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Tramadol (Ultram, Tramal ) is a centrally-acting analgesic, used for treating moderate to severe pain.
Tramadol possesses agonist actions at the μ-opioid receptor and affects reuptake at the noradrenergic and serotonergic systems. Tramadol is a compound with mild and delayed μ-agonist activity.
Tramadol is a synthetic stripped-down piperidine-analog of the phenantherane alkaloid Codeine and, as such, is an Opioid and also a pro-drug (Codeine gets metabolized to Morphine, Tramadol gets converted to M-1 aka O-desdol). Opioids are chemical compounds which act upon one or more of the human opiate receptors (the euphoria, addictive nature and respiratory depression are mainly caused by the Mu(μ) 1 and 2 receptor. The opioid agonistic effect of Tramadol and its major metabolite(s) are almost exclusively mediated by the substance’s action at the μ-receptor. This characteristic distinguishes Tramadol from many other substances (including Morphine) of the opioid drug class, which generally do not possess Tramadol’s degree of subtype selectivity.
Tramadol is used similarly to Codeine, to treat moderate to moderately severe pain and most types of neuralgia, including trigeminal neuralgia. Another popular use of Tramadol is as a remedy for opiate/opioid withdrawal, especially since it being uncontrolled has led to many addicts weaning down or altogether stopping their addiction to opiates. Tramadol is like Levorphanol (albeit with much lower μ-agonism), somewhat, pharmacologically, as both opioids are also NMDA-antagonists which also have SNRI activity (other such opioids to do the same are Kratom, Dextropropoxyphene (Darvon) & M1-like molecule Tapentadol (Nucynta, a new synthetic atypical opioid m
ade to mimick the agonistic properties of Tramadol’s metabolite, M1(O-Desmethyltramadol). It has been suggested that tramadol could be effective for alleviating symptoms of depression, anxiety, and phobias because of its action on the noradrenergic and serotonergic systems, (also) such as its “atypical” opioid activity – (function). However, health professionals have not endorsed its use for these disorders; It may be used as a unique treatment (only when other treatments failed), and must be used under control of a psychiatrist.
ULTRAM® (tramadol hydrochloride) tablets is a centrally acting analgesic. The chemical name for tramadol hydrochloride is (±)cis-2-[(dimethylamino)methyl]-1-(3methoxyphenyl) cyclohexanol hydrochloride. Its structural formula is:
tramadol The molecular weight of tramadol hydrochloride is 299.8. Tramadol hydrochloride is a white, bitter, crystalline and odorless powder. It is readily soluble in water and ethanol and has a pKa of 9.41. The n-octanol/water log partition coefficient (logP) is 1.35 at pH 7. ULTRAM® tablets contain 50 mg of tramadol hydrochloride and are white in color. Inactive ingredients in the tablet are pregelatinized corn starch, modified starch (corn), hypromellose, lactose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, sodium starch glycolate, titanium dioxide and carnauba wax.
Tramadol is generic name of ultram. Ultracet Tablets combines tramadol 37.5 mg and acetaminophen 325 mg.
TRamadol APAP Combination medicines containing opioid analgesics (nar-KOT-ik an-al-JEE-zicks ) such as tramadol (TRA-ma-dole) and acetaminophen (a-seat-a-MIN-oh-fen ) are used to relieve pain. An opioid analgesic and acetaminophen used together may provide better pain relief than either medicine used alone. In some cases, you may get relief with lower doses of each medicine.
Opioid analgesics act in the central nervous system (CNS) to relieve pain. Many of their side effects are also caused by actions in the CNS. When opioids are used for a long time, your body may get used to them so that larger amounts are needed to relieve pain. This is called tolerance to the medicine. Also, when opioids are used for a long time or in large doses, they may become habit-forming (causing mental or physical dependence). Physical dependence may lead to withdrawal symptoms when you stop taking the medicine.
Acetaminophen does not become habit-forming when taken for a long time but it may cause other unwanted effects, when taken in large doses including liver damage, if too much is taken.
Acetaminophen (4´-hydroxyacetanilide), is a non-opiate, non-salicylate analgesic and antipyretic. It has the following structural formula:
Acetaminophen Side Effects of Tramadol
Tramadol/Acetaminophen
All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome when using Tramadol/Acetaminophen:
Constipation; diarrhea; dizziness; drowsiness; increased sweating; loss of appetite; nausea.
Seek medical attention right away if any of these SEVERE side effects occur when using Tramadol/Acetaminophen:
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); severe seizures (convulsions).
Tramadol
All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome when using Tramadol:
Constipation; diarrhea; dizziness; drowsiness; dry mouth; headache; nausea; trouble sleeping; vomiting; weakness.
Seek medical attention right away if any of these SEVERE side effects occur when using Tramadol:
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); agitation; chest pain; difficult or painful urination; disorientation; fainting; hallucinations; irregular heartbeat; loss of coordination; mood or mental changes (eg, depression); red, blistered, swollen, or peeling skin; seizures; severe dizziness or lightheadedness.
Pharmacodynamics
ULTRAM® contains tramadol, a centrally acting synthetic opioid analgesic. Although its mode of action is not completely understood, from animal tests, at least two complementary mechanisms appear applicable: binding of parent and M1 metabolite to μ-opioid receptors and weak inhibition of reuptake of norepinephrine and serotonin.
Opioid activity is due to both low affinity binding of the parent compound and higher affinity binding of the O-demethylated metabolite M1 to μ-opioid receptors. In animal models, M1 is up to 6 times more potent than tramadol in producing analgesia and 200 times more potent in μ-opioid binding. Tramadol-induced analgesia is only partially antagonized by the opiate antagonist naloxone in several animal tests. The relative contribution of both tramadol and M1 to human analgesia is dependent upon the plasma concentrations of each compound (see CLINICAL PHARMACOLOGY, Pharmacokinetics).
Tramadol has been shown to inhibit reuptake of norepinephrine and serotonin in vitro, as have some other opioid analgesics. These mechanisms may contribute independently to the overall analgesic profile of ULTRAM®. Analgesia in humans begins approximately within one hour after administration and reaches a peak in approximately two to three hours.
Apart from analgesia, ULTRAM® administration may produce a constellation of symptoms (including dizziness, somnolence, nausea, constipation, sweating and pruritus) similar to that of other opioids. In contrast to morphine, tramadol has not been shown to cause histamine release. At therapeutic doses, ULTRAM® has no effect on heart rate, left-ventricular function or cardiac index. Orthostatic hypotension has been observed.
Pharmacokinetics
The analgesic activity of ULTRAM® is due to both parent drug and the M1 metabolite (see CLINICAL PHARMACOLOGY, Pharmacodynamics). Tramadol is administered as a racemate and both the [-] and [+] forms of both tramadol and M1 are detected in the circulation. Linear pharmacokinetics have been observed following multiple doses of 50 and 100 mg to steady-state.
