Reported Drugs With Mitochondrial Toxicity
Individuals suffering from Fluoroquinolone Toxicity are a very heterogeneous group that exhibit a wide variety of symptoms and levels of disability. In that group that are many that manifest symptoms
suggestive of mitochondrial dysfunction or disease. Documentation abounds showing the ability of the Fluoroquinolones to damage mitochondria. Because of this, some individuals have found it helpful to avoid substances that have a potential to damage mitochondria.
With that in mind, not all medications mentioned here will cause problems. 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 in research. 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. Also, if you can save this or print this PDF form. I have instructions on how to get a convenient copy at they very bottom of the page.
Document Updated 09/15/2019
| Reported Drugs with Mitochondrial Toxicity | ||||
| Pharmacologic Category | Medication | Adverse Reaction | Possible Effects | |
| 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 | Liver failure, hyperammoninaemia, hypoglycaemia, steatosis and encephalopathy | ||
| Dantrolene | Inhibits Complex I | |||
| Phenytoin | Inhibits Complex I | |||
| Psychotropics | ||||
| Antidepressants | Tricyclic antidepressants: amitriptyline, clomipramine (Elavil) |
Inhibits MRC | Extrapyramidal symptoms, memory impairment | |
| Amoxapine | ||||
| Fluoxetine (Prozac) | Inhibits OXPHOS (Cohen) Interferes with the lipid bilayer of the inner mitochondrial membrane (particularly at high dose) (103) | Gastrointestinal damage | ||
| Citalopram (Cipramil) | ||||
| Setaline (Zoloft) | Inhibits MRC I and V, inhibits oxidative phosphorylation | Hepatotoxicity | ||
| 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 | Extrapyramidal symptoms, metabolic syndrome | ||
| 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 |
Inhibits MRC I, reduces coenzyme Q10 levels, weak peroxisome proliferator activated receptor ligand, inhibits Complex III, induces mitochondrial permeability transition (MPT) | Causes myopathy, rhabdomyolysis | ||
| Bile acids- Cholestyramine | Inhibits ETC | |||
| Ciprofibrate | Inhibits MRC I, weak peroxisome proliferator activated receptor ligand | Myopathy and rhabdomyolysis | ||
| 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 | Hepatotoxicity (overdose) | ||
| Ibuprofen (Advil and Motrin) | Inhibits fatty acid oxidation and beta oxidation of medium and short chain fatty acids | Hepatotoxicity | ||
| Naproxen (Aleve) | Hepatotoxicity | |||
| Indomethacin (Indocin) | ||||
| Diclofenac | Hepatotoxicity | |||
| 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 |
Deafness or hearing loss; cardiac toxicity, renal toxicity, myopathy | ||
| Linezolid (Zyvox) | Inhibit mitochondrial translation- DIMD | lactic acidosis; optic and peripheral neuropathy, polyneuropathy | ||
| Antimycin | Inhibits Complex III | |||
| Cephaloidine | Inhibits Complex IV | |||
| Macrolide- erythromycin | Inhibits translation | |||
| Anti-arrhythmic | ||||
| Amiodarone | Inhibits MRC I and III and beta oxidation | Pulmonary toxicity, microvesicular steatosis and liver failure | ||
| Blood Pressure | ||||
| Beta-blockers: metoprolol, propranolol | Reduce transmembrane mitochondrial potential | Case Report of Muscle Wasting | ||
| Steroids | ||||
| Corticosteroids | Inhibit mt membrane potential, generate reactive oxygen species | Myopathy | ||
| Anti-viral | ||||
| Interferon | Impairs mtDNA transcription | |||
| Anti-retrovirals | ||||
| Nucleoside reverse transcriptase inhibitors: zidovudine, didanosine, lamivudine, abacavir |
Impairs mtDNA replication which causes mtDNA depletion, decreases Complex I and Complex IV activity | Encephalomyopathy, anaemia, polyneuropathy, pancreatitis and lactic acidosis | ||
| Cancer medications | ||||
| Doxorubicine (Adriamycin) | mtDNA mutation | Cardiomyopathy | ||
| Cis-platinum | Impairs mtDNA transcription | Cardiomyopathy | ||
| 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 | Causes lactic acidosis | ||
| Pioglitazone | Inhibits MRC I, weak, peroxisome proliferator activated receptor ligand | Increases anaerobic glycolysis | ||
| Anesthesia | ||||
| General | Halothane (Fluothane) | Inhibits Complex I | ||
| Isoflurane | Inhibits Complex III | Hepatotoxicity | ||
| Sevoflurane | Inhibits Complex III | Hepatotoxicity, neurotoxicity cardiac effects | ||
| Propofol (particularly > 4 mg/kg/h for > 48 hours) | Inhibits mitochondrial function; Inhibition of free fatty acid entry to mt, beta oxidation | Propofol infusion syndrome: metabolic acidosis, rhabdomyolysis, heart failure, hepatomegaly, asystole | ||
| Nitrous Oxide | Inhibits cis-acotinase and iron-containing electron enzymes; affecting energy production | |||
| Local | Bupivacaine (Marcaine) | Uncouples oxidation and phosphorylation; inhibits Complex I | Myopathy | |
| Lidocaine (Xylocaine) | Inhibits Complex I | Myopathy | ||
| 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. Table of Reported Drugs with Mitochondrial Toxicity, MitoAction: https://www.mitoaction.org/diagnosis-care/mito-toxic-list/ | ||||
| 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/ | ||||
| 6. Mitochondrial Disorders: Medicines to Avoid | ||||
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