HIV infection Rilpivirine (Edurant): Molecular formula: C22H18N6 General

HIV Protease Inhibitors.

Name: Farah nidal alashikID: 201610691
Section: 22
Dr: Richie
Introduction:
Acquired Immunodeficiency Syndrome (HIV) is a chronic condition that can lead to death due to HIV. HIV destroys your immune system and affects your body’s ability to resist pathogenic bacteria.

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HIV is a sexually transmitted infection (STI). It can also be spread by contact with contaminated blood or from mother to son during pregnancy, delivery or breastfeeding. Without treatment, HIV may take years to weaken your immune system to the point of being infected with AIDS.

There is no cure for HIV / AIDS, but there are treatments that can significantly slow the development of the disease. These drugs have reduced AIDS deaths in many developed countries.

Non-nucleoside reverse transcriptase inhibitors (NNRTI): inhibiting the protein action needed for HIV to replicate itself. Examples include:
Efavirenz (Sustiva):
Molecular formula: C14H9ClF3NO3
General structure:

Pharmacokinetics:
low solubility and high permeability
plasma concentration tmax = 3-5 hrs
increase Cmax and AUC
Adverse effect:
Depression
Nervousness
Dizziness
Insomnia
Rash
Metabolism:
By cytochrome C450 system
Etravirine (Intelence):
Molecular formula: C20H15BrN6O
General structure:

Pharmacokinetics:
low solubility and permeability ( lipid soluble)
plasma concentration tmax: 4 hrs
Adverse effect:
Rash
Diarrhea
Steven Johnson syndrome
Rhabdomyolysis
Hepatic failure
Myocardial infection

Rilpivirine (Edurant):
Molecular formula: C22H18N6
General structure:

Pharmacokinetics:
High oral bioavailability
Low soluble and high permeability
Decrease Cmax and AUC
Adverse effect:
Headache
Rash
Insomnia
Nucleoside reverse transcriptase inhibitors (NRTI):
They are defective copies of the basic building blocks that HIV needs to make copies of itself, used to prevent the HIV from replicating. Examples include:
Abacavir (Ziagen):
Molecular formula: C14H18N6O
General structure:
lefttopPharmacokinetics:
AUC = 0-12 hrs
Protein binding moderate approximately 50%
Adverse effect:
Diarrhea
Vomiting
Muscle pain
Fever
Allergic reaction
Tenofovir(Apropovir):
Molecular formula: C9H14N5O4P
General structure:

Adverse effect:
Diarrhea
Vomiting
Stomach pain
Weakness and headache
Increase cholesterol in the blood

Tenofovir Alafenamide:
Molecular formula: C21H29N6O5P
General formula:

Pharmacokinetics:
Tmax= 1 hr post oral administration
Adverse effects:
Nausea
Headache
Rash
Diarrhea
Vomiting
Metabolism:
Metabolism to tenofovir by cathepsin A in PBMCs and macrophages
And by carboxylesterase1 in hepatocytes

HIV Protease Inhibitors.

Name: Farah nidal alashikID: 201610691
Section: 22
Dr: Richie
Introduction:
Acquired Immunodeficiency Syndrome (HIV) is a chronic condition that can lead to death due to HIV. HIV destroys your immune system and affects your body’s ability to resist pathogenic bacteria.

We Will Write a Custom Essay Specifically
For You For Only $13.90/page!


order now

HIV is a sexually transmitted infection (STI). It can also be spread by contact with contaminated blood or from mother to son during pregnancy, delivery or breastfeeding. Without treatment, HIV may take years to weaken your immune system to the point of being infected with AIDS.

There is no cure for HIV / AIDS, but there are treatments that can significantly slow the development of the disease. These drugs have reduced AIDS deaths in many developed countries.

Non-nucleoside reverse transcriptase inhibitors (NNRTI): inhibiting the protein action needed for HIV to replicate itself. Examples include:
Efavirenz (Sustiva):
Molecular formula: C14H9ClF3NO3
General structure:

Pharmacokinetics:
low solubility and high permeability
plasma concentration tmax = 3-5 hrs
increase Cmax and AUC
Adverse effect:
Depression
Nervousness
Dizziness
Insomnia
Rash
Metabolism:
By cytochrome C450 system
Etravirine (Intelence):
Molecular formula: C20H15BrN6O
General structure:

Pharmacokinetics:
low solubility and permeability ( lipid soluble)
plasma concentration tmax: 4 hrs
Adverse effect:
Rash
Diarrhea
Steven Johnson syndrome
Rhabdomyolysis
Hepatic failure
Myocardial infection

Rilpivirine (Edurant):
Molecular formula: C22H18N6
General structure:

Pharmacokinetics:
High oral bioavailability
Low soluble and high permeability
Decrease Cmax and AUC
Adverse effect:
Headache
Rash
Insomnia
Nucleoside reverse transcriptase inhibitors (NRTI):
They are defective copies of the basic building blocks that HIV needs to make copies of itself, used to prevent the HIV from replicating. Examples include:
Abacavir (Ziagen):
Molecular formula: C14H18N6O
General structure:
lefttopPharmacokinetics:
AUC = 0-12 hrs
Protein binding moderate approximately 50%
Adverse effect:
Diarrhea
Vomiting
Muscle pain
Fever
Allergic reaction
Tenofovir(Apropovir):
Molecular formula: C9H14N5O4P
General structure:

Adverse effect:
Diarrhea
Vomiting
Stomach pain
Weakness and headache
Increase cholesterol in the blood

Tenofovir Alafenamide:
Molecular formula: C21H29N6O5P
General formula:

Pharmacokinetics:
Tmax= 1 hr post oral administration
Adverse effects:
Nausea
Headache
Rash
Diarrhea
Vomiting
Metabolism:
Metabolism to tenofovir by cathepsin A in PBMCs and macrophages
And by carboxylesterase1 in hepatocytes

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