etrasimod
Velsipity
Pharmaceutical company: Pfizer, Inc.
Pharmacologic classification: Sphingosine 1-phosphate (S1P) receptor modulator
Therapeutic classification: Immunosuppressant
AVAILABLE FORMS
Tablets: 2 mg
INDICATIONS AND DOSAGES
Moderately to severely active ulcerative colitis
Adults: 2 mg PO once daily.
CONTRAINDICATIONS AND CAUTIONS
- Contraindicated in patients who experienced MI, unstable angina pectoris, stroke, transient ischemic attack, decompensated heart failure (HF) requiring hospitalization, or Class III or IV HF in the last 6 months.
- Contraindicated in patients with a history or presence of Mobitz type II second-degree or third-degree AV block, sick sinus syndrome, or SA block, unless the patient has a functioning pacemaker.
- This drug may result in a transient decrease in heart rate (HR) and AV conduction delays. Consider cardiology consultation prior to initiating treatment for patients with significant QT prolongation, arrythmias requiring treatment with Class Ia or Class III anti-arrhythmic drugs or QT-prolonging drugs, unstable ischemic heart disease, Class I or II HF, history of cardiac arrest, cerebrovascular disease, or uncontrolled hypertension, resting HR less than 50, history of symptomatic bradycardia, recurrent cardiogenic syncope, severe untreated sleep apnea, or history of Mobitz type I second-degree AV block, unless the patient has a functioning pacemaker.
- Alert: Life-threatening and rare, fatal infections have occurred in association with other S1P receptor modulators. Wait to initiate treatment in patients with an active infection until infection is resolved. Consider interrupting or stopping treatment if a serious infection develops.
- Progressive multifocal leukoencephalopathy (PML) has been reported in patients with multiple sclerosis (MS) treated with S1P receptor modulators. If suspected, treatment should be paused and discontinued if confirmed.
- Immune reconstitution inflammatory syndrome (IRIS) has been reported in patients with MS who developed PML while being treated with S1P receptor modulators and subsequently discontinued treatment. Symptom onset is generally within a few months after treatment discontinuation and presents as clinical decline that may be rapid, can lead to serious neurologic complications, or death, and is often associated with characteristic changes on MRI.
- This drug may increase the risk of infection. Patients without a confirmed history of varicella or who have not been fully vaccinated against varicella zoster virus should be tested for antibodies to varicella zoster virus before initiating treatment.
- Fatal cryptococcal meningitis and disseminated cryptococcal infections have been reported with S1P receptor modulators. If suspected, treatment should be paused, and the patient should undergo diagnostic evaluation.
- Use isn't recommended in patients with Child-Pugh class C liver impairment.
- This drug may increase the risk of macular edema or malignancy (including skin malignancy), may increase blood pressure, or cause a decline in pulmonary function
- This drug may increase the risk of developing posterior reversible encephalopathy syndrome. Delay in diagnosis and treatment may lead to permanent neurologic sequelae.
- If patients have received immunosuppressive or immunomodulating drugs prior to starting etrasimod, consider the half-life and mode of action of prior therapies as unintended additive immune system effects may occur.
- Lymphocyte counts take 4 to 5 weeks to return to normal range after stopping drug. If the patient is receiving concomitant immunosuppressants, they remain at increased risk for infectious complications up to 5 weeks after the last dose of etrasimod.
- Use isn't recommended in patients who are CYP2C9 poor metabolizers.
- Safety and effectiveness in children haven't been established.
- Dialyzable drug: Unknown.
PREGNANCY-LACTATION-REPRODUCTION
- This drug may cause fetal harm. Patients of reproductive potential should use effective contraception during treatment with the drug and for one week following the last dose.
- There are no data on the presence of etrasimod in human milk. Animal studies suggest the drug is excreted in milk. Weigh risk versus benefit if use is necessary.
- Health care providers are encouraged to enroll patients in the Velsipity pregnancy exposure registry by calling 1-800-616-3791.
INTERACTIONS
Drug-drug. Antineoplastics, immunomodulators (cyclosporine), noncorticosteroid immunosuppressants (adalimumab, sirolimus): May increase immunosuppression. Avoid use together.
Beta blockers (metoprolol), calcium channel blockers (amlodipine, verapamil): May increase bradycardic effects. Seek cardiologist's advice before initiating drugs that may further decrease HR.
Combined strong CYP3A4, moderate CYP2C8, and moderate CYP2C9 inducer (rifampin): May decrease etrasimod level. Avoid use together.
Class Ia and Class III antiarrhythmics (quinidine, procainamide, amiodarone, sotalol), QT-prolonging drugs (ciprofloxacin, ketoconazole, amitriptyline, haloperidol, methadone): May increase the risk of QT prolongation and torsades de pointes. Seek cardiologist's advice before use together.
Live attenuated vaccines: May diminish the therapeutic effect of vaccine. Administer vaccine at least 4 weeks prior to starting etrasimod and avoid use during and for 5 weeks after treatment.
Moderate to strong inhibitors of both CYP2C9 and CYP3A4 (fluconazole): May increase etrasimod level. Avoid use together.
Drug-lifestyle. Sunlight, UV light: May increase risk of skin malignancy. Limit exposure to sunlight and UV light.
ADVERSE REACTIONS
CNS: headache, dizziness.
CV: hypertension, bradycardia.
EENT: decreased visual acuity.
GI: nausea.
GU: UTI.
Hepatic: elevated liver function tests.
Metabolic: hypercholesterolemia.
Musculoskeletal: arthralgia.
Other: herpes viral infection.
Reactions in bold italics are life-threatening.
Released: January 2024
Nursing Drug Handbook
© 2024 Wolters Kluwer
momelotinib
Ojjaara
Pharmaceutical company: GlaxoSmithKline
Pharmacologic classification: Kinase inhibitor
Therapeutic classification: Immunosuppressant
AVAILABLE FORMS
Tablets: 100 mg, 150 mg, 200 mg
INDICATIONS AND DOSAGES
Intermediate- or high-risk myelofibrosis in patients with anemia
Adults: 200 mg PO once daily.
Adjust-a-dose: In patients with Child-Pugh class C liver impairment, reduce starting dose to 150 mg PO once daily. Refer to the manufacturer's instructions for toxicity-related dosage adjustments. Discontinue the drug in patients unable to tolerate 100 mg once daily.
CONTRAINDICATIONS AND CAUTIONS
- This drug may increase the risk of serious infections, which may be fatal. Don't initiate in patients with an active infection.
- May increase hepatitis B virus (HBV) load, with or without associated elevations in ALT or AST in patients with chronic HBV. If hepatitis B surface antigen or anti-HBc antibody is positive, consultation with a liver specialist should be considered. Chronic HBV infection should be treated and monitored according to clinical HBV guidelines.
- This drug may cause liver toxicity. Delay starting therapy in patients presenting with uncontrolled acute and chronic liver disease until apparent causes have been investigated and treated as clinically indicated.
- Kinase inhibitors may increase the risk of major adverse CV events, including CV death, MI, and stroke. Use cautiously in patients who currently smoke or have a history of smoking or other CV risk factors.
- Kinase inhibitors may increase the risk of thrombosis, including deep vein thrombosis, pulmonary embolism, and arterial thrombosis.
- Kinase inhibitors may increase the risk of lymphoma and other malignancies. Use cautiously in patients with known or new malignancy and patients who currently smoke or have a history of smoking.
- Safety and efficacy haven't been established in children.
- Dialyzable drug: Unknown.
PREGNANCY-LACTATION-REPRODUCTION
- This drug may cause fetal harm and should only be used during pregnancy if the benefits outweigh fetal risk.
- Patients of childbearing potential should use highly effective contraception during therapy and for at least 1 week after the last dose.
- There is no data on the appearance of this drug in human milk, but it has been reported as present in rat milk. Breastfeeding isn't recommended during treatment and for at least 1 week after the last dose.
INTERACTIONS
Drug-drug. BCRP substrates (rosuvastatin, methotrexate, glyburide, cimetidine): May increase exposure of substrate. Initiate rosuvastatin at 5 mg and do not increase to more than 10 mg once daily. Dose adjustment of other BCRP substrates may also be needed.
OATP1B1/B3 inhibitors (cyclosporine, gemfibrozil, enalapril, cisplatin): Increases momelotinib level. Consider momelotinib dose modifications.
Vaccines (inactivated): May diminish therapeutic effect of vaccine. Administer vaccines at least 2 weeks prior to initiating momelotinib or revaccinate at least 3 months after therapy is discontinued.
Vaccines (live): May increase the risk of vaccine-associated infection and diminish the effect of vaccines. Avoid use together.
ADVERSE REACTIONS
CNS: paresthesia, dizziness, headache, fever, syncope, fatigue, neuralgia, peripheral neuropathy, peripheral motor neuropathy, polyneuropathy.
CV: arrhythmia, hypotension, hemorrhage, thrombosis, HF, peripheral edema, flushing.
EENT: blurred vision
GI: diarrhea, nausea, abdominal pain, vomiting.
GU: kidney infection, UTI, acute kidney injury.
Hematologic: thrombocytopenia, neutropenia.
Hepatic: elevated liver enzymes.
Musculoskeletal: extremity pain, back pain.
Respiratory: pneumonia, cough, respiratory failure.
Skin: pruritus, rash.
Other: bacterial infection, viral infection, fungal infection, vitamin B1 deficiency.
Reactions in bold italics are life-threatening.
Released: January 2024
Nursing Drug Handbook
© 2024 Wolters Kluwer
zilucoplan
Zilbrysq
Pharmaceutical company: UCB, Inc.
Pharmacologic classification: Complement C5 inhibitor
Therapeutic classification: Immunomodulator
AVAILABLE FORMS
Injection: 16.6 mg/0.416 mL, 23 mg/0.574 mL, 32.4 mg/0.81 mL in single-dose prefilled syringes
INDICATIONS AND DOSAGES
Generalized myasthenia gravis in patients who are anti-acetylcholine receptor antibody-positive
Adults weighing 77 kg or more: 32.4 mg subcut once daily.
Adults weighing 56 to less than 77 kg: 23 mg subcut once daily.
Adults weighing less than 56 kg: 16.6 mg subcut once daily.
CONTRAINDICATIONS AND CAUTIONS
- Boxed Warning: Meningococcal infections have occurred in patients treated with complement inhibitors. These infections may rapidly become life-threatening or fatal if not recognized and treated early. Because of the risk, zilucoplan is available only through a REMS program.
- Boxed Warning: Meningococcal vaccination (for serogroups A, C, W, and Y, and serogroup B) should be completed or updated at least 2 weeks prior to administering the first dose of this drug, unless the risk of delaying therapy outweighs the risk of developing a meningococcal infection.
- If urgent therapy is indicated in a patient who is not up-to-date with meningococcal vaccines, the patient should receive meningococcal vaccines as soon as possible and receive antibacterial drug prophylaxis.
- Boxed Warning: Patients receiving zilucoplan are at increased risk for invasive disease caused by Neisseria meningitidis, even if they develop antibodies following vaccination.
- Zilucoplan is contraindicated in patients with unresolved N. meningitidis infection.
- Patients may have increased susceptibility to infections caused by Streptococcus pneumoniae, Haemophilus influenzae, and N. gonorrhoeae. Administer vaccinations for the prevention of S. pneumoniae and H. influenzae type b according to the Advisory Committee on Immunization Practices guidelines. Even after vaccination, patients are at increased risk for infection due to these bacteria.
- Pancreatitis and pancreatic cysts have been reported.
- Safety and effectiveness in children haven't been established.
- Dialyzable drug: Unknown.
PREGNANCY-LACTATION-REPRODUCTION
- Studies during pregnancy are inadequate. Animal studies showed increased fetal risk.
- There are no data on the presence of this drug in human milk, the effects on the breastfed infant, or the effects on milk production. Use cautiously during breastfeeding.
INTERACTIONS
None reported.
ADVERSE REACTIONS
GI: nausea, vomiting, diarrhea.
GU: UTI.
Hepatic: increased lipase, increased amylase, pancreatitis, pancreatic cysts.
Respiratory: upper respiratory infection.
Skin: injection site reactions.
Reactions in bold italics are life-threatening.
Released: January 2024
Nursing Drug Handbook
© 2024 Wolters Kluwer