Desogestrel

Oral
Contraception

Severe: Contraindicated.

Undiagnosed abnormal vaginal bleeding, known or suspected sex-steroid sensitive malignancies, active venous thromboembolic disorder. Severe hepatic impairment (current or history of, particularly if LFTs have not returned to normal). Pregnancy.

Patient with history of breast cancer, history of thromboembolic disorders; hypertension, diabetes, liver tumour or cancer, SLE, porphyria; history of chloasma gravidarum. Patients undergoing surgery or those who experience prolonged immobilisation. Mild to moderate hepatic impairment. Lactation.

Significant: Bleeding irregularities, increased risk for breast cancer; increased risk of thromboembolism (e.g. DVT, pulmonary embolism), decreased glucose tolerance, significant or sustained hypertension, chloasma; depression and mood changes. Rarely, ectopic pregnancy.
Eye disorders: Contact lens intolerance.
Gastrointestinal disorders: Nausea, vomiting.
General disorders and administration site conditions: Fatigue.
Immune system disorders: Angioedema.
Investigations: Increased weight.
Nervous system disorders: Headache.
Reproductive system and breast disorders: Decreased libido, breast pain, irregular menstruation, amenorrhoea, dysmenorrhoea, ovarian cyst, vaginal infection.
Skin and subcutaneous tissue disorders: Acne, alopecia.

PO: Z (Not recommended or not indicated for use during pregnancy.)

Women predisposed to chloasma should avoid exposure to sunlight or UV light during treatment; use protective measures (e.g. sunscreen, loose-fitting clothes) when going outdoors.

Evaluate pregnancy status before treatment initiation. Monitor blood pressure, weight, BMI (at baseline to help check changes during therapy), health status changes, and glycaemic control (in diabetic patients). Assess for signs of depression (including suicidal thoughts) and abnormal vaginal bleeding.

Symptoms: Nausea, vomiting, and slight vaginal bleeding (in young women). Management: Symptomatic treatment.

Diminished contraceptive effect with enzyme inducers (e.g. barbiturates, bosentan, carbamazepine, phenytoin, primidone, rifampicin, efavirenz, felbamate, griseofulvin, oxcarbazepine, topiramate, rifabutin). May increase or decrease plasma concentrations with HIV protease inhibitors (e.g. ritonavir, nelfinavir), non-nucleoside reverse transcriptase inhibitors (e.g. nevirapine), and agents for hepatitis C virus (e.g. boceprevir, telaprevir). Strong (e.g. ketoconazole, itraconazole, clarithromycin) and moderate (e.g. fluconazole, diltiazem, erythromycin) CYP3A4 inhibitors may increase the plasma levels of desogestrel. Absorption and contraceptive effect may be reduced with activated charcoal. May increase the plasma and tissue concentrations of ciclosporin. May decrease the plasma and tissue concentrations of lamotrigine.

Diminished contraceptive effect with St. John's wort.

May interfere with the results of tests for coagulation factors, lipids, glucose tolerance, thyroxine-binding globulin, sex hormone-binding globulin, and cortisol-binding globulin.

Description:
Mechanism of Action: Desogestrel is a progestogen-only contraceptive agent. Its active metabolite, etonogestrel, exerts its contraceptive effect by inhibiting ovulation, increasing cervical mucous viscosity, and suppressing endometrial proliferation.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed. Bioavailability: Approx 70-80% (etonogestrel). Time to peak plasma concentration: Approx 2 hours (etonogestrel).
Distribution: Etonogestrel: Enters breast milk (small amounts). Plasma protein binding: 96-99%, mainly to albumin and to a lesser extent to sex hormone-binding globulin.
Metabolism: Metabolised in the liver and intestinal mucosa via hydroxylation and dehydrogenation by CYP3A4 isoenzyme into the active metabolite, etonogestrel (3-keto-desogestrel), then undergoes further metabolism via sulfate and glucuronide conjugation.
Excretion: Etonogestrel: Via urine (approx 60% as metabolites); faeces (approx 40% as metabolites). Elimination half-life: Approx 20-30 hours (etonogestrel).

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 40973, Desogestrel. https://pubchem.ncbi.nlm.nih.gov/compound/Desogestrel. Accessed June 25, 2025.

Store below 30°C. Protect from light and moisture.

Oral Contraceptives

G03AC09 - desogestrel ; Belongs to the class of progestogens. Used as systemic contraceptives.

Brayfield A, Cadart C (eds). Desogestrel. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/04/2025.

Cerazette Film-coated Tablets, 75 microgram (Organon Malaysia Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 10/04/2025.

Cerelle 75 microgram Film-coated Tablets (Gedeon Richter Plc.). MHRA. https://products.mhra.gov.uk. Accessed 10/04/2025.

Desogestrel. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 10/04/2025.

Joint Formulary Committee. Desogestrel. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/04/2025.

Organon (New Zealand) Limited. Cerazette 75 microgram Film-coated Tablet data sheet 20 July 2021. Medsafe. http://www.medsafe.govt.nz. Accessed 10/04/2025.