Ipriflavone

Last Editorial Review: 6/11/2021
Other Name(s):

FL-113, 7-isopropoxyisoflavone, 7-Isopropoxy-Isoflavone, Ipriflavona, TC-80.

Overview

Ipriflavone is made in the laboratory from another substance (daidzein) that is taken from soy. Soy is a plant.

Ipriflavone is used for preventing and treating weak bones (osteoporosis) in older women, preventing osteoporosis caused by certain medications, relieving pain associated with osteoporosis, and treating a bone disease called Paget's disease. It is also used for reducing bone loss caused by chronic kidney disease (renal osteodystrophy) and by paralysis associated with stroke. Researchers have found that paralyzed stroke patients have weaker bones on the affected side, possibly due to immobility as well as vitamin D deficiency. Vitamin D deficiency may stem from lack of exposure to sunlight.

Ipriflavone is also used by bodybuilders to increase metabolism.

How does it work?

Ipriflavone may prevent bone strength loss, and help improve the effects of estrogen in preventing osteoporosis. When used in combination with estrogens, it might allow lower estrogen doses to be used in postmenopausal women.

QUESTION

What is another medical term for osteoporosis? See Answer

Uses & Effectiveness

Likely Effective for...

  • Treating and preventing weak bones (osteoporosis) in postmenopausal women. Taking ipriflavone in combination with 1000 mg of calcium daily can prevent loss of bone mineral density (BMD) in postmenopausal women with osteoporosis or low bone strength. There is some evidence that it might actually increase bone strength in some of these women. The effect seems to be determined by the amount of calcium that is taken along with the ipriflavone. One study using ipriflavone with only 500 mg per day of calcium found no effect on bone strength. But taking more than 1000 mg of calcium daily may increase the benefit.
    Taking ipriflavone in combination with estrogen also seems to prevent osteoporosis and increase bone strength in older women. Adding calcium makes the combination work even better.
  • Reducing pain associated with osteoporosis. Ipriflavone can also significantly reduce pain due to osteoporosis and seems to be as effective as inhaling a medication called calcitonin.
  • Reducing bone loss in people who have been paralyzed on one side of their body by stroke (hemiplegic stroke). Ipriflavone in combination with vitamin D seems to prevent bone loss significantly better than vitamin D alone in hemiplegic stroke patients with vitamin D deficiency.

Possibly Effective for...

  • Bone pain in people with Paget's disease.
  • Bone disease due to chronic kidney disease (renal osteodystrophy).

Insufficient Evidence to Rate Effectiveness for...

  • Increasing metabolism in bodybuilders.
  • Other conditions.
More evidence is needed to rate the effectiveness of ipriflavone for these uses.

Natural Medicines Comprehensive Database rates effectiveness based on scientific evidence according to the following scale: Effective, Likely Effective, Possibly Effective, Possibly Ineffective, Likely Ineffective, and Insufficient Evidence to Rate (detailed description of each of the ratings).

Side Effects

Ipriflavone is LIKELY SAFE for most people when used with proper medical supervision. It can cause side effects such as stomach pain, diarrhea, or dizziness.

There is some concern that ipriflavone can cause a decreased white cell count (lymphocytopenia) in people taking it for greater than six months. White cell counts should be monitored, especially in people taking ipriflavone long-term.

SLIDESHOW

Osteoporosis Super-Foods for Strong Bones With Pictures See Slideshow

Special Precautions & Warnings

Pregnancy and breast-feeding: Not enough is known about the use of ipriflavone during pregnancy and breast-feeding. Stay on the safe side and avoid use.

Weak immune system: Ipriflavone can lower the body's white cell count, making it more difficult for the body to fight off infection. This is especially concerning in people who already have a weak immune system due to AIDS, drugs used to prevent organ rejection after transplant, chemotherapy, or other causes. If you have a weak immune system, check with your healthcare provider before starting ipriflavone.

Low white cell count (lymphocytopenia): Since ipriflavone can cause lymphocytopenia, there is a concern that it might make pre-existing lymphocytopenia worse.

Interactions


Medications changed by the liver (Cytochrome P450 1A2 (CYP1A2) substrates)Interaction Rating: Moderate Be cautious with this combination.Talk with your health provider.

Some medications are changed and broken down by the liver. Ipriflavone might decrease how quickly the liver breaks down some medications. Taking ipriflavone along with some medications that are changed by the liver might increase the effects and side effects of some medications. Before taking ipriflavone, talk to your healthcare provider if you take any medications that are changed by the liver.

Some of these medications that are changed by the liver include clozapine (Clozaril), cyclobenzaprine (Flexeril), fluvoxamine (Luvox), haloperidol (Haldol), imipramine (Tofranil), mexiletine (Mexitil), olanzapine (Zyprexa), pentazocine (Talwin), propranolol (Inderal), tacrine (Cognex), theophylline, zileuton (Zyflo), zolmitriptan (Zomig), and others.


Medications changed by the liver (Cytochrome P450 2C9 (CYP2C9) substrates)Interaction Rating: Moderate Be cautious with this combination.Talk with your health provider.

Some medications are changed and broken down by the liver. Ipriflavone might decrease how quickly the liver breaks down some medications. Taking ipriflavone along with some medications that are broken down by the liver can increase the effects and side effects of some medications. Before taking ipriflavone, talk to your healthcare provider if you take any medications that are changed by the liver.

Some medications that are changed by the liver include amitriptyline (Elavil), diazepam (Valium), zileuton (Zyflo), celecoxib (Celebrex), diclofenac (Voltaren), fluvastatin (Lescol), glipizide (Glucotrol), ibuprofen (Advil, Motrin), irbesartan (Avapro), losartan (Cozaar), phenytoin (Dilantin), piroxicam (Feldene), tamoxifen (Nolvadex), tolbutamide (Tolinase), torsemide (Demadex), warfarin (Coumadin), and others.


Medications that decrease the immune system (Immunosuppressants)Interaction Rating: Moderate Be cautious with this combination.Talk with your health provider.

Ipriflavone might decrease the immune system. Taking ipriflavone along with other medications that decrease the immune system might decrease the immune system too much. Avoid taking ipriflavone with medications that decrease the immune system.

Some medications that decrease the immune system include azathioprine (Imuran), basiliximab (Simulect), cyclosporine (Neoral, Sandimmune), daclizumab (Zenapax), muromonab-CD3 (OKT3, Orthoclone OKT3), mycophenolate (CellCept), tacrolimus (FK506, Prograf), sirolimus (Rapamune), prednisone (Deltasone, Orasone), corticosteroids (glucocorticoids), and others.


TheophyllineInteraction Rating: Moderate Be cautious with this combination.Talk with your health provider.

The body breaks down theophylline to get rid of it. Ipriflavone might decrease how quickly the body gets rid of theophylline. Taking ipriflavone along with theophylline might increase the effects and side effects of theophylline.

Dosing

The following doses have been studied in scientific research:

BY MOUTH:

  • For weak bones after menopause (postmenopausal osteoporosis): 200 mg of ipriflavone three times daily.
  • For a bone disorder called Paget's disease: 600-1200 mg of ipriflavone daily.
  • For treating weak bones due to kidney disease (renal osteodystrophy): 400-600 mg of ipriflavone daily.

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References

Agnusdei D, Adami S, Cervetti R, et al. Effects of ipriflavone on bone mass and calcium metabolism in postmenopausal osteoporosis. Bone Miner 1992;19,Suppl 1:S43-8. View abstract.

Agnusdei D, Bufalino L. Efficacy of ipriflavone in established osteoporosis and long-term safety. Calcif Tissue Int 1997;61,Suppl 1:S23-7. View abstract.

Agnusdei D, Camporeale A, Gonnelli S, et al. Short-term treatment of Paget's disease of bone with ipriflavone. Bone Miner 1992;19 Suppl 1:S35-42. View abstract.

Agnusdei D, Crepaldi G, Isaia G, et al. A double blind, placebo-controlled trial of ipriflavone for prevention of postmenopausal spinal bone loss. Calcif Tissue Int 1997;61:142-7. View abstract.

Agnusdei D, Gennari C, Bufalino L. Prevention of early postmenopausal bone loss using low doses of conjugated estrogens and the non-hormonal, bone-active drug ipriflavone. Osteoporos Int 1995;5:462-6. View abstract.

Agnusdei D, Zacchei F, Bigazzi S, et al. Metabolic and clinical effects of ipriflavone in established post-menopausal osteoporosis. Drugs Exp Clin Res 1989;15:97-104. View abstract.

Alexandersen P, Toussaint A, Christiansen C, et al. Ipriflavone in the treatment of postmenopausal osteoporosis: A randomized controlled trial. JAMA 2001;285:1482-8. View abstract.

Arjmandi BH, Birnbaum RS, Juma S, et al. The synthetic phytoestrogen, ipriflavone, and estrogen prevent bone loss by different mechanisms. Calcif Tissue Int 2000;66:61-5. View abstract.

Gambacciani M, Cappagli B, Piaggesi L, et al. Ipriflavone prevents the loss of bone mass in pharmacological menopause induced by GnRH-agonists. Calcif Tissue Int 1997;61:S15-8. View abstract.

Gambacciani M, Ciaponi M, Cappagli B, et al. Effects of combined low dose of the isoflavone derivative ipriflavone and estrogen replacement on bone mineral density and metabolism in postmenopausal women. Maturitas 1997;28:75-81. View abstract.

Gennari C, Adami S, Agnusdei D, et al. Effect of chronic treatment with ipriflavone in postmenopausal women with low bone mass. Calcif Tissue Int 1997;61,Suppl 1:S19-22. View abstract.

Gennari C, Agnusdei D, Crepaldi G, et al. Effect of ipriflavone-a synthetic derivative of natural isoflavones-on bone mass loss in the early years after menopause. Menopause 1998;5:9-15. View abstract.

Head KA. Ipriflavone: an important bone-building isoflavone. Altern Med Rev 1999;4:10-22. View abstract.

Hyodo T, Ono K, Koumi T, et al. A study of the effects of ipriflavone administration on hemodialysis patients with renal osteodystrophy: preliminary report. Nephron 1991;58:114-5.

Maugeri D, Panebianco P, Russo MS, et al. Ipriflavone-treatment of senile osteoporosis: results of a multicenter, double-blind clinical trial of 2 years. Arch Gerontol Geriatr 1994;19:253-63.

Melis GB, Paoletti AM, Bartolini R, et al. Ipriflavone and low doses of estrogens in the prevention of bone mineral loss in climacterium. Bone Miner 1992;19,Suppl 1:S49-56. View abstract.

Melis GB, Paoletti AM, Cagnacci A, et al. Lack of any estrogenic effect of ipriflavone in postmenopausal women. J Endocrinol Invest 1992;15:755-61. View abstract.

Monostory K, Vereczkey L, Levai F, et al. Ipriflavone as an inhibitor of human cytochrome P450 enzymes. Br J Pharmacol 1998;123:605-10. View abstract.

Nozaki M, Hashimoto K, Inoue Y, et al. Treatment of bone loss in oophorectomized women with a combination of ipriflavone and conjugated equine estrogen. Int J Gynaecol Obstet 1998;62:69-75. View abstract.

Ohta H, Komukai S, Makita K, et al. Effects of 1-year ipriflavone treatment on lumbar bone mineral density and bone metabolic markers in postmenopausal women with low bone mass. Horm Res 1999;51:178-83. View abstract.

Petilli M, Fiorelli G, Benvenuti S, et al. Interactions between ipriflavone and the estrogen receptor. Calcif Tissue Int 1995;56:160-5. View abstract.

Sato Y, Kuno H, Kaji M, et al. Effect of ipriflavone on bone in elderly hemiplegic stroke patients with hypovitaminosis D. Am J Phys Med Rehabil 1999;78:457-63. View abstract.

Scali G, Mansanti P, Zurlo A, et al. Analgesic effect of ipriflavone versus Calcitonin in the treatment of osteoporotic vertebral pain. Curr Ther Res 1991;49:1004-10.

Somekawa Y, Chiguchi M, Ishibashi T, et al. Efficacy of ipriflavone in preventing adverse effects of leuprolide. J Clin Endocrinol Metab 2001;86:3202-6.. View abstract.

Takahashi J, Kawakatsu K, Wakayama T, Sawaoka H. Elevation of serum theophylline levels by ipriflavone in a patient with chronic obstructive pulmonary disease. Eur J Clin Pharmacol 1992;43:207-8.

Ushiroyama T, Okamura S, Ikeda A, et al. Efficacy of ipriflavone and 1 alpha vitamin D therapy for the cessation of vertebral bone loss. Int J Gynaecol Obstet 1995;48:283-8. View abstract.

Valente M, Bufalino L, Castiglione GN, et al. Effects of 1-year treatment with ipriflavone on bone in postmenopausal women with low bone mass. Calcif Tissue Int 1994;54:377-80. View abstract.