Registered South Africa · SAHPRA

ZOLAMID 50 mg/10 ml

Midazolam

A40/2.2/0056 nervous system INN generic

What it does

Midazolam is a medication that belongs to the benzodiazepine class, often used to help with sedation and anxiety.

Commonly used for: anxiety, sedation, severe agitation

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Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.

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Answers come only from this medicine's registration record, BNF monograph and interaction data - not medical advice.

Medicine sourcing is available in Kenya only. We don't sell or dispense medicines - licensed pharmacies do.

Sourcing - Kenya only

Registration & product details

Registration no.
A40/2.2/0056
Registration date
2005/09/23
Expiry date
-
Status
Registered
Active ingredient
Midazolam
Dosage form
-
Strength
-
Pack size
-
Therapeutic class
-
ATC class (WHO)
N05CD - Benzodiazepine derivatives
Drug group
NERVOUS SYSTEM
RxNorm RxCUI
6960
Manufacturer / MAH
-
Applicant / LTR
Dezzo Trading 392 (Pty) Ltd
Country of origin
-

Source: South African Health Products Regulatory Authority · fetched 2026-04-15 21:15:24 · updated 2026-09-16 04:00:21

Drug Interactions

78
Check interactions

Pharmacodynamic Warnings

Midazolam appears in TABLE 11: Drugs with CNS depressant effects

Severe (11)

Benzodiazepines - increases exposure

Cobicistat moderately increases the exposure to benzodiazepines (alprazolam). Avoid.

Severe Study

Benzodiazepines - increases exposure

Ritonavir is predicted to increase the exposure to benzodiazepines (diazepam, flurazepam). Avoid.

Severe Theoretical

Benzodiazepines - increases exposure

Idelalisib moderately increases the exposure to benzodiazepines (alprazolam). Avoid.

Severe Study

Benzodiazepines - decreases exposure

Lorlatinib moderately decreases the exposure to benzodiazepines (midazolam). Avoid.

Severe Study

Benzodiazepines - decreases exposure

Lumacaftor is predicted to decrease the exposure to benzodiazepines (midazolam). Avoid.

Severe Theoretical

Moderate (38)

Benzodiazepines - increases exposure

Miconazole is predicted to increase the exposure to benzodiazepines (alprazolam). Use with caution and adjust dose.

Moderate Theoretical

Benzodiazepines - decreases exposure

Monoclonal antibodies (tocilizumab) are predicted to decrease the exposure to benzodiazepines (alprazolam, diazepam, midazolam). Monitor and adjust dose.

Moderate Theoretical

Benzodiazepines - increases exposure

Berotralstat moderately increases the exposure to benzodiazepines (midazolam). Monitor and adjust dose.

Moderate Study

Benzodiazepines - increases concentration

Cenobamate might increase the concentration of benzodiazepines (clobazam). Monitor and adjust dose. Also see TABLE 11 p. 1519.

Moderate Theoretical

Benzodiazepines - decreases exposure

Cenobamatemoderatelydecreasestheexposureto benzodiazepines(midazolam).Adjustdose.oStudy → AlsoseeTABLE11p.1519

Moderate Study

Unknown (29)

Benzodiazepines - decreases exposure

Apalutamide is predicted to decrease the exposure to benzodiazepines (diazepam). Avoid or monitor.

Unknown Study

Benzodiazepines - increases exposure

Dronedarone is predicted to increase the exposure to benzodiazepines (alprazolam).

Unknown Study

Benzodiazepines - increases concentration

Stiripentol increases the concentration of benzodiazepines (clobazam).

Unknown Study

Benzodiazepines - increases exposure

Antifungals, azoles (fluconazole, isavuconazole, posaconazole) are predicted to increase the exposure to benzodiazepines (alprazolam).

Unknown Study

Benzodiazepines - increases exposure

Bulevirtideslightlyincreasestheexposuretobenzodiazepines (midazolam).oTheoretical

Unknown Theoretical

Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: class

Disclaimer: This information is sourced from South African Health Products Regulatory Authority (South Africa). Always consult a qualified healthcare professional before using any medication.

About this medicine

Midazolam is a medication that belongs to the benzodiazepine class, often used to help with sedation and anxiety.

What it treats

  • anxiety
  • sedation
  • severe agitation

How it works

It works by calming the brain and nervous system, making you feel more relaxed.

Who it's for

This medication is for adults and children who need help with anxiety or sedation during medical procedures.

Drug class

Benzodiazepines

Cautions

  • • Be careful if you are taking other medications that can cause drowsiness or sedation.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

Clinical monograph: Midazolam

BNF-referenced

Midazolam is a short-acting benzodiazepine used primarily for its sedative, anxiolytic, amnestic, and muscle relaxant properties. It is commonly utilized in the management of status epilepticus, for sedation during procedures, and in intensive care settings. The drug acts on the central nervous system to produce calming effects, making it valuable in both emergency and elective medical situations.

Indications

  • Status epilepticus
  • Febrile convulsions
  • Sedation in intensive care
  • Conscious sedation for procedures
  • Preoperative sedation

Dosage

Adults: Initially 20-40 mg/24 hours for continuous infusion in status epilepticus, with adjustments based on response. For sedation, 2-2.5 mg administered slowly intravenously 5-10 minutes before the procedure; total usual dose is 3.5-5 mg, not exceeding 7.5 mg per course.

Mechanism of action

Midazolam enhances the activity of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) by binding to the benzodiazepine site on GABA-A receptors. This action increases the frequency of chloride channel opening, leading to hyperpolarization of neurons, which results in the sedative, anxiolytic, and muscle relaxant effects characteristic of benzodiazepines.

Pharmacodynamics

Midazolam exhibits a range of pharmacodynamic effects typical of benzodiazepines, including sedation, anxiolysis, muscle relaxation, and amnesia. After intramuscular administration, sedation onset occurs within 15 minutes, with peak effects observed between 30 to 60 minutes. Pediatric patients experience a quicker onset, with effects beginning within 5 minutes and peaking at around 15-30 minutes. The drug's ability to enhance GABA activity makes it effective in treating anxiety disorders, epilepsy, insomnia, and spasticity.

Pharmacokinetics

Midazolam is rapidly absorbed and has a short half-life, typically ranging from 1 to 4 hours. It undergoes extensive hepatic metabolism, primarily via cytochrome P450 3A4, resulting in active metabolites. The drug is excreted mainly through the urine. Dose adjustments may be necessary in patients with renal or hepatic impairment, as these conditions can affect drug clearance.

Contra-indications

  • Hypersensitivity to midazolam or other benzodiazepines
  • Acute narrow-angle glaucoma
  • Severe respiratory insufficiency
  • Sleep apnea syndrome

Adverse effects

  • Drowsiness
  • Dizziness
  • Confusion
  • Amnesia
  • Respiratory depression
  • Hypotension
  • Paradoxical reactions (e.g., agitation, increased muscle spasticity)
  • Nausea
  • Vomiting

Interactions

  • lumacaftor: severe decrease in exposure
  • efavirenz: severe effects on midazolam
  • dronedarone: moderate increase in exposure
  • miconazole: moderate increase in exposure
  • antifungals (azoles): moderate increase in exposure
  • berotralstat: moderate increase in exposure
  • cenobamate: moderate decrease in exposure
  • crizotinib: moderate increase in exposure
  • dabrafenib: moderate decrease in exposure
  • fedratinib: moderate increase in exposure

Precautions

  • Use with caution in elderly or debilitated patients
  • Risk of respiratory depression in patients with pre-existing respiratory conditions
  • Monitor for paradoxical reactions
  • Adjust dosage in renal impairment
  • Avoid concomitant use with other CNS depressants unless under medical supervision

Pregnancy

Midazolam is classified as a category D drug. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Midazolam is excreted in breast milk; use should be avoided if possible during breastfeeding.

Storage

Store at room temperature, away from light and moisture. Keep out of reach of children.

Formulations

  • Oral solution
  • Injectable solution
  • Tablet form
BNF 85 (British National Formulary) p.395 BNF for Children 2019-2020 p.251 PubChem / pathway

AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.

Molecular reference: Midazolam

PubChem CID 4192

Molecular formula: C18H13ClFN3

Mechanism of action

The actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the central nervous system. Benzodiazepines increase the activity of GABA, thereby producing a sedating effect, relaxing skeletal muscles, and inducing sleep, anesthesia, and amnesia. Benzodiazepines bind to the benzodiazepine site on GABA-A receptors, which potentiates the effects of GABA by increasing the frequency of chloride channel opening. These receptors have been identified in different body tissues including the heart and skeletal muscle, although mainly appear to be present in the central nervous system. Midazolam has neurotoxic properties when administered neuraxially in vivo. Furthermore, midazolam induces neurodegeneration in neonatal animal models in combination with other general anesthetics. Therefore, this study focuses on the mechanism of neurotoxicity by midazolam in neuronal and nonneuronal cells. The study aims to evaluate the apoptotic pathway and to investigate the protective effects of the benzodiazepine antagonist flumazenil and the caspase inhibitor N-(2-quinolyl)valyl-aspartyl-(2,6-difluorophenoxy)-methylketone. The apoptosis-inducing effect of preservative-free midazolam on human lymphoma and neuroblastoma cell lines was evaluated using flow cytometric analysis of early apoptotic stages (annexin V/7AAD) and caspase 3 activation. B-cell lymphoma (Bcl2) protein overexpressing and caspase 9-deficient lymphoma cells were used to determine the role of the mitochondrial (intrinsic) pathway. Caspase 8-deficient and Fas-associated protein with death domain (FADD)-deficient cells were used to evaluate the death receptor (extrinsic) pathway. The protective effects of flumazenil and the caspase inhibitor N-(2-quinolyl)valyl-aspartyl-(2,6-difluorophenoxy)-methylketone were investigated in neuroblastoma cells and primary rat neurons using metabolic activity assays (2,3-bis(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide) and immunofluorescence microscopy. Midazolam induced apoptosis in all investigated cell types in a concentration-dependent manner, indicated by flow cytometry. Bcl2-overexpression and caspase 9 deficiency protected against toxicity, whereas caspase 8 or FADD deficiency had no effect. Pancaspase inhibition had a strong protective effect, whereas flumazenil did not inhibit midazolam-induced apoptosis. Midazolam induces apoptosis via activation of the mitochondrial pathway in a concentration-dependent manner. The mechanism of midazolam toxicity switches from caspase-dependent apoptosis to necrosis with increasing concentrations. The induction of apoptosis and necrosis by midazolam is presumably unrelated to GABAA receptor pathway signaling. A consummatory conflict procedure that involves an abrupt reduction in magnitude of an expected reward (negative contrast) has been shown to be particularly sensitive to the effects of anxiolytic agents. Midazolam released suppressed consummatory performance in a dose-dependent manner. This effect was not due to a general appetite stimulation effect of the drug. The effects of three 5-HT antagonists on negative contrast were examined to evaluate the role serotonin may play in the anxiolytic action of benzodiazepine. Methysergide was found to be ineffective, cinanserin tended to reduce contrast at two intermediate doses, and cyproheptadine eliminated the contrast effect in a similar fashion as midazolam. The effectiveness of cyproheptadine may not be attributed to its anticholinergic or antihistaminergic actions since scopolamine and pyrilamine did not produce similar efects. The results are discussed in terms of the role serotonin may play in the anti-conflict action of benzodiaepine, as well as possible interactional effects of gamma-aminobutyric acid. The exact sites and mode of action of the benzodiazepines have not been fully elucidated, but the effects

Pharmacodynamics

**General effects** Midazolam is a short-acting benzodiazepine central nervous system (CNS) depressant. Pharmacodynamic properties of midazolam and its metabolites, which are similar to those of other benzodiazepine drugs, include sedative, anxiolytic, amnestic, muscle relaxant, as well as hypnotic activities. Benzodiazepines enhance the inhibitory action of the amino acid neurotransmitter gamma-aminobutyric acid (GABA). Receptors for GABA are targeted by many important drugs that affect GABA function and are commonly used in the treatment of anxiety disorder, epilepsy, insomnia, spasticity, and aggressive behavior. **Sedation and memory** The onset of sedation after intramuscular administration in adults is 15 minutes, with maximal sedation occurring 30-60 minutes after injection. In one study of adults, when tested the following day, 73% of the patients who were administered midazolam intramuscularly had no recollection of memory cards shown 30 minutes following drug administration; 40% had no recollection of the memory cards shown 60 minutes after drug administration. Onset time of sedative effects in pediatric patients begins within 5 minutes and peaks at 15-30 minutes depending upon the dose administered. In the pediatric population, up to 85% had no memory of pictures shown after receiving intramuscular midazolam compared to 5% of the placebo control group. Sedation in both adult and pediatric patients is reached within 3 to 5 minutes post intravenous (IV) injection. The time of onset is affected by the dose administered and the simultaneous administration of narcotic pre-medication. Seventy-one (71%) percent of the adult patients in clinical endoscopy studies had no memory of insertion of the endoscope; 82% of the patients had no memory of withdrawal of the endoscope. **Anesthesia induction** When midazolam is administered intravenously (IV) for anesthetic induction, induction of anesthesia occurs in about 1.5 minutes when narcotic pre-medication has been given and in 2 to 2.5 minutes without narcotic pre-medication/ other sedative pre-medication. Impairment in a memory test was observed in 90% of the patients.

Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.

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