Plecanatide, marketed under the trade name Trulance, is a relatively new drug designed to treat
chronic idiopathic constipation (CIC) and
irritable bowel syndrome with constipation (IBS-C). It was developed by
Synergy Pharmaceuticals and received FDA approval in 2017. Plecanatide is a synthetic analog of uroguanylin, a naturally occurring peptide in the human body that regulates intestinal fluid and pH levels. By targeting the guanylate cyclase-C (GC-C) receptor, Plecanatide helps to facilitate bowel movements and relieve symptoms associated with
constipation. Since its approval, it has garnered attention for its efficacy and safety profile in treating gastrointestinal conditions.
Plecanatide Mechanism of Action
The mechanism of action of Plecanatide revolves around its ability to mimic uroguanylin, which is an endogenous peptide involved in fluid homeostasis in the gut. Uroguanylin binds to the
GC-C receptors located on the luminal surface of the intestinal epithelium. When Plecanatide binds to these receptors, it activates them, leading to an increase in cyclic guanosine monophosphate (cGMP) levels. Elevated cGMP levels have a dual effect: they stimulate the secretion of chloride and bicarbonate into the intestinal lumen through the
cystic fibrosis transmembrane conductance regulator (CFTR) channel, and they also inhibit the absorption of sodium. This results in increased intestinal fluid, which softens stools and promotes bowel movements. Additionally, cGMP can reduce
visceral pain by decreasing the activity of pain-sensing neurons in the gastrointestinal tract, providing symptomatic relief for patients with
IBS-C.
How to Use Plecanatide
Plecanatide is administered orally once daily, with or without food. The standard dosage is a 3 mg tablet, which should be swallowed whole, not crushed or chewed, to ensure its efficacy. It is recommended to take the medication at the same time each day to maintain consistent therapeutic levels in the body. Plecanatide's onset of action varies among individuals but typically begins within a few days of starting the medication. Some patients may experience relief from constipation symptoms as early as the first week of treatment, while others may require a longer duration to observe significant improvements. It is important to adhere to the prescribed regimen and to consult a healthcare provider if there is no improvement in symptoms after several weeks of use.
What is Plecanatide Side Effects
While Plecanatide is generally well-tolerated, it can cause side effects in some individuals. The most common side effect reported is
diarrhea, which may occur in up to 16% of patients. In most cases, diarrhea is mild to moderate in severity and resolves with continued use of the drug. However, if diarrhea becomes severe or persistent, it is crucial to contact a healthcare provider, as this may require discontinuation of the medication. Other less common side effects include
nausea,
abdominal pain, and
abdominal distension. Plecanatide is contraindicated in patients with known or suspected
mechanical gastrointestinal obstruction, as its mechanism of action could exacerbate the condition. It is also not recommended for use in children under the age of 18 due to the risk of
dehydration and potential harm to the developing gastrointestinal system.
What Other Drugs Will Affect Plecanatide
Plecanatide has minimal systemic absorption, which reduces the likelihood of significant drug interactions. However, it is essential to inform healthcare providers of all medications currently being taken to ensure safe and effective use of Plecanatide. There are no known significant interactions with other commonly used medications, but caution should be exercised when used in combination with other drugs that can cause diarrhea, such as certain antibiotics or laxatives. Combining these medications with Plecanatide may increase the risk of severe diarrhea and
electrolyte imbalances. Additionally, patients should avoid taking Plecanatide with inhibitors of the GC-C receptor, as this may diminish the drug's effectiveness.
In conclusion, Plecanatide represents a valuable therapeutic option for individuals suffering from chronic idiopathic constipation and irritable bowel syndrome with constipation. Its targeted mechanism of action, ease of administration, and favorable safety profile make it a promising choice for managing these challenging gastrointestinal conditions. However, as with any medication, it is essential to use Plecanatide under the guidance of a healthcare provider and to be aware of potential side effects and contraindications. With proper use, Plecanatide can significantly improve the quality of life for those affected by
chronic constipation and IBS-C.
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