Arotril 0.5 mg
Description
Indications
Arotril is primarily prescribed for the treatment of panic disorder, with or without the presence of agoraphobia. Panic disorder is characterized by sudden and unexpected panic attacks, often accompanied by a fear of having additional attacks and a preoccupation with the possible consequences of these episodes.
Arotril is also used, either alone or in combination with other treatments, to manage Lennox-Gastaut syndrome (a type of epilepsy, particularly the petit mal variant), as well as akinetic and myoclonic seizures. In some cases, it may be used in patients suffering from absence seizures (petit mal) who have not responded to succinimides.
It is important to note that Arotril’s effectiveness in long-term use (more than 9 weeks) has not been systematically studied in controlled clinical trials. For patients requiring extended use, a physician should periodically assess the continued benefits of the medication.
Always follow a registered healthcare provider’s guidance when using this medication.
Pharmacology
Clonazepam, the active ingredient in Arotril, shares the common pharmacological properties of benzodiazepines, including anticonvulsant, sedative, muscle-relaxant, and anxiolytic (anti-anxiety) effects. These actions occur through the enhancement of GABAergic neurotransmission, which works to suppress overactive neuronal activity at inhibitory synapses. By enhancing the GABA receptor’s affinity for the neurotransmitter, clonazepam increases chloride ion influx, resulting in more significant inhibitory effects in the central nervous system.
Animal studies suggest that clonazepam may also have an impact on serotonin. Clinical and electroencephalographic data in humans demonstrate that clonazepam is effective in suppressing various types of paroxysmal activities, including the spike and wave discharges characteristic of absence seizures (petit mal), slow spike waves, and other generalized or focal seizures. Clonazepam is particularly effective in controlling generalized EEG abnormalities.
Dosage & Administration
Oral Administration:
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Adults: The initial dose for seizure disorders should not exceed 1.5 mg per day, divided into three doses. The dose may be gradually increased by 0.5 to 1 mg every three days until seizures are adequately controlled or side effects limit further increases. The maximum recommended daily dose is 20 mg.
For panic disorder, the initial dose is 0.25 mg, taken twice daily, with potential increases to 1 mg/day after three days based on patient response. -
Pediatric Patients: For children up to 10 years of age (or weighing 30 kg), the starting dose should range from 0.01 to 0.03 mg/kg/day, not exceeding 0.05 mg/kg/day, split into two or three doses.
Injection Administration:
- Infants and children: The initial dose is half a vial (0.5 mg), administered slowly via IV injection or infusion.
- Adults: The recommended dose is 1 vial (1 mg) by slow IV injection or infusion, which can be repeated as needed. The injection rate should not exceed 0.25 – 0.5 mg per minute, and a total dose of 10 mg should not be exceeded.
Always follow the guidance of a registered healthcare provider for appropriate dosing.
Drug Interactions
Arotril does not seem to affect the pharmacokinetics of phenytoin, carbamazepine, or phenobarbital. The influence of Arotril on the metabolism of other drugs has not been investigated in detail.
Contraindications
Arotril should not be used by individuals with a known hypersensitivity to benzodiazepines or those with significant liver disease, either clinically or biochemically evident. While it can be used in patients with open-angle glaucoma under appropriate therapy, it is contraindicated in individuals with acute narrow-angle glaucoma.
Side Effects
The most common side effects are related to central nervous system (CNS) depression. Approximately 50% of patients may experience drowsiness, and 30% may develop ataxia. These effects often diminish with continued use. Behavioral changes are noted in roughly 25% of patients. Other side effects may include abnormal eye movements, aphonia, coma, tremor, dizziness, confusion, depression, amnesia, hallucinations, psychosis, increased libido, insomnia, and palpitations.
Pregnancy & Lactation
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Pregnancy: Preclinical studies suggest that clonazepam may cause congenital malformations. While anticonvulsants are known to be teratogenic, it is difficult to pinpoint the exact causes from available data. Therefore, Arotril should only be used during pregnancy when the benefits outweigh the risks. High doses in late pregnancy may lead to adverse effects on the fetus, including irregular heartbeat and respiratory depression. Abrupt discontinuation during pregnancy may worsen epilepsy symptoms.
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Lactation: Although clonazepam passes into breast milk in small amounts, it is not recommended for breastfeeding mothers due to the potential for side effects in the infant.
Precautions & Warnings
Patients with multiple seizure disorders should be monitored carefully, as Arotril may increase the frequency or precipitate generalized tonic-clonic seizures, potentially requiring the addition of other anticonvulsants. Additionally, using Arotril in combination with valproic acid may result in absence status.
Use in Special Populations
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Pediatrics: In infants and young children, Arotril can lead to increased salivation and bronchial secretions, which may compromise airway patency.
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Geriatrics: The pharmacological effects of benzodiazepines tend to be more pronounced in elderly patients due to age-related changes in drug-receptor interactions and organ function.
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Renal Impairment: No dosage adjustments are required for patients with renal impairment.
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Hepatic Impairment: In patients with liver cirrhosis, the clearance of unbound Arotril may be reduced, although further investigation into this effect is required.
Overdose Effects
Symptoms of Overdose:
Excessive doses of Arotril may cause severe drowsiness, ataxia, speech difficulties, eye movement abnormalities, and confusion. In rare cases, overdose can lead to respiratory depression, hypotension, coma, and cardiac arrest, particularly in patients with pre-existing respiratory conditions.
Treatment:
Supportive care, including monitoring of vital signs, is critical. Activated charcoal may be administered to prevent further absorption, and gastric lavage may be considered in cases of mixed ingestion. If CNS depression is severe, flumazenil (a benzodiazepine antagonist) can be used with caution under close supervision.
Therapeutic Class
- Adjunctive Anti-Epileptic Drug
- Benzodiazepine Hypnotic
Reconstitution
Intravenous Administration:
- Slow Injection: Dilute the vial contents with 1 ml of water for injection to prevent vein irritation.
- Infusion: Arotril can be diluted for IV infusion with at least 85 ml of compatible fluids like saline or glucose solutions. Use non-PVC infusion bags and infuse within 24 hours. Infusion time should not exceed 8 hours.
Intramuscular Injection: Only used when IV administration is not feasible.
Storage Conditions
Store in a cool, dry place away from light and heat. Keep out of reach of children.
Common Questions
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Is Arotril a sleeping pill?
No, Arotril is not intended as a sleeping pill. It may cause sleep disturbances. -
Can Arotril be used for long-term treatment?
Arotril should only be used long-term as prescribed by a doctor. Discontinuing the medication suddenly can lead to seizures. -
What happens if Arotril is stopped abruptly?
Withdrawal symptoms can include sleep disturbances, mood changes, sweating, muscle pain, and anxiety. -
Can I take Arotril with other medications like zolpidem or quetiapine?
Co-administration with these drugs may increase side effects. Always consult with your healthcare provider before combining medications.
Quick Tips
- Addiction Risk: Arotril has a high potential for habit formation. Take it strictly as prescribed.
- Dizziness: Arotril may cause dizziness. Avoid activities requiring mental alertness, such as driving.
- Avoid Alcohol: Alcohol can intensify the sedative effects of Arotril.
- Pregnancy and Breastfeeding: Inform your doctor if you are pregnant, planning to conceive, or breastfeeding.
- Behavioral Changes: Seek medical advice if you experience mood changes, aggression, or other behavioral issues while on Arotril.
Additional information
Weight | 0.15 g |
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