Xanax is a short-acting drug in the benzodiazepine class, used to treat severe anxiety disorders, panic disorders and as an adjunctive treatment for anxiety associated with clinical depression.
Xanax is a trade name for the anti-anxiety medication alprazolam. Alprazolam is an antianxiety drug, a derivative of triazolo-benzodiazepine – a benzodiazepine with a triazolo-ring attached to its structure. Alprazolam a benzodiazepine, non-specifically binds with the benzodiazepine receptors BNZ1 and BNZ2. BNZ1 receptor mediates the sleep while BNZ2 receptor affects the muscle relaxation, motor coordination, anticonvulsant activity, and memory.
Benzodiazepines produce a variety of effects by modulating the GABA subtype of the GABA receptor, the most prolific inhibitory receptor within the brain. Alprazolam has anxiotic, 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) 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. Stimulation of GABA receptor in the peripheral nervous system may cause vasodilation, decrease cardiac contractility and enhance perfusion.
Alprazolam is completely absorbed from the gastrointestinal tract. The peak plasma concentration is achieved in 1-2 hours. Most of the drug (80%) is bound to plasma protein, mainly serum albumin. Alprazolam is hydroxylated in the liver to α-hydroxyalprazolam, which is also pharmacologically active. Alprazolam and its metabolites are mainly excreted by kidneys. This and other metabolites are later excreted in urine as glucuronides. Some of the drugs are also excreted in unchanged form.
Alprazolam is recommended for the short-term treatment (up to 8 weeks) of severe acute anxiety – panic disorder, with or without agoraphobia, essential tremor, panic attacks, stress, and deterioration of sleep, somatic disorders, neurotic depression and other types of convulsive behaviors.
Dosage and administration
Recommended doses of Alprazolam vary depending upon the age and diseased state of the patient.
- Anxiety disorder: 0.25-0.5mg thrice a day orally for 3-4 days, progressively enhance the dose in every 3-4 days. Maintenance dose: up to 4 mg daily in divided doses orally.
- Panic disorder: 5mg thrice a day orally. If required, progressively enhance the dose in every 3-4 days. Maintenance dose: 1 to 10mg daily in divided doses.
- Extended-release tablets: 0.5-1.0mg once a day orally. If required, progressively enhance the dose in every 3-4 days. Maintenance dose: 1 to 10mg once a day orally.
- Depression: 0.5mg thrice a day orally, progressively enhances the dose in every 3-4 days. Maintenance dose: up to 3mg (maximum 4.5mg) daily in divided doses orally.
- Anxiety disorder: 25mg twice or thrice a day orally. No need to increase the dose.
- Panic disorder: 25mg twice or thrice a day orally.
- Depression: 25mg twice or thrice a day orally. No need to increase the dose.
In the case of hepatic and renal impairment, the dosing recommendations are as follows:
- A dose in hepatic impairment: 25mg twice or thrice a day orally. A dose may be regularly increased if required.
- A dose in renal impairment: Caution should be taken in case of renal dysfunction.
Side effects of alprazolam which may occur are: hyperactivity, dry mouth or increased salivation, drowsiness, decreased inhibitions, no fear of danger, hallucinations, agitation, and hostility, feeling dizziness, light-headed or fainting, speech problems, urinating less than usual or not at all, depressed mood with thoughts of suicide, headache, fatigue, joint pain and unusual weakness (flu-like symptoms), changes in appetite (including changes in weight), muscle twitching, tremor and seizure (convulsions), nervousness, restlessness, sleeplessness and sweating, constipation, diarrhea, nausea and vomiting, complete memory loss, (amnesia) and concentration problems, pounding in the chest or rapid heartbeat, blurred vision, unsteadiness and clumsiness (impaired coordination and balance).
Medical attention should be sought immediately in case signs of an allergic reaction occur such as hives, difficulty breathing, swelling of the face, lips, tongue or throat. Medical attention should also be sought immediately if signs of jaundice appear such as yellowing of the skin or eyes.
Women who are pregnant or are planning on becoming pregnant should avoid the use of alprazolam. If you are currently planning to become pregnant, discuss this issue with your obstetrician or other doctors. It should be considered that the child born of a mother who is receiving benzodiazepines may be at risk of developing withdrawal symptoms from the drug during the postnatal period. It may cause neonatal flaccidity and respiratory problems in newborns. Also, alprazolam should not be used by nursing mothers – benzodiazepines are known to be passed into breast milk. This can cause infants to become lethargic and lose weight.
Special instructions and precautions
Like all central nervous system depressants, alprazolam in doses of 0.5 mg and above can cause significant deterioration in alertness, combined with increased feelings of sleepiness. People driving or conducting activities which require vigilance should exercise caution in using alprazolam. Older people as well should be cautious in the use of alprazolam due to the possibility of increased susceptibility to side effects, especially loss of coordination and drowsiness.
Xanax Retard drug interactions
Alprazolam may interact with other medications, vitamins or herbs. Be aware that if you are taking these drugs together, such interaction can be harmful and can cause serious side effects. Examples of the drugs which should not be taken concomitantly with Alprazolam:
- Activators or inhibitors of Cytochrome P450 3A (CYP3A). Activators or inhibitors of CYP3A) that interfere with the metabolism via CYP3A may show interaction with Alprazolam.
- Inhibitors of CYP3A bring about inhibition of the metabolism of Alprazolam and other related benzodiazepines and hence cause an increase in their plasma concentration. These include azole antifungal agents: Ketoconazole and itraconazole.
- Other inhibitors of CYP3A: nefazodone, fluvoxamine, cimetidine, erythromycin.
- CNS Depressants.
- Oral Contraceptives.
- Other drugs: clinical studies also indicate a possible drug interaction of Alprazolam with the other drugs such as Isoniazid, diltiazem, macrolide antibiotics such as erythromycin and clarithromycin, and grapefruit juice; sertraline and paroxetine; ergotamine, nicardipine, amiodarone, nifedipine, and cyclosporine.
Xanax overdose can be mild to severe depending on how much of the drug is taken and if any other depressants have been taken. Overdose may include one or more of the following symptoms: somnolence (difficulty staying awake), dizziness, hypotension, impaired coordination, mental confusion, impaired motor functions, impaired balance, respiratory depression, impaired or absent reflexes, hypoventilation, coma, death.
That is prohibited to take alprazolam with alcohol or drugs. In case of emergency/overdose treatment should be taken: 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).