Midazolam is among the best-known sedatives. The active ingredient, which is available by prescription, belongs to the group of benzodiazepines.
What is midazolam?
Midazolam is among the best-known sedatives. Midazolam is a hypnotic or sedative that belongs to the group of short-acting benzodiazepines. The name ‘midazolam’ is derived from ‘imidazole’, a heretocyclic organic compound. Midazolam is considered a relatively new sedative. While benzodiazepines of earlier generations had a long-lasting efficacy, midazolam stands for a safe mode of action whose duration is only about four hours. The reason for this is its breakdown within the body, which proceeds more rapidly than with its predecessors. The sedative has been used in Europe since the early 1980s. In this context, it is often used as a short-acting preparation to treat states of restlessness.
Pharmacologic action
Within the human nervous system, there are different neurotransmitters. These are messenger substances with inhibitory or activating effects. In humans, there is a balance among neurotransmitters that results in goal-directed actions in response to external circumstances such as fear, stress, or rest. The neurotransmitter GABA (gamma-aminobutyric acid) has a braking effect on the nervous system after binding to the corresponding receptors. By taking midazolam, the effect of GABA can be enhanced. This in turn results in relaxation of the muscles and a pronounced sedative effect. In addition, the drug promotes the patient’s sleep and reduces anxiety and convulsions. Because midazolam is rapidly broken down in the body, its duration of action is limited. If the drug is injected into a blood vessel or muscle, the patient suffers a brief loss of memory. As a result, the treated person cannot remember things that happen during the peak effect of midazolam. After taking midazolam, which is usually done orally, the drug enters the intestine after a short time. From there, it passes into the blood. Once the active substance has been distributed within the organism, it is broken down in the liver. Through the kidneys, the degradation products of the drug get out of the body again.
Medical use and application
Midazolam is used in both adults and children to put them to sleep for short periods of time. It also relieves pain and immobilizes patients before a surgical procedure performed for therapeutic or diagnostic purposes. Furthermore, midazolam is suitable as a sedative agent in intensive care units. In the context of anesthesia, midazolam is used in the preparation and induction of anesthesia in the case of combined anesthesia. In children, the drug is not used for induction of anesthesia, but it is used as an anesthetic. The use of midazolam is considered useful in babies and children for the treatment of acute and prolonged convulsions. Furthermore, the sedative is administered for short-term treatment of sleep disorders. Midazolam is usually taken in the form of tablets. Alternatively, the drug can be injected directly into the bloodstream or administered rectally. The normal dose is between 7.5 and 15 milligrams of midazolam. Because of its short-acting nature, it is recommended that the drug be taken about 30 minutes before the desired sedative effect. For example, tablets are administered just before bedtime. To avoid withdrawal symptoms from the use of midazolam, a gradual discontinuation of the sedative is recommended after prolonged therapy. Since midazolam is a prescription medication, treatment with the drug is controlled by a doctor. The latter prescribes the drug to the patient, who obtains it by presenting a prescription at the pharmacy.
Risks and side effects
Taking midazolam may cause unwanted side effects in some patients. In most cases, these are allergic reactions, hypersensitivity, agitation, confusion, muscle tremors, hallucinations, aggression, and hostility.Furthermore, dizziness, temporary memory loss, headaches, gait unsteadiness, low blood pressure, a slowing of the heartbeat, withdrawal cramps, inflammation of the veins, dilated blood vessels, hiccups, itching, hives, constipation, nausea, vomiting, fatigue, reddened skin, dry mouth and respiratory dysfunction are conceivable. In the worst cases, respiratory or cardiac arrest may occur. In babies, convulsions are within the realm of possibility. Midazolam should not be administered if the patient suffers from hypersensitivity to the drug or other benzodiazepines. Other contraindications include acute respiratory failure, severe respiratory dysfunction, and the nerve disease myasthenia gravis. The same applies to people who have significantly impaired liver function. Tight control is required with midazolam therapy if the patient is older than 60 years or if poor general health prevails. Caution should also be exercised in people with a history of alcohol or drug abuse. They may become rapidly addicted to midazolam as a result of taking it. Use of midazolam in pregnant and lactating women is not recommended. Better alternatives are available for them. The use of midazolam and other drugs can sometimes cause interactions. For example, the degradation of the drug by antifungal agents is inhibited, which leads to a significant increase in effect. Itraconazole, fluconazole, posaconazole, voriconazole and ketoconazole are considered to be of particular concern. For the same reasons, the AIDS drug saquinavir, the calcium channel blockers diltiazem and verapamil, and the macrolide antibiotics clarithromycin and erythromycin should not be taken.
