Systemic Antiparasitics

shevyatiwari's version from 2015-04-23 07:48

Section 1

Question Answer
Fully synthetic antihelminthicF, semi synthetic
Less effective than permethrinT
Peak levels in 2 hoursF, 4
Metabolised in the kidneyF, liver
Metabolised by CYP2D6F, 3A4
Predominantly urine excretionF, <1% in the urine
Dose adjustment required for biliary obstructionT
Dose adjustment required for renal failrueF
BA unchanged with foodF, increased with high fat meal
Binds to glutamate gated chloride channelsT
FDA approved for scabiesF, for strongyloides, onchocerca
Fatal encephalopathy is more likely if there are high loa loa burdensT
Mazotti reactions are in loa loaF, cutaneous and systemic reactions in onchocerciasis
Mazotti includes rash, systemic symptoms and opthalmological involvementT
Doxycycline can reduce the incidence of MazottiT
Pruritis, fever and lymphadenopathy are all rare S/EF
BBB is not crossed due to efflux by PGPT
PGP overactivity is a risk factor for neurotoxicityF, deficiency
Inhibits warfarin's activityF, increaes anticoagulant effect
Rifampicin, and phenobarbital can both decrease levelsT, phenobarbital to a greater degree in mouse models
Cat CT
Safe in lactationF, shouldn't be used in kids <15kg.

Section 2

Question Answer
Benzidamole carbamate with antihelminthic and antiprotozoal activityT
Well absorbed from GITF, poor absorption
Excreted unchangedF
Undergoes rapid conversion to sulfoxide metabolite before reaching the systemic circulationT
Most activity due to albendazole sulfoxide (metabolite)T
Oral BA increased with a fatty mealT
Peak levels in 2 hoursT, 2.5 hours
Half life of 6 hoursF 8 hours
Predominant biliary excretionT, <1% urine
98% protein boundF, 70%
Inhibits tubulin polymerisation 0> immobilisation and deathT
Approved for neurocystericosis onlyF, also hydatid
Anti-angiogenic effectsT
Can cause BM suppression, aplastic anaemia, agranulocytosisT
BM toxicity is restricted to those with hepatic dysfunctinF
Inhibitor of CYP1A2F, inducer
Praziquantel, dexamethasone, cimetidine levels decrease the level of active metaboliteF, increase lvel
Ritonavir increases AUC F, reduces
TeratogenicCat C

Section 3

Question Answer
Narrow spectrum antihelminthicF, broad spectrum
Metabolised by the kidneyF, liver
Excreted predominantly in the urineT
Requires adjustment in hepatic and renal dysfunctionT
Inhibits fumarate reductaseT
Live worms appears in the nose/mouthT
Caffeine and theophylline levels are increasedT
Inhibit CYP1A2T
Bloods need monitoring when used in conjunction with xanthine derivativesT. Dosage reduction may be neccessary
Cat CT

Recent badges