Midazolam
When ATH:
N05CD08
Characteristic.
Hypnotic from the group of benzodiazepines.
Midazolam - white or slightly yellow crystalline solid, water-insoluble. Midazolama hydrochloride is soluble in water.
Pharmacological action.
Snotvornoe, sedation.
Application.
Insomnia (violation of falling asleep and / or waking up early) - Inside, premedication before diagnostic and surgical procedures (inside, / m), long-term sedation in intensive care (/ m), induction of anesthesia during inhalation anesthesia or sedative in combined anesthesia (I /), ataralgesia children (V / m in combination with ketamine).
Contraindications.
Hypersensitivity, Sleep disorders in psychosis and severe depression, myasthenia, pregnancy (I trimester), delivery, lactation, childhood (orally).
Restrictions apply.
Organic brain damage, cardiac and / or respiratory and / or liver failure, sleep apnea, pregnancy (II and III trimester), childhood (for induction).
Pregnancy and breast-feeding.
Contraindicated in the I trimester of pregnancy and during labor. In II and III trimester of possible, if the effect of therapy outweighs the potential risk to the fetus.
Category actions result in FDA - D. (There is evidence of the risk of adverse effects of drugs on the human fetus, obtained in research or practice, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk, if the drug is needed in life-threatening situations or severe disease, when safer agents should not be used or are ineffective.)
At the time of treatment should stop breastfeeding.
Side effects.
Inside, parenterally.
From the nervous system and sensory organs: drowsiness, slackness, muscular weakness, blunting of emotions, reaction speed, headache, dizziness, ataxia, diplopia, anterogradnaya amnesia (dozozavisimaya), paradoxical reactions (ažitaciâ, psychomotor agitation, aggressiveness, etc..).
Other: dyspepsia, skin reactions, Local reactions (erythema and pain at the injection site, tromboflebit, thrombosis).
Perhaps the development of tolerance, Drug Dependence, withdrawal, the phenomenon of "return" (cm. Precautions).
For parenteral administration: reduction of tidal volume and / or respiratory rate (in 23,3% patients after / in and 10,8% After the / m), temporary cessation of breathing (in 15,4% patients after the on / in the) and / or heart, sometimes leading to fatal — effects are mostly and there are doses in elderly patients with chronic diseases together with the use of Narcotic analgesics, as well as rapid on / in; laringospazm, breathlessness; excessively severe sedation, convulsions (in premature and newborn), abstinence symptom (when a sudden cancellation of a long / in use); vasodilation, low blood pressure, tachycardia; nausea, vomiting, Ikotech, constipation; Allergic, incl. Skin (rash, hives, itch) and anaphylactoid reactions.
Cooperation.
Potentiates the effects of tranquillizers, Antidepressants, other hypnotics, analgesics, anesthetics, neuroleptics, narcotic drugs, alcohol (mutually). A solution of midazolam is incompatible in the same syringe with alkaline solutions. In / in the introduction of midazolam decreases the minimum alveolar concentration of halothane, need for general anesthesia. / M administration of midazolam in premedication may necessitate dose reduction of thiopental sodium 15%.
Itraconazole, fluconazole, Erythromycin, saquinavir uvelichivayut T1/2 midazolama, administered parenterally (the appointment of high doses of midazolam and conducting long-term induction is necessary to decrease the dose). Systemic effects of midazolam increase inhibitors of CYP3A4: ketoconazole, itraconazole and fluconazole (co-administration is not recommended), Erythromycin, saquinavir, diltiazem and verapamil (It requires co-administration of midazolam in the dose reduction 50% and more), roksitromitsin, azithromycin, cimetidine and ranitidine (a clinically significant interaction unlikely). Индукторы изофермента CYP3A4 (Carbamazepine, phenytoin, rifampicin) reduce the systemic effects of midazolam (ingestion) and determine the need to increase its doses.
Overdose.
Symptoms: muscular weakness, slackness, confusion, paradoxical reactions, amnesia, deep sleep; at very high doses is respiratory depression and cardiac activity, apnea, areflexia, coma.
Treatment: induction of vomiting and the appointment of activated carbon (If the patient is conscious), Gastric lavage through a tube (If the patient is unconscious), IVL, maintaining the cardiovascular system. The introduction of a specific antidote - benzodiazepine receptor antagonist flumazenil (in hospital).
Dosing and Administration.
Inside, / m, I /, rectally. The dose should be selected individually, cancel mode for the treatment of sleep disorders Individual.
When sleep disorders: adult, inside (without chewing, with some liquid), just before bedtime, the average dose of 7.5-15 mg once. The course of treatment should be short-lived (several days, maximum — 2 Sun). Elderly and debilitated patients, as well as in patients with impaired liver treatment should start with the lowest dose.
In anesthesiology and intensive care: adults and children-in/m, I / (slowly), rectally (for sedation in children), inside (for sedation in adults, if not shown / m). Dosage regimen (introduction rate, the dose) selected strictly individually depending on indications, the physical condition and age of the patient, as well as receive medical treatment. In patients at high risk, incl. senior 60 years, loose or patients with chronic diseases using smaller doses.
Precautions.
In / in the introduction should be undertaken only in hospitals if resuscitation equipment, as well as training of personnel for its use (Because of the possibility of oppression contractile function of the myocardium and respiratory arrest).
After injecting patients should be monitored at least 3 no. It will be appreciated, that too rapid in / introduction (especially in children with an unstable state of the cardiovascular system and in newborns) may cause apnea, gipotenziю, ʙradikardiju, cardiac arrest or breathing.
The development of paradoxical reactions occur most often in children and the sick elderly.
Use caution when driving, and when performing work, require high concentration and fine motor coordination, within one day after application of midazolam.
Do not take alcoholic beverages, as well as to use other means of, cause CNS depression, during 24 h after administration of Midazolam.
With repeated use for a few weeks may cause addiction (hypnotic effect may be somewhat weakened), as well as drug dependence, incl. at the therapeutic doses. In a dramatic treatment, you may experience withdrawal symptoms (headache and muscle pain, alarm, voltage, in severe cases, depersonalization, hallucinations et al.), as well as the development of the phenomenon of "impact" is a temporary reinforcement of the initial symptoms (insomnia).
