Drospi4 mg

Drospi is a synthetic progestin used for hormonal contraception, either alone or in combination with an estrogen.

Established / FDA-approved uses

• Prevention of pregnancy — as a standalone progestin-only pill (POP) containing Drospi 4 mg, taken continuously for women who prefer or require an estrogen-free method.
• Prevention of pregnancy — as the progestin component of combined oral contraceptives (COCs), where Drospi is paired with an estrogen (ethinylestradiol or estradiol).

Guideline-supported / adjunct uses (specific combination products only)

• Certain Drospi-containing combined oral contraceptives are additionally approved for treatment of moderate acne vulgaris in women who also desire contraception, and for premenstrual dysphoric disorder (PMDD) in women choosing an oral contraceptive for birth control.
• A combination of Drospi with estradiol is used for management of moderate-to-severe vasomotor symptoms (hot flashes) associated with menopause.

Note: Acne, PMDD, and menopausal symptom indications apply only to specific licensed combination products, not to Drospi used alone for non-contraceptive purposes.

Each tablet contains Drospirenone as the active pharmaceutical ingredient, either alone (progestin-only formulation) or combined with an estrogen component (ethinylestradiol or estradiol) in fixed-dose combination products, depending on the specific brand and formulation.

Drospi is a synthetic steroid hormone belonging to the progestin class. Chemically, it is an analogue of spironolactone and, unlike most progestins (which are derived from testosterone), it uniquely combines progestational activity with antimineralocorticoid (anti-aldosterone) and antiandrogenic properties.

Drospi is used in oral contraceptive products, either as a standalone progestin-only tablet or combined with an estrogen, to prevent pregnancy by suppressing ovulation and altering the cervical and endometrial environment.

Pharmacodynamics

Drospirenone is a progestin that binds to the progesterone receptor, producing negative feedback on the hypothalamic-pituitary axis that suppresses gonadotropin (LH/FSH) secretion, thereby inhibiting ovulation. It also thickens cervical mucus (impeding sperm penetration) and alters the endometrium (reducing the likelihood of implantation).

Unlike most progestins, Drospirenone also has antimineralocorticoid activity (it antagonizes aldosterone at the mineralocorticoid receptor, similar to spironolactone), which can cause mild natriuresis and a tendency toward potassium retention (hyperkalemia risk), and antiandrogenic activity, which contributes to its beneficial effect on acne and hirsutism in some formulations.

Pharmacokinetics

• Absorption: Rapidly and almost completely absorbed after oral administration; absolute bioavailability is approximately 76%.
• Distribution: Highly bound to plasma proteins (albumin and, to a lesser extent, sex hormone-binding globulin).
• Metabolism: Extensively metabolized in the liver, mainly by non-CYP450 pathways (acid hydrolysis) into inactive metabolites, with a minor contribution from CYP3A4.
• Elimination half-life: Approximately 30–34 hours.
• Excretion: Metabolites are excreted in both urine and feces.

Take Drospi tablets by mouth, in the exact order indicated on the blister pack, at approximately the same time every day to maintain contraceptive effectiveness, with or without food. Swallow the tablet whole; do not skip, double up, or stop tablets without medical advice. Continue taking a tablet every day, including during any withdrawal bleeding.

Only well-established, clinically significant interactions with Drospi are listed below.

• Drugs that increase serum potassium (ACE inhibitors, angiotensin receptor blockers, potassium-sparing diuretics, aldosterone antagonists, NSAIDs, potassium supplements): Concurrent use with Drospi raises the risk of hyperkalemia due to its antimineralocorticoid activity; serum potassium should be monitored during the first treatment cycle in at-risk patients.
• Strong CYP3A4 inducers (e.g., rifampicin, phenytoin, carbamazepine, St. John's Wort): May reduce plasma concentrations of Drospi and its contraceptive efficacy; an alternative or additional contraceptive method is advised.
• Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir): May increase exposure to Drospi, theoretically increasing the risk of hyperkalemia and other adverse effects.
• Other hormonal or hepatically-metabolized drugs: As with other hormonal contraceptives, effects on hepatic metabolism may alter levels of other co-administered drugs (e.g., some anticonvulsants, lamotrigine); consult a physician before combining therapies.

Common

• Irregular menstrual bleeding or spotting, especially during the first few cycles
• Headache
• Nausea
• Breast tenderness
• Mood changes
• Decreased libido
• Acne (uncommon; some formulations improve acne instead)

Serious (seek medical attention)

• Signs of hyperkalemia (muscle weakness, irregular heartbeat, fatigue) — see Precautions and Warnings
• Signs of venous or arterial thromboembolism (leg swelling/pain, chest pain, sudden shortness of breath, sudden severe headache, vision changes, weakness on one side of the body) — see Contraindications
• Severe abdominal pain or signs of liver problems (jaundice, dark urine)
• Signs of hypersensitivity/allergic reaction

Pregnancy: Drospi is contraindicated in known or suspected pregnancy; there is no indication for its use during pregnancy, and it should be discontinued immediately if pregnancy is confirmed. If pregnancy occurs while on Drospi, a physician should be consulted promptly.

Lactation: Small amounts of Drospi pass into breast milk. Hormonal contraceptives, particularly estrogen-containing combinations, may reduce milk quantity and quality; progestin-only formulations are generally preferred if contraception is needed during breastfeeding. Drospi should be used during breastfeeding only if clearly needed, and only after the potential benefit is weighed against potential risk to the infant, in consultation with a physician.

• Hyperkalemia: Because of its antimineralocorticoid activity, Drospi can increase serum potassium. Measure serum potassium during the first treatment cycle in patients with renal insufficiency, hepatic dysfunction, adrenal insufficiency, or those taking medications that increase potassium (see Interactions).
• Thromboembolism risk factors: Use with caution and assess individual risk in women with risk factors for venous or arterial thromboembolism (e.g., smoking, obesity, hypertension, family history, prolonged immobilization), particularly with combined (estrogen-containing) formulations.
• Irregular bleeding: Unscheduled spotting or bleeding is common, especially in the first few months; persistent or heavy bleeding should be evaluated.
• Ectopic pregnancy: Consider the possibility of ectopic pregnancy in women who become pregnant or complain of lower abdominal pain while on therapy.
• Mood changes: Monitor for depression or mood changes; discontinue if significant depression occurs.
• Does not protect against sexually transmitted infections, including HIV.

There is no specific antidote for Drospi overdose. Reported effects of acute overdose with hormonal contraceptives may include nausea, vomiting, and withdrawal bleeding in females. In case of suspected overdose, seek immediate medical attention or contact a poison control center; treatment should be symptomatic and supportive, including monitoring of serum potassium given Drospi's antimineralocorticoid activity. Do not attempt unsupervised home treatment.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

• Renal impairment: Contraindicated in renal insufficiency due to increased risk of hyperkalemia; use with caution and monitor potassium in mild renal impairment.
• Hepatic impairment: Contraindicated in significant hepatic disease or hepatic tumors (see Contraindications).
• Elderly: Drospi-containing contraceptives are not intended for use in postmenopausal women for contraception; combination products with estradiol used for menopausal symptoms should use the lowest effective dose.
• Smokers: Women over 35 who smoke should not use combined (estrogen-containing) Drospi products due to increased cardiovascular risk.
• Adrenal insufficiency: Contraindicated (see Contraindications).

Drospi is typically used long-term for ongoing contraception, for as long as pregnancy prevention is desired and no contraindications develop, with periodic medical review (e.g., annually) to reassess risk factors. When used for menopausal symptom relief (combined with estradiol), the lowest effective dose should be used for the shortest duration consistent with treatment goals, with periodic reassessment.

Progestins; Hormonal contraceptives; Antimineralocorticoid progestins. Drospirenone belongs to the spironolactone-derivative progestin subclass.

Drospirenone acts primarily as a progesterone receptor agonist, suppressing pituitary gonadotropin release to inhibit ovulation, thickening cervical mucus, and altering the endometrium to prevent implantation. It additionally exerts antimineralocorticoid (anti-aldosterone) and antiandrogenic activity via the mineralocorticoid and androgen receptors, respectively (see Pharmacology for full detail).

X (contraindicated in pregnancy; legacy FDA pregnancy category applicable to hormonal contraceptive products)

Safety and efficacy of Drospi have not been established in premenarchal (pre-pubertal) females, as it has no indication before menarche. In postmenarchal adolescents, Drospi-containing contraceptives may be used for approved indications (contraception, or acne/PMDD for specific licensed combination products) using the same dosage as adults, with careful counseling and physician supervision.