brands

Class

• Medical food (bioavailable form of folate)
• Trimonoamine modulator

METHYLFOLATE (L) commonly prescribed for

(Bold for FDA approved)

How METHYLFOLATE (L) works

• Folate is a water-soluble B vitamin (B9) that is essential for cell growth/reproduction, breakdown/utilization of proteins, formation of nucleic acids, and other functions

• L-methylfolate, or 6-(S)-5-methyltetrahydrofolate, is derived from folate and is the form that enters the brain and works directly as a methyl donor and monoamine synthesis modulator

• That is, it regulates tetrahydrobiopterin (BH4), a critical enzyme cofactor for trimonoamine neurotransmitter synthesis

• Methyl donor for DNA methylation and thus an epigenetic regulator

How long until METHYLFOLATE (L) works

• Onset of therapeutic actions in depression is usually not immediate, but often delayed 2–4 weeks

• If it is not working within 6–8 weeks for depression, it may require a dosage increase or it may not work at all

• May continue to work for many years to prevent relapse of symptoms

Notable Side Effects

• L-methylfolate does not typically cause side effects

Life Threatening Side Effects

• Theoretically, rare induction of mania or suicidal ideation and behavior (suicidality)

weight gain

unusual

sedation

unusual

What to do about METHYLFOLATE (L) side effects

• Wait

• Lower the dose or administer in divided doses

• Switch to another drug

usual dosage range

• 7.5–15 mg/day

Dosage Forms

• Tablet 7.5 mg, 15 mg

long term use

• Safe

habit forming

• No

Renal Impairment

• Dose adjustment not necessary

Hepatic Impairment

• Dose adjustment not necessary

Cardiac Impairment

• Dose adjustment not necessary

Elderly

• Dose adjustment not necessary

Children and Adolescents

• Use with caution, observing for activation of known or unknown bipolar disorder and/ or suicidal ideation, and inform parents or guardians of this risk so they can help observe child or adolescent patients

• Safety and efficacy have not been established

Pregnancy

• No controlled studies in humans or animals

• Controlled studies of folic acid at recommended doses have failed to demonstrate risk to the fetus

• There are no studies of folic acid at high doses

• Because pregnant women are advised to take folic acid or prenatal vitamins that contain folic acid, it is important to ask the patient about any supplements or vitamins she may be taking and consider this when deciding whether to prescribe l-methylfolate

Breast Feeding

• Some drug is found in mother’s breast milk