Inflammation: The Uniting Force
The role of inflammation in atherosclerosis development
and progression has gone from theory to treatment target
in 15 years. One of its chief proponents is Paul M. Ridker,
MD, from Brigham and Women’s Hospital, Harvard Medical School, Boston. MA. Dr. Ridker was among the first to
determine the prognostic usefulness of C-reactive protein
(CRP) to evaluate CV risk.
SAMSCA® (tolvaptan)
anaphylactic shock and rash generalized [see Contraindications (4.6)].
DRUG INTERACTIONS:
Effects of Drugs on Tolvaptan:
Ketoconazole and Other Strong CYP 3A Inhibitors: SAMSCA is metabolized primarily
by CYP 3A. Ketoconazole is a strong inhibitor of CYP 3A and also an inhibitor of P-gp. Coadministration of SAMSCA and ketoconazole 200 mg daily results in a 5-fold increase in exposure
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administered [see Dosage and Administration (2.3) and Contraindications (4.4)].
Moderate CYP 3A Inhibitors: 7KHLPSDFWRIPRGHUDWH&<3$LQKLELWRUV HJHU\WKURP\FLQ
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has not been assessed. A substantial increase in the exposure to tolvaptan would be expected
when SAMSCA is co-administered with moderate CYP 3A inhibitors. Co-administration of
SAMSCA with moderate CYP3A inhibitors should therefore generally be avoided [see Dosage and
Administration (2.3) and Warnings and Precautions (5.5)]. Grapefruit Juice: Co-administration
of grapefruit juice and SAMSCA results in a 1.8-fold increase in exposure to tolvaptan [see Dose
and Administration (2.3) and Warnings and Precautions (5.5)]. P-gp Inhibitors: Reduction in the
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HJF\FORVSRULQHEDVHGRQFOLQLFDOUHVSRQVH[see Dose and Administration (2.3) and Warnings
and Precautions (5.5)]. Rifampin and Other CYP 3A Inducers: Rifampin is an inducer of
CYP 3A and P-gp. Co-administration of rifampin and SAMSCA reduces exposure to tolvaptan
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have to be increased [Dosage and Administration (2.3) and Warnings and Precautions (5.5)].
Lovastatin, Digoxin, Furosemide, and Hydrochlorothiazide: &RDGPLQLVWUDWLRQRIORYDVWDWLQ
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the exposure to tolvaptan.
Effects of Tolvaptan on Other Drugs: Digoxin: Digoxin is a P-gp substrate. Co-administration
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Amiodarone, Furosemide, and Hydrochlorothiazide: Co-administration of tolvaptan does
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Lovastatin: SAMSCA is a weak inhibitor of CYP 3A. Co-administration of lovastatin and SAMSCA
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