Metreleptin parenteral
- Drugs List
- Therapeutic Indications
- Dosage
- Administration
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Parenteral formulations of metreleptin.
Drugs List
Therapeutic Indications
Uses
Lipodystrophy: Adjunct to diet
Adults and children over the age of 2 years with generalised lipodystrophy (Berardinelli-Seip syndrome and Lawrence syndrome).
Adults and children over the age of 12 years with partial lipodystrophy (including Barraquer-Simons syndrome), when standard treatments have failed.
Dosage
Adults
The recommended daily dose depends on the patient�s bodyweight and is adjusted based on the patient�s response to treatment. Clinical response is measured by triglyceride levels, HbA1c value and insulin requirements. Dose increases should not be made more frequently than every 4 weeks. Dose decreases based on weight loss may be made weekly.
The appropriate dose should be prescribed in both milligrams and volume in millilitres by the prescriber in order to ensure that patient and carers understand the correct dose to be injected.
Male and Female 40kg and less
Initial dose 0.06mg/kg (0.012ml/kg) daily.
Dose adjustments in increments of 0.02mg/kg (0.004ml/kg) up to a maximum daily dose of 0.13mg/kg (0.026ml/kg).
Male over 40kg
Initial dose 2.5mg (0.5ml) daily.
Dose adjustments in increments of 1.25mg (0.25ml) to 2.5mg (0.5ml) up to a maximum daily dose of 10mg (2ml).
Female over 40kg
Initial dose 5mg (1ml) daily.
Dose adjustments in increments of 1.25mg (0.25ml) to 2.5mg (0.5ml) up to a maximum daily dose of 10mg (2ml).
Children
Over 2 years
(See Dosage; Adult)
Under 2 years
Contraindicated.
Additional Dosage Information
If after 6 months a clinical response is not seen then it is important to ensure that the patient is compliant with the administration technique, is receiving the correct dose and is adhering to the diet. Before stopping treatment, consider a dose increase.
Dose increases based on incomplete clinical response in adults and children can be considered after a minimum of 6 months of treatment, allowing for lowering concomitant insulin, oral anti-diabetic and/or lipid lowering medication.
Administration
For subcutaneous injection at the same time each day.
The reconstituted solution should be injected into the abdomen, thigh or upper arm.
Contraindications
Children under 2 years
Breastfeeding
Positive HIV status
Pregnancy
Precautions and Warnings
Autoimmune disease
Children aged 2 to 12 years
Patients over 65 years
Severe infection
Diabetes mellitus
Haematological disorder
Hepatic impairment
Hypertriglyceridaemia
Leucopenia
Lymphoma
Myeloma
Neutropenia
Pancreatitis
Renal impairment
Advise ability to drive/operate machinery may be affected by side effects
Treatment to be initiated and supervised by a specialist
Rotate injection site each day when injecting the same region
Diabetic control may need adjustment
Monitor blood glucose closely in patients with diabetes mellitus
Monitor for autoimmune disorder flares
Review self injection technique every 6 months
Advise patient to report symptoms of infection immediately
Gradually withdraw over 2 weeks
Discontinue if serious allergic or anaphylactic reaction occurs
Female: Ensure adequate contraception during treatment
Female: Non-hormonal contraception advised in addition to hormonal
Advise patients with diabetes of the increased risk of hypoglycaemia
If while being treated with metreleptin a patient develops pancreatitis, it is advisable that metreleptin is continued uninterrupted, as stopping treatment abruptly may exacerbate the condition.
When discontinuing metreleptin in patients with risk factors for pancreatitis, during the 2 week tapering period, monitor triglyceride levels and consider initiating or adjusting the dose of lipid-lowering medicines as needed. Signs or symptoms of pancreatitis should be evaluated.
There is no data to support the safety and efficacy of metreleptin in patients with HIV-related lipodystrophy.
Pregnancy and Lactation
Pregnancy
Metreleptin is contraindicated during pregnancy.
The manufacturer recommends metreleptin is not used in pregnancy and in women of childbearing potential not using contraception. As the efficacy of hormonal contraceptives may be reduced if co-administered with metreleptin an additional non-hormonal contraceptive method should be considered during treatment. Animal studies have shown some reproductive toxicity. At the time of writing there is limited human data available. Abortions, stillbirths and preterm deliveries have been reported in women exposed to metreleptin during pregnancy. Risks are unknown.
Lactation
Metreleptin is contraindicated during breastfeeding.
The manufacturer advises that a decision must be made whether to discontinue breastfeeding or to discontinue or abstain from metreleptin therapy, taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman. The presence of metreleptin in human breast milk is unknown. Endogenous leptin is present in human milk. Effects on exposed infants are unknown.
Counselling
Administer at the same time every day.
Advise patient that they should use a different injection site each day when injecting in the same region.
Advise patient to report symptoms of infection immediately.
Advise patient to report any symptoms of an allergic reaction.
Advise women that metreleptin may increase their fertility due to the restoration of luteinising hormone (LH) release and that they should ensure adequate contraception during treatment.
Advise patient that dizziness and fatigue may affect ability to drive or operate machinery.
Side Effects
Abdominal pain
Acute appendicitis
Alopecia
Anaphylactic reaction
Antibody formation
Arthralgia
Bacteraemia
Blood glucose disturbances
Bruising at injection site
Cough
Decreased appetite
Deep vein thrombosis (DVT)
Development of neutralising antibodies
Diabetes mellitus
Diarrhoea
Dyspnoea
Ear infection
Elevated triglyceride levels
Erythema at injection site
Fat tissue increased
Fatigue
Gingivitis
Haemorrhage (injection site)
Headache
Hyperphagia
Hypoglycaemia
Increased glycated haemoglobin (HbA1c) levels
Influenza
Injection site reactions
Insulin resistance
Local pain (injection site)
Lymphoma
Malaise
Menorrhagia
Myalgia
Nausea
Pancreatitis
Peripheral oedema
Pleural effusion
Pneumonia
Pruritus
Rash
Sepsis
Swelling (injection site)
Tachycardia
Urticaria
Vomiting
Weight gain
Weight loss
Worsening hypertension
Overdosage
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Further Information
Last Full Review Date: March 2021
Reference Sources
Summary of Product Characteristics: Myalepta 3mg powder for solution for injection, Myalepta 5.8mg powder for solution for injection, Myalepta 11.3mg powder for solution for injection. Amryt Pharmaceuticals DAC. Revised November 2020.
NICE Evidence Services Available at: www.nice.org.uk Last accessed: 21 May 2021
Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content
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