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Feminization Regimen
A gender reassignment program for male to female transsexuals normally includes reducing androgen effects with spironolactone (cyproterone has been used in European countries) and stimulating feminization of secondary sex characteristics with estrogen.
There can be risks attached to hormone therapy in both men and women and therefore it is definitely inadvisable to take any form of hormone product unless it is medically prescribed.
The use of progesterone to augment breast development is controversial in physicians treating MTF transsexuals. When deciding on a hormone regimen, prescribers should remember that it is estrogen that causes the serious side effects, so the lowest effective dose should be used.
The manufacturers of oestrogen and progesterone products specify them for medical use in females and do not acknowledge their use for transsexuals, so there is little clinical data available regarding this usage.
Apart from a summary provided below, two excellent sites for information on hormones and dosages are:
http://www.scribd.com/doc/56618709/transsexual-transgendered-guide-to-obtaining-and-using-transsexual-hormones-hormone-replacement-therapy-hrt
Estrogens
Estrogen dosing regimens for gender transition vary widely. Estrogen should be prescribed at the lowest possible effective doses to avoid the serious complications of high-dose estrogen therapy.
Current recommendations for estrogen dosing range from starting doses of 0.625 to 2.5 mg of conjugated estrogen.
Estrogen is the most important part of any feminizing regimen.
Some typically-used estrogen dosages for pre-operative transsexual women who have not had an orchiectomy (castration) are as follows:
Oral Estrogens
Conjugated estrogens such as Premarin® 5 mg daily.
Estradiol such as Progynova (Oestradiol Valerate) or Estrofem 4 mg daily.
Injectable Estrogen
Progynon Depot is an alternative form of Oestradiol Valerate and comes in an injectable form.
Transdermal Estrogen
Estradiol 0.1 mg patch, changed twice weekly. Transdermal patches uniformly contain estradiol as the active medication, produced in 0.05mg (50 mcg), 0.075mg (75 mcg) and 0.1 mg (100 mcg) concentrations, and are branded under a variety of names such as Estradot / Vivelle, Climara and Estraderm.
Transdermal estrogen causes less clotting tendency than oral estrogen, possibly important to some patients; but this is a very expensive product.
Estrogen Gels
If you do not wish to use estradiol patches, an option is estradiol gel applied daily to the skin. The gel is usually alcohol based and is absorbed through the skin. The medication imparted into the skin usually takes about 12 hours for absorption into the blood stream, which produces a similar continuous action like the patch. Gels have the advantage as the wearer is not burdened with wearing a patch and the potential irritation from the adhesive that holds the patch in place.
Gels roughly corresponds to the daily doses found in the 50 mcg and 100 mcg patches.
Sandrena is an Estradiol Gel which comes in 1 gram sachets.
Estrodose Gel is the same as Estrogel. It is a clear, odorless, hydro-alcoholic gel that provides for delivery of estradiol for estrogen replacement in a non-patch transdermal form.
Other Forms of Estrogen
(!SITE_NAME!) is able to provide three other forms of Estrogen these are Premarin Cream which is a conjugated Estrogen Cream and Ovestin which is a low dose Estriol Cream.
Aerodiol - Aerodiol nasal spray containing estradiol hemihydrate 150µg per spray has been launched by Servier Laboratories The product is licensed for replacement therapy for oestrogen deficiency symptoms in postmenopausal women.
Serious health risks of estrogen therapy include stroke, pulmonary embolism, myocardial infarction, and breast cancer.
Combination estrogen and progesterone
(!SITE_NAME!) is able to supply Kliogest and Kliovance / Activelle, a combination of oestradiol and norethisterone and is used to produce female hormones estrogen and progesterone.
Antiandrogens
Besides providing estrogen, a hormone regimen should also reduce testosterone to normal female levels. This usually requires adding an anti-androgen.
Spironolactone acts as an antiandrogen of testosterone to dihydrotestosterone. Spironolactone in doses of 200–400 mg per day allows the practitioner to decrease exogenous estrogen doses tophysiologic or “hormone replacement” levels while still obtaining desired effects of breast development, feminization of skin, and female fat distribution.
Spironolactone can usually be discontinued after sex reassignment surgery.
Androcur (Cyproterone acetate) is a powerful antiandrogen and progestagen used in Europe for transgendered patients. Its use is limited by interference with corticosteroid production, high cost, and side effect profile.
Cyproterone is a generic form of Androcur. It performs is exactly same way as Androcur but at a cheaper cost.
Finasteride is an antiandrogen that opposes the formation of DHT, but not of testosterone itself. Finasteride is present in Proscar in a 5mg dosage and in Propecia in a 1mg doasge.
Dutasteride is also an antiandrogen that opposes the formation of DHT, but not of testosterone itself.
There are several other antiandrogens which are used for other indications but have no reported data in the transgendered patient. Flutamide and Bicalutamide are nonsteroidal antiandrogens normally used in the management of Management of Prostate Cancer.
Progesterone
Progesterone is the third and optional component of the MTF regimen.
Medroxyprogesterone is available as Provera and Depo-Provera. Medroxyprogesterone is a weak antiandrogen, and testosterone suppression may be accomplished with lower doses of estrogen. Medroxyprogesterone is less androgenic than norethindrone and orgestrel.
Micronized Progesterone is advantageous because it has a more favorable side effect profile (anxiety and irritability) than medroxyprogesterone. It is also less androgenic when higher progesterone doses are needed, but is more costly. Micronized progesterone is available as Prometrium or in a generic form as Microgest.
Duphaston (Dydrogesterone) may be used as an alternative to medroxyprogesterone acetate. It is not metabolised into testosterone within the body, and is therefore free of the virilising effects which some patients experience ftom other progesterones. A typical pre-op (or early post-op) dose would be 20mg in two doses, reducing to a single dose of 10mg daily post-op.
Crinone is another medication available and contains the female hormone progesterone.
Cyproterone plus Estrogen
While Androcur is available in 50 mg tablets, sometimes Diane-35 is used when small doses are desired. Diane-35 is a contraceptive with anti-acne properties (due to the cyproterone contained), and is comprised of 2 mg of cyproterone acetate and 0.035 mg ethinyl estradiol. Diane-35 generics are available.
(!SITE_NAME!) can supply Diane 35 which is comprised of 2 mg of cyproterone acetate and 0.035 mg ethinyl estradiol.
A generic form of Diane 35 is also available, this is manufactured by Cipla and is known as Ginette 35.
Climen is also a combination of an Estrogen with Cyproterone. Climen is normally used in Hormone Replacement Therapy Calendar-pack containing 11 tablets of 2 mg estradiol-17-valerate each, plus 10 tablets of 2 mg estradiol-17-valerate and 1 mg cyproterone acetate each. Brandnames in other countries - Climene, Climen/Clisin.
Facial Hair Reduction
Eflora / Vaniqa Cream is used for the reduction of unwanted facial hair. Eflora / Vaniqa Cream does not remove hair, it slows the regrowth.
Antagonists
Anastrozole is a non-steroidal aromatase inhibitor that decreases the amount of estrogen the body makes.
Arimidex contains the active ingredient anastrozole to decrease the body's production of estrogen.
(!SITE_NAME!) are unable to provide advice on treatment regimes. However the following sites may be of some assistance.
Transsexual Women's Resources
TransGenderCare - An educational offering of the Tampa Gender Identity Program. Has useful features on hormones and medical care.
http://www.transgendercare.com
and another excellent site is
http://www.scribd.com/doc/56618709/transsexual-transgendered-guide-to-obtaining-and-using-transsexual-hormones-hormone-replacement-therapy-hrt
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IVAX Pharmaceuticals
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Cholesterol Lowering
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Probenecid-AFT 500mg
Probenecid-AFT general information
What is Probenecid-AFT used for?
Probenecid-AFT tablets 500mg are used to treat gout and gouty arthritis to relieve painful symptoms at all stages of the condition, also to prevent attacks of gout in people at risk of developing gout. Gout is caused by build up of uric acid in the blood (hyperuricaemia) and the deposition of uric acid crystals in the joints and tissues. Probenecid-AFT 500mg is also used to prevent hyperuricaemia which can be induced or aggravated by some diuretics that are used to treat oedema and hypertension. Probenecid-AFT tablets 500mg also have another use in increasing the effectiveness of penicillin antibiotics by prolonging the length of time the antibiotic remains in the blood before it is excreted into the urine.
How does Probenecid-AFT work?
Probenecid-AFT tablets 500mg contain probenecid, which is a uricosuric drug that promotes the excretion of uric acid in the urine and this reduces the concentration of uric acid in the blood. Probenecid-AFT acts on the tubules of the kidneys and blocks the reabsorption of uric acid by competing with the membrane transporter for uric acid and preventing its uptake. High concentrations of uric acid in the blood (hyperuricaemia) result in the formation of crystals which are deposited in the joints and tissues, causing the painful symptoms associated with gout. As the amount of uric acid in the blood is reduced existing crystals are dissolved and the formation of new crystals is limited. Probenecid-AFT tablets 500mg relieve joint pain caused by gout which allows greater mobility of the affected joint; they also help prevent further joint destruction due to deposition of more uric acid crystals. Probenecid-AFT tablets 500mg also increase and prolong the blood concentration of beta-lactam antibiotics like penicillin, by inhibiting the secretion of penicillin by the kidneys into the urine, which means it stays in the blood for longer and is therefore more effective.
What does Probenecid-AFT contain?
Probenecid-AFT tablets 500mg contain the active ingredient probenecid, which is a uricosuric agent that is used to treat gout by lowering the blood levels of uric acid.
Treating gout with Probenecid-AFT
Probenecid-AFT tablets 500mg contain probenecid, which is a uricosuric drug that in that promotes the excretion of uric acid in the urine. Gout is a painful condition of the joints that is caused by build up of uric acid in the blood (hyperuricaemia) and the formation of uric acid crystals which are deposited in the joints and tissues. Probenecid-AFT 500mg acts on the tubules of the kidneys and blocks the reabsorption of uric acid by preventing its uptake into the tubules and this reduces the concentration of uric acid in the blood. As the amount of uric acid in the blood is reduced existing crystals are dissolved and the formation of new crystals is limited. Probenecid-AFT tablets 500mg relieve joint pain caused by gout which allows greater mobility of the affected joint; they also help prevent further joint destruction due to deposition of more uric acid crystals.
What are the side effects of Probenecid-AFT?
The most commonly reported side effects when taking Probenecid-AFT tablets 500mg include: urinating more than usual, mild nausea, vomiting, loss of appetite, headache, dizziness, sore gums, mild itching or skin rash, hair loss, flushing.
When should Probenecid-AFT not be used?
You should not use Probenecid-AFT tablets 500mg if you:
- are allergic to Probenecid-AFT or any ingredients in Probenecid-AFT tablets
- are pregnant or are breastfeeding, without discussion with your doctor
- have an acute gouty attack, you should wait until the attack has subsided
- have blood dyscrasias (blood cell disorder) such as anaemia, or decreased white blood cells
- have uric acid kidney stones
- have kidney disease or a history of peptic ulcer, without due caution
- are taking medicines that interact with Probenecid-AFT, including: methotrexate for cancer treatment, pyrazinamide for tuberculosis, the analgesic acetaminophen, NSAIDs like naproxen, indomethacin, ketoprofen and meclofenamate, lorazepam for anxiety, the antibiotic rifampicin, the antiretrovirals acyclovir, ganciclovir and zidovudine for HIV, sulfonylureas for diabetes, sulphonamide antibiotics, salicylates like aspirin
What medications interact with Probenecid-AFT?
Several medications interact with Probenecid-AFT tablets 500mg and should either not be taken while you are taking Probenecid-AFT or only after discussion and instruction from your doctor:
- Drugs that affect Probenecid-AFT: pyrazinamide for tuberculosis
- Drugs that are affected by Probenecid-AFT: methotrexate for cancer treatment, the analgesic acetaminophen, NSAIDs like naproxen, indomethacin, ketoprofen and meclofenamate, lorazepam for anxiety, the antibiotic rifampicin, the antiretrovirals acyclovir, ganciclovir and zidovudine for HIV, sulfonylureas for diabetes, sulphonamide antibiotics, salicylates like aspirin
How should Probenecid-AFT be taken?
You should take your Probenecid-AFT tablets 500mg with a glass of water twice daily. The dose you take should be as recommended by your doctor, which for gout will be to start with half a tablet (250mg) for the first week then a whole tablet after that. Your doctor may recommend that you increase your dose further, depending on your condition. If you are taking Probenecid-AFT tablets 500mg with an antibiotic your doctor will recommend the dose you take, which may be up to 2000mg (4 tablets) daily in divided doses. You should continue to take your Probenecid-AFT tablets 500mg until your blood levels of uric acid are within the normal range, your dose will then be reduced to a maintenance level for as long as recommended by your doctor.
How long should you take Probenecid-AFT?
You should continue to take your Probenecid-AFT tablets 500mg until your blood levels of uric acid are within the normal range, your dose will then be reduced to a maintenance level for as long as recommended by your doctor.
Missed dose of Probenecid-AFT
If you miss a dose of Probenecid-AFT tablets 500mg take it as soon as you remember, unless it is time to take the next dose, then skip the missed dose. Do not take a double dose.
How should Probenecid-AFT be stored?
You should store your Probenecid-AFT tablets 500mg between 15-30°C in a cool dry place.
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Cholesterol Lowering
What is cholesterol?
Cholesterol is an insoluble fatty substance that is needed by the body for many functions, such as building cell membranes, producing certain hormones and transporting fat soluble vitamins around the body. It is made in the liver and also obtained from the diet. Cholesterol is transported in the blood along with triglycerides, which is another type of fat. Since cholesterol is not soluble in blood it is carried to and from the liver by lipoproteins. These include low density lipoproteins (LDL) known as “bad” cholesterol because they carry cholesterol from the liver and deposit excess in the arteries. High density lipoproteins (HDL) carry cholesterol back to the liver and are therefore called “good” cholesterol.
High cholesterol and atherosclerosis
If there is more cholesterol in the blood than the body needs, it becomes deposited in the artery walls where it can build up, blocking the arteries and causing hardened areas called plaques, which increases risk of heart disease. This condition is known as atherosclerosis. High cholesterol in the blood and other fats (triglycerides) is known as hypercholesterolaemia and this condition is usually due to lifestyle, including high-fat diet, obesity and lack of exercise, but it can be inherited. The ratio of total cholesterol over HDL (good cholesterol) is also an important consideration.
Cholesterol lowering medications
Cholesterol lowering medications are available to treat hypercholesterolaemia in people who have not responded to a low-fat diet and lifestyle changes alone; also for those with an inherited condition and who cannot lower cholesterol levels by lifestyle changes alone. They include:
- Statins that block the production of cholesterol by the liver, by inhibiting the action of the enzyme HMG-CoA reductase that plays an important role in cholesterol synthesis. Statins only block cholesterol produced in the liver but have no effect on cholesterol that comes from fat in the diet. Several statins are available including, atorvastatin, simvastatin, pravastatin and rosuvastatin.
- Cholesterol absorption inhibitors, like ezetimibe act directly on the small intestine wall to block the action of the sterol transporter in the intestine wall. This action inhibits intestinal absorption of cholesterol from the diet and reduces cholesterol stores in the liver, which helps lower blood cholesterol levels.
- Fibrates like fenofibrate activate the enzyme Peroxisome Proliferator Activated Receptor type alpha (PPARα) that regulates the production of another enzyme involved in the breakdown of lipids in the blood. It also reduces the production of proteins that transport LDL lipids but increases the production of proteins that transport HDL. The overall effect is to lower triglycerides, total cholesterol, and LDL (bad) cholesterol, and increase HDL (good) cholesterol.
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