Saturday, July 30, 2011

Oseltamivir


Mechanism of action:
  • Selectively inhibit neuraminidase activity due to sialic acid analog characteristic. Neuraminidase is deployed by viruses to enable the release of virions. As neuraminidase is inhibited, newly formed virions accumulate at the internal cell surface
  • Keep in mind that oseltamivir needs to be metabolized by hepatic metabolism to oseltamivir carboxylate  first as it is administered as a prodrug
Adverse effects:

Adults:
  • Nausea and vomiting
  • Abdominal pain
  • Bronchitis
  • Insomnia
  • Vertigo
  • Diarrhea
  • Dizziness
  • Headache
  • Cough
  • Fatigue
  • Unstable angina ( Crescendo angina )
  • Anemia
  • Pseudomembranous colitis
  • Pneumonia
  • Pyrexia
  • Peritonsillar abscess
  • Elevated liver enzymes
  • Hepatitis
  • Aches and pains
  • Dyspepsia
  • Rhinorrhea
  • Upper respiratory tract infections
Children:
  • Vomiting
  • Gastrointestinal disturbances
  • Asthma 
  • Bronchitis
  • Conjunctivitis
  • Dermatitis
  • Epistaxis
  • Ear-disorders
  • Otitis media
  • Lymphadenopathy
  • Pneumonia
  • Sinusitis
Fatal adverse effects ( may occur to both adults and children ):
  • Anaphylaxis
  • Severe dermatologic reactions
Therapeutic uses:
  • Treatment of Influenza A and B infections
  • Prophylaxis of Influenza A and B
Pharmacokinetics:
  • Readily absorbed in the gastrintestinal tract after oral administration
  • 3% protein binding (carboxylate) and 42% parent drug
  • Extensive hepatic metabolism to oseltamivir carboxylate
  • Renal excretion via urine
Drug interactions:
  • With probenecid, probenate and probenecidum. All three increase toxicity levels of oseltamivir
Special precautions:
  • Moderate renal impairment
  • Hepatic impairment
  • Pregnancy and lactation
  • Chronic cardiac disorders
  • Respiratory disorders
  • Immunocompromised patients
Contraindications:
  • Severe renal impairment
  • Hypersensitivity
Administration:
  • Oral administration, preferably with food to avoid gastrointestinal discomfort
Pregnancy class:
  • C


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