Desogestrel


Concise Prescribing Info
Indications/Uses
Contraception.
Dosage/Direction for Use
Adult : PO 1 tab (75 mcg) once daily, exactly as directed from the blister pack. Refer to individual product guideline on how to manage missed doses and for detailed dosing instructions.
Dosage Details
Oral
Contraception
Adult: 1 tab (75 mcg) once daily, exactly as directed from the blister pack. Doses must be taken continuously at the same time each day. Refer to individual product guideline on how to manage missed doses and for detailed dosing instructions.
Hepatic Impairment
Severe: Contraindicated.
Contraindications
Known or suspected sex-steroid sensitive malignancies, undiagnosed vaginal bleeding, active venous thromboembolic disorder, acute porphyria. Severe hepatic impairment (active or history). Pregnancy.
Special Precautions
Women with breast cancer, liver cancer, functional ovarian cyst; hypertension, history of thromboembolic disorders; previous ectopic pregnancy; diabetes mellitus, severe gastrointestinal disturbances, SLE with positive (or unknown) antiphospholipid antibodies; depression, migraine; history of chloasma gravidarum. Women undergoing prolonged immobilisation due to surgery or illness. Mild to moderate hepatic impairment. Lactation.
Adverse Reactions
Significant: Breakthrough bleeding, venous thromboembolism (e.g. DVT, pulmonary embolism), hypertension, SLE, porphyria, chloasma; depressed mood and depression.
Eye disorders: Contact lens intolerance.
Gastrointestinal disorders: Nausea, vomiting.
General disorders and administration site conditions: Fatigue.
Investigations: Increased weight.
Nervous system disorders: Headache.
Pregnancy, puerperium and perinatal conditions: Rarely, ectopic pregnancy.
Psychiatric disorders: Mood alterations.
Reproductive system and breast disorders: Breast pain, irregular menstruation, amenorrhoea, dysmenorrhoea, ovarian cyst, decreased libido.
Skin and subcutaneous tissue disorders: Acne, alopecia.
MonitoringParameters
Screen for pregnancy and perform diagnostic measures for bleeding disturbances (e.g. amenorrhoea, oligomenorrhoea) before initiating treatment. Monitor for amenorrhoea or abdominal pain as it must be considered for the differential diagnosis of ectopic pregnancy; signs and symptoms of depression and breakthrough bleeding.
Overdosage
Symptoms: Nausea, vomiting, and slight vaginal bleeding in young women. Management: Symptomatic treatment.
Drug Interactions
Decreased contraceptive efficacy with enzyme inducers (e.g. barbiturates, bosentan, carbamazepine, phenytoin, primidone, rifampicin, efavirenz, felbamate, griseofulvin, oxcarbazepine, topiramate, and rifabutin). May increase the plasma concentrations with CYP3A4 inhibitors (e.g. ketoconazole, erythromycin, diltiazem). May increase or decrease the plasma concentrations with HIV protease inhibitors (e.g. ritonavir), agents for hepatitis C virus (e.g. boceprevir), and non-nucleoside reverse transcriptase inhibitors (e.g. nevirapine). May increase the plasma and tissue levels of ciclosporin. May decrease the plasma and tissue levels of lamotrigine.
Food Interaction
Diminished contraceptive effect with St. John’s wort.
Lab Interference
May affect the results of biochemical parameters of the thyroid, adrenal, liver, and renal function tests. May interfere with tests for carrier proteins (e.g. corticosteroid-binding globulin, lipid/lipoprotein fractions), carbohydrate metabolism, fibrinolysis and coagulation.
Action
Description: Desogestrel is a progestogen structurally related to levonorgestrel. It inhibits ovulation and increases the viscosity of cervical mucous to produce its contraceptive effect.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Absolute bioavailability: 70%. Time to peak plasma concentration: Approx 1-2 hours.
Distribution: Enters breast milk (as etonogestrel). Plasma protein binding: 95-99% (as etonogestrel), mainly to albumin and to a lesser extent to sex hormone binding globulin.
Metabolism: Metabolised in the liver and the intestinal mucosa via hydroxylation and dehydrogenation into its active metabolite, etonogestrel (3-keto-desogestrel); undergoes further metabolism via sulfate and glucuronide conjugation.
Excretion: Via urine and faeces (as free steroid hormone or as conjugates). Elimination half-life: Approx 30 hours (as etonogestrel).
Chemical Structure

Chemical Structure Image
Desogestrel

Source: National Center for Biotechnology Information. PubChem Database. Desogestrel, CID=40973, https://pubchem.ncbi.nlm.nih.gov/compound/40973 (accessed on July 28, 2020)

Storage
Store below 30°C. Protect from light and moisture.
MIMS Class
ATC Classification
G03AC09 - desogestrel ; Belongs to the class of progestogens. Used as systemic contraceptives.
References
Anon. Desogestrel. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 22/07/2020.

Buckingham R (ed). Desogestrel. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/07/2020.

Cerazette Film-Coated Tablets 75 microgram (Merck Sharp & Dohme [Malaysia] Sdn. Bhd.). MIMS Malaysia. http://www.mims.com/malaysia. Accessed 22/07/2020.

Cerelle 75 Microgram Film-Coated Tablet (Gedeon Richter Plc.). MHRA. https://products.mhra.gov.uk/. Accessed 07/07/2020.

Desogestrel Oral. Medecins Sans Frontieres. https://medicalguidelines.msf.org/. Accessed 22/07/2020.

Joint Formulary Committee. Desogestrel. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/07/2020.

Merck Sharp & Dohme (New Zealand) Limited. Cerazette 75 Microgram Film-Coated Tablet data sheet 26 February 2019. Medsafe. http://www.medsafe.govt.nz/. Accessed 07/07/2020.

Disclaimer: This information is independently developed by MIMS based on Desogestrel 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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