Escivex 5/Escivex 10

Escivex 5/Escivex 10

escitalopram

Manufacturer:

Vexxa Lifesciences

Distributor:

VE Pharma
Full Prescribing Info
Contents
Escitalopram oxalate.
Description
Escivex 5: Each film coated tablet contains: Escitalopram Oxalate USP eq. to Escitalopram 5 mg. Colour: Titanium Dioxide BP.
Escivex 10: Each film coated tablet contains: Escitalopram Oxalate USP eq. to Escitalopram 10 mg. Colour: Titanium Dioxide BP.
Escitalopram Oxalate is a Fine white to slightly-yellow powder and Freely soluble in methanol and dimethyl sulfoxide, sparingly soluble in water and in alcohol, very slightly soluble in ethyl acetate, and in isopropyl alcohol, insoluble in eptanes. Escitalopram Oxalate molecular weight is 414.43, Molecular formula is a C20H21FN2O·C2HO2 and chemical name is S-(+) 5-Isobenzofurancarbonitrile, 1-[3-(dimethylamino) propy1]-1-(4-fluorophenyl)-1, 3-dihydro-, oxalate; S-(+)-1-[3 (Dimethylamino) propy1]-1-(p-fluoropheny1)-5-phthalan-Carbonitrile oxalate.
Action
Pharmacological Classification: Antidepressant.
Pharmacology: Pharmacodynamics: Mechanism of action: Escitalopram is a selective inhibitor of serotonin (5-HT)-uptake. Escitalopram has minimal effect on noradrenaline (NA), dopamine (DA) and gamma aminobutyric acid (GABA) uptake. Escitalopram has no or very low affinity for a series of receptors including 5-HT1A, 5-HT2, DA, D1 and D2 receptors, alpha1-, alpha2-, beta-adrenoceptors, histamine H1, muscarine cholinergic, benzodiazepine and opioid receptors.
Pharmacokinetics: Absorption: Absorption is independent of food intake (mean Tmax is 4 hours after multiple dosing).
Distribution: The apparent volume of distribution (Vd, a/F) after oral administration is about 12 to 26 L/kg. The plasma protein binding of escitalopram is approximately 55%.
Biotransformation: Escitalopram is metabolised in the liver to the demethylated and didemethylated Metabolite. Alternatively, the nitrogen may be oxidised to form the N-oxide metabolite. Both parent substance and metabolites are partly excreted as glucuronides. Unchanged Escitalopram is the predominant compound in plasma. After multiple dosing the mean concentrations of the demethyl- and didemethyl metabolites are usually 28 - 31% and <5% of the escitalopram concentration, respectively. Biotransformation of escitalopram to the demethylated metabolite is mediated by a combination of CYP2C19, CYP3A4 and CYP2D6.
Elimination: The elimination half-life (t½ beta) after multiple dosing is about 30 hours and the oral plasma clearance (ClOral) is about 0.6 L/min. Escitalopram and major metabolites are - like racemic citalopram - assumed to be eliminated both by the hepatic (metabolic) and the renal routes with the major part of the dose excreted as metabolites in urine. Hepatic clearance is mainly by the P450 enzyme system. CYP2C19 is the primary isoenzyme involved in the demethylation of Escitalopram, followed by CYP3A4 and CYP2D6.
Indications/Uses
Treatment of major depressive disorder.
Dosage/Direction for Use
Adults: Major depressive episodes: Escitalopram Tablets should be administered as a single oral dose of 10 mg daily in otherwise healthy adults. Depending on individual patient response, the dose may be increased to a maximum of 20 mg daily.
Usually 2-4 weeks are necessary for an antidepressant response.
Panic disorder: A single oral dose of 5 mg is recommended for the first week before increasing the dose to 10 mg daily. The dose may be further increased, up to a maximum of 20 mg daily, dependent on individual patient response.
Elderly patients (>65 years of age): A longer half-life and a decreased clearance have been demonstrated in the elderly, therefore a lower initial and maximum dose should be considered.
Reduced renal function: Dosage adjustment is not necessary in patients with mild or moderate renal impairment. No information is available on the treatment of patients with severely reduced renal function (creatinine clearance <30 mL/min).
Reduced hepatic function: Dosages should be halved to the lower end of the dose range in patients with hepatic insufficiency. When stopping Escitalopram Tablets therapy, gradual dose reduction should be considered.
Escitalopram Tablets is administered as a single daily dose. Escitalopram Tablets may be taken without regard to food intake or as prescribed by the physician.
Overdosage
Symptoms: Doses of 190 mg have been taken without any symptoms being reported.
Treatment: There is no specific antidote. Treatment is supportive and symptomatic. Gastric lavage should be carried out as soon as possible after oral ingestion. Cardiac and vital signs monitoring are recommended along with general symptomatic supportive measures.
Contraindications
Children, as safety and efficacy have not been established in this population.
Monoamine Oxidase Inhibitors: Cases of serious reactions have been reported in patients receiving an SSRI such as Escitalopram in combination with a monoamine oxidase inhibitor (MAOI), and in patients who have recently discontinued an SSRI and have been started on an MAOI.
Some cases presented with features resembling serotonin syndrome.
Escitalopram should not be used in combination with a MAOI. Escitalopram may be started 14 days after discontinuing treatment with a MAOI. At least 7 days should elapse after discontinuing Escitalopram treatment before starting a MAOI.
Warnings
Mania: Escitalopram Tablets should be discontinued in any patient entering a manic phase. Escitalopram Tablets should be used with caution in patients with a history of mania/hypomania.
Paradoxical anxiety: Some patients with panic disorder may experience increased anxiety symptoms at the start of treatment with antidepressants. This paradoxical reaction usually subsides within two weeks during continued treatment. A low starting dose is advised to reduce the likelihood of a paradoxical anxiogenic effect.
Seizures: Escitalopram Tablets should be discontinued in any patient who develops seizures. Escitalopram Tablets should be avoided in patients with unstable epilepsy and patients with controlled epilepsy should be carefully monitored. Escitalopram Tablets should be discontinued if there is an increase in seizure frequency.
Diabetes mellitus: In patients with diabetes mellitus, treatment with Escitalopram Tablets may alter glycaemic control, possibly due to improvement of depressive symptoms. Insulin and/or oral hypoglycaemic dosage may need to be adjusted.
Suicide: As improvement may not occur during the first few weeks or more of treatment, patients should be closely monitored during this period. The possibility of a suicide attempt is inherent in depression and may persist until significant therapeutic effect is achieved.
Haemorrhage: There have been reports of cutaneous bleeding abnormalities, such as ecchymoses and purpura with Escitalopram Tablets. Caution is advised in patients taking Escitalopram Tablets, particularly in concomitant use with medicines known to affect platelet function (e.g. atypical anti-psychotics and phenothiazines, most tricyclic antidepressants, aspirin and non-steroidal anti-inflammatory medicines (NSAIDs)), as well as in patients with a history of bleeding disorders.
ECT (electroconvulsive therapy): There is limited published clinical experience of concurrent administration of Escitalopram Tablets and ECT, therefore caution is advisable.
Adverse Reactions
Adverse reactions observed with Escitalopram are most frequent during the first one or two weeks of treatment and may decrease in intensity and frequency with continued treatment.
After prolonged administration abrupt, cessation of Escitalopram may produce withdrawal reactions in some patients.
Cardiovascular disorders: Uncommon: Postural hypotension.
Metabolic and nutritional disorders: Common: Decreased appetite. Incidence unknown: Hyponatraemia, inappropriate ADH secretion.
Psychiatric disorders: Incidence unknown: Hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, nervousness.
Neurological disorders: Common: Insomnia, somnolence, dizziness, fatigue, drowsiness. Uncommon: Sleep disorder, taste disorder. Incidence unknown: Seizures, tremor, movement disorders, serotonin syndrome (typically characterised by a rapid onset of changes in mental state with confusion, mania, agitation, hyperactivity, shivering, fever, tremor, ocular movements, myoclonus, hyperreflexia and incoordination).
Respiratory, thoracic and mediastinal disorders: Common: Sinusitis, yawning.
Gastrointestinal disorders: Common: Nausea, vomiting, diarrhoea, constipation, anorexia. Incidence unknown: Dry mouth.
Hepato-biliary disorders: Incidence unknown: Abnormal liver function tests.
Skin and subcutaneous tissue disorders: Common: Increased sweating. Incidence unknown: Rash, pruritus, ecchymoses, angioedema.
Musculoskeletal, connective tissue and bone disorders: Incidence unknown: Arthralgia, myalgia.
Renal and urinary disorders: Incidence unknown: Urinary retention.
Reproductive system and breast disorders: Common: Decreased libido (men and women), ejaculation disorder and impotence (male), anorgasmia (female), galactorrhoea.
Eye disorders: Uncommon: Abnormal vision.
General disorders: Common: Pyrexia. Incidence unknown: Anaphylactic reactions.
Drug Interactions
Escitalopram has a low potential for clinically significant medicine interactions. In vitro studies have shown that the biotransformation of Escitalopram to its demethylated metabolites depends on three parallel pathways (cytochrome P450 (CYP) 2C19, 3A4 and 2D6). Escitalopram is a very weak inhibitor of isoenzyme CYP1A2, 2C9, 2C19, 2E1 and 3A and weak inhibitor of 2D6.
Effects of other medicinal products on Escitalopram in vivo.
The pharmacokinetics of single doses of Escitalopram were not changed by coadministration with a single dose of ritonavir (CYP3A4 inhibitor). Furthermore coadministration with ketoconazole (potent CYP3A4 inhibitor) did not change the pharmacokinetics of racemic citalopram.
Coadministration of racemic citalopram with cimetidine (potent CYP2D6, 3A4 and 1A2 inhibitor) resulted in increased plasma concentrations of the racemate (43% increase in AUC, 39% increase in Cmax). Thus, caution should be exercised at the upper end of the dose range of Escitalopram when used concomitantly with high doses of cimetidine.
Storage
Store at temperature not exceeding 30°C. Protect from light.
Shelf Life: Escivex 5: 2 years from date of manufacturing.
Escivex 10: 3 years from date of manufacturing.
MIMS Class
ATC Classification
N06AB10 - escitalopram ; Belongs to the class of selective serotonin reuptake inhibitors. Used in the management of depression.
Presentation/Packing
Escivex 5: FC tab 5 mg (white to off white round, biconvex, plain on the both side) x 30's.
Escivex 10: FC tab 10 mg (white to off white round, biconvex, plain on the both side) x 30's.
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