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Sodium Picosulfate; Uses, Dosage, Side Effects, Interactions

Dr. Harun Ar Rashid, MD - Arthritis, Bones, Joints Pain, Trauma, and Internal Medicine Specialist Dr. Harun Ar Rashid, MD - Arthritis, Bones, Joints Pain, Trauma, and Internal Medicine Specialist
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Drugs (A - Z)
  • Mechanism of Action of Sodium Picosulfate
  • Indications of Sodium Picosulfate
  • Contraindications of Sodium Picosulfate
  • Dosage of Sodium Picosulfate
  • Side Effects of Sodium Picosulfate
  • Drug Interactions of Sodium picosulfate
  • Pregnancy Category

Sodium picosulfate ( also known as sodium picosulphate) is a contact stimulant laxative used as a treatment for constipation or to prepare the large bowel before colonoscopy or surgery. Sodium picosulfate is not absorbed from the gastrointestinal tract, and its active metabolite, which is absorbed, is not detectable in breastmilk. Sodium picosulfate can be taken during breastfeeding and no special precautions are required.

Picosulfuric acid is found in laxative products. Sodium picosulfate is used to treat constipation or induce colon cleansing to prepare the large bowels before colonoscopy or surgery. The combination product containing sodium picosulfate and magnesium citrate was introduced to the Canadian market in 2005 and has been used in European countries for many years [rx].

Mechanism of Action of Sodium Picosulfate

Sodium picosulfate is a stimulant laxative that in conjunction with magnesium citrate, produces a purgative effect on stools. In a multicentre, observational study comprising of patients undergoing colonoscopy, more than 93.0% of the patients receiving sodium picosulfate-containing preparations reported the colon cleansing effect to be effective [rx]  Picosulfuric acid, as sodium picosulfate, is a contact laxative. Sodium picosulfate inhibits the absorption of water and electrolytes and increases their secretion into the intestinal lumen [rx]. It is hydrolyzed by colonic bacterial enzyme, sulfatase [rx], to form an active metabolite bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM), which acts directly on the colonic mucosa to stimulate colonic peristalsis [rx].

Indications of Sodium Picosulfate

  • Indicated for cleansing of the colon as a preparation for colonoscopy in adults [rx].
  • Bowel preparation therapy
  • Chronic idiopathic constipation
  • Occasional constipation
  • Opioid-induced constipation 
  • Constipation, drug-induced

Contraindications of Sodium Picosulfate

  • Kidney disease with a reduction in kidney function
  • Diarrhea
  • The high amount of magnesium in the blood
  • Low amount of sodium in the blood
  • Extreme loss of body water
  • Appendicitis
  • Stomach or intestine blockage
  • Seizures
  • Allergies to Magnesium Oxide, Magnesium, Citric Acid, Sodium Picosulfate

Dosage of Sodium Picosulfate

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

For cleansing of the colon

For oral dosage form (powder for solution)

  • Adults and children 9 years of age and older—Your doctor will prescribe your dosing regimen to be taken the day or night before your colonoscopy.
  • Split-dose dosing regimen – Take your first packet the night before colonoscopy, and the second dose the next day, in the morning or at least 5 hours before your colonoscopy.
  • Day-Before dosing regimen – Take your first packet in the afternoon or early evening, and the second dose at least 6 hours after the first dose, the night before colonoscopy.
  • Children younger than 9 years of age –Use and dose must be determined by your doctor.

For oral dosage form (solution)

  • Adults – Your doctor will prescribe your dosing regimen to be taken the day or night before your colonoscopy.
  • Split-dose dosing regimen – Take your first bottle the night before colonoscopy, and the second dose the next day, in the morning or at least 5 hours before your colonoscopy.
  • Day-Before dosing regimen – Take your first bottle in the afternoon or early evening, and the second dose at least 6 hours after the first dose, the night before colonoscopy.
  • Children – Use and dose must be determined by your doctor.

If you miss a dose of sodium picosulfate, magnesium, and citric acid, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Side Effects of Sodium Picosulfate

The most common

  • abdominal pain
  • allergic reaction or hypersensitivity (e.g., rash, hives, or itching)
  • anal pain
  • changes in electrolyte balance (e.g., numbness, skin tingling, muscle spasms, rapid heartbeat, muscle weakness, tremors)
  • diarrhea
  • fatigue
  • headache
  • confusion
  • nausea
  • seizures (convulsions)
  • rash

Common 

  • Bleeding of the rectum
  • confusion
  • cough
  • diarrhea
  • dizziness or fainting
  • dry mouth
  • fast, slow, or irregular heartbeat
  • fever
  • headache
  • hives, itching, skin rash
  • increased thirst
  • joint pain, stiffness, or swelling
  • loss of bowel control
  • muscle pain or cramps
  • numbness or tingling in the hands, feet, or lip skin
  • puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
  • seizures
  • stomach pain and tenderness
  • swelling of the eyelids, face, lips, ankles, hands, or feet
  • tightness in the chest
  • troubled breathing or swallowing
  • unusual tiredness or weakness
  • vomiting

Rare

  • Anxiety
  • change in vision
  • chest pain or tightness
  • confusion
  • a cough
  • Agitation
  • arm, back, or jaw pain
  • blurred vision
  • chest pain or discomfort
  • convulsions
  • extra heartbeats
  • hallucinations
  • a headache
  • irritability
  • lightheadedness
  • cold and clammy skin
  • fast and shallow breathing
  • swelling of your feet, legs, or hands purple spot on your skin caused by internal bleeding
  • fast or abnormal heart rate or palpitations
  • loss of appetite
  • lower back, side, or stomach pain
  • mental depression
  • muscle pain or cramps
  • yellowing of your skin or the whites of your eyes
  • upper stomach pain

Drug Interactions of Sodium picosulfate

Sodium picosulfate may interact with following drugs, supplements, & may change the efficacy of the drug

  • alfacalcidol
  • aluminum hydroxide
  • antibiotics (e.g., amoxicillin, azithromycin,  ciprofloxacin, penicillin, tetracycline)
  • antidiabetics (e.g., metformin, glyburide)
  • antiepileptics (e.g., carbamazepine, phenytoin)
  • antipsychotic medications (e.g., clozapine, quetiapine)
  • birth control pills
  • bisphosphonates (e.g., alendronate, etidronate, risedronate)
  • bulk-forming laxatives (e.g., psyllium)
  • calcitriol
  • calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
  • calcium polystyrene sulfonate
  • gabapentin
  • iron preparations and supplements
  • levothyroxine
  • medications are taken by mouth
  • medications that affect water or electrolyte balance (e.g., diuretics, corticosteroids)
  • medications that cause constipation (e.g., opioids, cholinergic)
  • multivitamins with fluoride
  • mycophenolate
  • nonsteroidal anti-inflammatory medications (NSAIDs; e.g., ibuprofen, naproxen)
  • oral contraceptives
  • phosphate supplements
  • raltegravir
  • selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, sertraline)
  • sodium polystyrene sulfonate
  • tricyclic antidepressants (e.g., amitriptyline, doxepin)

Pregnancy Category

FDA Pregnancy Category – B

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding

It is not known if this medication passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

Children: The safety and effectiveness of using this medication have not been established for children less than 1 year of age.

References

  • https://www.drugbank.ca/drugs/DB09268
  • European Chemicals Agency (ECHA)
    https://echa.europa.eu/substance-information/-/substanceinfo/100.030.097
    https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/97128
  • ClinicalTrials.gov
    https://clinicaltrials.gov/
  • DailyMed
    https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=PREPOPIK
    https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=SODIUM+PICOSULFATE
    https://www.drugs.com/cons/sodium-picosulfate-magnesium-and-citric-acid.html
  • Drugs and Lactation Database (LactMed)
    https://www.ncbi.nlm.nih.gov/books/NBK500568/
    https://chealth.canoe.com/drug/getdrug/picodan
  • EPA Chemical and Products Database (CPDat)
    https://comptox.epa.gov/dashboard/DTXSID7048663#exposure
    https://www.epa.gov/chemical-research/chemical-and-products-database-cpdat
  • EU Clinical Trials Register
    https://www.clinicaltrialsregister.eu/
  • FDA Orange Book
    https://www.fda.gov/Drugs/InformationOnDrugs/ucm129662.htm
  • FDA/SPL Indexing Data
    https://www.fda.gov/ForIndustry/DataStandards/SubstanceRegistrationSystem-UniqueIngredientIdentifierUNII/
    https://www.webmd.com/drugs/2/drug-161661/sodium-picosulfate-magnesium-oxide-citric-acid-oral/details/list-contraindications
  • NIPH Clinical Trials Search of Japan
    https://rctportal.niph.go.jp/en/
  • SpectraBase
    https://spectrabase.com/spectrum/4e5wa2e5DAl
    https://spectrabase.com/spectrum/JeCJEFC4tAs
    https://spectrabase.com/spectrum/ENYKl6C7Cnd
  • Springer Nature
  • Thieme Chemistry
  • WHO ATC
    https://www.whocc.no/atc/
    https://www.whocc.no/atc_ddd_index/
  • Wikipedia
    https://en.wikipedia.org/wiki/Sodium_picosulfate
  • https://pubchem.ncbi.nlm.nih.gov
  • MeSH
    https://www.ncbi.nlm.nih.gov/mesh/67005701
    http://www.nlm.nih.gov/mesh/meshhome.html
    https://www.ncbi.nlm.nih.gov/mesh/68002400

Sodium picosulfate

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