Quetiapine , marketed as Seroquel among other names, is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder. Sometimes it is also used as a sleeping pill because of its tranquilizing effect, but this use is not recommended. It was taken by mouth.
Common side effects include drowsiness, constipation, weight, and dry mouth. Other side effects include low blood pressure with standing, seizures, prolonged erections, high blood sugar, and neuroleptic malignant syndrome. In elderly people with dementia its use increases the risk of death. Use during the latter part of pregnancy can cause movement disorders in infants for the period after birth. Quetiapine is believed to work by blocking a number of receptors including serotonin and dopamine receptors.
Quetiapine was developed in 1985 and approved for medical use in the United States in 1997. Patent protection for the product expires in 2012; However, in some areas, long acting versions remain patentable until 2017. In the United States in 2017, short acting versions have wholesale costs of approximately 12 US per month. In the United Kingdom, the cost of one month NHS costs around Ã, Â £ 3.19.
Video Quetiapine
Medical use
Quetiapine is primarily used to treat schizophrenia or bipolar disorder.
Schizophrenia
Cochrane's 2013 review compares quetiapine with typical antipsychotics:
In a comparison of 2013 15 antipsychotics in effectiveness in treating schizophrenia, quetiapine demonstrated a standard effectiveness. It is 13-16% more effective than ziprasidone, chlorpromazine, and asenapine and is approximately as effective as haloperidol and aripiprazole.
There is tentative evidence about the benefits of quetiapine versus placebo in schizophrenia; however, definite conclusions are unlikely because of the high level of attrition in trials (over 50%) and lack of data on economic outcomes, social function, or quality of life.
It is debatable whether, as a class, typical or atypical antipsychotics are more effective. Both have the same drop-out and symptom relapse rates when typically used at low to moderate doses. While quetiapine has lower levels of extrapyramidal side effects, there is greater drowsiness and dry mouth level.
A Cochrane review comparing quetiapine with other atypical antipsychotic agents tentatively concluded that it may be less potent than olanzapine and risperidone; produce fewer movement-related side effects than paliperidone, aripiprazole, ziprasidone, risperidone and olanzapine; and produce weight gain similar to risperidone, clozapine and aripiprazole. They concluded that it resulted in suicide attempts, suicide, death, QTc prolongation, low blood pressure, tachycardia, sedation, gynecomastia, galactorrhoea, menstrual irregularities and white blood cell counts at the same level as first-generation antipsychotics.
Bipolar disorder
In those with bipolar disorder, quetiapine is used to treat depressive episodes, episodes of acute mania associated with bipolar I disorder (either as monotherapy or adjunctive therapy for lithium, valproate or lamotrigine), and bipolar I treatment treatment treatments (as adjunctive therapy for lithium or divalproex).
Major depressive disorder
Quetiapine is effective when used by itself and when used in conjunction with other drugs in major depressive disorder (MDD). However, sedation is often an undesirable side effect.
In the United States, the United Kingdom and Australia (while not subsidized by the Australian Pharmaceutical Scheme for MDD Treatment), quetiapine is licensed for use as an adjunct to treatment in MDD.
Alzheimer's Disease
Quetiapine does not decrease agitation among people with Alzheimer's. Quetiapine exacerbates the intellectual function in the elderly with dementia and is therefore not recommended.
More
The use of low doses of quetiapine for insomnia, while common, is not recommended; there is little evidence of benefits and concerns about side effects.
Sometimes used off-label, often as an augmentation agent, to treat conditions such as Tourette's syndrome, hallucinations of music and anxiety disorders.
Quetiapine and clozapine are the most widely used drugs for the treatment of psychosis of Parkinson's disease because they are extremely low in extrapyramidal side effects. Because of the risks associated with clozapine (eg agranulocytosis, diabetes mellitus, etc.), doctors often try treatment with the first quetiapine, although evidence to support quetiapine use for this indication is significantly weaker than clozapine.
Maps Quetiapine
Adverse effects
Sources for incident list:
- The side effects are very common (& gt; 10% incident)
- Dry mouth
- Dizzy
- Headaches
- Somnolen (drowsiness of the 15 quipiapine antipsychotics causes the 5th most sedation.) Extended release (XR) formulations tend to produce less sedation, dose-by-dosage than immediate release formulations)
- Common side effects (1-10% incident)
- Extrapyramidal diseases: quetiapine and clozapine are noted for their relapant extrapyramidal side-effects
- Weight: SMD 0.43 kg when compared with placebo. Produces approximately as much weight as risperidone, less weight than clozapine, olanzapine and zotepine and more weight gain than ziprasidone, lurasidone, aripiprazole and asenapine. Like many other atypical antipsychotics, this action is probably due to its action on histamine receptors H 1 and 5-HT2C receptors.
- Rare side effects (& lt; 1%)
- Neuroleptic malignant syndrome is a rare and potentially fatal complication of antipsychotic drugs. It is characterized by the following symptoms: tremor, rigidity, hyperthermia, tachycardia, altered mental status (eg confusion), etc.
- Tardive Dyskinesia. Rare and often irreversible neurological conditions are characterized by unconscious movements of the face, tongue, lips and the rest of the body. Most commonly occurs after prolonged treatment with antipsychotics. It is believed to be very rare with atypical antipsychotics, especially quetiapine and clozapine
Typical and atypical antipsychotics can cause tardive dyskinesia. According to one study, the rate was lower with atypicals 3.9% compared with typical at 5.5%. Although quetiapine and clozapine are atypical antipsychotics, switching to atypical is an option to minimize the symptoms of tardive dyskinesia caused by other atypicals.
Weight gain can be a problem for some people, with quetiapine causes an increase in body weight over fluphenazine, haloperidol, loxapine, molindone, olanzapine, pimozide, risperidone, thioridazine, thiothixene, trifluoperazine, and ziprasidone, but less than chlorpromazine, clozapine, perphenazine, and sertindole..
Studies conducted on beagles have resulted in the formation of cataracts. Despite reports of cataracts that occur in humans, controlled studies including thousands of patients have not shown a clear causal link between quetiapine therapy and these side effects. However, the Seroquel site still recommends users to perform an eye exam every six months.
Like some other anti-psychotic, quetiapine can lower the seizure threshold, and should be taken with caution in combination with drugs such as bupropion.
Termination and withdrawal
Quetiapine should be stopped gradually, with careful consideration from the prescribing physician, to avoid withdrawal symptoms or relapse.
The British National Formulary recommends gradual withdrawal when stopping anti-psychotic treatment to avoid acute withdrawal syndrome or rapid relapse. Due to changes in compensation in dopamine, serotonin, adrenergic and histamine receptors in the central nervous system, withdrawal symptoms may occur during sudden or over-rapid dose reduction. However, despite an increase in demand for safe and effective antipsychotic withdrawal protocols or dose-reduction schedules, no specific guidelines with proven safety and efficacy are currently available.
The reported withdrawal symptoms occur after antipsychotic stops include nausea, vomiting, dizziness, diaphoresis, dyskinesia, orthostatic hypotension, tachycardia, insomnia, nervousness, dizziness, headache, incessant crying, and anxiety. Some argue that additional somatic and psychiatric symptoms associated with dopaminergic super-sensitivity, including dyskinesia and acute psychosis, are a common feature of withdrawal in individuals treated with neuroleptics. Current evidence suggests that these symptoms affect a small number of susceptible individuals treated with quetiapine.
Pregnancy and lactation
The least placenta exposure to quetiapine compared with other atypical antipsychotics. The evidence is not enough to rule out any risk to the fetus but the available data suggest it is not possible to produce major fetal malformations. It is secreted in breast milk and therefore the mother given quetiapine is advised not to breastfeed.
Overdose
Most cases of acute overdose only cause sedation, hypotension, and tachycardia, but cardiac arrhythmias, coma, and death occur in adults. Serum or quetiapine plasma concentrations are usually in the range of 1-10 mg/L in overdose patients, whereas postmortem blood levels of 10-25 mg/L are generally observed in fatal cases. Non-toxic levels in postmortem blood extend to about 0.8 mg/kg, but toxic levels in postmortem blood can begin at 0.35 mg/kg.
Pharmacology
Pharmacodynamics
Quetiapine has the following pharmacological actions:
- Dopamine D 1 , D 2 , D 3 , D 4 , and D < sub> 5 receptor antagonist
- Serotonin 5-HT 1A partial agonist receptor, 5-HT 2A , 5-HT 2B , 5-HT 2C , 5-HT 3 , 5-HT 6 , and 5-HT 7 receptor antagonists, and 5-HT 1B , 5-HT 1E , and 5-HT 1F receptor ligand
- ? 1 - and? 2 receptor antagonist -adrenergik
- Histamine H 1 receptor antagonist
- Muscarinic acetylcholine receptor antagonist
This means quetiapine is a dopamine, serotonin, and adrenergic antagonist, and a potent antihistamine with some anticholinergic properties. Quetiapine binds to the serotonin receptor strongly; the drug acts as a partial agonist at the 5-HT receptor 1A . Serial PET scanning evaluating receptor D sub sub> 2 has shown that quetiapine is rapidly separated from D 2 receptors. Theoretically, it allows for normal dopamine physiological spikes to produce normal effects in areas such as the nigrostriatal and tuberoinfundibular pathways, thus minimizing the risk of side effects such as pseudo-parkinsonism as well as prolactin enhancement. Some antagonist receptors (serotonin, norepinephrine) are actually autoreptor-blockers that tend to increase the release of neurotransmitters.
At very low doses, quetiapine acts primarily as a histamine receptor blocker (antihistamine) and? 1 -adrenergic blocker. When the dose is increased, quetiapine activates the adrenergic system and binds strongly with serotonin receptors and autoreceptors. At high doses, quetiapine begins to block significant amounts of dopamine receptors. Unlabeled recipe, e.g. for chronic insomnia, low doses of quetiapine is not recommended because of dangerous side effects.
Pharmacokinetics
The main active metabolite of quetiapine is norquetiapine ( N -desalkylquetiapine).
Chemistry
Quetiapine is a tetracyclic compound and is closely related structurally with clozapine, olanzapine, loxapine, and other tetracyclic antipsychotics.
Synthesis
Quetiapine synthesis begins with dibenzothiazepinone. The lactam was first treated with phosphoryl chloride to produce dibenzothiazepine. Substitution of nucleophilic is used to introduce sidechain.
History
Sustained-release
AstraZeneca proposed a new drug application for a sustainable quetiapine version in the United States, Canada and the European Union in the second half of 2006 for the treatment of schizophrenia. AstraZeneca will retain the exclusive right to market the ongoing quetiapine release until 2017. The ongoing Quetiapine release is marketed primarily as Seroquel XR. Other marketing names are Seroquel Prolong, Seroquel Depot, and Seroquel XL
On May 18, 2007, AstraZeneca announced that the US FDA approved Seroquel XR for the acute treatment of schizophrenia. During the 2007 Q2 revenue conference, AstraZeneca announced plans to launch Seroquel XR in the US during August 2007. However, Seroquel XR has been available in US pharmacies only after FDA Seroquel XR approval for use as maintenance care for schizophrenia, in addition to acute disease treatment, on 16 November 2007. The company has not provided a reason to delay the launch of Seroquel XR.
Health Canada approved the sale of Seroquel XR on September 27, 2007.
The FDA approved Seroquel XR for the treatment of bipolar and bipolar mania depression in early October 2008. According to AstraZeneca, Seroquel XR is "the first drug approved by the FDA for the once-daily acute treatment of both bipolar and depression episodes."
On July 31, 2008, Handa Pharmaceuticals, based in Fremont, California, announced that a new, abbreviated drug application ("YOU") for the extended-release quetiapine fumarate tablet, a generic version of AstraZeneca SEROQUEL XR, was received by the FDA.
On December 1, 2008, Biovail announced that the FDA has accepted YOUR company to market its continuing quetiapine version. The ongoing Biovail release tablet will compete with AstraZeneca's Servoquel XR.
On December 24, 2008, AstraZeneca told shareholders that the FDA has requested additional information about the company's applications to expand the use of continuous release quetiapine for the treatment of depression.
Society and culture
Regulatory status
In the United States, the Food and Drug Administration (FDA) has approved quetiapine for the treatment of schizophrenia and episodes of acute beads associated with bipolar disorder (bipolar mania) and for the treatment of bipolar depression. In 2009, quetiapine XR was approved as adjuvant treatment for major depressive disorder.
Quetiapine received preliminary indications from the US FDA for the treatment of schizophrenia in 1997. In 2004, Quetiapine received a second indication for the treatment of bipolar disorder-related mania. In 2007 and 2008, studies were conducted on the efficacy of quetiapine in treating generalized anxiety disorders and severe depression.
Cost
In the United States by 2015, the extended release of branded 400 mg pills costs between US $ 9.68 and US $ 23.16 respectively.
Several lawsuits have been filed related to quetiapine side effects, in particular, diabetes.
Around 10,000 lawsuits have been filed against AstraZeneca alleging that quetiapine causes problems ranging from slurred speech and chronic insomnia to death.
Controversy
In 2004, a young man named Dan Markingson committed suicide in a controversial Seroquel clinical trial at the University of Minnesota when under an unintentional commitment commitment. A group of University of Minnesota bioethics experts alleged that the trial involved a number of worrisome ethical violations.
Nurofen Plus Destroyer
In August 2011, the UK's Agency for Medicines and Healthcare (MHRA) issued a 4th-grade warning after reports that some Nurofen plus groups contain Seroquel XL instead.
Following the issue of the 4th Class Remedy, Reckitt Benckiser (UK) Ltd received further reports on the naughty blister strip in a two additional carton of Nurofen Plus tablet. One of the new batches contains Seroquel XL 50 mg tablet and one contains Pfizer Neurontin 100 mg capsule product.
After discussing with the MHRA Disabled Medicines Research Center (DMRC), Reckitt Benckiser (UK) Ltd decided to recall any remaining remaining Nurofen Plus tablets in any packaging size, leading to a Class-1 Drug Warning. Contamination is then traced to customer disruptions at the store.
src: i.ytimg.com
References
src: www.buy-pharma.md
External links
- "Quetiapine". MedlinePlus . American Society of Health-System Pharmacists, Inc. 2008-09-01.
- NAMI Summary
- Internet Drug List Summary
- Compound # 1802: Quetiapine ChemBank
- US. National Drug Library: Drug Information Portal - Quetiapine
- Australian Public Assessment Report for Quetiapine (like fumarate)
Source of the article : Wikipedia
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