Web Page: http://www.rotapharm.co.uk/
ROTALUD (Tablets)
(Tizanidine)
1 tablet contains tizanidine (as tizanidine hydrochloride) 4 mg.
Tizanidine is a centrally acting muscle relaxant. It has direct effect on spinal cord, where it inhibits the release of excitatory amino acids that stimulate receptors sensitive towards N-methyl-Daspartate (NMDA receptors). This effect depends on stimulation of presynaptic α2-receptors. As a result, postsynaptic mechanisms, which are responsible for muscular hypertonicity, are supressed in spinal cord on the interneuron connections level, which leads to decrease of muscle tone. Apart from muscle relaxant properties, tizanidine also has central moderate analgesic effect.
Tizanidine is administered as antispasmodic in painful muscle spasms and muscle spasticity of spinal and cerebral origin. Tizanidine reduces passive resistance, spasms and clonic seizures and increases the strength of voluntary skeletal muscles contractions
When administered enterally, tizanidine is almost entirely absorbed. Total bioavailability of tizanidine reaches approximately 34% due to extensive presystemic metabolism in liver. Plasma Cmax is reached in approximately 1 hour after administration. When medication is taken with food Cmax is increased by approximately 1/3 and the maximum concentration time is reduced to approximately 40 minutes, however, the absorption level remains unchanged.
Tizanidine is well distributed in all body tissues; in enteral administration the steady-state average volume of distribution is 2.6 g/kg. Tizanidine is 30% bound to plasma proteins.
Tizanidine is rapidly metabolised in liver, approximately 95% of the administered dose is metabolised. Tizanidine metabolites are inactive.
The elimination half-life is on average 2-4 hours. Tizanidine is excreted primarily via kidneys, approximately 70%. Approximately 2.7% of tizanidine is excreted in unchanged form.
In patients with renal dysfunction (creatinine clearance less than 25 ml/min) the maximum plasma concentration is twice as high as that of healthy patients and the final period of elimination half-life is increased to approximately 14 hours and as a result AUC is increased 6 fold on average.
- developed after surgeries (e.g. due to spinal disc herniation or hip osteoarthritis);
Spasticity and pain associated with neurological disorders: multiple sclerosis, chronic myelopathy, spinal cord degenerative diseases, brain circulation disorders, stroke, head injuries, cerebral palsy, spasms of central origin.
- concomitant administration of tizanidine and fluvoxamine.
Tizanidine is usually well tolerated by the patients; in small doses the feeling of drowsiness, fatigue, dizziness, dryness of mouth, nausea or mild reduction of arterial pressure may occur. In higher doses muscle weakness, insomnia, hypotension or bradycardia are possible; in other cases – increase of blood serum transaminases.
The tablets are administered enterally with or without food and washed down with sufficient amount of water.
To relief painful skeletal muscle spasms the dose is 2-4 mg 3 times daily. If the effect is insufficient additional 2-4 mg may be administered in the evening.
In spasticity associated with neurological disorders the dose is adjusted individually, the initial dose should not exceed 6 mg (in 3 doses); the subsequent daily doses should be gradually increased by 2 – 4 mg every 3 – 7 days. Optimal therapeutic effect is reached with daily dose of 12 – 24 mg divided into 3 – 4 equally spread administrations. Daily dose should not exceed 36 mg.
The duration of treatment is determined individually.
The treatment of patients with renal impairment (creatinine clearance < 25 ml/min) should be initiated with 2 mg once daily. The dose should be increased gradually according to tolerability and efficacy of the medication. If the treatment is insufficiently effective, the dose should be increased; if there is no effect – the frequency of administration should be increased.
PACKAGING
Tablets.
10 tablets are in a blister.
1 blister together with a leaflet is in a carton box.
