DE2055813B2 - ORAL EFFECTIVE AGENT AGAINST HYPOTONIA - Google Patents

Description

Dose in blood pressure duration in minutes With the addition of 2 mg / kg AN 1

mg / kg i.V. Increase in mm / Hg Blood pressure increase Duration in minutes

in mm / Hg

1.0 0 0 10 20-30 40 - 60 5.0 20-30 5 - 40-60 140 - 160

Medical control attempts
Experimental set-up

20 patients aged 30 - 60 years with ortho- 55 The duration of the experiment was 14 days (= 2 weeks),

Static regulation disturbances were divided into 4 groups to objectify the success of the treatment

divided into 5 patients each: the blood pressure measurement carried out, since normalization a low blood pressure also one

Group A = placebo group normalization of orthostatic regulatory disturbances

Group B = treatment with coated tablets of 50 mg 60 mg.

Heptaminol hydrochloride The blood pressure was measured on 4 consecutive

Group C = treatment with coated tablets of 5 mg the following days before the start of the medication

«- Phenyl - α - (1 - methyl - 2 - phenyl month March 1972). From this the central

nyl) ethylaminoacetonitrile values determined. The medication was then carried out between

Group D = inventive combination of 65 see 8 and 9 o'clock in the morning in doses of 2 coated tablets each.

50 mg heptaminol hydrochloride and The blood pressure measurements were between 13 and

5 mg of a-phenyl-A-il-methyW-phe-2 p.m. The mean values obtained are

nyl) -äthylamino-acetonitrile listed in the table below:

Group blood pressure in now Hg before treatment. Blood pressure in now Hg after treatment

systolic diastolic systolic diastolic

A. 108.3 65.2 110.1 63.9 B. 110.5 66.4 114.2 65.3 C. 109.1 68.3 112.4 68.5 D. 108.7 66.5 123.8 66.3

The combination according to the invention thus showed an effect in 6-amino-2-methylheptanol- (2) hydrochloride Means a 108.7 rise in systolic blood pressure at 50 mg doses in non-hypertensive humans 123.8 mm Hg. This corresponds on average to an increase. But if 5 mg <x-phenyl - «- (l-methyl intake of 15.1 mm Hg. In contrast, the medi-2-phenyl) -äthylaminoacetonitril added, so one cation with the individual active ingredients alone dose that does not even have a performance-enhancing effect and (B and C) are practically ineffective in that they also have no blood pressure-increasing properties Dosage. The one through D is conspicuous, so a low blood pressure is increased and the given uniformity of increase in blood pressure. ao kept at the same level throughout the day without

Accordingly, the surprising, unexpected and that this blood pressure even with a higher dose in a

Unprecedented the invention that pathological increase in blood pressure passes.

So it is the essence of the invention, through addition

1. by combining a-phenyl-a- (l-methyl- or / and a combination of a-phenyl - * - (l-methyl-2-phenyl) ethylaminoacetonitrile) with the sym- 35 2-phenyl) -ethylamino-acetonitrile to 6-amino-2-mepathikomimetic Amine 6-amino-2-methylhep- thyl-heptanol- (2) a normalization of the lowered tanol- (2) -HCl a long-lasting normalization of blood pressure with a long and steady effect low blood pressure occurs. obtain.

2. to achieve such an effect only 10 to The low dose consequently also makes the new 60% practical and 50% of the normal individual drugs are less toxic and more digestible.

dose of the individual active ingredients are necessary
and that it is precisely at these doses that such an advantageous effect is given. example

From the results it can be seen that ₃₅ 6-amino-2-methylheptanol- (2) -

1. a, - Phenyl - α - (1 - methyl - 2 - phenyl) - ethylamine hydrochloride 50 mg

noacetonitril's antihypertensive effect

of the sympathomimetic amine convincingly «-Phenyl -« - (l-methyl-2-phenyl) -

able to increase, ethylamino-acetonitrile 5 mg

2. the only fleeting blood pressure-increasing effect of the 40th
6-amino-2-methyl-heptanol- (2) by a-phenyl-

«- (1 - methyl - 2 - phenyl) - ethylaminoacetonitrile Both ingredients are mixed and placed in capsules

is extended up to 20 times. filled.

Claims (1)

* J kings out? holds the same amount. This observation is Patent claim · surprisingly and so far in the same sense from none Substance or combination known. Means in the form of tablets, coated tablets or Demuach is the subject of the invention a means in Capsules against hypotension, characterized by 5 form of tablets, coated tablets or capsules against a content of a mixture of 10 parts by weight of hypotension, characterized by a content of 6-Amino-2-methylheptanol- (2) -hydrochloride and a mixture of 10 parts by weight of 6-amino-2-methyl-1 Part by weight of a-phenyl - "- (l-methyl-2-phenyl> ethyl-heptanol- (2) and 1 part by weight of" -phenyl - "- (l-methylamino-acetonitrile. 2-phenyl) -äthylaminoacetonitnl. ίο Even if the blood pressure-increasing effect of norephedrine, ephedrine and the like is _{favorably influenced by oc-phenyl a} - (l-niethyl-2-phenyl) -ethylaminoacetonitrile, these bodies have the disadvantage, as catechoiamine derivatives, that they are present in the organism It is known that only a few chemical substances are metabolized in mescaline bodies, so that they are non-punched undesired side effects arise if the oral route increases blood pressure effectively. That is with are. These include norephedrine, ephedrine, 6-amino-2-methyl-heptanol- (2) -hydrochloride not the 1- (4-Hydroxypbenyl) -2-methylaminoethanol, Hm-Hy- case. Accordingly, the appropriate Komdroxyphenyl) -2-äthylaminoäthanol turned out, m-Hydroxyphe- binination in all dates of use aJs am günnyl- (l) -ethanol- (l) -amine- (2) and 2-aminoheptanol. 20 th. It is known that the blood pressure increasing effect a - phenyl - χ - (1 - methyl - 2 - phenyl) - ethyl - ami- These compounds only last for a short time, even volatilely. It lasts after the peroral administration of the aforementioned pressure-increasing effect. It has a performance-enhancing substance the beneficial effect taken in relatively high doses, which is pharmacological like caffeine have to, hardly more than 3 hours. One had 25 logically similar. is already trying to reduce the blood pressure-increasing effect. A table should show the results of the blood pressure These sympathomimetics are led by various types of pressure increase. The blood pressure Preparation, such as retardation, addition of Kollidon was carried out on the cat under urethane chloralose anesthesia, etc., to extend. The results are modestly true. In the experiments, care was taken that and are by no means therapeutically satisfactory. 30 the initial pressure was between 80 and 100 mm Hg. The surprising observation has now been made. The experiments were once carried out with the known blood power, that a simultaneous administration of "-Phe- pressure-increasing body 6-amino-2-methylheptanyl-A- (l-methyl-2-phenyl) -ethylamino-acetonitrile, carried out with nol- (2) -HCl alone, then together with the blood pressure-increasing C-amino-2-methylhepta- & - phenyl - λ - (1 - methyl - λ - phenyl) - ethyl - aminonol- (2) -hydrochloride with a considerable amount of around 50% acetonitrile, which is given orally to the animals for 20 minutes each time lower dose than such a therapeutically prior to the beginning of the first-mentioned administered intravenously is written, does not only increase blood pressure, substance has been administered. Ask the results but also shows the same evenly, without Schwan, mean values from 5 tests each.