藥碼
AKU02
藥名
RIF/INH/PZA/EMB 150/75/400/275mg
英文商品名
Akurit-4 四合一 錠劑
中文商品名
立剋核-4膜衣錠
螢幕名
Akurit-4 四合一 錠劑
劑型
Tab
規格
Film coated tablet: Rifampin 150mg+ Isoniazid 75mg+ Pyrazinamide 400mg+ Ethambutol HCl 275mg/ tab
成分
藥理分類
Antituberculosis Agents
健保碼
BC25518100
ATC碼
適應症
結核病 Treatment of tuberculosis infection
藥理
Antitubercular Agent
AkuriT-4 is a four drug fixed dose combination of anti-TB drugs, including rifampin 150 mg, Isoniazid 75 mg, Pyrazinamide 400mg, and Ethambutol 275 mg.
AkuriT-4 is a four drug fixed dose combination of anti-TB drugs, including rifampin 150 mg, Isoniazid 75 mg, Pyrazinamide 400mg, and Ethambutol 275 mg.
藥動學
Rifampin:
1. Duration: ≤24 hours
2. Absorption: Well absorbed; food may delay or slightly reduce peak
3. Distribution: Highly lipophilic, crosses blood-brain barrier well; Vd ~1.1 L/kg; Protein binding: 80%
4. Metabolism: Hepatic; undergoes enterohepatic recirculation
5. Half-life elimination: (Infants and Children 6 months to <5 years) ~1 to 4 hours; (Adults) ~2-3 hours
6. Time to peak, serum: 1-2 hours
7. Excretion: Feces (60% to 65%) and urine (~30%) as unchanged drug
Isoniazid:
1. Absorption: Rapid and complete; food reduces rate and extent of absorption
2. Distribution: All body tissues and fluids including CSF; Protein binding: 10-15%
3. Metabolism: Hepatic to acetylisoniazid with decay rate determined genetically by acetylation phenotype; undergoes further hydrolysis to isonicotinic acid and acetylhydrazine
4. Half-life: May be prolonged in patients with impaired hepatic function or severe renal impairment; (Fast acetylators) 30-100 minutes; (Slow acetylators) 2-5 hours
5. Time to peak, serum: 1-2 hours
6. Excretion: Urine (75% to 95% as unchanged drug and metabolites); small amounts excreted in feces and saliva
Ethambutol:
1. Absorption: ~80%
2. Distribution: Widely throughout body; Protein binding: 20-30%
3. Metabolism: Hepatic (20%) to inactive metabolite
4. Half-life elimination: 2.5-3.6 hours; (ESRD) 7-15 hours
5. Time to peak, serum: 2-4 hours
6. Excretion: Urine (~50% as unchanged drug, 8% to 15% as metabolites); feces (~20% as unchanged drug)
Isoniazid:
1. Absorption: Well absorbed
2. Distribution: Widely into body tissues and fluids; Protein binding: 50%
3. Metabolism: Hepatic
4. Half-life elimination: 9 to 10 hours, prolonged with reduced renal or hepatic function
5. Time to peak, serum: Within 2 hours
6. Excretion: Urine (4% as unchanged drug)
1. Duration: ≤24 hours
2. Absorption: Well absorbed; food may delay or slightly reduce peak
3. Distribution: Highly lipophilic, crosses blood-brain barrier well; Vd ~1.1 L/kg; Protein binding: 80%
4. Metabolism: Hepatic; undergoes enterohepatic recirculation
5. Half-life elimination: (Infants and Children 6 months to <5 years) ~1 to 4 hours; (Adults) ~2-3 hours
6. Time to peak, serum: 1-2 hours
7. Excretion: Feces (60% to 65%) and urine (~30%) as unchanged drug
Isoniazid:
1. Absorption: Rapid and complete; food reduces rate and extent of absorption
2. Distribution: All body tissues and fluids including CSF; Protein binding: 10-15%
3. Metabolism: Hepatic to acetylisoniazid with decay rate determined genetically by acetylation phenotype; undergoes further hydrolysis to isonicotinic acid and acetylhydrazine
4. Half-life: May be prolonged in patients with impaired hepatic function or severe renal impairment; (Fast acetylators) 30-100 minutes; (Slow acetylators) 2-5 hours
5. Time to peak, serum: 1-2 hours
6. Excretion: Urine (75% to 95% as unchanged drug and metabolites); small amounts excreted in feces and saliva
Ethambutol:
1. Absorption: ~80%
2. Distribution: Widely throughout body; Protein binding: 20-30%
3. Metabolism: Hepatic (20%) to inactive metabolite
4. Half-life elimination: 2.5-3.6 hours; (ESRD) 7-15 hours
5. Time to peak, serum: 2-4 hours
6. Excretion: Urine (~50% as unchanged drug, 8% to 15% as metabolites); feces (~20% as unchanged drug)
Isoniazid:
1. Absorption: Well absorbed
2. Distribution: Widely into body tissues and fluids; Protein binding: 50%
3. Metabolism: Hepatic
4. Half-life elimination: 9 to 10 hours, prolonged with reduced renal or hepatic function
5. Time to peak, serum: Within 2 hours
6. Excretion: Urine (4% as unchanged drug)
禁忌症
1. Hypersensitivity to ethambutol to Rifampin, Isoniazid, Pyrazinamide or Ethambutol.
2. Concomitant use with atazanavir, darunavir, saquinavir, tipranavir, rilpivirine or elvitegravir/cobicistat
3. Acute liver disease
4. Severe adverse reactions to isoniazid, such as fever, chills, and arthritis
5. Optic neuritis
6. Acute gout
2. Concomitant use with atazanavir, darunavir, saquinavir, tipranavir, rilpivirine or elvitegravir/cobicistat
3. Acute liver disease
4. Severe adverse reactions to isoniazid, such as fever, chills, and arthritis
5. Optic neuritis
6. Acute gout
懷孕分類
C
哺乳分類
Avoided
副作用
| Drug | Rifampin | Isoniazid | Ethambutol | Pyrazinamide | |
|---|---|---|---|---|---|
| Significant |
1. Clostridioides difficile infection 2. Hematologic effects (Decreased hemoglobin, disorder of hemostatic components of blood, disseminated intravascular coagulation, eosinophilia, hemolysis, hemolytic anemia, hemorrhage, leukopenia, thrombocytopenia) 3. Hepatotoxicity 4. Hypersensitivity reactions (urticaria, angioedema, anaphylaxis, flu-like symptoms) 5. Pulmonary toxicity |
Increased serum transaminases |
1. Hepatotoxicity 2. Optic neuritis (changes in vision, color blindness, visual defects) |
- | |
| Adverse reactions | Cardiovascular | Decreased blood pressure, edema, shock | Vasculitis | Myocarditis, pericarditis | - |
| Endocrine | Adrenocortical insufficiency, increased uric acid | Gynecomastia, hyperglycemia, metabolic acidosis, pellagra, pyridoxine deficiency | Acute gout attack, hyperuricemia | Gout | |
| Gastrointestinal | Abdominal cramps, diarrhea, discomfort, flatulence, nausea, staining of tooth, vomiting | Epigastric distress, nausea, pancreatitis, vomiting | Abdominal pain, anorexia, gastric distress, nausea, vomiting | Anorexia, nausea, vomiting | |
| Genitourinary | Hematuria | Bilirubinuria | - | - | |
| Nervous system | Ataxia, behavioral changes, cerebral hemorrhage, confusion, dizziness, fatigue, headache, lack of concentration, myasthenia, numbness, psychosis, sore mouth | Brain disease, memory impairment, paresthesia, peripheral neuropathy, psychosis, seizure | Confusion, dizziness, headache, malaise, peripheral neuritis | Malaise | |
| Neuromuscular | Limb pain, myopathy | Lupus-like syndrome, rheumatic disease | Arthralgia | Arthralgia, myalgia | |
| Ophthalmic | Conjunctivitis | Optic atrophy, optic neuritis | Color blindness, decreased visual acuity, optic neuritis, scotoma, visual disturbance | - | |
| Dermatologic | - | Skin rash, toxic epidermal necrolysis | Dermatitis, erythema multiforme, pruritus, skin rash | Acne vulgaris, pruritus, skin photosensitivity, skin rash | |
| Hematologic | - | Agranulocytosis, anemia, eosinophilia, lymphadenopathy, thrombocytopenia | Eosinophilia, leukopenia, lymphadenopathy, neutropenia, thrombocytopenia | Acquired blood coagulation disorder, thrombocytopenia | |
| Renal | Acute interstitial nephritis, acute renal injury, increased blood urea nitrogen, renal insufficiency, renal tubular necrosis | - | Nephritis | Interstitial nephritis | |
| Respiratory | Dyspnea, flu-like symptoms | - | Pneumonitis, pulmonary infiltrates | - | |
| Hepatic | - | Hepatitis, hyperbilirubinemia, jaundice, hepatotoxicity | Abnormal hepatic function tests, hepatitis, hepatotoxicity | Hepatotoxicity | |
| Miscellaneous | fever | ||||
劑量和給藥方法
Dosage:
1. Body Weight 30-37kg: 2 tab PO QD
2. Body Weight 38-54kg: 3 tab PO QD
3. Body Weight 55-70kg: 4 tab PO QD
4. Body Weight ＞70kg: 5 tab PO QD
Administration:
Take 1 hour before meal or 2 hours after meal
1. Body Weight 30-37kg: 2 tab PO QD
2. Body Weight 38-54kg: 3 tab PO QD
3. Body Weight 55-70kg: 4 tab PO QD
4. Body Weight ＞70kg: 5 tab PO QD
Administration:
Take 1 hour before meal or 2 hours after meal
小兒調整劑量
腎功能調整劑量
肝功能調整劑量
安定性
藥袋資訊
臨床用途
抗結核劑
主要副作用
噁心、嘔吐、肝功能異常、過敏、視力減退
泡製方法
儲存方式
請置於 15-30℃ 乾燥處儲存
注意事項
其他說明
藥局 J2 | 藥庫 口A12
藥品外觀
顏色
16
形狀
04
剝痕
Y
標記1
標記2
其他
健保藥價
16.5
自費價
21.95
仿單
資料庫
健保給付規定