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Alprazolam


Alprazolam is a drug which is a benzodiazepine derivative. It is classified as short-acting, and is used to treat anxiety disorders and insomnia.
Alprazolam Drug

Pharmacology


Alprazolam is a triazolobenzodiazepine, that is, a benzodiazepine with a triazolo-ring attached to its structure. Alprazolam binds to the GABAA subtype of the GABA receptor, increasing inhibitory effects of GABA within the central nervous system. The binding site for benzodiazepines is distinct from the binding site for GABA on the GABA receptor.


Unlike other benzodiazepines, alprazolam may also have some antidepressant activity, although clinical evidence of this is lacking.
Pharmacokinetics
The mechanism of action is not fully understood; However, Alprazolam is readily absorbed from the gastrointestinal tract. The peak plasma concentration is achieved in 1-2 hours. Most of the drug is bound to plasma protein, mainly albumin. Alprazolam is hydroxylated in the liver to α-hydroxyalprazolam, which is also pharmacologically active. This and other metabolites are later excreted in urine as glucuronides. Some of the drug is also excreted in unchanged form.

Indications
The main medical uses for alprazolam include:

Treatment of panic disorder, with or without agoraphobia.
Alprazolam is very effective in preventing panic attacks. However, despite its efficacy, many psychiatrists are reluctant to use alprazolam for this condition because of the possibility of dependence and interdose anxiety due to its short-acting nature. An extended-release formulation of alprazolam known as Xanax XR® was introduced in 2001 and is often preferred.
Treatment of panic attacks.
Alprazolam is taken as needed (PRN); 4 to 6 doses per month are the acceptable limit. If dependence seems to develop and/or the limit is exceeded, therapy may be reconsidered and/or discontinued.
Long-term treatment of severe generalized anxiety disorders.
Alprazolam may be used for long-term treatment of anxiety if other therapies either do not work or are contraindicated. Duration of therapy in this case is often four months or longer. The decision to use alprazolam for this purpose must be carefully made by a specialized psychiatrist, taking into account the individual's suffering, quality of life, loss of social performance and risk of dependence.
Adjunctive treatment of depression.
Alprazolam is sometimes used together with SSRIs such as paroxetine, sertraline, or fluoxetine to alleviate initial SSRI-induced anxiety while waiting for the antidepressant to begin working. However, clinical experience has shown that SSRIs may actually provoke panic attacks in otherwise healthy individuals, and cause sexual dysfunction. In these cases, a tricyclic antidepressant may be used instead. Buspirone may also be useful in conjunction with alprazolam in cases of generalized anxiety disorder.
Other uses.
Alprazolam may be used by specialists to treat severe cases of Borderline Personality Disorder. Some studies have shown positive results.

Availability
Alprazolam is generally sold in generic form in the United States. It is also sold under many other brand names, depending on the country:

Xanax® - United States, Australia, United Kingdom, Turkey, Portugal, Ireland, Greece
Xanax XR® - (an extended release formulation) United States
Niravam® - (formulary that dissolves on the tongue) United States
Apo-Alpraz® - Canada (also made by other companies under different names)
Xanor® - Finland, Philippines, South Africa, Sweden, Norway, Austria
Kalma® - Australia, New Zealand
Ralozam® - Australia, New Zealand
Zamhexal® - Australia
Alplax® - Argentina
Alviz® - Indonesia
Alzolam® - India, Malaysia
Alprax® - India
Tranax® - India
Restyl® - Bahrain, Cyprus, Egypt, Iran, Iraq, Jordan, Kuwait, Lebanon, Libya, Oman, Qatar, Republic of Yemen, Saudi Arabia, Syria, United Arab Emirates
Tranquinal® - Ecuador, Peru
Trankimazin® - Spain
Tafil® - Costa Rica, Denmark, El Salvador, Germany, Guatemala, Honduras, Mexico, Nicaragua, Panama, Venezuela
Tafil AP® - (an extended release formulation) Mexico
Constan® - Japan
Solanax® - Japan
Zolarem® - Bahrain, Benin, Burkina-Faso, Cyprus, Egypt, Ethiopia, Gambia, Ghana, Guinea, Iran, Iraq, Israel, Ivory Coast, Jordan, Kenya, Kuwait, Lebanon, Liberia, Libya, Malawi, Mali, Mauritania, Mauritius, Morocco, Niger, Nigeria, Oman, Qatar, Republic of Yemen, Saudi Arabia, Senegal, Seychelles, Sierra-Leone, South Africa, Sudan, Syria, Tanzania, Tunia, Uganda, United Arab Emirates, Zambia, Zimbabwe
Zoldac® - Benin, Burkina-Faso, Ethiopia, Gambia, Ghana, Guinea, India, Ivory Coast, Kenya, Liberia, Malawi, Mali, Mauritania, Mauritius, Morocco, Niger, Nigeria, Senegal, Seychelles, Sierra-Leone, South Africa, Sudan, Tanzania, Tunia, Uganda, Zambia, Zimbabwe
Calmax® - Ireland
Frontin® - Slovakia and possibly other European countries

Side effects

Common side effects of alprazolam can include:

Somnolence (drowsiness)
Impaired motor functions
Dizziness
Clumsiness
Less common side effects can include:

Fatigue
Headache
Rare side effects can include:

Sleep apnea
Hypoventilation (Respiratory depression)
Blurred vision
Difficulty in depth perception
Slurred speech or dysarthria
Changes in personality
Confusion
Disorientation
Amnesia (memory impairment)
Vivid dreams and/or nightmares
Jaundice
Tachycardia
Bradycardia
Changes in plasma cortisol and ACTH levels
Blood dyscrasias
Decreased salivation
Increased salivation
Diarrhea
Constipation
Nausea
Elevated hepatic (liver) enzymes
Incontinence
Rare paradoxical side effects can include:

Nervousness
Anxiety
Agitation
Rage
Insomnia
Muscle spasms and rigidity
Long-term treatment with alprazolam may lead to physical and/or psychological dependence. Users often develop a tolerance to the drug's sedative effects, although its anxiolytic efficacy remains intact.

There is now a general consensus among many psychiatrists that alprazolam (a so-called 'high-potency' benzodiazepine) poses a particularly high risk for misuse, abuse and dependence. Withdrawal after long-term treatment should be done slowly over a period of weeks (or even months) to avoid serious withdrawal symptoms such as agitation, rebound anxiety, muscle cramps and seizures. Some patients may benefit from a substitution with diazepam.

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