ANUCORT (HYDROCORTISONE) | Crohn’s & Colitis Foundation

Dear @[email protected],

Your doctor has discussed the following medication with you: Anucort. Here is some additional information. Let us know if you have any questions regarding this information.

• This medication belongs to a class of drugs called corticosteroids.

• Corticosteroids (commonly referred to as steroids) are powerful and fast-acting medications that help reduce irritation and swelling (inflammation) in the intestines and throughout the body, including joints, skin, and eyes.

• This medication is given as a suppository to reduce inflammation in the rectum, or the last part of large intestine.

• You should notice an improvement of symptoms within days of starting this medication.

• While steroids can be used for weeks or months, they should only be used for short periods of time because of their side effects. Steroids can be used to get you well in the short term, but should never be used over a long period of time

• Because this medication is a suppository, the likelihood that it will be absorbed into the bloodstream is very low, but possible. Side effects can include minor infections like yeast infections (in the mouth or female reproductive organs) or urinary tract infections, serious infections, high blood pressure, high blood sugar levels, weight gain, stretch marks, acne, rounding of the face (“moon face”), facial hair, difficulty sleeping, mood swings, and psychiatric symptoms. These side effects will usually go away when the medication is stopped. Long-term use of steroids can result in a weakening of the bones (osteoporosis) and cataracts.

• Long-term use can result in damage and irritation of the skin of the anus.

• Before taking this medication, let your doctor know about other medical conditions that you may have or other medications (even over-the-counter medications or alternative therapies) you may be taking.

• The best way to control your disease is by taking your medication as directed. Even when you do not have any symptoms, it is very important to continue taking your medication to prevent your disease from becoming active again. Do not alter the amount of the medication or how frequently you take it without speaking to your doctor first.

• If you have any side effects or you continue to have symptoms, speak to your doctor immediately.

• If you have an allergy to this medication or other corticosteroids, do not take this medication without speaking to your doctor first.

For further information, please check out http://www.ibdmedicationguide.org/ or follow this link:

Hydrocortisone Rectal: MedlinePlus Drug Information

Hydrocortisone rectal comes as a cream, an enema, suppositories, and a foam to use in the rectum. Follow the directions on your prescription or your product label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Use rectal hydrocortisone exactly as directed. Do not use it more or less of it or use it more often than prescribed by your doctor.

For proctitis, hydrocortisone rectal foam usually is used one or two times a day for 2 to 3 weeks, then if necessary, every other day until your condition improves. Hydrocortisone rectal suppositories usually are used two or three times daily for 2 weeks; may require treatment for up to 6 to 8 weeks in severe cases. Proctitis symptoms may improve within 5 to 7 days.

For hemorrhoids, hydrocortisone rectal cream usually is used in adults and children 12 years and older up to 3 or 4 times daily. If you obtained hydrocortisone without a prescription (over the counter) and your condition does not improve within 7 days, stop using it and call your doctor. Do not put the cream into your rectum with your fingers.

For ulcerative colitis, hydrocortisone rectal enema usually is used every night for 21 days. Although colitis symptoms may improve within 3 to 5 days, 2 to 3 months of regular enema use may be required. Call your doctor if your colitis symptoms do not improve within 2 or 3 weeks.

Your doctor may change your dose of rectal hydrocortisone during your treatment to be sure that you are always using the lowest dose that works for you. Your doctor may also need to change your dose if you experience unusual stress on your body such as surgery, illness, or infection. Tell your doctor if your symptoms improve or get worse or if you get sick or have any changes in your health during your treatment.

Hydrocortisone rectal suppositories may stain clothing and other fabrics. Take precautions to prevent staining when you use this medication.

Before using hydrocortisone rectal foam the first time, carefully read the written instructions that come with it. Ask your doctor or pharmacist to explain any part you do not understand.

If using a hydrocortisone rectal enema, follow these steps:

1. Try to have a bowel movement. The medication will work best if your bowels are empty.
2. Shake the enema bottle well to make sure the medication is mixed.
3. Remove the protective cover from the applicator tip. Be careful to hold the bottle by the neck so that the medication will not leak out of the bottle.
4. Lie down on your left side with your lower (left) leg straight and your right leg bent toward your chest for balance. You can also kneel on a bed, resting your upper chest and one arm on the bed.
5. Gently insert the applicator tip into your rectum, pointing it slightly toward your navel (belly button).
6. Hold the bottle firmly and tilt it slightly so that the nozzle is aimed toward your back. Squeeze the bottle slowly and steadily to release the medicine.
7. Withdraw the applicator. Remain in the same position for at least 30 minutes. Try to keep the medicine inside of your body all night (while you sleep).
8. Wash your hands thoroughly. Throw away the bottle in a trash can that is out of the reach of children and pets. Each bottle contains only one dose and should not be reused.

Krames Online – Anucort-HC Rectal Suppository 25 mg

Uses

This medicine is used for the following purposes:

• anal itching or pain
• hemorrhoids
• inflammation

Instructions

This medicine is for use in the rectum or around the anus. DO NOT take this medicine by mouth.

Follow the instructions on the package to use this medicine correctly.

Wash your hands before and after using this medicine. However, do not get up right away to wash your hands if you are supposed to lie down for a period of time to give the medicine time to work.

Lie on your left side, with your right knee bent toward your chest. Or, you may kneel on both knees, with your arms folded on the floor with your head resting on your arms.

Unwrap the suppository and moisten it with a few drops of cool water. Insert the pointed end into the anus, and push it all the way in with your finger.

If the suppository becomes soft, you can make it firmer by refrigerating it. You can run it under cold water if the suppository is wrapped.

If your dose is one-half (1/2) suppository, carefully cut it lengthwise using a clean, sharp knife.

If you have hemorrhoids, you may coat the tip of the suppository with a water-soluble lubricant (for example K-Y Jelly) before inserting. Do NOT use vaseline.

Keep this medicine at room temperature.

If you forget to take a dose on time, take it as soon as you remember. If it is almost time for the next dose, do not take the missed dose. Return to your normal dosing schedule. Do not take 2 doses of this medicine at one time.

Please tell your doctor and pharmacist about all the medicines you take. Include both prescription and over-the-counter medicines. Also tell them about any vitamins, herbal medicines, or anything else you take for your health.

If your symptoms do not improve or they worsen while on this medicine, contact your doctor.

You may stop using this medicine if you no longer have symptoms.

Do not freeze the medicine.

Cautions

Do not use the medication any more than instructed.

Please check with your doctor before drinking alcohol while on this medicine.

Tell the doctor or pharmacist if you are pregnant, planning to be pregnant, or breastfeeding.

Ask your pharmacist if this medicine can interact with any of your other medicines. Be sure to tell them about all the medicines you take.

Please tell all your doctors and dentists that you are on this medicine before they provide care.

Do not start or stop any other medicines without first speaking to your doctor or pharmacist.

Side Effects

The following is a list of some common side effects from this medicine. Please speak with your doctor about what you should do if you experience these or other side effects.

• skin irritation such as redness, itching, rash, or burning
• rectal burning or irritation

Call your doctor or get medical help right away if you notice any of these more serious side effects:

• bleeding from rectum
• swelling of the legs, feet, and hands
• stomach pain
• dark, tarry stool
• thirst
• unusual or unexplained tiredness or weakness
• blurring or changes of vision

A few people may have an allergic reaction to this medicine. Symptoms can include difficulty breathing, skin rash, itching, swelling, or severe dizziness. If you notice any of these symptoms, seek medical help quickly.

Extra

Please speak with your doctor, nurse, or pharmacist if you have any questions about this medicine.

https://krames.meducation.com/V2.0/fdbpem/3021

IMPORTANT NOTE: This document tells you briefly how to take your medicine, but it does not tell you all
there is to know about it.Your doctor or pharmacist may give you other documents about your medicine.
Please talk to them if you have any questions.Always follow their advice. There is a more complete
description of this medicine available in English.Scan this code on your smartphone or tablet or use
the web address below. You can also ask your pharmacist for a printout. If you have
any questions, please ask your pharmacist.

DrugCentral 2021 Online drug Compendium

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PACKAGE LABEL.PRINCIPAL DISPLAY PANEL.

PRINCIPAL DISPLAY PANEL NDC 0713-0503-24 G&W ANUCORT-HCTM Hydrocortisone Acetate Suppositories 25 mg Rx only For Rectal Administration 24 Adult Suppositories Each suppository contains: Hydrocortisone Acetate 25 mg in a specially blended hydrogenated vegetable oil base. FOR RECTAL ADMINISTRATION. DOSAGE AND ADMINISTRATION: Read package insert for complete information before use. DIRECTIONS FOR USE: Detach one suppository from strip of suppositories. Hold suppository upright. Separate tabs at top opening and pull downward from the pointed end. Continue pulling downward to almost the full length of the suppository. Carefully remove the suppository from the pocket. Avoid excessive handling of the suppository, which is designed to melt at body temperature. Insert suppository into rectum with gentle pressure, pointed end first. Store at 20-25C (68-77F) [See USP Controlled Room Temperature]. Store away from heat. Protect From Freezing. NOTE: Staining of fabric may occur with the use of the suppository. Precautionary measures are recommended. WARNING: Keep this and all drugs out of the reach of children. In case of accidental ingestion, seek professional assistance or contact a Poison Control Center immediately. G&W Laboratories, Inc. South Plainfield, NJ 07080 Visit our website @ www.gwlabs.com

PREGNANCY SECTION.

PREGNANCY CATEGORY C In laboratory animals, topical steroids have been associated with an increase in the incidence of fetal abnormalities when gestating females have been exposed to rather low dosage levels. There are no adequate and well controlled studies in pregnant women. Hydrocortisone acetate suppositories should only be used during pregnancy if the potential benefit justifies the risk to the fetus. Drugs of this class should not be used extensively on pregnant patients, in large amounts, or for prolonged periods of time. It is not known whether this drug is excreted in human milk and because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from hydrocortisone acetate suppositories, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

ADVERSE REACTIONS SECTION.

ADVERSE REACTIONS The following local adverse reactions have been reported with hydrocortisone acetate suppositories: burning, itching, irritation, dryness, folliculitis, hypopigmentation, allergic contact dermatitis, secondary infection. To report SUSPECTED ADVERSE REACTIONS, contact G&W Laboratories, Inc. at 1-800-922-1038 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

INDICATIONS & USAGE SECTION.

INDICATIONSAND USAGE Hydrocortisone acetate suppositories are indicated for use in inflamed hemorrhoids, post-irradiation (factitial) proctitis; as an adjunct in the treatment of chronic ulcerative colitis; cryptitis; and other inflammatory conditions of anorectum and pruritus ani.

DRUG ABUSE AND DEPENDENCE SECTION.

DRUG ABUSE AND DEPENDENCE Drug abuse and dependence have not been reported in patients treated with hydrocortisone acetate suppositories.

DOSAGE & ADMINISTRATION SECTION.

DOSAGE AND ADMINISTRATION For rectal administration. Detach one suppository from strip of suppositories. Hold suppository upright. Separate tabs at top opening and pull downward from the pointed end. Continue pulling downward to almost the full length of the suppository. Carefully remove the suppository from the pocket. Avoid excessive handling of the suppository which is designed to melt at body temperature. Insert suppository into the rectum with gentle pressure, pointed end first. Insert one suppository in the rectum twice daily, morning and night for two weeks, in nonspecific proctitis. In more severe cases, one suppository three times a day or two suppositories twice daily. In factitial proctitis, the recommended duration of therapy is six to eight weeks or less, according to the response of the individual case.

HOW SUPPLIED SECTION.

HOW SUPPLIED Boxes of 12 suppositories NDC 0713-0503-12 Boxes of 24 suppositories NDC 0713-0503-24 Boxes of 100 suppositories NDC 0713-0503-01

DESCRIPTION SECTION.

DESCRIPTION Hydrocortisone Acetate is a corticosteroid designated chemically as pregn-4-ene 3, 20-dione,21-(acetyloxy)-11, 17-dihydroxy-(11) with the following structural formula: Each rectal suppository contains hydrocortisone acetate, USP 25 mg in a specially blended hydrogenated vegetable oil base.

OVERDOSAGE SECTION.

OVERDOSAGE If signs and symptoms of systemic overdosage occur, discontinue use.

PRECAUTIONS SECTION.

PRECAUTIONS Do not use hydrocortisone acetate suppositories unless adequate proctologic examination is made. If irritation develops, the product should be discontinued and appropriate therapy instituted. In the presence of an infection, the use of an appropriate antifungal or antibacterial agent should be instituted. If a favorable response does not occur promptly, hydrocortisone acetate should be discontinued until the infection has been adequately controlled. Carcinogenesis: No long term studies in animals have been performed to evaluate the carcinogenic potential of corticosteroid suppositories.

STORAGE AND HANDLING SECTION.

STORAGE AND HANDLING Store at 20-25C (68-77F) [See USP Controlled Room Temperature]. Store away from heat. Protect From Freezing. Manufactured by: G&W Laboratories, Inc. South Plainfield, NJ 07080 8-0503GW7 Rev. 11/13

INFORMATION FOR PATIENTS SECTION.

INFORMATION FOR PATIENTS Staining of fabric may occur with use of the suppository. Precautionary measures are recommended.

CLINICAL PHARMACOLOGY SECTION.

CLINICAL PHARMACOLOGY In normal subjects, about 26% of hydrocortisone acetate is absorbed when the suppository is applied to the rectum. Absorption of hydrocortisone acetate may vary across abraded or inflamed surfaces. Topical steroids are primarily effective because of their anti-inflammatory, anti-pruritic and vasoconstrictive action.

CONTRAINDICATIONS SECTION.

CONTRAINDICATIONS Hydrocortisone acetate suppositories are contraindicated in those patients having a history of hypersensitivity to hydrocortisone acetate or any of the components.

Which medications in the drug class Corticosteroids are used in the treatment of Pediatric Crohn Disease?

Hydrocortisone (Topical) | Memorial Sloan Kettering Cancer Center

This information from Lexicomp^® explains what you need to know about this medication, including what it’s used for, how to take it, its side effects, and when to call your healthcare provider.

Brand Names: US

Advanced Allergy Collection; Ala Scalp; Ala-Cort; Anti-Itch Maximum Strength [OTC]; Anucort-HC; Anusol-HC; Aquanil HC [OTC]; Beta HC [OTC]; Colocort [DSC]; Cortaid Maximum Strength [OTC] [DSC]; Cortenema; Corticool [OTC] [DSC]; Cortifoam; Curad Hydrocortisone [OTC] [DSC]; Dermasorb HC [DSC]; Hemmorex-HC; Hydrocortisone Anti-Itch [OTC]; Hydrocortisone in Absorbase [DSC]; Hydrocortisone Max St [OTC]; Hydrocortisone Max St/12 Moist [OTC]; Hydrocortisone/Aloe Max Str [OTC]; HydroSKIN [OTC] [DSC]; Instacort 5 [OTC]; Locoid; Locoid Lipocream; Med-Derm Hydrocortisone [OTC] [DSC]; Medi-First Hydrocortisone [OTC] [DSC]; MiCort-HC; NuCort; Pandel; Preparation H [OTC]; Procto-Med HC; Procto-Pak; Proctocort; Proctosol HC [DSC]; Proctozone-HC; Recort Plus [OTC]; Rederm [OTC] [DSC]; Sarnol-HC [OTC]; Scalacort DK; Scalpicin Maximum Strength [OTC]; Texacort; Vanicream HC Maximum Strength [OTC]; Westcort [DSC]

Brand Names: Canada

Barriere-HC; Cortenema; Cortifoam [DSC]; Cortoderm; Emo Cort [DSC]; Hyderm; Hydroval; NOVO-Hydrocort; Prevex HC [DSC]; SANDOZ Hydrocortisone; Sarna HC

What is this drug used for?

• It is used to treat skin irritation.
• It is used to treat skin rashes.
• It is used to treat signs of hemorrhoids or rectal irritation.
• It is used to treat ulcerative colitis.

What do I need to tell my doctor BEFORE I take this drug?

All products:

• If you are allergic to this drug; any part of this drug; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.

All rectal products:

• If you have any of these health problems: Bowel block; fistula; a fungal infection; holes, sores, or wounds on the rectal area; peritonitis; or recent bowel surgery.

This is not a list of all drugs or health problems that interact with this drug.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this drug with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take this drug?

All products:

• Tell all of your health care providers that you take this drug. This includes your doctors, nurses, pharmacists, and dentists.
• Do not put on cuts, scrapes, or damaged skin.
• This drug may cause harm if swallowed. If this drug is swallowed, call a doctor or poison control center right away.
• Do not use this drug for longer than you were told by your doctor.
• If the patient is a child, use this drug with care. The risk of some side effects may be higher in children.
• This drug may affect growth in children and teens in some cases. They may need regular growth checks. Talk with the doctor.
• Tell your doctor if you are pregnant, plan on getting pregnant, or are breast-feeding. You will need to talk about the benefits and risks to you and the baby.

All skin products:

• Talk with your doctor before you use other drugs or products on your skin.
• Use care when using on a large part of the skin. Talk with the doctor.
• Some products may not be for use in the diaper area. Talk with the doctor.
• If you are breast-feeding and use this drug on your breast or nipple, wash the area before breast-feeding your child.

All rectal products:

• Talk with the doctor before you use other drugs or products in the rectal area.

Suppository:

• This drug may stain clothing or fabric. Protect clothing and fabrics from staining.

What are some side effects that I need to call my doctor about right away?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

All products:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Signs of high blood sugar like confusion, feeling sleepy, more thirst, more hungry, passing urine more often, flushing, fast breathing, or breath that smells like fruit.
• Signs of a weak adrenal gland like a very bad upset stomach or throwing up, very bad dizziness or passing out, muscle weakness, feeling very tired, mood changes, not hungry, or weight loss.
• Signs of Cushing’s disease like weight gain in the upper back or belly, moon face, very bad headache, or slow healing.
• Change in eyesight.
• Very bad headache.
• Irritation where this drug is used.

All skin products:

• Signs of skin infection like oozing, heat, swelling, redness, or pain.
• Skin changes (pimples, stretch marks, slow healing, hair growth).
• Thinning of the skin.

All rectal products:

• Very bad bleeding from rectum or rectal pain.

What are some other side effects of this drug?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Burning or stinging.
• Dryness.
• Tingling.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to your national health agency.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

How is this drug best taken?

Use this drug as ordered by your doctor. Read all information given to you. Follow all instructions closely.

All skin products:

• Do not take this drug by mouth. Use on your skin only. Keep out of your mouth, nose, and eyes (may burn).
• Use as you have been told, even if your signs get better.
• Wash your hands before and after use. If your hand is the treated area, do not wash your hand after use.
• Clean affected part before use. Make sure to dry well.
• Put a thin layer on the affected skin and rub in gently.
• Do not use coverings (bandages, dressings) unless told to do so by the doctor.
• Do not put on the face, underarms, or the groin area unless told to do so by the doctor.
• Do not use tight-fitting diapers or plastic pants if treated part is in the diaper area. This may cause more drug to get into the body.

Lotion:

All rectal products:

• This drug is for rectal use only. Do not take this drug by mouth.
• Use as you have been told, even if your signs get better.
• Wash your hands before and after use.

Rectal enema:

Rectal foam:

• Shake well before use.
• Use an applicator to put in foam. Do not put the foam container right into the rectum.
• This drug may catch on fire. Do not use near an open flame or while smoking.

Suppository:

• Take foil off the rectal suppository and put in, pointed end first. Do not handle too much.
• If suppository is soft, chill in a refrigerator or run cold water over it.

What do I do if I miss a dose?

• Use a missed dose as soon as you think about it.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not use 2 doses at the same time or extra doses.

How do I store and/or throw out this drug?

All products:

• Store at room temperature. Do not freeze.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.

Rectal foam:

• Protect from heat or open flame. Do not puncture or burn even if it seems empty.

Suppository:

General drug facts

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else’s drugs.
• Some drugs may have another patient information leaflet. If you have any questions about this drug, please talk with your doctor, nurse, pharmacist, or other health care provider.
• Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about this drug, please talk with your doctor, nurse, pharmacist, or other health care provider.
• If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

Consumer Information Use and Disclaimer

This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine. The use of this information is governed by the Lexicomp End User License Agreement, available at https://www.wolterskluwer.com/en/solutions/lexicomp/about/eula.

Last Reviewed Date

2020-10-30

Copyright

© 2021 UpToDate, Inc. and its affiliates and/or licensors. All rights reserved.

Internal Hemorrhoids Trial in Huntsville, Sanford, Wyoming (Anucort-HC, 25 Mg Rectal Suppository, Placebo suppository)

Memorial Sloan Kettering Cancer Center

This document, provided by Lexicomp ^® , contains all the information you need to know about the drug, including the indications, route of administration, side effects and when you should contact your healthcare provider.

Trade names: USA

Crestor; Ezallor Sprinkle

Trade names: Canada

ACH-Rosuvastatin; ACT Rosuvastatin [DSC]; AG-Rosuvastatin; APO-Rosuvastatin; Auro-Rosuvastatin; BIO-Rosuvastatin; Crestor; DOM-Rosuvastatin; JAMP Rosuvastatin Calcium; JAMP-Rosuvastatin; M-Rosuvastatin; Mar-Rosuvastatin; MED-Rosuvastatin; MINT-Rosuvastatin [DSC]; MYLAN-Rosuvastatin [DSC]; NRA-Rosuvastatin; PMS-Rosuvastatin; Priva-Rosuvastatin; RIVA-Rosuvastatin; SANDOZ Rosuvastatin; TARO-Rosuvastatin; TEVA-Rosuvastatin

What is this drug used for?

• Used to lower bad cholesterol and raise good cholesterol (HDL).
• Used to lower triglyceride levels.
• Used to slow the progression of heart disease.
• Used in some people to reduce the risk of myocardial infarction, stroke, and certain heart problems.
• This medicinal product can be used for other indications. Consult your doctor.

What should I tell my doctor BEFORE taking this drug?

• If you are allergic to this drug, any of its ingredients, other drugs, foods or substances.Tell your doctor about your allergy and how it manifested itself.
• If you have liver disease or increased liver function.
• If you are taking any of the following drugs: gemfibrozil, ledipasvir in combination with sofosbuvir, or sofosbuvir in combination with velpatasvir and voxilaprevir.
• If you are or may become pregnant. Do not take this drug if you are pregnant.
• If you are breastfeeding. Do not breast-feed while taking this drug.

This list of drugs and diseases that may be adversely associated with this drug is not exhaustive.

Tell your doctor and pharmacist about all medicines you take (both prescription and over-the-counter, natural products and vitamins) and your health problems. You need to make sure that this drug is safe for your medical conditions and in combination with other drugs you are already taking.Do not start or stop taking any drug or change the dosage without your doctor’s approval.

What do I need to know or do while taking this drug?

• Tell all healthcare providers that you are taking this drug. These are doctors, nurses, pharmacists and dentists.
• High blood sugar has happened with this drug. This includes the development or worsening of pre-existing diabetes mellitus.
• Check your blood sugar as directed by your doctor.
• Perform blood tests as directed by your doctor. Please consult your doctor.
• Do not take the drug in higher doses than the doctor prescribed. Taking more than the prescribed amount of the drug increases the risk of serious side effects.
• Follow your doctor’s recommended diet and exercise program.
• Avoid or limit alcohol consumption to less than 3 servings per day.Drinking too much alcohol can increase your risk of liver disease.
• Take antacids that contain aluminum or magnesium at least 2 hours after taking this drug.
• If you are a native of Asia, take this medicine with caution. You may have more side effects.
• If you are 65 years of age or older, use this drug with caution. You may have more side effects.
• Potential adverse effects of this drug on the fetus.If you can become pregnant, you must use contraception during treatment. If you become pregnant, contact your doctor immediately.

What side effects should I report to my doctor immediately?

WARNING. In rare cases, some people with this drug can have serious and sometimes deadly side effects. Call your healthcare professional or get medical attention right away if you have any of the following signs or symptoms, which may be associated with serious side effects:

• Signs of an allergic reaction such as rash, hives, itching, reddened and swollen skin with blistering or scaling, possibly associated with fever, wheezing or wheezing, tightness in the chest or throat, difficulty breathing, swallowing or speaking, unusual hoarseness, swelling in the mouth, face, lips, tongue, or throat.
• Signs of high blood sugar, such as confusion, drowsiness, increased thirst and hunger, increased urination, facial flushing, rapid breathing, and fruity breath.
• Violation or loss of memory.
• Confusion of consciousness.
• Blood in the urine.
• Difficulty urinating or change in the amount of urine excreted.
• This drug may cause muscle pain, soreness, or weakness.The risk may be increased with thyroid dysfunction or kidney problems. It may also be raised when this drug is taken with certain other drugs, or for people 65 years of age or older. Occasionally, severe muscle abnormalities can occur, which can lead to impaired renal function. Fatalities occurred on rare occasions. If you experience muscle pain, tenderness, or weakness (with or without fever, or feeling unwell), seek medical attention immediately.Call your doctor right away if muscle problems persist after you stop taking this drug as directed by your doctor.
• Liver dysfunctions have been reported while taking drugs of this kind. Sometimes these cases were fatal. Call your doctor right away if you have signs of liver dysfunction, such as dark urine, tired feeling, lack of appetite, nausea or abdominal pain, light colored stools, vomiting, yellow skin or eyes.

What are some other side effects of this drug?

Any medicine can have side effects. However, many people have little or no side effects. Call your doctor or get medical help if these or any other side effects bother you or do not go away:

• Headache.
• Pain in the intestines.
• Nausea.
• Joint pain.
• Weakness.

This list of potential side effects is not exhaustive. If you have any questions about side effects, please contact your doctor. Talk to your doctor about side effects.

You can report side effects to the National Health Office.

You can report side effects to the FDA at 1-800-332-1088. You can also report side effects at https: // www.fda.gov/medwatch.

What is the best way to take this drug?

Use this drug as directed by your healthcare practitioner. Read all the information provided to you. Follow all instructions strictly.

All forms of issue:

• Take this drug at about the same time of the day.
• Continue taking this drug as directed by your doctor or other healthcare professional, even if you feel well.
• Take this medication with or without food.

Tablets:

• Should be swallowed whole with some water or other beverage.

Detachable capsule:

• Swallow whole. Do not chew or crumble.
• If you cannot swallow this drug whole, add the contents of the capsule to a small amount of soft food, such as applesauce or pudding.In this case, swallow the mixture within 60 minutes. Do not store the drug for future use.
• Patients with feeding tubes may use this medication. Apply as directed. Flush the feeding tube after using this drug.

What should I do if a dose of a drug is missed?

• Take the missed dose as soon as you can.
• If it is time for your next dose, do not take the missed dose and then return to your normal dose schedule.
• Do not take 2 doses within 12 hours of a previous dose.

How do I store and / or discard this drug?

• Store at room temperature in a dry place. Do not store in the bathroom.
• Store all medicines in a safe place. Keep all medicines out of the reach of children and pets.
• Dispose of unused or expired drugs.Do not empty into toilet or drain unless directed to do so. If you have any questions about the disposal of your medicinal products, consult your pharmacist. Your area may have drug recycling programs.

General information on medicinal products

• If your health does not improve or even worsens, see your doctor.
• You should not give your medicine to anyone and take other people’s medicines.
• Some medicines may have different patient information sheets. If you have questions about this drug, talk with your doctor, nurse, pharmacist, or other healthcare professional.
• Some medicines may have different patient information sheets. Check with your pharmacist. If you have questions about this drug, talk with your doctor, nurse, pharmacist, or other healthcare professional.
• If you think there has been an overdose of a drug, call a Poison Control Center immediately or seek medical attention. Be prepared to tell or show which drug you took, how much and when it happened.

Use of information by consumer and limitation of liability

This information should not be used to make decisions about taking this or any other drug. Only the attending physician has the necessary knowledge and experience to make decisions about which drugs are appropriate for a particular patient.This information does not guarantee that the drug is safe, effective, or approved for the treatment of any disease or specific patient. Here are only brief general information about this drug. It does NOT contain all available information on the possible use of the drug with instructions for use, warnings, precautions, information about interactions, side effects and risks that may be associated with this drug. This information should not be construed as a guide to treatment and does not replace the information provided to you by your healthcare professional.Check with your doctor for complete information on the possible risks and benefits of taking this drug. Use of this information is governed by the Lexicomp End User License Agreement available at https://www.wolterskluwer.com/en/solutions/lexicomp/about/eula.

Copyright

© UpToDate, Inc. and its affiliates and / or licensors, 2021. All rights reserved.

Memorial Sloan Kettering Cancer Center

This document, provided by Lexicomp ^® , contains all the information you need to know about the drug, including the indications, route of administration, side effects and when you should contact your healthcare provider.

Trade names: USA

Lipitor

Trade names: Canada

ACH-Atorvastatin Calcium; AG-Atorvastatin; APO-Atorvastatin; Atorvastatin-10; Atorvastatin-20; Atorvastatin-40; Atorvastatin-80; Auro-Atorvastatin; BIO-Atorvastatin; DOM-Atorvastatin; JAMP-Atorvastatin; Lipitor; M-Atorvastatin; Mar-Atorvastatin; MINT-Atorvastatin; MYLAN-Atorvastatin; NRA-Atorvastatin; PMS-Atorvastatin; PRIVA-Atorvastatin; RATIO-Atorvastatin [DSC]; REDDY-Atorvastatin; RIVA-Atorvastatin; SANDOZ Atorvastatin; TARO-Atorvastatin; TEVA-Atorvastatin

What is this drug used for?

• Used to lower bad cholesterol (LDL), triglycerides and raise good cholesterol (HDL).
• Used in some people to reduce the risk of myocardial infarction, stroke, and certain heart problems.
• Used to slow the progression of heart disease.
• This medicinal product can be used for other indications. Consult your doctor.

What should I tell my doctor BEFORE taking this drug?

• If you are allergic to this drug, any of its ingredients, other drugs, foods or substances.Tell your doctor about your allergy and how it manifested itself.
• If you have liver disease or increased liver function.
• If you are taking any of the following drugs: cyclosporine, gemfibrozil, glecaprevir in combination with pibrentasvir, letermovir, or tipranavir in combination with ritonavir.
• If you are or may become pregnant. Do not take this drug if you are pregnant.
• If you are breastfeeding. Do not breast-feed while taking this drug.

This list of drugs and diseases that may be adversely associated with this drug is not exhaustive.

Tell your doctor and pharmacist about all medicines you take (both prescription and over-the-counter, natural products and vitamins) and your health problems. You need to make sure that this drug is safe for your medical conditions and in combination with other drugs you are already taking.Do not start or stop taking any drug or change the dosage without your doctor’s approval.

What do I need to know or do while taking this drug?

• Tell all healthcare providers that you are taking this drug. These are doctors, nurses, pharmacists and dentists.
• If you have high blood sugar (diabetes), your blood sugar should be checked regularly.
• Perform blood tests as directed by your doctor. Please consult your doctor.
• Follow your doctor’s recommended diet and exercise program.
• Consult a healthcare professional if you frequently drink grapefruit juice or eat grapefruit.
• Avoid or limit alcohol consumption to less than 3 servings per day. Drinking too much alcohol can increase your risk of liver disease.
• If you are 65 years of age or older, use this drug with caution.You may have more side effects.
• Potential adverse effects of this drug on the fetus. If you can become pregnant, you must use contraception during treatment. If you become pregnant, contact your doctor immediately.

What side effects should I report to my doctor immediately?

WARNING. In rare cases, some people with this drug can have serious and sometimes deadly side effects.Call your healthcare professional or get medical attention right away if you have any of the following signs or symptoms, which may be associated with serious side effects:

• Signs of an allergic reaction such as rash, hives, itching, reddened and swollen skin with blistering or scaling, possibly associated with fever, wheezing or wheezing, tightness in the chest or throat, difficulty breathing, swallowing or speaking, unusual hoarseness, swelling in the mouth, face, lips, tongue, or throat.
• Signs of a urinary tract infection, including blood in the urine, burning or painful sensations when urinating, frequent or immediate urge to urinate, fever, pain in the lower abdomen or pelvis.
• Weakness on one side of the body, difficulty speaking or thinking, trouble maintaining balance, drooping one side of the face, or blurred vision.
• Difficulty urinating or change in the amount of urine excreted.
• Feeling extremely tired or weak.
• Confusion of consciousness.
• Violation or loss of memory.
• This drug may cause muscle pain, soreness, or weakness. The risk may be increased with thyroid dysfunction or kidney problems. It may also be raised when this drug is taken with certain other drugs, or for people 65 years of age or older. Occasionally, severe muscle abnormalities can occur, which can lead to impaired renal function. Fatalities occurred on rare occasions.If you experience muscle pain, tenderness, or weakness (with or without fever, or feeling unwell), seek medical attention immediately. Call your doctor right away if muscle problems persist after you stop taking this drug as directed by your doctor.
• Very bad and sometimes deadly liver problems have happened with this drug. Call your doctor right away if you have signs of liver problems, such as dark urine, tired feeling, lack of appetite, nausea or abdominal pain, light colored stools, vomiting, or yellow skin or eyes.

What are some other side effects of this drug?

Any medicine can have side effects. However, many people have little or no side effects. Call your doctor or get medical help if these or any other side effects bother you or do not go away:

• Diarrhea.
• Joint pain.
• Nausea.
• Nose or throat irritation.
• Sleep disorders.

This list of potential side effects is not exhaustive. If you have any questions about side effects, please contact your doctor. Talk to your doctor about side effects.

You can report side effects to the National Health Office.

You can report side effects to the FDA at 1-800-332-1088. You can also report side effects at https: // www.fda.gov/medwatch.

What is the best way to take this drug?

Use this drug as directed by your healthcare practitioner. Read all the information provided to you. Follow all instructions strictly.

• Take this drug at about the same time of the day.
• Take this medication with or without food.
• Continue taking this drug as directed by your doctor or other healthcare professional, even if you feel well.

What should I do if a dose of a drug is missed?

• Take the missed dose as soon as you can and then return to your regular schedule.
• If 12 or more hours have passed since a dose was missed, skip that dose and return to your normal schedule.
• Do not take 2 doses at the same time or an additional dose.

How do I store and / or discard this drug?

• Store at room temperature in a dry place.Do not store in the bathroom.
• Store all medicines in a safe place. Keep all medicines out of the reach of children and pets.
• Dispose of unused or expired drugs. Do not empty into toilet or drain unless directed to do so. If you have any questions about the disposal of your medicinal products, consult your pharmacist. Your area may have drug recycling programs.

General information on medicinal products

• If your health does not improve or even worsens, see your doctor.
• You should not give your medicine to anyone and take other people’s medicines.
• Some medicines may have different patient information sheets. If you have questions about this drug, talk with your doctor, nurse, pharmacist, or other healthcare professional.
• Some medicines may have different patient information sheets. Check with your pharmacist. If you have questions about this drug, talk with your doctor, nurse, pharmacist, or other healthcare professional.
• If you think there has been an overdose of a drug, call a Poison Control Center immediately or seek medical attention. Be prepared to tell or show which drug you took, how much and when it happened.

Use of information by consumer and limitation of liability

This information should not be used to make decisions about taking this or any other drug. Only the attending physician has the necessary knowledge and experience to make decisions about which drugs are appropriate for a particular patient. This information does not guarantee that the drug is safe, effective, or approved for the treatment of any disease or specific patient.Here are only brief general information about this drug. It does NOT contain all available information on the possible use of the drug with instructions for use, warnings, precautions, information about interactions, side effects and risks that may be associated with this drug. This information should not be construed as a guide to treatment and does not replace the information provided to you by your healthcare professional. Check with your doctor for complete information on the possible risks and benefits of taking this drug.Use of this information is governed by the Lexicomp End User License Agreement available at https://www.wolterskluwer.com/en/solutions/lexicomp/about/eula.

Copyright

© UpToDate, Inc. and its affiliates and / or licensors, 2021. All rights reserved.

90,000 What painkillers to take for hemorrhoids. Pain relievers for the treatment of hemorrhoids

Hemorrhoids is a proctological disease that occurs against the background of inflammation and varicose veins of the rectum and manifests itself in severe pain in the anal canal, the formation of hemorrhoids, anal fissures and bleeding.it is used as part of the complex therapy of the pathological process as an analgesic, anti-inflammatory and antipyretic agent.

Composition and pharmacodynamics of the drug

Ibuklin is a combined non-steroidal analgesic and anti-inflammatory agent. The drug is produced in tablet form for oral administration.

The main active ingredients of the drug are:

• paracetamol in the amount of 0.375 g;
• ibuprofen in the amount of 0.4 g.

As auxiliary components, the tablet contains certain proportions:

• microcrystalline cellulose;

90,017 corn starch;

• colloidal anhydrous silicon dioxide;
• glycerin;

90,017 talcum powder;

• sodium starch glycolate;
• magnesium stearate;
• hypromellose;
• dimethicone;
• sorbic acid;
• macrogol;
• polysorbate;
• titanium dioxide.

Helps to reduce the intensity of pain, eliminate the sensations of discomfort, itching and burning in the anorectal canal. In addition, the agent has pronounced anti-inflammatory and antipyretic properties. The drug is highly digestible. The formation of the first therapeutic effects occurs 20-30 minutes after taking the pill, the maximum therapeutic effect – after 2 hours. The average duration of the analgesic, antipyretic and anti-inflammatory effect is 6 to 24 hours.

The tool is effective both in the complex therapy of chronic hemorrhoids and in the acute course. During an exacerbation of hemorrhoids, an increase in the size of inflammatory elements occurs. This leads to their injury by fecal masses passing through the intestines, prolapse and pinching, the occurrence of anal fissures and bleeding, which cause an intensification of pain, uncomfortable, itching and burning sensations. Ibuklin from hemorrhoids
helps to reduce the severity of the inflammatory process in hemorrhoids and bumps, eliminate edema and hyperemia, feelings of pain and heat.

Ibuklin for hemorrhoids: how to use the drug?

Answer to the question, how to take Ibuklin for hemorrhoids
, can be found in the instructions for use of the medicinal product. The section “Method of administration” states that the tablets are intended for oral use.
Ibuklin tablets for hemorrhoids take 1 pc. 2-3 times a day, 2 hours before or 2 hours after eating, drinking plenty of clean drinking water.
The maximum daily dose is not more than 4 tablets.The maximum permissible duration of the therapeutic course with Ibuklin tablets should not exceed 3-5 days.
For elderly people, as well as for patients with impaired kidney and liver function, an adjustment in the daily dosage of the agent is necessary.

Contraindications to the use of Ibuclin

If hemorrhoids are diagnosed, Ibuklin, despite all its benefits, is prohibited from using if there are contraindications to its use.

90 016 90 017 children under the age of 12;

90,017 women, during the period of bearing a child and breastfeeding;

90,017 people with gastric ulcer and duodenal ulcer, dysfunction of the gastrointestinal tract;

90,017 patients with renal and hepatic insufficiency;

90,017 people with congenital hyperbilirubinemia;

90,017 patients with optic nerve damage;

Possible side effects

After using the anti-inflammatory and analgesic agent Ibuklin for hemorrhoidal disease, there is a risk of 90,075 side effects, such as:

• Various forms of allergic skin reactions;
• pain in the epigastrium, nausea and vomiting;

90,017 stool disorders and diarrhea;

90,017 headaches and dizziness;

• temporary visual impairment.

With long-term use of high doses of the drug, there is a possibility of erosive damage to the mucous membranes of the stomach and intestines. As well as violations in the functioning of the liver and urinary system, malfunctions of the hematopoietic system.
The appearance of the first signs of a negative effect of the drug on the body is a reason to abandon its use and switch to another anti-inflammatory and analgesic drug.
The drug does not have a hypnotic effect and does not affect the speed of reactions, the ability to drive vehicles or other mechanisms.

Ability to interact with other drugs and substances

With the simultaneous use of Ibuclin with drugs from the category of non-steroidal anti-inflammatory drugs, the risk of adverse reactions increases significantly.
The simultaneous use of Ibuclin with alcoholic beverages increases the toxic effect on the liver.

Important! Ibuklin has the ability to enhance the effect of anticoagulants, insulin and antidiabetic drugs, to neutralize the effects of diuretic and antihypertensive drugs.

Ibuklin for hemorrhoids: reviews of use

1. I have had hemorrhoids for over 6 years. Now he does not bother me at all, then he starts to hurt unbearably, bleed. Sometimes external nodes and bumps appear, which dissolve over time. During exacerbations, I always use painkillers, because otherwise I simply would not be able to fully work. How many drugs have I tried? In search of the best remedy, I came across an article about Ibuklin for hemorrhoids, reviews of its use claimed that the remedy effectively eliminates pain and helps to reduce inflammation.Indeed, the tool turned out to be very powerful. Now 4–5 days are enough for me to suppress the unpleasant symptoms (Grigory, 38 years old).
2. I have a comprehensive approach to solving the problem of hemorrhoids. During periods of exacerbation, I use rectal antihemorrhoidal suppositories and ointments, which I change periodically so as not to develop addiction. To normalize the state of blood vessels in the body, I take venotonic drugs. To eliminate pain, reduce the severity of inflammation, hyperemia and edema, I use Ibuklin during periods of exacerbation.The drug is fast acting. In addition, Ibuklin has fairly simple recommendations for use and is designed for a gentle therapeutic course (Valentina, 56 years old).

Ibuklin – non-steroidal anti-inflammatory, analgesic and antipyretic agent
in the form of tablets for oral use. The drug effectively relieves pain, helps to reduce the intensity of itching, burning and discomfort, eliminates the inflammatory process in the tissues and blood vessels of the large intestine, helps to eliminate edema and hyperemia.To achieve the best therapeutic effect, the tablets must be used in combination with laxatives, antihemorrhoidal suppositories and ointments, venotonic drugs, therapeutic diet and exercise therapy.

Hemorrhoids are manifested by enlarged or varicose veins in the anus and rectum. How can you relieve hemorrhoids at home?

Hemorrhoidal disease is a fairly common disease, especially in developed countries, and 90,075 affects almost 5% of the population
.There are two types of hemorrhoids, external and internal, which can occur separately or in combination. occurs in about 38% of women in the third trimester of pregnancy.

Hemorrhoids

Several risk factors are the etiology of the development of hemorrhoids, including aging, obesity, depressed mood and pregnancy. Meanwhile, some conditions associated with increased intra-abdominal pressure, such as constipation and prolonged tension, are thought to cause hemorrhoids as a result of impaired venous drainage of the hemorrhoidal plexus.

Several foods and lifestyles, including a low fiber diet, spicy foods, and alcohol consumption, have been linked to the development of hemorrhoids.

Hemorrhoid pain

External hemorrhoids develop under the skin, outside the opening of the anus. The dilated veins are usually painful, but if thrombosis develops, then they appear as round, purple bumps around the anus.

Internal hemorrhoids are often present in the distal intestine without causing any discomfort in the person
…He may not even be aware of the existence of varicose veins in the rectum. This is due to the fact that there is a rectal lining (mucous membrane) around the internal hemorrhoids, it has a very small number of nerve fibers.

Sometimes the patient may have a feeling of fullness in the rectum, like a false urge to defecate. If hemorrhoidal veins become thrombosed or bleed, bright red blood appears during and / or after a bowel movement. If hemorrhoids are pinched, they can become very painful.

Hemorrhoid pain relievers tablets can also relieve pain, but they work more slowly than topical medications.

Candles

How to quickly relieve hemorrhoids at home? help relieve pain in the distal intestine and reduce signs of inflammation.
However, suppositories have only a local effect without affecting the causes of the pathological process.

Candles:

1. Anucort.
2. Procaine.
3. Anestezol.
4. Procto-Glivenol.

Anucort

Anucort – This drug is used in proctology to treat hemorrhoidal itching and edema in the rectum. It is also prescribed with other drugs to treat certain intestinal problems (such as ulcerative colitis of the rectum and other rectal / anal inflammatory conditions).

Suppositories contain hydrocortisone, which helps relieve rectal pain and itching by reducing tissue swelling in the rectum and anus.

Anusol

Anusole – this drug is used to temporarily relieve unpleasant symptoms: the feeling of burning, pain and itching caused by hemorrhoids. This product contains beneficial ingredients such as cocoa butter, starch or zinc oxide to act as a protective barrier.

These components are designed to prevent irritating stool contact. This barrier helps protect inflamed, irritated skin and makes emptying the distal bowel less painful. Anusole is usually used up to 6 times a day or after each bowel movement.

Procaine

Procaine – candles with novocaine for quick relief of pain in hemorrhoidal disease. This drug is used in proctology to relieve internal hemorrhoids
, as well as before rectal examination or surgery.

Anestezol

Anestezol – rectal suppositories are similar in their pharmacological effect to novocaine. They relieve pain, inflammation and congestion.The preparation contains astringent and wound-healing substances.

In addition, Anestezol facilitates the passage of the chair, softens the act of defecation.

Olestezin

Olestezin

Olestezin – rectal suppositories that contain natural sea buckthorn oil. These are recommended for use in hemorrhoidal disease, anal fissures, ulcerative lesions of the intestine. Suppositories quickly reduce signs of inflammation, pain and gradually restore tissue integrity
…

Procto-Glivenol

Procto-Glivenol is a suppository for hemorrhoids with an analgesic effect. The drug contains two active pharmacological components: trienoside and lidocaine.

The first substance improves vascular tone and restores damaged capillaries of the rectum and anus. The second component of the drug provides a quick and effective analgesic effect.

Pain-relieving ointment

Creams and gels – pain relievers for hemorrhoids and cracks at home.They are recommended by doctors for quick pain relief, as all components are absorbed very quickly into the surrounding skin and begin to act almost immediately. They can be used in combination with rectal suppositories.

Ointments:

1. Troxevasin.
2. Proctosan.
3. Tronolan.
4. Hydrocortisone cream.
5. Analog.

Troxevasin

Troxevasin is a light gel with a pleasant smell.It restores well the elasticity of the venous and arterial walls, small capillaries, reducing the risk of hemorrhoids progression. It has anti-inflammatory, anti-edematous and mild analgesic effects. Gel can be used by women during pregnancy and lactation.

Proctosan

Proctosan – the active substance of the drug is bismuth, it has a quick analgesic effect. It is very effective for external hemorrhoids, thrombosis and bleeding.

Proctosan

Hydrocortisone cream is an inexpensive hormonal preparation for the treatment of hemorrhoids. Hydrocortisone reduces intestinal swelling, unpleasant itching and redness in the anal area
. However, long-term use of hormonal drugs is not recommended, as this can lead to atrophy of the mucous membrane of the distal intestine.

Analpram

Analpram – This combination drug is used to treat minor pain, itching, swelling and discomfort caused by hemorrhoids and other problems in the anal area (eg, anal fissures).This medication contains pramoxine, an anesthetic that works by temporarily numbing the rectal area. This product also contains hydrocortisone, a corticosteroid that reduces redness, itching and swelling.

Before use, wash the affected area with mild soap and water and dry well.

Tronolan

Tronolan is an ointment with an analgesic effect for hemorrhoids. This drug acts as an anesthetic to relieve pain by numbing the affected area.It can also provide quick relief from hemorrhoid symptoms such as pain and itching.

Trolonan is odorless and does not contain colorants. It lubricates and soothes hemorrhoids, preventing drying out and further irritation. Recommended for children over 12 years old and adults
. It can be applied 5 times a day, but not more than 7 days.

Tablets

Tablet forms:

1. Ibuklin.
2. Pentalgin.
3. Nise.
4. Detralex.

Ibuklin

Ibuklin is a non-steroidal anti-inflammatory drug
is recommended for relief of severe pain syndrome during the acute phase of the disease. The tablets relieve pain in the entire pelvic area without further affecting the hemorrhoidal veins.

Pentalgin

Pentalgin

Pentalgin – this drug very well and quickly relieves pain in hemorrhoids, but it cannot be taken for a long time due to numerous contraindications and side effects.

Nise

Nise tablets help to relieve hemorrhoids. It is a versatile medicine suitable for the treatment of pain and discomfort. However, it is contraindicated in violation of the blood coagulation system.

Detralex

Detralex is one of the most effective innovative drugs for the treatment of hemorrhoids. The main advantage of this medication is that it can be used at all stages of the pathological process.

The components of the preparation strengthen and restore the venous wall and reduce pain in this disease.But in order to achieve this effect, the medicine must be taken in courses.

Tablets for hemorrhoids Detralex

Treatment at home

Hemorrhoid pain is often relieved by sitting in a warm water bath for 10 or 15 minutes two to four times a day. It is also recommended to apply a cool compress or ice pack to the anal area to reduce swelling
(The ice bag should be wrapped in a cloth or towel to prevent direct skin contact).

You can make a candle from raw potatoes at home.
Peel the vegetable and cut a candle to a shape and size that resembles a pharmacy. You can enhance the effect by dripping camphor oil on the potatoes. Good for fighting inflammation and pain, potatoes also cool and heal small cracks. If you have external hemorrhoids, you can attach raw potatoes wrapped in gauze to the anus.

Conclusion

With this disease, you cannot self-medicate, search the Internet for the names of pain-relieving pills for hemorrhoids and cracks and drink them without a doctor’s prescription.

If pain occurs in the rectal area, you should consult a specialist who will prescribe adequate therapy.

A common proctological disease is hemorrhoids. It develops imperceptibly, goes into serious stages and can become chronic. At the first symptoms of pain, you need to choose the right pain reliever for hemorrhoids – suppositories, ointments or other drugs that eliminate discomfort. Pain-relieving medicines improve the patient’s condition, relieve inflammation of the blood vessels, and act in a complex on hemorrhoids and bumps.

How to relieve hemorrhoids

In medical practice, this is a chronic disease of the rectum resulting from varicose veins, the formation of cavernous bodies due to stagnation of blood in the vessels of the anus. The disease can worsen or subside, so it is important to know how to relieve the pain of hemorrhoids if an exacerbation occurs. The cause of pain symptoms is inflammation of the hemorrhoids and damage to the mucous membrane. For relief, local and systemic medicines are suitable – tablets, ointments, gels, creams, suppositories, injections and traditional medicine methods.

Drug treatment of hemorrhoids

Exacerbation of hemorrhoids is a pronounced inflammatory process. Its complete disappearance can be achieved only with medicines. Painkillers contain local anesthetics, which have anti-inflammatory, regenerating, analgesic effects. Creams, ointments and suppositories are considered popular remedies. Tablets are prescribed only in complex therapy – they have more side effects, have many contraindications, are absorbed for a long time for the onset of a therapeutic effect, act on the entire body, and not on the focus of inflammation.

Folk remedies for pain with hemorrhoids

If hemorrhoids are caught by surprise and discomfort needs to be removed urgently, folk remedies will help. These include self-made candles, lotions, baths, herbal microclysters. Here are some effective procedures:

• ice candles with chamomile – freeze decoction of flowers in the form of rectal suppositories, insert into the anus and hold until they melt;
• cold sitz baths with decoction of St. John’s wort, mountaineer, oregano, strawberry – take no longer than five minutes;
• lubrication of the damaged area with propolis, honey;
• beetroot or carrot juice enemas;
• candles with sea buckthorn oil or propolis.

How to relieve hemorrhoids at home

Rectal suppositories and ointments, which are effective in any form of hemorrhoids, have a pronounced reaction. They are composed of anesthetics, which give relief to the patient’s condition in a few hours. The effect lasts up to several hours. It is optimal to choose pain relievers and anti-inflammatory suppositories for treatment. The best suppositories are:

• Relief;
• Neo-Anusole;
• Posterisan;
• candles with sea buckthorn oil.

According to doctors, the best anesthetic ointments for home use are:

• heparin;
• Troxevasin;
• Proctosan;
• Relief;
• Levomekol;
• Ichthyol.

Effective tablets for use as a pain reliever during an exacerbation are:

• Detralex;
• Nise;
• Pentalgin.

Pain reliever for external hemorrhoids

Ointments are considered the best remedies designed to relieve pain with external hemorrhoids: they combine well with other medicines, are convenient for home use in the early or late stages of the disease.In addition to the analgesic effect, the agents have a regenerative, drying, hemostatic effect. The local action of ointments allows you to eliminate pain in a specific area.

Each pack of ointment or cream contains an applicator for easy application of the medication to the affected area. You need to apply the product up to five times a day according to the instructions for use, preferably after a bowel movement. The effect will be more pronounced, faster if tampons soaked in ointments are injected. Popular remedies for the treatment of external hemorrhoids are:

• Proctosedil;
• Hepatrombin;
• Aurobin;
• heparin ointment;
• ointment Vishnevsky, Fleming, ichthyol;
• Proctosan.

How to anesthetize internal hemorrhoids

For acute pain, it is good to use special means: doctors offer anesthetic for internal hemorrhoids in the form of suppositories, which have a composition with analgesics. Rectal suppositories quickly relieve pain, actively eliminate inflammation, irritation, and swelling. Popular candles for the treatment of this type of ailment are:

• Relief Advance;
• Neo-Anusole;
• with calendula, sea buckthorn oil, St. John’s wort, chamomile, yarrow;
• Betiol;
• Hemorol;
• with adrenaline, novocaine;
• Anestezol.

Pain relieving suppositories for hemorrhoids

Proctologists provide effective analgesic suppositories for the rectum, which are quickly absorbed into the bloodstream of the colon mucosa, blocking symptoms. Here they are:

• Neo-Anusole – effectively treat a weeping, protracted form of the disease, the composition contains components that kill microbes, relieve inflammation.
• Ginkor Prokto – with butamben in the composition, helps to get rid of pain, itching in the anus, to normalize the condition of the veins.
• Posterisan – reduces pain, heals injuries of the anus, rectal mucosa, increases local immunity.
• With adrenaline – a strong analgesic that helps to stop bleeding, contraindicated for hypertensive patients, dispensed by prescription, prescribed to young patients with blood from the nodes.
• With sea buckthorn oil – a natural analgesic substance, does not cause side effects, relieves pain, relieves burning, tissue inflammation, irritation, used during pregnancy.

Suppositories with lidocaine

Doctors prescribe a pain reliever for hemorrhoids with lidocaine to relieve seizures. Effective suppositories-analgesics are:

• Procto-glivenol – a strong analgesic, anti-inflammatory, venotonic agent, contraindications – the first trimester of pregnancy, liver failure.
• Proctosan – contains bufexamak, bismuth subgallate and titanium dioxide, has an anti-inflammatory, wound healing, astringent and drying effect.
• Hepazolone – contains prednisolone and sodium heparin, which have anti-inflammatory and anesthetic effects.

Suppositories with anesthesin

In addition to lidocaine, suppositories for hemorrhoids with analgesic effect may contain anesthesin or benzocaine. Such drugs actively relieve attacks of burning and itching:

• Anestezol – contains menthol, zinc oxide and bismuth subgallate with an astringent, anti-inflammatory effect, facilitates defecation, accelerates regeneration.
• Relief Advance – with shark liver oil, has an immunomodulatory, anti-inflammatory, wound healing effect.
• Olestezin – on sea buckthorn oil with sulfaetidol, a combined preparation with anti-inflammatory, analgesic and antibacterial effect.
• Nigepan – contains sodium heparin, which prevents the formation of blood clots, stops the progress of the development of nodes.

Anesthetic ointment

According to proctologists, the ointment is the best for this ailment: its medicinal components are quickly absorbed into the bloodstream, providing the maximum therapeutic effect.The best drugs from the pharmacy are:

1. Heparin – contains heparin, relieves pain and itching, blocks inflammation, thrombosis, edema. It is used for severe hemorrhoids without bleeding, has no contraindications.
2. Troxevasin – fights any stage and form of hemorrhoids, quickly relieves pain, swelling, tones veins.
3. Fleming’s ointment – suitable for elderly people, pregnant women, lactating women. Contains natural herbal ingredients to relieve pain and inflammation.
4. Levomekol – used after childbirth or surgery to remove nodes. Safe, has no contraindications and side effects.
5. Vishnevsky ointment – normalizes blood circulation in the small pelvis, prevents stagnation. It is used after compresses with potassium permanganate.
6. Ichthyol – relieves pain during bowel movements, antiseptic, heals cracks in the mucous membrane.

Injections for hemorrhoids

For severe pain, doctors may prescribe anesthetic injections.It is forbidden to make them on your own due to the complexity and unpredictability of the effect. A common method is novocaine blockade, in which the area around the anus is chipped off. Novocaine or lidocaine are used as pain relievers. They relieve exacerbations, severe pain, heal wounds after surgery.

Pain Relief Tablets

For most people, pain reliever tablets are the most convenient way to use them. Medicines are effective and contain natural or artificial ingredients.In the initial stages of the disease, pills can relieve pain and even cure the disease. An exacerbation of the disease is characterized by severe pain that can eliminate:

• Detralex – gives an effect in half an hour, prevents bloody discharge, congestion, increases the tone of the veins.
• Hemoroidin – contains herbal extracts that strengthen the walls of blood vessels, prevent bleeding, relieve pain and burning.
• Phlebodia – gives strong pain relief, relieves inflammation, reduces blood congestion, the effect occurs after five hours.
• Paylex – a combined medicine with a herbal composition, disinfects, relieves pain.
• Litovit B – contains bran, zeolite and burnet, removing pain during bowel movements, itching and burning.
• Asclezan A – capsules with hazelnut extract, used to prevent the development of hemorrhoids, improve blood circulation, increase venous tone.
• Ibuklin is a strong pain reliever with anti-inflammatory effect.
• Nise is an antipyretic drug that relieves inflammation and pain.

Video: suppositories for hemorrhoids – pain relievers and anti-inflammatory

In the presence of hemorrhoids in a patient, highly qualified specialists try to cure the disease with more gentle methods, namely, resorting to the use of drug therapy. This approach not only makes it possible to carry out more conservatively, but also helps to avoid surgical intervention.

Different degrees of the disease are treated with different types of pills. Appropriate medications are prescribed by the attending physician, who, after a general examination, will help you choose the most effective and optimal medications for your body.It is noteworthy that most of the pills for hemorrhoids are made on the basis of herbal extracts, so most of them are absolutely safe for health.

An experienced proctologist is able to select effective pills for hemorrhoids that suppress painful symptoms and eliminate discomfort in the shortest possible time, bringing life back to normal. The tablets are beneficial, first of all, because the course of the drug is able to simultaneously strengthen the walls of blood vessels, prevent bleeding and relieve swelling with inflammation.

Thus, the patient receives complex therapy. If you combine medication at the same time with gymnastic exercises and proper nutrition, then the disease will completely recede with an impressive speed.

The main advantages of pills for hemorrhoids include:

• An extensive assortment of selection, allowing you to choose the most suitable drug not only in terms of indications, but also in terms of cost;
• Natural base that makes tablets harmless to the gastrointestinal tract, liver and kidneys;
• Accelerated recovery, achieved through a modern formula that is used in the manufacture of most pills for hemorrhoids;
• Ease of use.Tablets, in contrast, are more rational to use, since they can easily be taken with you to work or on vacation;
• Some types of medications help to get rid of, which has a positive effect on the treatment of the disease;
• The active components of the tablets help to normalize blood outflow;
• Tablets relieve painful symptoms and relieve pain better than other drugs;
• Most of the drugs are approved for use by the elderly.

The main advantage of tablets is their absolute versatility, as they can be used by patients with initial and ailments. In addition, when using tablets, special hygiene recommendations are not required, which are extremely necessary in other cases.

To begin the optimal effective treatment, you need to understand the types of pills for hemorrhoids. First of all, it is necessary to deal with the misconception that any pills for a disease are equally capable of eliminating its causes and symptoms.But such assumptions are more erroneous.

There are several main types of drugs for hemorrhoids, which are selected taking into account the specific characteristics of the patient and his ailment. So, among them are the following:

1. Painkillers – mainly used during an exacerbation to eliminate particularly unpleasant and painful sensations. Additionally, anti-inflammatory drugs can be prescribed, which in the complex not only remove pain, but fight the factors that caused the appearance of the disease.
2. Venotonic – phlebotropic drugs that help to normalize venous outflow. Due to their action, the tablets improve blood circulation, tone the veins, and also improve microcirculation in the formations of the cavernous type.
3. Laxatives – used additionally in combination with the main treatment. Laxative tablets improve bowel motility, which helps prevent complications of the disease and the possibility of constipation.
4. Hemostatic – are used only after prior consultation with a doctor.Serious bleeding is a good reason for seeking immediate help in the form, since the pills will clearly not be enough.

Medicines for the treatment of hemorrhoids contain not only chemical components, but also most of the natural components. The most optimal use for the treatment of non-started forms of the disease is bioflavonoids. They are most effective in their action and at the same time consist exclusively of herbal ingredients.

Optimally cheap pills for hemorrhoids are a reality, since today’s assortment of drugs allows you to find a buyer of any financial category.Unfortunately, in most cases, drugs with too low cost do not perform as well as more expensive tablets.

The cost of tablets depends on the manufacturer – whether it is domestic or foreign. You also need to pay attention to the brand of the drug. Often, the total cost of a product is billed as the brand is promoted, and not due to its unique healing efficacy. In almost all cases, such tablets have cheaper counterparts that have an identical composition, but their purchase costs several times less.

• Expensive drugs: Olfen, Paylex, Detralex, Glivenol, Venoruton:
• Available drugs: Ibuklin, Eskuzan, Nise, Troxevasin, Ginkor Fort, Asklesan.

Expensive pills cannot guarantee you a 100% cure, so before using them, be sure to consult with your doctor.

Are there any differences between tablets?

Each drug has individual indications, so their thoughtless use for self-medication can lead to serious complications.In the treatment of hemorrhoids, these types of pills are used, the action of which is aimed at different types of problems, namely:

• Anesthetics – used for the acute form of the disease, allowing you to get rid of especially painful sensations and at the same time eliminate foci of inflammation. Without fail, the patient is assigned to the rest of the list of drugs.
• Hemostatics – improve blood clotting, are used for heavy bleeding from the anus.
• Anticoagulants – dissolve blood clots and improve blood flow.
• Bioflavonoids – used in the earliest stages of hemorrhoids, as they allow you to eliminate the first hints of the appearance of nodes, and also remove.

Pharmacy chains now offer a wide selection of different medicines for hemorrhoids. In order to properly use their useful properties and at the same time not harm yourself, you should first carefully read the instructions.

• Pain-relieving tablets for hemorrhoids: Phlebodia, Detralex, Litovit, Ibuklin, Pentalgin, Nise, Hemoroidin;
• Tablets for exacerbation of hemorrhoids: Voltaren, Nise, Movalis, Ibuprofen, Diclofenac, Ultrapoct, Troxevasin, Detralex;
• Tablets for acute hemorrhoids: Adroxon, Posterisan, Ginkor Fort, Detralex, Litovit.

The effect of painkillers is aimed at eliminating the discomfort that occurs in the initial stages of the disease. They do not require special prescriptions, so patients can use them as needed. Painkillers do an excellent job with pain syndrome, prevent the development of inflammation.

Preparations for exacerbation of hemorrhoids are taken in the presence of bleeding bumps, which bring significant inconvenience and cause pain when trying to go to the toilet.Such drugs have an excellent healing effect and quickly return a person to their original state.

In acute hemorrhoids, broad-spectrum drugs are used. They have a combined effect, allowing you to simultaneously eliminate inflammation, relieve swelling, itching. Such pills are prescribed according to the recommendations of the proctologist. When taking these funds, you should be especially careful, since in addition to the therapeutic effect, there are side effects.

Pills for hemorrhoids during pregnancy

At the initial stages, pregnant girls do not need treatment with pills, since the ailment is perfectly eliminated through diet and physical correction.However, when you can no longer do without aids, including without pills for hemorrhoids.

Preparations for pregnant women are prescribed both in the form of tablets and in the form of capsules. Vetotonics are often used – pills that are focused on strengthening the walls of the veins. They are assigned to girls after examination by a proctologist.

The general course lasts 3 weeks. In this case, the girl must comply with all the doctor’s prescriptions, from and ending with the daily lifestyle. It is possible to use it in conjunction with drugs, since pills can not always give a tangible and significant result.

Among the drugs used by pregnant girls, one can single out:

• Troxevasin;
• Courantil;
• Aspirin;
• Ginkor Forte.

In addition, the following laxatives can be used to facilitate the process of going to the toilet, which will significantly affect the process of new bumps.

• Prelax;
• Regulax;
• Duphalac;
• Forlax.

In more advanced cases of hemorrhoids, pills are prescribed only to relieve existing symptoms and reduce the degree of manifestation of the disease.Full treatment occurs after childbirth and only in an operative manner.

Ibuklin for hemorrhoids is an effective way to get rid of unpleasant symptoms of the disease. The drug can be used in complex treatment, with prolapse of hemorrhoids and in the stage of exacerbation of the disease. Ibuklin tablets help to quickly eliminate and help to transfer the acute course of the disease.

Ibuklin is a drug that can be used in the treatment of proctological diseases. The tablets eliminate painful sensations, thereby facilitating bowel movements, eliminating burning sensation and discomfort in the rectum.Ibuklin has a pronounced analgesic effect, so it is advisable to use the medicine to eliminate pain in hemorrhoids. The drug also has a mild anti-inflammatory effect.

The main purpose of Ibuklin is to relieve pain. A powerful anesthetic that eliminates pain in the entire pelvis. Inflamed hemorrhoids cause a lot of pain and discomfort in the acute phase. The drug Ibuklin provides quick elimination of pain of any intensity.

The components of the product are quickly absorbed into the bloodstream in the body and begin their therapeutic effect 15-20 minutes after administration. The active medicinal substances that are present in the tablet dilate blood vessels, relieve their spasm and act on the nerve endings. The medicine quickly blocks pain impulses.

The medication has anti-inflammatory and antipyretic effects. It relieves inflammation and prevents the development of complications in hemorrhoids.

Ingredients

The composition of the drug includes two powerful substances:

• paracetamol 323 mg;
• ibuprofen 400 mg.

Their combination can significantly reduce pain in the rectum and anus. Treatment of hemorrhoids with Ibuklin is aimed at rapid pain relief and partial removal of the infectious and inflammatory process. It is important to know that with increased use of pills can cause the development of bleeding.

This medication should only be taken as directed by a physician. If you experience any undesirable reactions and complications, you should consult your doctor.

How to use Ibuklin for hemorrhoids

The drug is taken orally, inside the body. The tablet should be swallowed whole, without chewing, and washed down with plenty of water. The tool is being used.
The recommended dosage of this medication is 1 tablet twice to three times a day.

Contraindications

Instructions for use indicate in detail the cases in which the medication cannot be used in the treatment of hemorrhoids. As with any medicine, there are contraindications to taking Ibuclin.The drug should not be taken at:

1. various blood diseases;
2. stomach ulcer;
3. intestinal lesions;
4. bleeding.

In other cases, the tablets are well tolerated by the body and rarely cause adverse reactions. Reviews for this drug indicate that it is advisable to use Ibuklin for quick pain relief.

After taking the pill, a significant improvement in well-being is observed, pain, burning and itching in the anal canal are eliminated.The drug also has anti-inflammatory effects. The drug is not used in the treatment of children under 12 years of age and with individual intolerance.

Side effects

In some cases, allergies, headaches, dizziness may occur. The various clinical symptoms are due to a powerful immune response. The appearance of side effects is associated with the characteristics of the human immune system.

Adverse reactions may also include itching, tingling, nausea, vomiting, and indigestion.The development of undesirable effects can lead to erosive lesions of the mucous membrane. If an adverse reaction occurs, the use of Ibuclin should be discontinued and a doctor should be consulted.

Special instructions

An overdose of a medicinal product may cause an increase in adverse reactions. The maximum dose of the drug should not exceed more. For anesthesia, the agent is used no longer than 5-6 days.

The drug affects the action of insulin and blood sugar levels.Ibuklin is undesirable to use in conjunction with drugs, the action of which is aimed at blood clotting. Ibuklin is incompatible with the drug Digoxin, Methotrexate, Probenecid. The drug must be stored in a dark place at room temperature.

Suvardio® | Sandoz in Russia

Pharmacodynamics

Rosuvastatin is a selective, competitive inhibitor of HMG-CoA reductase, an enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A into mevalonate, a cholesterol precursor.Rosuvastatin acts on the liver, where cholesterol (CS) synthesis and low-density lipoprotein (LDL) catabolism are carried out.

Rosuvastatin increases the number of LDL receptors on the surface of hepatocytes, which increase the uptake and catabolism of LDL, and inhibits the synthesis of very low density lipoproteins (VLDL) by the liver, thereby reducing the amount of LDL and VLDL.

Rosuvastatin reduces the concentration of low-density lipoprotein cholesterol (LDL-C), total cholesterol, triglycerides (TG), increases the concentration of high-density lipoprotein cholesterol (HDL-C), and also reduces the concentration of apolipoprotein B (ApoV), cholesterol-non-LDL Cholesterol-VLDL, TG-VLDL and increases the concentration of apolipoprotein A-1 (ApoA-1) (see.Table 1), reduces the ratio of cholesterol-LDL / cholesterol-HDL, total cholesterol / HDL cholesterol and cholesterol-non-HDL / HDL cholesterol and the ratio of ApoV / ApoA-1.

After the start of rosuvastatin therapy, the therapeutic effect appears within one week, after 2 weeks of treatment it reaches 90% of the maximum possible effect. The maximum therapeutic effect is usually achieved by 4 weeks and is maintained with regular administration of the drug.

Table 1. Dependence of response to treatment on the dose of rosuvastatin in patients with primary hypercholesterolemia (types IIa and IIb according to Fredrickson)
(mean adjusted percentage change from baseline concentration)

Clinical efficacy

Rosuvastatin is effective in adult patients with hypercholesterolemia, with or without hypertriglyceridemia, regardless of race, gender or age, including patients with diabetes mellitus and familial hypercholesterolemia.

In 80% of patients with hypercholesterolemia IIa and IIb types according to the Fredrickson classification (average initial concentration of LDL-C is about 4.8 mmol / L) when using rosuvastatin at a dose of 10 mg, the concentration of LDL-C reaches values ​​less than 3 mmol / L.

In patients with heterozygous familial hypercholesterolemia, who took rosuvastatin in doses from 20 to 80 mg according to the forced dose titration scheme, there was a positive dynamics of lipid profile parameters. After titration of the daily dose to 40 mg per day (12 weeks of therapy), the concentration of LDL-C decreased by 53%.In 33% of patients, a decrease in the concentration of LDL-C less than 3 mmol / l was achieved.

In patients with homozygous familial hypercholesterolemia, who took rosuvastatin at doses of 20 and 40 mg, the average decrease in the concentration of LDL-C was 22%.

An additive effect is observed in combination with fenofibrate in relation to the concentration of TG and with nicotinic acid (more than 1 g per day) in relation to the concentration of HDL-C.

In patients with a low risk of developing coronary heart disease (CHD) (risk on the Framingham scale less than 10% over a period of more than 10 years), with an average LDL-C concentration of 4.0 mmol / L (154.5 mg / dL) and subclinical atherosclerosis, which was assessed by the thickness of the intima-media complex of the carotid arteries (TCIM), rosuvastatin at a dose of 40 mg / day significantly slowed down the rate of progression of the maximum TCIM for 12 segments of the carotid artery compared with placebo at a rate of 0.0145 mm / year (95% confidence interval (CI): from -0.0196 to – 0.0093, at p <0.0001).A dose of 40 mg should be prescribed only to patients with severe hypercholesterolemia and a high risk of developing cardiovascular diseases.

Pharmacokinetics

Absorption

The maximum concentration (C _max ) of rosuvastatin in blood plasma is reached approximately 5 hours after oral administration. Absolute bioavailability is ≈ 20%.

Distribution

Rosuvastatin is metabolized primarily by the liver, which is the main site of cholesterol synthesis and LDL-C metabolism.The volume of distribution of rosuvastatin is approximately 134 liters. About 90% of rosuvastatin binds to plasma proteins, mainly albumin.

Metabolism

A limited amount of rosuvastatin (approximately 10%) undergoes biotransformation.

The metabolism of rosuvastatin is to a small extent associated with isoenzymes of the cytochrome P450 system. The isoenzyme CYP2C9 is the main isoenzyme involved in the metabolism of rosuvastatin, while the isoenzymes CYP2C19, CYP3A4 and CYP2D6 are involved in metabolism to a lesser extent.

The main metabolites of rosuvastatin identified are N-dismethylrosuvastatin and lactone metabolites.

N-desmethylrosuvastatin is approximately 50% less active than rosuvastatin, lactone metabolites are pharmacologically inactive. More than 90% of the pharmacological activity in inhibiting circulating HMG-CoA reductase is provided by rosuvastatin, the rest is provided by its metabolites.

Withdrawal

Approximately 90% of the taken dose of rosuvastatin is excreted unchanged through the intestines (including absorbed and unabsorbed rosuvastatin), the remainder is excreted by the kidneys.About 5% of the administered dose of the drug is excreted unchanged by the kidneys. The half-life (T _1/2 ) is 19 hours, it does not change with an increase in the dose of the drug. The geometric mean plasma clearance is approximately 50 l / h (coefficient of variation 21.7%). As in the case of other inhibitors of HMG-CoA reductase, the membrane transporter of cholesterol across membranes is involved in the process of hepatic uptake of rosuvastatin. This carrier plays an important role in the excretion of rosuvastatin by the liver.

Linearity

The systemic exposure of rosuvastatin increases in proportion to the dose. After repeated daily administration of the drug, no changes in pharmacokinetic parameters occur.

Genetic polymorphism

Inhibitors of MMC-CoA reductase, including rosuvastatin, bind to transport proteins OATP1B1 (organic anion transport polypeptide involved in the capture of statins by hepatocytes) and BCRP (efflux transporter).Carriers of genotypes SLCO1B1 (OATP1B1) C.521CC and ABCG2 (BCRP) C.421AA showed an increase in exposure (AUC – area under the concentration-time curve) of rosuvastatin by 1.6 and 2.4 times, respectively, compared with carriers genotypes SLCO1B1c.521TT and ABCG2 c.421AA.

Special patient populations

Age and gender

Age and sex do not have a clinically significant effect on the pharmacokinetic parameters of rosuvastatin.

Ethnic groups

Pharmacological studies have shown an approximately twofold increase in the median AUC and C _max rosuvastatin in patients of the Mongoloid race (Japanese, Chinese, Filipinos, Vietnamese and Koreans) compared with those of the Caucasian race; in Indian patients, an increase in the median AUC and C _max by approximately 1.3 times is shown. At the same time, the analysis of pharmacokinetic parameters for the entire study population did not reveal clinically significant differences in the pharmacokinetics of the drug among representatives of the Caucasian and Negroid races.

Renal failure

In patients with mild to moderate renal insufficiency, the plasma concentration of rosuvastatin or N-desmethylrosuvastatin does not change significantly. In patients with severe renal failure (creatinine clearance (CC) less than 30 ml / min), the concentration of rosuvastatin in the blood plasma is 3 times higher, and the concentration of N-desmethylrosuvastatin is 9 times higher than in healthy volunteers. The plasma concentration of rosuvastatin in hemodialysis patients is approximately 50% higher than in healthy volunteers.

Liver failure

patients with varying degrees of liver failure with a score of 7 and below on the Child-Pugh scale did not reveal an increase in T _1/2 rosuvastatin.