GB2129299A - Pharmaceutical compositions - Google Patents
Pharmaceutical compositions Download PDFInfo
- Publication number
- GB2129299A GB2129299A GB08231975A GB8231975A GB2129299A GB 2129299 A GB2129299 A GB 2129299A GB 08231975 A GB08231975 A GB 08231975A GB 8231975 A GB8231975 A GB 8231975A GB 2129299 A GB2129299 A GB 2129299A
- Authority
- GB
- United Kingdom
- Prior art keywords
- monoamine oxidase
- tryptophan
- oxidase inhibitor
- present
- compositions
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 12
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims abstract description 73
- 229940123685 Monoamine oxidase inhibitor Drugs 0.000 claims abstract description 38
- 239000002899 monoamine oxidase inhibitor Substances 0.000 claims abstract description 38
- 229960004799 tryptophan Drugs 0.000 claims abstract description 36
- 239000000203 mixture Substances 0.000 claims abstract description 33
- 239000000935 antidepressant agent Substances 0.000 claims abstract description 11
- 229940005513 antidepressants Drugs 0.000 claims abstract description 11
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims abstract description 10
- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 claims abstract description 10
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims abstract description 10
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 claims abstract description 10
- DFPAKSUCGFBDDF-UHFFFAOYSA-N nicotinic acid amide Natural products NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims abstract description 9
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims abstract description 7
- 235000005152 nicotinamide Nutrition 0.000 claims abstract description 6
- 239000011570 nicotinamide Substances 0.000 claims abstract description 6
- AUNGANRZJHBGPY-UHFFFAOYSA-N D-Lyxoflavin Natural products OCC(O)C(O)C(O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-UHFFFAOYSA-N 0.000 claims abstract description 5
- OVBPIULPVIDEAO-UHFFFAOYSA-N N-Pteroyl-L-glutaminsaeure Natural products C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-UHFFFAOYSA-N 0.000 claims abstract description 5
- JZRWCGZRTZMZEH-UHFFFAOYSA-N Thiamine Natural products CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N JZRWCGZRTZMZEH-UHFFFAOYSA-N 0.000 claims abstract description 5
- 239000011668 ascorbic acid Substances 0.000 claims abstract description 5
- 235000010323 ascorbic acid Nutrition 0.000 claims abstract description 5
- 229960005070 ascorbic acid Drugs 0.000 claims abstract description 5
- 235000019152 folic acid Nutrition 0.000 claims abstract description 5
- 239000011724 folic acid Substances 0.000 claims abstract description 5
- 229960000304 folic acid Drugs 0.000 claims abstract description 5
- 229960003512 nicotinic acid Drugs 0.000 claims abstract description 5
- 235000008160 pyridoxine Nutrition 0.000 claims abstract description 5
- 239000011677 pyridoxine Substances 0.000 claims abstract description 5
- 239000002151 riboflavin Substances 0.000 claims abstract description 5
- 229960002477 riboflavin Drugs 0.000 claims abstract description 5
- 235000019192 riboflavin Nutrition 0.000 claims abstract description 5
- 239000011721 thiamine Substances 0.000 claims abstract description 5
- 235000019157 thiamine Nutrition 0.000 claims abstract description 5
- KYMBYSLLVAOCFI-UHFFFAOYSA-N thiamine Chemical compound CC1=C(CCO)SCN1CC1=CN=C(C)N=C1N KYMBYSLLVAOCFI-UHFFFAOYSA-N 0.000 claims abstract description 5
- 229960003495 thiamine Drugs 0.000 claims abstract description 5
- 229940011671 vitamin b6 Drugs 0.000 claims abstract description 5
- IGLYMJRIWWIQQE-QUOODJBBSA-N (1S,2R)-2-phenylcyclopropan-1-amine (1R,2S)-2-phenylcyclopropan-1-amine Chemical compound N[C@H]1C[C@@H]1C1=CC=CC=C1.N[C@@H]1C[C@H]1C1=CC=CC=C1 IGLYMJRIWWIQQE-QUOODJBBSA-N 0.000 claims abstract description 4
- RMUCZJUITONUFY-UHFFFAOYSA-N Phenelzine Chemical compound NNCCC1=CC=CC=C1 RMUCZJUITONUFY-UHFFFAOYSA-N 0.000 claims abstract description 4
- 229960000964 phenelzine Drugs 0.000 claims abstract description 4
- 229960003741 tranylcypromine Drugs 0.000 claims abstract description 4
- 229960003966 nicotinamide Drugs 0.000 claims abstract description 3
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims description 24
- 230000001430 anti-depressive effect Effects 0.000 claims description 8
- 210000004556 brain Anatomy 0.000 claims description 6
- 239000003826 tablet Substances 0.000 claims description 5
- 206010005003 Bladder cancer Diseases 0.000 claims description 4
- 102000010909 Monoamine Oxidase Human genes 0.000 claims description 4
- 108010062431 Monoamine oxidase Proteins 0.000 claims description 4
- 206010028813 Nausea Diseases 0.000 claims description 4
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 4
- 150000001413 amino acids Chemical class 0.000 claims description 4
- 238000006243 chemical reaction Methods 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 230000008693 nausea Effects 0.000 claims description 4
- 239000002858 neurotransmitter agent Substances 0.000 claims description 4
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 4
- 229940088594 vitamin Drugs 0.000 claims description 4
- 229930003231 vitamin Natural products 0.000 claims description 4
- 235000013343 vitamin Nutrition 0.000 claims description 4
- 239000011782 vitamin Substances 0.000 claims description 4
- 239000002775 capsule Substances 0.000 claims description 3
- 239000008187 granular material Substances 0.000 claims description 3
- 239000006188 syrup Substances 0.000 claims description 3
- 235000020357 syrup Nutrition 0.000 claims description 3
- 208000020401 Depressive disease Diseases 0.000 claims description 2
- 102000004190 Enzymes Human genes 0.000 claims description 2
- 108090000790 Enzymes Proteins 0.000 claims description 2
- 150000001408 amides Chemical class 0.000 claims description 2
- 230000015556 catabolic process Effects 0.000 claims description 2
- 230000003247 decreasing effect Effects 0.000 claims description 2
- 230000007812 deficiency Effects 0.000 claims description 2
- 230000000994 depressogenic effect Effects 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 238000012423 maintenance Methods 0.000 claims description 2
- 201000003102 mental depression Diseases 0.000 claims description 2
- 230000036651 mood Effects 0.000 claims description 2
- 235000001968 nicotinic acid Nutrition 0.000 claims description 2
- 239000011664 nicotinic acid Substances 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims description 2
- 239000002243 precursor Substances 0.000 claims description 2
- 102000004169 proteins and genes Human genes 0.000 claims description 2
- 108090000623 proteins and genes Proteins 0.000 claims description 2
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Pharmaceutical compositions for use as antidepressants, comprise L- tryptophan and a monoamine oxidase inhibitor e.g. phenelzine or tranylcypromine the L-tryptophan and monoamine oxidase inhibitor being present at the ratio of not more than 1.5 g of L-tryptophan per daily dose of the monoamine oxidase inhibitor. The compositions may also contain folic acid, ascorbic acid, pyridoxine, thiamine, riboflavin, nicotinic acid or nicotinamide.
Description
SPECIFICATION
Pharmaceutical compositions
This invention relates to pharmaceutical compositions. In particular the invention relates to pharmaceutical compositions comprising Ltryptophan and a monoamine oxidase inhibitor.
L-tryptophan is a naturally occurring amino acid which is present in most foodstuffs containing protein. It is well known to administer Ltryptophan to patients as an antidepressant.
When L-tryptophan is administered in this way as an antidepressant it is usually administered in the form of tablets or powders in a dosage of 1 to 2 g three times a day i.e. at a daily dosage rate of 3 te 6 g. However there can be side effects, such as nausea, associated with the administration of Ltryptophan at such dosages. Also it has been postulated that the likelihood of bladder cancer may be increased by the administration of Ltryptophan at such doses.
L-tryptophan is a precursor of the important neurotransmitter 5-hydroxytryptamine to which it is converted in the brain. 5-hydroxytryptamine is generally considered to be essential for the normal maintenance of mood and it is postulated that a relative deficiency of this neurotransmitter may be one of the important causes of mental depression. L-tryptophan is often administered together with vitamins, e.g. folic acid, ascorbic acid, pyridoxine, thiamine, riboflavin and nicotinic acid or its amide, thought to increase its conversion to 5-hydroxytryptamine.
Monoamine oxidase inhibitors are also known antidepressants and have been used as such for many years. They act by inhibiting the enzyme monoamine oxidase, which enzyme is normally associated with breakdown of monoamines, including 5-hydroxytryptamine. Thus, when administered in appropriate doses, monoamine oxidase inhibitors inhibit monoamine oxidase to the extent that the brain concentration of monoamines, in particular of 5-hydroxytryptamine, will increase. Examples of known monoamine oxidase inhibitors are phenelzine and tranylcypromine though many other compounds have the same action.
According to the present invention there is provided a pharmaceutical composition which composition comprises L-tryptophan and a
monoamine oxidase inhibitor, the L-typtophan and monoamine oxidase inhibitor being present in the composition at the ratio of not more than 1.5 g of L-tryptophan per daily dose of the monoamine oxidase inhibitor.
I have found that the composition according to the present invention, which contains Ltryptophan at a substantially reduced dose compared with that conventionally used combined with a monoamine oxidase inhibitor at the normal dosage is a very effective antidepressant. The antidepressant action of the composition according to the present invention is greater than that of either compound given alone in their usual dosage. Also a wider range of depressed patients has been found to respond to this treatment than with either component alone. Moreover, because of the lower L-tryptophan intake associated with the use of the composition according to the present invention the side effects of L-tryptophan such as nausea are reduced and the likelihood of producing bladder cancer is decreased.
The daily dose of the monoamine oxidase inhibitor is of course that of accepted medical practice and will vary from monoamine oxidase inhibitor to monoamine oxidase inhibitor.
Rather than being administered once during the day, the compositions according to the present invention will generally be for taking twice or three times a day. This means that the compositions will contain one half or one third of the daily dose of the monoamine oxidase inhibitor and suitably about 0.5 g of L-tryptophan. Thus the total dose of L-tryptophan with the compositions according to the present invention will generally be 1 to 1.5 9 per day.
The compositions according to the present invention may if desired contain vitamins conventionally used for increasing the conversion of L-tryptophan to 5-hydroxytryptamine.
The compositions according to the present invention may be in any conventional form, for example in the form of tablets, capsules or granules in which case the compositions generally also contain an inert, physiologically acceptable, carrier in conventional manner. In addition the compositions according to the present invention may be syrups.
It should be appreciated that it is important that small doses of L-tryptophan are used according to the present invention (i.e. not more than 1.5 g daily). Higher doses of L-tryptophan would competitively inhibit the transport of other important amino acids to the brain.
Claims
1. A pharmaceutical composition which composition comprises L-tryptophan and a monoamine oxidase inhibitor, the L-tryptophan and monoamine oxidase inhibitor being present at the ratio of not more than 1.5 g of L-tryptophan per daily dose of the monoamine oxidase inhibitor.
2. A composition according to claim 1 wherein the L-tryptophan and monoamine oxidase inhibitor are present at the ratio of 1 to 1.5 g of Ltryptophan per daily dose of the monoamine oxidase inhibitor.
3. A composition according to claim 1 or claim 2 which also contains folic acid, ascorbic acid, pyridoxine, thiamine, riboflavin, nicotinic acid or nicotinamide.
**WARNING** end of DESC field may overlap start of CLMS **.
Claims (5)
1. A pharmaceutical composition which composition comprises L-tryptophan and a monoamine oxidase inhibitor, the L-tryptophan and monoamine oxidase inhibitor being present at the ratio of not more than 1.5 g of L-tryptophan per daily dose of the monoamine oxidase inhibitor.
2. A composition according to claim 1 wherein the L-tryptophan and monoamine oxidase inhibitor are present at the ratio of 1 to 1.5 g of Ltryptophan per daily dose of the monoamine oxidase inhibitor.
3. A composition according to claim 1 or claim 2 which also contains folic acid, ascorbic acid, pyridoxine, thiamine, riboflavin, nicotinic acid or nicotinamide.
4. A composition according to any one of claims 1 to 3 wherein the monoamine oxidase inhibitor is phenelzine or tranylcypromine.
5. A composition according to any one of the preceding claims which is in the form of tablets, capsules, or granules or in the form of a syrup.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB08231975A GB2129299A (en) | 1982-11-09 | 1982-11-09 | Pharmaceutical compositions |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB08231975A GB2129299A (en) | 1982-11-09 | 1982-11-09 | Pharmaceutical compositions |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| GB2129299A true GB2129299A (en) | 1984-05-16 |
Family
ID=10534141
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB08231975A Withdrawn GB2129299A (en) | 1982-11-09 | 1982-11-09 | Pharmaceutical compositions |
Country Status (1)
| Country | Link |
|---|---|
| GB (1) | GB2129299A (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1987001590A1 (en) * | 1985-09-20 | 1987-03-26 | Stephen Neil Kreitzman | A composition and pack for use in the treatment of obesity |
| WO1989003692A1 (en) * | 1987-10-22 | 1989-05-05 | Massachusetts Institute Of Technology | Treating premenstrual or late luteal phase syndrome |
| US4971998A (en) * | 1987-10-22 | 1990-11-20 | Massachusetts Institute Of Technology | Methods for treating the premenstrual or late luteal phase syndrome |
| US5223540A (en) * | 1987-10-22 | 1993-06-29 | Massachusetts Institute Of Technology | Method for treating the premenstrual or late luteal phase syndrome |
| JP2997280B2 (en) | 1988-10-26 | 2000-01-11 | マサチユセツツ・インスチチユート・オブ・テクノロジー | Composition for treating tobacco withdrawal symptoms |
| US6096737A (en) * | 1994-10-05 | 2000-08-01 | Loder; Cari | Treatment of multiple sclerosis (MS) and other demyelinating conditions using lofepramine in combination with L-phenylalanine, tyrosine or tryptophan and possibly a vitamin B12 compound |
-
1982
- 1982-11-09 GB GB08231975A patent/GB2129299A/en not_active Withdrawn
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1987001590A1 (en) * | 1985-09-20 | 1987-03-26 | Stephen Neil Kreitzman | A composition and pack for use in the treatment of obesity |
| WO1989003692A1 (en) * | 1987-10-22 | 1989-05-05 | Massachusetts Institute Of Technology | Treating premenstrual or late luteal phase syndrome |
| US4971998A (en) * | 1987-10-22 | 1990-11-20 | Massachusetts Institute Of Technology | Methods for treating the premenstrual or late luteal phase syndrome |
| JPH03500884A (en) * | 1987-10-22 | 1991-02-28 | マサチユセツツ・インスチチユート・オブ・テクノロジー | Treatment of premenstrual or late luteal phase syndrome |
| US5223540A (en) * | 1987-10-22 | 1993-06-29 | Massachusetts Institute Of Technology | Method for treating the premenstrual or late luteal phase syndrome |
| JP2997280B2 (en) | 1988-10-26 | 2000-01-11 | マサチユセツツ・インスチチユート・オブ・テクノロジー | Composition for treating tobacco withdrawal symptoms |
| US6096737A (en) * | 1994-10-05 | 2000-08-01 | Loder; Cari | Treatment of multiple sclerosis (MS) and other demyelinating conditions using lofepramine in combination with L-phenylalanine, tyrosine or tryptophan and possibly a vitamin B12 compound |
| US6569850B1 (en) | 1994-10-05 | 2003-05-27 | Cari Loder | Treatment of multiple sclerosis (MS) and other demyelinating conditions using lofepramine in combination with L-phenylalanine, tyrosine or tyrptophan and possibly a vitamin B12 compound |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| WAP | Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1) |