Chapter 4- Gastrointestinal Drugs

Lower Gastrointestinal System

small intestine (duodenum, jejunum, ileum) and the large intestine (cecum, colon, rectum, anus)

Crohn Disease

Affects the ileum and colon
Thickening of the intestinal wall, inflammation, and ulcers, interspersed with normal intestinal mucosa
(regional enteritis)

Ulcerative Colitis

Affects colon and rectum
Causes inflammation and ulcers

Corticosteroid Drugs

Powerful anti-inflammatory effect
Given orally, rectally, as a foam or suppository, or intramuscularly by injection

Betamethasone

Anti Histamine
Celestone

Budesonide

Anti Histamine
Entocort—-Ortikos—-Uceris

Cortisone

Anti Histamine

Hydrocortisone

Anti Histamine
Colocort—-Cortef—-Cortenema

Methylprednisolone

Anti Histamine
Depo-Medrol—-Medrol—-Solu-Medrol

Prednisolone

Anti Histamine
Orapred—-Pediapred

Prednisone

Anti Histamine

Interleukin Inhibitor

Bind to the inflammatory substances of interleukin-12 and interleukin-23 in the intestine and keep them from activating natural killer cells and tumor necrosis factor
Monoclonal antibody drug
-mab is common to generic antibody drugs

Ustekinumab

Interleukin Inhibitor
Stelara

Selective Adhesion-Molecule Inhibitor Drugs

Integrin antagonists or integrin inhibitors
Block integrin, a substance that normally would help leukocytes migrate and adhere to the areas of intestinal inflammation

Natalizumab

Selective Adhesion-Molecule Inhibitor Drugs
Tysabri
ONLY TREATS CROHNS

Vedolizumab

Selective Adhesion-Molecule Inhibitor Drugs
Entyvio
CAN TREAT CROHNS AND ULCERATIVE COLITIS

Tumor Necrosis Factor Blocker Drugs

Bind to and inactivate tumor necrosis factor and prevent it from causing inflammation in the intestinal mucosa and wall

Adalimumab

Tumor Necrosis Factor Blocker Drugs
Hulio—-Humira
CAN TREAT CROHNS AND COLITIS

Certolizumab

Tumor Necrosis Factor Blocker Drugs
Cimzia
ONLY TREATS CROHNS

Golimumab

Tumor Necrosis Factor Blocker Drugs
Simponi
ONLY TREATS ULCERATIVE COLITIS

Infliximab

Tumor Necrosis Factor Blocker Drugs
Avsola—-Inflectra—-Remicade—-Renflexis
CAN TREAT BOTH CROHNS AND COLITIS

5-ASA Drugs

The substance 5-aminosalicylic acid decreases intestinal inflammation by blocking the production of prostaglandin
Given orally and act systematically

Balsalazide

5-ASA Drugs
Colazal

Mesalamine

5-ASA Drugs
Apriso—-Asacol—-Delzicol—-Lialda—-Pentasa
Can be given rectally as an enema or suppository that acts topically on the intestinal mucosa

Olsalazine

5-ASA Drugs
Dipentum

Sulfasalazine

5-ASA Drugs
Azulfidine

Janus Associated Kinase Inhibitor

Restrict the Janus-associated kinase (JAK) enzymes that normally stimulate an immune response by natural killer cells and lymphocytes in the intestinal mucosa

Tofacitinib

Janus Associated Kinase Inhibitor
ONLY TREATS ULCERATIVE COLITIS
Xeljanz

Irritable Bowel Syndrome (IBS)

Chronic disease of the colon that is characterized by irritability of the intestine
Sx include: cramping, abdominal pain, bloating, excessive mucus secretion, and diarrhea alternating with constipation
Can be caused by food allergies, lactose intolerance, or emotional stress
Treated with anti-infective drugs, antispasmodic, chloride channel activator, GC-C agonist, opioid receptor agonist, serotonin 5-HT3 receptor blocker, serotonin 5-HT4 receptor agonist, sodium/NHE3 inhibitor

Rifaximin

Treats IBS
Anti Infective
Xifaxan

Dicyclomine

Antispasmodic
Treats IBSA

Antispasmodic

Have an anticholinergic effect that blocks the action of acetylcholine on the smooth muscles around the intestines—decreases peristalsis, cramping, spasms, and diarrhea

Chloride Channel Activator Drugs

Stimulate chloride channels in the mucosa of the intestinal wall—causes fluids to flow into the intestines and soften the stool

Iubiprostone

Chloride Channel Activator
Treats IBS
Amitiza

GC-C Agonist

Bind to an enzyme (guianylate cyclase-c) causes the secretion of the chloride, bicarbonate, and fluids into the intestine
Used to treat IBS associated with constipation

Linaclotide

GC-C Agonist
Treats IBS
Linzess

Plecanatide

GC-C agonist
Treats IBS
Trulance

Opioid Receptor Agonist

Stimulate opioid receptors in the intestine—creates the same effect as an opioid drug, in that it decreases pain and has a side effect of constipation—used to treat diarrhea related to IBS

Eluxadoline

Opioid receptor agonist
Treats IBS related diarrhea
Viberzi

Serotonin 5-HT3 Receptor Blocker

Selectively blocks only 5-HT3 receptors that act as ion channels on nerves around the intestines.. activation of these receptors and the ion channels normally causes pain, increased intestinal secretions, and increased peristalsis—-blocking these receptors decreases pain, secretions, and peristalsis

Alosetron

Serotonin 5-HT3 receptor blocker
Treats IBS
Lotronex

Serotonin 5-HT4 Receptor Blocker

Selectively stimulates (agonist action) only 5-HT4 receptors on nerves around the intestines.. increases intestional secretions and peristalsis—- treats IBS related constipation

Tegaserod

Serotonin 5-HT4 receptor agonist
Treats IBS related constipation
Zelnorm

Sodium/NHE3 Inhibitor

Inhibit the exchange of sodium and hydrogen in the intestine— increases intestinal secretions and peristalsis while decreasing intestinal hypersensitivity— used to treat IBS associated with constipation

Tenapanor

Sodium/NHE3 Inhibitor
Treats IBS constipation
Ibsrela

Amitriptyline

Antidepressant
Can be used to treat IBS

Rifaximin

Anti infective drug
Can be used to treat IBS
Xifaxan

Donnatal

Combination drug
Treats IBS
Atropine/hyoscyamine/scopolamine/phenobarbital

Librax

Combination drug
Treats IBS
Clidinium/chlordiazepoxide

Antidiarrheal

Slows peristalsis or absorbs extra water and secretions from the intestine back into the blood
Treats diarrhea associated with bacterial infections, inflammatory bowel disease, IBS, and cancer

Include anticholinergic, anti infective, chloride channel regulator, opioid

Anticholinergic

Block the action of acetylcholine, decreasing the rate of peristalsis in the intestine

Lioeramide

Anti diarrheal
Imodium A-D (anti diarrheal)

Anti Infective

Treats diarrhea associated with bacterial or protozoal infections

Bismuth

Anti infective

Anti Diarrheal

Devrom, Kaopectate, Pepto Bismol

Ciproflaxacine

Anti Diarrheal

Anti infective

Cipro

Nitazoxanide

Anti diarrheal

Anti Infective

Alinia

Rifamycin

Anti infective

Anti diarrheal

Aemcolo

Chloride Channel Regulator

Regulates the flow of calcium ions through calcium channels in the intestinal mucosa

Decreases intestinal secretions and fluid loss

Crofelemer

Used to treat diarrhea caused by infection of HIV

Mytesi

Opioid Drugs

Stops diarrhea

Paregoric

Opiod

Treats diarrhea

Lomotil

Combination drug to treat diarrhea

Atropine/diphenoxylate

Motofen

Combination drug used to treat dirrhea

Atropine/ difenoxin

Antiflatulent

Used to prevent or treat intestinal gas

Alpha D galaxtosidase

Helps digest carbs in gas forming food like beans

Antiflatulent

Beano

Lactase

Helps digest the lactose in milk that causes intestinal gas in people who are lactose intolerant

Antiflatulent

Lactaid

Simethicone

Decreases surface tension of gas bubbles to prevent the formation of large areas of gas in the intestine

Antiflatulent

Gas-X—-Phazyme

Laxative

Short term treatment of constipation, with attention being given to lifetstyle changes, including an increased intake of water and dietary fiber in the diet and adequate exercise
Include bulk forming, chloride channel activator, GC-C agonist laxative, irritant/stimulant, lubricant, opioid agonist, osmotic, serotonin 5-ht4 receptor agonist, stool softener

Bulk Forming Laxative

Contain indigestible dietary fiber and other substances that absorb and hold water in the intestines to create a bulkier stool that stimulates peristalsis

Most natural and safest

Calcium Polycarbophil

Bulk forming

Laxative

Equalactin, Fibercon

Methylcellulose

Laxative

Bulk forming

Citrucel

Psyllium

Bulk forming

Laxative

Metamucil

Wheat Dextrin

Laxative

Bulk forming

Benefiber

Chloride Channel Activator Laxative

Stimulates chloride channels in the mucosa of the intestinal wall

Causes fluid to flow into the intestines and soften the stool

Used to treat chronic constipation, constipation associated with IBS, and constipation caused by the use of opioid drugs

Lubiprostone

Chloride Channel Activator

Laxative

Amitiza

GC-C Agonist Laxative

Bind to an enzyme (guanylate cyclase-c) and this causes the secretion of chloride, bicarbonate, and fluids into the intestine to soften the stool

Linaclotide

GC-C agonist laxative

Laxative

Linzess

Plecanatide

GC-C agonist

Laxative

Trulance

Irritant/Stimulant Laxative

Act directly on the intestinal smooth muscles to stimulate peristalsis

Bisacodyl

Irritant/stimulant

Laxative

Correctol, Dulcolax, Ex-Lax Ultra, Feen-A-Mint

Sennosides

Irritant/stimulant

Laxative

Perdiem Overnight Relief, Senokot

Lubricant Laxative

Introduce extra oil or water to soften the stool, increase its bulk, and improve peristalsis

Castor Oil

Lubricant

Laxative

Mineral Oil

Lubricant

Laxative

Fleet Mineral Oil

Saline

Lubricant

Laxative

Fleet

Opioid Agonist Laxative

Treat patients who are taking opioid drugs for the relief of severe chronic pain

Block opioid receptors in the intestines

Do not cross the blood-brain barrier

Methylnaltexone

Opioid atagonist

Laxative

Relistor

Naldemidine

Opioid antagonist

Laxative

Symproic

Naloxegol

Opioid Antagonist

Laxative

Movantik

Osmotic Laxative

Use osmosis and osmotic pressure to attract water from the blood into the intestines to soften the stool

Glycerin

Osmotic

Laxative

Administered rectally

Lactilol

Osmotic

Laxative

Pizensy

Lactulose

Osmotic

Laxative

Constulose—-Enulose

Magnesium Hydroxide

Osmotic

Laxative

Milk of Magnesia (MOM)—-Pedia Lax

Polyethylene Glycol

Osmotic

Laxative

MiraLax

Serotonin 5-HT4 receptor Agonist

Selectively stimulate serotonin 5-ht4 receptors by increasing intestinal secretions and peristalsis

Causes suicidal thoughts and behavior

Prucalopride

Serotonin 5-ht4 receptor agonist

Laxative

Motegrity

Stool Softener

Emulsifier that allows fat in the stool to mix with fluid in the intestine to soften the stool

Docusate

Stool softener

Laxative

Colace—-Dulcolax Stool Softener—-Surfak

Peri- Colace and Senokot-S

Combination drug

Sennoside/docusate