- Tramadol Withdrawal: how to take, composition and reviews
- How Much Tramadol Can I Take: the benefits and harm, use in sports and bodybuilding
- Tramadol Withdrawal for twine beginners, exercises at home
Tramadol – Wikipedia
Invented in 1962 by Dr. Kurt Flick, an employee of the German pharmaceutical company GRÜNENTHAL GmbH (Grünental). Soon tramadol became the most prescribed monoalangetic of central action in the world. During the time that has passed since the creation of the drug, he was discharged to more than 70 million tramadol withdrawal: patients around the world. .
Pharmacological action [edit | edit code]
A synthetic analgesic that has a central action and action on the spinal cord (promotes the opening of K + and Ca2 + ion channels, causes hyperpolarization of the membranes and inhibits the conduction of pain impulses), enhances the effect of sedative drugs. Activates opiate receptors (μ-, Δ-, κ-) on the pre- and postsynaptic membranes of the afferent fibers of the nociceptive system and in the gastrointestinal tract. Slows down the destruction of catecholamines, stabilizes their concentration in the central nervous system.
The affinity of tramadol to opioid receptors is 10 times weaker than that of codeine, and 6000 times weaker than that of morphine, while the severity of analgesic action is only 5-10 times weaker than morphine.
Tramadol is a racemic mixture of 2 enantiomers – dextrorotatory (+) and levogyrate (-), each of which exhibits a different receptor affinity. (+) Tramadol is a selective agonist of mu-opiate receptors, and also selectively inhibits the reverse neuronal seizure of serotonin. (-) Tramadol inhibits the reverse neuronal capture of norepinephrine. Mono-O-desmethyltramadol (M1 metabolite) also selectively stimulates mu-opiate receptors.
In therapeutic doses, it does not significantly affect tramadol withdrawal: hemodynamics and respiration, does not alter the pressure in the pulmonary artery, and slightly slows down intestinal motility, without causing constipation. It has some antitussive and sedative effects. Inhibits the respiratory center, stimulates the starting area of the vomiting center, the nucleus of the oculomotor nerve.
With prolonged use may develop tolerance.
Tramadol Withdrawal: how to take, composition and reviews
Pharmacokinetics [edit | edit code]
Absorption – 90%; bioavailability – 68% when taken orally (increased with repeated use), 70% – with rectal, with intramuscular – 100%. TCmax after ingestion of tablets – 2 hours, when taking drops – 1 hour, with intramuscular administration – 45 minutes, M1 metabolite – 3 hours. Penetrates through the blood-brain barrier and the placenta, 0.1% is excreted in breast milk. The volume of distribution is 203 l with intravenous administration and 306 l with oral administration. Communication with plasma proteins – 20%.
In the liver, it is metabolized by N- and O-demethylation with subsequent conjugation with glucuronic acid. 11 metabolites were detected, of which mono-O-desmethyltramadol (M1) has pharmacological activity. CYP2D6 isoenzyme is involved in the metabolism of the drug. T1 / 2 in the second phase – 6 h (tramadol), 7.9 h (mono-O-dezmetiltramadol); in patients older than 75 years – 7.4 h (tramadol); in liver cirrhosis – 13.3 ± 4.9 h (tramadol), 18.5 ± 9.4 h (mono-O-dezmetiltramadol), in severe cases – 22.3 h and 36 h, respectively. T1 / 2 in chronic renal failure (CC less than 5 ml / min) – 11 ± 3.2 h (tramadol), 16.9 ± 3 h (mono-O-dezmetiltramadol), in severe cases – 19.5 h and 43.2 h, respectively.
Excreted by the kidneys (25-35% unchanged), the average cumulative rate of renal excretion – 94%. About 7% is excreted through hemodialysis.
Indications [edit | edit code]
Pain syndrome (strong and medium intensity, including inflammatory, traumatic, vascular origin, with cancer, neuralgia). Pain relief during painful diagnostic or therapeutic interventions. Tramadol has also been used to treat opiate withdrawal .
Contraindications [edit | edit code]
Hypersensitivity, alcohol poisoning, hypnotic drugs, narcotic analgesics and other psychoactive drugs, pregnancy, lactation period (in the case of long-term use), children’s age (up to 1 year – for parenteral administration; up to 14 years for oral administration), intake MAO inhibitors.
Opioid dependence, impaired consciousness of various origins, intracranial hypertension, traumatic brain injury, epileptic syndrome (cerebral genesis), bronchial asthma, conditions accompanied by worsening of breathing or marked deterioration of self-control.
Dosing regimen [edit | edit code]
Applied intravenously, intramuscularly, subcutaneously, by mouth, rectally. The total daily dose is 0.4 g. For children over the age of 1 year, by mouth, only drops or parenteral (intravenous, intramuscular, subcutaneous), in a dose of 1-2 mg / kg. The daily dose is 4-8 mg / kg (1 cap – 2.5 mg). The elderly and patients with renal insufficiency require an individual dosage (T1 / 2 lengthening is possible). When creatinine clearance is less than 30 ml / min and in patients with hepatic insufficiency, a 12-hour interval is necessary between taking regular doses of the drug.
How Much Tramadol Can I Take: the benefits and harm, use in sports and bodybuilding
Inside [edit | edit code]
For single use for adults and children over 14 years old – 50 mg. After 30-60 minutes, you can repeat the reception in the same dose, but not more than 8 doses per day. Retard tablets – 100-200 mg every 12 hours. Daily dose – 0.4 g (in exceptional cases, for example in cancer patients, a reduction in the interval to 6 hours and an increase in the daily dose is possible).
Rectally [edit | edit code]
Rectal – 0.1 g. Reception frequency – up to 4 times per day.
Intravenous, intramuscular, subcutaneous [edit | edit code]
Slowly, 0.05–0.1 g. If the effect is not sufficient, then 20–30 minutes after intravenous administration, the infusion can be continued at a rate of 12 mg / h or additionally administered tramadol withdrawal :.
Side Effects [edit | edit code]
The nervous system
Increased sweating, increased urination, dizziness, headache, weakness of tramadol withdrawal: fatigue, lethargy, paradoxical stimulation of the central nervous system (nervousness, agitation, anxiety, tremor, muscle cramps, euphoria, emotional lability, hallucinations), sleep, sleep, sleep, sleep, sleep, sleep, sleep, sleep, sleep, sleepiness consciousness, impaired motor coordination, convulsions of central genesis (with intravenous administration in high doses or with simultaneous prescription of antipsychotic drugs (neuroleptics)), depression I, amnesia, cognitive impairment, paresthesia, unsteady gait.
From the digestive system
Dry mouth, nausea, vomiting, flatulence, abdominal pain, constipation or diarrhea, difficulty swallowing.
Since the cardiovascular system
Manifestations of vasodilation – tachycardia, orthostatic hypotension, syncope, collapse.
Urticaria, pruritus, rash, bullous rash. A sharp decrease in blood pressure.
On the part of the urinary system
Difficulty urinating, dysuria, urinary retention.
From the senses
Visual impairment, taste.
On the part of the respiratory system
Violation of the menstrual cycle. With prolonged use – drug dependence. With a sharp cancellation – the syndrome of “cancel”.
Overdose [edit | edit code]
Mioz, vomiting, collapse, coma, convulsions, depression of the respiratory center, apnea.
Ensuring the airway, maintaining breathing and cardiovascular activity. Opiate-like effects can be stopped by naloxone, seizures by benzodiazepine.
Special instructions [edit | edit code]
Do not use ethanol at the same time. In the case of a single dose there is no need to interrupt breastfeeding. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.
Interaction [edit | edit code]
Pharmaceutically incompatible with solutions of diclofenac, indomethacin, phenylbutazone, diazepam, flunitrazepam, nitroglycerin. Enhances the action of drugs that inhibit the central nervous system, and ethanol. Inducers of microsomal oxidation (including carbamazepine, barbiturates) reduce the severity of the analgesic effect and the duration of action. Prolonged use of opioid analgesics or barbiturates stimulates the development of cross-tolerance. Anxiolytics increase the severity of the analgesic effect; the duration of anesthesia is increased when combined with barbiturates. Naloxone activates respiration, eliminating analgesia after the use of opioid analgesics. MAO inhibitors, furazolidone, procarbazine, antipsychotic drugs (neuroleptics) increase the risk of seizures (lowering the seizure threshold). Quinidine increases the plasma concentration of tramadol and reduces the metabolite M1 due to competitive inhibition of the isoenzyme
Legislative regulation [edit | edit code]
Tramadol Withdrawal for twine beginners, exercises at home
In some countries (in Ukraine  and in Belarus ) tramadol is included in the list of narcotic drugs.
In Russia, tramadol is included in the list of essential and essential medicines.
In March 2016, three criminal cases were initiated in Belarus against Russians detained at the Polish-Belarusian border with tablets containing tramadol . In this regard, the Belarusian Customs made a statement  that when transporting medicines for personal use, classified under the Belarusian legislation as narcotic, it is necessary to have supporting medical documents; otherwise, there is a risk of up to 10 years in prison.
Notes [edit | edit code]