Agencia Lei Va Hong
Concise Prescribing Info
Slows the progression of cyst development & renal insufficiency of autosomal dominant polycystic kidney disease (ADPKD) in adults w/ chronic kidney disease (CKD) stage 1-4 at initiation of treatment w/ evidence of rapidly progressing disease.
Dosage/Direction for Use
Split dose regimen (bd): Initially 60 mg/day as 45 mg + 15 mg (45 mg taken upon waking & prior the morning meal & 15 mg taken 8 hr later). Titrate upward to 90 mg/day (60 mg + 30 mg), then to a target dose of 120 mg/day (90 mg + 30 mg), if tolerated, w/ at least wkly intervals between titrations.
May be taken with or without food: Take morning dose at least 30 min before breakfast. Take 2nd dose w/ or w/out food. Swallow whole w/ a glass of water, do not chew/crush. Avoid grapefruit juice.
Hypersensitivity; elevated liver enzymes &/or signs/symptoms of liver injury prior to initiation of treatment; anuria; vol depletion; hypernatraemia; patients who cannot perceive or respond to thirst. Pregnancy & lactation.
Special Precautions
Idiosyncratic hepatic toxicity. Perform blood testing for hepatic transaminases & bilirubin prior to initiation of treatment, continuing mthly for 18 mth & at regular 3-mthly intervals thereafter. Monitor for symptoms that may indicate liver injury. Excessive thirst or dehydration. Monitor vol, fluid & electrolyte status. Urinary output must be secured. Discontinue in case of anaphylactic reaction or other serious allergic reactions. Rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption. Exclude pseudohyponatraemia in DM patients prior & during treatment. May cause hyperglycaemia. Evaluate uric acid conc prior to initiation of therapy & as indicated during treatment based on symptoms. Reversible reduction in GFR. Correct hyponatraemia/hypernatraemia prior to initiation w/ tolvaptan therapy. Minor influence on the ability to drive or use machines. Discontinue treatment if renal insufficiency progresses. Patients w/ severe hepatic impairment. Not recommended in the paed age group.
Adverse Reactions
Polydipsia; headache, dizziness; diarrhoea, dry mouth; nocturia, pollakiuria, polyuria; fatigue, thirst. Dehydration, hypernatraemia, decreased appetite, hyperuricaemia, hyperglycaemia; insomnia; palpitations; dyspnoea; abdominal pain, abdominal distension, constipation, dyspepsia, GERD; abnormal hepatic function; rash, pruritus; muscle spasms; asthenia; increased ALT & AST, decreased wt.
Drug Interactions
Increased exposure w/ moderate CYP3A inhibitors (eg, amprenavir, aprepitant, atazanavir, ciprofloxacin, crizotinib, darunavir/ritonavir, diltiazem, erythromycin, fluconazole, fosamprenavir, imatinib, verapamil) or strong CYP3A inhibitors (eg, itraconazole, ketoconazole, ritonavir, clarithromycin). Decreased exposure & efficacy w/ potent CYP3A4 inducers (eg, rifampicin). Higher risk for developing hypernatraemia w/ medicinal products that increase serum Na conc. Potential to lead to severe dehydration w/ loop & thiazide diuretics. Increased steady state conc of digoxin. Use w/ caution when co-administered w/ narrow therapeutic P-gp substrates (eg, dabigatran); OATP1B1 & OATP1B3 substrates (eg, statins), OAT3 substrates (eg, methotrexate, ciprofloxacin), BCRP substrates (eg, sulfasalazine) or OCT1 substrates (eg, metformin). Possible attenuation of effect of vasopressin analogues eg, desmopressin. Can potentially increase exposure to CYP3A4 substrates. Risk of orthostatic/postural hypotension w/ diuretics or non-diuretic antihypertensives.
MIMS Class
ATC Classification
C03XA01 - tolvaptan ; Belongs to the class of vasopressin antagonists. Used as diuretics.
Jinarc tab 30 mg
Jinarc tab 45 mg +15 mg
Jinarc tab 60 mg + 30 mg
Jinarc tab 90 mg + 30 mg
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