Insopin
Insopin Uses, Dosage, Side Effects, Food Interaction and all others data.
Insopin is a cyclopyrrolone derivative with hypnotic and sedative actions, anticonvulsant and muscle relaxant properties similar to benzodiazepines. It binds to a site in the GABA-A-benzodiazepine-chloride channel macromolecular-receptor complex which is different from that of the benzodiazepine binding site.
Insopin is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class and is indicated for the short-term treatment of insomnia. While Insopin is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Insopin binds selectively to the brain alpha subunit of the GABA A omega-1 receptor.
| Trade Name | Insopin |
| Generic | Zopiclone |
| Zopiclone Other Names | Zopiclona, Zopiclone, Zopiclonum |
| Type | |
| Formula | C17H17ClN6O3 |
| Weight | Average: 388.808 Monoisotopic: 388.105066147 |
| Protein binding | Approximately 45% |
| Groups | Approved |
| Therapeutic Class | Miscellaneous sedatives & hypnotics |
| Manufacturer | |
| Available Country | Malaysia, Taiwan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Insomnia and sleep disturbances
Insopin is also used to associated treatment for these conditions: Insomnia
How Insopin works
Insopin exerts its action by binding on the benzodiazepine receptor complex and modulation of the GABABZ receptor chloride channel macromolecular complex. Both zopiclone and benzodiazepines act indiscriminately at the benzodiazepine binding site on α1, α2, α3 and α5 GABAA containing receptors as full agonists causing an enhancement of the inhibitory actions of GABA to produce the therapeutic (hypnotic and anxiolytic) and adverse effects of zopiclone.
Dosage
Insopin dosage
Oral (Short-term management of insomnia):
- Adult: 7.5 mg at bedtime.
- Elderly: Initially, 3.75 mg at bedtime.
May be taken with or without food.
Side Effects
Metallic or bitter aftertaste; irritability, confusion, depressed mood, aggressiveness, incoordination, anterograde amnesia, mild increase in LFTs, drowsiness, lightheadedness, nausea, vomiting, urticaria, rashes.
Toxicity
Rare individual instances of fatal outcomes following overdose with racemic zopiclone have been reported in European postmarketing reports, most often associated with overdose with other CNS-depressant agent. Signs and symptoms of overdose effects of CNS depressants can be expected to present as exaggerations of the pharmacological effects noted in preclinical testing.
Precaution
Hepatic and renal insufficiency; elderly; psychiatric disorders; history of drug abuse. May impair ability to drive or operate machinery. Limit treatment duration to <4 wk to minimise risk of dependence and tolerance. Avoid abrupt discontinuation of therapy.
Interaction
Reduced hypnotic effect with phenytoin and carbamazepine. Increased drowsiness and incoordination with TCAs. Increased CNS depressant effect with alcohol and other CNS depressants. Decreased zopiclone concentration with rifampicin. Possible increase in zopiclone concentration with CYP3A4 inhibitors e.g. erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir.
Food Interaction
- Avoid alcohol. Ingesting alcohol may potentiate the CNS depressant actions of zopiclone.
- Avoid grapefruit products. Grapefruit may reduce the CYP3A4 metabolism of zopiclone, increasing its sedative effects.
Elimination Route
Rapidly absorbed following oral administration.
Half Life
Elimination half life is approximately 5 hours (range 3.8 to 6.5 hours) and is prolonged to 11.9 hours in patients with hepatic insufficiency.
Pregnancy & Breastfeeding use
Pregnancy category not classified
Contraindication
Myasthenia gravis; respiratory failure; severe sleep apnoea syndrome; severe hepatic impairment; pregnancy, lactation.
Special Warning
Renal Impairment: Initiate at 3.75 mg at bedtime.Hepatic Impairment: Mild to moderate: Initially 3.75 mg at bedtime. Severe: Contraindicated.
Acute Overdose
Symptoms: CNS depression ranging from drowsiness to coma depending on ingested amount. In mild cases, there may be drowsiness, confusion, and lethargy while in more serious cases, there may be ataxia, hypotonia, hypotension, respiratory depression and coma. Management: Treatment is symptomatic and supportive with close monitoring of the respiratory and CV functions. Gastric lavage is only of value if performed within 1 hr after ingestion. Haemodialysis is unlikely to be useful. Flumazenil may be a useful antidote in severe CNS depression.
Interaction with other Medicine
Store in a dry place below 30° C. Protect from light.
Innovators Monograph
You find simplified version here Insopin
Insopin contains Zopiclone see full prescribing information from innovator Insopin Monograph, Insopin MSDS, Insopin FDA label
FAQ
What is Insopin prescribed for?
Insopin is a type of sleeping pill that can be taken to treat bad bouts of insomnia. It helps you fall asleep more quickly, and also helps stop you waking up during the night.
How long will I sleep with Insopin?
Drowsiness can last for at least 11 hours after taking your dose.Extra care is needed when taking zopiclone because it can cause sleepiness and affect your concentration the next day.
Is Insopin good for anxiety?
Insopin reduces day time anxiety.
Can I take Insopin every night?
Insopin should be taken at the lowest dose possible for the shortest possible time. You may agree with your doctor not to take it every night, but perhaps every other night (alternate nights).So you do not get into the habit of taking it. You should take Insopin just before going to bed.
Do Insopin get me high?
Insopin can produce a euphoric effect when taken in large doses, it can be combined with other drugs to increase the effects.
Is Insopin good for depression?
As with other hypnotics,Insopin does not constitute a treatment for depression and may even mask its symptoms (suicide may be precipitated in such patients). Any underlying cause of the insomnia should be also addressed before symptomatic treatment to avoid under treating potentially serious effects of depression.
Does Insopin calm me down?
When taking Insopin you quiet your whole brain's activity level. This reduces anxiety and insomnia, but also causes changes to many of the body's essential systems.
What are the side effects of long term use of Insopin?
Over the long term,Insopin abuse can result in symptoms including chest pain,heart palpitations, nightmares,amnesia,abdominal pain,constipation,sinusitis,sore throat,dry mouth,lethargy,back pain, flu-like symptoms,dizziness,and depression which can result both from the direct effects of the drug upon the addict’s life prospects, self-esteem, and general outlook.
Can Insopin make me happy?
Insopin are initially prescribed to help with sleeping. It can hasten sleep onset by 15 minutes and induces a euphoric dream-like state.
What does Insopin do to the brain?
The brain naturally releases calming chemicals. One of these chemicals is called gamma-aminobutyric acid. Insopin works by boosting the effects of GABA and this helps to calm the brain, enabling you to get to sleep.
Can Insopin cause brain damage?
Studies have shown that Insopin has not been associated with significant morning-after memory loss. Although several cases of 'potentially serious' memory loss events have recently been reported in the United Kingdom, details of these cases are lacking.
Does Insopin affect my memory?
Insopin may cause a special type of memory loss (amnesia).You may not recall events that occurred during some period of time, usually several hours, after taking the drug.
Is Insopin safe long term?
Insopin and some benzodiazepines, such as temazepam and triazolam, are indicated for the short-term treatment of insomnia (four weeks or less). Long-term use of these medicines should be avoided where possible due to adverse effects and the potential for the development of dependence.
Is Insopin hard on the liver?
Liver disease or reduced liver function may cause this medication to build up in the body, causing side effects. If you have liver problems, you may require lower doses of this medication.
Can Insopin cause stroke?
The use of Insopin at ≥ 7.5 mg or equivalent is associated with absolute annual risks of stroke of 8.1% (compared to 4.4% in the sleep disturbance cohort).
Is Insopin safe for kidneys?
Hemodialysis of the severely ill renal patients did not increase the plasma clearance of Insopin. Finally, only small amounts of drug were found in urine in the three groups. Overall, results allow the conclusion that Insopin may be safely used in patients with various degrees of renal impairment.
What drugs interact with Insopin?
There may be an interaction between Insopin and any of the following:
- alcohol.
- anti-anxiety medications (e.g., alprazolam, clonazepam, lorazepam)
- anticonvulsants (medications used to prevent seizures; e.g., phenytoin, valproic acid, carbamazepine, gabapentin)
Does Insopin cause confusion?
Confusion, lack of coordination, and falling are more likely to occur in the elderly, who are usually more sensitive than younger adults to the effects of Insopin.
Who should not take Insopin?
Do not take Insopin if you're pregnant, as it may harm the developing baby. It can also cause side effects in newborn babies. There's some evidence that taking Insopin can increase your risk of having a baby born early (before 37 weeks) and the baby having a lower birth weight.
Can I take Insopin occasionally?
Insopin is intended for occasional use in adults at a dose of 7.5 mg orally shortly before bedtime. It should not be used for more than four weeks. The initial dose should be reduced in older people.
Is it safe to take two Insopin?
Insopin is usual to be prescribed one tablet (7.5 mg) to be taken just before going to bed. Do not take more than one dose during a single night.
