Acromegaly Drug Summary

Drug	Dosage	Remarks
Bromocriptine	Initial dose: 1.25-2.5 mg PO 24 hourly at bedtime May increase by 1.25-2.5 mg PO 24 hourly at 3-7 day intervals until optimal clinical response achieved Max dose: 100 mg/day	Adverse Reactions GI effects (nausea/vomiting, gastric hemorrhage); CNS effects (dizziness, drowsiness, headache, depression); Other effects (postural hypotension, pleural effusion, nasal congestion, fatigue)  Special Instructions Contraindicated in patients with severe ischemic heart disease, uncontrolled hypertension
Cabergoline	Initial dose: 0.5 mg PO 2x/week for 2 weeks then 1 mg PO 2x/week for 6 weeks then 0.5 mg PO 24 hourly Usual dose range: 1.5-2.5 mg/week	Adverse Reactions GI effects (nausea/vomiting, dyspepsia, abdominal pain, constipation, gastritis); CNS effects (headache, dizziness, vertigo, depression); Other effects (breast pain, hot flushes)  Special Instructions Use with caution in patients with severe CV disease, Raynaud’s syndrome, history of peptic ulcer or gastrointestinal bleeding Contraindicated in patients with uncontrolled hypertension and valvular abnormalities in prolonged high-dose treatment Monitor blood pressure (BP), serum prolactin, echocardiogram during treatment

Drug	Dosage	Remarks
Pegvisomant	Loading dose: 40 mg SC given under physician supervision Maintenance dose: 10 mg SC 24 hourly May adjust dose by 5-mg increments every 4-6 weeks based on IGF-1 levels Max dose: 30 mg/day	Adverse Reactions CV effects (chest pain, hypertension); GI effects (nausea, diarrhea); Other effects (peripheral edema, elevation of transaminase levels, glucose intolerance, infection, flu-like symptoms); Injection site reaction (lipohypertrophy)  Special Instructions Use with caution in patients with DM Monitor tumors that secrete GH with periodic imaging scans of the sella turcica Monitor patients for signs and symptoms of GH deficiency and monitor IGF-1 to keep it within the age-adjusted normal range by adjusting Pegvisomant dose Baseline LFTs, total bilirubin and alkaline phosphatase levels, blood glucose levels, and BP should be obtained prior to starting therapy followed by serial monitoring during therapy

Drug	Dosage	Remarks
Lanreotide acetate	Extended-release Powder for injection:  30 mg IM every 14 days May increase dose to 30 mg IM every 10 days based on GH and IGF-1 levels Autogel (solution for injection): 60-120 mg SC every 28 days Dose may be reduced, maintained or increased based on GH and IGF-1 levels If well controlled on a somatostatin analog, may treat with 120 mg every 42 or 56 days	Adverse Reactions Local effect (pain at injection site); GI effects (nausea/vomiting, abdominal pain, diarrhea); CV effects (flushing, edema, arrhythmia, bradycardia); Hepatobiliary effects (cholelithiasis, biliary sludge); Endocrine effects (hyperglycemia, hypoglycemia)  Special Instructions Autogel solution for injection is administered via deep SC route in the superior external quadrant of the buttock and injection site should alternate between the right and left side Monitor thyroid function tests (TFTs) during treatment
Octreotide (Oral)	For patients who respond to Octreotide or Lanreotide injection Initial dose: 20-30 mg PO 12 hourly May increase dose gradually by 20 mg PO 24 hourly Max dose: 80 mg/day	Adverse Reactions GI effects (nausea, abdominal pain, diarrhea, flatulence, constipation); CV effects (bradycardia, hypertension, arrhythmia); Endocrine effects (hyperglycemia, hypoglycemia, hypothyroidism); Hepatobiliary effects (cholelithiasis, biliary sludge)  Special Instructions Administered 1 hour before meals or 2 hours after meals Use with caution in patients with DM or insulinomas, CV disease, renal or hepatic impairment Gradual withdrawal is advised to assess disease activity Adjust dosage based on monthly assessment of GH and IGF-1 levels Monitor Vitamin B12 in patients on prolonged treatment
Octreotide (Short-acting)	Initial dose: : 0.05-0.1 mg SC 8-12 hourly May increase dose gradually up to 0.1-0.2 mg 8 hourly, if necessary Max dose: 1.5 mg/day	Adverse Reactions Local effect (pain at injection site); GI effects (nausea/vomiting, abdominal pain); CV effects (flushing, edema, arrhythmia, bradycardia); Endocrine effects (hyperglycemia, hypoglycemia, hypothyroidism); Hepatobiliary effects (cholelithiasis, biliary sludge) Special Instructions Use with caution in patient with gallbladder disease, DM, renal and hepatic impairment, CV disease Adjust dosage based on monthly assessment of GH and IGF-1 levels (target: GH <2.5 ng/mL; normalized IGF-1) Discontinue therapy if no improvement of symptoms or reduction of GH levels after 3 months Assess GH levels every 6 months for patients on stable doses of Octreotide Monitor TFTs and vitamin B12 levels during prolonged treatment
Octreotide  (Long-acting release [LAR] depot)	For patients controlled w/ short-acting somatostatin analog Initial dose: 20 mg IM every 4 weeks x 3 months If patients are not adequately controlled (GH >2.5 ng/mL, elevated IGF-1 and clinical symptoms) after 3 months: May increase dose to 30 mg IM every 4 weeks  If patients are adequately controlled (GH <1 ng/mL, normalized IGF-1, controlled clinical symptoms) after 3 months: May decrease dose to 10-20 mg IM every 4 weeks Max dose: 40 mg IM every 4 weeks	LAR depot preparations are Octreotide incorporated in biodegradable microspheres for prolonged actions Adverse Reactions Local effect (pain at injection site); GI effects (nausea/vomiting, abdominal pain); CV effects (flushing, edema, arrhythmia, bradycardia); Endocrine effects (hyperglycemia, hypoglycemia, hypothyroidism); Hepatobiliary effects (cholelithiasis, biliary sludge w/ prolonged use) Special Instructions Use with caution in patients with DM or insulinomas, renal and hepatic impairment, CV disease  Monitor GH and IGF-1 levels when dosage adjustments are made If starting therapy with LAR preparation, patient should be tested for tolerance and efficacy with SC preparation first It is advisable to continue SC injection for the first 2 weeks after initial LAR dose. Release occurs after 2-week lag from microspheres Ultrasonic examination of the gallbladder at 6 months intervals
Pasireotide	Initial dose: 40 mg IM every 4 weeks for 3 months then adjust dose by 20 mg increments to a max dose of 60 mg in patients whose GH and/or IGF-1 levels are not fully controlled after 3 months of treatment Max dose: 60 mg IM every 4 weeks	Adverse Reactions Metabolic effects (hyperglycemia, DM, glucose intolerance, adrenal insufficiency, increased glycosylated hemoglobin, blood glucose and γ-glutamyltransferase); GI effects (diarrhea, nausea/vomiting, abdominal pain, decreased appetite, abdominal distention); CV effects (sinus bradycardia, QT prolongation); CNS effects (headache, dizziness); Hepatobiliary effects (cholelithiasis, cholecystitis, cholestasis, increased LFTs); Other effects (fatigue, anemia, alopecia, pruritus, injection site reaction, increased blood creatine phosphokinase and lipase) Special Instructions Contraindicated in patients with severe hepatic and renal impairment, thyroid and CV diseases, patients at risk of developing QT prolongation Monitor LFTs prior to treatment and after the first 2-3 weeks, then monthly for 3 months on treatment Determine baseline fasting plasma glucose and/or HbA1c, electrocardiogram, serum K and Mg, thyroid and pituitary functions and monitor periodically during treatment Ultrasonic examination of the gallbladder before and at 6-12 months intervals Monitor for signs of hypocortisolism, pituitary function before and periodically during treatment

All dosage recommendations are for non-elderly adults with normal renal and hepatic function unless otherwise stated.   
Not all products are available or approved for above use in all countries.  
Products listed in the Drug Summary are based on indications stated in the locally approved product monographs.   
Please refer to local product monographs in Related MIMS Drugs for country-specific prescribing information.