Pharmacology (Drug Profile Midazolam) Essay Example | Topics and Well Written Essays - 2750 words

Pharmacology (Drug Profile Midazolam) - Essay Example b) Oral administration is also done for short term treatment. This is done mainly for the insomnia patients. c) Midazolam is also indicted for the management of schizopernia. 3. Midazolam is found to interact with many drugs. The drug interaction is found to either increase the activity or decrease the activity of Midazoalm. The drug interaction occurs mainly with the antipsychotic medications, barbiturates, antibiotics and antifungal, cimetidine, Diltiazem, Narcotics, Seizure and Sleep medications, alcohol and antidepressant medicines such as Antipsychotic drugs include: Aripipraxole , asenapine, chlorpromazine, clozapine, fluphenazine, haloperidol, Iloperidone, loxapine, lurasidone, molindone, olanzapine, paliperidone and perphenazine and pimozide. Barbutarates include: Amobarbital, Butalbital, Pentobarbital and Secobarbital. Antibiotics such as Clarithomycin, Erythromycin, Isoniazid, Itraconazole , ketoconazole and Telithromycin. Narcotics such as morphine and oxycodone are used i n combination with Midazolam. (drugs.emedtv.com) The pharmacokinetic drug interactions are found to occur based on the enzymes involved in the metabolism. The drug interaction with the CNS depressants such as alcohols, opioids and barbiturates are found to have lethal, clinical and forensic consequences with midazolam. Many studies have found that this interaction results in death. (Mozayani and Raymon 2004). Similarly when analgesics are used along with the midazolam, they are found to have greater sedative effects. The gastrointestinal agents when combined with midazolam are found to increase the rate of absorption of the drug. Cimetidine when used along with Midazolam is found to increase the retention time of Midazolam in the body. Similarly the antifungal agents are also found to inhibit the movement of Midazolam from the body. 4. a) The mechanism of interaction of Midozolam is understood well. The main target of Midazolam is the GABAa receptor. This is an ionotropic receptor w ith gamma amino butyric acid as the endogenous ligand. When GABAa receptor is activated then it transmits Chloride ions through their pores and polarizes the neurons. This polarization results in the inhibition of the neurotransmission. The benzodiazepines binds to the receptor found between the alpha and gamma receptor subunits. The five subunits of GABA receptor are sensitive to benzodiazepine. When benzodiazepine binds to the alpha and the gamma subunits of the GABA receptor, and brings the receptor into its control. The binding brings out a change in the conformation of the GABA – alpha and makes them to open the chloride ion channel and this polarizes the membrane. This process inhibits the signal transduction pathway by arresting the GABA molecules and creating sedatory and anxiolytic effects to the human. (Sigel 2002). b. Midozolam is the substrate for the receptor GABA only. This is very specific in nature. It binds to the GABA receptors that are having only alpha and gamma subunits. The binding of benzodiazepine modifies the GABAs response by the receptor. As these receptors are found in the cerebral cortex region, limbic system, cerebellar cortex and spinal cord, its effect can be felt in many parts of the body. The two compartmental model enables the specificity of the molecule and increases the sensitivity. (Stoelting and Miller 2007) c.