Main Information
- Drug : Tamoxifen Citrate
- What is : A selective estrogen receptor modulator (SERM), wich inhibits the estrogen in mammary tissue
- Concentrarion : 10mg / capsule
- Package : 90 capsules flask
- Excipients : Cellulose Microcrystalline, Magnesium Stearate
- Aspect : White / Blue capsule
- Pharmaceutical form : Capsule
- Administrarion : Oral
Synonyms
- Novaldex
- Nolgen
- Farmifeno
- Tamax
Descripition
Flask containing 90 capsules of Tamoxifen Citrate (10mg each), cellulose microcirstaline as filler and magnesium stearate as a lubricant.
Tamoxifen citrate is a type of antiestrogen. The citrate salt of an antineoplastic nonsteroidal selective estrogen receptor modulator (SERM). Tamoxifen competitively inhibits the binding of estradiol to estrogen receptors, thereby preventing the receptor from binding to the estrogen-response element on DNA. The result is a reduction in DNA synthesis and cellular response to estrogen. In addition, tamoxifen up-regulates the production of transforming growth factor B (TGFb), a factor that inhibits tumor cell growth, and down-regulates insulin-like growth factor 1 (IGF-1), a factor that stimulates breast cancer cell growth. Tamoxifen also down-regulates protein kinase C (PKC) expression in a dose-dependant manner, inhibiting signal transduction and producing an antiproliferative effect in tumors such as malignant glioma and other cancers that overexpress PKC.
Indications
Tamoxifen Citrate is a drug used to treat certain types of breast cancer in women and men. It is also used to prevent breast cancer in women who have had ductal carcinoma in situ (abnormal cells in the ducts of the breast) and in women who are at a high risk of developing breast cancer. Tamoxifen citrate is also being studied in the treatment of other types of cancer. It blocks the effects of the hormone estrogen in the breast.
Contraindications
Do not take Tamoxifen Citrate if:
- you are allergic to tamoxifen or any of the other ingredients
- you are pregnant or think you might be pregnant
- you are breastfeeding
- you are taking anastrozole
- you are taking any treatment for infertility
- you or someone in your family have had blood clots with unknown causes
- you have an illness which that increases the risk of blood clots
Drug Interactions
- Antidepressants (e.g. paroxetine, fluoxetine)
- Bupropion (used as an antidepressant or aid to smoking cessation)
- Quinidine (for example used in the treatment of cardiac arrhythmia)
- Cincalet/cinacalcet (for treatment of disorders of the parathyroid gland)
- Blood thinning medicines such as warfarin. These are known as 'anti-coagulants'
- Rifampicin which is used for tuberculosis
- Other 'aromatase inhibitors' including anastrozole, letrozole and exemestane
Dosage
The recommended dose for breast cancer is one 20 mg tablet daily.
The dose for infertility depends on your periods (menstrual cycle).
If you are having regular periods, the recommended dose is one 20 mg tablet daily on the
2nd, 3rd, 4th and 5th days of your period.
If this does not work, your doctor may suggest that you take a higher dose of Nolvadex
during your next period. If this happens, the usual dose is 40 mg or 80 mg daily on the 2nd,
3rd, 4th and 5th days of your period.
If you are not having regular periods, you can start taking the tablets on any day of the
month.
If you take more Tamoxifen Citrate than you should, talk to a doctor or pharmacist straight away.
Adverse Reactions
Like all medicines, Tamoxifen Citrate can cause adverse reactions or side effects, although not everybody gets them.
Stop taking Tamoxifene Citrate and tell your doctor straight away if you notice any of the following side effects:
- Symptoms of a blood clot : swelling of the calf or leg, chest pain, being short of breath, suddenly weakness.
- Symptoms of a stroke : These include sudden onset of the following: weakness or paralysis of the arms or legs, being unable to move the arms or legs, sudden difficulty speaking, walking, or holding things, or difficulty thinking. These symptoms are
caused by a reduced blood supply in the brain.
- Difficulty in breathing
- Swelling of the face, lips, tongue or throat which may make it difficult to swallow.
The following symptoms are uncommon but may happen:
- Allergic reactions
- Anaemia
- Changes in blood tests of liver function
- Changes in the womb (including changes to its lining and benign growths)
- Constipation
- Diarrhoea
- Feeling light-headed
- Fluid retention
- Formation of fatty liver cells
- Headache
- Hot flushes
- Itching of the genitals
- Leg cramp
- Menstrual irregularities
- Muscle pain
- Nausea
- Rash
- Sensory changes like: taste disorder, numbness or tingling in the skin
- Stomachache
- Thinning of the hair
- Tiredness
- Unusual bleeding from your vagina
- Visual disturbances
- Vomiting
Storage
Tamox 10 should be stored at 20° to 25°C (68° to 77°F).
History
Tamoxifen Citrate is a Selective Estrogen Receptor Modulator (SERM) that was created in 1961 by ICI now known as AstraZenaca. There are numerous brands including generic forms of Tamoxifen Citrate on the market, but Nolvadex is the most well known. Often referred to as an anti-estrogen, Tamoxifen Citrate is actually both an antagonist and agonist. This means it will act as an anti-estrogen in certain areas of the body while acting as an estrogen in other areas.
Tamoxifen Citrate has been used medically for decades and has been highly successful in breast cancer treatment, specifically hormone-responsive breast cancer. It is also a medication that is used by many anabolic steroid users, but it is not a steroid. This is a drug steroid users will sometimes use during steroid use to help with estrogenic related side effects brought on by specific steroids. However, it is most commonly used during Post Cycle Therapy (PCT). PCT is the 3-6 week period following steroid use that is implemented in order to help with natural testosterone production that is suppressed during anabolic steroid use.
Functions
Tamoxifen Citrate is a SERM that acts as both antagonist and agonist in relation to the estrogen hormone. It is an anti-estrogen in that it binds to estrogen receptors in certain parts of the body, particularly in the mammary tissue. This action prevents estrogen from acting on its originally intended point of binding. This makes Tamoxifen Citrate valuable to breast cancer patients as breast cancer feeds off of estrogen. And it's valuable to steroid users as increased estrogen levels can bind to the mammary tissue and lead to gynecomastia.
The relationship Tamoxifen Citrate has in being an anti-estrogen is fairly straightforward and well understood by many, but it's its relationship to being an estrogen in other areas that's surprising to some. Tamoxifen Citrate acts as an estrogen on the liver. Liver related estrogenic activity has been shown to improve cardiovascular health, particularly as it relates to cholesterol. This can be very advantageous for the bodybuilding steroid user as most steroids have a negative impact on cholesterol levels.
Beyond its estrogen related activity Tamoxifen Citrate possesses strong testosterone stimulating properties. The use of Tamoxifen Citrate will stimulate the pituitary to increase its production of Luteinizing Hormone (LH) and Follicle Stimulating Hormone (FSH) with a strong emphasis on LH. LH and FSH are the gonadotropins that signal to the testicles to produce testosterone. Without LH and FSH there is no testosterone production.
Effects
For the anabolic steroid user the positive effects of Tamoxifen Citrate can be seen both during and post anabolic steroid use with post use being primary. Anabolic steroids like Testosterone and Nandrolone among others will increase the body's serum estrogen levels. This occurs by the testosterone hormone converting to testosterone, which happens due to it being metabolized by the aromatase enzyme. Once aromatized you have more estrogen, and this can lead to gynecomastia and water retention. It can also lead to high blood pressure if water retention becomes severe. Tamoxifen Citrate does not lower serum estrogen levels, but it will bind to the receptors in the chest preventing the estrogen from binding. It will not do a lot for water retention if that is an issue. It is also not enough gynecomastia protection for all men, but that depends on how high estrogen levels go as well as genetics. If more or stronger protection is needed Aromatase Inhibitors (AI's) are recommended. AI's are anti-estrogens that inhibit aromatase activity and lower serum estrogen levels.
We then have the testosterone stimulating effects of Tamoxifen Citrate. This is by far the most important effect for the anabolic steroid user. When we use anabolic steroids we suppress our natural testosterone production, and this will occur regardless of the steroids used. Steroid use creates a negative feedback and tells your pituitary to stop making LH and FSH. This is why almost all steroid cycles include exogenous testosterone so that the negative feedback doesn't cause a low testosterone level. Once steroid use is complete something is then needed to jump start testosterone production. It will occur on its own, but it will be slow and Tamoxifen can both speed it up and make it more efficient. Tamoxifen Citrate is introduced, LH and FSH levels go up and as a result testosterone is produced.
Important Note: PCT use that includes Tamoxifen Citrate or any SERM, for it to be successful this assumes no prior low testosterone condition existed. It also assumes no damage was done to the Hypothalamic-Pituitary-Testicular-Axis (HPTA) during use. If prior low levels existed Tamoxifen Citrate won't magically fix this. If severe damage was done to the HPTA you will not recover and may be in need of low testosterone treatment.
Important Note: Many steroid users believe that a good PCT brings about full recovery, but this is a false belief. A PCT that includes Tamoxifen Citrate will stimulate recovery, but it will not end it. It will still take several months for full recovery to occur, but it stands a much better chance with PCT than without.
For the breast cancer patient the effects of Tamoxifen Citrate are perhaps even more straightforward than they are for the anabolic steroid user. Estrogen attaches and feeds the cancer, but Tamoxifen Citrate prevents it from attaching and starves the cancer. This is a simple yet effective means of treatment. This is not the only drug used in treatment; commonly treatment will begin with an AI and then will be switched to a SERM like Tamoxifen Citrate. It is also sometimes used as a preventative measure in those that have a strong family history of breast cancer.
Side Effects
Possible side effects of Tamoxifen Citrate do exist, but it is one of the more well-tolerated SERM's on the market. Most men will not have an issue with this medication, although it is possible. Side effects of Tamoxifen Citrate do appear to be more common in women, but they are still not what we'd call "common." The most common side effects of Tamoxifen Citrate include:
- Vaginal Itching, bleeding, discharge or discomfort
- Hot Flashes
- Upset Stomach
- Headaches
The above side effects of Tamoxifen Citrate are not extremely common but possible. Other possible side effects of the SERM's use but less common than the above include:
- Rash
- Decreased White Blood Cell Count
- Endometrial Changes
- Increased Triglyceride Levels
- Pulmonary Embolism
Important Note: Women who are pregnant or who may become pregnant should not use Tamoxifen Citrate or any SERM as use will potentially damage the developing child and with strong probability.
Administration
For the purpose of breast cancer treatment there are six Tamoxifen Citrate plans that encompass both male and female treatment. In any of the six plans doses normally fall in the 10-20mg twice per day range. A full 40mg per day (20mg twice per day) is very common during the first stage of Tamoxifen Citrate treatment. Many breast cancer patients will also continue 10-20mg per day indefinitely once the cancer is in remission in order to prevent it from coming back.
We then have the anabolic steroid user. For on cycle gynecomastia prevention 10-20mg per day is the standard range. If this dosing range does not help it is unlikely any dose will and AI's should strongly be considered. Some men are afraid to use AI's because they fear they might hinder their gains. It's true you will hold less water therefore weigh less, but water is not an actual gain. Besides, would you rather weigh just a little less or have massive and unattractive gynecomastia?
We're then left with PCT use. Most PCT plans will begin with Tamoxifen Citrate doses of 40mg per day and will continue at this dose for 2-3 weeks. The dose will then be reduced to 20mg per day and will continue at this dose for 2-3 weeks. For a proper PCT it will often include another SERM Clomiphene Citrate (Clomid). For a full PCT outline please see How to Come off Steroids.
Reviews
Of all the SERM's on the market, and there are quite a few, Tamoxifen Citrate is perhaps the most valuable and beneficial. For the breast cancer patient it can almost be labeled as an imperative medication; in fact, in many cases we can call it life saving or at least a major part of an overall life saving plan. For the steroid user, it's really not the best thing since sliced bread when it comes to on cycle use, but it can serve a p urpose for some. It is during PCT that the steroid user will find this product highly valuable. In fact, if the Nolvadex and Clomid combo cannot be used and you could only pick one SERM for your PCT recovery, undoubtedly Tamoxifen Citrate would be the way to go.
