Hormone Formulations

Hormone Formulations

Hormones are available as implanted pellets, transdermal creams, gels, patches, or drops, sublingual pellets, troches (wafers), or drops, vaginal suppositories, oral capsules, and injectables.

Pellets

We have been using implanted hormone pellets increasingly for years.  Although they have been available for the last fifty years, they are not well known in the United States, though they are popular in Europe.

Pellets are crystallized forms of estrogen and testosterone, compressed into small cylinders the size of grains of rice.  They are inserted under the skin of the buttock, after a small incision has been made under local anesthesia.  Most patients experience a numbness and slight pressure.  Insertion requires only a minute or two after the anesthesia takes hold.

The main benefit of the pellets is that blood hormone levels remain constant for 3-4 months, 24 hours a day, day in and day out.  Thus the hormonal effect is considerably stronger than with other formulations, and it is unchanging.  Symptoms of irritability and malaise, headache and insomnia, that women experience when hormone levels fluctuate, as in premenstrual syndrome, do not occur.

Women who have used other hormone preparations are pleasantly surprised when they first receive the pellets.  The sense of well-being, restored libido and energy go beyond what they have experienced before.  One woman stated that she felt completely different, that her sex drive was restored and she had more enthusiasm for life.  She smiled when she said, “You have saved my marriage.”

We measure blood hormone levels of estrogen, testosterone, and FSH before inserting the pellets, and one month later, to assess the changes made by the doses given.  Subsequently we may raise or lower the dose, although the main criterion for dosage change is the woman’s symptoms.  Too little or too much libido indicates a need to raise or lower the testosterone dose.  Breast tenderness or weight gain requires a reduction of the estrogen dose.

Women return for new pellets at a scheduled time, usually three or four months, up to six months later, or when they get a sense of hormone depletion.

The effect on bone density has been remarkable.  We strongly prefer hormone pellets for women with early or severe osteoporosis, since they are more rapidly effective than other hormonal preparations.

Men also benefit from testosterone given as pellets.  Again, they have constant, high and unchanging blood levels of testosterone for about four months.  Endurance, muscle mass, energy, sexual interest and performance substantially increase.  The dose we use is generally 1000-1200 mg, about 20 times higher than the dose in women.  Men can tell when their levels are declining, and will call to schedule another insertion.

In men we measure blood count and PSA about 3 months after the first pellets are inserted.  Testosterone may raise the blood count excessively, requiring a reduction in dosage.  If the PSA rises more than one point, we investigate the possibility of prostate tumor, uncovered by testosterone stimulation.  As in women, pellets are the hormonal treatment of choice for men with osteoporosis.  Pellets are the most effective way of raising bone density, because the hormone elevation is continuous.

Transdermal Cream or Gel

The cream or gel may be prescribed for both women and men.  It is applied topically to the skin of the forearms or thighs.

In women a cream preparation is used most commonly.  It contains estradiol, the most active form of estrogen, and often estriol, a weaker estrogen considered to be protective against breast cancer.  This combination is called Biest, usually in a ratio of four parts estriol to one part estradiol.  Initially the cream is applied both in the morning and at night.  Later, and in older women, it can be used just once a day.  It may be combined with progesterone in the same preparation for convenience and cost-saving.  It may also be combined with testosterone.  Transdermal testosterone, however, may cause hair growth where it is applied, so we usually recommend it to be applied to the thighs where it is less evident and more easily handled.

In men the cream or gel contains only testosterone, generally in a dose of 50-100 mg per gram.  It is applied once daily to the arms or thighs.

Sublingual Drops, Troches And Pellets

We have prescribed these on occasion for women. Sublingual drops are rapidly absorbed.  They should be placed and held under the tongue. Sublingual troches and pellets are also effective.  They take about fifteen minutes to dissolve, and should be administered between meals.  They are usually given twice daily.

All of these creams, gels and drops are specially made by compounding pharmacies according to the physician’s prescription.  They cannot be obtained through regular pharmacies.  The dosage is readily adjustable according to the clinical need and the patient’s response.  Most compounding pharmacies will mail the prescription to the patient’s home.  Insurance companies occasionally pay for these hormones.  Medicare does not.

Transdermal patches are commercial patches produced by pharmaceutical companies and carried in regular pharmacies.  In recent years they have contained bioidentical estradiol, and we consider them safe to use.  The progestin and testosterone formulations contained in some of them are not bioidentical, and we advise not using them. The various brands last from three to seven days.  They may cause skin rashes or slide off the skin.  The blood level declines gradually during the time of application.

All oral estrogen tablets or capsules are absorbed through the gastrointestinal tract into the blood stream.  Then they pass through the liver into systemic circulation.  They result in an increased formation of clotting factors, which may lead to thrombophlebitis,

pulmonary embolism, heart attacks or strokes.  The higher risk of adverse events approaches twice that of other formulations.  For this reason we generally avoid this mode of estrogen administration.  Progesterone, however, is quite safe when given as a capsule, and is the most effective form of progesterone for promoting sleep.

Vaginal estrogen suppositories are primarily intended for local effect.  They support the vaginal tissues, prevent atrophy and maintain moisture.  They are utilized when systemic effects are not desired, or when vaginal symptoms persist in spite of systemic hormone use.

We do not use injectable hormones in women.  Testosterone injections in men, however, are quite effective and often a preferred mode of administration.  They are given into the buttock, usually once or twice a week, in a dose of 50-100 mg.