What are the uses of Cardizem CD oral medication? What are the side effects of Cardizem CD? What interactions does Cardizem CD have? What warnings are associated with Cardizem CD? How should Cardizem CD be dosed?

Uses of Cardizem CD Oral Medication

Diltiazem, the active ingredient in Cardizem CD, is used to treat high blood pressure (hypertension) and prevent chest pain (angina). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. When used regularly, diltiazem can decrease the number and severity of episodes of chest pain from angina. It may also help increase your ability to exercise.

Diltiazem is a calcium channel blocker that works by relaxing blood vessels in the body and heart, allowing blood to flow more easily. It also lowers your heart rate, helping the heart work less hard and lowering blood pressure.

How to Use Cardizem CD

Take Cardizem CD by mouth with or without food, usually once daily or as directed by your doctor. Swallow the capsules whole – do not crush or chew them, as this can release all the drug at once and increase your risk of side effects.

Your doctor may gradually increase your dose. Follow their instructions carefully. The dosage is based on your medical condition, response to treatment, and other medications you may be taking.

Use Cardizem CD regularly to get the most benefit. Take it at the same time each day to help you remember. Continue taking it even if you feel well, as most people with high blood pressure do not feel sick. It may take 2-4 weeks to get the full benefit for high blood pressure.

Cardizem CD should not be used to treat angina attacks when they occur. Use other medications like nitroglycerin as directed by your doctor for that purpose.

Side Effects of Cardizem CD

Common side effects of Cardizem CD include dizziness, lightheadedness, weakness, nausea, flushing, constipation, and headache. If any of these effects persist or worsen, tell your doctor or pharmacist.

To lower the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.

Tell your doctor right away if you experience serious side effects like nausea/vomiting that doesn’t stop, fainting, new or worsening heart failure symptoms, slow/irregular heartbeat, mental/mood changes, severe abdominal pain, or dark urine.

A very serious allergic reaction to Cardizem CD is rare, but seek immediate medical help if you notice symptoms like rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, or trouble breathing.

Precautions and Interactions

Before taking Cardizem CD, tell your doctor or pharmacist if you are allergic to it or have a history of certain heart rhythm problems, liver disease, kidney disease, or heart failure.

Cardizem CD may make you dizzy. Avoid driving, using machinery, or doing anything requiring alertness until you know how this medication affects you. Limit alcohol and talk to your doctor if you use marijuana, as these can increase dizziness.

Inform your doctor and dentist that you are taking Cardizem CD before any surgery. Older adults may be more sensitive to the side effects of this drug.

Use Cardizem CD cautiously during pregnancy, discussing the risks and benefits with your doctor.

Cardizem CD Dosing

The dosage of Cardizem CD is based on your medical condition and response to treatment. Your doctor will determine the appropriate dose and may adjust it over time.

Cardizem CD is typically taken once daily. Swallow the capsules whole and do not crush or chew them.

Be sure to take Cardizem CD regularly as prescribed to get the full benefit. Do not stop taking it without first consulting your doctor, as this could worsen your condition.

Interactions and Warnings

Tell your doctor about all the medications, including prescription drugs, over-the-counter products, and herbal supplements, that you are taking. Cardizem CD can interact with many different drugs.

Avoid drinking grapefruit juice while taking Cardizem CD, as it can increase the level of the drug in your body and your risk of side effects.

Do not use Cardizem CD to treat angina attacks when they occur. Use other medications like nitroglycerin as directed by your doctor for that purpose.

Contact your doctor if your condition worsens, such as if your chest pain becomes more severe or your routine blood pressure readings increase.

Cardizem CD Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Uses

Diltiazem is used to treat high blood pressure (hypertension) and prevent chest pain (angina). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. When used regularly, diltiazem can decrease the number and severity of episodes of chest pain from angina. It may help increase your ability to exercise.Diltiazem is called a calcium channel blocker. It works by relaxing blood vessels in the body and heart so blood can flow more easily. Diltiazem also lowers your heart rate. These effects help the heart work less hard and lower blood pressure.

How to use Cardizem CD

Take this medication by mouth with or without food, usually once daily or as directed by your doctor. Swallow the capsules whole. Do not crush or chew the capsules. Doing so can release all of the drug at once and may increase your risk of side effects.

Your doctor may gradually increase your dose. Follow your doctor’s instructions carefully. The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Use this medication regularly to get the most benefit from it. To help you remember, use it at the same time each day. Keep taking this medication even if you feel well. Most people with high blood pressure do not feel sick. For the treatment of high blood pressure, it may take 2 to 4 weeks before you get the full benefit of this drug.

This medication must be taken regularly to prevent angina. It should not be used to treat angina when it occurs. Use other medications (such as nitroglycerin placed under the tongue) to relieve an angina attack as directed by your doctor. Consult your doctor or pharmacist for details.

Tell your doctor if your condition worsens (for example, your chest pain worsens or your routine blood pressure readings increase).

Side Effects

Dizziness, lightheadedness, weakness, nausea, flushing, constipation, and headache may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

To lower the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.

Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: nausea/vomiting that doesn’t stop, fainting, new or worsening symptoms of heart failure (such as shortness of breath, swelling ankles/feet, unusual tiredness, unusual/sudden weight gain), slow/irregular/pounding/fast heartbeat, mental/mood changes (such as depression, agitation), unusual dreams, severe stomach/abdominal pain, dark urine, yellowing eyes/skin.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Precautions

Before taking diltiazem, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: certain types of heart rhythm problems (such as sick sinus syndrome/atrioventricular block), liver disease, kidney disease, heart failure.

This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).

Before having surgery, tell your doctor or dentist that you are taking this medication.

Older adults may be more sensitive to the side effects of this drug, especially dizziness, constipation, or swelling ankles/feet.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

This drug passes into breast milk and may have undesirable effects on a nursing infant. Consult your doctor before breast-feeding.

Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Some products that may interact with this drug include: digoxin, fingolimod.

Other medications can affect the removal of diltiazem from your body, which may affect how this medication works. Examples include cimetidine, St. John’s wort, azole antifungals such as ketoconazole, macrolide antibiotics such as erythromycin, rifamycins including rifabutin and rifampin.

This medication can slow down the removal of other medications from your body, which may affect how they work. Examples of affected drugs include aprepitant/fosaprepitant, asunaprevir, buspirone, colchicine, elacestrant, flibanserin, ivabradine, lomitapide, certain benzodiazepines (triazolam, midazolam), among others.

Some products have ingredients that could raise your heart rate or blood pressure. Tell your pharmacist what products you are using, and ask how to use them safely (especially cough-and-cold products, diet aids, or NSAIDs such as ibuprofen/naproxen).

Does Cardizem CD interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

Do not share this medication with others. Talk with your doctor about making changes to your lifestyle that may help this medication work better (such as stress reduction programs, exercise, and dietary changes).

Lab and/or medical tests (such as kidney/liver function, pulse, blood pressure, EKG) may be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.

There are different brands and types of this medication available. Many do not have the same effects. Do not change brands or types without consulting your doctor or pharmacist.

Have your blood pressure and pulse (heart rate) checked regularly while taking this medication. Learn how to check your own blood pressure and pulse at home, and share the results with your doctor.

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Images

Cardizem CD 360 mg capsule,extended release

Color: light blue,whiteShape: oblongImprint: cardizem CD 360 mg

This medicine is a light blue white, oblong, capsule imprinted with “cardizem CD 360 mg”.

Cardizem CD 300 mg capsule,extended release

Color: light gray,blueShape: oblongImprint: cardizem CD 300 mg

This medicine is a light blue white, oblong, capsule imprinted with “cardizem CD 360 mg”.

Cardizem CD 240 mg capsule,extended release

Color: blueShape: oblongImprint: cardizem CD 240 mg

This medicine is a light blue white, oblong, capsule imprinted with “cardizem CD 360 mg”.

Cardizem CD 180 mg capsule,extended release

Color: light turquoise blue,blueShape: oblongImprint: cardizem CD 180 mg

This medicine is a light blue white, oblong, capsule imprinted with “cardizem CD 360 mg”.

Cardizem CD 120 mg capsule,extended release

Color: light turquoise blueShape: oblongImprint: cardizem CD 120 mg

This medicine is a light blue white, oblong, capsule imprinted with “cardizem CD 360 mg”.

Next

Save up to 80% on your prescriptions.

Available coupons

Save up to 80% on your prescription with WebMDRx

Drug Survey

Are you currently using Cardizem CD?

This survey is being conducted by the WebMD marketing sciences department.

Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.

CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

Diltiazem Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Uses

Diltiazem is used to treat high blood pressure (hypertension) and prevent chest pain (angina). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. When used regularly, diltiazem can decrease the number and severity of episodes of chest pain from angina. It may help increase your ability to exercise.Diltiazem is called a calcium channel blocker. It works by relaxing blood vessels in the body and heart so blood can flow more easily. Diltiazem also lowers your heart rate. These effects help the heart work less hard and lower blood pressure.

How to use diltiazem oral

Take this medication by mouth with or without food, usually once daily or as directed by your doctor. Swallow the capsules whole. Do not crush or chew the capsules. Doing so can release all of the drug at once and may increase your risk of side effects.

Your doctor may gradually increase your dose. Follow your doctor’s instructions carefully. The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Use this medication regularly to get the most benefit from it. To help you remember, use it at the same time each day. Keep taking this medication even if you feel well. Most people with high blood pressure do not feel sick. For the treatment of high blood pressure, it may take 2 to 4 weeks before you get the full benefit of this drug.

This medication must be taken regularly to prevent angina. It should not be used to treat angina when it occurs. Use other medications (such as nitroglycerin placed under the tongue) to relieve an angina attack as directed by your doctor. Consult your doctor or pharmacist for details.

Tell your doctor if your condition worsens (for example, your chest pain worsens or your routine blood pressure readings increase).

Side Effects

Dizziness, lightheadedness, weakness, nausea, flushing, constipation, and headache may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

To lower the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.

Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: nausea/vomiting that doesn’t stop, fainting, new or worsening symptoms of heart failure (such as shortness of breath, swelling ankles/feet, unusual tiredness, unusual/sudden weight gain), slow/irregular/pounding/fast heartbeat, mental/mood changes (such as depression, agitation), unusual dreams, severe stomach/abdominal pain, dark urine, yellowing eyes/skin.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Precautions

Before taking diltiazem, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: certain types of heart rhythm problems (such as sick sinus syndrome/atrioventricular block), liver disease, kidney disease, heart failure.

This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).

Before having surgery, tell your doctor or dentist that you are taking this medication.

Older adults may be more sensitive to the side effects of this drug, especially dizziness, constipation, or swelling ankles/feet.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

This drug passes into breast milk and may have undesirable effects on a nursing infant. Consult your doctor before breast-feeding.

Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Some products that may interact with this drug include: digoxin, fingolimod.

Other medications can affect the removal of diltiazem from your body, which may affect how this medication works. Examples include cimetidine, St. John’s wort, azole antifungals such as ketoconazole, macrolide antibiotics such as erythromycin, rifamycins including rifabutin and rifampin.

This medication can slow down the removal of other medications from your body, which may affect how they work. Examples of affected drugs include aprepitant/fosaprepitant, asunaprevir, buspirone, colchicine, elacestrant, flibanserin, ivabradine, lomitapide, certain benzodiazepines (triazolam, midazolam), among others.

Some products have ingredients that could raise your heart rate or blood pressure. Tell your pharmacist what products you are using, and ask how to use them safely (especially cough-and-cold products, diet aids, or NSAIDs such as ibuprofen/naproxen).

Does diltiazem oral interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

Do not share this medication with others. Talk with your doctor about making changes to your lifestyle that may help this medication work better (such as stress reduction programs, exercise, and dietary changes).

Lab and/or medical tests (such as kidney/liver function, pulse, blood pressure, EKG) may be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.

There are different brands and types of this medication available. Many do not have the same effects. Do not change brands or types without consulting your doctor or pharmacist.

Have your blood pressure and pulse (heart rate) checked regularly while taking this medication. Learn how to check your own blood pressure and pulse at home, and share the results with your doctor.

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Images

diltiazem CD 300 mg capsule,extended release 24 hr

Color: orangeShape: oblongImprint: 300 mg Andrx 600

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 240 mg capsule,extended release 24 hr

Color: dark greenShape: oblongImprint: par C831

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 180 mg capsule,extended release 24 hr

Color: dark green,blueShape: oblongImprint: par C830

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 120 mg capsule,extended release 24 hr

Color: light grayShape: oblongImprint: par C829

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 240 mg capsule,extended release 24 hr

Color: dark greenShape: oblongImprint: BVF 240 BVF 240

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 300 mg capsule,extended release 24 hr

Color: light gray,dark greenShape: oblongImprint: par C832

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 240 mg capsule,extended release 24 hr

Color: light blue,whiteShape: oblongImprint: 597

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 120 mg capsule,extended release 24 hr

Color: light green,whiteShape: oblongImprint: 595

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 180 mg capsule,extended release 24 hr

Color: light blue,grayShape: oblongImprint: 596

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 180 mg capsule,extended release 24 hr

Color: light blue,light turquoiseShape: oblongImprint: T027 180

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 300 mg capsule,extended release 24 hr

Color: light blue,grayShape: oblongImprint: T029 300

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 300 mg capsule,extended release 24 hr

Color: gray,blueShape: oblongImprint: 678 678

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 240 mg capsule,extended release 24 hr

Color: light blueShape: oblongImprint: T028 240

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 120 mg capsule,extended release 24 hr

Color: light turquoise blueShape: oblongImprint: T026 120

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 240 mg capsule,extended release 24 hr

Color: dark blue,light blueShape: oblongImprint: N367 240

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 300 mg capsule,extended release 24 hr

Color: dark blue,whiteShape: oblongImprint: N368 300

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 360 mg capsule,extended release 24 hr

Color: dark blueShape: oblongImprint: N369 360

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 180 mg capsule,extended release 24 hr

Color: light blueShape: oblongImprint: N366 180

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 120 mg capsule,extended release 24 hr

Color: whiteShape: oblongImprint: N365 120

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 360 mg capsule,extended release 24 hr

Color: light blue,whiteShape: oblongImprint: T030 360

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 300 mg capsule,extended release 24 hr

Color: ivory,dark greenShape: oblongImprint: BVF 300 BVF 300

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 360 mg capsule,extended release 24 hr

Color: white,blueShape: oblongImprint: 679 679

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 240 mg capsule,extended release 24 hr

Color: blueShape: oblongImprint: 677 677

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 180 mg capsule,extended release 24 hr

Color: light turquoise blue,blueShape: oblongImprint: 676 676

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 120 mg capsule,extended release 24 hr

Color: light greenShape: oblongImprint: BVF 120 BVF 120

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 180 mg capsule,extended release 24 hr

Color: light green,dark greenShape: oblongImprint: BVF 180 BVF 180

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 360 mg capsule,extended release 24 hr

Color: light blue,whiteShape: oblongImprint: cardizem CD 360 mg

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 360 mg capsule,extended release 24 hr

Color: white,grayShape: oblongImprint: 599

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 300 mg capsule,extended release 24 hr

Color: light green,grayShape: oblongImprint: 598

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

diltiazem CD 360 mg capsule,extended release 24 hr

Color: white,blueShape: oblongImprint: logo and 2918 logo and 2918

This medicine is a orange, oblong, capsule imprinted with “300 mg” and “Andrx 600”.

Next

Save up to 80% on your prescriptions.

Available coupons

Save up to 80% on your prescription with WebMDRx

Drug Survey

Are you currently using diltiazem oral?

This survey is being conducted by the WebMD marketing sciences department.

Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.

CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

Diltiazem Lannacher – official instructions for use, analogues, price, availability in pharmacies 002 International Nonproprietary Name (INN):

diltiazem

Dosage form:

prolonged release film-coated tablets.

Composition:

one tablet contains: active ingredient: diltiazem hydrochloride 90 mg, 180 mg; excipients: lactose monohydrate 60.0/120.0 mg, methyl methacrylate and ethyl acrylate copolymer [2 : 1] 4.5/9.0 mg, methacrylic acid and ethyl acrylate copolymer (1:1) 57.75/79, 5 mg, methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer [1 : 2 : 0. 1] 7.5/15.0 mg, hypromellose 5 mPa*s 9.5/15.0 mg, magnesium stearate 0.75/1, 5 mg; shell: macrogol 6000 2.247/2.996 mg, hypromellose 5 mPa*s 1.875/2.500 mg, titanium dioxide 1.017/1.356 mg, talc 9.303 / 12.404 mg, methyl methacrylate and ethyl acrylate copolymer [2: 1] 0.558 / 0.744 mg.

Description

Round, biconvex, white film-coated tablets, white tablet core in cross section.

Pharmacotherapeutic group:

slow calcium channel blocker.

ATX code C08DB01

Pharmacological properties

Pharmacodynamics

Diltiazem is a derivative of benzothiazepines; has antiarrhythmic, antianginal and hypotensive activity. Blocker of “slow” calcium channels (BCCC), reduces the intracellular content of calcium ions in cardiomyocytes and smooth muscle cells, dilates coronary and peripheral arteries and arterioles, reduces total peripheral vascular resistance (TPVR), smooth muscle tone, increases coronary, cerebral and renal blood flow , reduces the heart rate (HR).
The antiarrhythmic effect of is due to the suppression of the transport of ionized calcium in the tissues of the heart, which leads to an increase in the effective refractory period and a lengthening of the conduction time in the atrioventricular (AV) node (has clinical significance in patients with sick sinus syndrome, elderly patients who have blockade calcium channels can interfere with the generation of an impulse in the sinus node and cause sinoatrial (SA) blockade). The normal atrial action potential or intraventricular conduction is not altered (normal sinus rhythm is usually unaffected), but depolarization rate and conduction rate decrease as the amplitude of atrial contraction decreases. The anterograde effective refractory period in additional bypass conduction bundles may be shortened. The antianginal effect is due to the expansion of peripheral vessels and a decrease in systemic arterial pressure (afterload), which leads to a decrease in myocardial wall tension and its oxygen demand. In concentrations that do not lead to the appearance of a negative inotropic effect, it causes relaxation of the smooth muscles of the coronary vessels and dilatation of both large and small arteries.
The antihypertensive effect of is due to dilatation of resistive vessels and a decrease in peripheral vascular resistance. The degree of reduction in blood pressure (BP) correlates with its initial level (in “normotics” there is a minimal effect on blood pressure). Reduces blood pressure both in the “lying” and “standing” positions. Rarely causes postural arterial hypotension and reflex tachycardia. Does not change or slightly reduces the maximum heart rate during exercise. Long-term therapy does not lead to hypercatecholaminemia, an increase in the activity of the renin-angiotensin-aldosterone system. Reduces renal and peripheral effects of angiotensin II. Improves diastolic relaxation of the myocardium in arterial hypertension, coronary heart disease, hypertrophic obstructive cardiomyopathy, reduces platelet aggregation.
Has a minimal effect on the smooth muscles of the gastrointestinal tract (GIT). During long-term (8 months) therapy, tolerance does not develop. Does not affect the lipid profile of the blood.
Able to cause regression of left ventricular hypertrophy in patients with arterial hypertension. The onset of action when taken orally is 2-3 hours. The duration of action is 12-14 hours.
The maximum severity of the hypotensive effect is achieved within 2 weeks.

Firmacokinetics

After oral administration, it is rapidly and almost completely absorbed from the gastrointestinal tract. The time to reach the maximum concentration in blood plasma is 6-14 hours. Communication with blood plasma proteins is 70-80% (with albumins – 35-40%). It is intensively metabolized in the liver by deacetylation and demethylation (with the participation of CYP3A4, CYP3A5 and CYP3A7 isoenzymes) with the formation of an active metabolite of deacetyldilthiazem, which is determined in plasma by 5-10 times lower concentration than diltiazem, and has 2-4 times less activity.
Passes into breast milk.
The half-life of diltiazem when taken orally is biphasic: early – 20-30 minutes, final – 3.5 hours (5-8 hours – at high and repeated doses). The half-life of the drug Diltiazem Lannacher in the dosage form of a prolonged-release tablet of 90 mg and 180 mg is up to 10 hours. It is excreted through the intestines with bile (65%) and kidneys (35%, including 2-4% unchanged).
The pharmacokinetics of diltiazem does not change with long-term use.
The drug does not accumulate and does not induce its own metabolism. In patients with angina pectoris and impaired renal function, the pharmacokinetics of diltiazem does not change. In patients with hepatic insufficiency, bioavailability increases and the half-life is prolonged. Diltiazem clearance may also be reduced in the elderly. It is not excreted during hemodialysis and peritoneal dialysis.

Indications for use

• Arterial hypertension
• Prevention of angina attacks (including Prinzmetal’s angina)
• Prevention of attacks of supraventricular arrhythmias (paroxysmal tachycardia, atrial fibrillation or flutter, extrasystoles)

Contraindications

Hypersensitivity to the drug and to other benzothiazepine derivatives, sinoatrial and atrioventricular block II and III degree (except for patients with a pacemaker), severe bradycardia, sick sinus syndrome without the use of an artificial pacemaker, cardiogenic shock, Wolf’s syndrome Parkinson-White, Lown-Ganong-Levin syndrome in combination with atrial flutter or fibrillation (except for patients with a pacemaker), severe arterial hypotension (systolic blood pressure less than 90 mm Hg), acute heart failure, chronic heart failure (in the stage of decompensation), myocardial infarction with signs of left ventricular failure, ventricular tachycardia with a wide QRS complex, pregnancy, lactation, age up to 18 years (efficacy and safety have not been established ), lactose intolerance, lactase deficiency and glucose-galactose malabsorption.

With caution should be used in patients with severe impairment of liver and kidney function, acute porphyria, severe aortic stenosis, in the acute phase of myocardial infarction (without signs of left ventricular failure), hypertrophic obstructive cardiomyopathy, mild to moderate arterial hypotension, atrioventricular block I degree or prolongation of the PQ interval, with simultaneous use with beta-blockers or digoxin, compensated chronic heart failure, with a tendency to bradycardia, in old age.

Pregnancy and lactation

Diltiazem Lannacher is contraindicated during pregnancy and lactation.
Pregnancy should be excluded in women of childbearing age prior to the administration of diltiazem.

Dosage and Administration

Tablets should be taken orally, before meals, without chewing and with a small amount of liquid. The dosing regimen is set individually.
The initial dose of Diltiazem Lannacher is 1 tablet of 90 mg 2 times a day. The average daily dose is 180-270 mg. Correction of the dosing regimen can be carried out only after 2 weeks. The maximum daily dose is 360 mg. With long-term treatment with a good therapeutic effect, a dose reduction is possible.

Side effects

From the side of the cardiovascular system: bradycardia, ventricular extrasystole, chronic heart failure, sinoauricular blockade, atrioventricular blockade up to asystole, pronounced decrease in blood pressure, syncope, reddening of the skin, angina pectoris, arrhythmia (including flutter and ventricular fibrillation), tachycardia, shortness of breath, peripheral edema. When used in high doses – angina pectoris, bradycardia, atrioventricular blockade.
From the digestive system: dry mouth, increased appetite, vomiting, nausea, heartburn, diarrhea, hypertrophic gingivitis, constipation, hypercreatininemia, abdominal pain, liver dysfunction, intestinal obstruction.
From the side of the central nervous system: headache, general weakness, asthenia, increased fatigue, anxiety, dizziness, drowsiness, insomnia, depression, a state of pathological fear, extrapyramidal disorders, parkinsonism (ataxia, “masklike” face, “shuffling” gait , stiffness of the arms or legs, trembling of the hands and fingers, difficulty swallowing). When used in high doses – paresthesia.
From the senses: visual impairment (transient blindness).
Allergic reactions: increased photosensitivity, itching, skin rash, flushing of the facial skin, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis.
Others: taking the drug may lead to an increase in the concentration of “liver” enzymes in the blood serum, peripheral edema. When used in high doses – pulmonary edema (difficulty breathing, coughing, stridor breathing), thrombocytopenia, agranulocytosis, galactorrhea, weight gain. With a sharp withdrawal of the drug, a “withdrawal” syndrome may develop with concomitant tachycardia, arterial hypertension and worsening of the course of angina pectoris.

Overdose

Symptoms: bradycardia, pronounced decrease in blood pressure, turning into collapse, impaired atrioventricular and sinoatrial conduction, heart failure, cardiogenic shock, asystole, nausea, vomiting, metabolic acidosis, hyperkalemia.
Treatment: depending on the severity of overdose manifestations. It is necessary to wash the stomach, prescribe activated charcoal, further treatment is symptomatic. If necessary, it is recommended to prescribe atropine, isoprenaline, dopamine or dobutamine, and also, with severe conduction disturbances, the use of pacing is possible.
Hemodialysis and peritoneal dialysis are not effective.

Interaction with other drugs

Interaction with other drugs

Pharmacodynamic

At the same time taking diltiazem with antihypertensive drugs, an increase in the antihypertensive effect is noted.
Co-administration of diltiazem and digoxin may increase the concentration of digoxin in the blood.
While taking diltiazem with antiarrhythmic drugs, beta-blockers, cardiac glycosides, bradycardia, impaired atrioventricular conduction, and symptoms of heart failure may develop.
When used simultaneously with adenosine, the risk of developing prolonged bradycardia is increased.
Salicylates additionally inhibit the ability to aggregate platelets.
Ethanol: increased antihypertensive effect.
Procainamide, quinidine and other drugs that prolong the QT interval increase the risk of significant QT prolongation.
Means for inhalation anesthesia (derivatives of hydrocarbons), thiazide diuretics and other drugs that reduce blood pressure increase the hypotensive effect of diltiazem.
Phenytoin reduces the effect of diltiazem.
Antipsychotics (neuroleptics) enhance the antihypertensive effect of diltiazem.
Perhaps the simultaneous appointment of nitrates (including prolonged forms).
Lithium preparations may increase the neurotoxic effects of diltiazem (nausea, vomiting, diarrhea, ataxia, trembling and/or tinnitus).
Indomethacin and other non-steroidal anti-inflammatory drugs, glucocorticosteroids and estrogens, as well as sympathetic drugs reduce the hypotensive effect.
Enhances the cardiodepressive effect of general anesthetics.

Pharmacokinetic

Cimetidine weakens the process of biotransformation of diltiazem in the liver, slows down its excretion, increasing the duration of action of diltiazem.
Diltiazem increases the concentration of theophylline and karmazepine in blood plasma (40-70%) and increases the risk of adverse reactions, incl. ataxia, nystagmus, diplopia, headache, vomiting, confusion, and also increases the concentration of cyclosporine, digoxin (up to 50%), imipramine, lithium and midazolam.
Enhances the effect of oral hypoglycemic agents (eg chlorpropamide and glipizide).
With the simultaneous use of diltiazem and cyclosporine in patients with a transplanted kidney, it is possible to develop intoxication with the latter, paresthesia. Therefore, it is necessary to carefully monitor the level of plasma concentrations of cyclosporine in this group of patients. Food intake increases the absorption and bioavailability of diltiazem by 20-30%.
May increase the bioavailability of propranolol. Increases the concentration of moracizin in the blood plasma.
Phenobarbital, diazepam, rifampicin reduce the concentration of diltiazem in the blood plasma.
Increases blood levels of quinidine, valproic acid (dose reduction may be required).
Antivirals: Ritonavir may increase plasma concentrations of BMCC.
Anxiolytics and hypnotics: diltiazem inhibits the metabolism of midazolam (increased plasma concentration with increased sedative effect.
BMKC: excretion of nifedipine is reduced by diltiazem (increased plasma concentration).
Diltiazem significantly increases the concentration of lovastatin in plasma. It also enhances the effect of simvastatin, therefore, with their simultaneous use, the dose of simvastatin must be reduced. With the simultaneous use of diltiazem with lovastatin and simvastatin, monitoring of patients is necessary, due to the possibility of developing myositis or rhabdomyolysis.

Special instructions

Diltiazem reduces myocardial conduction, so it is prescribed with extreme caution in patients with first degree AV block and bradycardia. Caution is also necessary when used in patients with impaired left ventricular function.
Diltiazem is prescribed with caution to patients already taking other drugs, in particular beta-blockers. In this group of patients, the treatment process should be carried out under the close supervision of a cardiologist.
Diltiazem should be used with caution in patients with renal or hepatic impairment; in this group of patients, if necessary, the prescribed doses of the drug should be reduced and the content of urea in the urine, creatinine should be monitored. In patients with impaired liver function, the daily dose should not exceed 90 mg and regular monitoring of liver function is recommended.
For elderly patients, the dose is selected individually, because. may increase the half-life of diltiazem.
Since diltiazem reduces peripheral vascular resistance and can cause secondary arterial hypotension, it is necessary to control blood pressure, in particular at the beginning of a course of treatment, while therapeutic doses have not yet been clarified.
In the event of persistent skin rashes developing into erythema multiforme and exfoliative dermatitis, Diltiazem Lannacher should be discontinued.
If during therapy the patient requires surgery under general anesthesia, it is necessary to inform the anesthesiologist about the nature of the therapy being performed (the patient is taking Diltiazem Lannacher).

Influence on the ability to drive vehicles and mechanisms

The use of the drug Diltiazem Lannacher may adversely affect the performance of work that requires a high rate of mental and physical reactions (for example, driving vehicles, operating mechanisms, working at height, etc.). It is not recommended to drink alcohol while taking Diltiazem Lannacher.

Release form

Long-acting film-coated tablets 90 and 180 mg.
10 tablets in PVC/Al blister.
2 blisters (for 90 mg tablets) or 3 blisters (for 180 mg tablets) with instructions for use in a cardboard box.

Storage conditions

Store below 30°C.
Keep out of reach of children.

Shelf life

3 years.
Do not use after the expiration date.

Terms of dispensing from pharmacies

By prescription.

Registration certificate holder:

VALEANT LLC, 115162, Moscow, st. Shabolovka, 31, building 5, Russia

Producer, packer, packer:

“G.L. Pharma GmbH, Industristrasse 1, A-8502 Lannach, Austria

Released quality control:

Lannacher Heilmittel GmbH, Schlossplatz 1, A-8502 Lannach, Austria

Send consumer claims to OOO VALEANT:

115162, Moscow, st. Shabolovka, 31, str. 5, Russia

Graves’ disease: modern approaches to treatment uMEDp

Graves’ disease (diffuse toxic goiter) is one of the most common diseases of the thyroid gland. The article discusses the etiology, pathogenesis and clinical picture of the disease, as well as methods for its diagnosis and treatment.
Currently, laboratory diagnosis of thyrotoxicosis is based on clinical symptoms, increased concentrations of free thyroxine, triiodothyronine, and an undetectable level of thyroid-stimulating hormone. Medical and surgical methods, as well as radioiodine therapy, are used to treat Graves’ disease.

Table 1. Types of thyrotoxicosis and their causes

Table 2. Effects of excess thyroid hormones on the body

Table 3. Classification of thyrotoxicosis

Table 4. Clinical forms of hyperthyroidism

Table 5. Differential diagnosis of thyrotoxicosis

Table 6. Medical treatment of Graves’ disease

Table 7. Mechanism of action of the main groups of drugs used in the treatment of Graves’ disease

Table 8. Advantages and disadvantages of treatments for Graves’ disease

Introduction

Diseases of the thyroid gland (TG) affect all metabolic processes. It is no coincidence that their presence is associated with serious changes in many body systems, deterioration in the prognosis and quality of life of patients [1, 2]. That is why it is extremely important to know the clinical manifestations of thyroid pathologies, the principles of their diagnosis and treatment methods.

We have to admit that there is still terminological confusion regarding thyroid diseases. In the literature, two terms are used to designate them – “thyrotoxicosis” and “hyperthyroidism”. However, these concepts are not identical. In particular, hyperthyroidism is one of the common causes of thyrotoxicosis.

Hyperthyroidism should be understood as a condition caused by both excessive synthesis and excessive secretion of thyroid hormones (thyroxine (T4) and triiodothyronine (T3)). It can be considered as hyperfunction of the thyroid gland, for example, in diffuse toxic goiter (DTG).

Hyperfunction of the thyroid gland is not always observed in thyrotoxicosis. This pathology may be due to inflammatory processes in the thyroid gland, accompanied by destruction of the follicles and the release of ready-made reserves of thyroid hormones. This variant develops in subacute (de Quervain’s thyroiditis), postpartum, painless and cytokine-induced thyroiditis, thyrotoxic phase of chronic autoimmune thyroiditis, as well as in type 2 amiodarone-induced thyrotoxicosis. An overdose of drugs containing thyroid hormones (in particular, suppressive therapy) leads to the development of artificial forms of thyrotoxicosis (Table 1).

Diagnosis of thyrotoxicosis is based on clinical symptoms, increased concentrations of free T4 and T3 (free T4 and free T3) and an undetectable level of thyroid-stimulating hormone (TSH). In the case of a low level of TSH and an increase in at least one of the fractions of thyroid hormones, a diagnosis of “manifest thyrotoxicosis” is established, if both fractions are within the normal range – “subclinical thyrotoxicosis”. The next stage of diagnosis is the search for an etiological factor – the trigger of the disease. Differential diagnosis of thyrotoxicosis involves the determination of antibodies to thyroid-stimulating hormone receptors (AT-rTTH). Of the instrumental methods, ultrasound examination (ultrasound) is considered the simplest and most informative, which allows to determine with high accuracy the volume of the thyroid gland, the echogenicity of its structure, the presence of nodes and features of blood flow, as well as thyroid scintigraphy from ¹³¹ I or ⁹⁹ mTc, reflecting the functional activity of the thyroid tissue [3, 4].

Graves’ disease

Thyrotoxicosis is the main manifestation of Graves’ disease, also known as DTG.

Graves’ disease is a systemic autoimmune disease that develops as a result of the production of AT-rTTG (immunoglobulin (Ig) G) and is clinically manifested by thyroid damage with the development of thyrotoxicosis syndrome in combination with extrathyroid pathology (ophthalmopathy, pretibial myxedema, acropathy, damage to the cardiovascular system, etc. .) [2, 5]. Pathology develops more often in women than in men. Thus, the ratio of women and men with Graves’ disease varies from 5:1 to 10:1 [6].

Etiology and pathogenesis

The development of Graves’ disease is associated with a congenital defect of specific T-lymphocytes. As a result of the breakdown of immunological tolerance, B-lymphocytes are activated, producing thyroid-stimulating immunoglobulins – AT-rTTG. Binding of stimulatory antibodies to the TSH receptor leads to its activation. As a result, the production of hormones by thyrocytes increases and clinical manifestations of thyrotoxicosis develop [7, 8]. Unlike most other autoimmune diseases of the endocrine glands (type 1 diabetes mellitus, hypocorticism), Graves’ disease does not destroy, but stimulates the target organ (hyperthyroidism). T4 remains the main secretory product of the thyroid gland, but the T3/T4 ratio often increases. As the production of thyroid hormones increases, their free fractions increase [9, 10].

Inherited violation of immunological tolerance can contribute to the survival and proliferation of individual lymphocytes responsible for the autoimmune reaction against thyrocytes, as well as their secretion of IgG in response to environmental factors. Among the trigger factors, the role of viral infection, stress, and smoking is discussed. In particular, emotional stress leads to an increase in the secretion of cortisol, while the activity of T-lymphocytes is suppressed. As a result, autoreactive lymphocytes are released from their suppressive influence and can show their activity to the full extent. In particular, we are talking about the synthesis and production of thyroid-stimulating immunoglobulins. Smoking almost doubles the risk of developing the disease [11].

Often, Graves’ disease is associated with another autoimmune pathology, such as pernicious anemia, alopecia, vitiligo, myasthenia gravis, idiopathic thrombocytopenic purpura.

Symptoms of thyrotoxicosis

With thyrotoxicosis, changes occur in almost all types of metabolism, but the most pronounced are violations of fat metabolism. This affects the work of many systems and organs, primarily the cardiovascular, digestive and other endocrine glands in addition to the thyroid gland (Table 2).

Symptoms of the disease develop and progress quite quickly [12].

Patients with thyrotoxicosis are often observed by doctors of other specialties – cardiologists, internists, gastroenterologists and neurologists, they get to endocrinologists only when a detailed clinical picture appears. So, in elderly people, the symptoms of the disease are often regarded as a cardiovascular or oncological pathology.

It has been established that an excess of thyroid hormones disrupts the coupling of oxidation and phosphorylation processes at the level of tissue respiration. As a result, heat production increases. Increased heat transfer is achieved due to increased sweating, which is expressed by certain clinical symptoms on the part of the skin (becomes soft, moist and velvety). Therefore, in most patients with DTG, the temperature remains normal. Subcutaneous fat progressively decreases in all parts of the body, depending on the severity of thyrotoxicosis.

Accelerated metabolism is associated with increased oxygen consumption by various organs and tissues, which is achieved by accelerating blood circulation.

Persistent tachycardia, not dependent on physical activity, is considered one of the main symptoms of thyrotoxicosis. The second cause of tachycardia is the direct effect of thyroxine on the heart muscle [13].

Thyrotoxic tachycardia has the following features:

• shortening of diastole, as a result of which the lack of oxygen in the myocardium is aggravated;
• increase in total energy consumption per unit of time;
• increased risk of developing ectopic impulses, which leads to heart rhythm disturbance and, over time, to cardiovascular failure.

Most often, with DTG, atrial fibrillation develops. This symptom is so pathognomonic that it can become the basis for examining the patient for thyrotoxicosis.

Circulatory failure in thyrotoxicosis has a number of features. It develops according to the right ventricular type, accelerated blood flow and an increased cardiac index are preserved. In thyrotoxicosis, myocardial infarction rarely occurs, which is obviously associated with a lower risk of atherosclerosis and myocardial adaptation to hypoxia. An increase in the size of the heart is noted only with the appearance of atrial fibrillation and is primarily due to dilatation of the ventricles.

Signs of left ventricular hypertrophy on the electrocardiogram are observed in a third of patients, but they are functional in nature (after the elimination of thyrotoxicosis, pathological abnormalities disappear).

A classic manifestation of the disease is a heart rhythm disturbance – atrial fibrillation, and the frequency of arrhythmia increases with age. Atrial fibrillation is accompanied by an increased risk of thromboembolism [14].

Symptoms from the organs of vision are numerous. These include a characteristic staring frightened gaze with widening of the palpebral fissures, increased glare of the eyes, rare blinking, Graefe’s symptom (when fixing the gaze on an object slowly moving downward, a white strip of sclera remains between the upper eyelid and the iris), etc. These manifestations are most likely are caused by an increased tone of the sympathetic nervous system and disappear when thyrotoxicosis is compensated.

The most severe pathology complicating the course of Graves’ disease is endocrine ophthalmopathy (infiltrative orbitopathy). This is an autoimmune organ-specific disease that occurs with damage to the retrobulbar adipose and connective tissues, orbital muscles, optic nerve, and periorbital tissues [15].

Inflammatory exudation and infiltration of retrobulbar tissue, as well as extraocular muscles, lead to an increase in intraocular pressure with impaired blood flow in the tissues of the orbits and a sharp increase in the volume of orbital tissues with the development of exophthalmos [16, 17]. Retrobulbar edema is caused by a significant increase in the production of glycosaminoglycans by fibroblasts in the tissues of the orbits. The characteristic signs of pathology are photophobia, lacrimation, periorbital edema, foreign body sensation in the eyes, retroorbital pain. These symptoms are accompanied by diplopia, swelling of the conjunctiva, decreased visual acuity. Smoking and poorly controlled thyrotoxicosis significantly worsen the course of endocrine ophthalmopathy.

An excess of thyroid hormones also has a toxic effect on liver cells. They activate proteolytic cytoplasms, and also contribute to the formation of SH-radicals, which leads to a violation of cholesterol-synthesizing, glycogen-forming, and detoxifying functions of the liver. First, this is manifested by a low content of cholesterol in the blood, then by a violation of carbohydrate metabolism. As the severity of the disease increases, the level of hepatic transaminases increases. When thyrotoxicosis is eliminated, all disorders are eliminated [12].

The toxic effect of thyroid hormones on the central nervous system is realized due to the effect on cells and increasing their sensitivity to adrenaline and norepinephrine. Clinical signs of thyrotoxic encephalopathy are headache, emotional lability, rapid mental exhaustion, inability to concentrate, sleep disturbance. Against the background of treatment with thyreostatics, all changes disappear. In some cases, this can become a differential diagnostic sign [18].

Muscle weakness is especially evident when climbing a mountain or stairs, getting up from your knees or lifting weights. After the normalization of the thyroid status, muscle strength is restored quite quickly, and muscle mass takes longer.

Due to insomnia and muscle weakness, such patients often develop a feeling of fatigue.

In patients with thyrotoxicosis, there is also a violation of calcium-phosphorus metabolism. The loss of calcium and phosphorus in the urine is significantly increased relative to the norm. However, their concentration in blood serum, as a rule, is within the normal range. Osteoporosis is more common in older women. The results of numerous studies indicate that the excess content of thyroid hormones has a catabolic effect on bone tissue. Radiographic features are reminiscent of menopausal osteoporosis [19].

The reproductive system is also negatively affected by excess thyroid hormones. In men, libido decreases, sometimes gynecomastia develops. Women are characterized by menstrual irregularities, up to amenorrhea, and anovulation may occur.

In elderly patients, goiter is often absent or there is a slight increase in the size of the thyroid gland in combination with nodular goiter. A low or oligosymptomatic course of the disease is characteristic [18]. In an atypical course, there may be a pronounced loss of body weight with anorexia against the background of general and progressive muscle weakness, which raises the suspicion of an oncological disease. In elderly patients, cardiovascular disorders often predominate. Therefore, as noted earlier, all patients with newly diagnosed unexplained heart failure or atrial fibrillation should be examined for thyrotoxicosis. It should also be remembered that in old age the metabolic manifestations of thyrotoxicosis can be erased, while the clinical picture is often dominated by apathy, lethargy, depression, weakness (apathetic thyrotoxicosis), in other cases – signs of proximal myopathy.

Diagnostics and classification

The diagnosis of Graves’ disease, or DTG, is made on the basis of the above clinical symptoms, high levels of thyroid hormones (f. T4, f. T3) and low levels of TSH in the blood. An elevated titer of AT-rTTH, a marker of immunogenic thyrotoxicosis, is evidence that the cause of thyrotoxicosis is Graves’ disease. Preservation of this during treatment indicates a high risk of decompensation of the disease [3].

The name of the pathology “diffuse toxic goiter” implies the presence of a goiter. However, in some cases, the volume of the thyroid gland is not increased. Therefore, when establishing a diagnosis, it is recommended to indicate the volume of the thyroid gland in milliliters, especially since ultrasonic volumemetry is widely available in clinical practice.

Thyrotoxicosis is traditionally classified according to severity (Table 3). However, the evaluation criteria are based on highly variable parameters (heart rate, weight loss, etc.). In this regard, it seems more appropriate to distinguish subclinical, overt and complicated hyperthyroidism (Table 4).

Against the background of the treatment of overt or complicated hyperthyroidism, decompensation, compensation or relapse are possible. These conditions reflect the effectiveness of ongoing therapeutic measures, and therefore should be recorded in the clinical diagnosis.

When conducting differential diagnosis to determine the cause of thyrotoxicosis, ultrasound is of great importance, and in some cases thyroid scintigraphy (Table 5). In Graves’ disease, there is a decrease in the echogenicity of diffuse thyroid tissue, an increase in its volume and an increase in blood flow. A diffuse increase in radiopharmaceutical (RP) uptake during scintigraphy makes it possible to distinguish Graves’ disease from other causes of thyrotoxicosis. With functional autonomy of the thyroid gland (toxic adenoma, multinodular toxic goiter), a hot node (or nodes) and reduced capture of radiopharmaceuticals by the rest of the thyroid tissue are detected. Thyrotoxicosis, not associated with hyperfunction of the thyroid gland (with destructive thyroiditis), is characterized by reduced absorption of radiopharmaceuticals [4].

Ultrasound of the orbits, computed tomography and magnetic resonance imaging can be used to visualize pathological changes in retrobulbar tissues.

Methods of treatment

There are several methods of treating Graves’ disease: the use of antithyroid drugs (thionamides), radioiodine therapy, and surgery. Each of them has a number of advantages and disadvantages. The most promising method of treatment is radioiodine therapy.

Medical therapy

Regardless of the chosen method of exposure, thyrostatic therapy is first performed to achieve euthyroidism. With the help of thyreostatics, it is possible to achieve remission of Graves’ disease in 35–50% of patients. Long-term conservative treatment does not make sense for large goiters (thyroid volume > 35-40 ml), severe complications of thyrotoxicosis, recurrence of thyrotoxicosis after 12-18 months of full-fledged thyrostatic therapy [20, 21].

Thionamides (thiamazole, propylthiouracil) block the synthesis of thyroid hormones and stop the manifestations of thyrotoxicosis. It is assumed that thyreostatics are capable of exerting an immunosuppressive effect (Table 6).

At the initial stages of treatment, thyreostatics are prescribed in maximum doses: 30–40 mg / day of thiamazole (1-methyl-2-mercaptoimidazole) for two to three doses or 300 mg / day of propylthiouracil (6-propyl-2-thiouracil) for three to four taking after meals. The duration of action of thiamazole reaches 40 hours, while its activity is approximately ten times higher than that of propylthiouracil. Against the background of such therapy, after four to six weeks, 90% of patients with moderate thyrotoxicosis manage to achieve disease compensation. The laboratory sign of this is the normalization of the level of St. T4 (TSH levels may remain low for a long time) [22]. From this moment, the thyreostatic dose is gradually reduced to maintenance (thiamazole 2.5–10.0 mg/day, propylthiouracil 12.5–50.0 mg/day). Conservative treatment usually lasts from 12 to 24 months. The longer thyrostatic therapy is, the higher the probability of achieving a stable remission. In the presence of a goiter effect and / or prerequisites for the development of drug-induced hypothyroidism, a combination of thyreostatics with L-thyroxine (25–50 μg / day) is recommended to maintain a euthyroid state [23].

The main disadvantage of thionamide therapy is the development of side effects. Minor side effects, such as skin manifestations (urticaria, rash, itching), arthralgia, are observed in about 5% of patients and, as a rule, only during the first few weeks of therapy [24]. If minor skin reactions occur, antihistamines may be prescribed. In the presence of persistent moderate and mild side effects, the thyreostatic should be canceled and radioiodine therapy or surgery should be prescribed. If the last two methods of treatment are not indicated, a switch to another antithyroid agent is possible [25].

When prescribing thyreostatics, patients must be informed about the possibility of agranulocytosis (0.5–0.7% of cases). Agranulocytosis is characterized by symptoms of an infectious disease. When they appear, therapy is stopped.

In addition to antithyroid drugs, beta-blockers, glucocorticosteroids, sedatives and cardiac glycosides, and potassium preparations are used (Table 7).

Beta-blockers can reduce the period of preoperative preparation due to the relief of symptoms from the cardiovascular system, which is achieved by direct action on adrenaline beta receptors, as well as by affecting the peripheral metabolism of thyroid hormones. It should be emphasized that in order to assess the adequacy of the dose of thyreostatics, it is impossible to focus on the pulse rate.

For patients with obvious thyrotoxicosis, beta-blockers (Inaprilin 120 mg / day for three to four doses or long-acting drugs, such as Concor 5 mg / day, Atenolol 100 mg / day once) should be prescribed until medical euthyroidism is achieved, and often for a longer term. In severe, prolonged thyrotoxicosis and the presence of symptoms of adrenal insufficiency, glucocorticosteroids are indicated: prednisolone 10–15 mg/day orally or hydrocortisone 50–75 mg/day intramuscularly [26]. This group of drugs should be discontinued gradually. Beta-blockers should be used with caution in patients with asthma, congestive heart failure, bradyarrhythmia, and Raynaud’s phenomenon. As an alternative, they are shown calcium channel blockers [27].

Surgery

Surgical intervention was the first and main method of radical treatment of Graves’ disease [28]. With the advent of the 1940s and 1950s. less than 1% of experts recommend thyrostatic therapy and radioiodine therapy. However, according to recent foreign studies, surgery has again become the method of choice when indicated (against radioiodine therapy), especially in patients with low socioeconomic status [29, thirty]. In some cases, surgery is recommended immediately after the diagnosis is established, in others – after conservative treatment, sometimes quite long.

Absolute indications for surgical treatment for diffuse toxic goiter are [31, 32]:

• large goiter with signs of compression of surrounding organs and anatomical structures, regardless of the severity of thyrotoxicosis;
• combination of DTG with neoplastic processes in the thyroid gland;
• severe form of thyrotoxicosis with cardiac arrhythmias of the type of atrial fibrillation;
• intolerance to thyreostatics;
• lack of a lasting effect of conservative therapy for two years, relapse of the disease.

However, situations often arise that can be regarded as relative indications for surgical treatment:

• lack of qualified endocrinological care at the patient’s place of residence;
• social or living conditions that preclude the possibility of taking drugs regularly.

Surgical treatment of DTG requires preoperative preparation of patients. Its main goal is to achieve a euthyroid state.

Depending on the severity of thyrotoxicosis, the volume of the thyroid gland, the presence of concomitant diseases, drug compensation for thyrotoxicosis is achieved at different times using different doses of thyreostatics. It is important to remember that poor compensation for thyrotoxicosis poses a threat of massive entry of thyroid hormones into the bloodstream during surgery and the development of a thyrotoxic crisis in the early postoperative period, a condition in which mortality reaches 60% [33].

Radioiodine therapy

In some cases (intolerance to thyreostatics, relapse of DTG, contraindications to surgical treatment associated with severe somatic diseases), radioactive iodine therapy ( ¹³¹ I) can be considered as the most optimal method of treatment (Table 8). However, it has certain limitations. It cannot be used with a large volume of the thyroid gland and retrosternal location of the goiter. Treatment ¹³¹ I is contraindicated in pregnancy and breastfeeding. Hypothyroidism usually develops within 6-12 months after administration. In addition, in some situations, preparation for radioiodine therapy requires drug compensation for thyrotoxicosis with the help of thyreostatics. The latter are canceled five to seven days before the introduction of ¹³¹ I [34-39].

Before radioactive iodine therapy, treatment with thiamazole is justified if there is a risk of exacerbation of thyrotoxicosis (that is, in those patients who have severe symptoms or the level of free T4 is two to three times higher than normal, in patients with cardiovascular disorders, endocrine ophthalmopathy). Patients at risk before radioiodine therapy should also receive beta-blockers. However, with agranulocytosis, an allergic reaction to thyreostatics, radioactive iodine therapy can be prescribed without prior preparation.

Currently, most of the patients with Graves’ disease, as well as with other forms of toxic goiter, receive radioiodine therapy as a treatment. This is due to the fact that the method is effective, non-invasive, relatively cheap, devoid of the complications that can develop during surgery on the thyroid gland.

The goal of radioiodine therapy is to eliminate thyrotoxicosis by destroying hyperfunctioning thyroid tissue. With DTZ, proper activity ¹³¹ I should be administered once (10–15 mCi) in order to achieve hypothyroidism in patients. Follow-up includes determining the level of St. T4 and St. T3 with an interval of four to six weeks. If thyrotoxicosis persists six months after radioiodine therapy, re-treatment is indicated.

Conclusion

Thyrotoxicosis syndrome covers a wide range of pathologies, the main of which is Graves’ disease. Currently, the main ways to correct thyrotoxicosis are drug therapy, surgery and radioactive iodine therapy.