Dienogest

Registered South African indications: 

• Endometriosis

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy
• Breastfeeding
• Severe hepatic impairment
• Porphyria
• Undiagnosed abnormal vaginal bleeding
• Active venous thromboembolic disorder
• Arterial and cardiovascular disease or history thereof
• Diabetes mellitus with vascular involvement
• Hepatic neoplasia or history thereof
• Known or suspected sex-hormone-dependent malignancy
• Ocular lesions due to ophthalmic vascular disease
• Migraine with focal aura or history thereof

Cautions

• Mild to moderate hepatic impairment
• Elderly
• Children
• Diabetes or a history of gestational diabetes mellitus
• History of chloasma
• History of cholestatic jaundice during pregnancy or due to the use of sex steroids
• History of pruritus during pregnancy or due to use of sex steroids
• Risk factors for venous thromboembolism
• Multiple risk factors for cardiovascular disease
• Depression
• Smoker
• Fibroids
• Breast cancer

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

Endometriosis

• Oral (tab): 2mg, dly

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

Take at the same time each day

See additional prescribing points

Not indicated for use in premenarchal children

Pregnancy

• Contraindicated
• Dienogest is contraindicated during pregnancy. No adverse events have been observed when a foetus, was unknowingly exposed to dienogest. Pregnancy should be excluded before initiation of treatment

Breastfeeding

• Contraindicated
• The excretion of dienogest in breast milk is unknown. The risk to the breastfeeding infant cannot be excluded. Dienogest use in breastfeeding mothers is contraindicated

Fertility

• Dienogest is indicated for the prevention of pregnancy

Renal Impairment

• No dose adjustment recommended

Hepatic Impairment

• Mild to moderate: Caution; no dose adjustment recommended
• Severe: Contraindicated

Elderly

• Not indicated for use in geriatric patients

Porphyria Information

• Probably porphyrinogenic (PRP)

 Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Sleep disorder
• Nervousness
• Loss of libido
• Altered mood 
• Anxiety
• Depression
• Mood swings
• Headache
• Migraine
• Autonomic nervous system imbalance
• Disturbance in attention
• Aesthenia
• Irritability

Cardiovascular Disorders

• Unspecified circulatory system disorder
• Palpitations
• Hypotension

Respiratory Disorders

• Dyspnoea

Gastrointestinal Disorders

• Nausea and vomiting
• Abdominal pain
• Flatulence
• Abdominal distention
• Diarrhoea
• Constipation
• Abdominal discomfort
• Gastrointestinal inflammation
• Gingivitis

Genitourinary Disorders

• Urinary tract infection
• Breast discomfort
• Ovarian cyst
• Hot flush
• Uterine/vaginal bleeding
• Vaginal candidiasis
• Vulvovaginal dryness
• Genital discharge
• Pelvic pain
• Atrophic vulvovaginitis
• Breast mass
• Fibrocystic breast diseases
• Breast induration

Endocrine and Metabolic Disorders

• Increased weight 
• Decreased weight
• Increased appetite

Musculoskeletal Disorders

• Back pain 
• Bone pain
• Muscle spasm
• Pain in extremity
• Heaviness in extremities

Skin and Subcutaneous Tissue Disorders

• Acne
• Alopecia
• Dry skin
• Hyperhidrosis
• Pruritus
• Hirsutism
• Onychoclasis
• Dandruff
• Dermatitis
• Abnormal hair growth
• Photosensitivity reaction
• Pigmentation disorder
• Oedema

Sensory Disorders

• Dry eyes
• Tinnitus

• Acitretin
• Anticoagulants
• Aprepitant
• Artemether
• Atazanavir
• Barbiturates
• Bexarotene 
• Bile acid sequestrants
• Boceprevir
• Bosentan
• Brigatinib
• Carfilzomib
• Clobazam
• Cobicistat
• CYP3A4 inducers
• Dabrafenib
• Darunavir
• Efavirenz
• Eslicarbazepine
• Felbamate
• Fosamprenavir
• Fosaprepitant
• Griseofulvin
• Ixazomib
• Lesinurad
• Lixisenatide
• Lopinavir
• Mifepristone
• Mycophenolate
• Nelfinavir
• Nevirapine
• Oxcarbazepine
• Perampanel
• Pomalidomide
• Prucalopride
• Retinoic acid derivatives
• Saquinavir
• St John's wort
• Sugammadex
• Telaprevir
• Tipranavir
• Topiramate
• Tranexamic acid
• Ulipristal
• Vitamin K antagonists

• Pregnancy test
• Papanicolaou smear
• Breast examination
• Mammogram

Specific cases may require

• Endometrial sampling
• Bone mineral density
• Ophthalmic examination

Missed dose

• Take one tablet only, as soon as remembered, and continue to take tablet at usual time the following day

Vomiting/ Diarrhoea

• A tablet not absorbed due to vomiting or diarrhoea, within 4hrs of taking tablet, should likewise be replaced by one tablet

Dienogest is a nortestosterone derivative with no androgenic activity. Dienogest binds to the progesterone receptor of the human uterus with only 10% of the relative affinity of progesterones. Despite its low affinity to the progesterone receptor, dienogest has a strong progestogenic effect in vivo. Dienogest has no significant androgenic, mineralocorticoid or glucocorticoid activity in vivo. Dienogest acts on endometriosis by abolishing the trophic effects of estradiol on both the eutopic and ectopic endometrium. When given continuously, dienogest leads to a hypoestrogenic, hypergestagenic endocrine environment and decidualisation of endometrial tissue.

Tablet 2mg

• Visanne (Bayer) originator

COMBINATION PREAPARATIONS

Multiphase preparations

Estradiol valerate/ Estradiol valerate/ Estradiol valerate/ Dienogest/ Dienogest

Tablet 1mg/2mg/3mg/2mg/3mg

• Qlaira (Bayer) originator