Temazepam (Restoril)

Benzodiazepines are a gathering of medications that lull the focal sensory system and abatement neuronal excitement

Although there are different types, these drugs are used primarily as anxiolytics, hypnotics, and muscle relaxants. Temazepam is kind of  benzodiazepine used to help you nod off and diminish evening time renewals.

What is insomnia?

is an issue that comprises the capability to nod off or to keep it. It can also manifest itself through multiple awakenings throughout the night or an early morning awakening. The outcome is low quality of rest and inadequate rest.

This disorder significantly affects the quality of life and its most immediate consequences are daytime sleepiness, low concentration and the inability to maintain an active life. In the long term it can favor the development of various diseases. In fact, it is estimated that the risk of mortality increases significantly in those who sleep less than 6 hours a day.

Types of insomnia:

Onset insomnia: inconvenience beginning snooze under 30 minutes.

Maintenance insomnia: Problems to maintain sleep, producing nocturnal awakenings of more than 30 minutes in duration, or definitely waking up early, achieving a short total sleep time.

Causes of insomnia

Physiological changes: maturing produces changes in the rest design. In older people, a reduction in the hours and quality of sleep and an increase in daytime sleepiness are frequent.

Lifestyle: constant schedule changes, either due to work or travel reasons (jet-lag) cause circadian rhythm disorders.

Drugs: Among the drugs and substances that can alter sleep are antihypertensives, anticholinergics, hormones, stimulants, steroids, antidepressants, bronchodilators, decongestants, antineoplastics, caffeine and levodopa.

Insomnia symptoms are not difficult to distinguish, as the patient himself sees troubles in nodding off or gets up right away. Lack of rest manifests itself throughout the day causing fatigue, weakness and, in extreme cases, even slowness when processing information, irritability

Main uses

Temazepam is a drug from the group of benzodiazepines used primarily in the treatment of insomnia and severe or disabling sleep disorders. This drug is also used in anxiety disorders, since in addition to having hypnotic effects, it exerts an anxiolytic and sedative action.

Treatment of narcolepsy:

Adults: Doses of 15 to 30 mg temazepam given at bedtime have been used to reduce the number of narcoleptic episodes. Temazepam reduced the frequency of cataplexy and the ESS index (Epworth Sleepiness Scale) was reduced from 16.4 to 11.6

Treatment of anxiety:

Adults: the recommended doses are 5 mg / 8-12 h, the daily dose can be increased, depending on the response.

clinical, up to a maximum of 10 mg / 8-12 h (30 mg / day).

Elderly and debilitated patients: 5 mg / 12 h, up to a maximum of 5 mg / 8 h (15 mg / day).

Short-term treatment of insomnia:

Treatments longer than two or three weeks should be avoided, suggesting intermittent use of the drug during this period.

Adults: 15-30 mg / 24 h is recommended at bedtime.

Elderly and debilitated patients: 15 mg / 24 h.

Abuse

Benzodiazepines have been abused orally and intravenously Various benzodiazepines have diverse maltreatment potential; the more fast the expansion in the plasma level after ingestion, the more noteworthy the intoxication impact and the more open to abuse the drug becomes. The speed of the beginning of activity of a specific benzodiazepine corresponds well with the 'notoriety' of that medication for abuse. The two most regular explanations behind inclination were that a benzodiazepine was 'solid' and that it gave a decent 'high'.

A recent report found that temazepam is all the more quickly ingested and oxazepam is more gradually retained than most different benzodiazepines.

Another study found that temazepam and triazolam kept up funda. All test subjects reliably showed a solid inclination for temazepam and triazolam over the remainder of the benzodiazepines remembered for the investigation.

Background and history

This compound, Temazepam was synthesized in 1962 and was patented in 1964, and marketed for medical use in 1969 under the name "Restoril." But it came into use in 1981 when its ability to counter insomnia was realized. In In 1982 it was endorsed by the Food and Drug Administration (FDA). By the last part of the 1980s, temazepam was quite possibly the most mainstream and generally endorsed hypnotics available and it got perhaps the most broadly recommended drugs. Right now there are a few pharmaceutical companies assembling it in its generic form.

In North America, temazepam misuse is not widespread. Other benzodiazepines are more commonly prescribed for insomnia. In the United States, temazepam is the fifth-most recommended benzodiazepine, anyway there is a significant drop off from the best four generally endorsed (clonazepam, lorazepam, diazepam, and alprazolam)

People manhandling benzodiazepines get the medication by getting medicines from several specialists, manufacturing prescriptions, or purchasing redirected drug items on the unlawful market. North America has never had a major issue with temazepam abuse, but is becoming increasingly helpless against the illegal exchange of temazepam.

In the United States, Temazepam is presently a Schedule IV medication unJder the ICPS of 1971 and is only available by prescription. Specially coded prescriptions might be needed in specific states.

Mechanisms of action

Temazepam, in the same way as other comparative benzodiazepines, goes about as a modulator of gamma-aminobutyric corrosive (GABA) and is capable of causing an assortment of effects including: sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, and anxiolytic action.

GABA is considered the main inhibitory neurotransmitter in the human body. At the point when this synapse ties to GABAA receptors found at neuronal neurotransmitters, chloride particles are directed through the cell membranes of neurons through a particle channel at the receptors. With sufficient chloride ions, the membrane potentials of associated local neurons hyperpolarize, making it more difficult or less likely for action potentials to fire, resulting in less excitation of neurons.

Albeit the primary pharmacological movement of temazepam is to increase the effect of the neurotransmitter GABA, in animal studies (explicitly, in rodents) it has additionally been shown that the medication triggers the release of vasopressin in the paraventricular nucleus of the hypothalamus and diminishes the arrival of the adrenocorticotropic hormone under pressure conditions.

Characteristics

The pharmacokinetic properties of hypnotics are related to the ease and speed of absorption, distribution and elimination and with possible interactions with other drugs or substances in the body.

Regarding absorption, it is absorbed through the gastrointestinal tract without undergoing previous transformations. Once absorbed, the time it takes to reach the plasma peak ranges from 1 to 3 hours.

Zolpidem is one of the benzodiazepine analogues that does not have muscle relaxant properties, that is, it does not relax the muscles. For this reason, its main use is in sleep disorders such as insomnia.

With regard to disposal, from a practical point of view, benzodiazepines and new hypnotic families are classified according to their elimination half-life (the time it takes to decrease 50% plasma concentration) in the case of temazepam, the half-life is 8 to 12 hours and it does not has active metabolites.

Zolpidem

Zolpidem is one of the benzodiazepine analogues that does not have muscle relaxant properties, that is, it does not relax the muscles. For this reason, its main use is in sleep disorders such as insomnia.

Flurazepam

Flurazepam is a drug from the group of benzodiazepines that acts on the central nervous system. It has hypnotic properties and is one of the longest-lived benzodiazepines in plasma (the half-life reaches 250 hours). Treatment with this drug should be short-term, since it produces dependence and tolerance.

It is metabolized in the liver and its elimination is renal. It is generally prescribed in cases of insomnia and sleep rhythm disorders of considerable severity and to treat emergencies for short periods

Adverse Reactions

The adverse effects of temazepam are, in general, frequent and moderately important. The toxicological profile of this drug is similar to that of the other anxiolytic benzodiazepines. In most cases, adverse reactions are a prolongation of pharmacological action and mainly affect the central nervous system. 50% of patients experience transient drowsiness during the first days of treatment. Rarely are patients treated with this medicine forced to stop treatment.

The most characteristic adverse reactions are:

-Very common (> 25%):

drowsiness, confusion and ataxia, especially in the elderly and debilitated; if these symptoms persist, the dose should be reduced.

-Common (10-25%):

dizziness, sedation, headache, depression, disorientation, dysphasia or dysarthria, reduced concentration, tremor, changes in libido, urinary incontinence, urinary retention, nausea, vomiting, diarrhea, constipation, dryness mouth, hypersalivation, epigastric pain.

-Uncommon (1-9%):

hepatitis, jaundice, dermatitis, urticaria, pruritus, leukopenia, agranulocytosis, anemia, thrombocytopenia, eosinophilia, behavioral disturbances, anterograde amnesia, paradoxical excitement, psychosis, vision disturbances, diplopia, nystagmus , hearing disorders.

-Rare:

hypertension, bradycardia, tachycardia, palpitations.

Interactions

Cimetidine enhances the effect of temazepam. A case of temazepam toxicity caused by the administration of disulfiram has been described. Other benzodiazepines do not appear to interact with temazepam.

Temazepam can inhibit the effect of levodopa. Valproium acid may potentiate the toxicity of temazepam. Alcohol and all drugs that cause central nervous system depression can have additive effects with temazepam.

Tolerance

As with other benzodiazepines, taking this medicine (particularly if taken for a long time) can lead to tolerance to the effects of the medicine. This is manifested by a decrease in the effects of temazepam. If you notice that the medicine does not work the same way as in the beginning, consult your doctor.

Contraindications and precautions

Temazepam is contraindicated in patients with an allergy to benzodiazepines, as well as in patients with myasthenia gravis, coma or shock, acute alcohol poisoning, pregnant patients (especially during the first and third trimesters), nursing mothers and children (lack of clinical experience) .

Sleep disorders can be the manifestation of a disorder of an underlying physical and / or psychiatric illness. Therefore, a choice to start symptomatic treatment of insomnia ought to just be made after the patient has been painstakingly evaluated. Insomnia failure to remit after 7 to 10 days of treatment may indicate the presence of a primary psychiatric medical condition that should be evaluated.

Worsening insomnia may be the consequence of an unrecognized psychiatric or physical disorder as well as the appearance of new abnormalities of thinking or behavior. Such irregularities have likewise been accounted for to happen in relationship with the utilization of medications with central nervous system depressant activity, including those of the benzodiazepine class.

Because some of the most serious adverse effects of benzodiazepines, including temazepam, appear to be dose related, it is important to use the lowest effective dose possible. Elderly patients are especially at risk.

Can I take Temazepan if I am pregnant?

Temazepam is classified within category X of risk in pregnancy. Benzodiazepines can cause fetal damage when administered to a pregnant lady.. An increased risk of birth defects associated with the use of diazepam and chlordiazepoxide has been observed during the first trimester of pregnancy.

Transplacental distribution has resulted in neonatal CNS depression after ingestion of therapeutic doses of a hypnotic benzodiazepine during the last weeks of pregnancy.

Can I take Temazepan if I am breastfeeding?

Temazepam reaches a low level in the blood, also having a relatively short half-life. Both circumstances make the amounts of the drug ingested by the baby small, therefore, assuming a rather remote risk for the infant at the usual doses of use.

The amount received by the baby can even be minimized by taking the drug immediately after the feed that precedes the child's longest sleep period, which usually happens at night. However, it is suggested not to take benzodiazepines if you are breastfeeding.

How quickly does treatment work?

Restoril is really quick, generally, temazepam takes no more than 20 minutes to help you fall asleep. However, your sleeping problems should improve considerably within 7 to 10 days after you start taking this medicine. If after a week of using it, you do not notice improvement, you should consult your doctor.

Is it safe to take Temazepam?

Despite the fact that temazepam is a moderately protected and compelling medication, its utilization that builds tolerance to its hypnotic and anxiolytic effects, which makes the dosage be expanded.

Prescribing guidelines typically limit the use of these types of medications to two to four weeks, due to tolerance and dependency issues.

How long does a dose of Temazepam last?

Consumption of restoril is expected to sustain 6 to 8 hours of uninterrupted sleep. Although the half-life of temazepam in the body is about two and a half hours, its extended release presentations favor the maintenance of sleep throughout the night.

Are there any side effects of the treatment?

Yes, the most frequent side effects of zolpidem, are the following:

• Daytime sleepiness or a "hangover" feeling
• Headache
• Dizziness, tiredness
• Nausea
• Feeling nervous

Do I require a prescription for taking Temazepam?

Temazepam belongs to a class of medications called benzodiazepines. It works by slowing activity in the brain to allow you to sleep easily. So yes, temazepam is only available with prescriptions.

Why is it not safe to buy Temazepam online?

Buying drugs online may be dangerous, first, for using Restoril, you need a prescription, it means that a doctor should examine you before prescribing any drugs, because not everybody is able to use this drug.

On the other hand, there is the risk of buying drugs from unknown origin when you are buying medication online. We recommend not to take unnecessary risks.

Is this treatment option safe for children and ederly?

This medication ought not be taken by youngsters to treat rest problems.

It is advisable to use lower doses in patients 65 years of age or older, due to the slower elimination of the drug.

How long do I have to take Temazepam for?

Temazepam is a drug that must be used for short periods of time, that is, for less than four weeks, since it has been shown that its use for longer periods of time is capable of creating addiction and dependence.

Can I take Temazepam with other medications?

You should avoid taking zolpidem at the same time as any of the following medications:

• Cimetidine
• Valproic acid
• Levodopa
• Alcohol

Does Temazepam create tolerance?

As with other benzodiazepines, taking this medicine (particularly if taken for a long time) can lead to tolerance to the effects of the medicine. This is manifested by a decrease in the effects of temazepam. If you notice that the medicine does not work the same way as in the beginning, consult your doctor.

Who shouldn’t take Temazepam?

Temazepam is contraindicated in patients with an allergy to benzodiazepines, as well as in patients with myasthenia gravis, coma or shock, acute alcohol poisoning, pregnant patients (especially during the first and third trimesters), nursing mothers and children (lack of clinical experience).

Does Temazepam cause dependence?

This medicine can lead to dependence, so it should be used for the shortest possible time. The risk is also more important in patients who have a history of alcohol dependence or drug addiction.