methyl folate, methylcobalamin, and acetylcysteine

Action and Spectrum

Actions and Spectrum: 

Actions: 

• Folate Metabolism: methyl folate is the active form of folate, a B-vitamin that plays a crucial role in DNA synthesis, repair, and methylation reactions. Methylation reactions are essential for many cellular processes, including neurotransmitter synthesis, homocysteine metabolism, and gene expression regulation. 
• Methylation Support: methyl folate acts as a methyl donor in biochemical pathways, transferring a methyl group to various molecules, including DNA, proteins, and neurotransmitters. This process is crucial for regulating gene expression and synthesizing essential molecules in the body. 

Spectrum: 

methyl folate supplements address folate deficiency and support methylation processes in individuals with specific genetic variations that affect folate metabolism. It is commonly prescribed to pregnant women to prevent neural tube defects in developing fetuses. 

Drug Interaction

Adverse Reaction

Frequency Not Defined 

Diarrhea 

Upset stomach 

Headache 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

• Hypersensitivity 
• Drug interactions 
• Asthma 
• Medical conditions 
• Pediatric & geriatric use 
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding usage in pregnant women. 

Breastfeeding warnings:  

It is not known whether the drug is excreted in the breast milk. 

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

methyl folate plays a vital role in one-carbon metabolism, where it transfers methyl groups for various biochemical reactions in the body. It is essential for DNA synthesis, amino acid metabolism, and neurotransmitter synthesis (e.g., serotonin, norepinephrine). 

methylcobalamin is a cofactor for two essential enzymes, methionine synthase and methylmalonyl-CoA mutase. Methionine synthase uses methylcobalamin to convert homocysteine to methionine, playing a role in one-carbon metabolism similar to methyl folate. methylcobalamin is also involved in myelin synthesis and nerve function. 

acetylcysteine works as a mucolytic by breaking down disulfide bonds in mucus, making it less viscous and easier to clear from the airways. As an antioxidant, acetylcysteine is a precursor to glutathione, a crucial cellular antioxidant that helps protect cells from oxidative damage. 

Pharmacodynamics: 

acetylcysteine is used as a mucolytic agent to manage respiratory conditions characterized by excessive mucus production, such as cystic fibrosis and chronic obstructive pulmonary disease. In cases of acetaminophen (paracetamol) overdose, acetylcysteine is administered as an antidote to counteract the toxic effects of acetaminophen and replenish glutathione levels in the liver, reducing the risk of liver damage. 

It’s important to note that the pharmacodynamic effects of these substances can vary based on individual differences, dosages, and the presence of other medications or medical conditions. Always use these medications or supplements under the guidance of a qualified healthcare provider to ensure their safe and effective use. 

methylcobalamin supplementation treats or prevents vitamin B12 deficiency. By supporting the abovementioned enzymatic reactions, methylcobalamin helps maintain normal metabolic processes and nerve function. 

Pharmacokinetics: 

Absorption 

When taken orally, methylcobalamin is absorbed through the gastrointestinal tract, but its absorption can be impaired in individuals with certain medical conditions affecting the stomach or intestines.  

Oral acetylcysteine is well-absorbed from the gastrointestinal tract, but its absorption can be variable. 

Distribution 

methylcobalamin is distributed throughout the body, particularly in tissues with high metabolic activity, such as the liver, nervous system, and bone marrow. 

acetylcysteine is distributed throughout the body and can cross the blood-brain barrier. 

Metabolism 

methylcobalamin is involved in various enzymatic reactions, including converting homocysteine to methionine and methyl malonyl-CoA to succinyl-CoA. 

acetylcysteine is rapidly metabolized in the liver, primarily through deacetylation, to form cysteine and eventually glutathione. 

Elimination and Excretion 

The body eliminates excess folate through urine. 

The body eliminates acetylcysteine and its metabolites primarily through urine. 

Adminstartion

Administration: 

methyl folate, methylcobalamin, and acetylcysteine administration can vary depending on their specific formulations and intended use. It can be given as tablets or solutions through the oral route. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: methyl folate, methylcobalamin, and acetylcysteine 

Why do we use methyl folate, methylcobalamin, and acetylcysteine? 

Acetylcysteine plays a vital role in protecting cells from oxidative stress and damage. Methyl folate supplements are commonly used to address folate deficiency, support healthy pregnancy outcomes, and may also be helpful in particular mental health conditions like depression and anxiety.