Decrease synthesis of Mycolic acids. Mutation causes resistance becauses KatG(BACTERIAL Catalase peroxidase) needed to activate isoniazid. 2. Modification of the protein target binding site.
Isoniazid Dx
Mycobacterium TB and Prophylaxis of TB
Isoniazid Sx
Neurotoxicity can be prevented by giving b6, SLE, Hepatits(Hepatocyte damage) G6PD, Seizures
Isoniazid Antidote
Pyridoxine
Pyrazinamide
Pyrazinamidase → pyrazinoic acid. (Requires and Acidic Environment to kill TB inside the phagosome of macrophages and other intracellular organisms)
Ethambutol
Ethambutol-arab-carbohydrate Blocks Arabinosyltransferase → Decreases Carbohydrate polymerazation of cell wall. Mutation causes resistance Increases acitivty of enzymes involved in cell wall polysaccharide synthesis.
Ethambutol Sx
Optic Neuropathy/ Red green color blindness.
Streptomycin
TB drug. Resistance caused due to altered structure of bacterial ribosomal protein
Streptomycin
Inhibits initiation of protein synthesis by binding to and distorting the structure of prokaryotic 30 s ribosomal subunit
memorize
: Antifungal
Question
Answer
Amphotericin B
Binds ergosterol and forms leaky membrane pores TOPICAL
Competivily inhibit IMP Dehydrogenase → Inhibit synthesis of guanine Nucleotides → interfere with duplication Viral genetic material
Ribavirin Dx
RSV, Chronic Hepatitis C
Ribavirin Sx
Hemolytic Anemia, Extremely Teratogenic
Amantidine
Impairs uncoating or disassembly of influenza
Acyclovir
Purine nucleoside analogue → Viral thymidine kinase converts it into acyclo-GTP → Inhibits Viral DNA Polymerase & incorporation into viral DNA → chain termination.
Acyclovir Dx
HSV & VZV
Acyclovir Sx
Renal tube crystalline nephropathy – Adequate Hydration must be given
Valacyclovir
Given daily to prevent recurrence of HSV-2
FosCARnet
Pyrophosphate analogue that inhibits viral DNA polymerase by binding to pyrophosphate binding site of enzyme. No viral kinase required. Also inhibits NRTI
FosCARnet Dx
Used in acyclovir/ganiciclovir-Resistant hsv, Cmv retinitis, advanced Aids
Used for general prophylaxis and during pregnancy to reduce transmission risk. Decrease vertical transmiZion. Sx Blasts your bonemarrow, Megaloblastic anemia
Enfuvirtide
Bind HIV gp-41 protein leading to preventing gp41 from allowing virus to fuse to target cellullar membrane
NNRTI
Bind to reverse transcriptase at a different site. Do not need a thymidine kinase to be activated. Does not need activation via intracellular phosphorylation.
NNRTI Sx
Bone Marrow Suppression(G-csf), Peripheral Neuropathy, Lactic Acidosis(nucleosides), Rash(non-nucleosides), Megaloblastic anemia(ZDV)
NNRTI drugs
NeVIRapine, EfaVIRenz, DelaVIRDINE
ProTEASE Inhibitors – “navirs”
Inhibit viral in coded protease to cleave polyproteins → Prevent maturation
ProTEASE Inhibitors – “navirs Sx
Hyperglycemia, GI intolerance, Lipodystrophy (FAT REDISTRUBITION - Cushing)
ProTEASE Inhibitors – “navirs
LopiNAVIR, AtzaNAVIR, FozampreNAVIR,SaquiNAVIR
Integrase Inhibitor
Inhibits HIV viral genome integration into host cell chromosome by reversibly inhibting HIV integrase → Impairs Messenger RNA Transcription
RalTEGRAvir Integrase Inhibitor Sx
Hypercholesterolemia
Integrase Inhibitor Drug
RalTEGRAvir
memorize
: Antidotes
Question
Answer
Mushrooms
Death cap – Aamanitin → inhibits RNA polymerase II “MRNA” → liver fail
Acetaminophen
Inhibit COX enzyme → Inhibiting pro-inflammatory chemicals. Metabolized by AM404 → Reuptake of Anandamide by neurons/ Inhibit Na Channel(Anesthetic) Normal – Conjugated by liver → N-acetylbenzoiminoquinone → Glutahione molecules reacts → Urine
Acetamenophen Abnormal
Liver → ↑N-acetylbenzoiminoquinone → ↓Glutahione molecules → Zone III Centriolobular Hepatic necrosis.
Acetamenophen Antidote
N-acetylcysteine → glutahione precursor → ↑ Glutahione molecules for NAPQI
N-acetylcysteine
Also used in Cystic Fibrosis pts as mucolytic agent by cleaving or reducing the intermolecular disulfide bridges or bonds within mucus glycoproteins
N-acetylcysteine non toxic
Sulfhydryl group supplementation for acetaminophen toxicity