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Methotrexate (function)
inhibit dihydrofolate reductase
decreased tetrahydrofolate synthesis, which results in reduced DNA relication in mammalian cells due to less purines synthesized
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Methotrexate (definition)
- Cancer drug (chemotherapeutic);
- treat leukemias
- Competitive inhibitor,
- folic acid analog
- useful for rapidly growing cancers, but toxic to all dividing cells (hair, GI tract, respiratory tract, RBCs)
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sulfonamides (function)
- inhibit Dihydroptroate synthase in tetrahydrofolate synthesis.
- Only works on bacteria (microorganisms)
- DNA synthesis stops because cells cannot divide due to decreased nucelotide synthesis. (purine)
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sulfondamides (definition)
- anti-bacterial,
- for THF synthesis: PABA (p-aminobenzoic acid) analog.
- Competitive inhibitor
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Trimethoprim (definition)
anti-bacterial drug;
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Trimethoprim (mechanism)
inhibits dihydrofolate reducatse on PROKARYOTES.
reduced purine synthesis --> reduced DNA synthesis and inhibits cell divisions.
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Mycophenolic acid (definition)
- immunosurpressant drug
- prevent graft rejection
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Mycophenolic acid
reversible uncompetitive inhibitor of inosine monophosphate dehydrogenase ( GMP synthase)
deprives rapidly proliferating T and B cells of key components of nucleic aicds.
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Allopurinol (definition)
- anti-gout drug or treat hyperurecemia
- also known as Zyloprim, generic
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Allopurinol (mechanism)
- non-competitive inhibitor of xanthine oxidase
- to treat gout or hyperurecimea
Xanthine or hypoxanthine are excreted in urine
they are more water soluble thus, it's easier to get excreted in urine
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Colchicine (definition and mechanism)
gout treatment: microtubule inhibitor
inhibits migration of white cells to join where uric acid cystals are phagocytized.
DOES NOT reduces serum uric acid levels.
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hydroxyurea (definition and mechanism)
antineoplastic drug
- inhibits ribonucleotide diphosphate reductase
- decreased deoxyribonucleoside diphosphate synthesis --> decreased DNA synthesis
used for chemotherapy
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5-fluorouracil (definition)
- cancer drug;
- (5-fluorouracil-containing RNA is more detrimental to Cancer cells than to normal cells)
but it is non-selective; thus rapidly growing normal cells will be affected
AraC is commonly used to treat cancer
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5-fluorouracil (mechanism)
in dTMP (thymidine) synthesis from dUMP,
gets converted to 5 fluorodeoxyridylic acid (dFUMP), which inhibits thymidylate synthase
fluorine groups are the same size as hydrogen atom --> uracil analog
larger groups on bromodeoxyuridine and trifluorothymidine make them thymidine analogs.
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salycylates & sulfoneamides (function and affect)
dissociate albumin-bilirubin complex and form unconjugated bilirubin in blood. (Heme degradation step)
free bilirubin can cross the blood-brain-barrier and form deposits on the filter --> cause Kernicterus
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disulfiram (mechanism)
- -if ethanol is ingested, the amounts of acetaldehyde can increase by 5-10 folds.
- -side effects ie. flushing, nausea, are meant to prevent from consuming alcohol.
- -inhibits most of the acetaldehyde dehydrogenase in mitochondria isozyme.
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disulfiram (definition)
- -antabuse
- -treatment of alcoholism
- -causes nausea and vomiting if alcohol is ingested
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acetadote ( function and mechanism)
- -scavenger for NAPQ1, toxic compound formed from acetaminophen (tyrenol) during chronic alcoholic
- -contains cysteine and used for gultathione synthesis
- -
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phenobarbital (function and mechanism)
increases and stimulates CYP 450 by 3-4 fold.
Phenobarbital needs heme group; administering this drug to patients with AIP will worsen the condition since it would stimulate more heme synthesis and results in increase of ALA ( GABA analog)
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Orlistat (function)
- -Gastric& pancreatic lipase inhibitor
- -inhibits the digestion of dietary fats (TAGs)
- -reduces dietary TAG absorption
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Sibutramine (function)
an appetitie suppressant (increases the feeling of fullness)
helps to manage obesity
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Slow reacting substances of Anaphylaxis (SRS-A) (function)
- -cysteinyl-leukotrienes (LTC, LTD, LTE) are components of SRS-A
- -more potent than histamine
- -increase vascular permeability
- -could also lead to severe bronchoconstriction, vasoconstriction and lung edema
- -LTC4 = + GSH
- -LTD4 = - Glu
- -LTE4 = -Gly
- -LTF4 = + Glu
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isoniazide (definition and use)
a drug for tuberculosis
depletes PLP so needs to supply with vitamin B6 for patients.
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Non-steroidal anti-inflammatory drugs (NSAIDS) ( function)
- - inhibit both COX-1 and COX-2
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reduce inflammation - -
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Aspirin (definition and function)
- -NSAIDs
- -inhibit both COX-1 and COX-2 Irreviersibly by acetylation of a serine residue (active site)
- -low dose of aspirin can act as anti-coagulant agent ( decrease clotting)
- -favors prostacyclin produced by COX-2 in endothelial cells while COX-1 in platelets cannot synthesize new enzymes
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Cortisol ( function in eicosanoids)
- -glucocordico-steroids
- -inhibit PLA2 and COX-2
- -inhibits all prostacyclin, thoromboxane, and leukotriene synthesis
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Benoxaprofen (definition and function)
- -anti-inflammatory drug
- -inhibits 5-lipoxyogenase
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Zileuton (definition and function)
- -anti-inflammatory drug
- -inhibits 5-lipoxygenase
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Phenylbutazone (function and definition)
- -inhibit COX-1 & COX-2
- -reversible inhibitor
- -NSAIDs
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Dazoxiben (function and definition)
- -anti-coagulant drug
- -inhibits thromboxane synthase
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Dipyridamole (definition and function)
- -anti-coagulant drug
- -inhibit thromboxane synthase
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Indomethacin (definition and function)
- -NSAIDs
- -inhibit COX-1 and COX-2
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Asthma Treatment (3 options)
- 1. inhibit PLA2
- 2. inhibit 5-lipoxygenase
- 3. inhibit receptors for cysteinyl-leukotriene
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Zocor (definition and function)
- Statin drugs
- -inhibit HMG CoA reductase
- -reduce cholesterol synthesis
- -competitive inhibitor, structurally analog to HMG CoA
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Lipitor (definition and function)
- -Statin drug
- -inhibit HMG CoA reductase
- -reduce cholesterol synthesis
- -competitive inhibitor, structurally analog to HMG CoA
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Neomycin (function and definition)
- -treatment for acquired hyperammonemia
- -reduction of bacterial urease in the gut
- -
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lactulose (function and definition)
- -treatment for acquired hyperammonia
- -digested by bacteria in colon to form Lactic acid to neutralize and excrete ammonia
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Paroxonase and PAF acetylhydrolase (not drugs, but enzyme) (function, definition)
- -found in HDL
- -enzymes that reduces LDL oxidation
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bile acid sequestering drugs
- -bind to bile acids or bile salts in the intestine--> less dietary lipid digestion
- -bile acids/salts get excreted in feces
- -liver has to use new free cholesterol to resynthesize primary bile acids
- -helps to reduce free cholesterol level in the liver.
- -increases hepatic LDL-receptor
- -decreases serum LDL level
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Ezetimibe (definition and function)
- -a new drug that blocks a transporter protein.
- -reduces cholesterol absorption
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Plant Stanols and Sterols (definition and function)
- -treatment for hypercholesterolemias (type II and III)
- -instead of using statin will inhibit dolichol and CoQ enzyme synthesis
- -sterols and stanols will displace cholesterol from micelles during absorption into intestinal mucosal cells.
- -found in margarine or by pills.
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nitroglycerin (function)
- -used in treatment of myocardial ischemia
- -coverted to NO --> vasodilation of coronary blood vessels
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sapropterin (definition and function)
- -treatment of PKU
- -synthetic form of BH4
- -typically prescribed for mild forms of the disease
- -patients with enzymes that has low affinity for the cofactor
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Phencyclidine (PCP) (definition and function)
- antagonist to the NMDA (glutamate) receptor
- tranquilizer in animals
- hallucinogen in human
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cyanocobalamin (function)
- -treatment for Pernicious anemia
- -B12 deficiency due to autoimmune destruction of pareital cells
- -prietal cells produces intrinsic factor, which helps to absorb B12
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Benzodiazepines (definition and function)
- treatment for epilepsy (repeated seizures)
- anxiety reducer (ie. valium)
- bind to the GABA receptor
- potentiates GABA
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diazotized sulfanilic acid (function and defition)
- used for detecting bilirubin
- (Van den Bergh rxn)
- bilirubin reacts with diazo reagents- form red or purple colored complex
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Phenobarbital (in bilirubin)
- -treatment for Criggler-Najjar syndrome type II
- -80 % of UDP-glucuronyl transferase is gone
- -induces the synthesis of this enzyme to make more conjugate bilirubin
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Warferin
- slow acting anti-coaggulant
- inhibits Vitamin K by blocking exposide reductase
- Vitamin K is necessary cofactor for gamma-carboxylase, which carboxylates clotting factor II, VII, IX, X --> needed for better binding with platelet phospholipids
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Streptokinase (function)
- -activate plasminogen
- -cleaves hard clot of fibrin and dissolute the clotting
- (urokinase also breaks it down)
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Fomepizole (definition and function)
- competitive inhibitor drug, EtOH derivative, for alcohol dehydrogenase
- treat patients with methanol poisoning
- when methanol is digested, it forms formaldehyde (toxin in brain and visual disturbance)
- the alcohol dehydrogenase has higher affinity for ethanol than methanol.
- upon administration, treat them with sodium bicarb to neutralize the accumulated lactic acid (patients will have metabolic acidosis if just give them high EtOH)
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Metformin (function)
- decreases glucose output by liver
- increase glucose utilization by muscle (insulin resistance is improved)
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Sulfonylurea (function)
increase insulin secretion from pancreas
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tamoxifen (definition and function)
- breast cancer drug
- avoid consuming with grapefruit
- grapefruit inhibit CYP3A4 --> enzyme necessary for digesting tamoxifen
- without this enzyme, tamoxifen is less effective
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Avidin (definition and function)
- substance in white raw egg
- inhibits biotin absorption
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Menaquinone (defition)
- vitamine K
- formed by bacteria in intestine
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Phylloquinone (definition)
Vitamin K- dietary source
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Statin drugs (3 kinds)
- -Simvastatin (Zocov)
- -Pravastatin (Pravacol)
- -Lovastatin (Mevacor)
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