IE83776B1 - Use of sertraline to treat post traumatic stress disorder - Google Patents
Use of sertraline to treat post traumatic stress disorder Download PDFInfo
- Publication number
- IE83776B1 IE83776B1 IE2002/0411A IE20020411A IE83776B1 IE 83776 B1 IE83776 B1 IE 83776B1 IE 2002/0411 A IE2002/0411 A IE 2002/0411A IE 20020411 A IE20020411 A IE 20020411A IE 83776 B1 IE83776 B1 IE 83776B1
- Authority
- IE
- Ireland
- Prior art keywords
- sertraline
- traumatic stress
- stress disorder
- post traumatic
- disorder
- Prior art date
Links
- 201000008839 post-traumatic stress disease Diseases 0.000 title claims description 6
- 229960002073 Sertraline Drugs 0.000 title description 11
- VGKDLMBJGBXTGI-SJCJKPOMSA-N Sertraline Chemical compound C1([C@@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 VGKDLMBJGBXTGI-SJCJKPOMSA-N 0.000 title description 11
- 239000011780 sodium chloride Substances 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 11
- 201000010099 disease Diseases 0.000 claims description 8
- 150000001875 compounds Chemical class 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 3
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000003826 tablet Substances 0.000 description 5
- VTYYLEPIZMXCLO-UHFFFAOYSA-L calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 4
- 206010002855 Anxiety Diseases 0.000 description 3
- 206010057666 Anxiety disease Diseases 0.000 description 3
- 230000036506 anxiety Effects 0.000 description 3
- 239000007864 aqueous solution Substances 0.000 description 3
- 239000003085 diluting agent Substances 0.000 description 3
- 239000000945 filler Substances 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 239000007787 solid Substances 0.000 description 3
- BLFQGGGGFNSJKA-KELGLJHESA-N (1S,4R)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalen-1-amine;hydrochloride Chemical compound Cl.C1([C@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 BLFQGGGGFNSJKA-KELGLJHESA-N 0.000 description 2
- XJKJWTWGDGIQRH-BFIDDRIFSA-N Alginic acid Chemical compound O1[C@@H](C(O)=O)[C@@H](OC)[C@H](O)[C@H](O)[C@@H]1O[C@@H]1[C@@H](C(O)=O)O[C@@H](C)[C@@H](O)[C@H]1O XJKJWTWGDGIQRH-BFIDDRIFSA-N 0.000 description 2
- 229960003563 Calcium Carbonate Drugs 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N HCl Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 2
- 229960003660 Sertraline Hydrochloride Drugs 0.000 description 2
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K Trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 description 2
- 239000000783 alginic acid Substances 0.000 description 2
- 235000010443 alginic acid Nutrition 0.000 description 2
- 229920000615 alginic acid Polymers 0.000 description 2
- 229960001126 alginic acid Drugs 0.000 description 2
- 239000007900 aqueous suspension Substances 0.000 description 2
- 229910000019 calcium carbonate Inorganic materials 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 239000007903 gelatin capsule Substances 0.000 description 2
- -1 hydrochloric Chemical class 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 150000007522 mineralic acids Chemical class 0.000 description 2
- 230000003000 nontoxic Effects 0.000 description 2
- 231100000252 nontoxic Toxicity 0.000 description 2
- 150000007524 organic acids Chemical class 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 239000001509 sodium citrate Substances 0.000 description 2
- 239000008247 solid mixture Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000011778 trisodium citrate Substances 0.000 description 2
- RUFPHBVGCFYCNW-UHFFFAOYSA-N 1-Naphthylamine Chemical class C1=CC=C2C(N)=CC=CC2=C1 RUFPHBVGCFYCNW-UHFFFAOYSA-N 0.000 description 1
- YJISHJVIRFPGGN-UHFFFAOYSA-N 5-[5-[3,4-dihydroxy-6-(hydroxymethyl)-5-methoxyoxan-2-yl]oxy-6-[[3,4-dihydroxy-6-(hydroxymethyl)-5-methoxyoxan-2-yl]oxymethyl]-3,4-dihydroxyoxan-2-yl]oxy-6-(hydroxymethyl)-2-methyloxane-3,4-diol Chemical compound O1C(CO)C(OC)C(O)C(O)C1OCC1C(OC2C(C(O)C(OC)C(CO)O2)O)C(O)C(O)C(OC2C(OC(C)C(O)C2O)CO)O1 YJISHJVIRFPGGN-UHFFFAOYSA-N 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N D-Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N D-sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- RGHNJXZEOKUKBD-SQOUGZDYSA-N Gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 1
- 239000004705 High-molecular-weight polyethylene Substances 0.000 description 1
- GUBGYTABKSRVRQ-UUNJERMWSA-N Lactose Natural products O([C@@H]1[C@H](O)[C@H](O)[C@H](O)O[C@@H]1CO)[C@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1 GUBGYTABKSRVRQ-UUNJERMWSA-N 0.000 description 1
- 240000007472 Leucaena leucocephala Species 0.000 description 1
- 235000010643 Leucaena leucocephala Nutrition 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 241000985694 Polypodiopsida Species 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- 240000001016 Solanum tuberosum Species 0.000 description 1
- 235000002595 Solanum tuberosum Nutrition 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- CZMRCDWAGMRECN-GDQSFJPYSA-N Sucrose Natural products O([C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1)[C@@]1(CO)[C@H](O)[C@@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-GDQSFJPYSA-N 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H Tricalcium phosphate Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000001539 anorectic Effects 0.000 description 1
- 239000000935 antidepressant agent Substances 0.000 description 1
- 239000002830 appetite depressant Substances 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
- 229910000389 calcium phosphate Inorganic materials 0.000 description 1
- 235000011010 calcium phosphates Nutrition 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 150000002081 enamines Chemical class 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000007912 intraperitoneal administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 239000008203 oral pharmaceutical composition Substances 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 150000004760 silicates Chemical class 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N β-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
Description
Use of sertraline to treat/post traumatic stress disorder
This invention relates to a medicament for treating post traumatic
stress disorder, using the compound (1S-cis)(3,4-dichl0ro—
phenyl)— 1 ,2,3 ,4-tetrahydro—N-methy1-l-naphtha]enamine,
hereinafter referred to by its generic name
"sertraline"
. or a pharmaceutically acceptable salt
thereof.
Sertraline, which has the empirical formula
C12H17NCl2 and the structural. formula
HCH3
C1
C1
is a known antidepressant and anorectic agent.
United
States Patent 4,536,518
, assigned in common with the
present invention discloses sertraline and related compounds
of the formula
NRIRZ
W (C18)
3 I
wherein Z is
X
Y ,
and R1: R2:_ W: X and Y are as defined therein, and
States that such compounds exhibit.a.ntidepressant and
anorectic activity in vivo in" mammals.
The present medicament is used in a method of treating post traumatic
stress disorder, comprising administering to a patient in need of such
treatment an amount of sertraline, or a pharmaceutically acceptable salt
thereof, effective in preventing or alleviating the disorder and the symptoms
associated with such disorder.
Examples of pharmaceutically acceptable salts of sertraline
that can be used to treat the disorder in accordance with the
present invention are the acid addition salts of various mineral
and organic acids such as hydrochloric, hydrobromic, hydroiodide,
Sulfuric: Ph08Ph°riG; acetic, lactic, maleic, fumaric,
citric, tartaric, succinic, and gluconic.
Sertraline is therefore useful in the treatment and management of post
traumatic stress disorder. Other compounds of the formula 1 above may
be similarly effective.
Sertraline may be prepared as described in United
States Patent 4,536,518, and particularly, in Example 2
of that patent.
sertraliner Or a Pharmaceutically acceptable salt
‘thereof, when used to treat anxiety—related disorders,
may be administered either orally or parenterally. It
is generally administered in dosages ranging from
50—500 mg per day when used to treat obsessive-
compuleive disorder, and from 25-500 mg per day
when used to-treat other anxiety—related disorders,
although variations will necessarily occur depending
“Don the condition of the subject being treated and the
particular route of administration chosen. It may be
administered either alone or in combination with
pharmaceutically acceptable carriers by either of the
above routes, and Suchadministration can be carried out
in both Single and multiple dosages. More particu-
larly: Sertralinea or a pharmaceutically acceptable
salt thereof, may be administered in a wide variety of
different dosage forms, i.e., it may be combined with
various pharmaceutically acceptable inert carriers in
the form of tablets, capsules, lozenges, troches, hand
candies, powders. sprays, aqueous suspensions,
injectable solutions, elixirs, syrups, and the like.
Such carriers include solid diluents or fillers,
sterile aqueous media and various non-toxic organic
solvents, etc. Moreover, such oral pharmaceutical
formulations can be suitably sweetened and/or flavored
by means of various agents of the type commonly
employed for such purposes. In general, sertraline, or
a pharmaceutically_acceptable salt thereof, when used
to treat an anxiety-related disorder, is present in
such dosage ferns at concentration levels ranging from
0.5% to 90% by weight of the total
ccposition, i.s, in amounts that are sufficient to
provide the desired unit dosage. It may exist in
different polymorphic forms, i.e. different crystalline
forms. 7
For purposes of oral administration, tablets
containing various excipients such as sodium citrate,
calcium carbonate and calcium phosphate may be employed
along with various disintegrants such as starch,
preferably potato or tapioca starch, alginic acid and
certain complex silicates, together with binding agents
such as polyvinylpyrrolidone, sucrose, gelatin and
acacia. Additionally, lubricating agents such as
magnesium stearate, sodium lauryl sulfate and talc are
often very useful for tabletting purposes. Solid
compositions of a similar type may also be employed as
fillers in soft and hard-filled gelatin capsules:
preferred fillers would also include lactose or milk
sugar as well as high molecular weight polyethylene
glycols. When aqueous suspensions and/or e1iX8r8 are
— desired for oral administration, the sertraline, or
pharmaceutically acceptable salt thereof, may be
combined with various sweetening or flavoring agents,
coloring matter or dyes and, if so desired, emulsifYin9
and/or suspending agents, together with diluents such
as water, ethanol, propylene glycol, glycerin and
various like combinations thereof.
For purposes of parenteral administration,
solutions of sertralins, or a.pharmaceutically‘
acceptable salt thereof, in sesame or peanut oil or in
aqueous propylene glycol or N,N—dimethylformamide may
be employed, as well as sterile aqueous solutions of
the water-soluble, non-toxic mineral and organic acid
addition salts previously enumerated. Such aqueous
solutions should be suitably buffered it necessary and
the liquid diluent first rendered isotonic with
sufficient saline or glucose. These particular aqueous
solutions are especially suitable for intravenous,
intramuscular, subcutaneous and intraperitoneal~
injection purposes. In this connection, the sterile
aqueous media employed are all readily obtainable by
standard techniques well-known to those skilled in the
art. , u
A typical dry solid pharmaceutical composition is
prepared by blending the following materials together
in the proportions by weight specified below:
Cis-(ls)-N-methyl—4-(3,4-dichlorophenyl)—l,
2,3,4—tetrahydro-l—naphthalenamine hydrochloride: so
Sodium citrate: 25
Alginic acid: 10
Polyvinylpyrrolidone: 10
Magnesium stearate: 5
After the dried composition is thoroughly blended,
‘tablets are punched from the resulting mixture, each
tablet being of such size that it contains 100 mg of
sertraline hydrochloride. other tablets are also
prepared in a similar fashion containing 5, 10, 25, and
50 mg of sertraline hydrochloride respectively, by
using the appropriate amount of the naphthalenamine
salt in each case.
Another typical dry solid pharmaceutical composi-
tion is prepared by combining the following materials
together in the proportions by weight indicated below:
Cis—(lS)-N-methyl(3,4-dichlorophenyl)-1,
2,3,4-tetrahydronaphthalenamine hydrochloride: so
Calcium carbonate: 20
Polyethylene glycol, average molecular weight,
4000: 30
The dried solid mixture so prepared is then thoroughly
agitated so as to obtain a powdered product that is
completely uniform-in every respect. Soft elastic and
hard-filled gelatin capsules containing this
pharmaceutical composition are then prepared. employing
a sufficient gaantity of material in each instance so
as to provide each capsule with 50 mg of the active
ingredient.
Claims (2)
1. The use of the compound (1S-cis)—4—(3,4-dichIorophenyi)-1,2,3,4- tetrahydro—N—methylnaphthalenamine or a pharmaceuticaliy ’ acceptable salt thereof for the manufacture of a medicament to treat or prevent post traumatic stress disorder and the symptoms associated with such a disorder.
2. Use according to claim 1, substantially as hereinbefore described. ANNE RYAN & CO. AGENTS FOR THE APPLICANTS
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
USUNITEDSTATESOFAMERICA02/11/19894 |
Publications (1)
Publication Number | Publication Date |
---|---|
IE83776B1 true IE83776B1 (en) | 2005-01-26 |
Family
ID=
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