Quetiapine

Quetiapine

Basics

Quetiapine is an atypical antipsychotic medication (atypical neuroleptic) used to treat schizophrenia, bipolar disorder, and major depression. Quetiapine acts on both positive and negative symptoms of schizophrenia. It is taken by mouth and requires a prescription.

Effect

Pharmacodynamics

The mechanism of action of quetiapine is not yet fully understood. The antischizophrenic effect probably results from the interaction of the drug with dopamine type 2 (D2) and serotonin 2A (5HT2A) receptors. In bipolar depression and major depression, the effects of quetiapine could be attributed to the binding of this drug or its metabolite to the norepinephrine transporter. Additional effects of quetiapine, including somnolence, orthostatic hypotension, and anticholinergic effects, may result from antagonism of H1 receptors, adrenergic α1-receptors, and muscarinic M1-receptors, respectively.

Pharmacokinetics

The highest plasma concentration of quetiapine occurs 1.5 hours after oral administration. Plasma protein binding of quetiapine is 83%. The major active metabolite of quetiapine is norquetiapine (N-desalkylquetiapine). Quetiapine has an elimination half-life of 6 to 7 hours. Its metabolite, norquetiapine, has a half-life of 9 to 12 hours. Quetiapine is excreted after hepatic metabolism primarily via the kidneys (73%) and in the feces (20%), with the remainder (1%) excreted as the drug in its unmetabolized form.

Toxicity

Side effects

Very common (>10% incidence) adverse effects

  • dry mouth
  • Dizziness
  • Headache
  • Somnolence (drowsiness; of 15 antipsychotics, quetiapine causes the fifth most sedation. Extended-release (XR) formulations tend to produce less sedation at each dose than immediate-release formulations.)[16]

Common (1-10% incidence) adverse effects.

  • High blood pressure
  • Orthostatic hypotension
  • High pulse rate
  • Elevated blood cholesterol
  • Increased serum triglycerides
  • Abdominal pain
  • Constipation
  • Increased appetite
  • Vomiting
  • Elevated liver enzymes
  • Back pain
  • Asthenia
  • Insomnia
  • Lethargy
  • Tremor
  • Restlessness
  • Nasal congestion
  • Pharyngitis
  • Fatigue
  • Pain
  • Dyspepsia (indigestion)
  • Peripheral edema
  • Dysphagia
  • Weight gain

Rare (<1% incidence) adverse effects

  • Prolonged QT interval
  • Sudden cardiac death
  • Syncope
  • Diabetic ketoacidosis
  • Restless legs syndrome
  • Hyponatremia
  • Jaundice
  • Pancreatitis
  • Agranulocytosis
  • Leukopenia
  • Neutropenia
  • Eosinophilia
  • Anaphylaxis
  • Seizure
  • Hypothyroidism
  • Myocarditis
  • Cardiomyopathy
  • Hepatitis
  • Suicidal ideation
  • Priapism
  • Stevens-Johnson syndrome

Chemical & physical properties

ATC Code N05AH04
Formula C21H25N3O2S
Molar Mass (g·mol−1) 383,51
Physical State solid
Melting Point (°C) 172–173
PKS Value 6,83
CAS Number 111974-69-7
PUB Number 5002
Drugbank ID DB01224

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

The content of this page is an automated and high-quality translation from DeepL. You can find the original content in German here.

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