Oral hormonal contraceptive

BY MAGDY ABDELRAHMAN MOHAMED

2 0 1 5

ORAL HORMONAL CONTRACEPTIVE

CONTRACEPTIVE PILLS

1- Combined oral contraceptive pills.

(COCs)2- Progestogen only pills. (POPs)

COCs

Composition :1. Estrogen :

Ethinyl estradiol (20 times more active)100µg

50 µg35 µg30 µg20 µg

Mestranol (3-ethyl ester of ethinyl estradiol)

low dose pills

2. Progestogen:• 19-Nortestosterone derivatives:

Norethinderone “norethisterone”. Levonorgestrel (microcept) 150 µg Gestodene (gynera) 75 µg Desogestrel ( marvelon)150 µg Norgestimate ( cilest )250 µg

• 17-α spironolactone derivatives: Drospirenone (yasmin) 3mg

Action

Suppress ovulation through negative feedback to hypothalamic-pituitary axis.

Thickening of cervical mucus to prevent sperm entry.

May also slow tubal motility, disrupt transport of ova. (not proven)

Efficacy

COC is highly effective 99.9% in preventing pregnancy.

However the user failure rate is 3-8%.

Types of COCs

1. Monophasic pills. E.g. Microcept, Gynera, Cilest, Marvelon and

Yasmin.2. Biphasic pills.

Estrogen fixed dose throughout the cycle with doubled dose of progestin in the 2nd. Half of the cycle.

3. Triphasic pills. 1st. 6days : 30 µg EE + 50 µg LNG 2nd. 5days: 40 µg EE + 75 µg LNG 3rd. 10days: 30 µg EE + 125 µg LNG

Types of COCs

1st. Generation: EE > 50 µg2nd.Generation: EE<50 µg + any

progestin except( Gestodine, Desogestrel, Norgestimate or Drospirenone)

3rd. Generation: EE<50 µg + Gestodine, Desogestrel or Norgestimate.

4th. Generation: EE<50 µg + Drospirenone.

How and when to use it???

Start on the 1st 5 days of the cycle regularly every day.

21 days 0n, 7 days off.

Missed pills

One pill. No problem. Take the missed pill immediately.

2 pills or more. Take the pills Backup methods should be used. Emergency contraception if sexual

intercourse was occurred in preceding 7 days.

Advantages of COCs

1. Highly effective if used correctly.2. Rapid return of fertility after

stoppage.3. Suitable for nulligravida and newly

married couples.4. Completely controlled by the woman

and can be stopped at any time unlike other methods (IUD & Implants).

5. No need to do any thing at the time of intercourse.

Non contraceptive benefits of COCs

Regulation of the cycle with ↓ amount & duration.

So it helps in prevention & ttt of iron def. anemia.

↓risk of epithelial ovarian tumors. ↓Inc. of functional ovarian cysts. ↓ risk of ectopic pregnancy.

Non contraceptive benefits of COCs

↓risk of developing PID. ↓risk of endometrial cancer. ↓spasmodic dysmenorrhea and

PMS. ↓risk of benign breast lesions. May protect from colorectal

cancer. May ↓ Inc. of fibroid. Improvement of rhumatoid

arthritis.

Non contraceptive uses of COCs

Ttt of Dysfunctional uterine bleeding. Ttt of Endometriosis. Ttt of PMS. Ttt of spasmodic dysmenorrhea. Postponing of menstruation for social or

religious causes. Ttt of hirsutism: “ Yasmin” contains

antiandrogenic progestin Drosprirenone.

Disadvantages & Side effects

1- The need for daily use.2- GIT:

Nausea and vomiting. Increased incidence of gall bladder stones). Women with active hepatitis will have a

deterioration in liver functions. ↑inc. of hepatocellular adenoma ( rare).

3-central nervous system: Headache and migraine. Mood changes: depression, irritabilty.

4-Breast Not suitable with breast feeding. Mild breast tenderness may occur.

5-Genital tract. Cervix:

Cervical erosion is a common finding. Vagina:

Increased normal vaginal disharge. Vaginal candidiasis.

6-CVS: Increased risk of venous

thromboembolism. Increased risk of MI & stroke in elderly

patients with hypertension and smokers.7-Metabolic :

Increased body wt. In diabetic patients: leads to hyperglycemia

and increased risk of vascular complications.

Dyslipidemia:↑cholesterol, ↑triglycrides, ↑LDL& ↓HDL.

Absolute contraindications

< 6 months postpartum if breastfeeding Smoker over the age of 35 (≥ 15 cigarettes per day) Hypertension (systolic ≥ 160mm Hg or diastolic ≥

100mm Hg) Current or past history of venous thromboembolism

(VTE) Ischemic heart disease History of cerebrovascular accident

Absolute contraindications

Complicated valvular heart disease Migraine headache with focal neurological symptoms Breast cancer (current) Diabetes with retinopathy/nephropathy/neuropathy Severe cirrhosis Liver tumour (adenoma or hepatoma)

Relative contraindications Smoker over the age of 35 (< 15 cigarettes

per day) Hypertension (systolic 140–159mm Hg,

diastolic 90–99mm Hg) Currently symptomatic gallbladder disease Mild cirrhosis History of combined OC-related cholestasis Users of medications that may interfere

with combined OC metabolism

MYTHS AND MISCONCEPTIONS

1. The combined OC causes cancer.Fact:

The combined OC reduces the risks of ovarian and endometrial cancer.

The risk of ovarian cancer is reduced by at least half in women who use combined OCs.

MYTHS AND MISCONCEPTIONS

2. Women on the combined OC should have periodic pill

breaks.Fact:

This is unnecessary. Pill breaks place a woman at risk for unintended pregnancy and cycle irregularity.

MYTHS AND MISCONCEPTIONS

3. The combined OC affects future fertility.

Fact: Fertility is restored within

1 to 3 months after stopping the combined

pills.

MYTHS AND MISCONCEPTIONS

4. The combined OC causes birth defects if a woman

becomes pregnant while taking it.

Fact: There is no evidence that the

combined OC causes birth defects.

MYTHS AND MISCONCEPTIONS

5. The combined OC must be stopped in all women

over 35 years old.

Fact:Healthy, non-smoking women

may continue to use the combined OC until

menopause.

MYTHS AND MISCONCEPTIONS

6.The combined OC causes acne.

Fact: Acne improves in women using the combined OC due to a decrease in circulating free androgen.

All combined OCs will result in an improvement of acne

PROGESTOGEN ONLY PILLS ( POPS)

Types: Levonorgestrel 30µg ( microlut)

Lynestrenol 500µg (exluton)

Efficacy

Must be taken at same time every day to be effective.

Perfect use failure rate 0.5%Typical use failure rate 5-10%

Mechanism of action

1-Main mechanism is alteration of Cx mucous.

↓↓ volume of mucous↑↑ viscosity2- Ovulation is suppressed in 60% of the

women.3-Endometrial changes ↓↓ implantation.

How to use????

Start on the 1st 5 days of the cycle or after 6 weeks postpartum.

Daily tablet at the same time every day without discontinuation.

Woman consider her self fertile for the first week of use.

Missed pill

To be taken as soon as possible.Next pill to be taken at the regular time.If delayed > 3hrs use back up

contraception for 48 hrs.If 2 or more pills missed in a row 2 pills/day

for 2 days back up contraception for 48 hrs.Emergency contraception must be used if

intercourse occurred after a missed pill.

Advantages

Suitable when breast feeding.Suitable when EE is contraindicated.

Immediate return of fertility.Less likely to cause metabolic disturbances.

Disadvantages

Must be taken daily at the same timeLess effective than COCsMore likely to cause menstrual

irregularitiesHeadache, nausea, breast tenderness,

mood changes, depression and ↓libido.Less effective in preventing ectopic

pregnancy.