STEP1 Pharm Flashcards by Aubrey Ann

Glucocorticoids inhibit

Phospholipase A2

Cortisone, hydrocortisone,
“-sone, -olone”

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Glucocorticoids increase ____ which ____

IkB inhibits NF-kB (prevents increase COX-2)

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Inhibit COX-2 only

celecoxib

Glucocorticoids increase IkB which inhibits NF-kB which increases COX-2

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Inhibit COX1/2

Aspirin (irreversible)
NSAIDS
- Ibuprofen, naproxen, indomethacin

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Inhibit 5-Lipoxygense

Zileuton

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Inhibit Leukotriene receptor

Montelukast

Zafirlukast

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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)

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Acetaminophen MOA

reversibly inhibits cycloxygenase

Not anti-inflammatory

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Aspirin MOA

Irreversibly inhibits cycloxygenase
Covalent acetylation

Tinnitus, Acute renal failure, GI bleeding

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Celecoxib MOA

COX2 specific

Spares platelet fxn as TXA2 production is dependent on COX-1

Rheumatoid arthritis, osteoarthritis

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Leflunomide MOA

Reversibly inhibits dihydroorotate dehydrogenase
Preventing pyrimidine synthesis
Suppress T cell proliferation

RA, psoriatic arthritis

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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

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Teriparatide MOA

Recombinant PTH analog give SQ daily
Increase osteoblast activity

Osteoporosis

Increase risk of osteosarcoma

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Gout drugs (7)

Chronic

1) Allopurinol
2) Febuxostat
3) Pegloticase
4) Probenecid

Acute

5) NSAIDs
6) Glucocorticoids
7) Colchicine

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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

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Allopurinol MOA

Competitive inhibitor of xanthine oxidase

Decrease conversion to hypoxanthine and xanthine to urate

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Febuxostat MOA

Inhibits xanthine oxidase

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Inhibits xanthine oxidase

Allopurinol

Febuxostat

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Recombinant uricase that catalyzes metabolism of uric acid to allantoin (more water soluble product)

Pegloticase

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Probenecid MOA

inhibits reabsorption of uric acid in proximal convoluted tubule

Can precipitate uric acid calculi

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Colchicine MOA

Binds and stabilizes tubulin to inhibit microtubule polymerization, impairing neutrophil chemotaxis and degranulation

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TNF-alpha inhibitors

Etanercept

Infliximab
Adalimumab
Certolizumab
Golimumab

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Etanercept MOA

TNF-alpha inhibitor

Fusion protein (receptor for TNF-alpha + IgG Fc) produced by recombinant DNA

eTaNerCEPT interCEPTs TNf

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Infliximab
Adalimumab
Certolizumab
Golimumab

TNF-alpha inhibitor

Anti-TNF-alpha monoclonal ab

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-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

STEP1 Pharm Flashcards

(109 cards)