It is an opioid pain reliever, a derivative of cyclohexanol. It is a non-selective agonist of MU, delta, and kappa receptors in the central nervous system.
Relief of headaches, muscle aches, joints, teeth, ears, dysmenorrhea, post-traumatic, post-surgical and gynecological.
It is indicated in the symptomatic treatment of mild to moderate pain, whatever its type, intensity, origin and location. Mainly used in large doses in trauma, rheumatological, oncological, otorhinolaryngological, neurological, pre and postoperative and dental types.
Nefersil contains clonixin, vitamin B1 (thiamine hydrochloride), vitamin B1 (thiamine nitrate), vitamin B12 (cyanocobalamin), vitamin B12 (hydroxocobalamin), and vitamin B6 (pyridoxine hydrochloride).
Tramadol is a racemate (+) and (-) of isomers (50% / 50%) that in various ways are involved in analgesic effects.
The (+) isomer is a pure agonist opioid receptor, has a low tropism and has a pronounced selectivity for different receptor subtypes. The (-) isomer that inhibits neuronal uptake of norepinephrine activates downward noradrenergic influence.
That is why the transmission of pain impulses in the jelly-like substance of the spinal cord is broken.
Nefersil causes sedation. In therapeutic doses, this drug has almost no respiratory depression. Tramadol also has an antitussive effect.
Dosage and administration
Nefersil is used as subcutaneous, intravenous, intramuscular, intralumbar and oral injections.
After oral administration, Nefersil is rapidly and almost completely absorbed from the gastrointestinal tract (90%). Cmax in plasma obtained in 2 hours after taking this medicine. Bioavailability in a single dose is 68% and increases with repeated use.
The plasma protein binding is 20%. Tramadol is widely distributed in tissues. The volume of distribution after oral administration and intravenous injection is 306L and 203L, respectively.
This drug crosses the placental barrier in a concentration equal to the concentration of the active substance in plasma. 0.1% is excreted in human milk.
Tramadol metabolized by demethylation and conjugation to 11 metabolites, of which only 1 is active. This drug excreted by the kidneys 90% and through the intestines 10%.
With anemia associated with Nefersil deficiency it is introduced at 100 mcg to 200 mcg in 2 days.
After oral administration, Nefersil is absorbed from the gastrointestinal tract. The course of treatment with Nefersil is 2 weeks.
To prevent deficiency : intravenous or intramuscular for 1 mg once a month.
For treatment : intravenously or intramuscularly for 1 mg per day for 1-2 weeks, the maintenance dose is 1 to 2 mg intravenously or intramuscularly for 1 per week, up to 1 per month.
The duration of treatment is determined individually.
Simultaneous administration of Nefersil with:
In an application of Nefersil with hormonal contraceptives for oral administration may decrease the concentration of cyanocobalamin in plasma.
Drugs that exert a depressing effect on the central nervous system or with ethanol may increase the central nervous system depressant effects of tramadol. Monoamine oxidase inhibitors are probably the development of serotonin syndrome.
Serotonin reuptake inhibitors, tricyclic antidepressants, antipsychotics, other means to lower the threshold of seizure readiness, increases the risk of seizures, opioid analgesics are likely to reduce analgesic action.
The warfarin and phenprocoumon increase the anticoagulant effect, carbamazepine reduced plasma concentration of tramadol and its analgesic effect, paroxetine describes cases serotonin syndrome seizures. Sertraline, fluoxetine describes cases of serotonin syndrome.
Since lysine does not alter clonixinate clotting, it does not interact with anticoagulant drugs and does not require dose adjustments. Concomitant use of anticholinergic drugs that should be avoided due to the possibility that atropine improves its effects.
Acute intoxication with alcohol and drugs, providing a depressing effect on the central nervous system, children up to 1 year of age and hypersensitivity to Nefersil.
Hypersensitivity to any component. It should be used with caution in patients with a history of coronary artery disease, peripheral vascular disease, severe hypertension, advanced liver or kidney failure.
It is contraindicated in patients with active peptic ulcer or gastrointestinal bleeding. There is no association with macrolide antibiotics or beta blockers.
Occasionally, nausea, dizziness, and drowsiness were mild and transient. On rare occasions, and when administering high doses, the appearance of dry mouth or constipation is possible.
In patients with a history of peptic ulcer, it should be administered with caution. Safety studies in the gastrointestinal tract showed that lysine clonixinate has no deleterious effects on the mucosa and does not induce bleeding.
Restrictions on use during pregnancy and lactation: Although the effect on pregnancy has not been experimentally demonstrated, it is not recommended to administer it during pregnancy and lactation, unless the doctor considers that the potential benefit outweighs the potential risks.