Oxymark
Oxymark Uses, Dosage, Side Effects, Food Interaction and all others data.
Dextropropoxyphene is an opioid analgesic manufactured by Eli Lilly and Company. It is used in the symptomatic treatment of mild pain. It displays antitussive and local anaesthetic actions. Due to the risk of cardiac arrhythmias and overdose, possibly leading to death, dextropropoxyphene has been withdrawn from the market in Europe and the United States. The drug is often referred to as the general form, "propoxyphene", however only the dextro-isomer (dextropropoxyphene) has any analgesic effect. The levo-isomer appears to exhibit a very limited antitussive effect.
Propoxyphene, a synthetic opiate agonist, is structurally similar to methadone. Its general pharmacologic properties are those of the opiates as a group. The analgesic effect of propoxyphene is due to the d-isomer, dextropropoxyphene. It binds to the opiate receptors and leads to a decrease of the perception of pain stimuli. Propoxyphene possesses little to no antitussive activity and no antipyretic action.
Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, anti-pyretic, and analgesic properties. It inhibits prostaglandin synthetase/cyclooxygenase, which limits prostaglandin production. Its cyclooxygenase inhibiting potency is intermediate, but is relatively selective for the cyclo-oxygenase-2 (COX-2) thus the potential for gastric injury and intolerance is less. It is also a free radical scavenger, and helps protect against the tissue damage that occurs during inflammation.
Food, gender and advanced age have negligible effects on nimesulide pharmacokinetics.
| Trade Name | Oxymark |
| Generic | Nimesulide + Dextropropoxyphene |
| Weight | 100mg |
| Type | Tablet |
| Therapeutic Class | |
| Manufacturer | Unimarck Pharma India Limited |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Dextropropoxyphene is an opioid analgesic used to treat mild to moderate pain.
For the relief of mild to moderate pain.
Nimesulide is used for acute pain; extra-articular disorders; osteoarthritis; post-op pain; primary dysmenorrhoea
Oxymark is also used to associated treatment for these conditions: PainMenstrual Distress (Dysmenorrhea), Pain, Pain, Acute, NSAIDs
How Oxymark works
Propoxyphene acts as a weak agonist at OP1, OP2, and OP3 opiate receptors within the central nervous system (CNS). Propoxyphene primarily affects OP3 receptors, which are coupled with G-protein receptors and function as modulators, both positive and negative, of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is inhibited. Opioids such as propoxyphene also inhibit the release of vasopressin, somatostatin, insulin, and glucagon. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
The therapeutic effects of Nimesulide are the result of its complete mode of action which targets a number of key mediators of the inflammatory process such as: COX-2 mediated prostaglandins, free radicals, proteolytic enzymes and histamine.
Dosage
Oxymark dosage
100 mg twice daily.Should be taken with food. Take after meals.
Side Effects
Epigastric discomfort, heartburn or abdominal cramps, nausea, vomiting and diarrhoea; skin rash, pruritus, oedema, headache, dizziness, drowsiness; hypersensitivity reactions (e.g. bronchospasm, rhinitis, angioedema urticaria); GI haemorrhage/perforation; bullous/erosive stomatitis, purpura, thrombocytopenia, toxic epidermal necrolysis, haematuria, oliguria, and renal failure; increases in liver enzymes.
Toxicity
Coma, respiratory depression, circulatory collapse, and pulmonary edema. Seizures occur more frequently in patients with propoxyphene intoxication than in those with opiate intoxication. LD50=230mg/kg (orally in rat, Emerson)
Oral TDLO (human): 1.429 mg/kg; Oral TDLO (woman): 2 mg/kg; Oral LD50 (rat): 200 mg/kg; Oral LD50 (mouse): 392 mg/kg
Precaution
History of GI tract disease, infections, oedema, hypertension, elderly, lactation.
Interaction
Additive hepatotoxic effects with known hepatotoxins: anti-convulsants (e.g. valproic acid), anti-fungals (e.g. ketoconazole), anti-tuberculous drugs (e.g. isoniazid), tacrine, pemoline, amiodarone, methotrexate, methyldopa, amoxicillin/clavulanic acid. May decrease the oral bioavailability of furosemide and the natriuretic and diuretic response to furosemide. Increased risks of GI and hepatic adverse effects with other NSAIDs, including aspirin. May increase anti-coagulant effect of warfarin. Potentiates the action of phenytoin. May be displaced from binding sites with fenofibrate, salicylic acid, and tolbutamide. Interactions between NSAIDs and lithium, probenecid and ciclosporin, have been documented.
Volume of Distribution
- 16 L/kg
Elimination Route
Rapidly absorbed following oral administration.
Half Life
6-12 hours
1.8–4.7 hours
Clearance
- 2.6 L/min
Elimination Route
The major route of metabolism is cytochrome CYP3A4 mediated N-demethylation to norpropoxyphene, which is excreted by the kidneys. In 48 hours, approximately 20% to 25% of the administered dose of propoxyphene is excreted via the urine, most of which is free or conjugated norpropoxyphene.
Renal (50%), fecal (29%)
Pregnancy & Breastfeeding use
Category not classified
Contraindication
Hypersensitivity; GI bleeding, active peptic ulcer disease; severe renal and heart failure; hepatic impairment or known liver disease; coagulation disorders; pregnancy; children <12 yr.
Acute Overdose
Epigastric pain, nausea, vomiting, drowsiness, lethargy, GI haemorrhage, seizures, hypertension, apnoea, coma, anaphylactic reactions and renal failure. Treatment is supportive.
Storage Condition
Protect from heat and humidity; store at <25°C.
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