Mayzent 0.25 Mg Starter Pack
Mayzent 0.25 Mg Starter Pack Uses, Dosage, Side Effects, Food Interaction and all others data.
Mayzent 0.25 Mg Starter Pack, also known as Mayzent, by Novartis, is a new drug formulated for the management of Multiple Sclerosis (MS). It was approved by the FDA on March 26, 2019 and by Health Canada on February 20, 2020. This drug is considered a sphingosine-1-phosphate (S1P) receptor modulator and is thought to play a role in suppressing the central nervous system inflammation that is associated with MS .
Multiple Sclerosis (MS) is an autoimmune disease of the central nervous system that is chronic and inflammatory, disrupting communication between the brain and other parts of the body. Most patients diagnosed with this illness experience their initial disease symptoms between the age of 20 to 40, often the most productive years of life. Symptoms may include but are not limited to fatigue, gait changes, bowel or bladder dysfunction, abnormal muscle twitching, vision disturbance, and depressing or mood swings. MS is one of the most common causes of neurological disability in young adults and is found to occur more frequently in women than in men.
Immune system effects
| Trade Name | Mayzent 0.25 Mg Starter Pack |
| Availability | Prescription only |
| Generic | Siponimod |
| Siponimod Other Names | Siponimod |
| Related Drugs | Mayzent, Gilenya, Tysabri, Vumerity, Copaxone, Tecfidera, Aubagio, Avonex |
| Type | |
| Formula | C29H35F3N2O3 |
| Weight | Average: 516.605 Monoisotopic: 516.259977484 |
| Protein binding | Protein binding of siponimod is higher than 99.9% in healthy patients as well as hepatic and renal impaired patients . Because of the high plasma protein binding of siponimod, hemodialysis is not likely to change the total and unbound siponimod concentration and no dose adjustments are expected based on this . |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Mayzent 0.25 Mg Starter Pack is a medication used to treat relapsing multiple sclerosis.
This drug is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease in adults .
Mayzent 0.25 Mg Starter Pack is also used to associated treatment for these conditions: Relapsing Multiple Sclerosis (RMS)
How Mayzent 0.25 Mg Starter Pack works
Inflammation of the white and gray matter tissues in the central nervous system caused by localized immune cell infiltration and their cytokines are the initial cause of damage in MS. B lymphocytes and their cytokines are other factors in the pathogenesis of MS. Lymphotoxin [or transforming growth factor beta (TGF-β)] and TNF-α produced by these cells encourage inflammation . The S1P receptor is an important receptor related to the function of lymphocytes and can be found in the central nervous system . S1P receptor (S1PR) signaling is associated with a wide variety of physiological processes for lymphocytes, including their egress and recirculation .
Mayzent 0.25 Mg Starter Pack is classified as a sphingosine-1-phosphate (S1P) receptor modulator. Mayzent 0.25 Mg Starter Pack binds with high affinity to both S1P receptors 1 and 5. This drug blocks the ability of lymphocytes to release from the lymph nodes, decreasing the number of lymphocytes found in the peripheral blood. The mechanism by which siponimod exerts therapeutic effects in multiple sclerosis is not known at this time, but may involve the abovementioned decrease of lymphocytes into the central nervous system, decreasing the inflammatory effects of MS .
Toxicity
Carcinogenesis
Oral carcinogenicity studies of siponimod were performed in mice and rats. There was an increase in malignant lymphoma in females at all doses and in hemangiosarcoma and combined hemangioma and hemangiosarcoma at all doses in males and females. The lowest dose tested is approximately 5 times the recommended human dose (RHD) of 2 mg/day .
Mutagenesis
Mayzent 0.25 Mg Starter Pack was negative in several in vitro (Ames, chromosomal aberration in mammalian cells) and in vivo (micronucleus in mouse and rat) assays .
Impairment of fertility
When siponimod was administered orally (0, 2, 20, or 200 mg/kg) to male rats (mated with untreated females) before and throughout the mating period, there was a dose-related increase in the precoital interval at any dose. A decrease in implantation sites, an increase in preimplantation loss, and a decrease in the number of viable fetuses were noted at the highest dose tested. The higher no-effect dose for adverse effects on fertility (20 mg/kg) is approximately 100 times the recommended human dose .
When siponimod was administered orally (0, 0.1, 0.3, or 1 mg/kg) to female rats (mated with untreated males) prior to and during mating, and continuing to Day 6 of gestation, no effects on fertility were noted up to the highest dose studied (1 mg/kg). Plasma siponimod exposure (AUC) at the highest dose studied is about 16 times that in humans at the recommended human dose .
Use in pregnancy and lactation
Mayzent 0.25 Mg Starter Pack may cause fetal harm, based on the results of animal studies. Because it takes about 10 days to eliminate this drug from the body, women of childbearing potential should use adequate contraception to avoid pregnancy during and for 10 days after the cessation of treatment . No data currently exist regarding the presence of siponimod in human milk . A study in lactating rats demonstrated excretion of the drug and/or its metabolites in milk. The benefits nursing should be considered as well as the mother’s clinical requirement for this drug and any possible adverse effects on the breastfed infant from siponimod .
Food Interaction
- Avoid St. John's Wort. Avoid the use of St. John's wort in patients with CYP2C9 genotype *1/*3 and*2/*3.
- Take with or without food.
Mayzent 0.25 Mg Starter Pack Drug Interaction
Major: hydroxyzine, sotalolModerate: fluticasone / vilanterolMinor: sulfamethoxazole / trimethoprimUnknown: charcoal, phenazopyridine, calcium / vitamin d, ubiquinone, docusate, copper gluconate, estradiol topical, ethanol, omega-3 polyunsaturated fatty acids, fluticasone nasal, fluticasone, chondroitin / glucosamine / methylsulfonylmethane, heparin, vitamin a topical, bioflavonoids, cholecalciferol
Mayzent 0.25 Mg Starter Pack Disease Interaction
Major: cardiovascular diseaseModerate: encephalopathy, MS, infections, liver disease, macular edema, vaccinations
Volume of Distribution
Mayzent 0.25 Mg Starter Pack distributes to body tissues with an average volume of distribution of 124 L. Mayzent 0.25 Mg Starter Pack fraction mesaured in plasma is 68% in humans. Animal studies demonstrate that siponimod readily crosses the blood-brain-barrier .
Elimination Route
The time (Tmax) to attain maximum plasma concentrations (Cmax) after oral administration of immediate-release oral doses of siponimod was found to be approximately 4 hours ( with a range 3 - 8 hours). Mayzent 0.25 Mg Starter Pack is heavily absorbed (at a rate greater than or equal to 70%). The absolute oral bioavailability of siponimod is about 84%. Steady-state concentrations were attained after approximately 6 days of daily administration of a single dose of siponimod .
Effects of food on absorption
Food ingestion leads to delayed siponimod absorption (the median Tmax increased by approximately 2-3 hours). Food intake has no effect on the systemic exposure of siponimod (Cmax and AUC). Therefore, siponimod may be taken without regard to food .
Half Life
The apparent elimination half-life is approximately 30 hours .
Clearance
Apparent systemic clearance of 3.11 L/h has been estimated in MS patients .
Elimination Route
Mayzent 0.25 Mg Starter Pack is eliminated from the systemic circulation mainly due to metabolism, and subsequent biliary/fecal excretion. Unchanged siponimod was not detected in urine .
Innovators Monograph
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