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Antiparasit Drugs
Common Drugs
Used in Parasitic Diseases
I. A. Intestinal Anthelminthics
II. B. Extra Intestinal Anthelminthics
III. C. Amoebicides
IV. D. Anti Toxoplasmosis
V. E. Anti Malaria
A. Intestinal Anthelminthics
For:
-Nematode Infections
Pyrantel pamoate
Piperazine
Levamizole
Mebendazole
Thiabendazole
-Cestode infections
Niclosamide
Praziquantel
Albendazole
Pyrantel pamoate (Combantrin)
Broad spectrum
Rapidly absorbed
Has immuno-modulating effects
Binds tubulin beta inhibit microtubule polymerization
Dose 25 mg/kg 7 days for:
Strongyloides stercoralis
Cutaneus larva migrans/creeping eruption
Ascaris, Trichuris, Enterobius
Trichinosis
Preparation: Chewable tablets 500 mg
Niclosamid (Yomesan)
Broad spectrum
Well absorbed
Increases permeability of membrane parasite for Ca-ion spastic
paralysis
Dose for:
Schistosomiasis, cysticercosis, echinococciasis 20-40 mg/kg single
dose
Taeniasis : 10 mg/kg
Preparation : tablets 600 mg
Albendazole
Broad spectrum
Absorbed immediately
Blocks glucose intake of larvae and adult worms ATP decreases die
Teratogenic
Dose for:
Ascaris, Trichuris, Hookworms: 400 mg single dose
Enterobius : 400 mg single dose, repeat 1 week later
Cysticercosis : 15 mg/kg for 1 month
Hydatid disease : 800 mg/day for 30 days
Preparation : tablets 200 mg
B. Extra intestinal Anthelminthics
Rapidly absorbed
Used for treating Blood Nematode, Ascariasis and Cutaneus Larva
Migrans
Dosage: 5-6 mg/kg 1 day each week or month for 6 – 12 doses.
Preparation: tablet 50 mg or syrup 24 mg/ml
C. Amoebicides
Metronidazole (Flagyl)
Spiramycine
A macrolide antibiotic
Inhibit protein synthesis
Dose: 6-9 juta U, 2-3 x/day
E. Antimalarial drugs
Choloroquine
Acts mainly on the large ring-form and mature trophozoite
Well absorbed
inhibits peroxidative activity of hem and interferes with non-enzymatic
polymerization -> dead parasites
Dose: 25 mg base/kg spread over three days
Preparation: tablet and injection (s.c, i.m and i.v)
Quinine
Mechanism of action
The drug directly inhibits viral DNA-polymerase and viral inverse
transcriptase (it does not require phosphorylation for antiviral activity)
Antiviral spectrum and resistance
Antiviral spectrum includes HSV-1, HSV-2, VZV, CMV and HIV.
Administration: IV
Adverse effects
• Hypocalcemia and hypomagnesemia (due to chelation of the drug with
divalent cations) are common.
• Neurotoxicity (headache, tremor, irritability, hallucinations, seizures)
• Nephrotoxicity (acute tubular nephrosis, interstitial nephritis)
Therapeutic uses alternative drug for:
• HSV infections (due to thymidine kinase deficient strains which are
acyclovir resistant)
• HSV infections in immunocompromised patient
• CMV retinitis (gancyclovir resistant)
• CMV infections in immunocompromised patient
AMANTADINE
Mechanism of action
The drug is converted by cellular enzymes to its triphosphate analog which
inhibits viral DNA-polymerase.
Antiviral spectrum and resistance
• Antiviral spectrum of vidarabine includes HSV-1, HSV-2 and VZV.
• Resistant due to mutation in DNA-polymerase have been detected.
Administration: topical or IV.
Adverse effects
Dose-dependent toxicity (after IV administration):
• Neurotoxicity (headache, tremor, confusion, seizures)
• Anemia, leukopenia, thrombocytopenia.
• Syndrome of inappropriate secretion of ADH.
• The drug is mutagenic and teratogenic in animals.
Therapeutic uses: alternative drug for
• HSV keratoconjunctivitis (topical).
• Neonatal herpes.
• VZV infections in immunocompromised patient.
INTERFERONS
Three major classes of human interferons (IFN): alpha, beta, gamma
Mechanism of antiviral action
Binding to specific receptors of the host cells and Induction of enzymes (protein
kinase, oligoadenylate synthase, phosphodiesterase) inhibition of translation
(late viral RNA and protein synthesis)
Antiviral spectrum
Antiviral spectrum includes HBV, HCV, HDV, HSV, VZV, CMV and human
papillomavirus (HPV).
Adverse effects
Acute flu-like syndrome (fever, headache, myalgia, arthralgia, nausea and
vomiting)
Therapeutic uses
• Chronic hepatitis B and C
• HZV infection in cancer patients
• CMV infections in renal transplant patients
• Refractory condylomata acuminata
• AIDS related Kaposi’s sarcoma
Replicative cycle of HIV-1, an example of a retrovirus, showing the sites
of action of antiviral agents.
ZIDOVUDINE
Mechanism of action
• Phosphorylated by cellular thymidine kinase to the corresponding
nucleotide analog inhibits the RNA dependent DNA-polymerase
blocking DNA synthesis
Antiviral spectrum and resistance
• Antiviral spectrum includes HIV-1, HIV-2, HTLV-1 and other retroviruses.
• Highly resistant mutants have been recovered from many AIDS patients
treated for more than 6 months.
Adverse effects
Severe anemia and leukopenia, Malaise, fever, fatigue, headache, nausea and
vomiting, diarrhea, insomnia, agitation (mainly during first few weeks)
Therapeutic uses
• Initial drug of choice in AIDS patients with CD4 counts less than 500/mm3.
(the drug initially reduces morbidity and mortality, but the effect is
transient)
• In asymptomatic HIV-infected individuals the drug slow the rate of
progression of AIDS.
Didanosine, Zalcitabine and stavudine
Mechanism of action
Phosphorylated by cellular thymidine kinase to the corresponding nucleotide
analog inhibits the RNA dependent DNA-polymerase blocking DNA
synthesis
Antiviral spectrum and resistance
The drugs are active against HIV-1 and HIV-2, including most zidovudine
resistant strains
Adverse effects
• Painful peripheral neuropathy (up to 30% of patients)
• Pancreatitis (can be fatal)
• Headache, insomnia, agitation, seizures (didanosine)
• Arthralgia, fever, rash
• Stomatitis, esophageal ulceration (zalcitabine)
• Hepatic steatosis, lactic acidosis (can be fatal)
Therapeutic uses
Advanced HIV infection in patients who are intolerant of or deteriorating on
zidovudine.
PROTEASE INHIBITORS
Derivat
Atazanavir, Darunavir, Fosamprenavir, Lopinavir, Nelfinavir, Tipranavir,
Saquinavir, Ritonavir and Indinavir
Mechanism of action
inhibiting HIV protease the drugs block the maturation of the virus and
therefore are active in both acutely and chronically infected cells
Antiviral spectrum and resistance
The drugs are active against HIV-1 and HIV-2, including most strains resistant
to nucleoside analogs
Adverse effects
• Nausea and vomiting, diarrhea, abdominal pain
• Skin rashes, urticarial
Drug interactions
Drugs which inhibit the hepatic mixed function oxidase system may increase
plasma concentrations of HIV protease inhibitors.
Therapeutic uses
Advanced HIV infection (in combination with deoxynucleoside antiretroviral
drugs)
Entry Inhibitors (Efuvirtide)
Resistance can occur but there is no
cross resistance
Drug administration subcutaneously in
combination with other antiretroviral
drugs
Side effects: Local injection site
reaction, hypersensitivity reaction,
Eosinophilia