Antiretroviral Drugs
ANTIRETROVIRAL DRUGS
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Introduction
· Antiretroviral drugs
are medications used to treat infections caused by retroviruses, primarily HIV
(Human Immunodeficiency Virus).
· These drugs do not
cure HIV but help manage the virus, enabling individuals to lead longer,
healthier lives.
· The introduction of
antiretroviral therapy (ART) has dramatically improved the prognosis of
HIV-infected patients, transforming HIV from a fatal disease to a manageable
chronic condition.
Definition
· Antiretroviral drugs
are a class of medication specifically designed to inhibit the replication of
retroviruses, including HIV.
· By targeting various
stages of the viral lifecycle, these drugs reduce the viral load in the body,
maintain immune function, and prevent the progression to AIDS (Acquired
Immunodeficiency Syndrome).
Classification
Antiretroviral drugs are classified
into several categories based on their mechanism of action:
1.
Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
o
Examples: Zidovudine, Lamivudine, Abacavir
2.
Non-Nucleoside Reverse Transcriptase Inhibitors
(NNRTIs)
o
Examples: Efavirenz, Nevirapine, Etravirine
3.
Protease Inhibitors (PIs)
o
Examples: Ritonavir, Lopinavir, Atazanavir
4.
Integrase Strand Transfer Inhibitors (INSTIs)
o
Examples: Raltegravir, Dolutegravir, Elvitegravir
5.
Fusion Inhibitors
o
Examples: Enfuvirtide
6.
CCR5 Antagonists
o
Examples: Maraviroc
Pharmacokinetics
Pharmacokinetics refers to the
absorption, distribution, metabolism, and excretion of drugs:
·
Absorption: Most antiretroviral drugs are well
absorbed orally, though some require food to enhance absorption.
·
Distribution: These drugs are widely distributed
throughout the body, including reaching the central nervous system (CNS) to
target viral reservoirs.
·
Metabolism: Primarily metabolized in the liver by
cytochrome P450 enzymes.
·
Excretion: Excreted via urine or feces,
depending on the specific drug.
Mechanism of Action
·
NRTIs: Mimic natural nucleosides, get
incorporated into viral DNA, and terminate DNA chain elongation.
·
NNRTIs: Bind to and inhibit the reverse
transcriptase enzyme directly, preventing viral RNA conversion to DNA.
·
PIs: Inhibit the protease enzyme,
preventing the maturation of new viral particles.
·
INSTIs: Inhibit the integrase enzyme,
preventing the integration of viral DNA into the host genome.
·
Fusion Inhibitors: Prevent the virus from fusing with
the host cell membrane.
·
CCR5 Antagonists: Block the CCR5 co-receptor on host
cells, preventing viral entry.
Uses
·
HIV Treatment: Primary use is in the treatment and
management of HIV infection.
·
Pre-exposure Prophylaxis (PrEP): Used in high-risk
individuals to prevent HIV infection.
·
Post-exposure Prophylaxis (PEP): Administered after
potential HIV exposure to prevent infection.
Adverse Effects
·
NRTIs: Lactic acidosis, hepatic steatosis,
lipodystrophy
·
NNRTIs: Rash, hepatotoxicity,
neuropsychiatric symptoms
·
PIs: Lipid abnormalities, insulin
resistance, gastrointestinal symptoms
·
INSTIs: Insomnia, headaches, weight gain
·
Fusion Inhibitors: Injection site reactions
·
CCR5 Antagonists: Cough, fever, liver toxicity
Contraindications
·
Known hypersensitivity to any component of the drug.
·
Severe hepatic impairment (for drugs extensively metabolized by the
liver).
·
Certain drugs are contraindicated during pregnancy (consult specific
drug guidelines).
·
Co-administration with certain medications that have severe drug
interactions.
Role of Nurse
·
Education: Educate patients about the importance
of adherence to ART, potential side effects, and managing these effects.
·
Monitoring: Regularly monitor patients for drug
effectiveness (viral load and CD4 count) and adverse effects.
·
Support: Provide emotional support and
counseling, addressing stigma and psychological impacts.
·
Coordination: Work with a multidisciplinary team to
manage comorbid conditions and optimize overall health.
·
Prevention: Educate patients about preventive
measures, such as safe sex practices and needle exchange programs.
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