Ethinylestradiol/ Desogestrel

Registered South African indications:

• Contraception

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy
• Severe hepatic impairment
• Porphyria
• Current or history of arterial or venous thromboembolism
• Thrombophilia
• Major surgery with prolonged immobilisation
• Cerebrovascular disease
• Migraine with focal neurological symptoms
• Current or history of liver tumours
• Pancreatitis or history thereof
• Diabetes mellitus with vascular symptoms
• Severe hypertension
• Severe dyslipoproteinaemia
• Known or suspected sex-steroid influenced malignancies
• Undiagnosed vaginal bleeding
• Peanut or soya allergy

Cautions

• Breastfeeding
• Renal impairment
• Mild to moderate hepatic impairment
• Obesity
• Family history of venous thromboembolism
• Cancer
• Systemic lupus erythematosus
• Haemolytic uraemic syndrome
• Chronic inflammatory bowel disease
• Sickle cell disease
• Older than 35 years
• Smoking
• Positive family history of arterial thromboembolism
• Diabetes mellitus
• Hyperhomocysteinaemia
• Valvular heart disease
• Atrial fibrillation
• Hypertriglyceridaemia
• Conditions known to worsen during pregnancy
• Hereditary angioedema
• Depression
• Epilepsy
• Prolonged use
• Human papilloma virus
• Jaundice
• Chloasma gravidarum
• Cardiac dysfunction
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactore malabsorption

Forms avail. in SA and covered in this monograph: tab

Contraception

Ethinylestradiol/ Desogestrel
0.15/0.02 (mg)
0.15/0.03 (mg)

• Oral (tab): 1 tab, dly for 21 days

THEN

Inactive tablets

• Oral (tab): 1 tab, dly for 7 days

Initiate with active tablets on the appropriately marked day

Initiate on day 1 of the menstrual cycle (1st day of menstruation = 1st day of cycle)

See additional prescribing points

Not established for use in children below 18 years

Pregnancy

• Contraindicated
• Ethinylestradiol/desogestrel is not indicated in pregnancy. If pregnancy occurs during the use of ethinylestradiol/desogestrel the preparation should be withdrawn immediately. Extensive epidemiological studies have revealed neither an increased risk of birth defects in children born to women who used combined oral contraceptives (COCs) prior to pregnancy nor a teratogenic effect when COCs were taken inadvertently during pregnancy

Breastfeeding

• Caution; not recommended
• Lactation may be influenced by COCs as they may reduce the quantity and change the composition of breast milk. Therefore, the use of COCs should generally not be recommended until the breastfeeding mother has completely weaned her child. Small amounts of the contraceptive steroids and/or their metabolites may be excreted with the milk during COC use. These amounts may affect the child

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Mild (Child-Pugh Class A): Caution; no dose adjustment recommended
  Consider alternative methods for chronic use
• Moderate (Child-Pugh Class B): Avoid oral contraceptive formulations (pills/tab); Consider use/switch to other preparations such as patches, vaginal ring, injections, implants or IUD (condition-based preparation)
• Severe (Child-Pugh Class C):  Contraindicated

Elderly

• Not indicated for use in geriatric patients

Porphyria Information

• Probably porphyrinogenic (PRP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Depressed mood
• Altered mood
• Decreased libido
• Increased libido 
• Headache
• Dizziness
• Nervousness
• Migraine

Cardiovascular Disorders

• Hypertension
• Venous thromboembolism
• Arterial thromboembolism

Gastrointestinal Disorders

• Nausea and vomiting
• Abdominal pain

Genitourinary Disorders

• Vaginal candidiasis
• Irregular bleeding
• Amenorrhea
• Breast tenderness
• Breast pain
• Breast hypertrophy
• Metrorrhagia
• Vaginal discharge
• Breast discharge

Endocrine and Metabolic Disorders

• Fluid retention

Skin and Subcutaneous Tissue Disorders

• Acne
• Rash
• Urticaria
• Erythema nodosum
• Erythema multiforme
• Pruritus
• Alopecia

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity

Sensory Disorders

• Otosclerosis
• Contact lens intolerance

• CYP450 inducers
• Ampicillin
• Tetracyclines
• Ciclosporin
• Lamotrigine

• Physical examination
• Pregnancy test
• Blood pressure

Specific cases may require

• Mental status
• Blood glucose
• Lipid profile
• Hepatic function
• Weight
• Endometrial sampling

Initiating in special circumstances

• First trimester abortion: Can be initiated immediately (no additional contraception required)
• Postpartum or second trimester abortion: Initiate on day 21-28 postpartum/post-abortion; If initiating later than 28 days, additional non-hormonal contraception required for 9 days

Special circumstances requiring additional contraception

• Vomiting 3-4hrs after taking active tablet: Take addition, corresponding tablet from another blister pack

Missed dose

• Single tablet forgotten and less than 12hrs late: Take missed tablet as soon as remembered and take further tablets at their usual time
• Single tablet forgotten and more than 12hrs late: Take missed tablet as soon as remembered and take further tablets at their usual time. No more than 2 tablets to be taken on a given day. 

No preceding hormonal contraceptive use (in the past month)

• Tablet-taking has to start on day 1 of the woman's natural cycle (i.e. the first day of her menstrual bleeding). Starting on day 2-5 is allowed, but during the first cycle, a barrier method is recommended in addition for the first 7 days of tablet-taking.

Changing from another combined hormonal contraceptive (combined oral contraceptive (COC), vaginal ring, or transdermal patch)

• The woman should start treatment preferably on the day after the last active tablet (the last tablet containing the active substances) of her previous COC, but at the latest on the day following the usual tablet-free or placebo tablet interval of her previous COC.
• In case a vaginal ring or a transdermal patch has been used, the woman should start using treatment preferably on the day of removal, but at the latest when the next application would have been due.

Changing from a progestogen-only method (progestogen only-pill, injection, implant) or from a progestogen-releasing intrauterine system (IUS)

• The woman may switch any day from the progestogen-only pill (from an implant or the IUS on the day of its removal, from an injectable when the next injection would be due) but should in all of these cases be advised to additionally use a barrier method for the first 7 days of tablet-taking

The contraceptive effect of combined oral contraceptives is based on the interaction of various factors, the most important of which are seen as the inhibition of ovulation and changes in the cervical secretion. Ethinylestradiol is a well known synthetic oestrogen. Desogestrel is a synthetic progestogen. After oral administration it has a strong ovulation-inhibiting activity.

COMBINATION PREPARATIONS

Low dose monophasic preparations

Ethinylestradiol/ Desogestrel

Tablet 20μg/150μg

• Mercilon (MSD) originator
• Novynette ( Acino Pharma)

Tablet 30μg/150μg

• Marvelon (MSD) originator