Rotazona tablets are contraindicated in patients with:
- Heart failure of any severity: Rotazona and several of its metabolites are inhibitors of phosphodiesterase III. Several drugs with this pharmacologic effect have caused decreased survival compared to placebo in patients with class III-IV heart failure.
- Hypersensitivity to Rotazona or any components of Rotazona tablets (e.g., anaphylaxis, angioedema)
The total and unbound oral clearances, adjusted for body weight, of Rotazona and its metabolites were not significantly different with respect to age (50 to 80 years) or gender.
Rotazona is contraindicated in patients with heart failure of any severity. Rotazona and several of its metabolites are inhibitors of phosphodiesterase III. Several drugs with this pharmacologic effect have caused decreased survival compared to placebo in patients with class III-IV heart failure .
What should I avoid while taking Rotazona (Pletal)?
Grapefruit and grapefruit juice may interact with Rotazona and lead to unwanted side effects. Discuss the use of grapefruit products with your doctor.
Of the total number of subjects (n = 2,274) in clinical studies of PLETAL, 56 percent were 65 years old and over, while 16 percent were 75 years old and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be excluded. Pharmacokinetic studies have not disclosed any age-related effects on the absorption, distribution, metabolism, and elimination of Rotazona and its metabolites.
What is Rotazona (Pletal)?
Rotazona is a vasodilator that works by relaxing the muscles in your blood vessels to help them dilate (widen). Rotazona dilates arteries that supply blood to your legs. Rotazona also improves circulation by keeping platelets in the blood from sticking together and clotting.
Rotazona is used to treat the symptoms of intermittent claudication. This condition causes reduced blood flow to the legs, leading to pain while walking. Rotazona improves your ability to walk longer distances without pain.
Rotazona may also be used for purposes not listed in this medication guide.
What should I discuss with my healthcare prov >
Do not take Rotazona if you have congestive heart failure. Rotazona can make this condition worse.
To make sure Rotazona is safe for you, tell your doctor if you have:
It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.
It is not known whether Rotazona passes into breast milk or if it could harm a nursing baby. You should not breast-feed while using this medicine.
The total pharmacologic activity of Rotazona and its metabolites was similar in subjects with mild to moderate renal impairment and in healthy subjects. Severe renal impairment increases metabolite levels and alters protein binding of the parent. The expected pharmacologic activity, however, based on plasma concentrations and relative PDE III inhibiting potency of parent drug and metabolites, appeared little changed. Patients on dialysis have not been studied, but, it is unlikely that Rotazona can be removed efficiently by dialysis because of its high protein binding (95 -98%).
Carcinogenesis, Mutagenesis, Impairment Of Fertility
Dietary administration of Rotazona to male and female rats and mice for up to 104 weeks, at doses up to 500 mg/kg/day in rats and 1000 mg/kg/day in mice, revealed no evidence of carcinogenic potential. The maximum doses administered in both rat and mouse studies were, on a systemic exposure basis, less than the human exposure at the MRHD of the drug. Rotazona tested negative in bacterial gene mutation, bacterial DNA repair, mammalian cell gene mutation, and mouse in vivo bone marrow chromosomal aberration assays. It was, however, associated with a significant increase in chromosomal aberrations in the in vitro Chinese Hamster Ovary Cell assay.
In female mice, Rotazona caused a reversible contraceptive effect at a dose (300 mg/kg) that was approximately 7.4-fold greater than the Maximum Recommended Human Dose (MRHD) on a body surface area basis. These findings have not been demonstrated in other animal species.
Rotazona did not affect fertility or mating performance of male and female rats at doses as high as 1000 mg/kg/day. At this dose, systemic exposures (AUCs) to unbound Rotazona were less than 1.5 times in males, and about 5 times in females, the exposure in humans at the MRHD.
Rotazona may induce tachycardia, palpitation, tachyarrhythmia or hypotension. The increase in heart rate associated with Rotazona is approximately 5 to 7 bpm. Patients with a history of ischemic heart disease may be at risk for exacerbations of angina pectoris or myocardial infarction.
Rotazona did not inhibit the pharmacologic effects (PT, aPTT, bleeding time, or platelet aggregation) of R-and S-warfarin after a single 25-mg dose of warfarin. The effect of concomitant multiple dosing of warfarin and PLETAL on the pharmacodynamics of both drugs is unknown.
6.1 Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
Adverse reactions were assessed in eight placebo-controlled clinical trials involving patients exposed to either 50 or 100 mg twice daily Rotazona (n = 1301) or placebo (n = 973), with a median treatment duration of 127 days for patients on Rotazona and 134 days for patients on placebo.
The most frequent adverse reaction resulting in discontinuation of therapy in more than 3% of patients treated with Rotazona was headache . Other frequent causes of discontinuation included palpitation and diarrhea, both 1.1% for Rotazona (all doses) versus 0.1% for placebo.
The most common adverse reactions, occurring in at least 2% of patients treated with Rotazona 50 or 100 mg twice daily, are shown in Table 1 .
Is Rotazona safe to take if I'm pregnant or breastfeeding?
The use of Rotazona in pregnancy has not been adequately studied.
Rotazona has not been adequately studied in women who are breastfeeding.
Rotazona comes as a tablet to that is taken orally.
It's typically taken twice daily, at least 30 minutes before or two hours after breakfast and dinner.
Try to take this medicine around the same time each day.
Follow the directions on your prescription label carefully. Don't take more or less Rotazona than is prescribed by your doctor.
Population pharmacokinetic analysis suggests that smoking decreased Rotazona exposure by about 20%.
Serious Side Effects of Rotazona
Tell your doctor right away if you experience any of the following serious side effects:
- Fast or irregular heartbeat
- Unusual bruising or bleeding
- Sudden, severe headache or vomiting
- Vision changes
- Unusual weight gain
- Swelling of the hands, arms, feet, ankles, or lower legs
- Dark, tarry, or bloody stools
- Vomit that looks like coffee grounds
- Signs of infection, which may include fever, sore throat, rash, or chills