Index
It is a trademark that contains in its composition the following active principles:
- Ciclobenzaprine.
- Clonixino.
Forms and presentation
- Film-coated tablets: Box of 20.
Composition
- Each tablet contains: Lysine Clonixinate: 125mg, Cyclobenzaprine HCl: 5mg.
- Exipients: magnesium stearate, corn starch, hydroxypropyl methylcellulose, microcrystalline cellulose, patent blue V aluminum lake, triacetin, titanium dioxide.
Properties
Dorixina Relax, due to its lysine cloxinate component, is an NSAI drug, with mainly analgesic action. This exerts its effect by inhibiting the synthesis of prostaglandins .
It was recently shown that it acts mainly on the enzyme that catalyzes the production of prostaglandins responsible for inflammation (cyclooxygenase-2 or COX-2) with less activity in the kidneys (cyclooxygenase-1 or COX-1), where these substances play a role of protection
The cyclobenzaprine component relieves locally derived skeletal muscle spasm without interfering with muscle function.
Cyclobenzaprine relieves muscle spasm and reduces tonic somatic motor activity, which influences the gamma and alpha motor systems at the central nervous system level.
Pharmacokinetics
Lysine clonixinate is rapidly absorbed, reaching its peak plasma level between 40-60 minutes after consumption. Its bioavailability is approximately 56%, with some individual variability.
The plasma half-life of lysine cloxinate in humans is approximately 1.75 ± 0.10 hours (mean ± SD). It is excreted mainly in the urine (60%), in the form of metabolites. From the plasma concentration, its concentration in milk is approximately between 7-10%.
Cyclobenzaprine is easily absorbed and circulates highly bound to plasma proteins. It is primarily metabolized in the liver and predominantly excreted through the kidney. It is cleared fairly slowly with an effective half-life ranging from 1 to 3 days.
Indications
Dorixina Relax is indicated for the treatment of musculoskeletal pain, especially when it is associated with muscle spasms.
Contraindications
- Hypersensitivity to lysine clonixinate or cyclobenzaprine.
- Be pregnant.
- Pediatric patients under 15 years of age.
- Gastroduodenal hemorrhage or active peptic ulcer.
Also in patients with a history of:
- Nasal polyps.
- Bleeding
- Urticaria.
- Angioedema.
Caused by the administration of NSAIDs (non-steroidal anti-inflammatory drugs) or by the administration of acetylsalicylic acid (aspirin).
Due to the cyclobenzaprine component it is contraindicated during the concomitant administration of monoamine oxidase inhibitors (MAOIs) or within 2 weeks after its discontinuation. It should also not be administered to patients with:
- Arrhythmia.
- Heart failure.
- Recent acute myocardial infarction.
- Conduction disturbances.
- Heart block
- Hyperthyroidism
Precautions
In cases of allergic skin and / or mucosal reactions or symptoms of peptic ulcer or gastrointestinal bleeding, discontinue treatment with Dorixina Relax. The cyclobenzaprine component can enhance:
- Barbiturates.
- The CNS depressant effects.
- The depressant effects of alcohol.
Caution should be exercised when administered to patients with a history of digestive diseases such as gastroduodenal peptic ulcer or gastritis and in patients treated with anticoagulants.
Although no cases have been reported with the administration of lysine clonixinate, NSAIDs are known to inhibit the synthesis of prostaglandins that have a supporting role in the maintenance of renal perfusion.
The administration of NSAIDs (non-steroidal anti-inflammatory drugs) can precipitate a manifest renal decompensation, generally reversible with the discontinuation of the product in patients with impaired renal blood flow. Patients with the highest risk of presenting this reaction are:
- Nephrotic syndrome.
- Patients with congestive heart failure.
- Dehydrated patients.
- Patients taking diuretics.
- Patients who underwent major surgeries with subsequent hypovolemia.
- Patients with liver cirrhosis.
- Patients with other overt kidney diseases.
In these patients, urine output volume and renal function should be monitored before starting therapy.
Although it was also not observed during lysine clonixinate treatment, the administration of NSAIDs (non-steroidal anti-inflammatory drugs) may increase the plasma levels of other liver parameters or transaminases.
Cyclobenzaprine, chemically related to the tricyclic antidepressant and parasympatholytic drugs, should be used with caution in people:
- Who consume anticholinergic medications.
- History of closed glaucoma .
- With increased IOP.
- History of urinary retention.
Pediatric use
The use of this medicine is contraindicated in pediatric patients under 15 years of age, since there are no studies that verify the effects of the administration of cyclobenzaprine in these patients.
Geriatric use
This medicine must be administered with caution to the elderly, since, as with other anti-inflammatory drugs, it can cause damage to the liver or kidney and heart functions of these patients.
Interactions with other medications
NSAID medications (including high doses of acetylsalicylic acid): Due to their synergistic action, there is an increased risk of bleeding and gastroduodenal ulcers.
Ticlopidine, heparin (systemic administration), thrombolytics, oral anticoagulants: increased risk of bleeding.
It is necessary to maintain strict controls of blood coagulation by adjusting the doses of the drugs that modify the coagulation parameters in the event that joint use of these drugs is unavoidable.
Lithium: NSAIDs generally increase plasma levels of lithium. Monitor plasma lithium levels closely when starting, changing or stopping Dorixina Relax treatment.
Methotrexate: Concomitant treatment with methotrexate and NSAIDs may increase the haematological toxicity of methotrexate. Strict hematological controls should be done in these cases.
Diuretics: treatment with NSAIDs increases the risk of acute renal failure in dehydrated patients. In the cases of concomitant treatment with lysine clonixinate and diuretics, patients must be adequately hydrated and their renal function controlled before starting treatment.
Antihypertensives (eg beta-adrenergic receptor blockers, ACE inhibitors, vasodilators: during concomitant treatment with antihypertensives and NSAIDs, a decrease in the antihypertensive effect due to inhibition of vasodilator prostaglandins has been reported.
Due to the interaction of the cyclobenzaprine component with MAO inhibitors, it can trigger hyperpyretic seizures, seizures and fatal outcome. When co-administered with guanethidine and similarly acting compounds, it can theoretically block its antihypertensive action.
Ability to drive and use machinery
Cyclobenzaprine can affect the mental and / or physical abilities required to perform dangerous tasks, such as operating machinery or driving a motor vehicle.
Pregnancy
The administration of Dorixina Relax is not allowed when a woman is in condition.
This is because there is insufficient evidence of the effects of these drugs in pregnant women, despite the fact that preclinical toxicological studies did not show tetratogenic effects with the use of lysine clonixinate and cyclobenzaprine.
Lactation
Before the consumption of the drug in mothers who are breastfeeding, the risks and benefits should be evaluated since it is unknown if cyclobenzaprine passes into breast milk.
Side effects
At therapeutic doses, Dorixina Relax is well tolerated. In rare cases, especially when administered to sensitive patients, they may present some symptoms such as:
- Gastritis.
- Drowsiness.
- Sickness.
- Vomiting
Less frequently (only 1-3% of patients have these symptoms):
- Headache.
- Blurry vision.
- Dyspepsia.
- Asthenia.
- Sickness.
- Constipation.
- Unpleasant taste in the mouth.
With an incidence of <1%, the following adverse events were reported:
- Tachycardia.
- Hypotension
- General discomfort.
- Palpitations
- Arrhythmia.
- Vomiting
- Anorexia.
- Diarrhea.
- Gastritis.
- However.
- Flatulence.
- Abdominal pain.
- Abnormal liver function
Very rarely:
- Anaphylaxis.
- Facial edema
- Edema on the tongue.
- Acne.
- Vertigo.
- Ataxia.
- Temblor.
- Hypertonia
- Seizures
- Disorientation.
- Anxiety.
- To feel down.
- Insomnia.
- Abnormal thoughts and dreams
- Excitement.
- Diplopía.
- Ageusia.
- Tinnitus.
- Urinary frequency or retention.
- Perspiration.
- Hepatitis and cholestasis.
- Muscle spasms.
- Itching.
- Urticaria.
- Disartria.
Dosage and administration
Administer 1 tablet 3 times / day at regular intervals, according to the intensity of the pain. Consume the tablets with a lot of liquid and whole (they should not be chewed). Continuous administration for more than 2 to 3 weeks is not recommended.
Maximum daily dose: 6 tablets.
Storage conditions
- Keep in a dry place at a temperature below 30 ° C.
