What You Need To Know About Constipation Drug Linaclotide



1. What is Linaclotide (Linzess)?

Linaclotide (Linzess) is an FDA-approved oral drug which is commonly used by adult patients experiencing chronic constipation or constipation due to irritable bowel syndrome. Linaclotide 851199-59-2 comes at the top of the list of a new drug class referred to as guanylate cyclase-C agonists.

Linaclotide brand name is Linzess and it is important to bear in mind that at the moment there’s no Linaclotide generic version. So, if you are looking for Linaclotide for sale or personal use, be on the lookout for fraudulent online drug sellers who might be selling illegal Linaclotide generic drug.

Linzess is a guanylate cyclase-C agonist and a 14-amino acid peptide. it’s chemical name is L-cysteinyl-L-cysteinyl-L-glutamyl-L-tyrosyl-L-cysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-L-cysteinyl-L-threonyl-glycyl-L-cysteinyl-L-tyrosine, cyclic (1-6), (2-10), (5-13)-tris (disulfide).

Its molecular formula is C59H79N15O21S6 while the molecular weight is 1526.
Linaclotide powder is white to off-white and is slightly soluble in water. It can also dissolve slightly in aqueous sodium chloride (0.9%).

The final Linzess is in the form of hard gelatin capsules containing Linaclotide-coated beads. Calcium chloride dihydrate, L-leucine, titanium dioxide, microcrystalline cellulose, gelatin, together with hypromellose are among the active ingredients in Linzess

2. What is Linaclotide used for?

When it comes to Linaclotide uses, people use it as a treatment for particular bowel issues such as irritable bowel syndrome which characterized by constipation and chronic idiopathic constipation.

What You Need To Know About Constipation Drug Linaclotide

Linaclotide for irritable bowel syndrome symptoms

Irritable bowel syndrome (IBS) is a prolonged disorder which prevents the intestines to function normally. This Linaclotide indication is also referred to as spastic colon and sometimes functional bowel disease. The major symptoms of the disorder are constipation, diarrhoea and abdominal pain with constipation or alternating with diarrhoea.

In a clinical study to establish the efficacy of Linaclotide for the relief of irritable bowel syndrome symptoms, adult patients were used in two randomized, multicenter trials. The first trial involved 800 patients who were put on 290 mcg daily linzess treatment course while 804 were assigned to the second one which was on placebo.

All the patients used in both groups had met IBS Rome II criteria and were expected to achieve a mean score of abdominal pain of 3 at minimum on a scale of zero to ten and at least three complete spontaneous bowel movements every week the course of the treatment period.

By the end of the treatment period, the patients who were on linzess treatment course experienced more improved BIS symptoms as compared to their placebo counterparts in terms of:
  • Spontaneous bowel movement frequency
  • Stool consistency
  • Amount of time and physical effort one uses to pass stool.
  • Abdominal pain relief
That truly confirmed Linaclotide indication as an effective treatment for BIS.

Linaclotide for  Chronic Idiopathic Constipation (CIC) symptoms

In a study to assess the effectiveness of Linzess for CIC management symptoms, adult patients with chronic idiopathic constipation were placed in randomized, multicenter clinical trials, similarly to above-described BIS study.

Each of the patients had met the modified Rome II functional constipation criteria and received 72mg, 145 mcg Linzess, 290 mcg Linzess or placebo treatment daily throughout the 12-week treatment period.

Upon the end of the treatment period, the researchers observed more pronounced CIC symptom improvement among patients who were on Linzess treatment as compared to those who were on placebo. Particularly, they experienced a higher level improvement in terms of stool frequency, stool consistency and bowel movement strain amount.

Of all the three Linzess doses, had minimal side effects besides offering significant CIC symptoms. This proves the Linaclotide indication of its ability to treat CIC.

What You Need To Know About Constipation Drug Linaclotide

3. What is the mechanism of action of Linaclotide?

Unlike some medications that are used for treating the aforementioned health issues, Linaclotide mechanism is different- it isn’t absorbed into your body. Linaclotide mechanism takes place exclusively in your intestines by increasing fluid, consequently improving bowel movements and relieving pain that could be resulting from a bowel problem.

Linaclotide (Linzess) makes the intestines to produce more fluid by increasing the production of cyclic guanosine monophosphate.

When Linaclotide uses its power to increase fluid in your intestines, food moves through the gut faster and the stool texture improves. This improves the symptoms of bowel movement-related symptoms like bloating, stomachache/stomach discomfort and incomplete bowel movement feeling.

4. How should Linaclotide be used?

When you make a Linaclotide buy, of course with a doctor’s prescription, it important to ensure that you read the medication guide you’ll be given by your pharmacist prior to taking the medication. The guide will tell you the right Linaclotide dose for you, the right dosage intervals and the recommended treatment course period.

In case you need any clarification on Linaclotide dose, don’t hesitate to contact your doctor or pharmacist to avoid Linaclotide side effects or Linaclotide interactions.

Being an oral medication, Linaclotide should be taken by mouth. You should take it while stomach is empty, preferably 30 minutes before taking your first meal in a day. The final Linaclotide drug is in capsule form and should be swallowed whole. You shouldn’t break or chew Linaclotide capsules.

However, in case you’ve tried to swallow the capsules but in vain, you can open them and mix the contents in an applesauce spoonful. Then swallow the blend immediately and just as it is-don’t chew it. Mix only the amount you are supposed to take at that particular time because storing the mixture will make drug lose its effectiveness.

In case you don’t have applesauce, you can use water as an alternative. Measure one ounce or 30mm of water, open the prescribed Linaclotide dose capsules and empty the content in the water. Swirl the water- Linaclotide content for approximately 20 seconds and then drink it immediately. Just as with applesauce mixture, don’t chew the content- swallow it whole.

In case the medication is intended to be administered through a nasogastric or gastric tube, seek guidance on the administration from your pharmacist or doctor. However, here’s the general procedure for tube administration.
  • Measure 30 ml of clean and room-temperature water and put it into clean a clean container.
  • Open the Linaclotide capsule and empty its entire content (beads) into the water
  • Mid the water and the Linaclotide beads by swirling the mixture gently for not less than 20 seconds.
  • Draw up the Linaclotide bead-water mixture into a right syringe with a tip resembling that of a catheter and the right size. Then dispense the mixture into a nasogastric or gastric tube used by the patient by applying steady but rapid pressure of approximately 10 mL/10 seconds on the syringe.
  • In case there some Linaclotide beads that remained in the container, add 30ml of clean water into it, swirl the mixture, and administer it as previously described.
  • Once you are done with administering the mixture of Linaclotide beads and water, use at least 10 ml of water to flash the administration tube.

5. What is the dosage for Linaclotide (Linzess)?

The appropriate Linaclotide dose varies from one person to another, depending on the condition it is intended to treat as well as one’s response to the medication. Again, it is important to note that the drug shouldn’t be used by people who’ve not attained the age of 18 years.

Younger kids are at high risk of experiencing serious Linaclotide side effects should they use the drug.

(1) Usual Adult Dose for Irritable Bowel Syndrome

For an adult who’s suffering from Irritable Bowel Syndrome which is accompanied by constipation, he or she should take a Linaclotide dose of 290 mcg every day. As earlier mentioned, the drug should be taken on an empty stomach. To ensure that, take it before your first meal in a day.

(2) Usual Adult Dose for Constipation

According to the U.S. Food and Drug Administration, the recommended Linaclotide dose for an adult with chronic idiopathic constipation (CIC) is 72 mcg.

However, a 145 mcg dose can also be recommended for an adult patient with CIC, depending on his/her presentation and tolerability. You can checkout linzess 72 mcg reviews to get an idea of how the dose works and the users who’ve benefited from it.

According to various linzess 72 mcg reviews, among other feedbacks regarding the medication, a patient with the aforementioned health issues and looking forward to benefit from its potential should use it regularly to achieve the desired results. Besides, it should be taken at the same time every day throughout the prescribed treatment course period.

It is important to note that Linzess is likely cause Linaclotide interactions with various drugs. As such, you need to disclose to your doctor about any medication you are currently on before starting to use it (Linaclotide).

Also, pregnant women should exercise great caution when considering taking Linaclotide because the drug can pose significant danger to the fetus. They should seek doctor’s attention to confirm their safety and that of their unborn babies should they take the medication. The same case applies to nursing mothers and those you intend to get pregnant while using the drug.

However, even if they have CIC or Irritable Bowel Syndrome, patients who are below the age of 6 years shouldn’t take Linzess powder (851199-59-2). Clinical experiments observed that the drug caused deaths in juvenile mice with ages that are equivalent to below 6 years in humans.

As such, the drug is contraindicated for patients who have not attained the age as it put them at very high risk of developing diarrhea and its potentially serious adverse effects.

Besides, there’s clinical data showing the safety and efficacy of linzess among patients aged 6 years to 17 years. As such, in case of a child or a teenager below 18 years who needs a relief of ICI or BIS, doctor’s advice should be sought first.
You might take up to two weeks before you experience symptom relief as a result of the drug. So, be a little bit patient with it. Continue to use it as directed.

However, in case your symptom don’t improve or get worse even after using linzess, don’t take a dose that’s beyond the prescribed amount. You shouldn’t do that in any case. Instead, inform your doctor to establish the factor behind the drug’s ineffectivess and advice on the next course of action.

It is advisable to avoid using Linaclotide in case you’re allergic to it or your intestines have an obstruction.

If you happen to miss a Linaclotide dose, don’t try to make up for the missed dose. Forget about it and continue to take the next doses strictly at the scheduled time.
In case you or your loved one takes an excess Linaclotide dose (overdose), the incidence should be brought to the doctor’s attention immediately. Alternatively, you can contact the Poison Help services by dialing 1-800-222-1222.

What You Need To Know About Constipation Drug Linaclotide

6. What side effects can Linaclotide cause?

According to various Linaclotide reviews and scientific studies, the following are the common Linaclotide side effects:
  • Slight diarrhea
  • Mild stomach pain or discomfort
  • bloating
  • heartburn
  • vomiting,
  • Headache
  • Cold symptoms like stuffy/ runny nose, sore throat painful sinus or sneezing
  • chills
  • ear congestion
  • fever
  • voice loss
  • passing gas
  • stuffy or runny nose
  • rectal bleeding
  • convulsions
  • sunken eyes
  • tight chest
Although rarely, you can also experience one of the following Linaclotide side effects:
  • Severe or persistent diarrhoea
  • Diarrhoea which is accompanied by dizziness or a feeling which makes you feel like you are likely to pass out
  • Leg cramps
  • Mood swings
  • Unsteady feeling
  • Abnormal confusion
  • Irregular heartbeats
  • Increased and persistent thirst
  • Chest fluttering
  • Limp feeling
  • Muscle weakness
  • Severe stomach pain
  • black, bloody, or tarry feces
  • hives
  • difficult breathing
  • facial, lip, tongue, or throat swelling
You need to seek emergency help should you experience a swelling on the aforementioned parts, breathing problem or hives.
In case of the other rare Linaclotide side effects, you should cease to use the drug and contact your doctor immediately for further guidance.

7. Which drugs or supplements will interact with Linaclotide?

Linaclotide interactions may occur in case Linaclotide is used alongside other drugs including the over-the-counters, vitamin products, herbal products and prescribed medications. Some of the medications that have been reported likely to cause Linaclotide interactions include:
  • Abilify
  • Amitiza
  • Aspir 81
  • Aspirin Low Strength
  • Ativan
  • Colace
  • Dulcolax(minor interaction)
  • Concerta
  • Cymbalta
  • Dexilant
  • Flexeril
  • Metamucil(minor interaction)
  • Levothyroxine (moderate interaction)
  • lubiprostone
  • Metoprolol Succinate ER
  • Norco
  • Paracetamol
  • Restasis
  • Symbicort
  • Vitamin B12
  • Vitamin C
  • Vitamin D3
  • Xanax
  • Zyrtec

8. What are the differences between Linaclotide and lubiprostone?

Both Linaclotide and lubiprostone are DFA-approved drugs for chronic idiopathic constipation and irritable bowel syndrome in adults.  If you want increased bowel movements, you can choose any of the two.
However, they have a number of differences in terms of:

(1)Their respective classes

Lubiprostone belongs to a drug class known as chloride channel activators. On the other hand, Linaclotide (Linzess) is a member of a class of drug referred to as guanylate cyclase-C agonists.

(2)Daily dose

While the recommended Linaclotide dose is supposed to be taken once a day, particularly before breakfast, Lubiprostone is usually taken twice a day.  Therefore, if you have trouble remembering to take your medicines every day, Linaclotide will be a more favorable option for you.

Another thing that differentiates the two in terms of dose is the amount that one should take at once. For instance, for CIC, the recommended Linaclotide’s single dose is 72 mcg while that of Lubiprostone is 8 mcg.

(3)Drug interaction

Another difference Linaclotide powder (851199-59-2)  and lubiprostone is in terms of drug interaction. With about a whopping 58 drugs known to interact with Linaclotide, Linaclotide interactions are far much more as compared to lubiprostone which is associated with just one drug interaction.

(4)Date of approval

Linzess was approved on 30th August 2012 while the approval of lubiprostone took place on January 31, 2006

(5)Food interactions

When you have food in your stomach and you take Linaclotide, your gastrointestinal symptoms like  diarrhea, abdominal pain and gas are likely to get worse, thanks to Linaclotide-food interaction.  In case you develop more severe diarrhea and you are taking another oral medication, the absorption of the latter might be adversely interfered with.

To minimize gastrointestinal intolerance as a result of food interaction, Linaclotide is supposed to be taken on an empty stomach.

On the other hand, there’s scientific proven incident of Lubiprostone-food interactions. However, this is not to rule out on possible interactions. As such, it’s important to seek more clarification on the best time to use the medication from your healthcare provider

(6)Fetal risk in pregnant mothers

So far, a section of relevant research and Linaclotide reviews show that Lubiprostone is likely to cause harm on a fetus should a pregnant mother takes the medication. On the other hand, there’s no single study that shows that Linzess can cause fetal harm in case it’s taken by an expectant woman.

Scientists attribute this perceived safety to the low systemic absorption of the medication. However, the risk can’t be ruled out fully as more research is currently underway to ascertain the safety or danger of the drug to an unborn child.

Therefore, whether intending to take Lubiprostone or Linaclotide, a pregnant mother should consult a physician regarding the appropriateness of the decision.

(7)Prescription

Besides CIC, lubiprostone can b
e used as a treatment for Opioid-induced constipation (OIC) as well as Irritable bowel syndrome with constipation in women who are at least 18 years old.
When it comes to Linaclotide, apart from CIC, it also treats irritable bowel syndrome which is accompanied by constipation (IBS-C) in women and men. It isn’t used as a treatment for OIC.

(8)Linaclotide cost

When it comes to Linaclotide cost, it is slightly higher than that of lubiprostone. At the moment, Linaclotide cost is approximately $450 for 30 capsules while 60 capsules of lubiprostone might cost about $396. However, the prices vary from one seller to another and from time to time.

(9)Manufacturer

The manufacturer of Linaclotide is a company known as Allergan while lubiprostone is a product of Sucampo company.
Despite the above differences, it is important to note that lubiprostone and Linaclotide are sold to consumers in oral capsule form and they don’t have generics.  Also, both drugs require doctor’s prescription for one to obtain them from any seller.

9. What other information about Linaclotide should I know?

Just like any other drug, Linaclotide powder (851199-59-2) or capsules ought to be stored out of kid’s reach to prevent them from abusing it.  Also, being a prescription medicine, some people might be tempted to share the drug with others to avoid the hassle of going to a doctor for prescription.
However, sharing of Linaclotide risky because a doctor has to put many factors in consideration before prescribing the medication and bypassing the step might result in serious adverse effects.

In case you want to make a Linaclotide buy, you need to know that in most countries, including the U.S, you need a doctor’s prescription in order to get the medication. This is irrespective of whether you intend to buy it online or over-the-counter.

When it comes to storage, the recommended storage temperature for Linaclotide 851199-59-2 is 25°C (77°F). Whether you are dealing with Linaclotide powder or capsules, the medicine should be   stored in a moisture-free place and, shouldn’t be subdivided or repackaged. Instead, keep the entire drug in its original container.
Also, ensure that the container is tightly closed with its desiccant inside to keep off moisture.

Whether you want to buy Linaclotide 851199-59-2 for industrial use, Linaclotide for sale or other Linaclotide uses, ensure that you get it from a reputable and trustworthy source. The online Linaclotide reviews can guide you to a good seller.
Otherwise, without performing due diligence, that offline/online seller claiming to have genuine Linaclotide for sale might turn out to be selling contraband products or steal your hard-earned cash.

References
  1. Andresen, V., Camilleri, M., Busciglio, I. A., Grudell, A., Burton, D., McKinzie, S., … & Currie, M. G. (2007). Effect of 5 days linaclotide on transit and bowel function in females with constipation-predominant irritable bowel syndrome. Gastroenterology133(3), 761-768.
  2. Chey, W. D., Lembo, A. J., Lavins, B. J., Shiff, S. J., Kurtz, C. B., Currie, M. G., … & Baird, M. J. (2012). Linaclotide for irritable bowel syndrome with constipation: a 26-week, randomized, double-blind, placebo-controlled trial to evaluate efficacy and safety. The American journal of gastroenterology107(11), 1702.
  3. Cuppoletti, J., Blikslager, A. T., Chakrabarti, J., Nighot, P. K., & Malinowska, D. H. (2012). Contrasting effects of linaclotide and lubiprostone on restitution of epithelial cell barrier properties and cellular homeostasis after exposure to cell stressors. BMC pharmacology12(1), 3.
  4. Harris, A. (2013). LINACLOTIDE. Consultant.
  5. Johnston, J. M., Kurtz, C. B., Drossman, D. A., Lembo, A. J., Jeglinski, B. I., MacDougall, J. E., … & Currie, M. G. (2009). Pilot study on the effect of linaclotide in patients with chronic constipation. The American journal of gastroenterology104(1), 125.
  6. Lembo, A. J., Kurtz, C. B., MacDougall, J. E., Lavins, B. J., Currie, M. G., Fitch, D. A., … & Johnston, J. M. (2010). Efficacy of linaclotide for patients with chronic constipation. Gastroenterology138(3), 886-895.
  7. Lembo, A. J., Schneier, H. A., Shiff, S. J., Kurtz, C. B., MacDougall, J. E., Jia, X. D., … & Jeglinski, B. I. (2011). Two randomized trials of linaclotide for chronic constipation. New England Journal of Medicine365(6), 527-536.

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