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Laxatives and related agents

Bisacodyl (Dulcolax ®) Fleet Phospho-Soda
Docusate (Colace ® ) Glycerin
Lactulose Magnesium citrate
Magnesium hydroxide - MOM Methylcellulose (Citrucel ® )
Mineral Oil Polyethylene Glycol 3350 (MiraLAX®) Powder for Solution
Prepopik ® (sodium picosulfate, magnesium oxide, and anhydrous citric acid) Psyllium ( Metamucil® )
Senna (Senokot ®) Sorbitol
SUCLEAR® Fleet Enema warning - Detroit VAMC

Other

alvimopan - ENTEREG® linaclotide - LINZESS®new icon
lubiprostone (Amitiza ™ ) methylnaltrexone bromide -RELISTOR®
naloxegol -MOVANTIK™ tablets --
Please see package insert for additional information and possible updates. The authors make no claims of the accuracy of the information contained herein; and these suggested doses are not a substitute for clinical judgment. Neither GlobalRPh Inc. nor any other party involved in the preparation of this program shall be liable for any special, consequential, or exemplary damages resulting in whole or part from any user's use of or reliance upon this material. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER.    [  Read the disclaimer    |   <<Back     ]

Bisacodyl  (Dulcolax ®) top of page

Drug Category: Stimulant Laxative

Constipation
(Adult)
a) 5-15 mg orally once daily up to 30 mg/day [Onset of action: 6 to 10 hours]
b) 10 mg suppository rectally once daily  [Onset of action: 15 to 60 minutes]

Preparation of bowel for procedure
a) 10-15 mg orally once daily up to 30 mg/day
b) 10 mg suppository rectally once daily
Onset: bowel movement within 15 to 60 min .

Supplied:
Rectal suppository: 10 mg.
Tablet [enteric coated]: 5 mg.

Docusate  (Colace ® )top of page

Note: Docusate salts are interchangeable; the amount of sodium, calcium, or potassium per dosage unit is clinically insignificant.

Dosing (Adults)
Stool softener:
Oral: 50-500 mg/day in 1-4 divided doses  [Onset of action:  12 - 72 hours]
Rectal: Add 50-100 mg of docusate liquid to enema fluid (saline or water); give as retention or flushing enema.

MECHANISM OF ACTION — Reduces surface tension of the oil-water interface of the stool resulting in enhanced incorporation of water and fat allowing for stool softening.

Fleet Phospho-Soda top of page

Each 5 mL of Fleet-Phospho-soda® contains 2.4 g monobasic sodium phosphate monohydrate and 0.9 g dibasic sodium phosphate heptahydrate in a stable, buffered aqueous solution. Do not exceed the recommended dosage due to the potential of serious side effects. NEVER take more than 3 Tablespoons at one time.

Adults and children 12 years and older
1) Laxative: 15 to 45 mL. Dilute recommended dose with at least one-half glass (4 fl. oz.) of cold water or other clear liquid. Drink, then follow with at least one additional glass (8 fl. oz.) of water or other clear liquid.

fleet dosing

2) Standard bowel cleansing dosage is two 30- to 45-mL doses separated by 10-12 hours (in at-risk patients, - below - consider using the lower end of the dosing range.
AT RISK Patients: Debilitated or elderly; Pregnant or nursing; Increased risk for underlying renal impairment; Colostomy or ileostomy; Heart disease/acute myocardial infarction/unstable angina; Pre-existing electrolyte disturbance. In at-risk patients consider obtaining baseline and posttreatment electrolytes and using the lower end of the dosing range of Fleet® Phospho-soda® (two 30-mL doses given 10-12 hours apart).

Supplied: 748 mOsmol/45mL. The process is associated with transient serum electrolyte changes. Each Tablespoon (15 mL) of FLEET® Phospho-soda® oral saline laxative contains 7.2 g monobasic sodium phosphate monohydrate and 2.7 g dibasic sodium phosphate heptahydrate in a stable, buffered aqueous solution.

ELEMENTAL AND ELECTROLYTIC CONTENT
mEq Phosphate (PO4 )/mL: 12.45
mEq Sodium (Na)/mL: 4.82
mg Sodium (Na)/mL: 111
mmole Phosphorus (P)/mL: 4.15

Glycerin  top of page

Glycerin is a hyperosmotic laxative, which is given rectally, and it usually produces a bowel movement within 15 minutes to 1 hour. The laxative effect of glycerin is due to the local irritant effect of sodium stearate and glycerin's osmotic effect.

Dosage: Children >6 years and Adults: 1 adult suppository 1-2 times/day as needed.
[Onset of action: 15 - 30 minutes]

Lactulose top of page

Dosing (Adults)
Constipation
: 15-30 mL/day increased to 60 mL/day in 1-2 divided doses if necessary.
[Onset of action: 24 - 48 hours]

Acute Hepatic encephalopathy or portosystemic encephalopathy (PSE):
Adults: Oral: 20-30 g (30-45 ml) every 1-2 hours to induce rapid laxation. Adjust dosage daily to produce 2-3 soft stools. Doses of 30-45 ml may be given hourly to cause rapid laxation, then reduce to recommended dose.
Usual daily dose: 60-100 g (90-150 mL) daily. Rectal administration: 200 g (300 ml) diluted with 700 ml of H20 or NS - administer rectally via rectal balloon catheter and retain 30-60 minutes every 4-6 hours

linaclotide - LINZESS®: top of page


DrugLINZESS (linaclotide) capsules, for oral use
[Drug information  /  PDF]  
Dosing:  Click (+) next to Dosage and Administration section (drug info link)
ABBREVIATED MONOGRAPH - SEE PACKAGE INSERT.

Initial U.S. Approval:  2012

CONTRAINDICATIONS:
Pediatric patients up to 6 years of age.
Patients with known or suspected mechanical gastrointestinal obstruction.
WARNINGS:
WARNING: PEDIATRIC RISK
See full prescribing information for complete boxed warning.

LINZESS is contraindicated in pediatric patients up to 6 years of age. Avoid use of LINZESS in pediatric patients 6 through 17 years of age. Linaclotide caused deaths in young juvenile mice.

WARNINGS AND PRECAUTIONS
Diarrhea: Patients may experience severe diarrhea. Hold or stop LINZESS.
-------------------------

Mechanism of Action: Linaclotide is a guanylate cyclase-C (GC-C) agonist. Both linaclotide and its active metabolite bind to GC-C and act locally on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevation in intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly through activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in increased intestinal fluid and accelerated transit. In animal models, linaclotide has been shown to both accelerate GI transit and reduce intestinal pain. The linaclotide-induced reduction in visceral pain in animals is thought to be mediated by increased extracellular cGMP, which was shown to decrease the activity of pain-sensing nerves.

INDICATIONS AND USAGE:
1.1 Irritable Bowel Syndrome with Constipation (IBS-C)
LINZESS (linaclotide) is indicated in adults for the treatment of irritable bowel syndrome with constipation (IBS-C).

1.2 Chronic Idiopathic Constipation (CIC)
LINZESS is indicated in adults for the treatment of chronic idiopathic constipation (CIC).

DOSAGE AND ADMINISTRATION
2.1 Irritable Bowel Syndrome with Constipation (IBS-C)

The recommended dose of LINZESS is 290 mcg taken orally once daily on an empty stomach, at least 30 minutes prior to the first meal of the day.

2.2 Chronic Idiopathic Constipation (CIC)

The recommended dose of LINZESS is 145 mcg taken orally once daily on an empty stomach, at least 30 minutes prior to the first meal of the day.

2.3 Important Administration Instructions

Do not crush or chew capsule or capsule contents. Swallow LINZESS capsule whole, or for adult patients with swallowing difficulties, follow the instructions below for administration with applesauce or water. Sprinkling of LINZESS beads on other soft foods or in other liquids has not been tested.

For administration in applesauce:

  1. Place one teaspoonful of applesauce at room temperature into a clean container.
  2. Open the capsule.
  3. Sprinkle entire contents (beads) on applesauce.
  4. Consume the entire contents immediately. Do not chew the beads. Do not store the applesauce and beads for later use.

For administration in water:

  1. Pour approximately 1 ounce (30 mL) of bottled water at room-temperature into a clean cup.
  2. Open the capsule
  3. Sprinkle entire contents (beads) into the water
  4. Gently swirl beads and water for at least 10 seconds.
  5. Swallow the entire mixture of beads and water immediately.
  6. Add another 1 ounce of water to any beads remaining in cup, swirl for 10 seconds, and swallow immediately.
  7. Do not store the bead-water mixture for future use.

Note: The drug is coated on the surface of the beads and will dissolve off the beads into the water. The beads will remain visible and will not dissolve. Therefore, it is not necessary to consume all the beads to deliver the complete dose.

For nasogastric or gastric feeding tube administration in water:

  1. Open the capsule and empty the beads into a clean container with 1 ounce (30 mL) of room-temperature bottled water.
  2. Mix by gently swirling beads for at least 10 seconds
  3. Draw-up the beads and water mixture to an appropriately sized catheter-tipped syringe and apply rapid and steady pressure (10 mL/10 seconds) to dispense the syringe contents into the tube.
  4. After administering the bead-water mixture, flush nasogastric/gastric tube with a minimum of 10 mL of water.

Note: It is not necessary to flush all the beads through to deliver the complete dose.

After dosing of linaclotide in either applesauce or water, the first meal of the day can be consumed 30 minutes later.


HOW SUPPLIED:

145 mcg capsules are white to off-white opaque with gray imprint “FL 145”
290 mcg capsules are white to off-white opaque with gray imprint “FL 290”


lubiprostone  (Amitiza ™ ) top of page

Indications:   Amitiza is a chloride channel activator indicated for:

1] Treatment of chronic idiopathic constipation in adults
Dose: 24 mcg taken twice daily orally with food and water. Physicians and patients should periodically assess the need for continued therapy.

2] Treatment of irritable bowel syndrome with constipation in women  geq 18 years old
Dose: 8 mcg taken twice daily orally with food and water
 
Renal Impairment: Amitiza has not been studied in patients who have renal impairment.
Hepatic Impairment: Amitiza has not been studied in patients who have hepatic impairment.

Supplied: Gelatin capsules: 8 mcg and 24 mcg

WARNINGS AND PRECAUTIONS
  • Women who could become pregnant should have a negative pregnancy test prior to beginning therapy and should be capable of complying with effective contraceptive measures.
  • Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Patients may experience nausea; concomitant administration of food may reduce this symptom.
  • Do not prescribe for patients that have severe diarrhea.
  • Patients taking Amitiza may experience dyspnea within an hour of first dose. This symptom generally resolves within 3 hours, but may recur with repeat dosing.
  • Evaluate patients with symptoms suggestive of mechanical gastrointestinal obstruction prior to initiating treatment with Amitiza.
ADVERSE REACTIONS
  • Most common adverse reactions (incidence > 4%) in chronic idiopathic constipation are nausea, diarrhea, headache, abdominal pain, abdominal distension, and flatulence.
  • Most common adverse reactions (incidence > 4%) in irritable bowel syndrome with constipation are nausea, diarrhea, and abdominal pain.

Mechanism of Action:
Lubiprostone is a locally acting chloride channel activator that enhances a chloride-rich intestinal fluid secretion without altering sodium and potassium concentrations in the serum.

Magnesium citrate top of page

Onset: 30 minutes to 6 hours

Dosing (Adults): Cathartic: Oral: Adults: 1/2 to 1 full bottle (150-300 mL). May be taken as a single daily dose or divided doses. Maximum 300ml in a 24 hour period (manufacturer).
Dave's note: (MAXIMUM DOSE) Some sources list the daily maximum as 25 grams which is equivalent to ~425 ml.  [See renal impairment below - may not be indicated]

Supplied: Solution, oral: 290 mg/5 mL (300 mL).
Absorption: Oral: 15% to 30%. Excretion: Urine.

MECHANISM OF ACTION - Promotes bowel evacuation by causing osmotic retention of fluid which distends the colon with increased peristaltic activity

RENAL IMPAIRMENT - Patients in severe renal failure should not receive magnesium due to toxicity from accumulation. Patients with a Clcr <25 mL/minute should be monitored by serum magnesium levels.

Magnesium hydroxide -   MOM top of page

Laxative:
Children >/= 12 years and Adults: 30-60 mL/day (15-30 mL/day of liquid concentrate) or in divided doses.

Dosing in renal impairment: Patients in severe renal failure should not receive magnesium due to toxicity from accumulation. Patients with a Clcr<25 mL/minute receiving magnesium should be monitored by serum magnesium levels.

Administration
Liquid doses may be diluted with a small amount of water prior to administration. All doses should be followed by 8 ounces of water.

Methylcellulose  (Citrucel ® ) top of page

Citrucel Orange Flavor Powder - Actions: Promotes elimination by providing additional fiber (bulk) to the diet. This product generally produces bowel movement in 12 to 72 hours.
Indications
: For relief of constipation (irregularity). May also be used for relief of constipation associated with other bowel disorders such as IBS, diverticular disease, and hemorrhoids as well as for bowel management during postpartum, postsurgical, and convalescent periods when recommended by a physician.

Adult Dose
: dissolve one leveled scoop (one heaping tablespoon - 19g) in 8 ounces of cold water up to three times daily at the first sign of constipation. Children age 6 to 12 years of age: one-half the adult dose stirred briskly in 8 ounces of cold water, once daily at the first sign of constipation. The mixture should be administered promptly and drinking another glass of water is highly recommended

Mineral Oil   top of page

Adult (usual) - Constipation: 15-45 ml orally once daily at bedtime (max of 45 ml). Do not take within 2 hr of meals. Should not be used longer than 1 week, except under orders of a physician. Patient should not be reclining after oral administration to avoid aspiration of oil droplets.

Bowel clearance: 118 ml rectally once daily as an enema.

Protect clothing - may have oil leakage from rectum.

Polyethylene Glycol 3350 (MiraLAX®) Powder for Solution top of page

Supplied:
Bottle:
Active ingredient (in each dose) (Bottle Only)
Polyethylene Glycol 3350, 17 g (cap filled to line)

Packets:
Active ingredient (in each dose)
Polyethylene Glycol 3350, 17 grams / packet

--------------------
Purpose
Osmotic Laxative

Use
-relieves occasional constipation (irregularity)
-generally produces a bowel movement in 1 to 3 days
--------------------

Directions (Bottle Only):
  • do not take more than directed unless advised by your doctor
  • the bottle top is a measuring cap marked to contain 17 grams of powder when filled to the indicated line (white section in cap)
  • adults and children 17 years of age and older:
    • fill to top of white section in cap which is marked to indicate the correct dose (17 g)
    • stir and dissolve in any 4 to 8 ounces of beverage (cold, hot or room temperature) then drink
    • use once a day
    • use no more than 7 days
  • children 16 years of age or under: ask a doctor

Directions (Packet Only):
  • do not take more than directed unless advised by your doctor
  • adults and children 17 years of age and older:
    • stir and dissolve one packet of powder (17 g) in any 4 to 8 ounces of beverage (cold, hot or room temperature) then drink
    • use once a day
    • use no more than 7 days
  • children 16 years of age or under: ask a doctor
-------------------------
Unlabeled use:
-------------------------
Bowel prep - colonoscopy:
Mix 17grams of powder in 8 ounces of water of clear liquid and give q10min until 2 liters consumed (start within 6 hrs after ingesting 20mg bisacodyl delayed-release tabs).

Prepopik ® (sodium picosulfate, magnesium oxide, and anhydrous citric acid)  top of page

Drug UPDATESPrepopik ® (sodium picosulfate, magnesium oxide, and anhydrous citric acid) for oral solution
[Drug information  /  PDF]  
Dosing:  Click (+) next to Dosage and Administration section (drug info link)
ABBREVIATED MONOGRAPH - SEE PACKAGE INSERT.

Initial U.S. Approval:  2012

Mechanism of Action: Sodium picosulfate is hydrolyzed by colonic bacteria to form an active metabolite: bis-(p-hydroxy-phenyl)-pyridyl-2-methane, BHPM, which acts directly on the colonic mucosa to stimulate colonic peristalsis.

Magnesium oxide and citric acid react to create magnesium citrate in solution, which is an osmotic agent that causes water to be retained within the gastrointestinal tract

INDICATIONS AND USAGE
Prepopik® is a combination of sodium picosulfate, a stimulant laxative, and magnesium oxide and anhydrous citric acid which form magnesium citrate, an osmotic laxative, indicated for cleansing of the colon as a preparation for colonoscopy in adults

DOSAGE AND ADMINISTRATION
Prepopik®, supplied as a powder, must be reconstituted with cold water right before its use (2.1, 2.2)
Two dosing regimens, each requires two separate dosing times (2.1)

"Split-Dose" method is preferred method (2.3)
First dose: during evening before the colonoscopy
Second dose: next day, during the morning prior to the colonoscopy

"Day-Before" method is alternative method if "Split-Dose" is not appropriate (2.4)
First dose: during afternoon or early evening before the colonoscopy
Second dose: 6 hours later during evening before colonoscopy

Additional clear liquids (no solid food or milk) must be consumed after every dose in both dosing regimens (2.3, 2.4)

DOSAGE FORMS AND STRENGTHS
For oral solution: Each of 2 packets contains 16.1 g of powder for orange flavor or 16.2 grams of powder for cranberry flavor: 10 mg sodium picosulfate, 3.5 g magnesium oxide, and 12 g anhydrous citric acid

CONTRAINDICATIONS
Patients with severely reduced renal function (creatinine clearance less than 30 mL/minute).
Gastrointestinal (GI) obstruction or ileus
Bowel perforation
Toxic colitis or toxic megacolon
Gastric retention

WARNINGS AND PRECAUTIONS
Risk of fluid and electrolyte abnormalities, arrhythmia, seizures, and renal impairment: Encourage adequate hydration, assess concurrent medications, and consider laboratory assessments prior to and after use (5.1, 5.2, 5.3, 5.4)
Risks in patients with renal insufficiency or patients taking concomitant medications that affect renal function: Use caution, ensure adequate hydration and consider testing (5.3)
Mucosal ulcerations: Consider potential for mucosal ulcerations when interpreting colonoscopy findings in patients with known or suspected inflammatory bowel disease (5.5)
Suspected GI obstruction or perforation: Rule out diagnosis before administration (4, 5.6)
Patients at risk for aspiration: Observe during administration (5.7)
Not for direct ingestion: Dissolve and take with additional water (5.8)

Psyllium (Fiberall® , Genfiber®, Konsyl®, Metamucil® )  top of page

Usual Dose:  1 teaspoonful or 1 packet orally one to three times daily.
Dosing (Adults)
Constipation, IBS: Oral (administer at least 2 hours before or after other drugs):
Take 1 dose up to 3 times daily. All doses should be followed with 8 oz of water or liquid.
Capsule: 4 capsules/dose (range: 2-6); swallow capsules one at a time
Powder: 1 rounded tablespoonful/dose (1 teaspoonful/dose for many sugar free or select concentrated products) mixed in 8 oz liquid

Onset of action: 12-24 hours
Peak effect: 2-3 days

Senna  (Senokot ®)  top of page

Stimulant laxative.
Dosing (Adults):  Adults and children > 12 years of age: 2 tablets qd.
Senokot granules may be eaten plain, mixed with liquids such as milk to make a delicious drink, or sprinkled on foods.  

Each tablet contains 8.6 mg sennosides.
AGE
STARTING
MAXIMUM
Take preferably at bedtime.  Generally producing bowel movement in 6 to 12 hours.
Adults and children
12 years of age
and over
2 tablets
once a day (at bedtime)
4 tablets
twice a day
6 to under
12 years of age
1 tablet
once a day
2 tablets
twice a day
2 to under
6 years of age
1 / 2 tablet
once a day
1 tablet
twice a day

[Onset of action: 6 to 12 hours]

 [Supplied: Senokot tablets: Each tablet contains 8.6 mg sennosides. Senokot Granules: Each teaspoonful contains 15 mg sennosides. Senokot-S Tablets: Each tablet contains 8.6 mg sennosides and 50 mg of docusate sodium]

Sorbitol  top of page

Dosing (Adults)
Hyperosmotic laxative (as single dose, at infrequent intervals):
Children >12 years and Adults:
Oral: 70% solution 2 to 3 tablespoonfuls (27 to 40.5 g sorbitol) orally x 1.
  [reported range: 30-150 mL x 1]
   1 tablespoonful (15ml) of 70% sorbitol w/w = 13.5 grams
Rectal enema: 120 mL as 25% to 30% solution
Children 2-11 years:
Oral: 2 mL/kg (as 70% solution)
Rectal enema: 30-60 mL as 25% to 30% solution

----------------------------------------------
Adjunct to sodium polystyrene sulfonate: 15 mL as 70% solution orally until diarrhea occurs (10-20 mL/2 hours) or 20-100 mL as an oral vehicle for the sodium polystyrene sulfonate resin

----------------------------------------------

Poisoning:
When administered with charcoal
Oral
:
Adults:  (Sorbitol 70% w/w solution = 0.9 grams/ml):  1 g/kg (range: 1-2 grams/kg) may be given with the initial dose of activated charcoal.   Note: NOT recommended in young children-  may develop diarrhea ==> potentially dangerous fluid shifts and/or electrolyte imbalances.
Important:   American Academy of Clinical Toxicology (AACT) and European Association of Poisons Centers and Clinical Toxicologists (EAPCCT):  the administration of a cathartic alone (e.g. single agent) has no role in the management of poisoning cases - NOT recommended.    However, if combined with activated charcoal, sorbitol 70% w/w should be limited to a single dose.
Multiple doses of sorbitol can lead to excessive cathartic action.

Supplied
Solution, oral: 70% w/w (480 mL).   Contains 0.9 grams/ml or 13.5 grams/tablespoonful.


Note: activated charcoal with sorbitol (commercial product), if available contains:
              96 grams of sorbitol and 50 grams of activated charcoal

SUCLEAR® (Na sulfate, potassium sulfate and Mg sulfate oral soln; and PEG-3350 top of page

Drug UPDATES:  SUCLEAR (sodium sulfate, potassium sulfate and magnesium sulfate oral solution; and PEG-3350, sodium chloride, sodium bicarbonate and potassium chloride for oral solution)
[Drug information  /  PDF]  
Dosing:  Click (+) next to Dosage and Administration section (drug info link)

Initial U.S. Approval:  2013

Mechanism of Action: The primary mode of action of Suclear is the osmotic effect of the unabsorbed polyethylene glycol (PEG) and sulfate salts. Sulfate salts provide sulfate anions, which are poorly absorbed. The osmotic effect of unabsorbed sulfate anions and the associated cations causes water to be retained within the gastrointestinal tract.

PEG is also a largely unabsorbed osmotic agent which causes water to be retained within the gastrointestinal tract.

INDICATIONS AND USAGE:   Suclear is a combination of osmotic laxatives and indicated for cleansing of the colon in preparation for colonoscopy in adults.
DOSAGE AND ADMINISTRATION
Suclear, supplied as oral solution (Dose 1) and for oral solution (Dose 2), must be reconstituted with cool water before use.
Do not consume solid food/milk (clear liquids only); avoid alcohol.
Two dosing regimens, each requires two separate dosing times.
“Split-Dose (2-Day)” regimen is the preferred method:
       Dose 1 (oral solution): during evening before colonoscopy
       Dose 2 (for oral solution): during morning of colonoscopy
“Day-Before (1-Day)” regimen is an alternative method:
       Dose 1 (oral solution): during early evening before colonoscopy
       Dose 2 (for oral solution): 2 hours after starting Dose 1 during evening before colonoscopy
Consume additional water after every dose in dosing regimens

HOW SUPPLIED:  Oral solution: one 6 -oz bottle contains 17.5 g sodium sulfate, 3.13 g potassium sulfate, and 1.6 g magnesium sulfate.
For oral solution: one 2-L jug with powder contains 210 g PEG-3350, 5.6 g sodium chloride, 2.86 sodium bicarbonate, and 0.74 g potassium chloride

naloxegol -MOVANTIK™ tablets  top of page

Drug UPDATES:  MOVANTIK™ (naloxegol) tablets, for oral use
[Drug information  /  PDF]  
Dosing:  Click (+) next to Dosage and Administration section (drug info link)

Initial U.S. Approval:  2014

Mechanism of Action:  Naloxegol is an antagonist of opioid binding at the mu-opioid receptor. When administered at the recommended dose levels, naloxegol functions as a peripherally-acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids.

Naloxegol is a PEGylated derivative of naloxone, and is a substrate for the P-glycoprotein transporter (P-gp). Also, the presence of the PEG moiety in naloxegol reduces its passive permeability as compared with naloxone. Due to the reduced permeability and increased efflux of naloxegol across the blood-brain barrier, related to P-gp substrate properties, the CNS penetration of naloxegol is expected to be negligible at the recommended dose levels limiting the potential for interference with centrally mediated opioid analgesia.

INDICATIONS AND USAGE:  MOVANTIK (naloxegol) is an opioid antagonist indicated for the treatment of opioid-induced constipation (OIC) in adult patients with chronic non-cancer pain

HOW SUPPLIED:  Tablets: 12.5 mg and 25 mg

Reference(s)

National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates.  A local search option of this data can be found here.

Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.
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