Desogestrel + Ethinyl estradiol Pharmacology
Desogestrel + Ethinyl estradiol
Desogestrel
Desogestrel is generally used in combination with Ethinyl estradiol. Desogestrel is a potent inhibitor of ovulation. It binds to the Progesterone receptor situated in the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, Desogestrel will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge.
Distribution: It is distributed mainly in protein bound form.
Metabolism: Desogestrel is rapidly and completely metabolized by hydroxylation.
2. Nausea
3. Vomiting
4. Abdominal pain
5. Headache
6. Dizziness
7. Fatigue
8. Depression
2.Thromboembolic disorders
3.Coronary artery disease
4.Carcinoma of the breast
5.Carcinoma of the endometrium
6.Undiagnosed abnormal genital bleeding
7.Cholestatic jaundice
8.Hepatic adenomas
2. Migraine
3. High blood pressure
4. Mental depression
5. Cardiovascular disorders
6. Diabetes mellitus
7. Seizures
Adult(Female): 0.15mg/day for 21 days (starting from 5th day of menstruation)
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.
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