linaclotide (Rx)

Brand and Other Names:Linzess
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 72mcg
  • 145mcg
  • 290mcg
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Irritable Bowel Syndrome

Indicated in adults for irritable bowel syndrome with constipation

290 mcg PO qDay on empty stomach; administer at least 30 minutes before first meal of the day

Chronic Idiopathic Constipation

Indicated for adults with chronic idiopathic constipation

Recommended dose: 145 mcg PO qDay

72 mcg PO qDay may be used based on individual presentation

Tak on an empty stomach; administer at least 30 minutes before first meal of the day

<6 years: Contraindicated

6-17 years: Safety and efficacy not established (see Black Box Warnings and Cautions)

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Adverse Effects

>10%

Diarrhea (16-20%)

1-10%

Abdominal pain (7%)

Flatulence (4-6%)

URI (<2-5%)

Headache (<2-4%)

Viral gastroenteritis (<2-3%)

Sinusitis (<2-3%)

Abdominal distension (2-3%)

Severe diarrhea (2%)

Dyspepsia (1-<2%)

Fecal incontinence (1-<2%)

Viral gastroenteritis (1-<2%)

GERD (1-<2%)

Vomiting (1-<2%)

Fatigue (1-<2%)

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Warnings

Black Box Warnings

Contraindicated in pediatric patients up to 6 years of age

Avoid use in pediatric patients 6 through 17 years of age In nonclinical studies, administration of a single, clinically relevant adult oral dose of linaclotide caused deaths in young juvenile mice

Contraindications

Hypersensitivity

Children aged 6 years or younger

Known or suspected mechanical GI obstruction

Cautions

Diarrhea is the most common adverse reaction; severe diarrhea reported in 2% of linaclotide-treated patients; instruct patient to stop therapy if severe diarrhea occurs and to contact healthcare provider; consider dose suspension and rehydration

Pediatric risk

  • Contraindicated in <6 years of age; in nonclinical studies, death occurred within 24 hr in young juvenile mice (1 to 3 week-old mice; approximately equivalent to human pediatric patients <2 years) following administration of 1 or 2 daily oral doses
  • Avoid the use in pediatric patients 6 through 17 years of age; linaclotide did not cause deaths in older juvenile mice (approximately equivalent to humans ages 12 to 17 years), although there were no deaths in older juvenile mice, given the deaths in young juvenile mice and the lack of clinical safety and efficacy data in pediatric patients, avoid use in older children
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Pregnancy & Lactation

Pregnancy Category: C

Lactation: Unknown whether distributed in breast milk; however, linaclotide and its active metabolite are not measurable in plasma following administration of the recommended clinical doses

Pregnancy Categories

A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA:Information not available.

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Pharmacology

Mechanism of Action

Guanylate cyclase C (GC-C) agonist; activation of GC-C located on the luminal surface of intestinal epithelial cells leads to increased cyclic guanosine monophosphate (cGMP), anion secretion, fluid secretion, and intestinal transit

Appears to work topically rather than systemically; 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

Absorption

Minimal systemic absorption

Concentrations of linaclotide and its active metabolite in plasma are below the limit of quantitation after oral doses of 145 mcg or 290 mcg

Metabolism

Metabolized within the GI tract to its principal, active metabolite by loss of the terminal tyrosine moiety

Both linaclotide and the metabolite are proteolytically degraded within the intestinal lumen to smaller peptides and naturally occurring amino acids

Elimination

Excretion: 3-5% feces (parent compound) and virtually 100% of active metabolite

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Administration

Oral Administration

Take on an empty stomach at least 30 minutes before first meal of the day

Swallow capsule whole; do not chew or break apart

Patients who have difficulty swallowing capsules or those with a nasogastric or gastronomy tube, follow instructions below

  • Administration in applesauce
    • Place one teaspoonful of applesauce at room temperature into a clean container
    • Open the capsule
    • Sprinkle entire contents (beads) on applesauce
    • Consume entire contents immediately; do not chew beads; do not store applesauce and beads for later use
  • Administration in water
    • Pour approximately 1 ounce (30 mL) of bottled water at room-temperature into clean cup
    • Open capsule
    • Sprinkle entire contents (beads) into water
    • Gently swirl beads and water for at least 10 sec
    • Swallow entire mixture of beads and water immediately
    • Add another 1 ounce of water to any beads remaining in cup, swirl for 10 sec, and swallow immediately
    • Do not store the bead-water mixture for future use
    • Note: The drug is coated on surface of the beads and will dissolve off the beads into water; the beads will remain visible and will not dissolve; therefore, it is not necessary to consume all beads to deliver complete dose
  • Nasogastric or gastric feeding tube administration in water
    • Open capsule and empty the beads into clean container with 1 ounce (30 mL) of room-temperature bottled water
    • Mix by gently swirling beads for at least 10 sec
    • Draw-up the beads and water mixture to an appropriately sized catheter-tipped syringe and apply rapid and steady pressure (10 mL/10 sec) to dispense the syringe contents into the tube
    • 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

Storage

Store at 25°°C (77F); excursions permitted between 15-30°C (59-86°F)

Keep in the original container; do not subdivide or repackage

Protect from moisture

Do not remove desiccant from the container

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Formulary

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

Adding plans allows you to:

  • View the formulary and any restrictions for each plan.
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  • Compare formulary status to other drugs in the same class.
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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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