Names and pronunciation
(e′-voe-lok′-ue-mab) Repatha
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Drug reference
(e′-voe-lok′-ue-mab) Repatha
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Func. class.: Antilipemic
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Chem. class.: Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor
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ACTION: Binds to low-density lipopro- teins, a human monoclonal antibody (IgG1)
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USES: Heterozygous, familial hyper- cholesterolemia, atherosclerotic disease
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CONTRAINDICATIONS: Hyper- sensitivity Precautions: Pregnancy, breastfeeding, latex sensitivity
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SIDE EFFECTS CV: Hypertension MS: Myalgia, back pain, muscle spasms INTEG: Pruritus, injection site reaction, erythema, rash
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INTERACTIONS None known Drug/Lab Test Increase: LFTs Decrease: cholesterol
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DOSAGE AND ROUTES Primary hyperlipidemia with estab- lished clinical atherosclerosis: • Adult: SUBCUT 140 mg q2wk or 420 mg monthly Homozygous familial hypercholes- terolemia: • Adult/adolescent: SUBCUT 420 mg monthly Disorder of CV system, secondary prophylaxis and primary hypercholesterolemia, alone or in combination with other lipid- lowering therapies • Adult: SUBCUT 140 mg q2wk or 420 mg monthly
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Available forms: Autoinjector 140 mg/ mL, solutions for injection 120 mg/mL, 140 mg/mL
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Administer: • Visually inspect for particulate matter and discoloration; solution is clear, col- orless to pale yellow SUBCUT route Prefilled Syringe or SureClick Autoinjector • If stored in the refrigerator, warm to room temperature for ≥30 min prior to use. Do not shake • Give into areas of the abdomen (except for a 2-inch area around the umbilicus), thigh, or upper arm that are not tender, bruised, red, or indurated • To use the 420-mg dose, give 3 injec- tions consecutively within 30 min • Rotate the site with each injection • Do not administer with other inject- able drugs at the same injection site Prefilled syringe administration • Do not pick up or pull the prefilled syringe by the plunger rod or gray needle cap. Hold the syringe by the barrel • Pull the gray needle cap off. It is nor- mal to see a drop of solution at the end of the needle. Do not remove any air bubbles in the syringe • Pinch the skin injection site to create a firm surface approximately 2 inches wide. Hold the pinch, and insert the needle into the skin using a 45- to 90-degree angle • Push the plunger rod all the way down until the syringe is empty • When done, release the plunger and gently lift the syringe off skin SureClick autoinjector administration • Do not remove the orange cap until you are ready to inject • Pull the orange cap off • Firmly push down onto the skin when ready to inject; press the gray button. A click should be heard. Keep pushing on the skin and then lift the thumb. The injection could take about 15 sec
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Assess: • Hypercholesterolemia: diet history: fat content, lipid levels (triglycerides, LDL, HDL, cholesterol); LFTs at baseline, peri- odically during treatment • Pregnancy/breastfeeding: no well- controlled studies; use only if benefits outweigh fetal risk; cautious use in breast- feeding, excretion is unknown
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Evaluate: • Therapeutic response: decreased cho- lesterol, LDL; increased HDL
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That compliance is needed • That risk factors should be decreased: high-fat diet, smoking, alcohol consump- tion, absence of exercise • To notify prescriber if pregnancy sus- pected, planned, or if breastfeeding • To report confusion, injection site reactions
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PHARMACOKINETICS Absorption 40%, distribution extensive, metabolism liver (CYP3A4), excretion urine, feces; onset 4 hr, peak 3-7 days; half- life 2-3 days
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• Adult/adolescent: SUBCUT 420 mg monthly Disorder of CV system, secondary prophylaxis and primary hypercholesterolemia, alone or in combination with other lipid- lowering therapies
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