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EP0154009A1 Expired / Lapsed EP ⏱️ 0.0 years remaining

Use of a thiazide diuretic for the manufacture of a non-diuretic antihypertensive medicament

Assignee: Euro Celtique SA
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Filing: 1984-12-07
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Granted: —
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Expires: 2004-12-07
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Abstract

Abstract Antihypertension action is achieved without diuresis by administration of a thiazide diuretic in an amount which while being sufficient to achieve anti hypertension is insufficient to achieve diuresis. Such administration in a non-diuretic amount is effected in 4-8 consecutive hourly doses to achieve reduction of blood pressure without high urine output. The invention further relates to complexes of thiazides with mixed cation-anion exchange resins, to insoluble basic metal hydroxy thiazide salts, the salts of thiazide with calcium disodium edetate or disodium edetate, to molecular complexes of thiazides with long chain polymers such as hydroxy alkyl cellulose polymers, carboxy methyl cellulose and polyvinylpyrrolidone, to beta-adrenergic blocking amine-thiazide salts and to amiloride thiazide salts.

Inventors

  • 👤 Ronald B. Miller
  • 👤 Stewart Thomas Leslie
  • 👤 Peter Hofer
  • 👤 Alfred Halpern

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-02 18:24
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/54; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; A61K47/585; A61K47/61; A61P; A61P7/00; A61P7/10; A61P9/00; A61P9/12

Claims Analysis

Total Claims: 53
Claim 1
Independent Claim 51 words
WHAT IS CLAIMED IS: 1. Method of effecting antihypertensive action without diureses which comprises administering to a patient requiring antihypertensive effect a pharmaceutically acceptable thiazide diuretic having a predetermined diuretic effective dose, the amount of said thiazide diuretic administered being sufficient to achieve antihypertension while being insufficient to achieve effective diuresis.
Claim 2
Dependent Claim 21 words
Method according to claim 1 wherein the amount of said thiazide diuretic administered is 7-25 % of the diuretic effective dose.
Claim 3
Dependent Claim 19 words
Method according to claim 1 wherein said thiazide is administered 4-8 times at hourly intervals 1-2 times per day.
Claim 4
Dependent Claim 19 words
Method according to claim 3 wherein the amount administered each time is 7-25 % of the diuretic effective dose.
Claim 5
Dependent Claim 28 words
Method according to claim 1 wherein said thiazide diuretic is selected from the group consisting of chlorothiazide, flumethiazide, benzthiazide, hydrochlorothiazide, hydroflumethiazide, bendroflumethiazide, polythiazide, methycyclothiazide, trichlormethiazide, cyclothiazide and cyclopenthiazide.
Claim 6
Dependent Claim 20 words
Method according to claim 5 wherein the amount of the thiazide administered is 7-25 % of the diuretic effective dose.
Claim 7
Dependent Claim 19 words
Method according to claim 5 wherein said thiazide is administered 4-8 times at hourly intervals 1-2 times per day.
Claim 8
Dependent Claim 19 words
Method according to claim 7 wherein the amount administered each time is 7-25 % of the diuretic effective dose.
Claim 9
Dependent Claim 32 words
9 . Complex of a pharmaceutically acceptable thiazide diuretic and a pharmaceutically acceptable mixed cation-anion exchange resin, said complex having improved adsorption in the gastrointestinal tract as compared to said thiazide diuretic.
Claim 10
Dependent Claim 27 words
Complex according to claim 9, the amount of said mixed cation-anion exchange resin being 1-2 parts by weight for each part by weight of said thiazide diuretic.
Claim 11
Dependent Claim 27 words
Complex according to claim 9, the amount of said mixed cation-anion exchange resin being 2 parts by weight for each part by weight of said thiazide diuretic.
Claim 12
Dependent Claim 28 words
Complex according to claim 9 wherein said thiazide diuretic is selected from the group consisting of chlorothiazide, flumethiazide, benzthiazide, hydrochlorothiazide, hydroflumethiazide, bendroflumethiazide, polythiazide, methycyclothiazide, trichlormethiazide, cyclothiazide and cyclopenthiazide.
Claim 13
Dependent Claim 27 words
Method of effecting diuretic action in a patient requiring the same, which comprises administering to such patient a diuretic effective dose of the complex of claim 9.
Claim 14
Dependent Claim 27 words
Method of effecting antihypertensive action in a patient requiring the same which comprises administering to such patient an antihypertensive effective dose of the complex of claim 9.
Claim 15
Dependent Claim 40 words
Method of effecting antihypertensive action without diuresis in a patient requiring the same which comprises administering to such patient the complex of claim 9 in a dose which is sufficient to achieve antihypertension while being insufficient to achieve effective diuresis.
Claim 16
Dependent Claim 17 words
Insoluble basic hydroxymetalthiazide salt of a pharmaceutically acceptable thiazide diuretic and a pharmaceutically acceptable metal hydroxyl compound.
Claim 17
Dependent Claim 12 words
Salt of claim 16 wherein said metal is aluminum, calcium or magnesium.
Claim 18
Dependent Claim 18 words
Diuretic composition comprising a pharmaceutically acceptable filler and a diuretic effective amount of the salt of claim 16.
Claim 19
Dependent Claim 18 words
Diuretic composition comprising a pharmaceutically acceptable filler and a diuretic effective amount of the salt of claim 17.
Claim 20
Dependent Claim 27 words
Method of effecting diuretic action in a patient requiring the same which comprises administering to such patient a diuretic effective amount of the salt of claim 16.
Claim 21
Dependent Claim 27 words
Method of effecting diuretic action in a patient requiring the same which comprises administering to such patient a diuretic effective amount of the salt of claim 17.
Claim 22
Dependent Claim 38 words
Method of effecting antihypertensive action without diuresis in a patient requiring the same which comprises administering to such patient the salt of claim 16 in an amount sufficient to achieve hypertension while being insufficient to achieve effective diuresis.
Claim 23
Dependent Claim 38 words
Method of effecting antihypertensive action without diuresis in a patient requiring the same which comprises administering to such patient the salt of claim 17 in an amount sufficient to achieve hypertension while being insufficient to achieve effective diuresis.
Claim 24
Dependent Claim 14 words
Salt of a pharmaceutically acceptable thiazide diuretic and calcium disodium edetate of disodium edetate.
Claim 25
Dependent Claim 28 words
Salt according to claim 24 wherein said thiazide diuretic is selected from the group consisting of chlorothiazide, flumethiazide, benzthiazide, hydrochlorothiazide, hydroflumethiazide, bendroflumethiazide, polythiazide, methycyclothiazide, trichlormethiazide, cyclothiazide and cyclopenthiazide.
Claim 26
Dependent Claim 27 words
Method of effecting diuretic action in a patient requiring the same which comprises administering to such patient a diuretic effective amount of the salt of claim 24.
Claim 27
Dependent Claim 27 words
Method of effecting antihypertensive action in a patient requiring the same which comprises administering to such patient an antihypertensive effective amount of the salt of claim 24.
Claim 28
Dependent Claim 35 words
Method of effecting antihypertensive action without diuresis, which comprises administering to a patient requiring the same the salt of claim 24 in an amount sufficient to achieve antihypertension while being insufficient to achieve effective diuresis.
Claim 29
Dependent Claim 24 words
Thiazide composition wherein the thiazide is protected in the gastrointestinal tract, said composition comprising a thiazide diuretic and calcium disodium edetate or disodium edetate.
Claim 30
Dependent Claim 27 words
Composition according to claim 29 wherein said thiazide is selected from the group consisting of chlorothiazide, flumethiazide, benzthiazide, hydrochlorothiazide, hydroflumethiazide, bendroflumethiazide, polythiazide, methycyclothiazide, trichlormethiazide, cyclothiazide, and cyclopenthiazide.
Claim 31
Dependent Claim 27 words
Method of effecting diuretic action in a patient requiring the same which comprises administering to such patient a diuretic effective amount of the composition of claim 29.
Claim 32
Dependent Claim 27 words
Method of effecting antihypertensive action in a patient requiring the same which comprises administering to such patient a diuretic effective amount of the composition of claim 29.
Claim 33
Dependent Claim 32 words
Method of effecting antihypertensive action without diuresis which comprises administering to a patient the composition of claim 29 in an amount sufficient to achieve antihypertension while being insufficient to achieve effective diuresis.
Claim 34
Dependent Claim 30 words
3 4. Molecular complex of a pharmaceutically acceptable thiazide diuretic and a long chain polymer selected from the group consisting of hydroxy alkyl cellulose polymers, carboxy methyl cellulose and polyvinylpyrrolidone.
Claim 35
Dependent Claim 28 words
Molecular complex according to claim 34 wherein said thiazide is selected from the group consisting of chlorothiazide, flumethiazide, benzthiazide, hydrochlorothiazide, hydroflumethiazide, bendroflumethiazide, polythiazide, methcyclothiazide, trichlormethiazide, cyclothiazide and cyclopenthiazide.
Claim 36
Dependent Claim 28 words
Method of effecting diuretic action in a patient requiring the same which comprises administering to such patient a diuretic effective amount of the molecular complex of claim 34.
Claim 37
Dependent Claim 27 words
Method of effecting antihypertensive action in a patient requiring the same which comprises administering to such patient an antihypertensive amount of the molecular complex of claim 34.
Claim 38
Dependent Claim 33 words
Method of effecting antihypertensive action without diuresis which comprises administering to a patient the molecular complex of claim 34 in an amount sufficient to achieve antihypertension while being insufficient to achieve effective diuresis.
Claim 39
Dependent Claim 27 words
Composition having augmented antihypertensive action, said composition comprising an antihypertensive effective amount of a pharmaceutically acceptable thiazide diuretic and an effective amount of a beta-adrenergic blocking amine.
Claim 40
Dependent Claim 28 words
Composition according to claim 39 wherein said thiazide diuretic is selected from the group consisting of clorothiazide, flumethiazide, benzthiazide, hydrochlorothiazide, hydroflumethiazide, bendroflumethiazide, polythiazide, methcyclothiazide, trichlormethiazide, cyclothiazide and cyclopenthiazide.
Claim 41
Dependent Claim 24 words
Composition according to claim 40 wherein said beta-adrenergic blocking amine is alprenolol, butidrine, butoxamine, dichlorisoproterenol, nifenalol, oxy- prenolol, practolol, pronethalol, propanolol, sotalol or toliprolol.
Claim 42
Dependent Claim 24 words
Composition according to claim 39 wherein said beta-adrenergic blocking amine is alprenolol, butidrine, butoxamine, dichlorisoproterenol, nifenalol, oxypreno- lol, practolol, pronethalol, propanolol, sotalol or toliprolol.
Claim 43
Dependent Claim 13 words
43 . Compound of a pharmaceutically acceptable thiazide and a beta-adrenergic blocking amine.
Claim 44
Dependent Claim 27 words
Compound according to claim 43 wherein said thiazide is selected from the group consisting of chlorothiazide, flumethiazide, benzthiazide, hydrochlorothiazide, hydroflumethiazide, bendroflumethiazide, polythiazide, methcyclothiazide, trichlormethiazide, cyclothiazide and cyclopenthiazide.
Claim 45
Dependent Claim 24 words
Compound according to claim 44 wherein said beta-adrenergic blocking amine is alprenolol, butidrine, butoxamine, dichlorisoproterenol, nifenalol, oxypreno- lol, practolol, pronethalol, propanolol, sotalol or toliprolol.
Claim 46
Dependent Claim 36 words
Method of effecting antihypertensive action without diuresis which comprises administering to a patient requiring such action the composition of claim 39 in an amount sufficient to effect antihypertensive action while being insufficient to achieve effective diuresis.
Claim 47
Dependent Claim 36 words
Method of effecting antihypertensive action without diuresis which comprises administering to a patient requiring such action the composition of claim 41 in an amount sufficient to effect antihypertensive action while being insufficient to achieve effective diuresis.
Claim 48
Dependent Claim 36 words
Method of effecting antihypertensive action without diuresis which comprises administering to a patient requiring such action the composition of claim 42 in an amount sufficient to effect antihypertensive action while being insufficient to achieve effective diuresis.
Claim 49
Dependent Claim 36 words
Method of effecting antihypertensive action without diuresis which comprises administering to a patient requiring such action the composition of claim 44 in an amount sufficient to effect antihypertensive action while being insufficient to achieve effective diuresis.
Claim 50
Dependent Claim 9 words
Salt of amiloride and a pharmaceutically acceptable thiazide diuretic.
Claim 51
Dependent Claim 27 words
Salt according to claim 50 wherein said thiazide is selected from the group consisting of chlorothiazide, flumethiazide, benzthiazide, hydrochlorothiazide, hydroflumethiazide, bendroflumethiazide, polythiazide, methcyclothiazide, trichlormethiazide, cyclothiazide and cyclopenthiazide.
Claim 52
Dependent Claim 36 words
Method of effecting antihypertensive action without diuresis which comprises administering to a patient requiring such action the salt of claim 50 in an amount sufficient to effect antihypertensive action while being insufficient to achieve effective diuresis.
Claim 53
Dependent Claim 36 words
Method of effecting antihypertensive action without diuresis which comprises administering to a patient requiring such action the salt of claim 51 in an amount sufficient to effect antihypertensive action while being insufficient to achieve effective diuresis.

References Cited (Backward Citations)

GB906399A Cited
GB1495034A Cited
GB1525296A Cited
GB1509778A Cited
GB1584089A Cited
GB2010675A Cited
DE3027392A1 Cited

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