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Pharmacology - Final - Part 15

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davidwurbel7's version from 2016-08-14 07:12

Antimycobacterial

Question Answer
Mechanism of action inhibits mycolic acid synthesis and mycobacterial cell wallIsoniazid (INH)
Resistance is due to deletions of katG gene which encodes for catalaseIsoniazid (INH)
Prodrug that gets activated by catalaseIsoniazid (INH)
Adverse effects include Hepatotoxicity, Peripheral neuropathy due to Vitamin B6 deficiency, drug-induced lupus erythematous, can inhibit phenytoin metabolism and hemolysis in patients with G-6-PD deficiencyIsoniazid (INH)
Mechanism of action inhibits DNA dependent RNA polymeraseRifampin
Adverse effect is hepatitis is a major side effectRifampin
This drug is a CYP 450 enzyme inducerRifampin
A harmless side effect with this drug is orange/red discoloration of body fluids including urine, tears and scleraRifampin
Uses include TB, Leprosy. Prophylaxis of menigococcal and H.Influenza meningitis (to prevent carrier state)Rifampin
A prodrug which converted to active form pyrazinoic acid by enzyme pyrazinamidasePyrazinamide
Mechanism of action inhibits FAS I, the enzyme that synthesizes fatty acid from acteyl co A which is necessary for mycolic acid synthesis. Especially effective against the intracellular form of M. tuberculosisPyrazinamide
Adverse effects include Hepatotoxicity (1-5%) and HyperuricemiaPyrazinamide
Mechanism of action inhibits the synthesis of arabinogalactan (cell wall component)Ethambutol
Mechanism of resistance– mutation in arabinosyl transferase geneEthambutol
Adverse effects include hepatic toxicity and optic neuritis – decreased visual acuity / colour blindness unable to distinguish b/w red and green traffic light, not used in childrenEthambutol
1st phase of TB treatment2 Months
2nd phase of TB treatment4 Months
1st phase drugsRifampin, Isoniazid, Pyrazinamide, Ethambutol
2nd phase drugsRifampin, Isoniazid
Inhibition of folic acid synthesis - dihydropteroate synthaseDapsone
Adverse effects include hypersensitive reactions, Hemolytic anemia in G-6-PD deficiency patients and Lepra reactionDapsone
An arthus type of reaction due to release of antigens from killed bacilli. Fever, malaise, enlarged Lymph nodes, jaundice, anemiaLepra Reaction
A severe form of Lepra reactionErythema Nodosum Leprosum
Treatment of this is Clofazamine or Chloroquine or Thalidomide or CorticosteroidsLepra Reaction
This drug suppresses TNF-alpha produceThalidomide
This drug can be used for multiple myeloma, the skin manifestations of lupus erythematosus and severe Erythema Nodosum LeprosumThalidomide
A dye with leprostatic and anti-inflammatory actions. MOA: Binds to DNA & inhibits template function. Generates cytotoxic oxygen radicals that are toxic to bacteriaClofazamine
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Protozoan Infection

Question Answer
This drug kills hypnozoites. Prevents the relapse of infection Primaquine
This drug kills the merozoites.Chloroquine
Prophylaxis for chloroquine sensitive regionChloroquine +/- Primaquine
Prophylaxis for chloroquine resistance regionMefloquine
Treatment for P. falciparum and P. malariaeChloroquine
Treatment for P. vivax and P. ovaleChloroquine and Primaquine
4-AminoquinolineChloroquine
8-AminoquinolinePrimaquine
Treatment of chloroquine resistant P.falciparumQuinine
A mutated PfCRT (K76T) pumps the protonated chloroquine out of the food vacuoleChloroquine Resistance
Mechanism of action by entering food vacuole of the plasmodium and becomes protonated. It then prevent polymerization of heme to heomzoinChloroquine
This drug can also be used to treat amoebic liver abscess and rheumatoid arthritisChloroquine
Adverse effect may cause retinal damage with prolonged use of this drugChloroquine
Adverse effects include syncope, extrasystoles. Contraindicated – psychosis, seizures, cardiac conduction defectsMefloquine
Adverse Effects include hemolysis and methemoglobinemia in G-6-PD deficient patientsPrimaquine
Adverse effect include tinnitus, vertigo, headache, flushed and sweety skin, dizziness, visual disturbances, hypoglycemia and arrhythmiasQuinine
Also causes Hemolysis in G6PD deficient patients. Intravascular haemolysis – rare but fatal complication of therapy- called as blackwater feverQuinine
Obtained from a Chinese herb. Best in MDR cases. Not for prophylaxisArtemisinin
The mechanism of action accumulation of free radical tocis in bacterial cell which damage DNAMetronidazole
Uses include all forms of amebiasis, trichomoniasis, giardiasis and anaerobic bacterial infections (B. fragilis, Cl. difficile), H. pylori associated peptic ulcersMetronidazole
Adverse effect is the possibility of disulfiram reaction and metallic tasteMetronidazole
Treatment of giardiasisMetronidazole/tinidazole
Treatment of toxoplasmosisPyrimethamine + Sulfadiazine + TMP-SMX
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Antivirals

Question Answer
Herpes simplex, Varicella Zoster virusAcyclovir, cidofovir, foscarnet
CytomegalovirusGancyclovir, Cidofovir, foscarnet, fomiversin
HARRT treatment for HIVNRTI, NNRTI, PI
InfluenzaOseltamivir, zanamivir, Amantadine, Rimantadine
Hepatitis BInterferon –alpha, Lamivudine
Hepatitis CInterferon –alpha, Ribavarin
This enzyme activates acyclovir by phosphorylating it to monophosphateThymidine Kinase
Thymidine Kinase enzyme comes from hereVirus
The monophosphate form of acyclovir is phosphorylated again by this enzyme producing diphosphateTrifluidine cidofovir
Acyclovir is a competitive inhibitor of this in the virusDNA Polymerase
Lack of viral thymidine kinase and changes in the viral DNA polymerase are mechanisms by which viruses gain this to acyclovirResistance
1st step in phosporylation with viral thymidine kinase in HSv , whereas phosphotransferase in CMV—triphosphate form inhibits viral DNA polymeraseGanciclovir
Ganciclovir is activated by phosphorylation by this enzymePhosphotransferase
This drug can be used as a prophylaxis & Rx of CMV infections (retinitis) in in AIDS patients & transplants recipientsGanciclovir
Adverse effects of this drug include haematoxicity (Bone marrow suppression) - leukopenia, thrombocytopenia, Mucositis, Crystalluria. Seizures in overdoseGanciclovir
Phosphorylation to active form inside the cell is independent of viral enzymes. Inhibits the DNA polymeraseCidofovir
This drug can be used against HSV and CMVCidofovir
Adverse effects of this drug is nephrotoxicityCidofovir
This drug does not require phosphorylation for antiviral activity..Inhibits the DNA polymerase. Inhibits the viral RNA polymerase and HIV reverse transcriptaseFoscarnet
This drug is only used against CMVFoscarnet
Adverse effects of this drug include nephrotoxicity- acute tubular necrosis, electrolyte imbalance, hypocalcemiaFoscarnet
The mechanism of action of this drug is antisense oligonucleotide- binds to mRNA of CMV- inhibits protein synthesisFomiversen
This drug is injected intravitreally in CMV retinitis Fomiversen
Zidovudine (AZT), Stavudine (D4T), Didanosine (ddI), Lamivudine (3TC), Zalcitabine (ddC) are examples for this class of drugsNucleoside Reverse Transcriptase Inhibitors(NRTI)
Prodrugs- converted by host cell enzymes to active form. Competitive inhibit reverse transcriptaseNRTI
This drug is used for prophylaxis- following needlestick injury and to prevent vertical transmissionZidovudine
NRTI mechanism of action is the interruption of DNA synthesis due to thisLack 3' Hydroxyl Group
NRTIs cause this major side effect even at therapeutic levelsBone Marrow Suppression
The bone marrow suppression seen with NRTIs is treated withG-CSF and EPO
Mechanism of action of these drugs do not recquire phosphorylation to triphosphate form. Directly bind to site on HIV-1 reverse transcriptase and inhibits itNon-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)
Nevirapine, Delaviridine ,Efavirenz are examples of this class of drugNon-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)
These drugs used synergistically with NRTI and/or PI in HAART. Prevents vertical transmission and are not myelosuppressantNon-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)
The mechanism of action inhibit HIV protease- result in production of immature ,non infectious viral particlesProtease Inhibitors
Saquinavir, Ritonavir, indinavir, Nelfinavir are examples ofProtease Inhibitors
This drug binds to gp41 inhibits the fusion of viral and cellular membranesEnfuvirtide
This drug Inhibits integrase, an enzyme necessary for integration of HIV DNA to host cellsRaltegravir
This drug is a chemokine Receptor (CCR5 Receptor) antagonist preventing the binding of the viral particleMaraviroc
All NRTIs can cause this adverse effectLactic Acidosis
This is a side effect of unique to ZidovudineBone Marrow Suppression
This is a side effect unique to DidanosinePancreatitis
This is a side effect unique to IndinavirKidney Stone
Body habitus changes in fat deposition - Intrabdominal, Dorsocervical and Breasts. Fat atrophy - Extremity wasting and Facial lipoatrophyLipodystrophy
All protease inhibitors also have this adverse effectCYP Inhibitor
The adverse effect of these drugs are Hyperglycemia- due Insulin resistance, Hyperlipidemia and LipodystrophyProtease Inhibitors
Co-administration of ritanovir with other anti HIV drugs increased the plasma concentration of these drugsKinetic Boost
A potent anti-HIV drug It has pronounced inhibitory effect on CYP3A4 used for a kinetic boost of other protease inhibitorsRitanovir
AZT(zidovudine) + 3TC (lamivudine) for 1 monthNeedle Stick Prophylaxis
AZT + 3TC + IndinavirNeedle Stick Prophylaxis (High Risk)
AZT full dose in trimester 2 and 3 + 6 weeks to neonateVertical Transmission Prophylaxis
The mechanism of action inhibits the first step in replication of influenza A i.e. viral un coating (block M2 protein)Amantidine, Rimantidine
Toxicity - atropine like peripheral side effects, livedo reticularis Amantidine, Rimantidine
The mechanism of action inhibitors of neuraminidase, produced by influenza virus the enzyme required for preventing the clumping of virionsZanamivir, Oseltamivir
Can only be used with Influenza A; Parkinson’s diseaseAmantadine
Can be used for both influenza A and BZanamivir, Oseltamivir
The mechanism of action activate a host cell ribonuclease which preferentially degrades viral mRNAInterferon Alpha
Toxicity produces GI irritation and flu like syndromesInterferon Alpha
Uses include Hepatitis B (alone or with Lamivudine), Hepatitis C (with ribavarin), Kaposi's sarcoma, papilomatosis and genital wartsInterferon Alpha
Mechanism of action triphosphate form inhibits viral RNA polymeraseRibavirin
Uses include Respiratory syncytial virus infections (aerosol), Influenza A & B, Chronic hepatitis C infection (with IFN)Ribavirin
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HIV Treatment Medications

Question Answer
Zidivudine (AZT), Stavudine (D4T), Lamivudine (3TC), Stavudine (D4T), Didanosine (ddI), Zalcitabine (ddC)Nucleoside Reverse transcriptase inhibitors (NRTI)
-udine medicationsNucleoside Reverse transcriptase inhibitors (NRTI)
Efavirenz, nevirapine, delaviridine, etravirineNon-nucleoside RT’s Inhibitors
-ine medication Non-nucleoside RT’s Inhibitors
TenofovirNucleotide RT’s inhibitors
-fover medicationsNucleotide RT’s inhibitors
Ritonavir indinavir, nelfinavir,, saquinavir, lopinavir, darunavirProtease Inhibitors
-navir medicationsProtease Inhibitors
EnfurvitideFusion Inhibitors
RaltegravirIntegrase Inhibitors
-gravir medicationsIntegrase Inhibitors
MaravirocCCR5 Inhibitors
Highly Active Antiretroviral Therapy; uses combination therapy of drugsHAART
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Anti-Viral Agents

Question Answer
Attactment inhibitor that binds to CCR5 and block the interaction of gp120Maraviroc
Nucleoside analogue with modified nucleoside bases; Example RibavirinNucleoside RNA Polymerase Inhibitors
Analogue of guanosine but base ring is incomplete and open & inhibit nucleotide biosynthesis; only used in life-threatening situations; Target: HepC, RSVRibavirin
Nucleoside analogues with modified sugar residues; Ends with –LOVIRNucleoside DNA Polymerase Inhibitors
Works by preventing elongation by Herpes DNA polymeraseAcyclovir
Nucleoside analogues with modified sugar residues; Ends with –FOVIR and -UDINENucleoside Reverse Transcriptase Inhibitors (NRTI)
Examples of this class of anti-virals are Zidovudine (AZT) and LamivudineNucleoside Reverse Transcriptase Inhibitors (NRTI)
Directly binds to HIV Reverse Transcriptsase; Examples include Nevirapine, Delaviridine and Efavirenz Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)
Prevent integration of HIV cDNA of HIV into host chromosome by directly inhibiting Integrase; Examples include Raltegravir & ElvitegravirIntegrase Inhibitors
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