1)Oestrogens:- Oestradiol,Tibolone, Ethylnyl oestradiol, Conjugated oestrogens, Ethynyl oestradiol +Methyl testosterone combination.
2) Progestrogens:- Progesterone, Dedrogesterone, Medroxyprogesterone. hydraoxy progesterone caproate, Norethisterone, Allyloestrenol, Lynesterol.
3) Progesterone + Estrogen combination.
4) Other oral contraceptives: cenchroman..
Oestrogens:- oestradiol and oestrone are both natural estrogen secreted by Ovary. Oestrogens are necessary for normal development of breast and female genital tract and secondary sexual characteristic. Oestrogens are necessary for maintainance of pregnancy. Several estrogens preparations are available. The List includes ethinyl oestradiol, stilbestrol, conjugated estrogen, oestradiol, oestriol. Secretion of estrogen is regulated by FSH. Oestrogen also exerts feedback inhibition on pituitary.
Mode of action:- Oestrogens act by binding to nuclear oestrogen receptors. after activation oestrogen receptors binds to specific DNA sequences ( harmone response elements) that enhance the transcription of adjacent genes.
P/K :- Natural oestrigens circulate in blood and are bound to sex hormone binding globumin and albumin. Excretion occurs in the form of conjugates which are excreted by kidneys.
Indications:- Estrogen in oral contraception, post menstrual symptoms, serile vaginitis, Kraurosis-vulvae, dysmenorrhoea, acne, hirsutism, dysfunctional uterine bleeding, osteoporosis, suppression of postpartum Lactation.
Oestradiol:- Available for use as trans dermal patch.
Mode of action:- same as oestrogens
Special precautions:- Epilepsy, Migraine, cardiac failure, Hypertension, diabetic mellitus, Fibrocystic disease of breast, hepatic & renal dysfunction.
Indications:- HRT for menopausal symptoms due to estrogen deficiency, post menopausal osteoporosis, and clinical conditions requiring natural oestradiol(E2) replacement including primary ovarian failure, hyperandrogenism in females.
Preparation of oestradiol:- E2 gel (Beta estradiol) Sunpharma
dosage:- The usual dose is 1.5mg of oestradiol in 2.5mg of gel once a daily. After one month, if effective relief is not obtained, the dosage may be increased up to a maximum of 3mg daily. A maintainance dosage of 1gram of gel one to three times a week may be used. Apply gel to clean, dry, intact areas of skin, example arms/shoulders or inner thighs. The area of application should be at-least 750 square meter. Gel should not be applied on or near vulva region. Allow skin to dry for five minutes before covering with clothing.
Brand Name: Estraderm TTS ( oestradiol) Novertis 2×25microgram/patch.
Tibolone;- It is a synthetic steroid which combines oestrogenitic & progestogenic activity with weak androgenic activity. It needs to be given continuously within cyclical progestogen.
Mode of action:- it restores plasma endorphin level and post menopausal women and acts centrally to affect the thermo regulatory system.
Special precaution:- Renal impairment, epilepsy, Migraine diabetic melitus, hypercholesterolaemia, abnormal liver function tests or cholestatic jaundice.
Indications:- Vasomotor symptoms in oestrogen deficiency (natural or surgical menopause), osteoporosis, prophylaxis
Dosage:- Adults: 2.5mg daily (unsuitable for use within 12 months of last menstrual period.
Preparation of Tibolone:- Livial (Infar) tablet of 2.5mg.
Ethynyl oestradiol :-Mode of action:- Same as oestrogens.
Indications: oestrogen deficiency symptoms associated with natural/surgical menopause, menstrual cycle disturbances.
Dosage;- HRT : Initially 0.05mg 1-3 times daily reducing to maintainance leval of 0.025mg daily. Cyclical administration, along with progestogen from 16th to 25th day. Mammary Hypoplasia:- 0.05mg daily for 12 days with progestogen from 16th to 25th day starting therapy following menstrual period if applicable.
Male hypersexuality: 0.05mg daily. Children:- Not applicable.
Preparation of Ethynyl oestradiol : Brand name: Evalon (infar company) estriol 1mg tablet
conjugated estrogen:- Mode of action:- Same as oestrogens
Special precautions: Migraine, epilepsy, Asthma, renal and cardiac disease. may cause retetion of salt & water. Abnormal mamo grams to discontinue if cancer progression of hypercalcaemia occurs.
Indications:- Menopause, osteoporosis, prostatic carcinoma, atropic vaginitis, urethritic.
Dosage:- Adults:- Moderate to severe vasomotor symptoms associated with climacteric;: 0.625mg-1.25mg daily.
Atrophic vaginitis/urethritis: 0.3mg-1.25mg daily depending on response. Osteoporosis:- 0.625mg daily. Female hypogonadism:- 2.5mg-7.5mg daily in divided doses for 20days then no tablet for 10 days if no bleeding. repeat same. Primary ovarian failure:- 1.25mg daily, adjust upward or downward as per response.
Oestrogen replenishment: 0.625mg daily. Children:- not applicable
Preparation of Conjugated oestrogens: Brand name; Premarin(wyath lederle) 0.625 & 1.25mg tablet.
Ethinyl Oestradiol + methyl testosterone:-
Special precaution: Cardiac failure, vericose veins, Major surgery, chloasma , to discontinue therapy if virilization occurs, renal dysfunction, pain in breast, migraine epilepsy.
Indications;- Natural or surgical menopause associated with oestrogen deficiency symptoms
Dosage;- Adults: 1-2 tab daily alternatively 1ml I.M. every 3-4 weeks.
Children:- Not applicable
Preparetion of Ethinyl oestradol+ Methyl Testosterone: Brand name:Mixogen(infar) ( ethinyl oestradol; 4.4microgram+methyl testosterone 3.6mg)
Progestogens:- there are two main groups of progestgens. 1) progesterone and its analogue. ( hehydrogestrone, hydroxyprogesterone, Medroxyprogesterone. 2) Testosterone analogue: Norethisterone, Norgestrol.
Progesterone;- It is a chief harmone secreted by corpus luteum and cause induction of secretory activity in endometrium of oestrogen primed uterus. It causes glandular development of breast, increases basal body tempature, inhibits uterine contractions. Progestogens are allyestrenol, medroxy progesterone , hydraoxy progesterone, nor ethisterone, norgestral, lynoestrenol, norethisterone, norgestral, lyno estrenol. norethinodrel.
Mode of action:- After reaching cell nucleus it binds to progesterone receptors and influence the transcription of a limited set of genes.
P/K:- After oral administration, progesterone undergoes extensive first class metabolism in liver. It has a short plasma half life.
Special precautions: Diabetic, hypertension, hepatic, cardiac, or renal disease.
Indication:- primary or secondary Amenorrhoea, dysfunctional uterine bleeding, endometriosis, postponement of menstruation, premenstrual syndrome, uterine hypoplasia.
Preparetion of progesterone & progestogens:-Brand name: Microgest(walter bushell) (Natural micronised progesterone)
Noreta HRT ( german remedies) Norethindrone acetate 1mg tablet
Indications- Sequential administration during estrogen replacement therapy in post menopausal women with an intact uterus.
Dosage: In cyclic treatment with estrodiol, norethisterone acetate should be given during last 12 days of each 3 week period of estradiol administration, so that the 4th week of each cycle remains without treatment. In patient receiving continuous estradiol therapy, nor ethidrone acetate should be taken for 10-14 days ( preferably first 12 calender days of each month
Brand name : puregest (natural micronised progesterone) 100mg, 200mg, 400mg caps.
Indications:- supplemantation of the luteal phase in case of sterility due to luteal deficiency, treatment of puerperal depression, maintainance of pregnancy in cases of threatened or habitual abortion, premenstrual syndrome, benign mastopathies, in menopause to reduce the risk of endometrial hyperplasia and carcinoma in post menopausal women receiving conjugated estrogen.
Dosage:- Maintenance of pregnancy in cases of habitual or threatened abortion. 200-400mg per day in divided doses . For premenstrual syndrome: 200-400mg 1-2 times daily from 12th to 14th day of the cycle until on set of menstruation. For puerperal depression: 400mg twice daily in divided doses.
supplementation of luteal phase in case of sterility due to luteal deficiency; 400-600mg per day up to the 12th weak of pregnancy. May be given orally, vaginally, or rectally. for vaginal & rectal administration, capsule should be inserted deep into vagina or rectum.
Medroxy progesterone :- It is a synthetic progestogen structurally related to progesterone given by mouth or by I.M.injection.
Special precaution:- Cushin gold symptoms may occur with high dose therapy, thromboembotic disorders, genital neoplasm, breast carcinoma, fluid retention may occur.
Indications:- Dysfunctional uterine bleeding, Secondary amenorrhoea, Endometriosis.
Dosage:- Adults:- Dysfunctional uterine bleeding: 2.5-10mg for 5 to 10 days. repeat on 2-3 consecutive cycles. Secondary amenorrhoea: 2.5-10mg daily for 5 to 10 days starting on assumed 16th to 21st day of cycle. Repeat on 3 consecutive cycles. Endometriosis :- 10mg thrice a daily starting on the 1st day of cycle for 90 consecutive days.
Children: Not applicable.
Preparations of medroxyprogesterone ; Brand name: Depo-provera( Pharmacia-upjohn) 150mg vial of 1ml.
Dedroprogesterone:- special Precaution: same as medroxyprogesterone.
Indications: Dysnmenorrhoea, threatened or habitual abortion, Endometriosis,infertility due to inadequate luteal phase, premenstrual syndrome, adjunct to oestrogen replacement threapy.
Dosage: Adults:- Dysmenorrhoea 5to 10mg twice a daily from day 5 to day 25 of the cycle.
Endometriosis: 5-10mg 2-3 times daily from day 5th today 25 of the cycle or continuously.
Premenstrual syndrome:- 5 to 10mg daily from 12th to 26th day of the cycle.
Infertility, irregular cycles:- 10mg twice daily from 11th to 25th day for at least 6 cycles.
Habitual abortion:- 10mg twice daily from 11th to 25 th day of the cycle until conception, then continuously until 20th week of the pregnancy and gradually reduced.
Preparations of Dedroprogesterone:- Brand name: Duphaston: tablet of 10mg.
Hydroxy progesterone caproate:-
Special precaution:- Intra abdominal heamorrage due to malignant tumors, pregnancy to be excluded in indications other than threatened abortion.
Indications: Threatened abortion, habitual abortion, Primary amenorrhoea, Uterine hypoplasia, infertility due to corpus luteum insufficiency.
Dosage:- Amenorrhoea: start treatment at least 8 weeks after last menstruation. On 1st day estradiol valerate 20mg I.M., 14 days later estradiol valerate 10mg with 250mg Hydroxy progestrone caproate I.M. withdrawl bleeding start 28th day of treatment. Continue treatment for 2-3 cycles.
Preparation of hydraoxy progesterone:- Brand Name:- Proluton depot ( German remedies) 250mg per amp of 1ml.
Norethisterone:- Norethisterone & its acetate and enanthate esters are synthetic progestogens given by mouth given in treatment of abnormal uterine bleeding and endometriosis.
Contradications:- Carcinoma of breast or uterus, thromboembolic disorders, severe liver disease, severe diabetes, rotor syndrome, Dubin johnson syndrome.
Indications:- Primary & secondary amenorrhoea of long duration, metropathia, haemorrhagica, menorrhagia, dysmenorrhoea, polymenorrhoea, premenstrual syndrome, female subfertility, endometriosis, timing of menstruation, as contraceptive- drug.
Dosage: Adults:- Endometriosis: starting 5th day of cycle 5mg twice daily, increasing up to 10mg twice daily incase of spoting. DUB:- 5mg 3 times daily for 10 days.
Timings of menstruation:- 5mg 3 times daily for not more than 10-14 days, begining about 3 days before expected menstruation. Preparetion of Norethisterone:- Brand name :- Primolut N ( german remedies) 5mg tablet.
allyl estrenol: it stimulates placental progesterone synthesis and increases the secretion of placental hormones.
Contraindications:- Mammary Carcinoma, genital carcinoma, history of thromboembolic disorders, vaginal bleeding of unknown cause, history of herpes of pregnancy, hepatic impairment.
Indications:- Habitual abortion, failure of nedation, threatened abortion, premenstrual tension, metrorrhagia, threatened premature labour,IUGR
Dosage:- Threatened abortion: 5mg 3times daily for 5-7days, then reduce gradually till symptoms disappear. Habitual abortion:- 5-10 mg daily as soon as pregnancy has been diagnosed, with at least one month till critical period is over. threatened premature labour: Individually (up to 40mg daily.)
Preparation of Allyoestrenol:- Brand name: Gestin 5mg tablet.
Lynoestrenol : it is an oral progestogen.
Contraindications:- Thromboembolic processes, Caridvascular disorders, Cholestatic jaundice, History of jaundice of pregnancy or due to estrogen/ progestogen use, vaginal bleeding of unknown cause, porphyria, Haemoglobino-pathies, Hyperlipoproteinanemia, severe hypertension, severe pruritus, Dubin johnson syndrome, rotor syndrome.
Indications: Dysfunctional uterine bleeding, amenorrhoea, dysmenorrhoea, hypo & hyper menorrhoea, delay of menstrual period, Oligo and polymenorrhoea, benign breast diseases, endometriosis, metrorrhogia, endometrial carcinoma.
Dosage:- Adults: postponement of menstruation: 5-10 mg daily not later than 3days before expected date of menstruation.
Endometriosis;- 5mg daily for at least 6months. Polymenorrhoea: 5mg daily from 5th -25 th day of cycle for 2-3cycles.
Progestrogen + oestrogen combinations;- Contraindications: Jaundice, Rotor syndrome, Dubin johnson syndrome, cancer of breast, endometrial carcinoma, herpes of pregnancy, diabetes, undiagnosed vaginal bleeding, congestive heart failure, severe allergic condition.
Indications:-These drugs are used as oral contraceptives. also used for dysmenorrhoea, endometriosis, irregularities of the cycle without organic cause. Hypermenorrhoea, polymenorrhoea, intermenstual bleeding, Intermenstrual pain,( mittel-schmerz)DUb, delay of menstruation, ovulation & ovulation pain.
Ist day of bleeding is counted always as day 1 of the cycle.
Preparetion of progestrogen + oestrogen Combinations:- Brand name: Duoluton-L ( german remedies) Levonorgestral o.25mg, ethnyl estradiol ).05mg Adult dose; 1 tablet daily from 5th to 25th day of the cycle.
Centchroman:- It is an oral contraceptive pill.
On set of action:- 30-60 minutes, duration of action: up to 7 days.
Contraindications:- poly cystic ovarian disease, Tuberculosis, renal disease, liver disease, history of jaundice, cervical hyperplasia, severe allergic disease
Indications:- As a contraceptive
Dosage: Adults: First tab to be taken on day 1 ( monday of mensstrual cycle followed by 1 tab on day 4 ( that is thursday) Repeat this regime every week for 3 consecutive months exactly on the same days that is mondays & thursday. Dose to be reduced to once a week the same day, that is Monday for as long as contraception is desired. Children; not recommended
Preparation of cenchromen:- Brand name:- Centron ( Torrent) Tablet of 30mg
Recent Comments