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Hormones & Anti-Hormones

Including Drug & Hormone Interaction Chart

 

Medications, Supplements, Herbs & Other Substances

Question: I was told that my medication may be the reason why I feel like my hormones are low even though my lab tests (both saliva & blood) both show I have good levels. How do I find out if my medications are the cause of my hormone problems?

Quick Answer:

Your personal healthcare professional (who prescribed the medication) is you first source for answers. Just as valuable could be finding a local pharmacist who is available for consultation, to review your medications, supplements and other factors that may affect hormone function.

Hormones Affect Hormones

Any hormone, whether synthetic or bioidentical, will affect other hormones in the human body. When considering estrogens, progesterone and testosterone, realize that each one will help “balance/control/oppose” the other two.

Medications, Supplements, Herbs & Other Substances *

Some medications, supplements and other substances may also affect hormone levels and/or function. The affect may be due to decreased or increased production, interfering or competing with hormones binding to cells, or changes in how the hormone is metabolized and eliminated from the body. Review the following list. Talk to your healthcare professional if you suspect your hormones are being affected by any of these substances.

Learning More About Drugs & Hormones

This article will focus how steroid hormones are affected by various drugs. Hormones that are biochemically designated as “steroid hormones” include androgens, estrogens, progestogens & corticoids. These are also described as “sex hormones” and “adrenal gland hormones”. This document will focus on how this class of hormones is affected.

Prescription and non-prescription medications that affect hormones may be classified in various ways. This document will classify them by prescriptive class and by potential action significant to function of steroid hormones.

 

Prescriptive Classes:

Note: OTC = Over The Counter medications.

The prescriptive classes, which include medications that may affect steroid hormones, include the following. The classifications include both biochemical classes and functional classes. Not all medication in a class have the effects noted in this writing. Though this list in not comprehensive, it does attempt to include all information available at the time of this writing.

Estrogens - Noncontraceptive Use

Antifungals & Antibiotics (includes OTC)

Custom Compounded Estrogens

Psychiatric Medications

Progestogens - Noncontraceptive Use (includes OTC)

Cardiac Medications

Custom Compounded Progesterone & Pregnenolone

Fertility Drugs

Progestins  For Contraceptive Use

Anti-Ulcer Drugs (includes OTC)

Estrogen & Progestogen Oral Contraceptives

Endocrinology Drugs

Androgens (includes OTC)

Anti-Androgens

Custom Compounded Androgens

Aromatase Inhibitors

Corticosteroids (includes OTC)

5-alpha-reductase inhibitors

Custom Compounded Corticoids

Estrogen Receptor Antagonist

HMG-CoA Reductase inhibitors

Selective Estrogen Receptor Modulator (SERM)

Immunosuppressants

 

 

Potential Actions:

The potential action significant to function of steroid hormones may be classified into those that enhance or work with the hormones (agonists) or those that oppose or work against hormones (antagonists).

Androgenic (A) – androgens (such as testosterone or DHEA) or substances with an androgenic affect in some fashion (though they may not have the optimal, well balanced androgen function seen in bioidentical androgens).

Anti-Androgenic (aA) – substances with an anti-androgenic affect. The effect may be due to competitive binding, interference with metabolic production or increased metabolic degradation of androgens. Some substances may have both androgenic and anti- androgenic functions.

Estrogenic (E) – estrogens (such as estradiol) or substances with an estrogenic affect in some fashion (though they may not have the optimal, well balanced estrogen function seen in bioidentical estrogens). Estrogens have antiandrogen properties in and of themselves. In addition, estrogenic substances may increase the production of SHBG (sex-hormone-binding-globulin), which preferentially binds testosterone, resulting in further interference with testosterone function. Estrogens taken by mouth are more potent inducers of SHBG then if taken in a transdermal form.

Anti-Estrogenic (aE) - substances with an anti-estrogenic affect. The effect may be due to competitive binding, interference with production or increased metabolic degradation of estrogens. Some substances may have both estrogenic and anti-estrogenic function.

Progestogenic (P) – progestogens (such as progesterone) or substances with a progestogenic affect in some fashion (though they may not have the optimal, well balanced progesterone function seen in bioidentical progesterone).

Anti-Progestogenic (aP) - substances with an anti-progestogenic affect. The effect may be due to competitive binding, interference with production or increased metabolic degradation of progestogens. Some substances may have both progestogenic and anti- progestogenic functions.

2-Hydroxylation Inhibition (2h) – substances that inhibit 2-hydroxylation activity – a metabolic pathway for estrogen detoxification. The net affect of inhibiting 2-hydroxylation may be decreased metabolic degradation of estrogens resulting in an excessive estrogenic function.

5-Alpha Reductase inhibition (5a) - substances that inhibit 5-alpha reductase activity – a metabolic pathway for the conversion of testosterone to the more potent dihydrotestosterone (DHT), a normal androgen in both genders. The net affect may is decreased conversion to DHT resulting in relative anti-androgen function.

Aromatase Inhibition (ar) – Aromatase is the enzyme that converts androgens to estrogens. By inhibiting this enzyme the net affect is decreased estrogen production. Some, but not all aromatase inhibitors produce a net androgenic function.

Glucocorticoid (Gc) – The endogenous glucocorticoid is cortisol, which has many synonyms. Glucocorticoids appear to universally oppose androgens, estrogens, and progestogens.

HMG-CoA Reductase Inhibitor (Hc) – Often used to decrease cholesterol & LDL levels, this class of drugs may decrease the production of steroid hormones, which are all synthesized from cholesterol. Though debated in the literature, if class of drugs does inhibit steroidogenesis, it may possess anti-androgen, anti-estrogen and anti-progestogen activity. Since LDL cholesterol is the primary substrate for steroidogenesis in some tissues there may be a relative substrate deficiency in some individuals.

 

The prescriptive class and the potential actions are plotted in the following table for easy cross referencing.

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This table and the subsequent analysis of medications is part of the Menopause Type® Test and Wellness Report.

 

Medication Review

 

Key: (A) Androgenic, (aA) Anti-Androgenic, (E) Estrogenic, (aE) anti-Estrogenic, (P) Progestogenic, (aP) anti-Progestogenic, (2h 2-hydroxylation inhibition, (5a) 5-alpha reductase inhibition, (ar) Aromatase Inhibition, (Gc) Glucocorticoid, (Hc) HMG-CoA Reductase inhibitor.

 

Potential actions of various medications significant to androgens, estrogens, progestogens & corticoids.

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

A

aA

E

aE

P

aP

2h

5a

ar

Gc

Hc

Estrogens (For Noncontraceptive Use)

 

 

 

 

 

 

 

 

 

 

 

Conjugated Estrogens

 

aA

E

 

 

aP

 

 

 

 

 

Conjugated Estrogens, Synthetic

 

aA

E

 

 

aP

 

 

 

 

 

Diethylstilbestrol

 

aA

E

 

 

 

 

 

 

 

 

Esterified Estrogens

 

aA

E

 

 

 

 

 

 

 

 

Estradiol

 

aA

E

 

 

 

 

 

 

 

 

Estrone

 

aA

E

 

 

 

 

 

 

 

 

Estropipate

 

aA

E

 

 

 

 

 

 

 

 

Ethinyl Estradiol

 

aA

E

 

 

 

2h

 

 

 

 

Custom Compounded Estrogens

 

 

 

 

 

 

 

 

 

 

 

Estradiol

 

aA

E

 

 

 

 

 

 

 

 

Estrone

 

aA

E

 

 

 

 

 

 

 

 

Estriol

 

aA

E

 

 

 

 

 

 

 

 

Bi-est

 

aA

E

 

 

 

 

 

 

 

 

Tri-Est

 

aA

E

 

 

 

 

 

 

 

 

Progestogens (Noncontraceptive)

 

 

 

 

 

 

 

 

 

 

 

Hydroxyprogesterone

 

 

 

aE

P

aP

 

 

 

 

 

Medrogestone

 

aA

 

aE

P

aP

 

 

 

 

 

Medroxyprogesterone

 

aA

 

aE

P

aP

 

 

 

 

 

Megestrol

 

aA

 

aE

P

aP

 

 

 

 

 

Norethindrone

 

 

 

aE

P

aP

 

 

 

 

 

Progesterone (including OTC progesterone)

 

aA

 

aE

P

 

 

 

 

 

 

Custom Compounded Progestogens

 

 

 

 

 

 

 

 

 

 

 

Progesterone

 

aA

 

aE

P

 

 

 

 

 

 

Pregnenolone

 

aA

 

aE

P

 

 

 

 

 

 

Progestins  For Contraceptive Use

 

 

 

 

 

 

 

 

 

 

 

Levonorgestrel

 

 

 

aE

P

aP

 

 

 

 

 

Medroxyprogesterone

 

aA

 

aE

P

aP

 

 

 

 

 

Norethindrone

 

 

 

aE

P

aP

 

 

 

 

 

Norgestrel

 

 

 

aE

P

aP

 

 

 

 

 

Estrogen/Progestogen Contraceptives

 

 

 

 

 

 

 

 

 

 

 

Desogestrel & Ethinyl Estradiol

 

aA

E

aE

P

aP

2h

 

 

 

 

Ethynodiol Diacetate & Ethinyl Estradiol

 

aA

E

aE

P

aP

2h

 

 

 

 

Levonorgestrel & Ethinyl Estradiol

 

aA

E

aE

P

aP

2h

 

 

 

 

Norethindrone Acetate & Ethinyl Estradiol

 

aA

E

aE

P

aP

2h

 

 

 

 

Norethindrone & Ethinyl Estradiol

 

aA

E

aE

P

aP

2h

 

 

 

 

Norethindrone & Mestranol

 

aA

E

aE

P

aP

 

 

 

 

 

Norgestimate & Ethinyl Estradiol

 

aA

E

aE

P

aP

2h

 

 

 

 

Norgestrel & Ethinyl Estradiol

 

aA

E

aE

P

aP

2h

 

 

 

 

Androgens

 

 

 

 

 

 

 

 

 

 

 

Testosterone

A

 

 

 

 

 

 

 

 

 

 

Methyltestosterone

A

 

 

 

 

 

 

 

 

 

 

DHEA

A

 

 

 

 

 

 

 

 

 

 

Custom Compounded Androgens

 

 

 

 

 

 

 

 

 

 

 

Testosterone

A

 

 

 

 

 

 

 

 

 

 

DHEA

A

 

 

 

 

 

 

 

 

 

 

Corticosteroids

 

 

 

 

 

 

 

 

 

 

 

Betamethasone

 

aA

 

aE

 

aP

 

 

 

Gc

 

Budesonide

 

aA

 

aE

 

aP

 

 

 

Gc

 

Cortisone

 

aA

 

aE

 

aP

 

 

 

Gc

 

Dexamethasone

 

aA

 

aE

 

aP

 

 

 

Gc

 

Hydrocortisone

 

aA

 

aE

 

aP

 

 

 

Gc

 

Methylprednisolone

 

aA

 

aE

 

aP

 

 

 

Gc

 

Prednisolone

 

aA

 

aE

 

aP

 

 

 

Gc

 

Prednisone

 

aA

 

aE

 

aP

 

 

 

Gc

 

Triamcinolone

 

aA

 

aE

 

aP

 

 

 

Gc

 

Custom Compounded Corticoids

 

 

 

 

 

 

 

 

 

 

 

Cortisol

 

aA

 

aE

 

aP

 

 

 

Gc

 

Hydrocortisone

 

aA

 

aE

 

aP

 

 

 

Gc

 

HMG-CoA Reductase inhibitors

 

 

 

 

 

 

 

 

 

 

 

Atorvastatin

 

 

 

 

 

 

 

 

 

 

Hc

Fluvastatin

 

 

 

 

 

 

 

 

 

 

Hc

Lovastatin

 

 

 

 

 

 

 

 

 

 

Hc

Pravastatin

 

 

 

 

 

 

 

 

 

 

Hc

Simvastatin

 

 

 

 

 

 

 

 

 

 

Hc

Immunosuppressants

 

 

 

 

 

 

 

 

 

 

 

Tacrolimus

 

 

 

 

 

 

2h

 

 

 

 

Cyclosporin

 

 

 

 

 

 

2h

 

 

 

 

Antifungals & Antibiotics

 

 

 

 

 

 

 

 

 

 

 

Fluconazole

A

 

 

 

 

 

 

 

 

 

 

Ketoconazole

 

aA

 

 

 

 

 

 

 

 

 

Triacetyloleandomycin

 

 

 

 

 

 

2h

 

 

 

 

Psychiatric Medications

 

 

 

 

 

 

 

 

 

 

 

Haloperidol

 

 

 

 

 

 

2h

 

 

 

 

Risperidone

 

aA

 

 

 

 

 

 

 

 

 

Cardiac Medications

 

 

 

 

 

 

 

 

 

 

 

Diltiazem

 

 

 

 

 

 

2h

 

 

 

 

Verapamil

 

 

 

 

 

 

2h

 

 

 

 

Nicardipine

 

 

 

 

 

 

2h

 

 

 

 

Nisoldipine

 

 

 

 

 

 

2h

 

 

 

 

Nitrendipine

 

 

 

 

 

 

2h

 

 

 

 

Manidipine

 

 

 

 

 

 

2h

 

 

 

 

Spirinolactone

 

aA

 

 

 

 

2h

 

 

 

 

Fertility Drugs

 

 

 

 

 

 

 

 

 

 

 

Clomiphene

 

 

E

aE

 

 

 

 

 

 

 

Cyclofenil

 

 

 

aE

 

 

 

 

 

 

 

Anti-Ulcer Drugs

 

 

 

 

 

 

 

 

 

 

 

Omeprazole

 

 

 

 

 

 

2h

 

 

 

 

Cimetidine

 

aA

 

 

 

 

 

 

 

 

 

Endocrinology Drugs

 

 

 

 

 

 

 

 

 

 

 

Aminoglutethimide

 

aA

 

 

 

 

 

 

 

 

 

Domperidone

 

 

 

 

 

 

2h

 

 

 

 

Mifepristone

 

 

 

 

 

aP

 

 

 

 

 

Leuprolide

 

aA

 

aE

 

 

 

 

 

 

 

Anti-Androgens

 

 

 

 

 

 

 

 

 

 

 

Bicalutamide

 

aA

 

 

 

 

 

 

 

 

 

Flutamide

 

aA

 

 

 

 

 

 

 

 

 

Chlormadinone

 

 

 

 

 

 

2h

 

 

 

 

Aromatase Inhibitors

 

 

 

 

 

 

 

 

 

 

 

Letrozole

 

 

 

aE

 

 

 

 

ar

 

 

Anastrozole

 

 

 

aE

 

 

 

 

ar

 

 

Mesterolone

A

 

 

aE

 

 

 

 

ar

 

 

5-alpha-reductase inhibitors

 

 

 

 

 

 

 

 

 

 

 

Finasteride

 

aA

 

 

 

 

 

5a

 

 

 

Dutasteride (Avodart)

 

 

 

 

 

 

 

5a

 

 

 

Estrogen Receptor Antagonist

 

 

 

 

 

 

 

 

 

 

 

Fulvestrant

 

 

 

aE

 

 

 

 

 

 

 

Tamoxifen

 

 

 

aE

 

 

 

 

 

 

 

Selective Estrogen Receptor Modulator

 

 

 

 

 

 

 

 

 

 

 

Raloxifene

 

 

E

aE

 

 

 

 

 

 

 

Others (Report Customized as Needed)

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Potential actions of various medications significant to androgens, estrogens, progestogens & corticoids.

A

aA

E

aE

P

aP

2h

5a

ar

Gc

Hc

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Key: (A) Androgenic, (aA) Anti-Androgenic, (E) Estrogenic, (aE) anti-Estrogenic, (P) Progestogenic, (aP) anti-Progestogenic, (2h 2-hydroxylation inhibition, (5a) 5-alpha reductase inhibition, (ar) Aromatase Inhibition, (Gc) Glucocorticoid, (Hc) HMG-CoA Reductase inhibitor.

 

Other Considerations

Some of the functional classes may be considered subclasses of other classes. The following summary table demonstrates how 5-alpha-reductase inhibition can contribute to functional anti-androgen activity. It also demonstrates how 2-hydroxylase inhibition and aromatase inhibition contribute to functional anti-estrogenic activity.

 

 

 

 

 

 

 

 

 

 

 

 

 

Androgenic

 

anti-Androgenic

+

5-alpha reductase inhibition

=

Total Antiandrogens

 

 

 

 

 

 

 

 

 

 

 

 

 

Estrogenic

 

anti-Estrogenic

+

2-oh-inh.

+

Aromatase inh.

=

Total Antiestrogenic

 

 

 

 

 

 

 

 

 

 

 

 

 

Progestogenic

 

 

 

 

 

 

 

 

 

 

 

 

anti-Progestogenic

 

 

 

 

 

 

 

 

 

 

 

 

 

Glucocorticoid activity

 

 

 

 

 

 

 

 

 

 

HMG-CoA Reductase Inhibitors

 

 

Conclusion:

Proper management of menopause requires a comprehensive assessment that includes a medication survey which can provide valuable information to both the woman experiencing menopause and the healthcare professional advising her on optimal health.

If you discover that prescription medications may be associated with hormonal imbalances, this information may be shared with the prescribing healthcare professional who can discuss the options available to you. Be sure to discuss lifestyle choices that can have a powerful influence on your health.

NOTE: It is very important that a healthcare professional be contacted for guidance on choices to make regarding any medications.

 

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Partial List of References:

Collins, JJ. Discover Your Menopause Type. Roseville, CA. Prima, 2000. Chapter 10.

Tureck RW, Strauss JF 3rd. Progesterone synthesis by luteinized human granulosa cells in culture: the role of de novo sterol synthesis and lipoprotein-carried sterol. J Clin Endocrinol Metab. 1982 Feb;54(2):367-73.

Richie JP. Anti-androgens and other hormonal therapies for prostate cancer. Urology. 1999 Dec;54(6A Suppl):15-8.

Takashi Satoh, Haruka Munakata, Ken-ichi Fujita, Shinji Itoh, Shungo Itoh, Tetsuya Kamataki, & Itsuo Yoshizawa. Studies on the Interactions between Drug and Estrogen. II.1) On the Inhibitory Effect of 29 Drugs Reported to Induce Gynecomastia on the Oxidation of Estradiol at C-2 or C-17. Biol. Pharm. Bull. 26(5) 695—700 (2003)

Schmidt JB.Other antiandrogens. Dermatology. 1998;196(1):153-7.

Kerlan V, Dreano Y, Bercovici JP, Beaune PH, Floch HH, Berthou F. Nature of cytochromes P450 involved in the 2-/4-hydroxylations of estradiol in human liver microsomes. Biochem Pharmacol. 1992 Nov 3;44(9):1745-56.

Michnovicz JJ, Galbraith RA.Cimetidine inhibits catechol estrogen metabolism in women. Metabolism. 1991 Feb;40(2):170-4.

Van Cauteren H, Heykants J, De Coster R, Cauwenbergh G. Itraconazole: pharmacologic studies in animals and humans. Rev Infect Dis.  1987 Jan-Feb;9 Suppl 1:S43-6.

 

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