- Rosuvastatin Attenuates acute nephrotoxicity through modulation of oxidative stress in Sprague Dawley rats. [Journal Article]J Pak Med Assoc 2019; 69(Suppl 3)(8):S98-S102JP
- CONCLUSIONS: Rosuvastatin was found to be a reno-protective against gentamicin-induced nephrotoxicity through modulation of pro-inflammatory and oxidative/anti-oxidant pathways.
- Rosuvastatin-related rhabdomyolysis causing severe proximal paraparesis and acute kidney injury. [Journal Article]BMJ Case Rep 2019; 12(10)BC
- We describe the case of a 76-year-old man who presented with bilateral lower limb weakness associated with decreased urine output. His initial blood results showed acute kidney injury (AKI) stage 3 with substantially raised serum creatine kinase concentration of 37 950 IU/L (normal range <171 U/L). He had been on high-dose rosuvastatin for 4 years with a recent brand change occurring 1 week prior…
We describe the case of a 76-year-old man who presented with bilateral lower limb weakness associated with decreased urine output. His initial blood results showed acute kidney injury (AKI) stage 3 with substantially raised serum creatine kinase concentration of 37 950 IU/L (normal range <171 U/L). He had been on high-dose rosuvastatin for 4 years with a recent brand change occurring 1 week prior to onset of symptoms. There was no history of pre-existing neuromuscular disease. Statin-related rhabdomyolysis was suspected and rosuvastatin was withheld. His muscle strength gradually improved. He required haemodialysis for 10 weeks. He was discharged home after a complicated course of hospitalisation. His renal function improved and he became dialysis-independent; however, he was left with residual chronic kidney disease.
- In brief: Ezallor Sprinkle--a new formulation of rosuvastatin. [Journal Article]Med Lett Drugs Ther 2019; 61(1581):152ML
- Microdosing clinical study to clarify pharmacokinetic and pharmacogenetic characteristics of atorvastatin in Japanese hypercholesterolemic patients. [Journal Article]Drug Metab Pharmacokinet 2019DM
- The present study investigated whether the clinical pharmacokinetics of atorvastatin can be predicted from the results of microdosing study in Japanese patients with hypercholesterolemia whose SLCO1B1 and ABCG2 polymorphisms were analyzed. Forty seven statin-naive patients clinically indicated to LDL cholesterol-lowering therapy with atorvastatin were enrolled in a two-period crossover study. Mic…
The present study investigated whether the clinical pharmacokinetics of atorvastatin can be predicted from the results of microdosing study in Japanese patients with hypercholesterolemia whose SLCO1B1 and ABCG2 polymorphisms were analyzed. Forty seven statin-naive patients clinically indicated to LDL cholesterol-lowering therapy with atorvastatin were enrolled in a two-period crossover study. Microdose (100 μg) of atorvastatin was orally administered followed by therapeutic dose (10 mg) administration. Transport studies were performed with BCRP-expressing membrane vesicles. The dose-normalized plasma AUC following the therapeutic dose of atorvastatin was positively correlated with that following its microdose, but the AUC increased more than dose proportionally from microdose to therapeutic dose. The patients carrying SLCO1B1 c.521TC showed a significantly higher AUC compared with those carrying c.521TT following the microdose (175%) and therapeutic dose (139%). On the other hand, SLCO1B1 c.388G or ABCG2 c.421A variant alleles did not significantly affect the pharmacokinetics of atorvastatin. Atorvastatin showed ATP-dependent transport in BCRP-expressing membrane vesicles and it inhibited rosuvastatin transport with Ki of 6.3 ± 2.9 μM (mean ± SD). Microdosing study appears to be feasible to roughly estimate the pharmacokinetic and pharmacogenetic profiles of atorvastatin following the oral therapeutic dose in hypercholesterolemic patients.
- Clinically relevant drug interactions between statins and antidepressants. [Review]J Clin Pharm Ther 2019JC
- CONCLUSIONS: Pharmacodynamic (PD) drug-drug interactions (DDIs) are unlikely to occur as statins are highly selective inhibitors of HMG-CoA reductase with no relevant effect on other enzymes or receptor systems. Despite the numerous PK studies on individual drugs belonging to statins and antidepressant agents, only a few case reports regarding specific DDIs are present in the literature and no clinical studies have been performed. PK data allow to speculate on potential DDIs, comparing the metabolic pathways, intestinal and liver transporters and elimination routes. Overall, second-generation antidepressants, in particular citalopram, escitalopram, mirtazapine, reboxetine and venlafaxine, have weak inhibitory effects on various cytochrome (CYP) isozymes and seem to have a more advantageous DDIs profile in vivo. Conversely, nefazodone, fluoxetine, paroxetine and fluvoxamine influence considerably CYPs activity with potential effects on statins plasma levels, although pravastatin, pitavastatin and rosuvastatin are not susceptible to inhibition by any CYP. Albeit no studies have been performed on P-glycoprotein (P-gp), interactions of clinical relevance are unlikely.Although DDIs with antidepressants are potentially, but rarely clinically significant, the use of antidepressants with a more favourable drug interaction profile is advisable. An evaluation on DDIs between these drugs can be useful for future PK/PD studies on drug-drug interaction to provide clinicians with more data for appropriate multiple drug regimens.
- Physiologically Based Pharmacokinetic Modelling to Identify Pharmacokinetic Parameters Driving Drug Exposure Changes in the Elderly. [Journal Article]Clin Pharmacokinet 2019CP
- CONCLUSIONS: The progressive decrease in hepatic and renal blood flow, as well as glomerular filtration, rate led to a reduced clearance driving exposure changes in the healthy elderly, independent of the drug.
- Peripheral polyneuropathy in patients receiving long-term statin therapy. [Journal Article]Turk Kardiyol Dern Ars 2019; 47(7):554-563TK
- CONCLUSIONS: This study revealed an increased risk of peripheral neuropathy with long-term statin use (>1 year). Electrodiagnostic changes have been detected in motor and sensory nerves in nerve conduction studies of patients on long-term statin treatment. The assessment of neurological symptoms, like tingling, numbness, pain and tremor in the hands and feet, and unsteadiness during walking associated with peripheral neuropathy may be useful in the follow-up of the patients on long-term statin treatment. Early detection of peripheral neuropathy and changing hypercholesterolemia treatment may prevent permanent nerve damage.
- Rosuvastatin reduces expression of tissue factor through inhibiting RhoA/ROCK pathway to ameliorate atherosclerosis. [Journal Article]Panminerva Med 2019PM
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- REVERSIBLE NEUROTROPHIC KERATOPATHY ASSOCIATED WITH ROSUVASTATIN THERAPY: A CASE REPORT. [Journal Article]J Popul Ther Clin Pharmacol 2019; 26(2):e38-e42JP
- CONCLUSIONS: Rosuvastatin may result in reversible trigeminal nerve impairment and neurotrophic keratopathy.