Gestodene/ Ethinylestradiol

Registered South African indications:

• Contraception

Contraindications

• Hypersensitivity to the active ingredients or any of the excipients in this combination product
• Presence or history of venous or arterial thrombotic/thromboembolic events (e.g. deep venous thrombosis, pulmonary embolism, myocardial infarction) or cerebrovascular accident
• Cerebrovascular or coronary artery disease
• Thrombogenic valvulopathies
• Thrombogenic rhythm disorders
• Hereditary or acquired thrombophilias
• Presence or history of prodromi of a thrombosis (e.g. transient ischaemic attack, angina pectoris)
• History of migraine with focal neurological symptoms
• Diabetes mellitus with vascular involvement
• Uncontrolled hypertension
• A high risk of venous or arterial thrombosis
• Presence or history of hepatic disease as long as liver function values have not returned to normal
• Presence or history of liver tumours (benign or malignant)
• Known or suspected sex-steroid influenced malignancies (e.g. of the genital organs or breasts)
• Undiagnosed vaginal bleeding
• Pancreatitis or a history thereof if associated with severe hypertriglyceridaemia
• Concomitant use with certain anti-viral hepatitis C virus (HCV) medicines such as ombitasvir, paritaprevir, ritonavir, and dasabuvir
• Known or suspected pregnancy
• Depression not well controlled with treatment
• History of depression with the use of hormonal contraceptives

Cautions

• Breastfeeding
• Renal impairment
• Mild to moderate hepatic impairment
• Malignancy
• Haemolytic uraemic syndrome
• Chronic inflammatory bowel disease
• Sickle cell disease
• Family history of venous thromboembolism
• Older than 35 years
• Smoking
• Hypertension
• Obesity
• Family history of arterial thromboembolism
• Migraine
• Diabetes mellitus
• Hyperhomocysteinaemia
• Valvular heart disease
• Atrial fibrillation
• Systemic lupus erythematosus
• Porphyria
• Cardiovascular disease
• Hypertriglycerodaemia
• Hereditary angioedema
• Risk factors for breast cancer
• Risk factors for estrogen-dependant tumours
• Any other condition that is known to worsen during pregnancy or with previous use of combined oral contraceptives
• Galactose intolerance
• Lapp lactase deficiency
• Fructose intolerance
• Glucose-galactose malabsorption
• Sucrase-isomaltase deficiency

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

Contraception

Low dose monophasic preparation
Gestogene/ Ethinyloestradiol
60/15 (μg)

• Oral (tab): 1 tablet, dly for 24 days

THEN

• Inactive tablets: Oral (tab): 1 tablet, dly for 4 days

Low dose monophasic preparation
Gestogene/ Ethinyloestradiol
75/20 (μg)

• Oral (tab): 1 tablet, dly for 21 days

THEN

• Inactive tablets: Oral (tab): 1 tablet, dly for 7 days

Low dose monophasic preparation
Gestogene/ Ethinyloestradiol
75/30 (μg)

• Oral (tab): 1 tablet, dly for 21 days

THEN

• Inactive tablets: Oral (tab): 1 tablet, dly for 7 days

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For all low dose monophasic preparations:

Take tablets at the same time everyday

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

No additional contraception required if initiated on day 1 of the menstrual cycle; However if initiating on day 2-5 (which is also acceptable), a non-hormonal contraceptive required for 7 days

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A withdrawal bleed usually starts on days 2-3, after the last active tablet, and may not have finished before the next pack needs to be started

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Low dose triphasic preparations

• Oral (tab): 1 tablet, dly as per manufacturer recommendations

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

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Use additional non-hormonal method of contraception for the first 14 days of the first treated cycle

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See additional prescribing points

Not indicated for use in premenarchal children

Pregnancy

• Contraindicated

Breastfeeding:

• Caution; not recommended
• The use of gestodene/ethinyloestradiol during breastfeeding may lead to a reduction in the volume of milk produced and to a change in its composition. Minute amounts of the active substances are excreted with the milk. These amounts may affect the child particularly in the first 6 weeks postpartum. Mothers who are breastfeeding may be advised instead to use another method of contraception

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Contraindicated

Elderly

• Not indicated for use in geriatric patients

Porphyria Information

• Not yet classified (NC)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Headache
• Migraine
• Depressed mood
• Altered mood
• Decreased libido
• Increased libido
• Exacerbation of chorea

Cardiovascular Disorders

• Venous thromboembolism
• Arterial thromboembolism

Gastrointestinal Disorders

• Nausea and vomiting
• Abdominal pain
• Diarrhoea
• Ulcerative colitis

Hepatobiliary Disorders

• Disturbances in liver function

Genitourinary Disorders

• Vaginal discharge
• Abnormal uterine bleeding

Endocrine and Metabolic Disorders

• Increased weight
• Decreased weight
• Breast pain
• Breast hypertrophy
• Breast discharge
• Amenorrhoea

Skin and Subcutaneous Tissue Disorders

• Fluid retention
• Rash
• Urticaria
• Erythema nodosum
• Erythema multiforme
• Chloasma

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity reactions
• Exacerbation of hereditary angioedema

Sensory Disorders

• Contact lens intolerance

• Ombitasvir
• Paritaprevir
• Ritonavir
• Dasabuvir
• CYP3A4 inducers
• CYP3A4 inhibitors
• Etoricoxib
• Cyclosporin
• Tizanidine
• Theophylline
• Lamotrigine

• Blood pressure
• Physical examination

Specific cases may require

• Blood glucose
• Lipid profile

Initiating in special circumstances

• Post-partum: Combination oral contraceptives are discouraged immediately postpartum in the first 6 weeks due to the venous thromboembolic risk, and contraindicated in breastfeeding womenIn a non-lactating patient more than 6 weeks postpartum: initiate as per adult dosages section
• 1st trimester abortion: can be initiated immediately; No additional contraception required

Special circumstances requiring additional contraception

• If vomiting or diarrhoea occurs within 4 hours of taking active tablet dose, take another dose from another blister pack. Additional non-hormonal contraception required for the next 7 days. If the 7 days additional contraception will extend beyond the last active tablet, the user should finish taking all the active tablets, discard the placebo tablets and start a new pack of the next day with an appropriate active tablet

Missed dose

• If active tablet dose delayed by less than 12hrs, contraceptive protection is maintained. If longer than 12hrs, only the most recently delayed tablet should be taken, earlier missed tablets being omitted, and additional non-hormonal methods of contraception should be used for the next 7 days, while the next 7 active tablets are being taken. If the 7 days additional contraception will extend beyond the last active tablet, the user should finish taking all the active tablets, discard the placebo tablets and start a new pack on the next day with an appropriate active tablet

This oestrogen-progestogen combination acts by inhibiting ovulation by suppression of the mid-cycle surge of luteinising hormone, the inspissation of cervical mucus so as to constitute a barrier to sperm and the rendering of the endometrium unreceptive to implantation.

COMBINATION PREPARATIONS

Low dose monophasic preparations

Ethinyloestradiol/ Gestodene

Tablet 15μg/60μg

• Minesse (Pfizer) originator
• Mirelle (Bayer) originator

Tablet 20μg/75μg

• Melodene (Bayer) originator

Tablet 30μg/75μg

• Femodene ED (Bayer) originator
• Minulette (Pfizer) originator

Low dose triphasic preparations

Tablet 30μg/50μg

• Triodene (Bayer) originator (Discontinued)