Painrelipt

Uses

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

Painrelipt is also used to associated treatment for these conditions: Ankylosing Spondylitis (AS), Osteoarthritis (OA), Rheumatoid Arthritis

How Painrelipt works

The antiinflammatory effect of Painrelipt 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. Painrelipt blocks the Cox-1 enzyme, resulting into the disruption of production of prostaglandins. Painrelipt also inhibits the migration of leukocytes into sites of inflammation and prevents the formation of thromboxane A2, an aggregating agent, by the platelets.

Dosage

Painrelipt 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

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.

Food Interaction

• Avoid alcohol.
• Take with food.

Painrelipt Alcohol interaction

[Moderate] GENERALLY AVOID:

The concurrent use of aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol may lead to gastrointestinal (GI) blood loss.

The mechanism may be due to a combined local effect as well as inhibition of prostaglandins leading to decreased integrity of the GI lining.

Patients should be counseled on this potential interaction and advised to refrain from alcohol consumption while taking aspirin or NSAIDs.

Painrelipt Hypertension interaction

[Major] Fluid retention and edema have been reported in association with the use of nonsteroidal anti-inflammatory drugs (NSAIDs).

Therapy with NSAIDs should be administered cautiously in patients with preexisting fluid retention, hypertension, or a history of heart failure.

Blood pressure and cardiovascular status should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.

[Moderate] Nonsteroidal anti-inflammatory drugs (NSAIDs), including topicals, can lead to new onset of hypertension or worsening of preexisting hypertension, either of which can contribute to the increased incidence of cardiovascular events.

NSAIDs should be used with caution in patients with hypertension.

Blood pressure should be monitored closely during the initiation of NSAID therapy and throughout the course of therapy.

Painrelipt Drug Interaction

Major: celecoxibModerate: duloxetine, omega-3 polyunsaturated fatty acids, metoprolol, sertralineUnknown: amphetamine / dextroamphetamine, zolpidem, diphenhydramine, calcium / vitamin d, atorvastatin, pregabalin, esomeprazole, acetaminophen, montelukast, levothyroxine, cyanocobalamin, ascorbic acid, cholecalciferol, alprazolam, cetirizine

Painrelipt Disease Interaction

Major: asthma, fluid retention, GI toxicity, rash, renal toxicities, thrombosisModerate: anemia, heart failure, hepatotoxicity, hyperkalemia, hypertension, platelet aggregation inhibition

Volume of Distribution

• 0.14 L/kg

Elimination Route

Well absorbed following oral administration.

Half Life

30 to 86 hours

Elimination Route

Painrelipt 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. Painrelipt 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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