Ezolent Forte
Ezolent Forte Uses, Dosage, Side Effects, Food Interaction and all others data.
Citalopram is an orally administered selective serotonin reuptake inhibitor (SSRI) with a chemical structure unrelated to that of other SSRIs, tricyclic, tetracyclic or other available antidepressant agents. The mechanism of action of Citalopram as an antidepressant is presumed to be linked to potentiation of serotonergic activity in central nervous system resulting from its inhibition of CNS neuronal reuptake of serotonin (5-HT).
Citalopram belongs to a class of antidepressants known as selective serotonin reuptake inhibitors (SSRIs). It has been found to relieve or manage symptoms of depression, anxiety, eating disorders and obsessive-compulsive disorder among other mood disorders. The antidepressant, anti-anxiety, and other actions of citalopram are linked to its inhibition of CNS central uptake of serotonin . Serotonergic abnormalities have been reported in patients with mood disorders. Behavioral and neuropsychological of effects of serotonin include the regulation of mood, perception, reward, anger, aggression, appetite, memory, sexuality, and attention, as examples. The onset of action for depression is approximately 1 to 4 weeks. The complete response may take 8-12 weeks after initiation of citalopram .
In vitro studies demonstrate that citalopram is a strong and selective inhibitor of neuronal serotonin reuptake and has weak effects on norepinephrine and dopamine central reuptake. The chronic administration of citalopram has been shown to downregulate central norepinephrine receptors, similar to other drugs effective in the treatment of major depressive disorder. Citalopram does not inhibit monoamine oxidase .
Etizolam is a thienodiazepine which is chemically related to benzodiazepine (BDZ) drug class; it differs from BDZs in having a benzene ring replaced with a thiophene ring. It is an agonist at GABA-A receptors and possesses amnesic, anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. Initially introduced in 1983 in Japan as treatment for neurological conditions such as anxiety and sleep disorders, etizolam is marketed in Japan, Italy and India. It is not approved for use by FDA in the US; however it remains unscheduled in several states and is legal for research purposes.
Etizolam is a CNS depressant with anxiolytic, anticonvulsant, sedative-hypnotic and muscle relaxant effects. It acts on the benzodiazepine site of the GABA-A receptor as an agonist to increase inhibitory GABAergic transmission throughout the central nervous system. Studies indicate that etizolam mediates its pharmacological actions with 6 to 10 times more potency than that of diazepam. Clinical human studies performed in Italy showed clinical effectiveness of etizolam in relieving symptoms in patients with generalized anxiety disorders with depressive symptoms . Etizolam also mediates imipramine-like neuropharmacological and behavioral effects, as well as minor effects on cognitive functioning. It is shown to substitute the actions of a short-acting barbiturate, pentobarbitol, in a drug discrimination study .Etizolam is an antagonist at platelet-activating-factor (PAF) receptor and attenuates the recurrence of chronic subdural hematoma after neurosurgery in clinical studies . It is shown to inhibit PAF-induced bronchoconstriction and hypotension .
| Trade Name | Ezolent Forte |
| Generic | Citalopram + Etizolam |
| Weight | 0.5mg |
| Type | Tablet |
| Therapeutic Class | |
| Manufacturer | Talent India |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Citalopram is used for depressive illness and panic disorder. It is also used for substance abuse disorders and alcohol dependence. Citalopram has also been given in variety of anxiety disorders including obsessive-compulsive disorder and social phobia. It is also effective in generalized anxiety disorder, post-traumatic stress disorder, premenstrual syndrome, idiopathic Parkinson's disease and eating disorder.
Etizolam is a thienodiazepine derivative used to treat anxiety and insomnia.
Indicated for the treatment of generalized anxiety disorder with depression, panic disorder and insomnia.
Ezolent Forte is also used to associated treatment for these conditions: Anorexia Nervosa (AN), Bulimia Nervosa, Depression, Diabetic Neuropathies, Major Depressive Disorder (MDD), Obsessive Compulsive Disorder (OCD), Panic Disorder, Post Traumatic Stress Disorder (PTSD), Premature Ejaculation, Premenstrual Dysphoric Disorder, Social Anxiety Disorder (SAD)Anxiety, Insomnia
How Ezolent Forte works
The mechanism of action of citalopram results from its inhibition of CNS neuronal reuptake of serotonin (5-HT) . The molecular target for citalopram is the serotonin transporter (solute carrier family 6 member 4, SLC6A4), inhibiting its serotonin reuptake in the synaptic cleft .
Citalopram binds with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs . This drug has no or neglible affinity for 5-HT1A, 5-HT2A, dopamine D1 and D2, α1-, α2-, and_ β adrenergic, _histamine H1, gamma-aminobutyric acid (GABA), muscarinic, cholinergic, and benzodiazepine receptors. Antagonism of muscarinic, histaminergic, and adrenergic receptors is thought to be associated with several anticholinergic, sedative, and cardiovascular effects of other psychotropic drugs .
Etizolam is selectively a full agonist at GABA-A receptors to increase GABAergic transmission and enhance GABA-induced Cl- currents . It is reported to bind to the benzodiazepine binding site which is located across the interface between the alpha and gamma subunits. Benzodiazapines are reported to only bind to receptors that contain gamma 2 and alpha 1/2/3/5 subunits . Alpha-1-containing receptors mediate the sedative effects of etizolam whereas alpha-2 and alpha-3 subunit-containing receptors mediate the anxiolytic effect . Etizolam shows high potency and affinity towards GABA-A receptor with alpha 1 beta 2 gamma 2S subunit combination . By binding to the regulatory site of the receptor, etizolam potentiates GABA transmission by facilitating the opening of GABA-induced chloride channels . Etizolam is a specific antagonist at PAFR. It inhibits PAF-induced platelet aggregation by inhibiting PAF binding to the receptors located on the surface of platelets with an IC50 of 22nM .
Dosage
Ezolent Forte dosage
Depressive illness 20 mg daily as a single dose in the morning or evening; increased ifnecessary to maximum 60 mg daily (Elderly maximum 40 mgdaily).Panic disorder Initially 10 mg daily, increased to 20 mg after 7 days; usual dose 20-30 mg daily; maximum 60 mg daily (Elderly maximum 40 mgdaily).
Side Effects
SSRIs are less sedating and have fewer antimuscarinic and cardiotoxic effects than tricyclic antidepressants. However, side-effects may be seen, includes gastro-intestinal effects (nausea, vomiting, dyspepsia, abdominal pain, diarrhoea, constipation), anorexia with weight loss, palpitations, tachycardia, postural hypotension, cough, confusion, impaired concentration, amnesia, urinary retention, sweating, movement disorders, urticaria, anaphylaxis, arthralgia, myalgia and photosensitivity.
Toxicity
Oral (Human) LD: 56 mg/kg Intraperitoneal (Mouse) LD50: 179 mg/kg
Acute toxicity
Symptoms of toxicity include dizziness, sweating, nausea, vomiting, tremor, somnolence, and sinus tachycardia. Rarely, symptoms included amnesia, confusion, coma, convulsions, hyperventilation, cyanosis, rhabdomyolysis, and ECG changes (including QTc prolongation, nodal rhythm, ventricular arrhythmia, and extremely rare cases of cardiac torsade de pointes) may occur. Acute renal failure has been a rare occurrence .
In cases of overdose, establish and maintain the airway to ensure adequate ventilation and oxygen delivery. Due to the large volume of distribution of citalopram, forced diuresis, dialysis, hemoperfusion, and exchange transfusion are unlikely to be of benefit. Gastric evacuation by lavage and use of activated charcoal should be considered. Careful observation and cardiac and vital sign monitoring are advised, in addition to supportive care. With the large volume of distribution of citalopram, forced diuresis, dialysis, hemoperfusion, and exchange transfusion are unlikely to be of benefit .
Pregnancy
This drug is categorized as pregnancy category C. In animal reproduction studies, citalopram has been shown to have adverse effects on embryo/fetal and postnatal development, which includes teratogenic effects when given at doses higher than human therapeutic doses. There are no sufficient and well-controlled studies in pregnant women; therefore, citalopram should be used during pregnancy only in cases where the potential benefit justifies the possible risk to the fetus .
Pregnancy-Nonteratogenic Effects
Neonates exposed to celexa and other SSRIs or SNRIs, late in the third trimester, have undergone complications requiring prolonged hospitalization, respiratory support, and parenteral feeding. Complications such as these can arise immediately upon delivery .
Nursing Mothers
Citalopram is excreted in human breast milk. There have been two reports of infants demonstrating high levels of somnolence, reduced feeding, and weight loss associated with breastfeeding from a mother taking citalopram. In one specific case, the infant was reported to recover completely after the discontinuation of citalopram. In the second case, no follow-up information was available for assessment. The decision whether to continue or discontinue either nursing or celexa should consider the risks of citalopram exposure for the infant versus the benefits of celexa treatment for the mother .
Major adverse effects include drowsiness, sedation, muscle weakness and incoordination, fainting, headache, confusion, depression, slurred speech, visual disturbances and changes in libido and tremor . Flumazenil is a competitive antagonist of GABA-A receptors and can be also used to reverse the effect of etizolam overdosage. Etizolam demonstrates no effects on fertility, development and teratogenicity . LD50 values of etizolam when delivered orally, intraperitoneally, and subcutaneously are 3509mg/kg, 825mg/kg, and >5000mg/kg in rats, respectively, and 3070mg/kg, 783mg/kg and 5000mg/kg in mice, respectively .
Precaution
Caution should be taken in patients with epilepsy, concurrent electroconvulsive therapy, history of mania, cardiac disease, diabetes mellitus, angle-closure glaucoma, history of bleeding disorders, hepatic and renal impairment. Abrupt withdrawal of Citalopram should be avoided.
Interaction
Ketoconazole, Itraconazole or Macrolide antibiotics and Citalopram co-administration decreases the metabolism of Citalopram. Omeprazole and Citalopram co-administration might decrease the clearance of Citalopram.
Volume of Distribution
12 L/kg
Citalopram is highly lipophilic and likely widely distributed throughout the body, including the blood-brain-barrier. However, its metabolite, demethylcitalopram does not penetrate the blood-brain-barrier well .
Apparent distribution volume was 0.9 ± 0.2 L/kg following a single oral doing of 0.5mg etizolam .
Elimination Route
Rapidly and well absorbed from the GI tract. Peak plasma concentrations occur within 4 hours of a single orally administered dose. Bioavailability is 80% following oral administration. Food does not affect absorption .
Etizolam is well absorbed from the intestines with a biological bioavailability of 93% following oral administration. After a single oral dosing of 0.5mg etizolam, it takes approximately 0.9 hours to reach the peak plasma concentration of 8.3 ng/mL .
Half Life
About 35 hours .
The average elimination half life of etizolam following a single oral dose of 0.5mg is 3.4 hours but may be increased up to 17 hours depending on the rate of metabolism . The main metabolite α-hydroxyetizolam displays a longer elimination half life of 8.2 hours .
Clearance
The systemic clearance of citalopram is 330 mL/min, with approximately 20% renal clearance .
Elimination Route
12-23% of an oral dose of citalopram is found unchanged in the urine, while 10% of the dose is found in the faeces .
In a rat study, the amounts of etizolam excreted was 30% in urine was 70% in feces, while the values in a mouse study were 40% in urine and 60% in feces .
Pregnancy & Breastfeeding use
PregnancyThere are no adequate and well-controlled studies in pregnant women; therefore, Citalopram should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
LactationCitalopram is excreted in human breast milk. So, the decision whether to continue or discontinue either nursing or Citalopram therapy should take into account the risks of Citalopram exposure for the infants and the benefits of Citalopram treatment for the mother.
Contraindication
Citalopram should not be used if the patient enters a manic phase. Concomitant use in patients taking MAO inhibitor is contraindicated. Citalopram is contraindicated in patients with a hypersensitivity to this drug or any of its ingredients.
Acute Overdose
It is a very safe drug. There were no reports of fatal Citalopram overdose in clinical trials involving overdoses of up to 2000 mg.
Symptoms: Dizziness, sweating, nausea, vomiting, tremor, somnolence and sinus tachycardia. Rarely, amnesia, confusion, coma, seizures, hyperventilation, cyanosis, rhabdomyolysis and ECG changes (e.g. QT prolongation, sinus bradycardia, ventricular arrhythmias, nodal rhythm, torsade de pointes and left bundle branch block).
Management: Symptomatic and supportive treatment. Maintain and ensure adequate ventilation and oxygenation. Gastric evacuation by lavage and use of activated charcoal should be considered. Frequently monitor cardiac function and vital signs.
Storage Condition
Store at 25° C.
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