Upadacitinib oral
- Drugs List
- Therapeutic Indications
- Dosage
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Oral formulations of upadacitinib.
Drugs List
Therapeutic Indications
Uses
Axial spondyloarthritis
Moderate to severe active rheumatoid arthritis-other regimens unsuitable
Moderate/severe atopic dermatitis
Psoriatic arthritis when inadequate response or intolerant to prior DMARDs
Ulcerative colitis
Rheumatoid arthritis
Treatment of moderate to severe active rheumatoid arthritis in adults who have responded inadequately to or are intolerant to one or more disease-modifying anti-rheumatic drugs (DMARDs) as monotherapy or in combination with methotrexate.
Psoriatic arthritis
Treatment of active psoriatic arthritis in adults who have responded inadequately to or are intolerant to one or more disease-modifying anti-rheumatic drugs (DMARDs) as monotherapy or in combination with methotrexate.
Axial spondyloarthritis
Treatment of active radiographical ankylosing spondylitis in adult patients who have responded inadequately to conventional therapy.
Treatment of active non-radiographic axial spondyloarthritis in adult patients with indicators of inflammation as indicated by magnetic resonance imaging (MRI) or elevated C-reactive Protein, who have responded inadequately to nonsteroidal anti-inflammatory drugs.
Atopic dermatitis
Treatment of moderate to severe atopic dermatitis in adults and adolescents 12 years and older who are candidates for systemic therapy.
Ulcerative colitis
Treatment of moderate to severe active ulcerative colitis in adult patients who have responded inadequately to or are intolerant to conventional therapy or biologic agents.
Dosage
Adults
Rheumatoid arthritis, psoriatic arthritis and ankylosing spondylitis
15mg once daily.
Atopic dermatitis
15mg or 30mg once daily. Maintain lowest effective dose.
30mg once daily may be appropriate for patients with high disease burden or those with inadequate response to 15mg once daily.
Ulcerative colitis
Initial dose of 45mg once daily for 8 weeks. If adequate response is not received following this 8 week period, a further 8 weeks of 45mg once daily may be considered.
Maintenance dose of 15mg or 30mg once daily. Maintain lowest effective dose.
30mg once daily may be appropriate for patients with high disease burden, requiring a 16-week induction treatment or those with inadequate response to 15mg once daily.
Elderly
Rheumatoid arthritis, psoriatic arthritis and ankylosing spondylitis
(See Dosage; Adult).
Atopic dermatitis
15mg once daily.
Children
Atopic dermatitis
Children aged 12 to 18 years weighing at least 30kg
15mg once daily.
Patients with Renal Impairment
Upadacitinib 15mg once daily should only be used with caution in severe renal impairment and 30mg once daily is not recommended.
Additional Dosage Information
Ankylosing spondylitis
Consider discontinuing upadacitinib if there is no clinical response after 16 weeks of treatment. Patients with initial partial response may improve with continued treatment beyond 16 weeks.
Atopic dermatitis
Patients using upadacitinib with a strong CYP3A4 inhibitor long-term, the dose of 30mg once daily is not recommended.
Children aged 12 to 18 years weighing at least 30kg
Consider discontinuing upadacitinib if there is no clinical response after 12 weeks of treatment.
Ulcerative colitis
Patients using upadacitinib with a strong CYP3A4 inhibitor, an initial dose of 30mg once daily for up to 16 weeks is recommended, and a maintenance dose of 15mg once daily is recommended. The manufacturer recommends if long term use is required, alternatives to strong CYP3A4 inhibitor medicines should be considered.
Contraindications
Absolute lymphocyte count below 0.5 x 10 to the power of 9/L
Children under 12 years
Haemoglobin concentration below 8g / dL
Neutrophil count below 1.0 x 10 to the power of 9 / L at baseline
Severe infection
Breastfeeding
End stage renal disease
Pregnancy
Severe hepatic impairment
Tuberculosis
Precautions and Warnings
Children under 18 years
Elderly
High predisposition to thrombosis
History of recurrent infection
Obesity
Predisposition to infection
Predisposition to pulmonary embolism
Prolonged immobilisation
Risk factors for cardiovascular disorder
Surgery
Weight below 30kg
Diverticulitis
History of thromboembolic disorder
History of tuberculosis
Hyperlipidaemia
Hypertension
Malignant neoplasm
Severe renal impairment
Administration of live vaccines is not recommended
Before initiating screen all patients for viral hepatitis
HBV DNA: Refer to liver specialist to consider interruption
Interrupt therapy if herpes zoster occurs
Start antimicrobial regime if infection suspected during neutropenia
Before starting therapy ensure immunisations are up to date
Consider prophylactic anti-tuberculosis therapy if appropriate
May be increased risk of skin cancer
Monitor patients for non-melanoma skin cancer prior to and during treatment
Prior to starting therapy screen for latent tuberculosis
Treatment to be initiated and supervised by a specialist
Advise patient to report signs of gastrointestinal perforation immediately
Monitor serum transaminases (including ALT) before and during therapy
Monitor for and manage hepatitis reactivation during treatment
Monitor for symptoms of gastrointestinal perforation or fistula
Monitor patient for signs of serious infection
Monitor serum lipids 3 months after initiation
Monitor serum lipids in patients with hyperlipidaemia
Advise patient to seek med advice if signs/symptoms of tuberculosis develop
Advise patient to seek advice at first indications of pregnancy
Interrupt if haemoglobin falls below 8 g/dL
Interrupt if lymphocyte count less than 0.5 x 10 to the power of 9/L
Interrupt therapy if neutrophil count <1.0x10 to the power 9/L
Interrupt treatment if severe infection develops
Suspend if drug induced liver injury is suspected
Discontinue if symptoms of deep vein thrombosis occur
Discontinue if symptoms of pulmonary embolism occur
Not licensed for all indications in all age groups
Advise patient not to take St John's wort concurrently
Advise patient to avoid grapefruit products
Female: Contraception required during and for 1 month after treatment
Consider the risk of initiating upadacitinib treatment in patients who have resided or travelled in areas of endemic tuberculosis or endemic mycoses.
Pregnancy and Lactation
Pregnancy
Upadacitinib is contraindicated during pregnancy.
Use of upadacitinib during pregnancy is contraindicated by the manufacturer. At the time of writing there is limited human data available. Animal studies have shown reproductive toxicity. Risks are unknown.
Lactation
Upadacitinib is contraindicated during breastfeeding.
The manufacturer advises that the patient either discontinues upadacitinib or discontinues breastfeeding. Animal studies have shown excretion of upadacitinib and/or metabolites in milk. It is unknown whether upadacitinib and/or metabolites are excreted in human breast milk. Effects on exposed infants are unknown.
Side Effects
Abdominal pain
Acne
Alanine aminotransferase increased
Anaemia
Aspartate aminotransferase increased
Bronchitis
Candidiasis (mouth or throat)
Cough
Creatine phosphokinase increased
Diverticulitis
Fatigue
Folliculitis
Headache
Herpes simplex
Herpes zoster
Hypercholesterolaemia
Hyperlipidaemia
Hypertriglyceridaemia
Influenza
Lymphopaenia
Nausea
Neutropenia
Pneumonia
Pyrexia
Upper respiratory tract infection
Urinary tract infections
Urticaria
Weight gain
Overdosage
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management. The following number will direct the caller to the relevant local centre (0844) 892 0111 Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Further Information
Last Full Review Date: October 2022
Reference Sources
NICE Evidence Services Available at: www.nice.org.uk Last accessed: 25 October 2022
Summary of Product Characteristics: Rinvoq 15mg prolonged-release tablets. AbbVie Ltd. Revised August 2022.
Summary of Product Characteristics: Rinvoq 30mg prolonged-release tablets. AbbVie Ltd. Revised August 2022.
Summary of Product Characteristics: Rinvoq 45mg prolonged-release tablets. AbbVie Ltd. Revised August 2022.
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