Dosage regimens of buprenorphine achieving rapid pain relief without increasing nausea, vomiting, or other adverse effects, are described. Also described are buprenorphine dosage regimens for treating chronic pain comprising administering to the patient (1) a first buprenorphine-containing transdermal dosage form for a first dosing period that is no more than about 5 days; (2) a second buprenorphine-containing transdermal dosage form for a second dosing period that is no more than 5 days, the second dosage form comprising the same dosage of buprenorphine as, or a greater dosage of buprenorphine than, the first dosage form; and (3) a third buprenorphine-containing transdermal dosage form for a third dosing period, the third dosage form comprising a greater dosage of buprenorphine than the second dosage form.

Purdue Pharma L.P.

Transdermal buprenorphine dosage regimen for analgesia

The invention is directed to 4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB.sub.1 receptor modulators, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, to methods for preparing novel intermediates useful for their syntheses, and to methods for preparing compositions. The invention also relates to the uses of compounds and compositions administered to patients to achieve a therapeutic effect in multiple sclerosis, traumatic brain injury, pain including chronic pain, neuropathic pain, acute pain and inflammatory pain, osteoporosis, appetite disorders, epilepsy, Alzheimer's disease, Tourette's syndrome, cerebral ischaemia, emesis, nausea, and gastrointestinal disorders. Compounds of the present disclosure are directed to formula (I): ##STR00001## wherein the substituents have the definitions given in the specification.

Lange; Josephus H. M.

Wals; Hendrik C.

Van Vliet; Bernard J.

Yildirim; Mahmut

Solvay Pharmaceuticals B.V.

4,5 dihydro-(1H)-pyrazole derivatives as cannabinoid CB.sub.1 receptor modulators

The present invention relates to compressed tablets for peroral delivery of the cannabinoid .DELTA.9-tetrahydrocannabinol(THC). More particularly, the invention provides a compressed tablet having a tablet weight of 25-1000 mg, said tablet being composed of: compressed tablet containing delta 9-tetrahydrocannabinol, method for its manufacture and use of such tablet in oral treatment .cndot.30-90 wt % of a granulate; .cndot.10-70 wt % of lactose; and .cndot.0-30 wt % of other tablet excipients; wherein the granulate contains: a.2-5 wt % of .DELTA.9-tetrahydrocannabinol; b.2-20 wt % of sucrose fatty acid mono-ester; c.50-96 wt % of lactose; d.0.05-0.6 wt % of antioxidant; and e.0-25 wt % of other granulate excipients. The compressed tablets according to the invention can conveniently be used in the treatment of spasticity and pain caused by multiple sclerosis, neurophatic pain, chronic pain, behavioral disturbance by Alzheimer's disease, stroke, spinal cord injury, peripheral neuropathy, neurogenic pain, nociceptive pain and nausea. The invention further provides a method for the manufacture of the compressed tablets.

Echo Pharmaceuticals B.V.

Compressed tablet containing .DELTA.9-tetrahydrocannabinol, method for its manufacture and use of such tablet in oral treatment

chronic pain

náusea

nausea

chronic pain/náusea

Transdermal buprenorphine dosage regimen for analgesia

4,5 dihydro-(1H)-pyrazole derivatives as cannabinoid CB.sub.1 receptor modulators

Compressed tablet containing .DELTA.9-tetrahydrocannabinol, method for its manufacture and use of such tablet in oral treatment

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