Posts Tagged ‘analgesic’

Arthritis Definitions and Joint pain glossary

March 6th, 2009

Following are the definitions for terms commonly used in the diagnosis and treatment of arthritis.

Analgesic: Pain relief medication.

Arthralgia: Pain in the joints.

Arthritis: Inflammation of the joints. There are more than 100 kinds of arthritis.

Autoimmune: A process by which a person’s immune system attacks the body’s own tissues. Rheumatoid arthritis is an autoimmune disease.

Bacteria: Microscopic, one-celled organisms.

Cartilage: Firm, whitish substance at the ends of bones. It acts as the body’s “shock absorbers.”

Collagen: Substance making up the body’s connective tissues.? It gives cartilage its “bounce.”

Corticosteroid: Powerful steroid medication that reduces inflammation.

Glucosamine: An amino sugar occurring in vertebrate tissues including that of marine creatures, from which it’s harvested.

Glucosamine sulfate: A form of glucosamine that has been shown to reduce arthritis pain and rebuild damaged joints.

Gout: A painful inflammation primarily of the big toe, characterized by an excess of uric acid in the blood that leads to crystalline deposits in the small joints.

Ligament: A band of strong connective tissue that connects bones and holds organs in place.

Osteoarthritis: A type of arthritis in which cartilage wears out and joints become stiff and painful.

Prostaglandins: Hormone-like substances that play a part in inflammation.

Proteoglycans: Mortar-like substances made from protein and sugar that are the building blocks of cartilage.

Rheumatoid arthritis: A major form of the disease in which the body’s immune system attacks joints, causing hot, painful swelling and deformity.

Headache Medications: Analgesic, Abortive, and preventative medications

March 1st, 2009

Headache Medications are used in the following ways:

  • Analgesic, or pain relief. Such agents include over-the-counter (OTC) remedies, such as aspirin, acetaminophen, and non-steroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen, naprosyn, which are used to relieve headache symptoms. Some analgesics require prescriptions and include other NSAIDS,  neuroleptics, and opioids.
  • Abortive. These agents are used to reverse, abort or reduce headaches once they start. They include such medications as ergotamine and the newest class of abortives, the triptans, including sumatripan, rizatriptan, and naratriptan. These medications are most appropriate when used no more than two days a week to avoid the risk of rebound headaches or when prophylactic, or preventive, medicines either aren’t effective or can’t be used.
  • Prophylactic, or preventive. These agents are prescribed when headaches occur more than twice a week and/or are extremely painful. They are also prescribed when other medications or remedies used to treat headache symptoms either don’t work or cannot be used. Such agents include beta-blockers, calcium channel blockers and serotonin antagonists.

Migraine Headache Medications

Abortive treatments for migraines are used at the first sign of a migraine and can stop the process that causes the headache pain after it has started. By stopping the headache process, these medications help prevent common symptoms of migraines such as pain, nausea, and sound and light sensitivity. Some medications should not be used during a migraine aura; please follow the instructions of your doctor.

The following medications are used to stop the migraine headache process:

Category Generic Name Brand Name May be used during an aura? Possible Side Effects
Over-the-counter Ibuprofen Motrin   Stomach upset
  Aspirin-Acetominophen-Caffeine Excedrin Migraine, Excedrin, Goody’s   Heartburn
Anxiety
Insomnia
Allergic reaction
Liver Damage
Blood in stool or vomit
Dizziness
Easy bruising
  Naproxen Aleve   Gastrointestinal upset
Gastrointestinal bleeding
Nausea
Vomiting
Rash
Liver damage
Ergot dihydroergotamie DHE-45 injection Migranal intranasal Yes — as indicated for Migranal intranasal only Nausea
Numbness of fingers and toes
Vasoconstrictor Combination acetaminophen isometheptene mucate dichloralphenazone Midrin, Duradrin Yes Sedation
Nausea
Triptans sumatriptan succinate Imitrex injection, oral or intranasal No (injection) Yes (oral or intranasal) Head, jaw, chest and arm discomfort, tightening or tingling
Throat discomfort
Muscle cramps
Flushing
  zolmitriptan Zomig Yes Head, jaw, chest, and arm discomfort, tightening or tingling
Throat discomfort
Muscle cramps
Flushing
  rizatriptan Maxalt Yes Head, jaw, chest, and arm discomfort, tightening or tingling
Throat discomfort
Muscle cramps
Flushing
  naratriptan hydrochloride Amerge Yes Head, jaw, chest, and arm discomfort, tightening or tingling
Throat discomfort
Muscle cramps
Flushing
  almotriptan Axert Yes Head, jaw, chest, and arm discomfort, tightening or tingling
Throat discomfort
Muscle cramps
Flushing
  frovatriptan Frova No Head, jaw, chest, and arm discomfort, tightening or tingling
Throat discomfort
Muscle cramps
Flushing
  Eletriptan Relpax Yes Chest tightness
Dizziness
Dry mouth
Headache
Nausea
Numbness and tingling
Sleepiness
Jaw, throat discomfort

The following medications are used to prevent the migraine headache process:

Medications for Migraine Prevention

Category Generic Name Brand Name Symptoms Relieved Possible Side Effects
Nonsteroidal anti-inflammatories diclofenac Cataflam Headache pain relief Gastrointestinal upset,
drowsiness, dizziness,
vision problems,
ulcers
  Naproxen sodium Aleve Anaprox Headache pain relief Gastrointestinal upset,
gastrointestinal bleeding,
nausea,
vomiting,
rash,
liver damage
Tricyclic antidepressants amitriptyline Elavil Instructions: Frequently started at low dosages and slowly increased to a therapeutic level.
EKG optional.
Periodic blood tests are required while taking this medication.
Taken nightly.
Fatigue
Dry mouth
Weight gain
Constipation
Drowsiness
Blurred vision
Older adults also may experience confusion or faintness.
  imipramine Tofranil Instructions: Frequently started at low dosages and slowly increased to a therapeutic level. Dizziness
Drowsiness
Dry mouth
Weakness
Weight gain
SSRI antidepressants fluoxetine Prozac Not usually effective for treating chronic tension headaches. Instructions: Frequently started at low doses and slowly increased to a therapeutic level.
Usually taken in the morning.
Nausea
Dry mouth
Increased appetite
Agitation
  venlafazine Effexor Not usually effective for treating chronic tension headaches. Vision changes,
decrease in sexual desire or ability, headaches
Beta-Blockers propranolol Inderal Instructions: Depending on the form, may be taken one to three times a day. Fatigue
Depression
Weight gain
Memory disturbance
Faintness
Diarrhea
Calcium channel blockers diltiazem Cardizem Instructions: Frequently started at low dosages and slowly increased to a therapeutic level.
Taken twice a day; usually the first dose is taken in the morning.
Constipation
Dizziness
Anticonvulsants        
Anticonvulsants Topiramate Topamax Instructions: Frequently started at low dosages and slowly increased to a therapeutic level. Tingling in the arms
Nausea
Drowsiness
Weight loss
Botox   Botox    

Tension-Type Headache Medications

Tension-type headaches may actually be a form of migraine headache, which means that many of the medications that work for migraines may work for these headaches as well. See migraine headache treatment. (Your treatment may vary depending upon your sensitivity to certain medications or therapy approaches or your health-care provider’s recommendations.) Following are medications commonly used for treatment of tension-type headaches:

Mild Non-narcotic Analgesics – Aspirin, acetaminophen, and the nonsteroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen and naprosyn.
Comments
:? For mild headache, only. Daily use of aspirin and/or acetaminophen may lead to rebound headaches. Frequent use of aspirin and NSAIDs can lead to gastrointestinal bleeding and, in the case of aspirin, tinnitus (ear ringing).

 Mixed Analgesics, with and without Codeine – Includes acetaminophen/codeine and isometheptene (Midrin), a combination drug of isometheptene, acetaminophen, dichloralphenazone.
Comments:
For mild to moderate tension-type headaches. Isometheptene should not be used if you have coronary artery disease, or with monoamine oxidase inhibitors. Daily use may lead to rebound headaches.

Tricyclic Antidepressants – Includes amitriptyline (Elavil), nortriptyline (Pamelor), Doxepin (Sinequan).
Comments
: May cause dry mouth, blurry vision, urinary retention, constipation  or lightheadedness caused by lowering of blood pressure when suddenly arising, particularly in the elderly. Use with caution if you have heart disease.

Preventative Treatments

Calcium-Channel Blockers – Verapamil (Calan, Isoptin).
Comments
: First choice treatment to prevent cluster headaches, although weeks of therapy may be required to control headaches. Agents may cause water retention, fatigue or constipation.

Corticosteroids – Prednisone, dexamethasone (Decadron).
Comments:
While 80 percent to 90 percent reliable in preventing cluster headache attacks during active therapy, steroids are not appropriate for prolonged preventive therapy. Used regularly, they may cause side effects, including edema (water retention), hyperglycemia (elevated blood sugar), decreased wound healing, bone resorption and mood changes.

Daily Ergot Derivative Use – Ergotamine tartrate and Dihydroergotamine (DHE).
Comments:

  • Daily use of ergotamine tartrates (ErgostatSL, Cafergot, Wigraine) is reserved for the most extreme and debilitating cases due to a high incidence of side effects, including rebound or chronic headaches. As a result, ergotamine use typically is limited to no more than two days per week.
  • DHE is similar to ergotamine, but is not associated with rebound headaches.

The Triptans – Sumatriptan (Imitrex), Naratriptan (Amerge), Rizatriptan (Maxalt) and Zolmitriptan (Zomig).
Comments:
For best results, use these medications soon after the headache begins. Triptans should not be used if you have coronary artery disease, heart disease, or with ergotamine migraine medication. They may cause flushing, tingling, warmth, numbness or tightness in the chest. Do not use in aura phase of migraine with aura.? Sumatriptan comes in pill and spray form.

Anticonvulsants – Valproic Acid (Depakote).
Comments
: Recently approved by the FDA for migraine prevention, it may cause weight gain, nausea, vomiting, diarrhea and dizziness.? Warning: Cases of acute and fatal liver problems have been associated with Depakote use.

Daily Opioids
Comments: Reserved for extreme cases where all other reasonable treatments have failed or cannot be used to prevent cluster headaches.

Other Preventive Treatments – A number of other therapies have been used to prevent cluster headaches.? Among them are: lithium, methysergide/methylergonovine, divalproex sodium, and transdermal or oral clonidine.

Symptomatic Cluster Headache Medications/Therapies

Following are some medications and therapies commonly used to treat cluster headaches:

Oxygen Inhalation Therapy
Comments:
Inhaling pure oxygen via a facemask is useful in alleviating headache symptoms, particularly when taken at the first sign of headache pain. Do not use if you have chronic obstructive pulmonary disease.

Dihydroergotamine (DHE)
Comments
: Similar to ergotamine, DHE is not associated with rebound headaches. It is used as a preventive treatment as well.

The Triptans – Sumatriptan (Imitrex), Naratriptan (Amerge), Rizatriptan (Maxalt) and Zolmitriptan (Zomig).
Comments:
For best results, use these medications soon after the headache begins. Use early in the course of the headache for best results. Triptans should not be used if you have coronary artery disease, heart disease or with ergotamine medications. They may cause flushing, tingling, warmth, numbness or tightness in the chest. Sumatriptan comes in pill and spray form.

Lidocaine
Comments:
? A nasal spray, it results in rapid relief of migraine and lasts 10-15 minutes. Headache relapse may occur.

Neuroleptics – Used for symptomatic relief of headache pain and to treat headache-induced nausea and vomiting. These include metoclopramide (Reglan);
phenothiazines
: chlorpromazine (Thorazine), prochlorperazine (Compazine), perphenazine (Trilafon), promethezine (Phenergan), and Trimethobenzamide (Tigan); and
butyrophenones
: haloperidol (Haldol) and droperidol (Inapsine).
Comments
: Possible side effects include sleepiness, confusion and low blood pressure.? Prolonged regular use can lead to neurological disorders such as Pparkinsonism and tardive dyskinesia.

Opioids – Rectal or nasal sprays.
Comments
:? Avoid frequent use.

Other Symptomatic Cluster Headache Treatments – A number of other drugs have been used to treat the symptoms of cluster headaches. Among them are capsaicin and indomethacin (Midrin).

“Ordinary” Headache Medications

Following are some medications commonly used to treat so-called “ordinary” headaches:

Mild Non-narcotic Analgesics – aspirin, acetaminophen, and the nonsteroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen and naprosyn.
Comments:
? For mild headache, only. Daily use of aspirin and acetaminophen may lead to rebound headaches. Frequent use of aspirin and NSAIDs can lead to gastrointestinal bleeding and, in the case of aspirin, and/ or acctominophen may leat to reboun headaches and tinnitus (ear ringing).

Secondary Headaches Medications

Post-Traumatic Headache Treatment

Treatment of post-traumatic headaches requires a comprehensive, multidisciplinary approach.? In most cases, patients are treated according to specific headache patterns. See migraine headache treatment and tension headache treatment for specific treatments.?

Reactive Headache Treatment

Reactive headaches can be caused by virtually hundreds of external factors. Perhaps the best solution for reactive headache sufferers is to identify and, if possible, avoid or eliminate whatever triggers the headache. A visit to your physician to rule out the more serious causes of reactive headaches is the first step in treating such headaches.? For example, headaches caused by seasonal allergies typically respond to antihistamine medications, topical nasal cortisone and related sprays or desensitization injections used to treat various types of allergies.

Rebound Headache Treatment

Rebound headaches are caused by medication withdrawal following frequent or excessive use of headache pain medications. Treatment typically focuses on detoxification — slowly tapering medications — and on easing side effects, such as nausea.? While the headaches may intensify for a few days following medication withdrawal, rebound headaches usually disappear after three to five days.? Preventive medications are not effective in treating rebound headache until medication withdrawal is complete, which in more severe cases may require hospitalization.? While this detoxification process may eliminate the rebound headache, the original headache (such as migraine, tension-type or cluster) that prompted the overuse of pain medications may still be present following withdrawal. Following are some medications commonly used to treat rebound headaches:

Nonsteroidal Anti-Inflammatory Drugs (NASIDs) – Includes Ibuprofen and Naprosyn.
Comments
:? Unlike many other pain-relieving medications, NSAIDs do not cause rebound headaches. Taking small doses may help ease pain during medication withdrawal.

Neuroleptics – Chlorpromazine (Thorazine) or Prochlorperazine (Compazine).
Comments
:? Such drugs are used to treat medication withdrawal symptoms such as nausea and vomiting, which are a major side effect of ergotamine withdrawal.

Sinus Headache Medications

Acute or chronic sinusitis, or sinus infections, can cause headaches or trigger pre-existing headache conditions, such as migraines.? Because sinus headaches are among the most misdiagnosed headache conditions, a thorough medical examination is needed to make sure you are, indeed, suffering from a sinus infection-related headache. Headaches caused by acute sinusitis typically are relieved when the sinus infections are cleared up using oral antibiotics. Chronic, or recurring sinus infections may require intravenous antibiotics or surgically draining the sinus cavity, which in turn should relieve your headache.

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Tramadol: basic pharmacology and emerging concepts

February 10th, 2009

Tramadol hydrochloride is a widely prescribed, centrally acting analgesic marketed in over 90 countries. Before being released in the U.S. in 1995, the drug had been available in Europe for almost two decades.

Thus, the pharmacokinetic and pharmacodynamic properties of tramadol have been extensively investigated.  However, additional information about the drug continues to be discovered. Tramadol exists as a racemic mixture with the (+)-enantiomer and the (-)-enantiomer, and at least some of their metabolites, having different effects. Tramadol has dual mechanisms of action by which analgesia may be achieved: micro-opioid receptor activation and enhancement of serotonin and norepinephrine transmission.

Tramadol is available as drops, capsules and sustained-release formulations for oral use, suppositories for rectal use and solution for intramuscular, intravenous and subcutaneous injection. After oral administration, tramadol is rapidly and almost completely absorbed. Sustained-release tablets release the active ingredient over a period of 12 hours, reach peak concentrations after 4.9 hours and have a bioavailability of 87–95% compared with capsules. Tramadol is rapidly distributed in the body; plasma protein binding is about 20%.

 Serotonin syndrome may occur in patients taking combinations of tramadol and other agents that increase serotonin activity. The relative degree of contribution of each mechanism toward pain control is not fully understood.

Tramadol is mainly metabolised by O- and N-demethylation and by conjugation reactions forming glucuronides and sulfates. Tramadol and its metabolites are mainly excreted via the kidneys. The mean elimination half-life is about 6 hours.

 

The O-demethylation of tramadol to M1, the main analgesic effective metabolite, is catalysed by cytochrome P450 (CYP) 2D6, whereas N-demethylation to M2 is catalysed by CYP2B6 and CYP3A4. The wide variability in the pharmacokinetic properties of tramadol can partly be ascribed to CYP polymorphism. O- and N-demethylation of tramadol as well as renal elimination are stereoselective. Pharmacokinetic-pharmacodynamic characterisation of tramadol is difficult because of differences between tramadol concentrations in plasma and at the site of action, and because of pharmacodynamic interactions between the two enantiomers of tramadol and its active metabolites.

The analgesic potency of tramadol is about 10% of that of morphine following parenteral administration. Tramadol provides postoperative pain relief comparable with that of pethidine, and the analgesic efficacy of tramadol can further be improved by combination with a non-opioid analgesic. Tramadol may prove particularly useful in patients with a risk of poor cardiopulmonary function, after surgery of the thorax or upper abdomen and when non-opioid analgesics are contraindicated.

 

Tramadol is an effective and well tolerated agent to reduce pain resulting from trauma, renal or biliary colic and labour, and also for the management of chronic pain of malignant or nonmalignant origin, particularly neuropathic pain. Tramadol appears to produce less constipation and dependence than equianalgesic doses of strong opioids.

By increasing serotonin and norepinephrine neurotransmission, tramadol may conceivably also exert a degree of antidepressant effect. Therefore, tramadol may be of particular value in patients with chronic pain who also suffer from depression. This drug has been shown to be beneficial in the treatment of a wide range of acute and chronic pain syndromes, including neuropathic pain. While abuse of tramadol may occur, several large studies have demonstrated that the incidence of abuse is rather low, about one case per 100,000 patients.