Quetiapine

Quetiapine
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
Solubility sparingly soluble in water

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.

Pharmacology

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
Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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