Names and pronunciation
(nal-trex′one) ReVia, Vivitrol
Source page 932
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Individual generic drug information
Extracted information for naltrexone only.
(nal-trex′one) ReVia, Vivitrol
Source page 932
Func. class.: Opioid antagonist, antidote Func. class.: Ophthalmic vasocon- strictor Func. class.: Nonsteroidal antiinflam- matory, nonopioid analgesic
Source pages 932, 934
Chem. class.: Thebaine derivative Chem. class.: Sympathomimetic Chem. class.: Propionic acid derivative
Source pages 932, 934
Do not confuse: naltrexone/naloxone/naloxegol
Source page 932
ACTION: Competes with opioids at opioid-receptor sites ACTION: Inhibits COX-1, COX-2 by blocking arachidonate; synthesis analge- sic, antiinflammatory, antipyretic
Source pages 932, 934
USES: Blockage of opioid analge- sics; used for treatment of opiate addiction, alcoholism, opiate agonist overdose USES: Ocular congestion, irritation, itching of the eye USES: Osteoarthritis; rheumatoid, gouty arthritis; primary dysmenorrhea; ankylosing spondylitis, bursitis, tendini- tis, myalgia, dental pain, juvenile rheu- matoid arthritis
Source pages 932, 934
Extracted information for naltrexone only.
CONTRAINDICATIONS: Hyper- sensitivity, opioid dependence Precautions: Pregnancy, breastfeed- ing, children, renal disease, depres- sion, suicidal ideation, coagulopathy, respiratory depression, IV use, hepatic impairment CONTRAINDICATIONS: Preg- nancy third trimester; hypersensitivity to NSAIDs, salicylates; perioperative pain in CABG surgery; MI; stroke Precautions: Breastfeeding, children <2 yr, geriatric patients, bleeding disor- ders, GI disorders, cardiac disorders, hypersensitivity to other antiinflammatory agents, CCr <30 mL/min, asthma, renal failure, hepatic disease; corticosteroid, anticoagulant therapy
Source pages 932, 934
SIDE EFFECTS CNS: Stimulation, drowsiness, dizziness, confusion, seizures, headache, flushing, hallucinations, nervousness, irritability, suicidal ideation, syncope, anxiety CV: Rapid pulse, pulmonary edema, hyper- tension, DVT EENT: Tinnitus, hearing loss, blurred vision GI: Nausea, vomiting, diarrhea, heart- burn, hepatotoxicity, constipation, abdom- inal pain GU: Delayed ejaculation, impotence INTEG: Rash, urticaria, bruising, oily skin, acne, pruritus, inj-site reactions MISC: Increased thirst, chills, fever MS: Joint and muscle pain RESP: Wheezing, hyperpnea, nasal con- gestion, rhinorrhea, sneezing, sore throat, pneumonia SIDE EFFECTS CNS: Dizziness, drowsiness, fatigue, tremors, confusion, insomnia, anxiety, depression CV: Tachycardia, peripheral edema, pal- pitations, dysrhythmias, MI, stroke EENT: Tinnitus, hearing loss, blurred vision GI: Nausea, anorexia, vomiting, diarrhea, jaundice, hepatitis, constipation, flatu- lence, cramps, peptic ulcer, GI perfora- tion, bleeding GU: Nephrotoxicity: dysuria, hematuria, oliguria, azotemia HEMA: Blood dyscrasias, prolonged bleeding time INTEG: Purpura, rash, pruritus, sweating SYST: Anaphylaxis, Stevens-Johnson syndrome
Source pages 933, 935
INTERACTIONS Increase: Lethargy—phenothiazines Increase: Bleeding risk—anticoagulants Increase: Hepatotoxicity—disulfiram INTERACTIONS • Avoid use with adefovir, cidofovir, nephrotoxicity is increased Increase: renal impairment—ACE inhi bitors, angiotensin II antagonists Increase: toxicity risk—methotrexate, lithium, antineoplastics, probenecid, radi- ation treatment
Source pages 933, 935
Black Box Warning: GI bleeding, throm- boembolism Black Box Warning: Increase: bleeding risk—oral anticoagulants, thrombolytic agents, eptifibatide, tirofiban, clopidogrel, ticlopidine, plicamycin, SSRIs, SNRIs, tri- cyclics Increase: GI side effects risk—aspirin, corticosteroids, alcohol, NSAIDs Decrease: effect of antihypertensives, loop/thiazide diuretics N Decrease: absorption of naproxen— antacids, sucralfate, cholestyramine Drug/Herb • Bleeding risk: feverfew, garlic, ginger, ginkgo, ginseng (Panax) Drug/Lab Test Increase: BUN, alk phos, LFTs, potas- sium, glucose, cholesterol Decrease: potassium, sodium False increase: 5-HIAA, 17KS Black Box Warning: GI status: ulcera- tion, bleeding, perforation; may be fatal; obtain stool guaiac • Asthma, aspirin hypersensitivity or nasal polyps; increased risk of hypersensitivity • Renal, hepatic blood studies: BUN, creati- nine, AST, ALT, HB, LDH, blood glucose, Hct, WBC, platelets, CCr before treatment, peri- odically thereafter during long-term therapy • Monitor B/P baseline and periodically • Beers: avoid chronic use in older adults unless other alternatives are un- available; increased GI bleeding risk, peptic ulcer disease • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; avoid in ≥30 wk gestation; avoid use in breastfeeding Black Box Warning: To avoid aspirin, al- cohol, steroids, or other OTC medications without prescriber approval; increased risk of GI bleeding • To take with food or milk to prevent GI upset • To report use to all health care providers • To notify prescriber if pregnancy is planned or suspected; to avoid breastfeeding
Source pages 934, 935, 936
Extracted information for naltrexone only.
DOSAGE AND ROUTES Treatment should not be attempted until the patient has remained opioid free for 7-10 days Narcan challenge (to identify opioid-free state) • Should not be performed in a patient showing clinical signs of opioid with- drawal or urine positive for opioids • Positive signs: nausea, vomiting, dys- phoria, yawning, sweating, tearing, rhi- norrhea, stuffy nose, craving for opioids, poor appetite, abdominal cramps, un- easiness, poor ability to focus, mental lapses, muscle aches or cramps, pupil- lary dilation, piloerection, fever, changes in B/P, pulse, or temperature; anxiety, depression, irritability, backache, bone or joint pains, tremors, sensations of skin crawling • If signs or symptoms of withdrawal appear, the test is positive and no addi- tional Narcan (naloxone hydrochloride injection) should be administered • Adult: IV 0.5 mL (0.2 mg) Narcan (nal- oxone injection) (0.4 mg/mL); observe for 20 min for withdrawal; if no evidence of withdrawal, give another 1.5 mL (0.6 mg) of Narcan and observe for an additional 20 min • Adult: SUBCUT 2 mL (0.8 mg) Narcan (naloxone hydrochloride injection) (0.4 mg/mL); observe patient for 20 min for signs or symptoms of withdrawal Treatment of opioid dependence • Treatment should not be started until opioid free for 7-10 days. • Negative Narcan challenge; negative urine test • Adult: PO 25 mg naltrexone; if no withdrawal symptoms in 1 hr, then 25 mg naltrexone; if no withdrawal symp- toms, then 50 mg naltrexone daily, or 100 mg q2days or 150 mg q3days; IM 380 mg q 4 wks Treatment of alcoholism (within a com- prehensive psychosocial program) • Adult: PO 50 mg naltrexone daily × 12 wk; IM 380 mg q 4 wks DOSAGE AND ROUTES • Adult: OPHTH instill 1-2 drops in af- fected eye in the conjunctival sac every 3-4 hr, up to qid DOSAGE AND ROUTES 200 mg base = 220 mg naproxen sodium Ankylosing spondylitis, osteoarthri- tis, RA: • Adult: PO 500-1000 mg daily in 2 di- vided doses; may increase to 1500 mg/ day for limited period (<6 mo); ext rel 750-1000 mg once daily; may increase to 1500 mg daily for a limited time Child >2 yr: PO 10 mg/kg/day in 2 di- vided doses Acute gout • Adult: 750 mg once, then 250 mg q8h until attack has subsided Pain (mild to moderate), dysmenor- rhea, acute tendinopathy, bursitis: • Adult: PO 500 mg, then 250 mg q6- 8hr; max: 1250 mg/day; ext rel 1000- 1500 mg daily
Source pages 932, 933, 934, 935
Available forms: Tabs 50 mg; inj 380 mg kit Available forms: ophthalmic solution 0.012%, 0.03%, 0.1% Aleve, Anaprox , Anaprox DS , EC-Naprosyn, Maxidol , Mediproxen, Naprelan, Naprosyn Available forms: Naproxen: tabs 250, 375, 500 mg; del rel tabs (EC-Naprosyn, Naprosyn-E) 250 , 375, 500, 750 mg; oral susp 125 mg/5 mL; naproxen sodium: tabs 220, 275, 550 mg tab; capsules 200, 220 mg ; ext rel tabs (CR) 375, 500, 750 mg
Source pages 933, 934, 935
Administer: PO route • Give with food or after meals, to pre- vent nausea, vomiting • Store in tight container IM route • Do not give until opioid-free for 7-10 days to prevent opioid withdrawal (re- lapse only) • Allow to come to room temperature • IM deep in gluteal, alternate inj sites; use supplied needle to prevent inj-site reaction; aspirate before inj • Do not use IV or SUBCUT • Store refrigerated up to 1 wk, do not freeze Administer: • Store at room temperature • With food to decrease GI symptoms; take on empty stomach to facilitate absorption; give with full glass of liquid • Do not crush, break, or chew ext rel tabs • OTC for ≤10 days unless approved by prescriber • Adequately hydrate in those taking an- giotensin receptor blockers/angiotensin- converting enzyme inhibitors • Oral susp: shake well; use measuring cup provided or other calibrated de- vice
Source pages 933, 935
Extracted information for naltrexone only.
Assess: • Hepatic status: LFTs, jaundice, hepati- tis, hepatic failure, discontinue if hepatitis is diagnosed • ABGs including PO2, PCO2, LFTs, VS q3-5min • Signs of withdrawal in drug-dependent individuals; use naltrexone challenge to test opioid dependence; must be free of opioids for 7-10 days before using this product, or withdrawal symptoms can occur • Respiratory dysfunction: respiratory depression, character, rate, rhythm; if res- pirations <10/min, respiratory stimulant should be administered • Mental status: depression, suicidal ide- ation • Beers: avoid in older adults unless safer alternatives are unavailable; may cause ataxia, impaired psychomotor function • Pregnancy/breastfeeding: use only if clearly needed; use cautiously in breast- feeding Assess: • Pain: frequency, characteristics, inten- sity; relief before and 1-2 hr after product • Arthritis: range of motion, pain, swell- ing before and 1-2 hr after use • Fever: before, 1 hr after use • Cardiac status: CV thrombotic events, MI, stroke; may be fatal; not to be used with CABG
Source pages 933, 934, 935
Evaluate: • Therapeutic response: blocking opiate ingestion; successful nicotine, alcohol withdrawal Evaluate: • Therapeutic response: decreased pain, stiffness, swelling in joints; ability to move more easily
Source pages 934, 936
CLINICAL CONSIDERATIONS CLINICAL CONSIDERATIONS
Source pages 933, 935
Patient and caregiver information: • That patient must be drug-free to start treatment • That using opioid while taking this product could prove fatal because high dose is needed to overcome this antago- nist; not to self-dose with OTC products unless approved by prescriber • To carry emergency ID stating product used • That, if surgery is needed, all involved should be aware of this product • To use caution while driving or per- forming other hazardous tasks until ef- fect is known • That suicidal thoughts/behaviors may occur; to report these immediately (na-faz′oh-leen) Abalon , Clear Eyes, Clear Eyes Redness Relief, Naphcon Forte , Opti Tears , Red eye, Refresh Redness Relief Patient and caregiver information: • To report ringing, roaring in ears • To avoid driving, other hazardous ac- tivities if dizziness or drowsiness occurs • To report change in urine pattern, weight increase, edema (face, lower ex- tremities), pain increase in joints, fever, blood in urine (indicates nephrotoxicity); black stools, flulike symptoms, signs of MI, stroke • That therapeutic effects may take up to 1 mo in arthritis
Source pages 934, 936
Extracted information for naltrexone only.
PHARMACOKINETICS Metabolized by liver, excreted by kidneys; crosses placenta, excreted in breast milk; N half-life 4 hr; IM half-life 5-10 days; extensive first-pass metabolism; protein binding 21%-28% PO: Onset 15-30 min, peak 1 hr IM: Peak 2-3 days, duration >1 month PHARMACOKINETICS PO: Peak 2-4 hr, half-life 12-17 hr; metabolized in liver; excreted in urine (metabolites), breast milk; 99% protein binding
Source pages 933, 935
Filter the extracted dose blocks for this individual drug.
opioid free for 7-10 days Narcan challenge (to identify opioid-free state)
• Adult: IV 0.5 mL (0.2 mg) Narcan (nal- oxone injection) (0.4 mg/mL); observe for 20 min for withdrawal; if no evidence of withdrawal, give another 1.5 mL (0.6 mg) of Narcan and observe for an additional 20 min
Candidate age grouping · source pages 932, 933, 934, 935
opioid free for 7-10 days Narcan challenge (to identify opioid-free state)
• Adult: SUBCUT 2 mL (0.8 mg) Narcan (naloxone hydrochloride injection) (0.4 mg/mL); observe patient for 20 min for signs or symptoms of withdrawal Treatment of opioid dependence
Candidate age grouping · source pages 932, 933, 934, 935
opioid free for 7-10 days Narcan challenge (to identify opioid-free state)
• Adult: PO 25 mg naltrexone; if no withdrawal symptoms in 1 hr, then 25 mg naltrexone; if no withdrawal symp- toms, then 50 mg naltrexone daily, or 100 mg q2days or 150 mg q3days; IM 380 mg q 4 wks Treatment of alcoholism (within a com- prehensive psychosocial program)
Candidate age grouping · source pages 932, 933, 934, 935
opioid free for 7-10 days Narcan challenge (to identify opioid-free state)
• Adult: PO 50 mg naltrexone daily × 12 wk; IM 380 mg q 4 wks DOSAGE AND ROUTES
Candidate age grouping · source pages 932, 933, 934, 935
opioid free for 7-10 days Narcan challenge (to identify opioid-free state)
• Adult: OPHTH instill 1-2 drops in af- fected eye in the conjunctival sac every 3-4 hr, up to qid DOSAGE AND ROUTES 200 mg base = 220 mg naproxen sodium Ankylosing spondylitis, osteoarthri- tis, RA:
Candidate age grouping · source pages 932, 933, 934, 935
opioid free for 7-10 days Narcan challenge (to identify opioid-free state)
• Adult: PO 500-1000 mg daily in 2 di- vided doses; may increase to 1500 mg/ day for limited period (<6 mo); ext rel 750-1000 mg once daily; may increase to 1500 mg daily for a limited time Child >2 yr: PO 10 mg/kg/day in 2 di- vided doses Acute gout
Candidate age grouping · source pages 932, 933, 934, 935
opioid free for 7-10 days Narcan challenge (to identify opioid-free state)
• Adult: 750 mg once, then 250 mg q8h until attack has subsided Pain (mild to moderate), dysmenor- rhea, acute tendinopathy, bursitis:
Candidate age grouping · source pages 932, 933, 934, 935
opioid free for 7-10 days Narcan challenge (to identify opioid-free state)
• Adult: PO 500 mg, then 250 mg q6- 8hr; max: 1250 mg/day; ext rel 1000- 1500 mg daily
Candidate age grouping · source pages 932, 933, 934, 935