Diazepam (Adverse Reactions)

Diazepam is a benzodiazepine derivative with anxiolytic, muscle relaxant, anticonvulsant, and sedative properties. It facilitates the binding of the neurotransmitter GABA to its neuronal receptor and increases its activity, thus producing a relaxation of central nervous system activity. It acts on the limbic system, thalamus, and hypothalamus. It does not produce peripheral autonomic nervous system blockade or extrapyramidal side effects.

Diazepam is effective in controlling anxiety, seizures, and, in some cases, bipolar disorder. However, it is essential to take precautions, as its prolonged use can lead to adverse effects or physical and psychological dependence.

Contraindications

Diazepam is contraindicated in individuals with hypersensitivity to benzodiazepines or with dependence on other substances, including alcohol (except for the treatment of acute withdrawal reactions). It is also contraindicated in patients with myasthenia gravis, sleep apnea syndrome, severe respiratory insufficiency, severe hepatic insufficiency, narrow-angle glaucoma (only with rectal, oral administration), severe chronic hypercapnia (only with oral administration).

Diazepam is contraindicated during pregnancy due to its teratogenic potential. Studies have shown that its use during pregnancy can negatively affect fetal development, increasing the risk of malformations and complications in pregnancy. Additionally, the use of diazepam during pregnancy can cause sedative effects in the newborn, which can lead to respiratory difficulties and problems with thermal regulation.

Diazepam is contraindicated in patients with severe traumatic brain injuries due to the risk of respiratory depression and central nervous system side effects, which could worsen the patient's condition.

Diazepam is contraindicated in patients with ocular diseases such as narrow-angle glaucoma, as it can increase intraocular pressure and worsen the condition.

Diazepam is also contraindicated in neonates due to the risks associated with respiratory depression and sedative effects that can severely affect respiratory and cardiac function in newborns. Furthermore, neonates have a higher susceptibility to side effects due to their still immature nervous system.

Precautions

Precautions should be taken when administering diazepam to the elderly, to patients with renal insufficiency, mild or moderate hepatic insufficiency. Caution should be exercised when prescribing diazepam to children. Care should be taken when prescribing diazepam to patients with chronic respiratory insufficiency, porphyria, epilepsy, or with alcohol/drug dependence or a history of dependence.

It is essential to consider the risk of side effects such as anterograde amnesia, psychiatric or paradoxical reactions, and the possibility of developing physical and psychological dependence after prolonged use of the drug.

In patients with CNS lesions and epileptic seizures, extreme caution should be exercised as it may decrease cerebral circulation and blood oxygenation, potentially leading to irreversible brain damage. Risk of anterograde amnesia, psychiatric and paradoxical reactions.

After continuous use of diazepam, there is a risk of tolerance and dependence (physical and psychological). Abrupt discontinuation of treatment can trigger a withdrawal syndrome, which includes symptoms such as anxiety, insomnia, and in some cases, seizures.

Do not use in anxiety associated with depression or as primary treatment for psychotic illness.

Intravenous administration of diazepam carries a risk of apnea and/or cardiac arrest in the elderly, in very debilitated patients, or those with limited cardiac or pulmonary reserve.

Side Effects

Diazepam may cause drowsiness, emotional blunting, reduced alertness, confusion, fatigue, headache, dizziness, muscle weakness, ataxia or diplopia, amnesia, depression, psychiatric and paradoxical reactions; respiratory depression. The most common side effect of diazepam is drowsiness, which can interfere with daily activities. In addition, some people may experience dizziness or confusion, especially when starting treatment or increasing the dose.

Drug Interactions

The depressant effect of diazepam on the central nervous system (CNS) is potentiated by: neuroleptics, hypnotics, anxiolytics/sedatives, antidepressants, narcotic analgesics, antiepileptics, anesthetics, sedative antihistamines.

The sedative effect of diazepam is increased by: alcohol, cisapride, cimetidine, propofol, ethanol.

The action of diazepam is increased by: cytochrome P450 inhibitors, azole antifungals, isoniazid.

There is an additive depressant effect on the CNS and respiratory system with: barbiturates and centrally acting muscle relaxants.

Diazepam toxicity is increased by: ethinylestradiol and mestranol, fluoxetine, omeprazole, ketoconazole, fluvoxamine, valproic acid.

The effect of diazepam is decreased by: phenobarbital, carbamazepine, phenytoin, rifampicin.

Diazepam increases the action of digoxin and alters the action of phenytoin.

BRAND NAMES

• Stesolid ®
• Valium ®
• Aneurol®
• Ansium®
• Gobanal®
• Pacium®
• Tepazepan®