Cyproterone + Ethinyl estradiol Pharmacology

Cyproterone + Ethinyl estradiol

About Cyproterone + Ethinyl estradiol
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Mechanism of Action of Cyproterone + Ethinyl estradiol
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Pharmacokinets of Cyproterone + Ethinyl estradiol
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Onset of Action for Cyproterone + Ethinyl estradiol
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Duration of Action for Cyproterone + Ethinyl estradiol
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Half Life of Cyproterone + Ethinyl estradiol
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Side Effects of Cyproterone + Ethinyl estradiol
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Contra-indications of Cyproterone + Ethinyl estradiol
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Special Precautions while taking Cyproterone + Ethinyl estradiol
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Pregnancy Related Information
Contraindicated
Old Age Related Information
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Breast Feeding Related Information
Contraindicated
Children Related Information
N/A
Indications for Cyproterone + Ethinyl estradiol
Cyproterone competitively inhibits the effect of androgen at the target organs. The Ethinyl estradiol inhibits ovulation and changes the cervical mucus and the endometrium rendering them unfavourable for sperm penetration and nidation of a fertilised ovum, respectively.
1.Androgen-dependent acne
2.Androgen-dependent alopecia
3.Hirsutism mild forms
4.Oral contraceptive
Interactions for Cyproterone + Ethinyl estradiol
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Typical Dosage for Cyproterone + Ethinyl estradiol
Adult: 1tablet / day. The first course is started on the 1st day of the menstrual cycle. Usually it contains 21 hormone tablets and 7 non-hormonal tablets. Continue for 3 - 4 cycles
Schedule of Cyproterone + Ethinyl estradiol
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Storage Requirements for Cyproterone + Ethinyl estradiol
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Effects of Missed Dosage of Cyproterone + Ethinyl estradiol
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Effects of Overdose of Cyproterone + Ethinyl estradiol
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Cyproterone

About Cyproterone
A synthetic derivative of 17-hydroxyprogesterone, androgen receptor antagonist, Antiandrogen.
Mechanism of Action of Cyproterone
The drug exerts its action by acting as an anti-androgen. It blocks the normal activity of the androgen by competing with dihydrotestosterone for the intracellular androgen receptor sites and inhibits it`s binding. It also has mild progestational activity. Being structurally similar to testosterone it itself attaches to surface receptors in prostate cancer cells and thus blocks the attachment of testosterone.
Pharmacokinets of Cyproterone
Absorption: Well absorbed orally, Distribution: Distributed in the body preferentially in to fatty tissue. Distribution: Metabolism: Metabolized in to inactive metabolites in the body. Excretion: Drug is excreted as unchanged drug mainly through(about 60%) faeces and also through urine
Onset of Action for Cyproterone
N/A
Duration of Action for Cyproterone
N/A
Half Life of Cyproterone

40 hours
Side Effects of Cyproterone
1. Impotence
2. Decreased libido
3. Inhibition of spermatogenesis
4. Benign nodular hyperplasia of the breast
5. Gynaecomatia
6. Depression
7. Dry skin
8. Oedema
9. Hepatitis
10. Altered liver function tests
11. Nausea
12. Vomiting
13. Diarrhoea
14. Constipation
15. Exercise induced dyspnoea
16. Altered carbohydrate metabolism
17. Fatigue
18. Weakness
19. Lethargy
20. Hypercalcaemia.
Contra-indications of Cyproterone
1.Hypersensitivity to the drug
2.Hepatic impairment.
Special Precautions while taking Cyproterone
1.Monitor liver function before and periodically during therapy and stops the therapy if there is hepatic toxicity.
2.Depression
3.Renal impairment
4 Diabetes mellitus
5.Malignancy
6.Sickle cell anaemia
7.Thromboembolic disorders
8.Wasting disease.
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Contraindicated
Indications for Cyproterone
1. Contraception
2. Hirsutism
3. Male to female transsexuals
4. Hyper sexuality
5. Prostate cancer
Interactions for Cyproterone
N/A
Typical Dosage for Cyproterone
Oral:
Contraception: 2mg Cyproterone along with 35 to 50 mg ethenyl estradiol taken once daily for 21 days followed by 7days tablet free interval.
Hirsutism, Male to female transsexuals, hyper sexuality: 25 to 50mg/day.Maximum dose: 100mg/day
For treatment of women in child bearing age Cyproterone usually combines with oral contraceptive pills:
Hirsutism usual dosage is Cyproterone acetate 50mg twice daily for 10days from 5th day of menstrual cycle and contraceptive pills from 5thday to 21 days followed by a tablet free period of 7days.
Prostate cancer: 100 to 200mg/day in two to three divided doses taken after meals.
I.M.:
Prostate cancer: 300mg once weekly,
Schedule of Cyproterone
N/A
Storage Requirements for Cyproterone
Store at room temperature at a range of 15 to 30 degree C.in a well closed container.Protects from direct sunlight and moisture. Keep out of reach of children.
Effects of Missed Dosage of Cyproterone
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Cyproterone
Provide symptomatic treatment and supportive measures.

Ethinyl estradiol

About Ethinyl estradiol
Synthetic Estrogen(a derivative of estradiol), In Combined oral contraceptive,Anti neoplastic.
Mechanism of Action of Ethinyl estradiol
The drug exerts it`s pharmacological action by binding to specific nuclear estrogen receptors present in target cells and regulating protein synthesis and thus producing desired therapeutic effects. Estrogen receptors are found in female sex organs, breast, pituitary, liver, bone, blood vessels, heart, CNS, hormone sensitive breast carcinoma cells, hormone responsive prostate carcinoma cells. Agonist binding to ligand binding domain of these receptors results in receptor dimerization and interaction with "estrogen response elements" of target genes and thus promotes gene transcription; through certain coactivator proteins which ultimately leads to modification of protein synthesis.
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.
Pharmacokinets of Ethinyl estradiol
Absorption: Well absorbed orally, but substantially inactivated by liver.
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.
Onset of Action for Ethinyl estradiol
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Duration of Action for Ethinyl estradiol
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Half Life of Ethinyl estradiol
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Side Effects of Ethinyl estradiol
1. Urticaria
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
Contra-indications of Ethinyl estradiol
1. Thrombophlebitis
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.
Special Precautions while taking Ethinyl estradiol
1. Cerebrovascular diseases
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
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Contraindicated
Indications for Ethinyl estradiol
1. Female hypogonadism
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.
Interactions for Ethinyl estradiol
ACE Inhibitors: Antagonises hypotensive effect.
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.
Typical Dosage for Ethinyl estradiol
Oral : 0.02 to 0.2mg/day
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.
Schedule of Ethinyl estradiol
H
Storage Requirements for Ethinyl estradiol
Store at controlled room temperature at a range of 20 to 25 degree C.
Effects of Missed Dosage of Ethinyl estradiol
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Ethinyl estradiol
Provide symptomatic treatment and supportive care.

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