Ectris

Uses

Ectris is a 5-HT receptor modulator used for the treatment of selected premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD).

For the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women.

Ectris is also used to associated treatment for these conditions: Hypoactive Sexual Desire Disorder (HSDD)

How Ectris works

Flibansetrin has high affinity for serotonin receptors in the brain: it acts as an agonist on 5-HT1A and an antagonist on 5-HT2A. In vivo, flibanserin binds equally to 5-HT1A and 5-HT2A receptors. However, under higher levels of brain 5-HT (i.e., under stress), flibanserin may occupy 5-HT2A receptors in higher proportion than 5-HT(1A) receptors. It may also moderately antagonize D4 (dopamine) receptors and 5-HT2B and 5-HTB2C. Its action on neurotransmitter receptors may contribute to reduction in serotonin levels and increase in dopamine and norepinephrine levels, all of which may play part in reward processing.

Food Interaction

• Avoid alcohol. Avoid alcohol. Ingesting alcohol may increase the CNS depressant and hypotensive effects of flibanserin. If you have consumed two drinks, wait two hours before taking flibanserin. Do not take flibanserin if you have consumed more than three drinks.
• Avoid grapefruit products.
• Avoid St. John's Wort.
• Take with or without food. Taking flibanserin with food (especially a high-fat meal) may increase its AUC, Cmax, and Tmax.

[Major] CONTRAINDICATED: Grapefruit juice may increase the plasma concentrations of flibanserin.

The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.

In 26 healthy female subjects, administration of a single 100 mg dose of flibanserin with 240 mL grapefruit juice increased flibanserin peak plasma concentration (Cmax) and systemic exposure (AUC) by 1.1- and 1.4-fold, respectively, compared to administration of flibanserin alone.

In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands.

Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition.

ADJUST DOSING INTERVAL: Coadministration of flibanserin with alcohol may potentiate the risk of severe hypotension, syncope, and central nervous system depression.

In a dedicated alcohol interaction study, hypotension or syncope requiring therapeutic intervention (ammonia salts and

In these four subjects, systolic blood pressure reductions ranged from 28 to 54 mmHg and diastolic blood pressure reductions ranged from 24 to 46 mmHg.

In addition, 6 (25%) of 24 subjects coadministered flibanserin with 0.8 g

Systolic and diastolic blood pressure reductions in these 6 subjects ranged from 22 to 48 mmHg and 0 to 27 mmHg, respectively, with one requiring therapeutic intervention.

No adverse events requiring therapeutic intervention were observed when flibanserin or alcohol was administered alone.

Somnolence was reported in 67%, 74%, and 92% of subjects who received flibanserin alone, flibanserin with 0.4 g

Subsequent data from postmarketing trials showed that the risk of severe hypotension and syncope was reduced when women who consumed up to two alcoholic drinks waited at least two hours before taking flibanserin.

MANAGEMENT: Concomitant use of flibanserin with moderate or potent CYP450 3A4 inhibitors such as grapefruit juice is considered contraindicated.

The patient should be advised to avoid the consumption of grapefruit and grapefruit juice during treatment, and to take flibanserin at bedtime to minimize the risk of hypotension, syncope, accidental injury, and central nervous system depression.

In addition, patients should consume no more than 1 to 2 alcoholic drinks and discontinue drinking alcohol at least two hours before taking flibanserin at bedtime; otherwise, they should skip the flibanserin dose that evening.

Alcohol should not be consumed until at least the morning after taking flibanserin at bedtime.

A standard alcoholic drink contains 14 g of pure alcohol and is equivalent to one 12-ounce regular beer (5% alcohol), 5-ounces wine (12% alcohol), or 1.5 ounces of distilled spirits

Ectris Drug Interaction

Moderate: loxapine, lorazepam, lurasidone, asenapine, cetirizineUnknown: 5-hydroxytryptophan, amphotericin b lipid complex, isotretinoin, tocilizumab, corticotropin, alteplase, dapsone topical, sulfamethoxazole / trimethoprim, celecoxib, atorvastatin, benazepril, semaglutide, albuterol, infliximab, cholecalciferol

Ectris Disease Interaction

Major: acute alcohol intoxication, hypotension/syncope, liver disease

Elimination Route

Ectris has an absolute oral availability of 33%.

Half Life

≈11 hours

Elimination Route

Elimination via feces (51%) and urine (44%) following a single oral 50 mg dose of flibanserin solution.

Innovators Monograph

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