What MTHFR Medications To Avoid?

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Hi, there.

Wondering what medications to avoid if you have an MTHFR gene mutation?

If so, all the MTHFR medications to avoid are the subject I’m going to discuss today.

But please before you stop taking any medication please consult your doctor and establish a plan. We are not recommending that you just stop taking a medication that may be keeping you alive. 

What MTHFR medications to avoid

MTHFR Medications To Avoid – It’s An Important Topic!

Living with MTHFR mutation requires a few lifestyle adjustments. 

And the medications you use are one of them!

Sometimes we have to take medications to manage some health problems. 

But some of them can only aggravate the health of a person with MTHFR gene mutation.

That’s the last thing you want…

When you know what medications to avoid, you can ask the healthcare provider to give you an alternative. 

That’s why I decided to write about this incredibly important topic.

Scroll down to see all medications you should strive to avoid if you carry the MTHFR variant.

Medications To Avoid If You Carry The MTHFR Variant…

MTHFR Medications To Avoid

Birth Control Pills

Women with MTHFR gene mutation may want to avoid using oral contraceptives, and couples should opt for alternatives in terms of contraception.

What makes oral contraceptives so bad for you?

The answer is simple – they impair metabolism of folate and produce some degree of depletion of this vitamin.

Keep in mind that as someone with an MTHFR gene mutation, you already have trouble processing this vitamin (especially in synthetic form, folic acid), so birth control pills could only worsen this.

Also, one study found that women with MTHFR gene mutations who use oral contraceptives are at a higher risk of ischemic stroke.

This particular study included 193 women aged 20-49 years with ischemic stroke and 797 controls.

Scientists found that women with MTHFR gene mutations who used oral contraceptives had a 5.4-fold higher risk of suffering from ischemic stroke than counterparts who didn’t have the MTHFR gene variant.

If you’re on birth control pill and also have an MTHFR gene mutation, you may want to consult your healthcare provider or gynecologist regarding safer oral contraceptive choices and dosages.


Antacids are a class of medications that work to neutralize stomach acid. 

Since they’re over-the-counter (OTC) medicines, you don’t need a prescription to get them.

Chances are you already have an antacid in your home.

Although they help neutralize stomach acid, these medicines aren’t the safest option for people with MTHFR gene mutation.

Antacids block the absorption of vitamin B12 and other nutrients, thus setting you up for nutritional deficiencies.

Basically, antacids act as proton pump inhibitors, which block the absorption of vitamin B12 and may also worsen the body’s ability to detoxify by affecting detoxification pathways.

Nutrient deficiencies worsen your health and quality of life. 

This is particularly the case for people with MTHFR gene variant as their body is in high demand for vitamin B12.

Additionally, antacids and acid blockers may deplete the body of probiotics, which are crucial for gut health and the immune system.

Cholesterol-lowering Drugs

Drugs that lower high cholesterol levels, e.g., Cholestyramine, are usually prescribed to patients whose LDL or bad cholesterol is too high, and HDL or good cholesterol is too low.

These medicines aim to lower cholesterol levels and thereby help prevent cardiovascular problems that would occur otherwise.

However, men and women with MTHFR gene mutations may want to stay away from these drugs because they decrease the absorption of folate and cobalamin (vitamin B12).

Since they interfere with the absorption of much-needed micronutrients, cholesterol-lowering drugs impair methylation and allow more toxins to build up.

I just want to emphasize that you shouldn’t discontinue using some drugs on your own

If you’re prescribed with cholesterol-lowering drugs, you need to consult a doctor.

Your healthcare provider will prescribe drugs that are safe or adjust the dosage.

Drugs That Raise Homocysteine Levels

Homocysteine is an amino acid that may increase the risk of heart disease when its levels become too high.

People with MTHFR gene mutations tend to be more susceptible to higher homocysteine levels in the blood.

So, if you have the MTHFR gene variant and take some medications that increase homocysteine levels, you could put your cardiovascular health in danger.

The above-mentioned cholesterol-lowering drug, Cholestyramine, may increase homocysteine levels too, just like Metformin, a prescription drug used mainly to treat diabetes.

Studies show that both these drugs interfere with the absorption of vitamins from the gut and also elevate homocysteine.

Other drugs or ingredients known for their potential to raise homocysteine levels include:

  • Caffeine
  • Colestipol (Colestid) – used to lower cholesterol levels
  • Fenofibrate (Antara, Fenoglide, Lipofen, etc.) – used to lower cholesterol levels
  • Levodopa (Parcopa, Sinemet, Stalevo) – central nervous system agent
  • Methotrexate (Rheumatrex) – manages inflammatory types of arthritis
  • Niacin (Advicor, Ocuvite, etc.) – high doses of niacin also deplete vitamin B6
  • Pemetrexed (Alimta) – chemotherapy medication
  • Phenytoin (Dilantin, Phenytek) – an anti-seizure medication
  • Pyrimethamine (Daraprim, Fansidar) – antiparasitic prescription medicine
  • Sulfasalazine (Azulfidine) – prescribed for the management of rheumatoid arthritis, ulcerative colitis, and Crohn’s disease

Again, I’m not advising you to ditch these drugs entirely without consulting your healthcare provider. 

Your doctor will probably work with you to prescribe alternatives or modify the dose.

Medications to avoid if you carry MTHFR

Drugs That Affect Methylation Cycle

Men and women with the MTHFR gene variant should also strive not to use medications that affect the methylation cycle as their gene mutation impairs this cycle in the first place.

Besides antacids, which I mentioned above, other types of drugs also affect methylation include Cholestyramine.

Colestipol, sulfasalazine, nitrous oxide, phenytoin, methotrexate, high-dose niacin, metformin, oral contraceptives also affect methylation, just like:

  • Theophylline – treats lung diseases
  • Cyclosporin A – prevents transplant rejection
  • Antimalarials
  • Triamterene – treats high blood pressure
  • Bactrim – antibiotic
Understanding The Importance Of What MTHFR Medications To Avoid

Some medications can harm people with the MTHFR gene variant.

For example, they can increase homocysteine, impair methylation, decrease absorption of nutrients, and thereby increase the likelihood of health problems.

This post focused on what MTHFR medications to avoid, but make sure to discuss this subject with your doctor.