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Alprazolam is a mid-acting benzodiazepine anxiolytic drug that is used to treat panic disorders, anxiety disorders such as anxiety disorder or social phobia.

Other names: Alprazolam

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  • Active substance: Alprazolam - 0.25 mg or 1 mg.
  • Excipients: potato starch, magnesium stearate (magnesium stearate), milk sugar (lactose), low molecular weight medical polyvinylpyrrolidone (povidone).


Alprazolam has an anxiolytic, central muscle relaxant, anticonvulsant, sedative-hypnotic and anti-panic effect. It has a depressing effect on the central nervous system, which is realized mainly in the thalamus, hypothalamus and limbic system. It enhances the inhibitory effect of gamma-aminobutyric acid, which is one of the main mediators of pre- and postsynaptic inhibition of the transmission of nerve impulses in the central nervous system. The mechanism of action of alprazolam is determined by stimulation of benzodiazepine receptors of the supramolecular gamma-aminobutyric acid-benzodiazepine-chlorionophore prescription complex, leading to activation of the gamma-aminobutyric acid receptor, causing a decrease in the excitability of the subcortical structures of the brain, inhibition of polysynaptic spinal reflexes.

The anxiolytic effect is manifested in a decrease in emotional stress, weakening the symptoms of anxiety, fear.

Pronounced anxiolytic activity is combined with a moderate hypnotic effect; shortens the period of falling asleep, increases the duration of sleep, reduces the number of night awakenings. The mechanism of hypnotic action is to inhibit the cells of the reticular formation of the brain stem. Reduces the impact of emotional, vegetative and motor stimuli that disrupt the mechanism of falling asleep.

Virtually no effect on the cardiovascular and respiratory system.


When taken orally, the maximum plasma concentration is reached after about 1-2 hours. After a single oral dose of 0.5 mg, the mean maximum concentration was 7.1 mg/mL. There is a linear relationship between alprazolam dose and plasma concentration. When taken orally, approximately 80% of the dose is absorbed. About 80% of the drug binds to plasma proteins. It can pass through the placenta, the blood-brain barrier (BBB), penetrate into breast milk. Stable plasma concentration is usually achieved within a few (2-3) days. Alprazolam is actively metabolized in the liver, the main metabolite is the alpha-hydroxyl metabolite, which has biological activity. Excretion of the drug from the body occurs mainly through the kidneys in the form of compounds with glucuronic acid. The half-life (T1 / 2) is 11-16 hours. Accumulation with repeated administration is minimal (applies to benzodiazepines with an average T1 / 2), excretion after stopping treatment is fast.

Indications for use

Treatment of neurotic and neurosis-like disorders with manifestation of anxiety, incl. associated with depression, panic disorders.

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Hypersensitivity to alprazolam or other benzodiazepines. Coma, shock, angle-closure glaucoma, myasthenia gravis, acute alcohol poisoning, narcotic, sleeping pills and psychotropic drugs; severe chronic obstructive pulmonary disease, severe depression (suicidal attempts), sleep apnea syndrome, severe impairment of kidney and liver function, pregnancy (especially the first trimester), see "Special Instructions", breast-feeding period.

With caution, cerebral and spinal ataxia, a history of drug dependence, a tendency to abuse psychotropic drugs, hyperkinesis, organic brain diseases, psychosis (paradoxical reactions are possible), hypoproteinemia, old age. The safety of alprazolam in children and adolescents (under 18 years of age) has not been established.

Dosage and administration

Inside, 2-3 times a day, regardless of the meal. The dose of the drug is selected individually and corrected during treatment, depending on the effect and individual tolerance. The use of the lowest effective dose is recommended. In anxiety conditions, the initial dose is 0.25-0.5 mg three times a day. If necessary, this dose can be increased to 4 mg / day (divided into several doses).

In the elderly, the initial dose is 0.25 mg 2-3 times a day.

For anxiety associated with depression, the initial dose is 0.5 mg three times a day. If necessary, the dose is increased to 4.5 mg / day. The initial dose may be given at bedtime to minimize daytime sleepiness. The duration of treatment is 4-12 weeks. Discontinuation of the drug should be done with great caution. The dose should be reduced gradually and slowly, no more than 0.5-1 mg at bedtime or 0.5 mg three times a day. For most patients, a sufficient dose is 4-6 mg / day for 4-12 weeks. In some cases, if necessary, the dose can be increased to 10 mg / day (but not more than 1 mg every 3-4 days), and the duration of treatment - up to eight months. In the treatment of elderly and debilitated patients, smaller doses should be used: initial - 0.25 mg 2-3 times a day, if necessary and well tolerated, it is gradually increased to 0.5-0.75 mg / day.

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Side effects

Side effects, as a rule, occur at the beginning of treatment and gradually disappear as the drug is continued or the dose is reduced.

From the side of the central nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, fatigue, dizziness, impaired concentration, ataxia, disorientation, slowing down of mental and motor reactions; rarely - headache, euphoria, decreased mood, tremor, memory loss, impaired coordination of movements, confusion, dystonic extrapyramidal reactions (uncontrolled movements, including the eye), muscle weakness, blurred speech, extremely rarely - paradoxical reactions (aggressive flashes, confusion, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, anxiety, insomnia).

On the part of the hematopoietic organs: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, unusual fatigue or weakness), anemia, thrombocytopenia.

From the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, anorexia, constipation, diarrhea; abnormal liver function, increased activity of "liver" transaminases and alkaline phosphatase (AP), jaundice.

From the genitourinary system: urinary incontinence, urinary retention, impaired renal function, decreased or increased libido, dysmenorrhea.

Allergic reactions: skin rash, itching.

Effect on the fetus: teratogenicity (especially the first trimester), CNS depression, respiratory failure and suppression of the sucking reflex in newborns whose mothers used the drug.

Others: addiction, drug dependence; decrease in blood pressure (BP), rarely - visual impairment (diplopia), weight loss, tachycardia. With a sharp decrease in the dose or discontinuation of the intake, the "withdrawal" syndrome (increased irritability, sleep disturbance, dysphoria, spasm of the smooth muscles of the internal organs and skeletal muscles, depersonalization, increased sweating, decreased mood, nausea, vomiting, tremor, perception disorders, incl. including hyperacusis, paresthesia, photophobia, tachycardia, convulsions, rarely acute psychosis).


Overdose of the drug (reception 500-600 mg).

Symptoms: drowsiness, confusion, decreased reflexes, nystagmus, tremor, bradycardia, shortness of breath or shortness of breath, decreased blood pressure, coma.

Treatment: gastric lavage, activated charcoal. Symptomatic therapy (maintenance of breathing and blood pressure), the introduction of flumazenil (in a hospital setting). Hemodialysis is ineffective.

Interaction with other drugs

Alprazolam enhances the effect of other psychotropic drugs, anticonvulsants and antihistamines, ethanol and drugs that have a depressant effect on the central nervous system. Microsomal oxidation inhibitors - increase the risk of developing toxic effects. Inducers of microsomal liver enzymes - reduce the effectiveness of alprazolam.

Antihypertensive drugs can increase the severity of lowering blood pressure. With simultaneous administration with clozapine, it is possible to increase respiratory depression.

Reduces the effectiveness of levodopa in patients with parkinsonism. Potentially increased toxicity of zidovudine.

Alprazolam at a dose of 4 mg / day increases plasma concentrations of imipramine and desipramine (by 31% and 20%, respectively) when taken simultaneously. The metabolic clearance of alprazolam is reduced while taking the usual therapeutic doses of cimetidine and antibiotics from the macrolide group. Caution should be exercised and consideration should be given to reducing the dose of alprazolam when taken with cimetidine, macrolides, nefazodone, fluvoxamine, fluoxetine, propoxyphene, sertraline, daltiazem, digoxin, and oral contraceptives.

Special instructions

During treatment with alprazolam, patients are strictly prohibited from drinking alcohol (ethanol). With renal / liver failure and long-term treatment, it is necessary to monitor the picture of peripheral blood and "liver" enzymes.

Patients who have not previously taken psychotropic drugs, "respond" to the drug at lower doses compared with patients who took antidepressants, anxiolytics or suffering from alcoholism. In endogenous depression, alprazolam can be used in combination with antidepressants. When using alprazolam in patients with depression, there have been cases of the development of hypomanic and manic states.

Like other benzodiazepines, alprazolam has the ability to cause drug dependence with long-term use in high doses (more than 4 mg / day).

If patients experience such unusual reactions as increased aggressiveness, acute states of arousal, fear, suicidal thoughts, hallucinations, increased muscle cramps, difficulty falling asleep, superficial sleep, treatment should be discontinued.

During pregnancy, they are used only in exceptional cases and only for health reasons. It has a toxic effect on the fetus and increases the risk of congenital malformations when used in the first trimester of pregnancy. Taking therapeutic doses later in pregnancy may cause CNS depression in the newborn. Chronic use during pregnancy can lead to physical dependence with the development of a "withdrawal" syndrome in the newborn.

Children, especially at a younger age, are very sensitive to the CNS depressant effects of benzodiazepines.

Use immediately before or during labor may cause respiratory depression, reduced muscle tone, hypotension, hypothermia, and poor suckling (so-called "sluggish baby" syndrome) in the newborn.

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