Fetzima (levomilnacipran HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Levomilnacipran hydrochloride, the 1S, 2R-enantiomer of racemic milnacipran hydrochloride, is a selective serotonin- and norepinephrine-reuptake inhibitor (SNRI) and an antidepressant.
Levomilnacipran hydrochloride is a selective serotonin- and norepinephrine-reuptake inhibitor (SNRI). Levomilnacipran is the more active 1S, 2R enantiomer of the SNRI milnacipran, which is a racemic mixture of the 1S, 2R and 1R, 2S enantiomers that is used in the management of fibromyalgia. The precise mechanism of the antidepressant effect of levomilnacipran is not fully understood, but is thought to be related to potentiation of serotonin and norepinephrine activity in the CNS through selective inhibition of serotonin and norepinephrine reuptake.
Levomilnacipran potently and selectively inhibits the reuptake of serotonin and norepinephrine, with preferential activity at the norepinephrine transporters. Levomilnacipran demonstrated a 2-fold preference for norepinephrine- over serotonin-reuptake inhibition in vitro. In in vitro studies, the drug lacked substantial affinity for other receptors, ion channels, or transporters tested, including serotonergic (5-HT1-7), alpha- and beta-adrenergic, muscarinic, and histaminergic receptors, and calcium, sodium, potassium, and chloride channels.
Levomilnacipran does not inhibit monoamine oxidase (MAO).
The concentration of levomilnacipran at steady state is dose-proportional over the dosage range of 25--300 mg (2.5 times the maximum recommended dosage) once daily. Interconversion between levomilnacipran and its stereoisomer does not appear to occur in humans.
Relative oral bioavailability of levomilnacipran hydrochloride extended-release capsules is 92% compared with the oral solution. The median time to achieve peak plasma concentrations of levomilnacipran is 6-8 hours following oral administration of the drug. Administration of the drug with food did not substantially affect levomilnacipran concentrations.
Levomilnacipran is widely distributed and 22% protein bound. The elimination half-life of the drug is approximately 12 hours. Levomilnacipran undergoes desethylation, which is catalyzed primarily by cytochrome P-450 (CYP) isoenzyme 3A4 with minor contributions by CYP isoenzymes 2C8, 2C19, 2D6, and 2J2, to form desethyl levomilnacipran; the drug also undergoes hydroxylation to form p-hydroxy-levomilnacipran.
Both of these oxidative metabolites further undergo glucuronide conjugation.
Following oral administration of a single radiolabeled dose of levomilnacipran solution, approximately 58% of the dose is excreted in urine as unchanged drug. The principal metabolite excreted in urine is N-desethyl levomilnacipran, which accounted for approximately 18% of the dose; other metabolites excreted in urine include levomilnacipran glucuronide (4%), desethyl levomilnacipran glucuronide (3%), p-hydroxy levomilnacipran glucuronide (1%), and p-hydroxy levomilnacipran (1%). All of these metabolites are inactive.
USES: This medication is used to treat depression. Levomilnacipran belongs to a class of drugs known as serotonin-norepinephrine reuptake inhibitors (SNRIs). It works by helping to restore the balance of certain natural substances (serotonin and norepinephrine) in the brain.
Generic name: levomilnacipran HCl
Pronunciation: (LEE-voe-mil-NA-si-pran)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Fetzima
Indications
The following indications are listed for Fetzima:
- Major Depressive Disorder
Also known as: Major Unipolar Illness, Unipolar Mood Disorder.
Dosing
Dosage of levomilnacipran hydrochloride is expressed in terms of levomilnacipran.
The maximum recommended dosage of levomilnacipran should not exceed 80 mg once daily when used concurrently with strong cytochrome P-450 (CYP) 3A4 inhibitors.
Levomilnacipran hydrochloride is administered orally; it is commercially available as extended-release capsules containing 20 mg, 40 mg, 80 mg, or 120 mg of levomilnacipran.
Administer the capsules orally once daily, with or without food, at approximately the same time each day. Swallow the capsules whole; do not open, chew, or crush.
If a dose of levomilnacipran is missed, instruct patients to take the dose as soon as it is remembered, unless it is almost time for the next scheduled dose. If it is almost time for the next scheduled dose, instruct patients to skip the missed dose and take the next dose at the regularly scheduled time. Advise patients not to take 2 doses at the same time.
Store levomilnacipran capsules at 25degreesC (excursions permitted between 15-30degreesC).
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Levomilnacipran is metabolized primarily by cytochrome P-450 (CYP) isoenzyme 3A4 with minor contributions by CYP isoenzymes 2C8, 2C19, 2D6, and 2J2. In vitro studies demonstrate that levomilnacipran does not inhibit CYP isoenzymes 1A2, 2A6, 2C8, 2C9, 2C19, 2D6, or 2E1.
Levomilnacipran is a weak substrate of P-glycoprotein (P-gp), but is not a substrate of breast cancer resistance protein (BCRP), organic anion-transporting polypeptides (OATP) 1B1 and 1B3, organic cation transporter (OCT) 2, and organic anion transporters (OAT) 1 and 3. In vitro studies demonstrate that levomilnacipran does not inhibit OATP1B1, OATP1B3, OCT2, OAT1, OAT3, or P-gp.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to levomilnacipran hydrochloride, milnacipran hydrochloride, or any ingredient in the formulation.
*Concurrent or recent (i.e., within 14 days) therapy with a monoamine oxidase inhibitor (MAOI) intended to treat psychiatric disorders. Use of an MAOI intended to treat psychiatric disorders within 7 days of levomilnacipran discontinuance.
*Initiation of levomilnacipran therapy in patients receiving MAOIs such as linezolid or IV methylene blue.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in >=5% of patients with major depressive disorder receiving levomilnacipran and at an incidence of at least twice that reported with placebo in controlled studies include nausea, constipation, hyperhidrosis, increased heart rate, erectile dysfunction, ejaculation disorder, tachycardia, vomiting, and palpitations.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
The safety and effectiveness of levomilnacipran in pediatric patients for the treatment of major depressive disorder have not been established; levomilnacipran is not approved for use in pediatric patients. In 2 randomized, double-blind, placebo- and active-controlled trials in pediatric patients (7-17 years of age) with major depressive disorder, levomilnacipran was not superior to placebo in terms of change from baseline to week 8 in the Children's Depression Rating Scale-Revised (CDRS-R) total score.
An increased risk of suicidal thoughts and behaviors was observed in pediatric patients treated with antidepressants. Additionally, pediatric patients receiving levomilnacipran were more likely to develop new-onset and sustained hypertension compared to adults in clinical trials.
There is a pregnancy exposure registry that monitors pregnancy outcomes in patients exposed to antidepressants during pregnancy. Advise patients to register by calling the National Pregnancy Registry for Antidepressants at 1-844-405-6185 or by visiting https://womensmentalhealth.org/research/pregnancyregistry/antidepressants.
Available data on levomilnacipran use in pregnant women are insufficient to assess for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. There are risks associated with untreated depression in pregnancy as well as with exposure to SNRIs, including levomilnacipran, during pregnancy.
In observational studies, exposure to SNRIs, particularly during the month before delivery, has been associated with a <2-fold increase in the risk of postpartum hemorrhage. Neonates exposed to SNRIs or SSRIs, including levomilnacipran, late in the third trimester of pregnancy have developed complications requiring prolonged hospitalization, respiratory support, and tube feeding. Clinical findings reported to date in neonates have included respiratory distress, cyanosis, apnea, seizures, temperature instability, feeding difficulty, vomiting, hypoglycemia, hypotonia, hypertonia, hyperreflexia, tremor, jitteriness, irritability, and constant crying. These findings appear to be consistent with either a direct toxic effect of SNRIs or SSRIs or, possibly, a drug withdrawal syndrome. In some cases, the clinical picture was consistent with serotonin syndrome.
In animal reproduction studies, no malformations were observed when levomilnacipran was administered during the period of organogenesis at doses up to 8 or 16 times the maximum recommended human dose (MRHD) of 120 mg on a mg/m2 basis in rats and rabbits, respectively. However, an increase in early post-natal rat pup mortality was observed at a dose equivalent to 5 times the MRHD given during pregnancy and lactation.
There are risks associated with untreated depression in pregnancy. In a prospective longitudinal study, women who discontinued antidepressant therapy during pregnancy were more likely to experience a relapse of major depressive disorder than women who continued antidepressants. Consider the risk of untreated depression when discontinuing or changing antidepressants during pregnancy and postpartum.
It is unknown whether levomilnacipran is distributed into human milk; however, racemic milnacipran is present in human milk. The effects of levomilnacipran or milnacipran on the breast-fed infant or on milk production are also unknown.
There are reports of agitation, irritability, poor feeding, and poor weight gain in infants exposed to SSRIs or SNRIs through breast milk. Monitor infants exposed to levomilnacipran for these effects.
Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for levomilnacipran and any potential adverse effects on the breast-fed child from the drug or from the underlying maternal conditions.
Routine dosage adjustment is not necessary in geriatric patients; however, consider the renal clearance of levomilnacipran when determining the dosage in such patients.
In the 8-week clinical trials with levomilnacipran, 2.8% of patients were >=65 years of age.
According to the manufacturer, no dosage adjustment is recommended on the basis of age. However, because levomilnacipran is primarily eliminated by renal excretion, consider the renal clearance of levomilnacipran when determining the dosage in geriatric patients.
SNRIs, including levomilnacipran, have been associated with clinically important hyponatremia in geriatric patients, who may be at greater risk for this adverse effect.
ICD codes
No ICD codes are available for this drug.
Formulary status
Search health-plan coverage for this drug by ZIP code.
Choose the first character of a health plan name.
Last reviewed · Source: First Databank (FDB) drug data
On this page
Actions
Sign in to save favorites
Saving this drug requires a free Physicians Office Resource account.