Apresin 0.5 mg+10 mg Tablet

Uses

Fluphenazine & Nortriptyline is used for emotional disturbance, anxiety, tension, fatigue, depression, headache, sleep disorder, bodyache, gastric problems

Apresin 0.5 mg+10 mg Tablet is also used to associated treatment for these conditions: Chorea, Depression, Gilles de la Tourette's Syndrome, Psychosis, SedationIrritable Bowel Syndrome (IBS), Major Depressive Disorder (MDD), Myofascial Pain Syndrome, Orofacial Pain, Pain, Chronic, Post-Herpetic Neuralgia (PHN)

How Apresin 0.5 mg+10 mg Tablet works

Fluphenazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.

Though prescribing information does not identify a specific mechanism of action for nortriptyline, is believed that nortriptyline either inhibits the reuptake of the neurotransmitter serotonin at the neuronal membrane or acts at the level of the beta-adrenergic receptors. It displays a more selective reuptake inhibition for noradrenaline, which may explain increased symptom improvement after nortriptyline therapy. Tricyclic antidepressants do not inhibit monoamine oxidase nor do they affect dopamine reuptake. As with other tricyclics, nortriptyline displays affinity for other receptors including mACh receptors, histamine receptors, 5-HT receptors, in addition to other receptors.

Dosage

Apresin 0.5 mg+10 mg Tablet dosage

Adult: One tablet three times daily. The course of the treatment should be limited to three months. If the patient does not respond after 4 weeks, an alternative treatment should be given.

Children: Not indicated for the treatment of children.

Elderly: Elderly patients should be started on one tablet twice daily. If one tablet three times a day required subsequently three tablets may be given.

Side Effects

Dryness of mouth, drowsiness, constipation, tachycardia, nasal congestion, blurred vision and excitement.

Toxicity

The oral LD50 of nortriptyline in the rat is 405 mg/kg.Symptoms of overdose with nortriptyline include cardiac arrhythmias, severe hypotension, shock, congestive heart failure, pulmonary edema, convulsions, coma, and CNS depression. Changes in the electrocardiogram, particularly in QRS segment, may be indicative of tricyclic antidepressant toxicity.

Precaution

Patients with glaucoma, prostate enlargement, cardiac failure and myocardial infarction. The drug may impair alertness and abilities to drive a car or operating machinery.

Interaction

Interactions with barbiturates, alcohol, and narcotic drugs may occur, so central depressants should be administered with caution.

Volume of Distribution

The apparent volume of distribution (Vd)β, estimated after intravenous administration is 1633 ± 268 L within the range of 1460 to 2030 (21 ± 4 L/kg). Nortriptyline crosses the placenta and is found in the breast milk. It distributes to the heart, lungs, brain, and the liver.

Elimination Route

Nortriptyline is readily absorbed in the gastrointestinal tract with extensive variation in plasma levels, depending on the patient. This drug undergoes first-pass metabolism and its plasma concentrations are attained within 7 to 8.5 hours after oral administration. The bioavailability of nortriptyline varies considerably and ranges from 45 to 85%.

Half Life

The average plasma half-life of nortriptyline in healthy volunteers is about 26 hours, but is said to range from 16 to 38 hours. One study mentions a mean half-life of about 39 hours.

Clearance

The average plasma clearance of nortriptyline in a study of healthy volunteers was 54 L/h. The average systemic clearance of nortriptyline is 30.6 ± 6.9 L / h, within the range of 18.6 to 39.6 L/hour.

Elimination Route

Nortriptyline and its metabolites are mainly excreted in the urine, where only small amounts (2%) of the total drug is recovered as unchanged parent compound. Approximately one-third of a single orally administered dose is excreted in urine within 24 hours. Small amounts are excreted in feces via biliary elimination.

Pregnancy & Breastfeeding use

Do not use during pregnancy, especially in the first and last trimesters unless there are compelling reasons. There is no evidence as to drug safety in human pregnancy, nor are the results of animal studies conclusive. Breast feeding is not recommended for women receiving this combination.

Contraindication

It is contraindicated in :

• History of gradual epilepsy or organic brain damage
• Blood dyscrasia
• Severe cardiac insufficiency
• Renal or liver damage
• Patients taking monoamine oxidase inhibitor (MAOI)
• Younger children
• Hypersensitivity to any component of the preparation

Acute Overdose

Overdosage should be treated symptomatically and supportively. If the patient is conscious, prompt gastric lavage, dilution of the stomach contents to delay absorption, or stimulation of vomiting should be attempted. An open airway should be maintained. Extrapyramidal symptoms are amenable to anti-parkinsonian drugs.

In severe hypotension, all the standard procedures for the management of circulatory shock should be substituted, e.g. vasoconstrictors and/or intravenous fluids. If vasoconstrictors are required, metaraminol, mephentermine or noradrenaline should be administered but not adrenaline, as this will further lower the blood pressure through interaction with the phenothiazine.

Storage Condition

Store below 25˚C. Protect from light & moisture.

Innovators Monograph

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