Term
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Definition
Class: anti-fungal, echinocandins
Mechanism: cell wall synthesis inhibitor, 1,3-beta glucan synthase
Clinical use: invasive candidiasis; aspergillosis
Adverse Effects: well tolerated
Drug interactions: combo with immunosuppressant may cause hepatotoxicity
Absorption: IV ONLY
Distribution: high in tissue, poor to CNS
Metabolism: peptide hydrolysis and N-acetylation in liver
Elimination: HEPATIC |
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Term
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Definition
Class: anti-fungal, polyenes
Mechanism: binds ergosterol and forms pore in membranes
Clinical use: broad-spec serious fungal infections, some protozoa; CRYPTOCOCCUS MENINGITIS
Contraindication: RENAL IMPAIRMENT
Adverse effects: INFUSION-RELATED REACTIONS (cytokine storm: fever, chills, hypotension), NEPHROTOXICITY (80%, less so if liposome form), arrhythmias
Absorption: insoluble, poor oral, IV only; intrathecal for meningitis
Distribution: poor CNS, high tissue-bound (half-life 15days)
oral-topical for oral or cutaneous candidiasis (non-toxic) |
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Term
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Definition
Class: anti-fungal, allyamines
Mechanism: inhibit ergosterol synthesis, inhibit SQUALENE EPOXIDASE, causes accumulation of sterol in fungus (toxic), alters membrane fluidity and rigidity
Clinical use: DERMATOPHYTES, nail fungus, jock itch, athlete's foot
Contraindications: pregnant/nursing, liver/kidney impaired
Adverse effects (oral form): well tolerated
Absorption: high lipophilic, take with non-acid foods; topical forms
Distribution: accumulates in skin, nails and fatty tissues |
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Term
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Definition
Class: anti-fungal, azole
Mechanism: interfere with ergosterol synthesis, inhibit LANOSTEROL-14alpha DEMETHYLASE (A CYTOCHROME 450 ENZYME)
Clinical use: superficial and systemic fungal infections, candidiasis, cyrptococcal meningitis (in AIDS)
Contraindication: pregnancy unless topical form
Adverse effects: well tolerated, GI, headache, rash
Absorption: oral, IV
Distribution: well to tissues, GOOD TO CSF
Metabolism: INHIBITS HUMAN CYP3A4
Elimination: 1* renal, half life 30hrs |
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Term
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Definition
Class: anti-fungal, azole
Mechanism: interfere with ergosterol synthesis, inhibit LANOSTEROL-14alpha DEMETHYLASE (A CYTOCHROME 450 ENZYME)
Clinical use: very broad-spec; candidiasis, Cryptococcus, histoplasmosis, blastomycosis, onychomycosis, ASPERGILLOSIS
Contraindication: pregnancy unless topical form; HEART FAILURE
Adverse effects: well tolerated; HEPATOTOXICITY
Absorption: oral, IVA
Distribution: well to most tissues, not CSF
Metabolism: hepatic, INHIBITS HUMAN CYP3A4
Elimination: half-life 30-40hrs |
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Term
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Definition
Class: anti-fungal, DNA/RNA synthesis inhibition
Mechanism: cytosine nucleoside analogue, sensitive fungi convert drug by CYTOSINE DEAMINASE before it can be incorporated to inhibit DNA/RNA synthesis
Clinical use: systemic fungal infections, esp. candida, Cryptococcus; USED WITH AMP B TO TREAT CRYPTOCOCCAL MENINGITIS
Contraindications: pregnancy
Adverse effects: BONE MARROW SUPPRESION, liver enzyme rise, GI distress
Absorption: oral
Distribution: high in tissues, fluids, including CSF
Elimination: renal,
Half-life: 3-6hrs |
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Term
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Definition
Class: anti-fungal
Mechanism: bind microtubules, inhibits mitosis
Clinical use: DERMATOPHYTES, alt. for onychomycosis; RINGWORM by microsporum, epidermophyton or trichophyton; long treatment period
Contraindication: pregnancy
Adverse effects: well-tolerated, blood counts 1/wk for 1st month, headahche, photosensitivity, rash
Absorption: oral, topical powder
Distribution: DEPOSITS IN KERATIN CELLS (skin, hair)
Excretion: half-life 1 day, 50% in urine within 5days, induces hepatic CYPs |
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Term
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Definition
Class: anti-fungal
Mechanism: UNKNOWN
Clinical use: alt. tx for Pneumocystis jiroveci pneumona, Leismaniasis, African trypanosomiasis
Adverse effects: NEPHROTOXICITY (25%), CARDIOVASCULAR ARRHYTHMIAS AND HEART FAILURE, HYPOGLYCEMIA, hepatitis, inhaled form: cough/bronchospasm/headache
Drug interactions: other nephrotoxic drugs
MONITOR: blood sugar, BUN, CBC, creatinine, EKG, BP
Absorption: IM or SLOW IV infusion, INHALATION IS LESS TOXIC
Distribution: bound to tissues, no CNS penetration
Elimination: extensive hepatic metabolism, renal excretion |
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Term
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Definition
Class: anti-parasitic
Mechanism: anaerobic ETS generates damaging free radicals
Clinical use: anaerobic protozoa and bacteria; GENERALLY SAFE FOR CHILDREN
Contraindication: pts with active disease in CNS
Adverse effects: usually mild, headache/nausea; AVOID ALCOHOL
Absorption: oral, IV, topical gel
Distribution: penetrate well into body tissues/fluids and CSF
Metabolism: liver
Excretion: metabolites release in urine, sometimes turns it red-brown |
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Term
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Definition
Class: anti-parasitic
Mechanism: binds toxic heme preventing polymerization, oxidative damage kills parasite
Clinical use: noncomplicated malaria, erythrocytic forms of plasmodium; prophylaxis and treatment
Contraindication: pt with epilepsy or myasthenia gravis, pt w/ psoriasis, hemolysis in pts with G6PD deficiency
Absorption: oral
Metabolism: two active metabolites generated by P450 system
Excretion: renal
Adverse effects: well tolerated, safest |
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Term
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Definition
Class: anti-parasitic
Mechanism: inhibition of heme polymerization
Clinical use: non-complicated malaria, erythrocytic forms of plasmodium
Contraindications: pts with epilepsy or myasthenia gravis, pts with tinnitus or optic neuritis, hemolysis in G6PD deficiency
Adverse effects: more toxic, less effective than chloroquine; cinchonism, hypoglycemia, hypotension
Absorption: oral
Metabolism: hepatic P450 system
Excretion: renal |
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Term
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Definition
Class: anti-parasitic
Mechanism:
Ato - selective mitochondrial inhibitor (structural analogue of ETS)
Pro - enhance collapse of mito membrane potential and its metabolite is DHFR inhibitor
Clinical use: non-complicated MALARIA, prophylaxis and treatment; TOXOPLASMA and PNEUMOCYSTIS
Contraindication: SEVERE RENAL IMPAIRMENT
Adverse effects: well-tolerated
Absorption: oral
Distribution: plasma protein bound
Metabolism: minimal
Excretion: bile, feces |
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Term
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Definition
Class: anti-parasitic
Mechanism:
Clinical use: COMBO TX FOR MALARIA WITH DOXYCYCLINE AND CLINDAMYCIN
Adverse effects: cardiotoxic, hypotension, hypoglycemia, prolonged QT interval |
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Term
| sulfadiazine + pyrimethamine |
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Definition
Class: anti-parasitic
Mechanism: DHPS and DHFR inhibitors, blocks production of THFA
Clinical use: TOXOPLASMA GONDII, malaria, antibacterial; DOES NOT ELIMINATE ENCYSTED FORMS
Adverse effects: allergies to sulfa drugs, bone marrow suppression,
Absorption: oral |
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Term
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Definition
Class: anti-parasitic, pentavalent antimonial
Mechanism: interfere with unique trypanothione antioxidant system
Clinicaly use: LEISHMANIASIS cutaneous or visceral
Adverse effects: well tolerated, pain at injection site
Absorption: IV or IM
Excretion: renal w/in 24hrs |
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Term
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Definition
Class: anti-parasitic, kinetoplastid drug
Mechanism: metabolized to toxic free radicals
Clinical use: American CHAGAS DISEASE (T. CRUZI)
Adverse effects: anorexia, vomiting, memory loss, convulsions
Absorption: oral
Metabolism: rapidly to uncharacterized metabolites
Excretion: metabolite in urine
Half-life: 3hrs |
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Term
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Definition
Class: anti-parasitic, kinetoplastid drug
Mechanism: ornithine decarboxylase inhibitor (prevents synthesis of polyamines)
Clinical use: CHRONIC STAGE OF T. BRUCEI
Adverse effects: "arsenic in antifreeze", kills 10% of patients
Administration: IV only |
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Term
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Definition
Class: anthelmintics
Mechanism: inhibits microtubule polymerization/mitotic spindle poison, binds worm B-tubulin with higher affinity than mammalian
Clinical use: nematodes, roundworms
Adverse effects: well tolerated
Absorption: oral, poorly absorbed (good for GI worms)
Metabolism: rapid first pass converts to inactive form
Excretion: bile, little in urine |
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Term
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Definition
Class: anthelmintics
Mechanism: depolarizing neuromuscular blocking agents, results in spastic paralysis
Clinical use: nematodes/roundworms, esp. Ascaris, hookworm, pinworm
Adverse effects: well tolerated
Absorption: oral, poor absorbtion
Excretion: <15% in urine, most in feces |
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Term
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Definition
Class: anthelmintics
Mechanism: kills larvae in host; not effective against adult worm, induces paralysis via glutamate-gated Cl- channels found only in invertebrates
Clinical use: broad-spec anti-parasisitic, nematode, esp. filariae causing onchocerciasis (river blindness, black fly assoc.)
Contraindicated: BBB injure/impaired, due to effects on mammalian GABA receptors
Adverse effects: well tolerated
Absorption: oral, one dose/year, conc. in liver and fat, little in brain
Metabolism: liver
Excretion: long terminal half-life of 60hrs |
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Term
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Definition
Class: anthelmintics
Mechanism: causes spastic paralysis and tegument damage
Clinical use: flatworms and cestodes (schistosomes and tapeworms, resp.)
Contraindication: ocular cysticercosis (larvae in eye) as host response to dead worm damages eye; ophthalmologic surgery instead
Adverse effects: well tolerated, GI, CNS effects
Absorption: oral
Metabolism: extensive first-pass into inactive (induction of CYP dec. F)
Excretion: metabolites in urine w/in 24hr, some in bile |
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