Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0012833 (dizziness)
 9,689 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Valsartan competitively and selectively inhibits the actions of angiotensin II at the AT1 receptor subtype which is responsible for most of the known effects of angiotensin II. In clinical trials in patients with mild to moderate essential hypertension valsartan was as effective as losartan, lisinopril, enalapril, amlodipine and hydrochlorothiazide. Addition of the latter reduced blood pressure in patients who did not respond sufficiently to valsartan monotherapy. Preliminary data also suggest valsartan may be effective in patients with severe essential hypertension. The drug was as effective as lisinopril as treatment for mild to moderate essential hypertension in patients with renal insufficiency and did not worsen renal function. Headache, dizziness and fatigue were the most common adverse events in placebo-controlled studies; the incidence of these adverse events was not significantly different between placebo and valsartan recipients. Compared with ACE inhibitors, valsartan was associated with a significantly lower incidence of dry cough. Thus, valsartan is an effective treatment for mild to moderate essential hypertension and may be particularly useful in patients who experience persistent cough during ACE inhibitor therapy.
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PMID:Valsartan. A review of its pharmacology and therapeutic use in essential hypertension. 925 84

A cross-sectional study involving 60 women from Sydney, Australia, and 99 women from Los Angeles, California (US), evaluated the impact of three different insertion regimens on the transient nausea associated with the contraceptive vaginal ring. The ring released 20 mcg of ethinyl estradiol and 1 mg of norethindrone acetate per day. 128 women completed the 6-month study, providing 831 woman-months of exposure. The one pregnancy recorded during the 6-month study occurred during the 7-day break between cycles 5 and 6. 53% of women experienced nausea in at least one cycle. No significant differences in side effects were noted based on insertion group: 1) early evening (5-7 p.m.); 2) late night (10 p.m. to midnight); and 3) early evening insertion, removal at bedtime, and reinsertion the next morning. In each insertion group, the incidence of nausea was greatly reduced (to 6-9%) in the second cycle of use. 9% of women experienced transient vomiting in the 24 hours after first insertion of a new ring. The remaining side effects--headache, dizziness, uterine cramps, breakthrough bleeding, weight gain, and expulsion--were rare and occurred with equal frequency in all three insertion groups. Women at both study sites expressed a high degree of satisfaction with the vaginal ring, primarily because of its convenience and effectiveness. Overnight soaking of the ring before first use has the potential to reduce the side effect of transient nausea, presumed attributable to the accumulation of ethinyl estradiol on the ring surface during storage.
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PMID:Effect of different insertion regimens on side effects with a combination contraceptive vaginal ring. 940 4

It is reported that medroxyprogesterone acetate (MPA) causes venous thrombosis as one of the side effects. A 49-year-old woman suffering from metastatic lung carcinoma from breast carcinoma was administered MPA 1200 mg/day for about four months. Thereafter she complained of dizziness about two weeks but the general practitioners could detect no abnormality on physical examinations and on brain CT X-ray findings. Six days later, she died suddenly at her home. Forensic autopsy findings revealed the marked superior sagital sinus thrombosis and the malignant lymphadenomatosis caused by metastatic lung carcinoma. As the patient had not disease or trauma causing dural sinus thrombosis except for the administration of MPA, we concluded that superior sagital sinus thrombosis was due to the medication of MPA. This case illustrates that forensic pathologist should consider the major side effect of some drugs like our case.
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PMID:[A case of dural sinus thrombosis during the medication of medroxyprogesterone acetate]. 954 61

Progesterone is the natural progestagen produced by the corpus luteum during the luteal phase. It is absorbed when administered orally, but is greater than 90% metabolized during the first hepatic pass. This greatly limits the efficacy of once-daily administration and also results in unphysiologically high levels of progesterone metabolites, particularly those reduced at the 5-a position. These metabolites can cause dizziness and drowsiness to the point of preventing the operation of a motor vehicle. Synthetic progestins, such as medroxyprogesterone acetate and norethindrone acetate (NETA), have been specifically designed to resist enzymatic degradation and remain active after oral administration. However, these compounds exert undesirable effects on the liver and often cause severe psychological side effects. The permeability of the skin does not allow for administration of progesterone in the quantities normally produced by the corpus luteum, i.e., up to 25 mg/day during the mid-luteal phase. To avoid this problem, synthetic progestins such as NETA have been administered transdermally. These compounds, though, just like synthetic estrogens administered non-orally, retain undesirable hepatic effects even when administered transdermally. Transvaginal administration of progesterone is a practical non-oral route available for administering progesterone. Early experience was gained with vaginal suppositories, which lack manufacturing controls. Recently, a new progesterone gel formulation has been designed for vaginal use. The clinical acceptability of this product has been enhanced by the bioadhesive characteristics of its polycarbophil-based gel, which conveys controlled and sustained-released properties. Investigations have shown that because of local direct vagina-to-uterus transport, which results in a preferential uterine uptake of progesterone, this formulation given in conjunction with physiological amounts of estradiol produces endometrial changes similar to those seen in the luteal phase, despite plasma progesterone levels that remain subphysiologic. Studies in infertility show that vaginal progesterone in this form allows secretory transformation of the endometrium and the development of pregnancy despite providing low systemic progesterone concentrations. Fewer side effects occur when used for hormone replacement than typically encountered with progestins and oral progesterone. Uses in patients with infertility and hypoestrogenism and secondary amenorrhea are reviewed.
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PMID:Uses of progesterone in clinical practice. 1033 67

The Atlas Study was set up to compare the efficacy and safety of low doses and high doses of ACE inhibition by lisinopril on the risk of death and hospitalization in chronic heart failure. Three thousand one hundred sixty-four patients with class II to IV heart failure and an ejection fraction below 30% were randomly assigned to double blind treatment with either low doses (2.5-5 mg/daily, n = 1596) or high doses (32.5-35 mg/daily, n = 1568) of the ACE inhibitor lisinopril for 39 to 58 months while background therapy for heart failure was continued. Patients in the high dose group had a non significant 8% lower risk of death (p = 0.128), but a significant 12% lower risk of death or hospitalizations for any reason (p = 0.002) and 24% fewer hospitalizations for heart failure (p = 0.002). Side-effects such as dizziness and renal insufficiency were more frequently encountered in the high dose group, but there was no difference between the two groups in terms of number of patients requiring discontinuation of study medication. These findings indicate that patients with heart failure should not, as too frequently is, be maintained on very low dose of an ACE inhibitor unless this is the only dose that can be tolerated. The patients are expected to benefit more if they receive higher doses close to those used in the large clinical trials which have demonstrated a reduction by ACE inhibition in morbidity and mortality in heart failure.
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PMID:[Clinical study of the month. The ATLAS study]. 1068 3

Angiotensin II receptor blockers (ARBs) represent a new class of effective and well tolerated orally active antihypertensive agents. Recent clinical trials have shown the added benefits of ARBs in hypertensive patients (reduction in left ventricular hypertrophy, improvement in diastolic function, decrease in ventricular arrhythmias, reduction in microalbuminuria, and improvement in renal function), and cardioprotective effect in patients with heart failure. Several large long-term studies are in progress to assess the beneficial effects of ARBs on cardiac hypertrophy, renal function, and cardiovascular and cerebrovascular morbidity and mortality in hypertensive patients with or without diabetes mellitus, and the value of these drugs in patients with heart disease and diabetic nephropathy. The ARBs specifically block the interaction of angiotensin II at the AT1 receptor, thereby relaxing smooth muscle, increasing salt and water excretion, reducing plasma volume, and decreasing cellular hypertrophy. These agents exert their blood pressure-lowering effect mainly by reducing peripheral vascular resistance usually without a rise in heart rate. Most of the commercially available ARBs control blood pressure for 24 h after once daily dosing. Sustained efficacy of blood pressure control, without any evidence of tachyphylaxis, has been demonstrated after long-term administration (3 years) of some of the ARBs. The efficacy of ARBs is similar to that of thiazide diuretics, beta-blockers, angiotensin-converting enzyme inhibitors or calcium channel blockers in patients with similar degree of hypertension. Higher daily doses, dietary salt restriction, and concomitant diuretic or ACE inhibitor administration amplify the antihypertensive effect of ARBs. The ARBs have a low incidence of adverse effects (headache, upper respiratory infection, back pain, muscle cramps, fatigue and dizziness), even in the elderly patients. After the approval of losartan, five other ARBs (candesartan cilexetil, eprosartan, irbesartan, telmisartan, and valsartan) and three combinations with hydrochlorothiazide (irbesartan, losartan and valsartan) have been approved as antihypertensive agents, and some 28 compounds are in various stages of development. The ARBs are non-peptide compounds with varied structures; some (candesartan, losartan, irbesartan, and valsartan) have a common tetrazolo-biphenyl structure. Except for irbesartan, all active ARBs have a carboxylic acid group. Candesartan cilexetil is a prodrug, while losartan has a metabolite (EXP3174) which is more active than the parent drug. No other metabolites of ARBs contribute significantly to the antihypertensive effect. The variation in the molecular structure of the ARBs results in differences in the binding affinity to the receptor and pharmacokinetic profiles. The differences observed in lipid solubility, absorption/distribution, plasma protein binding, bioavailability, biotransformation, plasma half-life, and systemic elimination influence the time of onset, duration of action, and efficacy of the ARBs. On the basis of the daily mg dose, the antihypertensive potency of the ARBs follows the sequence: candesartan cilexetil > telmisartan approximately = losartan > irbesartan approximately = valsartan > eprosartan. After oral administration, the ARBs are rapidly absorbed (time for peak plasma levels = 0.5-4 h) but they have a wide range of bioavailability (from a low of 13% for eprosartan to a high of 60-80% for irbesartan); food does not influence the bioavailability, except for valsartan (a reduction of 40-50%) and eprosartan (increase). A limited dose-peak plasma levels/areas under the plasma level-time curve proportionality is observed for some of the ARBs. Most of these drugs have high plasma protein binding (95-100%); irbesartan has the lowest binding among the group (90%). The steady-state volumes of distribution vary from a low of 9 L (candesartan) to a high of 500 L (telmisartan). (ABSTRACT TRUNCATE
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PMID:Clinical pharmacokinetics of angiotensin II (AT1) receptor blockers in hypertension. 1085 85

The authors present the results of clinical trail about treatment of arterial hypertension with ENAP (Enalapril) fo KRKA in centers of Bulgaria. Enalapril is ACE-inhibitor usually administered orally once daily, decreases blood pressure by lowering peripheral vascular resistance without increasing heart rate or output. In this clinical trail are given results about blood pressure, heart rate and biochemical indexes. The most frequent adverse events--headache, dizziness, orthostatic effects, abdominal pain e.t.s. occurring in less than 10%. More important side effects like dry persistent cough occurring in 8.6%. The results of clinical trail define high efficacy and good tolerability of ENAP in the treatment of arterial hypertension.
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PMID:[Enalapril-clinical experience in Bulgaria]. 1122 62

This study was designed to investigate the effect of delapril, an ACE inhibitor, and manidipine, a long action calcium antagonist, on persistent microalbuminuria in normotensive type 2 diabetic patients. Sixty type 2 diabetic patients were randomized to take delapril 30 mg/day or manidipine 10 mg/day for 48 weeks, in an open label design. Twenty eight of thirty subjects in the delapril group and twenty nine of thirty in the manidipine group completed the study. Urine albumin excretion as measured by the urinary albumin creatinine ratio decreased significantly in both groups (112.0+/-60.9 to 95.3+/-64.9 mg/g and 108.5+/-51.0 to 96.4+/-53.5 mg/g in the delapril and manidipine group respectively, p < 0.05, by paired t-test). Systolic and diastolic blood pressure were not significantly changed after treatment in the delapril group but significantly decreased in the manidipine group (130.9+/-7.1/80.2+/-6.1 to 127.2+/-7.1/78.0+/-5.3 mm/Hg, p < 0.05, by student's paired t-test). After 48 weeks of treatment, two patients in the delapril group and one patient in the manidipine group converted to normoalbuminuria (urinary albumin:creatinine ratio < 30 mg/g) and one patient in each group progressed to overt nephropathy (urinary albumin:creatinine ratio > 300 mg/g). There were no significant changes in fasting plasma glucose, HbA1c, serum fructosamine, creatinine, potassium and lipid profiles after 48 weeks of treatment in both groups. Two cases in the delapril group were withdrawn during the study because of an intolerable cough and one case in the manidipine group because of intolerable dizziness and headache. In conclusion, both delapril and manidipine are effective in the reduction of microalbuminuria in normotensive type 2 diabetic patients with persistent microalbuminuria.
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PMID:Effects on urinary albumin excretion and renal function changes by delapril and manidipine in normotensive type 2 diabetic patients with microalbuminuria. 1133 83

Ambulatory blood-pressure monitoring (ABPM) is accepted in the evaluation and management of hypertension. The use of ABPM in heart failure has received considerably less attention. Many patients with advanced heart failure experience disabling fatigue, orthostatic dizziness and symptoms of coronary and cerebrovascular insufficiency that may relate to periods of hypotension. These may be exacerbated by vasodilator drug therapy and may be difficult to evaluate by casual clinic recordings. ABPM in heart failure may help in the following: (i) evaluating time-dependent pharmacodynamic drug effects, such as peak and end-of-dose phenomena, tolerance and rebound; (ii) titrating ACE inhibitors and other drugs to highest-tolerated doses; and (iii) correlating circadian blood-pressure profiles with symptoms, quality of life, severity of heart failure, progression of ventricular and renal dysfunction, risks of stroke and myocardial infarction, and life expectancy. Devices for ABPM have been beset by problems of inaccuracy and unreliability. Standards for their manufacture and sale (including bench tests of accuracy against sphygmomanometry and intra-arterial recordings, and field tests of reliability) have been devised independently by several agencies, including the British Hypertension Society (BHS) and US Association for the Advancement of Medical Instrumentation (AAMI). A joint BHS/AAMI set of guidelines is in preparation. These guidelines emphasize the suitability of ABPM devices for hypertensive patients and those under general anesthesia, and may not be applicable to ambulant individuals with heart failure and blood pressures at or below the lower end of the evaluated ranges. Prospective studies of the accuracy and reliability of ABPM devices, their clinical utility and research potential should be undertaken in patients with heart failure before their informal and uncontrolled use in this population becomes widespread.
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PMID:Ambulatory blood pressure in heart failure. 1152 34

Intracranial aneurysms (ICA) are a well-known feature of autosomal dominant polycystic kidney disease. There is only one report about ICA in an adult patient with autosomal recessive polycystic kidney disease (ARPKD). We observed a 2-year, 6-month old girl with ARPKD and multiple ICA. The family history is negative for kidney disease. The diagnosis of ARPKD was based on the typical findings in ultrasonography and computed tomography. Cystic ectasia of biliary ducts 6.3/4.8 cm in diameter was found in the liver. Arterial hypertension in a range of 140/100-170/120 mm Hg was registered. The child has polyuria, polydipsia and enuresis. Blood urea was 15 mmol/l, creatinine in a range of 120 to 75 micromol/l. One episode of vomiting, dizziness and lethargy was the reason for a brain magnetic resonance imaging. Multiple fusiform and saccular aneurysms in the branches of middle and posterior cerebral arteries were seen bilaterally. The girl is growing well without neurological symptoms during an observation period of 1.5 years. Blood pressure is well controlled with an ACE inhibitor (Enalapril 2.5 mg daily). It was concluded that ICA can be found in patients with ARPKD. Blood pressure control is essential to reduce the risk of intracranial hemorrhage.
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PMID:Intracranial aneurysms in a child with autosomal recessive polycystic kidney disease. 1179 94


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