Highlighting pharmacokinetics, pharmacodynamics and mechanism of action

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US brand name: Latuda
Generic name: lurasidone

Pharmacology

Latuda’s Half-Life & How Long Until It Clears Your System

18 hours. Cleared in approximately 5 days.

Steady State

7 days.

Half-life is the average time it takes for you to process half of the drug’s active ingredient. If a drug has a half-life of around 24 hours and you take a dose of 100mg, you’ll have roughly the equivalent a 50mg dose after one day, a 25mg dose after two days, and so on. The rule of thumb is: multiply the half-life by five and you get how long it is for the dose you took to be cleared from your bloodstream1.

Steady state is the flipside of half-life. This is when you can expect to get over side effects caused by fluctuating amounts of a medication in your bloodstream. Often, but not always the same amount of time as the plasma clearance above.



How lurasidone Works

the current best guess at any rate

Lurasidone Pharmacodynamics & Mechanism of Action

According to Sunovion, the same as all SGAs / AAPs when it comes to schizophrenia:

[T]hrough a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. Latuda PI sheet

In English: Blocking excess brain juice at the bits of your brain responsible for both the positive symptoms (the dopamine receptors) of schizophrenia, like delusions and hallucinations, and its negative symptoms and bipolar depression (the serotonin receptors). The effect on

Latuda is a really potent D2 antagonist. It’s also a really potent 5HT7 antagonist, which explains why it knocks some people out when it doesn’t touch H1 histamine receptors. Like Saphris, Latuda doesn’t touch M1 muscarinic receptors. Latuda is also a moderate partial 5HT1A agonist like Geodon and Seroquel. Latuda’s effect on 5HT1A, 5HT2A and 5HT7 explain why it’s a pretty good antidepressant and helps with negative symptoms.

The activity of LATUDA is primarily due to the parent drug. LATUDA is metabolized into two active metabolites (ID-14283 and ID-14326) and two major non-active metabolites (ID-20219 and ID-20220).

Lurasidone Pharmacokinetics

The pharmacokinetics of LATUDA is dose-proportional within a total daily dose range of 20 mg to 160 mg. Steady-state concentrations of LATUDA are reached within 7 days of starting LATUDA.

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

Absorption and Distribution: LATUDA 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 LATUDA, the mean (%CV) apparent volume of distribution was 6173 (17.2) L. LATUDA is highly bound (~99%) to serum proteins.

In a food effect study, LATUDA mean Cmax and AUC were about 3-times and 2-times, respectively, when administered with food compared to the levels observed under fasting conditions. LATUDA exposure was not affected as meal size was increased from 350 to 1000 calories and was independent of meal fat content [see Dosage and Administration (2.2)].

In clinical studies, establishing the safety and efficacy of LATUDA, patients were instructed to take their daily dose with food [see Dosage and Administration (2.2)].

Metabolism and Elimination: LATUDA is metabolized mainly via CYP3A4.

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 LATUDA.

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

Active Ingredient

lurasidone hydrochloride

The active ingredient is usually the same as the generic name, but more often than not it’s a chemical salt of the substance identified as the generic. E.g. Fluoxetine is the generic for Prozac, but the active ingredient is fluoxetine hydrochloride (or HCl). It usually doesn’t make much of a difference outside of the more esoteric aspects of a drug’s pharmacology, but not always.



Shelf Life

4 years



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1 After five times the half-life you'll have reached what's called "Plasma clearance," or "not enough left in your bloodstream to latch onto your brain and do anything." It's based on Julien's calculations from A Primer of Drug Action, and half-life multiplied by five is the generally accepted estimate of how long it takes a single dose of any given drug to be eliminated from the blood stream/plasma of someone with a normal metabolism. That's also the rough estimate for steady state if they can't get, or won't provide a number for that.
The next level is "Complete clearance", and is a complex equation based on a lot of factors which may or may not: be published in the PI sheet, include personal data like your weight, or even completely figured out by corporate and independent researchers. It usually winds up being within (as in usually, but not always, after) 2-5 days of plasma clearance no matter what, but sometimes can take weeks. Sometimes a drug will clear from your brain and other organs before it clears from your blood.
That's how it works for crazy meds. I have no idea what the average complete clearance is for other types of medications. For all I know there are drugs that utterly vanish from your system in under five passes, and others that won't let go of your squishy bits for years after you stop taking them.


Last modified on Wed, 04 May, 2016 at 17:23:40 by JerodPoorePage Author Date created Tuesday, 14 May 2013 at 09:18:44
“Latuda (lurasidone) Pharmacology” by Jerod Poore is copyright © 2013 Jerod Poore Published online 2013/05/14

Latuda, and all other drug names on this page and used throughout the site, are the trademarks of someone else. Latuda’s PI Sheet will probably have the name of the manufacturer and trademark owner (they’re not always the same company) at or near the very bottom. Or ask Google who the owner is. The way pharmaceutical companies buy each other and swap products like Monopoly™ real estate, the ownership of the trademark may have changed without my noticing. It may of changed hands by the time you finished reading this article.



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Don’t automatically believe everything you read on teh Intergoogles. No warranty is expressed or implied in this information. Consult one or more doctors and/or pharmacists before taking, or changing how you take any neurological and/or psychiatric medication. Your mileage may vary. What happened to us won’t necessarily happen to you. For more details see the Crazymeds big-ass disclaimer.

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