Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Packet, Oral:
Macrilen: 60 mg (1 ea) [contains saccharin sodium]
Pharmacology
Mechanism of Action
Stimulates GH release by activating GH secretagogue receptors in the pituitary and hypothalamus.
Pharmacokinetics/Pharmacodynamics
Metabolism
Hepatic via CYP3A4
Time to Peak
0.5 to 1.5 hours
Half-Life Elimination
4.1 hours
Use: Labeled Indications
Diagnostic use: Growth hormone deficiency: Diagnosis of adult growth hormone (GH) deficiency
Limitations of use: The safety and diagnostic performance has not been established for patients with BMI >40 kg/m2.
Contraindications
There are no contraindications listed in the manufacturer's labeling
Dosage and Administration
Dosing: Adult
Diagnostic use: Growth hormone deficiency: Oral:
≤40 kg/m2: 0.5 mg/kg as single dose
>40 kg/m2: Dose has not been established
Dosing: Geriatric
Refer to adult dosing.
Reconstitution
After determining dosage and number of pouches needed, dissolve entire contents of each pouch with 120 mL of water (final concentration equals 0.5 mg/1 mL). Stir solution gently for about 2 to 3 minutes (a small amount of undissolved particles will remain). Transfer volume needed for dose using a syringe (without needle) graduated in mL into a drinking glass.
Administration
Oral: Patient must drink entire dose within 30 seconds after fasting for at least 8 hours.
Storage
Store pouches under refrigeration at 2°C to 8°C (36°F to 46°F). Solution must be used within 30 minutes after preparation. Discard unused portion.
Drug Interactions
Aspirin: May diminish the diagnostic effect of Macimorelin. Avoid combination
Atropine (Systemic): May diminish the diagnostic effect of Macimorelin. Avoid combination
Bosentan: May diminish the diagnostic effect of Macimorelin. Monitor therapy
CloNIDine: May diminish the diagnostic effect of Macimorelin. Avoid combination
Corticosteroids (Systemic): May diminish the diagnostic effect of Macimorelin. Avoid combination
CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
CYP3A4 Inducers (Strong): May decrease the serum concentration of Macimorelin. Avoid combination
Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification
Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
Efavirenz: May diminish the diagnostic effect of Macimorelin. Monitor therapy
Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
Etravirine: May diminish the diagnostic effect of Macimorelin. Monitor therapy
Growth Hormone Products: May diminish the diagnostic effect of Macimorelin. Avoid combination
Haloperidol: QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of Haloperidol. Monitor therapy
Insulins: May diminish the diagnostic effect of Macimorelin. Avoid combination
Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
Levodopa-Containing Products: May diminish the diagnostic effect of Macimorelin. Avoid combination
Lorlatinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences. Consider therapy modification
Modafinil: May diminish the diagnostic effect of Macimorelin. Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May diminish the diagnostic effect of Macimorelin. Avoid combination
Propylthiouracil: May diminish the diagnostic effect of Macimorelin. Avoid combination
QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Monitor therapy
Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
Somatostatin Analogs: May diminish the diagnostic effect of Macimorelin. Avoid combination
St John's Wort: May decrease the serum concentration of Macimorelin. Avoid combination
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
Adverse Reactions
1% to 10%:
Cardiovascular: Sinus bradycardia (1%)
Central nervous system: Dizziness (4%), fatigue (4%), headache (4%), feeling hot (1%)
Dermatologic: Hyperhidrosis (1%)
Gastrointestinal: Dysgeusia (5%), hunger (3%), nausea (3%), diarrhea (2%)
Respiratory: Upper respiratory tract infection (2%), nasopharyngitis (1%)
Frequency not defined:
Cardiovascular: Prolonged Q-T interval on ECG
Warnings/Precautions
Concerns related to adverse effects:
- QT prolongation: Prolongation of the QTc interval (~11 msec) has been observed in clinical trials at doses 2- and 4-times the recommended dosage; avoid concurrent use with other agents known to prolong the QT interval.
Disease-related concerns:
- Endocrine disorders: Correct deficiencies in sex or thyroid hormones and/or glucocorticoids prior to administration.
- Hypothalamic disease: GH deficiency due to hypothalamic lesion may not be detected early in the disease process; macimorelin stimulates release of stored GH from the anterior pituitary, which may lead to false negative result. Repeat testing may be necessary.
Concurrent drug therapy issues:
- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Other warnings/precautions:
- Appropriate use: Discontinue GH therapy at least 1 week prior to administration.
Monitoring Parameters
Serum GH at 30, 45, 60, and 90 minutes following administration
Pregnancy
Pregnancy Considerations
Animal reproduction studies have not been conducted.
Patient Education
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Have patient report immediately to prescriber fast heartbeat, abnormal heartbeat, or passing out (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
