Tramadol

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Tramadol has been in clinical use in Germany since the late 1970s and has proven effective in both experimental and clinical pain without causing serious cardiovascular or respiratory side effects. Moreover, the negligible abuse potential of tramadol has meant that it has never been a restricted drug, and it therefore very quickly became the most popular analgesic of its class in Germany. Although tramadol has been used in myocardial emergencies, in trauma and obstetric pain, or to supplement balanced anaesthesia, most studies have investigated postoperative patients. The focus of this article is to review clinical experience with tramadol in the treatment of acute postoperative pain. Tramadol, a synthetic opioid of the aminocyclohexanol group, is a centrally acting analgesic with weak opioid agonist properties, and effects on noradrenergic and serotonergic neurotransmission. In addition, these opioid and nonopioid modes of action appear to act synergistically. Tramadol has been shown to provide effective analgesia after both intramuscular and intravenous administration for the treatment of postoperative pain. The drug is available in formulations suitable for oral, rectal and parenteral administration. Clinically effective analgesic doses of tramadol were comparable to those of pethidine (meperidine) and about 10 times higher than those of morphine. While it is not recommended as a supplement to general anaesthesia because of its insufficient sedative activity, tramadol has been successful in the treatment of postoperative pain. A randomised double-blind study reported acceptable analgesia with postoperative intravenous tramadol 50mg, repeated once if required after 30 minutes. It produced an effect similar to that of morphine 5mg or the alpha 2 agonist, clonidine 150 micrograms. In another study, it was shown that the 50mg dose of tramadol fulfilled the requirements of an analgesic for the treatment of moderate postoperative pain, whereas for severe pain a higher dose was recommended. Tramadol is generally well tolerated, the most common adverse events being nausea and vomiting. In contrast to agents such as morphine and pethidine, clinically relevant respiratory depression is rarely observed during tramadol administration at equipotent doses and consequently it can be recommended for first-line management of postoperative pain instead of morphine. It is also associated with a low incidence of cardiac depression and significantly less dizziness and drowsiness than morphine. Finally, the dependence and abuse potential with tramadol is negligible. Comparative studies have generally shown that tramadol is more effective than NSAIDs for controlling post operative pain. Use of a combination of tramadol and NSAIDs allows the tramadol dose to be reduced and results in a lower incidence of adverse effects. Patient controlled analgesia (PCA) with tramadol has been frequently used and is well accepted by patients. Wide individual variations exist with regard to analgesic requirements and, nowadays, it is generally accepted that adequate pain management implies systematic individualisation of the therapy, i.e. titration of the analgesic effect to individual needs. Demand and loading doses play a decisive role in the success of PCA. Analgesic failures requiring rescue medication are rare, but it should be stressed that these can always occur with weak opioids. In conclusion, tramadol can be recommended as a basic analgesic for the treatment of moderate to severe pain. In the event of analgesic failure with tramadol, there is no reason not to switch to more potent opioids. Although no studies are available regarding its use in the management of postoperative pain after day case surgery, tramadol is frequently administered with good results in such patients. The most important side effects of tramadol are nausea and emesis, which can often be prevented by slow injection and administration of a prophylactic antiemetic such as metoclopramide.

Tramadol is a synthetic analogue of codeine. It is a central analgesic with a low affinity for opioid receptors. Its selectivity for mu receptors has recently been demonstrated, and the M1 metabolite of tramadol, produced by liver O-demethylation, shows a higher affinity for opioid receptors than the parent drug. The rate of production of this M1 derivative (O-demethyl tramadol), is influenced by a polymorphic isoenzyme of the debrisoquine-type, cytochrome P450 2D6 (CYP2D6). Nevertheless, this affinity for mu receptors of the CNS remains low, being 6000 times lower than that of morphine. Moreover, and in contrast to other opioids, the analgesic action of tramadol is only partially inhibited by the opioid antagonist naloxone, which suggests the existence of another mechanism of action. This was demonstrated by the discovery of a monoaminergic activity that inhibits noradrenaline (norepinephrine) and serotonin (5-hydroxytryptamine; 5-HT) reuptake, making a significant contribution to the analgesic action by blocking nociceptive impulses at the spinal level. (+/-)-Tramadol is a racemic mixture of 2 enantiomers, each one displaying differing affinities for various receptors. (+/-)-Tramadol is a selective agonist of mu receptors and preferentially inhibits serotonin reuptake, whereas (-)-tramadol mainly inhibits noradrenaline reuptake. The action of these 2 enantiomers is both complementary and synergistic and results in the analgesic effect of (+/-)-tramadol. After oral administration, tramadol demonstrates 68% bioavailability, with peak serum concentrations reached within 2 hours. The elimination kinetics can be described as 2-compartmental, with a half-life of 5.1 hours for tramadol and 9 hours for the M1 derivative after a single oral dose of 100mg. This explains the approximately 2-fold accumulation of the parent drug and its M1 derivative that is observed during multiple dose treatment with tramadol. The recommended daily dose of tramadol is between 50 and 100mg every 4 to 6 hours, with a maximum dose of 400 mg/day; the duration of the analgesic effect after a single oral dose of tramadol 100mg is about 6 hours. Adverse effects, and nausea in particular, are dose-dependent and therefore considerably more likely to appear if the loading dose is high. The reduction of this dose during the first days of treatment is an important factor in improving tolerability. Other adverse effects are generally similar to those of opioids, although they are usually less severe, and can include respiratory depression, dysphoria and constipation. Tramadol can be administered concomitantly with other analgesics, particularly those with peripheral action, while drugs that depress CNS function may enhance the sedative effect of tramadol. Tramadol should not be administered to patients receiving monoamine oxidase inhibitors, and administration with tricyclic antidepressant drugs should also be avoided. Tramadol has pharmacodynamic and pharmacokinetic properties that are highly unlikely to lead to dependence. This was confirmed by various controlled studies and postmarketing surveillance studies, which reported an extremely small number of patients developing tolerance or instances of tramadol abuse. Tramadol is a central acting analgesic which has been shown to be effective and well tolerated, and likely to be of value for treating several pain conditions (step II of the World Health Organization ladder) where treatment with strong opioids is not required.

In a post-marketing-surveillance study the use of a sustained-release tramadol preparation (Tramal long 100, 150, 200 mg) was investigated in 3153 patients. The intention was to comply with the legal obligation to carry out product surveillance and to collect data on prescribing behaviour. We focused our attention on drug safety and efficacy. Tramal long was used mainly for severe and very severe pain. The most frequently reported causes of pain were diseases of the locomotor system (49.9%), tumours (24.3%), traumas and fractures (10.1%), and neurogenic (9.3%). The mean daily dose was 235.7 mg, usually divided into two doses. The analgesic effect was described as very good or good by 82.5% of the patients. Adverse events occurred in 6.5% of the patients, mostly in the form of typical opioid side-effects such as nausea (3.4%), dizziness (1.5%) and vomiting (1.1%). Severe or unknown side-effects were not reported.
 
The present study was conducted to characterise the centrally active analgesic drug tramadol hydrochloride [(1RS,2RS)-2-[(dimethyl-amino)-methyl]-1-(3-methoxyphenyl)-cyclohexanol hydrochloride] and its metabolites M1, M2, M3, M4 and M5 at the cloned human mu-opioid receptor. Membranes from stably transfected Chinese hamster ovary (CHO) cells were used to determine the four parameters of the ligand-receptor interaction: the affinity of (+/-)-tramadol and its metabolites was determined by competitive inhibition of [3H]naloxone binding under high and low salt conditions. The agonist-induced stimulation of [35S]GTPgammaS binding permits the measurement of potency (EC50), efficacy (Emax = maximal stimulation) and relative intrinsic efficacy (effect as a function of receptor occupation). The metabolite (+)-M1 showed the highest affinity (Ki=3.4 nM) to the human mu-opioid receptor, followed by (+/-)-M5 (Ki=100 nM), (-)-M1 (Ki=240 nM) and (+/-)-tramadol (Ki=2.4 microM). The [35S]GTPgammaS binding assay revealed an agonistic activity for the metabolites (+)-M1, (-)-M1 and (+/-)-M5 with the following rank order of intrinsic efficacy: (+)-M1>(+/-)-M5>(-)-M1. The metabolites (+/-)-M2, (+/-)-M3 and (+/-)-M4 displayed only weak affinity (Ki> 10 microM) and had no stimulatory effect on GTPgammaS binding. These data indicate that the metabolite (+)-M1 is responsible for the mu-opioid-derived analgesic effect.

The pharmacology, pharmacokinetics, efficacy, adverse effects, and dosage and administration of tramadol are reviewed. Tramadol is a synthetic analogue of codeine that binds to mu opiate receptors and inhibits norepinephrine and serotonin reuptake. It is rapidly and extensively absorbed after oral doses and is metabolized in the liver. Analgesia begins within one hour and starts to peak in two hours. In patients with moderate postoperative pain, i.v. or i.m. tramadol is roughly equal in efficacy to meperidine or morphine; for severe acute pain, tramadol is less effective than morphine. Oral tramadol can also be effective after certain types of surgery. Tramadol and meperidine are equally effective in postoperative patient-controlled analgesia. In epidural administration for pain after abdominal surgery, tramadol is more effective than bupivacaine but less effective than morphine. In patients with ureteral calculi, both dipyrone and butylscopolamine are more effective than tramadol. For labor pain, i.m. tramadol works as well as meperidine and is less likely to cause neonatal respiratory depression. Oral tramadol is as effective as codeine for acute dental pain. In several types of severe or refractory cancer pain, tramadol is effective, but less so than morphine; for other types of chronic pain, such as low-back pain, oral tramadol works as well as acetaminophen-codeine. Common adverse effects of tramadol include dizziness, nausea, dry mouth, and sedation. The abuse potential seems low. The recommended oral dosage is 50-100 mg every four to six hours. Tramadol is an effective, if expensive, alternative to other analgesics in some clinical situations.

Tramadol is usually marketed as the hydrochloride salt (tramadol hydrochloride); the tartrate is seen on rare occasions, and rarely (in the US at least) Tramadol is available for both injection (intravenous and/or intramuscular) and oral administration. It is also available in conjunction with acetaminophen (APAP) as Ultracet, a non-generic form of a smaller dose of 37.5 mg Tramadol and 325 mg of APAP. The solutions suitable for injection are used in Patient-Controlled Analgesia pumps under some circumstances, either as the sole agent or along with another agent such as morphine.

Tramadol comes in many forms, including:

• capsules (regular and extended release)
• tablets (regular, extended release, chewable, low-residue and/or uncoated tablets that can be taken by the sublingual and buccal routes)
• suppositories
• effervescent tablets and powders
• ampoules of sterile solution for SC, IM, and IV injection
• preservative-free solutions for injection by the various spinal routes (epidural, intrathecal, caudal, and others)
• powders for compounding
• liquids both with and without alcohol for oral and sub-lingual administration, available in regular phials and bottles, dropper bottles, bottles with a pump similar to those used with liquid soap and phials with droppers built into the cap
• tablets and capsules containing (acetaminophen/APAP), aspirin and other agents.

Tramadol has been experimentally used in the form of an ingredient in multi-agent topical gels, creams, and solutions for nerve pain, rectal foam, concentrated retention enema, and a skin plaster (transdermal patch) quite similar to those used with lidocaine.

Tramadol has a characteristic taste which is mildly bitter but much less so than morphine and codeine. Oral and sublingual drops and liquid preparations come with and without added flavoring. Its relative effectiveness via transmucosal routes (sublingual, buccal, rectal) is around that of codeine, and, like codeine, it is also metabolized in the liver to stronger metabolites (see below).

The maximum dosage for tramadol in any form is 400 mg/day. Certain manufacturers or formulations have lower maximum doses. For example, Ultracet (37.5 mg/325 mg tramadol/APAP tablets) is capped at 8 per day (300 mg/day). Other popular formulations such as Ultram ER are available in 100, 200, and 300 mg/day doses. Patients with impaired liver function or using SSRIs should consult with their doctor regarding adjusted dosing.

Tramadol is used to treat post-operative, injury-related, and chronic (e.g., cancer-related) pain in dogs and cats as well as rabbits, coatis, many small mammals including rats and flying squirrels, guinea pigs, ferrets, and raccoons. Tramadol comes in ampoules in addition to the tablets, capsules, powder for reconstitution, and oral syrups and liquids; the fact that its characteristic taste is not very bitter and can be masked in food and diluted in water makes for a number of means of administration. No data that would lead to a definitive determination of the efficacy and safety of tramadol in reptiles or amphibians is available at this time, and, following the pattern of all other drugs, it appears that tramadol can be used to relieve pain in marsupials such as North American opossums, Short-Tailed Opossums, sugar gliders, wallabies, and kangaroos among others.

Tramadol for animals is one of the most reliable and useful active principles available to veterinarians for treating animals in pain. It has a dual mode of action: mu agonism and mono-amine reuptake inhibition, which produces mild anti-anxiety results. Tramadol may be utilized for relieving pain in cats and dogs. This is an advantage because the use of some non-steroidal anti-inflammatory substances in these animals may be dangerous.

When animals are administered tramadol, adverse reactions can occur. The most common are constipation, upset stomach, decreased heart rate. In case of overdose, mental alteration, pinpoint pupils and seizures may appear. In such case, veterinarians should evaluate the correct treatment for these events. Some contraindications have been noted in treated animals taking certain other drugs. Tramadol should not be co-administered with Deprenyl or any other psychoactive ingredient such as serotonin reuptake inhibitors, tricyclic antidepressants, or mono-amine oxidase inhibitors. In animals, tramadol is removed from the body via liver and kidney excretion. Animals suffering from diseases in these systems should be monitored by a veterinarian, as it may be necessary to adjust the dose.

Dosage and administration of tramadol for animals: in dogs a starting dosage of 1–2 mg/kg twice a day will be useful for pain management. Cats are administered 0.5-1 mg/kg twice a day.