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Anti Retroviral Drugs by Abdul Rehman

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Hafiz AbdulRehman
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28 views8 pages

Anti Retroviral Drugs by Abdul Rehman

Uploaded by

Hafiz AbdulRehman
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PDF, TXT or read online on Scribd
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Anti Retroviral Drugs or Anti-

HIV
By Abdul Rehman
3rd prof
Cadson College of Pharmacy

◾ Classification:
◾NRTIs:
Nucleotide\Nucleoside reverse transcriptase
inhibitors include drugs like zidovudine,
lamivudine & abacavir.

Mechanism of Action:
▪️RT is a RNA dependent DNA polymerase which
converts RNA into DNA double helix
▪️NRTIs are 1st phosphorylated into active form
and then are incorporated into DNA chain by RT.
▪️ Because 3 hydroxyl group is not present in
NRTIs, DNA chain can’t further grow and is
terminated

Pharmacokinetics:
▪️ Administered orally (zidovudine can also be
administered IV)
▪️ Excretion occurs through urine except
abacavir.
Therapeutic uses:
HIB treatment

Adverse effect:
▪️ Toxicities like prepheral neuropathy,
pancreatitis & lipoatropy.
▪️ Abacavir can cause hypersensitivity reaction.

Resistance:
Occurs due to mutation at viral RT codon 184.

◾NNRTIs:
Includes delaviridine & nevirapine

Mechanism of Action:
▪️ Don’t require activation
▪️Bind at allosteric site of RT and inhibit it.
Pharmacokinetics:
▪️ Oral Administration (tablet)

Therapeutic uses:
HIV treatment

Adverse effect:
▪️Skin rash
▪️ Hepatotoxicity
▪️ Psychiatric effects

◾ Entry Inhibitors:
includes Enfuvirtide &Maraviroc which is a
polypeptide

Mechanism of Action:
▪️It is a fusion inhibitor which stops virus entry
into host cell.
▪️Viral transmembrane glycoprotein Gp41 is
responsible for virus’s entry due to some
conformational changes occuring in it after
fusion.
▪️ Enfuvirtide binds to Gp41 and prevent these
conformational changes.
▪️ Maraviroc blocks CCR5 co-receptor which
facilities gp41

Pharmacokinetics:
Is a peptide so injected Subcutaneously

Therapeutic uses:
Used in HIV patients which are already on
multiple HIV medications
Adverse effect:
▪️ Injection site irritation
▪️prepheral neuropathy(numbness, weakness)
◾Integrase Inhibitors:
Includes Bictegravir & Raltegravir

Mechanism of Action:
▪️Integrase is responsible for insertion of viral
DNA into host chromosomal DNA.
▪️These drugs bind to this enzyme and prevent
the above process of integration.

Pharmacokinetics:
▪️Well orally absorbed
▪️ Metabolism occurs through glucoronidation
▪️ Excretion occurs through bile

Therapeutic uses:
HIV infection
Adverse effect:
Well tolerable so general ADRs like headache,
nausea, Diarrhea etc

Resistance:
▪️Can occur due to single point mutation in
Integrase gene.
▪️Cross resistance can also occur.

◾ Protease Inhibitors:
Includes Darunavir, Atazanavir & Indinavir

Mechanism of Action:
▪️ Viral Protease or retropepsin is responsible for
cleavage of viral polyprotien into a no. of essential
enzymes.
▪️These drugs reversibly inhibit this enzyme.
Pharmacokinetics:
▪️Fatty meals increase bioavailability.
▪️ metabolized by CYP3A4.
▪️ Metabolism is extensive and very little drug is
excreted through urine.

Therapeutic uses:
▪️HCV infection
▪️HIV infection

Adverse effect:
▪️ General
▪️ chronic administration results in fat
redistribution
▪️ Disturbances in glucose and lipid metabolism.

Resistance:
Can occur due to mutations in protease gene

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