Pharm of Nausea, Vomiting, Diarrhea Flashcards
Antiemetics - categories
5-HT3 Antagonists D2-Receptor Antagonists Antihistamines Antimuscarinics Cannabinoids Neurokinin-REceptor Antagonists Corticosteroids Benzodiazepines
Antiemetics- 5HT3 Antagonists
- Ondansetron
Dolasetron
Granisetron
Palonosetron
Antiemetics- D2-Receptor Antagnoists
Substituted Benzamide:
* Metoclopramide (Reglan)
Phenothiazines:
Chlorpromazine (Thorazin)
* Prochlorperazine (Compazine)
Thiethylperazine
Butyrophenones:
Droperidol
Antiemetics: Antihistamines
Dimenhydrinate (Dramamine) * Diphenhydramine (Benadryl) Hydroxyzine (Vistaril) Meclizine (Antivert) * Promethazine (Phenergan)
Antiemetics- Antimuscarinics
Scopalamine
Antiemetics- Cannabinoids
Dronabinol
Opioids
anti-diarrheal
- Loperamide (Imodium)
- Diphenoxylate (Lomotil)
Difenoxin
Paregoric (generic, camphorated opium tincture, morphine)
Somatostatin Analog
anti-diarrheal
Octreotide acetate
Mucosal Protective Agents
anti-diarrheal agent
Bismuth subsalicylate
Bulk-Forming Laxatives
- Psyllium (Metamucil)
Methylcellulose (Citrucel)
Polycarbophil (FiberCon)
Stool Softeners
- Docusate (Colace)
Glycerin
Mineral Oil
Osmotic Laxatives
- Saline Laxatives
Nondigestible sugars and alcohols - Polyethylene Glycol-Electrolytes
Stimulant Laxatives
Aloe
* Senna (Senokot)
Cascara
* Bisacodyl (Dulcolax)
Opioid Receptor Antagonists
Alvimopan
* Methylnaltrexone (Relistor)
(laxative)
motion sickness pathophys
vestibular system
H1 and M1 receptors
mechanism of action for the agent most appropriate for motion sickness?
H1 receptor agonist
Pick which drug is best for motion sickness:
Dronabinol Fosaprepitant Loperamide Ondansetron Promethazine
Promethazine- H1 receptor antagonist
Dronabinol - CB1 receptor agonist Fosaprepitant- NK1 receptor antagonist Loperamide- Opioid receptor agonist Promethazine- Ondansetron is the 5-HT3 receptor antagonist
When do we use dronabinol?
Chemotherapy– breakthrough or refractory vomiting
When do we use Fosaprepitant
primary agent for chemotherapy
When do we use Loperamide?
slows GI motility
useful for diarrhea
ADRs of promethazine
dizziness
sedation, urinary retention, constipation, confusion, dry mouth; use caution when performing activities where you need to pay attention
When dimenhydrinate is not enough for rough waters induced motion sickness, waht should we take?
scopolamine
ADRs are the anti-muscarinic ones again
pyelonephritis –> nausea
pt also taking Risperidone (mixed seratonin 5-HT2 and dopamine D2 antagonist activity) and Sertraline (SSRI)
What’s the best medication?
don’t want to combine metoclopramide or prochlorperazine and resperidone because they are all D2 antagonists; can –> sedation, drowsiness, and Parkinson’s like issues (dyskinesia, anxiety, etc.: Extrapyramidal reactions)
Ondansetron is a good plan, but be careful of serotonin syndrome (hyperthermia, hypertension, tremor, vomiting, etc.)
How does diphenhydramine work?
H1 receptor antagonis
How does Metoclopramide work?
D2 receptor antagonist
How does ondansetron work?
5HT3 receptor antagonis
How does Prochlorperazine work?
D2 receptor antagonist
Agents for acute CINV
Acute CINV: 5HT3 receptor antagonist NK1 receptor antagonist Corticosteroid Olanzapine
Agents for Delayed CINV
NK1 receptor antagonist
corticosteroid
olanzapine
Agents for anticipatory CINV
benzodiazepines
agents for breakthrough and refractory CINV
an antiemetic from different pharmacological class (prochlorperazine, promethazine, lorazepam, olanzapine, metoclopramide, 5HT3 antagonist, dexamethasone, cannabinoids)
Chemotherapy nausea and vomiting pathophysiology
Chemorecetpor trigger zone (area postrema): D2 receptor, NK1 receptor? (5-HT3 receptor)
Vomiting center (nucleus of tractus solitarius: H1 receptor, M1 receptor, NK1 receptor? (5-HT3 receptor)
GI tract: mechanoreceptors, chemoreceptors, 5-HT3 receptors
CNS areas: cortex, thalamus, hypothalamus, meninges (related to anxiety)
What agent causes QT prolongation?
ondansetron
espectially in combination with a bunch of other anti- drugs.
negative effects of 5-HT3 receptor antagonist?
headache, dizziness, constipation
negative effects of CB1 receptor agonist
euphoria, dysphoria, sedation, hallucinations, dry mouth
side effects of H1 receptor antagonist
dizziness, sedation, confusion, dry mouth, urinary retention
side effects of NK1 receptor antagonist?
fatigue, dizziness, diarrhea
side effects of opioid receptor agonist?
constipation
constipated guy (3 days no poo) on lisinopril, verapamil, acetaminophen, oxycodone.
What do we think?
acute constipation
potential causes: oxycodone (slows GI motility) and verapamil
Best therapy would be bisacodyl; fastest
psyllium will take too long (3-5 days)
docusate won’t help increase GI tract motility; better for prevention
Bisacodyl suppository is what kind of drug?
stimulant laxative
stimulates enteric nervous system
docusate table works how?
stool softener
allows lipids and water to penetrate the stool
methylnaltrexone works how?
opioid antagonist
psyllium powder works how?
bulk forming; absorbs water, distends colon, increases peristalsis
sodium phosphate oral solution works how?
osmotic laxative - results in increased liquid in the stool
time course of drug therapies- what softens stools in 1-3 days?
bulk-forming laxatives
emollients
osmotic laxatives (polyethylene glycol- low dose, lactulose, sorbitol)
time course of drug therapies- what softens stools in 6-12 hours?
bisacodyl (PO, Senna, magnesium sulfate
Time course of drug therapies- what causes watery evacuation in 1-6 horus?
magnesium citrate magnesium hydroxide magnesium sulfate (high dose) sodium phosphates bisacodyl (PR) Polyethylene glycol (bowel prep)
methylnaltrexone MOA, use, CI
MOA: selective inhibition of mu - opioid receptors. Does not cross BBB. Inhibits peripheral receptors without affecting analgesia
Therapeutic use: opioid induced constipation in patients receiving palliative care for advanced illness (with inadequate response to other therapy)
CI: GI obstruction
Very effective but also very expensive
Guy ate raw oysters and has watery, non-bloody diarrhea
viral gastroenteritis
address rehydration- he is still tolerating juice, so glucose/ soups rich in electrolytes
What should we give for the diarrhea?
an oral opioid agonist such as loperamide
docusate therapeutic class?
stool softener
loperamide therapeutic class?
opioid agonist
octreotide therapeutic class?
somatostatin analog
ondansetron therapeutic class?
antiemetic
Senna therapeutic class?
stimulant laxative
what do we reserve octreotide for?
endocrine tumors
Best choices for acute chemotehrapy-induced nasuea and vomiting
(within 24 hours of chemotherapy administration)
COMBINATIONS: 5-HT3 receptor antagonist, NK1 receptor antagonist, dexamethasone, olanzapine, prochlorperazine, metoclopramide, diphenhydramine, lorazepam
Best choices for delayed CINV?
Delayed (more than 24 hours after chemotherapy received)
Best management = prevent acute CINV
Best choice for anticipatory (prior to chemotherapy) CINV?
benzodiazepine night before and morning of chemotherapy
agents for Postoperative Nausea & Vomiting (PONV)
5-HT3 receptor antagonist + dexamethasone
Dimenhydrinate
Prochlorperazine
Metoclopramide
agents for motion sickness
Scopolamine, dimenhydrinate, promethazine
agents for pregnancy
pyridoxine
agents for gastroparesis
metoclopramide
Diarrhea- acute vs severe
Acute
- Self-limiting 3-7 days
- Outpatient, oral rehydration, symptomatic treatment, diet
Severe
- Recover in days with timely management
- Require hospitalization, restore fluid status (IV fluids + electrolytes), empiric antibiotics
treating constipation
Identify cause and treat if appropriate
Increase fluid intake, physical activity, and dietary fiber
- FIBER! Gradually increase intake to 20-25 g/day
Effects in 3-5 days
Prevention
Bulk-forming laxatives & docusate first-line