Overview:
Baricitinib is a Janus kinase inhibitor that is used to relieve pain, stiffness, and joint swelling in individuals with rheumatoid arthritis when all other treatment methods have failed. Baricitinib also has the additional benefit of slowing the course of bone and joint damage. Baricitinib is also being investigated for its potential application in the treatment of coronavirus. The Food and Drug Administration (FDA) of the United States has approved the emergency use of Baricitinib for the treatment of COVID-19 in adults and children over the age of two who are hospitalized and are on supplemental oxygen or a ventilator due to the illness. The use of Baricitinib to treat coronavirus or COVID-19 has not yet been approved.
How Does Baricitinib Work?
Baricitinib functions as a Janus kinase (JAK) inhibitor, specifically targeting the selective enzymes JAK1 and JAK2. Baricitinib's mechanism of action is by disrupting the JAK-STAT signaling pathway, a series of interactions between proteins and cells that play crucial roles in various biological processes, including immune response, cell proliferation, apoptosis, and tumor development.
Indications and Usage
Baricitinib is recommended for adult patients with moderate to severe rheumatoid arthritis who have not had enough improvement with TNF blockers. It can be used by itself or in combination with Methotrexate or other DMARDs.
What Are the Uses of Baricitinib?
Baricitinib can be administered alone or alongside other therapies, including Methotrexate and DMARDs, to manage moderately to severely active rheumatoid arthritis in individuals who have not had success with prior treatments, such as TNF antagonists. It is also prescribed for hospitalized patients with coronavirus disease (COVID-19) who require oxygen therapy or assistance with breathing. In addition, Baricitinib is effective in treating severe alopecia areata, an autoimmune disorder that leads to patchy hair loss.
Before Using Baricitinib, Tell the Doctor:
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About any allergies to Baricitinib, other medications, or any components found in Baricitinib tablets.
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Share any other prescription or over-the-counter medications, vitamins, nutritional supplements, and herbal products the patient is taking with the doctor and pharmacist.
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If a patient is pregnant or planning to become pregnant, inform the doctor immediately.
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Also, notify the doctor if the patient is breastfeeding, as it is advised not to breastfeed while taking Baricitinib and for four days after the last dose.
Dosage and Administration
Baricitinib is given once daily as a tablet. In some cases, such as if a patient is over 75 years old or has had recurring infections, the doctor may choose to decrease the normal dose.
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Baricitinib may be taken with or without food.
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Stick to the guidelines mentioned on the prescription label. Read in detail any special instructions or warnings. Take the medication as prescribed.
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Sometimes, one may be more susceptible to infections, including severe or deadly diseases, if they are taking this drug. One will require frequent medical examinations.
If one has ever had shingles (herpes zoster), utilizing Baricitinib may trigger the reactivation of these viruses or worsen the existing condition. So, inform the doctor if they have had any of these infections.
While utilizing Baricitinib for COVID-19, one must be under the care of a physician. Continue to take Baricitinib for the whole duration indicated (usually for 14 days or until leaving the hospital).
1. Adults With Rheumatoid Arthritis: Used in adult patients with moderate to severe active rheumatoid arthritis who have not responded to one or more tumor necrosis factor (TNF) antagonists. This medicine can be taken alone or in combination with other DMARDs (disease-modifying antirheumatic drugs).
Dosage - 2 milligrams once daily.
2. Adults with COVID-19 Infection: Used with Remdesivir to treat COVID-19 in hospitalized patients requiring supplementary oxygen, invasive mechanical ventilation, or ECMO (extracorporeal membrane oxygenation).
Dosage - 4 mg Remdesivir once daily. Therapy lasts 14 days or until hospital discharge.
3. Pediatric COVID-19 Patients: It is recommended only for research purposes in the pediatric population.
Dosage - In two to nine years, 2 milligrams once daily. For children nine years and older, Baricitinib 4 mg twice daily. Therapy lasts 14 days or until hospital discharge.
Warnings and Precautions:
In combination with other medications, Baricitinib may increase the chance of developing life-threatening medical problems such as major infections, a hole or rip in the digestive tract, a heart attack or stroke, blood clots, or cancer. Inform the doctor if one has had any of the following:
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A compromised immune system or chronic infection (e.g., tuberculosis, shingles, HIV, or hepatitis).
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Cancer of any type.
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Illness of the kidneys.
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Diverticulitis is a stomach or intestinal ulcer.
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Cardiovascular difficulties.
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A coronary artery bypass, a stroke, or a blood clot.
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Excessive cholesterol.
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Hepatic disease (especially hepatitis B or C).
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A chronic pulmonary disease.
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Diabetes.
Inform the doctor if one has been unwell with fever, chills, muscle pains, cough, difficulty breathing, skin sores, diarrhea, or painful urination. Let the doctor know if a patient has a history of tuberculosis, has been exposed to it, or if they have recently traveled. Certain infections are more prevalent in particular regions of the world, and one may have been exposed while traveling. Do not hide the pregnancy from the doctor. Do not breastfeed. Keep it out of the reach of children, as it is not recommended for use by anyone under the age of 18.
For Patients:
What to Do in Case of a Missed Dose?
If one forgets a dose, take the medication as soon as possible. Skip the missed dose if it is already time for the next dose. Do not double up the doses to compensate.
Overdose
If someone experiences an overdose of Baricitinib, it is important to monitor for any signs or symptoms of adverse reactions related to Baricitinib. Appropriate treatment should be provided as needed.
Adverse Effects:
If someone develops any of the following symptoms of an allergic reaction while taking Baricitinib, discontinue treatment and seek emergency medical attention:
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Hives.
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Breathing difficulties.
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Face, lips, tongue, and throat swelling.
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Certain individuals using Baricitinib have experienced heart attacks, strokes, or life-threatening blood clots. If someone develops the following symptoms, discontinue taking it and seek emergency medical attention:
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Sudden onset of shortness of breath.
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Soreness or pressure in the chest that may move to the jaw, shoulder, arms, or back.
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Nausea, vomiting, and chills.
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A lightheaded sensation, as if someone is about to faint out.
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Lack of strength on one side of the body.
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Slurred speech.
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Drooping lips on one side.
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An arm or a leg may experience discomfort, swelling, or redness.
For Doctors:
Drug Interactions:
There are 384 drugs known to interact with Baricitinib, 259 of which are major, 119 of which are moderate, and 6 of which are minor. This list does not include all possible drug interactions. Several drugs may interact with one another, including some of the following:
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Methotrexate (sometimes combined with Baricitinib).
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Probenecid.
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Medication containing steroids, such as Prednisone or Dexamethasone.
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Aspirin, Ibuprofen, Naproxen, Celecoxib, Diclofenac, Indomethacin, and Meloxicam are some, among others.
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Prescription and over-the-counter medications, as well as several other medicines like vitamins, herbal supplements, etc., may also interact with Baricitinib.
Use in Specific Populations:
Pregnancy: Animal studies indicate that therapy might harm the fetus during pregnancy. Current clinical trials and reports do not provide enough information to determine the risk of major birth defects, miscarriage, or other negative outcomes for mothers and babies. There is no data on long-term Baricitinib use during pregnancy, and there are risks for both the mother and fetus linked to rheumatoid arthritis. It's important to weigh the risks and benefits of long-term use during pregnancy. Research shows that higher disease activity can lead to poor pregnancy outcomes in women with rheumatoid arthritis, such as preterm birth, low birth weight, and being small for gestational age. Therefore, women who can become pregnant should consider planning and prevention.
Lactation: It is unclear if Baricitinib is found in human breast milk. Studies show that it is in the milk of nursing rats. However, differences in how different species lactate make it hard to know what this means for humans. Due to possible serious side effects for breastfeeding infants, women with rheumatoid arthritis should be advised not to breastfeed while using Baricitinib.
Description:
Baricitinb is a JAK inhibitor.
Chemical Formula:
C16H17N7O2S
Molecular Weight
Average: 371.42
Pharmacodynamics
Baricitinib is classified as a disease-modifying antirheumatic drug (DMARD) that helps improve symptoms and slow down rheumatoid arthritis. Research on animals with inflammatory arthritis indicated that Baricitinib effectively reduces inflammation and protects cartilage and bone. It does not appear to harm the immune system or cause negative effects on blood health. In people with rheumatoid arthritis, Baricitinib was found to reduce immunoglobulin levels and serum C-reactive protein.
Absorption
Baricitinib has an absolute bioavailability of about 80 %. After taking it orally, the highest concentration in the blood occurs after one hour. Eating a high-fat meal reduces the average AUC and Cmax of Baricitinib by around 11 % and 18 %, and it also delays the time to reach maximum concentration by 0.5 hours.
Metabolism:
Baricitinib is broken down by the enzyme CYP3A4. About 6 % of the dose taken by mouth appears as metabolites in urine and feces, but no metabolites were found in the blood.
Route of Elimination:
Baricitinib mainly leaves the body through the kidneys. It is removed through both filtration and active secretion. Around 75 % of the dose is found in urine, with 20% of that being the drug itself. About 20 % is found in feces, with 15 % being the unchanged drug.
Half-life:
The half-life of Baricitinib in patients with rheumatoid arthritis is roughly 12 hours. In patients with COVID-19 who were intubated and received the drug through a nasogastric or orogastric tube, the half-life was about 10.8 hours.
What Are the Contraindications of Baricitinib?
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Serious and advanced kidney failure (stages 4 and 5).
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Significant liver damage.
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Previous cases of blood clots (like deep vein thrombosis or pulmonary embolism) or higher chances of blood clots (such as obesity or long periods of being inactive).
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Current infections include tuberculosis, hepatitis B, and hepatitis C.
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Allergy to Baricitinib or any ingredients in the product.
All the information regarding this drug Baricitnib is for educational purposes and based on general information. The drug interactions and complications may vary depending on one’s health-related issues and conditions. Consult the healthcare practitioner to check that the information in this article applies to a patient's specific situation.
