Indications for INVOKAMET:
Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus who are not adequately controlled on a regimen containing metformin or canagliflozin or who are already being treated with both canagliflozin and metformin. Limitations of use: not for treating type 1 diabetes or diabetic ketoacidosis.
Adult Dose for INVOKAMET:
See full labeling. Individualize. Take twice daily with meals; increase dose gradually. Max daily dose: 300mg/2000mg. Moderate renal impairment (eGFR 45–<60mL/min/1.73m2): max canagliflozin 50mg twice daily. Concomitant UGT inducers in patients with eGFR ≥60mL/min/1.73m2: consider increase to canagliflozin 150mg twice daily; if eGFR 45–<60mL/min/1.73m2: consider other antihyperglycemics.
Children's Dose for INVOKAMET:
<18yrs: not established.
Pharmacological Class:
Sodium-glucose co-transporter 2 inhibitor + biguanide.
Contraindications:
Renal impairment (SCr ≥1.5mg/dL [men], ≥1.4mg/dL [women], or eGFR <45mL/min/1.73m2), ESRD, or on dialysis. Metabolic acidosis, diabetic ketoacidosis.
Warnings/Precautions:
Confirm normal renal function before starting and monitor thereafter (esp. in elderly). Discontinue if lactic acidosis, renal impairment, shock, acute MI or CHF, dehydration, sepsis, hypoxemia, pancreatitis, or hypersensitivity reactions occur. Avoid in hepatic disease. Discontinue prior to any intravascular radiocontrast study or surgery; withhold for 48hrs after procedure. Correct volume depletion before initiating. Monitor for symptomatic hypotension after starting therapy (esp. elderly, renal impairment, low systolic BP, on diuretics or drugs that interfere with the RAAS system [eg, ACEIs, ARBs]). Monitor serum K+ levels in patients predisposed to hyperkalemia. Elderly, debilitated, uncompensated strenuous exercise, malnourished or deficient caloric intake, adrenal or pituitary insufficiency, or alcohol intoxication: increased risk of hypoglycemia. Monitor for genital mycotic infections, hematology (esp. serum Vit. B12), increases in LDL-C; treat if occur. Pregnancy (Cat.C). Nursing mothers.
Interactions:
Cationic drugs eliminated by renal tubular secretion (eg, amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim, vancomycin); may increase metformin levels; monitor. Increased risk of lactic acidosis with topiramate, other carbonic anhydrase inhibitors (eg, zonisamide, acetazolamide, dichlorphenamide). Diuretics, steroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, sympathomimetics, nicotinic acid, CCBs, and isoniazid may cause hyperglycemia. Avoid excessive alcohol. Concomitant drugs that may affect renal function or metformin disposition; monitor and adjust dose. Antagonized by UGT inducers (eg, rifampin, phenytoin, phenobarbital, ritonavir): see Adults. Concomitant digoxin: monitor. Concomitant insulin or insulin secretagogue: consider a lower dose of insulin/insulin secretagogue to reduce risk of hypoglycemia. May cause false (+) urine glucose tests or unreliable measurements of 1, 5-AG assay; use alternative methods to monitor glycemic control.
Adverse Reactions:
Female genital mycotic infections, UTI, increased urination, GI upset, flatulence, asthenia, indigestion, abdominal discomfort, headache.
How Supplied:
Tabs—60
强生Invokamet（坎格列净/二甲双胍固定剂量复方药物）新药获FDA批准
强生旗下杨森制药公司于8月8日宣布，美国食品药品监督管理局（FDA）正式批准旗下新药Invokamet（坎格列净/二甲双胍固定剂量复方药物）用于2型糖尿病)成人患者的治疗。
坎格列净（商品名Invokana，杨森制药）是首个获批的钠葡萄糖协同转运蛋白2（SGLT2）抑制剂，于2013年3月获得美国FDA的批准用于2型糖尿病治疗。而二甲双胍则是2型糖尿病的常用药。
此次FDA对Invokamet的批准基于杨森公司发布的III期临床试验数据。该III期临床试验共有4732人参与，数据表明，相较二甲双胍和其他单药治疗，INVOKAMET能大幅度降低患者体内的HbA1c水平，INVOKAMET与相应剂量坎格列净+二甲双胍联合治疗方案具有等效性。
FDA批准Invokamet作为一种辅助药物，结合运动和饮食，用于改善2型糖尿病成人患者的血糖控制，主要用于（1）服用坎格列净或二甲双胍单药不能充分控制血糖水平的患者；（2）已经在接受坎格列净+二甲双胍两种药物联合治疗的患者。Invokamet不适用于1型糖尿病和糖尿病酮症酸中毒的治疗。
在美国，Invokamet是首个SGLT2抑制剂和二甲双胍固定剂量复方产品。此前，Invokamet已于2014年4月获欧盟批准上市。
Invokamet同时还附带黑框警告，即二甲双胍累积有可能会出现乳酸酸中毒，可致死。患者如果有严重肾功能或属于血液透析治疗阶段，也禁止服用该药物。 |
