Lipid Lowering Drugs and Hyperlipidaemia

Levy, Robert I.; Rifkind, Basil M.

doi:10.2165/00003495-197306010-00003

Cited by 23 publications

(4 citation statements)

References 50 publications

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“…Administration of a hypolipidaemic drug should be considered, if the appropriate dietary regimen alone does not reduce plasma lipid levels satisfactorily, if the patient does not observe the diet restrictions, or if severity of the disease and imminent complications make adjunctive drug therapy advisable (Levy and Rifkind, 1973). Since the benefit of lowering plasma lipids by hypolipidaemic drugs is not proven without doubt -for reasons descFibed-above, the decision to treat hyperlipidaemic patients by a drug must be carefully weighed and all individual factors of disease and patient must be taken into account, because all drugs concerned have a number of potential side effects and may be even considered dangerous for specific patient populations (The Coronary Drug Project, 1972;Stamler, 1975).…”

Section: Since Hypo/ipidaemic Drugs Are Widely Used Despite the Stilmentioning

confidence: 99%

“…Since the benefit of lowering plasma lipids by hypolipidaemic drugs is not proven without doubt -for reasons descFibed-above, the decision to treat hyperlipidaemic patients by a drug must be carefully weighed and all individual factors of disease and patient must be taken into account, because all drugs concerned have a number of potential side effects and may be even considered dangerous for specific patient populations (The Coronary Drug Project, 1972;Stamler, 1975). The commonly used hypolipidaemic drugs, their effect on lipoprotein metabolism, and their use in the various types of hyperlipoproteinaemia is shown in table I (Levy et ai., 1974;Levy and Rifkind, 1973;Sloman, 1976).…”

Section: Since Hypo/ipidaemic Drugs Are Widely Used Despite the Stilmentioning

confidence: 99%

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Clinical Pharmacokinetics of Hypolipidaemic Drugs

Gugler

1978

Clinical Pharmacokinetics

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Since hypo/ipidaemic drugs are widely used, despite the still unanswered question whether lowering of plasma lipids has a protective effect on the development of atherosclerosis, discussion of the clinical pharmacokinetics of the main representatives of this group of drugs is warranted.Clofibrate is quantitatively transformed to its active metabolite, chlorophenoxyisobutyric acid (CPlB), immediately after oral administration. Absorption of CPlB is complete, but relatively slow with peak concentrations being attained 2 to 6 hours after the dose. The apparent volume of distribution is between 6 and 12 litres; plasma protein binding is higher than 90 % • but is reduced in the nephrotic syndrome. in renal failure. and in cirrhosis. The elimination half-life ofCPlB ranges between 10 and 25 hours, is shorter in patients with the nephrotic syndrome, but is prolonged in renal failure ill close c:urrelation with the degree of renal impairment. The plasma clearance of the total drug (mean of 7ml/min) appears to be increased in the nephrotic syndrome. but is decreased in renal failure and is unchanged in liver cirrhosis. Clearance of the unbound drug (mean of 240ml/ min) is markedly reduced in renal failure, but is also reduced in liver cirrhosis. No pharmacokinetic changes are observed in acute hepatitis. Urinary excretion of CPlB is normally 10 to 15 % of the dose; excretion is reduced in .renal failure, but is unaffected in the nephrotic syndrome and in liver cirrhosis.Nicotinic acid is rapidly absorbed with peak concentrations being attained after 45 minutes.The systemic availability is about 90 % . Accumulation of the drug is reported in red blood cells.but no information is available on its distribution and on its plasma protein binding. The plasma elimination half-life is about 45 minutes. One third of an oral dose is excreted in urine unchanged. With pharmacological doses the major metabolite is nicotinuric acid; other metabolites being N-methyl-nicotinamide, 2-pyridone.and 4-pyridone, respectively. A measurable pharmacological effect is achieved with plasma concentrations of 0.1 to 0.2pg/ml, while a therapeutic range of 0.5 to 1.0Jlg/ml is suggested. Flushing of the skin is reported to-occur only at the beginning of treatment when the plasma concentration of nicotinic acid increases. Several analogues of nicotinic acid have been developed with the intention of achieving a sustained effect by a gradual in vivo liberation of nicotinic acid. . Cholestyramine is not absorbed from the gastrointestinal tract. As it is an anion exchange resin it may interfere with the absorption of a number of drugs by binding them to the resin.~-Sitosterol absorption is normally less than 5 %. but has been 25% in 2 sisters. so that a genetically determined influence on absorption is assumed.

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Section: Since Hypo/ipidaemic Drugs Are Widely Used Despite the Stilmentioning

confidence: 99%

Section: Since Hypo/ipidaemic Drugs Are Widely Used Despite the Stilmentioning

confidence: 99%

Clinical Pharmacokinetics of Hypolipidaemic Drugs

Gugler

1978

Clinical Pharmacokinetics

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“…Only 14% of the patients had definitely treat able hypertension (HT) with a diastolic blood pressure greater than 110 mm Fig, and though the prevalence of coronary heart disease (83%) appeared higher in this group than in those with lower blood pressure, the numbers were too small for significance to be established. 44% of patients gave a 2 Upper limits of desirable vs. treatable levels of diastolic blood pressure, fasting serum triglycerides and cholesterol were set arbitrarily from the data of the Veterans Administra tion Study Group [39], and groups from Stockholm, Sydney and Washington [40][41][42]. The 50 and 80 percentile fasting serum triglyceride values from the Stockholm study, for example, were 97 and 133 (females) and 118 and 164 mg/dl (males), aged 30-70 years [40].…”

Section: Evaluation O F Risk Factorsmentioning

confidence: 99%

Increased Prevalence of Coronary Heart Disease in Analgesic Nephropathy: Relation to Hypertension, Hypertriglyceridemia and Combined Hyperlipidemia

Kaladelfos¹,

Edwards²

1976

Nephron

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The prevalence of coronary heart disease (58%) in 43 patients with analgesic nephropathy with moderate to severe chronic renal failure was significantly higher than in the general population of the same age and sex. Mean serum triglyceride concentration and mean diastolic blood pressure were significantly higher in the group with coronary heart disease (214 mg/dl and 102 mm Hg, respectively) than in the group without it (162 and 94). Serum triglyceride values correlated inversely with GFR, indicating that hypertriglyceridemia was largely due to associated chronic renal failure; a specific effect of analgesic abuse on prevalence of heart disease, noted by others, could not be assessed in the absence of GFR-matched controls. The prevalence of coronary heart disease was significantly higher (81 %) in the group with combined hyperlipidemia (hypertriglyceridemia and hypercholesteremia) compared to the groups without it or with normal serum triglyceride concentrations (44 and 41%, respectively). Hypotryptophanemia (a possible cause of hyperlipidemia in the nephrotic syndrome) was present in 77% of patients.

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“…30,31 In children or in patients with renal failure, cholestyramine can lead to hyperchloremic acidosis. 40 Colesevelam therapy is considered to have fewer gastrointestinal complaints; however, common side effects reported with colesevelam therapy are constipation and dyspepsia. 32,33…”

Section: Aesmentioning

confidence: 99%