Term
| What are the four categories of antiemetics to know? |
|
Definition
Phenothiazines
5HT3 Inhibitors
Benzamides
H1 antihistamines |
|
|
Term
| What is the phenothiazine to know? |
|
Definition
|
|
Term
| What are the three 5-HT3 inhibitors to know? What do they all end in? |
|
Definition
Ondansetron*
Granisetron
Dolasetron
-setron |
|
|
Term
| What is the one benzamide to know? |
|
Definition
|
|
Term
| What are the four H1 antihistamines to know? |
|
Definition
Diphenhydramine (Benadryl)*
Meclizine
Hyoscine |
|
|
Term
| Most efficacious class of antiemetic? |
|
Definition
|
|
Term
| What antiemetic is used in patients with unrelenting nausea and vomiting, traveler's diarrhea? |
|
Definition
|
|
Term
| MOA of Phenothiazines (Prochlorperazine)? |
|
Definition
| Blockade of dopamine receptors |
|
|
Term
| Adverse effects of Prochlorperazine? |
|
Definition
Increase in dose improves antiemetic effect, but limited by adverse effects:
sedation
extrapyramidal symptoms |
|
|
Term
| What is the most important 5-HT3 inhibitor to know? |
|
Definition
Ondansetron (Zofran)*
"At a party but feeling queasy? Keep ON DANCing with ONDANSetron!" |
|
|
Term
| MOA of Ondansetron (and the other -setrons)? |
|
Definition
| Central 5-HT3 receptor blockade in the vomiting center and chemoreceptor trigger zone |
|
|
Term
| What are 5-HT3 inhibitors useful for? |
|
Definition
Highly efficacious for prevention of chemotherapy induced emesis (administered prior to chemotherapy)
Also, post-operative nausea & vomiting and radiotherapy-induced nausea & vomiting.
Long duration of action (8-10 hours) |
|
|
Term
| When must dosage be adjusted for the 5-HT3 inhibitors? |
|
Definition
| Dosage adjustment required in hepatic insufficiency |
|
|
Term
|
Definition
The antiemetic action of Metoclopramide* is due to its antagonist activity at D2 receptors in the chemoreceptor trigger zone (CTZ) in the central nervous system (CNS)—this action prevents nausea and vomiting triggered by most stimuli.
Metoclopramide also has gastroprokinetic activity that is mediated by muscarinic activity, D2 receptor antagonist activity and 5-HT4 receptor agonist activity. |
|
|
Term
| Adverse effects of Metoclopramide? |
|
Definition
| Avoid high doses due to extrapyramidal side effects** Knocks out dopamine and induces Parkinsonian effects |
|
|
Term
| What is Metoclopramide useful for? |
|
Definition
Prevention of chemotherapy induced emesis.
Gastroperesis (acts on gastric smooth muscle to accelerate GI emptying).
(Also increased lower esophageal sphincter tone to prevent gastric reflux)***KNOW THIS FOR KRISNA! |
|
|
Term
| How are the H1 antihistamines used to prevent nausea & vomiting? |
|
Definition
| H1 antihistamines are combined with other antiemetics for the prevention of motion sickness. |
|
|
Term
| Adverse effects of H1 antihistamines? |
|
Definition
| Use is limited by sedation, dizziness, confusion, dry mouth, and urinary retention (spillover to anti-muscarinic effects) |
|
|
Term
|
Definition
Bulk-forming laxatives
Stool surfactant agents (softeners)
Osmotic laxatives
Stimulant laxatives |
|
|
Term
What two drugs have huge side effects of constipation and need laxatives for treatment?**
What laxative is used to treat these conditions? |
|
Definition
Morphine
Verapamil
Use Docusate, a stool softener |
|
|
Term
| Name a Bulk-forming laxative? |
|
Definition
| Psyllium (nonabsorbably agents that increase water retention and stool bulk; this distends the bowel and stimulates peristalsis) |
|
|
Term
| Name a Stimulant laxative? |
|
Definition
| Senna (acts directly on intestinal smooth muscle to increase peristalsis) |
|
|
Term
|
Definition
| Docusate (emulsifies stool, softening it and making its passage easier) |
|
|
Term
| Name two Osmotic laxatives? (In FA, but not covered in class much) |
|
Definition
Magnesium citrate*
Lactulose* |
|
|
Term
| What class of drugs are the most effective antidiarrheal agents? |
|
Definition
| Opioids (and their derivatives) |
|
|
Term
| What are the two opioids to know for treating diarrhea? |
|
Definition
Diphenoxylate*
Loperamide* |
|
|
Term
| General MOA of opioid antidiarrheal agents? |
|
Definition
| These are derivatives of an opioid that slow GI peristaltic activity through actions of peripheral opioid receptors. This prolongs the transit time of intestinal contents. |
|
|
Term
| What opioid antidiarrheal has sedative effects? |
|
Definition
Diphenoxylate* - it has peripheral and CNS opiate effects
It is formulated with an antimuscarinic alkaloid (atropine) to reduce abuse - results in patient with anti-muscarinic side effects (blurriness, dry mouth) if abused. |
|
|
Term
| What opioid antidiarrheal has peripheral opiate effects ONLY? |
|
Definition
|
|
Term
| What opiod would be given to a patient with unrelenting diarrhea for the last 72 hours (traveler's diarrhea) who has had little or no sleep?** |
|
Definition
Give Diphenoxylate because it has peripheral & CNS opiate effects**
It has sedative effects so that the patient can sleep. |
|
|
Term
| What antisecretory agent helps in treatment of diarrhea? |
|
Definition
|
|
Term
| What are the four classes of drugs used to treat IBD? |
|
Definition
Aminosalicylates
Corticosteroids
Immunosuppressive antimetabolites
Monoclonal antibodies |
|
|
Term
| Into what two major subtypes is IBD usually divided? |
|
Definition
Ulcerative colitis
Crohn's disease |
|
|
Term
| What is the aminosalicylate used to treat IBD? |
|
Definition
|
|
Term
|
Definition
| Acts as an anti-inflammatory drug (5-aminosalicylic acid) and antibacterial (sulfapyridine). |
|
|
Term
| Where does Sulfasalazine* work better? |
|
Definition
| It works much better against the symptoms of ulcerative colitis thatn Crohn's disease, since Crohn's often involves the small bowel, where the drug is not active. |
|
|
Term
| What are the Mesalamine compounds to know? |
|
Definition
Pentasa (time release)
Asacol
Rowasa |
|
|
Term
| MOA of Mesalamine compounds? |
|
Definition
| These release 5-aminosalicyclic acid to have an anti-inflammatory effect. Also a free radical scavenger or inhibitor of TNF. |
|
|
Term
| What corticosteroids could you use to treat IBD? |
|
Definition
Prednisone/Prednisolone
Methylprednisolone
Hydrocortisone |
|
|
Term
| What are the five immunosuppressants to know for treating IBD? |
|
Definition
Azathioprine*
6-Mercaptopurine*
Methotrexate*
Cyclosporine
Infliximab* |
|
|
Term
| What BRM is used to treat IBD? |
|
Definition
Infliximab*
This is a LAST RESORT for treating IBD (noted for treating Crohn's specifically) |
|
|
Term
|
Definition
| Monoclonal antibody to TNF-alpha. Inhibition of induction of pro-inflammatory cytokines (IL-1, IL-6) |
|
|
Term
| Algorithm for treatment of IBD? |
|
Definition
(Drugs should be used in this order)
Aminosalicylates (Sulfasalazine*)
Antibiotics
Non-systemic steroids
Systemic corticosteroids
Immunosuppressive antimetabolites (Azathioprine*, Methotrexate*, Cyclosporine*)
Monoclonal antibodies (Infliximab*)
Surgery |
|
|
Term
| What four treatments are used to relieve Irritable Bowel Syndrome? |
|
Definition
Make dietary modifications
Antispasmodic agents
Antidiarrheal agents
Antidepressants - TCAs & SSRIs |
|
|
Term
| What two antispasmodic agents are used in IBS? |
|
Definition
Dicyclomine
Scopolomine* (motion sickness drug) |
|
|
Term
| What treatments are used to relieve Gastroesophageal Reflux Disease (GERD)? |
|
Definition
Lifestyle changes
Antacids
H2 antagonists
Proton pump inhibitors (PPIs) |
|
|
Term
| What treatment is most effective in treating GERD? What treatment is least effective? |
|
Definition
| PPIs are most efficacious because it knocks out the hydrogen-potassium pump. Antacids are the least efficacious because they provide symptomatic relief only. |
|
|
Term
| What condition can GERD progress into? |
|
Definition
Peptic ulcer disease
They are lesions in the stomach or duodenum occurring as a result of excessive pepsin and acid activity. |
|
|
Term
| What is Zollinger-Ellison syndrome? |
|
Definition
| Hypersecretion due to a gastrin-secreting tumor |
|
|
Term
| Causative factors in peptic ulcer disease? |
|
Definition
NSAID use (NSAIDS remove the cytoprotective prostaglandins)
Alcohol
Smoking
Stress
H. pylori infection (90% of patients) |
|
|
Term
| What is the most efficacious way to diagnose an H. pylori infection? |
|
Definition
Urea breath test (UBT)
Stool antigen test (second best test) |
|
|
Term
| What are the therapeutic objective to treating peptic ulcers? |
|
Definition
1. Elimination of H. pylori
2. Reduction of gastric acid secretion or acid neutralization
3. Protection of gastric mucosa from further damage |
|
|
Term
| What five categories of drugs are used to treat peptic ulcer disease? |
|
Definition
Antacids
H2 antagonists
Cytoprotective agents
PPIs
Antimicrobial agents |
|
|
Term
| What is the triple therapy to treat peptic ulcer disease? |
|
Definition
| PPI plus two antimicrobial agents |
|
|
Term
|
Definition
Gastric antacids are weak bases that react with gastric HCl to form a salt and water -> increased gastric pH.
Effective SYMPTOMATIC treatment for pain of peptic ulceration. ONLY neutralizes gastric acid that has ALREADY been released; will not prevent gastric acid release and has no cytoprotective effect. |
|
|
Term
| Name the active ingredients of antacids? |
|
Definition
Aluminum hydroxide*
Magnesium hydroxide*
Calcium carbonate* (Rolaids, Tums)
Magnesium carbonate
Sodium bicarbonate |
|
|
Term
| What are the antacids to know? |
|
Definition
Aluminum hydroxide + Magnesium hydroxide (Maalox)
Aluminum hydroxide + Magnesium hydroxide + Simethicone (Mylanta)
Aluminum hydroxide + Magnesium carbonate (Gaviscon)
Calcium carbonate* (Rolaids, Tums) |
|
|
Term
| Adverse effects of antacids? |
|
Definition
Prolonged use -> systemic alkalosis
Diarrhea
May interfere with drug absorption (by making environment alkaline) -> some drugs require acid environment (Digosin, Ketoconazole, Isoniazid)
Increased gastric pH may cause premature dissolution of enteric-coated drugs
Certain drugs may form complexes with aluminum, magnesium, and calcium
Significant reduction in drug bioavailability (Tetracycline, Ciprofloxacillin) |
|
|
Term
| What drug does antacids increase the acidity and toxicity of? |
|
Definition
| Quinidine (a basic drug) -> absorption is INCREASED in an alkaline environment |
|
|
Term
| Four H2 antagonists to know? |
|
Definition
Cimetidine* (Tagamet)
Ranitidine* (Zantac)
Nazatidine* (Axid)
Famotidine* (Pepcid) |
|
|
Term
Most potent H2 antagonist?
Lest potent H2 antagonist? |
|
Definition
|
|
Term
| MOA of H2 antagonists in reducing gastric acid? |
|
Definition
Competitively and reversibly bind H2 receptors on parietal cells
Diminish cytosolic cAMP production and secretion of histamine-stimulated gastric acid
Complete inhibition of gastric acid secretion induced by histamine or gastrin.
Partial inhibition of gastric acid secretion induced by ACh. |
|
|
Term
| Adverse effects of Cimetidine*? |
|
Definition
| Cimetidine is a strong inhibitor of the cytochrome P-450 system and therefore can slow the metabolism of drugs normally broken down through this system. Decreases metabolism of Warfarin, Phonobarbital, Phenytoin, Diazepam, Propranolol |
|
|
Term
| What other adverse effect may Cimetidine* cause? |
|
Definition
| Gynecomastia** and decreased libido (due to its antiandrogenic effects) |
|
|
Term
| What H2 antagonist can be used at a lower dose and doesn't mess with cytochrome P-450 much? |
|
Definition
|
|
Term
| What drug is the most efficacious in treating Peptic ulcer disease? |
|
Definition
|
|
Term
| Three PPIs to know for treating Peptic ulcer disease? |
|
Definition
Omeprazole* (Prilosec)
Lansoprazole* (Prevacid)
Esomeprazole* (Nexium)
-prazole |
|
|
Term
|
Definition
Irreversible inhibitors of H+/K+ ATPase.
Marked suppression of acid secretion by stomach parietal cells. |
|
|
Term
| When should PPIs be taken? |
|
Definition
| Most effective when taken 30 minutes before meals |
|
|
Term
| What two PPIs have dangerous adverse effects? What are the adverse effects? |
|
Definition
| Omeprazole* and Esomeprazole* selectively inhibit cytochrome P-450. can slow the metabolism of drugs normally broken down through this system. Decreases metabolism of Warfarin, Phenytoin, Diazepam. Rabeprazole* and Pantoprazole* have almost no interaction with the cytochrome P-450 system. |
|
|
Term
| What drug acts as a cytoprotective agent? |
|
Definition
| Bismuth* Subsalicylate (Pepto-Bismol) |
|
|
Term
|
Definition
| Bismuct compounds appear to work by selectively binding to an ulcer, coating it and protecting it from acid and pepsin. |
|
|
Term
| What other therapeutic actions are possible? |
|
Definition
| Bismuch compounds may have some antimicrobial activity against H. pylori. |
|
|
Term
| What is the drug regimen for eradication of H. pylori? |
|
Definition
Combination therapy ("triple therapy")
PPI + Metronidazole or Amoxicillin + Clarithromycin |
|
|
Term
| What PPI is used in the combination therapy regimen? |
|
Definition
Omeprazole*
Regimen:
Omeprazole*
Metronidazole or Amoxicillin
Clarithromycin |
|
|
Term
| Why is Clarithromycin used in the combination therapy to eliminate H. pylori? |
|
Definition
| Clarithromycin doesn't interact with the cytochrome P450 system |
|
|
Term
| When would a Bismuth*-based regimen be used to eliminate H. pylori? |
|
Definition
| If there is an open ulcer bed |
|
|
Term
| What is the Bismuth*-based four drug regimen for eliminating H. pylori? |
|
Definition
Omeprazole*
Bismuth* subsalicylate
Metronidazole
Tetracycline |
|
|
Term
| If a patient gets an ulcer from taking NSAIDs, what do you do? |
|
Definition
| If the patient needs to continue taking NSAIDS, put them on a COX-2 inhibitor. If cardiac issues, give a single dose of PPI. |
|
|
Term
| What is the DOC to treat Zollinger-Ellison (ZE) syndrome? |
|
Definition
|
|
