Alprazolam about

Disposition in the Body. Readily absorbed after oral administration and undergoes extensive metabolism. The major metabolites are a-hydroxyalprazolam (active) and a benzophenone derivative of alprazolam. About 80% of a dose is excreted in the urine in 72 hours of which 11% is unchanged drug, 15% is a-hydroxyalprazolam, and 9% is the benzophenone metabolite. 

Benzodiazepines, ie, the hiU BZR agonists, are prescribed for anxiety, insomnia, sedation, myorelaxation, and as anticonvulsants (97). Those benzodiazepines most commonly prescribed for the treatment of anxiety disorders are lorazepam (19), alprazolam (20), diazepam (21), bromazepam (22), chlorazepate (23), and oxazepam (24). These dmgs together represent about 70% of total... 

Adulteration, which can be accidental or deliberate, is another problem. Many herbal products have been found to contain prescription or OTC drugs and dangerous heavy metals. In 1998, for example, the California Department of Health reported that 32% of Asian herbal medicines sold in that state contained undeclared pharmaceuticals or heavy metals. A subsequent study of more than 500 Chinese herbal medicines found that about 10% of them contained undeclared drugs or toxic levels of metals. The FDA and other investigators have also detected sildenafil, colchicine, adrenal steroids, alprazolam, and other prescription drug ingredients in products claimed to contain only natural ingredients. 

The pharmacological effects of alprazolam do not differ appreciably from those of diazepam. However, alprazolam is about 10 times more potent than diazepam. 

Several open trials have reported significant improvement or remission of panic attacks in patients given clonazepam ( 60, 61, 62, 63, 64, 65 and 66). One double-blind, placebo-controlled study comparing the efficacy of alprazolam, clonazepam, and placebo found both drugs superior to placebo and comparable with each other (67). Because favorable response to clonazepam usually occurs early in treatment, lack of initial improvement may predict treatment failure ( 42, 61, 68). Interdose and morning rebound anxiety have not been reported. Clonazepam is not approved by the FDA for panic attacks, and because there are only a few controlled studies, there is only limited knowledge about its efficacy for this indication. 

Some naturally occurring neurotransmitters may be similar to drugs we use. For example, it is well known that the brain makes its own morphine (i.e., beta endorphin), and its own marijuana (i.e., anandamide). The brain may even make its own antidepressants, it own anxiolytics, and its own hallucinogens. Drugs often mimic the brain s natural neurotransmitters. Often, drugs are discovered prior to the natural neurotransmitter. Thus, we knew about morphine before the discovery of beta-endorphin marijuana before the discovery of cannabinoid receptors and anandamide the benzodiazepines diazepam (Valium) and alprazolam (Xanax) before the discovery of benzodiazepine receptors and the antidepressants amitriptyline (Elavil) and fluoxetine (Prozac) before the discovery of the serotonin transporter site. This un-... 

The results demonstrated some of the characteristics of UPLC-MS. Shorter retention times were observed, along with reduced chromatographic peak width. This in turn leads to less analyte dilution and improved S N. With the HPLC approach, the alprazolam peak is about 4.8 seconds wide (Fig. 1.18) and the same peak... 

First-trimester exposure appears to confer a small but definite increased risk (from a baseline of 0.06% up to 0.7%) of oral cleft in infants (27). However, second-generation effects are infrequent and usually reversible (28), although some doubt remains about the extent of developmental delay in children who have been exposed in utero (27). A review has emphasized that concerns about second-generation effects are mainly theoretical, and has concluded that some agents (for example chlor-diazepoxide) are probably safe during pregnancy and lactation and that others (for example alprazolam) are best avoided (29). 

FLUOXETINE, FLUVOXAMINE, PAROXETINE BZDs - ALPRAZOLAM, DIAZEPAM, MIDAZOLAM t in plasma concentrations of these BZDs. Likely t sedation and interference with psychomotor activity Alprazolam, diazepam and midazolam are subject to metabolism by CYP3A4. Fluvoxamine, fluoxetine and possibly paroxetine are inhibitors of CYP3A4 sertraline is a weak inhibitor. SSRIs are relatively weak compared with ketoconazole, which is possibly 100 times more potent as an inhibitor Warn patients about risks associated with activities that require alertness. Consider use of alternatives such as oxazepam, lorazepam and temazepam, which are metabolized by glucuronidation >- For signs and symptoms of CNS depression, see Clinical Features of Some Adverse Drug Interactions, Central nervous system depression... 

Alprazolam and alprazolam XR generally dosed about twice the dosage of clonazepam... 

The benzodiazepines and their active metabolites bind to plasma proteins. The extent of binding correlates strongly with Upid solubility and ranges from about 70% for alprazolam to nearly 99% for diazepam. The concentration in the cerebrospinal fluid is approximately equal to the concentration of free drug in plasma. Competition with other protein-bound drugs may occur, but no clinically significant examples have been reported. 

Tricyclic antidepressants Alprazolam has been found to increase imipramine and desipramine serum levels by about 25%. The mechanism is unknown. ... 

Which one of the following statements about the use of alprazolam in this patient is false ... 

CICLOSPORIN BZDs-ALPRAZOLAM, MIDAZOLAM, DIAZEPAM Likely t plasma concentrations and risk of t sedation These BZDs are metabolized primarily by CYP3A4, which is moderately inhibited by cidosporin Warn patients about t sedation. Consider using alternative drugs, e.g. ffurazepam, quazepam. Warn about activities requiring attention For signs and symptoms of CN5 depression, see Qinkal Features of Some Adverse Drug Interactions, Central nervous system depression... 

The male client diagnosed with a brain tumor tells the clinic nurse that he has been having seizures more frequently. The client is taking the anticonvulsant phenytoin (Dilantin), the narcotic morphine sulfate (Roxanol), the analgesic acetaminophen (Tylenol), and the antianxiety medication alprazolam (Xanax). Which question about the client s medications should the nurse ask next ... 

After oral administration, chlordiazepoxide, diazepam, lorazepam, halazepam, and alprazolam are rapidly and completely absorbed, with peak serum levels occurring at about 1 to 2 h. 

Ketoconazole. A study in healthy subjects found that ketoconazole 200 mg twice daily decreased the clearance of alprazolam 1 mg by about two-thirds, and prolonged its half-life fourfold, but the maximum serum levels remained unchanged. ... 

The interactions of nefazodone with alprazolam, midazolam, triazolam and zopiclone are established and clinically important. The practical consequences are that the effects of alprazolam, midazolam and triazolam are expected to be increased but the extent is uncertain. Be alert for any evidence of any psychomotor impairment, drowsiness etc. and reduce the benzodiazepine dosage if necessary. More study is needed. Lorazepam does not interact with nefazodone. There seems to be no direct information about other benzodiazepines and related drugs. 

The concurrent use of fluoxetine 60 mg daily has been found to reduce the clearance of alprazolam 1 mg four times daily by about 21% and to increase its plasma levels by about 30%. These changes were accompanied by increased psychomotor impairment. This appears to be due to reduced alprazolam metabolism. Another study also reported impaired alprazolam metabolism, considered to be due to the inhibition of cytochrome P450 isoenzyme CYP3A4 by fluoxetine, although no significant changes in alprazolam pharmacodynamics were found. ... 

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