Macimorelin (Macrilen) is a synthetic growth hormone secretagogue receptor agonist that is used in the diagnosis of adult patients with growth hormone deficiency.
Macimorelin Uses:
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Diagnostic use:
- It is indicated for diagnostic purposes in adult patients with growth hormone deficiency.
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Limitations of use:
- The safety and diagnostic performance of the drug in patients with a BMI (Body Mass Index) exceeding 40 kg/m² has not been established.
Macimorelin (Macrilen) Dose in Adults:
Macimorelin (Macrilen) Dose for Diagnostic purposes:
-
Growth hormone deficiency: Oral:
- ≤40 kg/m²:
- 5 mg/kg as single dose
- >40 kg/m²:
- Dose has not been established
- ≤40 kg/m²:
Macimorelin (Macrilen) Dose in Childrens:
Macimorelin (Macrilen) Dose for Diagnostic purposes:
-
Growth hormone deficiency: Oral:
- ≤40 kg/m²:
- 5 mg/kg as single dose
- >40 kg/m²:
- Dose has not been established
- ≤40 kg/m²:
Pregnancy Risk Category: N (Not assigned)
- It has not been used in animal reproduction studies.
Macimorelin use during breastfeeding:
- It is unknown if the drug will be excreted into breastmilk.
- Manufacturers recommend that you weigh the risks to infants and the benefits to nursing mothers of giving the drug to them.
Dose in Kidney Disease:
There are no dosage adjustments provided in the manufacturer's labeling.
Dose in Liver disease:
There are no dosage adjustments provided in the manufacturer's labeling.
Side Effects of Macimorelin (Macrilen):
-
Cardiovascular:
- Sinus bradycardia
-
Central nervous system:
- Dizziness
- Fatigue
- Headache
- Feeling hot
-
Dermatologic:
- Hyperhidrosis
-
Gastrointestinal:
- Dysgeusia
- Hunger
- Nausea
- Diarrhea
-
Respiratory:
- Upper respiratory tract infection
- Nasopharyngitis
Macimorelin (Macrilen) Rare Side effects:
-
Cardiovascular:
- Prolonged Q-T interval on ECG
Contraindications to Macimorelin (Macrilen):
The manufacturer's labeling does not contain any contraindications.
Warnings and precautions
-
Extension of QT
- Clinical trials have shown that the QTc interval lengthening of approximately 11mseconds can be observed when the drug dose is increased by two to four times the recommended dose. Avoid using other agents which may prolong the QT interval with concomitant drug administration.
-
Endocrine disorders:
- Before the drug can be administered, it must be checked for thyroid, gonadotropin, and glucocorticoid deficiency.
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Hypothalamic disease
- Hypothalamus dysfunction may cause growth hormone deficiency, which can be difficult to detect early in the disease process.
- Macimorelin stimulates release of anterior pituitary growth hormone, which can lead to false-negative results. These patients may need repeat testing.
Macimorelin: Drug Interaction
|
Bosentan |
May diminish the diagnostic effect of Macimorelin. |
|
CYP3A4 Inducers (Moderate) |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
|
Deferasirox |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
|
Efavirenz |
May lessen Macimorelin's diagnostic effectiveness. |
|
Erdafitinib |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
|
Etravirine |
May lessen Macimorelin's diagnostic effectiveness. |
|
Haloperidol |
The QTcprolonging action of haloperidol may be enhanced by QT-prolonging agents (Indeterminate Risk - Avoid). |
|
Ivosidenib |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
|
Modafinil |
May lessen Macimorelin's diagnostic effectiveness. |
|
QT-prolonging Agents (Highest Risk) |
The QTc-prolonging action of QT-prolonging Agents may be enhanced by QT-prolonging Agents (Indeterminate Risk - Avoid) (Highest Risk). Management: When these medications are combined, keep an eye out for QTc interval prolongation and cardiac arrhythmias. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
|
Sarilumab |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
|
Siltuximab |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
|
Tocilizumab |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
|
Risk Factor D (Consider therapy modification) |
|
|
Dabrafenib |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: When possible, look for substitutes for the CYP3A4 substrate. If concurrent therapy cannot be avoided, pay special attention to the substrate's clinical consequences (particularly therapeutic effects). |
|
Lorlatinib |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: Avoid taking lorlatinib at the same time as any CYP3A4 substrates for which even a small drop in serum levels of the substrate could result in therapeutic failure and negative clinical outcomes. |
|
Risk Factor X (Avoid combination) |
|
|
Aspirin |
May diminish the diagnostic effect of Macimorelin. |
|
Atropine (Systemic |
May diminish the diagnostic effect of Macimorelin. |
|
CloNIDine |
May diminish the diagnostic effect of Macimorelin. |
|
Corticosteroids (Systemic) |
May lessen Macimorelin's diagnostic effectiveness. |
|
CYP3A4 Inducers (Strong) |
May lower the level of Macimorelin in the serum. |
|
Growth Hormone Products |
May diminish the diagnostic effect of Macimorelin. |
|
Insulins |
May diminish the diagnostic effect of Macimorelin. |
|
Levodopa-Containing Products |
May diminish the diagnostic effect of Macimorelin. |
|
Nonsteroidal Anti-Inflammatory Agents |
May diminish the diagnostic effect of Macimorelin. |
|
Propylthiouracil |
May diminish the diagnostic effect of Macimorelin. |
|
Somatostatin Analogs |
May diminish the diagnostic effect of Macimorelin. |
|
St John's Wort |
May lower the level of Macimorelin in the serum. |
Monitoring parameters:
- Monitor serum GH at 30, 45, 60, and 90 minutes after the drug administration.
How to administer Macimorelin (Macrilen)?
It is administered orally. The patient must drink the entire dose within thirty minutes after fasting for at least eight hours.
Mechanism of action of Macimorelin (Macrilen):
It stimulates growth hormone release by activating Growth hormone secretagogue (hypothalamus) receptors.
Metabolism:
- It is metabolized in the liver via CYP3A4
Half-life elimination:
- 4.1 hours
Time to peak plasma concentration:
- 0.5 to 1.5 hours
International Brand Names of Macimorelin:
- Macrilen
- Macimorelin Aaterna Zentaris
- Macimorelin Aeterna Zentaris
Brand Names in Pakistan:
No Brand Names are available in Pakistan.
