Adult: Available preparations:
Desogestrel 0.15 mg and ethinylestradiol 0.02 mg tab
Desogestrel 0.15 mg and ethinylestradiol 0.03 mg tab
1 tab 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
Contraindicated.
Contraindications
Current, suspected, or history of breast cancer, or other oestrogen- or progestin-dependent malignancies; presence or history of hepatic tumours (benign or malignant), endometrial hyperplasia, undiagnosed vaginal bleeding, venous or arterial thromboembolism (VTE/ATE) (e.g. DVT, pulmonary embolism, MI, angina pectoris, stroke, TIA), multiple risk factors for VTE/ATE (e.g. diabetes mellitus with vascular changes, severe or uncontrolled hypertension, severe dyslipoproteinaemia, coronary artery disease, major surgery with prolonged immobilisation, obesity [BMI >30 kg/m2]), known hereditary or acquired predisposition to VTE/ATE (e.g. activated protein C [APC] resistance, Factor V Leiden mutation, antithrombin-III-deficiency, protein C and S deficiency, hyperhomocysteinaemia, antiphospholipid antibodies), presence or history of CVA, history of migraine with aura (focal symptoms); pancreatitis, previous cholestatic jaundice of pregnancy or jaundice prior oral contraceptive use; SLE with unknown or positive antiphospholipid antibodies; acute porphyria. Women >35 years who smoke. Hepatic impairment. Pregnancy and lactation. Concomitant use with hepatitis C combination therapy containing ombitasvir/paritaprevir/ritonavir with or without dasabuvir.
Special Precautions
Women with CV disease-related risk factors (e.g. hypertension, prediabetes or diabetes, low HDL, high LDL or triglycerides), gallbladder disease, diseases exacerbated by fluid retention (e.g. asthma, epilepsy), SLE, hereditary angioedema, depression, history of migraine, chloasma gravidarum, haemolytic uraemic syndrome, sickle cell disease, chronic inflammatory bowel disease, severe gastrointestinal disturbances; who wear contact lens or undergone bariatric surgery. Smokers. Not recommended in women with complicated organ transplant and acute viral hepatitis. Not indicated for use prior to menarche, or in postmenopausal women. Renal impairment.
Adverse Reactions
Significant: Breakthrough or intracyclic bleeding, spotting; breast cancer, cervical cancer, impaired lipid levels (including serum triglycerides), impaired glucose tolerance, increased blood pressure, retinal vein thrombosis, depression or depressed mood, persistent or severe headache/migraine, gallbladder disease, induced or exacerbated angioedema, chloasma, cholestasis; Crohn’s disease, ulcerative colitis, jaundice, porphyria, SLE. Rarely, hepatocellular carcinoma (prolonged use). Eye disorders: Contact lens intolerance. Gastrointestinal disorders: Nausea, vomiting, abdominal pain, diarrhoea. Investigations: Weight gain. Metabolism and nutrition disorders: Fluid retention. Reproductive system and breast disorders: Breast pain, breast tenderness, amenorrhoea, decreased libido. Skin and subcutaneous tissue disorders: Acne, rash, urticaria. Potentially Fatal: Increased risk of VTE/ATE (e.g. DVT, pulmonary embolism, MI). Rarely, hepatic adenomas or tumours (benign or malignant).
Screen for pregnancy before initiating treatment. Perform adequate diagnostic measures to rule out malignancy in all cases of undiagnosed abnormal vaginal bleeding; physical exams concerning the breasts, pelvis, and cervical screening when necessary. Monitor blood pressure prior to therapy and yearly; glucose (in diabetics), lipid profiles (in hyperlipidaemic patients), LFT, BMI at baseline. Assess for vision changes; signs and symptoms of thromboembolic disorders, breakthrough bleeding, and depression.
Overdosage
Symptoms: Nausea, vomiting, and slight vaginal bleeding in young women. Management: Symptomatic treatment.
Drug Interactions
Diminished efficacy and an increased risk of breakthrough bleeding with enzyme inducers (e.g. phenytoin, barbiturates, carbamazepine, bosentan, felbamate, griseofulvin, oxcarbazepine, rifampicin, topiramate, rifabutin, rufinamide, ritonavir, efavirenz). May increase the plasma concentrations with CYP3A4 inhibitors (e.g. ketoconazole, clarithromycin, diltiazem). May increase the plasma concentrations of ciclosporin. May significantly decrease the plasma concentrations of lamotrigine. May increase or decrease the plasma levels with HIV protease inhibitors (e.g. nelfinavir), non-nucleoside reverse transcriptase inhibitors (e.g. nevirapine) and agents for hepatitis C virus (e.g. boceprevir, telaprevir).
Ethinylestradiol: Plasma concentrations and exposure may be increased by ascorbic acid and atorvastatin or rosuvastatin, respectively. May inhibit the metabolism and increase the plasma levels of theophylline and tizanidine. Potentially Fatal: Increased risk of ALT elevations with ombitasvir/paritaprevir/ritonavir and dasabuvir.
Food Interaction
Diminished efficacy and increased risk of breakthrough bleeding with St. John’s wort. Increased plasma concentrations if given with grapefruit juice.
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: Mechanism of Action: Desogestrel and ethinylestradiol suppress ovulation by negative feedback mechanism on the hypothalamus that changes the normal gonadotropin secretion pattern of FSH and LH by the anterior pituitary gland, thereby blocking the follicular FSH phase and midcycle surge of gonadotropins. They also alter the tubal transport of the ova through the fallopian tubes and the genital tract. The changes in cervical mucus and in the endometrium lead to the inhibition of sperm penetration and unfavourable environment for nidation, respectively.
Desogestrel is a progestogen structurally related to levonorgestrel.
Ethinylestradiol is a synthetic oestrogen with similar effects as estradiol. Pharmacokinetics: Absorption: Desogestrel: Rapidly and completely absorbed from the gastrointestinal tract. Bioavailability: Approx 62-84%. Time to peak plasma concentration: Approx 1-2 hours.
Ethinylestradiol: Rapidly and completely absorbed from the gastrointestinal tract. Bioavailability: Approx 40-60%. Time to peak plasma concentration: 1-2 hours. Distribution: Enters breast milk.
Desogestrel: Plasma protein binding: 98-99% (as etonogestrel), mainly to albumin and to sex hormone-binding globulin (SHBG).
Ethinylestradiol: Plasma protein binding: 98%, mainly to albumin. Metabolism: Desogestrel: Metabolised in the liver and intestinal mucosa via hydroxylation into its active metabolite, 3-keto-desogestrel (etonogestrel).
Ethinylestradiol: Undergoes significant gut and hepatic first-pass metabolism; metabolised in the liver via aromatic hydroxylation by CYP3A4 isoenzyme into 2-hydroxyethinylestradiol and other methylated metabolites. Excretion: Via urine and faeces (as metabolites).
Desogestrel: Terminal elimination half-life: Approx 30 hours (as etonogestrel).
Ethinylestradiol: Terminal elimination half-life: Approx 24 hours.
Chemical Structure
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)
Ethinylestradiol Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5991, Ethinylestradiol. https://pubchem.ncbi.nlm.nih.gov/compound/Ethinylestradiol. Accessed Apr. 27, 2022.
G03AA09 - desogestrel and ethinylestradiol ; Belongs to the class of progestogens and estrogens in fixed combinations. Used as systemic contraceptives.
References
Anon. Estrogen-Progestin Combinations. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 08/07/2020.Anon. Ethinyl Estradiol and Desogestrel. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/07/2020.Apri 28 Day (Teva Pharmaceuticals USA, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 08/07/2020.Azurette (Mayne Pharma Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/07/2020.Buckingham R (ed). Desogestrel. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/07/2020.Buckingham R (ed). Ethinylestradiol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/07/2020.Joint Formulary Committee. Ethinylestradiol with Desogestrel. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/07/2020.Marvelon (Merck Sharp & Dohme Limited). MHRA. https://products.mhra.gov.uk/. Accessed 08/07/2020.Mercilon Tablets (Merck Sharp & Dohme [Malaysia] Sdn. Bhd.). MIMS Malaysia. http://www.mims.com/malaysia. Accessed 23/07/2020.
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