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 Chemical Pharmacology :. tramadols is an analgesic that has both novel opioid agonist and inhibition of monoamine reuptake leading to its analgesic efficacy. Natural action of opioids is due to the parent compound and metabolite O-desmethyl more active. tramadols acts in the system of monoamine reuptake resorption bottling nerve endings both norepinephrine and 5-hydroxytryptamine Apart from analgesia, tramadol may produce a variety of symptoms including dizziness, drowsiness, nausea, constipation and similar to other opioids. tramadols high curses Venus, often in combination monoamine oxidase (MAO) inhibitors or selective serotonin reuptake King (SSRIs), have been matched with serotonin syndrome is unrest, hyperthermia, muscle stiffness and pain.

Tramadols pain medication is one of the most popular on the market painkillers. You must have come across this name many times in your life. If you have not used yourself, then you must have known the family or friends who have used it for years. Or at some point, your doctor may have suggested this medication for the treatment of any type of physical pain in your body. Many people know that tramadols is a good medicine for pain, but many do not know the medical aspects of pain medication. Read on to find out what these facts.


Tramadols is a pain medication that can be used to treat moderate to moderately severe pain. In the category of opioid agonists. Some people do not understand this medicine for an NSAID, but it is not. It facilitates the patient's pain by changing the way the body senses pain. Tramadols pain medication can be found in two formulations for immediate release and sustained release. One tablet of 50 mg is indicated for the immediate relief of pain, while greater than 100, 200 or 300 mg tablets are recommended for power prolonged pain relief.


One thing to keep in mind is that the pain medication tramadol tablets should be taken as a whole tablet. You should never try to divide it into pieces to make it easier to take. It should not be chewed or crushed or. There are some instructions for taking this drug, which will be provided by your doctor. Remember to follow anyone if you do not want to have side effects from pain medication. Another thing to consider is related to the dose. It is recommended not to increase the dose of tramadol pain medication without first consulting your doctor. The increased dosage requirements, could be addictive and dangerous for the body.


tramadol pain medication should be avoided by pregnant women and nursing mothers also. Not sure is these situations. Additionally, you may have certain drug interactions when combined with certain drugs. So if you are taking any other medicines, do not do well checked by a doctor. Your doctor can advise you whether it would be safe to take tramadol with other medicines you are taking. tramadol pain medication is a very popular pain relief medication, but you should know the medical facts to make the most of the medicine!

Tramadol is well absorbed orally. It can be done in less than 50-100 mg lozenges as needed for pain relief every 4 to 6 hours, not more than 400 mg per day.

Pharmacological Properties

Tramadol is an opioid analgesic that acts on the central nervous system. It is a nonselective pure agonist opioid receptors μ, d,? with a higher affinity for the μ receptor. In addition, in vitro inhibits the reuptake of norepinephrine and serotonin. These mechanisms contribute synergistically to the analgesic effect of tramadol. Unlike morphine, analgesic doses of tramadol not produce respiratory depressant effect. Similarly, gastrointestinal motility is not modified. Cardiovascular effects are usually mild. The precise mechanism of the analgesic properties of paracetamol is unknown and may involve central and peripheral effects.


Tramadol is administered in racemic form and the forms [-] and [+] of tramadol and its metabolite M1 are detected in the blood. [- Tramadol / (-) - (+) tramadol] After a single oral administration of a tablet ZALDIAR, maximum plasma concentrations of 64.3 / 55.5 ng / ml are reached and 4.2 ug / ml (paracetamol) after 1.8 h [(+) - tramadol / (-) - tramadol] and 0.9 h (paracetamol) respectively. Half-lives t1 / 2 are 5.1 / 4.7 h [(+) - tramadol / (-) - tramadol] and 2.5 h (paracetamol). We did not observe significant changes in the kinetic parameters of either active compared with the parameters of the active substances when these are used alone.

Racemic tramadol is absorbed rapidly and almost completely after oral administration .. The oral absorption of paracetamol is rapid and almost complete and occurs primarily in the small intestine. Peak plasma concentrations of paracetamol are reached in one hour and are not modified by the concomitant administration of tramadol. Oral administration of food ZALDIAR only changes the rate and speed of absorption slightly; consequently, it may be administered independently ZALDIAR meals.

Tramadol is extensively metabolized after oral administration. About 30% of the dose is excreted unchanged in the urine, while 60% is excreted as metabolites.

Tramadol and its metabolites are primarily eliminated by the kidneys. The half-life of paracetamol is approximately 2 to 3 hours in adults. It is shorter in children and slightly longer in the newborn and in cirrhotic patients. Paracetamol is mainly eliminated by proportional to the dose of glucurono derivatives and sulfoconjugates training. Less than 9% of paracetamol is excreted unchanged in the urine. In renal insufficiency, the half-life of both compounds is prolonged.


INDICATIONS: Symptomatic treatment of moderate to severe pain that does not respond to the use of peripherally acting analgesics used alone.



• Known hypersensitivity to tramadol or paracetamol.

• Acute intoxication with alcohol, hypnotics, centrally acting analgesics, opioids or psychotropic drugs.

• prior or concomitant treatment in the last 15 days for inhibitors and non-selective MAO in the last 24 hours for selectively inhibit MAO A and MAO B.

• severe respiratory insufficiency,

• hepatocellular insufficiency.

• epilepsy not controlled by treatment

• Concomitant use of nalbuphine, buprenorphine, pentazocine

• Breast-feeding if long term treatment


tramadol is not a suitable substitution treatment for opioid-dependent patients. Although tramadol is an opioid agonist, it can not suppress withdrawal symptoms by suppressing morphine treatment.

• convulsions have been observed mainly in predisposed or treated with drugs that can lower the seizure threshold patients. Epileptic patients controlled or predisposed to seizures should only be treated with tramadol when absolutely necessary.

• In adults should not exceed the limit dose of 4 grams per day.

• It is not recommended to drink alcohol during treatment.

• use in children under 16 is not recommended, use with caution in elderly, Use with caution in patients with a history of convulsiones.Tratamiento should be brief or intermittent, prolonged use can cause addiction.

Special Precautions


Preclinical data paracetamol have revealed no specific hazard for humans.

ZALDIAR should be used with caution in patients dependent or hypersensitivity to opioids or in patients with cranial trauma, in shock, in a state of altered consciousness for unknown reasons, with problems affecting the respiratory center or the respiratory function, or with high intracranial pressure.

tramadols has a low dependence potential.

Carcinogenicity / mutagenicity results of carcinogenicity tests do not suggest that tramadol pose a potential risk to humans. Results of standard mutagenicity tests did not reveal a potential genotoxic risk associated with the use of tramadol in man.

Pregnancy / Fertility:

• Data regarding paracetamol: The results of epidemiological studies in humans have shown that paracetamol has no teratogenic or fetotoxic effects.

• Data regarding tramadol: Animal studies have shown no evidence that there is a teratogenic or on fertility. In humans, there are currently insufficient data to assess the teratogenic potential of tramadols effect when administered during the first trimester of pregnancy. Therefore, it is not advisable to use tramadol during the first trimester of pregnancy.

From the 2nd trimester, you can consider using carefully (preferably short).

Lactation: Approximately 0.1% of the maternal dose of tramadols is excreted in breast milk:

Pediatrics: The safety and efficacy of tramadol has not been established in children under 15 years of age. Therefore, treatment is not recommended in this population.

Geriatrics: In patients over 75 years of age is recommended that the interval between dose increases to 9 hours

Renal impairment: Tramadol use in patients with severe renal impairment (creatinine clearance <10 mL / min) is not recommended. In cases of moderate renal insufficiency (creatinine clearance 10 to 30 mL / min) the dosage should be increased at intervals of 12 hours.

Effects on ability to drive and use machines

The potential effect on care can make driving and using machines is dangerous, particularly after the concomitant intake of alcohol or antidepressants of the central nervous system.



The adverse reactions most commonly reported during clinical trials with the combination of paracetamol / tramadol include nausea, dizziness and somnolence, observed in 10% of patients.

Cardiovascular system disorders:

• Uncommon (0.1% -1%): hypertension, palpitations, tachycardia, arrhythmia.

Disorders of the central and peripheral nervous system:

• Very common (> 10%): Dizziness, drowsiness.

• Regular (1% -10%): Headache, tremors.

• Uncommon (0.1% -1%): involuntary muscle contractions, paresthesia, tinnitus.

• Rare (<0.1%): ataxia, seizures.

Respiratory system disorders:

• Uncommon (0.1% -1%): dyspnea.

Gastrointestinal disorders:

• Very common (> 10%): nausea.

• Regular (1% -10%): vomiting, constipation, dry mouth, diarrhea, abdominal pain, dyspepsia, flatulence.

• Uncommon (0.1% -1%): Dysphagia mane.

Disorders of the liver and biliary system:

• Uncommon (0.1% -1%): elevated liver transaminases.

Disorders of the skin and appendages:

• Regular 1% -10%): sweating, pruritus.

• Uncommon (0.1% -1%): dermal reactions (eg rash, urticaria).



Concomitant use with:

• MAO inhibitors: In case of recent treatment with non-selective inhibitors of monoamine oxidase, should be delayed 15 days starting treatment with tramadol . In case of recent treatment with MAO inhibitors or selective B should be delayed 24 hours of treatment with tramadol.

• opioid agonists-antagonists (buprenorphine, nalbuphine, pentazocine): Due to the decline of the analgesic effect by competitive blocking effect at the receptors.

Concomitant use is not recommended:

Alcohol. Alcohol increases the sedative effect of opioid analgesics. Decreased alertness can make driving dangerous and use of machines. Avoid drinking alcoholic beverages and medications containing alcohol.

Carbamazepine: Risk of decreased plasma concentrations of tramadol.

Precautions to be taken into account in case of concomitant use:

Other opioid derivatives (including antitussive drugs and substitutive treatments), benzodiazepines and barbiturates. Increased risk of respiratory depression, which can be fatal in overdose.

Other central nervous system depressants, other opioid derivatives (including antitussive drugs and substitutive treatments), barbiturates, benzodiazepines, other anxiolytics, hypnotics, sedative antidepressants, sedative antihistamines, neuroleptics, centrally-acting antihypertensive drugs, thalidomide and baclofen.

These drugs can cause increased central depression. The effect on care can make dangerous driving and using machines.

Drugs that reduce the seizure threshold, such as bupropion, antidepressants reuptake inhibitors of serotonin, tricyclic antidepressants and neuroleptics. Concomitant use of tramadol with these drugs may increase the risk of seizures.



Symptoms of overdose due to tramadol: miosis, vomiting, cardiovascular collapse, somnolence including coma, convulsions and respiratory depression, which could lead to respiratory arrest.

Overdose symptoms due to paracetamol: An overdose is a particular concern in elderly patients, especially in young children, which can be fatal.

Emergency Treatment

Move immediately to a specialized unit, Keep respiratory and circulatory functions, before starting treatment, take a blood sample as soon as possible to measure the plasma concentration of paracetamol and tramadol and in order to perform tests hepáticas.Realizar tests liver at the start (of overdose) and repeated every 24 hours. Usually an increase in liver enzymes (AST, ALT), which normalizes after one or two weeks is observed.

Empty stomach causing vomiting (when the patient is conscious) by irritation or washing gástrico.El antidote in case of respiratory depression due to overdose of tramadol is naloxone.

Regardless of the amount of paracetamol ingested communicated should administer the antidote to acetaminophen, acetylcysteine, orally or intravenously, as soon as possible. If possible, in the 10 hours following the overdose.



One or two tablets every 4 to 6 hours and a maximum of 8 tablets per day. The dose should preferably be taken at intervals of 6 hours with a minimum interval of four hours. tramadol should not be given longer than is strictly necessary. If a long-term treatment of pain precise tramadol only be possible by prescription and close medical supervision. The tablets should be swallowed whole with a sufficient amount of liquid. They must not break or chew.



Store in cool, dry place

Keep out of the reach and sight of children

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