Coltinib

Indications

Upadacitinib is a tablet used to control long-term inflammatory conditions when other treatments have not worked well enough or are not suitable. It is used for moderate to severe rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis and related spine inflammation, moderate to severe atopic dermatitis (eczema), and moderate to severe ulcerative colitis and Crohn's disease. It is started and monitored by a specialist.

How It Works

Upadacitinib belongs to a group called JAK inhibitors. Janus kinases (JAKs) are enzymes inside immune cells that pass on signals from inflammatory messengers. By blocking mainly JAK1, Upadacitinib calms the overactive immune response that causes joint swelling, pain, skin itching or gut inflammation.

Dosage and Administration

Take exactly as prescribed by your specialist; the dose depends on the condition and may be higher for the first weeks in bowel disease. The tablet is usually taken once a day, with or without food. Swallow the extended-release tablet whole: do not crush, split or chew it. If you miss a dose, take it as soon as you remember that day, then continue as normal. Do not stop without talking to your doctor.

Before starting, your doctor will usually check for tuberculosis and hepatitis, and order blood tests (blood counts, liver tests and cholesterol), which are repeated during treatment.

Interactions

• Strong CYP3A4 blockers such as Ketoconazole, Itraconazole or Clarithromycin can raise Upadacitinib levels; grapefruit juice should be avoided.
• Strong enzyme inducers such as Rifampicin, Carbamazepine or Phenytoin can make it less effective.
• Other strong immune-suppressing medicines (for example Azathioprine, Ciclosporin or biologic drugs) increase the risk of infection and are usually not combined.
• Live vaccines should not be given during treatment; get any needed vaccines before starting.

Tell your doctor and pharmacist about every medicine, herbal product and supplement you take.

Contraindications

• Allergy to Upadacitinib or any tablet ingredient.
• Active tuberculosis or any active serious infection.
• Severe liver disease.
• Pregnancy.

Side Effects

Common side effects include colds and sore throat, cough, nausea, acne, headache, tiredness, raised cholesterol, raised muscle enzyme (CK) and changes in blood counts or liver tests. Cold sores and shingles (herpes zoster) are more likely.

Less common but serious effects include serious infections (including tuberculosis and fungal infections), blood clots in the legs or lungs, heart attack or stroke, certain cancers (including skin cancer), and a tear in the bowel. These risks are higher in people aged 65 or over, smokers and people with heart disease risk factors.

Get urgent medical help if you have fever with chills or feel very unwell, a painful swollen leg, sudden chest pain or breathlessness, weakness on one side or trouble speaking, severe stomach pain, or signs of an allergic reaction such as swelling of the face or difficulty breathing.

Pregnancy and Lactation

Upadacitinib may harm an unborn baby and must not be used in pregnancy. Women who could become pregnant should use reliable contraception during treatment and for at least 4 weeks after the last dose. Do not breastfeed while taking it and for about 6 days after the last dose.

Precautions and Warnings

Tell your doctor if you have a current or recurring infection, past tuberculosis or hepatitis B or C, a history of blood clots, heart disease, cancer, diverticulitis, liver or kidney problems, or if you smoke. Have regular skin checks and blood tests as advised. Report any infection early. Avoid live vaccines.

Overdose

Taking too much may increase side effects, especially effects on blood counts and infection risk. Contact a doctor or poison centre straight away; treatment is supportive and monitoring.

Therapeutic Class

Janus kinase (JAK) inhibitor; targeted synthetic disease-modifying immunosuppressant.

Storage

Store below 30°C in a dry place, in the original pack away from light and moisture, and out of the reach of children.