Levonorgestrel + Ethinyl estradiol Pharmacology

Levonorgestrel + Ethinyl estradiol

About Levonorgestrel + Ethinyl estradiol
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Mechanism of Action of Levonorgestrel + Ethinyl estradiol
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Pharmacokinets of Levonorgestrel + Ethinyl estradiol
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Onset of Action for Levonorgestrel + Ethinyl estradiol
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Duration of Action for Levonorgestrel + Ethinyl estradiol
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Half Life of Levonorgestrel + Ethinyl estradiol
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Side Effects of Levonorgestrel + Ethinyl estradiol
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Contra-indications of Levonorgestrel + Ethinyl estradiol
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Special Precautions while taking Levonorgestrel + Ethinyl estradiol
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Pregnancy Related Information
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Old Age Related Information
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Breast Feeding Related Information
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Children Related Information
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Indications for Levonorgestrel + Ethinyl estradiol
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Interactions for Levonorgestrel + Ethinyl estradiol
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Typical Dosage for Levonorgestrel + Ethinyl estradiol
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Schedule of Levonorgestrel + Ethinyl estradiol
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Storage Requirements for Levonorgestrel + Ethinyl estradiol
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Effects of Missed Dosage of Levonorgestrel + Ethinyl estradiol
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Effects of Overdose of Levonorgestrel + Ethinyl estradiol
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Levonorgestrel

About Levonorgestrel
A synthetic Progestagen . Hormonal contraception.
Mechanism of Action of Levonorgestrel
It is a progestin derivative exerts it`s action through nuclear progesterone receptors situated in female genital tract, breast, CNS, and pituitary. When the drug binds to progesterone receptors it undergoes dimerisation and attaches to progesterone response element of target genes and regulates transcription through coactivators. It inhibits growth hormone release from pituitary by reinforcement of normal feedback inhibition. It reduces frequency of LH secretary pulses, attenuate LH surge, and suppresses ovulation. It causes thickening of cervical mucous and induces sloughing of the endometrium. It also disrupts fertilization and inhibits implantation.
Pharmacokinets of Levonorgestrel
Absorption: Well absorbed orally and bioavailability is about 100%.Distribution: Distributed in to the target sites in a protein bound form. Metabolism: Undergoes partial metabolism in liver.Excretion: Drug and it`s metabolites are excreted mainly through urine and a small portion is excreted in faeces.
Onset of Action for Levonorgestrel
N/A
Duration of Action for Levonorgestrel
N/A
Half Life of Levonorgestrel
N/A
Side Effects of Levonorgestrel
1. Breast tenderness
2. Nausea
3. Vomiting
4. Abdominal pain
5. Headache
6. Dizziness
7. Fatigue
8. Depression
Implants:
1. Breast tenderness
2. Nausea
3. Vomiting
4. Abdominal pain
5. Headache
6. Dizziness
7. Fatigue
8. Depression
9. Tingling
10. Numbness
11. Amenorrhoea
12. Irregular bleeding
13. Prolonged bleeding
14. Spotting
15. Cervicitis
16. Vaginitis
17. Leucorrhoea
18. Brest discharge
19. Decreased thyroxin levels
20. Weight gain
21. Mastalgia
22. Musculoskeletal pain
23. Dermatitis
24. Acne
25. Hirsutism
26. Alopecia
27. Itching



Contra-indications of Levonorgestrel
Oral:
1. Hypersensitivity to the drug
2. Undiagnosed genital bleeding
Implants:
1. Hypersensitivity to the drug or implant system
2. Undiagnosed genital bleeding
3. Thrombophlebitis
4. Thromboembolic disorders
5. Intracranial hypertension
6. Breast cancer
7. Liver tumors
8. Acute hepatic diseases
Special Precautions while taking Levonorgestrel
1. Emergency contraceptive method should not replace normal contraceptive method
2. Use implants preferably in women who already have one child
3. Avoid use of implants in pelvic inflammatory diseases
4. Hepatic impairment
5. Cardiovascular disorders
6. Diabetes mellitus
7. Seizures
8. Mental depression
9. Migraine
10. High blood pressure
Pregnancy Related Information
Contraindicated
Old Age Related Information
N/A
Breast Feeding Related Information
Use with caution
Children Related Information
Contraindicated
Indications for Levonorgestrel
1. Emergency contraception
2. Long term prevention of pregnancy (up to 5years)
Interactions for Levonorgestrel
Simultaneous administration of certain anticonvulsant drugs (phenobarbital, phenytoin, primidone, carbamazepine, certain antibiotics such as rifabutin, rifamycin and griseofulvin) can reduce or suppress the effectiveness of emergency contraception.

Typical Dosage for Levonorgestrel
Oral:
Emergency contraception: 750mcg Levonorgestrel soon after unprotected sex; not later than 72hours. Take a second tablet after 12 hours of taking first dose.
Implant:
Long term prevention of pregnancy (up to 5years):
A total dose of 216mg present in 6 silastic capsules are surgically implanted in the superficial plane beneath the skin of upper arm during first week of onset of menses.
Intrauterine implant:
Long term prevention of pregnancy (up to 5years): The product is inserted in to the uterus by a trained person; once every 5years.
Schedule of Levonorgestrel
H
Storage Requirements for Levonorgestrel
Store at controlled room temperature below 25 degree C.Keep away from excess heat and moisture. Keep out of reach of children.
Effects of Missed Dosage of Levonorgestrel
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.
Effects of Overdose of Levonorgestrel
Give supportive measures and symptomatic treatment

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
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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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