Temazepam for Insomnia - A Sleep Rescuer

Overview:

Temazepam is a medication of the class benzodiazepines that is generally prescribed to treat severe or debilitating forms of insomnia. Temazepam is officially indicated for insomnia and certain other severe and disabling sleep disorders. This medication is taken orally. This drug is rapidly and well absorbed, instituting significant hypnotic effects in less than thirty minutes while lasting up to a period of eight hours.

Drug Group:

Benzodiazepines are a class of psychoactive drugs that typically act as central nervous system (CNS) depressants. These drugs are prescribed for a range of medical illnesses, including insomnia, anxiety, muscle spasms, and seizures. These medications function by enhancing the effects of the neurotransmitter called gamma-aminobutyric acid (GABA), which generally has a calming influence on the brain.

Available Doses and Dosage Forms:

Forms:

• Capsule.

• Schedule intravenous (IV) administration.

Strengths:

• 7.5 milligrams.

• 15 milligrams.

• 22.5 milligrams.

• 30 milligrams.

For Patients

What Is Insomnia?

Insomnia is typically a sleep disorder manifested by difficulty in falling asleep, staying asleep, and experiencing non-restorative sleep, resulting in daytime fatigue and impaired daily functioning. This condition can be transient or chronic, potentially resulting from a range of factors like stress, underlying medical conditions, and lifestyle choices. The symptoms associated with insomnia include the following.

• Trouble falling and staying asleep.

• Non-restorative sleep.

• Fatigue and sleepiness during daytime.

• Tension headaches.

• Gastrointestinal issues like constipation.

• Difficulty common concentration.

• Irritability.

• Mood disturbances.

How Does Temazepam Work?

Temazepam is prescribed for the treatment of insomnia on a short-term basis, generally seven to ten days. Insomnia is a profound condition referring to trouble in falling asleep or remaining asleep. Temazepam belongs to a group of pharmacological drugs called benzodiazepines. This drug functions by reducing or slowing the activities that take part in the brain, allowing one to sleep. Benzodiazepines, in turn, belong to the group of medications known as central nervous system (CNS) depressants. These are agents that slow down or hinder the nervous system.

How Effective Is Temazepam?

Temazepam is often effective in the treatment of insomnia, predominantly by helping with sleep initiation. It belongs to a drug class called benzodiazepines and possesses sedative properties that could promote sleep and relaxation. Nevertheless, its efficacy can vary from person to person, and it is to be used under the supervision of a healthcare provider. Moreover, Temazepam is generally recommended for a brief period due to the risk of dependency and potential side effects.

Things to Inform the Doctor Before Taking Temazepam:

• One must inform the doctor in the case of allergy or hypersensitivity to Temazepam, any other drug belonging to the benzodiazepines class, any ingredients of the given formulation, or other medications in general.

• Inform the doctor about the medication one takes or is about to take in the succeeding days. This includes prescription drugs, non-prescription medications, vitamins, herbal products, and nutritional supplements.

• Be certain to mention any of the drugs, including antihistamines (Digoxin, Diphenhydramine), antidepressants, anxiety medications, medicines for mental illness, anti-seizure drugs, sedatives, tranquilizers, and sleeping pills. The healthcare providers might change the dosage of the drug Temazepam or monitor conscientiously for side effects.

• Inform the doctor if one has or ever had suicidal thoughts or attempted any time before. The presence of such a tendency could affect seizures, breathing status, and kidney or liver functions.

• Inform the doctor if one is pregnant or has any plans in the future. One should not take Temazepam medication during pregnancy since it is known to harm the fetus (unborn child). Call and tell the doctor rightly if one becomes pregnant while on Temazepam short-term treatment.

• Addedly, women who are under lactation should be informed. This drug is likely to affect the infant. The doctors might prescribe an alternative drug, outweighing the potential benefits and risks.

How Is Temazepam Administered?

• Temazepam comes in capsule form and can be taken by mouth.

• This medication is generally taken as needed during bedtime.

• It is vital to follow the healthcare provider's directions and manufacturers' labeled guidelines.

• Take Temazepam medication exactly as per the directions.

• One should not take more or less than the prescribed frequency.

• This medication will probably make one sleep soon after one takes the medication, remaining sleepy for some time after it is taken.

• Hence, plan accordingly, go to bed straight after the oral administration of Temazepam medication, and stay in bed for seven to eight hours.

• Swallow the capsule with water.

• Do not chew, crush, or break them.

What Are the Side Effects of Temazepam?

Temazepam is a safe drug used to treat insomnia for a short period that helps with the relief by sleep Onset. Like any other medication, Temazepam also possesses certain side effects or undesirable reactions.

Common Side Effects:

The following common side effects are less severe, while they don’t generally require medical attention. However, report to the doctor if such symptoms are not resolving on their own, influencing the daily function.

• Daytime hangover feeling.

• Dizziness.

• Drowsiness.

• Euphoria.

• Diarrhea.

• Weakness.

• Confusion.

• Lethargy.

• Vertigo (spinning sensation).

Serious Side Effects:

Allergic reactions can occur with the drug Temazepam, resulting in hives, rashes, breathing problems, and swelling of the face and throat. In that case, it is crucial to report to the doctor and get prompt medical care. The other serious side effects that require medical attention include the following.

• Nausea.

• Vomiting.

• Shallow breathing.

• Agitation.

• Confusion.

• Difficulty waking up after sleep.

• Hallucinations.

• Depressed mood.

• Break during breathing.

• Self-harm thoughts.

• Suicidal tendencies.

• Activities of eating, driving, having sex, and making phone calls with no memory of the activity.

The following serious side effects have also been reported with Temazepam therapy. Seek medical care or emergency services if one experiences them.

• Severe headache, slurred speech, confusion, difficulty walking, unsteadiness, stiffened muscles, loss of coordination, weakness in extremities, profound sweating, high fever, or tremors.

• Serious eye symptoms include blurred vision, tunnel vision, abrupt vision impairment, eye pain, or feeling halos around the lights.

• Serious symptoms associated with the heart include irregular, rapid, or profound heartbeats, shortness of breath, fluttering in the chest, abrupt dizziness, and lightheadedness.

Dietary Considerations: It is generally recommended to follow the routine classic diet while on Temazepam treatment. However, it is strictly advised to avoid alcohol intake during this period. Temazepam with alcohol intake can result in potentially dangerous side effects and sometimes be fatal.

Missed Dose

Temazepam is usually given on a short-term basis, potentially seven to ten days. This medication is usually prescribed to take during bedtime. If one misses the Temazepam dosage at bedtime and cannot fall asleep, one might take the dosage if one can remain in the home or bed for another seven to eight hours. On the contrary, one can leave the forgotten dosage and continue with the next day's bedtime, sticking to the regular schedule. However, one should not take Temazepam if one is not ready to sleep straight away or stay asleep for a minimum of seven to eight hours.

Overdose

Reach out to the emergency medical services or poison control helpline straight away, in case of an overdose of Temazepam. The symptoms of overdose manifest as drowsiness, fainting, confusion, loss of consciousness, dizziness, collapse, and difficulty breathing. An overdose of the drug Temazepam is considered fatal when one takes it with opioid medicine, alcohol, and certain other drugs that induce drowsiness and shortness of breath.

Storage

• Keep the Temazepam medications in a firmly packed container and out of the reach of younger children.

• It is vital to store the medication at room temperature and away from excessive moisture and heat.

Disposal

Unused and expired medications should be disposed of in a specific manner to ensure that children, pets, and neighbors cannot reach them. It is unacceptable to flush the medication in the toilet or throw it in the trash. In contrast, the optimal way to dispose of the medicine is by means of a take-back program. Discuss with the pharmacist about this.

For Doctors:

Indication:

Temazepam is typically indicated for the short-period management of insomnia. This management is substantially associated with the symptomatic cure of transient and short-term forms of insomnia that is characterized by difficulty falling asleep and constant awakening during morning or night. Specifically, Temazepam's official prescribing information accentuates the instructions given for the dispensed prescription of the medicine, which should indicate that the individuals are only supposed to use the treatment for a short time, generally for seven to ten days and not exceeding that. Hence, the Temazepam treatment should neither overdo seven to ten consecutive days nor be prescribed in large quantities beyond a month of supply.

Temazepam can sometimes be used as premedication before certain minor surgical interventions and other associated procedures.

Dose:

Adults:

• The recommended dosage of Temazepam for the brief-term management of insomnia in adults is 15 to 30 milligrams orally every night during bedtime.

• The recommended dosage for debilitated patients is 7.5 milligrams orally during bedtime.

• Abrupt discontinuation should be avoided if extended therapy is required. On the contrary, consider gradual tapering of the dosage.

Geriatrics:

• The recommended dosage of Temazepam for short-term insomnia relief is 7.5 milligrams orally once during bedtime.

• The usage of Temazepam in geriatrics should be limited to 10 to 14 days.

• However, Temazepam is the most preferred drug in elderly people when there is an indication of benzodiazepine due to a lack of active metabolite.

Dosing Considerations:

• The drug Temazepam is not indicated for use in the pediatric population.

• For discontinuation, taper the dosage slowly following extensive Temazepam treatment. Abrupt cessation of the treatment should be avoided.

What Are the Pharmacological Aspects of Temazepam?

Mechanism of Action:

Gamma-aminobutyric (GABA) is regarded as the chief inhibitory neurotransmitter in the body. GABA usually binds to GABA (a) receptors in the neuron synapses, resulting in the conduction of chloride ions across the neuron by means of an ion channel in the receptor. When adequate chloride ions are conducted, the local and the associated neuron membrane potentials get hyperpolarized. This makes it more challenging or less potential for action potentials to activate, leading to less excitation of the neurons.

In the same manner, benzodiazepines, including Temazepam, could bind to the components of certain varieties of GABA (a) receptors called the benzodiazepine receptors. This binding promotes the effect of gamma-aminobutyric acid by reducing and enhancing the GABA affinity towards the GABA (a) receptor, which ultimately improves the GABA ligand binding potential at the receptors. The augmented ligand binding concerning the inhibitory neurotransmitter of GABA to its receptors raises the chloride ion conduction, leading to a hyperpolarized cell membrane. This prevents the subsequent excitation of the related neuron cells. There is also an impression that such benzodiazepine receptor-related GABA (a) receptors endure in the peripheral system and the central nervous system (CNS). As a consequence, this activity facilitates certain effects such as hypnosis, sedation, anticonvulsant effect, skeletal muscle relaxation, and anxiolytic action.

Pharmacokinetics

Absorption:

• The clinical findings demonstrate that about 90 to 100 percent of orally administered dosage of Temazepam is well absorbed.

• The oral administration of 15 to 45 milligrams of Temazepam has resulted in rapid and adequate absorption, with substantial blood levels achieved in 30 minutes while peak limits at two to three hours.

• The direct clinical studies revealed that the measurable plasma concentrations were attained 10 to 20 minutes after the administration, with peak plasma levels ranging between 666 to 982 ng/mL, manifesting 1.2 to 1.6 hours after the dosing.

• Hence, a dose-proportional association was determined for the area under the plasma concentration or time curve exceeding the 15 to 30 milligrams of dosing range.

Distribution:

• The volume of distribution of Temazepam was documented as 1.3 to 1.5 liters per kilogram of body weight.

• The value is 43 to 68 liters per kilogram for an unbound fraction.

• The protein binding capacity of unchanged Temazepam is about 96 percent.

Metabolism:

• The first-pass metabolism of the drug is usually minimal, accounting for about five to eight percent of the administered dosage.

• However, Temazepam is chiefly metabolized in the liver.

• Here, the most unchanged drug form gets directly conjugated into glucuronide before its elimination through urine.

• The primary metabolite of Temazepam seen in the blood is the O-conjugate form of the drug.

• About five percent of Temazepam is demethylated into Oxazepam, with the subsequent elimination as glucuronide.

• These glucuronides of the drug have no determined CNS activity, and it is known that there is no formation of active metabolites.

• As the drug Temazepam significantly undergoes phase two of conjugation reactions, it is established that the drug is devoid of CYP450 interactions.

Elimination:

• Following a single dosage of oral administration of Temazepam, 80 to 90 percent of the dosage is eliminated in the urine, mainly as the O-conjugate metabolite.

• About 3 to 31 percent of the drug is recovered in the feces.

• Less than two percent of Temazepam is recovered in unchanged or N-desmethyl temazepam form in the urine.

Half-Life and Clearance:

• The terminal half-life period of Temazepam is determined to be within 3.5 to 18 hours, with a mean value of nine hours.

• The clinical findings regarding the clearance of the drug have been recorded as 1.03 milliliters per minute per kilogram for a total clearance of the drug.

• The value is 31 milliliters per minute per kilogram for the clearance of unbound Temazepam.

Adverse Effects: Temazepam is a safe and effective medication when used for the short-term relief of insomnia and associated sleep discrepancies. Nevertheless, like any other medication, this also possesses certain adverse effects.

One to Ten Percent:

• Dizziness.

• Drowsiness.

• Lethargy.

• Diarrhea.

• Hangover.

• Euphoria.

• Confusion.

• Vertigo.

• Weakness.

Less Than One Percent:

• Amnesia.

• Blood dyscrasias (imbalance of blood cells, plasma, and vital components in the blood)

• Sleep-related behaviors like sleep eating, sleep cooking, and sleep driving.

• Ataxia (impaired balance and coordination).

What Are the Contraindications of Temazepam?

Temazepam is considered safe for many groups of people. However, certain contraindications and factors are to be considered, taking the adverse reactions into account. The potential contraindications for the drug Temazepam include the following.

• Documented history of hypersensitivity to Temazepam or other drugs belonging to the same class (benzodiazepines).

• Acute alcohol intoxication.

• Narrow-angle glaucoma. This condition is questionable, requiring extensive research studies to validate its contraindication.

• Ataxia (impaired coordination).

• Severe hypoventilation.

• Severe hepatic deficiencies, including liver cirrhosis and hepatitis.

• Sleep apnea.

• Severe degrees of renal insufficiency.

• Patients on dialysis.

• Severe depression, specifically when this condition is associated with suicidal tendencies.

• Myasthenia Gravis (an autoimmune disorder resulting in severe muscle weakness).

• Acute intoxication with narcotic drugs and several other psychoactive substances.

Warnings and Precautions:

• Use the drug Temazepam cautiously in people with sleep apnea, chronic obstructive pulmonary disease (COPD), open-angle glaucoma, hepatic disease, renal dysfunction, respiratory problems, suicidal ideation, depression, and alcoholism.

• Temazepam is known to impair the potential to reform hazardous tasks.

• It is crucial to use this drug deliberately during intravenous administration in the case of foam, shock, respiratory depression, and in individuals who are recently receiving respiratory depressant medications.

• Use of Temazepam in myasthenia gravis is recommended only in limited circumstances.

• Prescribe Temazepam with caution in people with a history of drug abuse or acute alcoholism since psychological and physical dependence is known to result from prolonged exposure.

• Anterograde amnesia might occur with Temazepam treatment.

• This drug might cause aggressive or hyperactive conduct in some cases. Paradoxical hyperactive aggressive behavior has been observed in Temazepam therapy.

• Temazepam treatment can cause drowsiness and reduced levels of consciousness in patients, especially in the elderly group. Elderly patients are more likely to have a higher risk of falls.

• Use this drug prudently in people with severe respiratory depression and depressed neuroses since it can induce psychotic reactions.

• The use of Temazepam in patients, specifically those who are at increased risk of abuse, requires comprehensive counseling regarding the risk and appropriate use of medication, along with monitoring for signs of abuse, addiction, and misuse. It is crucial to not exceed the recommended dosage frequency.

• Evade or minimize the concomitant use of Temazepam with CNS depressants and other substances associated with misuse, abuse, and addiction. This includes stimulants and opioid analgesics. Guide the patients with the proper disposal of unused drugs. Evaluate the patient and begin early treatment if there is any suspicion of substance use disorder.

• For people under long-term treatment than recommended, it is preferable to use a gradual taper for the discontinuation in order to reduce the risk and symptoms associated with the withdrawal.

Specific Considerations:

• Pediatric: Reliable and adequate studies have not been performed to determine the relationship of age to the Temazepam effects in pediatric patients. Hence, the safety and efficacy of Temazepam have not been established in the case of children.

• Geriatrics: Reliable studies have not been conducted to demonstrate the geriatric-specific issues that would limit the use of Temazepam in the elderly population. Nevertheless, elderly people are more likely to experience certain unwanted effects with Temazepam. They include confusion, dizziness, drowsiness, unsteadiness, and clumsiness. It can also contribute to several age-related heart, liver, and kidney problems. Hence, the prescription of Temazepam in geriatric populations requires caution and a dosage modification.

• Lactation: The clinical studies regarding the use of the drug Temazepam in breastfeeding women have demonstrated certain harmful effects on the infant. Therefore, an alternative medication to Temazepam should be given or one should stop breastfeeding while on Temazepam therapy.

• Pregnancy: Use of benzodiazepines during pregnancy is not recommended in most cases. Benzodiazepines can cross the placenta, causing hypotonia, respiratory depression, and sedation in neonates.