Brand Name: Dormicum 15mg – Midazolam
Generic Name: Midazolam
Product Form: Tablets/Pills
Packing Details: Blisters
Buy Dormicum 15mg online – Midazolam manufactured by Roche in blister packing.
Contents – Midazolam – Description
Dormicum 15mg – Midazolam tablet contains midazolam maleate while the ampoule contains midazolam HCl.
Each ampoule also contains sodium chloride, hydrochloric acid, sodium hydroxide and water for injection as excipients.
Midazolam is 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4] benzodiazepine.
Short-acting benzodiazepine for premedication, sedation, induction and maintenance of anesthesia.
Tablet: Sleep-inducing agent.
Pharmacology Dormicum 15mg – Midazolam:
Midazolam has a very rapid sedative and sleep-inducing action of pronounced intensity. It also exerts an anxiolytic, an anticonvulsant and a muscle-relaxant effect.
Ampoule: Midazolam is a derivative of the imidazobenzodiazepine group. The free base is a lipophilic substance with low solubility in water.
The basic nitrogen in position 2 of the imidazobenzodiazepine ring system enables midazolam to form water-soluble salts with acids. These produce a stable and well-tolerated injection solution.
The pharmacological action of midazolam is characterized by rapid onset, and because of rapid metabolic transformation, short duration. Because of its low toxicity, midazolam has a wide therapeutic range.
After parenteral administration, anterograde amnesia of short duration occurs (the patient does not recall events that occurred during the peak of activity of the compound).
Tablet: Absorption: Dormicum is absorbed rapidly and completely after oral administration. Due to the first-pass effect, bioavailability is approximately 40%.
With a dose of 15 mg, a Cmax of 70-120 ng/mL is reached at Tmax 0.5-1.5 hrs.
Distribution: The concentrations in the plasma decrease in 2 phases with half-lives of 0.3-0.5 hrs (distribution phase) and 1.5-3.5 hrs (elimination phase). 96-98% of midazolam becomes bound to plasma proteins. The volume of distribution ranges from 0.7-1.2 L/kg.
Metabolism: Midazolam is rapidly and completely metabolized. 30-50% of the active ingredient is already metabolized in the course of the first passage through the liver.
The main pharmacologically active metabolite is α-hydroxy midazolam, the elimination half-life of which is shorter than that of the parent substance.
There is no accumulation of midazolam or its active metabolites on prolonged once-daily administration.
Elimination: Midazolam is eliminated via metabolism. The metabolites formed undergo conjugation with glucuronic acid and are eliminated as glucuronides via the kidneys.
Absorption After IM Injection: Absorption of midazolam from the muscle tissue is rapid and complete. Maximum plasma concentrations are reached within 30 min. Bioavailability is over 90%.
Distribution: When midazolam is injected IV, the plasma concentration-time curve shows 2 distinct phases of distribution. The volume of distribution calculated under steady-state conditions is 0.7-1.2 L/kg body weight. Studies show a protein-binding of 96-98%.
In animals and humans, midazolam has been shown to cross the placenta and to enter fetal circulation. Small quantities of midazolam are found in human milk.
Midazolam is metabolized rapidly and completely. The primary metabolite is a α-hydroxy-midazolam. The fraction of the dose extracted by liver has been estimated at 40-50%. Many medicaments have been found to inhibit the production of this metabolite in vitro. For some of these drugs, this has been confirmed in vivo (see Interactions).
In healthy volunteers, the elimination half-life is between 1.5 and 2.5 hrs. Plasma clearance is in the range of 300-400 mL/min. When midazolam is given by IV infusion, its elimination kinetics do not differ from those following bolus injection. The elimination half-life of the main metabolite, α-hydroxy-midazolam, is shorter than that of the parent substance. It is conjugated with glucuronic acid (inactivation).
The metabolites are renally excreted.
Pharmacokinetics in Special Clinical Situations: In adults >60 years, the elimination half-life may be prolonged up to 3 times and in some intensive-care patients requiring midazolam by IV infusion for long-term sedation, up to 6 times. In these patients, infusion at an unchanged rate results in higher plasma levels at steady state.
The elimination half-life may also be prolonged in patients with congestive heart failure and with reduced hepatic function.
In children (3-10 years), the elimination half-life is between 1 and 1.5 hrs.
In neonates, the half-life of elimination is prolonged with a mean of 6 hrs (3-12 hrs) due to liver immaturity.