List Of Medications For Lupus (SLE)

Medications for Lupus are aimed to improve the patient’s symptoms, prevent disease flares, and prevent the target organs from inflammatory damage.

Until very recently, corticosteroids and NSAIDs were the only medications used to treat patients with Lupus. These drugs are associated with significant side effects including kidney damage, diabetes, and hypertension which can also occur in patients with SLE.

Some of the latest FDA-approved drugs are very effective and targeted, however, they may further suppress the immune system and increase the risks of infections.

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New Medications for Lupus:

Among the newly approved medication for Lupus, Anifrolumab, and Voclosporin are the latest approved drugs.

Here is a table of the FDA-approved drugs for lupus that have recently been approved:

Class	Medications for Lupus	Date of Approval
Interferon antagonist	Anifrolumab	2^nd August 2021
Calcineurin Inhibitor	Voclosporin	22^nd January 2021
B-cell depleting drugs	Rituximab	Not FDA Approved
a human monoclonal antibody that targets BLyS (B lymphocyte stimulator)	Belimumab	9^th March 2011

In addition, the JAK-STAT inhibitor, Baricitinib (Olumiant) is also being studied for the treatment of Lupus. However, it has not been approved for the treatment of SLE by the FDA until today.

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Medication for Lupus:

Apart from corticosteroids and NSAIDs which are briefly reviewed at the end, all the FDA-approved medications for Lupus are given in the table below:

Class	Medications for Lupus
Antimalarials	Hydroxychloroquine
DMARDs, Immunomodulators	Cyclophosphamide
	Methotrexate
	Mycophenolate
Immunoglobulins	IVIG
B-cell depleting therapy	Rituximab
Other Novel Antirheumatics	Belimumab
Interferon Antagonists	Anifrolumab
Calcineurin Inhibitors	Voclosporin

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Hydroxychloroquine for Lupus:

Hydroxychloroquine (Plaquenil) is the cornerstone medicine for the treatment of Lupus. It reduces inflammation and hence improves symptoms of pain and rash.

It also protects the skin, heart, lungs, and kidneys from inflammatory damage and is used in combination with other strong medications to prevent organ damage.

Hydroxychloroquine also prevents blood clots in the vessels and is one of the safest medications that is used to treat lupus.

Generic Name	Hydroxychloroquine sulfate
Trade Name	Plaquenil
Company Name	Concordia Pharmaceuticals Inc
Date of Approval	1956 [ref]
Mechanism of action of Plaquenil:
Antimalarial drugs like hydroxychloroquine have several pharmacological activities that may contribute to their therapeutic benefit in treating systemic lupus erythematosus, while the exact nature of each activity is unknown. These include: interactions with sulphydryl groups, suppression of enzymes activity (such as phospholipase, NADH-cytochrome C reductase, cholinesterase, proteases, and hydrolases), DNA binding, stabilization of lysosomal membranes, inhibition of prostaglandin synthesis, inhibition of polymorphonuclear cell chemotaxis and phagocytosis, potential suppression of neutrophil superoxide release and interference with interleukin 1 synthesis from monocytes
Uses of Plaquenil:
It is used to treat systemic lupus erythematosus (SLE), and discoid lupus erythematosus.
Major Contraindications:
Hypersensitivity to 4-aminoquinoline derivatives

Hydroxychloroquine (Plaquenil) is used as one of the first-line medications for Lupus and is continued until the patient can not tolerate it.

Advantages and disadvantages of using Hydroxychloroquine for Lupus:

Advantages	Disadvantages of Hydroxychloroquine for Lupus
Reduces inflammation and pain	Can cause gastrointestinal upset, such as nausea, vomiting, and diarrhea
Prevents disease flares	May cause changes in vision or color perception, particularly in high doses or with long-term use
Protects against organ damage	May cause skin rashes or itching
Reduces risk of blood clots	Rarely, may cause serious side effects such as heart or liver damage
Can be taken long-term	Not effective for all people with SLE
Low cost	May interact with other medications or medical conditions
Generally well-tolerated	Rarely, may cause severe allergic reactions or other serious side effects

The EULAR guidelines recommend adding Hydroxychloroquine to the treatment regimen of all patients with Lupus.

In addition, Hydroxychloroquine is also the first-line medication for Lupus with skin involvement. It is also recommended as an adjunctive treatment for patients with lupus nephritis.

The EULAR also recommends continuing Hydroxychloroquine during pregnancy. It has been shown to prevent flares and improve survival in all patients with lupus.

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Cyclophosphamide (Cytoxan) for Lupus:

Cyclophosphamide is a strong immunosuppressive drug. However, because of the toxicities associated with it, it is only used in life-threatening or organ-threatening lupus flares.

It is also used as a rescue therapy in patients who are non-responsive to other first-line of medications.

Cyclophosphamide is considered the first-line treatment for patients with lupus nephritis. It may be used in combination with mycophenolate mofetil in patients with severe lupus nephritis.

Generic Name	Cyclophosphamide
Trade Name	Cytoxan
Company Name	Pfizer Laboratories LTD
Date of Approval
Mechanism of action of Cyclophosphamide:
Metabolites inhibit malignant cell growth by cross-linking tumor cell DNA; the medicine has no specificity for any phase of the cell cycle; and it also has strong immunosuppressive properties.
Uses of Cyclophosphamide:
It is used for the therapy of SLE.
Major Contraindications:
Hypersensitivity Urinary outflow obstruction Severe myelosuppression.

Cyclophosphamide has also been used in combination with Rituximab and methylprednisolone in patients with refractory lupus.

Cyclophosphamide may also be used in the emergency department if lupus is complicated by any of the following conditions:

Lupus cerebritis or CNS involvement
Lupus vasculitis
Severe thrombocytopenia with TTP-like picture
Rapidly progressive glomerulonephritis
Diffuse alveolar hemorrhage.

It is important to note that Cyclophosphamide should be strictly avoided during pregnancy.

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Methotrexate for Lupus:

Methotrexate is an immunosuppressive drug. It is widely used as a steroid-sparing drug in various conditions such as Rheumatoid arthritis.

In patients with Lupus, the EULAR recommends using Methotrexate or Azathioprine in patients who are non-responsive to corticosteroids and hydroxychloroquine.

Generic Name	Methotrexate
Trade Name	Trexall, Otrexup, Rasuvo
Company Name	Pfizer Laboratories LTD
Date of Approval
Mechanism of action of Methotrexate:
Methotrexate inhibits dihydrofolic acid reductase; blocks purine and thymidylic acid production, interfering with DNA synthesis, repair, and cellular replication; The S phase of the cell cycle is unique. It has the potential to stop the fast proliferation of epithelial cells in the skin.
Uses of Methotrexate:
Methotrexate is used to treat systemic lupus erythematosus patients who have not responded to other treatments due to its potential risks and side effects.
Major Contraindications:
Hypersensitivity, serious reaction observed. Pregnant women with nonmalignant illness.

Methotrexate may also be used for refractory antibody-positive lupus in patients in combination with Belimumab (Benlysta).

It is strictly contraindicated in pregnant women.

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Azathioprine for Lupus:

Azathioprine is a commonly used immunosuppressive drug. The EULAR recommends using it in patients with SLE who have persistent symptoms despite prednisolone and hydroxychloroquine.

Azathioprine is used in Lupus patients who have severe thrombocytopenia and are not responsive to prednisolone.

It may also be used as a maintenance therapy for patients with lupus nephritis. It is also used in combination with glucocorticoids for the maintenance treatment of proliferative lupus nephritis.

The 2021 KDIGO guideline recommends using Mycophenolate mofetil (Cellcept) as the first line of maintenance treatment for Class III and Class IV Lupus nephritis. Azathioprine may be used as an alternative to mycophenolate.

Generic Name	Azathioprine
Trade Name	Azasan, Imuran
Company Name	Prometheus Laboratories Inc.
Date of Approval
Mechanism of action of Azathioprine:
Purine antimetabolite transformed to 6-MP; may limit DNA, RNA, and protein synthesis; disrupts cellular metabolism; may inhibit mitosis.
Uses of Azathioprine:
Azathioprine is a drug used for the treatment of autoimmune disorders, such as systemic lupus erythematosus, as well as for organ transplantation
Major Contraindications:
Pregnancy, lactation Documented hypersensitivity Patients with RA who were previously treated with alkylating agents.

Azathioprine is one of the immunosuppressants that can be used by pregnant women in addition to glucocorticoids and hydroxychloroquine.

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Mycophenolate (Cellcept) for Lupus:

Mycophenolate is a strong immunosuppressant drug. It is indicated in the treatment of lupus patients with the renal and non-renal disease.

It is, however, not indicated in lupus cerebritis and is also contraindicated in pregnancy.

Generic Name	Mycophenolate Mofetil
Trade Name	Cellcept, Myfortic
Company Name	Roche Pharmaceuticals.
Date of Approval
Mechanism of action of Mycophenolate Mofetil:
Mycophenolic acid, the active metabolite of mycophenolate, inhibits the development of cytotoxic T-cells and antibodies as well as T-cell and B-cell proliferation. Acts as a selective, reversible, noncompetitive inhibitor of inosine monophosphate dehydrogenase (IMPDH).
Uses of Mycophenolate Mofetil:
Mycophenolate mofetil is used for the treatment of autoimmune disorders, such as systemic lupus erythematosus, and the prophylaxis of organ rejection in transplant recipients.
Major Contraindications:
IV formulation (Cellcept) in patients allergic to polysorbate 80. Hypersensitivity

Mycophenolate is also recommended in lupus nephritis at a dose of 1 gm twice daily with the newly-approved Volcosporin.

In addition, some physicians prefer Mycophenolate to Azathioprine for the long-term treatment of patients with lupus.

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Immune globulin IV (IGIV) for Lupus:

Intravenous immunoglobulins may be given to patients with lupus-associated immune thrombocytopenia.

It is recommended in the emergency setup for patients with severe thrombocytopenia of less than 30,000/ul.

Generic Name	Immune globulin IV (IVIG)
Trade Name	Bivigam, Carimune, Gammagard S/D, Felbogamma, Gamunex-C
Company Name	Baxalta US Inc
Date of Approval
Mechanism of action of Immune globulin IV (IVIG):
Human immune globulins collected from donors are used as replacement therapy for both primary and secondary immunodeficiencies; they may interfere with Fc receptors on reticuloendothelial system cells for autoimmune disorders like cytopenias and ITP; and they may provide passive immunity by raising antibody titers and the likelihood of antigen-antibody reactions
Uses of Immune globulin IV (IVIG):
It is used to treat systemic lupus erythematosus
Major Contraindications:
Hyperprolinemia (Privigen) Hypersensitivity to gamma globulin, thimerosal Isolated IgA deficiency

IVIG use is associated with an increased risk of fluid overload and heart failure. It should be administered as a slow intravenous infusion in a hospital setting where treatment for anaphylactic reactions is available.

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Rituximab for Lupus:

Rituximab is not an FDA-approved treatment for lupus. However, it is considered in severe cases of lupus with renal or brain involvement.

It is usually administered when other first-line therapies fail to induce remission. It is indicated for refractory lupus nephritis.

Generic Name	Rituximab
Trade Name	Rituxan
Company Name	IDEC Pharmaceuticals
Date of Approval
Mechanism of action of Rituximab:
A humanized monoclonal antibody that binds to the CD20 antigen and causes complement- or antibody-mediated cytolysis.
Uses of Rituximab:
Rituximab is another medication used to treat SLE.
Major Contraindications:
None

Rituximab is also being studied in combination with other novel therapies such as Dapirolizumab pegol and Abatacept.

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Belimumab (Benlysta) for Lupus:

Belimumab is a human monoclonal antibody that inhibits a protein responsible for activating B-lymphocytes, hence the name, a B-lymphocyte stimulator-specific inhibitor.

It is recommended by the EULAR guidelines for all patients who have active lupus despite using the first-line medication for lupus.

Belimumab has been proven to significantly affect the outcome of patients with frequent lupus flares. It can be used in combination with other immunosuppressive therapies in patients who are not responding and whose disease is progressing.

Generic Name	Belimumab
Trade Name	Benlysta
Company Name	GlaxoSmithKline (GSK)
Date of Approval	March 2011 [ref]
Mechanism of action of Belimumab:
Belimumab acts by inhibiting the action of a protein known as a B-lymphocyte stimulator (BLyS), which is implicated in the creation of autoantibodies and the development of inflammation in SLE. Belimumab identifies and binds to BLyS, suppresses BLyS-stimulated B-cell growth, and finally restores the ability of autoantibody-producing B cells to undergo the normal apoptotic process (programmed cell death).
Uses of Belimumab:
Belimumab is another medicine used to treat systemic lupus erythematosus.
Major Contraindications:
Anaphylaxis to belimumab

Belimumab (Benlysta) has also been approved, along with Voclosporin, in combination with Cellcept (Mycophenolate) for the treatment of active lupus nephritis.

Advantages and disadvantages of using belimumab in patients with SLE:

Advantages of Belimumab	Disadvantages of Benlysta (Belimumab)
Effective in reducing disease activity and flares	Not effective for all people with SLE
May improve symptoms such as joint pain and fatigue	May increase the risk of infections
Can be taken with other SLE medications	May cause allergic reactions, such as hives or swelling
Administered by intravenous infusion or self-injection	May cause infusion or injection reactions, such as skin rash or itching
No known interactions with other medications	May cause flu-like symptoms, such as fever or headache
Generally well-tolerated	Rarely, may cause serious side effects such as depression or suicidal thoughts
Can be used long-term	Cost may be a barrier for some people

It is noteworthy that Belimumab (Benlysta) may not be of benefit to patients who have advanced kidney disease and proteinuria of more than 3 gm/day.

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Anifrolumab for Lupus:

Anifrolumab (Saphnelo) is a human IgGk monoclonal antibody that inhibits the activity of all type 1 INFs by binding to its receptors and inhibiting its function.

It is indicated for moderate to severe Lupus. It has been found effective in patients with lupus regardless of the interferon levels.

Generic Name	Anifrolumab
Trade Name	Saphnelo
Company Name	AstraZeneca
Date of Approval	July 2021[ref]
Mechanism of action of Anifrolumab:
Anifrolumab is a monoclonal antibody that works by targeting the type I interferon (IFN-I) pathway. This pathway is overactive in patients with systemic lupus erythematosus (SLE), leading to inflammation and tissue damage. Blocking type 1 IFN receptor-mediated communication prevents the production of IFN-responsive genes as well as subsequent inflammatory and immune responses. Preventing type 1 IFN normalizes peripheral T-cell subsets and prevents the development of plasma cells.
Uses of Anifrolumab:
Anifrolumab is used for the treatment of moderate to severe active systemic lupus erythematosus (SLE) in adults.
Major Contraindications:
Anaphylaxis history related with anifrolumab

Anifrolumab (Saphnelo) has been associated with a reduction in disease severity.

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Voclosporin (Lupkynis) for Lupus Nephritis

Voclosporin is a calcineurin inhibitor that is mainly used for the treatment of lupus nephritis. Early treatment with Voclosporin prevents irreversible kidney damage and results in better long-term clinical outcomes in patients with lupus nephritis.

It is reported to be more stable and highly potent as compared to cyclosporin. [ref]

Generic Name	Voclosporin
Trade Name	Lupkynis
Company Name	Aurinia Pharmaceuticals Inc.
Date of Approval	January 2021 [ref]
Mechanism of action of Voclosporin:
Voclosporin suppresses the hyperactive immune response that causes inflammation and damage to many organs and tissues in the body in systemic lupus erythematosus (SLE) by inhibiting calcineurin. Voclosporin helps to lessen the signs and symptoms of SLE and enhance kidney function by calming the immune system.
Uses of Voclosporin:
Voclosporin is used in the therapy of SLE.
Major Contraindications:
Hypersensitivity to Voclosporin and its excipients. Coadministration of potent CYP3A4 inhibitors (eg, itraconazole, ketoconazole, clarithromycin)

Voclosporin is recommended as an add-on to the background immunosuppressive therapy in patients with severe lupus nephritis. However, it should be avoided in patients with a GFR of less than 45 ml/minute.

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Methylprednisolone for Lupus:

Methylprednisolone is one of the most potent glucocorticosteroids. It is available as an injectable medicine for intravenous and intramuscular use.

It is particularly used for lupus flares and lupus-associated organ damage such as severe lupus nephritis and lupus cerebritis as pulse therapy.

Generic Name	Methylprednisolone
Trade Name	A-Methapred, Medrol, Solu-Medrol, Depo-Medrol
Company Name	Pfizer laboratories LTD
Date of Approval
Mechanism of action of Methylprednisolone:
A potent glucocorticoid with negligible to zero mineralocorticoid activity. Maintains fluid and electrolyte balance and modifies the metabolism of carbohydrates, proteins, and lipids. Regulates or prevents inflammation by modulating the rate of protein synthesis, preventing the migration of fibroblasts and polymorphonuclear leukocytes (PMNs), reversing capillary permeability, and stabilizing lysosomes at the cellular level.
Uses of Methylprednisolone:
It is used to treat SLE, rheumatoid arthritis, and inflammatory bowel disease.
Major Contraindications:
Intrathecal administration Traumatic brain injury (high doses) Untreated severe infections Hypersensitivity to the medication or its components that have been documented (e.g., lactose monohydrate from cow milk). Fungal infection in the body (except intra-articular injection in localized joint conditions). Premature infants (formulations containing benzyl alcohol only). In individuals taking immunosuppressive doses of corticosteroids, administration of live or live, attenuated vaccinations is contraindicated. In idiopathic thrombocytopenic purpura, the intravenous approach is not recommended.

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Prednisone for Lupus:

Prednisone and prednisolone are glucocorticoids that are available for oral use. Prednisolone is usually given as a maintenance treatment as an adjunct to DMARDs and Biological therapies.

Generic Name	Prednisone
Trade Name	Rayos, Prednisone Intensol
Company Name	Horizon Pharma, Inc.
Date of Approval
Mechanism of action of
Prednisone is a Glucocorticosteroid; evokes mild mineralocorticoid activity and moderate anti-inflammatory effects; controls or restricts inflammation by regulating protein synthesis, reversing capillary permeability, suppressing migration of polymorphonuclear leukocytes (PMNs) and fibroblasts, and stabilizing lysosomes at the cellular level; Corticosteroids are given in physiologic amounts to replace low levels of endogenous hormones, and at higher (pharmacologic) dosages, they reduce inflammation
Uses of
Prednisone is used to treat conditions such as systemic lupus erythematosus (SLE), rheumatoid arthritis, and other inflammatory conditions.
Major Contraindications:
Untreated severe infection Documented hypersensitivity Administration of live or attenuated live vaccine Varicella

Prednisolone is usually recommended for arthritis, serositis, and hematological disease associated with lupus.

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Medications for Lupus Pain:

Lupus or SLE is a condition with arthritis, joint pains, muscle pains, and visceral pains as among the most common symptoms associated with lupus.

NSAIDs are among the most commonly used medications to relieve pain and inflammation. However, their use should be limited to minimize the gastrointestinal side effects and cardiovascular and renal adverse effects of these drugs.

Ibuprofen for Lupus Pain:

Ibuprofen (Advil) is one of the commonly used NSAIDs. It has a short onset of action and is a relatively safe medicine for patients at risk of renal impairment.

Generic Name	Ibuprofen
Trade Name	Advil, Motrin
Company Name	Pfizer Inc., Wyeth Pharmaceuticals Company
Date of Approval
Mechanism of action of Ibuprofen:
Inhibits prostaglandin formation in bodily tissues by inhibiting at least two cyclo-oxygenases (COX) isoenzymes, COX-1 and COX-2. It may block chemotaxis, modify lymphocyte activity, decrease proinflammatory cytokine activity, and inhibit neutrophil aggregation; these effects may contribute to anti-inflammatory efficacy.
Uses of Ibuprofen:
SLE is another condition for which ibuprofen is occasionally used
Major Contraindications:
Hypersensitivity to medication, other NSAIDs, or excipients. Perioperative discomfort in the setting of coronary artery bypass graft (CABG) surgery.

Ibuprofen, like all other NSAIDs, should be avoided in the last trimester of pregnancy.

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Naproxen (Aleve) for Lupus Pain:

Naproxen is another very potent pain medicine. It also relieves inflammation and improves most symptoms of arthritis in patients with lupus.

Naproxen is more potent in relieving pain compared to ibuprofen and acetaminophen. It may have a slight edge over diclofenac in terms of safety in patients with cardiovascular diseases.

Generic Name	Naproxen
Trade Name	Aleve, Anaprox, Naprosyn
Company Name	Bayer HealthCare
Date of Approval
Mechanism of action of Naproxen:
Inhibits prostaglandin formation in bodily tissues by inhibiting at least two cyclooxygenases (COX) isoenzymes, COX-1 and COX-2. These effects may contribute to anti-inflammatory efficacy by inhibiting chemotaxis, altering lymphocyte function, decreasing proinflammatory cytokine activity, and inhibiting neutrophil aggregation.
Uses of Naproxen:
Naproxen is commonly used to relieve pain, reduce inflammation, and lower fever associated with lupus.
Major Contraindications:
Aspirin allergy Preoperative discomfort in the setting of coronary artery bypass graft (CABG) surgery Late pregnancy Renal impairment Hepatic disease Peptic ulcer Delayed esophageal transit Bleeding disorder Stomatitis

Naproxen is also available in combination with other medications like sumatriptan which may be a preferred medicine for patients with lupus and migraine.

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Diclofenac for Lupus Pain:

Diclofenac is a non-selective NSAID. It is one of the most commonly used pain medicines. However, like all NSAIDs, it is also associated with gastrointestinal, cardiovascular, and renal adverse outcomes.

Generic Name	Diclofenac
Trade Name	Voltaren XR, Cataflam
Company Name	GlaxoSmithKline (GSK)
Date of Approval
Mechanism of action of Diclofenac:
Inhibits cyclooxygenase (COX)-1 and COX-2, consequently inhibiting prostaglandin production. It may also suppress neutrophil aggregation/activation, chemotaxis, proinflammatory cytokine levels, and alter lymphocyte activity.
Uses of Diclofenac:
It is typically used as an adjunctive treatment in conjunction with other medications that target the autoimmune process in SLE.
Major Contraindications:
Hypersensitivity (e.g., anaphylaxis, severe skin responses) to diclofenac or any of the product’s components Asthma, urticaria, or other allergic-type symptoms after taking aspirin or other NSAIDs in the past During coronary artery bypass graft (CABG) surgery Zipsor capsules are not recommended for those with a history of bovine protein hypersensitivity.