Dienogest

Oral
Endometriosis

Severe: Contraindicated.

May be taken with or without food.

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.

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.

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.

Avoid smoking.

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.

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).

Decreased therapeutic effect w/ St John’s wort. Increased exposure w/ grapefruit juice.

May interfere w/ LFT and endocrine function test.

Description:
Mechanism of Action: 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.

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

Store between 15-30°C.

Oestrogens, Progesterones & Related Synthetic Drugs

G03DB08 - dienogest ; Belongs to the class of pregnadien derivative progestogens used in progestogenic hormone preparations.

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.