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Pharmacology Test 3 Drug List

Categorized

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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.


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