Usage
Adalimumab is prescribed for various autoimmune and inflammatory conditions. These include:
- Rheumatoid Arthritis: Moderate to severe active rheumatoid arthritis in adults.
- Psoriatic Arthritis: Active psoriatic arthritis in adults.
- Ankylosing Spondylitis: Active ankylosing spondylitis in adults.
- Crohn’s Disease: Moderate to severe Crohn’s disease in adults and children 6 years and older.
- Ulcerative Colitis: Moderate to severe ulcerative colitis in adults.
- Hidradenitis Suppurativa: Moderate to severe hidradenitis suppurativa in adults.
- Non-infectious Uveitis: Non-infectious intermediate, posterior, and panuveitis in adults and children 2 years of age and older.
- Plaque Psoriasis: Moderate to severe chronic plaque psoriasis in adults and children 4 years of age and older.
- Juvenile Idiopathic Arthritis:
- Polyarticular juvenile idiopathic arthritis in children 2 years of age and older.
- Enthesitis-related arthritis in children 6 years of age and older.
Pharmacological Classification: Tumor Necrosis Factor (TNF) inhibitor, Disease-Modifying Antirheumatic Drug (DMARD), Biologic
Mechanism of Action: Adalimumab works by blocking the activity of TNF-alpha, a protein that plays a key role in inflammation. By inhibiting TNF-alpha, adalimumab reduces inflammation and other disease processes in the targeted conditions.
Alternate Names
While “adalimumab” is the generic name, various brand names exist:
- Humira: This is the most widely recognized brand name globally.
- Amjevita: A biosimilar version of Humira.
- Hulio: Another biosimilar.
- Cyltezo, Hyrimoz, Abrilada, Idacio, Yusimry: Additional biosimilars.
How It Works
Pharmacodynamics: Adalimumab binds specifically to TNF-alpha, preventing its interaction with cell surface TNF receptors p55 and p75. This blockade inhibits the inflammatory cascade initiated by TNF-alpha, leading to a reduction in inflammation and symptom improvement.
Pharmacokinetics:
- Absorption: After subcutaneous injection, adalimumab is slowly absorbed, reaching peak serum concentrations in approximately 5 days.
- Metabolism: As a large protein molecule, adalimumab is primarily catabolized into small peptides and amino acids.
- Elimination: Elimination is slow, with a half-life of about 2 weeks. The major route of elimination is not fully elucidated, but likely involves systemic catabolism similar to endogenous immunoglobulins.
Mode of Action: Adalimumab acts by specifically targeting and binding to TNF-alpha, thereby neutralizing its biological activity. This involves blocking TNF-alpha from interacting with its receptors on the cell surface.
Receptor Binding: Adalimumab binds to both soluble and transmembrane forms of TNF-alpha, effectively preventing its interaction with the p55 and p75 cell surface TNF receptors.
Enzyme Inhibition/Neurotransmitter Modulation: Not applicable, as adalimumab’s primary mechanism is receptor blockade of TNF-alpha rather than enzyme inhibition or neurotransmitter modulation.
Elimination Pathways: Adalimumab is not primarily eliminated through renal or hepatic pathways. It undergoes catabolism like other endogenous immunoglobulins, resulting in small peptides and amino acids. No specific cytochrome P450 enzyme involvement has been documented.
Dosage
Standard Dosage
Adults:
Dosage and frequency depend on the specific condition. For conditions like rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis, 40 mg subcutaneously every other week is the usual dose. For other conditions like plaque psoriasis, Crohn’s disease, ulcerative colitis, hidradenitis suppurativa, and non-infectious uveitis, different dosing regimens are used, often including a loading dose followed by maintenance doses. The information provided in this answer is based on the sources as of February 16, 2025. Given the dynamic nature of medical knowledge, it is advisable to consult up-to-date guidelines and resources, such as official prescribing information.
Children:
Pediatric dosing is typically weight-based and varies depending on the condition being treated. Children with plaque psoriasis, for instance, usually receive 0.8 mg/kg (up to 40 mg) weekly for the first two doses, then every other week. For other conditions like polyarticular juvenile idiopathic arthritis or Crohn’s disease, different weight-based dosing regimens exist. Pediatric safety considerations include increased risk of infection. Specific dosage information for children must be determined and monitored by a physician.
Special Cases:
- Elderly Patients: While no specific dosage adjustments are explicitly indicated, caution is advised due to increased risk of infections.
- Patients with Renal Impairment: No specific dosage adjustments based on renal impairment are currently recommended.
- Patients with Hepatic Dysfunction: No specific dosage adjustments based on hepatic dysfunction are currently recommended.
- Patients with Comorbid Conditions: Patients with comorbidities, especially those receiving concomitant immunosuppressants like methotrexate or corticosteroids, are at higher risk of serious infections. Close monitoring and dose adjustments might be considered on a case-by-case basis.
Clinical Use Cases
Adalimumab is not typically used in acute clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. It is primarily a long-term treatment for chronic inflammatory conditions.
Dosage Adjustments
Dose modifications might be necessary depending on the individual patient’s response and tolerability. Patients with an inadequate response might require a dose increase. If a patient develops serious infections, adalimumab should be discontinued.
Side Effects
Common Side Effects:
- Injection site reactions (redness, pain, swelling, itching)
- Upper respiratory infections (cold symptoms)
- Headache
- Rash
- Nausea
Rare but Serious Side Effects:
- Serious infections (tuberculosis, sepsis, fungal infections)
- Lymphoma and other malignancies
- Liver injury
- Allergic reactions
- Nervous system disorders (e.g., optic neuritis, multiple sclerosis)
- Heart failure
Long-Term Effects:
The long-term effects of adalimumab are still being studied. Increased risk of certain cancers and serious infections are potential long-term concerns.
Adverse Drug Reactions (ADR):
Severe allergic reactions, serious infections, new or worsening heart failure, liver injury, and nervous system disorders are all clinically significant ADRs that require immediate medical attention.
Contraindications
- Active serious infections (e.g., tuberculosis, sepsis)
- Known hypersensitivity to adalimumab
Drug Interactions
- TNF blockers (e.g., etanercept, infliximab): Increased risk of serious infections.
- Immunosuppressants (e.g., methotrexate, corticosteroids): Increased risk of infections.
- Live vaccines: Concomitant use contraindicated.
- Anakinra, Abatacept: Increased risk of serious infections.
- Rituximab: Increased risk of infections.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: B (Although studies haven’t shown increased birth defects in humans, small amounts do cross the placenta, possibly increasing infection risk in the infant).
- Breastfeeding: Adalimumab passes into breast milk in small amounts. Limited information suggests minimal infant risk, but long-term effects are unknown. Data as of February 16, 2025. Consult up-to-date resources.
Drug Profile Summary
- Mechanism of Action: TNF-alpha inhibitor.
- Side Effects: Injection site reactions, infections, headache, rash. Rarely: serious infections, malignancies, liver damage.
- Contraindications: Active serious infections, hypersensitivity.
- Drug Interactions: Other TNF blockers, immunosuppressants, live vaccines, anakinra, abatacept.
- Pregnancy & Breastfeeding: Can be used during pregnancy if needed. Excreted in breast milk at low concentrations.
- Dosage: Varies depending on condition; typically 40 mg subcutaneously every other week for many conditions.
- Monitoring Parameters: Signs and symptoms of infection, liver function tests, complete blood counts.
Popular Combinations
Adalimumab is sometimes used in combination with methotrexate for rheumatoid arthritis, even though this can increase the risk of infections. This combination may improve treatment efficacy compared to adalimumab alone.
Precautions
- General Precautions: Screen for infections (e.g., TB) before and during treatment. Monitor for signs and symptoms of infection.
- Specific Populations: Close monitoring for pregnant/breastfeeding women, children, and the elderly.
- Lifestyle Considerations: No specific lifestyle restrictions are associated with adalimumab other than avoiding live vaccines.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Adalimumab?
A: The dosage depends on the condition. Common dosages include 40 mg subcutaneously every other week, but other regimens exist, sometimes with loading doses. Pediatric dosing is weight-based. Always consult prescribing information for the specific indication.
Q2: What are the most common side effects?
A: Injection site reactions, respiratory infections, headache, and rash are among the most common side effects.
Q3: What are the serious side effects to watch for?
A: Serious infections, malignancies, liver damage, allergic reactions, and nervous system disorders are rare but potentially life-threatening side effects.
Q4: Can Adalimumab be used during pregnancy?
A: Yes, if clinically needed. Although studies don’t show a significant increased birth defect risk, adalimumab crosses the placenta and could potentially increase the infant’s risk of infection.
Q5: Can Adalimumab be used during breastfeeding?
A: Adalimumab is present in breast milk in low amounts. Limited data suggest that it is acceptable during breastfeeding, but long-term effects on the infant are unknown. Information accurate as of February 16, 2025. Consult up-to-date resources for any changes.
Q6: What are the major contraindications for Adalimumab?
A: Active serious infections, such as tuberculosis, and known hypersensitivity to adalimumab are the major contraindications.
Q7: What drugs interact with Adalimumab?
A: Other TNF blockers, immunosuppressants, live vaccines, anakinra, and abatacept have clinically significant interactions with adalimumab.
Q8: How is Adalimumab administered?
A: Adalimumab is administered via subcutaneous injection using a pre-filled syringe or pen.
Q9: What are the long-term safety concerns with Adalimumab?
A: The long-term safety profile is still being investigated, but there is a potential increased risk of certain cancers and serious infections with prolonged use.
Q10: Should any specific monitoring be done for patients on Adalimumab?
A: Patients on adalimumab should be monitored for signs and symptoms of infection, and regular liver function tests and complete blood counts may be indicated.
