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PubMed1979

[Infectious toxic hypotension--effect and dosage of midodrine (author's transl)].

A new alpha-sympathicomimetic drug with peroral effect is midodrine. The effective oral dosage in infancy and childhood is 0.06 mg/kg/dosi. The therapeutic effect, comparing the drug with etilefrin is shown in 120 children with pneumonia, enteritis, meningitis in a random study. The results give an increase in blood pressure and a decrease in heart frequency, statistically proved, on the first day of treatment. Therefore it seems that midodrine is qualified for the treatment of hypotension in infectious diseases.

Bacterial Infections↗
PubMed1995

Observations on midodrine in a case of vasodepressor neurogenic syncope.

A 43-year-old man presented with recurrent syncope and dizziness after he had a dual chamber pacemaker fitted for presumed sino-atrial disease. Head-up tilt produced vasodepressor neurocardiogenic syncope, despite appropriate heart rate support during pacing, and reproduced symptoms. Symptoms were not improved by disopyramide. A double-blind cross-over trial of midodrine, an alpha-receptor agonist, was effective in reducing symptoms: it abolished syncope and reduced frequency and severity of dizziness, coupled with improved haemodynamic responses to head-up tilt.

Adrenergic alpha-Agonists↗
PubMedDate not supplied

The in vitro metabolism of desglymidodrine, an active metabolite of prodrug midodrine by human liver microsomes.

The human cytochrome P450 (CYP) isoforms catalyzing the oxidation metabolism of desglymidodrine (DMAE), an active metabolite of midodrine, were studied. Recombinant human CYP2D6, 1A2 and 2C19 exhibited appreciable catalytic activity with respect to the 5'-O-demethylation of DMAE. The O-demethylase activity by the recombinant CYP2D6 was much higher than that of other CYP isoforms. Quinidine (a selective inhibitor of CYP2D6) inhibited the O-demethylation of DMAE in pooled human microsomes by 86%, while selective inhibitors for other forms of CYP did not show any appreciable effect. Although the activity of CYP2D6 was almost negligible in the PM microsomes, the O-demethylase activity of DMAE was found to be maintained by about 25% of the pooled microsomes. Furafylline (a selective inhibitor of CYP1A2) inhibited the M-2 formation in the PM microsomes by 57%. The treatment of pooled microsomes with an antibody against CYP2D6 inhibited the formation of M-2 by about 75%, whereas that of the PM microsomes did not show drastic inhibition. In contrast, the antibody against CYP1A2 suppressed the activity by 40 to 50% in the PM microsomes. These findings suggest that CYP2D6 have the highest catalytic activity of DMAE 5'-O-demethylation in human liver microsomes, followed by CYP1A2 to a small extent.

Animals↗
PubMed1998

Human alpha1-glycoprotein acid as chiral selector in the enantioseparation of midodrine and deglymidodrine racemates by HPLC.

Human alpha1-acid glycoprotein (alpha1-AGP) has been used as a chiral stationary phase (CSP) for the enantioseparation of midodrine and deglymidodrine racemates in the same HPLC run. The imobilized AGP resulted as the best chiral selector for the enantioresolution of two compounds. Due to the modification of alpha1-AGP characters as a result of changing the composition of the mobile phase, an attempt study of the watery mobile phase (ionic strength and pH of the buffer, nature and concentration of the organic modifier) allowed for an increase in the enantioselectivity of the chromatographic system and an optimization of the resolution base-line of both enantiomeric pairs.

Chemistry Techniques, Analytical↗
PubMed2002

N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.

N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1) is a novel alpha(1) agent having the unique profile of alpha(1A) (rabbit urethra, EC(50) = 0.60 microM) agonism with alpha(1B) (rat spleen, pA(2) = 5.4) and alpha(1D) (rat aorta, pA(2) = 6.2) antagonism. An in vivo dog model showed 1 to be more selective for the urethra over the vasculature than A-61603 (2), ST-1059 (3, the active metabolite of midodrine), and phenylpropanolamine (4).

Adrenergic alpha-Agonists↗
PubMed1982

Partial ejaculatory incompetence: the therapeutic effect of midodrine, an orally active selective alpha-adrenoceptor agonist.

The syndrome of partial ejaculatory incompetence has been reviewed. 6 patients, diagnosed as suffering from partial ejaculatory incompetence, were studied. For each subject, large numbers of spermatozoa were present in the post-masturbation urine sample providing evidence of disturbed ejaculatory function. The effect of a potent alpha-adrenoceptor agonist (Midodrine) was evaluated in these patients by means of a double-blind crossover study. Active treatment resulted in a significant increase in intensity of orgasmic sensation, and in a statistically significant improvement in ejaculatory function.

Adult↗
PubMed1992

A case of vasovagal syncope with convulsions--the effects of midodrine hydrochloride.

A 42-year-old female had suffered from repeated syncope. She had vasovagal syncope with convulsions from vasodilatation and cardiac standstill which lasted for 9.8 sec. The 60 degrees head-up tilt test, nitroglycerin injection and isoproterenol infusion provoked vasovagal reaction. Although a beta blocker was not effective in preventing tilt-induced hypotension and bradycardia, midodrine hydrochloride (alpha-1 stimulant) or atropine prevented it. In this patient, insufficient constriction of capacitance vessels might have played an important role in activation of an inhibitory reflex from cardiopulmonary mechanoreceptors which caused hypotension and bradycardia.

Adult↗
PubMed2000

[Use of midodrine and frozen semen to treat semen transport disturbances. Report of 2 cases].

Retrograde ejaculation severely compromises male fertility. The use of sympathicomimetics for the treatment of this condition has poor results, except in patients with partial retrograde ejaculation, whose semen has a higher spermatozoa concentration. The semen of two patients with partial retrograde ejaculation was collected and frozen after the injection of a sympathicomimetic (Midodrine). The frozen/thawed samples were mixed with fresh semen recently ejaculated to obtain a minimal number of motile spermatozoa, and used for intrauterine insemination (> de 1 x 10(6) motile spermatozoa/ml). In both cases, pregnancies that developed satisfactorily, were obtained.

Adult↗
PubMed2004

[Successful midodrin treatment for vasovagal syncopes accompanied by asystole].

Vasovagal syncopes (WS) are fainting fits whose manifestations are systemic vasodilation and bradycardia. The development of WS is frequently accompanied by short-term cardiac arrest. Recent data show that implantation of a cardiac pacemaker fails to prevent the development of fainting fits in these patients. On the basis of the pathogenesis of WS, the use of alpha-adrenomimetic midodrine is justifiable. The presented case demonstrates the successful use of the agent in the treatment of vasovagal syncope accompanied by asystole.

Adrenergic alpha-Agonists↗
PubMed1986

Midodrine for female incontinence: a preliminary report.

Twenty-six women (aged 26 to 60) with stress incontinence underwent urodynamic investigation before and after oral administration of 5 mg of midodrine, a new adrenergic agent with alpha-stimulant activity. A significant increase in maximum urethral closing pressure combined with a nonsignificant increase in flow time and maximum flow was observed after treatment.

Adult↗
PubMed1981

[The use of midodrin in the treatment of the orthostatic syndrome (author's transl)].

Midodrin, a new alpha-mimetic drug, has been studied with respect to its therapeutic effectiveness in children suffering from orthostatic hypotension. The study was carried out as a double blind trial against placebo. A statistically significant improvement was found only in relation to the following symptoms: "tendency to collapse", "dizziness", "headache", "change of colour". Blood pressure- and ECG alterations within the framework of the Schellong orthostatic and functional test were not significantly different statistically. This might be due to the small number of patients examined, to a placebo-effect or perhaps due to the inconsistent findings inherent in this last test.

Child↗
PubMed1981

Midodrine. A new agent in the management of idiopathic orthostatic hypotension and Shy-Drager syndrome.

Five patients with idiopathic orthostatic hypotension, two of whom had central nervous system manifestations (Shy-Drager syndrome), were treated with midodrine, an investigational alpha-adrenergic agonist, in a dosage of 2.5 to 5 mg three times daily. Significant improvement was observed in the standing systolic and diastolic blood pressures at the end of 1 week of therapy in all patients and has been maintained for 10 to 15 months in all patients. No symptomatic side effects were noted. Supine systolic hypertension occurred in two patients and was treated with small doses of metoprolol.

Adult↗
PubMed1994

[Clinical effect of midodrine hydrochloride on the patients with urinary incontinence].

The effects of midodrine hydrochloride (Brand name: Metligine tablet 2 mg, Manufacturer: Taisho Pharmaceutical Co., Ltd.), alpha-1 adrenalin receptor agonist against urinary incontinence was examined on 5 female patients with stress urinary incontinence and 5 male urinary incontinent patients of various causes. Metligine was administered in the dose of 4 mg daily for 2 to 4 weeks. Eighty per cent of the stress incontinent patients showed improvement and five incontinent male also showed improvement of symptoms. No side effects were recognized.

Administration, Oral↗
PubMed1993

Midodrine, a new therapeutic agent: recent experience.

Midodrine, marketed as Gutron by Hafslund Nycomed, was given at a dose of 2.5 mg three times daily always half an hour after the main meal for a period of 84 days to 8 women in the age of 25.42 years--average 34.5 yrs--and BMI of 19.8. These women with a blood pressure value below 100/60 mmHg most of the time displayed signs of neuroticism but had no organic and neurologic lesion. Clinical internal examination, Jarmatz-de Marée test, ECG-supine, standing, Holter dynamic ECG, ergometry, arterial and venous plethysmography, Doppler distal pressures-supine, standing, clinical neurological examination, EEG, perfusion brain tomography-supine, standing, urine examination--chemically and microscopically--, blood count, Na, K, Cl, glucose, urea, creatinine, uric acid, bilirubin, gamma-GT, alk. phosphatase, LDH, ALT, AST, thrombocyte index and the count of desquamated endothelia in blood before and after the end of 84-days Gutron therapy were carried out. It was ascertained that: (1) Gutron had no side effects; the marked subjective improvement reported by all patients persisted for months after the end of therapy. (2) No changes in biochemical parameters, ECG, Holter ECG monitoring, pulse rate, Doppler index and EEG were found. (3) Gutron did not raise the tendency to platelet aggregation and had no toxic effect on the vascular endothelium as demonstrated by unchanged thrombocyte index and endothelaemia. (4) Gutron administration was associated with a significant rise in upright diastolic pressure, especially when standing for prolonged periods--Jarmatz-de Marée test.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗