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Benzodiazepines are an important class of bioactive molecules, widely used as an anxiolytic agent. Their pharmacological actions are mediated through specific receptors located in a supramolecular complex with gamma-aminobutyric acid (GABA) receptors. Benzodiazepines enhance GABA neurotransmission, thus indirectly changing the activity of other neurotransmitters such as serotonin and noradrenaline. Benzodiazepines are indicated for the short-term relief of anxiety that is severe, disabling, or subjecting the individual to unacceptable distress. The efficacy of benzodiazepines (particularly alprazolam - a high potency benzodiazepine-) in the treatment of panic disorder is well established. However, in generalized anxiety disorder, high drop-out rates due to adverse effects limit their effectiveness; in social phobia, little is known about their long-term affect; and they have uncertain efficacy in either acute or continuation treatment in post-traumatic stress disorder. Apart from their frequent use in anxiety disorders, benzodiazepines are widely prescribed for acutely disturbed patients (mania, schizophrenia, agitated depression, agitation in medical conditions), addiction (alcohol and opiate withdrawal), neurological disorders (epilepsy, muscular spasm, spasticity), and antidepressant or antipsychotic-induced side effects. Benzodiazepines are also frequently prescribed in the treatment of sleep disorders. However, they should only be used to treat insomnia when it is severe, disabling, or causing extreme distress. Only short-term (2-4 weeks) use is recommended. Since benzodiazepines may cause dependency, withdrawal needs to be gradual; a withdrawal syndrome may occur as long as 3 weeks after stopping the drug. Benzodiazepines also adversely impair the individual’s ability to operate machinery or drive. They may also, paradoxically, cause increased aggression and hostility. The key points for safe and effective use of benzodiazepines are, the careful selection of patients who might benefit from them, prescription of lower doses and in conjunction with an antidepressant, administration in clinical situations in which they are more likely to be beneficial, monitoring and managing their side-effects and minimizing the risk of withdrawal symptoms and relapse, mainly through tapering the dose and/or combining with effective psychological interventions.