sodium picosulfate/magnesium oxide/anhydrous citric acid (Prepopik)

Dosing and uses of Prepopik (sodium picosulfate/magnesium oxide/anhydrous citric acid)

• Adult
• Pediatric

 

Adult dosage forms and strengths

sodium picosulfate/magnesium oxide/anhydrous citric acid

powder for oral solution

• Each of the 2 packets contains: 10mg/3.5g/12g per 16.1 g of powder
• Flavors: Orange, cranberry

 

Bowel Preparation

Indicated for colon cleansing as a preparation for colonoscopy in adults

Split dose

• Preferred dosing method
• First dose: Take during the evening before the colonoscopy (eg, 5:00 to 9:00 PM) followed by five 8-ounce drinks (upper line on the dosing cup) of clear liquids before bed; consume clear liquids within 5 hr
• Second dose: Take the next day ~5 hr before the colonoscopy followed by at least three 8-ounce drinks of clear liquids before the colonoscopy; consume clear liquids within 5 hr up until 2 hr before the time of the colonoscopy

Day before dose

• Alternate method
• First dose: Take in the afternoon or early evening (eg, 4:00 to 6:00 PM) before the colonoscopy followed by five 8-ounce drinks (upper line on the dosing cup) of clear liquids before the next dose; consume clear liquids within 5 hr
• Second dose: Take ~6 hr later in the late evening (eg, 10:00 PM to 12:00 AM), the night before the colonoscopy followed by three 8-ounce drinks of clear liquids before bed; consume clear liquids within 5 hr

 

Administration

Do not prepare solution in advance

Reconstitute powder with cold water immediately before each dose

Fill the supplied dosing cup with cold water up to the lower (5-ounce) line on the cup and pour in the contents of 1 packet of Prepopik powder

Stir solution for 2-3 minutes; reconstituted solution may become slightly warm as the powder dissolves

Take with additional clear liquids according to either split-dose or day-before dose directions

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Prepopik (sodium picosulfate/magnesium oxide/anhydrous citric acid) adverse (side) effects

>10%

Decreased eGFR (10-13.1%)

Increased magnesium (8.7-11.6%)

 

1-10%

Increased serum creatinine (1.9-4.5%)

Vomiting (3-4%)

Decreased potassium (4.7-7.3%)

Decreased sodium (1-3.7%)

Decreased chloride (1-3.7%)

Nausea (2.6-3%)

Headache (1.6-2.7%)

 

Postmarketing Reports

Allergic reactions including rash, urticaria, and purpura

Electrolyte abnormalities including hypokalemia, hyponatremia, and hypermagnesemia

Gastrointestinal reactions including abdominal pain, diarrhea, fecal incontinence, and proctalgia; also isolated reports of aphthoid ileal ulcers and ischemic colitis (causal relationship not established)

Neurologic effects including generalized tonic-clonic seizures associated with and without hyponatremia in epileptic patients

 

Warnings

Contraindications

Hypersensitivity

Severe renal impairment (ie, CrCl <30 mL/minute)

GI obstruction or ileus

Bowel perforation

Toxic colitis or toxic megacolon

Gastric retention

 

Cautions

Adequate hydration essential before, during, and after the use

Caution with congestive heart failure when replacing fluids

If significant vomiting or signs of dehydration including signs of orthostatic hypotension develop after use, consider performing post-colonoscopy lab tests (electrolytes, creatinine, and BUN) and treat accordingly

Fluid and electrolyte disturbances can lead to serious adverse events including cardiac arrhythmias or seizures and renal impairment

Reports of generalized tonic-clonic seizures with the use of bowel preparation products in patients with no prior history of seizures; these cases were associated with electrolyte abnormalities

Orthostatic changes occurred in ~20% of patients in clinical trials on the day of colonoscopy and were documented out to 7 days post colonoscopy

Uncorrected magnesium concentration reached a maximum of ~1.9 mEq/L, which occurred at 10 hr post initial packet administration; this represents an ~20% increase from baseline

Increased magnesium plasma levels may occur with severe renal impairment (ie, CrCl <30 mL/min)

Renal impairment or coadministration with medications that may affect renal function (eg, diuretics, ACE inhibitors, ARBs, NSAIDs) may increase risk for renal injury; adequate hydration before during and after the use is particularly important in these patients; consider performing baseline and post-colonoscopy laboratory tests (electrolytes, creatinine, and BUN)

Caution with severe active ulcerative colitis; osmotic laxatives may cause colonic mucosal aphthous ulcerations and there have been reports of more serious cases of ischemic colitis requiring hospitalization

Rule out significant GI disease before use (eg, obstruction, perforation) (see Contraindications)

Caution with impaired gag reflex or patients prone to aspiration; these patients should be observed during administration

Must reconstitute powder into solution, direct ingestion of powder may result in nausea, vomiting, dehydration, and electrolyte disturbances

Oral medications taken within 1 hour of each dosing may be flushed from GI tract and not properly absorbed

Administer drugs prone to chelation with magnesium (eg, tetracycline, iron, digoxin) at least 2 hr before or at least 6 hr after administration

Prior or concomitant antibiotics may reduce efficacy by decreasing colonic bacteria-mediated conversion of sodium picosulfate to the active metabolite (BHPM)

 

Pregnancy and lactation

Pregnancy category: B

Lactation: Unknown whether distributed in breast milk

 

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.

 

Pharmacology of Prepopik (sodium picosulfate/magnesium oxide/anhydrous citric acid)

Mechanism of action

The stimulant laxative activity of sodium picosulfate together with the osmotic laxative activity of magnesium citrate produces a purgative effect which, when ingested with additional fluids, produces watery diarrhea

Sodium picosulfate: Hydrolyzed by colonic bacteria to form an active metabolite, bis-(p-hydroxy-phenyl)-pyridyl-2-methane (BHPM); BHPM acts directly on the colonic mucosa to stimulate colonic peristalsis

Magnesium oxide and anhydrous citric acid: These 2 ingredients react to create magnesium citrate in solution, an osmotic agent that causes water to be retained within the GI tract

 

Absorption

Peak Plasma Time: 7 hr (sodium picosulfate, 2 packets)

Peak Plasma Concentration: 3.2 ng/mL (sodium picosulfate after 2 doses); active metabolite BHPM below level of quantification

 

Metabolism

Sodium picosulfate, a prodrug, is converted to its active metabolite, bis-(p-hydroxy-phenyl)-pyridyl-2-methane (BHPM), by colonic bacteria

Magnesium oxide and citric acid react in water to create magnesium citrate

 

Elimination

Half-life: 7.4 hr (sodium picosulfate)