Drug information:

Why is this medication prescribed?Return to top

Tramadol is used to relieve moderate to moderately severe pain. It may be used to treat pain caused by surgery and chronic conditions such as cancer or joint pain. Tramadol is in a class of medications called opiate (narcotic) analgesics. It works by decreasing the body's sense of pain.

How should this medicine be used?Return to top

Tramadol comes as a tablet to take by mouth. It may be taken with or without food. Your doctor may start you on a low dose of tramadol and gradually increase your dose not more often than every 3 days. Tramadol may be taken every 4-6 hours as needed. If you take too much tramadol, you may experience serious side effects.Ask your doctor about the maximum number of tablets that you may take for each dose or for a 24-hour period.Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take tramadol exactly as directed.

Tramadol can be habit-forming. Do not take a larger dose, take it more often, or take it for a longer period of time than prescribed by your doctor. Call your doctor if you find that you want to take extra medication or notice any other unusual changes in your behavior or mood.

Do not stop taking tramadol suddenly without talking to your doctor. If you suddenly stop taking tramadol, you may experience side effects. Your doctor will probably decrease your dose gradually.If you suddenly stop taking tramadol you may experience withdrawal symptoms such as nervousness; panic; sweating; difficulty falling asleep or staying asleep; runny nose, sneezing, or cough; numbness, pain, burning, or tingling in your hands or feet; hair standing on end; or rarely, hallucinations (seeing things or hearing voices that do not exist).

Other uses for this medicineReturn to top

This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

What special precautions should I follow?Return to top

Before taking tramadol,

• tell your doctor and pharmacist if you are allergic to tramadol or other narcotic pain medications such as meperidine (Demerol), morphine, codeine (or medications that contain codeine such as Tylenol with Codeine), hydrocodone (e.g., Vicodin), hydromorphone (e.g., Dilaudid), oxycodone (e.g., Percocet), propoxyphene (e.g., Darvon, Darvon N), any other medications, or corn.
• tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking. Be sure to mention any of the following: amiodarone (Cordarone, Pacerone); antihistamines; bupropion (Wellbutrin);celecoxib (Celebrex); cimetidine (Tagamet);cyclobenzaprine (Flexeril); digoxin (lanoxin); doxorubincin (Adriamycin);haloperidol (Haldol); imipenem and cilastatin (Primaxin); methadone (Dolophine, Methadose); monoamine oxidase (MAO) inhibitors, including isocarboxazid (Marplan), phenelzine (Nardil), selegiline (Eldepryl), and tranylcypromine (Parnate); medications for anxiety, mental illness, nausea, pain; medications for seizures, such as carbamazepine (Tegretol); metoclopramide (Reglan); nefazodone; promethazine (Phenergan); quinidine (Quinaglute; Quinidex); ranitidine (Zantac); ritonavir (Norvir, in Kaletra); sedatives; sleeping pills; selective serotonin reuptake inhibitors (SSRIs) such as citalopram (Celexa), fluoxetine (Prozac, Sarafem), fluvoxamine (Luvox), paroxetine (Paxil), and sertraline (Zoloft); ticlopidine (Ticlid); tranquilizers; tricylic antidepressants such as amitriptyline (Elavil), amoxapine (Asendin), clomipramine (Anafranil), desipramine (Norpramin), doxepin (Adapin, Sinequan), imipramine (Tofranil), nortriptyline (Aventyl, Pamelor), protriptyline (Vivactil), and trimipramine (Surmontil);venlafaxine (Effexor);warfarin (Coumadin). Many other medications may also interact with tramadol, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
• tell your doctor if you have or have ever had seizures, head injury, infection in your brain or nervous system, increased intracranial pressure (increased pressure within the skull), diabetes, breathing problems or lung disease, or kidney or liver disease. Also tell your doctor if you drink or have ever drunk large amounts of alcohol, use or have ever used street drugs, or have overused prescription medications.
• tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking tramadol, call your doctor.
• if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking tramadol.
• you should know that this drug may make you drowsy and may affect your coordination. Do not drive a car or operate machinery until you know how this drug affects you.
• remember that alcohol can add to the drowsiness caused by this drug. The manufacturer states that tramadol should not be taken with alcohol containing beverages.
• you should know that tramadol may cause dizziness, lightheadedness, and fainting when you get up from a lying position. To avoid this, get out of bed slowly, resting your feet on the floor for a few minutes before standing up.

What should I do if I forget a dose?Return to top

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

What side effects can this medication cause?Return to top

Tramadol may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

• dizziness
• weakness
• headache
• nervousness or anxiety
• agitation
• shaking hands that you cannot control
• increased muscle tightness
• changes in mood
• drowsiness
• blurred vision
• heartburn or indigestion
• upset stomach
• vomiting
• diarrhea
• constipation
• itching
• sweating
• flushing
• dry mouth

Some side effects can be serious. If you experience any of these symptoms, call your doctor immediately:

• hives
• rash
• sores on the inside of your mouth, nose, eyes, or throat
• flu-like symptoms
• itching
• difficulty swallowing or breathing
• swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
• fast heartbeat
• hoarseness
• difficulty swallowing or breathing
• changes in urination
• seeing things or hearing voices that do not exist (hallucinating)
• seizures

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online [at http://www.fda.gov/MedWatch/report.htm] or by phone [1-800-332-1088].

What storage conditions are needed for this medicine?Return to top

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.

In case of emergency/overdoseReturn to top

In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.

Symptoms of overdose may include:

• confusion
• vomiting
• decreased size of the pupil (the black circle in the center of the eye)
• difficulty breathing
• extreme drowsiness
• unconciousness
• coma
• seizure
• heart attack

What other information should I know?Return to top

Keep all appointments with your doctor.

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.

Brand namesReturn to top

Web Pills - TRAMADOL.

Some additional information about Tramadol

Tramadol

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Tramadol
Systematic (IUPAC) name
rac-(1R,2R)-2-(dimethylaminomethyl)-1- (3-methoxyphenyl)-cyclohexanol
Identifiers
CAS number	27203-92-5
ATC code	N02AX02
PubChem	33741
DrugBank	APRD00028
Chemical data
Formula	C16H25NO2
Mol. weight	263.4 g/mol
Pharmacokinetic data
Bioavailability	68-72% Increases with repeated dosing.
Protein binding	20%
Metabolism	Hepatic demethylated & glucuronidated
Half life	5-7 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C(AU) C(US)
Legal status	Prescription Only (S4)(AU) POM(UK)
Routes	oral, IV, IM

Tramadol (INN) (IPA: [ˈtræməˌdɒl]) is an atypical opioid which is a centrally acting analgesic, used for treating moderate to severe pain. It is a synthetic agent, unrelated to other opioids, and appears to have actions on the GABAergic, noradrenergic and serotonergic systems. Tramadol was developed by the German pharmaceutical company Grünenthal GmbH and marketed under the trade name Tramal. Grünenthal has also cross licensed the drug to many other pharmaceutical companies that market it under various names, some of which are listed below.

Tramadol is usually marketed as the hydrochloride salt (tramadol hydrochloride) and is available in both injectable (intravenous and/or intramuscular) and oral preparations (e.g. Zydol® in UK and Ultram® in US). It is also available in conjunction with paracetamol (acetaminophen) as Ultracet® or Tramacet®.

Dosages vary depending on the degree of pain experienced by the patient. Tramadol is approximately 10% as potent as morphine, when given by the IV/IM route. Oral doses range from 50–400 mg daily, with up to 600 mg daily when given IV/IM. The 'combination' pills each contain 37.5 mg of tramadol and 325 mg of paracetamol, with the recommended dose being one or two pills every four to six hours.

Note that unlike most other opioids/opiates, Tramadol is not considered a controlled substance in many countries (US and Canada, among others), and is available with only a normal prescription. According to Erowid, there have also been reports that, in a few countries, Tramadol is available over-the-counter without a prescription at all.

Contents [hide] 1 Mechanism of action 2 Metabolism 3 Adverse effects 4 Dependence 5 Recreational use 6 Proprietary preparations 7 Often used to treat 8 Trivia 9 References 10 External links

[edit] Mechanism of action

The mode of action of tramadol has yet to be fully understood, but it is believed to work through modulation of the GABAergic, noradrenergic and serotonergic systems. The contribution of non-opioid activity is demonstrated by the analgesic effects of tramadol not being fully antagonised by the μ-opioid receptor antagonist naloxone.

Tramadol is marketed as a racemic mixture with a weak affinity for the μ-opioid receptor (approximately 1/6th that of morphine). The (+)-enantiomer is approximately four times more potent than the (-)-enantiomer in terms of μ-opioid receptor affinity and 5-HT reuptake, whereas the (-)-enantiomer is responsible for noradrenaline reuptake effects (Shipton, 2000). These actions appear to produce a synergistic analgesic effect, with (+)-tramadol exhibiting 10-fold higher analgesic activity than (-)-tramadol (Goeringer et al., 1997).

The serotonergic modulating properties of tramadol mean that it has the potential to interact with other serotonergic agents. There is an increased risk of serotonin syndrome when tramadol is taken in combination with serotonin reuptake inhibitors (e.g. SSRIs), since these agents not only potentiate the effect of 5-HT but also inhibit tramadol's metabolism.

It is suggested that tramadol could be effective for alleviating symptoms of depression and anxiety because of its action on GABAergic, noradrenergic and serotonergic systems. However, health professionals generally do not suggest use of the drug for treatment of such disorders.

Tramadol may also be used to treat hypertension when other treatments have failed.

[edit] Metabolism

Tramadol undergoes hepatic metabolism via the cytochrome P450 isozyme CYP2D6, being O- and N-demethylated to 5 different metabolites. Of these, M1 is the most significant since it has 200 times the μ-affinity of (+)-tramadol, and furthermore has an elimination half-life of 9 hours compared to 6 hours for tramadol itself. In the 6% of the population who have slow CYP2D6 activity, there is therefore a slightly reduced analgesic effect. Phase II hepatic metabolism renders the metabolites water-soluble and they are renally excreted. Thus reduced doses may be used in renal and hepatic impairment.

[edit] Adverse effects

The most commonly reported adverse drug reactions are nausea, vomiting and sweating. Drowsiness is reported, although it is less of an issue compared to other opioids. Respiratory depression, a common side effect of most opioids, is not clinically significant in normal doses. By itself, it can decrease the seizure threshold. When combined with SSRIs, tricyclic antidepressants, or in patients with epilepsy, the seizure threshold is further decreased. Seizures have been reported in humans receiving excessive single oral doses (700 mg) or large intravenous doses (300 mg).

[edit] Dependence

Some controversy exists regarding the dependence liability of tramadol. Grünenthal has promoted it as an opioid with a low risk of dependence compared to traditional opioids, claiming little evidence of such dependence in clinical trials. They offer the theory that since the M1 metabolite is the principal agonist at μ-opioid receptors, the delayed agonist activity reduces dependence liability. The noradrenaline reuptake effects may also play a role in reducing dependence.

Despite these claims it is apparent, in community practice, that dependence to this agent does occur. This would be expected since analgesic and dependence effects are mediated by the same μ-opioid receptor. However, this dependence liability is considered relatively low by health authorities, such that tramadol is classified as a Schedule 4 Prescription Only Medicine in Australia, rather than as a Schedule 8 Controlled Drug like other opioids (Rossi, 2004). Similarly, tramadol is not currently scheduled by the U.S. DEA, unlike other opioid analgesics. Nevertheless, the Prescribing Information for Ultram warns that tramadol "may induce psychological and physical dependence of the morphine-type."

[edit] Recreational use

Tramadol can be used recreationally. Its low affinity for opiate receptors produces an euphoria similar to that of traditional opioids. In addition to opiate receptor binding, it also produces central nervous system stimulation which, according to some users, is similar to that produced by amphetamines. Tramadol can cause nausea and epileptic seizures in supertherapeutic doses. A recent study concluded that its abuse liability is markedly less than that of traditional opioids such as hydrocodone or oxycodone. Tramadol has been known to produce severe withdrawal symptoms with abrupt cessation of prolonged use.^[1]

[edit] Proprietary preparations

Grünenthal, which still owns the patent to tramadol, has cross-licensed the agent to various pharmaceutical companies internationally. Thus tramadol is marketed under many trade names including: Adolonta, Anadol, Calmador, Contramal, Crispin, Lumidol, Mandolgine, Mosepan, Nobligan, Poltram, Siverol, Tiparol, Toplagic, Tradol, Tradolan, Tralgit, Tramacet, Tramacip, Tramadin, Tramal, Tramahexal, Tramazac, Tramedo, Ultracet, Ultram, Zamadol and Zydol.

[edit] Often used to treat

• Moderate pain
• Severe pain
• Most types of Neuralgia, including Trigeminal Neuralgia.^{[citation needed]}
• Post operative pain in canines.

[edit] Trivia

• Rapper Russell Jones (a.k.a. Ol' Dirty Bastard) died from an overdose of a combination of cocaine and tramadol on November 13, 2004.^[2]

[edit] References

1. ^ Adams, Edgar; Breiner, Scott; Cicero, Theodore; Geller, Anne; Inciardi, James; Schnoll, Sidney; Senay, Edward; Woody, George (May 2006). "A Comparison of the Abuse Liability of Tramadol, NSAIDs, and Hydrocodone in Patients with Chronic Pain". Journal of Pain and Symptom Management 31 (5): 465-476. Retrieved on 2007-01-13.
2. ^ Zahlaway, Jon. "Autopsy shows ODB died of accidental drug overdose", LiveDaily, December 15, 2004. Retrieved on 2007-01-13.

• Goeringer K, Logan B, Christian G. "Identification of tramadol and its metabolites in blood from drug-related deaths and drug-impaired drivers.". J Anal Toxicol 21 (7): 529-37. PMID 9399121.
• (2004) Ed. Rossi S: Australian Medicines Handbook. Adelaide: Australian Medicines Handbook. ISBN 0-9578521-4-2. 
• Shipton E (2000). "Tramadol--present and future.". Anaesth Intensive Care 28 (4): 363-74. PMID 10969362.
• Ultram (PDF). Ortho-McNeil. – U.S. Prescribing Information
• McDiarmid T, Mackler L, Schneider D (January 2005). "Clinical inquiries. What is the addiction risk associated with tramadol?". J Fam Pract 54 (1): 72-3. PMID 15623411.
• Tramadol Opioids (HTML). Ortho-McNeil. – U.S. Prescribing Information
• McDiarmid T, Mackler L, Schneider D (January 2005). "Clinical inquiries. What is the addiction risk associated with tramadol?". J Fam Pract 54 (1): 72-3. PMID 15623411.

[edit] External links

• http://www.jnj.com/news/jnj_news/20050725_120712.htm - Press release regarding tramadol/acetaminophen combination pill now available in Canada

• Links to external chemical sources.