Week 1 Drugs Flashcards
Etanercept
Anti-inflammatory
Cytokine inhibitor
TNFa_ R analog
Infliximab
Anti-inflammatory
cytokine inhibitor
Monoclonal TNFa- Ab
Aspirin
Anti-inflammatory
Prostaglandin synthesis Inhibitor
—/ COX 1 and 2
NSAID
Non-Steroidal Anti-inflammatory Drugs
Prostaglandin Inhibitor—/ COX 1 and 2
Zileuton
Anti-inflammatory
Leukotriene SYNTHESIS Inhibitor—/ lipoxygenase
Zafirlukast
Anti-inflammatory
Leukotrienes RECEPTOR Inhibitor
Steroid
Anti-inflammatory
inhibits cytokines, PG, Leukotrienes, CAMs
—/ COX and Pospholipase A2
- IFkB
Dinoprostone
PGE2 Analog 1. cervical ripening EP4 R--> collagenase and relax cervical sm 2. terminate pregnancy EP1/3 R--> uterine cntxn (-) GI sxs uterine rupture fever
Carboprost
PGF2a Analog 1. termination of 2nd trimester preg FP-R--> uterine cntxn 2. control postpartum hemorrhage FP-R--> uterine cntxn (-) GI sxs fever uterine rupture
Misoprostol
PGE1 Analog
1. prevention of ulcers from long-term NSAID use
EP3–/ gastric acid secretion
reduce cAMP–> ^ bicarb and mucin, ^ mucosal blood flow
(-) diarrhea
(o) pregnancy
Alprostadil
PGE2 Analog
1. impotence/erectile dysf
^ cAMP–/ sm cntxn of corpus cav
- maintain patent ductus arteriosus
^ cAMP–/ sm cntxn
Epoprostenol
PGI2 Analog (IV) 1. primary pulmonary HTN ^ cAMP--/ sm cntxn= dilation of pulmonary artery sm
Bimatoprost
PGF2a Analog
1. glaucoma
^ outflow of aq humor
- eyelash hypotrichosis
^ % and duration of lash in growth phase
Aldosterone
Mineralcorticoid (MC)- Steroid
Cortisol
Glucocorticoid (GC)- Steroid
Dexamethasone
Glucocorticoid (GC)- Steroid
Prednisolone
Glucocorticoid (GC)- Steroid
Immunosuppressant
Fludrocortisone
Glucocorticoid (GC)- Steroid
Metyrapone
Steroid Synthesis Inhibitor
inhibits 11-B-hydroxylase –/ cortisol synthesis
(X) ^^ACHT from AP diagnostic
Mifepristone
Competitive Antagonist of GC and Progesterone R
(X) termination of pregnancy
(X) treat Cushing’s Disease
Spironolactone
Competitive antagonist of MC-R (X) diuretic - HTN -cardiac hypertrophy and heart failure *same as eplerenone
Eplerenone
Competitive antagonist of MC-R (X) diuretic - HTN -cardiac hypertrophy and heart failure *same as spironolactone
Drospirenone
1. MC-R Antagonist (X) diuretic--/ salt retain of estrogen 2. Progesterone-R Agonist (X) suppress ovulation, hormone replacement for post-menopausal 3. Androgen-R Antagonist
Azathioprine
Immunosuppressant
metabolized to 6-mercaptopurine –/ purine synthesis (de novo and salvage)
(X) prevent rejection, autoimmune diseases
(-) bone marrow suppression
GI and hepatotoxicity
Cyclophosphamide
Immunosuppressant
alkylating cross-links dsDNA–> kill replicating and NON cells (*B cells–/ humoral immunity)
(X) autoimmune disease
(-) bone marrow suppression
Methotrexate
Immunosuppressant
Inhibit Dihydrofolate reductase–/ folate dep steps of purine synthesis
(X) autoimmune diseases, pregnancy termination
(-) hepatic toxicity
Mycophenolate Mofetil
Immunosuppressant metabolized> mycophenolic acid--/ IMP-DH (IMP>GMP) inhibit de novo purine synthesis salvage pathway in tact *selectively toxic to Lymphocytes* (X) prevent renal allograft rejection -autoimmune diseases (-) infection, leukopenia, anemia (O) contraindicated in pregnancy
Cyclosporine
Immunosuppressant Lipophilic peptide Abx 1. bind cyclophilin--/ Calcineurin 2. block activation of NFAT (TF) 3. inhibit IL-2 production --/ Th cell function and Tcell prolif and cytotoxicity (X) prevent rejection (-) nephrotoxicity, hepatotoxicity
Tacrolimus
Immunosuppressant similar mechanism to cyclosporine 1. bind FKBP--> bind calcineurin 2. inhibit activation of NFAT (TF) 3. prevent synth of IL-2 (X) prevent rejection (+) more potent, less toxic
Sirolimus
Immunosuppressant
inhibit T cell activation and prolifieration downstream of IL-2
1. bind FKBP-12–> mTOR
2. inhibit G1>S phase transition
(X) prevent rejection, coat cardiac stents
Ibuprofen
NSAID---/ COX 1 and 2 t 1/2= 2 hrs (naproxen) (X) rheumatoid arthritis/osteoarthritis mild-mod pain fever dysmenorrhea
Indomethacin
NSAID ---/ COX 1 and 2 (X) gouty arthritis mod-severe osteoarth/rheumatorid ankylosing spondylitis close ductus arteriosis (IV)
Nabumetone
NSAID—/ COX 2» 1
converted to active* 6methoxy-2naphthylacetic acid
-anti inflam and analgesic
(X) osteoarthritis, rheum arth
Naproxen
NSAID---/ COX 1 and 2 t 1/2= 14 hrs (ibuprofen) (X) ankylosing spondylitis osteoarthitis/rheumatoidarthritis acute gout mild-mod pain tendonitis, bursitis dysmenorrhea fever
Sulfasalazine
NSAID—/ production of IL1 and TNFa, lipoxygenase, NFkB, scavenge free radicals
(X) ulcerative colitis
rheumatoid arthritis
ankylosing spondylitis
Piroxicam
NSAID—/ COX 1 and 2
(X) acute/chronic osteo/rheumatoid arthritis
(+) long half life t1/2=50hrs (99% plasma bound)
Diphenydramine
H1 blocker- 1st gen (Benadryl) (-) profound sedation (X) Allergies Motion Sickness Sleep aid end-stage Parkinson's
Dimenhydrinate
H1 blocker- 1st gen
(Dramamine)
(X) motion sickness
Chloropheniramine
H1 blocker- 1st gen
*most potent
less prone to drowsiness
(X) allergies
Promethazine
H1 blocker- 1st gen
X) motion sickness (anti chol
Fexofenadine
H1 blocker- 2nd gen
terfenadine> fexofenadine
(Allegra)
Loratidine
H1 blocker- 2nd gen
> desloratidine
(Claritin)
(X) allergies
Desloratidine
H1 blocker- 2nd gen
>from loratidine
(Clarinex)
(X) allergies
Citirizine
H1 blocker- 2nd gen
(-) most sedation for 2nd gen
(Zyrtec)
(X) allergies
Cimetidine
H2 blocker–/ parietal cell acid secretion
(X)GERD
gastric, duodenal ulcers
prevent stress ulcers
zollinger-ellison syndrome (non B cell tumor of pancreas)
(-)–/ CYP450 and –/ Testosterone binding= gynecomastia, reduced sperm count, impotence
Famotidine
H2 blocker–/ parietal cell acid secretion
(X)GERD
gastric, duodenal ulcers
prevent stress ulcers
Ranitidine
H2 blocker –/ parietal cell acid secretion
(X)GERD
gastric, duodenal ulcers
prevent stress ulcers
Cromolyn Sodium
Anti-histamine—/ Release
stabilize mast cell membrane
(X) asthma, rhinitis, conjunctivitis
Omalizumab
Anti-histamine —/ Release
monoclonal Ab–/ IgE sensitization of mast cells
(X) allergic asthma
Acetaminophen
NSAID (Tylenol) ---/ COX peroxidase (NO affinity for COX 1 or 2 active site) NO anti-inflammatory (X) mild-mod pain and fever (-) overdose- CYP 2E1 path> toxic
Acetylsalicylic Acid
(Aspirin) NSAID *IRREVERSIBLE*acetylation of serine --/COX 1 and 2 (X) anti-platelet anti-inflammatory analgesia anti-pyretic (-) overdose risk -zero order kinetics (O) pregnancy and children
Celecoxib
NSAID selective inhib---/ COX 2 (X) rheumatoid arthritis/osteoarthritis dysmenorrhea reduce intestinal polyps (O) sulfa toxicity , GI disease, deficiency of CYP2C9
Ketorolac
NSAID —/ COX 1 and 2
analgesia and anti-pyretic
(X) mod/severe pain opioid level (IV)
