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Drugs 4 Albin

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ruvehici's version from 2016-07-14 03:10

Section

: Aminoglycosides AT30
Question Answer
Aminoglycosides Dx1. Severe -gram rod Infections (Klebsiella, E.coli, Enterobacter, Citrobacter, Serratia, Shigella, Salmonella, Proteus, Pseudomonas+)
Aminoglycosides SxNephrotoxic/cephalosporins, Ototoxicity/loop dirutics/Vancomycin/ Dosedependant, Teratogen
Aminoglycosides GNATSGNATS can NOT kill anerobes
GentamycinMost Sx. Resistant to organism that is in involved in acetyl group transfer to exogenous substance.
NeomycinUsed in bowel surgery to kill bacteria that kill ammonia
AmikacinHepatic Metabolism, Renal Excretion
SteptomycinBest for Tb/Tularemia
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Question Answer
DaptomycinRapid depolarization of cell membrane → disruption of DNA,RNA synthesis → cell death.
Daptomycin DxVancomycin Resistant, MRStaph Aureus, Cornybacteria
Daptomycin SxDiarrhea, Nausea, Rhabdomyolysis
TrimethoprinInhibits bacterial dihydrofolate reductase(pyrimidine synthesis)- converting dihydrofolic - tetrahydrfolic
Trimethoprin DxTMP-SMX → UTI, Shigella, Salmonella, Pneumocystis Jirovecii(<200 Aids Prophylaxis)
Trimethoprin SxMegaloblasticAnemia, Steven Johnson Syndrome, Toxic epidermal necrolysis, Leukopenia, Granulocytopenia, Sulfa Allergy
RifampinInhibits DNA dependant RNA polymerase. Rapid resistance if used by itself(Altered structure of bacterial ribosomal proteins).
Rifampin DxMycobacterium TB, Leprosy, Meningococcal Prophylaxis(MONOTHERAPY).
Rifampin SxRed orange or orange body fluids, Hepatotoxic.
IsoniazidDecrease 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 SxNeurotoxicity can be prevented by giving b6, SLE, Hepatits(Hepatocyte damage) G6PD, Seizures
Isoniazid AntidotePyridoxine
PyrazinamidePyrazinamidase → pyrazinoic acid. (Requires and Acidic Environment to kill TB inside the phagosome of macrophages and other intracellular organisms)
EthambutolEthambutol-arab-carbohydrate Blocks Arabinosyltransferase → Decreases Carbohydrate polymerazation of cell wall. Mutation causes resistance Increases acitivty of enzymes involved in cell wall polysaccharide synthesis.
Ethambutol SxOptic Neuropathy/ Red green color blindness.
StreptomycinTB drug. Resistance caused due to altered structure of bacterial ribosomal protein
StreptomycinInhibits initiation of protein synthesis by binding to and distorting the structure of prokaryotic 30 s ribosomal subunit
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: Antifungal
Question Answer
Amphotericin B Binds ergosterol and forms leaky membrane pores TOPICAL Dx-Cyptococcus, Blastomyces, Coccidioides, Histoplasma, Candida, Mucormycosis.
Amphotericin B SxRenal Toxicity, Optic Neuropathy, Redgreen color blindness
Amphotericin B Major SxSerum potassium and magnesium needs to be monitored.
FlucytosineFluctysoine converted to 5-FU in fungal cells → Inhibits DNA and RNA synthesis.
Flucytosine DxCryptococcal Meningitis with Ampotericin b
NystatinBinds ergosterol and forms leaky membrane pores TOPICAL
Nystatin DxCandidiasis, topical- Diaper rash, Vaginal Candidiasis.
AzolesInhibit 14α-demethylase, a cytochrome P450 enzyme required for ergosterol synthesis.
Azoles DxCryptococcal Meningitis in AIDS, Blastomyces, Coccidioides, Histoplasma, Candida.
Azoles SxInhibiton of testosterone synthesis → Gynocomastia. Liver dysfunction → Inhibit P450.
TerbinafineInhibits Fungal Squalene Epoxidase → Ergosterol Synthesis Inhibited
Terbinafine DxDermatophyte infections TOPICAL Sx- Abnormal Liver function tests & Visual Disturbances
GriseofulvinBinds to microtubules → Disrupts mitotic spindles Dx- Superficial infections, Dermatophyte infections TOPICAL
Griseofulvin SxCarcinogenic, Teratogenic, Confusion, headache, Induce p450
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: Anti-protozoan
Question Answer
ChloroquineBlocks detoxification of Heme → Heme accumulates Dx-Plasmodial infections except P.falciparum Sx- Retinopathy
Pyrimethamine and SulfadiazineToxoplasma gondii – HIV – Ring or spherical frontal lobe calcifications MRI
Primaquine ALWAYS+ WITH chloroquineFOR P.Vivax & P.Ovale = Prevent Disease relapse due to intrahepatic stages.
MebendazoleEnterobiasis FIRST-LINE
MefloquineFirst line for Plasmodium
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: Viral
Question Answer
AbacavirNRTI Hypersensitivity to pts with + HLA B57:01 RASH, GI, FEVER, MALAISE
ZanaMiViR, OseltaMiViRInhibit Influenza neuraminidase → decreased Membrane Viral Release (Lysogeny), viron particle release
ZanaMiViR, OseltaMiViR DxInfluenza A&B = Prevention and treatment Sx Retinopathy
Ribavirin dxCompetivily inhibit IMP Dehydrogenase → Inhibit synthesis of guanine Nucleotides → interfere with duplication Viral genetic material. Dx-RSV, Chronic Hepatitis C
Ribavirin SxHemolytic Anemia, Extremely Teratogenic
AmantidineImpairs uncoating or disassembly of influenza
AcyclovirPurine nucleoside analogue → Viral thymidine kinase converts it into acyclo-GTP → Inhibits Viral DNA Polymerase & incorporation into viral DNA → chain termination Dx- HSV & VZV
Acyclovir SxRenal tube crystalline nephropathy – Adequate Hydration must be given
ValacyclovirGiven daily to prevent recurrence of HSV-2
FosCARnetPyrophosphate analogue that inhibits viral DNA polymerase by binding to pyrophosphate binding site of enzyme. No viral kinase required. Also inhibits NRTI
FosCARnet DxUsed in acyclovir/ganiciclovir-Resistant hsv, Cmv retinitis, advanced Aids
FosCARnet SxNephrotoxicity → Hypocalcemia, Hypomagnesemia,Hypokalemia → Seizures
ZidovudineUsed for general prophylaxis and during pregnancy to reduce transmission risk. Decrease vertical transmiZion. Sx Blasts your bonemarrow, Megaloblastic anemia
EnfuvirtideBind HIV gp-41 protein leading to preventing gp41 from allowing virus to fuse to target cellullar membrane
NNRTIBind to reverse transcriptase at a different site. Do not need a thymidine kinase to be activated. Does not need activation via intracellular phosphorylation.
NNRTI SxBone Marrow Suppression(G-csf), Peripheral Neuropathy, Lactic Acidosis(nucleosides), Rash(non-nucleosides), Megaloblastic anemia(ZDV)
NNRTI drugsNeVIRapine, EfaVIRenz, DelaVIRDINE
ProTEASE Inhibitors – “navirs”Inhibit viral in coded protease to cleave polyproteins → Prevent maturation
ProTEASE Inhibitors – “navirs SxHyperglycemia, GI intolerance, Lipodystrophy (FAT REDISTRUBITION - Cushing)
ProTEASE Inhibitors – “navirsLopiNAVIR, AtzaNAVIR, FozampreNAVIR,SaquiNAVIR
RalTEGRAvir Integrase InhibitorImpairs Messenger RNA Transcription by Inhibiting HIV viral genome integration into host cell chromosome by reversibly inhibiting HIV integrase
RalTEGRAvir Integrase Inhibitor SxHypercholestrolemia
EmtricitabineNRTI asymptomatic macular rash palmsor soles
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: Antidotes
Question Answer
MushroomsDeath cap – Aamanitin → inhibits RNA polymerase II “MRNA” → liver fail
AcetaminophenInhibit 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 AbnormalLiver → ↑N-acetylbenzoiminoquinone → ↓Glutahione molecules → Zone III Centriolobular Hepatic necrosis Antidote- N-acetylcysteine → glutahione precursor → ↑ Glutahione molecules for NAPQI
N-acetylcysteineAlso used in Cystic Fibrosis pts as mucolytic agent by cleaving or reducing the intermolecular disulfide bridges or bonds within mucus glycoproteins
N-acetylcysteine non toxicSulfhydryl group supplementation for acetaminophen toxicity
↑Iron - Hemachromatosis SxCNS, Bloody Diarrhea, Metabolic acidosis, Restrictive cardiopathy, joint pain, diabetes, skin bronze. Antidote- Deferoxamine
Lead SxMicrocytic anemia, abdominal pain, purple lines on gingivia, Peripheral Neuropathy Antidote- Edta, Dimercaprol~
Methemoglobin “Chocolate apperance Blood”Sx Cyanosis, Fatigue, Confusion, Coma Antidote -Methylene Blue
ArsenicDimercaprolGarlic smelling breath, Watery diarrhea, Qt prolongation. CNS, Mees Lines(white horizontal lines on fingernails
Copper – Skin yellow, Wilsons liver disease(low ceruloplasmin)Penicillamine
Mercury – Fish, fluorescent light bulbDimercarpol(Tx aresnic also)
Prinzmitel AnginaElevated ST segment with lead changes
ErgonovineUsed to test for prinzmitel Angina
CyanideSxReddish skin discoloration without cyanosis, Almond scent breath, trismus, apnea, seizures, coma, cardiac arrest.
CyanideTxHydroxycobalaminB12precurser– Convert to Methhemoglobin - > ferrous iron means cyanide binds more to ferrous iron and NOT mitochondrial enzymes = LESS DAMAGE
Nitropusside poisioning↑Cyanide → Metabolic Acidosis → ↑Venous po2 = REVERSE WITH SULFUR which increases-> Sodium thiosulfate coverts it to Thiocyanate → excreted
Bromodeoxyuridine (Thymidine)Increase uptake means high number of tumor cells in s phase waiting to replicate and signifies High grade
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Sideeffect

Question Answer Column 3
StatinsTreat High LdlHepatits, Myopathy
NiacinTreat low HdLCutaneous Vasodilation, Hyperuricemia(gout), Hyperglycemia(Acanthosis nigracians), Hepatits
FibratesTreat High TriglycerideGallstones, Myopathy(worse with statins)
Bile acid resinsTreat High LdLGI Upset, Hypertriglyeridemia, Malabsorption
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MRSA Infection drugs

Question Answer
Vancomycinblocks glycopeptide polymerization by binding tightly to d-ala-d-ala
VancomycinRedman Syndrome, Nephrotoxicity
DaptoMYCINDepolarization of cellular membrane Sx- Myopathy and CPK elevation Sx- Inactivated by pulmonary surfactant
linezolidBinds to 50s and inhibits protein synthesis
LinezolidThrombocytopenia, Optic Neuritis, Risk for serotonin Syndrome
C.difficileMetrondiazole, vancomycin, Fidaxomicin
Severe CdifficileVancomycin
Recurrent CdifficileFidaxomicin
FidaxomicinOral drug with minimal systemic absorpotionand less affecton normal colon than vancomycin and metrondiazole
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Teratogenic

Question Answer
TetracyclinesTeeth Discoloration
AspirinNeonatal Bleeding
CocaineFetal growth retardation
AlcoholFetal Alcohol Syndrome (retardation, mid face abnormalities)
DiabetesCaudal Regression Syndrome (sacrum & lumbar not developed leading to flaccid paralysis/absent ankle reflex)
MarijuanaLow birth weight
Vitamin Deficiency(Folate)NTD
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Overdose

Question Answer
PhencyclidineNystagmus, Violent behavior,ataxia
LSDVisual Hallucinations
CoccaineChestpain, seizures
MethamphetamineToothdecay, Tachycardia, diaphoresis, violent behavior, choreiform movements
MarijuanaIncrease Appetite, Impaired Time perception, Conjunctival injection
HeroinDepressed mental status, Miosis, Respiratory depression
Alcohol withdrawal DOCDiazapam & Chlordiazepoxide
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Withdrawal

Question Answer
AlcoholDelirium , Tremors, Seizures, Papitations
BenzodiazapinesPsychosis, Insomnia, Seizures, Perceptual disturbances
HeroinNausea vomiting, abdominal cramping, Dilated pupils, yawning, piloerection, lacrimation, Hyperactive bowel sounds
Cocaine & AmphetaminesIntense psychomotor retardation, severe depression , Increased appetite
NicotineIncreased Appetite, Dysphoria, Anxiety, Irritability
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Benzodiazepines

Question Answer
MOAAllosteric binding to the gaba receptor and increasing the frequency of ion channel opening
ZolpidemLeast addictive sleeping aid
TriazolamSHORT
AlprozalamShort
Lorazepam, Oxazepam, TemazepamIntermediate & For liver disease pts
DiazepamLONG
FlurazepamLONG
ChlordiazepoxideLONG
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: Antiandrogens
Question Answer
Finasteride moa5a reductase inhibitor → ↓testosterone to DHT → Decrease in ONLY DHT levels. Dx Baldness, B+PH
Finasteride SxGyncomastia
Flutamide moaCompetitive Inhibitor of testosterone receptor and DHT → Dx prostate carcinoma
Ketoconazole moaInhibits 17,20 Desmolase → Dx In Poly Cystic Ovarian Disease Prevent Hirsuitism
Spirnolactone moaInhibits androgen receptor with its interaction with DHT
Spirnolactone SxGyncomastia, Hair Loss
Leydig Cells -> Testosterone synthesis inhibited bySpirnolactone
Peripheral tissues -> Testosterone to DHTFinasteride
Target organs -> Androgen receptor bindingFlutamide, Cyproterone, Spirnolactone
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: Dopaminergic
Question Answer Column 3
Mesolimbic - MesocorticalRegulates BehaviorSchizophrenia
NigrostriatalCordination of voluntary movementsParkinsonism
TuberoinfundibularControls Prolactin secretionHyperprolactinemia
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Beta blocker sideffect
Question Answer Column 3
BronchicBronchoconstriction and can asthma or COPD worseB2 Blocker
Muscle vasculatureVasospasm Make peripheral artery disease worseB2 blocker
Glucagon SecretionDiminished in pts with DMB2 Blocker
Heart ONLYB1 BlockerDecrease Sa & Av Node helpful in atrial arythemias
Heart OnlyB1 blockerReduce O2 consumption leading to less angina in MI
Heart OnlyB1 BlockerDecrease HR & Contractility to lower BP
Insulin inhibitedA receptorStimulated
Insulin secretedB & H2 receptorStimulated
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: New Drugs
Question Answer
RifaximinAntibiotic that alter gi Flora which decrease production and absorption of ammonia. Also used in traveler diarrhea by inhibiting bacterial RNA synthesis through binding with DNA dependent Rna polymerase
LactuloseCatabolized by intestinal bacterialflora to short chain fatty acids, lowering the colonic pH and increasing conversion of ammonia to ammonium
RISEdonateBisphosphonate inhibits mature osteoclast mediated bone resorption
TeriparatidePTH ANALOG 1. Decreased urinary calcium excretion 2. Increased intestinal calcium absorption 3. Stimulation of pre-osteoblasts to mature osteoblasts.
DenosumabMonoclonal antibody that decreases bone resorption bu binding to the receptor activator of RANKL(Osteoclasts)
ReloxifenEstrogen receptor modulator decrease bone loss by inhibiting osteoclast differentiation and maturation
LeflunomideMOA- Inhibit Dihydroorotate Dehydrogenase, blocking pyrimidine synthesis DX- RA. Psoriatic Arthritis SX- Diarrhea, Hypertension, Teratogen, Hepatotoxic
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: Blood
Question Answer Column 3
Unfractioned HeparinNormal PT, Prolonged PTT,TT
Direct thrombin inhibitorsProlonged PT, PTT, TTDabigatran
Direct VIIa inhibitorsProlonged PT, Normal PTT, TT
Direct Xa inhibitors Prolonged PT, PTT, Normal TTApixaban, Rivaroxaban
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: Drug Sx
Question Answer
Ca & Beta BlockersAtrioventricular conduction delay
Amphetamines, Ergotamine, Chemotherapeutic agentsRaynaud Phenomenon
Iron, Opiod, Ca blockers, AtropineConstipation
ThiazideJoint pains due to Hyperuricemia
TCA(Amytriptyline)/ Anti-Histamines(Diphenydramine)Urinary retention
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: Resistance
Question Answer
Altered structure of bacterial ribosomal proteinsStreptomycin
Altered structure of enzymes involved in RNA synthesisRifampin
Decreased activity of bacteria catalase peroxidaseIsoniazid
Increased activity of enzymes involved in cell wall synthesisEthambutol
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