No Deprine tablets
Trade name:
n0 Deprine tablets.
Generic name:
Tofisopam.
Composition :
1- Active Ingredients:
Each tablet contains: Tofisopam 50 mg.
2- Inactive Ingredients:
– Starch, Lactose, Talc, Avicel & Magnesium Stearate.
Pharmaceutical form:
Scored tablets.
Pharmacological actions:
– Tofisopam belongs to an anti-anxiety group of medications known as homophthalazines (e.g. girisopam, nerisopam, tofisopam). which show strong anxiolytic potency with insignificant muscle relaxant and anticonvulsive activity, so differ from ordinary benzodiazepines e.g. diazepam. They are Formerly called 2,3-benzodiazepine derivatives.
– In contrast to diazepam (10 mg) and lorazepam (2.5 mg), tofisopam (75-\50 mg) did not impair psychomotor Function (sedation, dizziness, mood enhancing effect. muscle relaxation or fatigue) in volunteers.
– The administration of tofizopam does not lead to physical or psychic dependence.
– Tofisopam was screened against approximately 60 receptors. The compound exhibited little or no affinity at any site tested, including the OABA/benzodiazepine receptor. These data indicate that tofisopam has a unique neurochemical and behavioral profile, clearly distinct from classical benzodiazeplnes.
– Tofisopam. in contrast to clinically effective 1,4-benzodiazepines, does not displace the binding of (‘H)-BDZs From their binding site at GABAA receptors in vitro or in vivo, It enhances the binding of GABA agonists to GABA receptors (GABA binding site on GABA receptors).
– A Further potential site of action of tofisopam is the BDZ peripheral-type binding site.
Pharmacokinetics :
– The pharmacokinetics and metabolism of tofisopam were-studied in animals and humans, The phannacokinetics profile of the compound can be described by a two-compartment open model, where the absorption and distribution r,hase were found to be rapid, The unchanged tofisopam and I Ctotal radioactivity were eliminated From human plasma with a biological half-life (t beta 1/2) of 2.7-3.5 hours and 15-21 hours, respectively, which show a slower elimination of the metabolites. The main route of elimination was the excretion of the mainly conjugated metabolites in urine and/or faeces, depends on the species. The major route of biotransfonnation was mono-, di-, tri- and tetra-O-demethylation in
the various degree and positions of aromatic ring(s).
indications :
1- n0 Deprine (tofisopam) has demonstrated efficacy in a wide range of therapeutic applications, including anxiety, functional gastrointestlnal (GI) disorders, perimenopausal symptoms, hypertension, depression, and disorders of autonomic function,
2- n0 Deprine (tofisopam) is indicated as an adjuvant therapy to control psychosomatic symptoms such as headache, fatigue, tachycardia, sweating,
3- n0 Deprine (tofisopam) is effective as adjuvant therapy For treatment of paroxysmal supraventricular tachycardia.
4- n0 Deprine (tofisopam) is indicated as an adjuvant therapy to improve intestinal passage in patients with irritable colon syndrome.
5- n0 Deprine (tofisopam) is indicated as an adjuvant therapy in hypermotor dysfunction of the biliary ducts.
6- No Deprine (tofisopam) is indicated for reduction of preoperative anxiety.
Dosage and administraation:
The average daily dose is I to 2 tablets one to three times daily (50 to 300 mg per day). In case of occasional administration I to 2 tablets should be used.
Contraindications:
Presence of known hypersensitivity to any of the product ingredients.
Side effects:
– n0 Deprine (tofisopam) is well tolerated. It has a very low toxicity and mild side effects. The administration of tofizopam does not lead to physical or psychic dependence.
– Side effects are rare and include nausea, anorexia, stomach discomfort, individual increased irritability.
Drug Interactions:
– High doses of tofisopam enhance the effect of barbiturates and ethanol.
– Tofisopam has been shown to act as an inhibitor of the liver enzyme C¥P3A4. This seems to be of insignificant clinical importance.
– Tofisopam increased the blood level of medications metabolized by C¥P3A4 system (such as immunosuppressive agents) leading to clinically relevant adverse drug reaction and necessitating reduction of the dose of the drugs or discontinuation of the administration of tofisopam.
Usage In pregnancy and lactation:
– Usage in Pregnancy: Negative results have been reported in prospective studies investigating the teratogenicity of human exposure with diazepam, alprazolarn. oxazepam, lorazepam, clonazepam, medazepam. tofisopam and nitrazepam suggesting that the risk of malformation with first trimester exposure to
benzodiazepines or benzodiazepine-related agents at therapeutic doses is minimal to low.
– Usage In Lactation: Special attention should be paid to premature neonate or lf the maternal dose is particularly high.
precautions and warnings :
Excitation and hyperactivity may occur. These symptoms can be reversed by reduction of dosage or by discontinuing medication.
package :
– carton boxes of L 2, or 3 (AL{fransparent PVC) strips, each of 10 tablets & and an inner leaflet.
Storage :
– Store at temperature not exceeding 30° C and in dry place.
– Keep all medicines out of reach of children
Product of:
Alphamoun pharmaceuticals
badr city cairo egypt
