Alprazolam is an anxiolytic drug (tranquilizer), a derivative of triazolo-benzodiazepine. This medication has anxiolytic, sedative, hypnotic, anticonvulsant, central muscle relaxant effect. The mechanism of action is to enhance the inhibitory effect of endogenous GABA in the CNS by increasing the sensitivity of the GABA-receptor mediator as a result of stimulation of benzodiazepine receptors located in the allosteric center of postsynaptic GABA-receptor activating ascending reticular formation of brain stem neurons and the lateral horns of the spinal cord; reduces the excitability of the subcortical brain structures (the limbic system, thalamus, hypothalamus), inhibits the polysynaptic spinal reflexes.
Pronounced anxiolytic activity (reduction of emotional tension, easing anxiety, fear, anxiety) is combined with moderate soporific effect; it shortens the period of sleep, increases sleep duration and reduces the number of nighttime awakenings. The mechanism of hypnotic action is inhibition of cell reticular formation of the brain.
After oral administration alprazolam is rapidly and completely absorbed from the gastrointestinal tract. Cmax plasma levels achieved within 1-2 hours. Binding to plasma proteins is 80%. This drug metabolized in the liver. T1/2 is an average of 12-15 hours. Alprazolam and its metabolites are mainly excreted by kidneys.
Why is Xanax Retard prescribed?
- anxiety, neurosis accompanied by anxiety, anger, stress, deterioration of sleep, irritability, and somatic disorders
- mixed anxiety-depressive conditions
- neurotic reactive depression accompanied by depressed mood, loss of interest in his surroundings, anxiety, loss of sleep, decreased appetite, and somatic disorders
- anxiety and neurotic depression that developed on the background of systemic diseases
- panic disorder in combination and without symptoms of phobias
Dosage and administration
Individual. It is recommended to use the minimum effective dose. The dose is corrected in the treatment process depending on the achieved effect and tolerability. If necessary, increase the dose should be increased gradually, first in the evening and then in the daytime reception.
The initial dose is 250-500 mg 3 times/day, if necessary, it gradually increases to 4.5 mg/day.
For elderly or debilitated patients the initial dose is 250 mg 2-3 / day, maintenance doses – 500-750 mg/day, if necessary, taking into account the tolerance dose can be increased.
Cancellation or reduction of the dose of alprazolam should be done gradually by reducing the daily dose of no more than 500 mcg every 3 days; sometimes can be needed even more slowly canceling.
Xanax Retard side effects
CNS: at the beginning of treatment (especially in elderly patients) drowsiness, fatigue, dizziness, decreased ability to concentrate, ataxia, disorientation, unsteady gait, slowing of mental and motor responses; rare – headache, euphoria, depression, tremors, memory loss, impaired coordination of movements, depressed mood, confusion, extrapyramidal dystonic reactions (involuntary movements, including for eyes), weakness, myasthenia gravis, dysarthria; in some cases – paradoxical reactions (aggressive flare, confusion, psychomotor agitation, fear, suicidal tendencies, muscle spasms, hallucinations, agitation, irritability, anxiety, insomnia).
Digestive system: possible dry mouth or excessive salivation, heartburn, nausea, vomiting, decreased appetite, constipation or diarrhea, abnormal liver function, elevated liver transaminases and alkaline phosphatase, jaundice.
Hematopoietic system: possible leukopenia, neutropenia, agranulocytosis (chills, pyrexia, sore throat, extreme tiredness or weakness), anemia, thrombocytopenia.
Urinary tract: possible urinary incontinence, urinary retention, renal failure, decreased or increased libido, dysmenorrhea.
Endocrine system: possible change in body weight, disturbances in libido, menstrual irregularities.
Cardiovascular system: possible decrease in blood pressure, tachycardia.
Allergic reactions: possible skin rash, itching.
Coma, shock, myasthenia gravis, angle-closure glaucoma (acute attack or predisposition), acute alcohol poisoning (with the weakening of the vital functions), narcotic analgesics, hypnotics and psychotropic drugs, chronic obstructive airways disease with incipient respiratory failure, acute respiratory failure, severe depression (suicidal tendencies may occur), pregnancy (especially the I trimester), lactation, childhood and adolescence to 18 years, increased sensitivity to benzodiazepines.
Using during pregnancy and breastfeeding
Alprazolam has a toxic effect on the fetus and increases the risk of birth defects when used in the I trimester of pregnancy. The constant use during pregnancy can cause physical dependence with the development of withdrawal syndrome in the newborn. Reception at therapeutic doses in the later stages of pregnancy can cause neonatal CNS depression. Using of alprazolam immediately before birth or during labor can cause neonatal respiratory depression, decreased muscle tone, hypotension, hypothermia and a weak act of sucking (sucking flaccid syndrome baby).
It is possible to excretion of the benzodiazepines in breast milk that can cause drowsiness in the newborn and hinder feeding.
In experimental studies have been shown that alprazolam and its metabolites are excreted in breast milk.
Keep in mind that anxiety or conditions related to everyday stress usually does not require treatment with anxiolytics.
If you experience paradoxical reactions then stop taking the drug. During the period of treatment is unacceptable to use of alcoholic drinks. With caution use alprazolam for drivers of vehicles and people whose profession is associated with increased concentration.
Xanax Retard drug interactions
The simultaneous use with psychotropic, anticonvulsant medications and ethanol is observed enhancement inhibitory action alprazolam on the CNS.
The simultaneous use with blockers of histamine H2-receptor reduce the clearance of alprazolam and increase the inhibitory effect of alprazolam on the CNS; macrolide antibiotics reduce the clearance of alprazolam.
The simultaneous use with hormonal oral contraceptives increased T1/2 of alprazolam.
Simultaneous administration with dextropropoxyphene observed a more pronounced CNS depression than in combination with other benzodiazepines, as may increase the concentration of alprazolam in blood plasma.
Simultaneous treatment with digoxin increases the risk of intoxication by cardiac glycosides.
Alprazolam increases the concentration of imipramine in plasma.
Simultaneous administration with itraconazole, ketoconazole increases the effects of alprazolam.
Simultaneous administration with paroxetine may increase the effects of alprazolam due to the inhibition of its metabolism.
Fluvoxamine increases the concentration of alprazolam in plasma and risk of its side effects.
Simultaneous administration with fluoxetine may increase the concentration of alprazolam in plasma by decreasing its metabolism and clearance under the influence of fluoxetine which is accompanied by psychomotor disorders.
It cannot exclude the possibility of strengthening the effect of alprazolam for simultaneous administration with erythromycin.
Xanax Retard in case of emergency/overdose
Symptoms: Varying degrees of CNS oppression (from sleepiness to coma) – drowsiness, confusion; in more severe cases (especially in patients receiving other drugs depressing the central nervous system or alcohol) – ataxia, decreased reflexes, hypotension, coma.
Treatment: induction of vomiting, gastric lavage, symptomatic therapy, monitor vital signs. In severe hypotension prescribed an injection of norepinephrine. The specific antidote is benzodiazepine receptor antagonist flumazenil (administration only in a hospital).