Drug |
Dosage |
Remarks |
Azathioprine |
Initial dose: 1-3 mg/kg/day PO in 2-3 divided doses
Maintenance dose:
<1-3 mg/kg/day or 50-100 mg/day |
Adverse Reactions
- Hematologic effects (bone marrow disorders, leukopenia, thrombocytopenia, anemia); GI effects (GI disturbance, nausea, pancreatitis, cholestasis, liver damage); Other effects (increased risk of secondary infection and neoplasia, hypersensitivity reaction)
Special Instructions
- Monitor CBC with differential and platelet, LFTs, total bilirubin, CrCl, symptoms of infection
- At least once weekly CBC on the first month; twice monthly on the second and third month, and monthly or more frequently if dosage alterations or other therapy changes are necessary
- Patient should promptly report any signs of infection, bruising or bleeding or other manifestations of bone marrow depression; most neutropenia associated with immunosuppressants occurs sporadically many months after starting therapy
- Contraindicated in patients with chickenpox/herpes zoster
- Use with caution in patients with renal or hepatic impairment
|
Cyclophosphamide |
Lupus nephritis induction dose:
500 mg IV on week 0, 2, 4, 6, 8 and 10
Organ-threatening disease: 0.75-1 g/m2 BSA IV monthly for 6 months |
Adverse Reactions
- Dermatologic effects (alopecia, skin and nails hyperpigmentation); GI effects (nausea/vomiting, mucositis); Other effects (inappropriate ADH secretion, carbohydrate metabolism disturbances, gonadal suppression, interstitial pulmonary fibrosis)
- Severe reactions: Anaphylactic reactions, bone marrow failure, severe immunosuppression, urotoxicity, cardiotoxicity, hyponatremia, hemorrhagic cystitis
Special Instructions
- Patient should promptly report any signs of infection, bruising or bleeding or other manifestations of bone marrow depression; most neutropenia associated with immunosuppressants occurs sporadically many months after starting therapy
- Contraindicated in patients with impaired bone marrow function, bladder inflammation, urinary outflow obstruction and active infections
- Use with caution in patients with renal or hepatic impairment, DM, severe immunosuppression
|
Mycophenolic acid
(Mycophenolate mofetil) |
As Mycophenolate mofetil
Organ-threatening disease or lupus nephritis induction dose: 750-1,500 mg PO 12 hourly (daily dose of up to 3 g)
Mild to moderate disease or maintenance dose of lupus nephritis: 500-1,000 mg PO 12 hourly
As Mycophenolate sodium
Induction and maintenance dose of lupus nephritis: 720 mg PO 12 hourly |
Adverse Reactions
- CV effects (hypertension, hypotension, peripheral edema, chest pain, tachycardia); CNS effects (pain, headache, insomnia, dizziness, anxiety); GI effects (abdominal pain, diarrhea, nausea/vomiting); Metabolic effects (hyperglycemia, hypercholesterolemia, hypomagnesemia, hypokalemia, hypocalcemia, hyperkalemia); Other effects (rash, fever, abnormal CBC)
Special Instructions
- Use with caution in patients with severe renal impairment, active GI disorders, and in those with intrauterine devices (due to increased risk of infection)
- Risk of infection and activation of latent viral infection is increased; neutropenia (including severe neutropenia) may occur, requiring dose reduction or interruption of treatment
|
Biologic Agents
|
Anifrolumab |
300 mg IV infusion over a 30-minute period every 4 weeks |
Adverse Reactions
- Respiratory effects (nasopharyngitis, upper respiratory tract infections, bronchitis, cough); Other effects (infusion-related reactions, herpes zoster)
- Serious hypersensitivity reactions including angioedema and anaphylaxis have been reported
Special Instructions
- Avoid initiating treatment during an active infection and avoid use of live or live-attenuated vaccines
- Before prescribing Anifrolumab, consider the individual benefit-risk in patients with known risk factors for malignancy
- Contraindicated in patients with a history of anaphylaxis with Anifrolumab-fnia
|
Belimumab |
SLE
10 mg/kg IV infused over 1 hour on days 0, 14 and 28 then every 4 weeks thereafter
or
200 mg SC once weekly
Transition from IV to SC:
Administer first SC injection 1-4 weeks after the last IV dose
Lupus Nephritis
10 mg/kg IV infused over 1 hour every 2 weeks for the first 3 doses then every 4 weeks thereafter
or
Initial therapy with Belimumab:
400 mg (two 200-mg injections) SC once weekly for 4 doses, then 200 mg SC once weekly thereafter
Continuing therapy with Belimumab: 200 mg SC once weekly
Transition from IV to SC:
May transition any time after receipt of the first 2 IV doses
Administer first SC dose of 200 mg 1-2 weeks after the last IV dose |
Adverse Reactions
- CNS effect (migraine); GI effects (nausea, diarrhea); Psychological effects (suicide/suicidal ideation, depression); Dermatologic effects (rash, urticaria, pruritus, hypersensitivity reaction), Respiratory effects (upper respiratory tract infection, bronchitis); Other effects (fever, leukopenia, injection site reactions, urinary tract infection)
Special Instructions
- Not recommended for use in patients with severe active CNS lupus, HIV, history of/currently with hepatitis B/C, hypogammaglobulinemia or IgA deficiency, history of major organ transplant, hematopoietic stem cell/marrow transplant, or renal transplant
- Patient's condition should be evaluated continuously
- Should not be administered as an IV bolus
|
Calcineurin Inhibitors |
Tacrolimus
|
Lupus nephritis:
1-3 mg PO 24 hourly |
Adverse Reactions
- CNS effects (headache, tremor, paresthesia, hearing loss, visual disturbances, peripheral neuropathies, convulsions); CV effects (hypertension, cardiac arrest, heart failure, ventricular arrhythmias, palpitations, cardiomyopathies); GI effects (nausea, diarrhea, dyspepsia, constipation, GI hemorrhage and ulceration); Respiratory effects (dyspnea, parenchymal lung disorders, pleural effusions, cough, nasal congestion, pharyngitis, asthma); Dermatologic effects (acne, alopecia, skin rashes, pruritus); Musculoskeletal effects (muscle cramps, asthenia, arthralgia); Hematologic effects (pancytopenia, agranulocytosis, coagulation disorders); Other effects (renal impairment, hyperlipidemia, febrile disorders, edema, liver dysfunction)
- Potentially fatal: Polyoma virus infections, GI perforation
Special Instructions
- Use with caution in patients with renal impairment and hepatic impairment, patient with risk factors for QT prolongation
- Monitor for infections, ECG, BP, FBS, hematological, neurological (including visual) and coagulation parameters, electrolytes, hepatic and renal function, whole blood Tacrolimus trough concentration (especially during diarrhea episodes)
|
Voclosporin
|
Lupus nephritis:
23.7 mg PO 12 hourly |
Adverse Reactions
- GI effects (diarrhea, abdominal pain, dyspepsia, mouth ulceration); Renal effects (decreased GFR, renal impairment, acute kidney injury); Other effects (hypertension, headache, anemia, cough, UTI, alopecia, fatigue, tremor, decreased appetite)
Special Instructions
- Establish an accurate baseline estimated GFR (eGFR) and check BP prior to starting Voclosporin; modify dose based on eGFR
- Contraindicated in patients with known serious or severe hypersensitivity reaction to Voclosporin or any of its excipients, concomitantly using Ketoconazole, Itraconazole or Clarithromycin
- Use with caution in patients with risk factors for hyperkalemia or QT prolongation
- Monitor for neurologic abnormalities, drug interactions, renal function, serum potassium levels
- Consider discontinuing therapy if without therapeutic benefit by 24 weeks
- Avoid live vaccines
|