Vismodegib (mechanism and use)
Molecular inhibitor in the PTCH Hedghog pathway
Used to treat basal cell carcinoma
Imiquimod (mechanism and 2 uses)
TLR7 agonist (induces inflammation) Used to treat verrucae vulgaris, condyloma acuminatum
Belimumab (mechanism and use)
Inhibits Blys -> decreases B cell survival and differentiation
Used in SLE joint & muscle problems
Teriparatide (mechanism)
Recombinant PTH (increases osteoblast activity)
Teriparatide (use)
Severe osteoporosis
Teriparatide (side effects)
Paget disease of the bone
Elevated alk phos
Orthostatic hypotension
Nausea, hypercalcemia
Aspirin (mechanism)
NSAID
Irriversibly inhibits COX-1 & 2 (covalent acetylation)
No effects on PT, PTT, but increases bleeding time
Aspirin (3 uses)
Low dose: inhibits platelet aggregation
Intermediate dose: antipyretic and analgesic
High dose: anti-inflammatory
Aspirin (5 side effects)
Gastric ulceration
Tinnitus
Acute renal failure, interstitial nephritis
Reye syndrome in children
Stimulates resp center (get hyperventilation and resp alkalosis)
Bronchoconstriction (from stimulating lipooxygenase pathway and increasing LTC4, LTD4, LTE4) -> “aspirin-sensitive asthma”
Ibuprofen (mechanism)
NSAID: same as naproxen, indomethacin, ketorolac, diclofenac
Reversibly inhibit COX-1 & 2
Ibuprofen (3 uses)
NSAID: same as naproxen, indomethacin, ketorolac, diclofenac
Antipyretic, analgesic, anti-inflammatory
Ibuprofen (2 side effects)
NSAID: same as naproxen, indomethacin, ketorolac, diclofenac
GU
Interstitial nephritis, renal ischemia (PGs normally vasodilate afferent arteriole)
Naproxen (mechanism)
NSAID: same as ibuprofen, indomethacin, ketorolac, diclofenac
Reversibly inhibit COX-1 & 2
Naproxen (3 uses)
NSAID: same as ibuprofen, indomethacin, ketorolac, diclofenac
Antipyretic, analgesic, anti-inflammatory (acute gout)
Naproxen (2 side effects)
NSAID: same as ibuprofen, indomethacin, ketorolac, diclofenac
GU
Interstitial nephritis, renal ischemia (PGs normally vasodilate afferent arteriole)
Indomethacin (mechanism)
NSAID: same as ibuprofen, naproxen, ketorolac, diclofenac
Reversibly inhibit COX-1 & 2
Indomethacin (4 uses)
NSAID: same as ibuprofen, naproxen, ketorolac, diclofenac
Close PDA (different from other NSAIDs)
Antipyretic, analgesic, anti-inflammatory (acute gout)
Indomethacin (2 side effects)
NSAID: same as ibuprofen, naproxen, ketorolac, diclofenac
GU
Interstitial nephritis, renal ischemia (PGs normally vasodilate afferent arteriole)
Ketorolac (mechanism)
NSAID: same as ibuprofen, naproxen, indomethacin, diclofenac
Reversibly inhibit COX-1 & 2
Ketorolac (3 uses)
NSAID: same as ibuprofen, naproxen, indomethacin, diclofenac
Antipyretic, analgesic, anti-inflammatory
Ketorolac (2 side effects)
NSAID: same as ibuprofen, naproxen, indomethacin, diclofenac
GU
Interstitial nephritis, renal ischemia (PGs normally vasodilate afferent arteriole)
Diclofenac (mechanism)
NSAID: same as ibuprofen, naproxen, indomethacin, ketorolac
Reversibly inhibit COX-1 & 2
Diclofenac (3 uses)
NSAID: same as ibuprofen, naproxen, indomethacin, ketorolac
Antipyretic, analgesic, anti-inflammatory
Diclofenac (2 side effects)
NSAID: same as ibuprofen, naproxen, indomethacin, ketorolac
GU
Interstitial nephritis, renal ischemia (PGs normally vasodilate afferent arteriole)
Celecoxib (mechanism)
Reversibly inhibits COX-2 (so no effects on gastric mucosa or platelet fx)
Celecoxib (4 uses)
RA
Osteoarthritis
Gastritis
Ulcers
Celecoxib (2 side effects)
Risk of thrombosis (CI in cardiovascular disease)
Sulfa allergy
Acetaminophen (mechanism)
Tylenol is an example
Reversibly inhibits COX, mostly in CNS (inactivated peripherally)
Acetaminophen (2 uses)
Antipyretic, analgesic
NOT anti-inflammatory
Use this if problems with stomach irritation (no COX-1i) or sulfa allergy/CAD (no COX-2i)
Acetaminophen (side effect and antidote)
Hepatic necrosis in overdose (NAPQI metabolite depletes glutathione and forms toxin in liver) -> fixed w/ N-acetylcysteine (acts as glutathione substitue and provides sulfhydryl groups to enhance sulfation elimination)
Allopurinol (mechanism)
Noncompetitively inhibits xanthine oxidase (so less production of uric acid)
Allopurinol (2 uses)
Gout (chronic drug)
Prevents tumor lysis-associated urate nephropathy in lymphoma, leukemia
Allopurinol (side effects)
Increases conc of azathioprine and 6-MP
Don’t give salicylates
Can precipitate gout attack
Febuxostat (mechanism an use)
Inhibits xanthine oxidase (so less production of uric acid) For gout (chronic drug)
Probenecid and sulfinpyrazone (mechanism)
Inhibits reabsorption of uric acid in PCT (so increases excretion of uric acid)
Probenecid and sulfinpyrazone (2 uses)
Gout (chronic drug)
Probenezid: to prolong action of penicillin by decreasing its renal clearance (inhibits tubular organic acid secretion system)
Probenecid and sulfinpyrazone (side effects)
Inhibits penicillin secretion
Don’t use in pts w/ kidney stones or those excreting excessive amounts of uric acid in urine
Colchicine (mechanism)
Binds and stabilizes tubulin -> inhibits microtubule polymerization -> impairs leukocyte (neutrophil) chemotaxis and degranulation
Colchicine (use)
Acute gout attack
Colchicine (side effect)
GI (massive diarrhea, maybe n/v & abd pain)
Etanercept (mechanism)
Fusion protein (TNF-a receptor + IgG1 Fc) produced by recombinant DNA -> so a TNF DECOY receptor
Etanercept (3 uses)
RA
Psoriasis
Ankylosing spondylitis
Etanercept (side effect)
TB reactivation (or predisposition to infection in general)
Certolizumab pegol (mechanism and use)
Targets TNF-a, lacks Fc region so doesn’t activate complement and cell-mediated toxicity
Used for autoimmune diseases assc. w/ elevated TNF-a
Vemurafenib (mechanism and use)
BRAF kinase inhibitor
For melanoma in pts w/ BRAF V600E
Hydroxychloroquine (3 uses)
Seroneg RA
SLE
Malaria
Hydroxychloroquine (side effect)
Permanent retinal damage
Rasburicase (mechanism and use)
RasbURICase
Recombinant urate oxidase -> converts uric acid to allantoin which is much more soluble
For prevention and tx of renal manifestations of tumor lysis syndrome
Calcipotriene (calcipotriol), calcitriol, and tacalcitol (mechanism and use)
Vit D analogs -> activate vit D nuclear TF -> inhibits keratinocyte proliferation and stimulates its differentiation
Topical for psoriasis