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Maraviroc use for HIV | Mechanism of Maraviroc


Maraviroc new medicine for the treatment of HIV


Maraviroc is use as antiretroviral medication. it is the stop the growth of the HIV virus first stage. This medicine is new to the treatment of HIV / AIDS . it is also known as an entry inhibitor. This medicine is also used for the treatment of homograft bone marrow transplantation in leukemia.
Maraviroc tablets
Maraviroc tablets

Side effect

Maraviroc is common side effect like
  • Cough
  • Infection in lung
  • Fever                                                                                                                                
  • Rash
  • Stomach pain
  • Dizziness
  • Itching
  • Sleep problems
  • Muscle pain

These side effect are go away after some day use of this medicine if the problem are not cure after some time after taking medication take advice form your doctor.
Some life threatening side effect are also seen like

Hepatotoxicity

Those patients are previously affected in the liver disease please don’t take this medication with out consulting your doctor .this medicine show rash, fever, eosinophilia , elevation Ige with hepatotoxicity. Before taking this medicine you must doing some test like ALT. AST, bilirubin for avoiding the side effect. Those patient are suffer hepatitis B or C those patient are consult your doctor or pharmacist before taking the medicine.

Sever skin etching and hypersensitivity reaction

When patient take these medicine sever reaction occur in the body like stevens- jonson  syndrome (serious disorder of skin and mucous membrane) toxic epidermal necrolysis.
Immune Reconstitution syndrome

Mechanism of action

Maraviroc is use for the treatment of the HIV virus. it prevent entry of virus in to the human cell . this medicine is block the CCR5 receptor by attaching it self with CCR5 receptor.

How Maraviroc act on CCR5 receptor

HIV virus are like attack some cell which contains the CD4+ receptor-like T-helper cell, monocytes, macrophage, microglia, Langerhans and follicular cell . in the HIV virus two types of protein are present GP120 and GP41 which is helps to primary attacks the CD4+ cell . when virus enters human GP120 domain is attach with CD4 cell and then some conformational changes are occur and another domain of GP120 is bound with CCR5 receptor for the complexion of binding. After successfully binding GP41 helps virus enters into cells. CCR5 are chemokine receptors. Maraviroc are competitively bound with CCR5 receptor to prevent the binding with HIV virus with cells. So the growth of the virus are stopped.
Hiv virus are also attacks the CXCR4 which is the co-receptor of CCR5. but more interesting is when virus are enters into human cell it only binds with the CCR5 receptor not CXCR4. After replication in human body only replicant virus are binds with CCR5 receptor.

Pharmacokinetics

Absorption

If you give Maraviroc to uninfected patient plasma concentration peak is attained 0.5 to 4 hour in a single dose . this medicine are not oral dose proportional. High fat contain food are reduce the absorption of maraviroc.

Distribution

It bound with plasma protein aprox. 76% and binding capacity with albumin and alpha-1 acid glycoprotein is very slow. Volume of distribution is 194 /liter.

Metabolism

This medicine is metabolized by cytochrome P450. CYP3A is responsible for the metabolism of this medicine.

Excretion

T1/2 of Maraviroc is 14-18 hours. Excreation of this medicine is 20 % through urine and 76 % are excreated through feces.

Dose of maraviroc

Before taking this medicine patient must doing tropism test. Tropism test is doing to identify the virus are affecting to CCR5 or CXCR4 .if the virus are binds with the CXCR4 then there are no action of Maraviroc .

This medicine brand name seizentry and celsentri. This medicine are available solid and liquid dasage form . tablets or capsule are taken by orally with or without food . if the patient are not comfortblae or small child solution are given to the patient for better effect. This medicine also given with combination of other antiretroviral medicine .
Dose is adjusted by taking CYP3A inhibitor . some study say if any patient are taking 150 mg medicine with CYP3A inhibitor show the same effect if patient take 300 mg without CYP3A inhibitor.

History

Maraviroc was developed by Pfizer pharmaceutical company in united Kingdom USFDA approval get on April 2007 as new medicine for the treatment of HIV/AIDS. Fully approval for use or treatment of HIV given by USFDA on August 2007. Pfizer get the approval to European commission regulatory on septmber 2007.

Price

Selzentry tablets 300 mg price for 30 tablets price 758 dollar . celsentri 150 mg tablet price is 21.87 dollar per tablet. This medicine is very costly normal people are not take this medication. This medicine maraviroc is only manufacture Pfizer pharmaceutical.

  How HIV is treated by maraviroc?

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