tolvaptan (Rx)

Brand and Other Names:Samsca
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 15mg
  • 30mg
more...

Hyponatremia

Indicated for hospitalized adults with clinically significant euvolemic or hypervolemic hyponatremia (serum sodium <125 mEq/L or less marked hyponatremia that is symptomatic and has resisted correction with fluid restriction), including patients with heart failure, cirrhosis, and SIADH

Initial: 15 mg PO qDay

Maintenance: Increase PRN after >24 hr to 30 mg qDay; may increase further, not to exceed 60 mg qDay

Not to exceed 30 days of treatment

Monitor: Serum sodium

Renal Impairment

CrCl 10-79 mL/min: No dosage adjustment required

CrCl <10 mL or dialysis: Not studied

Anuria: Contraindicated; no benefit expected

Hepatic Impairment

Moderate and severe hepatic impairment do not affect exposure to tolvaptan to a clinically relevant extent

Avoid use of tolvaptan in patients with underlying liver disease

Administration

Do not exceed 30 days of administration to minimize risk of liver injury (see Cautions)

Following discontinuation, patients should be advised to resume fluid restriction and should be monitored for changes in serum sodium and volume status

Safety and efficacy not established

Next:

Interactions

Interaction Checker

and tolvaptan

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 
            Previous
            Next:

            Adverse Effects

            >10%

            Nausea (21%)

            Thirst (16%)

            Dry mouth (13%)

            Pollakiuria (4-11%)

            Urinary frequency/output increased (11%)

            1-10%

            GI bleeding with pre-existing cirrhosis (10%)

            Weakness (9%)

            Constipation (7%)

            Hyperglycemia (6%)

            Anorexia (4%)

            Postmarketing Reports

            Neurologic: Osmotic demyelination syndrome

            Investigations: Hypernatremia

            Immune system disorders: Hypersensitivity reactions including anaphylactic shock and rash

            Previous
            Next:

            Warnings

            Black Box Warnings

            Initiate or reinitiate only in a hospital where serum sodium level can be monitored closely

            Too-rapid correction of hyponatremia (eg, >12 mEq/L/24 hr) can cause osmotic demyelination resulting in dysarthria, mutism, dysphagia, lethargy, affective changes, spastic quadriparesis, seizures, coma, and death

            In susceptible patients, including those with severe malnutrition, alcoholism, or advanced liver disease, slower rates of correction may be advisable

            Contraindications

            Urgent correction of hypovolemia required

            Inability to feel/respond to thirst

            Hypovolemic hyponatremia

            Concomitant strong CYP3A4 inhibitors

            Anuria

            Hypersensitivity (eg, anaphylactic shock, rash generalized)

            Cautions

            Cirrhosis, hypovolemia, dehydration

            Too rapid correction can cause serious neurologic damage (see Black Box Warnings)

            Risk of dehydration/hypovolemia; encourage patient to drink whenever thirsty; interrupt if occurs

            Osmotic demyelination syndrome reported

            Risk of hyperkalemia

            May need dose adjustments with concomitant moderate CYP3A4 inhibitors, CYP inducers or Pgp inhibitors (also see Contraindications)

            Avoid/limit grapefruit juice consumption

            Liver injury

            • Can cause serious and potentially fatal liver injury; increased ALT (>3 xULN)
            • Increased ALT observed in 4.4% of patients (compared with 1% taking placebo) typically starting ~3 months after therapy initiated
            • Limit duration of treatment to 30 days
            • If symptoms indicating liver injury occur (eg, fatigue, anorexia, right upper abdominal discomfort, dark urine, jaundice), discontinue tolvaptan
            • Avoid use with underlying liver disease, including cirrhosis, because the ability to recover from liver injury may be impaired
            Previous
            Next:

            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: not known if excreted in breast milk, do not nurse

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
            Previous
            Next:

            Pharmacology

            Mechanism of Action

            Selective vasopressin V2-receptor antagonist that causes an increase in urine water excretion that results in an increase in free water clearance (aquaresis), a decrease in urine osmolality, and a resulting increase in serum sodium concentration

            Pharmacokinetics

            Half-Life, Terminal: 12 hr

            Absorption: >40%

            Pgp substrate and inhibitor

            Peak effect: 4-8 hr

            Duration: At 24 hr 60% of peak serum sodium elevation is retained

            Peak Plasma Time: 2-4 hr

            Vd: 3 L/kg  

            Protein Bound: 99%

            Metabolism: Hepatic through CYP3A4

            Excretion: Feces

            Previous
            Next:

            Images

            Previous
            Next:

            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Additional Offers
            Email to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Email Forms to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Previous