STEP1 Pharm Flashcards
Glucocorticoids inhibit
Phospholipase A2
Cortisone, hydrocortisone,
“-sone, -olone”
Glucocorticoids increase ____ which ____
IkB inhibits NF-kB (prevents increase COX-2)
Inhibit COX-2 only
celecoxib
Glucocorticoids increase IkB which inhibits NF-kB which increases COX-2
Inhibit COX1/2
Aspirin (irreversible)
NSAIDS
- Ibuprofen, naproxen, indomethacin
Inhibit 5-Lipoxygense
Zileuton
Inhibit Leukotriene receptor
Montelukast
Zafirlukast
Arachidonic pathway
Membrane phospholipids –> Arachidonic acid [Phosphlipase A2]
Arachidonic acid –> 5-HPETE [5-Lipoxygenase] –> Leukotrienes
Arachidonic acid –> cyclic enoperoxides [COX1/2] –> Prostacyclin (PGI2), Prostglandins (PGE), Thromboxane (TXA)
Acetaminophen MOA
reversibly inhibits cycloxygenase
Not anti-inflammatory
Aspirin MOA
Irreversibly inhibits cycloxygenase
Covalent acetylation
Tinnitus, Acute renal failure, GI bleeding
Celecoxib MOA
COX2 specific
Spares platelet fxn as TXA2 production is dependent on COX-1
Rheumatoid arthritis, osteoarthritis
Leflunomide MOA
Reversibly inhibits dihydroorotate dehydrogenase
Preventing pyrimidine synthesis
Suppress T cell proliferation
RA, psoriatic arthritis
Bisphosphonates
- Examples (4)
- MOA
- Clinical (5)
- AE (3)
Alendronate, ibandronate, risedronate, zoledronate
Pyrophosphate analog, bind hydroxyapatite in bone, inhibiting osteoclast activity
Osteoporosis, hypercalcemia, Paget dises of bone, metastatic bone disease, osteogenesis imperfecta
Epophagitis, osteonecrosis of jaw, atypical stress fracture
Teriparatide MOA
Recombinant PTH analog give SQ daily
Increase osteoblast activity
Osteoporosis
Increase risk of osteosarcoma
Gout drugs (7)
Chronic
1) Allopurinol
2) Febuxostat
3) Pegloticase
4) Probenecid
Acute
5) NSAIDs
6) Glucocorticoids
7) Colchicine
Purine excretion pathway (1,1, 3)
Purines –> hypoxanthine –> xanthine [Xanthine oxidase]
Xanthine –> Plasma uric acid [Xanthine oxidase]
Plasma uric acid –> Urate crystals in joints –> Gout
- -> Tubular reabsorption - -> Urine
Allopurinol MOA
Competitive inhibitor of xanthine oxidase
Decrease conversion to hypoxanthine and xanthine to urate
Febuxostat MOA
Inhibits xanthine oxidase
Inhibits xanthine oxidase
Allopurinol
Febuxostat
Recombinant uricase that catalyzes metabolism of uric acid to allantoin (more water soluble product)
Pegloticase
Probenecid MOA
inhibits reabsorption of uric acid in proximal convoluted tubule
Can precipitate uric acid calculi
Colchicine MOA
Binds and stabilizes tubulin to inhibit microtubule polymerization, impairing neutrophil chemotaxis and degranulation
TNF-alpha inhibitors
Etanercept
Infliximab
Adalimumab
Certolizumab
Golimumab
Etanercept MOA
TNF-alpha inhibitor
Fusion protein (receptor for TNF-alpha + IgG Fc) produced by recombinant DNA
eTaNerCEPT interCEPTs TNf
Infliximab
Adalimumab
Certolizumab
Golimumab
TNF-alpha inhibitor
Anti-TNF-alpha monoclonal ab
-sartan
Angiotension receptor blockers
-stigmine
cholinesterase inhibitors
-curium/ -curonium
Non-depolarizing neuromuscular blocking drugs
-glitazone
thiazolidinediones
-dipine
dihydropyridine calcium channel blockers
-azepam
Benzodiazepine
-conazole
antifungal drugs
-caine
local anesthetics
-cycline
tetracycline antibiotics
-navir
protease inhibitors
cholinesterase inhibitors
-stigmine
local anesthetics
-caine
dihydropyridine calcium channel blockers
-dipine
protease inhibitors
-navir
Non-depolarizing neuromuscular blocking drugs
-curium/ -curonium
Angiotension receptor blockers
-sartan
antifungal drugs
-conazole
tetracycline antibiotics
-cycline
Benzodiazepine
-azepam
thiazolidinediones
-glitazone
Proteasome inhibitor
Bortezomib
Carfilzomib
Boronic acid contain dipeptide
Bortezomib
Proteasome inhibitor
Proteasome inhibitor MOA
Results in accumulation of toxic intracellualr proteins
Excess pro-apoptotic proteins –> induce apoptosis
Tx of hypercalcemia
Hydration
Corticosteroids (mild)
Bisphosphonates (moderate to severe hypercalcemia)
-sartan
Angiotensin II receptor blocker
-stigmine
AChE inhibitor
-curium/ curonium
Nondepolarizing paralytic
-glitazone
PPAR-gamma activator
-azole
Ergosterol synthesis inhibitor
-bendazole
Antiparasitic/ antihelminthic
-cillin
transpeptidase (penicillin binding protein)
-cycline
Protein synthesis inhibitor
-ivir
Neuraminidase inhibitor
-navir
Protease inhibitor
-ovir
DNA polymerase inhibitor
-thromycin
Macrolide antibiotic
-ane
inhalational general anesthetic
-azine
typical antipsychotic
-barbital
barbiturate
-caine
local anesthetic
-etine
SSRI
- ipramine
- triptyline
TCA
-triptan
5-HT agonist
-zepam, -zolam
Benzodiazepine
-chol
Cholinergic agonist
-olol
beta blocker
-terol
beta2 agonist
-zosin
alpha 1 antagonist
-afil
PDE-5 inhibitor
-dipine
Dihydropyridine Ca channel blocker
-pril
ACE inhibitor
-statin
HMG-CoA reductase inhibitor
-xaban
Direct factor Xa inhibitor
-dronate
Biphosphonate
-prazole
Proton pump inhibitor
-prost
Prostaglandin analog
-tidine
H2 antagonist
-tinib
tyrosine kinase inhibitor
-tropin
Pituitary hormone
-ximab
chimeric monoclonal Ab
-zumab
Humanized monoclonal ab
ACE inhibitors adn ARBs AE
renal failure
Oligohydramnios
Aminoglycosides AE
[Antibiotics]
Ototoxicity
Fluoroquinolones AE
[Antibiotics]
Cartilage damage
Tetracyclines AE
[Antibiotics]
Discolored teeth
Cyclophosphamide AE
[Cancer drug]
Ear/ facial anomalies
limb hypoplasia
Absence of digits
Methotrexate AE
[Cancer drug]
Neural tube defects
Abortion
Carbamazepine AE
[Seizure drug]
Neural tube defects
Valproic acid AE
[Seizure drug]
Neural tube defects
Phenytoin AE
Fetal hydantoin syndrome
Lithium AE
[Mood stabilizer]
Ebstein anomaly
Statins AE
CNS and limb abnormalities
Warfarin AE
Bone/ cartilage defects
Nasal hypoplasia
Isotretinoin AE
Spontaneous abortion
Birth defects
Diethylstilbestrol (DES) AE
Clear cell vaginal adenocarcinoma
Thalidomide AE
Phocomelia
Limb deformities
Metformin
- type
- MOA (2)
- SE (2)
[Biguanide]
Decrease gluconeogenesis in liver
Improve insulin sensitivity
SE: GI upset, lactic acidosis
Glimepiride
- type
- two others
- MOA (1)
- SE (2)
[Sulfonylureas]
also glipizide, glyburide
Close K channels in beta cells –> increased secretion insulin
Hypoglycemia
Weight gain
Sulfonylureas (3)
Glimepiride
GLipizide
Glyburide
Glipizide
- type
- two others
- MOA (1)
- SE (2)
[Sulfonylureas]
also glimepiride, glyburide
Close K channels in beta cells –> increased secretion insulin
Hypoglycemia
Weight gain
Glyburide
- type
- two others
- MOA (1)
- SE (2)
[Sulfonylureas]
also glipizide, Glimepiride
Close K channels in beta cells –> increased secretion insulin
Hypoglycemia
Weight gain
Pioglitazone
- type
- other one
- MOA (3)
- SE (2)
[thiazolidinediones]
Rosiglitazone
Increased sensitivity to insulin in peripheral tissue
Decrease hepatic gluconeogenesis
Bind to PPAR-gamma receptor (regulate FA storage and glucose metabolism, improve insulin secretion)
Fluid retention
Weight gain
Liraglutide
- type
- others (3)
- MOA (3)
- SE (2)
GLP-1 agonists
Exenatide
Albiglutide
Dulaglutide
Increases glucose-dep insulin release
Decrease glucagon release
Promote delayed gastric emptying
WL
Nausea
Sitagliptin
- type
- others (3)
- MOA (2)
- SE (1)
DDP-4 inhibitors
Alogliptin
Saxagliptin
Linagliptin
Prevents DDP-4 from inactivating GLP-1
Increases glucose-dependent insulin release
Low side effet profile
Dapagliflozin
- type
- others (2)
- MOA (1)
- AE (3)
SGLT-2 inhibitors
Empagliflozin
Canagliflozin
More glucose lost in urine
Recurrent UTI and mycotic infection
Dehydration
Diabetic ketoacidosis