Flupirtine in the treatment of fibromyalgia and related...

Details Flupirtine in the treatment of fibromyalgia and related... Flupirtine in the treatment of fibromyalgia and related...

2000-03-24

2003-08-26

Page, Thurman K. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

C424S045000, C424S489000, C424S434000

Reexamination Certificate

active

06610324

ABSTRACT:

FIELD OF THE INVENTION
The present invention is directed to medical treatments for fibromyalgia and related conditions. Specifically, the invention is directed to the administration of the drug flupirtine as a means for alleviating the symptoms associated with these disorders.
BACKGROUND OF THE INVENTION
Fibromyalgia is a chronic condition characterized by pain in muscles, fascia and joints. Other symptoms typically include sleep disturbances, chronic fatigue and major depression. The etiology and pathophysiology of fibromyalgia are unknown, but it is clear that the central nervous system is involved. Patients may obtain a degree of relief from analgesic drugs, antidepressants and adjunctive treatments such as moderate exercise, proper diet and stress reduction techniques. Table 1 summarizes the studies that have been carried out in an effort to find an effective drug treatment.
TABLE 1
Drug Treatments for Fibromyalgia
Drug
Study
Treatment
Class*
Method**
Efficacy
Reference
fluoxetine
1
open
+
Johnson, J. Fam. Pract.,
44: 128-30 (1997)
fluoxetine
1
open
+
Finestone, et al., J.A.M.A.,
264: 2869-70 (1990)
fluoxetine
1
open
+
Goldenberg, et al., Arthritis
Rheumatol., 39: 1852-9 (1996)
fluoxetine
1
db
±
Wolfe, et al., Scand. J.
Rheumatol., 23: 255-9 (1994)
fluoxetine
1
open
−
Cortet, et al., Rev. Rheum.
Mal. Osteoartic, 59: 497-500
(1992)
citalopram
1
db
−
Norregaard, et al., Pain,
61: 445-9 (1995)
amitriptyline
1
db
+
Carette, et al., Arthritis
Rheum., 37: 32-40 (1994)
amitriptyline
1
db
+
Carette, et al., Arthritis
Rheumatol., 29: 655-9 (1986)
amitriptyline
1
db
+
Goldenberg, et al., Arthritis
Rheum., 39: 1852-9 (1996)
amitripthline
1
db
+
Goldenberg, et al., Arthritis
Rheum., 29: 1371-7 (1986)
amitriptyline
1
db
+
Jaeschke, et al., J. Rheumatol.,
18: 447-51 (1991)
amitriptyline
1
db
+
Scudds, et al., J. Rheumatol.,
16: 98-103 (1989)
fluphenazine plus
7, 1
open
+
Connolly, Del. Med. J.,
amitriptyline
53: 189-91 (1981)
naproxen plus
1, 2
db
+
Goldenberg, et al., Arthritis
amitriptyline
Rheum., 29: 1371-7 (1986)
ondansetron
9
db
+
Hrycaj, et al., J. Rheumatol.,
23: 1418-23 (1996)
tropisetron
9
open
+
Samborski, et al., Mater Med.
Pol., 28: 17-9 (1996)
katenserin
9
open
+
Stratz, et al., Z. Rheumatol.,
50: 21-2 (1991)
lithium carbonate
6
open
Teasell, Can. Med. Assoc. J.,
144: 122-3 (1991)
lithium carbonate
6
open
Tyber, Can., Med Assoc. J.,
143: 902-4 (1990)
fluoxetine plus
1, 3
open
+
Cantini, et al., Minerva Med.,
cyclobenzaprine
85: 97-100 (1994)
cyclobenzaprine
3
db
+
Carette, et al., Arthritis
Rheum., 37: 32-40 (1994)
cyclobenzaprine
3
db
+
Bennett, Arthritis Rheum.,
31: 1535-42 (1988)
cyclobenzaprine
d
db
+
Quimby, et al., J. Rheumatol
Suppl., 19: 140-3 (1989)
low-dose hs
3
db
+
Santandrea, et al., J. Int. Med.
cyclobenzaprine
Res., 21: 74-80 (1993)
cyclobenzaprine plus
3, 2
open
+
Fossaluzza, et al., Int. J. Clin.
ibuprofen
Pharmacol. Res., 12: 99-102
(1992)
carisoprodol plus
3, 12,
db
+
Vaeroy, et al., Clin.
acetaminophen plus
13
Rheumatol., 8: 245-50 (1989)
caffeine
Zolpidem
4
db
±
Moldofsky, et al., J.
Rheumatol., 23: 529-33 (1996)
ibuprofen plus
4
db
±
Russell, et al., Arthritis
alprazolam
Rheum., 34: 552-60 (1991)
ketamine
15
open
±
Oye, et al., Tidsskr. Nor.
Laegeforen, 116: 3130-1
(1996)
indomethacin
2
open
+
Kelly, J. Am. Geriatr. Soc.,
14: 48-55 (1996)
naproxen
2
db
±
Goldenberg, et al., Arthritis
Rheum., 29: 1371-7 (1986)
tenoxicam
2
db
+
Schorn, S. Afr. Med. J.,
69: 301-3 (1986)
ibuproxam
2
open
+
Ferri, et al., Minerva Med.,
74: 331-6 (1983)
tolmetin
2
db
+
Balme, et al., Curr. Med. Res.
Opin, 7: 127-30 (1980)
tiaprofenic acid
2
db
+
Donald, et al., J. Int. Med.
Res., 8: 382-7 (1980)
aspirin
2
db
+
Donald, et al., J. Int. Med.
Res., 8: 832-7 (1980)
ibuprofen
2
db
+
Le Gallez, et al., Curr. Med.
Res. Opin., 10: 663-7 (1988)
ibuprofen
2
db
−
Yunus, et al., J. Rheumatol.,
16:527-32 (1989)
ibuprofen plus
2, 9
db
+
Le Gallez, et al., Curr. Med.
meptazinol
Res. Opin., 10: 663-7 (1998)
phenylbutazone
2
db
+
Balme, et al., Curr. Med. Res.
Opin., 7: 127-30 (1980)
phenylbutazone plus
2, 8
open
Settel, Curr. Ther. Res. Clin.
prednisone
Exp., 9: 197-9 (1967)
topical capsaicin
10
open
+
Mathias, et al., Am. J. Phys.
Med. Rehabil., 74: 39-44
(1995)
local trigger point
11
open
±
Hong, et al., Arch. Phys. Med.
injections
Rehabil., 77: 1161-6 (1996)
local trigger point
11
open
Jayson, Bull. Hosp. Jt. Dis.,
injections
55: 176-7 (1996)
antibiotics specific for
5
open
−
Dinerman, et al., Ann. Inter.
Lyme disease
Med., 117: 281-5 (1992)
prednisone
8
db
−
Clark, et al., J. Rheumatol.,
12: 980-3 (1985)
chlormezanone
16
db
−
Pattrick, et al., Br. J.
Rheumatol., 32: 55-8 (1993)
proglumetacin
16
open
+
Gusso, et al., Minerva Med.,
76: 567-73 (1985)
acetaminophen
12
db
−
Hrycaj, et al., J. Rheumatol.,
23: 1418-23 (1996)
s-adenosyl-methionine
16
db
+
Jacobsen, et al., Scand. J.
Rheumatol., 20: 294-302
(1991)
zopiclone
16
db
±
Drewes, et al., Scand. J.
Rheumatol., 20: 288-93 (1991)
zopiclone
16
db
−
Gronblad, et al., Clin.
Rheumatol., 12: 186-91 (1993)
intravenous lignocaine
14
open
+
Bennett, et al., Int. J. Clin.
Pharmacol. Res., 15: 115-9
(1995)
5-OH-L-tryptophan
16
open
+
Puttini, et al., J. Int. Med. Res.
20: 182-9 (1992)
malic acid + magnesium
16, 16
db
+
Russell, et al., J. Rheumatol.,
22: 953-8 (1995)
tamoxifen
16
open
Simonson, Lakartidningen,
93: 340 (1996)
botulinum toxin
16
open
−
Paulson, et al., Mov. Disord.,
11: 459 (1996)
*Drug class key: 1 = antidepressant; 2 = NSAIDs; 3 = muscle relaxants (nonbenzodiazepine); 4 = benzodiazepine; 5 = antibiotics; 6 = mood stabilizer; 7 = antipsychotic agent; 8 = corticosteroid; 9 = serotonin (2 or 3) receptor antagonist; 10 = topical agents;
# 11 = trigger point injection; 12 = acetaminophen; 13 = caffeine; 14 = intravenous anesthetics; 15 = NMDA (glutamate) receptor ligand; 16 = miscellaneous agents.
**Study method: db = double-blind
Despite the efforts that have been made, there is still no treatment that is effective in the majority of patients with fibromyalgia. Thus, there is a clear need for new therapies designed to alleviate the suffering of patients with this, and closely related, conditions.
SUMMARY OF THE INVENTION
Flupirtine is an analgesic that has been used in Europe to treat the pain associated with surgery, cancer, trauma, and liver disease. It acts via the central nervous system through non-opite pain pathways, possibly involving the thalamus or spinal pain pathways. In some, but not all, studies flupirtine has been found to be as effective as opiates in relieving pain. Moreover, flupirtine offers a clear advantage over opiates in that it is not addictive and there have been no reports of abuse. The present invention is based upon the unexpected discovery that flupirtine is capable of completely eliminating the chronic and severe body pain present in some patients with fibromyalgia. Relief is possible even when high doses of opiates, non-steroidal anti-inflammatory drugs and placquenil fail to alleviate pain.
In its first aspect, the invention is directed to a method of treating a patient with fibromyalgia by administering a pharmaceutical composition containing flupirtine. The dosage of flupirtine should be sufficient to reduce or eliminate one or more of the symptoms that have been associated with fibromyalgia. These symptoms include diffuse musculoskeletal pain, fatigue, ocular and vestibular disturbances, headaches, paresthesias, esophageal dysmotility, sleep disturbances, and severe depression. The flupirtine may be administered in any dosage form including tablets, capsules, gels, or topical preparations and should be given at a daily dosage of between 50 and 900 mg, calculated on the basis of the free base form of

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