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Clinical Pharmacology I > Exam 3 - GI Part 2 > Flashcards

Exam 3 - GI Part 2 Flashcards

1
Q

Anti-Emetic Drugs

A

Anti-Emetic Drugs

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2
Q

Indications for use of Anti-Emetic Drugs:

A

Severe N/V
Motion sickness
Post-op N/V
N/V post-chemotherapy

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3
Q

Two initiation centers of N/V:

A

Direct stimulants on GI tract

CNS - chemoreceptor trigger zone (CTZ)

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4
Q

What anti-muscarinic is used for motion sickness?

A

Scopolamine

MOA: Blocks Ach from binding to musc. receptors in CTZ.

Patch applied every 3 days, behind ear

ADR: Wash hands! - Can cause midriasis in one eye.

SE: dry mouth, blurred vision, urine retention

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5
Q

What antihistamines are used as anti-emetics?

A

Dimenhydrinate (Dramamine)
Promethazine (Phenergan)

MOA: H1 receptor blockers
Antimuscarinic

Inhibit N/V, cause sedation

Phenergan comes as a suppository! YAY

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6
Q

What are anti-seritonergic medications used to treat N/V?

A

Odansetron (Zofran)
Dolasetron (Anzemet)
Granisetron (Kytril)

Block 5HT-3 receptors (Serotonin) in stomach and brain.

Well tolerated, minus headache, diarrhea, constipation, and QT PROLONGATION, which he ALWAYS asks

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7
Q

What anti-serotinergic drug is used for severe N/V from chemotherapy?

A

Granisetron (Kytril)

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8
Q

How do you treat severe N/V due to pregnancy?

A

Doxylamine (Unison) + B12

If refractory, may use Zofran, but not enough data to know if it has teratogen effects.

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9
Q

Anti-dopaminergic drugs used to treat N/V?

A

Metoclopramide (Reglan)

Phenothiazines - Prochlorperazine (Compazine), Chlorpromazine, Fluphenazine, Haloperidol

Block D2 receptor antagonist in CTZ (dopamine receptors).

Parkinson’s have decreased dopamine levels, these drugs can trigger those symptoms.

Block muscarinic receptors, so might see dizziness, fatigue, seizures.

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10
Q

When you block dopamine receptors, what can occur?

A

Neuroleptic malignant syndrome

High potency dopamine blockers - skeletal muscle will contract and not let go leading to hyper-rigidity of the arm and legs. Produces heat and acid, leads to metabolic acidosis and rhabdomyolysis.

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11
Q

Cannabinoids

A

Dronabinol (Marinol)

Similar to Cannabis. Derivate of delta-9-THC.

Treats N/V associated with chemotherapy when other agents have failed. Stimulates appetite.

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12
Q

What is a substance P antagonist?

A

Aprepitant (Emend)

Antagonist at NK1 substance P receptor

A P receptor is a NT stimulated when you eat spicy foods (pain), stimulates GI tract to cause N/V. Drug inhibits P receptor to stop nausea or vomiting.
Stops N/V from cisplatin and other chemotherapy drugs.

Interacts with CYP3A4!

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13
Q

Treatment for acute and delayed phase of N/V?

First 24hrs?
36-72hrs?

A

Acute phase: 5HT3 receptor antagonist (Zofran)

Delayed phase: Substance P antagonists (Aprepitant)

This is why we give both drugs together.

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14
Q

Prokinetic Drugs

A

Metoclopramide (Reglan)

Stimulate GI tract for those with delayed gastric emptying or gastroporesis.
Common in type 2 diabetics.

Blocks D2 (dopamine) receptors to suppress release of Ach. Increases gastric emptying, GI motility, and increases LES tone to help push food along.

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15
Q

What prokinetic drug was removed from the market due to QT prolongation and CYP3A4 interaction?

A

Cisapride (Propulsid)

Works on 5HT4 and 5HT3

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16
Q

What is used in addition to metoclopramide (Reglan)?

A

Erythromycin; macrolide abx that interacts with motilin receptors on GI tract to increase motility.

Used for gastroporesis and peds with delayed gastric emptying.

Toxicity may cause cramps or impair motility.

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17
Q

Laxatives

A

Laxatives

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18
Q

Laxative Mechanisms:

A

Increase motility
Increase water content of stool
Decrease colonic water and NaCl absorption

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19
Q

Indications for laxatives

A 
Preparation for bowel surgery
Hasten bowel excretion of toxins
Post-op constipation
Minimize straining in CV disease
Relieve constipation
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20
Q

CI laxatives

A

Bowel disease

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21
Q

Long list of side effects for laxatives

A

Acute - nausea, abd cramps, diarrhea

Chronic - Cathartic colon syndrome

Leads to mucosal inflammation, atrophy of outer muscle layers, damage to nerve plexus, malabsorption, dehydration, protein loss, disruption of gut flora — b/c tract was dependent on drug.

Don’t use them chronically :)

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22
Q

Types of Laxatives

A

Stimulants or irritants
Bulk forming - dietary fiber
Stool softeners
Osmotic agents

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23
Q

Stimulant Laxatives

A

Castor oil
Bisacodyl (Dulcolax)
Senna (Senokot)

MOA: increases motility, water, and electrolyte secretion

SE: abd cramps, diarrhea, muscle weakness

Do not use a lot or patient will lose the natural urge to go. As needed basis only.

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24
Q

Bulk forming, non-digestable dietary fiber

A

Can be used safely every day to regulate normal defecation.

Psyllium (Metamucil)
Methylcellulose (Citrucel)

Mix with water before taking.
Increase bulk and water content of stool to increase motility.
Increased volume augments peristalsis.
Binds drugs, flatulence, and cramps.

Can bind to iron, FQ
Cause cramps/flatulence

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25
Stool Softeners
Emulsify stools to make them easier to pass. Good for those with dry, hard stools. Mineral oil Glycerin Docusate sodium (Colace)
26
Osmotic Agents
``` Magnesium Sulfate (Causes diarrhea) Magnesium Hydroxide (Milk of Magnesia) Lactulose Mannitol Polyethylene glycol (MiraLax and GoLYTELY) ``` Increase water content and motility.
27
MiraLax
occasional relief of constipation
28
GoLYTELY
Flush; used for irrigation of drug packets (Cocaine smugglers)
29
Anti-diarrheal agents
Enhance water absorption and decrease GI motility locally. Opioids: - Diphenoxylate (Lotomil) * formulated with atropine * Doesn't cross BBB - Loperamide OTC Common side effect of opioids is that they slow GI tract and cause constipation. SE - constipation, cramping, flatulence, megacolon Not for infectious diarrhea.
30
Why is diphenoxylate formulated with atropine?
Worried IVDA injecting it. Atropine causes IVDA to get sick when injecting it. Abuse deterrent.
31
Megacolon
Blockage from overuse of antidiarrheal agents
32
Drug abusers and Loperamide
Doesn't cross blood-brain barrier due to P-glycoprotein, which prevents absorption. PGP inhibitor like grapefruit juice allows levels to go up of drug. Pt overdosed on cytomegaline and loperamide. by doing this, inhibit PGP for loperamide to be absorbed and cause a high. Torsades induced coma as a result.
33
Bismuth subsalicylate (Pepto-bismol)
Used as an antidiarrheal to inhibit intestinal secretions. Effective in infectious diarrhea. Can turn stools black.
34
Why don't we use Loperamide or Dyphenyloxate in infectious diarrhea?
Want patient to get rid of infection.
35
IBS/IBD
IBS/IBD
36
Crohn's disease vs. Ulcerative Colitis
Crohn's affects entire GI tract; UC affects colon/rectum. *test question*
37
Etiology of Crohn's and UC
Cause unknown, thought to be polygenic on chromosome 12. More prone when on NSAIDs. Smoking decreases UC.
38
UC
Inflamamtion confined to rectum and colon Primary lesion: crypts of lieberkuhn Pseudopolyps, collar-button ulcer
39
Crohn's
Inflammation of GI tract, terminal ileum is most common. Discontinuous inflammation - sip lesions.
40
UC common sxs
Diarrhea, Abd pain, Weight loss Passage of mucus/pus Blood in stool Fever, Tachycardia, Hypotension, increased WBC and ESR
41
Crohn's common sxs
Diarrhea, Abd pain, Weight loss Fatigue Fever Abd mass GI bleeding, perianal/rectal lesions, and increased WBC and ESR
42
What is the purpose of probiotics?
Help restore normal gut flora
43
Are rectal suppositories better for UC or Crohn's?
UC - can get away with rectally administered meds, bc they work locally. Crohn's - systemic tx
44
Aminosalicylates
Sulfasalazine (Azulfidine) -Prodrug - Broken down to form two active components: sulfapyridine and 5-ASA. ``` Mesalamine (5-ASA) Asacol Lialda Pentasa Canasa Rowasa ``` Helps reduced inflammation by inhibiting COX and LOX. ADR: Anorexia, diarrhea, blood dyscrasia (thrombocytopenia)
45
Mesalamine
Less side effects than sulfasalazine; used more frequently
46
Rowasa
Aminosalicylate | Enema can be applied
47
What aminosalicylate is apropriate for UC?
``` Lower rectum and colon Suppository tx (Canasa) ```
48
Why don't suppositories work for Crohn's?
They only affect lower colon and rectum; Crohn's is all over the GI tract. Tablets preferred for Crohn's.
49
Canasa
Rectal suppository; give before bedtime.
50
Benefits of rectal suppossitory?
You bypass first pass effect Good absorption Good for patients who can't take it orally Good, locally, for UC.
51
Enema
Liquid preparation, inserted into rectum Patient lays on side, expel product into colon
52
Drug Therapy options for IBD:
Olsalazine -Dimer of mesalamine (prodrug) Balsalazide -Prodrug that contains 5-ASA and inert carrier molecule
53
Corticosteroids for IBD
Topical (Anusol, Colocort) -for UC Oral (Budenoside, Prednisone) -Chron's IV (Hydrocortisone, Prednisone) AE: Weight gain, diarrhea, nausea, glucose intolerance, osteoperosis, Cushing's
54
Immunosuppressants: Thiopurines
Decrease metabolism of purines and inhibit DNA and RNA synthesis Prevent replication of cells Azathioprine (Imuran) 6-mercaptopurine (Purinethol) AE: Myelosuppression, secondary infections
55
Immunosuppressants: Cyclosporine
Inhibit release of IL-2 limiting T-cell act. AE: nephrotoxic, HTN, hirsutism
56
Immunosuppressants: Methotrexate
Inhibits folic acid AE: stomatitis, myelosuppression, hepatotoxicity
57
Monoclonal antibodies (MAB's): Infliximab
Chimerical mab targeted at TNF-alpha AE: infections, secondary malignancy
58
Monoclonal antibodies (MAB's): Adalimumab
Chimeric mab against TNF-alpha AE: Secondary malignancy Both are produced in bacteria, targeted against specific antigen.
59
Antibiotics
Decrease bacteria Used for fistulas in CD -Cipro, Flagyl
60
Treatment for UC:
Basically, 1. Topical 5-ASA (Mesalamine) 2. Topical/Oral corticosteroid 3. Oral 5-ASA/AZA, 6-MP 4. MAB
61
Treatment for extensive UC:
1. Oral 5-ASA 2. AZA or 6-MP 3. MAB
62
Treatment for CD:
1. Oral 5-ASA + Oral abx + Oral CS 2. IV CS 3. AZA/6-MP 4. MAB
63
Maintenance therapy:
UC: Sulfasalazine, 5-ASA, AZA/6-MP, MAB CD: Same but + Methotrexate and abx NO CS.
64
IBS Non-pharm therapy:
Education, diet (keep dairy, avoid caffeine, dietary triggers, increase fiber) Exercise Psychotherapy
65
Pharm therapy for IBS 3 forms:
IBS-C: - Bulk-forming laxatives - Osmotic laxative - Lubiprostone - TICA/SSRI - 5HT4 partial agonist IBS-D: - Loperamide/Cholestyramine - 5HT3 antagonist IBS-U: - Probiotics - Antispasmodic Small intestine bacterial overgrowth: Rifaximin
66
IBS: Bulk Forming Laxatives
Absorbs water Metamucil, Citrucel, Fiber Lax
67
IBS: Osmotic Laxatives
Increases water retention Milk of Magnesia MiraLax
68
IBS: Chloride channel activator
PGE1 derivative: Increases intestinal secretion secondary to Cl channel act. Lubiprostone (Amitiza)
69
IBS: Tricyclic antidepressants (TCA's)
Effects on muscarinic receptors and serotonin reuptake Amitriptyline Imipramine Not used often
70
IBS: 5HT4 partial agonist
Hard to get, only for women Zelnorm Postmarket warnings about ischemic colitis and diarrhea severe
71
IBS: Anti-diarrheals
Loperamide (Imodium) Cholestyramine (Questran) -For refractory pt's
72
IBS: 5-HT3 Antagonists
Hard to get, only for women Lotronex Restricted use due to ischemic colitis and DEATH! Dangerous AF don't take.
73
IBS: Antispasmodic agents
Decrease GI smooth muscle and motility Anti-Ach Use PRN, due to tachyphylaxis Bentyl, Robinul, Librax, Donnatal
74
IBS: Antibiotics
Bacterial overgrowth contributes to IBS Rifaxamin
75
Tx IBS-C:
1. Bulk laxative 2. Osmotic laxative 3. Lubiprostone
76
Tx IBS-D:
1. Bulk laxative 2. Loperamide/Cholestyramine 3. TCA/SSRI
77
Tx IBS-U:
1. Probiotics 2. TCA/SSRI 3. Antispasmodic
78
Summary IBD:
IBD tx depends on inflammation and severity Aminosalicyclates and CS - Mild/mod dz IV CS, thiopurines, infliximab, adalimumab, cyclosporine, tacrolimus, MTX - Severe IBD

Clinical Pharmacology I (7 decks)

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