Esparon
Esparon Uses, Dosage, Side Effects, Food Interaction and all others data.
Esparon is a triazolo analogue of the 1,4-benzodiazepine class of drugs. It is an anxiolytic with hypnotic and anticonvulsive properties. Esparon is presumed to produce its effects via interacting with the Gamma Aminobutyric Acid (GABA) - benzodiazepine receptor complex. Like all benzodiazepines, it causes a dose related CNS depressant activity varying from mild impairment of task performance to hypnosis.
Esparon is indicated to treat anxiety and panic disorders. The mechanism by which its cell receptor interactions translate to a clinical effect is not known.
Esparon exerts its effects through interaction with BNZ-1, BNZ-2, and GABA-A receptors. Esparon binding to BNZ-1 is thought to influence sedation and anti-anxiety, BNZ-2 may influence memory, coordination, muscle relaxation, and anticonvulsive activity, and GABA-A may calm patients by increasing the affinity of GABA-A receptors for GABA.
The metabolism of alprazolam is mediated largely through the action of CYP3As and so alprazolam is contraindicated with CYP3A inhibitors such as ketoconazole and itraconazole.
| Trade Name | Esparon |
| Availability | Prescription only |
| Generic | Alprazolam |
| Alprazolam Other Names | Alprazolam |
| Related Drugs | sertraline, escitalopram, fluoxetine, duloxetine, hydroxyzine, clonazepam, Lexapro, Zoloft, Xanax, Cymbalta |
| Type | |
| Formula | C17H13ClN4 |
| Weight | Average: 308.765 Monoisotopic: 308.082874143 |
| Protein binding | Alprazolam is 80% protein bound in serum. The majority of this protein binding is to serum albumin. Alprazolam is also bound to alpha1-acid glycoprotein with low frequency. |
| Groups | Approved, Illicit, Investigational |
| Therapeutic Class | Benzodiazepine sedatives |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
- * Anxiety disorder
- * Short term relief of anxiety
- * Anxiety associated with depression
- * Panic disorder, with or without agoraphobia.
Esparon is also used to associated treatment for these conditions: Anxiety, Generalized Anxiety Disorder (GAD), Panic Disorder
How Esparon works
Esparon is a triazolobenzodiazepine used to treat certain anxiety and panic disorders. Esparon acts on benzodiazepine receptors BNZ-1 and BNZ-2. The active metabolites 4-hydroxyalprazolam acts on these receptors with 0.20 times the potency of alprazolam and alpha-hydroxyalprazolam acts on these receptors with 0.66 times the potency.
The effect of alprazolam on BNZ-1 mediates the sedation and anti-anxiety effects of the drug while the action on BNZ-2 mediates effects on memory, coordination, muscle relaxation, and anticonvulsive activity.
Esparon also couple with GABA-A receptors to enhance GABA binding to its receptor. This interaction mediates inhibition of the nervous system and results in a calming effect.
The molecular mechanisms as well as the clinical effects of alprazolam have both been well demonstrated, however the means by which the molecular mechanism translates to a clinical effect is still not understood.
Dosage
Esparon dosage
Treatment should be initiated with a dose of 0.25 to 0.5 mg three times daily. Depending on the response, dose may
be increased at intervals of 3 to 4 days in increments of no more than 1 mg per day. The maximum dose should not
exceed 4 mg/day. Occasional patients with panic disorder may need as much as 10 mg a day to achieve a
successful response and in these cases periodic reassessment and consideration of dosage adjustment is required.
Dosage should be individualized for maximum beneficial effect with a lowest possible dose. If side-effects occur at
starting dose, dose may be lowered. When discontinuing therapy, dosage should be reduced gradually by no more
than 0.5 mg every three days.
In elderly patients or in patients with advanced liver disease, the usual starting dose is 0.25 mg, two or three times
daily and may be gradually increased if needed and tolerated. Safety and effectiveness of Esparon in individuals
below 18 years of age have not been established.
Esparon XR 1 should be administered once daily, preferably in the morning by patients who are on multiple dosage
regimen of Esparon 0.25/0.5 mg. The tablets should be taken intact, they should not be chewed, crushed, or broken.
Side Effects
Side effects, if occur, are generally observed at the beginning of therapy and usually disappear upon continued medication. The most frequent side effects are drowsiness and light headedness. The other side effects, that may occur include depression, headache, confusion, dry mouth, constipation etc.
Toxicity
Esparon overdose can present as sleepiness, confusion, poor coordination, slow reflexes, coma, and death. Taking alprazolam with alcohol lowers the threshold for overdose. Patients should have their respiration, pulse, and blood pressure monitored. Patients can be treated by gastric lavage and intravenous fluids.. If hypotension occurs, patients may be treated with vasopressors. In known, or suspected overdoses, patients can be given the benzodiazepine receptor antagonist flumazenil in addition to other methods of management.
Oral LD50 in rats is 331-2171mg/kg.
Esparon is a pregnancy category D teratogen meaning there is evidence of risk to the fetus of a mother taking alprazolam but in some cases the benefit may outweigh the risk. Children born to these mothers are also at risk of withdrawal symptoms, flaccidity, and respiratory issues.
Benzodiazepines are expressed in human breast milk and so nursing is generally not recommended in mothers taking alprazolam.
Esparon is not associated with carcinogenicity, mutagenicity, or impairment of fertility.
Precaution
Because Esparon may produce psychological and physical dependence, increment of dose or abrupt discontinuation of Esparon therapy should not be done without physician's advice. Duration of therapy must be determined by the physicians. Esparon should be administered with caution to patients with hepatic or renal disease, chronic pulmonary insufficiency or sleep apnea.
Interaction
Esparon produces additive CNS depressant effects when co-administered with other psychotropic medications, anticonvulsants, antihistaminics, ethanol and other drugs which themselves produce CNS depression.
Food Interaction
- Avoid alcohol. Alcohol may potentiate the CNS depressant effects of this drug.
- Avoid grapefruit products.
- Limit caffeine intake.
- Take with or without food. Food increases the Cmax of extended release alprazolam by 25%, but the AUC and half life are not affected.
[Moderate] GENERALLY AVOID: The pharmacologic activity of oral midazolam, triazolam, and alprazolam may be increased if taken after drinking grapefruit juice.
The proposed mechanism is CYP450 3A4 enzyme inhibition.
In addition, acute alcohol ingestion may potentiate CNS depression and other CNS effects of many benzodiazepines.
Tolerance may develop with chronic ethanol use.
The mechanism may be decreased clearance of the benzodiazepines because of CYP450 hepatic enzyme inhibition.
Also, it has been suggested that the cognitive deficits induced by benzodiazepines may be increased in patients who chronically consume large amounts of alcohol.
MANAGEMENT: The manufacturer recommends that grapefruit juice should not be taken with oral midazolam.
Patients taking triazolam or alprazolam should be monitored for excessive sedation.
Alternatively, the patient could consume orange juice which does not interact with these drugs.
Patients should be advised to avoid alcohol during benzodiazepine therapy.
Esparon Drug Interaction
Moderate: duloxetine, duloxetine, escitalopram, escitalopram, pregabalin, pregabalin, metoprolol, metoprololUnknown: amphetamine / dextroamphetamine, amphetamine / dextroamphetamine, aspirin, aspirin, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Esparon Disease Interaction
Major: acute alcohol intoxication, closed-angle glaucoma, drug dependence, renal/liver disease, respiratory depression, seizuresModerate: depression, obesity, paradoxical reactions
Volume of Distribution
Volume of distribution following oral administration is 0.8-1.3L/kg. Esparon crosses the blood-brain barrier.
Elimination Route
Oral bioavailability of a standard release tablet of alprazolam is 84-91% with a time to maximum concentration of 1.8 hours. A 1mg oral dose of alprazolam leads to a maximum plasma concentration of 12-22mcg/L. Esparon is rapidly absorbed in the gastrointestinal tract.
Data for the area under the curve and the effect of taking alprazolam with food are not readily available.
Half Life
11.2 hours in healthy patients. The half life is 16.3h in the elderly, 5.8-65.3h in patients with alcoholic liver disease, 9.9-40.4h in obese patients. The half life is 25% higher in Asian patients compared to Caucasians. Other studies have shown the half life to be 9-16h.
Clearance
Oral clearance is 0.90±0.21mL/min/kg but this increases to 2.13±0.54mL/min/kg when given with CYP3A inducers. Other studies have demonstrated a clearance of 0.70-1.5mL/min/kg.
Elimination Route
Esparon is mainly eliminated in the urine. A large portion of the dose is eliminated as unmetabolized alprazolam. 2
Pregnancy & Breastfeeding use
Pregnancy: Esparon has been categorized in pregnancy category D; that means, it should be avoided in pregnancy.
Lactation: Like other benzodiazepines, Esparon is assumed to be excreted in breast milk. Therefore, nursing should not be undertaken by mothers who must use Esparon.
Contraindication
Contraindicated in patients with hypersensitivity to alprazolam or other benzodiazepines. Esparon is also contraindicated in patients with myasthenia gravis, acute narrow angle glaucoma, during pregnancy and also in infants.
Special Warning
Use in Children: Safety and efficacy of Esparon in patients under the age of 18 years has not been established.
Acute Overdose
Manifestations of Esparon over dosage include somnolence, confusion, impaired coordination, diminished reflexes and coma. In such cases of over dosage general supportive measures should be employed along with immediate gastric lavage.
Interaction with other Medicine
The CNS-depressant action of Esparon may be aggravated by concomitant use of other psychotropic drugs, anticonvulsants, antihistaminics, alcohol and oral contraceptives.
Storage Condition
Esparon tablets should be stored in a cool and dry place, protected from light and moisture.
Innovators Monograph
You find simplified version here Esparon
Esparon contains Alprazolam see full prescribing information from innovator Esparon Monograph, Esparon MSDS, Esparon FDA label
FAQ
What does Esparon do?
Esparon is used to treat anxiety and panic disorders. It belongs to a class of medications called benzodiazepines which act on the brain and nerves (central nervous system) to produce a calming effect. It works by enhancing the effects of a certain natural chemical in the body (GABA).
What is Esparon used for?
Esparon is used to treat anxiety disorders and panic disorder (sudden, unexpected attacks of extreme fear and worry about these attacks). Alprazolam is in a class of medications called benzodiazepines. It works by decreasing abnormal excitement in the brain.
Is Esparon a sleeping pill?
Esparon belong to a class of medicines called benzodiazepines and hydrocodone belongs to the class of medicines called opioids. Both the classes cause sedation (increased tendency to sleep) and respiratory depression (slow and difficult breathing).
What are the side effects of Esparon?
Common side effects of Esparon include:
- Drowsiness
- Depression
- Headache pain
- Constipation
- Diarrhea
- Dry mouth
- Impaired coordination
- Increased or decreased appetite
- Fatigue
- Memory problems
- Irritability
- Decreased salivation
- Cognitive disorders
- Insomnia
- Lightheadedness
- Fainting
- Difficulty speaking
- Nausea/vomiting
- Weight gain or weight loss
- Nasal congestion
- Decreased or increased libido
- Menstrual disorder
- Difficulty urinating
- Fast heart rate
- Confusion
- Blurred vision
- Low blood pressure (hypotension)
- Agitation/restlessness
- Dizziness
- Increased salivation
- Nervousness
- Tremor
- Talkativeness
- Incontinence
What should avoid while taking Esparon?
Notes for Consumers: Grapefruit juice and grapefruit-containing foods may increase the actions or side effects (such as drowsiness or slowed breathing) of Esparon. Avoid taking Esparon with grapefruit juice (or grapefruit) whenever possible, and do not increase your intake of grapefruit while taking Esparon.
Does anyone take Esparon daily?
People stop feeling the effects of Esparon long before it leaves the body, which is why it is often taken more than once a day. It's important to take it as prescribed. Taking too many doses can lead to dependence and accidental overdose.
Is Esparon a steroid?
Esparon is a Schedule IV controlled substance and is a common drug of abuse.
Is Esparon an antidepressant?
Esparon appears to be an effective antidepressant in the treatment of outpatients who have a diagnosis of major depressive disorder. The authors have reviewed six controlled double-blind studies of Esparon in the treatment of depression.
Does Esparon cause liver damage?
Esparon, like other benzodiazepines, is rarely associated with serum ALT elevations, and clinically apparent liver injury from Esparon is extremely rare. There have been a few case reports of acute liver injury from Esparon and recurrence on reexposure has been reported.
Is one .25 Esparon a day addictive?
Esparon is a benzodiazepine used to treat anxiety and insomnia. The drug is extremely addictive and should only be used under a doctor's supervision.
Will doctors prescribe Esparon long-term?
It can be used short-term as a way to offer people immediate relief from their symptoms or as part of a long-term management plan for GAD or panic disorder. Esparon is often prescribed for panic attacks, which can occur as part of SAD.
How long should I take Esparon?
Esparon is a powerful benzodiazepine that is only recommended for use for up to six weeks.
Does Esparon cause memory loss?
Several research studies have found that chronic or heavy Esparon use can cause short-term memory loss. This is listed by the National Institutes of Health (NIH) as one of the more serious side effects of Esparon requiring immediate medical attention.
Does Esparon help with racing thoughts?
Esparon may be prescribed to treat symptoms of the manic phase of bipolar disorder. These symptoms include: racing thoughts and speech. high energy.
Can Esparon help mild depression?
Esparon is a medication that is approved by the Food and Drug Administration (FDA) to treat anxiety and panic disorders. Esparon, which is the Esparon name for the generic drug alprazolam, isn't usually used to treat depression because there are several newer and safer medications available.
Is Esparon safe to use?
Esparon is a safe and effective medication when used as directed. Benzodiazepines may produce emotional and/or physical dependence (addiction) even when used as recommended. Physical dependence may develop after 2 or more weeks of daily use.
What is the most Esparon a doctor can prescribe?
For anxiety disorders, the dosage for adults typically starts at 0.25 mg to 0.5 mg three times per day. A doctor may incrementally increase the dosage to maximize the effect. However, the maximum dosage does not usually exceed 4 mg per day. For panic disorders, the required dose of Esparon may exceed 4 mg per day.
Can Esparon make anxiety worse?
Recent studies evaluating the effectivity of Esparon for anxiety have shown that after just 8 weeks, those that were on a Esparon prescription had worse anxiety than those who took a placebo. Despite these results, doctors continue to prescribe these benzos for anxiety disorders at an alarming rate.
How long does the Esparon high last for?
Esparon has an average half-life of roughly 11 hours in healthy adults. In other words, it takes 11 hours for the average healthy person to eliminate half of the dose of Esparon.
