Counterpain-PXM

Uses

Eugenol is a phenol used for the temporary relief of toothaches.

Eugenol is not currently available in any FDA-approved drug products. There are a number of unapproved OTC products that advertise it for the use of toothache. Eugenol is is also commonly used in combination with zinc oxide in dental procedures for the cementation of temporary prostheses and the temporary restoration of teeth and cavities.

Methyl salicylate is a topical counter-irritant used for the symptomatic relief of acute musculoskeletal pain in the muscles, joints, and tendons.

Ointments or liniments containing methyl salicylate are applied topically as counter irritant for relief of acute pain associated with lumbago,sciatica and rheumatic conditions. Local analgesics for human and veterinary medicine.

Carefully consider the potential benefits and risks of Piroxicam and other treatment options before deciding to use Piroxicam. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals. Piroxicam is used for relief of the signs and symptoms of osteoarthritis, for relief of the signs and symptoms of rheumatoid arthritis.

Counterpain-PXM is also used to associated treatment for these conditions: Contusions, Insect Bites, Soreness, Muscle, Sprains, Itching skin, Oral discomfort and painAcute Muscle Pain, Arthritis, Back Pain Lower Back, Backache, Contusions, Joint Pain, Ligament pain, Muscle Inflammation, Muscle Injuries, Muscle Strain, Muscle swelling, Pain, Pain of the Bone and Bones, Pain, Nerve, Partial-Onset Seizures, Postherpetic Neuralgia, Soreness, Muscle, Sprains, Tendon pain, Minor aches, Muscle, joint painsAnkylosing Spondylitis (AS), Osteoarthritis (OA), Rheumatoid Arthritis

How Counterpain-PXM works

The exact mechanism of action of eugenol is unknown. However, eugenol has been shown to interrupt action potentials, which may be involved in its anti-pain activity. Research has also shown eugenol to have anti-inflammatory, neuroprotective, antipyretic, antioxidant, antifungal and analgesic properties.

Counter-irritation is thought to be effective at alleviating musculoskeletal pain as the irritation of the sensory nerve endings is thought to alter or offset pain in the underlying muscle or joints that are served by the same nerves . This is thought to mask the underlying musculoskeletal pain and discomfort. When applied topically, methyl salicylate is thought to penetrate the skin and underlying tissues where it reversibly inhibits cyclooxygenase enzyme and locally and peripherally prevents the production of inflammatory mediators such as prostaglandin and thromboxane A2.

The antiinflammatory effect of Piroxicam may result from the reversible inhibition of cyclooxygenase, causing the peripheral inhibition of prostaglandin synthesis. The prostaglandins are produced by an enzyme called Cox-1. Piroxicam blocks the Cox-1 enzyme, resulting into the disruption of production of prostaglandins. Piroxicam also inhibits the migration of leukocytes into sites of inflammation and prevents the formation of thromboxane A2, an aggregating agent, by the platelets.

Dosage

Counterpain-PXM dosage

Oral-

Ankylosing spondylitis, Osteoarthritis, Rheumatoid arthritis:

• Adult: 20 mg daily as a single dose, divided doses may be used if necessary. Treatment should be reviewed w/in 14 days of starting.
• Elderly: Use the lowest effective dose for the shortest duration.

Should be taken with food.

Side Effects

Oedema, CHF, HTN, syncope, tachycardia; anorexia, abdominal pain, constipation, diarrhoea, dyspepsia, flatulence, heartburn, nausea, vomiting, dry mouth, esophagitis, gastritis, glossitis, haematemesis, melaena, stomatitis; anaemia, increased bleeding time, ecchymosis, eosinophilia, epistaxis, leucopenia, thrombocytopenia; cystitis, dysuria, haematuria, hyperkalaemia, interstitial nephritis, nephritic syndrome, oliguria/polyuria, proteinuria, renal failure; dizziness, headache, anxiety, asthenia, confusion, depression, dream abnormalities, drowsiness, insomnia, malaise, nervousness, paraesthesia, somnolence, tremors, vertigo; tinnitus, blurred vision; elevated LFT results; pruritus, rash, alopecia, bruising, desquamation, erythema, petechial rash, photosensitivity, purpura, sweating, serum sickness-like reactions; fever, infection, sepsis, wt changes, asthma, dyspnoea.

Toxicity

Oral LD50 values (mg/kg) for mouse, rat and rabbit are 1110, 887 and 1300, respectively. Oral LD50 values for child and adult human (mg/kg) are 228 and 506, respectively. Although systemic toxicity from topical administration is rare, methyl salicylate can be absorbed in intract skin to cause stimulation of the central nervous system respiratory center, disturbance of lipid and carbohydrate metabolism, and disturbance of intracellular respiration. Severe toxicity can result in acute lung injury, lethargy, coma, seizures, cerebral edema, and death. In case of salicylate poisoning, the treatment consists of general supportive care, gastrointestinal decontamination with activated charcoal in cases of salicylate ingestion, and monitoring of serum salicylate concentrations. Bicarbonate infusions or hemodialysis can be used to achieve enhanced salicylate elimination .

Symptoms of overdose include drowsiness, nausea, stomach pain, and/or vomiting.

Precaution

Patient with known CV disease or risk factors for CV disease, fluid retention or heart failure, cerebrovascular disease, uncontrolled HTN, asthma. Elderly. Renal and hepatic impairment. Pregnancy and lactation.

Interaction

Increased risk of GI bleeding with anti-platelets and SSRIs. May exacerbate cardiac failure, reduce GFR and increase plasma glycoside levels. Increased risk of nephrotoxicity with ciclosporin and tacrolimus. Increased absorption with cimetidine. Increased risk of GI ulceration with corticosteroids. May interfere with the natriuretic action of diuretics. May displace other highly protein-bound drugs. May increase steady state plasma lithium levels. May antagonise the effect of antihypertensives. May reduce the excretion of methotrexate, leading to acute toxicity. Increased risk of convulsions with quinolones. May interfere with mifepristone-mediated termination of pregnancy.

Volume of Distribution

After absorption, methyl salicylate is distributed throughout most body tissues and most transcellular fluids, primarily by pH dependent passive processes. Salicylate is actively transported by a low-capacity, saturable system out of the CSF across the choroid plexus. The drug readily crosses the placental barrier.

• 0.14 L/kg

Elimination Route

Approximately 12-20% of topically applied methyl salicylate may be systemically absorbed through intact skin within 10 hours of application, and absorption varies with different conditions such as surface area and pH. Dermal bioavailability is in the range of 11.8 – 30.7%. For the assessment of potential oral exposure to salicylates, bioavailability is assumed to be 100% .

Well absorbed following oral administration.

Half Life

The plasma half-life for salicylate is 2 to 3 hr in low doses and about 12 hr at usual anti-inflammatory doses. The half-life of salicylate may be as long as 15 to 30 hr at high therapeutic doses or when there is intoxication.

30 to 86 hours

Elimination Route

Excreted by kidneys as free salicylic acid (10%), salicyluric acid (75%), salicylic phenolic (10%) and acyl glucuronide (5%), and gentisic acid (less than 1%).

Piroxicam and its biotransformation products are excreted in urine and feces, with about twice as much appearing in the urine as in the feces. Approximately 5% of a piroxicam dose is excreted unchanged. However, a substantial portion of piroxicam elimination occurs by hepatic metabolism. Piroxicam is excreted into human milk.

Pregnancy & Breastfeeding use

Pregnancy catagort C (in 1st & 2nd trimester), D (in 3rd trimester)

Contraindication

Hypersensitivity or asthma-type reactions to piroxicam, aspirin or other NSAIDs. History or active GI ulceration, bleeding and perforation; history of GI disorders that predispose to bleeding disorders (e.g. ulcerative colitis, Crohn’s disease, GI cancers or diverticulitis). Treatment of perioperative pain in the setting of CABG surgery. Concomitant use with aspirin, other NSAIDs and anticoagulants.

Acute Overdose

Symptoms: Lethargy, drowsiness, nausea, vomiting, epigastric pain, GI bleeding, anaphylactoid reactions. Rarely, HTN, acute renal failure, resp depression and coma.

Management: Symptomatic and supportive treatment. Emesis and/or activated charcoal (60-100 g in adults, 1-2 g/kg in childn) and/or osmotic cathartic may be indicated. If patient is comatose, having seizures or lacks the gag reflex, gastric lavage may be done if an endotracheal tube w/ cuff inflated is in place to prevent aspiration of gastric contents.

Innovators Monograph

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