Esperal tablets

Esperal

  • Active Ingredient: Disulfiram
  • 500 mg, 250 mg
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What is Esperal?

The active ingredient of Esperal brand is disulfiram. Disulfiram blocks an enzyme that is involved in metabolizing alcohol intake. Disulfiram produces very unpleasant side effects when combined with alcohol in the body. C10H20N2S4 M.W. 296.54 Disulfiram, USP occurs as a white to off-white, odorless, and almost tasteless powder, soluble in water to the extent of about 20 mg in 100 mL, and in alcohol to the extent of about 3.8 g in 100 mL. Each tablet for oral administration contains 250 mg or 500 mg Disulfiram, USP. Tablets also contain colloidal silicon dioxide, lactose anhydrous, magnesium stearate, microcrystalline cellulose, sodium starch glycolate, and stearic acid.

Used for

Esperal is used to treat diseases such as: Alcohol Dependence.

Side Effect

Possible side effects of Esperal include: Decreased sexual ability in males; headache; numbness, tingling, pain, or weakness in hands or feet; Darkening of urine; skin rash; Drowsiness; Eye pain or tenderness or any change in vision; unusual tiredness.

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Concomitant Conditions

Because of the possibility of an accidental Esperal-alcohol reaction, Esperal should be used with extreme caution in patients with any of the following conditions: diabetes mellitus, hypothyroidism, epilepsy, cerebral damage, chronic and acute nephritis, hepatic cirrhosis or insufficiency.

Does Esperal actually eliminate Bb?

We don’t know how much residual inflammation related to ongoing microbial colonization resides in us after treatment with antimicrobials. And we don’t know if Esperal actually eradicates Borrelia burgdorferi and Babesia. But it clearly results in sustained remissions.

We still have a lot to learn about Esperal. Dr. Jayakamur Rajadas at Stanford is the pioneer who first considered Esperal in the treatment of Lyme disease. He tested over 4,000 drugs against Borrelia burgdorferi and published his results in 2016. (3)

Esperal ranked number one of all the drugs tested. He is still working to clarify its antimicrobial activity, and come up with analogues that have less toxicity. He also wants to test Esperal against Babesia and Bartonella in mice.

As we gain more experience with Esperal, I plan write additional blogs updating the topic.

Dr. Daniel Kinderlehrer is an internal medicine physician with a private practice in Denver, Colorado, devoted to treating patients with tick-borne illness. He is the author of the forthcoming book, “Recovery From Lyme: The Integrative Medicine Guide to the Diagnosis and Treatment of Tick-Borne Illness.” It will be released next year.

“A complete game-changer”

I have been particularly impressed by the impact of Esperal in patients who appeared to be in remission. The following is an email from Otto, who appeared asymptomatic after being treated for Lyme disease and babesiosis but then went on Esperal:

I wanted to reach out with my first update after stopping taking Esperal.

I cannot remember the last time I felt like this. I have so much more energy, so much more space in my head, so much more connection from my mind to my body allowing me to experience my life in a way that had become a distant memory.

My ability to think clearly, make and execute plans, have the energy to accomplish said plans and then carry onto the next is amazing. This experience of continuing to “wake up” from a bad dream I forgot I was in is truly amazing. It feels like the movie Limitless where the main character discovers a drug that allows him to use the entire capacity of his brain.

I feel like I am actually able to use my mind and body after only being able to control a fraction for so long.

I am definitely noticing the Esperal leaving my system now that I have stopped. The more it leaves the better I feel. I will continue to keep you updated as time progresses.

I sincerely cannot thank you enough. This is a complete game changer.

Otto explained to me that he forgot what it was like to feel well, before he became sick with tick-borne disease. I have other patients who have expressed similar sentiments.

DESCRIPTION

Esperal is an alcohol antagonist drug.

Chemical Name: bis(diethylthiocarbamoyl) disulfide.

C10H20N2S4 M.W. 296.54

Esperal occurs as a white to off-white, odorless, and almost tasteless powder, soluble in water to the extent of about 20 mg in 100 mL, and in alcohol to the extent of about 3.8 g in 100 mL.

Each tablet for oral administration contains 250 mg or 500 mg Esperal, USP. Tablets also contain colloidal silicon dioxide, anhydrous lactose, magnesium stearate, microcrystalline cellulose, sodium starch glycolate, and stearic acid.

What other drugs will affect Antabuse?

Tell your doctor about all medicines you use, and those you start or stop using during your treatment with Antabuse, especially:

seizure medications such as phenytoin (Dilantin)

blood thinning medications (including warfarin, Coumadin, Jantoven); or

This list is not complete and other drugs may interact with Esperal, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

Contraindications

Patients who are receiving or have recently received metronidazole, paraldehyde, alcohol, or alcohol-containing preparations, e.g., cough syrups, tonics and the like, should not be given Esperal.

Esperal is contraindicated in the presence of severe myocardial disease or coronary occlusion, psychoses, and hypersensitivity to Esperal or to other thiuram derivatives used in pesticides and rubber vulcanization.

Esperal Side Effects

While there are many benefits to the use of Esperal for treating alcoholism, this medication may cause adverse and unwanted side effects in some patients. Be sure to talk with your treatment specialist about your medical history, as well as any medications you are currently taking. In some cases, prescription and over-the-counter drugs can have a negative interaction when taken with Esperal.

Minor side effects of Esperal do not pose a medical threat and typically subside within a few days. These effects may include:

  • Headaches
  • Drowsiness
  • Skin rash or acne

Though unusual, severe side effects of the medication require immediate medical assistance. Serious side effects of Esperal may include:

  • Loss of appetite
  • Vomiting
  • Yellowing of the skin or eyes
  • Dark urine

In some cases, the drug may cause a sedative effect. If this happens, ask your healthcare provider about taking the medicine later in the day or before bed.

PRECAUTIONS

Patients with a history of rubber contact dermatitis should be evaluated for hypersensitivity to thiuram derivatives before receiving Esperal (see CONTRAINDICATIONS).

Alcoholism may accompany or be followed by dependence on narcotics or sedatives. Barbiturates and Esperal have been administered concurrently without untoward effects; the possibility of initiating a new abuse should be considered.

Hepatic toxicity including hepatic failure resulting in transplantation or death have been reported. Severe and sometimes fatal hepatitis associated with Esperal therapy may develop even after many months of therapy. Hepatic toxicity has occurred in patients with or without prior history of abnormal liver function. Patients should be advised to immediately notify their physician of any early symptoms of hepatitis, such as fatigue, weakness, malaise, anorexia, nausea, vomiting, jaundice, or dark urine.

Baseline and follow-up liver function tests (10-14 days) are suggested to detect any hepatic dysfunction that may result with Esperal therapy. In addition, a complete blood count and serum chemistries, including liver function tests, should be monitored.

Patients taking Esperal tablets should not be exposed to ethylene dibromide or its vapors. This precaution is based on preliminary results of animal research currently in progress that suggest a toxic interaction between inhaled ethylene dibromide and ingested Esperal resulting in a higher incidence of tumors and mortality in rats. A correlation between this finding and humans, however, has not been demonstrated.

Concomitant Conditions

Because of the possibility of an accidental Esperal-alcohol reaction, Esperal should be used with extreme caution in patients with any of the following conditions: diabetes mellitus, hypothyroidism, epilepsy, cerebral damage, chronic and acute nephritis, hepatic cirrhosis or insufficiency.

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What is Antabuse?

Antabuse (Esperal) blocks an enzyme that is involved in processing alcohol. Esperal produces very unpleasant side effects (such as fast heartbeat, chest pain, nausea, dizziness, flushing, and thirst) when combined with alcohol in the body.

Antabuse is used in certain people with chronic alcoholism. This medicine can help keep you from drinking because of the unpleasant side effects that will occur if you consume alcohol while taking Antabuse.

Antabuse is used together with therapy and counseling support to help you stop drinking. This medicine is not a cure for alcoholism.

Geriatric Use

A determination has not been made whether controlled clinical studies of Esperal included sufficient numbers of subjects aged 65 and over to define a difference in response from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy.

Marty Ross MD on Antabuse for Chronic Lyme Disease

This is mainly a video article. You will need to listen to the whole video for my thoughts on Antabuse (Esperal) as a new treatment for chronic Lyme disease. Below this video I provide additional points I did not mention during Conversations with Marty Ross MD on 7/18/19 when I recorded these comments.

Precautions

Patients with a history of rubber contact dermatitis should be evaluated for hypersensitivity to thiuram derivatives before receiving Esperal (see CONTRAINDICATIONS).

Alcoholism may accompany or be followed by dependence on narcotics or sedatives. Barbiturates and Esperal have been administered concurrently without untoward effects; the possibility of initiating a new abuse should be considered.

Hepatic toxicity including hepatic failure resulting in transplantation or death have been reported. Severe and sometimes fatal hepatitis associated with Esperal therapy may develop even after many months of therapy. Hepatic toxicity has occurred in patients with or without prior history of abnormal liver function. Patients should be advised to immediately notify their physician of any early symptoms of hepatitis, such as fatigue, weakness, malaise, anorexia, nausea, vomiting, jaundice, or dark urine.

Baseline and follow-up liver function tests (10 to 14 days) are suggested to detect any hepatic dysfunction that may result with Esperal therapy. In addition, a complete blood count and serum chemistries, including liver function tests, should be monitored.

Patients taking Esperal tablets should not be exposed to ethylene dibromide or its vapors. This precaution is based on preliminary results of animal research currently in progress that suggest a toxic interaction between inhaled ethylene dibromide and ingested Esperal resulting in a higher incidence of tumors and mortality in rats. A correlation between this finding and humans, however, has not been demonstrated.

DRUG INTERACTIONS

Esperal appears to decrease the rate at which certain drugs are metabolized and therefore may increase the blood levels and the possibility of clinical toxicity of drugs given concomitantly.

DISULFIRAM SHOULD BE USED WITH CAUTION IN THOSE PATIENTS RECEIVING PHENYTOIN AND ITS CONGENERS, SINCE THE CONCOMITANT ADMINISTRATION OF THESE TWO DRUGS CAN LEAD TO PHENYTOIN INTOXICATION. PRIOR TO ADMINISTERING DISULFIRAM TO A PATIENT ON PHENYTOIN THERAPY, A BASELINE PHENYTOIN SERUM LEVEL SHOULD BE OBTAINED. SUBSEQUENT TO INITIATION OF DISULFIRAM THERAPY, SERUM LEVELS OF PHENYTOIN SHOULD BE DETERMINED ON DIFFERENT DAYS FOR EVIDENCE OF AN INCREASE OR FOR A CONTINUING RISE IN LEVELS. INCREASED PHENYTOIN LEVELS SHOULD BE TREATED WITH APPROPRIATE DOSAGE ADJUSTMENT.

It may be necessary to adjust the dosage of oral anticoagulants upon beginning or stopping Esperal, since Esperal may prolong prothrombin time.

Patients taking isoniazid when Esperal is given should be observed for the appearance of unsteady gait or marked changes in mental status, the Esperal should be discontinued if such signs appear.

In rats, simultaneous ingestion of Esperal and nitrite in the diet for 78 weeks has been reported to cause tumors, and it has been suggested that Esperal may react with nitrites in the rat stomach to form a nitrosamine, which is tumorigenic. Esperal alone in the rat's diet did not lead to such tumors. The relevance of this finding to humans is not known at this time.


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