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(Midazolam as HCL)
(Midazolam as HCL)
CNS depression /Sedation
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- IDAZOL 5MG/5ML INJECTION
Idazol also contains sodium chloride 9mg and sterile water for injection as excipients. Midazolam is 8-chloro-6-(2-flurophenyl)-1-methyl-4H-imidazo[1,5-a][1×4] benzodiazepine.
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.
Anesthetic use in premedication, induction and maintenance of general anesthesia, sedation in diagnostic procedure and local anesthetic (endoscopy, bronchoscopy).
Standard Dosage and Mode of Administration: In the case of elderly patients with organic cerebral changes or impaired cardiac and respiratory function, the dosage should be determined with caution, the special factors relating to each patient being taken into consideration.
IV injections must be given slowly (approximately 2.5mg in 10 sec for induction of anesthesia and 1mg in 30 sec for basal sedation). The drug takes effect about 2 min after the injection is started.
PREMEDICATION BEFORE AN OPERATION:
IV: For Sedation in Diagnostic or Surgical Interventions Carried Out Under Local Anesthesia: The initial dose is 2.5mg 5-10 min before the beginning of the operation. Further doses of 1mg may be given as necessary. In cases of severe illness, particularly if the patient is in poor general oral condition or of advanced age, the initial dose must be reduced to 1-1.5mg.
IM: Patients Suffering from Pain Before an Intervention: Administration alone or in combination with anticholinergics and possibly analgesics.
INDUCTION OF ANESTHESIA:
IV: As an induction agent in inhalation anesthesia or a sleep-inducing component in combined anesthesia.
The dose is 10-15mg IV. A Sufficiently deep level of sleep is generally achieved after 2-3 min.
MAINTENANCE OF ANESTHESIA:
IV: For maintenance of the desired level of unconsciousness, further small doses should be injected IV. The dose and the intervals between doses vary according to the individual reaction of the patient.
When idazol is given with potent analgesics, the latter should be administered first so that the sedative effects of idazol can be safely titrated on top of any sedation caused by the analgesic.
The effects of overdoses can be vary well controlled with the benzodiazepine antagonist.
Patients who are hypersensitive to benzodiazepines. Patients with history of acute narrow glaucoma.
USE IN CHILDERN:
Idazol is also contraindicated in premature infants.
Particular care is needed when administering idazol to a patient with myasthenia gravis, owing to preexisting muscle weakness, insomnia in psychosis, organic brain damage, can cause dependence and withdrawal symptoms.
After receiving idazol parenterally, patients should not be discharged from hospital or consulting room for at least 3 hours and then only if accompanied by an attendant.
Effects on the Ability to Drive or Operate Machinery:
Patients should be warned not to drive a vehicle or operate a machine for at least 12 hrs.
Use in pregnancy:
idazol, like any other drug, should not be used in the first 3 months of pregnancy unless considered absolutely necessary by the physician.
Use in the elderly:
Caution should be exercised when administering idazol parenterally to elderly patients or patients with impaired cardiac and respiratory function.
ADVERSE DRUG REACTIONS:
Idazol is well tolerated. Changes in arterial blood pressure, pulse rate and breathing are usually slight. As a rule, the systolic blood pressure falls by a maximum of 15% while the pulse rate simultaneously shows a corresponding rise.
Nausea, vomiting, headache, hiccoughs, laryngospasm, dyspnea, hallucination, ataxia, skin rash, paradoxical reactions and amnesic episodes may also occur in elderly patients and those with preexisting respiratory insufficiency, particularly when the injection is given too rapidly or when a high dosage is administered. Therefore, idazol ampoules should only be used when resuscitation facilities are available.
Idazol enhances the central sedative effect of neuroleptics, tranquilizers, antidepressants, sleep-inducing drugs, analgesics and anesthetics. This potentiation can be advantage therapeutically in certain cases. Special attention must be paid to the possibility of potentiation in patients at particular risk. In some cases, the mutual potentiation of alcohol and idazol can produce unforeseeable reactions. No alcoholic beverages should be allowed for at least 12 hrs after parenteral administration. Potentiation occurs with concomitant use of erythromycin, ketoconazole, itraconazole, diltiazem, verapamil, cimetidine and hepatic enzyme inhibitors.
There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
MECHANISM OF ACTION:
Short-acting, sleep-inducing agent for premedication as well as for induction and maintenance of anesthesia.
idazol is characterized by rapid onset and because of rapid metabolic inactivation, short duration of action. Because of its very low toxicity, idazol has a wide therapeutic range.
Idazol has a very rapid sedative and sleep-inducing action of pronounced intensity. It also exerts an anticonvulsant and a muscle-relaxant effect. After IM or IV administration, anterograde amnesia of short duration occurs (the patient does not recall events that occurred during the peak of activity of the compound).
Absorption After IM Injection: Absorption of midazolam from the muscle tissue is rapid and complete.
Bioavailability is >90%.
ABSORPTION AFTER RECTAL ADMINISTRATION:
Midazolam is absorbed quickly. Maximum concentration is reached within 30 min. In children, the area under the plasma concentration-time curve (AUC) after rectal administration is comparable to the AUC of adults.
Midazolam is completely metabolized in the body. The primary metabolite is hydroxy midazolam, which can be traced in the plasma. Its half-life is shorter than that of the parent substance. Immediately after its formation, it is conjugated with glucuronic acid (inactivation) and 60-70% of the dose is then eliminated by the kidneys.
DISTRIBUTION AND ELIMINATION:
When idazol is injected IV, the time course of the plasma concentration shows 2 distinct phases of distribution as well as the elimination phase. The fraction extracted by the liver is 40-50% and plasma clearance is in the range of 300-400 mL/min. The volume of distribution calculated under steady-state conditions is 50-60L. Ninety-five percent of midazolam becomes bound to plasma proteins. The elimination half-life is between 1½ and 2½ hrs.
Ampoule 5mg/5 mL x 5’s.