DRUGS ACTING ON IMMUNE SYSTEM

 Immune system  ANTIRETROVIRAL AGENTS

 Protect the people from the effects of invasion of the body by  Nursing Considerations
microscopic organisms, bacteria, virus, protozoa, molds, pollens,  All NRTI’s except Didasone should be take with food for optimal
spores tolerability
 Neutralizes, eliminates, or destroys the invading microorganisms  Didasone should be taken 1 hr before or 2 hrs after meal for
 Antibody-Mediated Immunity optimal absorption
 (Humoral immunity)  Patient with renal insufficiency should adjust dosage of NRTI’s
 Involves antigen-antibody interactions that neutralizes, eliminate except for Abacavir (creatinine clearance <50 ml/min.) ; fixed
or destroy foreign proteins dose combination should be avoided in patient with RI.
 Antigen-Antibody interactions
 Antibodies are produced by populations of B-lymphocytes ANTIRETROVIRAL AGENTS

 Side effects:
 ANTIGEN-ANTIBODY INTERACTIONS  Nausea, diarrhea, abdominal pain (these are transient and may
 Occur in the body’s internal environment improve within first 2 weeks of therapy
 The body must first be exposed to the antigen to the degree that  NRTI’s are associated with changes in the body’s metabolism
the antigen enters the body. It make the antibody exerts it’s effect secondary to mitochondrial toxicity
 ACQUIRING ANTIBOBY-MEIATED IMMUNITY  Complication: peripheral neuropathy, myopathy, pancreatitis, and
 Innate immunity  is genetically determined characteristic of an lipoatrophy
individual, group, or species
 A person either has or does not have innate immunity ZIDOVUDINE
 Example: humans have many innate immunities to viruses and
other microorganisms that cause specific diseases in animals. As a  Drug Class: Nucleoside reverse transcriptase inhibitor
result, humans are not susceptible to such diseases as hog  Trade names: ZDV, AZT, Retrovir
cholera, ASF, or any variety of animal inflictions. This type of  Pregnancy category : C
immunity cannot be developed or transferred from one person to  Dosage:
another and is not an adoptive response to exposure or invasion  Prevention of maternal-fetal HIV transmission
by foreign proteins  Maternal therapy: 100mg 5times/d until the start of labor
 ACQUIRING ANTIBODY-MEDIATED IMMUNITY  Intrapartum:
 Acquired immunity IV: 2mg/kg loading dose over 30-60 min. followed by continuous
 Is the immunity that every person’s body makes (or can receive) infusion of 1 mg/kg/h until cord is clamped. For scheduled
as an adaptive response to invasion by foreign proteins Cesarean delivery, IV 3 h before surgery
 It occurs either naturally or artificially and can be either active and
passive Dosage:
 CELL-MEDIATED IMMUNITY
 Newborn (syrup): PO: Continue dose through 6 week of age
 Cellular immunity
 Infant (full-term): PO: 4 mg/kg/dose b.i.d . (IV: 1.5 mg/kg/dose
 Involves many leukocyte actions, reactions, and interactions that
q6h)
range from the simple to the complex
 Infant (30-36wk gestation of birth) PO: 2 mg/kg/dose q12h
 ANTIRETROVIRAL AGENTS
 Infant (<30 weeks gestation at birth): PO: 2mg/kg/dose q12 h at
 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors
4wk of age 3mg/kg/dose q12h (I.V: 1.5 mg/kg/dose q12h at 4 wk
 Zidovudine Retrovir)
of age, 2-3mg/kg/dose q12h)
 Didanosine (Videx)
 A: PO: 200mg q8h or 300 mg q12h; IV: 1mg/kg q4h (ATC : 5-6
 Stavudine (Zerit)
dose/d)
 Lamivudine (Epivir)
 C: 4 wk to <18 y: PO: >30 kg: 300 mg b.i.d.: 9-29 kg: 9 mg/kgf/
 Abacavir (Ziagen)
dose b.i.d.
 Tenofovir (Viread)
 4-8 kg: 12mg/kg/dose b.i.d.
 Emtricitabine (Emtriva)
 C: 6 wk – 11 y: IV: 120 mg/m2/dose q6h or 20 mg/ m2/h;> 12y
 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors
1mg/kg/dose 14h ATC (5-6 doses/d)
 Act by interviewing with HIV viral RNA-dependent DNA
polymerase, resulting in inhibition of viral replication Contraindication
 Two of these agents are typically included I intial ART regimens
 ANTIRETROVIRAL AGENTS  Life threatening allergies to Zidovudine or it’s components
 Six fixed-dose combination products  Drug: Ganciclovi, probenecid, valproic acid may increase
 Combivir (Lamivudine/zidovudine) concentration/ adverse effects
 Trizivir (Abacavir /lamivudine/zidovudine)  Rifampin may decrease concentration/effects
 Epzicom (abacavir/lamivudine)  Lab may increase ALT, AST
 Atripla (efavirenz/ emtricitabine/ tenofovir)  CAUTION: Bone marrow compromise, renal and hepatic
 Truvada (emtricitabine/ tenofovir) dysfunction: decreased hepatic blood flow
 Complera (rilpivirine/ emtricitabine/ tenofovir)
 Tenofovir (Viread) the only nucleotide analogue
Pharmacokinetics other antiretroviral patients with HIV that was resistant to an
NNRTI and other antiretroviral agents
 Absorption: PO: 60-70%  Many drug interaction if combined with:
 Distribution: PB: 25%-38%, crosses brain barrier, crosses placenta, - Fosamprenavic/ritonavir, atazanavir/ritonavir,
peak serum levels 30-90 min carbamazepine, phenobarbital and rifampin
 Metabolism: t1/2: 0.5-3h, extensive first=pass effect in liver - Side effects: rash (1st 6 weeks of therapy), diarrhea, nausea,
 Excretion: 63%-95% in urine fatigue, abdominal pain, peripheral neuropathy, headache,
and hypertension
Therapeutic Effects/Uses - Fatal skin reactions (Stevens-Johnson syndrome)

 Management of patients with HIV infection: prevention of PROTEASE INHIBITORS

maternal-fetal HIV transmission
 Mode of action: Inhibits viral enzyme reverse transcriptase  PI-based regimens (one or two PI’s plus two NRTI’s)
 Revolutionized the treatment of HIV infection, leading to
Side Effects: sustained viral suppression, improved immunologic function, and
prolonged patient survival
 Numbness, tingling, burning, pain in the lower extremities,  9 PI’s approved by FDA:
abdominal pain, rash, GI intolerance, fever sore throat, headache,
pruritus, muscle pain, difficulty swallowing, arthralgia, insomnia, 1. Lopinavir/ritonavir (Kaletra)
confusion, mental changes, bluish brown bands on fingernails 2. Atazanavir (Reyataz)
3. Fosamprenavir (Lexiva)
Adverse Reaction 4. Tipranavir (Aptivus)
5. Darunavir (Prezista)
Nausea, vomiting, anemia (pale skin, unusual fatigue or weakness)
6. Saquinavir (Invirase)
neutropenia, (fever, child, sore throat) seizure
7. Indivavir (Crixivan)
8. Ritonavir (Norvir)
NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
9. Nelfinavir (Viracept)
 Efavirenz (Sustiva)  Act at the end of the HIV life cycle to target viral assembly by
inhibiting the activity of protease
 Delavirdine (Rescriptor)
 Darunavir or atazanavir (both “boosted” with ritonavir) first-line
 Nevirapine (Viramune)
choices of PI’s in ART (Antiretroviral therapy)
 Rilpivirine (Edurant)
 GI side effects: (may negatively affects adherence)
 Etravirine (Intelence)
- Vomiting
 Prevent viral replication by competing with binding of the reverse
- Nausea
transcriptase enzyme at the active site
- Diarrhea
Afavirenz – first choice drug in NNRTI class  Metabolic abnormalities
 Elevation of cholesterol and triglycerides
Should be used with caution in pregnancy because neural tube defects after  Fat maldistribution
early human gestational esposure  Insulin resistance (DM associated with PI use)
 Atazanavir a preferred PI no reported insulin resistance, and
CNS toxicities: elevation of cholesterol and triglycerides

 Dizziness, sedation, nightmares, euphoria, loss of concentration Atazanavir Dosage:

 Should not be used in patients with depression and history of
psychiatric or mental illness Protease Inhibitor A: PO: 300 mg plus ritonavir 100 mg
OD or 400 mg. OD if unable yo
 Given once daily at bedtime on an empty stomach or with low fat
Trade name: Reyataz tolerate ribonavir
meal to prevent excessive drug absorption Pregnancy category: B C: PO: 6-17 y>39 kg same as adult
32-38 kg 250 mg with ribonavir 100
Nevirapine mg OD 25-31 kg 200 mg with
ribonavir 100 mg OD, 15-24 kg 150
 May be used as an alternative in adult patients during pregnancy mg with ribonavir 80 mg OD
(first trimester) or in patients who are planning to conceive or are Contraindications Drug-Lab-Food Interactions
not using effective and consistent contraception Hypersensitivity to Atazanavir or any
 A/E: rash, hepatotoxicity component, concurrent use with Drug azole antifungals,
Alfuzosin, ergot derivatives, clarithromycin may increase
lovastatin, midazolam (oral), level/adverse effects, Antacids,
Delavirdine
rifamcin, simvastatin, St. John’s Wart carbamazepine, H2 antagonists,
proton pump inhibitors, rifamcin
 Has the least potent antiviral activity and is not recommended as Caution patients with pre-existing may decrease evels/effects
part of initial regimen conduction abnormalities (may
prolong PR interval), hepatitis B or C Lab: may increase liver function
Etravirine hepatic impairment tests, cholesterol, triglycerides,
glucose
 Is the first agent to show antiviral activity in treatment-
experienced patients with HIV that was resistant to an NNRTI and
Pharmacokinetics Therapeutic effects/uses - Diarrhea
- Pyrexia
Absorption: Treatment of HIV-1 infection in
PO: rapidly increased with food combination with other Dolutegravir
antiretroviral agents
Distribution: PB: 98% peak levels
 Administer OD
attained In 2-3h Mode of Action: Inhibits HIV
protease rendering enzyme  B.I.D. when given with efavirenz, fosamprenavir/ritonavir,
Metabolism: t1/2: 7-8h (9-18h when incapable of processing tipranavir/ritonavir, or rifamcin)
boosted with ritonavir) metabolized polyprotease precursors;  Common side effects: insomnia and headache
in liver Production of noninfectious
immature HIV particles results IMUNNE RECONSTITUTION INFLAMMATORY SYNDROME
Excretion: Primarily fecal elimination
(70&); urine (13%) Adverse reactions:  (IRIS) is a condition seen in some cases of AIDS or
Hypergycemia, diabetes, mellitus,
immunosuppression, in which the immune system begins to
Side effects: jaundice
Rash, nausea, cough recover, but then responds to a previously acquired opportunistic
infection with an overwhelming inflammatory response that
paradoxically makes the symptoms of infection worse
A. Assessment of the patient’s physiologic and psychosocial health
 Ritonavir boosting is a relatively new concept and one of the needs
mainstays of PI therapy B. Adherence to therapy, patients are ask achieve adherence of 95%
 Boosting new concept and mainstay of PI therapy or greater
A. Reduce dietary restrictions C. Assessment on asking the reasons for missing medications
B. Increase drug exposure, inhibit metabolism, maximize drug  Patient education should include the purpose of each medication,
levels of the co-administered PI dosage schedule, food, and fluid restrictions, recommended food
C. Reducing dose frequency, overcome viral resistance choices and storage of medications
D. Boosted regimen less complex and patients may be able to
tolerate them better Insert picture

Entry Inhibitors 1**

Enfuvirtide (Fuzeon) 2**

 Targets prevention of the fusion of the HIV and CD4 cell DRUGS FOR EYE AND EAR DISORDERS
 Combined with 3-5 other antiretroviral agents (requiring salvage
therapy) Problems related
 Taken by Subcutaneous injection
 Injuries
 DoseL 990 mg B.I.D.
 Infections
 Side effects: rash, diarrhea
 Specific disorder Glaucoma
 Allergic reactions: anaphylaxis, fever, hypotension in less than 1%
 Macular degeneration
of patients

Insert picture
CCR5 Co-Receptor Antagonists

Diagnostic Stains
Maravirac

 Frequently used to locate lesions or foreign objects, evaluate dry

 Blocks the CCR5 co-receptor needed for CCR5-tropic HIV entry
eye, or evaluate eye changes from poorly titting contact lenses
into immune system cells, preventing viral replication
 Stains may be combined with local anesthetics to allow more
 When combined with two other antiretroviral agents effective in
examination when pain is present
50 % of patients having resistance to most classes of antiretroviral
agents  May stain nasal secretions if the Lacrimal ducts are potent
 A blood test documenting he presence of the CCR5 receptor  May discolor soft contact lenses (should be removes before
(tropism test) must be obtained before starting the medication administration)
 The stain should be flushed out with Normal saline
Integrase Inhibitors
DIAGNOSTIC STAINS FOR EYE DISORDERS
Raltegravir and DOlutegravir
Fluorescein sodium (Fluorescite
 Interfere with INTEGRASE  the enzyme that HIV needs to
multiply, limiting the ability to the virus to replicate and infect  Demonstration of defects in corneal epithelium
new cells  When viewed through the cobalt blue filter of the opthalmoscope
 Combined with 2 or 3 other antiretroviral agents in both or
treatment naive and experienced patients  Under a Wood’s lamp, corneal scratches and lesions
 Side effects: (Raltegravir): administered B.I.D.  Fluoresce a bright yellow-green
- Nausea
- Headache
Rose Bengal  Opthalmic Histamines
1. Emedastine (Emadine)
 Demonstration of defects and dryness of the cojunctival tissue 2. Epinastine (Elastat)
 Defects are stained a pink-violet color  Ophalmic most cell stabilizers
1. Cromolyn (Crolom)
Topical Anesthetics 2. Nedrocromil ophthalmic (Alocril)

 Used in selective aspects of a comprehensive eye examinations, in Azalatine (Optivor)

a variety of ophthalmic procedures
Epinastine
Two most common Topical Opthalmic Anesthetics
Ketotipen (Zpditor)
a. Proparacaine HCI
b. Tatracaine HCI (pantocaine) Olopaladine (Patanol)

Both administered as drios  These drugs have both antihistamin and most cell stabilizer effects

LOCAL anesthetics A/E: bursing, headache, and stinging may occur in some patients, most
frequent adverse effects
Topical Anesthetics
Decongestants
 Corneal anesthesia
 Onset: within 1 minute  Used for patient with eye inflammation and redness due to
 Duration: 15 minutes vascular congestion of the conjunctiva
 What happens
 The blink reflex is temporarily lost Opthalmic decongestants
 Corneal epithelium become dry
 NSG. Action:  Are vasoconstrictors that manage these effects by narrowing
 Protect the eye, patch until effect of drug are gone these blood vessels
 Remove patch once sensation and the blink reflex return
Examples:
Antiinfectives
1. Phenylephrine (Neo-Synephrine Opthalmic)
Uses 2. Naphazoline (Clear eyes)

OPTHALMIC ANTIINFECTIVES
 Infections (conjunctivitis)
 Blepharitis (infection or margins of eyelid)
GENRIC (BRAND) ROUTE AND DOSAGE USES AND
 Chalazion ( infection of meibomian glands of the eyelid, may
CONSIDERATIONS
produce cysts, causing blockage of the ducts) Antibacterials A/C: Opthalmic: Instill For severe ophthalmic
 Bacterial and fungal endopthalmitis (infection and inflammation Chloramphenicol 1-2 gtts or ½ inch infections that are
of structures of the inner eye ribbon of oint a3-4 h unresponsive to other
 Hordeolum (local infection of eyelash follicles and glands on lid for 48 h: increase antibiotics
margins, STYE interval to b.i.d./t.i.d.
Effective against gram-
 Infectious keralilis (corneal infection and inflammation)
negative and gram-
 Infectious uveitis (infections of vascular layer of the eye (ciliary positive bacteria
body, choroid, and iris)
 Nursing Action: Boxed warning: Bone
 1. Before administering antiinfectives, check for previous ellergic marrow suppression
reactions and deaths have
resulted from topical
 S/E:
administration
 A. Non infectious conjunctivitis
 B. Local sin and eye irritation Continue treatment for
at least 48 h after eye
Antiinflammatories appears normal

 Require treatment with an anti-inflammatory drugs Contact lenses should

not be worn for
 NSAIDS
duration of treatment
- Corticosteroids
 IF the inflammation is secondary to a bacterial or fungal infection Pregnancy category: C
 Antibiotic or antifungal is included in the medication regimen
 Antiinflammataries should not be given if the patient has a viral
infection
 Opthalmic antihistamines and most cell stabilizer  if allergies
are the cause of eye inflammation
Decongestants eye once/d. Greater
than 1 gtt of 0.5%
3. Tetrahydrozoline (Opti-Clear) preparation b.i.d.
4. Oxymetrazoline (Ocuclear) generally does not
further reduce IOP nd
 If these are absorbed in significant amounts, their sympathetic
is not recommended
nervous system effects may pose problems for patients with
hypertension Neonates: apply a
 Patients who have narrow-angled glaucoma should not use these ribbon of 0.5%
drugs because they may contribute to acute angle closure, which ophthalmic ointment
is a medical emergency into each lower
conjunctival sac no late
than 1 hour after birth
GENERIC (BRAND) ROUTE AND DOSAGE USES AND
CONSIDERATIONS Gentamycin sulfate A/C: Sol 0.3%: 1-2 gtt For blephanlis,
(Gentamycin q4h, may increase of blepharon-conjunctivis,
For bacterial
Opthalmic Gentak gtt q 1 hr for severe bacterial conjunctivitis
conjunctivitis and
infections corneal ulcer,
corneal ulceration
dacrocystitis, keratitis,
Oint: 0.3& ½ inch kerato-conjunctivitis,
Contact lenses should
ribbon b.i.d/t.i.d. and acute
not be worn for
meibomiantis,
duration of treatment
Opthalmia neonatorum
secondary to N.
Pregnancy category: C
gonorrhea
Ciprofloxacin (Ciloxan) Solution: A/C: > 1 y: 1-2 Bacterial conjunctivitis
May cause ototoxicity
5 mg/ml sol gtt q2h while awake for
(toxic effects on eight
2 day, then q4h while
cranial nerve) which
awake for 5 days
may be permanent
Ointment: A/C:>2y:1/2
Contact lenses should
inch ribbon t.i.d. for 2
not be worn for
d. then ½ inch ribbon
duration of treatment
b.i.d. for 5 d.
Pregnancy category C
A/C:> 1 y: Day 1:2 gtt q Corneal ulcer
15 min for 6 h; then 2 Levoflaxocin A: 1- gtt max: 8 For bacterial
gtt 1 30 min for the doses/d for 5 d conjunctivitis and
rest of day corneal ulcers
(Systemic therapy is
Day2:2 gtt q 1 h required for treatment
of hordeolum,
Days: 3-14: 2 gtt q 4 h docryocystitis and
meibomiantis).
Chlamydial For chlamydial
conjunctivitis or conjunctivitis caused Contact lenses should
opthalmia neonatorum by C. trachomatis and not be worn for
caused by Chlamydia opthalmia neonatorum duration of treatment
trachomatis: Oral caused by C. trache
dosage: matis or N. gonorrhea. Pregnancy category C
Neonates/infants: CDC Prolonged use can lead
recommends 50 to acquired sensitivity Silver nitrate 1% (Dey- Neonate: instill 2 gtt in For prophylaxis of
mg/kg/d PO divided Drop) each eye within 1 h at opthalmia neonatarum
q.i.d. for 14 d Contact lenses should birth caused by N.
not be worn for Gonorrhea
Second course may be duration of treatment Sulfacetamide (Bleph- A/C:> 12yr:sol: 1 gtt q For conjunctivitis,
required CDC states 10) 1-3h while awake, then corneal ulcer, and
that topical therapy Pregnancy Category B q3-4 adjunctive therapy for
alone is inadequate chlamydial
and unnecessary when conjunctivitis:
systemic therapy Is Effectiveness of
administered sulfanomides
decreased in presence
Erythromycin Opthalmia of PABA and purulent
neonotorum: caused drainage. Hence,
by Neisseria remove exudates
gonorrheae or before instilling drops
Chlamydia
trachomatis: Opthalmic Contact lenses should
Dosage: A: instill 1-2 gtt not be worn for
or 0.25% sol into each duration of treatment
affected eye b.i.f..or
instill 1-2 gtt of 0.5% Pregnancy category C
sol into each affected
 Kerarolac (Acular) Allergic conjunctivitis: For relief of itching due
A/C:> 2 y; to allergic conjunctivitis
Tobromycin (Tobrex) A/C:>12 y oint 0.3%1/2 For external ocular and management of
inch ribbon b/i/d//t.i.d. infections Sol: 0.5%: instill 1 gtt inflammation post-
q.i.d. cataract surgery
Sol 0.3% 1-2 gtt q4h Contact lenses should
not be worn for Following cataract May increase bleeding
For severe infections duration of treatement surgery A:begin q.i.d. and delay healing
24h postop and
Oint: ½ inch ribbon 3- Pregnancy category D continue for 2 weeks Pregnancy category C
4h Corticosteroids A/C: Oint: Apply into For uveltis, allergic
Dexamethasone conjunctival sa conditions, anf
Sol: 2 gtt q30-60 min (moxldex) t.i.d./q.i.d. gradually inflammation of
until improvement: decrease to conjunctiva, cornea,
then decrease discontinue and lids
frequency
Tetracycline HCI A: instill 1-2 gtt Bacteriostatic action, Susp: instill 2 gtt q1h Not recommended for
b.i.d./q.i.d. alternative to silver while awake and q2h minor abrasions and
A: instill ½ inch ribbon nitrate for prevention during night: taper to wounds
q2-12h of opthalmia q3-q4h; then t.i.d./qi.d.
neonatorum May delay healing

Pregnancy category D Avoid use with viral

Triple antibiotic A/C:>12y: 1 c applied in Combination antibiotic infections
ophthalmic conjunctival sac q3-4h effective against many
Ointment (neomycin, gram-positive and Pregnancy category C
polymycin B sulfate gram-negative Prednisone acetate A: Initially instill 1-2gtt For uveitis: allergic
bacitracin ophthalmic) organisms (Econopred Plus) in conjunctival sac q1h conditions, burns, and
while awake, q2h inflammation of
Do not use longer than during night until conjunctiva, cornea,
10d. Contact lenses desired effect and lids
should not be worn for
duration of treatment Maint: 1 gtt q4h-6h Ma delay healing

Pregnancy category C Susp: 0.125% and 1% Avoid use with viral

Antifungals A/C: Sol , 5%: 1 gtt q2h May cause transient infections
Nalamycin (natacyn (for 3-4 d: then 1 gtt stinging or temporary
ophthalmic) q3h for 12-21 d) blurring of vision Pregnancy category C
Pregnancy category C d
Antivirals A/C: Sol 4%: Initially 1
Idoxuridine (IDU, gtt q 1h during day and
Herplex Liquifim) 12h at night when
defining improvement
occurs, use 1 gtt q2h
during day and q4h at
night, continue 3-7m
day after healing
occurs

Oint 0.5%, Place ½ inch

ribbon q4h while
awake
Sol. 1%: instill 1 gtt into For herpetic
infected eye q2h while ophthalmic infections
awake, max: 9 gtt/d and keratocojunctivitis
until corneal ulcer caused by HSV-1 and
reopthelialized , then I HSV-2
gtt q4h for 7m days,
max 21 d of treatment Pregnancy category C
Diclofenac sodium A: 1gtt to affected eye For postoperative
(valtaren ophthalmic) q.i.q. for 2 weeks, start inflammation and
24 h after cataract photophobia after
surgery cataract surgery

May increase bleeding

and delay haling

Increased risk for

keratitis and elevated
IOP

Pregnancy category C