Laxitives

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Bran
Psyllium (Metamucil)
Methylcellulose (Citrucel)

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Bulk-forming Laxative

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MgSO4 (Epsom salt)
Mg(OH)2 (Milk of Magnesia)

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Saline Laxatives:

Front 3

Lactulose (Chronulac, Cephulac)

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Osmotic Laxatives:

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Bisacodyl (Dulcolax)
Sennosides (Senokot)

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Stimulant Laxatives:

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Docusate Na+ (Colace)
Docusate K+ (Dialose)

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Surfactants:

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2 other laxitives

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Mineral Oil
Tegaserod (Zelnorm)

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Diphenoxylate + atropine (Lomitil)
Loperamide (Imodium)

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Opioids Antidiarrheals

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Sulfasalazine (Azulfidine);
Olsalazine (Dipentum)
Mesalamine (5-ASA, Asacol)

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Rxs for Diarrhea with IBD & AIDS:

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Ondansetron (Zofran)
Granisetron (Kytril)
Dolasetron (Anzemet)
Alosetron (Lotrenox)

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Antiemetics--5-HT3 Antagonists

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Chloropromazine (Thorazine)
Promethazine (generic)
Droperidol (Inapsine)

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Antiemetics
D2 Antagonists:

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-- Diphenhydramine (Benadryl)
-- Meclizine (Antivan)
-- Cyclizine (Marezine)

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Antiemetics: Antihistamines

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Chloropromazine (Thorazine)
Promethazine (generic)
Droperidol (Inapsine)

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D2 Antagonist Antiemetics

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Diphenhydramine (Benadryl)
Meclizine (Antivan)
Cyclizine (Marezine)

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Antihistamine Antiemetics

Front 14

Scopolamine (Transderm-Scop)

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Anticholinergic Antiemetics

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Dronabinol (Marinol)

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Cannbinoid Antiemetics

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Aprepitant (Emend)

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Substance P Receptor Antagonists Antiemetics

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Avoid these if taking tetracycline

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Bulk-Forming Laxatives

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MOA:
Nonabsorbable, indigestible & hydrophilic colloids that absorb water & expand → softening & ↑ bulk→ intestinal distention & promotes peristalsis

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Bulk-Forming Laxatives

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safest & most physiologic laxitives

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Bulk-Forming Laxatives

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Onset of this is 12-24 hrs after administration

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Bulk-Forming Laxatives

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this drug causes ↓ plasma cholesterol. it binds bile acids → ↑ their excretion

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psyllium

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Adverse reactions:
Impaction, intestinal obstruction

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Bulk-Forming Laxatives

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Avoid in obstructive bowel ds or Crohn’s Ds.

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Bulk-Forming Laxatives

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↓ intestinal absorption of many Rx (e.g. salicylates, digoxin)

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Bulk-Forming Laxatives

Front 25

Oral onset of these laxitives is within 4 hrs; Rectal is within 5-30 minutes.

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Saline Laxatives

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MOA of this group of laxitives is osmotic. They trap fluid in lumen → softening & distention → peristalsis
b. Mg 2+ stimulates CCK release → ↑ GI secretion & motility

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Saline Laxatives

Front 27

Clinical Uses of these laxitives is to empty bowel prior to surgery or radiologic or colonscopic procedures

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Saline Laxatives

Front 28

Chronic of these laxitives use can cause HYPERmagnesemia → lethargy, muscle weakness, respiratory paralysis, EKG changes, confusion

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MgSO4 (Epsom salt)
Mg(OH)2 (Milk of Magnesia)

Front 29

Adverse reactions of this laxitive include edema & CHF
and hyperphosphatemia which can lead to hypocalcemia in children

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Na+Phosphate/Biphosphate

Front 30

This laxitive acts osmoticly to trap water, softening stool. It is metabolized to lactate , acetate & formate by colonic bacteria. This decreases luminal pH and ↑ secretion & motility

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Lactulose (Chronulac, Cephulac

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onset of this laxitive is 1-3 days

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Lactulose (Chronulac, Cephulac

Front 32

This drug also tx hepatic encephalopathy: Associated with ↑ plasma NH3→ lethargy, stupor, coma; behavior changes & tremor by ↓ plasma NH 3

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Lactulose

Front 33

Adverse reactions of this laxitive includes
- Fatulence & cramping (20%)
- NVD, loss of fluid & K+

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lactulose

Front 34

1. MOA:
a. Directly stimulates intestinal motility.
b. Inhibits Na+-K+ATPase → fluid/electrolyte accumulation in lumen
c. ↑ synthesis of PGs & cAMP → ↑ fluid/ electrolyte secretion

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Stimulant Laxatives (Irritants)

Front 35

OTC laxative & use to evacuate bowel before diagnostic tests.
Prodrug – activated to desacetyl metabolite
Onset is > 6 hrs

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Bisacodyl (Dulcolax)-

Front 36

Prodrug- reduced by colonic bacteria to active form. Onset~ 6-12 hrs. Chronic use can→ Melanosis Coli –dark pigmentation of colonic mucosa. Benign & reversible, but suggests abuse. Also discolor urine into yellowish brown & red.

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Sennosides (Senokot)

Front 37

Adverse reactions: Abdominal cramps. Chronic misuse → cathartic colon (atony & dilation) - Can be Habit-Forming. Chronic use→ loss of normal bowel functions,electrolyte imbalance, malabsorption & wt. loss.

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Stimulant Laxatives

Front 38

These drugs are anionic surfactants; softening stool → allow water & lipids to penetrate.

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Docusates: Stool softeners

Front 39

These drugs are weakly laxative; onset : 1-3 days

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Docusates: Stool softeners

Front 40

These drugs may ↑ absorption of other Rxs → ↑ Rx toxicity

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Docusates: Stool softeners

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Mixture of liquid hydrocarbons obtained from petroleum--indigestible.
MOA: Penetrates & softens the stool; may ↓ absorption of water.
NOT for routine use because:
↓ absorption of fat-soluble vitamins.
Lipid pneumonia if aspirated.
Seepage of oil past anal sphrincter.
Avoid use with docusates → ↑ absorption → Hepatotoxic

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Mineral Oil

Front 42

A 5-HT4 partial agonist; stimulates 5-HT4 receptors on GI mucosa ↑ peristalsis & intestinal secretions.

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Tegaserod (Zelnorm)

Front 43

Used for chronic constipation & irritable bowel syndrome with constipation

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Tegaserod (Zelnorm)

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SE include diarrhea & headache

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Tegaserod (Zelnorm)

Front 45

These 2 sets of laxitives act by softening feces and usually act within 1-3 days

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Bulk forming laxitives
Surfactant laxitives

Front 46

These laxitives produce soft or semifluid stool and act within 6-8 hours

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Stimulent laxitives

Front 47

These laxitives produce watert evacuation and act within 1-3 hours

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osmotic laxitives

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The _______ are the most effective & prompt acting nonspecific antidiarrheal agents.

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opioids

Front 49

These drugs act by binding opioid receptors on myenteric & submucosal neurons
→ Presynaptic ↓ ACH release → ↓ propulsive, peristaltic contractions
↓ GI secretions→delays passage of bowel contents & ↑ absorption of water → constipation

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Opioids

Front 50

Side effects: Constipation; high doses → CNS effects & ANTI -SLUD

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Opioids

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Contraindications:
Young children
Inflammatory bowel disease – Excessive dilation & fecal retention
→ Toxic Megacolon
→ ↑ perforation

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Opioids

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Kaolin/pectin (Kapectolin) is an ________ laxitive

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Adsorbent

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Used empirically for diarrhea; can interfere w/ Rx absorption

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Adsorbent
(Kaolin/pectin (Kapectolin))

Front 54

MOA: Hydrolyzed by intestinal coliforms to:
a. bismuth oxychloride = bactericidal
b. salicylate = antisecretory & anti-inflammatory

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Bismuth Subsalicylate (PeptoBismol)

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For nonspecific diarrhea & Travelers’ diarrhea.

Caution: Turns tongue & stool black Impaction in infants & elderly

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Bismuth Subsalicylate

Front 56

MOA: Cleaved by colonic bacteria to:
- 5-aminosalicylic acid – inhibits PG synthesis → anti-inflammatory
- sulfapyridine – toxicity

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Sulfasalazine (Azulfidine):

Front 57

Side effects:
- NV, headache, GI upset, malaise
- Allergic rn, including blood dyscrasias, folate deficiency

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Sulfasalazine (Azulfidine):

Front 58

MOA:
- Inhibits secretion of VIP→ ↓ GI secretion
- Inhibits GI motility & gallbladder contract.

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Octreotide (Sandostatin)

Front 59

Used for AIDS-related diarrhea. Diarrhea associated w/ IBD & dumping syndrome.

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Octreotide (Sandostatin)

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May cause NVD, abdominal pain, fat malabsorption w/ gallstones

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Octreotide (Sandostatin)

Front 61

These drugs block stimulation of the CTZ in the area postrema or signals from the GI tract & vestibular system in inner ear to the vomiting center.
Involves 5-HT3, D2, H1 and muscarinic mechanisms

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Antiemetics

Front 62

MOA: Peripheral 5HT3 R blockade on the GI vagal afferents + Central 5HT3 R blockade in CTZ

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5-HT3 Antagonist antiemetics

Front 63

These drugs work best when used with Dexamethasone (Decadron)

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5-HT3 Antagonist antiemetics

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Adverse reactions:
- Headache (10-20%), dizziness, constipation, prolonged QT-interval

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Antiemetic 5-HT3 Antagonists

Front 65

ONLY indicated for women w/ severe diarrhea predominant IBS resistant to other tx.

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Alosetron (Lotrenex)

Front 66

Adverse reactions: Constipation (30%); serious GI side effects (ischemic colitis, etc.) →hospitalization, surgery & death.

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Alosetron

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Metoclopramide (Reglan) is a _______________

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Mixed D2/5HT3 Antagonists

Front 68

MOA:
-Antiemetic-blocks D2 R in CTZ.
- Prokinetic agent that↑ GI motility→ gastric emptying by ↑ ACh release.

Back 68

Metoclopramide (Reglan)

Front 69

Uses: Chemo/radiation-induced emesis & nausea with pregnancy
Prokinetic: Esophageal reflux (GERD)
Impaired gastric emptying after surgery
Facilitate GI intubation

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Metoclopramide

Front 70

Caution: Can prolong Q-T interval --> Torsades

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D2 antagonist Antiemetics

Front 71

Adverse reactions:
Extrapyramidal reactions
Orthostatic hypotension (α- block)
Sedation, drowsiness

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D2 Antagonist Antiemetic

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For NV due to Motion Sickness & vertigo

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Antihistamine antiemetic

Front 73

MOA: ↓ impulse from vestibular apparatus

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Antiemetic Antihistamine

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Best for motion sickness

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Scopolamine (Transderm-Scop)

Front 75

MOA: ↓ impulse conduction from the vestibular system to the emetic center.

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Scopolamine (Transderm-Scop)

Front 76

Anti-SLUD side-effects
sedation, dry mouth, urinary retention, etc.

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Scopolamine (Transderm-Scop)

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Synthetic ∆9-THC; unknown MOA
Scheduled II controlled substance; NOT first-line; for refractory cases
Dysphoria, hallucinations, sedation -- limit use.

Back 77

Dronabinol (Marinol)

Front 78

↑ effects of other Rxs.

Back 78

Benzodiazepines

Front 79

A centrally acting antagonist of Sub P/NK1 receptor; present in vagal afferent fibres innervating the STN and area postrema.

Used in conjunction with 5-HT3 antagonists and a corticosteroid.

Metabolized by hepatic CYP3A4; may interact with dexamethasone & warfarin.

Back 79

Aprepitant (Emend)