Desogen 15 mcg + 150 mcg Tablets

Brand Name

The medication is marketed under the brand name Desogen, a widely recognized label in the domain of hormonal contraception and reproductive health management.

International Nonproprietary Name (INN)

The active ingredients in this product are identified internationally as ethinyl estradiol and desogestrel, names standardized for consistency across global pharmacological practices.

Form of Release

Desogen is available as film-coated tablets, designed for oral administration. These tablets are typically packaged in 28-day blister packs, comprising 21 active hormone-containing tablets and 7 placebo tablets to maintain a continuous daily dosing routine.

Composition

Each active tablet of Desogen contains 0.03 mg of ethinyl estradiol and 0.15 mg of desogestrel as the primary hormonal components. The formulation includes several inactive ingredients, such as lactose monohydrate, which acts as a filler, and microcrystalline cellulose, providing structural support. Additional excipients like magnesium stearate serve as lubricants, while the film coating consists of hypromellose, polyethylene glycol, and titanium dioxide, often tinted with iron oxides to differentiate active from placebo tablets. The placebo tablets contain no hormones but mirror the inactive components to ensure uniformity in appearance and administration.

Pharmacologic Properties

Pharmacodynamics

Desogen operates as a combined oral contraceptive, harnessing the complementary actions of ethinyl estradiol and desogestrel to prevent pregnancy. The ethinyl estradiol, a synthetic estrogen, suppresses follicle-stimulating hormone (FSH) release from the pituitary, inhibiting follicular development, while also stabilizing the endometrial lining. Desogestrel, a third-generation progestin, blocks luteinizing hormone (LH) secretion, preventing the ovulatory LH surge, and thickens cervical mucus to hinder sperm passage. Together, these effects create a multi-layered barrier to conception, including endometrial changes that reduce implantation likelihood.

The low-dose estrogen and highly selective progestin formulation minimize androgenic activity compared to older contraceptives, offering a favorable profile for cycle control and side effect reduction. Clinical data show it achieves near-complete ovulation suppression when taken consistently, with additional benefits like lighter, more predictable menstrual bleeding. Its mechanism also mitigates symptoms of hormonal imbalance, such as acne or excessive hair growth, in some users. This dual-hormone approach ensures reliable contraception while supporting gynecological health.

Pharmacokinetics

Upon oral ingestion, Desogen components are absorbed rapidly from the gastrointestinal tract, with ethinyl estradiol peaking in plasma within 1 to 2 hours and desogestrel within 1 to 3 hours. Food intake has minimal impact on bioavailability, allowing dosing flexibility. Ethinyl estradiol binds to plasma proteins at 95–97%, mainly albumin, while desogestrel, after conversion to its active metabolite etonogestrel, binds at 95–98%, predominantly to sex hormone-binding globulin (SHBG) and albumin, targeting reproductive tissues.

Metabolism occurs primarily in the liver, where ethinyl estradiol undergoes extensive first-pass metabolism via cytochrome P450 enzyme CYP3A4, forming sulfate and glucuronide conjugates. Desogestrel is metabolized into etonogestrel, its bioactive form, also via CYP3A4, with further breakdown into inactive derivatives. The half-life of ethinyl estradiol is about 24 hours, and etonogestrel’s is 25–30 hours, supporting once-daily dosing. Excretion is chiefly urinary for ethinyl estradiol metabolites and biliary for desogestrel metabolites, with clearance completed within days of stopping the regimen.

Indications for Use

Desogen is primarily indicated for the prevention of pregnancy in women seeking a dependable hormonal contraceptive method. It is designed for those preferring a consistent withdrawal bleed that mimics a natural menstrual cycle. The medication is also prescribed to regulate irregular menstrual periods, reducing variability in timing and volume, and to alleviate dysmenorrhea by moderating hormonal fluctuations.

Secondary benefits may include improvement in acne or hirsutism due to desogestrel’s low androgenic activity, making it a suitable choice for women with these concerns. It can also decrease the incidence of functional ovarian cysts by suppressing ovulation, though this is not its primary purpose. These applications highlight its role as a versatile option for reproductive-age women balancing contraception and menstrual health needs.

Contraindications

Desogen is contraindicated in women with a history of venous or arterial thromboembolism, such as deep vein thrombosis, pulmonary embolism, or stroke, due to the heightened clotting risk linked to estrogen. It is also prohibited in those with known or suspected breast cancer, endometrial cancer, or other hormone-sensitive malignancies, as it could exacerbate these conditions.

Severe liver disease, including tumors or active hepatitis, rules out its use, given its hepatic metabolism. Uncontrolled hypertension, migraine with aura, or a history of myocardial infarction further restrict its application due to cardiovascular concerns. Women over 35 who smoke heavily should avoid it, as this combination significantly increases thromboembolism risk. Hypersensitivity to ethinyl estradiol, desogestrel, or any tablet component, such as lactose, is another absolute barrier.

Method of Administration and Dosage

Administration Guidelines

The tablets should be taken orally, swallowed whole with water to ensure consistent absorption. They can be consumed with or without food, offering flexibility in daily routines. Taking them at the same time each day optimizes efficacy, especially for the 21 active tablets, followed by 7 placebo tablets to maintain continuity during the hormone-free interval.

Dosage for Adults and Children

For adult women of reproductive age, the standard regimen of Desogen involves one tablet daily for 28 days, starting with an active tablet (0.03 mg ethinyl estradiol and 0.15 mg desogestrel) on the first day of menstruation or the first Sunday after it begins, depending on the prescribed schedule. The cycle repeats seamlessly, with each pack providing 21 hormonal tablets and 7 placebos. Adolescents post-menarche may use the same regimen under medical guidance, but pre-pubertal children are not eligible, as the drug targets ovulatory cycles.

Dose Adjustment in Specific Conditions

No dose adjustments are typically needed for renal impairment, as kidney clearance is secondary. In mild to moderate liver dysfunction, caution is advised due to metabolic reliance on the liver, but severe hepatic impairment contraindicates use entirely. Missed doses should be taken as soon as remembered, even if it means two tablets in one day, though backup contraception is recommended if more than 24 hours lapse. Adjustments for specific conditions should be tailored by a healthcare provider based on individual response.

Side Effects

Desogen may induce various side effects, though many women experience only mild or temporary reactions. Common issues include nausea, breast tenderness, or breakthrough bleeding, especially in the first few cycles as the body adapts. Headaches and mood changes, such as mild anxiety or irritability, are also reported, often resolving with continued use.

Less frequent effects include fluid retention, weight gain, or changes in libido, tied to hormonal shifts. Serious but rare reactions, such as thromboembolism (e.g., leg pain or shortness of breath), liver dysfunction (e.g., jaundice), or severe hypertension, require immediate cessation and medical attention. Allergic responses, like rash or swelling, are uncommon but warrant discontinuation if significant. Regular monitoring helps manage these effects and ensures the therapy remains suitable.

Overdose

Symptoms of Overdose

Excessive intake of Desogen is unlikely to cause acute, life-threatening symptoms due to its low hormonal doses. Overdose may present as intensified side effects, such as nausea, vomiting, or vaginal bleeding, reflecting an exaggerated hormonal response. Severe outcomes are rare, but prolonged excess could heighten risks like headache or fatigue.

First Aid Measures

In case of overdose, medical advice should be sought, though emergency measures are seldom needed. No specific antidote exists, so treatment focuses on symptom relief, such as antiemetics for nausea or rest for discomfort. Monitoring is advised until symptoms resolve, typically within hours to days, given the drugs’ rapid clearance.

Drug Interactions

Effects on Other Medications

Desogen can be affected by drugs that induce cytochrome P450 enzymes, particularly CYP3A4, such as rifampin, phenytoin, or St. John’s wort, which may accelerate metabolism and reduce contraceptive efficacy. This interaction necessitates backup contraception during and for 28 days after such co-administration. Inhibitors like ketoconazole might increase hormone levels, though this is rarely significant.

The medication may elevate levels of drugs like cyclosporine by competing for metabolic pathways, requiring dose adjustments. Broad-spectrum antibiotics like penicillin typically do not interfere, unless they indirectly affect enzyme activity. A comprehensive medication review with a healthcare provider ensures safe co-use.

Compatibility with Alcohol and Food

Moderate alcohol consumption does not diminish the drug’s effectiveness, allowing typical social use without concern. Food intake has minimal impact on absorption, so tablets can be taken with meals or on an empty stomach, accommodating individual preferences effortlessly.

Special Precautions

Use During Pregnancy and Breastfeeding

Desogen is contraindicated in pregnancy, as it is designed to prevent conception, and hormonal exposure could pose risks to fetal development if continued inadvertently. Women should discontinue use immediately if pregnancy is confirmed and consult a doctor. During breastfeeding, it is not recommended, especially in the first six weeks postpartum, as desogestrel may pass into milk and affect infant growth, while ethinyl estradiol could reduce milk production.

Progestin-only options are preferred during lactation until breastfeeding stabilizes, with Desogen considered only if non-hormonal methods are unsuitable and benefits outweigh risks.

Impact on Driving and Operating Machinery

The medication does not typically impair cognitive or motor functions, making it safe for most women to drive or operate machinery. Rare instances of dizziness or fatigue suggest caution during initial use until personal response is established, particularly in the first cycle.

Considerations for Elderly and Pediatric Populations

Elderly women beyond reproductive age rarely use Desogen, as its contraceptive purpose becomes irrelevant post-menopause, and hormonal risks outweigh benefits. Adolescents post-menarche can use it effectively, with no significant differences in safety compared to adults, though pre-pubertal children are excluded due to lack of ovulatory cycles and untested safety in this group.