2011 Hormonal Contraception

LOGO

HORMONAL CONTRACEPTION

Nani Maharani

Pharmacology & Therapeutics DepartmentFaculty of Medicine Diponegoro University

Semarang2011

FEMALE HORMONAL FEMALE HORMONAL CONTRACEPTIONCONTRACEPTION

Company name

www.themegallery.comHormonal contraception

Company name

www.themegallery.com

HORMONAL CONTRACEPTION

Oral Contraceptives

Injected Contraceptives

Implanted Contraceptives

Hormonal contraception

Transdermal Patch

Company name


ORAL CONTRACEPTIVES

Combination of Estrogens & Progestins (Combined oral contraceptive = COC .

Oral contraceptives

Progestins only (mini pill)

Why is estrogen added to combined OC?


Components

Estrogens :- Ethynil estradiol- Mestranol

Progestins :- Norgestrel- L-norgestrel- Norethindrone- Drospirenone- Norgestimate- Ethynodiol diacetate

Company name


COMBINATION AGENTS

1. Monophasic: constant dosage of both components during the cycle

2. Biphasic or triphasic: dosage of both components is changed once or twice during the cycle

usually taken for 21 days with a 7 days gap

What is the rationale for taking active OC pills for 21 days?

Company name


PROGESTINES ONLY

Mini Pill - Progestin only - Long term risks of estrogen ↓ - Daily-No interruption- Efficacy lower- Irregular bleeding

Company name



PHARMACOLOGICAL EFFECTS

Mechanism Mechanism of actionof action

22

33

44

11Effects on the ovary

Effects on the uterus & uterine tube

Effects on the breast

Effects on other organs:CNS, endocrin, blood, liver, lipid metabolism, carbohydrate metabolism,

CV system, skin


Effects on the Ovary

Depressed ovarian function Minimized follicular development Corpora luteal, larger follicle, etc are

absent

Company name


Effects on the Uterus

“underdeveloped” of endometrium Thicker mucous Decreased motility of uterine tube

Company name


Effects on the breast

Enlarged breast, especially on estrogen-containing compound

Suppressed lactation

Company name


Effects on Other organs

CNS: changes on mood, affect, and behaviour

Endocrine function: alter adrenal structure & function, alter the renin-angiotensin-aldosterone system

Blood: increase in factors VII, VIII, IX, X; decrease antithrombin III; increase serum ion & TIBC

CV system: higher blood pressure & heart rate

Company name


Effects on Other organs (2)

Liver: changes on liver metabolism, alteration on hepatic drug excretion, increase in cholelithiasis

Lipid metabolism: increased: serum TG, free & esterified cholesterol, HDL, Phospholipids; decreased: LDL estrogen

Carbohydrate metabolism: reduction in the rate of absorption. Progesterone increase basal insulin level. More potent progestin (norgestgrel) may cause decrease carbohydrate tolerance in several years.

Skin: increased skin pigmentation, production of sebum, acne & terminal hair growth

Company name


EMERGENCY CONTRACEPTION

Not used routinelyPreventing pregnancy after unprotected

sexual intercourseCombined and progesterone-only pills are

taken in high dosesThey are effective (~75%) if taken within

72 hours after coitusIt won't terminate an existing pregnancy

Company name


INJECTION CONTRACEPTION

Medroxyprogesterone acetate - Dose 150mg IM - 3 monthly

Medroxyprogesterone (25mg) & estradiol cypionate (5mg) - IM injection.- 1 monthly

Company name


IMPLANTS

1.Levonorgestrel (6x36 mg) duration of action 5 years

2.Levonorgestrel (2x70 mg) duration of action 3 years

Silastic rods, placed under the skin of the inside lower arm

3. Etonogestrel (1x68 mg) duration of action 1 year

ethylen-vinyl-acetate (EVA) rod, placed under the skin of the inside lower arm

Company name


Company name


INTRA-UTERINE DEVICE

Progestine-containing (Levonorgestrel) IUD

5 years (20 mg/day initially, and 10 mg/day

The mechanisms of action : 1. Preventing implantation mechanically2. Causing progesterone effects locally, like: thickening of cervical mucus, preventing passage of sperm into the uterus, inhibition of sperm survival, and causing changes in the endometrium.

Company name


Company name


TRANSDERMAL PATCH

Combination of estrogen and progestines 0.75mg ethinyl estradiol and 6mg

norelgestromin Releases 150mcg norelgestromin and

20mcg ethinyl estradiol each day Applied to the buttock, abdomen, upper

torso, or outer upper arm Changed at day 8 and day 15

Company name


SIDE EFFECTS

Current preparations have low-dose of estrogen, so the incident of dose-dependent toxicity is much less

1. Thrombo-embolic events: myocard infarct, stroke, DVT, pulmo.embolism

2. Breast Ca3. Other: edema, breakthrough bleeding, nausea,

breast tenderness, headache, skin pigmentation, depression, weight gain, acne

4. More often vaginal infection5. Amenorrhea

Company name


CONTRAINDICATIONS

Thrombophlebitis Thromboemboli Cardiovascular disorders Cerebrovascular disorders Known/suspected breast tumour or other

estrogen-dependent neoplasms Liver disease

Use with cautions in: asthma, eczema, migraine, DM, HT, convulsive disorders

Company name


PHARMACOKINETICS

Absorbed well in GI tract, skin, sc, im Deposited in fat tissues Metabolized in the liver Normal GI flora increase bioavailability

anti microba that interfere these flora will reduce the efficacy of OC

Company name


PHARMACOKINETICS (2)

Metabolized by cytochrome P450 3A4 interaction with the drugs that induce the isozymes barbiturates, rifampin, carbamazepines, corticosteroids, griseofulvin, pioglitazone

Narrow margin between effective-ineffective serum concentration drug interaction might cause risk of uninted pregnancy

What should be done if one of these drugs is prescribed to the combined hormonal contraception users?

Company name


MALE HORMONAL MALE HORMONAL CONTRACEPTIONCONTRACEPTION

Company name


MALE HORMONAL CONTRACEPTION

Company name


Clinical pharmacology & Therapeutics | VOLUME 89 NUMBER 1 | january 2011


THE GOALS

Suppress spermatogenesis Azoospermia

Without decreasing male potency and libido

Using exogenous androgens (testosterone), or in combination with progestines (medroxyprogesterone acetate, norethistrone)

Company name


PREPARATIONS

Company name


Royth MY, Amory JK. Pharmacologic development of male hormonal contraceptive agents. Clinical pharmacology & therapeutics. 2011: 89(1);133-136

Company name


Documents

2011 Hormonal Contraception