Tezam

Tezam Uses, Dosage, Side Effects, Food Interaction and all others data.

Tezam is a short-acting benzodiazepine with anxiolytic, hypnotic/sedative, muscle relaxant properties. It increases neuronal membrane permeability to Cl ions by binding to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron within the CNS and enhancing the GABA inhibitory effects resulting in hyperpolarisation and stabilisation.

Tezam is a benzodiazepine used as a hypnotic agent in the management of insomnia . Tezam produces CNS depression at limbic, thalamic, and hypothalamic levels of the CNS . Tezam increases the affinity of the neurotransmitter gamma-aminobutyric acid (GABA) for GABA receptors by binding to benzodiazepine receptors . Results are sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, and anxiolytic action .

In sleep laboratory studies, the effect of temazepam was compared to placebo during a two week period . The studies demonstrated a linear dose-response improvement in total sleep time and sleep latency with substantial drug-placebo differences apparent for total sleep time and for sleep latency at higher doses of temazepam . Regardless, REM sleep was ultimately unchanged but slow wave sleep was decreased .

Moreover, a transient syndrome, known as "rebound insomnia", wherein the symptoms that led to treatment with temazepam in the first place recur in an enhanced form, may happen on withdrawal of temazepam treatment . The possibility of this occurrence is in part why long term use of temazepam is not recommended due to worries over tolerance and dependence wherein patients' bodies become physiologically accustomed to the regular presence and pharmacological effect of higher and higher doses of the benzodiazepine used .

Trade Name Tezam
Availability Prescription only
Generic Temazepam
Temazepam Other Names Temazepam
Related Drugs amitriptyline, lorazepam, melatonin, zolpidem, diphenhydramine, Ativan
Weight 30mg
Type Tablet
Formula C16H13ClN2O2
Weight Average: 300.74
Monoisotopic: 300.066555377
Protein binding

It has been recorded that about 96% of unchanged temazepam is bound to plasma proteins .

Groups Approved, Investigational
Therapeutic Class Benzodiazepine hypnotics, Benzodiazepine sedatives
Manufacturer Drug Pharm (pvt) Ltd,
Available Country Pakistan
Last Updated: September 19, 2023 at 7:00 am
Tezam
Tezam

Uses

Tezam is used for the short-term treatment of insomnia (generally 7 to 10 days).

For patients with short-term insomnia, instructions in the prescription should indicate that Tezam should be used for short periods of time (7 to 10 days).

The clinical trials performed in support of efficacy were 2 weeks in duration with the final formal assessment of sleep latency performed at the end of treatment.

Tezam is also used to associated treatment for these conditions: Insomnia

How Tezam works

Gamma-Aminobutyric acid (GABA) is considered the principal inhibitory neurotransmitter in the human body . When GABA binds to GABA(a) receptors found in neuron synapses, chloride ions are conducted across neuron cell membranes via an ion channel in the receptors . With enough chloride ions conducted, the local, associated neuron membrane potentials are hyperpolarized - making it more difficult or less likely for action potentials to fire, ultimately resulting in less excitation of the neurons .

Subsequently, benzodiazepines like temazepam can bind to benzodiazepine receptors that are components of various varieties of GABA(a) receptors . This binding acts to enhance the effects of GABA by increasing GABA affinity for the GABA(a) receptor, which ultimately enhances GABA ligand binding at the receptors . This enhanced ligand binding of the inhibitory neurotransmitter GABA to the receptors increases the aforementioned chloride ion conduction (perhaps reportedly via an increase in the frequency of the chloride channel opening), resulting in a hyperpolarized cell membrane that prevents further excitation of the associated neuron cells . Combined with the notion that such benzodiazepine receptor associated GABA(a) receptors exist both peripherally and in the CNS, this activity consequently facilitates various effects like sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, and anxiolytic action .

Dosage

Tezam dosage

While the recommended usual adult dose is 15 mg before retiring, 7.5 mg may be sufficient for some patients, and others may need 30 mg. Intransient insomnia, a 7.5 mg dose may be sufficient to improve sleep latency. In elderly or debilitated patients, it is recommended thattherapybe initiated with 7.5 mg until individual responses are determined.

May be taken with or without food.

Side Effects

Complex behaviour (e.g. sleep-driving, making phone calls, preparing and eating food). Dyspnoea, nausea and vomiting, throat closing, anterograde amnesia, agitation, restlessness, irritability, excitement, aggressiveness, rage, delusions, confusion, nightmares, psychoses, hallucinations, nervousness, dizziness, drowsiness, fatigue, headache, lethargy, hangover, anxiety, depression, euphoria, ataxia, anorexia, tremor and backache.

Toxicity

Manifestations of acute overdosage of temazepam, as with other benzodiazepines, can be expected to reflect the increasing CNS effects of the drug and include somnolence, confusion, and coma, with reduced or absent reflexes . With large overdoses, respiratory depression, hypotension, and finally coma can occur .

Benzodiazepines like temazepam might cause fetal harm when administered to a pregnant woman. Transplacental distribution has in the past resulted in neonatal CNS depression following the ingestion of therapeutic doses of related benzodiazepine hypnotics like diazepam during the last weeks of pregnancy .

It is not known whether this drug is excreted in human milk . Caution should, therefore, be exercised when temazepam is administered to a nursing woman .

Safety and effectiveness in pediatric patients have not been established .

Lower doses of temazepam, like 7.5 mg is recommended as the initial dosage for patients aged 65 and over since the risk of the development of oversedation, dizziness, confusion, ataxia and/or falls increases substantially with larger doses of benzodiazepines in elderly and debilitated patients .

No evidence of carcinogenicity was observed in animal studies although hyperplastic liver nodules were observed in female mice exposed to the highest doses of temazepam . The clinical significance of this finding is not known .

Fertility in male and female rats was not adversely affected by temazepam toxicity studies .

No mutagenicity tests have been done with temazepam .

Precaution

Patient with severe depression, chronic pulmonary insufficiency, personality disorders, history of alcohol or drug addiction. Avoid abrupt withdrawal. Renal and hepatic impairment. Elderly or debilitated patient. Lactation.

Interaction

May enhance CNS depressant effect with Na oxybate, antipsychotics, tranquilisers, neuroleptics, antidepressants, hypnotics, anaesth, analgesics, sedative antihistamines, barbiturates. Effect may be reduced with theophylline.

Food Interaction

  • Avoid alcohol.
  • Take with or without food.

Tezam Alcohol interaction

[Moderate] GENERALLY AVOID:

Acute ethanol ingestion may potentiate the CNS effects of many benzodiazepines.

Tolerance may develop with chronic ethanol use.

The mechanism may be decreased clearance of the benzodiazepines because of CYP450 hepatic enzyme inhibition.

Also, it has been suggested that the cognitive deficits induced by benzodiazepines may be increased in patients who chronically consume large amounts of alcohol.



Patients should be advised to avoid alcohol during benzodiazepine therapy.

Volume of Distribution

The volume of distribution documented for temazepam is 1.3-1.5 L/kg body weight - and in particular, 43-68 L/kg for the unbound fraction .

Elimination Route

Studies demonstrate that between 90 to 100% of an orally administered temazepam dose is absorbed, making the medication very well absorbed . The oral administration of 15 to 45 mg temazepam resulted in rapid absorption with significant blood levels achieved in 30 minutes and peak levels at 2-3 hours . In particular, direct studies following the oral ingestion of 30 mg of temazepam revealed measurable plasma concentrations were obtained 10-20 minutes after dosing with peak plasma levels ranging between 666-982 ng/mL (with a mean of 865 ng/mL) presenting approximately 1.2-1.6 hours (with a mean of 1.5 hours) after the dosing . Finally, a dose-proportional relationship was established for the area under the plasma concentration/time curve over the 15 to 30 mg dose range .

Half Life

The terminal half-life determined for temazepam is recorded as being between 3.5-18 hours, with a mean of 9 hours .

Clearance

Studies regarding the clearance of temazepam have recorded the values of 1.03 ml/min/kg and 31 ml/min/kg for the clearance of total temazepam and the clearance of unbound temazepam, respectively .

Elimination Route

Following a single dose, 80-90% of the dose appears in the urine, predominantly as the O-conjugate metabolite, and 3-13% of the dose appears in the faeces . Less than 2% of the dose is excreted unchanged or as N-desmethyltemazepam in the urine .

Pregnancy & Breastfeeding use

Pregnancy category X. Studies in animals or human beings have demonstrated fetal abnormalities or there is evidence of fetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Nursing Mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Restoril is administered to a nursing woman.

Contraindication

Benzodiazepines may cause fetal harm when administered to a pregnant woman. An increased risk of congenital malformations associated with the use of diazepam and chlordiazepoxide during the first trimester of pregnancy has been suggested in several studies. Transplacental distribution has resulted in neonatal CNS depression following the ingestion of therapeutic doses of a benzodiazepine hypnotic during the last weeks of pregnancy.

Reproduction studies in animals with temazepam were performed in rats and rabbits. In a perinatal-postnatal study in rats, oral doses of 60 mg/kg/day resulted in increasing nursling mortality. Teratology studies in rats demonstrated increased fetal resorptions at doses of 30 and 120 mg/kg in one study and increased occurrence of rudimentary ribs, which are considered skeletal variants, in a second study at doses of 240 mg/kg or higher. In rabbits, occasional abnormalities such as exencephaly and fusion or asymmetry of ribs were reported without dose relationship. Although these abnormalities were not found in the concurrent control group, they have been reported to occur randomly in historical controls. At doses of 40 mg/kg or higher, there was an increased incidence of the 13th rib variant when compared to the incidence in concurrent and historical controls.

Restoril is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus. Patients should be instructed to discontinue the drug prior to becoming pregnant. The possibility that a woman of childbearing potential may be pregnant at the time of institution of therapy should be considered.

Special Warning

Renal Impairment: Short-term management of insomnia: 5 mg at bedtime. May be increased to 10-20 mg in severe cases.

Hepatic Impairment: Short-term management of insomnia: 5 mg at bedtime. May be increased to 10-20 mg in severe cases.

Severe: Contraindicated.Premedication in surgery: Severe: Contraindicated.

Pediatric Use: Safety and effectiveness in pediatric patients have not been established.

Geriatric Use: Clinical studies of Restoril did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in response between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy commonly observed in this population. Restoril 7.5 mg is recommended as the initial dosage for patients aged 65 and over since the risk of the development of oversedation, dizziness, confusion, ataxia and/or falls increases substantially with larger doses of benzodiazepines in elderly and debilitated patients.

Acute Overdose

Symptoms: Somnolence, confusion, coma, reduced or absent reflexes, resp depression, and hypotension.

Management: Supportive and symptomatic treatment. Empty stomach by vomiting or gastric lavage. Treat hypotension with IV pressor agents. IV fluids should be given to induce diuresis. Flumazenil may be used for the complete or partial reversal of the sedative effects but there is a risk of seizure esp in long-term benzodiazepine users and in cyclic antidepressant overdose.

Storage Condition

Store at 20° to 25°C

Innovators Monograph

You find simplified version here Tezam

Tezam contains Temazepam see full prescribing information from innovator Tezam Monograph, Tezam MSDS, Tezam FDA label

FAQ

What is Tezam used for?

Tezam is used to treat sleeping problems (insomnia). It can also be taken to help you relax before an operation or other medical or dental treatments.

How safe is Tezam?

Tezam is a safe hypnotic for use by older adults over an 8-week treatment period. There are few adverse effects and behavioural tolerance to those effects develop over time.

What are the common side effects of Tezam?

common side effects are include:

  • indigestion.
  • drowsiness.
  • inducing of a relaxed easy state.
  • dizziness.
  • loss of muscle coordination.
  • slurred speech.

Is Tezam safe during pregnancy?

Tezam is not usually recommended during pregnancy. If you become pregnant while taking Tezam, speak to your doctor.

Is Tezam safe during breastfeeding?

Tezam can be used during breastfeeding at low doses occasionally, or for a short time. Tezam passes into breast milk in small amounts, but it's unlikely to cause any side effects in your baby.

Is it safe to take Tezam every night?

Tezam is used to help people get to sleep. It is habit-forming and should not be used for more than seven to ten nights in a row.

Does Tezam affect the heart?

Tezam caused a fall in systolic blood pressure and an increase in heart rate after morning administration.

How long does Tezam last in my system?

Restoril can be detected in your body from one to 90 days, depending on factors like dosage, age, weight, and metabolism, as well as the type of detection test used.

Is Tezam bad for my liver?

Clinically apparent liver injury from Tezam is extremely rare, if it occurs at all. There have been no case reports of symptomatic, acute liver injury from Tezam .

Can I drink alcohol with Tezam?

Alcohol can increase nervous system side effects such as dizziness, drowsiness, and difficulty concentrating. Some people may also experience impairment in thinking and judgment. You should avoid or limit the use of alcohol while being treated with Tezam.

Can Tezam cause death?

Taking Tezam with certain drugs puts you at serious risk of severe drowsiness, slowed breathing, coma, or death.

How bad is Tezam for me?

Tezam may cause serious allergic reactions, including anaphylaxis and angioedema, which can be life-threatening and require immediate medical attention.

Will Tezam affect my contraception?

Tezam does not affect how contraception works, including the combined pill and emergency contraception.

Does taking Tezam increase the chance for miscarriage?

Miscarriage can occur in any pregnancy. Studies have not been done to see if Tezam could increase the chance for a miscarriage.

Can I drive aftyer taking Tezam?

Once you have taken Tezam, do not drive, operate machinery, or perform tasks that require mental alertness.

How long does Tezam stay in your system?

Tezam can be detected in your body from one to 90 days, depending on factors like dosage, age, weight, and metabolism, as well as the type of detection test used.

How long do I sleep on Tezam?

Its effects last approximately seven to eight hours. Do not take Tezam if you do not intend to stay asleep or in bed for at least eight hours.

*** Taking medicines without doctor's advice can cause long-term problems.
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