Biochem drugs

inhibit dihydrofolate reductase 

decreased tetrahydrofolate synthesis, which results in reduced DNA relication in mammalian cells due to less purines synthesized

• 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)

• inhibit Dihydroptroate synthase in tetrahydrofolate synthesis. 
• Only works on bacteria (microorganisms) 
• DNA synthesis stops because cells cannot divide due to decreased nucelotide synthesis. (purine)

• anti-bacterial, 
• for THF synthesis: PABA (p-aminobenzoic acid) analog. 
• Competitive inhibitor

anti-bacterial drug;

inhibits dihydrofolate reducatse on PROKARYOTES.  

reduced purine synthesis --> reduced DNA synthesis and inhibits cell divisions.

• immunosurpressant drug
• prevent graft rejection

reversible uncompetitive inhibitor of inosine monophosphate dehydrogenase ( GMP synthase) 


deprives rapidly proliferating T and B cells of key components of nucleic aicds.

• anti-gout drug or treat hyperurecemia 
• also known as Zyloprim, generic

• 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

gout treatment: microtubule inhibitor

inhibits migration of white cells to join where uric acid cystals are phagocytized. 

DOES NOT reduces serum uric acid levels.

antineoplastic drug 

• inhibits ribonucleotide diphosphate reductase 
• decreased deoxyribonucleoside diphosphate synthesis --> decreased DNA synthesis 

used for chemotherapy

• 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

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.

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

• -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.

• -antabuse
• -treatment of alcoholism
• -causes nausea and vomiting if alcohol is ingested

• -scavenger for NAPQ1, toxic compound formed from acetaminophen (tyrenol) during chronic alcoholic
• -contains cysteine and used for gultathione synthesis
• -

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)

• -Gastric& pancreatic lipase inhibitor
• -inhibits the digestion of dietary fats (TAGs) 
• -reduces dietary TAG absorption

an appetitie suppressant (increases the feeling of fullness) 

helps to manage obesity

• -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

a drug for tuberculosis 

depletes PLP so needs to supply with vitamin B6 for patients.

• - inhibit both COX-1 and COX-2
• - reduce inflammation 
• -

• -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

• -glucocordico-steroids 
• -inhibit PLA2 and COX-2 
• -inhibits all prostacyclin, thoromboxane, and leukotriene synthesis

• -anti-inflammatory drug
• -inhibits 5-lipoxyogenase

• -anti-inflammatory drug
• -inhibits 5-lipoxygenase

• -inhibit COX-1 & COX-2 
• -reversible inhibitor 
• -NSAIDs

• -anti-coagulant drug
• -inhibits thromboxane synthase

• -anti-coagulant drug
• -inhibit thromboxane synthase

• -NSAIDs
• -inhibit COX-1 and COX-2

• 1. inhibit PLA2 
• 2. inhibit 5-lipoxygenase 
• 3. inhibit receptors for cysteinyl-leukotriene

• Statin drugs
• -inhibit HMG CoA reductase
• -reduce cholesterol synthesis 
• -competitive inhibitor, structurally analog to HMG CoA

• -Statin drug
• -inhibit HMG CoA reductase
• -reduce cholesterol synthesis 
• -competitive inhibitor, structurally analog to HMG CoA

• -treatment for acquired hyperammonemia 
• -reduction of bacterial urease in the gut
• -

• -treatment for acquired hyperammonia 
• -digested by bacteria in colon to form Lactic acid to neutralize and excrete ammonia

• -found in HDL
• -enzymes that reduces LDL oxidation

• -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

• -a new drug that blocks a transporter protein. 
• -reduces cholesterol absorption

• -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.

• -used in treatment of myocardial ischemia 
• -coverted to NO --> vasodilation of coronary blood vessels

• -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

• antagonist to the NMDA (glutamate) receptor 
• tranquilizer in animals 
• hallucinogen in human

• -treatment for Pernicious anemia 
• -B12 deficiency due to autoimmune destruction of pareital cells 
• -prietal cells produces intrinsic factor, which helps to absorb B12

• treatment for epilepsy (repeated seizures)
• anxiety reducer (ie. valium)
• bind to the GABA receptor
• potentiates GABA

• used for detecting bilirubin
• (Van den Bergh rxn)
• bilirubin reacts with diazo reagents- form red or purple colored complex

• -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

• 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

• -activate plasminogen 
• -cleaves hard clot of fibrin and dissolute the clotting
• (urokinase also breaks it down)

• 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) 

• decreases glucose output by liver
• increase glucose utilization by muscle (insulin resistance is improved)

increase insulin secretion from pancreas

• breast cancer drug
• avoid consuming with grapefruit
• grapefruit inhibit CYP3A4 --> enzyme necessary for digesting tamoxifen 
• without this enzyme, tamoxifen is less effective

• substance in white raw egg
• inhibits biotin absorption

• vitamine K 
• formed by bacteria in intestine

Vitamin K- dietary source

• -Simvastatin (Zocov)
• -Pravastatin (Pravacol)
• -Lovastatin (Mevacor)