Gestodene + Ethinyl Estradiol Pharmacology

Gestodene + Ethinyl Estradiol

About Gestodene + Ethinyl Estradiol
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Mechanism of Action of Gestodene + Ethinyl Estradiol
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Pharmacokinets of Gestodene + Ethinyl Estradiol
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Onset of Action for Gestodene + Ethinyl Estradiol
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Duration of Action for Gestodene + Ethinyl Estradiol
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Half Life of Gestodene + Ethinyl Estradiol
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Side Effects of Gestodene + Ethinyl Estradiol
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Contra-indications of Gestodene + Ethinyl Estradiol
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Special Precautions while taking Gestodene + 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 Gestodene + Ethinyl Estradiol
Oral Contraception
Interactions for Gestodene + Ethinyl Estradiol
Concurrent use with hepatic enzyme inducers reduces the contraceptive efficacy
Broad-spectrum antibiotics may also reduce the efficacy of the oral contraceptive
May increase plasma concentrations of ciclosporin and decrease the serum levels of lamotrigine
Typical Dosage for Gestodene + Ethinyl Estradiol
One tablet is taken every day for 21 days and you then have a seven day break from pill-taking. During your seven day break, the levels of the hormones in your blood drop, which results in a withdrawal bleed that is similar to your normal period. You start the next pack after the seven pill-free days are up, even if you are still bleeding
Schedule of Gestodene + Ethinyl Estradiol
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Storage Requirements for Gestodene + Ethinyl Estradiol
Stored in a well closed container. Keep out of the reach of children
Effects of Missed Dosage of Gestodene + Ethinyl Estradiol
N/A
Effects of Overdose of Gestodene + Ethinyl Estradiol
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Gestodene

About Gestodene
Hormonal contraceptive, Synthetic Progesterone
Mechanism of Action of Gestodene
It is a progestin derivative its action through nuclear progesterone receptor situated in female genital tract, breast, CNS, and pituitary.It inhibit growth hormone release from pituitary.It suppress ovulation.It also disrupts fertilization and inhibits implantation
Pharmacokinets of Gestodene
Absorption: Absorbed after oral administration
Distribution: Extensively bound to plasma proteins (75-87% to sex hormone binding globulin, and 13-24% to albumin)
Metabolism: Metabolised via hepatically
Excretion: Excreted mainly through urine
Onset of Action for Gestodene
N/A
Duration of Action for Gestodene
N/A
Half Life of Gestodene
16 to 18 hrs
Side Effects of Gestodene
1.GI disturbances
2.Changes in appetite or wt
3.Fluid retention
4.Oedema
5.Acne
6.Chloasma (melasma)
7.Allergic skin rashes
8.Urticaria
9.Mental depression
10.Breast changes including discomfort or occasionally gynaecomastia
Contra-indications of Gestodene
1.Breast cancer
2.Circulatory system diseases
3.Genital bleeding
4.Disturbance of lipid metabolism
Special Precautions while taking Gestodene
1.CV or renal impairment
2.Asthma
3.Epilepsy and migraine
4.Depression
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
N/A
Children Related Information
Contraindicated
Indications for Gestodene
1.Contraception
2.Menopausal HRT
Interactions for Gestodene
Carbamazepine, Griseofulvin, Phenobarbital, Phenytoin, and Rifampicin may reduce the effectiveness of gestodene
Gestodene may inihibit ciclosporin metabolism
Typical Dosage for Gestodene
Contraception: 75 mcg daily in monophasic preparations, 50-100 mcg daily in triphasic preparations
Menopausal HRT: 25 or 50 mcg daily for 12 days of a 28-day cycle
Schedule of Gestodene
H
Storage Requirements for Gestodene
Stored in a well closed container in below 25 degree celcius. Protect from moisture. Keep out of the reach of children
Effects of Missed Dosage of Gestodene
N/A
Effects of Overdose of Gestodene
N/A

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
N/A
Duration of Action for Ethinyl estradiol
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Half Life of Ethinyl estradiol
N/A
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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