Olapine

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

Olapine is an antipsychotic agent and has affinities for serotonin 5HT2A/2C, 5HT3, 5HT6; dopamine D1, D2, D3, D4, D5; cholinergic muscarinic receptors M1-M5; α1 adrenergic; and histamine H1 receptors. The mechanism of action of Olapine, as with other drugs having efficacy in schizophrenia, is unknown. However, it has been proposed that this drug’s efficacy in schizophrenia is mediated through a combination of dopamine and serotonin type 2 (5HT2) antagonism. 

Olapine is well absorbed after oral administration, reaching peak plasma concentrations within 5 to 8 hours. The absorption is not affected by food. Olapine is not mutagenic or clastogenic as well as not carcinogenic.

The effect of olanzapine in the D2 receptor is reported to produce the positive effects of this drug such as a decrease in hallucinations, delusions, disorganized speech, disorganized thought, and disorganized behavior. On the other hand, its effect on the serotonin 5HT2A receptor prevents the onset of anhedonia, flat affect, alogia, avolition and poor attention. Based on the specific mechanism of action, olanzapine presents a higher affinity for the dopamine D2 receptor when compared to the rest of the dopamine receptor isotypes. This characteristic significantly reduces the presence of side effects.

Clinical trials for the original use of olanzapine demonstrated significant effectiveness in the treatment of schizophrenia and bipolar disorder in adults and acute manic or mixed episodes associated with bipolar disorder in adolescents.

The effect of olanzapine on dopamine and serotonin receptors has been suggested to reduce chemotherapy-induced nausea and vomiting as those receptors are suggested to be involved in this process. For this effect, several clinical trials have been conducted and it has been shown that olanzapine can produce a significant increase in total control of nausea and vomiting. In a high-level study of the effect of olanzapine for this condition, a complete response on the delay phase was observed in 84% of the individual and control of emesis of over 80% despite the phase.

Trade Name Olapine
Availability Prescription only
Generic Olanzapine
Olanzapine Other Names Olanzapin, Olanzapina, Olanzapine, Olanzapinum
Related Drugs Rexulti, Vraylar, sertraline, trazodone, Lexapro, Zoloft, citalopram, quetiapine, lamotrigine, Abilify
Weight 10mg, 5mg
Type Tablet
Formula C17H20N4S
Weight Average: 312.432
Monoisotopic: 312.14086735
Protein binding

Olanzapine is largely bound to plasma proteins and hence, about 93% of the administered dose is bound. The main proteins for binding are albumin and alpha-1 acid glycoprotein.

Groups Approved, Investigational
Therapeutic Class Atypical neuroleptic drugs
Manufacturer Drug International Ltd
Available Country Bangladesh
Last Updated: September 19, 2023 at 7:00 am
Olapine
Olapine

Uses

Olapine is used for the acute and maintenance treatment of schizophrenia and related psychoses where positive symptoms (e.g. delusions, hallucinations, disordered thinking, hostility and suspiciousness) and/or negative symptoms (e.g. flattened affect, emotional and social withdrawal, poverty of speech) are prominent.

Olapine is used for the treatment of acute manic or mixed episodes in bipolar disorder, with or without psychotic features and with or without a rapid cycling course

Olapine is also used to associated treatment for these conditions: Acute Agitation, Acute Depressive Episode, Bipolar 1 Disorder, Bipolar Disorder With Manic or Mixed Episodes, Delirium, Delusional Parasitosis, Gilles de la Tourette's Syndrome, Major depressive disorder, recurrent episode, Mixed manic depressive episode, Post Traumatic Stress Disorder (PTSD), Psychosis, Schizophrenia, Acute Manic episode

How Olapine works

The activity of olanzapine is achieved by the antagonism of multiple neuronal receptors including the dopamine receptor D1, D2, D3 and D4 in the brain, the serotonin receptors 5HT2A, 5HT2C, 5HT3 and 5HT6, the alpha-1 adrenergic receptor, the histamine receptor H1 and multiple muscarinic receptors.

As abovementioned, olanzapine presents a wide profile of targets, however, its antagonistic effect towards the dopamine D2 receptor in the mesolimbic pathway is key as it blocks dopamine from having a potential action at the post-synaptic receptor. The binding of olanzapine to the dopamine D2 receptors is easily dissociable and hence, it allows for a certain degree of dopamine neurotransmission.

On the other hand, olanzapine acts in the serotonin 5HT2A receptors in the frontal cortex in a similar manner than the reported on dopamine D2 receptors. This determined effect allows for a decrease in adverse effects.

Dosage

Olapine dosage

The recommended starting dose for Olapine is 10 mg/day, administered as a single daily dose without regard to meals. Daily dosage may subsequently be adjusted on the basis of individual clinical status within the range of 5-20 mg daily. An increase to a dose greater than the routine therapeutic dose of 10 mg/day i.e. to a dose of 15 mg/day or greater, is recommended only after appropriate clinical reassessment.

Children: Olapine has not been studied in subjects under 18 years of age.

Elderly patients (age 65 and over): starting dose 5 mg/day

Patients with hepatic and/or renal impairment: starting dose 5 mg/day 

When more than one factor is present which might result in slower metabolism (female gender, geriatric age, non-smoking status), consideration should be given to decreasing the starting dose. Dose escalation, when indicated, should be conservative in such patients.

Side Effects

Very common undesirable effects are somnolence and weight gain. Besides increased appetite, elevated glucose levels, elevated triglyceride levels, dizziness, akathisia, Parkinson's disease, dyskinesia, orthostatic hypotension, mild and transient anticholinergic effects including constipation and dry mouth, asthenia, edema and photosensitivity reaction etc. may be observed.

Toxicity

The toxicity symptoms of olanzapine are known to include somnolence, mydriasis, blurred vision, respiratory depression, hypotension, extrapyramidal symptoms and anticholinergic effects. The overdosage effects in children are generally associated with more significant side effects.

The maximum registered dosage of olanzapine in clinical trials was of 300 mg and it was reported to present drowsiness and slurred speech. However, on post-marketing surveillance, a wide range of symptoms have been presented including agitation, dysarthria, tachycardia, extrapyramidal symptoms, and reduced consciousness. One case of overdosage-driven death was reported after ingestion of 450 mg of olanzapine. In the cases of acute overdosage, the establishment of adequate oxygenation and ventilation, gastric lavage and administration of activated charcoal with a laxative is recommended.

In carcinogenesis studies, olanzapine was showed to present an increase in the incidence of liver hemangiomas and hemangiosarcomas as well as mammary gland adenomas, and adenocarcinomas. On fertility studies, there was solely found impairment in male mating performance and delays in ovulation. There is no evidence of mutagenic, genotoxic potential not adverse events on fertility.

Precaution

Olapine should be used cautiously in patients who have a history of seizures or have conditions associated with seizures. Olapine should be used cautiously in patients with low leukocyte and/or neutrophil counts for any reason, drug induced bone marrow depression/toxicity caused by radiation therapy or chemotherapy, hypereosinophilic conditions, impaired hepatic function, and patients using hepatotoxic medicines, centrally acting drug and medicines know to increase QT interval, especially in the elderly. Patients should be cautioned about operating hazardous machinery, including motor vehicles.

Interaction

Drugs that induce CYP1A2 or glucoronyl transferase enzymes (omeprazole, rifampicin), inhibitor of CYP1A2 (fluvoxamine), centrally acting drugs, antihypertensive agents.

Food Interaction

  • Avoid alcohol. Alcohol may potentiate CNS adverse effects and orthostatic hypotension.
  • Take with or without food. The absorption of olanzapine is unaffected by food.

[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.

Olapine 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.

Volume of Distribution

The volume of distribution of olanzapine is reported to be of 1000 liters which indicate a large distribution throughout the body.

Elimination Route

Olapine presents a linear pharmacokinetic profile and, after daily administration, it reaches steady-state in about a week. Under the administration of a normal dosage of olanzapine, the steady-state plasma concentration does not seem to exceed 150 ng/ml with an AUC of 333 ng/h/ml.

The absorption of olanzapine is not affected by the concomitant administration of food. The pharmacokinetic profile of olanzapine is characterized by reaching peak plasma concentration of 156.9 ng/ml approximately 6 hours after oral administration.

Half Life

Olapine presents a half-life ranging between 21 to 54 hours with an average half-life of 30 hours.

Clearance

The mean clearance rate of olanzapine is of 29.4 L/hour however, some studies have reported an apparent clearance of 25 L/h.

Elimination Route

Olapine is mainly eliminated through metabolism and hence, only 7% of the eliminated drug can be found as the unchanged form. It is mainly excreted in the urine which represents around 53% of the excreted dose followed by the feces that represent about 30%.

Pregnancy & Breastfeeding use

Olapine should be used in pregnancy only if the potential benefits justify the potential risk to the foetus. So, patients should be advised to notify their physician if they become pregnant or intend to become pregnant during treatment with Olapine. There is no report to show teratogenecity. Patients should not breast feed if they are taking Olapine.

Contraindication

This is contraindicated in those patients with a known hypersensitivity to Olapine as well as in patients with known risk for narrow-angle glaucoma.

Concomitant illness: Olapine in patients with concomitant illness is limited, caution is advised when prescribing for patients with prostatic hypertrophy, or paralytic ileus and related conditions.

Neuroleptic Malignant Syndrome (NMS): If a patient develops signs and symptoms indicative of NMS, or presents with unexplained high fever without additional clinical manifestations of NMS, all antipsychotic medicines, including olanzapine must be discontinued.

Acute Overdose

Symptoms: Tachycardia, agitation/aggressiveness, dysarthria, extrapyramidal symptoms, reduced level of consciousness ranging from sedation to coma. 

Management: Symptomatic and supportive treatment. Gastric lavage and admin of activated charcoal may be effective.

Storage Condition

Store below 30˚ C. Protect from light and moisture. Keep out of the reach of children.

Innovators Monograph

You find simplified version here Olapine

Olapine contains Olanzapine see full prescribing information from innovator Olapine Monograph, Olapine MSDS, Olapine FDA label

FAQ

What is Olapine used for?

Olapine is an atypical antipsychotic primarily used to treat schizophrenia and bipolar disorder. For schizophrenia, it can be used for both new-onset disease and long-term maintenance.

How safe is Olapine?

Olapine is safe and effective in nonselected schizophrenic outpatients and are consistent with the efficacy and safety profile that Olapine has shown in previous controlled clinical trials.

How does Olapine work?

Olapine works by affecting naturally occurring chemical messengers in your brain.

What are the common side effects of Olapine?

Common side effects of Olapine are include:

  • dizziness, feeling unsteady, or having trouble keeping your balance
  • restlessness
  • unusual behavior
  • depression
  • difficulty falling asleep or staying asleep
  • weakness
  • difficulty walking
  • constipation
  • weight gain
  • dry mouth
  • pain in arms, legs, back, or joints
  • breast enlargement or discharge
  • late or missed menstrual periods
  • decreased sexual ability

Is Olapine safe during pregnancy?

Olapine should be used in pregnancy only when potential benefit justifies potential risk to the fetus. Olapine should only be considered during breastfeeding when the potential benefit justifies the potential risk to the infant.

Is Olapine safe during breastfeeding?

A safety scoring system finds Olapine to be acceptable during breastfeeding.

Can I drink alcohol with Olapine?

Avoid drinking alcohol or using illegal drugs while you are taking Olapine.

Can I drive after taking Olapine ?

Do not drive a car or operate machinery until you know how this medication affects you.

When should be taken of Olapine?

It is usually recommended to take Olapine at bedtime because it can cause sleepiness as a side effect. However, it is important to choose a time of day to take it that you can easily remember, which could be bedtime, a mealtime, or when you brush your teeth.

Can I take Olapine on an empty stomach?

You can take Olapine once daily with food or on an empty stomach.

How long does Olapine take to work?

When you first start taking Olapine, it may make you feel more relaxed and calm. Within 2 to 3 weeks, your other symptoms may start to improve. You may find Olapine makes you: able to concentrate better, and think more clearly.

Can I take Olapine for a long time?

Yes, many people take Olapine for a long time, including for many months or years, without any problems. Olapine can increase the amount of sugar in your blood and this can sometimes lead to diabetes.

What happens when I stop taking Olapine?

Stopping Olapine suddenly can cause withdrawal effects and stopping it too early could cause your illness to come back. See your doctor if you want to stop taking Olapine because it is better to come off it gradually.

Does Olapine help me sleep?

Olapine seems to preserve the normal structure of sleep and increase the amount of slow-wave sleep, which might be of additional benefit in treatment of schizophrenia.

Who should not take Olapine?

Olapine is not approved for use in older adults with dementia-related psychosis.

What happens if I miss a dose?

Take Olapine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention.Overdose symptoms may include drowsiness, agitation, aggression, slurred speech, confusion, increased heart rate, jerky or uncontrolled muscle movements, trouble breathing, or fainting.

What happen If I just stop taking Olapine?

Stopping Olapine suddenly can cause withdrawal effects and stopping it too early could cause your illness to come back. See your doctor if you want to stop taking Olapine because it is better to come off it gradually.

Does Olapine cause brain damage?

When taken together, both Olapine and illness relapse have an effect on brain structure.

Does Olapine help me sleep?

Olapine seems to preserve the normal structure of sleep and increase the amount of slow-wave sleep, which might be of additional benefit in treatment of schizophrenia. The effective clinical dose may be lower for females than males.

Does Olapine make me hungry?

Olapine is associated with elevated appetite and food intake and decreased activity or impairment of metabolic regulation.

Will Olapine affect my fertility?

Olapine may increase the level of a hormone called prolactin in the body for a short time when you start taking it, but not to a very high level. If prolactin levels do rise for a short time after starting Olapine, this may affect fertility, regardless of gender.

Can Olapine affect kidneys?

Several adverse outcomes attributed to atypical antipsychotic drugs, specifically Olapine are known to cause acute kidney injury.

*** Taking medicines without doctor's advice can cause long-term problems.
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