2819 Alprazolam Alprazolam is only found in individuals that have used or taken this drug. It is a triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of panic disorders, with or without agoraphobia, and in generalized anxiety disorders. (From AMA Drug Evaluations Annual, 1994, p238) Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABA_A) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. 28981-97-7 2118 C17H13ClN4 308.082870 White powder. 228-229.5°C 40 mg/L at pH 7; 12 mg/mL at pH 1.2 Oral. Readily absorbed from the gastrointestinal tract. Bioavailability is 80-90%. Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABA_A) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. Hepatic. Hydroxylated in the liver to &alpha;-hydroxyalprazolam, which is also active. This and other metabolites are later excreted in urine as glucuronides. Route of Elimination: Alprazolam and its metabolites are excreted primarily in the urine. Half Life: 6.3-26.9 hours LD50: 1020 mg/kg (Oral, mouse) No indication of carcinogenicity to humans (not listed by IARC). For the management of anxiety disorder or the short-term relief of symptoms of anxiety and for the treatment of panic disorder, with or without agoraphobia. They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive. Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time. As in all cases of drug overdosage, respiration, pulse rate, and blood pressure should be monitored. General supportive measures should be employed, along with immediate gastric lavage. Intravenous fluids should be administered and an adequate airway maintained. If hypotension occurs, it may be combated by the use of vasopressors. Dialysis is of limited value. Flumazenil, a specific benzodiazepine receptor antagonist, is indicated for the complete or partial reversal of the sedative effects of benzodiazepines and may be used in situations when an overdose with a benzodiazepine is known or suspected. (L1712) 2009-07-21T20:26:48Z 2014-12-24T20:25:51Z Alprazolam C06817 2611 Alprazolam DB00404 08H true CC1=NN=C2CN=C(C3=CC=CC=C3)C3=C(C=CC(Cl)=C3)N12 C17H13ClN4 InChI=1S/C17H13ClN4/c1-11-20-21-16-10-19-17(12-5-3-2-4-6-12)14-9-13(18)7-8-15(14)22(11)16/h2-9H,10H2,1H3 InChIKey=VREFGVBLTWBCJP-UHFFFAOYSA-N 308.765 308.082874143 Exogenous Solid 2.12 HMDB14548 CHEMBL661 2034 <p>Hester, J.B., Jr.; US. Patent 3,681,343; August 1,1972; assigned to The Upjohn Company. Hester, J.B., Jr.; US.Patent 3,781,289; December 25,1973;assigned to The Upjohn Company. Hester, J.B., Jr.; U S . Patent 3,709898; January 9,1973; assigned to The Upjohn Company.</p>