Lovastatin
Risk Factor: XM
Class: ANTILIPEMIC AGENTS
Contents of this page:
Fetal Risk Summary
Breast Feeding Summary
References
Questions and Answers
Fetal Risk Summary
Lovastatin, a 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, is used to lower elevated levels of cholesterol. The drug is teratogenic in mice and rats, producing decreased fetal weight and skeletal malformations in exposed fetuses, at doses of 800 mg/kg/day (40 and 80 times the recommended maximum human dose based on body surface area [MRHD], respectively) (1,2). No teratogenic effects were observed in rabbits administered doses up to 15 mg/kg/day (3 times the MRHD), the maximum tolerated dose (1,2).
A surveillance study of lovastatin exposures during pregnancy, conducted by the manufacturer, was reported in 1996 (2). Among 76 women, most taking the drug before conception and then discontinuing it sometime during the 1st trimester when pregnancy was diagnosed, 19 (25%) outcomes were unknown, 1 (1.3%) outcome was pending, and 8 (11%) were electively aborted. None of the products of conception from the elective abortions underwent morphologic and/or chromosomal evaluations (3). Of the 48 pregnancies with known outcomes, there were 3 (6.3%) spontaneous abortions, 1 (2.1%) stillbirth (cord wrapped around newborn's neck; mother took unknown dose throughout gestation), 1 (2.1%) case of foot edema (probably because of labor arrest requiring cesarean section; mother took 20 mg/day during first 5 weeks), 4 (8.3%) infants with congenital defects, and 39 (81.3%) normal outcomes (all exposed during all or a portion of the 1st trimester). The details of the infants with defects (all reported retrospectively) were (dose and exposure in weeks from last menstrual period): atrial, ventricular septal defect, cerebral dysfunction, infant died at 1 month of age (40 mg/day, 05 weeks); vertebral defect, anal atresia, tracheo-esophageal fistula with esophageal atresia (VATER association), mother also took dextroamphetamine at same time (10 mg/day, 611 weeks); spina bifida, elective abortion at 18 weeks (20 mg/day, 03 weeks); holoprosencephaly (dose unknown, 06 weeks). The case involving the VATER association is also described below. Based on the timing of exposure, only the case of spina bifida can be excluded as being lovastatin-induced because the critical period for neural tube defects does not begin until the 5th week (3rd week postconception) and the mother took the drug only during the 1st week postconception (conception was estimated to have occurred in all cases 2 weeks after the last menstrual period) (2). Although the remaining three defects may have occurred by chance, an association with lovastatin cannot be excluded.
In a surveillance study of Michigan Medicaid recipients involving 229,101 completed pregnancies conducted between 1985 and 1992, 3 newborns had been exposed to lovastatin during the 1st trimester (F. Rosa, personal communication, FDA, 1993). One (33.3%) major birth defect was observed (none expected), a cardiovascular defect. Eight other exposures to lovastatin occurred after the 1st trimester without apparent fetal harm (4).
Three retrospective spontaneous reports of birth defects suspected of being associated with 1st-trimester use of lovastatin have been received by the FDA (4). The anomalies described were aortic hypoplasia, ventricular septal defect with cerebral dysfunction, death (one case); anal atresia and renal dysplasia (one case); and short forearm, absent thumb, and thoracic scoliosis (one case).
A case report describing the use of lovastatin in a human pregnancy was published in 1992 (5). A woman was treated for 5 weeks with lovastatin and dextroamphetamine, starting approximately 6 weeks from her last menstrual period, for progressive weight gain and hypercholesterolemia. Therapy was discontinued when her pregnancy was diagnosed at 11 weeks' gestation. A female infant was delivered by cesarean section at 39 weeks' gestation. Gestational age was confirmed by an ultrasound examination at 21 weeks' gestation and the Dubowitz score at birth. The infant had a constellation of malformations termed the VATER association (vertebral anomalies, anal atresia, tracheoesophageal fistula with esophageal atresia, renal and radial dysplasias) (5). Specific anomalies included an asymmetric chest, thoracic scoliosis, absent left thumb, foreshortened left forearm, left elbow contracture, fusion of the ribs on the left, butterfly vertebrae in the thoracic and lumbar spine, left radial aplasia, and a lower esophageal stricture (5). Chromosomal analysis was normal, and the family history was noncontributory. This case is also described above (see Reference 2).
The cause of the defects in the above infant is unknown. Experiments with mice and rabbits indicate that amphetamines are teratogenic, but the anomalies primarily involve the heart and central nervous system (6). Moreover, the use of amphetamines during human pregnancy for medical indications has not been found to present a significant risk to the fetus in terms of fetotoxicity or teratogenicity (see Amphetamines). Although the cause of the infant's defects cannot be determined, drug-induced teratogenicity cannot be excluded because in utero exposure occurred during a critical period (i.e., 4th9th weeks of embryogenesis) and in light of the skeletal defects observed in rats with lovastatin (6).
In summary, infants with malformations following in utero exposure to lovastatin have been described in published and unpublished reports, but a causal relationship between the drug and the defects cannot be determined. In addition, some of the cases described above appear to be duplicate reports. The diversity of the malformation reports, moreover, lessens the probability of any association between lovastatin and the outcomes. However, because there is apparently no maternal benefit for the use of lovastatin during gestation and because of the human cases and the teratogenicity observed in one animal species, the drug should be avoided during pregnancy.
Breast Feeding Summary
Lovastatin is excreted in the milk of lactating rats (7), but no studies involving humans have been published. Because there is potential for adverse effects in the infant, the drug should probably not be used by women who are nursing.
References
- Product information. Mevacor. Merck, 2000.
- Manson JM, Freyssinges C, Ducrocq MB, Stephenson WP. Postmarketing surveillance of lovastatin and simvastatin exposure during pregnancy. Reprod Toxicol 1996;10:43946.
- Postmarketing surveillance of lovastatin and simvastatin exposure during pregnancy (Reply). Reprod Toxicol 1997;11:6412.
- Rosa F. Anti-cholesterol agent pregnancy exposure outcomes. Presented at the 7th International Organization for Teratogen Information Services, Woods Hole, MA, April 1994.
- Ghidini A, Sicherer S, Willner J. Congenital abnormalities (VATER) in baby born to mother using lovastatin. Lancet 1992;339:14167.
- Shepard TH. Catalog of Teratogenic Agents. 6th ed. Baltimore, MD:Johns Hopkins University Press, 1989:1978.
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Product information. Mevacor. Merck Sharp & Dohme, 1993.
Questions and Answers
Lovastatin?, I was recently in the hospital, where they tested my liver and found the starting of damage, and took me off Lipitor. Is Lovastatin going to be any better on my Liver
The elevation of liver enzymes by statin drugs (Lipitor/atorvastatin, lovastatin, etc) appears to be a "class effect", and if it happened with one statin it will likely happen with another.
Whether or not minor elevations in enzymes when taking statins actually represents liver injury is somewhat controversial. Talk to your doctor about your liver test results, if you might be able to safely take a statin with close monitoring, or potential alternative cholesterol lowering medications. Best of luck.
Where can I find the lovastatin quantities in the various red rice yeast products available?, Red rice yeast is still available, but it's effectiveness in lowering cholesterol depends on the amount of lovastatin contained. I've been frustrated in trying to figure out which products have the most lovastatin and how much each product contains. Anyone know where I can get this info without paying for it.
Thanks!!!!
Have you got high cholesterol?
If so go onto a low fat diet. It is safest and can't kill you like statins may do, they kill off the michochondia and so the cells die.
The liver makes all the cholesterol you need anyway.
G
Why is grapefruit taken with my Lovastatin a bad thing?, Does it make it weaker or stronger and if it makes it stronger couldn't I just take half with a grapefruit? I love grapefruit!
Grapefruit contains a chemical (bergamottin) that is a strong inhibitor of the enzyme that metabolizes lovastatin (and all other statins, except for pravastatin). This means there is less statin metabolized and therefore more in your bloodstream. Unfortunately, the effects of bergamottin on an individual's metabolism are unpredictable so a doctor or pharmacist cannot tell how they will respond or adjust dosage. What this means is you cannot have grapefruit juice while taking any statin (other than pravastatin). If it is any consolation, bergamottin is not present in orange juice, so you can try substituting OJ or other citrus fruits for grapefruits. I'm sorry, because I love grapefruits as well!
Has anyone suffered hair loss, due to taking Lovastatin?, I am losing my hair at an alarming rate. I have to wonder if it is due to the drug Lovastatin? After i started taking it i noticed that i was losing a lot. I have had blood tests and came up with no reason for it. Help!
better is doctor advice...
Why does Lovastatin require that I take it with a meal while other cholesterol medications don"t?, I have friends who take Lipitor for example and are not told that it must be taken with a meal. Is there some sort of reaction with the food in the case of Lovistatin or is it simply that it is more irritating to the stomach?
It is important to take Lovastatin with a meal. All drugs work differently. Lets say your prescribed amount of lovastatin is 100%, because of the way the drug is absorbed into your blood by your intestines, only 35% gets to your liver (Everything absorbed by your intestines must go through your liver before entering general circulation). And once it is in your liver and gets metabolized, only 5% actually gets into your general circulation. These are the percentages if you take lovastatin with a meal as directed. If you take it on an empty stomach it decreases the amount of drug absorbed by 1/3 meaning only about 24% is absorbed and even less gets to your general circulation, and thus it doesn't work as well because theres not enough of it. Lipitor works differently in the liver, and some foods can block the absorption of the drug. For example, if lipitor is taken with grapefruit juice it will not be absorbed at all, so it wont work. So, I hope this explanation helps!
What is the difference in Lovastatin and Simvastatin?,
Not a whole lot.
Lovastatin : generic for Mevacor; 1st generation
Simvastatin : generic for Zocor; 2nd generation
Mg for Mg, simvastatin is stronger. However, both can work well.
Does lovastatin (a cholesterol-lowering drug) reduce the risk of heart attack?, Does lovastatin (a cholesterol-lowering drug) reduce the risk of heart attack? In a Texas study,
researchers gave lovastatin to 2,325 people and an inactive substitute to 2,081 people (average age
58). After 5 years, 57 of the lovastatin group had suffered a heart attack, compared with 97 for the
inactive pill. (a) State the appropriate hypotheses. (b) Obtain a test statistic and p-value. Interpret
I am with squatting dog. I get bored with all of this p-value junk, but statins have been shown to be good for prevention of a secondary event (such as a person who has already had one heart attack), but the evidence is still up in the air as to whether it really helps prevent a first heart attack. If it were me, though, and my cholesterol was bad, I would want to take it just because it's a possible benefit.
What are the side effects of RANBAXY Lestric (Lovastatin Tablets USP 20mg)?, As the question above, what are the possible side effects? My friend is suffering from high blood pressure and he has been taking this tablet for three years. He has no known allergy but lately he has stiff muscle. So far his blood pressure is ok. What could be the problem, was it some side effect? Thank you.
Muscle pain is a side effect noted with most statins - the side effect profile for lovastatin can be viewed at any website that has approved product information. eg http://www.medicinenet.com/lovastatin/ar...
It is recommended that you friend see their Doctor who prescribed the product - even if just to be cautious
What are possible side effects of lovastatin?,
Go www.webmd.com you can get the side effects etc. there or call your pharmacist.
