Betaine
/api/v1/drug/betaineMechanism of action
Sourced from openFDAMechanism-of-action class: Methylating Activity.
Indications
Sourced from openFDA- CYSTADANE ® is indicated for the treatment of homocystinuria to decrease elevated homocysteine blood concentrations in pediatric and adult patients. Included within the category of homocystinuria are: Cystathionine beta-synthase (CBS) deficiency 5,10-methylenetetrahydrofolate reductase (MTHFR) deficiency Cobalamin cofactor metabolism (cbl) defect CYSTADANE is a methylating agent indicated in pediatric and adult patients for the treatment of homocystinuria to decrease elevated homocysteine blood concentrations.
Contraindications
Sourced from openFDA- None.contraindicated
Dosage & administration
Sourced from openFDAAdults and Pediatric Patients 3 Years of Age and Older The recommended dosage is 6 grams per day, administered orally in divided doses of 3 grams twice daily. ( 2.1 ) Pediatric Patients Less than 3 Years of Age The recommended starting dosage is 100 mg/kg/day, administered orally in divided doses of 50 mg/kg twice daily, and then increased weekly by 50 mg/kg increments. ( 2.1 ) Monitor patient response by plasma homocysteine concentrations. ( 2.1 ) Increase the dosage gradually until the plasma total homocysteine concentration is undetectable or present only in small amounts. ( 2.1 ) Preparation and Administration Instructions Prescribed amount of CYSTADANE should be measured with the measuring scoop provided and then dissolved in 4 to 6 ounces of water, juice, milk, or formula until completely dissolved, or mixed with food for immediate ingestion. ( 2.2 ) 2.1 Dosage Therapy with CYSTADANE should be directed by physicians knowledgeable in the management of patients with homocystinuria. Adults and Pediatric Patients 3 Years of Age and Older The recommended dosage is 6 grams per day, administered orally in divided doses of 3 grams twice daily. Pediatric Patients Less than 3 Years of Age The recommended starting dosage is 100 mg/kg/day divided in twice daily doses, and then increased weekly by 50 mg/kg increments. Monitoring Monitor patient response to CYSTADANE by homocysteine plasma concentration. Increase the dosage in all patients gradually until the plasma total homocysteine concentration is undetectable or present only in small amounts.
Warnings & precautions
Sourced from openFDAHypermethioninemia in Patients with CBS Deficiency: CYSTADANE may worsen elevated plasma methionine concentrations and cerebral edema has been reported. Monitor plasma methionine concentrations in patients with CBS deficiency. Keep plasma methionine concentrations below 1,000 micromol/L through dietary modification and, if necessary, a reduction of CYSTADANE dosage. ( 5.1 ) 5.1 Hypermethioninemia in Patients with CBS Deficiency Patients with homocystinuria due to cystathionine beta-synthase (CBS) deficiency may also have elevated plasma methionine concentrations. Treatment with CYSTADANE may further increase methionine concentrations due to the remethylation of homocysteine to methionine. Cerebral edema has been reported in patients with hypermethioninemia, including patients treated with CYSTADANE [ see Adverse Reactions ( 6.2 ) ]. Monitor plasma methionine concentrations in patients with CBS deficiency. Plasma methionine concentrations should be kept below 1,000 micromol/L through dietary modification and, if necessary, a reduction of CYSTADANE dosage.
Adverse reactions
Sourced from openFDAThe following serious adverse reactions are described elsewhere in labeling: Hypermethioninemia and cerebral edema in patients with CBS deficiency [ see Warnings and Precautions ( 5.1 ) ]. Most common adverse reactions (> 2%) are: nausea and gastrointestinal distress, based on physician survey. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Recordati Rare Diseases Inc. at 1-888-575-8344, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The assessment of clinical adverse reactions is based on a survey study of 41 physicians, who treated a total of 111 homocystinuria patients with CYSTADANE. Adverse reactions were retrospectively recalled and were not collected systematically in this open-label, uncontrolled, physician survey. Thus, this list may not encompass all types of potential adverse reactions, reliably estimate their frequency, or establish a causal relationship to drug exposure.
Use in specific populations
Sourced from openFDA8.1 Pregnancy Risk Summary Available data from a limited number of published case reports and postmarketing experience with CYSTADANE use in pregnancy have not identified any drug associated risks for major birth defects, miscarriage, or adverse maternal or fetal outcomes. Animal reproduction studies have not been conducted with betaine. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. 8.2 Lactation Risk Summary There are no data on the presence of betaine in human or animal milk, the effects on the breastfed child, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for CYSTADANE and any potential adverse effects on the breastfed child from CYSTADANE or from the underlying maternal condition. 8.4 Pediatric Use The safety and effectiveness of CYSTADANE have been established in pediatric patients.
Overdosage
Sourced from openFDAThere is no information on CYSTADANE overdose in humans. In an acute toxicology study in rats, death occurred frequently at doses equal to or greater than 10 g/kg.
Approval history
Sourced from openFDA- Oct 25, 1996NDANDA020576Recordati Rare
- Nov 23, 2021ANDAANDA214864Novitium Pharma
- Jan 28, 2022ANDAANDA210508Eton
FAERS reports
- 1Off Label Use15410%
- 2Diarrhoea966.3%
- 3Vomiting926.0%
- 4Overdose895.8%
- 5Nausea744.9%
- 6Product Dose Omission634.1%
- 7Headache583.8%
- 8Product Dose Omission Issue543.5%
- 9Pneumonia513.4%
- 10Seizure483.2%
- 11Product Use Issue463.0%
- 12Pain453.0%
- 13Pyrexia453.0%
- 14Fatigue442.9%
- 15Drug Ineffective412.7%
Literature
Recent PubMed references pinned to Betaine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.
- Particle Design via Lactosome-Based Polycarboxybetaine Modification and Initial Evaluation of the Accelerated Blood Clearance Phenomenon.Biological & pharmaceutical bulletin · 2026 · Takahashi R, Yamamoto Y, Saito Y, et al.PMID 42236221DOI 10.1248/bpb.b26-00081
- Effects of dietary methionine, betaine, and turmeric extract on growth performance, myogenic gene expression, serum protein profile, and intestinal histomorphology in broiler chickens.Tropical animal health and production · 2026 · Abdelzaher GM, Baloza SH, Khalifa OA, et al.PMID 42223732DOI 10.1007/s11250-026-05080-z
- Montmorillonite-reinforced alginate/polyacrylamide semi-IPN hydrogel fertilizers engineered with betaine for enhanced crop resilience under cold and drought stress.International journal of biological macromolecules · 2026 · Xu R, Tian Y, Zhu B, et al.PMID 42202652DOI 10.1016/j.ijbiomac.2026.152745
- Effects of Loop Nucleobase Substitution on G-Quadruplex Thermal Stability in Aqueous Glycine Betaine, Proline, TMAO, and Urea Solutions.Biomolecules · 2026 · Schwinefus JJ, Corluka M, Dobrinski I, et al.PMID 42194045DOI 10.3390/biom16050697
- Association of Maternal and Cord Blood Choline and Betaine Concentrations with Birthweight: A Prospective Mother-Infant Cohort Study.Nutrients · 2026 · Aihemaitijiang S, Wen J, Li K, et al.PMID 42124057DOI 10.3390/nu18091456
- Betaine Alters the Interplay of the Adenosine and NO Systems in the Control of Renal Regional Haemodynamics and Excretion in Diabetic Female Rats.International journal of molecular sciences · 2026 · Dobrowolski L, Monchakivska AV, Rogozińska M, et al.PMID 42123657DOI 10.3390/ijms27094076
- Glycine Betaine-Induced Metabolic Responses Under Heat and Cold Stress in Passiflora edulis f. flavicarpa.International journal of molecular sciences · 2026 · de Almeida Oliveira L, Nguyen NTT, Kenth Solde Antesco D, et al.PMID 42123393DOI 10.3390/ijms27093811
- Molecular Mechanism of Glycine Betaine-Driven Endogenous Brassinosteroid Synthesis in Improving Soybean Atrazine Tolerance.Journal of agricultural and food chemistry · 2026 · Li Y, Meng X, Dai K, et al.PMID 42117892DOI 10.1021/acs.jafc.6c00989
Clinical trials
The 10 most recently updated of 80 ClinicalTrials.gov registrations naming Betaine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.
- Efficacy of a New Composition (BU002) for Debridement of Chronic Cutaneous UlcersRecruiting · Interventional · 80 enrolled · Universidad del DesarrolloNCT07607106updated 2026-05-26
- Effect of Betaine and Choline on Metabolic HealthCompleted · Interventional · 34 enrolled · University of GuelphNCT06758856updated 2026-05-12
- Effect of a Novel Topical Composition on the Incidence of Severe Oral Mucositis in Head & Neck Cancer Radiated Patients and Quality of Life Assessed by PROMs.Recruiting · Interventional · 63 enrolled · Mucosa Innovations, S.L.NCT05635929updated 2026-04-15
- Effects of 5-Methyltetrahydrofolic Acid Supplementation on Maternal Health and One-Carbon Metabolism During LactationNot yet recruiting · Phase 1 · Phase 2 · Interventional · 36 enrolled · Fundació Sant Joan de DéuNCT07508917updated 2026-04-02
- Maternal Betaine Supplementation During BreastfeedingActive not recruiting · Phase 1 · Phase 2 · Interventional · 47 enrolled · Fundació Sant Joan de DéuNCT04633044updated 2026-03-24
- Modulating Early-life Nutrition for Childhood Obesity PreventionActive not recruiting · Interventional · 50 enrolled · Fundació Sant Joan de DéuNCT06091917updated 2026-03-20
- Pharmacokinetic Assessment of Betaine Supplementation in Lactating MothersActive not recruiting · Interventional · 10 enrolled · Fundació Sant Joan de DéuNCT07243678updated 2026-03-20
- Nicotinamide Mononucleotide Supplementation for Exercise Tolerance Improvement in Healthy Older AdultsRecruiting · Interventional · 40 enrolled · Scott SilveiraNCT07144527updated 2026-02-20
- Efficacy of Essential Phospholipid Versus Betaine HCL/L-Glutamic Acid in MAFLDNot yet recruiting · Observational · 200 enrolled · Assiut UniversityNCT07194863updated 2026-01-13
- Betaine vs. Placebo for Serologically Diagnosed Metabolic Dysfunction-associated Steatohepatitis (MASH)Not yet recruiting · Phase 2 · Interventional · 70 enrolled · Southern California Institute for Research and EducationNCT07276204updated 2026-01-08
Frequently asked questions
- How does Betaine work?
- Mechanism-of-action class: Methylating Activity.
- What is Betaine used for?
- According to FDA labeling, Betaine carries indications including: CYSTADANE ® is indicated for the treatment of homocystinuria to decrease elevated homocysteine blood concentrations in pediatric and adult patients. Included within the category of homocystinuria are: Cystathionine beta-synthase (CBS) deficiency 5,10-methylenetetrahydrofolate reductase (MTHFR) deficiency Cobalamin cofactor metabolism (cbl) defect CYSTADANE is a methylating agent indicated in pediatric and adult patients for the treatment of homocystinuria to decrease elevated homocysteine blood concentrations.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
- What class of drug is Betaine?
- Betaine is classified as Amino acids and derivatives, Methylating Agent, Methylating Activity, Hematologic Activity Alteration.
- What are the brand names for Betaine?
- Betaine is marketed under brand names including Cystadane.
- What are the contraindications for Betaine?
- Betaine labeling lists contraindications including: None.. Always consult the full prescribing information and a clinician.
betaine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.