Comparative Pharmacology
Head-to-head clinical analysis: GILDESS 1 5 30 versus GILDESS 1 20.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GILDESS 1 5 30 versus GILDESS 1 20.
GILDESS 1.5/30 vs GILDESS 1/20
Head-to-head clinical comparison of therapeutic indices and safety profiles.
Combination of estrogen (ethinyl estradiol) and progestin (desogestrel) that inhibits gonadotropin release, suppressing ovulation, increasing cervical mucus viscosity, and altering endometrial morphology.
GILDESS 1/20 is a combination oral contraceptive containing ethinyl estradiol (an estrogen) and gestodene (a progestin). Its primary mechanism is inhibition of ovulation via suppression of gonadotropin-releasing hormone (GnRH), leading to reduced follicle-stimulating hormone (FSH) and luteinizing hormone (LH) secretion. Additionally, it alters cervical mucus (increasing viscosity to impede sperm penetration) and endometrial structure (rendering it unsuitable for implantation).
Oral contraception
Prevention of pregnancyTreatment of moderate acne vulgarisContraceptive for women with menstrual disorders
One tablet orally once daily at the same time each day.
One tablet orally daily, each containing 20 mcg ethinyl estradiol and 150 mcg desogestrel.
None Documented
None Documented
Ethinylestradiol: terminal half-life 13-17 hours (mean 15 h). Desogestrel active metabolite 3-keto-desogestrel: terminal half-life 23-28 hours (mean 25 h). Clinical: steady-state achieved by cycle day 7-10; missed pill instructions based on half-life.
Ethinylestradiol: terminal half-life ~13-27 hours (mean 17 hours). Gestodene: terminal half-life ~12-15 hours. Steady-state reached within 5-7 days.
Ethinyl estradiol undergoes first-pass metabolism in gut wall and liver via CYP3A4; desogestrel is metabolized by CYP2C9 and CYP2C19 to active metabolite etonogestrel.
Both ethinyl estradiol and gestodene are metabolized primarily in the liver via the cytochrome P450 3A4 (CYP3A4) pathway. Ethinyl estradiol undergoes first-pass metabolism and enterohepatic recirculation; gestodene is hydroxylated and conjugated.
Renal: ~55-60% as ethinylestradiol glucuronide and sulfate conjugates; ~40% as desogestrel metabolites (largely as 3-keto-desogestrel glucuronide). Fecal: ~30-35% of desogestrel metabolites; <5% for ethinylestradiol. Biliary: minor for both.
Renal (estradiol: ~40-50% as glucuronide and sulfate conjugates; gestodene: ~30-40% as metabolites) and fecal (estradiol: ~20-30%; gestodene: ~30-40%). Less than 1% excreted unchanged.
Ethinylestradiol: ~97% bound to albumin (90%) and SHBG (minor). 3-Keto-desogestrel: ~95% bound: albumin (65%) and SHBG (30%).
Ethinylestradiol: 98% bound to albumin. Gestodene: 75-90% bound to sex hormone-binding globulin (SHBG) and albumin.
Ethinylestradiol: Vd ~2.5-3.0 L/kg; distributes extensively into body tissues (breast, liver). 3-Keto-desogestrel: Vd ~1.5-2.0 L/kg; moderate tissue binding.
Ethinylestradiol: ~2.4 L/kg. Gestodene: ~0.7 L/kg. Indicates extensive tissue distribution.
Oral: ethinylestradiol ~40-50% (due to first-pass metabolism); desogestrel ~76% (≥60% converted to active 3-keto-desogestrel after first pass).
Oral: Ethinylestradiol ~40-60% (first-pass metabolism). Gestodene ~99% (highly bioavailable due to minimal first-pass effect).
Contraindicated in patients with renal impairment (eGFR <60 mL/min/1.73 m2) due to increased risk of hyperkalemia and reduced efficacy.
No dosage adjustment required for mild-to-moderate renal impairment. Insufficient data for severe renal impairment; use with caution.
Contraindicated in patients with hepatic impairment (Child-Pugh class B or C) due to impaired hormone metabolism and potential for adverse effects.
Contraindicated in hepatic adenomas, active liver disease, or Child-Pugh class B/C cirrhosis. For mild hepatic impairment (Child-Pugh A), no dosage adjustment; monitor.
Not indicated for use in pediatric patients. Safety and efficacy have not been established in females under 18 years of age.
Not indicated for use in pediatric patients before menarche. Post-menarche, same as adult dosing; use only after establishment of regular menstrual cycles.
Not indicated for use in postmenopausal women. Efficacy in women over 40 years of age has not been fully established; consider alternative contraception due to increased cardiovascular risk.
Not indicated for use in postmenopausal women. No specific geriatric dosing; generally not used in elderly women due to increased risk of thromboembolism.
Cigarette smoking increases risk of serious cardiovascular events from combination oral contraceptive use. Risk increases with age and smoking intensity (especially in women over 35).
Cigarette smoking increases the risk of serious cardiovascular events from combination oral contraceptive use. This risk increases with age and with heavy smoking (≥15 cigarettes per day) and is particularly pronounced in women over 35 years of age. Women who use combination oral contraceptives should be strongly advised not to smoke.
["Increased risk of thromboembolic disorders (e.g., DVT, PE)","Myocardial infarction and stroke risk","Hepatic neoplasia","Gallbladder disease","Hypertension","Carbohydrate/lipid effects","Ocular lesions","Dose-related risk of VTE from desogestrel-containing pills"]
["Risk of thromboembolic disorders (venous and arterial), including myocardial infarction and stroke","Increased risk of hypertension and associated vascular complications","Potential hepatic neoplasia (benign and malignant)","Possible exacerbation of cholestatic jaundice or gallbladder disease","May cause fluid retention, which can aggravate conditions such as migraine, asthma, cardiac, or renal dysfunction","Altered carbohydrate metabolism: monitor glucose in diabetic patients","May worsen depression or epilepsy"]
["Thrombophlebitis or thromboembolic disorders","History of DVT or PE","Cerebrovascular or coronary artery disease","Known or suspected breast carcinoma","Estrogen-dependent neoplasia","Undiagnosed abnormal genital bleeding","Pregnancy","Hepatic adenoma or carcinoma","Active liver disease with abnormal function"]
["Known or suspected pregnancy","Current or history of thrombosis (deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke)","History of cerebrovascular accident","Current or history of breast cancer or other estrogen-sensitive neoplasia","Undiagnosed abnormal uterine bleeding","Active liver disease or impaired liver function","Hypersensitivity to any component of the product","Uncontrolled hypertension","Diabetes with vascular involvement","Headaches with focal neurological symptoms (e.g., migraine with aura) at age ≥35","Major surgery with prolonged immobilization"]
Data Pending Review
Data Pending Review
No specific food restrictions. Grapefruit juice does not significantly interact with ethinylestradiol or gestodene. St. John's Wort (Hypericum perforatum) reduces contraceptive efficacy by inducing CYP3A4 metabolism; avoid concurrent use. High-fat meals may increase ethinylestradiol absorption slightly but no dose adjustment needed.
No specific food interactions are reported for GILDESS 1/20. However, grapefruit juice may increase estrogen levels; advise patients to consume grapefruit products in moderation. Alcohol may impair judgment regarding missed doses; recommend moderate intake.
First trimester: Combination oral contraceptives are not associated with a major increase in risk of birth defects. Second and third trimesters: Prolonged use may be associated with fetal harm including cardiovascular and skeletal anomalies, though data are limited. Known pregnancy contraindicates use.
GILDESS 1/20 (ethinyl estradiol 20 mcg/desogestrel 0.15 mg) is category X in pregnancy. First trimester: increased risk of congenital anomalies (e.g., heart defects, limb reduction) from estrogen component; cardiovascular and nervous system malformations reported. Second and third trimesters: associated with masculinization of female fetus from progestin; increased risk of IUGR and preterm birth. Use contraindicated in pregnancy.
Ethinyl estradiol and levonorgestrel are excreted in breast milk in small amounts. M/P ratio not established. Potential for adverse effects in nursing infant, including reduced milk production and jaundice. Use not recommended in breastfeeding women.
Excreted in breast milk; ethinyl estradiol M/P ratio ~0.4, desogestrel M/P ratio ~0.6. May reduce milk quantity and quality; small amounts pose theoretical risk of estrogenic effects in infant. Generally not recommended during breastfeeding; alternative contraception advised.
Contraindicated in pregnancy. No dose adjustments applicable; use should be discontinued immediately if pregnancy occurs.
No dose adjustments applicable as drug is contraindicated in pregnancy. Pharmacokinetic changes in pregnancy (increased hepatic metabolism, increased renal clearance) would reduce efficacy, but use is not recommended.
Category C
Category C
GILDESS 1.5/30 is a combined oral contraceptive (COC) containing ethinylestradiol 30 µg and gestodene 75 µg. Gestodene is a third-generation progestin with high progestogenic activity and low androgenic effects, reducing acne and hirsutism. This formulation has a higher risk of venous thromboembolism (VTE) compared to second-generation COCs. Avoid in women with migraines with aura, hypertension (BP >160/100), or BMI >30 due to increased VTE risk. For missed pills: if one pill is missed, take it as soon as remembered and continue; if two or more pills are missed, take the last missed pill, use backup contraception for 7 days, and consider emergency contraception if unprotected intercourse occurred.
GILDESS 1/20 is a monophasic oral contraceptive containing 20 mcg ethinyl estradiol and 1 mg norethindrone acetate. It is indicated for contraception and may be used for acne vulgaris in women at least 15 years old. Monitor for breakthrough bleeding, especially in the first cycles. Counsel patients to take at the same time daily to maintain efficacy. Caution in women with migraine with aura, hypertension, or history of thromboembolism. Prescribe as a 21-day regimen with a 7-day hormone-free interval.
Take one tablet daily at the same time, preferably in the evening, to reduce nausea.If you miss a pill, follow the instructions in the package leaflet; if you miss more than one pill, use additional contraception (e.g., condoms) for 7 days.Smoking increases the risk of serious cardiovascular side effects; do not smoke while taking this medication, especially if you are over 35.Tell your doctor if you experience severe headache, chest pain, leg pain or swelling, visual disturbances, or jaundice.This medication does not protect against sexually transmitted infections; use condoms for additional protection.Vomiting or severe diarrhea within 4 hours of taking the pill reduces efficacy; consider it as a missed pill and use backup contraception.
Take one pill at the same time every day, even if you do not have sex often.If you miss a pill, follow the instructions in the package insert or consult your healthcare provider.Use a backup method (like condoms) if you miss more than one pill or start late.Common side effects include nausea, breast tenderness, and spotting, especially in the first few cycles.Contact your doctor if you experience severe abdominal pain, chest pain, headache, vision changes, or leg pain/swelling.Smoking increases the risk of serious cardiovascular side effects; avoid smoking while on this medication.Do not take GILDESS if you are pregnant or suspect pregnancy.