Sevelamer Carbonate 250mg 100 Tablets PHOSBLOCK Tablets 250mg Chronic Kidney Disease Hyperphosphatemia

Phosphate-containing binders, which bind to phosphorus in the gastrointestinal tract, prevent its absorption, and reduce blood phosphorus levels. They are suitable for hyperphosphatemia in chronic kidney disease (especially dialysis patients) and prevent complications related to phosphorus accumulation.

1. Basic information of the drug

1. Generic name : Sevelamer Hydrochloride
2. English name : PHOSBLOCK Tablets
3. Product Name : Fukurota Tablets 250mg
4. Dosage form : Film-coated tablets (white to slightly yellowish white, diameter 9 mm, thickness 6.2 mm, weight about 302 mg, identification code KR01, PTP packaging)
5. Indications : Improvement of hyperphosphatemia in patients with chronic renal insufficiency on dialysis
6. Element :
   • Active ingredient: Each tablet contains 250 mg of cebalamin.
   • Additives: カルナウバロウ, crystalline セルロース, hardened oil, acidified チタン, etc.
7. Appearance : White to slightly yellowish white film-coated tablets with specific physical specifications (diameter, thickness, weight).
8. Storage and shelf life : Store at room temperature, shelf life is 3 years; keep away from moisture after opening the aluminum foil packaging.

2. Usage and Dosage

• Conventional dose : Adults: 1-2 g each time (calculated as ceramer hydrochloride), 3 times a day, orally before meals;
• Dosage adjustments :
  • For patients who do not use precipitated carbonic acid carbamide: if blood phosphorus is less than 8.0mg/dL, start with 1g/time; if blood phosphorus is ≥8.0mg/dL, start with 2g/time;
  • Switching from precipitated carbonic acid carboxylate: if the original dose is less than 3g/day, start with 1g/time; if the original dose is ≥3g/day, start with 2g/time;
  • Subsequent adjustments are made based on blood phosphorus: ≥6.0 mg/dL, increase by 0.25-0.5 g/time; 4.0-6.0 mg/dL, maintain; <4.0 mg/dL, decrease by 0.25-0.5 g/time;
• Maximum dose : 9g per day.

3. Taboo

1. Those who have a history of allergy to the ingredients of this drug;
2. Patients with intestinal obstruction (may aggravate the condition).

IV. Precautions

1. Special Populations :
   • Pregnant women/women of childbearing potential: Use only when the benefits of treatment outweigh the risks;
   • Lactating women: decide whether to discontinue medication after weighing the benefits of treatment and breastfeeding;
   • Children: No effectiveness and safety data;
   • Elderly people: pay attention to side effects on the digestive system (decreased physiological function).
2. Patients with comorbidities :
   • Patients with intestinal stenosis, constipation, intestinal diverticulum, and a history of abdominal surgery: intestinal perforation and intestinal obstruction may occur, and bowel movements and abdominal symptoms need to be closely monitored;
   • Patients with hemorrhoidal disease, peptic ulcer/past history, or severe peptic ulcer motility disorder: This drug may cause swelling in the intestines and aggravate symptoms;
   • People with bleeding tendency: The risk of bleeding may be increased due to the obstruction of vitamin K absorption;
   • Patients with history of gastric/intestinal resection and dysphagia: Not included in clinical trials, so caution is required.
3. Medication Instructions :
   • The concentrations of blood phosphorus, calcium, chloride, and bicarbonate should be monitored regularly to be alert to hypocalcemia and hyperchloremic acidosis;
   • It may affect the absorption of fat-soluble vitamins (A, D, E, K) and folic acid, and long-term medication should be considered for supplementation;
   • Avoid chewing or crushing the tablet before taking it, and swallow it quickly (it will swell if kept in the mouth for a long time);
   • The tablets must be taken out of the PTP package before consumption to avoid accidental swallowing of PTP tablets which may cause damage to the esophagus.

5. Adverse Reactions

1. Serious side effects :
   • Intestinal perforation, intestinal obstruction (frequency unknown): manifested as severe constipation, persistent abdominal pain, vomiting, etc., requiring immediate discontinuation of medication and examination;
   • Diverticulitis, ischemic enteritis (frequency unknown): may progress to intestinal perforation and require prompt treatment;
   • Gastrointestinal bleeding (0.3%), gastrointestinal ulcer (0.1%): If vomiting blood or blood in stool occurs, the drug should be discontinued;
   • Liver dysfunction (frequency unknown): accompanied by significant increase in AST and ALT.
2. Common side effects :
   • Digestive system: constipation/worsened constipation (24.9%), abdominal pain (3.2%), abdominal distension (7.9%), upper abdominal pain (13.9%), etc.;
   • Metabolism: decreased blood calcium, decreased blood bicarbonate, decreased blood zinc/copper, etc.;
   • Others: anemia, rash, joint pain, etc. (frequency < 5%).

6. Drug Interactions

• May delay or reduce the absorption of concurrent oral medications (such as antiepileptic drugs, antiarrhythmic drugs, etc.);
• When used together, the drugs need to be administered at intervals and changes in efficacy should be closely observed (the mechanism is unclear, but may be related to intestinal binding).

7. Pharmacological Action

• Mechanism of action : As a phosphorus-binding polymer, it binds to phosphorus in the intestine, promotes fecal excretion, reduces intestinal absorption, and thus reduces blood phosphorus concentration;
• Other effects : It can inhibit the progression of abnormal calcification, improve serum parathyroid hormone (PTH) concentration, and inhibit the progression of renal osteodystrophy.

8. Pharmacokinetics

• Absorption : Not absorbed by the intestines, more than 99% is excreted in feces within 7 days after administration;
• Distribution/Metabolism/Excretion : No systemic absorption, mainly excreted through the intestines, no accumulation in the body.

IX. Clinical Research

• Hemodialysis patients : Phase III trials showed that blood phosphorus dropped from 7.96 mg/dL to 5.62 mg/dL after medication, with an 8-week target achievement rate of 92.4% and a long-term (48-week) target achievement rate of 94.4%, without affecting blood calcium.
• Peritoneal dialysis patients : The target achievement rate in the Phase III trial was 72.7% at 8 weeks;
• Side effects : Mainly digestive system symptoms (constipation, abdominal pain, etc.), with an incidence rate of 60.9%~72.0%.

10. Packaging specifications

• PTP packaging (including desiccant): 100 tablets (10 tablets × 10), 1000 tablets (10 tablets × 100).

11. Production Information

Manufacturer : Kyowa Kirin Co., Ltd.