Quetiapine

ATC CodeN05AH04
CAS number111974-69-7
PUB number5002
Drugbank IDDB01224
Empirical formulaC21H25N3O2S
Molar mass (g·mol−1)383,51
Physical statesolid
Melting point (°C)172–173
PKS value6,83

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, BSc

Markus Falkenstätter, BSc

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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