Neuraminidase Inhibitor

Aka: Neuraminidase Inhibitor, Zanamivir, Relenza, Oseltamivir, Tamiflu, Peramivir, Rapivab

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II. Indications: Covers both Influenza A and Influenza B

  1. Influenza
  2. Influenza prophylaxis

III. Contraindications: Zanamivir (Relenza)

  1. Asthma
  2. COPD

IV. Precautions

  1. Influenza A (H1N1 Strain) was resistant to Tamiflu in 2008 (Relenza was used)
  2. Symptom reduction is minimal (<14-16 hours) compared with those not treated
  3. Best efficacy if started within first 48 hours (although may still initiate later in high risk cases)
  4. Reserve use for those at highest risk of complications (although efficacy is limited even in high risk cases)
    1. Age under 2 years old or age over 65 years old
    2. Pregnancy
    3. Hospitalized patients
    4. Serious comorbidity

V. Dosing: Oseltamivir (Tamiflu)

  1. Indicated for age 2 weeks and older (reduced from 1 year in U.S. as of 2013)
  2. Suspension may be compounded if not available
    1. Pharmacist can compound or
    2. Parents can mix contents of a Tamiflu capsule ort suspension with thick liquid (and give appropriate fraction of dose)
      1. Examples: Coffee Creamer, Chocolate syrup or similar
  3. Treatment
    1. Infants (approved for 2 weeks old and over)
      1. Dose: 3 mg/kg twice daily for 5 days
    2. Children
      1. Age <1 year: Dose: 3 mg/kg/dose up to 75 mg orally twice daily for 5 days
      2. Weight <15 kg: 30 mg orally twice daily for 5 days
      3. Weight 15 to 23 kg: 45 mg orally twice daily for 5 days
      4. Weight 23 to 40 kg: 60 mg orally twice daily for 5 days
    3. Teens and Adults
      1. Weight >40kg or Adult: 75 mg orally twice daily for 5 days
    4. Renal Dosing
      1. Creatinine Clearance 30-60 ml/min
        1. Dose 30 mg twice daily for 5 days
      2. Creatinine Clearance 10-30 ml/min
        1. Dose 30 mg once daily for 5 days
      3. Dialysis
        1. Dose 30 mg after Dialysis
  4. Prevention
    1. Not routinely recommended due to medication shortage and resistance risk
      1. However, consider in high risk patients and their contacts (e.g. pregnancy, Immunocompromised)
      2. Postexposure Prophylaxis is very effective in preventing severe disease
        1. (2018) Pediatrics 142(4): e20182367 +PMID:30177511 [PubMed]
    2. Age <3 months: Discuss with specialist
    3. Age 3 months to 1 year: 3 mg/kg daily for 7-10 days
    4. Weight <15 kg: 30 mg orally daily for 7-10 days
    5. Weight 15 to 23 kg: 45 mg orally daily for 7-10 days
    6. Weight 23 to 40 kg: 60 mg orally daily for 7-10 days
    7. Weight >40kg or Adult: 75 mg orally daily for 7-10 days
    8. Advanced renal disease (Creatinine Clearance 10-30)
      1. 75 mg every other day or 30 mg orally daily for 7-10 days
    9. Nursing Home
      1. Treat for at least 2 weeks and for at least 7 days after the last infected case in Nursing Home
      2. Isolate index patient to room and follow standard droplet precautions

VI. Dosing: Peramivir (Rapivab)

  1. IV antiviral with no better efficacy than Oseltamivir (Tamiflu) except in resistant cases, at 10 times the cost
  2. Indicated in hospitalized Influenza patients with <2 days of symptoms, unable to take oral Oseltamivir (Tamiflu)
  3. Dose 600 mg IV as single dose in adults >18 years old (Category C in pregnancy)
    1. Adjust dose for renal Impairment

VII. Dosing: Zanamivir (Relenza)

  1. Contraindicated in bronchospastic disease
  2. Treatment (age 7 years and older)
    1. Dose: 10 mg (2 inhalations) twice daily for 5 days
  3. Prevention (age 5 years and older)
    1. Dose: 10 mg (1 inhalation daily) for 10 days

VIII. Efficacy: Oseltamivir (Tamiflu)

  1. Reduces myalgias, fever and flu-like symptoms by 1 day (if started in first 48 hours)
    1. As of 2014, symptom reduction appears to be as little as <16 hours than if not treated
  2. Does NOT reduce Influenza complications (Pneumonia, mortality) including in the elderly and chronically ill
    1. However is still recommended for high risk and hospitalized patients when started early
  3. References
    1. Jefferson (2012) Cochrane Database Syst Rev 1: CD008965 [PubMed]

IX. Adverse effects

  1. Nausea and Vomiting (Tamiflu)
  2. Diarrhea (common with Peramivir)
  3. Bronchospasm (with Relenza only)
  4. Neuropsychiatric effects
  5. Stevens-Johnson Syndrome (rare)

X. Resources

  1. CDC Influenza Antivirals summary
    1. http://www.cdc.gov/flu/professionals/antivirals/summary-clinicians.htm

XI. References

  1. (2014) Presc Lett 21(12): 70
  2. (2002) Pediatrics 110(6):1246-52 [PubMed]
  3. Stiver (2003) CMAJ 168(1):49-57 [PubMed]

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Related Studies

Cost: Medications

oseltamivir (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
OSELTAMIVIR PHOS 30 MG CAPSULE Generic $8.15 each
OSELTAMIVIR PHOS 45 MG CAPSULE Generic $8.10 each
OSELTAMIVIR PHOS 75 MG CAPSULE Generic $8.83 each
tamiflu (on 4/19/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
TAMIFLU 30 MG CAPSULE Generic $8.15 each
TAMIFLU 45 MG CAPSULE Generic $8.10 each
TAMIFLU 6 MG/ML SUSPENSION $2.30 per ml
TAMIFLU 75 MG CAPSULE Generic $8.83 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

Ontology: Zanamivir (C0216660)

Definition (NCI) A sialic acid-analogue neuraminidase inhibitor with antiviral activity. Administered into the respiratory tract by aerosol inhalation, zanamivir selectively binds to and inhibits influenza A and B virus neuraminidase-mediated cleavage of sialic acid residues in host cell membrane-bound glycoprotein receptors for influenza viruses, preventing the release of progeny viruses from host cell surfaces and, so, further viral replication.
Definition (NCI_NCI-GLOSS) A drug used to prevent and to treat influenza virus infections. It blocks the release of the virus from infected cells. It is a type of antiviral agent.
Definition (MSH) A guanido-neuraminic acid that is used to inhibit NEURAMINIDASE.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D053243
SnomedCT 116100000, 387010007
LNC LP101309-5, MTHU047708
English 4-Guanidino-2,4-dideoxy-2,3-dehydro-N-acetylneuraminic Acid, 5-Acetamido-2,6-anhydro-3,4,5-trideoxy-4-guanidino-D-glycero-D-galacto-non-2-enonic Acid, GANA, Zanamivir, 5-acetylamino-4-guanidino-6-(1,2,3-trihydroxypropyl)-5,6-dihydro-4H-pyran-2-carboxylic acid, Acid, 4-Guanidino-2-Deoxy-2,3-Didehydro-N-Acetylneuraminic, 2,3-Didehydro-2,4-Dideoxy-4-Guanidino-N-Acetyl-D-Neuraminic Acid, 2,3-Didehydro-2,4-Dideoxy-4-Guanidinyl-N-Acetylneuraminic Acid, 4 Guanidino 2 Deoxy 2,3 Didehydro N Acetylneuraminic Acid, 4 Guanidino Neu5Ac2en, 4-Guanidino-2,4-Dideoxy-2,3-Didehydro-N-Acetylneuraminic Acid, 4-Guanidino-2-Deoxy-2,3-Didehydro-N-Acetylneuraminic Acid, 5-Acetylamino-2,6-Anhydro-4-Guanidino-3,4,5-Trideoxy-D-Galacto-Non-Enoic Acid, 4-Guanidino-Neu5Ac2en, zanamivir, zanamivir (medication), ZANAMIVIR, Zanamivir [Chemical/Ingredient], Zanamivir (product), Zanamivir (substance)
Portuguese Zanamivir
Spanish Zanamivir, zanamivir (producto), zanamivir (sustancia), zanamivir
Russian ЗАНАМИВИР, 4-ГУАНИДИНО-2,4-ДИДЕЗОКСИ-2,3-ДИДЕГИДРО-N-АЦЕТИЛНЕЙРАМИНОВАЯ КИСЛОТА, ZANAMIVIR, 4-GUANIDINO-2,4-DIDEZOKSI-2,3-DIDEGIDRO-N-ATSETILNEIRAMINOVAIA KISLOTA
Italian Zanamivir
German 2,3-Didehydro-2,4-Dideoxy-4-Guanidino-N-Acetyl-D-Neuraminsäure, 4-Guanidino-2,4-Dideoxy-2,3-Didehydro-N-Acetylneuraminsäure, 4-Guanidino-2-Deoxy-2,3-Didehydro-N-Acetylneuraminsäure, 4-Guanidino-Neu5Ac2en, Zanamivir, 2,3-Didehydro-2,4-Dideoxy-4-Guanidinyl-N-Acetylneuraminsäure
French Zanamivir, Acide 5-acétamido-2,6-anhydro-4-guanidino-3,4,5-tridésoxy-D-glycéro-D-galacto-non-2-énonique, Acide N-acétyl-2,3-déhydro-2,4-didésoxy-4-guanidino-neuraminique
Finnish Tsanamiviiri
Czech zanamivir
Japanese ザナミビル
Swedish Zanamivir
Polish Zanamiwir
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Oseltamivir (C0874161)

Definition (NCI) A synthetic derivative prodrug of ethyl ester with antiviral activity. Osetamivir blocks neuraminidases on the surfaces of influenza viruses, interfering with host cell release of complete viral particles.
Definition (MSH) An acetamido cyclohexene that is a structural homolog of SIALIC ACID and inhibits NEURAMINIDASE.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D053139
SnomedCT 386142008, 412261005
LNC LP101308-7, MTHU036068
English ethyl (3R,4R,5S)-4-acetamido-5-amino-3-pentan-3-yloxy-cyclohexene-1-carboxylate, Oseltamivir [Chemical/Ingredient], OSELTAMIVIR, oseltamivir, Oseltamivir, Oseltamivir (product), Oseltamivir (substance)
Portuguese Oseltamivir
Spanish Oseltamivir, oseltamivir (producto), oseltamivir, oseltamivir (sustancia)
Russian ТАМИФЛУ, ОЗЕЛТАМИВИР, GS 4071, ТАМИФЛЮ, TAMIFLU, OZELTAMIVIR, TAMIFLIU
Italian Oseltamivir
German Oseltamivir
Finnish Oseltamiviiri
Czech oseltamivir
Japanese オセルタミビル
Swedish Oseltamivir
French Oséltamivir
Polish Oseltamiwir
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Relenza (C0876148)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D053243
English Relenza, Biota Brand of Zanamivir, Glaxo Wellcome Brand of Zanamivir, GlaxoSmithKline Brand of Zanamivir, Zanamivir Biota Brand, Zanamivir GlaxoSmithKline Brand, relenza
German Relenza
Czech Relenza
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Tamiflu (C0876173)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D053139
English Tamiflu, oseltamivir phosphate (Tamiflu), tamiflu
French Tamiflu
German Tamiflu
Italian Tamiflu
Czech Tamiflu
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Neuraminidase inhibitor (C1443650)

Concepts Pharmacologic Substance (T121)
SnomedCT 409228005, 409227000
English Sialidase inhibitor, Neuraminidase inhibitor, Neuraminidase inhibitor (product), Neuraminidase inhibitor (substance)
Spanish inhibidor de la neuraminidasa (producto), inhibidor de la neuraminidasa (sustancia), inhibidor de la neuraminidasa
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: peramivir (C1675326)

Definition (NCI) A cyclopentane derivative with activity against influenza A and B viruses. Peramivir is a neuraminidase inhibitor which prevents normal processing of virus particles such that virus particles are not released from infected cells.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C414210
English Peramivir, (1S,2S,3R,4R)-3-((1S)-1-acetylamino-2-ethylbutyl))-4-((aminoiminomethyl)amino-2-hydroxycyclopentanecarboxylic acid, trihydrate, peramivir, PERAMIVIR, 3-(1-acetamido-2-ethyl-butyl)-4-guanidino-2-hydroxy-cyclopentane-1-carboxylic acid
Derived from the NIH UMLS (Unified Medical Language System)

Related Topics in Pharmacology

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