Ritonavir

Indications
 Oral
HIV infection
Adult: Combined with other antiretrovirals: Initially, 300 mg bid for 1 day. May increase dose gradually by 100 mg bid over a period of up to 14 days to 600 mg bid.
Child: Combined with other antiretrovirals: >2 yr: 250 mg/m2 bid. Increase dose by 50 mg/m2 bid at 2-3 day intervals up to 400 mg/m2 bid. Max: 600 mg bid.
Hepatic impairment: Dosage reduction may be required.
Oral
As a pharmacokinetic enhancer
Adult: To enhance the efficacy of other protease inhibitors: 100-200 mg once or twice daily.

Special Populations: Renal/hepatic impairment: No recommended dosage adjustments.
Contraindications
 Hypersensitivity; lactation; severe hepatic impairment.
Warnings / Precautions
 Pregnancy; child; hepatic impairment; DM; haemophilia; pancreatitis. Monitor glucose, lipid, uric acid and blood counts. Ensure adequate hydration to reduce risk of nephrolithiasis. Discontinue treatment if patient develops haemolytic anaemia.
Adverse Reactions
 Syncope, orthostatic hypotension; dry mouth, mouth ulcers, throat irritation, cough; dyspepsia, nausea, vomiting, diarrhoea, taste disturbance, seizures, anxiety, sweating, fever, asthenia, fatigue, headache, dizziness, paraesthesia, myalgia, skin rashes, pruritus, renal insufficiency, anaemia, raised WBC, raised prothrombin time, lipodystrophy, pancreatitis, electrolyte imbalance.
Potentially Fatal: Hypersensitivity, anaphylaxis and Stevens-Johnson syndrome.
Overdose Reactions
 Treatment includes general supportive measures such as vital sign monitoring and observation of clinical status of the patient.
Drug Interactions
 Decreased plasma conc with phenobarbital, carbamazepine, dexamethasone, phenytoin, rifabutin and rifampicn. Increased plasma conc of certain drugs highly metabolized by CYP3A. May increase serum levels of sildenafil.
Potentially Fatal: Avoid concurrent admin of oral solution (contains alcohol) with disulfiram or metronidazole. Increased risk of myopathy when used with simvastatin or lovastatin. Concurrent use with alfuzosin may lead to serious hypotension. Increased risk of cardiac arrhythmias when used with amiodarone, cisapride, propafenone, quinidine, flecainide and pimozide. Risk of acute ergot toxicity when used with ergot derivatives. Increased risk of serious adverse reactions when used with midazolam or triazolam.
See Below for More ritonavir Drug Interactions
Food Interactions
 Co-admin with St. John's wort may lead to a substantial decrease in the plasma levels of ritonavir.
Mechanism of Actions
 Ritonavir, a selectively competitive reversible inhibitor of HIV protease, interferes with the formation of essential proteins and enzymes. Afterwhich, the formation of immature and non-infectious viruses follows. It also interferes with the production of infectious HIV and limits further infectious spread of the virus.
Absorption: Peak plasma concentrations occur about 2-4 hr after oral admin.
Distribution: Protein binding: about 98%.
Metabolism: Extensively metabolised in the liver by CYP450 isoenzymes.
Excretion: Mainly excreted in the faeces. Half-life: 3-5 hr.
Administration
 Should be taken with food.
ATC Classification
 J05AE03 - ritonavir ; Belongs to the class of protease inhibitors. Used in the systemic treatment of viral infections.
Available As
  • Ritonavir 100 mg
  • Ritonavir 250 mg
  • Ritonavir 33.3 mg
  • Ritonavir 50 mg

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