Quetiapine

Introduction to Quetiapine

[​IMG]
Quetiapine was developed by AstraZenica from 1992 to 1996, and received FDA approval in 1997. Annual sales exceed US$1.3b, and several generic versions are now available.

Using Quetiapine

Ways of Administration

Oral

Dose

Column 1 Column 2
Threshold mg
Light 150
Medium 300
Strong 800

Effects of Quetiapine

Quetiapine can decrease hallucinations, increase concentration, think more postively about yourself, prevent mood swings and reduce the frequency of mood swings.

Quetiapine combinations

Recreational drug combinations with Quetiapine

Concurrent use with stimulants (Amphetamines, MDMA, Cocaine) may reduce the efficacy of either or both agents. [2]

Dangerous interactions with Quetiapine

No dangerous combinations with Quetiapine have been added to this wiki yet.

Medication interactions with Quetiapine

Quetiapine can in combination with hepatic enzyme inducers result in lower plasma concentrations, and increased dosage may be required.

Potentiators of Quetiapine

No Potentiation combinations with Quetiapine have been added to this wiki yet.

Different Uses for Quetiapine

Quetiapine is commonly used for the treatment of insomnia, however this is not recommended and there is little evidence of it's benefit and concerns about the dangerous side effects.[3]

Recreational use of Quetiapine

No data

Pharmacology of Quetiapine

General

Quetiapine and its active metabolite norquetiapine interact with a range of neurotrasmitter receptors. Both quetiapine and norquetiapine are antagonists of the serotonin 5HT2 and Dopamine D1 and D2 receptors, with a higher affinity for the 5HT2 receptors over the D2 receptors. Both have a high affinity for the histiminergic and adrenergic aplpha1 receptors and moderate at the adrenergic alpha2 receptors. Quetiapine has no affinity for the norepinephrine transporter (NET) or the 5HT1A receptors. Norquetiapine has a high affinity for both, which may account for it's antidepressant effects. Norquetiapine has a moderate to high affinity for the muscarinic receptors which may explain its anticholinergic effects [4]

Targets, Enzymes, and Transporters

Targets

Target​
Action​
5HT2A Antagonist
5HT1A Partial Agonist
D1 Antagonist
D2 Antagonist
H1 Antagonist
α1 Antagonist
[5]

Chemistry of Quetiapine

Property[/b]​
Values[/b]​
Systematic(IUPAC) name: 2-(2-(4-dibenzo(b,f)(1,4)thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol
Synonyms: 204636 ICI, Ethanol, 2-(2-(4-dibenzo(b,f)(1,4)thiazepin-11-yl-1-piperazinyl)ethoxy)-, (E)-2-butenedioate (2:1) (salt), Fumarate, Quetiapine, Seroquel
Molecular Formula: C21H25N3O2S
Molar mass: 383.5071 g/mol
CAS Registry Number: 111974-69-7
Melting Point: no data
Boiling Point: no data
Flash Point: 9.7 ℃
Solubility: 0.5869 mg/L at 25 deg C (est)
Additional data: none.
Notes:


[6]

Reagent test results of Quetiapine

The Dangers of Quetiapine

General Warnings

Pregnancy – Neonates exposed during pregnancy are at risk of extrapyrimidal neurological disturbances and withdrawal symptoms. The safety of quetiapine during pregnancy has not been established.

Lactation – There have been reports of quetiapine excretion into human breast milk.

Driving or operating heavy machinery – Due to its sedating properties patients should not drive or operate machinery until their individual sensitivity to the medication is established.

Side Effects and Interactions

Potential Side Effects

Dry mouth
Elevations in serum triglyceride levels
Elevations in total cholesterol (predominantly LDL cholesterol)
Decreases in HDL cholesterol
Weight gain
Decreased haemoglobin
Dizziness
Somnolence
Extrapyramidal symptoms
Leukopenia
Tachycardia
Palpitations
Vision blurred
Constipation
Dyspepsia
Vomiting
Mild asthenia
Peripheral oedema
Irritability
Pyrexia
Elevations in serum alanine aminotransferase (ALT)
Elevations in gamma-GT levels
Neutrophil count decreased
Eosinophils increased
Blood glucose increased to hyperglycaemic level
Elevations in serum prolactin
Decreases in Total T4
Decreases in Free T4
Decreases in Total T3
Increases in TSH2
Dysarthria
Increased appetite
Dyspnoea
Orthostatic hypotension
Abnormal dreams and nightmares
Bradycardia
Dysphagia
Hypersensitivity
Angioedema
Elevations in serum aspartate aminotransferase (AST)
Platelet count decreased
Decreases in Free T3
Seizure
Restless legs syndrome
Tardive dyskinesia
Syncope
Rhinitis Urinary retention
Neuroleptic malignant syndrome
Hypothermia Hepatitis (with or without jaundice)
Elevations in blood creatine phosphokinase
Agranulocytosis
Somnambulism and other related events
Priapism Galactorrhoea
Intestinal obstruction/Ileus
Anaphylactic reaction

Potential Drug Interactions

Due to the central nervous system effects quetiapine should not be comined with other central nervous acting substances.

Quetiapine should be used with caution with other medications that may cause electrolyte imbalance or increase QT interval.

Quetiapine should be used with caution with other medications that have anticholinergic (muscaranic) effects.

Potential Food Interactions

Physical Health Risks

Mental Health Risks

Suicide

Risk of suicide is associated with depression, schizophrenia and bipolar disorders. Close supervision of at risk patients should accompany therapy.

Overdose

Survival has been reports in overdoses of up to 30 grams. Death has been reported in an overdose of 13.6 grams. Most people who overdose on quetiapine make a full recovery with no adverse effects. People with cariovascular problems may be at increased risk during overdose.

Reported Deaths

Death has been reported in an overdose of 13.6 grams.

Producing Quetiapine

Forms of Quetiapine

Quetiapine is available in standard release and sustained release oral adminstration forumulations.

Legal Status of Quetiapine

United Nations

USA

Unscheduled but available on prescription only.

EU

Other Countries

History of Quetiapine

Quetiapine was developed by AstraZenica from 1992 to 1996, and received FDA approval in 1997.

References

  1. ^Gugger, J. J, Cassagnol, M. (2008). Low-dose quetiapine is not a benign sedative-hypnotic agent. The American Journal on Addictions, 17 (5), 454–455.
  2. ^Dean, A. (2006). Illicit drugs and drug interactions. Australian Pharmacist. 25 9. 684-689.
  3. ^Coe, H. V, Hong, I. S. (2012). Safety of Low Doses of Quetiapine When Used for Insomnia. Annals of Pharmacology, 718-722.
  4. ^Astrazenica. (2015). Seroquel Data Sheet 161115.
  5. ^Guzman, F. Psychopharmacological Institute. Mechanism of Action of Quetiapine.
  6. ^National Center for Biotechnology Information. PubChem Compound Database; CID=5002

This page has been seen 19,206 times.