PREFACE
The use of antiretroviral therapy can effectively control HIV and its
disease progress.
Successful treatment depends on how you know about and get the most from
your medicine over a long period of time.
Stay on your medication and work together with your health care providers
is a smart way to reach the goal.
This booklet aims to promote your understanding about how antiretroviral
therapy can help you live a longer and healthier life.
If you have further questions after reading this booklet, please be sure
to talk to your doctor and / or other health care providers to obtain
the feedback.
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1. The Human Immunodeficiency Virus
(HIV) life cycle HIV enters a healthy CD4 cell. Once inside the cell,
HIV coverts its own genetic material RNA into DNA using the enzyme reverse
transcriptase. This new DNA acts as a blueprint directing the infected
cell to make new virus particles. Mature viral cores are produced through
action of viral protease after budding. The new virus is then released
and can infect other healthy cells. Thus, the function of immune system
will be progressively destroyed.

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2. What is antiretroviral
therapy (ART) ?
The antiretroviral agents attack HIV at different stages of its life cycle
to inhibit HIV replication and thus bring the viral load down. Combination
therapy of two or more drug components has become the standard of treatment
of HIV disease.
Cocktail" is a colloquial term for HIV combination therapy. Highly active anti-retroviral therapy (HAART)
HAART refers to very potent regimen in which almost invariably inhibits
viral replication to an undetectable level in the blood. An example of
HAART is the use of triple therapy comprises 2 Nucleoside Reverse Transcriptase
Inhibitors (NRTI) and 1 Protease Inhibitors (PI).
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3. Effects of antiretroviral therapy
Restore
health and defense function
Decline
in AIDS morbidity, hospitalization and mortality
Improve
well-being
Improve
the quality of life
Prolong
survival of the patients with AIDS
Goals of Therapy
Suppression of viral replication to an undetectable level is the goal
of HAART. Effectiveness of the treatment is readily demonstrable by a
precipitous fall in plasma viral load and often a rise in CD4 count.
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4. What kinds of antiretroviral
therapy are available in Hong Kong? There are three classes of antiretroviral drugs
available in Hong Kong (Appendix I): (I) Nucleoside/Nucleotide Reverse Transcriptase
Inhibitors (NRTI)
Action: HIV's enzyme called reverse transcriptase convert RNA to DNA.
NRTI block reverse transcription by providing faulty building blocks that
interrupt the process.
Currently available drugs in this class are:
1. Zidovudine |
(AZT) |
(Retrovir) |
2. Didanosine |
(ddI) |
(Videx) |
3. Didanosine EC |
(ddIEC) |
(Videx EC) |
4. Lamivudine
|
(3TC) |
(Epivir) |
5. Zalcitabine
|
(ddC)
|
(Hivid) |
6. Stavudine
|
(d4T) |
(Zerit) |
7. Combivir
|
(CBV) |
|
8. Abacavir
|
(ABC) |
(Ziagen) |
9. Tenofovir
|
(TDF) |
(Viread) |
10. Trizivir |
(ABC+AZT+3TC) |
|
(II) Non-Nucleoside
Reverse Transcriptase Inhibitors (NNRTI)
Action: NNRTI stop HIV production by binding directly onto reverse transcriptase
and prevent the enzyme from converting RNA to DNA.
Currently available drugs in this class are:
1. Efavirenz
|
(EFZ)
|
(Sustiva) |
2. Nevirapine |
(NVP) |
(Viramune) |
(III) Protease Inhibitors
(PI)
Action : PI block the action of an enzyme, called Protease that cuts HIV
protein chains into specific proteins needed to assemble a new copy of
HIV. Therefore, PI prevent the cell from producing new HIV.
Currently available drugs in this class are:
1. Indinavir |
(IDV) |
(Crixivan) |
2. Saquinavir |
(SQV) |
(Hard gel-Invirase, Soft gel-Fortovase) |
3. Ritonavir |
(RTV) |
(Norvir) |
4. Nelfinavir |
(NFV) |
(Viracept) |
5. Kaletra |
(LPV+RTV) |
|
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5. When to consider
using antiretroviral therapy?
The doctor will consider using antiretroviral therapy when the infected
individual has suffered clinically or immunologically from the virus or
has at a heightened risk of disease progression. The following are the
indicators for treatment: *
- Low CD4 count
- High viral load level
- Signs of opportunistic infection
- Psychologically well prepared to comply with this
long-term treatment in order to achieve the goal of therapy
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6. Special attention
while taking antiretroviral drugs
Different drugs would have different precautions, e.g.:
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7. Nine tips on successful drug
taking
Commit
to drug taking strongly
Fit
the drug regimen into your daily activities
Keep
drugs in the places you usually go
Know
well your drug regimen in terms of the right dosage, frequency and ways
of drug taking
Bring along a bottle of water for drug taking
Make
use of an alarm clock, a pager or chart to remind yourself the time
of drug taking
Use
a pill box to contain one-day medication to remind yourself of the correct
dosage
Seek
help from health care providers to work out a drug schedule that suit
you most
Seek
support from significant others
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8. How to control over antiretroviral
therapy?
Make
a personal commitment to your therapy
Keep
in close touch with your health care providers
Attend
regular follow-up
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9. How to know whether
treatment is working?
Health monitoring blood test: CD4 count - reflect how strong immune system is Viral load measurement - measure level of HIV in blood
In general, treatment is considered to be working if the viral load is
falling or remains low, and the CD4 level is rising or remains stable.
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10. What is meant
by "undetectable" viral load?
Undetectable viral load means that HIV level is too low to be picked up
by the viral load test. HIV are still in the body and can transmit to
others through sexual and blood contact. Therefore, it is essential to
continue treatment and take precautions against its spread e.g. safer
sex.
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11. The importance
of drug adherence
The most important element in the success of your anti-HIV treatment is
to strictly adhere to the drug regimen. Good drug adherence can prevent
treatment failure and the emergence of resistance. Poor drug adherence
will lead to the development of drug resistance, limiting the effectiveness
of therapy.
Thus, the most important thing you can do to stay healthy is always to
take your drugs in the right way and at the right time.
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12. Degree of drug
adherence
The nurse counsellor usually calculates your degree of drug adherence
by:

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13. Non-adherence
can lead to drug resistance
Drug resistance means the reduction of a drug's ability to work against
HIV. Resistance is thought to occur when its target mutates, changing
its structure so that the drug can no longer bind to work as well as it
used to.
Missing doses or taking even short "drug holidays" give the
virus change its form and multiply. When you start taking your drugs again,
they may not work as well. Thus, non-adherence to drug regimen can lead
to drug resistance. Cross-resistance:
The mechanism by which HIV that has developed resistance to one drug may
also be resistant to other similar drugs.
DRUG RESISTANCE

Taking your drugs on time, every time is essential
and has its reward:
- Lower or undetectable viral load result
- Higher CD4 count, increase/maintain immune
function.

The
best way to avoid resistance is to adhere to the regimen - EVERYDAY, EVERY
TIME
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14. Signs of treatment failure
- Increase viral load
- Decrease CD4 count
- Increase risk of disease progression
- Increase hospitalization and risk of death
Missing doses or taking
the wrong doses can lead to drug resistance. You can quickly become resistant
to antiretroviral drugs if you do not take them at the right time, in
the right way and in the right dose. If drug failure is evident in terms
of clinical, immunological, or virological deterioration, change of antiretroviral
regimen is indicated.
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15. Side effects
of antiretroviral therapy
Many side effects are temporary. If you encounter unpleasant side effects,
do not discontinue the drugs or alter the dosage by yourself. You should
discuss your problem with the health care providers to understand the
alternatives of the way and time of drug taking, so that a more appropriate
drug taking plan could be developed.
Transient side effects:
- Nausea/ vomiting
- Diarrhoea
- Allergy
- Headache
- Fatigue
- Fever
- Central Nervous System (CNS) symptoms (e.g. dizziness,
insomnia, drowsiness, nightmares, inability to concentrate, etc.)
Potential long term side effects:
- Anaemia (low red blood cell count)
- Kidney stones
- Deranged liver function
- Peripheral neuropathy
- Pancreatitis
- Redistribution of fat (lipodystrophy)
- Metabolic problems (e.g. increase blood fats/ blood
sugar)
- Neutropenia (an abnormal decrease in the number of
neutrophils in the blood)
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16. Managing side
effects
Side effects to antiretroviral drugs are common during the first few weeks
of treatment. However, these symptoms will often pass as your body gets
used to the drugs. You should report any unusual symptoms to your doctor/health
care providers. If necessary, your doctor will prescribe medications to
help you get over the initial period. The following is a quick reference
for managing side effects of antiretroviral drugs.
Managing side effects: A quick reference chart
Diarrhoea |
Self
management:
-
Eat white rice, toast,
oatmeal, apple sauce, or bananas
-
Avoid spicy foods, fatty
foods, and foods that promote gas, e.g. peanuts, onion
-
Avoid high fibre food,
such as brown rice or whole grain bread
-
Drink a lot of liquid
to replace fluids lost
|
Upset
Stomach (Nausea, Vomiting, Poor Appetite) |
Self
management:
-
Eat dry foods like crackers,
toast, and dry cereal
-
Sip clear liquids like ginger
ale or juice mixed with water
-
Eat foods that appeal to you
even when you are not hungry
-
Eat small and frequent meals
-
Avoid eating very sweet , spicy
or fatty food
-
Avoid lying down directly after
a meal
-
Avoid drinking fluids immediately
before, with or after meals
-
Prescribe medications for upset
stomach
-
Prescribe medications to improve
your appetite
-
Clarify with your doctor about
your drug taking pattern and the suitable timing of meals to
avoid gastric upset
|
Feeling
Tired (Fatigue) |
Self
management:
|
Dizziness,
Confusion, and Sleeping Problems |
Self
management:
-
Consider other causes,
leading to the side effect e.g. depression
-
Enquire about the change
of drugs or time of drug taking
-
Prescribe medications
for discomfort
|
Headache |
Self
management:
-
Take adequate rest
-
Do relaxation exercise
-
Listen to light music
|
Fat
Problems (Lipodystrophy) |
Self
management:
|
Nerve
Problems, Tingling Hands and Feet (Neuropathy) |
Self
management:
-
Avoid walking or standing for
a long period of time
-
Soak your feet in cool water
-
Massage hands and feet
-
Avoid wearing tight socks or
shoes
-
Enquire the possibility
of change of drugs
-
Refer to see a neurologist
-
Prescribe medications
for neuropathy
|
Liver
Problems |
Self
management:
|
Metabolic
Problems |
Self
management:
|
Bone
Problems |
Self
management:
-
Get enough calcium and vitamin
D from food, such as fortified soy, rice milk
-
Do weight-bearing exercise like
walking or weight lifting
|
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17. The use of antiretroviral agents
for prophylaxis Effectiveness of antiretroviral drugs is already
well-proven as prophylaxis to reduce the risk of HIV transmission in two
specific health care settings:
- Perinatal infection (mother to child transmission)
- Post occupational exposure prophylaxis
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18. Conclusion By using antiretroviral therapy and adopting good
drug adherence practice, you can stay a healthy life. Be relax, take nutritious
food, do regular exercise, join a support group and develop a hobby are
some smart ways to maintain good health and improve your quality of life.
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APPENDIX I
Classes
of antiretroviral drugs
(A) Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTI)
|
Drug |
Dosage |
Potential side effects |
Remarks |
1. |
Zidovudine
(AZT)
Retrovir
100mg/cap |
200mg
3 times/day
or
300mg
2 times/day |
- Anaemia
- neutropenia
- G I intolerance
- Headache
- Insomnia
- Asthenia
- Lactic acidosis with hepatic steatosis (rare): fatigue,
severe vomiting, dyspnoea
|
- If nausea, take after a meal
|
2. |
Didanosine (ddI)
Videx
25mg/tab
100mg/tab
|
125mg or 200mg
2 times/day |
- Peripheral neuropathy
- Pancreatitis
- Nausea
- Diarrhea
- Lactic acidosis with hepatic steatosis (rare): fatigue,
severe vomiting, dyspnoea
|
- Chewed/crushed/ dissolved
- Take on empty stomach
- Take with IDV at least 1 hr apart
|
3. |
Didanosine EC (ddIEC)
Videx EC
250mg/tab
400mg/tab |
250mg or 400mg daily |
- Peripheral neuropathy
- Pancreatitis
- Nausea
- Diarrhea
- Lactic acidosis with hepatic steatosis (rare): fatigue,
severe vomiting, dyspnoea
|
- Take on empty stomach
- Take with IDV at least 1 hr apart
- Take with meal if take TDF together
|
4. |
Lamivudine
(3TC)
Epivir
150mg/tab |
150mg 2 times/day |
- Minimal toxicity
- Lactic acidosis with hepatic steatosis (rare): fatigue,
severe vomiting, dyspnoea
|
- Rapid emergence of resistant strains if non-adherent
|
5. |
Zalcitabine (ddC)
Hivid
0.75mg/tab |
0.75 mg
3 times/day |
- Peripheral neuropathy
- Stomatitis
- Pancreatitis
- Lactic acidosis with hepatic steatosis (rare): fatigue,
severe vomiting, dyspnoea
|
|
6. |
Stavudine(d4T)
Zerit
30mg/cap
40mg/cap |
30mg or 40mg
2 times/day |
- Peripheral neuropathy
- Lipodystrophy
- Lactic acidosis with hepatic steatosis (rare): fatigue,
severe vomiting, dyspnoea
- Pancreatitis
- Rapidly progressive ascending neuromuscular weakness (rare)
|
|
7. |
Combivir (CBV)
=150mg 3TC + 300mg AZT/tab |
1 tab
2 times/day |
- Anaemia
- Neutropenia
- Headache
- G I intolerance
- Insomnia
- Asthenia
- Lactic acidosis with hepatic steatosis (rare): fatigue,
severe vomiting, dyspnoea
|
|
8. |
Abacavir (ABC)
Ziagen
300mg/tab |
300mg
2 times/day |
- Hypersensitivity reaction (5% of people) symptoms may
include fever, rash, nausea, vomiting, malaise, fatigue
or loss of appetite, respiratory symptoms such as sore throat,
cough, shortness of breath
|
- If there is fever , rash, report to health care workers
at once
|
9. |
Tenofovir (TDF)
Viread
300mg/tab |
300mg daily |
- Asthenia
- Headache
- G I intolerance
- Flatulence
- Lactic acidosis with hepatic steatosis (rare): fatigue,
severe vomiting, dyspnoea
- Rare report of renal insufficiency
|
- Take with meal
- Dosage adjustment in renal insufficiency
|
10. |
Trizivir
(ABC + AZT + 3TC) |
1 tab
2 times/day |
- Anaemia
- Neutropenia
- G I intolerance
- Headache
- Insomnia
- Asthenia
- Lactic acidosis with hepatic steatosis: fatigue, severe
vomiting, dyspnoea
- Hypersensitivity reaction
|
- If there is any flu like symptom fever, rash, report to
health care workers at once
|
B) Non-Nucleoside
Reverse Transcriptase Inhibitors (NNRTI)
|
Drug |
Dosage |
Potential side effects |
Remarks |
1. |
Efavirenz (EFZ)
Stocrin, Sustiva
200mg/cap
600mg/tab |
600mg daily
(preferably at bed time) |
- Rash
- CNS symptoms: dizziness, somnolence, insomnia, drowsiness,
nightmares, hallucinations, poor concentration (usually
subside in 2-4 weeks if really appear)
- Increased transaminase levels
|
- Decrease CNS symptoms if take at bed time
- Pregnancy is contraindicated
|
2. |
Nevirapine
(NVP)
Viramune
200mg/tab |
200mg daily for 2 weeks,
then 200mg
2 times/day |
- Rash
- Symptomatic hepatitis
|
- Anti-TB drugs and oral contraceptive pills should be used
with caution
- Rapid emergence of resistant strains if non-adherent
|
(C) Protease Inhibitors
(PI)
|
Drug |
Dosage |
Potential side effects |
Remarks |
1. |
Indinavir (IDV)
Crixivan
200mg/cap
400mg/cap |
800mg Q8h 3 times/day |
- Nephrolithiasis
- G I intolerance
- Increased indirect bilirubinemia
- Misc.: headache, asthenia, blurred vision, dizziness,
rash, metallic taste, thrombocytopenia, alopecia, and hemolytic
anaemia
- Fat redistribution
- Lipid abnormalities
- Hyperglycemia
|
- Take with empty stomach
- Drink water 1.5 litre/day
- Avoid grapefruit juice
|
2. |
Saquinavir (SQV)
Invirase (hard gel)
200mg/cap
Fortovase (soft gel)
200mg/cap |
Invirase 600mg 3 times/day
Fortovase 1200mg 3 times/day |
- Headache
- G I intolerance
- Elevated transaminase enzymes
- Hyperglycemia
- Fat redistribution
- Lipid abnormalities
- Possible increased bleeding episodes in patients with
hemophilia
|
- Take after meal, preferably fatty to increase absorption
- Rifampicin & Rifabutin are contraindicated with SQV
- Fortovase (soft gel) should be refrigerated or stored
at room temperature <25簞C (up to 3 months)
|
3. |
Ritonavir (RTV)
Norvir
100mg/cap
syrup 80mg/ml |
600mg 2 times/day |
- Headache
- G I intolerance
- Paresthesias �� circumoral and extremities
- Hepatitis
- Pancreatitis
- Asthenia
- Taste perversion
- Lab.: Triglycerides increase >200%, transaminase elevation,
elevated CPK and uric acid
- Hyperglycemia
- Fat redistribution
- Lipid abnormalities
- Possible increased bleeding episodes in patients with
hemophilia
|
- Capsules should be refrigerated. If stored at room temperature
<25簞C, it is stable for
30 days
- Take after meal to improve tolerance
- Need dosage adjustment if take with SQV
- Avoid self-prescribe drugs because of drug interaction
|
4. |
Nelfinavir
(NFV)
Viracept
250mg/tab |
750mg 3 times/day
or
1250mg 2 times/day |
- Diarrhoea
- Hyperglycemia
- Fat redistribution
- Lipid abnormalities
- Serum transaminase elevation
- Possible increased bleeding episodes in patients with
hemophilia
|
|
5. |
Kaletra
= Lopinavir (LPV) 133.3mg + Ritonavir (RTV) 33.3mg/cap |
3 capsules 2 times/day |
- Diarrhoea
- G I intolerance
- Asthenia
- Elevated serum transaminases
- Hyperglycemia
- Fat redistribution
- Lipid abnormalities
- Possible increased bleeding episodes in patients with
hemophilia
|
- Take with meal
- Use additional type of contraception since Kaletra may
reduce the effectiveness of oral contraceptives
- Should be refrigerated. If stored at room temperature
<25簞C, it is stable for 2 months
|
Reference:
Department of Health, Guidelines for the Use of Antiretroviral Agents
in HIV-I-Infected Adults and Adolescents. convened by DHHS. March,
2004. P.59-64
|
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APPENDIX II
Progress
Sheet
Date |
CD4 Count |
Viral Load |
Remarks |
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APPENDIX III
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