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  • CLASSES

    Calcitonin Gene-Related Peptide (CGRP) Antagonists

    DEA CLASS

    Rx

    DESCRIPTION

    Injectable, selective calcitonin gene-related peptide (CGRP) receptor antagonist
    Used for migraine prophylaxis in adults
    Significantly reduces monthly migraine days

    COMMON BRAND NAMES

    Aimovig

    HOW SUPPLIED

    Aimovig Subcutaneous Inj Sol: 1mL, 70mg, 140mg

    DOSAGE & INDICATIONS

    For migraine prophylaxis.
    Subcutaneous dosage
    Adults

    70 mg subcutaneously once monthly. Some patients may benefit from a dosage of 140 mg subcutaneously once monthly.

    MAXIMUM DOSAGE

    Adults

    140 mg/month subcutaneously.

    Geriatric

    140 mg/month subcutaneously.

    Adolescents

    Safety and efficacy have not been established.

    Children

    Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

    Renal Impairment

    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    ADMINISTRATION

    Injectable Administration

    Visually inspect parenteral products for particulate matter and discoloration prior to administration whenever solution and container permit. Do not use if the erenumab solution is cloudy or discolored or contains flakes or particles. Erenumab is a clear to opalescent, colorless to light yellow solution.[63162]

    Subcutaneous Administration

    Erenumab is intended for patient self-administration. Provide proper training to patients and/or caregivers on how to prepare and administer erenumab, including aseptic technique.
    Before administration, allow erenumab to sit at room temperature for at least 30 minutes protected from direct sunlight. Do not warm using a heat source such as hot water or microwave.
    Do not shake.
    Clean injection site on the abdomen, thigh, or upper arm with an alcohol wipe, and allow skin to dry.
    Do not leave cap off the autoinjector or prefilled syringe for more than 5 minutes; this can dry out the medicine.
    Do not inject into areas where the skin is tender, bruised, red, or hard. Avoid injecting directly into raised, thick, red, or scaly skin patch or lesion, or areas with scars or stretch marks.
    If using the same body area for the 2 separate injections needed for the 140 mg dose, ensure the second injection is not at same location used for the first injection.
    Discard the autoinjector or prefilled syringe in a FDA-cleared sharps disposal container. Do not discard in household trash.
    Storage: After removing erenumab from the refrigerator, it can be stored at room temperature between 68 to 77 degrees F (20 to 25 degrees C) for up to 7 days. Do not return erenumab to the refrigerator after it has reached room temperature.[63162]
     
    Single-dose, Prefilled SureClick Autoinjector
    Pull white or orange cap straight off autoinjector.
    Do not place fingers into the green or yellow safety guards. The needle is inside the safety guard.
    Stretch or pinch skin to create a firm injection site.
    Firmly push the autoinjector down onto the skin.
    When ready to inject, press the start button; a click will be heard. The injection could take about 15 seconds. When the injection is complete, a click may be heard or felt, and the window will turn yellow.
    Remove the autoinjector from the skin.[63162]
     
    Single-dose, Prefilled Syringe
    Always hold syringe by the barrel.
    Pull gray needle cap straight out and away from body.
    Pinch injection site skin firmly between thumb and fingers.
    Hold the pinch, and insert the syringe into skin at 45 to 90 degrees.
    Using slow and constant pressure, push the plunger rod all the way down with thumb until the prefilled syringe stops moving.
    When done, release thumb, and gently lift syringe off the skin.[63162]

    STORAGE

    Aimovig:
    - Discard product if it contains particulate matter, is cloudy, or discolored
    - Discard unused portion. Do not store for later use.
    - Do not freeze
    - Protect from light
    - Refrigerate (between 36 and 46 degrees F)
    - Store in original container
    - Unrefrigerated product can be stored at temperatures not exceeding 77 degrees F for no more than 7 days prior to administration

    CONTRAINDICATIONS / PRECAUTIONS

    Latex hypersensitivity

    Erenumab is contraindicated in patients with serious hypersensitivity to erenumab or any of the excipients. Hypersensitivity reactions, including rash, angioedema, and anaphylaxis, have been reported with erenumab. Most hypersensitivity reactions were not serious and occurred within hours of administration, although some occurred more than 1 week after administration. Discontinue erenumab and begin appropriate therapy if a serious or severe hypersensitivity reaction occurs. Advise latex-sensitive patients that the needle shield within the white or orange cap of the erenumab prefilled autoinjector and the gray needle cap of the prefilled syringe contain dry natural rubber (a derivative of latex), which may cause allergic reactions in individuals with latex hypersensitivity.[63162]

    Hypertension

    Monitor patients treated with erenumab for new-onset hypertension or worsening of pre-existing hypertension during treatment. If hypertension occurs, consider discontinuing erenumab if an alternative etiology cannot be established. Cases of hypertension and worsening of pre-existing hypertension, some requiring pharmacological treatment and/or hospitalization, have been reported after erenumab use in the postmarketing setting. Many patients had pre-existing hypertension or risk factors for hypertension. Hypertension may occur at any time during treatment but was most frequently reported within 7 days of administration. In the majority of the cases, the onset or worsening of hypertension was reported after the first dose. Erenumab was discontinued in many of the reported cases.[63162]

    Pregnancy

    There are no adequate data on the developmental risk associated with erenumab use during human pregnancy. No adverse effects on offspring were observed when monkeys were given erenumab throughout pregnancy at exposures approximately 20 times those in humans at a dose of 140 mg once monthly.

    Breast-feeding

    There are no data on the presence of erenumab in human milk, the effects on the breast-fed infant, or the effects on milk production. Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for erenumab and any potential adverse effects on the breast-fed infant from erenumab or the underlying maternal condition.

    ADVERSE REACTIONS

    Severe

    alopecia / Delayed / 17.0-17.0
    angioedema / Rapid / Incidence not known
    anaphylactic shock / Rapid / Incidence not known
    anaphylactoid reactions / Rapid / Incidence not known
    cardiac arrest / Early / Incidence not known
    arrhythmia exacerbation / Early / Incidence not known

    Moderate

    constipation / Delayed / 1.0-20.0
    antibody formation / Delayed / 2.6-6.2
    oral ulceration / Delayed / Incidence not known
    erythema / Early / Incidence not known
    depression / Delayed / Incidence not known
    palpitations / Early / Incidence not known
    hypertension / Early / Incidence not known
    loss of consciousness / Rapid / Incidence not known

    Mild

    injection site reaction / Rapid / 5.0-6.0
    muscle cramps / Delayed / 0-2.0
    myalgia / Early / Incidence not known
    musculoskeletal pain / Early / Incidence not known
    arthralgia / Delayed / Incidence not known
    rash / Early / Incidence not known
    pruritus / Rapid / Incidence not known

    DRUG INTERACTIONS

    There are no drug interactions associated with Erenumab products.

    PREGNANCY AND LACTATION

    Pregnancy

    There are no adequate data on the developmental risk associated with erenumab use during human pregnancy. No adverse effects on offspring were observed when monkeys were given erenumab throughout pregnancy at exposures approximately 20 times those in humans at a dose of 140 mg once monthly.

    There are no data on the presence of erenumab in human milk, the effects on the breast-fed infant, or the effects on milk production. Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for erenumab and any potential adverse effects on the breast-fed infant from erenumab or the underlying maternal condition.

    MECHANISM OF ACTION

    Erenumab is a human immunoglobulin G2 (IgG2) monoclonal antibody that has high affinity binding to the calcitonin gene-related peptide (CGRP) receptor and antagonizes CGRP receptor function. CGRP is distributed throughout the nervous system, and it is concentrated at anatomical sites, such as the trigeminovascular system, which are involved in migraine pathophysiology. Centrally, CGRP is involved in nociceptive transmission through second and third order neurons and pain modulation in the brainstem. Peripherally, CGRP mediates vasodilation through smooth muscle receptors. CGRP concentrations are elevated during acute migraine attacks and may be chronically elevated in chronic migraineurs.

    PHARMACOKINETICS

    Erenumab is administered subcutaneously. Erenumab exhibits non-linear kinetics. Serum trough concentrations approach steady state by 3 months of dosing. At low concentrations, elimination is predominately through saturable target binding at the calcitonin gene-related peptide (CGRP) receptor; at higher concentrations, elimination is predominantly through a non-specific, non-saturable proteolytic pathway. The half-life of erenumab is 28 days.
     
    Affected cytochrome P450 isoenzymes and drug transporters: none

    Subcutaneous Route

    After single doses of 70 or 140 mg, the mean Cmax (SD) of erenumab was 6.1 (2.1) mcg/mL and 15.8 (4.8) mcg/mL, respectively. Median peak serum concentrations occurred in approximately 6 days. The estimated bioavailability was 82%. In patients with episodic migraine, Cmin (SD) was 5.7 (3.1) mcg/mL and 12.8 (6.5) mcg/mL for 70 mg monthly and 140 mg monthly, respectively. In patients with chronic migraine, Cmin was 6.2 (2.9) mcg/mL and 14.9 (6.5) mcg/mL for 70 mg monthly and 140 mg monthly, respectively.