Antivirals

Drugs for Herpes virus infection

DRUG clinical use Drug type action side effect drug interaction pharmacokinetic other details
s

Acyclovir HSV/VZV Nucleoside analog binds to DNA IV: renal prodrug: renal excretion resistance:
prophylaxis in chain irreversibly tubular Valacyclovir altered viral TK
and causes chain Congeners:
AIDS termination
obstuctions or DNA pol
Herpes encepalitis because of Doconasol,
and neonatal HSV Famciclovir, Activated by viral
crystals Penciclovir
infection TK
Oral: HA, D, N
(monophosphate)
&Vom and two more
toxic: delirium, phosporilarion by
tremor, seizures, host kinases
hypotension &
nephrotoxicity
Ganciclovir CMV retinitis and Nucleoside analog inhibits DNA pol Myelosuppresion, if used with renal extcretion acyclovir
infection and causes chain hepatic myelosuppresive Distributes in analog(se activa
(treatment and termination dysfunction and drug may cause TBW+CSF igual)
prophylaxis) seizures neutropenia (ZDV,
INF-gamma)

Foscarnet CMV in inorganic Inhibits RNA seizures, sometimes deposited on no

immunocompro pyrophosphate pol, DNA pol, arrhitmia, anemia, combined with bones phosphorilation
analog divalent cation ganciclovir renal clearance
mised pts HIV RT chelation
required
acyclovir resistant Blocks resistance:
HSV/ VZV pyrophoshate mutations in DNA
binding site pol and RT
 DRUG clinical use Drug type action side effect drug interaction pharmacokinetic other details
s

Cidofovir CMV retinitis Nucleotide analog Competitively dose-dep prox. administered

Mucocutaneus (ya esta fosfatado) inhibits DNA syn. tubular with probencid
and incorporated
HSV inf in chain
nephrotoxicity to decrease
Genital warts proteinuria, nephrotoxicity
azotemia,met
acidosis and
Fanconi syn.

Drugs For Retroviruses

Drug Drug type action side effect drug interaction pharmacokinetics other

Enfurvirtide (T-20) inhibition of binds to gp41 protein pain in site of

attachment on virus injection, D,
peripheral
neuropathy

Maraviroc inhibition of Clocks CCR5 on cell cough, D, muscle oral

attachment joint pain CYP3A4 substrate
Zidovudine NRTI Competitive bone marrow adminitered with Oral all NRTIs may
(ZDV)/azitothimidin inhibition of HIV- suppression, lamivudine Cross BBB associate with mit
e (AZT)
RT1 fatigue, HA, Rifampin: renal excretion toxicity because
incorporation to the hepatitis, increases Glucorionated in liver of inhibition of pol
chain and premature myopathy, N,Vom metabolism and gamma
termination neutropenia lowers effectivity
Resistance:
mutated RT w.
lower affinity to
ZDV
fetal protection
Drug Drug type action side effect drug interaction pharmacokinetics other

Didanosine (ddl) NRTI dose-dependent avoind drugs that F is reduced by

pancreatitis cause pancreatitis food and
periferal neuropathy, (zalcitabine,
stavudined,
chelating agents
D, hepatitis, Distibutes to CSF
esophageal hydroxyurea)
eliminated by cell
ulceration, metabolism and renal
cardiomyopathy CNS excretion
toxicity,
hypertriglyceridemia

Lamivudine (3TC) NRTI dideoxynucleosid Pancreatitis in administered with kidney excretion

e that terminates pediatric pt. ZDV
the synthesis of Trimethoprimsulfame
DNA and also thoxazole decreases
renal excretion and
inhibits RT elevates serum
does not affect levels
mtDNA

Staduvine (d4T) NRTI same ase SDV but Periferal neuropathy, Vincristine: oral, penetrates BBB
also inhibits celular lactic acidosis with chemotherapy drug, and half of the drug
DNA pol beta and hepatic steatosis increases toxicity is excreted in urine
gamma

Tenofovir NRTI igual que los GI probs,HA, prodrug: tenofovir HL: 60hrs
nucleotide analog of otros NRTIs Tenofovir- disopoxilfumarate glomerular filtration
adenine only needs two associated coadm with and active tubular
phosphorilations secretion.
proximal rebal emtricitabine
tubulopathy may impede
(excessive renal elimination of
acyclovir and
Ca and PO3 loss ganciclovir
and vit D defects)
osteomalacia
Drug Drug type action side effect drug interaction pharmacokinetics other

Zalcitabine (ddC) NRTI action similar to ZDV priferal neuropathy, aminogycosides, food reduces
analog of pancreatitis, amphotecin B, absorption
deoxtcytidine esophaguarl urina and fecal
ulceration, stomatitis,
foscarnet reduce
clearance elimination
arthralgias
no pancretitis
causing drugs

Delavirdine NNRTI noncompetitive NNRIs usually decresed BL: ddl, oral, highly lipophilic, inhibits metabolism
inhibitors of HIV- cause GI antacids, reach CNS, of CYP3A4 and
extensively CYP2D6
RT1 intolerance and phenytoin, metabolised before
do not require rash, HA, N,F and rifampin, undergoing fecal
phosphorilation D nelfinavir annd renal excretion
do not incorporate to increased BL:
viral DNA Rash azole antifungals,
teratogenic in macrolide
pregnancy antibiotics

increased toxicity:
astemizol,benzod
iazepins,
cisapride,
rifabutin
rifampin/ rifabutin:
increase
delaviridine
metabolism
Drug Drug type action side effect drug interaction pharmacokinetics other

Efavirenz NNRTI " toxicity increases given with: HL:40hrs should be taken on a
if taken with a lamivudine and ZDV metabolized bye empty stomach
high fat meal CYP3A4 and
CNS dysfunction, Cyp2B6
rash, elevation of remainder eliminated
plasma cholesterol, in feces
teratogenis on first
trimester of
pregnancy

Nevirapine NNRTI " liver damage, rash, acelerates metabolized by Used for fetal
allergies, Steve- metabolism and CYP3A4 protection during
johnson syndrome decrease effects of BL increases:
contraceptive
labor
cimetidine, inducer of CYP450
steroids and PIs macrolide, rifampin

Etravine NNRTI (newest) inhibition of RT that Most common: substrate and this drug and
are resistant to first rash, N, D inducer of Rilpivirine wiggle and
generation NNRTIs Less com: blurred jiggle themselves into
Cyp3A4 the pockets of
vision, numbness, inhibitor of CYP2C9
tingling, pain, mutated RT
and Cyp2C19
dizziness, HA,
nervousness,
pounding in ears,
weakness of
extremities
Drug Drug type action side effect drug interaction pharmacokinetics other

Atazanavir PI Inhibits the cleave of D, N, Vom, Abd pain, CSF and seminal should be taken
Gag-Pol and viral HA, periferal fluids, biliary with a light meal
proteins can't be neuropathy, rash, elimination
formed hyperbilirubinemia
beacause of UGT i required acid
environment to
be absorbed
inhibits CYP3A4 and
CYP2C9

Darunavir PI D, HA, rahs, Abd administered with inhibits and is Hay que tener
pain, N, Vom, Ritonavir metabolised by cuidado con los
anorexia pacientes con
Cyp3A4 sulfonamide allergies
HL:15hrs
excretion unrine and
feces

Fosamprenavir PI " HA,N,D,perioral prodrug of HL: 7-11hrs high fat meals

paresthesis, amprenavir CYP3A4 metabolized decrease
depression, rashes,
absorption
Inducer and inhibitor
of CYP3A4
Drug Drug type action side effect drug interaction pharmacokinetics other

Indunavir PI highest CSF nefrolithiasis hepatic requires acid

penetration (piedra, hay que metabolism environment to be
absorbed so empty
esta bn inhibits CYP3A4 stomach or small low
hidratado) fat, low protein meal
Bening
hyperbilirubinemi
a
trombocytopenia,
aminitransferase
elevation,
N,D,insomnia, dry
throat and skin
Nelfinavir PI " D, N, gas, metabolized in liver 98%protein
stomach pain, bye CYPs and bound
excretion in feces EMS impurities have
loss of appetite, and urine
rash, hives, been extracted
itching, difficulty
breathing and
swallowing
teratogenic in preg
Ritonavir PI " asthesia, GI and Metabolite: metabolized in liver 99% protein
neuro distubances, isopropylthiazole bound
N, D, Vom, anorexia,
abd pain, taste
oxidation
perversion, metabolite (M-2) Read powerpoint s.
circumoral and 51
periferal paresthesis anticonvulsants
and rifamycins
reduce serum
levels,
Azole antifungals,
cimetidine,
erythromycin
Drug Drug type action side effect drug interaction pharmacokinetics other

increase serum
levels

Saquanivir PI " Abd pain, N, D, azole, antifungals, low F has to be taken 2

dyspepsia and clarithromycin, Substrate and hrs fates high fat
rhinitis grapefruit juice,
indinavir and ritonavir
inhibitor of meal
increase plasma CYP3A4 98%prot bound
levels excretion: feces

Tipranavir PI D, Vom, N, Abd ain, must be taken with Low F but increased have to be careful
rash (maculopapular ritonavir to achieve with high fat meal with patients with
or urticarial) serum levels sulfa allergies
Respiratory infection drugs (influenza A and RSV)
Drug type of drug clinical Action pharmacokineticts adverse effects other

Amantidine/ Influenza A prevents uncoating of oral Amntanidine: resistance: altered

Rimatidie prophylactic and influenza vision, metabolized in liver release of Dopa M2 or hemagglutinin
treatment (before 48 binds to M2 proton
hrs) channel
in CNS
(nervousenes,
ansiedad,
insomnia, dif
concentrating)

Neuroaminidase Influenza A y B analogs of sialic oseltamivir: oral broncospasm should be taken

inhibitors acidinterfears Zanamivir: nasal, (zanamivir) within 48hrs of
(zanamivir/oseltami rapid renal clearance symptoms
vir)
with release
halts spread of not recommended for
infection within patients with airway
respiratory tract, diseases
inhibit replication of
influenza A and B
Ribavirin synthetic guano sin Influenza A y B, inhibits replicarion IV, Aerosol adm dose related anemia, should not be
analog RSV, hepatitis of DNA and RNA Metabolized and myelosuppresion, combined with ZDM
excreted in urine aerosol may cause
viruses, conjunctival and
Inhibits influenza bronchial irritation,
RNA pol and HIV- Teratogenic on
RT pregnancy
prevents caping of
mRNA and blocks
RNAdependant RNA
pol
 Drug Clinical action pharmacokinetis adverse effects other

Interferons (IFN) IFNalpha2a and 2b: inhibits protein IV, eliminated by local Fever, lethargy,
Hepatitis C translation inactivation bonemarrow
INF alpha: HCV, expression of PKR with depression,
HepB (w. Ribavirin) dsRNA, PKR Congestive heart
phosphorilates a
Kaposis sarcoma, component of host
failure, acute
papillomatosis,genita translational machinery, hypersensitivity
l warts, HZ turns off protein reactions
synthesis and production
INF beta: MS of virus infected cells toxicity: flulike sym,
neutropenia,fatigue and
myalgia, alopesia,
hearing loss, thyroid
dysfunction, mental
confusion and
depression
adefovir dipivoxil Hep B inhibits HBV DNA pol renal elimination nephrotoxicity, lactic prodrug of adefovir
and incorporation, acidosis, sever
premature termination hepatomegaly

entecavir Hep B inhibits HBV DNA pol oral

Lamivudine Hep B and HIV

Telbivudine Hepatitis nucleoside analog

Tenofovir hepatitis B/ HIV active against lamivudine

and entecavir resistan
strains
Drugs for Hepatitis Viruses