How midazolam works
Midazolam is a so-called benzodiazepine. Benzodiazepines bind to the gamma-aminobutyric acid receptor (GABA receptor) in the central nervous system and enhance the effect of the natural messenger GABA. In this way, they have dose-dependent antianxiety (anxiolytic), sedative, muscle relaxant and anticonvulsant effects.
One of these messenger substances is GABA. It has an inhibitory effect on the nervous system as soon as it binds to its docking sites (receptors). Midazolam increases the likelihood that GABA will bind to its receptor, thus leading to the effects described at the beginning.
Absorption, degradation and excretion
When is midazolam used?
The indications for use (indications) of midazolam include:
- Sedation before surgical or diagnostic procedures
- Sedation in the intensive care unit (especially of ventilated patients)
- Induction of anesthesia
- Short-term treatment of sleep disorders
- Treatment of prolonged acute seizures
How midazolam is used
Normally, the dosage is between 7.5 and 15 milligrams of midazolam, and between 2.5 and 5 milligrams for infants and young children. Since the effect is relatively rapid, the drug should be administered about half an hour before the desired sedation.
For acute seizures, the oral solution is placed directly into the oral cavity between the gums and cheek.
What are the side effects of midazolam?
Repeated use may prolong the duration of action of midazolam.
What should be considered when using midazolam?
Contraindications
Midazolam must not be used in:
- severe respiratory diseases
- @ drug dependence
- Sleep apnea syndrome
- myasthenia gravis (autoimmune-mediated muscle weakness)
- severe liver dysfunction
Drug interactions
In particular, centrally acting drugs (such as psychotropic drugs, painkillers, sleeping pills, allergy medications) enhance the effects and side effects of midazolam. Simultaneous consumption of alcohol is strictly prohibited because the sedative effects reinforce each other.
Some substances slow down the degradation of the sedative by inhibiting the enzyme CYP3A4. As a result, they enhance the sedative effects of midazolam. These include:
- antifungals (such as ketoconazole, itraconazole)
- HIV medications (such as ritonavir)
- heart medicines (like diltiazem, verapamil)
- foods like grapefruit juice
Other drugs are able to increase the activity of CYP3A4. Midazolam is then broken down more quickly, which weakens its effect. Examples of such drugs are:
- Antiepileptic drugs (such as phenobarbital, phenytoin, carbamazepine).
- HIV medications (such as efavirenz)
- antibiotics (like rifampicin and rifabutin)
- Antidiabetic drugs (such as pioglitazone)
Driving ability and operation of heavy machinery
Midazolam significantly impairs the ability to react. Therefore, after ingestion, patients are advised against operating heavy machinery or actively participating in road traffic.
Addictive potential
Age restriction
Midazolam is approved from birth if indicated. The dosage is adjusted individually.
Pregnancy and lactation
The active substance may also be used during pregnancy for surgical procedures. To date, no cases have been reported in which this has caused damage to the unborn child.
Single doses during breastfeeding usually do not require a break from breastfeeding. For long-term treatment, the data are not sufficient to make an explicit recommendation.
In principle, preference should be given to primarily non-drug measures during pregnancy and breastfeeding.
How to obtain medication with midazolam
How long has midazolam been known?
Midazolam is a relatively young representative of the long-known group of benzodiazepines. The earlier generations of these sedatives were effective for a very long time. Midazolam, on the other hand, guarantees safe sedation that lasts for only about four hours.
