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- Pharmacology For Oestradiol + Norgestrel
Oestradiol + Norgestrel Pharmacology
Oestradiol + Norgestrel
About Oestradiol + NorgestrelN/AMechanism of Action of Oestradiol + NorgestrelN/APharmacokinets of Oestradiol + NorgestrelN/AOnset of Action for Oestradiol + NorgestrelN/ADuration of Action for Oestradiol + NorgestrelN/AHalf Life of Oestradiol + NorgestrelN/ASide Effects of Oestradiol + NorgestrelN/AContra-indications of Oestradiol + NorgestrelN/ASpecial Precautions while taking Oestradiol + NorgestrelN/APregnancy Related InformationContraindicatedOld Age Related InformationN/ABreast Feeding Related InformationContraindicatedChildren Related InformationN/AIndications for Oestradiol + Norgestrel1.Estrogen deficiency due to menopause or hypogonadism
2.Castration or primary ovarian failure in women with an intact uterus
3. Postmenopausal osteoporosis
4.Irregular menstrual cycles
5.Primary or secondary amenorrhea
Interactions for Oestradiol + NorgestrelN/ATypical Dosage for Oestradiol + NorgestrelStarting on the 5th day of the cycle, 1 tab daily for 21 days, then 7 tab-free days.Schedule of Oestradiol + NorgestrelN/AStorage Requirements for Oestradiol + NorgestrelStore in a well closed container. Keep out of the reach of children.Effects of Missed Dosage of Oestradiol + NorgestrelN/AEffects of Overdose of Oestradiol + NorgestrelN/AOestradiol
About OestradiolEstrogenic hormone, Estrogen Derivative.Mechanism of Action of OestradiolThe 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 excerts week anabolic action, and also maintain 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 OestradiolAbsorption: Well absorbed orally; but substantial inactivation by liver limits it`s oral administration and administered parenterally. Well absorbed after topical administration. 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 OestradiolN/ADuration of Action for OestradiolN/AHalf Life of OestradiolN/ASide Effects of Oestradiol1.Urticaria
2.Pruritus
3.Irritations of skin
4.Exanthema
5.Breakthrough bleeding
6.Breast tenderness
7.Breast enlargement
8.Gastrointestinal disturbances
9.Nausea
10.Vomiting
11.Pancreatitis
12.Headache
13.Dizziness
14.Seizures
15.Thrombophlebitis
16.Thromboembolism
17.Hypertension
18.Increased risk of endometrial cancer
19.Increased risk of breast cancer
20.Increased risk of Cerebrovascular accident
21.Cholestatic jaundice
22.Hepatic adenoma
Contra-indications of Oestradiol1.Thrombophlebitis
2.Thromboembolic disorders
3.Estrogen dependent neoplasia
4.Undiagnosed genital bleeding
5.Hypertension
6.Estrogen dependent breast carcinoma
7.Hepatic impairment
8.Jaundice
9.Thrombosis
10.Porphyria
11.Sickle cell anaemia
12. Hyperlipoprotinaemia
13.Dubin Johnson syndrome
14.Rotor syndrome
15.Endometriosis
16.Endometrial hyperplasia
Special Precautions while taking Oestradiol1.Migraine
2.Epilepsy
3.Heart failure
4.Hypertension
5.Diabetes mellitus
6.Renal impairment
7.Fibrocystic disease of breast
8.Abnormal mammographic findings
9.Cerebrovascular diseases
10.Coronary artery diseases
11.Asthma
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with cautionIndications for Oestradiol1.Menopausal symptoms due to estrogen deficiency
2.Primary ovarian failure
3.Atrophic vaginitis
4.Inoperable breast cancer
5.Female hypogonadism
6.Hyper androgenism in females
Interactions for Oestradiol1.CYP1A2 and CYP3A4 inducers e.g. aminoglutethimide, carbamazepine, phenobarbital, and rifampin may decrease the effects of estradiol.
2.May enhance the effects of hydrocortisone and prednisolone when used together.
Typical Dosage for OestradiolOral: 1 to 2mg/day in cycles of 21days on and 7days off or 23 days on and 5 days off.
Inoperable breast cancer: 10mg 8th hourly for 3 months.
Topical: 1.5mg once daily. Increases the dosage up to 3mg; if required after one month.
(3mg Oestradiol in 5g gel)
Maintenance dosage: 1g gel once to thrice weekly
Transdermal: Place one transdermal patch twice weekly on trunk of the body; preferably the abdomen in cycles of 3 weeks on and 1week off.
Schedule of OestradiolHStorage Requirements for OestradiolStore at room temperature at a range of 15 to 30 degree C.
Intramuscular: Store at room temperature.
Oral: Store at room temperature.
Transdermal: Store at room temperature.
Vaginal: Store at room temperature.
Effects of Missed Dosage of OestradiolTake 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 OestradiolProvide symptomatic treatment and supportive care.NORGESTREL
About NORGESTRELSynthetic Progestogens, ContraceptiveMechanism of Action of NORGESTRELNorgestrel binds to the progesterone and estrogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like Norgestrel will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge. Thickening the cervical mucus to inhibit sperm penetration, slowing the movement of the ovum through the fallopian tubes, and altering the endometriumPharmacokinets of NORGESTRELAbsorption: Absorbed after oral administration
Metabolism: Metabolised in the liver
Onset of Action for NORGESTRELN/ADuration of Action for NORGESTRELN/AHalf Life of NORGESTREL5 - 14 hrsSide Effects of NORGESTREL1.Dizziness
2.Nausea
3.Vomiting
4.Sleepiness
5.Withdrawal bleeding in females
Contra-indications of NORGESTREL1.Liver disease
2.Genital bleeding
3.Endometrial Cancer
4.Thrombo embolic complications
5.Hypersensitivity to any component of the product
Special Precautions while taking NORGESTREL1.Kidney disease
2.Liver Disease
3.Heart disease
4.Blood clots
5.Stroke
6.Depression
Pregnancy Related InformationContraindicatedOld Age Related InformationN/ABreast Feeding Related InformationContraindicatedChildren Related InformationN/AIndications for NORGESTRELContraceptionInteractions for NORGESTRELN/ATypical Dosage for NORGESTRELOne tablet is taken every day, at the same time. It is also used combination with estrogenSchedule of NORGESTRELN/AStorage Requirements for NORGESTRELStore at controlled room temperature 20? to 25?C (68? to 77?F) in a well closed container. Keep out of the reach of childrenEffects of Missed Dosage of NORGESTRELN/AEffects of Overdose of NORGESTRELN/AHome Delivery for Oestradiol + Norgestrel in Your City
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