Tapazole

What is methimazole (Tapazole)?

Methimazole prevents the thyroid gland from producing too much thyroid hormone.  Methimazole is used to treat hyperthyroidism (overactive thyroid). It is also used before thyroid surgery or radioactive iodine treatment. Methimazole may also be used for other purposes not listed in this medication guide.

TAPAZOLE® (methimazole) Tablets, USP (1-methylimidazole-2-thiol) is a white, crystalline substance that is freely soluble in water. It differs chemically from the drugs of the thiouracil series primarily because it has a 5-instead of a 6-membered ring.

Each tablet contains 5 or 10 mg (43.8 or 87.6 μmol) methimazole, an orally administered antithyroid drug. Each tablet also contains lactose monohydrate, magnesium stearate, starch (corn), pregelatinized starch and talc.

The molecular weight is 114.16, and the molecular formula is C4H6N2S. The structural formula is as follows:

TAPAZOLE® (Methimazole) Structural Formula Illustration

TAPAZOLE is indicated:

  • In patients with Graves’ disease with hyperthyroidism or toxic multinodular goiter for whom surgery or radioactive iodine therapy is not an appropriate treatment option.
  • To ameliorate symptoms of hyperthyroidism in preparation forthyroidectomy or radioactive iodine therapy.

DOSAGE AND ADMINISTRATION

TAPAZOLE is administered orally. The total daily dosage is usually given in 3 divided doses at approximately 8-hour intervals.

Adult –The initial daily dosage is 15 mg for mild hyperthyroidism, 30 to 40 mg for moderately severe hyperthyroidism, and 60 mg for severe hyperthyroidism, divided into 3 doses at 8-hour intervals. The maintenance dosage is 5 to 15 mg daily.

Pediatric –Initially, the daily dosage is 0.4 mg/kg of body weight divided into 3 doses and given at 8-hour intervals. The maintenance dosage is approximately 1/2 of the initial dose.

HOW SUPPLIED

TAPAZOLE Tablets are available in:

The 5-mg tablets are round, white to off-white, scored on one side and the other side debossed with “J94”.

They are available as follows:

Bottles of 100 NDC 60793-104-01

The 10-mg tablets are round, white to off-white, scored on one side and the other side debossed with “J95”.

They are available as follows:

Bottles of 100 NDC 60793-105-01

Store at controlled room temperature, 15° to 30°C (59° to 86°F).

Distributed by: King Pharmaceuticals, Inc. Bristol, TN 37620. Manufactured by: AAI Pharma, 1726 North 23rd St., Wilmington, NC 28405. Revised February 2012

This monograph has been modified to include the generic and brand name in many instances.

What are the possible side effects of methimazole (Tapazole)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop using methimazole and call your doctor at once if you have a serious side effect such as:

  • fever, chills, sore throat, body aches, flu symptoms;
  • easy bruising or bleeding, unusual weakness;
  • blood in your urine or stools;
  • severe blistering, peeling, and red skin rash; or
  • nausea, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

Less serious side effects may include:

  • headache, drowsiness, dizziness;
  • mild nausea, vomiting, or stomach upset;
  • itching, minor skin rash;
  • muscle, joint, or nerve pain;
  • swelling; or
  • hair loss.

SIDE EFFECTS

Major adverse reactions (which occur with much less frequency than the minor adverse reactions) include inhibition of myelopoieses (agranulocytosis, granulocytopenia, thrombocytopenia, and aplastic anemia), drug fever, a lupus-like syndrome, insulin autoimmune syndrome (which can result inhypoglycemic coma), hepatitis (jaundice may persist for several weeks after discontinuation of the drug), periarteritis, and hypoprothrombinemia.  Nephritis occurs very rarely.

Minor adverse reactions include skin rash, urticaria, nausea, vomiting, epigastric distress, arthralgia, paresthesia, loss of taste, abnormal loss of hair, myalgia, headache, pruritus, drowsiness, neuritis, edema, vertigo, skin pigmentation, jaundice, sialadenopathy, and lymphadenopathy.

DRUG INTERACTIONS

Anticoagulants (oral)

Due to potential inhibition of vitamin K activity by methimazole, the activity of oral anticoagulants (e.g., warfarin) may be increased; additional monitoring of PT/INR should be considered, especially before surgical procedures.

β-adrenergic blocking agents

Hyperthyroidism may cause an increased clearance of beta blockers with a high extraction ratio. A dose reduction of beta-adrenergic blockers may be needed when a hyperthyroid patient becomes euthyroid.

Digitalis glycosides

Serum digitalis levels may be increased when hyperthyroid patients on a stable digitalis glycoside regimen become euthyroid; a reduced dosage of digitalis glycosides may be needed.

Theophylline

Theophylline clearance may decrease when hyperthyroid patients on a stable theophylline regimen become euthyroid; a reduced dose of theophylline may be needed.

methimazole5mg-eon methimazole5mg-mut methimazole5mg-par methimazole10mg-eon methimazole10mg-mut tapazole5mg tapazole10mg

WARNINGS

Congenital Malformations

Methimazole readily crosses the placental membranes and can cause fetal harm, particularly when administered in the first trimester of pregnancy. Rare instances of congenital defects, including aplasia cutis, craniofacial malformations (facial Amalformations (esophageal atresia with or without tracheoesophageal fistula; umbilical abnormalities) have occurred in infants born to mothers who received TAPAZOLE during pregnancy. If TAPAZOLE is used during pregnancy or if the patient becomes pregnant while taking this drug, the patient should be warned of the potential hazard to the fetus.

Since the above congenital defects have been reported in offspring of patients treated with TAPAZOLE, it may be appropriate to use other agents in pregnant women requiring treatment for hyperthyroidism, particularly during organogenesis, in the first trimester of pregnancy. If TAPAZOLE is used, the lowest possible dose to control the maternal disease should be given.

Agranulocytosis

Agranulocytosis is potentially a life-threatening adverse reaction of TAPAZOLE therapy. Patients should be instructed to immediately report to their physicians any symptoms suggestive of agranulocytosis, such as fever or sore throat. Leukopenia, thrombocytopenia, and aplastic anemia(pancytopenia) may also occur. The drug should be discontinued in the presence of agranulocytosis, aplastic anemia (pancytopenia), ANCA-positive vasculitis, hepatitis, or exfoliative dermatitis and the patient’s bone marrow indices should be monitored.

Liver Toxicity

Although there have been reports of hepatotoxicity (including acute liver failure) associated with TAPAZOLE, the risk of hepatotoxicity appears to be less with methimazole than with propylthiouracil, especially in the pediatric population. Symptoms suggestive of hepatic dysfunction (anorexia, pruritis, right upper quadrant pain, etc.) should prompt evaluation of liver function (bilirubin, alkaline phosphatase) and hepatocellur integrity (ALT, AST). Drug treatment should be discontinued promptly in the event of clinically significant evidence of liver abnormality including hepatic transaminase values exceeding 3 times the upper limit of normal.

Hypothyroidism

TAPAZOLE can cause hypothyroidism necessitating routine monitoring of TSH and free T4 levels with adjustments in dosing to maintain a euthyroid state. Because the drug readily crosses placental membranes, methimazole can cause fetal goiter and cretinism when administered to a pregnant woman. For this reason, it is important that a sufficient, but not excessive, dose be given during pregnancy

OVERDOSE

Signs and Symptoms

Symptoms may include nausea, vomiting, epigastric distress, headache, fever, joint pain, pruritus, and edema. Aplastic anemia (pancytopenia) oragranulocytosis may be manifested in hours to days. Less frequent events are hepatitis, nephrotic syndrome, exfoliative dermatitis, neuropathies, and CNS stimulation or depression. No information is available on the median lethal dose of the drug or the concentration of methimazole in biologic fluids associated with toxicity and/or death.

Treatment

To obtain up-to-date information about the treatment of overdose, a good resource is your certified Regional Poison Control Center. In managing overdosage, consider the possibility of multiple drug overdoses, interaction among drugs, and unusual drug kinetics in the patient.

CONTRAINDICATIONS

TAPAZOLE is contraindicated in the presence of hypersensitivity to the drug or any of the other product components.

This monograph has been modified to include the generic and brand name in many instances.

CLINICAL PHARMACOLOGY

Methimazole inhibits the synthesis of thyroid hormones and thus is effective in the treatment of hyperthyroidism. The drug does not inactivate existingthyroxine and tri-iodothyronine that are stored in the thyroid or circulating in the blood nor does it interfere with the effectiveness of thyroid hormones given by mouth or by injection.

Methimazole is readily absorbed in the gastrointestinal tract, metabolized in the liver, and excreted in the urine.

How should I take methimazole (Tapazole)?

Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Take methimazole with a full glass of water.

Methimazole can be taken with or without food, but you should take it the same way each time.

Methimazole can increase your risk of bleeding. If you need to have any type of surgery, tell the surgeon ahead of time that you are using this medication.

Methimazole can lower blood cells that help your body fight infections. This can make it easier for you to bleed from an injury or get sick from being around others who are ill. Your blood may need to be tested often. Visit your doctor regularly.

It is important to use methimazole regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.

Keep using this medication even if you feel fine or have no symptoms of hyperthyroidism. You may need to keep taking methimazole long term to control your condition. Stopping the medication could cause your symptoms to return.

Temporomandibular Joint Dysfunction

The temporomandibular joint (TMJ) connects your jaw to the side of your head. When it works well, it enables you to talk, chew, and yawn. For people with TMJ dysfunction, problems with the joint and muscles around it may cause

  • Pain that travels through the face, jaw, or neckIllustration of the skull and jaw bones
  • Stiff jaw muscles
  • Limited movement or locking of the jaw
  • Painful clicking or popping in the jaw
  • A change in the way the upper and lower teeth fit together

Jaw pain may go away with little or no treatment. Treatment may include simple things you can do yourself, such as eating soft foods or applying ice packs. It may also include pain medicines or devices to insert in your mouth. In rare cases, you might need surgery.

Tendinitis

Tendons are flexible bands of tissue that connect muscles to bones. They help your muscles move your bones. Tendinitis is the severe swelling of a tendon.

Tendinitis usually happens after repeated injury to an area such as the wrist or ankle. It causes pain and soreness around a joint. Some common forms of tendinitis are named after the sports that increase their risk. They include tennis elbow, golfer’s elbow, pitcher’s shoulder, swimmer’s shoulder, and jumper’s knee.

Doctors diagnose tendinitis with your medical history, a physical exam, and imaging tests. The first step in treatment is to reduce pain and swelling. Rest, wrapping or elevating the affected area, and medicines can help. Ice is helpful for recent, severe injuries. Other treatments include ultrasound, physical therapy, steroid injections, and surgery.

Thiamine

Thiamine is a vitamin, also called vitamin B1. Vitamin B1 is found in many foods including yeast, cereal grains, beans, nuts, and meat. It is often used in combination with other B vitamins, and found in many vitamin B complex products. Vitamin B complexes generally include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (niacin/niacinamide), vitamin B5 (pantothenic acid), vitamin B6 (pyridoxine), vitamin B12 (cyanocobalamin), and folic acid. However, some products do not contain all of these ingredients and some may include others, such as biotin, para-aminobenzoic acid (PABA), choline bitartrate, and inositol.

B1 rich foods, thiamine

Vitamin B1, also called thiamine, is a B complex vitamin. It is found in many foods and is vitally important to keeping a body operating properly.

“Thiamine is involved in many body functions including the nervous system, heart and muscles,” said Dr. Sherry Ross, gynecologist and Women’sHealth Expert at Providence Saint John’s Health Center in Santa Monica, California. “It is also important in the flow of electrolytes in and out of nerve and muscle cells, enzymatic processes and carbohydrate metabolism.”

According to the University of Maryland Medical Center (UMM), thiamine was named B1 because it was the first B complex vitamin to be discovered. According to the Mayo Clinic, it was also one of the first vitamins of any kind ever be classified.

People take thiamine for conditions related to low levels of thiamine (thiamine deficiency syndromes), including beriberi and inflammation of the nerves (neuritis) associated with pellagra or pregnancy.

Thiamine is also used for digestive problems including poor appetite, ulcerative colitis, and ongoing diarrhea.

Thiamine is also used for AIDS and boosting the immune system, diabetic pain, heart disease, alcoholism, aging, a type of brain damage called cerebellar syndrome, canker sores, vision problems such as cataracts and glaucoma, motion sickness, and improving athletic performance. Other uses include preventing cervical cancer and progression of kidney disease in patients with type 2 diabetes.

Some people use thiamine for maintaining a positive mental attitude; enhancing learning abilities; increasing energy; fighting stress; and preventing memory loss, including Alzheimer’s disease.

Healthcare providers give thiamine shots for a memory disorder called Wernicke’s encephalopathy syndrome, other thiamine deficiency syndromes in critically ill people, alcohol withdrawal, and coma.

How effective is it?

Natural Medicines Comprehensive Database rates effectiveness based on scientific evidence according to the following scale: Effective, Likely Effective, Possibly Effective, Possibly Ineffective, Likely Ineffective, Ineffective, and Insufficient Evidence to Rate.

The effectiveness ratings for THIAMINE (VITAMIN B1) are as follows:

Effective for…

  • Metabolic disorders. Taking thiamine by mouth helps correct metabolic disorders associated with genetic diseases, including Leigh’s disease, maple syrup urine disease, and others.
  • Thiamine deficiency. Taking thiamine by mouth helps prevent and treat thiamine deficiency.
  • Brain disorder due to thiamine deficiency (Wernicke-Korsakoff syndrome). Thiamine helps decrease the risk and symptoms of a specific brain disorder called Wernicke-Korsakoff syndrome (WKS). This brain disorder is related to low levels of thiamine (thiamine deficiency) and is often seen in alcoholics. Between 30% and 80% of alcoholics are believed to have thiamine deficiency. Giving thiamine shots seems to help decrease the risk of developing WKS and decrease symptoms of WKS during alcohol withdrawal.

Possibly effective for…

  • Cataracts. High thiamine intake as part of the diet is associated with a reduced risk of developing cataracts.
  • Kidney disease in people with diabetes. Early research shows that taking high-dose thiamine (100 mg three times daily) for 3 months decreases the amount of albumin in the urine in people with type 2 diabetes. Albumin in the urine is an indication of kidney damage.
  • Painful menstruation (dysmenorrhea). Early research suggests that taking thiamine for 90 days stops pain associated with menstruation in girls 12-21 years-old.

Possibly ineffective for…

  • Repelling mosquitos. Some research shows that taking B vitamins, including thiamine, does not help repel mosquitos.

Insufficient evidence to rate effectiveness for…

  • Athletic performance. Some research suggests that taking thiamine together with pantethine and pantothenic acid (vitamin B5) does not improve muscle strength or endurance in athletes.
  • Preventing cervical cancer. Some research suggests that increasing intake of thiamine from dietary and supplement sources, along with other folic acid, riboflavin, and vitamin B12, might decrease the risk of precancerous spots on the cervix.
  • Poor appetite.
  • Ulcerative colitis.
  • Chronic diarrhea.
  • Stomach problems.
  • Brain conditions.
  • AIDS.
  • Heart disease.
  • Alcoholism.
  • Stress.
  • Aging.
  • Canker sores.
  • Other conditions.

More evidence is needed to rate thiamine for these uses.

How does it work?

Thiamine is required by our bodies to properly use carbohydrates.

Are there safety concerns?

Thiamine is LIKELY SAFE when taken by mouth in appropriate amounts, although rare allergic reactions and skin irritation have occurred. It is also LIKELY SAFE when given appropriately intravenously (by IV) by a healthcare provider. Thiamine shots are an FDA-approved prescription product.

Thiamine might not properly enter the body in some people who have liver problems, drink a lot of alcohol, or have other conditions.

Special precautions & warnings:

Pregnancy and breast-feeding: Thiamine is LIKELY SAFE for pregnant or breast-feeding women when taken in the recommended amount of 1.4 mg daily. Not enough is known about the safety of using larger amounts during pregnancy or breast-feeding.

Are there interactions with medications?

It is not known if this product interacts with any medicines.

Before taking this product, talk with your health professional if you take any medications.

Are there interactions with herbs and supplements?

Areca
Areca (betel) nuts change thiamine chemically so it doesn’t work as well. Regular, long-term chewing of betel nuts may contribute to thiamine deficiency.
Horsetail
Horsetail (Equisetum) contains a chemical that can destroy thiamine in the stomach, possibly leading to thiamine deficiency. The Canadian government requires that equisetum-containing products be certified free of this chemical. Stay on the safe side, and don’t use horsetail if you are at risk for thiamine deficiency.

Are there interactions with foods?

Coffee and tea
Chemicals in coffee and tea called tannins can react with thiamine, converting it to a form that is difficult for the body to take in. This could lead to thiamine deficiency. Interestingly, thiamine deficiency has been found in a group of people in rural Thailand who drink large amounts of tea (>1 liter per day) or chew fermented tea leaves long-term. However, this effect hasn’t been found in Western populations, despite regular tea use. Researchers think the interaction between coffee and tea and thiamine may not be important unless the diet is low in thiamine or vitamin C. Vitamin C seems to prevent the interaction between thiamine and the tannins in coffee and tea.
Seafood
Raw freshwater fish and shellfish contain chemicals that destroy thiamine. Eating a lot of raw fish or shellfish can contribute to thiamine deficiency. However, cooked fish and seafood are OK. They don’t have any effect on thiamine, since cooking destroys the chemicals that harm thiamine.

What dose is used?

The following doses have been studied in scientific research:

BY MOUTH:

  • For adults with somewhat low levels of thiamine in their body (mild thiamine deficiency): the usual dose of thiamine is 5-30 mg daily in either a single dose or divided doses for one month. The typical dose for severe deficiency can be up to 300 mg per day.
  • For reducing the risk of getting cataracts: a daily dietary intake of approximately 10 mg of thiamine.

As a dietary supplement in adults, 1-2 mg of thiamine per day is commonly used. The daily recommended dietary allowances (RDAs) of thiamine are: Infants 0-6 months, 0.2 mg; infants 7-12 months, 0.3 mg; children 1-3 years, 0.5 mg; children 4-8 years, 0.6 mg; boys 9-13 years, 0.9 mg; men 14 years and older, 1.2 mg; girls 9-13 years, 0.9 mg; women 14-18 years, 1 mg; women over 18 years, 1.1 mg; pregnant women, 1.4 mg; and breast-feeding women, 1.5 mg.

BY INJECTION:

  • Healthcare providers give thiamine shots for treating and preventing symptoms of alcohol withdrawal (Wernicke-Korsakoff syndrome).

Other names

Aneurine Hydrochloride, Antiberiberi Factor, Antiberiberi Vitamin, Antineuritic Factor, Antineuritic Vitamin, B Complex Vitamin, Chlorhydrate de Thiamine, Chlorure de Thiamine, Complexe de Vitamine B, Facteur Anti-béribéri, Facteur Antineuritique, Hydrochlorure de Thiamine, Mononitrate de Thiamine, Nitrate de Thiamine, Thiamine Chloride, Thiamine HCl, Thiamine Hydrochloride, Thiamin Mononitrate, Thiamine Mononitrate, Thiamine Nitrate, Thiaminium Chloride Hydrochloride, Tiamina, Vitamin B1, Vitamin B-1, Vitamina B1, Vitamine Anti-béribéri, Vitamine Antineuritique, Vitamine B1.

Methodology

To learn more about how this article was written, please see the Natural Medicines Comprehensive Database methodology.

Toe Injuries and Disorders

Fourteen of the 26 bones in your feet are in your toes. The toes, particularly your big toe, help you move and keep your balance. Playing sports, running, and receiving a blow to the foot can damage your toes. Wearing shoes that are too loose or too tight can also cause toe problems. Certain diseases, such as severe arthritis, can cause toe problems and pain. Gout often causes pain in the big toe.

Common toe problems include

  • Corns and bunions
  • Ingrown toenails
  • Toe joint sprains and dislocations
  • Fractured toe bones

Treatments for toe injuries and disorders vary. They might include shoe inserts or special shoes, padding, taping, medicines, rest, and in severe cases, surgery.

 

Tramasol

What is Tramasol™

Tramasol™ combines 540 mg of two alkaloids that act as analgesics, and 60 mg of C6H8O6 or ascorbic acid. The chemical composition of Tramasol™ contains the following: 7-hydroxymitragynine, Mitragynine pseudoindoxyl, Raubasine, Corynantheidine, and Rhynchophyline.

The chemical name for Tramasol™ is Mitragynine + 7-hydroxymitragynine + C6H8O6. Tramasol™ is a bitter, crystalline and odorless powder pressed into 600 mg capsules.

Usage

Tramasol™ provides superior pain relief from a variety of immediate and chronic pain triggers such as migraines, muscle pain, back pain, and more. It contains powerful alkaloids such as mitragynine and 7-hydroxymitragynine, which react with the human brain by tapping into the sensors that receive pain signals and define mood patterns. Tramasol™ can be used either as a stimulant or depressant, depending on the approved dosage. Tramasol™ is also rich in C6H8O6, or ascorbic acid, whose antioxidant properties help boost the immune system, thus giving you a faster recovery time.

Tramasol™ is an effective analgesic or painkiller, and chronic pain patients have reported experiencing little to no side effects while using Tramasol™. This provides patients with a better option compared to alternative prescription drugs in the market today.

Tramasol™ can also be used to relieve the symptoms of opiate withdrawal because of its superior pain-relieving powers and chemically identical effects on the brain as opiates. Tramasol™ contains potent alkaloids that are more effective than morphine. When taken at the right dosage, it can be used to transition to a healthier lifestyle without harmful drawbacks or withdrawals.

How Does it Work?

There are 28 known naturally occurring alkaloids found in Tramasol™, and these alkaloids work together to produce powerful pain-relieving effects. The most dominant alkaloids are mitragynine and 7-hydroxymitragynine, both of which act as opioid receptor agonists. Aside from pain relief, the alkaloids in Tramasol™ also work on stimulating one’s cognitive abilities and enhancing overall mood.

Mitragynine

Mitragynine consists of the majority of Tramasol™’s alkaloid content. While mitragynine’s effects will vary from person to person, here are the most common effects to be expected from this alkaloid:

  • Pain relief
  • Stimulation
  • Anti-malarial
  • Anti-diarrheal
  • Anti-tussive

Of these effects, the two most prominent are stimulation and pain relief. When you feel a sudden burst of energy or liveliness after taking Tramasol™, it is mostly the mitragynine working.

Mitragynine’s effects vary greatly depending on the dosage. At lower doses, mitragynine tends to be more stimulating. At increased doses, mitragynine can produce a calming effect that is good for treating pain.

Mitragynine has varying effects because it works with three different receptors in the brain. The effects that you feel vary according to how much mitragynine has interacted with these sensors.

When reacting with the adrenergic receptors, mitragynine is mainly a stimulant because it releases adrenaline into your body’s system.

When mitragynine interacts with mu opioid receptors, its primary effects are mostly for pain relief.

7-hydroxymitragynine

Although there is only very little of this alkaloid in Tramasol™, this is the most potent of them all. Unlike mitragynine, this alkaloid acts only in a very small area, thus making it act quicker and stronger.