elderly cause?
Quickly experience dehydration
Usually self limited
Antidiarrheals three main classes of drugs?
Absorbent preparations
Opiates
Anticholinergics
Antidiarrheal’s: absorbent preparations?
Bismuth subsalicylate (Pepto-Bismal, Kaopectate)
Antidiarrheal’s: Opiates?
Diphenoxylate with atropine (Lomotil)
Antidiarrheals: Anticholinergics (IBS)?
Belladonna
Scopalamine
Antidiarrheal’s MOA of absorbent preparations??
Bismuth subsalicylate (Pepto-Bismal, Kaopectate
Absorb moisture in stool without effecting total water loss
Bismuth has anti-secretory and antimicrobial effect
Mucosal protectant - good for erosive bacteria etc
Antidiarrheal’s MOA of opiates?
Diphenoxylate with atropine (Lomotil)
Constipating effect
atropine is anticholinergic slows peristalsis
no used if C.diff cause you do not want to encapsulate it and keep it in
slowing down peristalsis can keep bacteria in the gut an cause more problems
Antidiarrheal’s MOA of Anticholinergics (IBS)
Belladonna, scopolamine
Inhibits peristalsis direct effect on smooth muscle intestinal wall
Diminishes loss fluids and electrolytes
No direct opioid effect
Adverse reactions and interactions with Bismuth?
Pg. 181
ASA
TCL
Coumadin
Tongue and stools gray-black
Adverse reactions and interactions with Lomotil?
CNS
Alcohol
Antihistamines
Opioids
**remember contents of lomotil *
Adverse reactions and interactions with Pectin?
Digitalis will be extremely elevated
yellow vision if dig is to high
in a lot of the anti-diarrheal
Adverse reactions and interactions with Imodium?
CNS
Alcohol
Antihistamines
opioids
Antidiarrheal’s contrindications?
Atropine ( ACH) with glaucoma
Children with Downs hypersensitive to atropine
Atropine can cause urinary retention in older people
Use all _____________ with caution in elderly
antidiarrheal’s
antidiarrheal’s are not used in children under _ years old, under _ they have more supportive care.
2
2
Antidiarrheal’s (cont’d) make sure to use caution in?
Caution in digoxin, cephalosporins, warfarin, heparin, CND depressants
Antidiarrheal’s patient education?
Hand washing
BRAT diet
bananas, rice, apple sauce, toast = bulk agents
Stop Milk / lactose
Causes of constipation?
what drugs? Pg 190
Non-pharmacological intervention for constipation?
Fiber intake
Hydration
Physical activity
Constipation treatment categories?
Bulk forming agents
Emollient stool softeners
Rapidly acting lubricants and laxatives
Constipation: bulk producing laxatives?
Metamucil
Fiberall
FiberCon
Citracel
Constipation: emollient stool softeners?
Mineral oil - slow colonic fecal water absorption
Constipation: rapidly acting lubricants and laxatives?
Magnesium citrate
Constipation: GI stimulant?
Reglan
Constipation: stool softeners?
MiraLax
Lactulose
Ducusate / Colace - degeneration of nerve plexus
Adverse reactions and interactions with constipation meds?
Nausea, vomiting, anal irritation, flatulence
Obstruction
Contraindications with constipation meds?
Signs of appendicitis
Obstruction
Undiagnosed abd pain - work up further
Saline enemas MOA?
draw water into the colon.
Mineral oil enemas MOA?
ease passage of stool, lubricating passage
moisten and soften the hardened stool.
Emollient enemas MOA?
reduces tension in the lumen - allows easier passage
contain substances that softenthe stool.Examples are Microenema and Colace.
Phosphate enemas MOA?
cause contractions of the muscle in the colon
cause contractions in the muscles of the colon.Examples are Fleet phosphosoda
What is one of the most common gastric pathogens?
H. Pylroi
H. Pylori has an important role in the pathogenesis of?
Peptic ulcer disease
Gastric malignancy
Chronic gastritis
Tx of H. Pylori?
Clarithromycin-based triple therapy
Bismuth quadruple therapy
Clarithromycin-based triple therapy contains?
a PPI, clarithromycin, and amoxicillin, or metronidazole for 14 days ( usually 2 times a day )
Bismuth quadruple therapy
contains?
H2 or PPI blocker , bismuth, metronidazole, and tetracycline for 10–14 days to eradicate
used first line in clindamycin resistant area or active infections
Cytoprotective Agents combats ulcers bot by reducing gastric acid but by increasing _______________
mucosal protection
Prostaglandins physiology?
protect the stomach mucosa against injury by increasing gastric mucus secretion
commonly utilized agents: sucralfate, misoprostol
**more of a bandaid over the area , long tern NSAIDs medications nd need to promote healing *
Cytoprotective Agents examples?
Sucralfate
Misoprostol (Cytotec)
Sucralfate is what ?
sucrose sulfate-aluminium complex - alumni covers the ulcer and acts as a barrier - prevent degradation fo the mucosa
Sucralfate MOA?
binds to the ulcer, creating a physical barrier that protects the gastrointestinal tract from stomach acid and prevents the degradation of mucus
promotes bicarbonate production and acts like an acid buffer
**used main in pregs and non- NSAIDS induced treatment more for local treatment take on empty stomach *
Misoprostol (Cytotec) is what?
Prostaglandin analog - mucosa protective quality
Misoprostol (Cytotec) MOA?
use in the prevention of NSAID-induced gastric
inhibiting the secretion of gastric acid decreased intracellular cyclic AMP levels
**used more in NSAID - induced ulcers it is systemically absorbed take on full stomach *
Misoprostol is a prostaglandin _______?
analog
what cytoprotective agent is used to initiate labor in pregnancy?
Misoprostol (Cytotec)
Misoprostol (Cytotec)
uses?
Used to initiate labor in pregnancy
Post-partum bleeding contraction uterus
Used in other countries to produce abortion
Decrease the effects of Warfarin - make sure to watch INR
Misoprostol (Cytotec) pregnancy category?
X
What is IBS?
Chronic functional bowel disorder characterized by abdominal pain and altered bowel habits in the absence of specific and unique organic pathology
IBS treatment drugs?
IBS-A- alternating
IBS-C- constipation dominant
IBS-D- diarrhea
IBS-M- mixed
What are the two drugs used to treat IBS and both agents decrease GI motility?
Anticholinergics
Antispasmodics
**act on smooth muscle *
Anticholinergics example?
Glycopyrrolate (Robinul)
Glycopyrrolate (Robinul)
MOA?
Mechanism of Action antagonizes acetylcholine receptors (anticholinergic)
relieves smooth muscle spasms GI tract
Glycopyrrolate (Robinul)
adverse reactions and interactions?
hypersensitivity rxn
anaphylaxis
intestinal obstruction
seizures
arrhythmias
Glycopyrrolate (Robinul)
contraindications?
neonates (benzyl alcohol-containing INJ forms) “Gasping Syndrome” - causing death in neonates - so avoid in any neonate - significant catastrophic events
glaucoma, angle-closure
obstructive uropathy
GI obstruction
Glycopyrrolate (Robinul)
pregnancy cat?
B
Glycopyrrolate (Robinul)
Lactation and dose?
Lactation: Safety Unknown
Dose - 1 mg TID
Antispasmodics example?
Dicyclomine (Bentyl)
Dicyclomine (Bentyl)
MOA?
antagonizes acetylcholine at muscarinic receptors (anticholinergic)
relaxes smooth muscle
inhibits bradykinin- and histamine-induced spasms
Dicyclomine (Bentyl)
adverse reactions and interactions?
psychosis
Hallucinations, delirium
paralytic ileus
dizziness, blurred vision,
nausea, somnolence
Dicyclomine (Bentyl)
pregnancy cat?
B
Dicyclomine (Bentyl)
lactation and dose?
Lactation: Possibly Unsafe
Dose- 20 mg QID , can be used PO / IM
Anticholinergic/Belladonna Alkaloids
examples?
Atropine sulfate (Donnatal)
atropine, hyoscamine, scopolamine
Anticholinergic/Belladonna Alkaloids MOA?
antagonize acetylcholine at muscarinic receptors
relaxing GI smooth muscle
decreasing GI motility and gastric secretion (anticholinergic)
Sedating effect
affect CNS sites and does cross BBB so it cause sedating affects in patients
Atropine sulfate (Donnatal) interactions and cautions?
urinary hesitancy/retention
blurred vision
palpitations/tachycardia
Mydriasis, cycloplegia, IOP incr. ( glaucoma)
loss of taste
Headache, nervousness,
drowsiness, weakness
atropine sulfate (Donnatal) Pregnancy category?
C
atropine sulfate (Donnatal) lactation and dose?
Lactation: Possibly Unsafe
Dose - 0.4 mgs PO q4-6