Drugs...Medications

Drugs...Medications:

Codeine (Schedule II drug)

Codeine is the most widely used, naturally occurring narcotic in medical treatment in the world. This alkaloid is found in opium in concentrations ranging from 0.7 to 2.5 percent. However, most codeine used in the United States is produced from morphine. Codeine is also the starting material for the production of two other narcotics, dihydrocodeine and Hydrocodone.
Codeine is medically prescribed for the relief of moderate pain and cough suppression. Compared to morphine, codeine produces less analgesia, sedation, and respiratory depression, and is usually taken orally. It is made into tablets either alone (Schedule II) or in combination with aspirin or acetaminophen (I.e., Tylenol with Codeine, Schedule III). As a cough suppressant, codeine is found in a number of liquid preparations (these products are in Schedule V). Codeine is also used to a lesser extent as an injectable solution for the treatment of pain. Codeine products are diverted from legitimate sources and are encountered on the illicit market

Hydrocodone (Schedule III drug)

Hydrocodone is an effective antitussive (anti-cough) agent, and as an opiate it is also an effective analgesic for mild to moderate pain control. Five mg of Hydrocodone is equivalent to 30 mg of codeine when administered orally. Early comparisons concluded that Hydrocodone and morphine were equipotent for pain control in humans. However, it is now considered that a dose of 15 mg (1/4 gr) of Hydrocodone is equivalent to 10 mg (1/6 gr) of morphine. Hydrocodone is considered to be morphine-like in all respects.

There are over 200 products containing Hydrocodone in the U.S. In its most usual product forms Hydrocodone is combined with acetaminophen (Vicodin, Lortab), but it is also combined with aspirin (Lortab ASA), ibuprofen (Vicoprofen), and antihistamines (Hycomine). Both tablet and liquid forms of Hydrocodone are available (e.g., Tussionex)

Hydrocodone is in Schedule II of the Controlled Substances Act. Preparations containing Hydrocodone in combination with other non-narcotic medicinal ingredients are in Schedule III.

Vicodin, Hydrocodone in combination with acetaminophen, is a commonly abused version of Hydrocodone. Vicodin, as with all narcotic analgesics, can be habit forming---causing dependence, tolerance, and withdrawal symptoms if not used as it is prescribed. Even when used as prescribed, the following effects are possible:

COMMON SIDE EFFECTS MAY INCLUDE: dizziness, light-headedness, nausea, sedation, vomiting, and constipation.

LESS COMMON SIDE EFFECTS: allergic reactions, blood disorders, mood changes, mental cloudiness, anxiety, lethargy, urine retention, ureteral spasm, irregular breathing, respiratory depression, and skin rash.

SYMPTOMS OF OVERDOSE: bluish tinge to skin, cold and clammy skin, extreme sleepiness progressing to a possible state of unresponsiveness or coma, heart problems, heavy perspiration, kidney problems, limp muscles, liver failure, low blood pressure, nausea, slow heartbeat, troubled or slowed breathing, and vomiting.

Hydrocodone
or search: Hydrocodone Hydrocodone is an effective antitussive (anti-cough) agent, and as an opiate it is also an effective analgesic for mild to moderate pain control. Five mg of Hydrocodone is equivalent to 30 mg of codeine when ... (Vicodin, Lortab), but it is also combined with aspirin (Lortab ASA).

The Controlled Substances Act in the United States, divides drugs and medications into five schedules dependent on their potential for abuse. The list below contains many, but not all, commonly abused prescription medications:

• Schedule I (high potential for abuse, has no accepted medical use in the U.S. and lack of safety for use under medical supervision)
• Schedule II (high potential for abuse, has a currently accepted medical use, may lead to severe physical dependence or addiction)
• Alfentanil (Alfenta)
• Amobarbital (Amytal, Tuinal)
• Amphetamine (Dexedrine, Biphetamine, Adderall, Obetrol)
• Codeine
• Dihydrocodeine (Didrate, Parzone)
• Fentanyl (Duragesic, Sublimaze, Innovar)
• Glutethimide (Doriden, Dorimide)
• Hydromorphone (Dilaudid)
• Levomethadyl (ORLAAM)
• Levorphanol (Levo-Dromoran)
• Marinol (Dronabinol)
• Methadone (Dolophine, Amidone, Methadose)
• Methamphetamine (Desoxyn)
• Methylphenidate (Ritalin)
• Mepridine (Demorol, Mepergan)
• Morphine (MS Contin, Oramorph, Duramorph, Roxanol)
• Oxycodone (OxyContin, Percodan, Percocet, Tylox, Roxicodone)
• Oxymorphone (Numorphan)
• Pentobarbital (Nembutal)
• Phendimetrazine (Preludin)
• Secobarbital (Seconal, Tuinal)
• Sufentanil (Sufenta)
• Schedule III (has a potential for abuse less than Schedule I or II, has a currently accepted medical use, may lead to moderate or low physical dependence or addiction)
  
  
• Amobarbital compounds
• Anabolic Steroids
• Benzphetamine
  (Didrex, Inapetyl)
• Boldenone
  (Equipoise, Parenabol, Vebonol)
• Buprenorphine
  (Buprenex, Temgesic)
• Hydrocodone 15 mg/du
  (Tussionex, Tussend, Lortab, Vicodin, Hycodan, Anexsia
• Schedule IV (has a potential for abuse less than Schedule III, has a currently accepted medical use, may lead to limited physical dependence or addiction)
• Alprazolam (Xanax)
• Chloral Hydrate (Noctec)
• Chlordiazepoxide
  (Librium, Libritabs, Limbitrol)
• Clonazepam (Klonopin, Clonopin)
• Dextropropoxyphene (Darvon, Darvocet, Dolene, Propacet)
• Diazepam
  (Valium, Valrelease)
• Estazolam (ProSom, Domnamid, Eurodin, Nuctalon)
• Ethchlorvynol (Placidyl)
• Ethinamate (Valmid, Valamin)
• Flunitrazepam (Rohypnol, Narcozep, Darkene, Roipnol)
• Flurazepam
  (Dalmane)
• Lorazepam (Ativan)
• Maxindol (Sanorex, Maxanor)
• Meprobamate (Miltown, Equanil, Deprol, Equagesic, Meprospan)
• Modanafinil (Provigil)
• Oxazepam (Serax, Serenid-D)
• Oxazolam (Serenal, Convertal)
• Pentazocine (Talwin, Talacen)
• Quazepam (Doral, Dormalin)
• Sibutramine (Meridia)
• Temazepam (Restoril)
• Triazolam (Halcion)
• Zaleplon
  (Sonata)
• Zolpidem (Ambien, Stilnoct, Ivadal)
• Schedule V (has a potential for abuse less than Schedule IV, has a currently accepted medical use, may lead to limited physical dependence or addiction)

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Tramadol

Tramadol
From Wikipedia, the free encyclopedia

Systematic (IUPAC) name
rac-(1R,2R)-2-(dimethylaminomethyl)-1-
(3-methoxyphenyl)-cyclohexanol

Identifiers
CAS number 27203-92-5
ATC code N0 2AX02
PubChem 33741
DrugBank APRD00028

Chemical data
Formula C16H25NO2
Mol. mass 263.4 g/mol

SMILES search in eMolecules,
PubChem

Pharmacokinetic data
Bioavailability 68–72% Increases with
repeated dosing.
Protein binding 20%
Metabolism Hepatic demethylation
and glucuronidation
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, as a 4-phenyl-piperidine analogue of codeine,[1][2] 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, Ultram in U.S., Zytrim in Spain and Canada, and Calmador in Argentina). 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.

Unlike most other opioids/opiates, Tramadol is not considered a controlled substance in many countries (U.S. and Canada, among others), and is available with a normal prescription. Tramadol is available over-the-counter without prescription in a few countries.[3]

Contents

1 Mechanism of action
2 Metabolism
3 Adverse effects
4 Dependence
5 Recreational use
6 Proprietary preparations
7 Uses
7.1
Veterinary
8 Trivia
9 Footnotes
10 References
11 External links

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 metabolism.

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 excreted by the kidneys. Thus reduced doses may be used in renal and hepatic impairment.


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). An Australian study finds that of 97 confirmed new-onset seizures, 8 were associated with Tramadol, and that in the authors' First Seizure Clinic, "Tramadol is the most frequently suspected cause of provoked seizures" (Labate 2005). Dosages of coumadin/warfarin may need to be reduced for anticoagulated patients to avoid bleeding complications.


Dependence
Some controversy exists regarding the dependence liability of tramadol. Grünenthal has promoted it as an opioid with a low risk of opioid 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." In addition, there are widespread reports by consumers of extremely difficult withdrawal experiences.


Recreational use
As an opioid analgesic, tramadol can be abused. Its low antagonism (interference with the action of) of the μ opiate receptor produces effects similar to other narcotics (i.e. morphine, hydrocodone), albeit not nearly as intense. In addition to acting as an opiate, tramadol is also a rapidly-acting SSRI. At higher-than-therapeutic doses, tramadol can cause seizures (typically tonic-clonic) and severe nausea, which could deter abuse to some extent. Tramadol has been known to produce severe withdrawal symptoms with abrupt cessation of prolonged use.[4]


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: Adolan, Adolonta, Anadol, Calmador, Contramal, Crispin, Lumidol, Mandolgine, Mosepan, Nobligan, Poltram, Sintradon, Siverol, Tiparol, Toplagic, Tradol, Tradolan, Tralgit, Tramacet, Tramacip, Tramadin, Tramal, Tramahexal, Tramazac, Trama-Klosidol, Tramedo, Trodon, Ultracet, Ultram, Zaldiar, Zamadol, Zydol and Zytram.

Uses
Tramadol is often used to treat moderate and severe pain and most types of neuralgia, including trigeminal neuralgia.[citation needed]

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

Veterinary
Tramadol is used to treat post-operative and/or chronic (e.g. cancer-related) pain in dogs.


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.[5]

Footnotes
^ Dayer P, Desmeules J, Collart L (1997). "[Pharmacology of tramadol]". Drugs 53 Suppl 2: 18–24. PMID 9190321.
^ Opioids.com
^ Erowid
^ 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.
^ Zahlaway, Jon. "Autopsy shows ODB died of accidental drug overdose", LiveDaily, December 15, 2004. Retrieved on 2007-01-13.

References
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.
Labate A, Newton M, Vernon G, Berkovic S (2005). "Tramadol and new-onset seizures.". emja: The Medical Journal of Australia 182 (1): 42-43.
(2004) in 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.

External links
Press release from Johnson & Johnson regarding tramadol/acetaminophen combination pill now available in Canada
[hide]v • d • eAnalgesics (N02A, N02B)
Opioids Buprenorphine, Butorphanol, Codeine, Dextropropoxyphene, Diamorphine, Dihydrocodeine, Fentanyl, Hydrocodone, Hydromorphone, Ketobemidone, Levorphanol, Methadone, Morphine, Nicomorphine, Opium, Oxycodone, Oxymorphone, Pethidine (see also longer list)
Salicylic acid and derivatives Aspirin (Acetylsalicylic Acid), Diflunisal, Ethenzamide, Salicin, Salicylamide -- See also: NSAIDs
Pyrazolones Aminophenazone, Metamizole, Phenazone
Cannabinoids Cannabis, AM404
Anilides Paracetamol (acetaminophen), Phenacetin
Others Ziconotide, Tetrahydrocannabinol, Ibuprofen, Ketoprofen, Mefenamic Acid, Naproxen, Diclofenac, Flurbiprofen, Diflunisal, Indomethacin, Ketorolac, Meloxicam, Piroxicam

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