Duration: IM: Following a single injection, a steady concentration is achieved within 2 to 3 weeks and maintained for an additional 2 to 3 weeks; steady-state levels are achieved after 3 injections administered at 4-week intervals.
Absorption: IM: Released slowly (via microsphere degradation in the muscle).
Distribution: Vd: 13.6 L (21.6 ± 8.5 L in acromegaly).
Protein binding: 65%, primarily to lipoprotein (41% in acromegaly).
Metabolism: Extensively hepatic.
Bioavailability: IM: 60% to 63%.
Time to peak, plasma: IM: Transient peak occurs 1 hour after injection, then steady plateau is reached after 2 to 3 weeks.
Excretion: Urine (32% as unchanged drug).
Clearance: Healthy adults: 7 to 10 L/hour; Adults with acromegaly: 18 L/hour; Decreased in patients with ESRD requiring dialysis.
禁忌症
Hypersensitivity to octreotide or any component of the formulation.
懷孕分類
B; Octreotide crosses the placenta and can be detected in the newborn at delivery.
哺乳分類
Octreotide is present in breast milk.
副作用
>10%: hypertension (≤13%), sinus bradycardia (19% to 25%), alopecia (1% to 13%), diaphoresis (21%), hyperglycemia (2% to 27%), hypothyroidism (1% to 12%), abdominal distress (≤61%), abdominal pain (≤44%), biliary tract disease (52% to 63%), biliary obstruction (12%), cholelithiasis (5% to 38%), constipation (≤21%), diarrhea (≤61%), flatulence (≤38%), gallbladder sludge (24%), nausea (≤61%), upper abdominal pain (8% to 11%), vomiting (≤21%), anemia (≤15%), antibody development (25%), pain at injection site (2% to 50%), dizziness (5% to 12%), fatigue (1% to 11%), headache (6% to 33%), arthralgia (1% to 26%), asthenia (1% to 22%), flu-like symptoms (1% to 20%).
劑量和給藥方法
1. Acromegaly: IM: Initial: 20 mg intragluteally every 4 weeks for 3 months; after initial 3 months, adjust dose as necessary based on clinical response.
2. Carcinoid syndrome; Gastroenteropancreatic neuroendocrine tumors, functional: IM: Initial: 20 mg intragluteally every 4 weeks or 20 to 30 mg intragluteally every 4 weeks; Titration: may decrease to 10 mg every 4 weeks after 2 months if initially responsive to 20 mg dose; Increase to 30 mg every 4 weeks if symptoms are inadequately controlled after 2 months.
3. Gastroenteropancreatic neuroendocrine tumors, metastatic, tumor control (off-label use): IM: 30 mg intragluteally every 4 weeks until tumor progression or death.
小兒調整劑量
腎功能調整劑量
Hemodialysis, intermittent (thrice weekly): IM: Initial: 10 mg intragluteally every 4 weeks; may titrate based on tolerability and response.
Peritoneal dialysis: IM: Initial: 10 mg intragluteally every 4 weeks; titrate based on tolerability and response.
PIRRT (eg, sustained, low-efficiency diafiltration): IM: consider reducing initial dose to 10 mg every 4 weeks; titrate based on tolerability and response.
肝功能調整劑量
Patients with established cirrhosis of the liver: IM: Initial: 10 mg IM every 4 weeks; titrate based upon response.