Reported Drugs With Mitochondrial toxicity

Dangerous Drugs

Those damaged by Fluoroquinolones (FQ’s) are a very heterogeneous group exhibiting a wide variety of symptoms and levels of disability.  In that group that are many that exhibit symptoms suggestive of mitochondrial dysfunction or disease.  Documentation abounds showing the ability of the FQ’s to damage mitochondria.  Some individuals benefit from avoiding substances that have a potential to damage mitochondria.

Not all medications here will cause problems in floxed folks but, in the interest of safety and information, and to spawn further discussions with medical professionals, I am publishing a list of drugs that have been show to possess the ability to induce dysfunction or cause damage to the mitochondria.  This list is not meant to be all inclusive, nor does it indicate whether a person will have a negative adverse event if they use one or more of these pharmaceuticals.  There are plenty of drugs that are on the market that can be toxic to the human body that are not listed here. Again, these are drugs that have shown the ability to harm the mitochondria. Obviously, when faced with a decision, one needs to weight the risk/rewards associated with the usage of a particular drug. It is highly recommended that you consult a medical professional regarding all medications and their use.

Please note that this list will change as new information is received.

Document Updated 07/09/2018

Reported Drugs with Mitochondrial Toxicity
Pharmacologic Category Medication Adverse Reaction
Anticonvulsants
Valproate (Depakote, Valproic Acid) Sequesters and depletes carnitine; decreases fatty acid oxidation; Krebs cycle, Electron Transport Chain (ETC) activity and oxidative phosphorylation; Complex IV inhibition
Dantrolene Inhibits Complex I
Phenytoin Inhibits Complex I
Psychotropics
 Antidepressants Amitriptyline (Elavil) Causes autonomic dysfunction
Amoxapine
Fluoxetine (Prozac) Inhibits OXPHOS  (Cohen) Interferes with the lipid bilayer of the inner mitochondrial membrane (particularly at high dose) (103)
Citalopram (Cipramil)
Setaline (Zoloft) liver toxicity, mitochondrial dysfunction
Antipsychotics
   . Chlorpromazine (Thorazine) Inhibits brain and liver mitochondrial respiration

 

Haloperidol (Haldol), Fluphenazine (Prolixin) Depletes glutathione and inhibits mitochondrial respiration in brain and Complex I activity
Resperidone (Risperdol)  
Barbiturates
Phenobarbital Reduces mitochondrial protein synthesis; decrease number and size of mitochondria
Secobarbital (Seconal) Inhibits Complex I
Butalbital (Fiorinal)  
Amobarbital (Amytal)  
Pentobarbital (Nembutal)  
Anxiety Medications
Benzodiazepines Alprazolam (Xanax) Inhibit adenosine nucleotide translocase
Diazepam (Valium, Diastat) Inhibit adenosine nucleotide translocase
Cholesterol medications
Statins

Cerivastatin

Fluvastatin

Atrovastatin

Simvastatin

Lovastatin

Reduce endogenous Coenzyme Q10,   inhibits Complex III, induces mitochondrial permeability transition (MPT)

myopathy

Bile acids- Cholestyramine Inhibits ETC
Ciprofibrate Inhibits Complex I
Fenofibrate Inhibits Complex I
Clofibrate Inhibits Complex I
Analgesics
Anti-inflammatory ASA (Aspirin, Acetylsalicylic Acid) Inhibits ETC and uncouples oxidative-phosphorylation

Reye Syndrome (hepatic failure)

Acetaminophen (Tylenol) increases oxidative stress
Ibuprofen (Advil and Motrin) Inhibits fatty acid oxidation and beta oxidation of medium and short chain fatty acids
Naproxen (Aleve)  
Indomethacin (Indocin)  
Diclofenac  
Antibiotics
Tetracycline Inhibits beta-oxidation; inhibits mitochondrial protein synthesis and fatty acid oxidation
Fluoroquinolones- Trovafloxacin, Grepafloxacin, Ciprofloxacin, Gatifloxacin, Clinafloxacin, Levofloxacin Depletes glutathione and increases reactive oxygen species

 

Minocycline Inhibits beta-oxidation; inhibits mitochondrial protein synthesis
Chloramphenicol Inhibits mitochondrial protein synthesis
Aminoglycosides       streptomycin gentamycin     neomycin       kanamycin Impairs mtDNA translation

hearing loss; cardiac toxicity and renal toxicity

Linezolid (Zyvox) Inhibit mitochondrial translation- DIMD

lactic acidosis; optic and peripheral neuropathy

Antimycin Inhibits Complex III
Cephaloidine Inhibits Complex IV
Macrolide- erythromycin Inhibits translation
Anti-arrhythmic
Amiodarone Inhibits beta-oxidation
Steroids
Reduce transmembrane mitochondrial potential
Anti-viral
Interferon Impairs mtDNA transcription
Anti-retrovirals
Zidovudine Impairs mtDNA replication which causes mtDNA depletion, decreases Complex I and Complex IV activity
Cancer medications
Doxorubicine (Adriamycin)
Cis-platinum Impairs mtDNA transcription
Tamoxifen Depletes ATP, inhibits Complex III, IV, V
Cyclophosphamide Inhibits Complex II
Pain medication
Capsaisin Inhibits Complex I
Anti-fungal medication
Ketoconazole Inhibits Complex II
Diabetes Medication
Biguanides (Metformin) Inhibits oxidative-phosphorylation; enhances glycolysis; inhibits Complex I
 

Anesthesia

General Halothane (Fluothane) Inhibits Complex I
Isoflurane Inhibits Complex III
Sevoflurane Inhibits Complex III
Propofal Inhibits mitochondrial function
Nitrous Oxide Inhibits cis-acotinase and iron-containing electron enzymes; affecting energy production
Local Bupivacaine (Marcaine) Uncouples oxidation and phosphorylation; inhibits Complex I
Lidocaine (Xylocaine) Inhibits Complex I
Sources:         
1.  Cohen, BH (August 11, 2011) The Mitochondrial Toxicity of Prescription Pharmacopoeia, webcast, Akron Children’s Hospital: http://www.orlive.com/akronchildrens/mitochondrial
2.  Sims, K (June 4, 2010) Table of Reported Drugs with Mitochondrial Toxicity, audiocast, MitoAction: http://www.mitoaction.org/blog/medication-exposures-mitochondrial-toxicity
3.  Dykens, JA, Will, Yvonne. Drug-Induced Mitochondrial Dysfunction. New Jersey: Wiley; 2008.
4. Josef Finsterer and Liane Segall (2010) Drugs interfering with mitochondrial disorders
5. (Zoloft) https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5736306/

 

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