Dienogest


Concise Prescribing Info
Indications/Uses
Endometriosis.
Dosage/Direction for Use
Adult : PO 2 mg once daily.
Dosage Details
Oral
Endometriosis
Adult: 2 mg once daily given in a continuous regimen regardless of menstrual bleeding.
Child: ≥12 yr (postmenarche): Same as adult dose.
Hepatic Impairment
Severe: Contraindicated.
Administration
May be taken with or without food.
Contraindications
Active venous thromboembolic disorder, active or history of arterial and CV disease (e.g. MI, CVA, ischaemic heart disease), DM w/ vascular involvement, presence or history of liver tumour, sex-hormone dependent malignancies, undiagnosed vag bleeding, ocular lesion due to vascular ophth disease (e.g. partial or complete visual loss, defect in visual fields), migraine w/ focal aura. Severe hepatic (e.g. cirrhosis) impairment. Pregnancy and lactation.
Special Precautions
Patient w/ multiple risk factors for CV disease (e.g. old age, HTN, DM, hypercholesterolemia, morbid obesity, smoker), history of depression or gestational DM. Childn.
Adverse Reactions
Significant: Menstrual bleeding irregularity (e.g. amenorrhea, prolonged bleeding, frequent/infrequent bleeding), increased risk of venous thromboembolism, plateauing and loss of BMD, HTN, chloasma, ovarian cyst. Rarely, liver tumours.
Nervous: Depression, headache, dizziness, lethargy, sleep disorder, nervousness, irritability, migraine.
GI: Nausea, vomiting, abdominal pain.
Hepatic: Cholestatic jaundice.
Genitourinary: Vag haemorrhage, spotting.
Endocrine: Decreased libido, wt gain, breast discomfort.
Musculoskeletal: Weakness.
Dermatologic: Acne, alopecia, androgenic effects (e.g. hirsutism, greasy hair).
Immunologic: Hypersensitivity.
Patient Counseling Information
Avoid smoking.
MonitoringParameters
Perform pregnancy test prior to initiation of therapy. Assess BP, pap smear, breast exam, mammogram. Monitor BMD (adolescent females), signs and symptoms of thromboembolic disorders, vision changes.
Drug Interactions
Increased exposure w/ CYP3A4 enzyme inhibitors (e.g. azole antifungals, verapamil, macrolides, diltiazem, antidepressants). Decreased therapeutic effect w/ CYP3A4 enzyme inducers (e.g. phenytoin, barbiturates, primidone, carbamazepine, rifampicin, topiramate, griseofulvin).
Food Interaction
Decreased therapeutic effect w/ St John’s wort. Increased exposure w/ grapefruit juice.
Lab Interference
May interfere w/ LFT and endocrine function test.
Action
Description: Dienogest, a nonethinylated progestogen, reduces oestradiol production, thereby suppressing oestradiol’s trophic effects on both eutopic and ectopic endometrium. It leads to hypoestrogenic, hyperestagenic endocrine environment causing initial decidualisation of endometrial tissue followed by atrophy of endometriotic lesions when continuously given. It also has immunologic, antiproliferative, and antiangionenic effects which inhibit cellular proliferation.
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed. Bioavailability: Approx 91%. Time to peak plasma concentration: Approx 1.5 hr.
Distribution: Volume of distribution: 40 L. Plasma protein binding: Approx 90%.
Metabolism: Metabolised in the liver by CYP3A4 enzyme to inactive metabolites.
Excretion: Via urine, mainly as inactive metabolite. Elimination half-life: 14 hr.
Chemical Structure

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Dienogest, CID=68861, https://pubchem.ncbi.nlm.nih.gov/compound/Dienogest (accessed on Jan. 21, 2020)

Storage
Store between 15-30°C.
ATC Classification
G03DB08 - dienogest ; Belongs to the class of pregnadien derivative progestogens used in progestogenic hormone preparations.
References
Anon. Dienogest. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/05/2017.

Buckingham R (ed). Dienogest. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/05/2017.

Disclaimer: This information is independently developed by MIMS based on Dienogest from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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