Peripheral Analgesics

Daily doses of 10-20 g (40 g) based on paracetamol or acetylsalicylic acid (aspirin), also in combination with alcohol, are often kept up over several years by alcohol- or medicament-dependent people. These substances are not of great importance for drug users. Sometimes phenacetin is consumed as this, like aspirin and paracetamol, has a euphoric effect in high doses, but this substance has not been sold in Germany since 1987. Metamizol, ibuprofen and propylphenazone are also relevant. 

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Central and peripheral analgesic agents from kappa-opioid agonists 95E405. 

The duration of action of acetaminophen is limited by the formation of water-soluble derivatives of the phenol (glucuronide and sulfate) that are then excreted via the kidney. Protection i)f the phenol as an ether inhibits such inactivation without diminishing biologic activity. Acetylation of p-ethoxyaniline iffords the widely used peripheral analgesic, phenacetin (25). ... 

Polyfibrospongia sp. Dictyocer., Porif./antiviral and peripheral analgesic... 

Stein, C. Peripheral analgesic actions of opioids, J. Pain Symptom. Manage. 1991, 6, 119-124. 

Pathirathna S, Brimelow BC, Jagodic MM et al. (2005) New evidence that both T-type calcium channels and GABAa channels are responsible for the potent peripheral analgesic effects of 5a-reduced neuroactive steroids. Pain 114 429-443... 

Pang WW, Huang PY, Chang DP, Huang MH. The peripheral analgesic effect of tramadol in reducing propofol injection pain a comparison with lidocaine. Reg Anesth Pain Med 1999 24(3) 246-9. 

The antiviral marine natural product 93, [( )-hennoxazo e A] is synthesized by a convergent approach and the final step includes the coupling of oxazole carboxylic acid (95) and pyran derivative (94) using DEPC.36,37 Hennoxazole A is active against herpes with peripheral analgesic activity comparable to that of indomethacin. 

On the other hand, the peripheral analgesic action of the oil, evaluated in mice by inhibition of writhings induced by formic acid injection [49], was only moderate and weaker than the action of indomethacin. In this case also, the effect seems to be attributable to the oxygenated compounds of the oils. 

The habit of abusing peripherally active analgesics is often established at an early age. Later, appetite suppressants, amphetamines as stimulants, and benzodiazepines or laxatives may be taken. Peripheral analgesics therefore play a not inconsiderable role as starter drugs, and there is a special danger of dose increase due to addiction and chronic abuse. 

Some anticonvulsants appear to exhibit antiinflammatory effects. The woimd-healing effects of phenytoin and its associated gingival hypertorophy may reflect its action on fibroblast activity. It appears in animal studies that gabapentin and lamotrigine have peripheral analgesic effects, suggesting an effect on peripheral neurotransmission. 

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