Linaclotide (Linzess) Pharmacology
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Questions and Answers

What is the mechanism of action of Diphenoxylate/Atropine in treating diarrhea?

  • Increasing the viscosity of stool
  • Inhibiting the release of gastrin and VIP
  • Inhibiting excessive GI motility and propulsion (correct)
  • Reducing fluid and electrolyte loss

    • What is the primary function of Loperamide in treating diarrhea?

  • Inhibiting the release of serotonin
  • Inhibiting peristalsis and prolonging transit time (correct)
  • Increasing the secretion of gastrin and VIP
  • Reducing the visceral sensation of stool

    • What is the primary mechanism of action of Sulfate salts in bowel preparation?

  • Inhibiting peristalsis and prolonging transit time
  • Reducing the viscosity of stool
  • Increasing the osmotic effect in the gastrointestinal tract (correct)
  • Inhibiting the release of gastrin and VIP

    • What is a common adverse effect of Sucralfate?

    <p>Constipation</p> Signup and view all the answers

    What is a contraindication for the use of Diphenoxylate/Atropine?

    <p>All of the above</p> Signup and view all the answers

    What is a serious adverse effect of Loperamide?

    <p>Torsades de pointes</p> Signup and view all the answers

    What is the mechanism of action of Somatostatin Analogs?

    <p>Inhibiting the secretion of gastrin, VIP, insulin, glucagon, secretin, motilin, and pancreatic polypeptide</p> Signup and view all the answers

    What is a serious adverse effect of Sulfate salts in bowel preparation?

    <p>All of the above</p> Signup and view all the answers

    Which medication is a chloride channel activator that acts locally on the apical membrane of the gastrointestinal tract to increase intestinal fluid secretion and improve fecal transit?

    <p>Lubiprostone</p> Signup and view all the answers

    What is the mechanism of action of lactulose in treating constipation?

    <p>It promotes stool water content by acidifying intestinal contents</p> Signup and view all the answers

    Which medication is used to treat opioid-induced constipation?

    <p>Methylnaltrexone</p> Signup and view all the answers

    What is the effect of linaclotide on gastrointestinal motility?

    <p>It increases intestinal fluid secretion</p> Signup and view all the answers

    Which of the following medications is not approved for males with IBS-C?

    <p>Lubiprostone</p> Signup and view all the answers

    What is the primary mechanism of action of metoclopramide in treating gastrointestinal motility disorders?

    <p>It enhances the response to acetylcholine of tissue in upper GI tract</p> Signup and view all the answers

    What is the main adverse effect of lactulose?

    <p>Flatulence</p> Signup and view all the answers

    Which medication is used to treat hepatic encephalopathy?

    <p>Lactulose</p> Signup and view all the answers

    What is the primary mechanism of action of dicyclomine?

    <p>Blocking the action of acetylcholine at parasympathetic sites</p> Signup and view all the answers

    What is a common side effect of dicyclomine?

    <p>Anticholinergic symptoms</p> Signup and view all the answers

    Which of the following medications is used to decrease growth hormone (GH) and IGF-1 in acromegaly?

    <p>Octreotide</p> Signup and view all the answers

    What is a serious potential complication of octreotide therapy?

    <p>Bradyarrhythmia</p> Signup and view all the answers

    Which of the following is a contraindication for the use of dicyclomine?

    <p>Glaucoma</p> Signup and view all the answers

    What is the brand name of octreotide?

    <p>Sandostatin</p> Signup and view all the answers

    What is the route of administration for dicyclomine?

    <p>PO, IM</p> Signup and view all the answers

    What is an off-label use of octreotide?

    <p>Esophageal varices bleeding</p> Signup and view all the answers

    What is the mechanism of action of Polyethylene glycol 3350?

    <p>It draws water into the stool, thus softening the stool</p> Signup and view all the answers

    What is the indication for Alosetron?

    <p>Irritable bowel syndrome with severe constipation-predominant symptoms</p> Signup and view all the answers

    Which medication is a guanylate cyclase-C agonist?

    <p>Linzess</p> Signup and view all the answers

    What is the role of CYP2C19 in the metabolism of certain medications?

    <p>It is involved in the metabolism of certain proton pump inhibitors and antiplatelet medications</p> Signup and view all the answers

    What is the difference between an osmotic laxative and a stool softener?

    <p>Osmotic laxatives increase stool frequency, while stool softeners soften the stool</p> Signup and view all the answers

    What is the potential serious adverse effect of Alosetron?

    <p>Ischemic colitis</p> Signup and view all the answers

    Which medication is used to treat H. pylori infection?

    <p>Pylera</p> Signup and view all the answers

    What is the precaution when using Alosetron in patients with hepatic impairment?

    <p>Use with caution in mild-moderate hepatic impairment</p> Signup and view all the answers

    What is the primary mechanism of action of Roflumilast?

    <p>Blockage of PDE causing increased cAMP</p> Signup and view all the answers

    What is the brand name of the glucocorticoid Methylprednisolone?

    <p>Medrol</p> Signup and view all the answers

    What is a common side effect of systemic glucocorticoids?

    <p>Increased appetite</p> Signup and view all the answers

    What is the relative potency of Dexamethasone?

    <p>0.75 mg</p> Signup and view all the answers

    What is a contraindication for live vaccines in glucocorticoid therapy?

    <p>Serious systemic infections</p> Signup and view all the answers

    What is a long-term side effect of glucocorticoid therapy?

    <p>Osteoporosis</p> Signup and view all the answers

    What is the brand name of Hydrocortisone?

    <p>Solucortef</p> Signup and view all the answers

    What is a serious side effect of Roflumilast?

    <p>Suicidal thoughts</p> Signup and view all the answers

    What is the mechanism of action of Inhaled Steroids in the airways?

    <p>Inhibition of inflammatory response and increased sensitivity of beta-2 receptors</p> Signup and view all the answers

    What is the effect of LABAs on bronchial smooth muscle?

    <p>Relaxation of bronchial smooth muscle by action on beta-2 receptors</p> Signup and view all the answers

    What is the mechanism of action of Montelukast?

    <p>Inhibition of leukotriene receptors</p> Signup and view all the answers

    What is the effect of Short Acting Beta Agonist on bronchial smooth muscle?

    <p>Relaxation of bronchial smooth muscle by action on beta-2 receptors</p> Signup and view all the answers

    What is the mechanism of action of Phosphodiesterase 4 inhibitor?

    <p>Increases cAMP levels, leading to a reduction in lung inflammation</p> Signup and view all the answers

    What is the effect of Systemic glucocorticoids on the inflammatory response?

    <p>Inhibition of inflammatory response and reverses capillary permeability</p> Signup and view all the answers

    What is the mechanism of action of Xanthine Derivative?

    <p>Blocks PDE causing increased cAMP, which promotes epinephrine release</p> Signup and view all the answers

    What is the benefit of combining corticosteroid and LABA?

    <p>Improvement in pulmonary function and control over using the products alone</p> Signup and view all the answers

    What is the mechanism of action of Long Acting Muscarinic Antagonist?

    <p>Induction of bronchodilation via inhibition of the M3 receptor on airway smooth muscle</p> Signup and view all the answers

    What is the mechanism of action of Zileuton?

    <p>Decreases the formation of leukotrienes, which causes bronchodilation</p> Signup and view all the answers

    Which medication acts on the luminal surface of intestinal epithelium to increase intestinal fluid secretion and improve fecal transit?

    <p>Linaclotide</p> Signup and view all the answers

    What is the mechanism of action of Antihistamine (H1 Receptor Antagonists)?

    <p>Block H1 receptors to decrease the actions of histamine</p> Signup and view all the answers

    Which medication is used to treat opioid-induced constipation?

    <p>Linaclotide</p> Signup and view all the answers

    What is the mechanism of action of Proton Pump Inhibitors?

    <p>Decrease acid secretion in gastric parietal cells through inhibition of (H+, K+)-ATPase enzyme system</p> Signup and view all the answers

    Which medication is a Somatostatin Analog?

    <p>Octreotide</p> Signup and view all the answers

    What is the mechanism of action of Osmotic Laxative?

    <p>Causes water retention in the stool; increases stool frequency</p> Signup and view all the answers

    Which medication is used to treat gastroesophageal reflux disease (GERD)?

    <p>Proton Pump Inhibitors</p> Signup and view all the answers

    What is the mechanism of action of Antidiarrheal (Loperamide)?

    <p>Acts directly on circular and longitudinal intestinal muscles, through the opioid receptor, to inhibit peristalsis and prolong transit time</p> Signup and view all the answers

    Which medication is used to treat nausea and vomiting?

    <p>5-HT3 Antagonist</p> Signup and view all the answers

    What is the mechanism of action of Ammonium Detoxicant?

    <p>Bacteria in the colon degrade lactulose into lactic acid resulting in an increase in osmotic pressure and acidification of intestinal contents</p> Signup and view all the answers

    What is the mechanism of action of Direct Thrombin Inhibitors?

    <p>They bind to the active thrombin site of free and clot-associated thrombin</p> Signup and view all the answers

    What is the effect of Vitamin K Antagonist on the human body?

    <p>It competitively inhibits vitamin K reductase, which reduces Vitamin K epoxide</p> Signup and view all the answers

    What is the mechanism of action of ACE-Inhibitors?

    <p>They competitively inhibit Angiotensin-Converting Enzyme, which prevents the conversion of Angiotensin I to Angiotensin II</p> Signup and view all the answers

    What is the effect of NSAIDS on platelet function?

    <p>They inhibit platelet function by acetylation of the platelet cyclooxygenase</p> Signup and view all the answers

    What is the mechanism of action of P2Y12 Inhibitors?

    <p>They irreversibly inhibit P2Y12 on platelets, which results in inhibition of platelet activation and aggregation</p> Signup and view all the answers

    What is the mechanism of action of Angiotensin Receptor Blocker?

    <p>They specifically intercept the binding of angiotensin II to the AT(1) receptor</p> Signup and view all the answers

    What is the effect of Antidiuretic Hormone Analog on vasodilatory shock?

    <p>It stimulates V1 to increase systemic vascular resistance and mean arterial blood pressure</p> Signup and view all the answers

    What is the mechanism of action of Fibrinolytics?

    <p>They break down clots by binding to fibrin in a thrombus and converting plasminogen to plasmin</p> Signup and view all the answers

    What is the effect of ADH Inhibitor on the human body?

    <p>It inhibits ADH-mediated water reabsorption in the distal tubule</p> Signup and view all the answers

    What is the primary function of insulin in glucose metabolism?

    <p>Facilitates glucose uptake by cells</p> Signup and view all the answers

    Which process is directly involved in the conversion of glucose to glycogen?

    <p>Glycogenesis</p> Signup and view all the answers

    What triggers the release of glucagon from the pancreas?

    <p>Low blood glucose levels</p> Signup and view all the answers

    What defines the homeostatic response to high blood glucose levels?

    <p>Insulin secretion to lower blood glucose</p> Signup and view all the answers

    In glycolysis, which phase involves the phosphorylation of glucose using ATP?

    <p>Investment Phase</p> Signup and view all the answers

    What is the primary role of glycogen in the body?

    <p>To store excess glucose for later use</p> Signup and view all the answers

    What process does glucagon primarily stimulate in the liver?

    <p>Glycogenolysis</p> Signup and view all the answers

    Which mechanism helps maintain stable blood glucose levels?

    <p>Negative feedback involving insulin and glucagon</p> Signup and view all the answers

    Study Notes

    Linaclotide (Linzess)

    • Used to treat IBS with constipation and opioid-induced constipation
    • Acts locally on the apical membrane of the gastrointestinal tract to increase intestinal fluid secretion and improve fecal transit

    Lubiprostone (Amitiza)

    • Used to treat IBS with constipation and opioid-induced constipation
    • Chloride channel activator that increases intestinal fluid secretion and improves fecal transit
    • Not approved for males with IBS-C

    Lactulose

    • Used to treat constipation (osmotic laxative)
    • Bacteria in the colon degrade lactulose into lactic acid, increasing osmotic pressure and acidifying intestinal contents
    • Softens stool by promoting stool water content
    • Alters colonic flora to decrease ammonia production
    • Used to treat hepatic encephalopathy

    Metoclopramide (Reglan)

    • Used to treat GERD, diabetic gastroparesis, and hiccups
    • Dopamine antagonist that blocks dopamine receptors and enhances the response to acetylcholine in the upper GI tract
    • Contraindications: GI obstruction, perforation or hemorrhage, history of seizure, use with other drugs causing EPS
    • Side effects: drowsiness, insomnia, extrapyramidal symptoms, depression, neuroleptic malignant syndrome, tardive dyskinesia

    Sucralfate (Carafate)

    • Used to treat duodenal ulcers
    • Antiulcer activity is the result of formation of an ulcer-adherent complex that covers the ulcer site and protects it against further attack by acid, pepsin, and bile salts

    Sodium/Potassium/Magnesium (Suprep Bowel Kit)

    • Used for colonoscopy preparation
    • Sulfate salts provide sulfate anions, which are poorly absorbed, causing water retention in the GI tract
    • Contraindications: GI obstruction, bowel perforation, gastric retention, ileus, toxic colitis
    • Side effects: discomfort, abdominal distention/pain, N/V, fluid/electrolyte abnormalities, cardiac arrhythmia, seizure

    Diphenoxylate/Atropine (Lomotil)

    • Used to treat diarrhea
    • Diphenoxylate inhibits excessive GI motility and GI propulsion
    • Contraindications: obstructive jaundice, diarrhea associated with pseudomembranous enterocolitis or enterotoxin-producing bacteria
    • Side effects: drowsiness, euphoria, N/V, flushing, paralytic ileus, toxic megacolon, anaphylaxis, anticholinergic effects, respiratory depression

    Loperamide (Imodium)

    • Used to treat diarrhea
    • Acts directly on circular and longitudinal intestinal muscles to inhibit peristalsis and prolong transit time
    • Reduces fecal volume, increases viscosity, and diminishes fluid and electrolyte loss
    • Demonstrates antisecretory activity
    • Contraindications: children younger than 2 years, abdominal pain without diarrhea, acute dysentery, active ulcerative colitis, bacterial enterocolitis
    • Side effects: dizziness, abdominal pain, constipation, torsades de pointes

    Esomeprazole (Nexium)

    • Used to treat difficile infection
    • Somatostatin analog that inhibits serotonin release and the secretion of gastrin, VIP, insulin, glucagon, secretin, motilin, and pancreatic polypeptide
    • Interacts with Pylera, Risedronate DR, CYP2C19 inx, Clopidogrel, Atazanavir, and Rilpivirine

    Dexlansoprazole (Dexilant)

    • Interacts with Pylera, Risedronate DR, CYP2C19 inx, Clopidogrel, Atazanavir, and Rilpivirine

    Polyethylene glycol (Miralax)

    • Used to treat constipation
    • Osmotic laxative that causes water retention in the stool, increasing stool frequency

    Docusate (Colace)

    • Used to treat constipation
    • Stool softener that draws water into stool, softening the stool and achieving ease in bowel movement

    Alosetron (Lotronex)

    • Used to treat irritable bowel syndrome

    • Selective 5-HT3 receptor antagonist

    • Contraindications: constipation, colitis, intestinal obstruction, Crohn's disease, severe hepatic impairment

    • Side effects: constipation, abdominal pain, ischemic colitis### Acromegaly Treatment

    • Octreotide (Sandostatin) decreases growth hormone (GH) and IGF-1 in acromegaly, available in IV and PO forms

    • Common side effects of octreotide include hyperhidrosis, abdominal pain, and headache

    • Serious side effects of octreotide include bradyarrhythmia, hyper/hypoglycemia, and cholelithiasis

    Antispasmodic

    • Dicyclomine (Bentyl) blocks the action of acetylcholine at parasympathetic sites in smooth muscle, secretory glands, and the CNS
    • Dicyclomine is used to treat functional bowel/IBS, available in PO and IM forms
    • Contraindications of dicyclomine include obstructive disease of GI tract, severe ulcerative colitis, glaucoma, Myasthenia gravis, and breast feeding in infants
    • Common side effects of dicyclomine include anticholinergic effects and lightheadedness
    • Serious side effects of dicyclomine include tachyarrhythmia, psychosis, and dyspnea

    COPD Treatment

    • Roflumilast (Daliresp) is used to treat COPD, available in PO form
    • Common side effects of roflumilast include weight loss, diarrhea, nausea, and decrease in appetite
    • Serious side effect of roflumilast is suicidal thoughts
    • Contraindication of roflumilast is moderate-severe liver impairment (Child Pugh B or C)

    Systemic Glucocorticoids

    • Systemic glucocorticoids cause inhibition of inflammatory response, suppress neutrophil migration, and decrease inflammatory mediators
    • Glucocorticoids reverse capillary permeability and have immunosuppressive effects
    • Dexamethasone (DexPak) is available in PO, IV, and ophthalmic forms
    • Hydrocortisone (Cortef, Solucortef) is available in PO, rectal, and injectable forms
    • Methylprednisolone (Medrol, Solumedrol) is available in PO and injectable forms
    • Prednisone (Deltasone) is available in PO form
    • Prednisolone (Millipred) is available in PO and ophthalmic forms
    • Common side effects of systemic glucocorticoids include increased appetite, weight gain, Na/H2O retention, hypokalemia, CNS effects, indigestion, HTN, and hyperglycemia
    • Chronic side effects of systemic glucocorticoids include Cushing's syndrome, dermal thinning, diabetes, glaucoma, cataracts, amenorrhea, growth retardation, acne, and pancreatitis
    • Relative potency of glucocorticoids: dexamethasone 0.75 mg, methylprednisolone 4 mg, hydrocortisone 20 mg, prednisone/prednisolone 5 mg

    Respiratory Agents

    • Inhaled steroids inhibit inflammatory responses in airways and increase beta-2 receptor sensitivity
    • ICS/LABA combination improves pulmonary function and control by combining corticosteroid and LABA
    • Corticosteroids have anti-inflammatory, immunosuppressive, and antiproliferative actions
    • LABAs relax bronchial smooth muscle by acting on beta-2 receptors
    • Short-acting muscarinic antagonists work on M3 receptors, decreasing secretions and causing bronchodilation
    • Long-acting muscarinic antagonists induce bronchodilation by inhibiting M3 receptors on airway smooth muscle
    • Short-acting beta agonists relax bronchial smooth muscle and inhibit mediator release from mast cells by activating beta-2 receptors
    • Leukotriene modifiers, such as montelukast, inhibit leukotriene receptors, facilitating bronchodilation
    • Phosphodiesterase 4 inhibitors increase cAMP levels, reducing lung inflammation

    Thyroid Hormones and Antithyroid Agents

    • Thyroid hormones increase cellular metabolism and play a role in growth, development, CNS, and bone functions
    • Antithyroid agents inhibit the synthesis of thyroid hormones

    Gastrointestinal Agents

    • Antihistamines (H1 receptor antagonists) block H1 receptors, decreasing histamine actions
    • Histamine (H2) receptor antagonists competitively inhibit histamine at H2 receptors, reducing gastric acid secretion
    • Proton pump inhibitors decrease acid secretion by inhibiting (H+, K+)-ATPase enzyme system
    • Osmotic laxatives, such as polyethylene glycol, cause water retention in stool, increasing stool frequency
    • Selective 5-HT3 receptor antagonists block 5-HT3 receptors on enteric neurons in the GI tract
    • Guanylate cyclase agonists bind to guanylate cyclase-C, increasing intracellular and extracellular cGMP, and decreasing GI transit time
    • Chloride channel activators increase intestinal fluid secretion and improve fecal transit
    • Ammonium detoxicants, such as lactulose, soften stool by promoting stool water content
    • Dopamine antagonists block dopamine receptors, enhancing tissue response to acetylcholine in the upper GI tract
    • Sucralfate has antiulcer activity, forming an ulcer-adherent complex that protects against acid, pepsin, and bile salts
    • Bowel prep agents, such as sulfate salts, provide sulfate anions that cause water retention in the GI tract
    • Antidiarrheal agents, such as diphenoxylate and loperamide, inhibit excessive GI motility and propulsion
    • Somatostatin analogs mimic natural somatostatin, inhibiting serotonin release and secretion of various hormones
    • Antispasmodics block the action of acetylcholine at parasympathetic sites in smooth muscle, secretory glands, and the CNS

    Cardiovascular Agents

    • Direct thrombin inhibitors directly inhibit thrombin, binding to the active thrombin site
    • Factor Xa inhibitors reversibly and selectively inhibit Factor Xa, resulting in decreased thrombin generation and thrombus formation
    • Glycoprotein IIb/IIIa inhibitors specifically bind to GPIIb/IIIa, preventing fibrinogen-mediated platelet aggregation
    • Unfractioned heparin binds to antithrombin, which inactivates thrombin and Factor Xa
    • Low molecular weight heparin binds to antithrombin, inhibiting Factor Xa more than thrombin
    • Vitamin K antagonists competitively inhibit vitamin K reductase, reducing vitamin K epoxide and depleting clotting factors
    • NSAIDS inhibit platelet function by acetylating platelet cyclooxygenase, blocking thromboxane A2 formation
    • P2Y12 inhibitors irreversibly inhibit P2Y12 receptors on platelets, preventing platelet activation and aggregation
    • Fibrinolytics break down clots by binding to fibrin and converting plasminogen to plasmin
    • Antidiuretic hormone analogs stimulate V1 to increase systemic vascular resistance and mean arterial blood pressure, and V2 to increase water permeability in renal tubules

    Insulin Regulation

    • Insulin is a hormone secreted by pancreatic beta cells, essential for reducing blood glucose levels.
    • It promotes cellular glucose uptake, particularly in muscles and fat tissues.
    • Insulin facilitates glycogenesis, converting glucose to glycogen in the liver and muscles for storage.
    • It enhances lipid storage and suppresses gluconeogenesis, the process of generating glucose from non-carbohydrate substrates.
    • Insulin release is triggered by increased blood glucose levels following meals.

    Glycogen Storage

    • Glycogen serves as the stored form of glucose, primarily found in liver and muscle tissues.
    • Glycogenesis, the conversion of glucose into glycogen, is stimulated by insulin.
    • The liver's glycogen acts to maintain blood glucose levels, while muscle glycogen is utilized for energy during physical activity.
    • Glycogen stores are depleted during fasting, exercise, and when glucose availability is low.

    Glucagon Function

    • Glucagon is produced by alpha cells in the pancreas and acts to elevate blood glucose levels.
    • It stimulates glycogenolysis, the process where glycogen is broken down into glucose in the liver.
    • Glucagon encourages gluconeogenesis, creating glucose from non-carbohydrate sources like amino acids.
    • Its secretion is triggered by low blood glucose levels and during fasting states.

    Homeostatic Feedback Mechanisms

    • A negative feedback loop regulates blood glucose levels: high levels stimulate insulin secretion, lowering glucose and subsequently decreasing insulin release.
    • Conversely, low glucose levels trigger glucagon secretion, raising glucose and leading to reduced glucagon production.
    • This feedback ensures blood glucose remains stable within a narrow range, typically between 70-100 mg/dL.

    Glycolysis Pathway

    • Glycolysis is a key metabolic process that converts glucose into pyruvate, yielding energy in the form of ATP.
    • It consists of three phases:
      • Investment Phase: ATP is utilized to phosphorylate glucose, enhancing its reactivity.
      • Cleavage Phase: The 6-carbon glucose molecule is split into two 3-carbon molecules.
      • Payoff Phase: Produces ATP and NADH, converting the 3-carbon derivatives into pyruvate.
    • Under aerobic conditions, pyruvate enters the Krebs cycle; under anaerobic conditions, it is converted to lactate in animals or ethanol in yeast.
    • Glycolysis is crucial for energy production and plays a significant role in cellular respiration.

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