Ethinyl estradiol + Methyl testosterone Pharmacology
Ethinyl estradiol + Methyl testosterone
Ethinyl estradiol
It causes growth and development of female sex organs, maintains proper female sexual functioning. It exerts week anabolic action, and also maintains bone mass primarily by preventing bone resorption. It inhibits osteoclast pit formation and increases the expression of bone matrix proteins and also improves lipid profile (rises HDL and lowers LDL levels). It inhibits growth of hormone responsive carcinoma cells in prostate cancer and certain breast cancer.
Distribution: Extensively distributed in the body with highest levels in the fatty tissue. About 50% to 80% is plasma protein bound.
Metabolism: Metabolized primarily in liver by glucuronide and sulfate conjugation.
Excretion: Excreted through urine as sulfate or glucuronide conjugates.
2. Pruritus
3. Irritations of skin
4. Feminization in males
5. Gynaecomastia(male)
6. Breakthrough bleeding
7. Breast tenderness
8. Breast enlargement
9. Gastrointestinal disturbances
10. Nausea
11. Vomiting
12. Pancreatitis
13. Headache
14. Dizziness
15. Seizures
16. Thrombophlebitis
17. Thromboembolism
18. Hypertension
19. Oedema
20. Increased risk of endometrial cancer
21. Increased risk of breast cancer
22. Increased risk of Cerebrovascular accident
23. Pulmonary embolism
24. Myocardial infarction
25. Cholestatic jaundice
26. Hepatic adenoma
2. Thromboembolic disorders
3. Estrogen dependent neoplasia
4. Undiagnosed genital bleeding
5. Estrogen dependent breast carcinoma
6. Hepatic impairment
7. Endometrial hyperplasia
8. Severe hypertension
9. Cholestatic jaundice
10. Dubin Johnson syndrome
11. Rotor syndrome
12. Haemoglobinopathies
13. Porphyria.
2. Coronary artery diseases
3. Migraine
4. Epilepsy
5. Heart failure
6. Hypertension
7. Diabetes mellitus
8. Renal impairment
9. Fibrocystic disease of breast
10. Abnormal mammographic findings
11. Asthma
2. Vasomotor menopausal symptoms
3. Menstrual disturbances
4. Certain cases of amenorrhoea
5. Male hyper sexuality
6. Mammary hypoplasia
7. Palliative treatment of certain breast cancer
8. Palliative treatment of prostatic cancer.
Anti-coagulants: Efficacy of anticoagulants reduced.
Antidiabetics: Antagonism of hypoglycaemic effect.
TCAs: Pharmacological effects of TCAs altered, increased incidence of toxicity.
Antifungals: Griseofulvin accelerates metabolism of ethinyl oestradiol, reduced contraceptive effect.
Barbiturates, Rifampicin: Efficacy of ethinyloestradiol reduced; failure of contraception.
Beta blockers: Hypotensive action antagonised.
Corticosteroids: Clearance reduced and elimination half-life of corticosteroids increased.
Cyclosporine: Increased plasma cyclosporine concentration.
Dantrolene: Hepatotoxicity, especially in women > 35 yrs of age.
Lab. Tests: With high doses of ethinyloestradiol: Increased Sulfobromophthalein retention. Increased Prothrombin and factors VII, VIII, IX & X; decreased antithrombin III; increased norepinephirine :induced platelet aggregability. Increased thyroid binding globulin (TBG) leading to increased circulating total thyroid hormone, as measured by PBI, T4 by column or T4 by radioimmuno assay. Free T3 resin uptake decreased, reflecting elevated TBG; Free T4 concentration unaltered. Impaired glucose tolerance, decreased pregnanediol excretion, reduced serum folate concentration, increased serum triglyceride and phospholipid concentration.
Female hypogonadism: 0.05mg 1 to 3 times daily for two weeks monthly followed by two week progesterone therapy. Continue for 3 to 6month dosing cycles followed by two months off.
Maintenance dosage: 0.025mg/day
Vasomotor menopausal symptoms: 0.025 to 0.05mg/day cyclically as 3 weeks on and 1 week off.
Mammary hypoplasia: 0.05mg/day for 12 days along with progesterone from 16th to 25th day.
Male hyper sexuality: 0.05mg/day
Palliative treatment of breast cancer: 1mg thrice daily for 3 months
Palliative treatment of prostatic cancer: 0.15mg to 2mg/day.
Methyl testosterone
Methyl testosterone is combined with various estrogen to treat menopausal symptoms, dysmenorrhea, menorrhagia, osteoporosis and to suppress post partum lactation.
2.Hypernatreamia
3.Hyperkalaemia
4.Hyperphosphataemia
5.Impaired glucose tolerance
6.Altered thyroid function tests
7.Retention of water
8.Weight gain
9.Oedema
10.Abnormal liver function tests
11.Cholestatic jaundice
12.Hepatic carcinoma
13.Gynaecomastia
14.Hypo estrogenic effects in females
15.Flushing
16.Diaphoresis
17.Vaginitis
18.Menstrual irregularities
19.Androgenic effects in women
20.Hirsutism
21.Excessive hormonal effects in men
22.Premature epiphyseal closure
23.Acne
24.Priapism
25.Increased libido
26.Testicular atrophy
27.Oligospermia
28.Allergic manifestations
29.Pin and induration at injection site
30.Headache
31.Anxiety
32.Depression
33.Sleep apnea
2.Male breast cancer
3.Overt cardiac failure
4.Severe hepatic impairment
5.Severe renal impairment
6.Hypercalcaemia
2.Hepatic impairment
3.Cardiovascular disorders
4.Epilepsy
5.Migraine
6.Discontinue Transdermal system if oedema occurs
7.Women of child bearing age
2.Delayed puberty in males
3.Infertility
4.Post partum breast pain
5.Carcinoma of breast
Replacement therapy in androgen-deficient males: 10 to 50 mg daily.
Breast carcinoma in females: 50-200 mg daily
Postpartum Breast Pain and Engorgement: 80 mg daily for 3-5 days after parturition.
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