The drug Halcion is used as a sleeping aid. Its active ingredient, Triazolam, affects the processes that take place in the brain. The drug effectively fights insomnia caused by various reasons. The drug is used under the supervision of a doctor, as it is capable of causing addiction with prolonged use.
Active ingredient and product form
Halcion in the United States and Mexico is available in tablet form. Each tablet contains 0.125 mg of the active ingredient. One package contains 30 tablets for oral administration.
The active ingredient is Triazolam. According to the chemical structure, it is a benzodiazepine. According to physical properties, it is a fine crystalline powder of white color. It is almost insoluble in water, but soluble in alcohol. Triazolam as a sleeping pill was patented in the United States in 1970. Preparations based on it went on sale in 1987.
Bioavailability of triazolam during oral administration reaches 44%. The substance is absorbed into the bloodstream through the villi of the small intestine. The drug acts quickly and effectively, so it is prescribed even for severe forms of insomnia. The maximum concentration of the active substance is fixed in the bloodstream 1-2 hours after oral administration.
Triazolam is 89% bound to plasma proteins. It is transformed into metabolites in liver cells. The active substance is eliminated from the body by 80% with urine and 8% with feces. The remaining active substance leaves the body unchanged. It does not accumulate in tissues.
Pharmacological action of Halcion
Triazolam acts directly on the CNS. The chemical compound interacts with benzodiazepine receptors. These structures are located in the lateral horns of the spinal cord, brainstem, hippocampus, limbic system.
Administration of Triazolam promotes sensitization of receptors to GABA. As a result, membrane channels open for free access of chlorine ions. This causes hyperpolarization of neuronal membranes, which in turn leads to an increase in the inhibitory effect of GABA.
The effect of the drug
Halcion is a powerful tranquilizer, which eliminates problems with falling asleep. By inhibiting the activity of the brain stem, the drug has a sedative and hypnotic effect. It is also proven that the tablets have a moderate anxiolytic, anticonvulsant and muscle relaxant effect.
Against the background of taking Halcion:
the period of falling asleep is shortened;
increases the total duration of sleep;
reduces the number of night wakings;
anxiety is relieved;
emotional tension is controlled;
uncontrollable spasms and cramps are eliminated.
Studies confirm that Halcion tablets induce sleep that is close to natural. The active ingredient has practically no effect on the structure of sleep. Triazolam does not affect the third and fourth phases of sleep (slow-wave sleep). The tranquilizer suppresses CNS activity and stimulates the first phase of sleep - drowsiness, and partially supports the second phase - superficial sleep.
Indications for use of Halcion
The tranquilizer is prescribed in the therapy of temporary insomnia associated with disruption of circadian rhythms. For long-term sleep disorders, the drug with triazolam in its composition can be used for a short course as part of complex therapy. The effectiveness of sleeping pills for frequent morning awakenings has not been proven.
Features of treatment
Taking a therapeutic dose of the drug provides a sound sleep for at least seven hours. It is not recommended to take the tranquilizer if less time is planned for rest. The pill acts quickly. The patient relaxes and falls asleep in 10-30 minutes.
The recommended course length is no more than two weeks. If you do not stop using the tranquilizer, its effectiveness begins to gradually decline. In addition, on the first or second day after withdrawal, most patients develop a recoil syndrome if the treatment is prolonged. The person cannot fall asleep for a long time.
Contraindications to taking
Halcion is an effective remedy for insomnia, but it is not always possible to use it. The list of absolute contraindications includes the following conditions: allergy to triazolam; individual intolerance to other benzodiazepines, including Alprazolam, Chlordiazepoxide, Clorazepate, Diazepam or Lorazepam; age under 18 years; pregnancy; lactation.
There are no reliable studies on the teratogenicity of the tranquilizer, but the risk to the fetus is rated as high. Laboratory experiments have confirmed that the concentration of triazolam in the fetal brain is similar to that of the substance in the mother's CNS. In pregnancy, it is necessary to discuss with the doctor another tactic of insomnia treatment. If intake of the drug is needed already after delivery, lactation is stopped.
Restrictions on administration
In some cases, the drug is prescribed with caution. The list of relative contraindications includes glaucoma; renal pathology; severe liver disease; myasthenia; depression; apnea.
Halcion, like other synthetic tranquilizers, directly affects the CNS by stimulating the inhibitory effect of GABA. Because of this, the drug should not be used by people with pronounced psychological disorders, against which suicidal thoughts arise. Do not treat insomnia with tablets with triazolam in the composition of persons who have alcohol or drug addiction, including in the anamnesis.
Side effects of treatment with Halcion
Long-term oral administration of the tablets is fraught with the development of adverse reactions from various organ systems. Patients are most often diagnosed with: drowsiness; rapid fatigue; headache; dizziness; nervousness; tremors of limbs; uncontrollable movements; feeling of euphoria; tinnitus; distortion of tastes and smells; nightmares; nausea; vomiting; constipation; dry mouth.
The side effects of Halcion pills are mild to moderate in intensity. In most cases, they go away on their own. Some patients need adjustment of the daily dose of the drug. Symptomatic treatment is not required.
Allergic reactions to the tranquilizer
The patient may complain of allergic reactions to the active ingredient or excipients. The risk of such a condition is higher with intolerance to other benzodiazepines. Characteristic signs of Halcion allergy are skin rash; itching and burning; swelling of the face, lips, tongue; and difficulty in breathing.
If a sudden development of a severe allergic reaction, it is required to cancel the drug and seek medical attention.
Overdose of the drug
An independent increase in the therapeutic dose is fraught with intoxication with the active substance. In case of overdose, the following symptoms are observed:
In severe cases, sudden respiratory depression is possible, leading to death. The risk of death is higher if the patient has previously been diagnosed with pathologies of the lungs, heart, kidneys, liver.
Aid measures in case of overdose
When poisoning with triazolam, the following measures are necessary:
Gastric lavage by inducing vomiting. The measure is effective if less than two hours have passed since ingestion. Then the active substance has already had time to be absorbed into the systemic bloodstream. After lavage, the patient is given sorbents.
Monitoring of physiological indicators. The patient's blood pressure is regularly measured. Additionally, electrocardiography is performed. These measures are necessary to assess the state of the heart and blood vessels.
Intravenous injection of solutions. Injections are necessary to restore the amount of extracellular free fluid, accelerate metabolism, remove such signs of intoxication as weakness, drowsiness.
Artificial lung ventilation. Connection to the ventilator is necessary when the respiratory center is inhibited and there is a high risk of death due to hypoxia.
Because of the fast and complete binding of the active substance with plasma proteins, hemodialysis is not used. A specific antidote, flumazenil, is used in hospital settings for patients with Halcion overdose. It is the only benzodiazepine receptor antagonist. The substance blocks the effects of the tranquilizer and restores CNS function.
Halcion should not be combined with other drugs with sedative effects. Combined administration increases drowsiness, increases the risk of side effects and intoxication with the active component. Anterograde amnesia has not been ruled out. In this condition, the patient's memory functions are impaired. A person cannot remember some events that occurred during the treatment period.
Other drug combinations:
when combined with anticonvulsants, the effectiveness of the tranquilizer is reduced;
in combination with caffeine-based medications slows down the effect of sleeping pills;
in combination with antifungal drugs increases the sedative effect and prolongs the period of sleep;
in combination with anti-tuberculosis drugs slows down the elimination of triazolam from the body;
in combination with nefazodone-based antidepressants further depresses the central nervous system;
when combined with drugs to reduce acidity in the stomach, there is an increased risk of impaired coordination of movements;
when combined with erythromycin- and clarithromycin-based antibiotics, the plasma concentration of triazolam increases.
Combination with alcohol
During therapy with Halcion tablets, it is strictly forbidden to consume alcoholic beverages, even those with a minimum percentage of alcohol. The combination of triazolam and ethanol increases the risk of severe side effects and overdose, up to and including death. This is due to the acceleration of absorption of the active component in blood and increased burden on the liver and kidneys involved in the metabolization and excretion of decay products of ethanol and spent drug.
During the treatment of insomnia with tranquilizers, it is necessary to refrain from working with complex mechanisms and driving a car. Reaction speed may be significantly reduced during admission.
Halcion is addictive, so it can be used strictly as prescribed by the doctor for a course of up to 14 days. Withdrawal should be gradual, especially in persons with epilepsy and elderly patients. The drug should be stored in a place out of the reach of children.
The information provided is for guidance and should not be used as an indication for self-medication. Only a physician has the authority to prescribe the drug and set the dosage in each case.