Alepsal
Alepsal Uses, Dosage, Side Effects, Food Interaction and all others data.
Alepsal is a long-acting barbiturate. It depresses the sensory cortex, reduces motor activity, changes cerebellar function and produces drowsiness, sedation and hypnosis. Its anticonvulsant property is exhibited at high doses.
Alepsal acts on GABAA receptors, increasing synaptic inhibition. This has the effect of elevating seizure threshold and reducing the spread of seizure activity from a seizure focus. Alepsal may also inhibit calcium channels, resulting in a decrease in excitatory transmitter release. The sedative-hypnotic effects of phenobarbital are likely the result of its effect on the polysynaptic midbrain reticular formation, which controls CNS arousal.
Alepsal, the longest-acting barbiturate, is used for its anticonvulsant and sedative-hypnotic properties in the management of all seizure disorders except absence (petit mal).
Trade Name | Alepsal |
Availability | Prescription only |
Generic | Phenobarbital |
Phenobarbital Other Names | Fenobarbital, Phenobarbital, Phenobarbitol, Phenobarbitone, Phenobarbituric Acid, Phenyläthylbarbitursäure, Phenylethylbarbiturate, Phenylethylbarbituric Acid, Phenylethylbarbitursäure, Phenylethylmalonylurea |
Related Drugs | trazodone, hydroxyzine, lorazepam, diazepam, topiramate, promethazine, fentanyl, Ativan, levetiracetam, Keppra |
Type | |
Formula | C12H12N2O3 |
Weight | Average: 232.2353 Monoisotopic: 232.08479226 |
Protein binding | 20 to 45% |
Groups | Approved, Investigational |
Therapeutic Class | Adjunct anti-epileptic drugs, Barbiturates |
Manufacturer | |
Available Country | Argentina |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Alepsal is used as-
- Sedative and hence it relieves anxiety, tension and fear
- Hypnotic and hence it is used for short term insomnia
- Pre-anaesthetics
- Anti-epileptic in epilepsy with Partial seizure or Generalized Tonic-clonic seizure, status epilepticus
- Certain acute convulsive episodes
Alepsal is also used to associated treatment for these conditions: Alcohol Withdrawal Syndrome, Anxiety, Febrile Convulsions, Hyperbilirubinemia, Insomnia, Menopausal Symptoms, Partial-Onset Seizures, Withdrawal Symptoms, Generalized seizure, Sedation
How Alepsal works
Alepsal acts on GABAA receptors, increasing synaptic inhibition. This has the effect of elevating seizure threshold and reducing the spread of seizure activity from a seizure focus. Alepsal may also inhibit calcium channels, resulting in a decrease in excitatory transmitter release. The sedative-hypnotic effects of phenobarbital are likely the result of its effect on the polysynaptic midbrain reticular formation, which controls CNS arousal.
Dosage
Alepsal dosage
Adults:
- Hypnosis: 100 to 320 mg
- Sedation: 30 to 120 mg/day in 2 to 3 divided doses
- Epilepsy: 60 to 250 mg/day
- Convulsion: 50 to 100 mg/day in 2 to 3 divided doses
- Status epilepticus: IV 10-20 mg/Kg, repeat if needed
Children:
- Preoperative: 1-3 mg/Kg body weight
- Convulsion: 4-6 mg/Kg/day
- Status epilepticus: IV 15-20 mg/Kg over 10-15 minutes
Dilute with most IV infusion soln (e.g. NaCl 0.45% or 0.9%, lactated Ringer's, dextrose 5%, Ringer's).
Side Effects
Drowsiness is the most common side effect. Less common side effects are CNS depression, nervousness, agitation, psychiatric disturbance, lethargy, mental depression, ataxia, nightmares, bradycardia, apnea, nausea, vomiting, constipation, restlessness and confusion in the elderly and hyperkinesia in children.
Toxicity
CNS and respiratory depression which may progress to Cheyne-Stokes respiration, areflexia, constriction of the pupils to a slight degree (though in severe poisoning they may wshow paralytic dilation), oliguria, tachycardia, hypotension, lowered body temperature, and coma. Typical shock syndrome (apnea, circulatory collapse, respiratory arrest, and death) may occur.
Precaution
Alepsal is potentially habit forming if taken over an extended period of time. When being prescribed to overcome insomnia, the drug should not be used for a period longer than two weeks. Caution should be taken in patients who are mentally depressed, have hepatic damage, suicidal tendencies or a history of drug abuse.
Interaction
Alepsal can interact with a number of prescription and nonprescription medications including acetaminophen, anticoagulants such as warfarin, chloramphenicol, monoamine oxidase inhibitors (MAOIs), antidepressants, asthma medicine, cold medicine, anti-allergy medicine, sedatives, steroids, tranquilizers, and vitamins. Interactions with these medications can increase the drowsiness caused by phenobarbital.
Food Interaction
- Administer vitamin supplements.
- Avoid alcohol.
- Limit caffeine intake.
- Take on an empty stomach. Taking this medication on an empty stomach increases the speed of absorption.
Alepsal Alcohol interaction
[Major] GENERALLY AVOID:
Concurrent acute use of barbiturates and ethanol may result in additive CNS effects,
including impaired coordination, sedation, and death.
Tolerance of these agents may occur with chronic use.
The mechanism is related to inhibition of microsomal enzymes acutely and induction of hepatic microsomal enzymes chronically.
The combination of ethanol and barbiturates should be avoided.
Alepsal Hypertension interaction
[Major] The intravenous administration of barbiturates may produce severe cardiovascular reactions such as bradycardia, hypertension, or vasodilation with fall in blood pressure, particularly during rapid infusion.
Parenteral therapy with barbiturates should be administered cautiously in patients with hypertension, hypotension, or cardiac disease.
The intravenous administration of barbiturates should be reserved for emergency treatment of acute seizures or for anesthesia.
Alepsal Drug Interaction
Moderate: lorazepam, diphenhydramine, duloxetine, divalproex sodium, phenytoin, levetiracetam, clonazepam, lamotrigine, acetaminophen, acetaminophen, diazepam, cholecalciferol, alprazolamMinor: carbamazepine, topiramate, lacosamideUnknown: fluticasone nasal, polyethylene glycol 3350, ascorbic acid, ondansetron
Alepsal Disease Interaction
Major: acute alcohol intoxication, drug dependence, liver disease, porphyria, rash, respiratory depression, cardiovascular, prolonged hypotension, renal dysfunctionModerate: suicidal tendency, adrenal insufficiency, depression, hematologic toxicity, osteomalacia, paradoxical reactions
Elimination Route
Absorbed in varying degrees following oral, rectal or parenteral administration. The salts are more rapidly absorbed than are the acids. The rate of absorption is increased if the sodium salt is ingested as a dilute solution or taken on an empty stomach.
Half Life
53 to 118 hours (mean 79 hours)
Pregnancy & Breastfeeding use
Pregnancy Category D. Alepsal can cause potential fetal damage. Their use in pregnancy alone, or in combination with other anticonvulsants, can cause coagulation defects in the newborn infant which may be preventable by the prophylactic administration of Vitamin K to the mother prior to delivery. Alepsal is excreted through human milk; so caution should be taken during lactation period.
Contraindication
Alepsal is contraindicated in patients with acute intermittent porphyria and who have a natural or idiosyncrasy to barbiturates
Special Warning
Debilitated patient: Reduce dose
Renal Impairment: Reduce dose. Severe: Contraindicated
Hepatic Impairment: Reduce dose. Severe: Contraindicated
Acute Overdose
Alepsal should not be used more than the dosage guide line. 1 gm Alepsal oral dose may cause serious poisoning and 2 gm may cause even death. Over dosage produces severe, persistent depression. Treatment includes artificial respiration, maintenance of fluid balance and antibiotics to prevent pneumonia. Alkalinisation of the urine and forced diuresis or haemodialysis have been used in cases of severe poisoning.
Storage Condition
Protect from light, store in cool and dry place. Keep out of reach of children.
Innovators Monograph
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