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Cyproterone

Bayer Pharma AG
1533 Items
2019-09-19
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Clinical Pharmacology

Androcur - antiandrogenic, gestagennoe.

Pharmacodynamics

Oral anti-androgenic drug. Inhibits the effects of male sex hormones (androgens), in small amounts also produced by the woman’s body. It has a gestagenic, antiandrogenic and antigonadotropic action.

In men, while taking the drug, there is a weakening of sexual desire and potency, as well as a decrease in the function of the testes. These changes disappear after cessation of treatment. The drug reduces or completely eliminates the effect of androgens on the target organs (including the prostate gland).

In women, while taking Androcur, both pathologically excessive hair growth on the face and body, and hair loss caused by androgens, is reduced. In addition, the increased function of the sebaceous glands is reduced and ovarian function is inhibited during the treatment period.

Pharmacokinetics

Suction

After taking the drug inside cyproterone acetate is completely absorbed from the gastrointestinal tract. After taking 10 mg Cmax is reached in 1.5 hours and is 75 ng / ml, after taking 50 mg - 140 mg / ml. After taking the pill 100 mg Cmax reaches an average of 2.8 ± 1.1 hours. Bioavailability is 88%.

Distribution and metabolism

Plasma protein binding is about 96%. Biotransformed in the liver by hydroxylation and conjugation, the main metabolite, as determined in human plasma, is a 15β-hydroxyl derivative.

Removal

T1/2 for pills of 10 mg and 50 mg, it is equal to 43.9 ± 12.8 hours; for 100 mg, it is 42.8 ± 9.7 hours. It is excreted in bile and urine mainly as metabolites in the ratio 3: 7.

Indications

Manifestations of moderate androgenization in women, such as:

  • moderate hirsutism (pathological body hair of the face and body of moderate severity);
  • moderate androgenic alopecia (moderately severe baldness due to androgens);
  • severe and moderate forms of acne (acne), accompanied by inflammation, nodulation or the risk of scarring, and seborrhea.

Composition

1 tablet contains:

Active substances: cyproterone acetate, micro 20 - 10 mg;

Excipients: lactose monohydrate - 63.4 mg, corn starch - 44 mg, povidone 25 000 - 1.35 mg, colloidal micronized silicon dioxide - 1 mg, magnesium stearate - 0.25 mg.

Cyproterone is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Androcur Bayer Pharma AG Germany pills
Cyproterone-Teva Teva Israel pills

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Cyproterone

Dosage and Administration

Standard Dosing for the Treatment of Retinitis CMV 
Initial therapy:IV infusion at a dose of 5 mg / kg for 1 hour, every 12 hours (10 mg / kg / day) for 14-21 days (for patients with normal renal function).
Maintenance Therapy:at 5 mg / kg by intravenous infusion for 1 hour, daily for 7 days a week, or at 6 mg / kg body weight daily for 5 days a week.

Standard dosage for prophylaxis in patients after transplantation 
Initial therapy:IV infusion at a dose of 5 mg / kg for 1 hour, every 12 hours, for 7-14 days (for patients with normal renal function).
Maintenance Therapy:5 mg / kg by intravenous infusion for 1 hour, daily for 7 days a week, or 6 mg / kg body weight daily for 5 days a week.

Adverse reactions

HIV-infected patients
Clinical adverse events that occurred in 2% of patients who received intravenous ganciclovir, regardless of their causal relationship with the drug and severity:
from the blood system and lymphatic system:neutropenia, anemia, thrombocytopenia, leukopenia, lymphadenopathy;
on the part of the digestive system:diarrhea, abdominal pain, dysphagia, esophageal candidiasis;
organism as a whole:fever, candidiasis, infections at the injection site, sepsis, secondary sepsis, anorexia, mycobacteriosis (mycobacterium avium), pain of different localization, chest pain, bacteremia;
from the central and peripheral nervous system:hypoesthesia, anxiety;
from skin and its appendages:itching;
on the part of the respiratory system:cough, pneumocystic pneumonia, cough with sputum, congestion in the paranasal sinuses;
laboratory values:increased activity of alkaline phosphatase in the blood, increased levels of creatinine in the blood, neutropenia, anemia, thrombocytopenia, increased levels of creatinine;
from the musculoskeletal system:arthralgia.

Patients after transplantation

Clinical adverse events that were observed in ≥ 5% of patients who received ganciclovir intravenously for the treatment or prevention of manifest CMV infection after bone marrow transplantation, regardless of their causal relationship with the drug and severity:
on the part of the blood-forming organs:pancytopenia, leukopenia;
organism as a whole:mucosal lesions, fever, tremors, sepsis, anorexia, swelling of the face;
on the part of the digestive system:diarrhea, dyspepsia;
laboratory values:increased creatinine, liver transaminase activity, hypomagnesemia, hypocalcemia, hypokalemia;
nervous system:headache, tremor, confusion;
from the skin and its appendages:exfoliative dermatitis;
on the part of the respiratory system:rhinitis, shortness of breath;
on the part of the cardiovascular system:tachycardia, hypotension;
from the organs of the urogenital tract:hematuria;
senses:bleeding in the eye;
musculoskeletal system:myalgia

Clinical adverse events that occurred in ≥ 5% of patients who received intravenous ganciclovir after a heart transplant, regardless of the causal relationship with the drug or the severity of:
The body as a whole:infections (18%).
Metabolism and nutrition disorders:swelling (9%).
Central and peripheral nervous system:headache (18%), confusion (5%), peripheral neuropathy (7%).
Respiratory system:pleural effusion (5%).
The cardiovascular system:arterial hypertension (20%).
Genitourinary tract:deterioration of renal function (14%), renal failure (12%).

Due to the high bioavailability of intravenously administered ganciclovir, it cannot be ruled out that the same adverse effects can be observed with intravenous administration of the drug, as in studies with oral administration of ganciclovir.

To fully characterize the safety profile of intravenously administered ganciclovir, the following are the relevant adverse events identified with greater frequency when orally taking ganciclovir in HIV-infected or patients after organ transplantation, regardless of their severity and causal relationship with the drug.Some undesirable effects when taking oral ganciclovir may be associated with this method of taking the drug.
Blood system and lymphatic system:leukocytosis.
Digestive organs:constipation, cholangitis, flatulence, vomiting.
The body as a whole:ascites, asthenia, bleeding, bacterial, fungal and viral infections, malaise.
The cardiovascular system:vasodilation (decrease in blood pressure, redness of the skin of the face).
Central and peripheral nervous system:depression, dizziness, insomnia.
Liver and biliary tract:cholestatic jaundice.
Leather:increased sweating.
Sense organs:amblyopia, taste disturbances.
Metabolism and nutrition disorders:diabetes mellitus, hyponatremia, hypoproteinemia, weight loss.

Other adverse events

The following are significant adverse events that were not mentioned above, because did not meet the inclusion criteria (less than 2%).
Blood system and lymphatic system:aplastic anemia, myelosuppression, eosinophilia.
Digestive organs:gastrointestinal bleeding, belching, fecal incontinence, ulcerative stomatitis, pancreatitis, glossitis.
Infections:episodes of infections caused by inhibition of the bone marrow and immune system (local and systemic infections and sepsis).
Bleeding:potentially life-threatening bleeding due to thrombocytopenia.
The body as a whole:cachexia, dehydration, weakness, thrombosis at the injection site, abscess at the injection site, edema at the injection site, pain at the injection site, hemorrhage at the injection site, malaise, photosensitivity reactions.
Central and peripheral nervous system:excitement, convulsions, hallucinations, psychosis, thought disorder, "nightmarish" dreams, ataxia, coma, dry mouth, euphoria, nervousness, drowsiness.
Skin and its appendages:dermatitis, acne, alopecia, herpes simplex, urticaria.
Sense organs:retinal detachment, visual impairment, blindness, hearing loss, pain in the eyeball, glaucoma, vitreous destruction.
Laboratory indicators:increased activity of creatine phosphokinase and lactate dehydrogenase in the blood, hypoglycemia.
Genitourinary tract:frequent urination.
The cardiovascular system:arrhythmias (including ventricular), deep vein thrombophlebitis, migraine, phlebitis.
Musculoskeletal system:myasthenic syndrome.

Hypersensitivity to Cymevene®u, valganciclovir or any other component of the drug.
Because of the similarity of the chemical structure of Cymevene® and acyclovir and valacyclovir, cross-hypersensitivity reactions are possible between these drugs.
The absolute neutrophil count is less than 500 cells in 1 mcl, or the platelet count is less than 25,000 cells in 1 mcl, or the hemoglobin level is less than 8 g / dl.
Children's age up to 12 years.

Drug interactions

Interactions with the intravenous administration of ganciclovir

The degree of binding of ganciclovir with plasma proteins is only 1-2%, therefore, interactions caused by the displacement of drugs from the sites of communication with proteins should not be expected.

Didanosine:It was found that with the simultaneous administration of didanosine and intravenous or oral administration of ganciclovir, didanosine plasma concentrations steadily increase. With intravenous administration of ganciclovir in doses of 5–10 mg / kg per day, the AUC of didanosine increased by 38–67%. This increase cannot be explained by a change in the tubular secretion of the drug, since the percentage of didanosine excretion has increased. This increase in AUC can be caused either by increased bioavailability or a decrease in metabolic rate. There were no clinically significant changes in the concentrations of ganciclovir. However, given the increased plasma concentrations of didanosine in the presence of ganciclovir, patients should be carefully monitored for the toxicity of didanosine.

Imipenem / Cilastatin:convulsions were observed in patients simultaneously receiving ganciclovir and imipenem / cilastatin. These drugs should be prescribed in combination with Cymevene only if the possible benefits exceed the risk.

Mycophenolate mofetil:co-administration of these drugs, potentially competing with tubular secretion, may lead to an increase in the concentration of ganciclovir and mfcc (phenolic glucuronide mycophenolic acid). Significant changes in the pharmacokinetics of mycophenolic acid (MPA) are not expected, adjusting the dose of mycophenolate mycophenolate is not required. In patients with impaired renal function, who simultaneously receive ganciclovir and MMF, it is necessary to follow the recommendations for dosing ganciclovir and conduct careful monitoring.

Other possible drug interactions 
Perhaps increased toxicity in the appointment of ganciclovir concurrently with other drugs with myelosuppressive effects or impaired renal function (such as dapsone, pentamidine, flucytosine, vincristine, vinblastine, adriamycin, amphotericin B, nucleoside analogues and hydroxyurea). Therefore, these drugs should be prescribed simultaneously with ganciclovir only if the potential benefits outweigh the potential risks.

Pregnancy and Lactation

During treatment with ganciclovir, women of childbearing age should be advised to use reliable methods of contraception. Men are advised to use a barrier method of contraception during treatment and for at least 90 days after its termination.
In animal studies revealed the teratogenicity of the drug. Safety of ganciclovir during pregnancy in humans has not been established. Administration of the drug to pregnant women should be avoided, unless the potential positive effect for the mother does not exceed the possible risk to the fetus.
Peri- and postnatal development after exposure to ganciclovir has not been studied, but it cannot be ruled out that ganciclovir can be eliminated with milk and cause serious adverse reactions in an infant. Therefore, the decision to discontinue the drug or to discontinue breastfeeding should be made taking into account the potential positive effect of ganciclovir on a nursing mother.

Special instructions

Ganciclovir has a potential teratogenic and carcinogenic effect can cause congenital malformations and malignant neoplasms. Ganciclovir may temporarily or firmly inhibit spermatogenesis (see "Pregnancy" and "Side Effects").
Cases of severe leukopenia, neutropenia, anemia, thrombocytopenia, pancytopenia, myelosuppression and aplastic anemia were observed in patients taking ganciclovir. Do not start treatment with ganciclovir if the absolute number of neutrophils is less than 500 cells in 1 μl, or the number of platelets is less than 25,000 cells in 1 μl, or the hemoglobin level is less than 8 g / dl (see "Dosing Special Instructions" and "Side Effects" ).
During treatment, it is recommended to monitor the unfolded blood count, including platelet count. In patients with severe leukopenia, neutropenia, anemia and / or thrombocytopenia, treatment with hematopoietic growth factors is recommended and / or temporary interruption of drug therapy.
In case of impaired renal function, it is recommended to adjust the dose of the drug depending on creatinine clearance.
In patients taking imipenem / cilastatin and ganciclovir, the development of seizures has been described, so ganciclovir should not be administered concomitantly with imipenem / cilastatin, unless the potential benefits of therapy exceed the potential risk (see "Drug Interactions").
Both ganciclovir and zidovudine can cause neutropenia and anemia, so some patients may not tolerate the simultaneous use of these drugs in full doses (see"Drug Interactions").
While taking ganciclovir, didanosine plasma concentrations can increase, so these patients should be carefully monitored for the toxicity of didanosine (see "Drug Interactions"). The simultaneous intake of ganciclovir and drugs with myelosuppressive or nephrotoxic effects can lead to the development of additive toxicity.

Overdosage

With an overdose in some cases, no adverse events have occurred. Most patients had one or more of the following adverse events:
Hematologic toxicity:pancytopenia, myelosuppression, bone marrow aplasia, leukopenia, neutropenia, granulocytopenia.
Hepatotoxicity:hepatitis, abnormal liver function.
Nephrotoxicity:hematuria increase in a patient with already existing kidney damage, acute renal failure, increased creatinine level.
Gastrointestinal toxicity:abdominal pain, diarrhea, vomiting.
Neurotoxicity:generalized tremor, convulsions.

In addition, an excess volume of intravenous ganciclovir solution was injected intravitally into one adult, after which he developed a temporary loss of vision and occlusion of the central retinal artery due to an increase in intraocular pressure caused by the injected fluid volume.

Hemodialysis and hydration can be used to reduce the plasma level of ganciclovir in oral overdose of Cymeven.

  • Brand name: Cymevene®
  • Active ingredient: Ganciclovir
  • Dosage form: Lyophilisate for preparation of solution for infusions.
  • Manufacturer: Hoffmann la roch
  • Country of Origin: Switzerland

Studies and clinical trials of Cyproterone (Click to expand)

  1. Cleavage of poly(ADP-ribose) transferase during p53-independent apoptosis in rat liver after treatent with N-nitrosomorpholine and cyproterone acetate
  2. Cyproterone acetate in advanced male breast cancer
  3. Cyproterone acetate in the treatment of metastatic cancer of the male breast
  4. Combined treatment with buserelin and cyproterone acetate in metastatic male breast cancer
  5. Luteinizing hormone-releasing hormone agonists in prostate cancer. Elimination of flare reaction by pretreatment with cyproterone acetate and low-dose diethylstilbestrol
  6. Cyproterone acetate–-mechanism of action and clinical effectiveness in prostate cancer treatment
  7. A further analysis of european organization for research and treatment of cancer protocol 30805. Orchidectomy versus orchidectomy plus cyproterone acetate versus low-dose diethylstilbestrol
  8. Short-term versus long-term addition of cyproterone acetate to buserelin therapy in comparison with orchidectomy in the treatment of metastatic prostate cancer
  9. Effects of neonatal cyproterone acetate administration on isolation-induced fighting behavior and mounting behavior in male and female TO strain albino mice
  10. Effects of neonatal treatment with cyproterone acetate on aggressive behavior induced by footshock in adult male rats
  11. Fine structure of the testis and epididymis of rats treated with cyproterone acetate
  12. Direct action upon avian target organs by the antiandrogen cyproterone acetate
  13. Alterations in the fine structure of the prostate and seminal vesicle of rats treated with cyproterone acetate
  14. Effect of cyproterone acetate on structure and function of rhesus monkey reproductive organs
  15. Effect of Prolactin and Bromocriptine on the Population of Prostate Neuroendocrine Cells from Intact and Cyproterone Acetate-Treated Rats: Stereological and Immunohistochemical Study
  16. Effect of Prolactin on the Population of Epithelial Cells From Ventral Prostate of Intact and Cyproterone Acetate-Treated Peripubertal Rats: Stereological and Immunohistochemical Study
  17. Hormonal modulation in systemic lupus erythematosus. Preliminary clinical and hormonal results with cyproterone acetate
  18. Efficient Synthesis of 16α-Methyl Cyproterone Acetate.
  19. The First Syntheses of 16β-Chloro- and 16β-Bromo-cyproterone Acetate.
  20. Effect of cyproterone acetate and conjugated estrogens on the human insulin receptor
  21. Normalization of sexual behaviour in a female with dementia after treatment with cyproterone
  22. The antiandrogen cyproterone acetate induces synthesis of transforming growth factor β1 in the parenchymal cells of the liver accompanied by an enhanced sensitivity to undergo apoptosis and necrosis without inflammation
  23. Liver cell proliferation induced by nafenopin and cyproterone acetate is not associated with increases in activation of transcription factors NF-κB and AP-1 or with expression of tumor necrosis factor α
  24. Effect of antiandrogen cyproterone acetate on the development of the antler cycle in Southern pudu (Pudu puda)

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