PHARMACODYMICS OF ANTIVIRAL DRUGS BY Kings NDIPENDOH-2018.

INCREASING IMPACT
THROUGH
TRANSPARENCY, ACCOUNTABILITY
&
PARTNERSHIP. 1
SECGH SHISONG
18 January 2018 BY PAPA KINGS: BORN TO SERVE (BTS) 679201766

SECGH SHISONG
PROCUREMENT DEPARTMENT
ndipendoh@yahoo.co.uk
679201766 2
A PRESENTATION FROM

SECGH SHISONG
3
TOPIC

1. To enlighten audience / participants on the
replication of HIV VIRUS and the mechanism
of action of ARV drugs.
2. To reassure audience/Patients on the
effectiveness of anti-retroviral drugs
4
OBJECTIVE

1. Basic Introduction.
2. The brief morphology of HIV
virus.
3. The physiology of HIV virus.
4. Drug targets in the HIV
physiology.
5
OUTLINE OF PRESENTATION
5. Classes of anti-retroviral drugs.
6. Recommended anti-retroviral
regimens ( FIRST LINE).
7. Conclusion.
8. QUESTIONS AND ANSWER

HUMAN IMMUNODEFICIENCY
VIRUS(HIV)
18 January 2018 BY PAPA KINGS: BORN TO SERVE (BTS) 679201766 6
RNA VIRUSES
Human diseases caused
by RNA viruses include
EBOLA
INFLUENZA
HEPATITIS
MEASLES
POLIO.
AIDS

•HIV is a retrovirus with RNA.
•The replication of HIV is a multi-step
process and each step is crucial as a
POTENTIAL TARGET for anti-retroviral
drugs.
•Step 1 is infection of a CD4 positive T-
lymphocyte.
•Entry of HIV into CD4 cell requires CD4
receptors on the cell surface membrane
and co receptors such as CCR5 or

• The cell membrane of HIV is composed of two
glycoproteins which are GP120 and the trans-
membrane GP41.
• When HIV approaches a CD4 cell, GP120 binds to
the CD4 receptor and promotes further binding to a
co-receptor resulting to a conformational change in
GP120.
• This allows GP41 to unfold and insert its terminals
into the cell membrane pulling the virus toward the
CD4 cell facilitating the fusion of the membranes.18 January 2018 BY PAPA KINGS: BORN TO SERVE (BTS) 679201766 8

• The virus breaks open releasing two RNA strands
and 3 enzymes; -INTEGRASE, PROTEASE
and REVERSE TRANSCRIPTASE.
• Reverse transcriptase changes viral RNA, to a RNA-
DNA helix.
• Ribonuclase breaks down the RNA-DNA helix and
polymerase then completes the remaining DNA
strand to form a DNA helix.

• INTEGRASE transfers the viral DNA into the
CD4 nucleus and facilitates it integration into
the CD4 DNA.
• The CD4 cell DNA now contains the genetic
information of HIV.
• Activation of the cell induces transcription of
pro-viral DNA into mRNA which migrates
into the cytoplasm where building blocks for
a new virus are synthesized.18 January 2018 BY PAPA KINGS: BORN TO SERVE (BTS) 679201766 10

Enfuvirtide, inhibits the fusion of HIV to
the CD4 cell, and is licensed for cases that
have not respond to other antiretroviral
drugs.
Enfuvirtide should be combined with
potentially active antiretroviral drugs.18 January 2018 BY PAPA KINGS: BORN TO SERVE (BTS) 679201766 13
CRUCIAL DRUG TARGETS

Didanosine
Acyclovir,
Tenofovir
Valaciclovir, etc.
ESSENTIAL STAGES IN VIRAL REPLICATION & CRUCIAL DRUG TARGETS
SYNTHESIS of viral DNA from RNA can be
inhibited by NRTIs like;
lamivudine,
Stavudine,
Zalcitabine,
Zidovudine Didanosine and
Zalcitabine should not be
combined.Zidovudine antagonizes Stavudine.

ALSO SYNTHESIS of viral DNA from RNA is inhibited by NNRTIs like;
Nevirapine.
Efavirenz
Delavirdine
Hepatitis is associated with Nevirapine
Efavirenz is
associated with
neuropsychiatric
effects.

Integrase which incorporates viral
DNA into CD4 DNA can be inhibited
by zintevir and Raltegravir used
during NRTIs intolerance, drug
interactions, or resistance.
ESSENTIAL STAGES IN VIRAL REPLICATION & CRUCIAL DRUG TARGETS

Viral protease which activates immature HIV viruses
can be inhibited by protease inhibitors LIKE;
Saquinavir,
Retonavir,
Neltinavir
Abacavir,
Atazanavir
 etc.

Penetration of matured virus into new CD4 cells can be arrested by
neuraminidase antagonists like
 Zanamivir
 Laninamivir
 Etc.
 Zanamivir,
 oseltamivir,
 Peramivir
Maraviroc is an antagonist of the CCR5 chemokine receptor.

SUMMARY OF ANTI-RETROVIRAL DRUGS
 Protease
Inhibitors
 Neuramidase
inhibitors.
 CCR5 receptor
blockers.
 Fusion
inhibitors
 NRTIs
 NNRTIs,
 Integrase
Inhibitors

Recommended regimen for adults
2 NRTIs
LAMIVUDINE + TENOFOVIR
LAMIVUDINE + ZIDOVUDINE
YOUR DEVOTIONAL VISITS AT TREATMENT CENTRES WILL
ENLARGE YOUR KNOWLRDGE ON CURRENT DRUGS

2 NRTIs + 1 PI
2 NRTI 1 PI

2 NRTIs + 1NNTIs
2 NRTI 1 NNRTI

1 NRTIs + 1NNTIs
2 PI + 1 NRTIs or 1 NNRTI
1 PI +1 NRTI + NNTI
1 NRTI 1 NNRTI

YOUR STORY IS NOT YET OVER

QUESTIONS
26
THANKS FOR PARTICIPATING
&

PHARMACODYMICS OF ANTIVIRAL DRUGS BY Kings NDIPENDOH-2018.

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