non-selective NSAID

Low dose: analgesic, antipyretic

High dose: anti-inflammitory

Acetylation and inhibition of COX 1 and 2 is irreversible

Adverse effects

GI tract (due to COX-1 inhibition)

GI irritation -inhibition of cytoprotective PG's - PGE2, PGI2

Platelet inhibition

Hepatic and renal toxicity

Hypersensitivity - pruritis (itching)

Tinnitus - altered hearing at toxic doses

Reye's Syndrome: encephalopathy (brain disorder)

Analgesic and anti-pyretic effects

No anti-inflammitory activity

No GI tract irritation

Adverse effects

Hepatotoxicity at high doses

Metabolism by cytochrome P450 2E1

Non-selective NSAID

GI and renal adverse effects limit use

Non-selective NSAID

Possibly associated with greatest toxicity overall

used in the acute treatment of Gout

Non-selective NSAID

One of the least toxic

Non-selective NSAID

associated with increased liver function abnormalities

Non-selective NSAID

COX-2 specific NSAID

Safest for patients with high risk for GI bleeding

May have increased risk of CV toxicity

very expensive

Acute treatment of Gout

Not first line anymore

Produces anti-inflammitory effect by inhibiting leukocyte migration and phagocytosis (via inhibition of microtubule aggregation)

Xanthine oxidase inhibitor

Blocks conversion of xanthine to uric acid

standard agent for periods between acute attacks of Gout

Xanthine oxidase inhibitor

Blocks conversion of xanthine to uric acid

More selective than Allopurinol

Uricosuric drug

Promotes uric acid renal excretion - increases renal clearance by inhibiting tubular absorption

Decreases the body pool of urate

GI and kidney stone side effects may limit use

Uricosuric drug

Promotes uric acid renal excretion - increases renal clearance by inhibiting tubular absorption

Decreases the body pool of urate

GI and kidney stone side effects may limit use

DMARD

First line treatment of RA

Inhibits AICAR transformylase

DMAR

Polypeptide antibiotic

Inhibits interleukin-1 and interleukin-2 receptor production- interferes with cytokine signaling

DMARD

Cytostatic cross-link DNA to prevent cell replication

DMARD

Interferes with nucleic acid metabolism and synthesis and inhibits cell proliferation

Suppresses B cell and T call function, immunoglobulin production and interleukin-2 secretion

DMARD

Inhibits ribonucleotide synthesis and causes cell cycle arrest

First agent for RA indicated for both symptomatic improvement and retardation of strucutral joint damage

DMARD

Anti-malarial agent

anti-inflammatory action in RA is unclear

DMARD

Anti-malarial agent

anti-inflammatory action in RA is unclear

DMARD

Gold compound

Alters the morphology and functional capabilities of human macrophages

Not used much anymore

DMARD

Gold compound

Alters the morphology and functional capabilities of human macrophages

Not used much anymore

DMARD

IgA and IgM rheumatoid factor production is decreased

Biologic DMARD

Anti-TNF agent

Biologic DMARD

anti-TNF agent

Biologic DMARD

anti-TNF agent

Biologic DMARD

B-cell depleting agent

Biologic DMARD

T-cell costimulation inhibitor

Biologic DMARD

IL-1 inhibitor

Acute migraine drug

Vasoconstriction due to stimulation of alpha-adrenergic and 5-HT receptors

Acute migraine drug

Vasocontriction due to stimulation of alpha-adrenergic and 5-HT receptors

ergotamine + caffeine - facilitates absorption of ergotamine

Acute migraine drug

Selective 5-HT1D and 5-HT1B receptor agonists

Acute migraine drug

Selective 5-HT1D and 5-HT1B receptor agonists

Narrow spectrum penicillin

DOC for streptococci, meningococci, enterococci, penicillin-susceptible pneumococci and non-beta-lactamase producing staphylococci

IV

Narrow spectrum penicillin

indicated only in minor infections (poor bioavalibility, 4X day dosing and narrow spectrum of activity)

PO

Antistaphylococcal penicillin

treats serious beta-lactamase producing staph infections (acute endocarditis and osteomyelitis)

Staph that are resistant to these penicillins are MRSA

Extended spectrum penicillin

greater activity against gram - bacteria

treats UTIs, sinusitis, otitis and lower resp. tract infections

often combined with beta-lactamase inhibitors

Extended spectrum penicillin

greater activity against gram - bacteria

treats UTIs, sinusitis, otitis and lower resp. tract infections

often combined with beta-lactamase inhibitors

often combined with gentamicin for the treatment of serious infections (enterococcal endocarditis)

Antipseudomonal penicillin

active against gram negative rods and gram +

susceptible to beta-lactamases

Antipseudomonal penicillin

active against gram negative rods and gram +

susceptible to beta lactamases

more effective against P. auroginosa then ticarcillin

First generation cephalosporin

does not cross BBB

First generation cephalosporin

Does not cross BBB

DOC for surgical prophylaxis and an alternative to penicillin in pts with allergies

Second generation cephalosporin

treatment for CA pneumonia

only 2nd generation that crosses BBB

Third generation cephalosporin

less susceptible to beta-lactamases and can cross the BBB

use can lead to psuedomembranous colitis (C.dif)

used in combo with aminoglycoside to treat meningitis from P. aeruginosa

active against N. gonorrhea

Third generation cephalosporin

less susceptible to beta-lactamases and can cross the BBB

use can lead to psuedomembranous colitis (C.dif)

used in combo with aminoglycoside to treat meningitis from P. aeruginosa

Fourth genration cephalosporin

more resistant to hydrolysis via beta-lactamases

Highly active against H. influenzae and N. Gonorrhea

Has the gram + coverage of a 1st generation and the gram - coverage of a 3rd generation

Beta-Lactamase inhibitor

very weak antibacterial activity

only available in fixed combos with specific penicillins

Beta-Lactamase inhibitor

very weak antibacterial activity

only available in fixed combos with specific penicillins

Beta-Lactamase inhibitor

very weak antibacterial activity

only available in fixed combos with specific penicillins

Monobactam

effective against gram negative bacilli

Penicillin allergic patients tolerate it without rxn

Side effect: bone marow suppression-induced leukopenia

Carbapenem

wide spectrum with good activity against gram +, gram - rods and anaerobes

activated by dehydropeptidases in the renal tubules

Bacterial cell wall synthesis inhibitor

active against gram + cocci and bacilli

inhibits cell wall synthesis by interfering with elongation of the peptidoglycan backbone and cross-linking

Bacterial cell wall synthesis inhibitor

inhibits early stage of cell wall formation

MOR - due to decreased transport of drug into bacteria

gram + and gram - organisms

Mainly used for UTIs

Bacterial cell wall synthesis inhibitor

blocks regeneration of bactoprenol, a lipid carrier molecule that transfers PG subunits to the growing cell wall

active aginst gram + cocci

limited to topical use - too nephrotoxic for systemic use

Bacterial cell wall synthesis inhibitor

inhibits the incorporation of D-alanine into peptidoglycan pentapeptide

primarily used to treat multidrug resistant TB

mycobacteria and gram -

side effects - psychosis, sedation, confusion, vertigo

Aminoglycoside

binds to the 30S subunit - blocks protein synthesis

Enzymatic modification is the most common MOR

Renal, vestibular and neuromuscular toxicities

Aminoglycoside

binds to the 30S subunit - blocks protein synthesis

Enzymatic modification is the most common MOR

Renal, vestibular and neuromuscular toxicities

Aminoglycoside

binds to the 30S subunit - blocks protein synthesis

Enzymatic modification is the most common MOR

Renal, vestibular and neuromuscular toxicities

Aminoglycoside

binds to the 30S subunit - blocks protein synthesis

Enzymatic modification is the most common MOR

Renal, vestibular and neuromuscular toxicities

Aminoglycoside

binds to the 30S subunit - blocks protein synthesis

Enzymatic modification is the most common MOR

Renal, vestibular and neuromuscular toxicities

Tetracycline

blocks 30S subunit by binding tRNA to the A site

Broad spectrum and bacteriostatic

MOR - bacteria gain efflux pumps by conjugation

DOC for Rocky Mountain Spotted Fever and other Rickettsia infections

DOC for borrelia induced lyme disease and relapsing fever

May cause discoloration of the teeth and hypoplasia of the enamel in children under 8

Can cause phototoxicity

Tetracycline

blocks 30S subunit by binding tRNA to the A site

Broad spectrum and bacteriostatic

MOR - bacteria gain efflux pumps by conjugation

DOC for Rocky Mountain Spotted Fever and other Rickettsia infections

DOC for borrelia induced lyme disease and relapsing fever

May cause discoloration of the teeth and hypoplasia of the enamel in children under 8

Can cause phototoxicity

Tetracycline

blocks 30S subunit by binding tRNA to the A site

Broad spectrum and bacteriostatic

MOR - bacteria gain efflux pumps by conjugation

DOC for Rocky Mountain Spotted Fever and other Rickettsia infections

DOC for borrelia induced lyme disease and relapsing fever

May cause discoloration of the teeth and hypoplasia of the enamel in children under 8

Can cause phototoxicity

Macrolide

block 50S subunit by blocking peptidyl transferase

MOR - efflux of drug out of bacteria and mutations in 50S subunit that decrease drug binding

Potent inhibitor of P450s - drug interaction alert

Macrolide

Affects the 50S ribosomal subunit

Blocks peptidyl transferase (translocation step)

Macrolide

Affects the 50S ribosomal subunit

Blocks peptidyl transferase (translocation step)

Macrolide

Affects the 50S ribosomal subunit

Blocks peptidyl transferase (translocation step)

blocks peptidyl transferase

broad spectrum antibiotic

readily crosses the BBB - good for treating meningitis

can induce fatal bone marrow suppression - this restricts its use to a few life-threatening infections

MOR - mutations in ribosome binding site, mutations in porins decrease influx, plasmids encode for enzymes that degrade antibiotic

Can cause Idiosyncratic aplestic anemia and Gray baby syndrome at high levels

Streptogramin

Inhibits protein synthesis

used for vancomycin resistant enterococcus

very expensive

Streptogramin

Inhibits protein synthesis

used for vancomycin resistant enterococcus

very expensive

Oxazolidinone

binds to the P site of the 50S subunit

Gram + organisms

Sulfonamide

inhibit folate synthesis

used for burn infections

broad spectrum

do not administer to pregnant women or newborns

used as an antiparasitic drug

Sulfonamide

blocks the synthesis of dihydrofolate

used for occular infections and trachoma

broad spectrum

do not administer to pregnant women or newborns

Inhibits Dihydrofolate reductase (DHFR)

MOR - plasmid encodes resistant DHFR, mutation in DHFR, overexpression of DHFR

used for bacterial prostatitis and vaginitis

often used in combo with sulfamethoxazole

first generation Quinolone

DNA gyrase inhibitor

bacteriostatic (but if bacteria cannot repair the damage can be bacteriacidal)

MOR - DNA gyrase mutation, porin mutation, increased efflux - note: no plasmid mediated resistance

limited gram - activity : UTIs only

do not prescribe to children and pregnant women

second generation Quinolone

DNA gyrase inhibitor

bacteriostatic (but if bacteria cannot repair the damage can be bacteriacidal)

MOR - DNA gyrase mutation, porin mutation, increased efflux - note: no plasmid mediated resistance

do not prescribe to children and pregnant women

third generation Quinolone

DNA gyrase inhibitor

bacteriostatic (but if bacteria cannot repair the damage can be bacteriacidal)

MOR - DNA gyrase mutation, porin mutation, increased efflux - note: no plasmid mediated resistance

do not prescribe to children and pregnant women

Behaves as a free radical to disrupt replication, transcription and DNA repair

Indicated for C. diff, H. pylori and D. medinensis

Used prophylactically for surgical procedures

antiparasitic

activated under anaerobic conditions by PFOR

disulfiram like effect - avoid alcohol consumption

Trichomoniasis - sexual partners should be treated simultaneously

Giardiasis - 90% success rate

Amebiasis - DOC for treating symptomatic DZ

Cyclic lipopeptide

disrupts membrane function in gram + organisms

blocks the formation of isoleucine-tRNAs

most staph and strep strains incuding MRSA

inhibits DNA dependent RNA polymerase

MOR - mutations in RNA polymerase

indicated for meningococcal carriers

used for prophylaxis and treatment of UTIs

can cause GI problems

disrupts cell membrane integrity

often used in creams or ointments

too nephrotoxic to give parenterally

Antiparasitic

effective at eliminationg E. histolytica from intestines

mild or asymptomatic cases of amebiasis

aminoglycoside antibiotic - inhibits protein synthesis

effective at eliminating E. histolytica from intestine

used to treat asymptomatic or mild cases of amebiasis

Interference with PFOR

treatment of Cryptosporidiosis and Giardiasis in individuals over 1 year of age

Antiparasitic drug

Inhibits DHFR

Antimalarial

half life in the body of 4 days

eliminates asexual erythrocytic stages of all species of plasmodium

BIG TIME resistance

Antimalarial drug

poorest therapeutic:toxic ratio of all antimalarial drugs - cinchonism and hypoglycemia

eliminates asexual erythrocytic stages of all species of plasmodium

Antimalarial drug

some reports demonstrate severe neuropsychiatric rxns in .5% of patients

Effective against all species of plasmodium

Antimalarial drug

only drug that has activity against the liver (hypozoite) forms of P. vivax and P. ovale

patients should be screened for G6PD - RBC lysis

Malarone

Antimalarial drug

treatment of P. falciparum malaria

Antimalarial drug - tetracycline

inhibits growth of plasmodium by disrupting protein synthesis

major side effects - photosensitivity dermatitis and staining of teeth in children - contraindicated in children and pregnant women

Antihelminthic - Benzimidazole

ascariasis, pinworm, hookworm and whipworm infections

Antihelminthic - Benzimidazole

ascariasis, pinworm, hookworm and whipworm infections

Antihelminthic - Benzimidazoles

second line drug used in the treatment of strongyloidiasis

used topically to treat cutaneous larval migrans

Antihelminthic

causes hyperpolarization in muscle cells - paralysis

no affect on mammalian cells

DOC for treating strongyloidiasis

Antihelminthic

activates cholinergic nicotinic receptors in nematodes - depolarizing neuromuscular blockade

no effect on humans

DOC for treating pinworms

TREATMENT OF THE ENTIRE HOUSEHOLD IS RECOMMENDED

Tapeworm and Fluke infection

Increase calcium permeability of the worm's tegument

Flukes : 3 doses in a single day

Tapeworms : a single dose

Cysticercosis : two weeks treatment

Polyene antifungal

Affinity for ergosterol sites - disrupt internal environment

Main toxicity is renal

Resistance is rare and slow to develop

Antifungal

Block the production of ergosteol by inhibiting a demethylation step

Significant inhibition of human CYP450 - drug interactions

Liver toxicity

Antifungal

Block the production of ergosteol by inhibiting a demethylation step

Significant inhibition of human CYP450 - drug interactions

Liver toxicity

Antifungal

Block the production of ergosteol by inhibiting a demethylation step

Significant inhibition of human CYP450 - drug interactions

Liver toxicity

Antifungal

Inhibition of cell wall synthesis - block production of chitin

indicated for inavasive aspergillosis when other therapy fails

Antifungal

Inhibition of cell wall synthesis - block production of chitin

indicated for inavasive aspergillosis when other therapy fails

Antifungal

Inhibition of nucleic acid synthesis (ultimately thymidylate synthase)

Antifungal

Squalene epoxidase inhibitor

superficial infections

Antifungal

binds to tubulin to inhibit mitosis

deposited in nails

for superficial infections, but not used as much as Terbinafine

Antimycobacterial

DOC for the chemotherapy of TB

Inhibits biosynthesis of mycolic acid

Bacteriostatic for resting bacilli

Bacteriocidal for dividing bacilli

specifically activated by catalase-peroxidase

Extensively metabolized by hepatic acetyltransferase

drug induced hepatitis - rapid acetylators

peripheral neuritis, SLE like symptoms - slow acetylators

Antimycobacterial

inhibits RNA polymerase of bacilli

hepatic activation

broad spectrum

used prophylactically in pts with isoniazid resistance

most used with isoniazid for treatment of TB

Hypersensitivity rxn in 50% of pts

potential hepatitis

discoloration of body fluids

Antimycobacterial

used to treat M. avium intracellulare infections

HIV+ pts

Antimycobacterial

M. tuberculosis or M. avium

used in resistant and HIV+ patients

May alter vision (color discrimination)

Antimycobacterial

good for active TB infection

inhibits fatty acid synthetase I

must be used in combo therapy with other drugs

antimycobacterial

first drug used to treat TB

not used much, only when resistant to other drugs

Antimycobacterial

sulfone

bacteriostatic inhibition of folic acid synthesis in M. leprae

antimycobacterial

bacteriostatic activity against M. leprae and MAC

anti-inflammatory and immunologic activity

erythema nodosum leprosum (skin lesions)

highly lipophilic - long half life

skin and body fluid discoloration

Antimycobacterial

alleviates the presentation of erythema nodosum leprosum

Teratogenic - babies born with missing limbs (phocomelia)

Antiviral

Parkinson's - blocks nicotinic cholinergic receptor

viral infections - binds M2 membrane protein

Not active against influenza B

accelerates recover from fever if administered within 48 hours of exposure

prophylacically to protect children and elderly from flu

antiviral

inhibits neuraminidase of influenza A and B virus

reduce the length of illness

antiviral

inhibits neuraminidase of influenza A and B virus

reduce the length of illness

antiviral

prodrug - activated by herpesvirus thymidine kinase (binds to TK very specifically)

inhibits DNA replication

used for HSV-1 and VZV (chicken pox)

antiviral

prodrug - activated by viral phosphorylation

potent vs. HSV and CMV

low margin of safety - granulocytopenia and thrombocytopenia

teratogenic and embryotoxic

antiviral

CMV, HSV-1 and 2 and VZV

IV administration only

CMV retinitis pts with AIDS and acyclovir resistant HSV infections in immunocompromised pts

antiviral

nucleoside analog of thymidine and adenosine

inhibit viral DNA synthesis

limited to topical treatment of HSV and HPV

Ribavirin

antiviral

nasal aerosol for RSV

prodrug that must be phosphorylated

disrupts purine metabolism - viral DNA synthesis inhibited

contraindicated in pregnancy and lactation

antiviral

used for viral hepatitis

flu-like symtoms post-administration

anti-HIV

NRTI

anti-HIV

NRTI

anti-HIV

NRTI

anti-HIV

NRTI

anti-HIV

NRTI

anti-HIV

NRTI

1st drug of its kind

anti-HIV

NNRTI

anti-HIV

NNRTI

anti-HIV

Protease inhibitor

N/V/D

anti-HIV

Protease inhibitor

N/V/D

anti-HIV

Protease inhibitor

N/V/D

anti-HIV

Protease inhibitor

1st of its class - trials shortened due to efficacy

N/V/D

anti-HIV

fusion (entry) inhibitor

targets gp41 protein on HIV surface

use in HIV+ pts who have developed resistance

Immunosuppresant

Calcineurin inhibitor - blocks T cell activation

prevention and treatment of acute organ rejection

avoid tropical fruits and grapefruit

nephrotoxicity and renal failure possible

Immunosupressant

calcineurin inhibition

prophylaxis of acute rejection

avoid grapefruit

nephrotoxicity, hyperkalemia, hypomagnesemia, hyperglycemia (inhibits insulin release)

Immunosupressant

Antimetabolite

inactivated by hepatic xanthine oxidase

Leukopenia and thrombocytopenia

May be contraindicated in pregnancy and breast feeding (risk D)

Hepatotoxicity

Immunosupressant

Antimetabolite

inhibits T cell and B cell proliferation

prophylactic at time of transplant

used in combo with steroids and calcineurin inhibitors

use with caution in pregnancy and lactation (risk C)

Immunosuppresant

Antilymphocyte - reduces number and alters function of T-lymphocytes

Major ADR: Hx of sensitivity to horse serum

Immunosuppresant

Antilymphocyte

horrible drug - produces anaphylactic rxns

Immunosuppresant

antilymphocyte

prophylaxis of acute renal rejection

have epi pen ready: hypersensitivity rxns

Immunosuppresant

antilymphocyte

hydrocortisone pretreatment recommended - hypersensitivity rxns