What is trihexyphen. Trihexyphenidyl: A Comprehensive Guide to Uses, Dosage, and Side Effects
What is trihexyphenidyl used for. How does trihexyphenidyl work. What are the potential side effects of trihexyphenidyl. How should trihexyphenidyl be taken. What precautions should be considered when using trihexyphenidyl.
Understanding Trihexyphenidyl: An Overview
Trihexyphenidyl, pronounced as (trye hex ee fen’ i dil), is a medication primarily used in the treatment of Parkinson’s disease and to control extrapyramidal symptoms caused by certain medications. As an antimuscarinic drug, it works by relaxing muscles and modulating nerve impulses that control muscle function. This comprehensive guide will delve into the various aspects of trihexyphenidyl, including its uses, dosage, side effects, and important precautions.
The Role of Trihexyphenidyl in Parkinson’s Disease Treatment
Trihexyphenidyl plays a crucial role in managing the symptoms of Parkinson’s disease (PD). But how exactly does it work?
- It helps control tremors and muscle stiffness associated with PD
- Improves balance and coordination in patients
- Works synergistically with other PD medications for better symptom management
By targeting the muscarinic receptors in the brain, trihexyphenidyl helps to restore the balance of certain neurotransmitters, thereby alleviating some of the motor symptoms of Parkinson’s disease. This medication is often prescribed as part of a comprehensive treatment plan, working alongside other drugs to provide optimal symptom relief for patients.
Dosage and Administration of Trihexyphenidyl
Proper administration of trihexyphenidyl is crucial for its effectiveness. How should patients take this medication?
- Available as tablets and elixir (liquid) for oral consumption
- Typically taken three to four times daily, with or without food
- Dosage is individualized based on patient response and tolerability
It’s important to follow the prescribed dosage regimen carefully. Patients should take trihexyphenidyl at consistent times each day to maintain steady levels of the medication in their system. If a dose is missed, it should be taken as soon as remembered, unless it’s almost time for the next scheduled dose. In such cases, the missed dose should be skipped to avoid doubling up.
Special Considerations for Dosage
Are there any special considerations for trihexyphenidyl dosage?
- Elderly patients may require lower doses due to increased sensitivity
- Dosage may be adjusted gradually to minimize side effects
- Abrupt discontinuation should be avoided to prevent symptom rebound
Healthcare providers will carefully titrate the dose to find the optimal balance between symptom relief and side effect management. Patients should never adjust their dosage without consulting their doctor first.
Potential Side Effects and Adverse Reactions
Like all medications, trihexyphenidyl can cause side effects. What are the most common adverse reactions associated with this drug?
- Dry mouth
- Blurred vision
- Constipation
- Dizziness
- Nausea
- Urinary retention
While these side effects are generally mild and may subside as the body adjusts to the medication, it’s important for patients to report persistent or severe symptoms to their healthcare provider. In rare cases, more serious side effects may occur, requiring immediate medical attention.
Serious Side Effects to Watch For
What are the serious side effects that require immediate medical intervention?
- Fast or irregular heartbeat
- Severe confusion or hallucinations
- High fever
- Allergic reactions (rash, itching, swelling)
- Severe constipation or abdominal pain
Patients experiencing any of these symptoms should seek medical help promptly. While rare, these severe reactions can be indicative of more serious underlying issues that need to be addressed.
Precautions and Contraindications for Trihexyphenidyl Use
Before starting trihexyphenidyl, patients should be aware of certain precautions and potential contraindications. What factors should be considered?
- Allergies to trihexyphenidyl or its components
- Pre-existing medical conditions such as glaucoma, urinary problems, or heart disease
- Pregnancy and breastfeeding considerations
- Interactions with other medications, particularly tranquilizers
It’s crucial for patients to provide a comprehensive medical history to their healthcare provider before starting trihexyphenidyl. This includes information about all current medications, supplements, and herbal products, as well as any known allergies or medical conditions.
Special Precautions for Older Adults
Are there specific considerations for elderly patients taking trihexyphenidyl?
- Increased sensitivity to side effects in older adults
- Higher risk of cognitive impairment and confusion
- Potential for increased fall risk due to dizziness or blurred vision
Healthcare providers often exercise caution when prescribing trihexyphenidyl to older adults, carefully weighing the potential benefits against the risks. In many cases, alternative medications may be considered for this population.
Drug Interactions and Dietary Considerations
Understanding potential drug interactions is crucial for safe and effective use of trihexyphenidyl. What types of interactions should patients and healthcare providers be aware of?
- Increased anticholinergic effects when combined with other anticholinergic drugs
- Potential interactions with certain antipsychotics and antidepressants
- Possible effects on the absorption of other medications
Patients should always inform their healthcare provider about all medications they are taking, including over-the-counter drugs and supplements. This allows for a comprehensive assessment of potential interactions and appropriate adjustments to the treatment plan.
Dietary Considerations
Are there any specific dietary restrictions or recommendations for patients taking trihexyphenidyl?
- No specific dietary restrictions are typically required
- Maintaining adequate hydration is important, especially if experiencing dry mouth
- Alcohol consumption should be discussed with a healthcare provider
While trihexyphenidyl doesn’t have strict dietary requirements, patients should be mindful of their overall health and discuss any significant dietary changes with their healthcare provider.
Proper Storage and Disposal of Trihexyphenidyl
Proper storage and disposal of trihexyphenidyl are important for both safety and efficacy. How should this medication be handled?
- Store at room temperature, away from excessive heat and moisture
- Keep out of reach of children in a tightly closed container
- Dispose of unused medication through proper channels, such as drug take-back programs
Patients should never share their medication with others, even if they have similar symptoms. Proper storage not only ensures the medication’s effectiveness but also prevents accidental ingestion by children or pets.
Safe Disposal Methods
What are the recommended methods for safely disposing of unused trihexyphenidyl?
- Participate in community drug take-back programs
- Use FDA-approved in-home disposal methods if take-back options are unavailable
- Follow specific disposal instructions provided by a healthcare provider or pharmacist
Proper disposal of medications helps prevent environmental contamination and reduces the risk of accidental ingestion or misuse.
Monitoring and Follow-up Care for Trihexyphenidyl Users
Regular monitoring and follow-up care are essential components of trihexyphenidyl therapy. What should patients expect in terms of ongoing care?
- Regular check-ups to assess medication effectiveness and side effects
- Potential adjustments to dosage based on response and tolerability
- Monitoring for long-term effects on cognitive function and physical health
Patients should maintain open communication with their healthcare provider, reporting any changes in symptoms or new side effects promptly. This collaborative approach ensures that the treatment plan remains optimized for each individual’s needs.
Long-term Considerations
What long-term considerations should patients and healthcare providers keep in mind with trihexyphenidyl use?
- Potential for developing tolerance over time
- Need for periodic reassessment of the medication’s benefits versus risks
- Monitoring for potential cognitive impacts, especially in older adults
Long-term use of trihexyphenidyl requires ongoing evaluation to ensure that the benefits continue to outweigh any potential risks or side effects. Healthcare providers may periodically reassess the need for the medication or consider alternative treatment options as part of a comprehensive care plan.
In conclusion, trihexyphenidyl is a valuable medication in the management of Parkinson’s disease and certain medication-induced movement disorders. While it can provide significant symptom relief, its use requires careful consideration of potential side effects, drug interactions, and individual patient factors. By following proper dosing guidelines, maintaining regular communication with healthcare providers, and adhering to recommended precautions, patients can maximize the benefits of trihexyphenidyl while minimizing potential risks. As with any medication, individualized care and ongoing monitoring are key to ensuring optimal outcomes in trihexyphenidyl therapy.
Trihexyphenidyl: MedlinePlus Drug Information
pronounced as (trye hex ee fen’ i dil)
To use the sharing features on this page, please enable JavaScript.
Trihexyphenidyl is used along with other medications to treat the symptoms of Parkinson’s disease (PD; a disorder of the nervous system that causes difficulties with movement, muscle control, and balance) and to control extrapyramidal symptoms (tremor, slurred speech) caused by certain medications. Trihexyphenidyl is in a class of medications called antimuscarinics. It works by relaxing muscles and nerve impulses that control the function of muscles.
Trihexyphenidyl comes as a tablet and elixir (liquid) to take by mouth. It usually is taken with or without food three or four times a day. Take trihexyphenidyl at around the same time(s) every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take trihexyphenidyl exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Do not stop taking trihexyphenidyl suddenly without talking with your doctor, especially if you are also taking other medications. Sudden stoppage can cause symptoms of Parkinson’s disease to return.
This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.
Before taking trihexyphenidyl,
- tell your doctor and pharmacist if you are allergic to trihexyphenidyl, any other medications, or any of the ingredients in trihexyphenidyl preparation. Ask your doctor or pharmacist or check the package label for a list of the ingredients.
- tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: tranquilizers.
- tell your doctor if you have or have ever had glaucoma, high blood pressure, problems with your urinary system or prostate, stomach problems, or heart, kidney, or liver disease.
- tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while taking trihexyphenidyl, call your doctor.
- if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking trihexyphenidyl.
- talk to your doctor about the risks and benefits of taking trihexyphenidyl if you are 65 years of age or older. Older adults should not usually take trihexyphenidyl because it is not as safe or effective as other medications that can be used to treat the same condition.
Unless your doctor tells you otherwise, continue your normal diet.
Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
Trihexyphenidyl may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
- dizziness or blurred vision
- dry mouth
- upset stomach
- vomiting
- constipation
- headache
- difficulty urinating
Some side effects can be serious. If you experience any of the following symptoms, call your doctor immediately:
- rash
- fast, irregular, or pounding heartbeat
- fever
- confusion
- delusions or hallucinations
Trihexyphenidyl may cause other side effects. Call your doctor if you have any unusual problems while you are taking this medication.
If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).
Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom).
It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org
Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.
In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.
- Artane®¶
- Tremin®¶
¶ This branded product is no longer on the market. Generic alternatives may be available.
Last Revised – 07/15/2018
Browse Drugs and Medicines
Trihexyphenidyl Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing
Uses
Trihexyphenidyl is used to treat symptoms of Parkinson’s disease or involuntary movements due to the side effects of certain psychiatric drugs (antipsychotics such as chlorpromazine/haloperidol). Trihexyphenidyl belongs to a class of medication called anticholinergics that work by blocking a certain natural substance (acetylcholine). This helps decrease muscle stiffness, sweating, and the production of saliva, and helps improve walking ability in people with Parkinson’s disease.Anticholinergics can stop severe muscle spasms of the back, neck, and eyes that are sometimes caused by psychiatric drugs. It can also decrease other side effects such as muscle stiffness/rigidity (extrapyramidal signs-EPS). It is not helpful in treating movement problems caused by tardive dyskinesia and may worsen them.
How to use Trihexyphenidyl HCL
Take this medication by mouth as directed by your doctor, usually 3 to 4 times a day with meals and at bedtime. Your doctor may start you at a low dose and increase your dose slowly to find the best dose for you. The dosage is based on your medical condition, age, and response to therapy.
If you are using the liquid form of this medication, measure your dose with a special measuring spoon or device. Do not use a household spoon because it may not provide the correct dose.
Take this medication regularly in order to get the most benefit from it. To help you remember, take it at the same times each day.
Take this medication at least 1 hour before antacids containing magnesium, aluminum, or calcium. Allow at least 1-2 hours between doses of trihexyphenidyl and certain drugs for diarrhea (adsorbent antidiarrheals such as kaolin, pectin, attapulgite). Take this medication at least 2 hours after ketoconazole. Antacids and some drugs for diarrhea may prevent the full absorption of trihexyphenidyl, and this product may prevent the complete absorption of ketoconazole when these products are taken together.
If you are taking this medication for side effects from another medication, your doctor may instruct you to take it on a regular schedule or only as needed. If you are taking this medication for Parkinson’s disease, your doctor may change the dose of your other medications (such as levodopa). Follow your doctor’s instructions closely.
Though it helps many people, this medication may sometimes cause addiction. This risk may be higher if you have a substance use disorder (such as overuse of or addiction to drugs/alcohol). Do not increase your dose, take it more often, or use it for a longer time than prescribed. Properly stop the medication when so directed. Some conditions may become worse when the drug is suddenly stopped. Your dose may need to be gradually decreased.
When used for an extended period, this medication may not work as well and may require different dosing. Talk with your doctor if this medication stops working well. Inform your doctor if your condition lasts or gets worse.
Side Effects
Drowsiness, dizziness, constipation, flushing, nausea, nervousness, blurred vision, or dry mouth may occur. These effects usually lessen as your body gets used to the medicine. If any of these effects last or get worse, contact your doctor or pharmacist promptly.
To relieve dry mouth, suck on (sugarless) hard candy or ice chips, chew (sugarless) gum, drink water, or use a saliva substitute.
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: decreased sexual ability, severe stomach/abdominal pain, difficult/painful swallowing, difficulty urinating, weakness.
Get medical help right away if you have any very serious side effects, including: chest pain, severe dizziness/fainting, high fever, fast/irregular/slow heartbeat, mental/mood changes (such as confusion, hallucinations, memory problems), eye pain/swelling/redness, vision changes (such as seeing rainbows around lights at night).
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 trihexyphenidyl, 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: glaucoma, breathing problems (such as asthma, emphysema), diarrhea caused by an infection, heart problems (such as angina, heart attack, heart failure, fast/irregular heartbeat), high/low blood pressure, stomach/intestinal problems (such as chronic constipation, ileus, blockage, ulcerative colitis, acid reflux, ulcer), kidney disease, liver disease, mental/mood problems (such as anxiety, dementia, psychosis), certain muscle disease (myasthenia gravis), certain nerve disease (autonomic neuropathy), seizure, stroke, overactive thyroid (hyperthyroidism), problems urinating (such as due to enlarged prostate, neurogenic bladder), personal or family history of a substance use disorder (such as overuse of or addiction to drugs/alcohol).
This drug may make you dizzy or drowsy or blur your vision. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness or clear vision until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).
To minimize dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.
This medication decreases saliva production, an effect that can increase gum and tooth problems (such as cavities, gum disease). Take special care with your dental hygiene (such as brushing, flossing) and have regular dental check-ups.
Liquid forms of this product may contain alcohol. Caution is advised if you have diabetes, alcohol dependence, or liver disease. Some medications (such as disulfiram, metronidazole) may cause a serious reaction when combined with alcohol. Tell your doctor if you are taking any medication that should not be used with alcohol. Ask your doctor or pharmacist about using this product safely.
This drug can cause decreased sweating, which could cause a severe rise in your body temperature (hyperthermia). The risk of this serious side effect is greater in hot weather, during vigorous exercise, and/or if you drink alcohol. Drink plenty of fluids and dress lightly while in hot weather and when exercising. If you experience signs of hyperthermia such as mental/mood changes, headache, or dizziness, promptly seek cool or air-conditioned shelter and/or stop exercising, and get medical help right away. Consult your doctor for more details.
Older adults may be more sensitive to the side effects of this drug, especially dizziness, drowsiness, heatstroke, memory problems, difficulty urinating, and constipation. Dizziness and drowsiness can increase the risk of falling.
Children may be more sensitive to the side effects of this drug, especially the effects on heart rate.
During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.
It is not known if this drug passes into breast milk. 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 are: pramlintide, corticosteroids (such as prednisone), potassium tablets/capsules.
Tell your doctor or pharmacist if you are taking other products that cause drowsiness such as opioid pain or cough relievers (such as codeine, hydrocodone), alcohol, marijuana (cannabis), drugs for sleep or anxiety (such as alprazolam, lorazepam, zolpidem), muscle relaxants (such as carisoprodol, cyclobenzaprine), or antihistamines (such as cetirizine, diphenhydramine).
Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.
Does Trihexyphenidyl HCL 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. Symptoms of overdose may include: unusually fast/slow heartbeat, slow/shallow breathing, unconsciousness, seizures, loss of coordination, fever, hot/dry/flushed skin, widened pupils, change in vision, change in the amount of urine, confusion, hallucinations.
Do not share this medication with others.
Lab and/or medical tests (such as eye exams) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.
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
trihexyphenidyl 2 mg tablet
Color: whiteShape: roundImprint: 212 N
This medicine is a white, round, scored, tablet imprinted with “212 N”.
trihexyphenidyl 5 mg tablet
Color: whiteShape: roundImprint: 211 N
This medicine is a white, round, scored, tablet imprinted with “212 N”.
trihexyphenidyl 5 mg tablet
Color: whiteShape: roundImprint: N T 5
This medicine is a white, round, scored, tablet imprinted with “212 N”.
trihexyphenidyl 2 mg tablet
Color: whiteShape: roundImprint: N T 2
This medicine is a white, round, scored, tablet imprinted with “212 N”.
trihexyphenidyl 0.4 mg/mL oral elixir
Color: colorlessShape: Imprint:
This medicine is a white, round, scored, tablet imprinted with “212 N”.
trihexyphenidyl 2 mg tablet
Color: whiteShape: roundImprint: DAN DAN 5335
This medicine is a white, round, scored, tablet imprinted with “212 N”.
trihexyphenidyl 5 mg tablet
Color: whiteShape: roundImprint: DAN DAN 5337
This medicine is a white, round, scored, tablet imprinted with “212 N”.
trihexyphenidyl 0.4 mg/mL oral elixir
Color: colorlessShape: Imprint:
This medicine is a white, round, scored, tablet imprinted with “212 N”.
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 Trihexyphenidyl HCL?
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.
Tamoxifen – description of the substance, pharmacology, use, contraindications, formula
Contents
Structural formula
Russian name
English title
Latin name
chemical name
Gross formula
Pharmacological group of the substance Tamoxifen
Nosological classification
CAS code
pharmachologic effect
Characteristic
Pharmacology
The use of the substance Tamoxifen
Contraindications
Application restrictions
Use during pregnancy and lactation
Side effects of Tamoxifen
Interaction
Dosage and administration
Precautionary measures
Trade names with the active substance Tamoxifen
Structural formula
Russian name
Tamoxifen
English name
Tamoxifen
Latin name
Tamoxifenum ( born 90 062 Tamoxifeni)
Chemical name
(Z)-2-[4-(1, 2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethanamine (as citrate)
Gross formula
C 26 H 29 NO
Pharmacological group of substance Tamoxifen
Estrogens, gestagens; their homologues and antagonists
Anticancer hormonal agents and hormone antagonists
Nosological classification
ICD-10 code list
C50 Malignant neoplasms of the mammary gland
C54. 1 Endometrium
CAS code
10540-29-1
Pharmacological action
Pharmacological action –
antiestrogen , anticancer .
Description
Antitumor agent (antiestrogen). Tamoxifen citrate is a white, odorless crystalline powder. Very slightly soluble in water (1:5000), easily hot (1:2), soluble in ethanol, methanol, acetone. Hygroscopic at high humidity, sensitive to ultraviolet. Molecular weight 563.65.
Pharmacology
Competitively binds to estrogen receptors in target organs, like estrogens it translocates together with the receptor into the nucleus of the tumor cell and thus blocks the action of estrogens.
Well absorbed from the gastrointestinal tract, T max – 4-7 hours, the time to reach C ss – 3-4 weeks. Plasma protein binding – 99%. Metabolized in the liver by hydroxylation and demethylation. The main metabolite, N-desmethyl-tamoxifen, has activity similar to that of tamoxifen. The excretion is biphasic with an initial T 1/2 – 7-14 hours followed by slow terminal T 1/2 – 7 days. It is excreted mainly through the intestines, mainly in the form of metabolites, a small amount – by the kidneys.
Application of the substance Tamoxifen
Breast cancer: especially in menopausal women, in men after castration, carcinoma in situ breast duct; adjuvant therapy for breast cancer. estrogen-sensitive tumors; endometrial cancer.
Contraindications
Hypersensitivity, pregnancy, lactation.
Restrictions on use
History of deep vein thrombosis and pulmonary embolism during treatment with indirect coumarin anticoagulants, thrombocytopenia, leukopenia, hypercalcemia, hyperlipidemia, cataracts or visual impairment.
Use in pregnancy and lactation
Contraindicated in pregnancy (pregnancy must be excluded before starting treatment).
FDA fetal category D.
Stop breastfeeding for the duration of treatment (it is not known if tamoxifen passes into breast milk).
Side effects of substance Tamoxifen
From the side of the nervous system and sensory organs: headache, dizziness, fatigue, depression, confusion, visual impairment, corneal changes, cataracts and retinopathy.
From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): thrombophlebitis, thromboembolism, transient leukopenia, thrombocytopenia.
From the digestive tract: abdominal pain, nausea, vomiting, loss of appetite, constipation, increased levels of liver enzymes, severe liver dysfunction (cholestasis, hepatitis).
From the genitourinary system: bleeding or vaginal discharge, amenorrhea or irregularity of the onset of menstruation in patients in the premenopausal period, the occurrence of a reversible cystic ovarian tumor, fluid retention, itching in the genital area.
Allergic reactions: skin rash.
Others: alopecia, pain in the lesion and / or in the bones, an increase in the size of soft tissue formations (accompanied by severe erythema of the affected areas and adjacent areas), hypercalcemia, paroxysmal sensation of heat, fever; with prolonged use – cases of changes in the endometrium, including hyperplasia, polyps, intrauterine fibroma and, in isolated cases, endometrial cancer.
Interactions
When combined with cytostatics, the risk of thrombosis increases. Estrogens may reduce the therapeutic effect of tamoxifen. Can be used in combination with progestins. Potentiates the effect of indirect anticoagulants.
Dosage and administration
Inside. Dosing regimen is set individually depending on the indications. For breast cancer – 20-40 mg 1-2 times a day, endometrial cancer – 20-30 mg 1-2 times a day. The highest daily dose is 40 mg. Treatment is carried out for a long time (until signs of regression of the process appear).
Precautions
Before starting treatment, women should undergo a thorough gynecological examination. Tamoxifen causes ovulation, which increases the risk of pregnancy, so women of reproductive age should use reliable methods of contraception (non-hormonal) during treatment and for 3 months after the end of treatment.
The drug should be discontinued if there is bloody discharge from the vagina or vaginal bleeding, signs of thrombosis of the veins of the lower extremities (pain in the legs or their swelling), thromboembolism of the branches of the pulmonary artery (shortness of breath).
In the course of treatment, it is necessary to monitor blood coagulation parameters, blood counts (leukocytes, platelets), liver function parameters. An ophthalmological examination is recommended prior to and periodically during treatment.
In patients with bone metastases, serum calcium should be measured periodically during the initial period of treatment (in case of severe hypercalcemia, tamoxifen should be temporarily discontinued). In patients with hyperlipidemia during treatment, it is necessary to control the concentration of cholesterol and TG in the blood serum.
Ineffective in the treatment of patients with metastases (especially in the liver).
Trade names with active substance Tamoxifen
Reset filters
Lek. form
All lek. forms substance-powder tablets tablets, film-coated tablets
Dosage
All dosages 10 mg 20 mg 30 mg 40 mg No dosage
Manufacturer
All manufacturers Valenta Pharmaceutical JSC (Valenta Pharm JSC) Valenta Pharmaceutical JSC Veropharm JSC Veropharm JSC Chemische Fabrik Werg GmbH Obolenskoe is a pharmaceutical company JSC Obolenskoe is a pharmaceutical company CJSC Ozon LLC Orion Corporation Salutas Pharma GmbH Pharmasyntez-Nord JSC Shreya Life Sciences Pvt. Ltd. Yantze River Pharmaceutical (Group) Co. Yantze River Pharmaceutical Group Co., Ltd. Jiangsu Haiqi Biological Pharmaceutical Co. Ltd.
Information for healthcare professionals only.
Are you a healthcare professional?
Analogues, side effects, for which
is prescribed CONTRAINDICATIONS. POSSIBLE SIDE EFFECTS. A SPECIALIST’S CONSULTATION IS REQUIRED.
Author of the article
Sumenkova Anna Mikhailovna,
pharmacist
All authors
Contents of the article
- Tamoxifen: side effects
- How to take Tamoxifen: before or after meals
- Tamoxifen alternatives
- Tamoxifen or Anastrozole
- Abstract
- Ask an expert about the article
According to the World Health Organization, breast cancer is the most common cancer. It occurs in women of any age after reaching puberty. The chance of getting breast cancer increases with age.
WHO says that in the period 1930-1970s mortality from this disease was at the same level. And only since the 1980s, survival rates began to increase due to the introduction of programs for the early diagnosis of this type of cancer, an integrated approach to treatment, and the discovery of new drugs.
Tamoxifen is included in the Clinical Guidelines of the Russian Ministry of Health for the treatment of breast cancer (BC). We answer the most frequently asked questions about its use. Compare with the drug Anastrozole, which is also prescribed in the complex therapy of breast cancer.
All products Tamoxifen
24 reviews
Tamoxifen: side effects
The antitumor effect of Tamoxifen is associated with its antiestrogenic action. The main female sex hormone, estrogen, stimulates the growth and division of breast tumor cells. Tamoxifen blocks estrogen-sensitive cell receptors and stops their reproduction.
Tamoxifen is an adjuvant (additional) therapy. It is prescribed in combination with surgical treatment and radiation therapy. In this case, it improves the survival of patients with early breast cancer.
Tamoxifen is prescribed for the long term: 2 to 10 years. With this regimen, side effects often occur. Most of them are related to the anti-estrogen action of the drug:
- hot flushes, hot flashes
- vaginal discharge and bleeding
- itching in the genital area
- alopecia
- chest pain
- weight gain
- bone pain
- Other most common adverse reactions:
- fluid retention
- anorexia
- nausea, vomiting, constipation
- fatigue, drowsiness, depression
- dizziness, headache
- leg cramps
- allergic reactions
- visual disturbances, cataracts
- thrombosis, thromboembolism
Long-term therapy with Tamoxifen may cause endometrial hyperplasia, polyps, uterine fibroids.
How to take Tamoxifen before or after meals
The instruction does not contain clear instructions on the sequence of taking the drug with food. Food does not affect its effectiveness. Tamoxifen tablets are taken both before and after meals, without chewing and with a small amount of water.
If the doctor has prescribed a single dose, then Tamoxifen is taken in the morning, if twice a day, then in the morning and in the evening. The standard daily dose is 20 mg, the maximum daily dose is 40 mg.
Tamoxifen: analogues
Under the name Tamoxifen, the drug is produced by several companies: Orion (Finland), Ozone Medica (Russia), PO FP Obolenskoye (Russia), Novosibkhimfarm (Russia), Shreya Life Science (India). Also in Russia, the following drugs with the active substance tamoxifen are registered:
- Sinfen (Pharmasintez-Nord, Russia)
- Vero-tamoxifen (Veropharm, Russia)
- Tamoxifen Geksal (Sandoz, Slovenia)
These analogues are interchangeable provided that the dosage is observed.
Tamoxifen or Anastrozole
Clinical guidelines for the treatment of breast cancer include the drug Anastrozole. Which one to prescribe is decided by the attending physician, because Anastrozole has a different mechanism of action.
In women, estrogen can still be synthesized in the body from androgens, which are produced by the kidneys and adrenal glands. The transformation process takes place under the influence of the aromatase enzyme. Anastrozole is an inhibitor of this enzyme and blocks the conversion of androgens to estrogens. If a woman’s ovarian function is turned off (menopause, removal of the ovaries), then the drug completely suppresses her estrogen synthesis.
Anastrozole is contraindicated in patients with preserved ovarian function (they continue to produce estrogen) and is prescribed only for the treatment of breast cancer in postmenopausal women.
Tamoxifen has a wider range of applications: it is used regardless of ovarian function. In addition, it is also indicated for the treatment of men in case of breast cancer after castration and prostate cancer in case of ineffectiveness of other drugs.
Tamoxifen is more likely to have endometrial complications and thromboembolism, while Anastrozole is more likely to have cardiovascular complications and osteoporosis.
Concomitant use of Tamoxifen and Anastrozole is contraindicated. Clinical guidelines contain sequential treatment regimens with these drugs. For example, for patients who have reached persistent menopause by the time they stop taking tamoxifen, Tamoxifen is first prescribed for 2-3 years, then Anastrozole for 2-3 years (a total of therapy lasts 5 years).
Summary
- Tamoxifen is an antineoplastic agent with antiestrogen action.
- Taking the drug in the complex therapy of breast cancer in the early stages allows a complete cure or long-term remission.
- Tamoxifen is taken from 2 to 10 years.