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PHARMACOLOGY

MECHANISM OF ACTION

Daruvir 300mg is an human immunodeficiency virus (HIV)-1 protease inhibitors . It specifically prohibit the separation of HIV-1 encoded Gag-Pol polyproteins in infected cells, hence Daruvir 300mg will inhibits the formation of mature virus molecule.

Absorption

the time to high plasma level is 2.5-4 hr and bioavailability without Ritonavir 37% and with Ritonavir is 82%

Distribution

Human plasma bounding is 95%

Metabolism

CYP344

ELIMINATION

Combination with Ritonavir will excreted approx 79.5% in feces and 13.9% in urine. The end excretion half life is 15hrs



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Brand : Daruvir
Ingredients : Darunavir
Strength : 300mg
Manufactured : Cipla
Package : 60 Tablets

SIDE EFFECTS

Common effects

Insomnia Itching and rashes, Change in body shape (fat). Mild nausea, Stomach ache,

Serious side effects

Severe hepatomegaly with steatosis; Chest discomfort; Wheezing; Cold sore; Signs of allergic reaction like Hives, Dyspnae, Swelling of (face, lips, throat, tongue); Increased heart rate; Lumbar pain

PRECAUTIONS

Discuss with the doctor about allergic to any drugs or Allergy to darunavir, ritonavir, or any other drug which involves about rash; hives; itching; Dyspnea; wheezing; cough; swelling of (face, lips, tongue, or throat); or any other signs. Heptotoxicity: Drug induced hepatitis is resulted with Daruvir 300mg with Ritonavir combination. When the patients with pre existing liver problems receiving the combination drug will increase risk of liver function abnormalities and serious hepatic side effects Sulfa allergy: Patient has a sulfa allergy, if you are not taking Ritonavir then talk with your doctor. It will leads to incidents and severity rash occurs.

CONTRAINDICATION

While interaction of Daruvir 300mg with Ritonavir co-administration are more based on CYP3A for clearance and increased plasma concentration causes life threatening reactions similarly with 1. Alfuzosin cause hypotension 2. Dihydroergotamine causes peripheral vasospasm sand ischemia. 3. Cisapride and pimozide causes cardiac arrhythmias 4. Midazolam and triazolam causes respiratory depression.



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Warning and precaution

Interaction Daruvir 300mg with ritonavir combined with drugs metabolized by CYP3A & CYP2D6, causes elevation of plasma concentration of these drugs which leads to cause extended therapeutic effect. Concomitant use with ritonavir are metabolized by CYP3A, drug which promote the CYP3A effect leads to elevate the clearance of darunavir & ritonavir which concluded as diminishing the plasma concentration of darunavir & ritonavir.

When Daruvir 300mg & ritonavir interaction with drugs which inhibits the CYP3A may leads to cause depleting the clearance of darunavir & ritonavir results as elevation of concentration of darunavir & ritonavir.

Combination of Daruvir 300mg with Didanosine, affect the exposure of Didanosine. To overcome the problem Didanosine should be administered one hour earlier or two hours after the dose of Daruvir 300mg Concomitant use with indinavir, causes increasing the effect of concentration of both darunavir & indinavir.


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