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4. Oral contraceptives

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ORAL CONTRACEPTIVES Prepared by: Mirza Anwar Baig M.Pharm (Pharmacology) Anjuman I Islam's Kalsekar Technical Campus, School of Pharmacy. New Panvel,Navi Mumbai
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Page 1: 4. Oral contraceptives

ORAL CONTRACEPTIVESPrepared by: Mirza Anwar Baig

M.Pharm (Pharmacology)Anjuman I Islam's Kalsekar Technical Campus,

School of Pharmacy.New Panvel,Navi Mumbai

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Outlines:

1.Secretion of FSH & LH2.Role of estrogen and progesterone3.Events in hormonal secretion4.Menstrual cycle5.Mechanism of action6.Methods of use

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Secretion of Estrogen ad Progesterone

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•Secretion of FSH & LH

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Naturally occurring estrogens

Estradiol

Estrone

Estriol

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Synthetic Estrogens

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Progesterone:

•Produced by–Adrenal glands,Gonads–Brain,Placenta (only during pregnancy) •Regulation- stimulated by the production of LH•Hypothalamus→GnRH→ Pituitary→LH→Corpus luteum→Progesterone•Primary Effect- prepares uterus for implantation by the proliferation of endometrium; prepares body for pregnancy•Natural progesterone- destroys by digestive system when consumed orally

ALL oral contraceptives contain progestin, synthetic form of progesterone

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Progestins•Types1) C19- derived from testosterone2) C21- derived from progesterone•Role–in adequate doses it inhibits ovulation–Reduces levels of FSH and LH•Binding–Interacts with progesterone receptors either by entering cells through phospholipid bilayer or by interacting with surface proteins

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•Events in hormonal secretion

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Menstrual cycle•The menstrual cycle is a complex system of changes that occur in the female body due to the regular rise and fall of hormone levels. These changes help to prepare body for a potential pregnancy each month.•The length of a menstrual cycle is measured from the first day of a period to the day before the next period begins. •The average cycle is 28 days although this can vary between women, and from one cycle to the next in individuals.

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•The menstrual cycle is controlled by a number of glands and a series of hormonal changes beginning in the brain. A brain structure called the hypothalamus signals the nearby pituitary gland to release hormones known as FSH & LH which prompt the ovaries to secrete the sex hormones, oestrogen and progesterone.•There are four distinct phases of the menstrual cycle.

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1. The follicular phase•The follicular phase is the time from the first day of menstruation until the moment of ovulation.•During this phase, the pituitary gland releases a hormone which causes between 10 and 20 follicles to begin developing within the ovary.•These follicles, each housing an immature egg (ovum), bead on the surface of the ovary. Usually, only one follicle will mature into an egg (FSH)•The growth of the follicles produces the hormone oestrogen, which causes the lining of the uterus (endometrium) to become thick in preparation for the possible embedding of a fertilised egg.

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2. Ovulation•Ovulation is the release of a mature egg from the ovary surface.•In this phase, the pituitary gland increases production of a hormone which triggers the follicle and ovary to open up and release the mature egg.(LH)•This occurs mid-way through the menstrual cycle, between days 12 and 16 for women with a 28 day cycle.COMPILED BY: PROF.ANWAR BAIG

(AIKTC,SOP) 15

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3. The luteal phase•The luteal phase is the time from ovulation until the first day of menstruation.•During this phase the follicle from which the mature egg was released transforms into a structure known as the corpus luteum and produces large amounts of the hormone progesterone, as well as small amounts of oestrogen., These hormones contribute to the further thickening and maintenance of the lining of the uterus in preparation for the embedding of a fertilised egg.•If fertilisation of the egg does not occur, the corpus luteum dies and progesterone levels decline leading to the breakdown of the uterus lining, which is shed through the vagina as a period (menstruation).

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4.Menstruation•Menstruation occurs when the broken down lining of the uterus flows from the body through the vagina. •Menstruation generally lasts from 3 to 7 days. The length of a period can differ between women, and between cycles in individuals.

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Mechanism of action(The goal is to suppress ovulation)

1.Combinations of estrogen and progestin work by preventing ovulation by suppressing the secretion of gonadotropins (FSH and LH) through negative feedback inhibition.

2.Also change the lining of the uterus (womb) to prevent pregnancy from developing and change the mucus at the cervix (opening of the uterus) to prevent sperm from entering.

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Mechanism of Action:

1.low dose of progesterone prepration alter the endometrium and put it out of phase with ovulation.•There is no disruption of the cycle and ovulation continues.

2.Large dose of oestrogen in case of post coital pills alter the motility of fallopian tube and character of the endometrium.•therefore there is interferacne between the process of fertilization.

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Special precautions:•each women before starting oral contraceptive must be subjected to gynocological examination,evaluation of cvs and liver function.

Drug interaction:•May be with Rifampicine, tetracycline & anticonvulsants causes failure of oral contraception.

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Types of Formulation:

1.Oestrogen-Progesterone combination:The combination pill is adminestered from day5 to day 25 of MC, in between have 7 pill free day.On repeating the schedule the cycle becomes anovulatory with regular cyclic bleeding.Almost 100 percent effective in preventing conception.

2. Sequentional oestrogen-progesterone prepration:It is adminestered from day5 to day 25 of MC, in between have 7 pill free day during which withdrawal bleeding occurs.Serial packs are available having 16 pill of estrogen,5 estrogen and progesterone pills and 7 placebo pills.Inhibition of ovulation is due to oestrogen and progesterone is added for satisfactory bleeding.

3. Low dosage progesterone prepration:containing progesterone alone.taken daily to control fertility.Less effective than combined and sequential regimen.

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Side effects

•Mild side effects:•Nausea,vomitting , headache,lethargy,breast discomfort,breakthrough bleeding (spotting), mild depression.

•serious side effects:•weight gain,amenorrhoea, increased skin pigmentation.

•very serious side effects: •deep vain thrombosis, pulmonary embolism, cerebral and cronary thrombosis,hypertension, decreased glucose tolerance,liver damage and juandice.•severe depression may require urgent cessation of therapy.•Antenatal exposure of oral contraceptive may give birth defects.

•Benefit to risk ratio justify their use as reversible oral contraceptives

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Formulation of oral contraceptives (Combined pills / Sequentional pills)

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THANK YOU


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