GB2129299A - Pharmaceutical compositions - Google Patents

Pharmaceutical compositions Download PDF

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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
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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Withdrawn
Application number
GB08231975A
Inventor
Alec James Coppen
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Individual
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Individual
Priority date (The priority date 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 date listed.)
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Publication date
Application filed by Individual filed Critical Individual
Priority to GB08231975A priority Critical patent/GB2129299A/en
Publication of GB2129299A publication Critical patent/GB2129299A/en
Withdrawn legal-status Critical Current

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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

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)

**WARNING** start of CLMS field may overlap end of DESC **. 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.
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.
GB08231975A 1982-11-09 1982-11-09 Pharmaceutical compositions Withdrawn GB2129299A (en)

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

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GB08231975A Withdrawn GB2129299A (en) 1982-11-09 1982-11-09 Pharmaceutical compositions

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GB (1) GB2129299A (en)

Cited By (5)

* Cited by examiner, † Cited by third party
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
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

Cited By (8)

* Cited by examiner, † Cited by third party
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
JP2938463B2 (en) 1987-10-22 1999-08-23 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
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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