Save up -80% on Dextropropoxyphene
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2018 Price of Dextropropoxyphene
Propoxyphene N-APAP 50-325 mg tablet
* price without discount in nearest pharmacy. Price may vary.
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Dextropropoxyphene volume of distribution
* 16 L/kg
Discount Cards 16,000+
Clients Benefit 29%
Total savings $4,735,080
What is Dextropropoxyphene
Dextropropoxyphene is an analgesic in the opioid category, patented (1955) and manufactured by Eli Lilly and Company. It is intended to treat mild pain and also has antitussive and local anaesthetic effects. The drug has been taken off the market in Europe and the US due to concerns of fatal overdoses and heart arrhythmias. An estimated 10 million patients have used these products. 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.
Dextropropoxyphene mechanism of action
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.
Dosage forms of Dextropropoxyphene
Pendopharm Division Of De Pharmascience Inc
Humans and other mammals
Indication of Dextropropoxyphene
For the relief of mild to moderate pain
Toxicity of Dextropropoxyphene
Coma, respiratory depression, circulatory collapse, and pulmonary edema. Seizures occur more frequently in patients with propoxyphene intoxication than in those with opiate intoxication. LD sub50 /sub=230mg/kg (orally in rat, Emerson)
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