Olanzapine

ATC CodeN05AH03
CAS number132539-06-1
PUB number135398745
Drugbank IDDB00334
Empirical formulaC17H20N4S
Molar mass (gยทmolโˆ’1)312,432
Physical statesolid
Density (gยทcmโˆ’3)1,3
Melting point (ยฐC)189-195
Boiling point (ยฐC)476
PKS value10,57
Solubility0.0942 mg/mL

Basics

Olanzapine is an active substance that is used to treat schizophrenia and bipolar disorder. It belongs to the group of atypical neuroleptics. Olanzapine has an antipsychotic effect, combats manic episodes and stabilizes mood. Olanzapine is very similar to clozapine. It is a yellow, crystalline powder that is insoluble in water.

Graphic structural formula of the active substance olanzapine

Effect

Olanzapine acts by binding to the neurotransmitters in the brain, specifically to the dopamine-2 receptors and the 5HT2A serotonin receptors. Olanzapine also binds to a small extent to the muscarinic receptors, the adrenoreceptors and the histamine receptors. However, its main effect is based on blocking the dopamine 2 receptors (D2 receptors), which inhibits the effect of dopamine. The advantage of olanzapine over other active substances of the same class is that extrapyramidal motor disorders occur much less frequently - and if they do, then only at very high doses. At the same time, the risk of agranulocytosis is also reduced. As with other neuroleptics, olanzapine must also be taken for several days to weeks before it takes full effect.

Olanzapine is broken down via the liver, mainly via the enzymes CYP1A2 and CYP2D6. It is excreted 53% via urine and 30% via feces.

The half-life of olanzapine, i.e. the time it takes the body to excrete half of the active substance, is around 30 hours.

Dosage

Always take olanzapine exactly as described in the package leaflet or as agreed with your doctor.

The usual recommended dose for adults is between 5 mg and 15 mg daily .

The maximum dose for adults is 20 mg per day .

The recommended dose for children/adolescents (10-17 years ) is between 2.5 mg and 5 mg daily.

The maximum dose for children is 12.5 mg per day.

Side effects

The following side effects may occur:

Very common:

  • Weight gain
  • drowsiness
  • Increased prolactin levels in the blood
  • dizziness

Frequent:

  • Changes in the levels of some blood cells and blood lipids
  • Increased liver values (especially at the beginning)
  • Increased sugar levels in the blood and urine
  • Increased uric acid and creatinine phosphokinase levels in the blood
  • Increased feeling of hunger
  • restlessness
  • trembling
  • unusual movements
  • constipation
  • dry mouth
  • rash
  • weakness
  • severe fatigue
  • Water retention in the tissue
  • fever
  • joint pain
  • Sexual dysfunction

Occasionally:

Rarely:

Very rare:

  • severe allergic reactions

Olanzapine can cause strokes, pneumonia, falls, hallucinations and walking difficulties in elderly patients with dementia.

Olanzapine can worsen Parkinson's disease.

Olanzapine can cause extreme weight gain and increase the risk of diabetes.

Interactions

Interactions may occur if the following medicines are taken at the same time:

Contraindications

Olanzapine must NOT be taken in the following cases

  • if you are allergic to olanzapine
  • eye problems(glaucoma)

Age restriction

In some preparations, the use of olanzapine is approved from the age of 10, in most other preparations only from the age of 18.

However, this should always be discussed with your doctor beforehand.

Pregnancy & breastfeeding

Olanzapine should only be taken during pregnancy after consultation with your doctor.

In the first trimester of pregnancy , no increased risk of malformation has been demonstrated, but pregnant women are at increased risk of excessive weight gain and gestational diabetes.

In the 2nd and 3rd trimester of pregnancy, if taken up to birth, adaptation disorders may occur in the newborn. These include respiratory, gastrointestinal and nervous system disorders. In very rare cases, seizures may also occur. These adaptation disorders pass after a few days and the newborn develops normally.

Quetiapine can be used as an alternative.

During breastfeeding, olanzapine should only be taken after consultation with your doctor. Small amounts of olanzapine pass into breast milk. In some cases, sedation, tremors and hyperexcitability have occurred in infants. The Pharmacovigilance and Advisory Center for Embryonal Toxicology of the Charitรฉ-Universitรคtsmedizin Berlin is of the opinion that breastfeeding is acceptable with reservations when olanzapine is used alone and the child is well observed.

History of the active ingredient

Olanzapine is marketed under the trade name Zyprexa by the pharmaceutical company Eli Lilly. The company had to pay billions in compensation in the Zyprexa scandal. Olanzapine can sometimes lead to extreme weight gain and an increased risk of diabetes. This was deliberately concealed or downplayed by the manufacturing company. In addition, the drug was illegally advertised for the treatment of certain illnesses for which it has no indication.

Thomas Hofko

Thomas Hofko


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Zalasta 5 mg orodispersible tablets

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Zalasta 20 mg tablets

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Zalasta 15 mg tablets

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Zalasta 10 mg tablets

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