Arotril 1 mg

Description

Indications Arotril is prescribed for the treatment of panic disorder, with or without agoraphobia. Panic disorder is characterized by sudden and unexpected panic attacks, often accompanied by excessive concern about future attacks and their potential consequences.

Additionally, Arotril is used alone or in combination for managing Lennox-Gastaut Syndrome (petit mal variant), akinetic seizures, and myoclonic seizures. It may also be beneficial for patients experiencing absence seizures (petit mal) who have not responded to succinimides.

The long-term effectiveness of Arotril, beyond nine weeks, has not been extensively studied in controlled clinical trials. Physicians prescribing this medication for extended periods should periodically reassess its continued usefulness for each patient.

Pharmacology Clonazepam, the active ingredient in Arotril, belongs to the benzodiazepine class and exhibits anticonvulsant, sedative, muscle-relaxing, and anxiolytic properties. Its central effects are mediated through the enhancement of GABAergic neurotransmission at inhibitory synapses. Benzodiazepines increase the affinity of GABA receptors for neurotransmitters, leading to an amplified action of released GABA and improved chloride ion flux across postsynaptic membranes.

Research indicates that clonazepam may also affect serotonin activity. Animal studies and electroencephalographic investigations in humans show that clonazepam quickly suppresses various types of paroxysmal activity, including spike-and-wave discharges in absence seizures, slow and generalized spike waves, and other irregular wave patterns. These findings support its effectiveness in treating both generalized and focal epilepsy.

Dosage & Administration Oral Administration:

• Adults (Seizure Disorders): Initial dosage should not exceed 1.5 mg/day, divided into three doses. The dosage can be increased by 0.5 to 1 mg every three days until seizures are controlled or side effects prevent further escalation. The maximum recommended daily dose is 20 mg.
• Adults (Panic Disorder): The initial dose is 0.25 mg divided into two doses. After three days, the dose may be increased to a target of 1 mg/day.
• Pediatric Patients: To minimize drowsiness, the initial dose for infants and children (up to 10 years or 30 kg body weight) should be 0.01 to 0.03 mg/kg/day, not exceeding 0.05 mg/kg/day, divided into two or three doses.

Injection Administration:

• Infants & Children: 0.5 mg (half of a vial) via slow IV injection or IV infusion.
• Adults: 1 mg (one vial) via slow IV injection or infusion. This dose may be repeated as needed, usually requiring 1-4 mg to manage status epilepticus. The injection rate should not exceed 0.25-0.5 mg per minute, with a maximum total dose of 10 mg.

Drug Interactions Arotril does not significantly alter the metabolism of phenytoin, carbamazepine, or phenobarbital. The effect of Arotril on the metabolism of other drugs remains uninvestigated.

Contraindications Arotril should not be used in patients with known hypersensitivity to benzodiazepines or those with significant liver disease. It may be used in individuals with open-angle glaucoma receiving appropriate therapy but is contraindicated in acute narrow-angle glaucoma.

Side Effects Common side effects include drowsiness (in 50% of patients) and ataxia (in 30% of cases). These effects may diminish over time. Behavioral disturbances occur in approximately 25% of patients. Additional side effects may include abnormal eye movements, tremors, confusion, hallucinations, mood changes, increased libido, insomnia, and palpitations.

Pregnancy & Lactation

• Pregnancy: Clonazepam may pose a risk of congenital malformations. Anticonvulsant drugs are linked to potential teratogenic effects, although the precise causes are unclear. Clonazepam should be used during pregnancy only if the potential benefits outweigh the risks. High doses in the third trimester or during labor can cause irregular fetal heartbeats, hypotonia, mild respiratory depression, and feeding difficulties in newborns.
• Lactation: Small amounts of clonazepam pass into breast milk. If treatment is necessary, breastfeeding should be discontinued.

Precautions & Warnings

• In patients with multiple seizure types, Arotril may increase the occurrence of generalized tonic-clonic seizures, requiring adjustments in anticonvulsant therapy.
• Co-administration with valproic acid may induce absence status.
• In pediatric patients, increased saliva and bronchial secretions may require airway monitoring.
• Elderly patients may experience heightened sensitivity to benzodiazepines.
• No dose adjustment is needed for patients with renal impairment.
• Liver cirrhosis may alter the pharmacokinetics of Arotril.

Overdose Effects & Management Symptoms of overdose include drowsiness, ataxia, slurred speech, nystagmus, apnea, hypotension, and respiratory depression. Severe cases may lead to coma, particularly in elderly patients. Patients should be monitored for vital signs and given supportive treatment. Activated charcoal may reduce drug absorption if administered within 1-2 hours. In severe CNS depression, flumazenil (a benzodiazepine antagonist) may be used under medical supervision.

Therapeutic Class Arotril belongs to the class of benzodiazepine hypnotics and adjunct anti-epileptic drugs.

Reconstitution & Storage

• IV Injection: Dilute the vial contents with 1 ml of water for injection before administration.
• IV Infusion: Mix 1 mg of Arotril with at least 85 ml of suitable diluents (e.g., sodium chloride 0.9%, glucose 5%). Solutions should be infused within 24 hours using non-PVC bags.
• IM Injection: Should only be used in exceptional cases when IV administration is not possible.
• Store in a dry place, away from heat and light. Keep out of reach of children.

Common Questions

• Is Arotril a sleeping pill? No, it is not primarily used for sleep disorders.
• Can it be used long-term? It should be taken as prescribed. Sudden discontinuation may cause withdrawal symptoms.
• What are withdrawal symptoms? Symptoms include insomnia, mood changes, sweating, muscle pain, tremors, and anxiety.
• Does it affect memory? While it does not directly cause memory loss, some patients may experience difficulty recalling recent events.
• Can it cause weight changes? Yes, both weight gain and weight loss have been reported.
• Can it be taken with zolpidem or quetiapine? Combining these drugs may increase the risk of side effects such as drowsiness, confusion, and respiratory issues.

Quick Tips

• Arotril has a high potential for dependency; use only as directed by a physician.
• It may cause dizziness; avoid activities requiring full alertness, such as driving.
• Alcohol consumption can increase drowsiness and should be avoided.
• Notify your doctor if you experience mood changes, aggression, or suicidal thoughts.
• Do not abruptly stop taking Arotril without consulting your doctor.