Our new product: Olanzapine

In autumn 2014 the Russian Ministry of healthcare approved production of a new medicine named “Olanzapine” in the form of tablets for a producer “ALSI Pharma” (registration certificate number ЛП-002640 from 25.09.2014). This preparation is new for us, but it extends the range of “Neurology and psychiatric” portfolio. We have been steadily producing only one antipsychotic remedy, named Haloperidol. Not taking into account, that Haloperidol is a “gold standard” for psychiatric application (it is a derivate of butyrophenone), there are some newer and more reliable and effective medicines in the pharmaceutical market. This group of drugs can be characterized as typical (derivates of phenothiazine or butyrophenone) or atypical neuroleptics (antipsychotic drugs). The second class of antipsychotics (atypical ones) possesses stronger effect and they don’t have many of group adverse reactions (which reside in many antipsychotics), such as, for example, extrapyramidal symptoms. That is why the therapy with atypical antipsychotics is safer and, as a rule, more effective. Olanzapine belongs to the second (atypical) group of antipsychotics.

Olanzapine

Olanzapine, a thienobenzodiazepine, is an antipsychotic agent that demonstrates a broad pharmacologic profile across a number of receptor systems. Olanzapine displays high receptor affinity binding in vitro at dopamine D2, D3, D4, 5-HT2A/C, 5-HT3, 5-HT6, muscarinic M1-M5, adrenergic α1, and histamine H1 receptor subtypes, while displaying a lower affinity at dopamine D1 and D5 receptor subtypes. In a behavioural paradigm predictive of antipsychotic activity, olanzapine reduced conditioned avoidance response in rats at doses lower than 4 times those required to produce catalepsy. In a single dose (10 mg) PET study in healthy subjects, olanzapine produced higher 5-HT2A than dopamine D2 receptor occupancy. The percent of D2 occupancy was less than the threshold value predictive of extrapyramidal events.

Olanzapine is well absorbed after oral administration, reaching peak plasma concentrations within 5 to 8 hours. The absorption is not affected by food. Olanzapine is metabolized in the liver by conjugative and oxidative pathways. The major circulating metabolite is the 10-N-glucuronide, which is pharmacologically inactive and does not pass the blood brain barrier. The major activity of Olanzapine can be produced by olanzapine itself and it can pass the blood brain barrier. After oral administration to healthy subjects, the mean terminal elimination halflife was 33 hours (21-54 hours for 5-95%). The pharmacokinetic profile of Olanzapine is depended on smoking status, gender and age.

According to meta-analysis data, olanzapine exceeds haloperidol in probability of successful therapy, ascension of psychiatric level (lowering of severity of psychiatric disorders), lowering of productive and negative disturbances. As some studies show, olanzapine exceeds haloperidol in the positive influence on cognitive functions, but some other studies show that there is no difference between these two drugs on cognitive function. The studies are evidence of lower level of relapse during olanzapine therapy in comparison with the treatment, using haloperidol [1].

Olanzapine by “ALSI Pharma” is going to be manufactured in the form of usual tablets 5 mg or 10 mg, packed into a carton box with the quantity of 30 tablets (3 blisters, 10 tablets in each). Olanzapine is a prescription only product in the vast majority of countries. The specialists, who can prescribe this medicine, are mainly doctors, such as psychiatrists or neurologists. They can practice in hospitals or ambulances. Read carefully the specialist’s or patient’s leaflet, attached to any drug’s package, before prescribing or taking these tablets. Seek for your doctor’s or pharmacist’s advice in case you have any doubts or don’t feel confident about this remedy. 

References:

1)    Lehman AF, Lieberman JA, Dixon LB, McGlashan TH, Miller AL, Perkins DO, Kreyenbuhl J Practice Guideline for the Treatment of Patients With Schizophrenia. — 2nd ed. — American Psychiatric Association, 2004.