Yasmin
Yasmin
Generic Name
Yasmin
Mechanism
- Estrogen component (EE):
- Suppresses luteinizing hormone (LH) and follicle‑stimulating hormone (FSH) release → prevents follicular maturation and ovulation.
- Enhances endometrial decidualization, reducing implantation potential.
- Progestin component (drospirenone):
- Progesterone receptor agonist → creates a hostile endometrial environment.
- Antimineralocorticoid & anti‑androgenic activity → reduces fluid retention, breast tenderness, and acne.
- Inhibits aromatase, lowering ovarian estrogen production.
The combined effect results in effective contraception, thickening of cervical mucus and alteration of fallopian tube motility.
Pharmacokinetics
| Parameter | Estinyl Estradiol | Drospirenone |
| Absorption | Rapid, >90% oral, peak at 2–3 h | Rapid, peak at ~3 h |
| Distribution | Highly protein‑bound (albumin 90%) | 80–90% bound (serum albumin & α‑1‑acid glycoprotein) |
| Half‑life | ~10 h | 3–4 h (steady‑state ~18 h) |
| Metabolism | Hepatic CYP3A4, CYP2C9 → mainly glucuronidation | Hepatic CYP3A4, CYP2C9 (oxidation) |
| Elimination | Urine & feces (mild metabolites) | Urine & feces (mild metabolites) |
| Drug‑Drug Interactions | Inhibited by ketoconazole, rifampin → ↑VTE risk; induced by CYP3A4 enhancers → ↓contraceptive efficacy | Same as EE; adds risk for hyponatremia when combined with diuretics |
Indications
- Primary:
- Reliable contraception (Repair 95% effective)
- Adjunctive/therapeutic:
- Dysmenorrhea and menorrhagia
- Acne vulgaris (due to anti‑androgenic effect)
- Premenstrual dysphoric disorder (PMDD)
- Endometriosis‑related pain
- Hirsutism or androgen excess in PCOS (low dose)
- Calendar‑based menstrual regulation
Contraindications
- Absolute contraindications:
- Current pregnancy, lactation during initial 35 days postpartum
- History of venous thromboembolism (VTE) or thrombophilia
- Uncontrolled hypertension (>160/100 mm Hg)
- Symptoms of estrogen‑sensitive cancers (breast, ovarian, endometrial)
- Active hepatic disease or liver dysfunction
- Certain medications (e.g., carbamazepine, phenytoin, rifampin) that reduce efficacy
- Relative contraindications (use with caution):
- Women >35 y who smoke ≥15 cigarettes/day
- Migraine with aura
- Untreated psychiatric disorders
Warnings:
• Monitoring for thrombotic events, hypertension, and hyponatremia (especially with concurrent diuretics).
• Mildly increase the risk of breast tenderness and nausea early in therapy.
Dosing
- Regimen: 21 active pills (EE 0.0125 mg + drospirenone 3.5 mg) + 7 placebo (or 2‑day hormone‑free interval).
- Start: First active pill on the first day of menstruation (Day 1) or any day if using “flex” dosing.
- Missed pill:
- ≤1 missed in cycle → discard next active pill, resume routine.
- 2+ missed within 24 h → use backup contraception for 7 days.
- 2+ missed in 3 consecutive cycles → hold the next cycle.
- Cycle‑length extension: 4 days > 7 days allows birth‑control planning.
- Drug interaction adjustment: Adjust dose or switch methods if on enzyme inducers (e.g., ketoconazole, rifampin).
Adverse Effects
- Common (≥5 %):
- Nausea, breast tenderness, headache, mood changes, acne improvement, spotting.
- Mild weight gain (~1–2 kg).
- Menstrual changes: lighter flow, shorter cycle.
- Serious (≤1 %):
- Venous thromboembolism (incidence ~9–12/10,000 per year in women 20‑30 y).
- Hypertension (new onset or worsening).
- Hepatic adenoma or cystic lesions.
- Hyponatremia with usage of potassium‑sparing diuretics.
- Increased risk of breast, cervical, and endometrial cancers (small absolute increase).
Monitoring
| Parameter | Frequency | Rationale |
| Blood pressure | At each visit or when changing regimen | Detect hypertension early |
| Weight & BMI | Every 3–6 mo | Monitor fluid retention |
| Serum creatine kinase & CK-MB | At baseline for high‑risk | Detect myocardial ischemia |
| Liver function tests | Baseline, then annually | Detect hepatic dysfunction |
| Pregnancy test | After missed >48 h pill | Confirm non‑pregnancy |
| Adverse‑effect assessment | Monthly | Evaluate mood, bleeding, pain |
| Electrolytes (particularly Na⁺) | If on diuretics | Detect hyponatremia |
Clinical Pearls
1. Drospirenone’s dual anti‑androgenic/antimineralocorticoid effect – Useful for acne and fluid‑overload patients, but increases risk of hyponatremia. Tighten sodium monitoring with NSAIDs or spironolactone.
2. Start timing – Initiate on the first day of menses for the most predictable cycle; otherwise, use flexible start that calls for a 2‑day hormone‑free interval to avoid breakthrough bleeding.
3. Severe nausea in the first week – Consider taking pills with food or switching to a non‑combination progestin‑only pill for the first month.
4. Pregnancy after a missed pill – Use condoms until the missed pill is taken. No safe “recovery” period as with other oral contraceptives.
5. Stopping Vasomotor instability – Patients frequently present with hot flashes or night sweats; drospirenone can lessen these, improving compliance.
6. Hypertension in smokers >35 y – Counsel on smoking cessation; re‑assess if blood pressure rises.
7. Safety in lactation – Though some formulations are used in lactating women after 35 days postpartum, paired‑type progestins are preferred; Yasmin is typically avoided in lactation due to potential drug‑dependent neonatal effects.
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• *All recommendations are based on current evidence and guidelines as of June 2024. Practitioners should consider individual patient risk factors and local regulations when prescribing Yasmin.*