Lurasidone Actions

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Actions of Lurasidone in details

infoThe action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Lurasidone is an atypical antipsychotic that is a D2 and 5-HT2A (mixed serotonin and dopamine activity) to improve cognition. It is thought that antagonism of serotonin receptors can improve negative symptoms of psychoses and reduce the extrapyramidal side effects that are often associated with typical antipsychotics.

How should I take Lurasidone?

Take Lurasidone only as directed by your doctor even if you feel well. Do not take more of Lurasidone and do not take it more often than your doctor ordered. Lurasidone works best if there is a constant amount in the blood. To keep blood levels constant, take Lurasidone at the same time each day and do not miss any doses.

You must take Lurasidone with food (containing at least 350 calories).

Dosing

The dose of Lurasidone will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Lurasidone. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (tablets):
    • For schizophrenia:
      • Adults—At first, 40 milligrams (mg) once a day. Your doctor may increase your dose as needed. However, the dose is usually not more than 160 mg per day.
      • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of Lurasidone, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Lurasidone administration

infoAdministration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Lurasidone should be taken with food (at least 350 calories).

Use Lurasidone regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.

It may take several weeks before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve.

Store at room temperature away from moisture and heat.

Lurasidone pharmacology

infoPharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.

Mechanism of Action

The mechanism of action of Lurasidone in the treatment of schizophrenia and bipolar depression is unknown. However, its efficacy in schizophrenia and bipolar depression could be mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism.

Pharmacodynamics

Lurasidone is an antagonist with high affinity binding at the dopamine D2 receptors (Ki=1 nM) and the 5-hydroxytryptamine (5-HT, serotonin) receptors 5-HT2A (Ki=0.5 nM) and 5-HT7 (Ki=0.5 nM) receptors. It also binds with moderate affinity to the human α2C adrenergic receptors (Ki=11 nM), is a partial agonist at serotonin 5-HT1A (Ki=6.4 nM) receptors, and is an antagonist at the α2A adrenergic receptors (Ki=41 nM). Lurasidone exhibits little or no affinity for histamine H1 and muscarinic M1 receptors (IC50 > 1,000 nM).

ECG Changes

The effects of Lurasidone on the QTc interval were evaluated in a randomized, double-blind, multiple-dose, parallel-dedicated thorough QT study in 43 patients with schizophrenia or schizoaffective disorder, who were treated with Lurasidone doses of 120 mg daily, 600 mg daily and completed the study. The maximum mean (upper 1-sided, 95% CI) increase in baseline-adjusted QTc intervals based on individual correction method (QTcI) was 7.5 (11.7) ms and 4.6 (9.5) ms, for the 120 mg and 600 mg dose groups respectively, observed at 2 to 4 hours after dosing. In this study, there was no apparent dose (exposure)-response relationship.

In short-term, placebo-controlled studies in schizophrenia and bipolar depression, no post-baseline QT prolongations exceeding 500 msec were reported in patients treated with Lurasidone or placebo.

Pharmacokinetics

The activity of Lurasidone is primarily due to the parent drug. The pharmacokinetics of Lurasidone is dose-proportional within a total daily dose range of 20 mg to 160 mg. Steady-state concentrations of Lurasidone are reached within 7 days of starting Lurasidone.

Following administration of 40 mg of Lurasidone, the mean (%CV) elimination half-life was 18 (7) hours.

Absorption and Distribution: Lurasidone is absorbed and reaches peak serum concentrations in approximately 1-3 hours. It is estimated that 9-19% of an administered dose is absorbed. Following administration of 40 mg of Lurasidone, the mean (%CV) apparent volume of distribution was 6173 (17.2) L. Lurasidone is highly bound (~99%) to serum proteins.

In a food effect study, Lurasidone mean Cmax and AUC were about 3-times and 2-times, respectively, when administered with food compared to the levels observed under fasting conditions. Lurasidone exposure was not affected as meal size was increased from 350 to 1000 calories and was independent of meal fat content.

In clinical studies, establishing the safety and efficacy of Lurasidone, patients were instructed to take their daily dose with food.

Metabolism and Elimination: Lurasidone is metabolized mainly via CYP3A4. The major biotransformation pathways are oxidative N-dealkylation, hydroxylation of norbornane ring, and S-oxidation. Lurasidone is metabolized into two active metabolites (ID-14283 and ID-14326) and two major non-active metabolites (ID-20219 and ID-20220). Based on in vitro studies, Lurasidone is not a substrate of CYP1A1, CYP1A2, CYP2A6, CYP4A11, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 or CYP2E1 enzymes. Because Lurasidone is not a substrate for CYP1A2, smoking is not expected to have an effect on the pharmacokinetics of Lurasidone.

Total excretion of radioactivity in urine and feces combined was approximately 89%, with about 80% recovered in feces and 9% recovered in urine, after a single dose of [14C]-labeled Lurasidone.

Following administration of 40 mg of Lurasidone, the mean (%CV) apparent clearance was 3902 (18.0) mL/min.


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References

  1. DailyMed. "LURASIDONE HYDROCHLORIDE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).

Reviews

The results of a survey conducted on ndrugs.com for Lurasidone are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Lurasidone. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.

User reports

1 consumer reported administration

When best can I take Lurasidone, on an empty stomach, before or after food?
ndrugs.com website users have also released a report stating that Lurasidone should be taken With a meal. In any case, this may not be the right description on how you ought to take this Lurasidone. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Lurasidone can be taken.
Users%
With a meal1
100.0%


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Information checked by Dr. Sachin Kumar, MD Pharmacology

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