Сафрис

Сафрис Uses, Dosage, Side Effects, Food Interaction and all others data.

Developed by Schering-Plough after its merger with Organon International, asenapine is a sublingually administered, atypical antipsychotic for treatment of schizophrenia and acute mania associated with bipolar disorder. Сафрис also belongs to the dibenzo-oxepino pyrrole class. It is also for severe post-traumatic stress disorder nightmares in soldiers as an off-label use. FDA approved on August 13, 2009.

Сафрис is a serotonin, dopamine, noradrenaline, and histamine antagonist in which asenapine possess more potent activity with serotonin receptors than dopamine. Sedation in patients is associated with asenapine's antagonist activity at histamine receptors. Its lower incidence of extrapyramidal effects are associated with the upregulation of D1 receptors. This upregulation occurs due to asenapine's dose-dependent effects on glutamate transmission in the brain. It does not have any significant activity with muscarinic, cholinergic receptors therefore symptoms associated with anticholinergic drug activity like dry mouth or constipation are not expected to be observed. Сафрис has a higher affinity for all aforementioned receptors compared to first-generation and second-generation antipsychotics except for 5-HT1A and 5-HT1B receptors.

Сафрис
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Сафрис
Availability	Prescription only
Generic	Asenapine
Asenapine Other Names	asenapina, Asenapine
Related Drugs	Vraylar, quetiapine, lamotrigine, Abilify, Seroquel, aripiprazole, olanzapine, risperidone, lithium
Type
Formula	C₂₁H₂₀ClNO₅
Weight	Average: 401.84 Monoisotopic: 401.103000462
Protein binding	95% protein bound
Groups	Approved
Therapeutic Class
Manufacturer
Available Country	Russia
Last Updated:	September 19, 2023 at 7:00 am

Uses

Сафрис is an atypical antipsychotic used to treat patients with bipolar I disorder and patients with schizophrenia.

Used for treatment in psychosis, schizophrenia and schizoaffective disorders, manic disorders, and bipolar disorders as monotherapy or in combination.

Сафрис is also used to associated treatment for these conditions: Mixed manic depressive episode, Schizophrenia, Acute Manic episode

How Сафрис works

Сафрис is an atypical antipsychotic multireceptor neuroleptic drug which shows strong 5HT2A (serotonin) and D2 (dopamine) receptor antagonism, which has been shown to enhance dopamine (DA) and acetylcholine (Ach) efflux in rat brains. Сафрис may improve cognitive function and negative symptoms in patients with schizophrenia.

Food Interaction

Take separate from meals. Do not have food or water for 10 minutes after administration.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Сафрис Cholesterol interaction

[Moderate] Atypical antipsychotic drugs have been associated with undesirable alterations in lipid levels.

While all agents in the class have been shown to produce some changes, each drug has its own specific risk profile.

Before or soon after initiation of antipsychotic medication, obtain a fasting lipid profile at baseline and monitor periodically during treatment.

Сафрис Drug Interaction

Major: haloperidol, escitalopramModerate: aripiprazole, lorazepam, buspirone, duloxetine, divalproex sodium, paliperidone, clonazepam, lamotrigine, lurasidone, lithium, quetiapine, lisdexamfetamine, olanzapineUnknown: charcoal, methylphenidate, sodium iodide, methylphenidate, cholecalciferol

Сафрис Disease Interaction

Major: severe hepatic impairment, dementia, QT Prolongation, NMS, tardive dyskinesiaModerate: depression, aspiration, seizure, hematologic abnormalities, hyperglycemia/diabetes, hypotension, lipid alterations, weight gain, hyperprolactinemia

Volume of Distribution

20-25 L/kg

Elimination Route

Cmax, single 5 mg dose = 4 ng/mL (within 1 hour); Bioavailability, sublingual administration = 35%; Bioavailability, oral administration (swallowed) = <2%; Time to steady state, 5 mg = 3 days; Peak plasma concentration occurs within 0.5 to 1.5 hours. Doubling dose of asenapine results in 1.7-fold increase in maximum concentration and exposure. Drinking water within 2-5 minutes post administration of asenapine results in a decrease in exposure.