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| Drug Name | Category | Comments |
| Allopurinol | Anti-Inflammatory; Anti-Gout | It inhibits Xanthine Oxidase. Can cause an attack of acute gouty arthritis when first administered, caused by
resorption of uric acid from the tissues. Concurrent Colchicine can be given during the first week of therapy to prevent
this side-effect.
Drug Interactions: Increases blood levels of Mercaptopurines, Cyclophosphamide. |
| Colchicine | Anti-Inflammatory; Anti-Gout | Binds to tubulin to prevent polymerization of microtubules ------> prevent granulocyte migration and
phagocytosis of urate crystals ------> prevent foreign-body granulomatous inflammation in joints.
Adverse Effects: Alopecia, agranulocytosis, aplastic anemia. Myopathy, nausea, and vomiting. |
| Sulfinpyrazone | Anti-Inflammatory; Anti-Gout
Uricosuric Platelet Inhibitor |
Promotes the excretion of uric acid in the proximal tubule. Do not use when urinary uric acid levels are already high,
as urate calculi may result. Adverse Effects: Allergic dermatitis, GI disturbances.
Platelet Inhibitor: Blocks the chemical mediators of platelet aggregation. However, it also prolongs platelet survival, limiting its use in this capacity. |
| Probenecid | Anti-Inflammatory; Anti-Gout
Uricosuric Agent Anti-Microbial; Anti-Bacterial Adjunct |
Promotes the excretion of uric acid in the proximal tubule. Do not use when urinary uric acid levels are already high,
as urate calculi may result. Adverse Effects: Allergic dermatitis, GI disturbances.
Penicillin Adjunct: It blocks the urinary secretion of penicillin, prolonging its half-life. |
| Hydroxychloroquine | Anti-Inflammatory; Anti-RA
Anti-Parasitic; Anti-Malarial |
Low dose, long-term treatment for RA refractory to treatment with NSAID's. Contraindications: Porphyria, Psoriatic Arthritis. |
| Auranofin | Anti-Inflammatory; Anti-RA
Gold Salts |
29% gold, PO. Mech: Macrophages uptake the drug ------> suppress phagocytic and lysosomal activity. Gold accumulates in multiple tissues. |
| Aurothioglucose | Anti-Inflammatory; Anti-RA
Gold Salts |
50% gold, IM. Mech: Macrophages uptake the drug ------> suppress phagocytic and lysosomal activity. Gold accumulates in multiple tissues. |
| Aurothiomalate | Anti-Inflammatory; Anti-RA
Gold Salts |
50% gold, IM. Mech: Macrophages uptake the drug ------> suppress phagocytic and lysosomal activity. Gold accumulates in multiple tissues. |
| D-Penicillamine | Anti-Inflammatory; Anti-RA
Toxicity Metal Chelator |
Analog of cysteine. Retards progression of bone and articular cartilege destruction. 3-4 month latency period required.
Serious adverse effects: Leukopenia, thrombocytopenia, aplastic anemia. Cancels the effects of gold salts. Chelator: It chelates copper, mercury, zinc, lead. Indicated for Wilson's Disease. Used as adjunct in lead, mercury, gold, arsenic poisoning. Indicated for gold salt toxicity. Cystinuria: Forms a soluble penicillamine-cysteine complex, promoting the excretion of cysteine. |
| Acetominophen
(Tylenol) |
Anti-Inflammatory; Non-Opioid Analgesic | Lacks anti-inflammatory properties of other NSAID's, but is a good analgesic and anti-pyretic. Blocks prostaglandins only in the CNS. Alcohol and starvation can lead to fatal hepatotoxicity. |
| Phenacetin | Anti-Inflammatory; Non-Opioid Analgesic | Pro-drug that is rapidly converted to Acetominophen by Cyt-P450. Because of severe nephrotoxicity, phenacetin is not available in the United States. Also, metabolite, phenetidine causes methemoglobinemia. |
| Bufferin | Anti-Inflammatory; NSAID | Contains aspirin in enteric-coated granules, which are intended to prevent absorption of aspirin in the stomach, and protect the stomach mucosa from aspirin. |
| Diclofenac | Anti-Inflammatory; NSAID | Hepatotoxic, due to reactive carboxy-glucuronidate metabolites. Displaces warfarin from plasma proteins, and should not be used with warfarin. |
| Diflunisal | Anti-Inflammatory; NSAID | |
| Meclofenamate | Anti-Inflammatory; NSAID | |
| Sulindac | Anti-Inflammatory; NSAID | Pro-Drug must first be metabolized before it inhibits COX. |
| Tolmetin | Anti-Inflammatory; NSAID | Does not displace drugs from plasma binding proteins as much as others. Preferred drug for use with Warfarin. |
| Indomethacin | Anti-Inflammatory; NSAID
Anti-Gout |
Stronger and more toxic than other NSAID's.Indications: Osteoarthritis of the hip, acute gouty arthritis, ankylosing sponylitis, patent ductus arteriosus. |
| Phenylbutazone | Anti-Inflammatory; NSAID
Anti-Gout |
Potent anti-inflammatory, but weak analgesic and anti-pyretic. Indications: Acute gouty arthritis, RA that is
refractory to treatment with other NSAID's.
Adverse Effects: GI distress, peptic ulcer; can be worse than aspirin. Also soar throat, agranulocytosis. |
| Nabumetone
(Relafen) |
Anti-Inflammatory; NSAID
Long-acting |
Can be given only once a day to treat RA. |
| Oxaprozin
(Daypro) |
Anti-Inflammatory; NSAID
Long-acting |
Can be given only once a day to treat RA. |
| Piroxicam | Anti-Inflammatory; NSAID
Long-acting |
Can be given only once a day to treat RA. Causes GI disturbances in 20% of patients. |
| Acetylsalicylic Acid
(Aspirin) |
Anti-Inflammatory; NSAID
Platelet Inhibitor |
Irreversibly inhibits COX. Can cause GI disturbances, unlike other NSAID's.
Has anti-platelet activity at low doses via its inhibition of TXA2. Has anti-inflammatory properties at high doses via its inhibition of PGE1. |
| Fenoprofen | Anti-Inflammatory; NSAID
Propionic Acid Derivative |
Short-acting. Must be given 4 times a day for RA. |
| Ibuprofen
(Motrin) |
Anti-Inflammatory; NSAID
Propionic Acid Derivative |
Short-acting. Must be given 4 times a day for RA. Does not displace drugs from plasma binding proteins as much as others. Preferred drug for use with Warfarin. |
| Ketoprofen
(Orudis) |
Anti-Inflammatory; NSAID
Propionic Acid Derivative |
Short-acting. Must be given 4 times a day for RA. Unique in that it inhibits both cyclooxygenase and lipoxygenase. Does not displace drugs from plasma binding proteins as much as others. Preferred drug for use with Warfarin. |
| Naproxen | Anti-Inflammatory; NSAID
Propionic Acid Derivative |
Longer acting than the other propionic-acid derivatives. Half-life of about 13 hours. Can be given twice a day for RA. |
| Cilastatin | Anti-Microbial; Anti-Bacterial
Adjunct |
Dihydropeptidase Inhibitor in the kidney. It is coadministered with the carbapenems (imipenem), in order to prevent its destruction in the kidney. |
| Clavulanic Acid | Anti-Microbial; Anti-Bacterial
Adjunct |
beta-Lactamase Inhibitor can be used as an adjunct, only with penicillins that are not already beta-Lactamase resistant. It is counterproductive to use Clavulanic Acid with beta-Lactamase-Resistant penicillins: Naficillin, Oxacillin, Cloxacillin, Methicillin. |
| Folinic Acid | Anti-Microbial; Anti-Bacterial
Adjunct |
Given with Trimethoprim, it is the reduced form of THF. It prevents the anti-folate side-effects of trimethoprim: Megaloblastic anemia, granulocytopenia, leukopenia. |
| Pyridoxine (Vit. B6) | Anti-Microbial; Anti-Bacterial
Adjunct |
Given with Isoniazid, it prevents the peripheral neuritis side-effect that can be seen with this drug. The peripheral neuritis results from an anti-pyridoxine effect. |
| Sulbactam | Anti-Microbial; Anti-Bacterial
Adjunct |
beta-Lactamase Inhibitor, similar to Clavulinic Acid. |
| Dapsone | Anti-Microbial; Anti-Bacterial
Anti-Mycobacterial |
Indicated for treating Leprosy. Resistance is on the rise.
Adverse Effects: Hemolytic anemia in people with G6PD deficiency, Erythema Nodosum, Methemoglobinemia. |
| Ethambutol | Anti-Microbial; Anti-Bacterial
Anti-Mycobacterial; 1st-line |
First line drug. Mech: probably inhibits polyamine synthesis. Gets into CNS.
Adverse effect: Optic Neuritis with loss of visual acuity. |
| Isoniazid | Anti-Microbial; Anti-Bacterial
Anti-Mycobacterial; 1st-line |
First line drug, and used for chemoprophylaxis. Mech: it blocks mycolic acid synthesis. Gets into CNS.
Adverse Effects: Hepatotoxicity in elderly, peripheral neuritis in slow acetylators. Optic neuritis, teratogenic. |
| Pyrazinamide | Anti-Microbial; Anti-Bacterial
Anti-Mycobacterial; 1st-line |
First-line drug. Adverse Effects: Hepatotoxicity, Hyperuricemia. |
| Rifampin | Anti-Microbial; Anti-Bacterial
Anti-Mycobacterial; 1st-line |
First line drug. Mech: It inhibits RNA synthesis by binding to the beta-subunit of bacterial RNA-Polymerase. Gets into CNS. Adverse Effects: Hepatotoxicity. |
| Capreomycin | Anti-Microbial; Anti-Bacterial
Anti-Mycobacterial; 2nd-line |
|
| Ethionamide | Anti-Microbial; Anti-Bacterial
Anti-Mycobacterial; 2nd-line |
Second-line drug. Mech: Analog of Isioniazid that also inhibits mycolic acid synthesis.
Adverse Effects: Intense gastric pain, may be neurotoxic. |
| Para aminosalicylic acid (PAS) | Anti-Microbial; Anti-Bacterial
Anti-Mycobacterial; 2nd-line |
Second-line drug. PO. Mech: It blocks dihydropteroate synthesis in mycobacteria but not in other bacteria. This is
same mode of action as the sulfonamides, but on different bugs.
Adverse Effects: Severe GI disturbances and pain; hypersensitivity. Impaired liver function. |
| Cycloserine | Anti-Microbial; Anti-Bacterial
Anti-Mycobacterial; 2nd-line ICWS |
Second-line anti-mycobacterial drug. Mech: It inhibits alanine racemase.
Adverse Effects: CNS Toxicity, drug-induced psychosis greatly limit its use. |
| Ciprofloxacin | Anti-Microbial; Anti-Bacterial
DNA Gyrase Inhibitor |
Fluoroquinolone. PO or IV. |
| Nalidixic Acid | Anti-Microbial; Anti-Bacterial
DNA Gyrase Inhibitor |
Quinolone that blocks Topoisomerase II. Effective against gram-negatives. |
| Norfloxacin | Anti-Microbial; Anti-Bacterial
DNA Gyrase Inhibitor |
Fluoroquinolone. PO. |
| Ofloxacin | Anti-Microbial; Anti-Bacterial
DNA Gyrase Inhibitor |
Fluoroquinolone. |
| Imipenam | Anti-Microbial; Anti-Bacterial
ICWS; Carbopenem |
Broad-spectrum antibiotic. Pseudomonas can develop resistance, so give this drug with an aminoglycoside.
Must be coadministered with cilistatin, to prevent its degradation (by dihydropeptidase) in the kidney. |
| Meropenem | Anti-Microbial; Anti-Bacterial
ICWS; Carbopenem |
|
| Primaxin
(Imipenam + Cilistatin) |
Anti-Microbial; Anti-Bacterial
ICWS; Carbopenem |
Combination of imipenam and cilistatin is called primaxin. |
| Cefadroxil | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 1st generation |
PO administration. |
| Cefazolin | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 1st generation |
IV. Excreted mainly by glomerular filtration (rather than active tubular secretion), thus it has a longer half-life. |
| Cephalexin | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 1st generation |
PO administration. |
| Cephalothin | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 1st generation |
IV. Short-half life, due to active (probenecid-sensitive) tubular secretion. |
| Cefaclor | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 2nd generation |
PO administration. |
| Cefamandole | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 2nd generation |
May show Disulfarim-like reaction; don't take with EtOH.
Cephalosporinase-resistant. |
| Cefonicid | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 2nd generation |
Excreted mainly by glomerular filtration (rather than active tubular secretion), thus it has a longer half-life. |
| Ceforanide | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 2nd generation |
|
| Cefoxitin | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 2nd generation |
IV. Cephalosporinase-resistant. |
| Cefuroxine | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 2nd generation |
IV |
| Cefixime | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 3rd generation |
PO administration. Can penetrate into the CNS. |
| Cefoperazone | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 3rd generation |
Active against Pseudomonas.
Can penetrate into the CNS. Biliary excretion, longer half-life. Cephalosporinase-resistant. May show Disulfarim-like reaction; don't take with EtOH |
| Cefotaxime | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 3rd generation |
IV. Can penetrate CNS.
Cephalosporinase-resistant. |
| Ceftazidime | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 3rd generation |
IV. |
| Ceftazidime | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 3rd generation |
Active against Pseudomonas. |
| Ceftizoxime | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 3rd generation |
Can penetrate CNS. |
| Ceftriaxone | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 3rd generation |
IV. Biliary excretion, longer half-life. |
| Moxalactam | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 3rd generation |
IV. Penetrates CNS.
Adverse Effects: May show Disulfarim-like reaction; don't take with EtOH. May also see occassional bleeding. |
| Cefepine | Anti-Microbial; Anti-Bacterial
ICWS; Cephalosporin 4th generation |
Actually a fourth generation, brand new drug, with extended spectrum and greater resistance to beta-Lactamase inactivation. |
| Bacitracin | Anti-Microbial; Anti-Bacterial
ICWS; Intracellular |
Bactericidal. It is only used as a topical antibacterial. Severe nephrotoxicity prevents systemic use. Inhibits cell-wall synthesis intracellularly. |
| Vancomycin | Anti-Microbial; Anti-Bacterial
ICWS; Intracellular |
Given IV for gram-positives, or PO for GI superinfections (as a topical, intraluminal antibiotic). It is not absorbed
through the GI tract.
MECH = inhibit peptidoglycan synthesis intracellularly -- rather than extracellularly as in the beta-lactams. Resistance is a recent problem. |
| Aztreonam | Anti-Microbial; Anti-Bacterial
ICWS; Monobactam |
beta-Lactamase resistant. Effective against gram-negative aerobes such as Pseudomonas, Serratia. Little or no activity against gram-positives or anaerobes. |
| Augmentin
(Amoxicillin + Clavulanic Acid) |
Anti-Microbial; Anti-Bacterial
ICWS; Penicillins |
Combination of Amoxicillin and Clavulanic Acid is called Augmentin. Good choice for pediatric Otitis Media. |
| Benzathine Penicillin G | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins |
Relatively insoluble salt of penicillin is given IM as a "depot" preparation, for long-term storage in muscle and sustained release. |
| Penicillin G | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins |
Active against gram-positives. |
| Penicillin V | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins |
Acid-stable Pencillin G, thus it can be given PO. Active against Gram-positives. |
| Amoxacillin | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Broad-Spectrum |
Broad-spectrum agent. Increased gram-negative activity |
| Ampicillin | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Broad-Spectrum |
Broad-spectrum agent. PO. Increased gram-negative activity. Acid-stable, but beta-lactamase sensitive.
90% of patients with Mononucleosis get a rash while receiving this drug. |
| Carbenicillin indamyl | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Extended-Spectrum |
Extended-Spectrum agent.
Acid-stable ester of carbenicillin, recently developed, that can be given orally. |
| Carbenicillin | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Extended-Spectrum |
IV, acid-labile drug.
Extended-Spectrum agent. Proteus and Pseudomonas. For Pseudomonas, use combination therapy with aminoglycoside, as rapid resistance can develop. |
| Mezlocillin | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Extended-Spectrum |
Extended-Spectrum agent. Proteus and Pseudomonas. |
| Piperacillin | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Extended-Spectrum |
Extended-Spectrum agent. Proteus, Pseudomonas and Klebsiella. |
| Ticarcillin | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Extended-Spectrum |
Extended-Spectrum agent. Proteus and Pseudomonas. |
| Cloxacillin | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Penicillinase-Resistant |
Similar to Penicillin G. PO. Highly protein-bound.
beta-Lactamase Resistant, Acid Stable |
| Dicloxacillin | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Penicillinase-Resistant |
Similar to Penicillin G. PO. Highly protein-bound.
beta-Lactamase Resistant, Acid Stable |
| Floxacillin | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Penicillinase-Resistant |
Similar to Penicillin G. PO. Highly protein-bound.
beta-Lactamase Resistant, Acid Stable |
| Methicillin | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Penicillinase-Resistant |
Given only IV, because it is acid-labile. Altered PBP's appears to be the mode of resistance in the case of Staph. Aureus. beta-Lactamase Resistant. |
| Nafcillin | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Penicillinase-Resistant |
Similar to Penicillin G. PO. Unique biliary excretion.
beta-Lactamase Resistant, Acid Stable |
| Oxacillin | Anti-Microbial; Anti-Bacterial
ICWS; Penicillins Penicillinase-Resistant |
Similar to Penicillin G. PO. Highly protein-bound.
beta-Lactamase Resistant, Acid Stable |
| Colistmethate | Anti-Microbial; Anti-Bacterial
Membrane-Active |
Only used topically: ointment, or injection into pleural or joint cavities. Can be used topically for gram-negative bacterial overgrowth. |
| Polymixin B | Anti-Microbial; Anti-Bacterial
Membrane-Active |
Only used topically: ointment, or injection into pleural or joint cavities. Can be used topically for gram-negative bacterial overgrowth. |
| Trimethoprim | Anti-Microbial; Anti-Bacterial
Metabolic Inhibitor |
Inhibits dihydrofolate reductase. Indicated for complicated UTI's. as a second-line drug, and AIDS Pneumocystic Pneumonia. Other uses too. |
| Co-Trimoxazole
(Sulfamethoxazole-Trimethoprim) |
Anti-Microbial; Anti-Bacterial
Metabolic Inhibitor; Sulfonamide |
Adverse Effects: May see adverse effects of either constituent drug, as well as fever, rashes, vomiting, diarrhea. Side-effects prominent in AIDS patients receiving the drug for the treatment of Pneumocystis Pneumonia. |
| Mafenide
(Sulfamylon) |
Anti-Microbial; Anti-Bacterial
Metabolic Inhibitor; Sulfonamide |
Does not have a para-amino group, thus it has a different structure and mode of action, and it is not an analog of PABA. It is not inactives by the presence of pus or necrotic tissue, thus it is ideal to use with burn patients. |
| Silver Sulfadiazine | Anti-Microbial; Anti-Bacterial
Metabolic Inhibitor; Sulfonamide |
Topical administration, for treating burn patients. |
| Sodium Sulfacetamide | Anti-Microbial; Anti-Bacterial
Metabolic Inhibitor; Sulfonamide |
Ophthalmic administration, for treating conjunctivitis. |
| Sulfacytine | Anti-Microbial; Anti-Bacterial
Metabolic Inhibitor; Sulfonamide |
|
| Sulfadiazine | Anti-Microbial; Anti-Bacterial
Metabolic Inhibitor; Sulfonamide |
Used to treat systemic infections. |
| Sulfamethoxazole | Anti-Microbial; Anti-Bacterial
Metabolic Inhibitor; Sulfonamide |
Used widely in UTI's. |
| Sulfapyridine | Anti-Microbial; Anti-Bacterial
Metabolic Inhibitor; Sulfonamide |
Used to treat Dermatitis Herpetiformis. |
| Sulfasalazine
(Salicyl-azosulfapyridine) |
Anti-Microbial; Anti-Bacterial
Metabolic Inhibitor; Sulfonamide |
Poorly absorbed in GI tract. Used for the topical treatment of inflammatory bowel disease. The drug is cleaved by bacteria in the colon, into sulfonamide and amino-salicylate. Amino-salicylate then has local anti-inflammatory effects in the colon. |
| Sulfisoxazole | Anti-Microbial; Anti-Bacterial
Metabolic Inhibitor; Sulfonamide |
Used widely in UTI's. Also used to treat Nocardiosis. |
| Chloramphenicol | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor |
Indicated for CNS infections, Salmonella Typhoid Fever, H. Influenzae.
Toxicity: (1) Dose-dependent anemia, (2) aplastic anemia, (3) gray-baby syndrome, due to lack of glucuronyl-transferase in babies. |
| Clindamycin | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor |
Similar to erythromycin. C. Difficile is resistant, thus Pseudomembranous Colitis is a feared complication of the drug. Indicated for mixed anaerobic infections. |
| Spectinomycin | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor |
Structurally related to aminoglycosides. Administered IM for treatment of penicillin-resistant gonorrhea. |
| Azithromycin | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor; Macrolide |
|
| Clarithromycin | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor; Macrolide |
|
| Erythrmoycin | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor; Macrolide |
IV or PO. Orally, it must be given in an acid-resistant (enteric coated) capsule, to prevent acid-breakdown in the
stomach.
Often used in penicillin-allergic patients. Indications: Chlamydia, Mycoplasma Pneumonia, Cornybacteria, Legionnaire's Disease. |
| Erythromycin Estolate | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor; Macrolide |
Acid-resistant ester of erythromycin can be given PO. Cholestatic hepatitis can occur with use. |
| Spiramycin | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor; Macrolide Anti-Parasitic |
Indicated for treatment of Cryptosporidiosis. |
| Chlortetracycline | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor; Tetracycline |
Very incomplete oral absorption. Like tetracycline. |
| Demeclocycline | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor; Tetracycline |
Complete oral absorption. Intermediate half-life. Used to treat the Syndrome of Inappropriate ADH secretion (SIADH). Photosensitive: especially photosensitive and associated with Fanconi-like syndrome if it has been photo-degraded. |
| Doxycycline | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor; Tetracycline |
Complete oral absorption. Exclusively hepatic clearance. |
| Minocycline | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor; Tetracycline |
Complete oral absorption. Long-lasting. |
| Oxytetracycline | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor; Tetracycline |
Incomplete oral absorption |
| Tetracycline | Anti-Microbial; Anti-Bacterial
Synthesis Inhibitor; Tetracycline |
Incomplete oral absorption, but it's still given orally.
Indicated for Rickettsiae, Chlamydia, Mycoplasma, Lyme Disease. It's a broad-spectrum antibiotic, so you can also see bacterial superinfection. It chelates calcium: never use during pregnancy, never give to children, do not take with food. |
| Amikacin | Anti-Microbial; Anti-Bacterial
Synthesis Inhitor; Aminoglycoside |
Newest agents. Currently effective against strains that are resistant to the other aminoglycosides. |
| Gentamicin | Anti-Microbial; Anti-Bacterial
Synthesis Inhitor; Aminoglycoside |
Older drug. Popular choice for gram-negatives, in combination with penicillins. |
| Kanamycin | Anti-Microbial; Anti-Bacterial
Synthesis Inhitor; Aminoglycoside |
Older drug. Now only used as topical agent, due to severity of adverse effects. |
| Neomycin | Anti-Microbial; Anti-Bacterial
Synthesis Inhitor; Aminoglycoside |
Now only used as topical agent, due to severity of adverse effects. |
| Netilmicin | Anti-Microbial; Anti-Bacterial
Synthesis Inhitor; Aminoglycoside |
Newest agents. Currently effective against strains that are resistant to the other aminoglycosides. |
| Tobramycin | Anti-Microbial; Anti-Bacterial
Synthesis Inhitor; Aminoglycoside |
Newer drug. Popular choice for gram-negatives, in combination with penicillins. Slightly less nephrotoxic than gentamicin. |
| Streptomycin | Anti-Microbial; Anti-Bacterial
Synthesis Inhitor; Aminoglycoside Anti-Mycobacterial; 1st-line |
IM. Older drug with severe adverse effects. Now has widespread resistance. First-line drug for TB infections. |
| Nitrofurantoin | Anti-Microbial; Anti-Bacterial
UTI Antiseptic |
Used solely for treatment of UTI's. Cleared extremely quickly to urine, where it can have bacteriostatic or bactericidal effects. Mech = formation of oxidative intermediates in urinary tract. |
| Flucytosine | Anti-Microbial; Anti-Fungal | Gets into CNS. Converted to 5-fluorocytosine by fungal enzymes, then it inhibits thymidilate synthetase and DNA
synthesis. Resistance develops rapidly, so it is used in conjunction with Amphotericin-B.
Relatively non-toxic. May see alopecia, bone-marrow suppression. |
| Griseofulvin | Anti-Microbial; Anti-Fungal | It binds to fungal microtubules, inhibiting their growth. It is only effective for skin infections.
It is given PO and binds to keratin, thus it concentrates in skin. High fat meal increases absorption. Indications: skin infections, ring worm, athlete's foot. Adverse effects: allergic reactions, headache, malaise. |
| Potassium Iodide (KI) | Anti-Microbial; Anti-Fungal | Singularly effective against Sporothrix Schenkii cutaneous infection. |
| Fluconazole | Anti-Microbial; Anti-Fungal
Imidazole (Systemic) |
Pharmacokinetics: PO or IV. Readily enters CNS. Inhibits Cyt-P450 in liver. Primarily urinary excretion.
Adverse Effects: Hepatotoxicity, nausea and vomiting. Indicated for Cryptococcal Meningitis. |
| Itraconazole | Anti-Microbial; Anti-Fungal
Imidazole (Systemic) |
Broader spectrum and fewer adverse effects than ketoconazole. |
| Ketoconazole | Anti-Microbial; Anti-Fungal
Imidazole (Systemic) |
Pharmacokinetics: PO, with good oral absorption. Inhibits Cyt-P450 in liver. Biliary excretion.
Adverse Effects: Hepatotoxicity, gynecomastia, thrombophlebitis. Can be used in treatment of prostate cancer, due to anti-androgenic effects. |
| UK-109,496 | Anti-Microbial; Anti-Fungal
Imidazole (Systemic) |
Experimental imidazole that binds so strongly to ergosterol, it is classified as fungicidal. Broad-spectrum of action, and effective against Aspergillus. |
| Miconazole | Anti-Microbial; Anti-Fungal
Imidazole (Topical, Systemic) |
Pharmacokinetics: Topical or IV. Not absorbed orally. Biliary excretion.x
Adverse Effects: Nausea and vomiting when given IV. It potentiates warfarin. |
| Clotrimazole | Anti-Microbial; Anti-Fungal
Imidazole (Topical) |
Topical use only. Not absorbed orally. |
| Amphotericin B | Anti-Microbial; Anti-Fungal
Polyene |
Attacks ergosterol causing cell lysis. Broad-spectrum. Is not absorbed orally. Given IV for systemic infections, but
doesn't readily penetrate CNS.
Adverse Effects: "Amphoterrible" fever, chills, nephrotoxicity, anemia, hepatotoxicity. |
| Nystatin | Anti-Microbial; Anti-Fungal
Polyene (Topical) |
Topical use only. Drug is not absorbed orally, and side-effects are too severe for systemic use. Available OTC for dermal fungal infections, or used orally for intraluminal GI fungal overgrowth infections. Can also be used for intestinal amebiasis. |
| Mebendazole | Anti-Microbial; Anti-Parasitic
Anti-Helminthitic |
Given PO, but only about 10% is absorbed (poorly absorbed). It inhibits microtubule synthesis in nematodes. Indicated for pinworms, hookworms, ascariasis. |
| Piperazine | Anti-Microbial; Anti-Parasitic
Anti-Helminthitic |
Mech: It inhibits acetylcholine in helminths (non-depolarizing blockade). It thus antagonizes the effects of Pyrantel Pamoate. |
| Praziquantel | Anti-Microbial; Anti-Parasitic
Anti-Helminthitic |
Well-absorbed orally. It increases permeability of helminthitic cell membrane to calcium, causing contraction, paralysis, death. Indicated for Schistosomiasis and other fluke infections. |
| Pyrantel Pamoate | Anti-Microbial; Anti-Parasitic
Anti-Helminthitic |
Poorly absorbed orally. Triggers the release of acetylcholine in helminths, causing depolarizing neuromuscular blockade, paralysis. Indicated for broad-spectrum treatment of luminal intestinal infections. Ascariasis, pinworm. |
| Thiabendazole | Anti-Microbial; Anti-Parasitic
Anti-Helminthitic |
Well-absorbed orally. It blocks microtubule synthesis., and may also inhibit fumarate reductase in the parasite. Indicated for nematode infections. |
| Amodiaquine | Anti-Microbial; Anti-Parasitic
Anti-Malarial |
Blood schizonticide. |
| Mefloquine | Anti-Microbial; Anti-Parasitic
Anti-Malarial |
Only PO. Primarily used for prophylaxis and treatment of Chloroquine-resistant P. Falciparum strains. Adverse Effects: Can have bad CNS and psychological effects. |
| Primaquine | Anti-Microbial; Anti-Parasitic
Anti-Malarial |
It is the one and only tissue schizonticide, required for treatment of P. Ovale and P. Vivax hypnozoite (dormant) tissue-infections. Adverse Effects: Hemolytic anemia in persons with G6PD-Deficiency. |
| Pyrimethamine | Anti-Microbial; Anti-Parasitic
Anti-Malarial |
Inhibits Plasmodium dihydrofolate reductase, similar to trimepthoprim. Indicated for treatment of Chloroquine-resistant P. Falciparum. Adverse Effects: Anti-Folate effects, megaloblastic anemia. |
| Quinidine Gluconate | Anti-Microbial; Anti-Parasitic
Anti-Malarial |
|
| Chloroquine | Anti-Microbial; Anti-Parasitic
Anti-Malarial Anti-Inflammatory; Anti-Arthritis |
Usually PO, also IV, IM. Most popular blood schizonticide. Extensive tissue binding requires large loading dose.
Resistance is common and occurs by P. Falciparum making phosphoglycoprotein pumps to pump out the drug.
Adverse Effects: generally well-tolerated; long-term retinopathyy, myopathy, ototoxicity.
Also: Low dose, long-term treatment for RA refractory to treatment with NSAID's. |
| Fansidar (Pyrimethamine-Sulfadoxine) | Anti-Microbial; Anti-Parasitic
Anti-Malarial Anti-Protozoal |
Similar to Co-Trimoxazole, except for parasites. Pyrimethamine: inhibit dihydrofolate reductase. Sulfadoxine: inhibit
dihydropteroate synthetase.
Slow-acting, and resistance can be a problem. |
| Diloxanide Furoate | Anti-Microbial; Anti-Parasitic
Anti-Protozoal |
Given orally, Diloxinide is the active drug, released by gut bacteria. Mild drug used to combat intestinal amebiasis. Well-tolerated. |
| Melarsoprol | Anti-Microbial; Anti-Parasitic
Anti-Protozoal |
Indicated for the late meningeal stages of Trypanosomiasis (T. Gambiense). |
| Nifurtimox | Anti-Microbial; Anti-Parasitic
Anti-Protozoal |
Indicates for Chagas Disease (T. Cruzi) |
| Paromomycin | Anti-Microbial; Anti-Parasitic
Anti-Protozoal |
Indicated for intestinal amebiasis. |
| Pentamidine | Anti-Microbial; Anti-Parasitic
Anti-Protozoal |
IM or aerosol; not absorbed orally. Indications: Trypanosomiasis, first-line therapy for Pneumocystic Cariini
infection in AIDS patients. Second-line therapy for many other parasitic infections.
Adverse Effects: Histamine degranulation can lead to life-threatening hypotension. Also can see hypoglycemia or hyperglycemia, TPP, nephrotoxicity, anemia. |
| Sodium Stibogluconate | Anti-Microbial; Anti-Parasitic
Anti-Protozoal |
Indicated for Leshmaniasis. |
| Suramin | Anti-Microbial; Anti-Parasitic
Anti-Protozoal |
Indicated for Tryanosomiasis. |
| Metronidazole | Anti-Microbial; Anti-Parasitic
Anti-Protozoal Anti-Bacterial |
Mech: Parasites reduce a nitro group on the drug and form oxidative intermediates that do oxidative damage. Indicated for a wide variety of intestinal and tissue parasitic infections: Trichomoniasis, Giardiasis, Amebiasis, Leshmaniasis. Also indicated for treating Bacteroides and other serious anaerobic bacterial infections. |
| Foscarnet | Anti-Microbial; Anti-Viral | Indicated for treatment of (1) CMV Retinitis (administer with Ganciclovir), and (2) Serious HSV or VZV infections that are resistant to treatment by Acyclovir. Serious Adverse Effect: It chelates Ca+2 which can lead to life-threatening hypocalcemia. |
| 3-Deoxythmidin-2-ene
(d4T)
(Stavudine) |
Anti-Microbial; Anti-Viral
Anti-AIDS; Nucleoside Analog |
|
| Dideoxycytosine (ddC) | Anti-Microbial; Anti-Viral
Anti-AIDS; Nucleoside Analog |
|
| Dideoxyinosine (ddI) | Anti-Microbial; Anti-Viral
Anti-AIDS; Nucleoside Analog |
|
| Lamivudine (3TC) | Anti-Microbial; Anti-Viral
Anti-AIDS; Nucleoside Analog |
|
| Azidothymidine (AZT)
(Zidovudine) |
Anti-Microbial; Anti-Viral
Anti-AIDS; Nucleoside Analog Immunosuppressant |
Half-life of 1-3 hrs. Gets into CNS (60%). Mech: It is phosphorylates to the triphosphate form, which is the active
form. Then, (1) It competitively inhibits HIV Reverse Transcriptase, and (2) It is a chain-terminator of HIV viral
DNA synthesis. Resistance is common, due mutations in viral Reverse Transcriptase.
Adverse Effects: May be severe. Bone marrow depression. Headaches, agitation, insomnia. |
| Indinavir | Anti-Microbial; Anti-Viral
Anti-AIDS; Protease Inhibitor |
|
| Ritonavir | Anti-Microbial; Anti-Viral
Anti-AIDS; Protease Inhibitor |
|
| Saquinavir | Anti-Microbial; Anti-Viral
Anti-AIDS; Protease Inhibitor |
Well tolerated, but low oral bioavilability (5%). |
| Interferon-alpha (IFN-alpha) | Anti-Microbial; Anti-Viral
Endogenous Factor |
Enhances host-cell resistance to viral infections, and possibly some tumors. Adverse effects: fever, malaise, headaches, anemia, GI distress. |
| Acyclovir | Anti-Microbial; Anti-Viral
Nucleoside Analog |
Indicated for HSV-1, HSV-2, VZV. Used topically for skin lesions, or IV for encephalitis or neonatal disease. It is
activated by HSV viral Thymidine Kinase ------> (1) it binds and inhibits viral DNA polymerase, and (2) it is
incorporated into viral DNA, where it acts as a chain-terminator.
Resistance in HSV is due to mutations in Thymidine Kinase or the DNA Polymerase.. |
| Ganciclovir | Anti-Microbial; Anti-Viral
Nucleoside Analog |
Indicated for CMV. Deoxyguanosine analog, it reversibly inhibits viral DNA polymerase. Works similar to
Acyclovir.
Adverse Effects are bad: Neutropenia (common), anemia, eosinophila. Also CNS changes (headache, behavioral changes, seizure, coma), fever, rash, phlebitis, nausea. |
| Ribavirin | Anti-Microbial; Anti-Viral
Nucleoside Analog |
Aerosol spray. Nucleoside analog blocks the formation of GTP. Indicated for severe Respiratory Syncitial Virus (RSV) infections in infants. No serious adverse effects. |
| Vidarabine (Ara-A) | Anti-Microbial; Anti-Viral
Nucleoside Analog |
Topical or IV. It inhibits DNA synthesis by affecting DNA polymerase. Indicated for HSV, Varicella-Zoster. Adverse effects are minimal: nausea, vomiting, possible neurotoxicity. |
| Amantidine | Anti-Microbial; Anti-Viral
Uptake Inhibitor |
It inhibits viral absorption and uptake. Indicated for Influenza A, Rubella. Used prophylactically after Influenza-A exposure.Adverse Effects: Insomnia, restlessness, nervousness, depression. |
| Rinantidine | Anti-Microbial; Anti-Viral
Uptake Inhibitor |
Longer half-life than Amantadine, biliary excretion. Perhaps fewer CNS effects. |
| Taxol | Chemotherapy
Alkaloid; Paclitaxel |
IV only; biliary excretion. Extensively metabolized by the liver. It stabilizes the mitotic spindle during metaphase,
causing metaphase arrest.
Indications: head and neck carcinomas, ovarian carcinomas, breast cancers, lung cancers. Adverse Effects: bone marrow suppression, peripheral neuropathy. |
| Etoposide (VP-16) | Chemotherapy
Alkaloid; Podophyllotoxin |
IV only; urinary excretion. It inhibits topoisomerase II ------> cause DNA strand breaks, increase DNA degradation.
Indications: small-cell lung cancer, lymphomas and leukemias, testicular carcinoma. |
| Teniposide (VM-26) | Chemotherapy
Alkaloid; Podophyllotoxin |
|
| Vinblastine | Chemotherapy
Alkaloid; Vinca Alkaloid |
IV only; biliary excretion. Binds to microtubules ------> inhibits the mitotic spindle, causing metaphase arrest.
More likely to show bone marrow toxicity than Vincristine.
Indications: Testicular carcinoma, breast cancers, lymphomas. |
| Vincristine | Chemotherapy
Alkaloid; Vinca Alkaloid |
IV only; biliary excretion. Binds to microtubules ------> inhibits the mitotic spindle, causing metaphase arrest.
Less likely to suppress bone marrow than Vinblastine, but do see peripheral neuropathy which is dose-limiting.
Indications: Part of the MOPP group of drugs, to fight Hodgkin's Disease. Also acute leukemias, Non-Hodgkin's Lymphomas. |
| Glutatione S-Transferases (GST's) | Chemotherapy; Adjunct | Experimental. In rats and monkeys, when injected directly into lymphocytes (inject in vitro and then reimplant in the animal), it prevents lymphocyte death, helping to alleviate bone-marrow suppression before it occurs. Hasn't been tried in humans yet. |
| Granulocyte Colony Stimulating Factor
(G-CSF) |
Chemotherapy; Adjunct | It is thought to mobilize peripheral hematopoeitic stem cells. It can be given to combat the bone-marrow suppression side-effects of chemotherapy drugs. |
| Ondansetron | Chemotherapy; Adjunct | Serotonin antagonist can be given to alleviate nausea associated with chemotherapy. Phenothiazines and other drugs can also be used. |
| Verapamil | Chemotherapy; Adjunct | Ca+2-channel blocker can competitively inhibit phosphoglycoprotein pumps in tumor cells, thus hopefully helping to combat this form of resistance. Clinical trials are under way. |
| Busulfan | Chemotherapy; Alkylating Agent
Alkylsulfonate |
Alkylsulfonate, pro-drug, oral. Indicated for Chronic Myelogenous Leukemia.
Adverse Effects: Adrenal Insufficiency, increased skin pigmentation. Pulmonary fibrosis. |
| Thiotepa | Chemotherapy; Alkylating Agent
Aziridine |
Aziridine, pro-drug. IV. |
| Triethylenemalamine | Chemotherapy; Alkylating Agent
Aziridine |
Aziridine, pro-drug. IV. |
| Procarbazine | Chemotherapy; Alkylating Agent
Hydrazine |
Hydrazine. Part of the MOPP group of drugs, to fight Hodgkin's Disease. Adverse Effects: Has especially high incidence of secondary malignancies, particularly leukemias. |
| Chlorambucil | Chemotherapy; Alkylating Agent
Nitrogen Mustard |
Nitrogen Mustard, Oral. Indicated for lymphomas, CLL. |
| Mechlorethamine | Chemotherapy; Alkylating Agent
Nitrogen Mustard |
Nitrogen Mustard, IV. Directly toxic. It has the shortest half-life (a few minutes) and is the least stable of all alkylating agents. Is often infused directly into artery supplying the tumor, due to its short half-life. Part of the MOPP group of drugs, to fight Hodgkin's Disease. |
| Melphalan | Chemotherapy; Alkylating Agent
Nitrogen Mustard |
Nitrogen Mustard, Oral. Indicated for Multiple Myeloma. |
| Cyclophosphamide | Chemotherapy; Alkylating Agent
Nitrogen Mustard Immunosuppressant |
Pro-drug, oral. It is converted to its active form by Cytochrome-P450 enzyme.
Broad-spectrum agent Useful at fighting solid tumors, leukemias, ovarian carcinoma. Immunosuppresant: Bone marrow transplants (but it does not prevent GVHD), autoimmune disorders (PRCA, Wegener's Granulomatosis). Adverse Effect: Hemorrhagic cystitis, higher incidence of alopecia than other drugs. |
| Carmustine (BCNU) | Chemotherapy; Alkylating Agent
Nitrosurea |
Nitrosurea, pro-drug. IV. Gets into CNS, thus useful for treating brain cancers. |
| Lomustine (CCNU) | Chemotherapy; Alkylating Agent
Nitrosurea |
Nitrosurea, pro-drug. IV. Gets into CNS, thus useful for treating brain cancers. |
| Streptozotocin | Chemotherapy; Alkylating Agent
Nitrosurea |
Indicated for malignant pancreatic insulinoma. |
| Carboplatin | Chemotherapy; Alkylating Agent
Platinum Complex |
Platinum complex, similar to Cis-Platin. |
| Cis-Platin | Chemotherapy; Alkylating Agent
Platinum Complex |
Forms Platinum complex, a unique platinum-bond with DNA causes both damage and cross-linkage of DNA strands.
Broad-spectrum agent. Useful at fighting solid tumors: breast, ovarian, testicular, lung, bladder cancers.
Adverse Effect: Relatively non-toxic to bone marrow, but does have nephrotoxicity which is dose-limiting. |
| Bleomycin | Chemotherapy; Antibiotic | Only IV. Bleomycin hydrolase inactivates the drug in the liver and kidney, but the enzyme is not found in skin and
lungs.
It is the only cell-cycle specific (CCS) agent among the antibiotics. It intercalates between DNA base pairs, and it also chelates iron, generating oxygen radicals which further damage the DNA. Indicated for testicular carcinoma. Adverse Effects: Irreversible pulmonary fibrosis. |
| Dactinomycin | Chemotherapy; Antibiotic | Only IV. It tightly intercalates DNA between G-C base pairs, blocking transcription. DNA replication is only slightly affected. |
| Mithramycin | Chemotherapy; Antibiotic | |
| Mitomycin C | Chemotherapy; Antibiotic | Only IV. It is metabolized to 6-Mercaptopurine, active metabolite, which then cross-links with DNA.
Indications: Solid tumors of cervix, stomach, pancreas, lung, bladder, colon. May be instilled directly into bladder to treat bladder carcinoma. Adverse Effects: pronounced and long-lived bone-marrow suppression. |
| Plicamycin | Chemotherapy; Antibiotic | Only IV. It binds to DNA as a ternary complex with Mg+2, blocking transcription.
Indications: used primarily to combat paraneoplastic hypercalcemia. It has an inhibitory effect on osteoclasts, slowing down bone resorption. |
| Daunorubicin | Chemotherapy; Antibiotic
Anthracycline |
Only IV. Undergoes extensive metabolism in the liver. They are intercalating agents, blocking both replication and
transcription by non-covalent interactions. Adverse Effect = Cumulative cardiotoxicity, which can be potentially fatal.
Indications: Narrower in spectrum, used only against Acute Leukemias. |
| Doxorubicin | Chemotherapy; Antibiotic
Anthracycline |
Only IV. Undergoes extensive metabolism in the liver. They are intercalating agents, blocking both replication and
transcription by non-covalent interactions. Cumulative cardiotoxicity, which can be potentially fatal.
Indications: Broad-spectrum agent, used in combo chemotherapy to treat many tumors. |
| Mitoxantrone | Chemotherapy; Antibiotic
Anthracycline; Synthetic |
The only synthetic anti-cancer antibiotic, with properties similar to the other Anthracyclines. They are intercalating
agents, blocking both replication and transcription by non-covalent interactions. Cumulative cardiotoxicity, which can
be potentially fatal.
Indications: Used for Acute Myelogenous Leukemia (AML), non-Hodgkin's Lymphomas, breast cancer. |
| 5-Fluorouracil (5-FU) | Chemotherapy; Antimetabolite | Pyrimidine antagonist. Must be given IV. Active metabolite is 5-FdUMP, which inhibits thymydilate synthetase
------> cell death due to lack of thymine. Resistance: decreased bioactivation of 5-FU, mutations in thymydilate
synthetase, increased levels of thymidilate synthetase.
Indications: GI tumors, head and neck carcinomas. |
| 6-Mercaptopurine (6-MP) | Chemotherapy; Antimetabolite | Purine antagonist. Effective orally. It is converted to its active nucleotide form by HGPRT. Resistance primarily due
to lower amounts of HGPRT; increased levels of alkaline phosphphydrolase can also inactivate the active metabolites.
Drug is eliminated by xanthine oxidase, so Allopurinol raises its blood levels and potentiates its effects. |
| 6-Thioguanine (6-TG) | Chemotherapy; Antimetabolite | Purine antagonist. Effective orally. It is converted to its active nucleotide form by HGPRT. Resistance primarily due to lower amounts of HGPRT; increased levels of alkaline phosphphydrolase can also inactivate the active metabolites. |
| Azacitidine | Chemotherapy; Antimetabolite | |
| Cytarabine (Cytosine Arabinoside, AraC) | Chemotherapy; Antimetabolite | Pyrimidine antagonist. Must be given IV. Active metabolite is AraCTP, which inhibits DNA polymerase during the
S-Phase. Resistance: decreased uptake of AraC by tumor cells, decreased conversion of AraC to AraCTP, increased
breakdown of AraCTP. Indicated for acute leukemias (ALL) and lymphomas.
Adverse Effects: Ocular toxicity, neurotoxicity. |
| Floxuridine | Chemotherapy; Antimetabolite | Pyrimidine antagonist. |
| Fludarabine | Chemotherapy; Antimetabolite | Pyrimidine antagonist. |
| Gemcitabine | Chemotherapy; Antimetabolite | Pyrimidine antagonist, similar to Cytarabine. |
| Aminoglutethamide | Chemotherapy; Hormonal Agent | Aromatase Inhibitor decrease the conversion of androstenedione to estrone. Interrupts estrogen synthesis and is thus useful in metastatic breast cancer. |
| Diethylstilbestrol (DES) | Chemotherapy; Hormonal Agent | Can induce remission of prostatic carcinoma. |
| Estrogens | Chemotherapy; Hormonal Agent | Can induce remission of prostatic carcinoma. |
| Flutamide | Chemotherapy; Hormonal Agent | Anti-androgen used in the treatment of prostate cancer. |
| Leoprulide Acetate | Chemotherapy; Hormonal Agent | Synthetic analog of GnRH ------> blocks FSH and LH in pituitary ------> decreased androgen synthesis and an inhibitory effect on prostatic carcinoma. |
| Progestins | Chemotherapy; Hormonal Agent | Can induce remission of metastatic endometrial cancer. Has shown some success with breast cancer. |
| Tamoxifen | Chemotherapy; Hormonal Agent | Estrogen receptor antagonist is effective against susceptible breast cancers. The tumor must have an estrogen-receptor to be susceptible. |
| Corticosteroids
(Prednisone, etc.) |
Chemotherapy; Hormonal Agent
Anti-Inflammatory; Anti-RA Immunosuppressant |
Actions: (1) They inhibit Phospolipase-A2, (2) They inhibit the induction of COX-2
Chemotherapy: They suppress proliferation of lymphocytic cells, thus they are useful at combating lymphomas. Part of the MOPP group of drugs, to fight Hodgkin's Disease. RA: It is a potent anti-inflammatory, but it does nothing to prevent destruction of bone and cartilege. Immunosuppressant: Organ transplantation, auto-immune diseases, asthma. |
| Amsacrine (AMSA) | Chemotherapy; Miscellaneous | |
| Hydroxyurea | Chemotherapy; Miscellaneous | |
| L-Asparaginase | Chemotherapy; Miscellaneous | For Leukemia. Leukemic cells are deficient in asparagine synthetase and thus cannot replenish asparagine when it is broken down by this drug. That makes them selectively susceptible to the drug. Adverse Effects: Allergy, hepatitis, mental depression, pancreatitis. |
| Erythropoeiten | Hemopoeitic; Anemia | Useful for treating the hypoproliferative anemia caused by end-stage renal disease. Produced by recombinant DNA techniques. |
| Ferrous Fumarate | Hemopoeitic; Anemia
Iron-Deficiency Anemia |
Like Ferrous Sulfate |
| Ferrous Sulfate | Hemopoeitic; Anemia
Iron-Deficiency Anemia |
Take them on an empty stomach. Enteric-coated iron preparations are not used, because we want to absorb the iron in
the stomach and proximal duodenum. 200-400 mg of iron daily are required to treat iron deficiency.
Adverse Effects: Black stools, constipation, nausea, epigastric discomfort, abdominal cramps, diarrhea. |
| Ferrous Gluconate | Hemopoeitic; Anemia
Iron-Deficiency Anemia |
Like Ferrous Sulfate |
| Iron Dextran | Hemopoeitic; Anemia
Iron-Deficiency Anemia |
Parenteral iron administration, IM or IV. IM can be painful.
Indications: Parenteral iron is given for severe iron deficiency, after a bowel resection or after Inflammatory Bowel Disease involving the proximal jejunum. Adverse Effects: Headache, light-headedness. Nausea, vomiting, back pain, fever, arthralgia, urticaria, anaphylaxis (rare), flushing. |
| Folic Acid | Hemopoeitic; Anemia
Megaloblastic Anemia |
Folic acid will cure dietary folate deficiency. It will not cure folate deficiency due to anti-folate drugs (such as
Trimethoprim). For that you use folinic acid.
No adverse effects. |
| Hydroxycobalamin
(Vitamin B12) |
Hemopoeitic; Anemia
Megaloblastic Anemia |
IM. Highly bound to plasma proteins and remains in circulation longer than cyanocobalamin. Therapy continues for life. |
| Cyanocobalamin
(Vitamin B12) |
Hemopoeitic; Anemia
Megaloblastic Anemia Toxicity |
IM. The drug of choice in patients who are hypersensitive to the Hydroxycobalamin-Transcobalamin-II Complex.
Therapy continues for life.
Cyanide Toxicity: Co2 EDTA + Hydroxycobalamin takes up free cyanide, neutralizing it and forming cyanocobalamin (Vit B12). |
| Dextran | Hemopoeitic; Clotting
Anti-Coagulant |
Used to prevent post-operative thrombosis. Long chain sugars physically interfere with platelet function and fibrin polymerization. |
| Heparin | Hemopoeitic; Clotting
Anti-Coagulant |
IV or SQ anti-coagulant. It potentiates Antithrombin-III and is monitored using the PTT. It has a fast onset of action and short duration of action. |
| Warfarin
(Coumadin) |
Hemopoeitic; Clotting
Anti-Coagulant |
Oral anti-coagulant. It is an analog of Vitamin-K and inhibits Vit-K-dependent factors. It is monitored using the PT. It has a slow onset of action and longer duration of action. It is eliminated by P450 metabolism and has lots of drug interactions. |
| Dipyridamole | Hemopoeitic; Clotting
Platelet Inhibitor |
Inhibits phosphodiesterase ------> potentiate prostacyclin, which is a cAMP dependent factor.
In combination with warfarin, it is effective in preventing arterial embolization in patients with prosthetic heart valves. |
| Ticlopidine | Hemopoeitic; Clotting
Platelet Inhibitor |
Inhibits ADP-Induced platelet aggregation. Effective in preventing the recurrence of arterial thrombosis in patients
with a history of MI, Transient Ischemic Attacks (TIA's), stroke, unstable angina pectoris.
Adverse Effects: GI Disturbances in 20% of patients, Hemorrhage in 5% of patients, Leukopenia in 1% of patients. |
| Timolol | Hemopoeitic; Clotting
Platelet Inhibitor beta-Blocker |
Has been approved for the prophylaxis and prevention of first MI. It is not known whether the beneficial effects are due to inhibited platelets, beta-blocking activity, or combination of both. |
| Desmopressin Acetate | Hemopoeitic; Clotting
Prothrombogenic |
Useful as an adjunct in treatment of mild Hemophilia A. It potentiates the activity of Factor VIII. |
| Factor VIII | Hemopoeitic; Clotting
Prothrombogenic |
Given to treat primary Hemophilia A (Factor VIII Deficiency). Administration of the blood-derived factor carries a risk of getting viral infections such as Hepatitis-C. |
| Aminocaproic Acid | Hemopoeitic; Clotting
Prothrombogenic Toxicity |
They inhibit the conversion of plasminogen to plasmin. Used as adjunctive therapy in treating hemophilias.
Indicated for tPA, streptokinase toxicity. |
| Factor IX | Hemopoeitic; Clotting
Prothrombogenic Toxicity |
Given for treatment of warfarin overdose, whenever immediate coagulation needs to take effect.
Given to treat primary Hemophilia B (Factor IX Deficiency). Administration of the blood-derived factor carries a risk of getting viral infections such as Hepatitis-C. |
| Phytonadione
(Vitamin-K) |
Hemopoeitic; Clotting
Prothrombogenic Toxicity |
Given for treatment of warfarin overdose, or whenever the effects of warfarin need to be reversed, such as in preparation for surgery. The effect is delayed by about 24 hours, the time required to synthesize new clotting factors.
Given prophylactically before gallbladder surgery. |
| Tranexamic Acid | Hemopoeitic; Clotting
Prothrombogenic Toxicity |
Analog of aminocaproic acid. They inhibit the conversion of plasminogen to plasmin. Used as adjunctive therapy in
treating hemophilias.
Indicated for tPA, streptokinase toxicity. |
| Anistreplase | Hemopoeitic; Clotting
Thrombolytic Agent |
The acylated form of the Streptokinase-Plasminogen Activated Complex (APSAC); no risk of systemic fibrinolysis. Longer lasting than the others. Infused IV for 3-5 minutes. |
| Streptokinase | Hemopoeitic; Clotting
Thrombolytic Agent |
From Streptococcus. Can cause systemic fibrinolysis and DIC. May see allergies, in patients who have anti-streptococcal antibodies. Given as IV loading dose, then 24-48 hours of infusion. |
| Tissue Plasminogen Activator (tPA) | Hemopoeitic; Clotting
Thrombolytic Agent |
Active only at the site of the clot; no risk of systemic fibrinolysis. Given as IV loading dose, then 2 hours of infusion.
Particularly efficacious for post-MI treatment, and that is the only indication currently approved.
Adverse Effect: Higher risk for hemorrhagic stroke than with the other drugs. |
| Urokinase | Hemopoeitic; Clotting
Thrombolytic Agent |
Isolated from human kidney. Can cause systemic fibrinolysis and DIC. Given as IV loading dose, then 12 hours of infusion. |
| Adjuvants
Bacille Calmette-Guerin (BCG) |
Immunomodulating Agent | Attenuated M. Bovis strain can be employed as immunostimulant in cancer therapy. It activates macrophages, making them more apt at killing tumor cells. |
| Inosiplex | Immunomodulating Agent | Enhanced T-Cell and monocyte activities. Potentially useful in AIDS. |
| Thymosin | Immunomodulating Agent | 10 kDa protein. Thymic hormone that induces and stimulates the maturation of lymphoid stem-cells and pre-T-Cells into T-Cells. Indications: DiGeorge Syndrome, other conditions of T-Cell Deficiency. |
| Levamisole | Immunomodulating Agent
Anti-Inflammatory; Anti-RA |
It is an immunostimulatory drug that has paradoxical effect in treating RA. Treament has not yet been approved by FDA. Latency period of 3 - 4 months. May also be useful for Hodgkin's Disease. |
| Tacrolimus (FK-506) | Immunosuppressant
Anti-Bacterial; Macrolide |
Macrolide antibiotic of fungal origin, similar in use to Cyclosporin. Used in situations where Cyclosporin is ineffective, toxic, or cannot otherwise be used. |
| Anti-Lymphocyte Globulin | Immunosuppressant
Antibody |
It activates complement-mediated destruction of lymphocytes ------> decreased cellular immunity. There is little
effect on humoral immunity. Indications: Organ transplantations, GVHD.
Adverse Effects: Pain, erythema, possibly lymphoma at site of injection. Anaphylactic shock, serum sickness. |
| Anti-T-Cell Antibody OKT3 | Immunosuppressant
Antibody |
Mouse monoclonal antibody against the CD3 T-Cell Receptor.It inhibits the interaction between antigen-presenting
cells and T-Cells.
Indications: Kidney transplantation. |
| Anti-Thymocyte Globulin | Immunosuppressant
Antibody |
Indications: Idiopathic aplastic anemia, or to counter the auto-immune effects of gamma-Interferon, secondary to hemopoeitic suppression. |
| Rh0(D) Globulin
(Rhogam) |
Immunosuppressant
Antibody |
For the primary prevention of Erythroblastosis Fetalis (hemolytic anemia of newborn). It is given to Rh- mothers, 72 hours after first childbirth of an Rh+ fetus, to prevent formation of anti-Rh antibodies in the mother. |
| Methotrexate | Immunosuppressant
Chemotherapy; Antimetabolite Anti-RA |
Inhibits dihydrofolate reductase. Well absorbed orally, or intrathecal. Polyglutamic-acid conjugates of methotrexate
are retained intracellularly, where they have activity.
Indications: GVHD, Acute Lymphocytic Lymphoma, Choriocarcinoma, RA, psoriasis. Adverse Effects: Oral, gastric ulcerations, and liver cirrhosis with long-term use. High dose methotrexate may be followed by high-dose folinic acid in order to "rescue" the anti-folate effects of the drug. |
| Cyclosporin A | Immunosuppressant
Chemotherapy; Miscellaneous |
From the fungus, Tolypocladium Inflatum. Binds to cyclophillins ------> inhibit IL-2 production in T-Cells
------> inhibit T-Cell differentiation and activation. Extensive Cyt-P450 metabolism.
Indications: Suppress organ rejection after transplantation, IDDM. Adverse Effects: Viral infections, lymphoma. Nephrotoxicity, but it can be prevented with mannitol. |
| Azathioprine | Immunosuppressant
Chemotherapy; Miscellaneous Anti-RA |
Pro-drug, it is converted by glutathione S-transferase to 6-Mercaptopurine, active form of drug. It is toxic to proliferating T-Cells and B-Cells, after antigen exposure. Allopurinol, renal disease raise its blood levels.
Indications: kidney transplants, autoimmune diseases (glomerulonephritis, hemolytic anemia). Adverse Effects: Nausea, vomiting, diarrhea. Bone marrow suppression. Fever, skin rashes. Liver dysfunction and jaundice, ocassionally. Azothioprine or Methotrexate can be used to treat severe RA. |
| 2-PAM
(Pralidoxime) |
Toxicity | Organophosphate poisoning: Only effective within the first few minutes of exposure. It is a strong nucleophile that can bind with the organophosphate, releasing it from cholinesterase, before the bond has aged. |
| 4-methylpyrazole | Toxicity | A specific inhibitor of alcohol dehydrogenase that may be used instead of ethanol, for methanol and ethylene glycol poisoning. |
| Atropine | Toxicity | Treatment of choice after the bond has aged and become irreversible, in organophosphate poisoning. First-line treatment for carbamate poisoning. |
| Deferoxamine (Desferal) | Toxicity | IM or IV to chelate iron in blood, for iron toxicity. |
| Digoxin-specific antibody fragments. | Toxicity | Indicated for Digitalis toxicity. |
| Ethanol | Toxicity | It is given to displace the substrates and prevent their metabolism, in methanol and ethylene glycol poisoning. Prevent methanol from going to formic acid, and prevent ethylene glycol from going to oxalic acid. |
| Factor IX | Toxicity | Used for immediate coagulation, in the event of warfarin toxicity. |
| Fluazenil | Toxicity | Indicated for Benzodiazepine toxicity. |
| Methylene Blue | Toxicity | Indicated for treatment of methemoglobinemia, such as that due to nitrite poisoning. Methylene Blue speeds the conversion of methemoglobin back to hemoglobin. |
| N-Acetylcysteine | Toxicity | Indicated for Acetominophen toxicity. It provides reduced sulfhydryl groups and restores glutathione to its reduced form. |
| Nalorphine | Toxicity | Indicated for opioid overdose, alternative to naloxone. |
| Naloxone | Toxicity | Opioid antagonist, indicated for acute opioid toxicity. |
| Nitrite | Toxicity | It causes methemoglobinemia which can then bind up all of the extra cyanide, driving it away from the cytochrome oxidase. For cyanide poisoning. |
| Phytonadione (Vitamin-K) | Toxicity | Given to reverse the effects of warfarin toxicity, but it takes 24 hours to take effect. |
| Protamine Sulfate | Toxicity | Given IV for treatment of heparin overdose. It is a basic peptide that binds to heparin. Must dose it carefully, as protamine sulfate is itself an anti-coagulant! |
| Prussian Blue | Toxicity | Thallium poisoning: It interrupts the enterohepatic circulation of Thallium, enhancing its excretion. |
| Pyridoxine (Vit B6) | Toxicity | Can reverse convulsions and peripheral neuritis associated with Isoniazid toxicity. |
| Thiosulfate | Toxicity | Given to promote the formation of thiocyanate and its subsequent excretion, in cyanide poisoning. |
| Dimercaprol
(British Anti-Lewisite, BAL) |
Toxicity
Metal Chelator |
Administered in oil by deep IM injection. Fast-acting and short half-life. Enters tissues more readily than does EDTA.
Forms stable complexes with mercury, arsenic, gold. It can free the sulfahydral compounds bound by the metals, but it is better at primary prevention. Adverse Effects: It can cause transient hypertension. Used in combination with CaNa2 EDTA for lead poisoning, particularly when there are signs of Lead Encephalopathy. |
| Edetate Calcium Disodium
(CaNa2 EDTA) |
Toxicity
Metal Chelator |
Poor oral absorption. Usually administered IV or IM. Half-life 20 - 60 minutes. Urinary excretion. Water soluble;
does not easily enter tissues or get into cells.
Indications: Primarily used for lead poisoning. Not effective against mercury, arsenic, most other metals. |
| Succimer | Toxicity
Metal Chelator |
New drug that can be given PO. Both urinary and biliary excretion, with enterohepatic circulation.
Chemically similar to Dimercaprol. Indications: Severe Lead Poisoning: Used to treat children with lead poisoning above 45 µg / dL. It does not metabolize essential minerals like zinc, copper, iron, making it more attractive. Has been shown in labs to chelate arsenic, cadmium, mercury. |