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SIMILARITIES AND DISSIMILARITIES OF PROGESTINS. DR.RASHMI. INTRODUCTION. PROGESTINS ARE CHEMICAL DERIVATIVES OF TESTOSTERONE KNOWN AS 19- NORTESTSTERONE DERIVATIVES 8 TYPE OF PROGESTINS AVAILABLE. CLASSIFICATION OF PROGESTINS. Mechanisms of action of PROGESTINS IN COC components.
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INTRODUCTION • PROGESTINS ARE CHEMICAL DERIVATIVES OF TESTOSTERONE KNOWN AS 19- NORTESTSTERONE DERIVATIVES • 8 TYPE OF PROGESTINS AVAILABLE
Mechanisms of action of PROGESTINS IN COC components Speroff L. Oral contraception. In: Clinical Gynecologic Endocrinology and Infertility; 8th Edition; Philadelphia:Lippincott Williams & Wilkins, 2011:974-975. 4
PROFILE OF PROGESTINS • PROGESTATIONAL EFFECT- Progestational selectivity is the degree to which progestational effects are maximised and androgen effect minimised • ANDROGENIC ACTIVITY- Side effects like acne and hirsutism
ESTROGENIC ACTIVITY- capacity to counter the oestrogrenic effect of EE • GLUCOCORTICOID ACTIVITY • MINERALOCORTICOID ACTIVITY
Evolution of progestrogens Ideal progestogen: Should have the closest profile to progesterone. 7
Parameters • LNG+EE • DSG+EE • P-Value • Weight • Base Weight (Kg) • 63.2±15.6 • 65.3±10.6 • 0.576 • Terminal Weight (Kg) • 65.8±15.6 • 65.3±11.0 • 0.902 • Weight Changes (Kg) • 3.3±3.6 • 0.0±2.5 • 0.000 • Acne • Base number of acne • 4.3±7.0 • 4.8±8.2 • 0.758 • Terminal number of acne • 4.7±6.7 • 1.8±3.6 • 0.011 • Number of acne changes • 0.4±3.3 • -3.0±6.2 • 0.001 • Hirsutism • Base hirsutism severity • 2.5±4.3 • 2.7±4.4 • 0.836 • Terminal hirsutism severity • 2.8±4.2 • 1.0±2.0 • 0.012 • Hirsutism severity changes • 0.3±1.8 • -1.7±2.9 • 0.000 The effect of the pill on weight, hirsutism and acne Sanam and Ziba, Saudi Med J 32:23-26, 2011
RELATIVE RISK OF CVS EVENTS IN USERS OF 2ND GEN COMPARED WITH 3RD GEN
RELATIVE RISK OF VENOUS THROMBOEMBOLISM IN USERS OF 2ND GEN COMPARED WITH 3RD GEN OCP USERS
DROSPIRENONE vs LEVONORGESTREL DRSP – 1 . Similar contraceptive efficacy and good cycle control. 2 . Has better tolerance. 3 . Fewer prevalence of premenstrual symptoms. 4 . Better anti-mineralocorticoid activity 5 . Increased risk of venous thromboembolism . 6 . Increases HDL and no significant change in LDL. 7 . No effect on carbohydrate metabolism . 8 . Increases potassium level .
DROSPRINONE vs DESOGESTREL NO SIGNIFICANT EFFECT ON CARBOHYDRATE METABOLISM
LONG TERM EFFECTS • REDUCES WEIGHT BY 2% . • REDUCES ACNE . • BETTER CYCLE TOLERANCE . • CAUSES NON FATAL VENOUS THROMBOEMOLISM .
BEING A SPRINOLACTONE DERIVATIVE , IT HAS POTASSIUM SPARING PROPERTIES. • SO ITS CONTRAINDICATED IN PATIENTS WITH HEPATIC AND RENAL FAILURE.
KEY RESULTS • COMBINED ORAL CONTRACEPTIVES CONTAINING DESOGESTREL,DROSPRINONE ARE ASSOCIATED WITH A HIGHER RISK OF VENOUS THROMBOEMBOLISMTHAN LEVONORGESTREL CONTRACEPTIVES. • DISCONTINUATION DUE TO SIDE EFFECTS INCLUDING CYCLE DISTURBANCES WERE MORE LIKELY TO OCCUR IN LNG GROUP
Pregnancy and discontinuation rates were similar in third and fourth generation progestin's. • Overall, a similar number of women in both groups reported side effects, except for breast tenderness which was more common in the DRSP group. • There was a trend towards more nausea and vomiting in the DRSP group.
What do women want from contraception? • Survey 2009 of 16-49 year olds BSP • Older women Younger women • Highly effective No side effects • Safe Easy to get • Good cycle control Non invasive • Well tolerated • Added benefits • No side effects
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