Arotril1 mg

Arotril 1 mg serves as a treatment for panic disorder, whether with or without agoraphobia. Panic disorder manifests through unexpected panic attacks and the accompanying worry about experiencing more of these episodes, along with concerns about their implications or consequences. 

Additionally, it is indicated for use on its own or as an adjunct in treating Lennox-Gastaut Syndrome (specifically the petit mal variant), akinetic seizures, and myoclonic seizures. It may also be considered for patients with absence seizures (petit mal) who have not responded to succinimides.

It's important to note that the long-term effectiveness of the medicine, specifically for durations exceeding 9 weeks, hasn't been comprehensively studied in controlled clinical trials. Therefore, physicians who choose to prescribe Arotril 1 mg for extended periods should periodically reassess its long-term suitability for each patient.

Adjunct anti-epileptic drugs, Benzodiazepine hypnotics

Arotril 1 mg works by reducing nerve transmission in the motor cortex, effectively suppressing the spike and wave discharges associated with absence seizures. This mechanism is thought to be linked to its ability to enhance the activity of GABA. In clinical applications, it has proven effective in improving both focal epilepsy and generalized seizures.

Oral Dosage for Adults with Seizure Disorders:

Begin with 1.5 mg per day, divided into three doses. Adjust by 0.5-1 mg every three days, up to a maximum of 20 mg per day.

Oral Dosage for Adults with Panic Disorder:

Start with 0.25 mg twice daily. After three days, increase to 1 mg per day as needed.

Pediatric Patients:

To minimize drowsiness, infants and children (up to 10 years or 30 kg) should take 0.01-0.03 mg/kg/day, not exceeding 0.05 mg/kg/day, split into multiple doses.

Injection Dosage:

Children: Administer 0.5 mg via slow IV injection or infusion. 

Adults: Use 1 mg via slow IV injection or infusion, with the option to repeat if necessary (typically 1-4 mg). 

Ensure a controlled IV rate of 0.25 - 0.5 mg per minute (equivalent to 0.5-1.0 ml of the solution), and do not exceed a total dose of 10 mg.

Arotril 1 mg does not seem to impact the pharmacokinetics of phenytoin, carbamazepine, or phenobarbital. However, its effect on the metabolism of other drugs remains unexplored

Avoid prescribing it to patients with a history of hypersensitivity to benzodiazepines or those showing clinical or biochemical signs of significant liver disease. It can be administered to patients with open-angle glaucoma who are receiving appropriate treatment but should not be used in cases of acute narrow-angle glaucoma.

The most commonly observed side effects of Arotril 1 mg are related to central nervous system (CNS) depression. Experience in treating seizures has revealed that drowsiness occurs in around 50% of patients, while approximately 30% experience ataxia. In some instances, these effects may diminish over time. 

Additionally, behavior problems have been reported in about 25% of patients. Other potential side effects include abnormal eye movements, aphonia, coma, tremor, vertigo, confusion, depression, amnesia, hallucinations, hysteria, increased libido, insomnia, psychosis, and palpitations.

Arotril 1 mg should be considered during pregnancy only when the potential benefits outweigh the risks to the fetus. It is recommended that women taking the medicine should avoid breastfeeding.

When administered to patients with multiple coexisting seizure disorders, this medication can potentially raise the occurrence or trigger the onset of generalized tonic-clonic seizures. In such cases, it may be necessary to supplement with suitable anticonvulsants or adjust their dosages accordingly. Combining valproic acid with Arotril 1 mg may lead to the development of absence status.

Symptoms: Benzodiazepines commonly result in drowsiness, ataxia, dysarthria, and nystagmus. In cases of Arotril 1 mg overdose taken alone, it is rarely life-threatening but may lead to areflexia, apnea, hypotension, cardiorespiratory depression, and coma. Coma, if it occurs, typically lasts a few hours, but it may be more prolonged and cyclical in elderly patients. 

Elevated seizure frequency can occur with supratherapeutic plasma concentrations. It's important to note that benzodiazepine-induced respiratory depression poses a greater risk for individuals with respiratory conditions. Additionally, benzodiazepines can amplify the effects of other central nervous system depressants, including alcohol.

Treatment: Monitor the patient's vital signs and provide appropriate supportive care based on their clinical condition. Symptomatic treatment for cardiorespiratory and central nervous system effects may be necessary. To prevent further drug absorption, consider timely administration of activated charcoal within 1-2 hours. When using activated charcoal, ensure airway protection for drowsy patients. 

Gastric lavage may be considered in cases of mixed ingestion but should not be routine. In cases of severe CNS depression, flumazenil, a benzodiazepine antagonist, may be an option. However, it should be administered under close monitoring due to its short half-life (approximately one hour). Patients given flumazenil will require monitoring after its effects wear off. Use flumazenil with extreme caution when other drugs that lower the seizure threshold (e.g., tricyclic antidepressants) are present. For detailed information on the correct use of flumazenil, refer to the prescribing information.

Keep in a dry place away from light and heat. Keep out of the reach of children.

For slow intravenous injection, it's crucial to dilute the vial's contents with 1 ml of water for injection before administering to prevent irritation of the veins. This injection solution should be prepared just before use. During IV injection, it should be administered slowly while continuously monitoring EEG, respiration, and blood pressure.

When opting for intravenous infusion, Arotril 1 mg (from the vial) can be diluted for infusion at a ratio of 1 vial (1 mg) to at least 85 ml of diluting media. Suitable diluting media options include sodium chloride 0.9%, sodium chloride 0.45% + glucose 2.5%, glucose 5%, or glucose 10%. These mixtures remain stable for 24 hours at room temperature. 

If PVC infusion bags are used, the mixture should be infused immediately or within 4 hours. The infusion should not exceed 8 hours. Avoid preparing Arotril 1 mg infusions using sodium bicarbonate solution, as it may cause solution precipitation.

Intramuscular injection should be reserved for exceptional cases or when IV administration is not possible.

Adjunct anti-epileptic drugs, Benzodiazepine hypnotics

Arotril 1 mg shares pharmacological properties common to benzodiazepines, encompassing anticonvulsive, sedative, muscle-relaxing, and anxiolytic effects. The central actions of benzodiazepines involve enhancing GABAergic neurotransmission at inhibitory synapses. In the presence of benzodiazepines, the GABA receptor's affinity for the neurotransmitter is boosted through positive allosteric modulation, resulting in an increased impact of released GABA on the postsynaptic transmembrane chloride ion flux.

Animal studies also indicate that this pill may affect serotonin. Both animal data and electroencephalographic investigations in humans have demonstrated that Arotril 1 mg rapidly suppresses various forms of paroxysmal activity, including spike and wave discharges in absence seizures (petit mal), slow spike waves, generalized spike waves, spikes with temporal or other locations, as well as irregular spikes and waves. Generalized EEG abnormalities are more consistently suppressed than focal abnormalities. Based on these findings, Arotril 1 mg offers beneficial effects in both generalized and focal epilepsies.

Pediatric Use: In infants and young children, the use of this medication may lead to increased saliva and bronchial secretions. Therefore, it's essential to ensure clear airways.

Geriatric Use: Elderly patients may experience more pronounced benzodiazepine effects compared to younger individuals, even with similar plasma benzodiazepine concentrations. This heightened sensitivity may result from age-related changes in drug-receptor interactions, post-receptor mechanisms, and organ function.

Renal Impairment: Renal issues do not affect the pharmacokinetics of this medication, necessitating no dosage adjustment for patients with kidney impairment.

Hepatic Impairment: In cirrhotic patients, the plasma protein binding of this medication significantly differs from that in healthy subjects, with a higher free fraction (17.1±1.0% vs. 13.9±0.2%). Although hepatic impairment's influence on Arotril 1 mg pharmacokinetics hasn't been extensively studied, experience with a closely related nitrobenzodiazepine (nitrazepam) suggests that the clearance of unbound Arotril 1 mg may be reduced in liver cirrhosis cases.