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Brand Name :
Zulresso
Synonyms :
brexanolone
Class :
Antidepressants and GABA Receptor Positive Modulators
Brand Name :
Zulresso
Synonyms :
brexanolone
Class :
Antidepressants and GABA Receptor Positive Modulators
Dosage Forms & Strengths
Adult
Intravenous solution
5mg/ml
For a total of 60 hours (2.5 days), administer ZULRESSO as a continuous intravenous (IV) infusion as follows:
0-4 (hrs): Initiate with a dosage of 30 mcg/kg per hour continuous intravenous (IV) infusion
4-24 (hrs): the dose be increased to 60 mcg/kg per hour continuous intravenous (IV) infusion
24-52 (hrs): the dose be increased to 90 mcg/kg per hour (For individuals who cannot tolerate 90 mcg/kg per hour, decrease dose to 60 mcg/kg per hour) continuous intravenous (IV) infusion
52-56 (hrs): reduce to 60 mcg/kg per hour continuous intravenous (IV) infusion
56-60 (hrs): reduce to 30 mcg/kg per hour continuous intravenous (IV) infusion
Pediatric
Intravenous solution
5mg/ml
For a total of 60 hours (2.5 days), administer ZULRESSO as a continuous intravenous (IV) infusion as follows:
Age: >15 years
0-4 (hrs): Initiate with a dosage of 30 mcg/kg per hour continuous intravenous (IV) infusion
4-24 (hrs): the dose be increased to 60 mcg/kg per hour continuous intravenous (IV) infusion
24-52 (hrs): the dose be increased to 90 mcg/kg per hour (For individuals who cannot tolerate 90 mcg/kg per hour, decrease dose to 60 mcg/kg per hour) continuous intravenous (IV) infusion
52-56 (hrs): reduce to 60 mcg/kg per hour continuous intravenous (IV) infusion
56-60 (hrs): reduce to 30 mcg/kg per hour continuous intravenous (IV) infusion
Refer to adult dosingÂ
may increase the metabolism of tricyclic antidepressants
may increase the metabolism of tricyclic antidepressants
may increase the metabolism of tricyclic antidepressants
may increase the metabolism of tricyclic antidepressants
may increase the metabolism of tricyclic antidepressants
CNS Depressants may enhance the CNS depressant effect of brexanolone
CNS Depressants may enhance the CNS depressant effect of brexanolone
CNS Depressants may enhance the CNS depressant effect of brexanolone
CNS Depressants may enhance the CNS depressant effect of brexanolone
CNS Depressants may enhance the CNS depressant effect of brexanolone
CNS Depressants may enhance the CNS depressant effect of brexanolone
CNS Depressants may enhance the CNS depressant effect of brexanolone
CNS Depressants may enhance the CNS depressant effect of brexanolone
CNS Depressants may enhance the CNS depressant effect of brexanolone
CNS Depressants may enhance the CNS depressant effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
may have an increased CNS depressant effect when combined with brexanolone
may have an increased CNS depressant effect when combined with brexanolone
may have an increased CNS depressant effect when combined with brexanolone
may have an increased CNS depressant effect when combined with brexanolone
may have an increased CNS depressant effect when combined with brexanolone
may have an increased CNS depressive effect when combined with brexanolone
may have an increased CNS depressive effect when combined with brexanolone
may have an increased CNS depressive effect when combined with brexanolone
may have an increased CNS depressant effect when combined with Brexanolone
may have an increased CNS depressant effect when combined with Brexanolone
may have an increased CNS depressant effect when combined with Brexanolone
may have an increased CNS depressant effect when combined with Brexanolone
may have an increased CNS depressant effect when combined with Brexanolone
may enhance the risk of adverse effect of amphetamines
may enhance the risk of adverse effect of amphetamines
may enhance the risk of adverse effect of amphetamines
may enhance the risk of adverse effect of amphetamines
may enhance the risk of adverse effect of amphetamines
may increase the vasopressor effect
may have an increased CNS depressant effect when combined with brexanolone
may have an increased CNS depressant effect when combined with brexanolone
may have an increased CNS depressant effect when combined with brexanolone
may enhance the tachycardic effect
may enhance the tachycardic effect
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
CNS depressants increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
SSRIs increase the CNS depressing effect of brexanolone
SSRIs increase the CNS depressing effect of brexanolone
SSRIs increase the CNS depressing effect of brexanolone
SSRIs increase the CNS depressing effect of brexanolone
SSRIs increase the CNS depressing effect of brexanolone
When brexanolone is used together with bromisoval, the risk or seriousness of CNS depression is enhanced
dexchlorpheniramine, dextromethorphan, and phenylephrine
brexanolone: they may decrease the therapeutic effect of antihistamines
brexanolone: they may decrease the therapeutic effect of antihistamines
brexanolone: they may decrease the therapeutic effect of antihistamines
brexanolone: they may decrease the therapeutic effect of antihistamines
brexanolone: they may decrease the therapeutic effect of antihistamines
When brexanolone is used together with medazepam, the risk or seriousness of CNS depression is enhanced
The potential for CNS depression may enhanced when brexanolone is used together with fencamfamin
When brexanolone is used together with niaprazine, the risk or seriousness of CNS depression is enhanced
When brexanolone is used together with levosulpiride, the risk or seriousness of CNS depression is enhanced
When chlordiazepoxide is used together with brexanolone, this leads to enhanced risk or seriousness of CNS depression
When brexanolone is used together with capsaicin, this leads to enhanced risk or seriousness of methemoglobinemia
When brexanolone is used together with norelgestromin, this leads to a rise in norelgestromin’s metabolism
When brexanolone is used together with melitracen, this leads to enhanced risk or seriousness of CNS depression
When emylcamate is used together with brexanolone, this leads to enhanced risk or seriousness of CNS depression
When brexanolone is used together with etizolam, this leads to enhanced risk or seriousness of CNS depression
When acepromazine is used together with brexanolone, this leads to enhanced risk or seriousness of CNS depression
brexanolone: it may increase the excretion rate of oxtriphylline
brexanolone: it may increase the risk of CNS depression with tolperisone
brexanolone: it may decrease the therapeutic efficacy of etynodiol
Decreased therapeutic activity of brexanolone.
CNS depressants increase the effect of brexanolone
CNS depressants increase the effect of brexanolone
It may lead to sedation, respiratory depression, and coma
It may lead to sedation, respiratory depression, and coma
It may lead to sedation, respiratory depression, and coma
CNS depressants increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
SSRIs increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
SSRIs increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
CNS depressants increase the CNS depressing effect of brexanolone
barbiturates may increase the metabolism of tricyclic antidepressants
barbiturates may increase the metabolism of tricyclic antidepressants
barbiturates may increase the metabolism of tricyclic antidepressants
barbiturates may increase the metabolism of tricyclic antidepressants
barbiturates may increase the metabolism of tricyclic antidepressants
may increase the CNS depressant effect
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the serotonergic effects
may increase the serotonergic effects
may increase the serotonergic effects
may increase the serotonergic effects
may increase the serotonergic effects
may increase the serotonergic effects
may increase the serotonergic effects
may increase the serotonergic effects
may increase the serotonergic effects
may increase the serotonergic effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the CNS depressant effect of CNS Depressants
Action and Spectrum:
Brexanolone is a synthetic neuroactive steroid that increase GABA receptors activity and gives relief from anxiety.
It is a potent sedative drug, so it causes drowsiness and make it easier to fall asleep.
Brexanolone offers new and promising therapy for postpartum depression in adult females, those who lacking treatment options.
Adverse reaction:
>10%
Sedation
Presyncope
Vertigo
Somnolence
Dizziness
Dry mouth
1-10%
Loss of consciousness
Tachycardia
Oropharyngeal pain
Flushing
Hot flush
Black box warning:
It increases the risk of excessive sedation and loss of consciousness.
Contraindications/caution:
Caution:
Sedation and drowsiness
Alcohol consumption
History of depression and suicide
Cardiovascular disease
Pregnancy Warnings:
Pregnancy category: N/A
Lactation: Excretion of the drug into the human breast milk is known
Pregnancy categories:
Category A: Satisfactory and well-controlled studies show no evidence of risk to the fetus in the first trimester or in the later trimester.
Category B: No evidence of risk to fetus found in animal reproduction studies and there are not enough studies on pregnant women.
Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.
Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.
Category X: Drugs listed in this category clearly outweigh risks over benefits. These category drugs should be prohibited for pregnant women.
Category N: There is no data available for the drug under this category.
Pharmacology:
Neurons with negative membrane potential can stabilize through GABA-A receptors which is more difficult for excitatory neurotransmitters to work.
The level of GABA-A receptor reduces during pregnancy due to postpartum depression.
Pharmacodynamics:
It enhances GABA effects on various GABA-A receptors in mammalian cells expressing specific sub-units.
Brexanolone is a natural neuroactive steroid from the female hormone progesterone.
Pharmacokinetics:
Distribution:
The volume of distribution as per study is up to 3 L/kg.
Metabolism:
It undergoes extensive metabolism with non-CYP pathways.
Elimination and excretion:
It has half-life around 9 hours.
Administration:
It is administered via intravenous route i.e., deep into veins.
Patient information leaflet:
Generic Name: Brexanolone
Why do we use Brexanolone?
Brexanolone is indicated in treatment of moderate-to-severe postpartum depression in matured women.
Postpartum depression may develop in women with depressive symptoms, from third trimester to 4 weeks post-delivery.
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