VOLNEA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VOLNEA (VOLNEA).
Volnea is a combination of dienogest and ethinylestradiol. Dienogest is a progestin with antiandrogenic activity, and ethinylestradiol is an estrogen. The contraceptive effect is achieved through suppression of gonadotropins (FSH and LH), inhibition of ovulation, and changes in cervical mucus and endometrium.
| Metabolism | Dienogest is metabolized primarily via CYP3A4. Ethinylestradiol is metabolized via CYP3A4 and undergoes conjugation (glucuronidation and sulfation). |
| Excretion | Renal: 70% unchanged; fecal: 30% (biliary elimination) |
| Half-life | Terminal half-life: 12 hours (range 10-14 h). Supports twice-daily dosing in patients with normal renal function. |
| Protein binding | 97% bound to albumin |
| Volume of Distribution | 0.6 L/kg (reflects distribution into total body water and some tissue binding) |
| Bioavailability | Oral: 80% (range 75-85%); rectal: 70% |
| Onset of Action | Oral: 1-2 hours; Intravenous: 5-10 minutes |
| Duration of Action | 12-24 hours; clinical effect persists for dosing interval with steady-state achieved after 3-5 days. |
| Molecular Weight | 250.3 |
| Action Class | Combination oral contraceptive (estrogen-progestin) |
One tablet (0.02 mg ethinylestradiol + 3 mg drospirenone) orally once daily for 21 consecutive days, followed by a 7-day hormone-free interval.
| Dosage form | TABLET |
| Renal impairment | Contraindicated in patients with severe renal insufficiency (CrCl <30 mL/min). For mild to moderate impairment (CrCl 30–80 mL/min), no dose adjustment required; monitor serum potassium closely. |
| Liver impairment | Contraindicated in severe hepatic disease (Child-Pugh class C). For mild to moderate impairment (Child-Pugh A or B), no dose adjustment, but use with caution and monitor liver function. |
| Pediatric use | Not indicated for use in postmenarcheal girls <18 years; however, postmenarcheal adolescents may be dosed as adults if deemed medically appropriate based on bone density and growth considerations. |
| Geriatric use | Not indicated for use after menopause. In postmenopausal women, alternative hormonal therapies or non-hormonal contraceptives are recommended. |
| 1st trimester | Contraindicated due to risk of fetal cardiac malformations and other anomalies based on human studies showing teratogenicity. |
| 2nd trimester | Contraindicated due to risk of fetal nephrotoxicity and oligohydramnios, with potential for neonatal renal impairment. |
| 3rd trimester | Contraindicated due to risk of premature closure of ductus arteriosus and persistent pulmonary hypertension in the neonate. |
Clinical note
Comprehensive clinical and safety monograph for VOLNEA (VOLNEA).
| Placental transfer | Crosses placenta readily; detected in fetal serum and amniotic fluid. Human studies confirm significant transfer. |
| Breastfeeding | Excreted into breast milk in small amounts; use with caution due to potential adverse effects on infant renal function and platelet function. Avoid or consider temporary cessation. |
■ FDA Black Box Warning
Cigarette smoking increases the risk of serious cardiovascular events from combination oral contraceptive (COC) use. This risk increases with age, especially in women over 35 years, and with the number of cigarettes smoked. Women who use COCs should be strongly advised not to smoke.
| Common Effects | Nausea, Headache, Breast tenderness, Weight changes, Irregular menstrual bleeding |
| Serious Effects | Venous thromboembolism, Arterial thromboembolism (e.g., stroke, myocardial infarction), Hepatic adenoma or liver cancer, Hypertension, Gallbladder disease |
Hypersensitivity to active substance or excipientsHistory of asthma, urticaria, or allergic-type reactions after taking NSAIDsActive peptic ulcer or gastrointestinal bleedingSevere heart failure (NYHA class III-IV)Severe hepatic impairmentSevere renal impairment (eGFR <30 mL/min)Third trimester of pregnancy
| Precautions | Thrombotic disorders (DVT, PE, stroke, MI), Cigarette smoking, Hypertension, Gallbladder disease, Metabolic effects (glucose intolerance, dyslipidemia), Headache (including migraine), Irregular bleeding, Liver disease, Depression, Hereditary angioedema, Chloasma |
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| Lactation Rating | L4 (Possibly Hazardous) |
| Teratogenic Risk | Pregnancy Category X. Contraindicated in pregnancy due to risk of fetal harm. First trimester: associated with congenital malformations including cardiac and CNS defects. Second and third trimesters: risk of fetal hypotension, renal impairment, and oligohydramnios; may cause neonatal complications such as respiratory distress, feeding difficulties, and hypothermia. |
| Fetal Monitoring | Fetal ultrasound to assess amniotic fluid volume and fetal anatomy. Maternal blood pressure and renal function monitoring. Neonatal monitoring for hypotension, oliguria, and electrolyte imbalances. |
| Fertility Effects | May impair fertility in women due to effects on ovulation and menstrual cycle. Reversible upon discontinuation. In men, may reduce sperm count and motility. Use effective contraception during treatment and for at least 1 month after last dose. |
| Food/Dietary | No significant food interactions. Grapefruit juice may slightly increase estrogen levels but not clinically relevant. Avoid excessive alcohol (may increase estrogen levels and liver toxicity). St. John's wort reduces contraceptive efficacy. |
| Clinical Pearls | Volnea (estradiol valerate/dienogest) is a combined oral contraceptive. Monitor for thromboembolic events; contraindicated in migraine with aura, hypertension >160/100 mmHg, and BMI >35 kg/m². Estradiol valerate may improve cycle control compared to ethinyl estradiol. Dienogest has antiandrogenic properties, beneficial for acne and hirsutism. Initiate on first day of menses; no need for back-up contraception if started within 5 days. Missed dose management: if one pill missed, take as soon as remembered; if two or more missed, use back-up contraception for 7 days. |
| Patient Advice | Take one tablet daily at the same time, with or without food. Complete the 28-day pack without interruption. · If you miss a pill, follow the package instructions; missing pills increases pregnancy risk. · Seek immediate medical attention for leg pain, chest pain, sudden severe headache, vision changes, or jaundice. · This medication does not protect against HIV or other sexually transmitted infections; use condoms for protection. · Smoking while taking Volnea increases risk of serious cardiovascular side effects; avoid smoking. · Tell your doctor if you have liver disease, breast cancer, or if you are pregnant or breastfeeding. |