Pharm-Micro Block 3 pt. 2

ptheodore's version from 2015-11-28 11:47

Antiviral drugs

Question Answer
Inhibit viral DNA polymerase (inhibit the DNA synthesis)Anti herpes drugs (Acyclovir, Ganciclovir, Famciclovir, Cidofovir, Foscarnet, Vidarabine, Fomivirsen)
Viral enzyme _____ in HSv phosphorylates Acyclovir and activates itThymidine kinase
Viral enzyme _____ in CMV activates GanciclovirPhosphotransferase
The loss of ability to produce viral thymidine kinase causes resistance toAcyclovir
Bone marrow suppression - dose dependent- causing Aplastic anaemiaChloramphenicol, Flucytosine, Ganciclovir
Rx for bone marrow suppressionGranulocyte Colony Stimulating Factor (G-CSF) – filgrastim & Granulocyte/Macrophage Colony Stimulating Factor (GM-CSF) - Sargramostim
Its phosphorylation to active form inside the cell is independent of viral enzymes. Inhibits the DNA polymeraseCidofovir
NephrotoxicityVancomycin, Aminoglycosides, Amphotericin B, Tetracyclines, Cidofovir, Foscarnet
Does not require phosphorylation for antiviral activity. Inhibits the DNA polymerase.Foscarnet
Rx for Acyclovir resistant strains of HSVFoscarnet
Inhibits the first step in replication of influenza A i.e. viral un-coating (block M2 protein)Amantidine, Rimantidine
Inhibitors of neuraminidase, produced by influenza virus the enzyme required for preventing the clumping of virionsZanamivir (intranasal use) and Oseltamivir
Drugs for hepatitisInterferon α
DOC for Respiratory syncytial virus infectionsRibavirin

HIV Drugs

Question Answer
Nucleoside reverse transcriptase inhibitors (NRTI)Zidovudine (AZT), Stavudine (D4T), Didanosine (ddI), Lamivudine (3TC), Zalcitabine (ddC)
Lack a 3′-hydroxyl group on the ribose ring, attachment of the next nucleotide is impossible. Thus they interrupt DNA chain elongationNucleoside Reverse Transcriptase Inhibitors (NRTI)
Competitive Inhibit reverse transcriptaseNucleoside reverse transcriptase inhibitors (NRTI)
Used for Prophylaxis - following needlestick injury (Post exposure prophylaxis)AZT (zidovudine)
Used to prevent Vertical transmission (mother to fetus)AZT (zidovudine)
Does not require phosphorylation to triphosphate form. NOT a prodrug. Directly bind to site on HIV-1 reverse transcriptase and inhibits it.NonNucleoside reverse transcriptase inhibitors (NNRTI) ( Nevirapine, Delaviridine, Efavirenz)
Protease (pol gene encoded) is responsible for viral assemblyProtease inhibitors ("navir")
Mechanism of resistance: specific point mutations in pol geneProtease inhibitors ("navir")
Binds to gp41 inhibits the fusion/penetration of viral and cellular membranesEnfuvirtide
Chemokine Receptor (CCR5 Receptor) antagonist on White blood cells, prevents fusion/penetration of viral and cellular membranesMaraviroc
Inhibits integrase, an enzyme necessary for integration of HIV DNA to host cellsRaltegravir
Antiretroviral Drugs Toxicities; BM suppressionZidovudine
Antiretroviral Drugs Toxicities; PancreatitisDidanosine
Antiretroviral Drugs Toxicities; lactic acidosisNRTI
Antiretroviral Drugs Toxicities; Peripheral neuropathyNRTI
Antiretroviral Drugs Toxicities; Kidney stonesIndinavir
Antiretroviral Drugs Toxicities; Kinetic BoostRitonavir
Antiretroviral Drugs Toxicities; Hyperglycemia, Hyperlipidemia, LipodystrophyProtease Inhibitors
Antiretroviral Drugs Toxicities; CYP inhibitorsProtease Inhibitors
DOC for Cryptosporidium diarrheaHAART
DOC for Pneumocystis jiroveci PneumoniaTMP-SMX
DOC for Esophageal candidiasisFluconazole
DOC for HistoplasmosisFluconazole/Itraconazole
DOC for ToxoplasmosisSulfadiazine + pyrimethamine
DOC for CMV retinitisCidofovir
DOC for Cryptococcal meningitisFluconazole + flucytosine
DOC for Mycobacterium avium (MAC)Azithromycin

Antifungal drugs

Question Answer
DOC for DermatophytosisTerbinafine
DOC for CandidiasisFluconazole
DOC for CryptococosisFluconazole
DOC for AspergillosisCapsofungin
DOC for Mucormycosis
DOC for BlastomycosisItraconazole
DOC for SporothrixItraconazole
DOC for histoplasmosisFluconazole
DOC for CoccidiodomycosisFluconazole
DOC for ParacoccidiodomycosisKetoconazole
Inhibit Fungal cell wall by inhibiting synthesis of β-glucanCapsofungin
Binds to ergosterol in fungal cell membranes. Forms pore in membrane creating a transmembrane ion channelPolyene Antibiotics (Amphotericin B & Nystatin)
Inhibit fungal cell membranePolyene Antibiotics (Amphotericin B & Nystatin)
Inhibit fungal nuclear division (mitosis)Griseofulvin
Inhibit fungal mitosis by binding to intracellular microtubular proteinGriseofulvin
Inhibit fungal nuclear acid synthesis5-Flucytosine
Topically (as a cream) used to treat vaginal candidiasisNystatin
Used orally to treat oropharyngeal candidiasis (swish and swallow)Nystatin
Antifungal with Disulfiram like reaction with alcoholGriseofulvin
Antifungal that is nephrotoxicAmphotericin B
Antifungal that is CYP Enzyme inducerGriseofulvin
Antifungal that inhibits thymidylate synthase leading to Inhibition of DNA synthesisFlucytosine
Antifungal that causes Bone marrow suppressionFlucytosine
Inhibit fungal CYP3A (lanosterol 14α-demethylase) enzyme which is responsible for converting lanosterol to ergosterol'Azoles'
inhibit Squalene epoxidase responsible for ergosterol synthesis'Azoles'
Antifungal that causes gynaecomastia, loss of hair and libido, oligospermia Ketoconazole (KTZ)
Antifungal that can't be used with antacidsKetoconazole (KTZ)
Antifungal that's a CYP3A4 inhibitorKetoconazole (KTZ)
DOC for tinea pedis. Concentrated in dermis, epidermis and adipose tissue. Used to treat fungal infections of the nails (Onychomycosis)Terbinafine


Question Answer
Inhibits mycolic acid synthesis and mycobacterial cell wall (Mycolic Acid responsible for the acid fastness)Isoniazid (INH)
Resistance due to deletions of katG gene - encodes catalase neededIsoniazid (INH)
Antimycobacterial reistance by expression of a gene that encodes a catalaseIsoniazid (INH)
Peripheral neuropathy due to Vit B6 (pyridoxine) deficiency, therefore supplement Vit B6Isoniazid (INH)
Hemolysis in G-6-PD deficiencySulfonamides, Isoniazid (INH), Dapsone, Quinine, Primaquine (Malaria drugs)
Antimycobacterial that inhibits DNA dependent RNA polymeraseRifampin
Antimycobacterial that causes orange red color to urine (harmless side effect)Rifampin
Antimycobacterial that is CYP 450 (CYP 3A4) enzyme inducerRifampin
Antimycobacterial used as Prophylaxis of menigococcal and H.Influenza meningitis (to prevent carrier state) Rifampin
Antimycobacterial that inhibits FAS I, the enzyme that synthesizes fatty acid from acteyl co A which is necessary for mycolic acid synthesis. Acts on cell wall (Mycolic Acid). Need ACID Environment Pyrazinamide
Antimycobacterial that Inhibits the synthesis of arabinogalactan (CARBOHYDRATE part of cell wall component)Ethambutol
Antimycobacterial that decreased visual acuity / colour blindness unable to distinguish b/w red and green traffic lightEthambutol
Mechanism of resistance – mutation in arabinosyl transferase geneEthambutol
TB drug for MAC in AIDSClarithromycin + Ethambutol (life long)
DOC For LeprosyDapsone
Inhibition of folic acid synthesis - dihydropteroate synthaseDapsone & Sulfamethaxazole (SMX)
DOC for Lepra reaction/ Erythema Nodosum LeprosumClofazamine
Rx for a Jarish Herxheimer (arthus) type of reaction due to release of antigens from killed bacilli. Fever, malaise, enlarged Lymph nodes, jaundice, anemiaClofazamine

Antiprotozoal Drugs

Question Answer
Primary cause for MalariaP.falciparum
Causes relapse of malariaP. Vivax & P.ovale
DOC for malariaChloroquine
DOC for malaria resistant to chloroquineQuinine (oral), Quinidine, Mefloquine (quinine analog) or Fansidar
DOC that kills the Tissue (liver) schizontocides (kill the extrahepatic/hypnozoites)Primaquine
DOC to prevent relapse of malariaPrimaquine
Malaria drug given 1-2 weeks before departure, weekly during stay and 4 weeks after leaving endemic areaMefloquine
Malaria drug given 1-2 days before departure, daily during stay and 7 days after leaving endemic areaProguanil+Atovaquone
Accumulates in food vacuole of parasite. Prevents conversion of heme to hemozoin. Heme accumulation leading to deathMOA for Chloroquine, hydroxychloroquine
Mechanism of resistance to chloroquineMutations in Plasmodium falciparum chloroquine resistant transporter (pfcrt)
Freely enters the food vacuole, in acidic environment it is protonated making it unable to diffuse out of the vacuole (it accumulates in high concentration in food vacuole). It prevents polymerization of heme to hemozoinChloroquine
Hemolysis in G-6-PD deficiencySulfonamides, Isoniazid (INH), Dapsone, Quinine, Primaquine (Malaria drugs)
Causes; Blackwater fever is a complication of malaria in which red blood cells burst in the bloodstream, releasing hemoglobin directly into the blood vessels and into the urine, frequently leading to kidney failureQuinine
Tinnitus, vertigo, headache, flushed and sweaty skin, dizziness, visual disturbances, hypoglycemia, arrhythmias….CINCHONISMQuinine
Malaria drug Contraindicated – psychosis (hallucinations)Mefloquine
Is the only active agent against dormant liver forms of vivax and ovale (HYPNOZOITES)Primaquine
DOC for Pneumocystosis (Pneumocystis jerovecii)TMP-SMX (Cotrimaxozole)
DOC for AmebiasisMetronidazole
Antibiotics that contain methylthiotetrazole group (MTT group) and may cause disulfiram like reactions with ethanol. Pesents as nausea, vomiting, headache, tachycardia, CV collapseMetronidazole & Cephalosporins (Cefamandole, Cefoperazone, Cefotetan), & Chlorpropramine (Diabetic Sulfonamide) & Griseofulvin
DOC for Anaerobic bacterial infections i.e - B.fragilis, Cl.difficileMetronidazole

Drugs for Helminthic infections

Question Answer
DOC for Ascaris lumbricodesMebendazole, Albendazole
DOC for Ankylostoma duodenaleMebendazole, Albendazole
DOC for Strongolides stercoralisMebendazole, Albendazole
DOC for Trichinella spiralisMebendazole, Albendazole
DOC for enterobius vermicularisMebendazole, Albendazole
DOC for ankylostoma duodenaleMebendazole, Albendazole
DOC for Loa LoaDiethylcarbamazine
DOC for Toxocara canisDiethylcarbamazine
DOC for W.bancroftiDiethylcarbamazine
DOC for Taenia SoliumPraziquantel
DOC for Diphyllobothrium latumPraziquantel
DOC for EchinococcusPraziquantel
DOC for trematodes (flukes-Schistosoma)Praziquantel

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