Diindolylmethane
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2019-09-19
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Clinical Pharmacology
The preparation Cervicon®-DIM as an active ingredient contains diindolylmethane, which is a means of stimulating apoptosis of human papillomavirus (HPV) infected and transformed cells, as well as a stimulator of expression of γ-interferon receptors. Thus, the basis of the therapeutic effect of diindolylmethane is its ability to accelerate the elimination of human papillomavirus infected and transformed cells and enhance the nonspecific immune response to the infection. In addition, diindolylmethane normalizes the metabolism of estradiol in HPV-infected cells, preventing the formation of a carcinogenic estrogen metabolite (16α-hydroxyestrone) that stimulates the expression of HPV oncogenes. By suppressing the expression of human papillomavirus E7 oncogene, diindolylmethane blocks hormone-dependent pathological proliferation of HPV-infected cells.
Diindolylmethane is a practically non-toxic drug (LD50 more than 5 g / kg).
Pharmacokinetics
With intravaginal use, diindolylmethane has a high local bioavailability and, at the same time, practically does not enter the systemic circulation.
Diindolylmethane is a practically non-toxic drug (LD50 more than 5 g / kg).
Pharmacokinetics
With intravaginal use, diindolylmethane has a high local bioavailability and, at the same time, practically does not enter the systemic circulation.
Indications
Treatment of dysplasia (cervical intraepithelial neoplasia) of the cervix (regardless of the results of the detection of human papillomavirus infection by PCR).
Composition
One suppository contains: active ingredient: diindolylmethane 100 mg;
excipients: solid fat (Witepsol H-15) (1.9795 g); Crospovidone (Kollidon CL) (0.0200 g); Carmine red dye, E 120 (0.0005 g).
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Dosage and Administration
Intravaginal 100 mg 2 times a day. Duration of treatment is 3-6 months. The duration of treatment is determined by the dynamics of clinical and laboratory parameters.
Recommendations on the method of drug administration:
The drug is introduced into the vagina 2 times a day (morning and evening) and 1 suppository. Immediately before the introduction, you must thoroughly wash your hands. The suppository is inserted deep into the vagina while lying down. After insertion, use of a sanitary pad is recommended.
Adverse reactions
The drug is usually well tolerated by patients. In some cases, the following are listed, usually reversible, adverse events. The adverse events presented below are listed depending on the anatomical and physiological classification and frequency of occurrence. The incidence of side effects is classified by WHO and has gradations: very often (≥1 / 10), often (≥1 / 100 and <1/10), rarely (≥1 / 1000 and <1/100), rarely (≥1 / 10,000 and <1/1000), very rarely (<1/10000), not established.
| Undesirable effects | often (≥1 / 100 and <1/10) | infrequently (≥1 / 1000 and <1/100) |
| Immune system disorders | urticaria, itching | |
| Heart disorders | shortening atrioventricular conduction | |
| Vascular disorders | high blood pressure | |
| Disorders of the gastrointestinal tract | diarrhea | |
| Violations of the skin and subcutaneous tissue | petechial rash on the skin; slow hair growth on the head, body | |
| Disorders of the genitals and breast | discomfort, burning, itching in the vagina; leucorrhea and flocculent discharge from the genital tract | vaginal dryness during sexual contact; delayed menstruation |
| Laboratory and instrumental data | increased activity of aspartate aminotransferase and alanine aminotransferase in the blood plasma; thrombocytopenia and increased erythrocyte sedimentation rate; bacteriuria, leukocyturia, proteinuria, ketonuria | decrease in plasma creatinine concentration; leukocytosis in a cervical smear; vaginal dysbiosis; signs of myocardial hypoxia on an electrocardiogram |
If any of the undesirable reactions indicated in the instruction are manifested or aggravated, or if you notice any other undesirable reactions that are not indicated in the instruction, inform your doctor.
Contraindications
- Individual intolerance to any of the components of the drug.
- Period of pregnancy and breastfeeding.
- Children's age up to 18 years.
Drug interactions
Not studied. Due to the lack of systemic pharmacokinetics, no interaction with systemic drugs is expected. The drug should not be used simultaneously with local preparations for intravaginal use, belonging to the group of antiseptics-oxidizers (potassium permanganate, iodine, hydrogen peroxide).
Special instructions
In the treatment of vaginal infections, the drug should not be used during menstruation, it is advisable to begin treatment after menstruation. During the period of treatment is recommended to refrain from sexual contact. During treatment it is recommended to use contraception.
Influence on ability to drive vehicles and mechanisms
The preparation Cervikon®-DIM does not affect the ability to drive vehicles by means of mechanisms.
Overdosage
Symptoms of an overdose are unknown.
- Brand name: Cervikon -DIM
- Active ingredient: Diindolylmethane
- Manufacturer: Ferrer Internacional S.A.
Studies and clinical trials of Diindolylmethane (Click to expand)
- Zur Reaktion von Tryptophan mit Aldehyden: 2,2′-Diindolylmethane
- Diindolylmethane, 4. Mitt. Säure-katalysierte Kondensation von 3-Methylindol und Tryptophanmethylester mit sterisch anspruchsvollen aromatischen Aldehyden
- Diindolylmethane, 5. Mitt. Chlorwasserstoffkatalysierte Kondensation von Yohimbin mit 4-Dimethylaminobenzaldehyd — Untersuchungen zur Yohimbin-Farbreaktion
- Zur Chemie des Indols, VI. α.β′-Diindolylmethane und -methene. Der Urorosein-Chromophor
- InCl3-HMTA as a Methylene Donor: One-Pot Synthesis of Diindolylmethane (DIM) and Its Derivatives.
- The anticarcinogen 3,3′-diindolylmethane is an inhibitor of cytochrome P-450
- Inactivation of uPA and its receptor uPAR by 3,3′-diindolylmethane (DIM) leads to the inhibition of prostate cancer cell growth and migration
- Down-regulation of uPA and uPAR by 3,3′-diindolylmethane contributes to the inhibition of cell growth and migration of breast cancer cells
- Cell Cycle-Dependent Effects of 3,3′-Diindolylmethane on Proliferation and Apoptosis of Prostate Cancer Cells
- A controlled safety study of diindolylmethane in the immature rat model
- Broccoli-derived phytochemicals indole-3-carbinol and 3,3′-diindolylmethane exerts concentration-dependent pleiotropic effects on prostate cancer cells: Comparison with other cancer preventive phytochemicals
- Eco-friendly synthesis and study of new plant growth promoters: 3,3′-Diindolylmethane and its derivatives
- Structure in solid state of 3,3′-diindolylmethane derivatives, potent cytotoxic agents against human tumor cells, followed X-ray diffraction and 13C CP/MAS NMR analyses
- Novel 3,3′-diindolylmethane derivatives: Synthesis and cytotoxicity, structural characterization in solid state
- SBA-15-supported poly(4-styrenesulfonyl(perfluorobutylsulfonyl)imide) as heterogeneous Brønsted acid catalyst for synthesis of diindolylmethane derivatives
- Induction of G1 and G2/M cell cycle arrests by the dietary compound 3,3'-diindolylmethane in HT-29 human colon cancer cells
- Therapeutic activity of 3,3′-diindolylmethane on prostate cancer in an in vivo model
- Antiandrogenic and growth inhibitory effects of ring-substituted analogs of 3,3′-diindolylmethane (Ring-DIMs) in hormone-responsive LNCaP human prostate cancer cells
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