Triazolam

Triazolam, A benzodiazepine sedative-hypnotic drug called Triazolam is authorized for the temporary treatment of insomnia. Has anxiolytic properties (relieves anxiety), much like other benzodiazepines, although it is rarely given for this purpose. It doesn’t have an active metabolite and has an intermediate half-life of 1.5-5.5 hours. A single dosage taken at bedtime may cause sleepiness and sedation during the day for certain people.   

• Withdrawn in the United Kingdom due to the risk of psychiatric adverse drug reactions. This drug continues to be available in the U.S. Internationally, triazolam is a Schedule IV drug under the Convention on Psychotropic Substances.
• Triazolam is a short-acting benzodiazepine with a rapid onset of action that is commonly used for short-term and intermittent use in patients with recurring insomnia and poor sleeping habits.
• The mean apparent half-life of triazolam is3.5 hours.

Triazolam usually shouldn’t be used for more than a week. Some patients may, however, occasionally require extended usage; in these situations, close monitoring is required to avoid developing a physical or psychological dependence. Like other benzodiazepines, triazolam is categorized as a restricted drug by federal and state legislation because of its association with dependency and misuse.

How does Triazolam work?

Triazolam works pharmacologically in the brain at certain receptor locations, which may help explain why it is such an excellent anxiety treatment. The neurotransmitter γ-aminobutyric acid (GABA) in that area of the brain is facilitated in its inhibitory effect by the combined action of benzodiazepines on the receptors. 

It appears that benzodiazepines’ anxiolytic, sedative, and anticonvulsant effects are due to their interaction with GABA receptors.

What is the recommended dose of Triazolam? 

Adults:0.125 to 0.25 mg at bedtime. Your doctor may adjust your dose as needed. However, the dose is usually not more than 0.5 mg per day.

Older adults: at first, 0.125 mg at bedtime. Your doctor may adjust your dose as needed. However, the dose is usually not more than 0.25 mg per day.

Children: Use and dose must be determined by your doctor.

•  Dose increases should be initiated with care.

What happens when you take an overdose of Triazolam?

Oral benzodiazepine overdoses are rarely lethal. Benzodiazepines sometimes cause mortality when taken with other CNS depressants, particularly alcohol, narcotics, and barbiturates.   

Drowsiness, confusion, somnolence, weariness, dropped coordination, clumsiness while walking (ataxia), and sluggish reflexes are some of the mild indications of benzodiazepine overdose.  

When taken alone, benzodiazepines hardly cause death. When some drugs participate in benzodiazepine overdose, severe symptoms such as trouble breathing, slowing heart rate, decreased blood pressure, lack of coordination, and loss of consciousness lead to coma and death. 

• Every potential overdose should be considered an emergency at the ER. The prescription bottle of the drug along with any extra drugs linked to the overdose should also be brought, as the data on the prescription label can help the treating physician estimate the quantity of pills consumed.

What are the side effects of Triazolam administration?

Sedation and drowsiness are the most often reported, particularly in the early stages of therapy. Other common symptoms include difficulty focusing and remembering things, a dissociative or “spacey” feeling, and trouble with coordination.  

• Constipation, change in appetite, decreased interest in sexual intercourse.
• Suicidal thoughts or behaviors, hyperventilation, change in consciousness, confusion, loss of memory, seizures, and palpitations.

In some individuals, benzodiazepines may possess paradoxical effects. In susceptible individuals, the drug stimulates enthusiasm, aggression, hostility, uncontrolled behavior, and wrath rather than the expected depressive effects. These reactions are especially common in the elderly, people with brain injuries, and people with personality and impulse control difficulties.

What are the precautions taken with Triazolam administration?

• Triazolam, like other benzodiazepines, is categorized as a restricted substance due to its potential for misuse and dependence, according to state and federal laws. 
• The drug impairs awareness and coordination; therefore, patients should use caution when driving or performing other tasks that require alertness while taking this medicine. 
• The dose should be reduced when there is concurrent administration with CYP3A4.

Seniors may be more vulnerable due to impaired coordination and reflexes, perhaps leading to falls and injuries. 

• Co-administration with other central nervous system (CNS) depressants such as alcohol, opioids, and barbiturates may exacerbate these CNS effects. So quit drinking while taking the drug. 
• Prolonged usage of benzodiazepines such as triazolam could end in dependence. When the medicine is abruptly stopped, the withdrawal symptoms may appear. Headaches, vomiting, decreased attention, confusion, tremors, muscle cramps, and seizures are among withdrawal symptoms. 
• Benzodiazepines, such as triazolam, are systemically acting depressants that might reduce breathing. This is especially challenging for people with chronic obstructive lung disease and emphysema. The respiratory depressive effect of benzodiazepines may further suppress respiratory drive in these patients, putting them at greater risk for respiratory depression and death. 

If you miss a dose, take it right away. If it is near the next planned dose, cancel the missed dose and resume your normal dosing schedule. Avoid taking double the prescribed dose.

• Triazolam should only be taken when needed for sleep. Do not take more than the prescribed dose.
• Triazolam can be taken before or after meals. 
• Keep the medication in the original labeled, light-resistant container, away from heat and moisture, to avoid drug degradation by them. 
• Keep triazolam away from your children.

How does triazolam affect pregnancy and lactation? 

• Triazolam is classified as pregnancy category x.

Benzodiazepines and their metabolites are known to cross the placenta and accumulate in the fetal circulation. 

• They are associated with a risk of congenital malformations when used during pregnancy, causing cleft lip and heart deformities in the fetus. 
• Benzodiazepines such as triazolam should be avoided during pregnancy, particularly in the first trimester. The use of benzodiazepines during pregnancy should only be considered only when the need for the medication outweighs its risk, and alternative therapies have failed. 

Nursing mothers should not take triazolam because it will pass into breast milk and be ingested by the baby. If stopping the drug is not an alternative, breastfeeding should not be started or should be discontinued.

What are the drugs contraindicated with triazolam?

 Triazolam and its metabolites, principally as conjugated glucuronides, which are presumably inactive, are excreted primarily in the urine.

• Grapefruit may reduce the CYP3A4 metabolism of triazolam, which increases the serum concentration of triazolam.
• CNS depressants (alcohol, narcotics, barbiturates, and hypnotics) and antihistamines could affect coordination and breathing while increasing drowsiness.

• Cimetidine, fluoxetine, ketoconazole, propranolol, divalproex sodium, propoxyphene, isoniazid, and protease inhibitors: these medications may inhibit the metabolism of triazolam, thus increasing the level and pharmacological effects of the drug and producing excessive sedation and other adverse CNS effects.