Gossypol - Uses and Side Effects

First identified as an anti-fertility agent in China in the 1950s, gossypol is also a component of cottonseed oil, which is used for cooking. It's derived from the stems, roots, and seeds of plants from the Malvaceae family. The cotton plant (Gossypium species) is the most common source. Gossypol is the active ingredient found in seeds and other parts of the plant; however, content varies significantly from specjes to species.

Gossypol exerts antifertility action by inhibiting sperm production and motility. It possesses antitumorigenic activity and may also have anti-human immunodeficiency virus properties. It's available as liquid extracts and tinctures.

Reported uses

Gossypol is used in China as a male contraceptive. It's also used topically as a spermicide.

Administration

Dosage is 20 mg by mouth every day for 2 to 3 months until the sperm count is decreased to less than 4 million/ml. The dosage is reduced to a maintenance ranging from 50 mg weekly to 75 to 100 mg twice a month.

Hazards

Adverse effects associated with gossypol include paralysis, circulatory problems, diarrhea, malnutrition, hypokalemia, muscle fatigue, muscle weakness, and hair discoloration.

Pregnant and breast-feeding patients shouldn't use this herb. Patients with renal insufficiency should use with caution.

Safety Risk Gossypol has been associated with heart failure and nephrotoxicity. There's increased risk of nephrotoxicity when gossypol is given with nephrotoxic drugs. Administration with potassium-wasting diuretics could lead to hypokalemia.

Clinical considerations

The contraceptive effect of gossypol in men is higher than 99%. Fertility usually returns to normal within 3 months of discontinuation; however, inhibition of spermatogenesis may persist in up to 20% of men 2 years after discontinuation.

Monitor serum electrolyte levels, especially potassium, creatinine, and BUN levels.

Monitor patient for muscle weakness and fatigue.

If using formulation containing alcohol, avoid using in patients taking disulfiram, metronidazole, cephalosporins, or any CNS depressants.

If patient is pregnant or breast-feeding, advise her not to use gossypol.

Inform men of the potential for permanent sterility after using oral gossypol.

Advise women who are considering the use of gossypol as a topical spermicide about the lack of adequate information on safety and efficacy. Inform them that there are alternative, safe, and effective contraceptive methods.

Advise patient to keep herb out of the reach of children and pets.

Tell patient to notify pharmacist of any herbal or dietary supplement that he's taking when obtaining a new prescription.

Advise patient to consult his health care provider before using an herbal preparation because a conventional treatment with proven efficacy may be available.

Research summary

Gossypol has been approved to be used as a male contraceptive drug in China due to its ability to inhibit sperm production and motility.

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