Buzzwords 2 Flashcards
MOA - bind cyclophilin, inhibit calcineurin -> prevent IL-2 transcription -> block T-cell activation
Cyclosporine
MOA
MOA - bind FK506 binding protein (FKBP), inhibit calcineurin -> prevent IL-2 transcription -> block T-cell activation
Tacrolimus (FK506)
MOA
MOA - binds FKBP, inhibits mTOR -> prevent
response to IL-2 -> block T-cell activation and B-cell differentiation
Sirolimus (rapamycin)
MOA
Compare the AE of cyclosporin, tacrolimus, and sirolimus.
Cyclosporine and tacrolimus both cause nephrotoxicity. Sirolimus does NOT.
Cyclosporine causes gingival hyperplasia and hirsutism. Tacrolimus does NOT.
Which drug is synergistic with Cyclosporine?
Sirolimus
Synergistic with what drug?
MOA - Ab against IL-2 receptor
Basiliximab
MOA
MOA - reversible inhibition of IMP dehydrogenase -> prevents purine synthesis in B and T cells
Mycophenolate mofetil
MOA
Immunosuppressant associated with invasive CMV infection
Mycophenolate mofetil
Unique association
MOA of corticosteroids
Inhibit NFKB (pro-inflammatory transcription factor) -> suppress both B and T cell function by decreasing transcription of cytokines; also induces T cell apoptosis
What recombinant cytokine may be used to treat anemia, especially in renal failure?
EPO
Epoietin alfa (EPO analog)
What recombinant cytokines may be used to treat leukopenia and recovery granulocyte and monocyte counts?
Colony stimulating factors
Filgrastim (G-CSF) and Sargramostim (GM-CSF)
What recombinant cytokines may be used to treat AI thrombocytopenia?
Thrombopoietin
Romiplostim (TPO analog)
Eltrombopag (TPO receptor antagonist)
Name of recombinant IL-2?
Aldesleukin
Uses of IL-2?
RCC, metastatic melanoma
Uses of IFN-alpha?
Chronic hepatitis C (not first line) and B, RCC
Use of IFN-beta?
MS
Rx - CGD?
IFN-gamma
Alemtuzumab - target?
CD52
Bevacizumab - target?
VEGF
Cetuximab - target?
EGFR
Rituximab - target?
CD20
Trastuzumab - target?
HER2
Adalimumab - target?
Soluble TNF-alpha
Certolizumab - target?
Soluble TNF-alpha
Golimumab - target?
Soluble TNF-alpha
Infliximab - target?
Soluble TNF-alpha
Daclizumab - target?
CD25 (part of IL-2 receptor)
Eculizumab - target?
C5 (complement)
Natalizumab - target?
Alpha-4-integrin (plays a role in WBC adhesion)
Ustekinumab - target?
IL-12/IL-23
Abciximab - target?
GP 2b/3a
Denosumab - target?
RANKL
Digoxin immune Fab - target?
Digoxin
Omalizumab - target?
IgE
Palivizumab - target?
RSV F protein
Important use of bevacizumab?
Colorectal cancer
also RCC, non-small cell lung cancer, neovascular-related eye problems
Important use of cetuximab?
Stage IV colorectal cancer
also head and neck cancer
Important uses of trastuzumab?
Breast cancer and gastric cancer
Why does it make sense that rituximab is used for cancers like B-cell NH lymphoma and CLL?
Anti-CD20 (found on B cells)
How is etanercept different from soluble TNF-alpha antibodies?
It is a decoy TNF-alpha receptor, not a monoclonal Ab
Important use of daclizumab?
Relapsing MS
Important use of eculizumab?
Paroxysmal nocturnal hemoglobinuria
Antiplatelet agent for prevention of ischemic complications in patients undergoing percutaneous coronary intervention?
Abciximab (anti-GP2b3a)
Important use of Denosumab?
Osteoporosis (inhibits osteoclast maturation by mimicking OPG)
Important use of Omalizumab?
Refractory allergic asthma (prevents IgE binding to Fc-E-receptor)
Important use for Palivizumab?
RSV prophylaxis for high-risk infants
Which two immunosuppressants are specifically used to prevent KIDNEY transplant rejection?
Sirolimus
Basiliximab
Med used instead of aspirin to avoid Reye syndrome in children with a viral infection?
Acetaminophen
Aspirin toxicity - early vs. late effects on pH?
Early - respiratory alkalosis
Late - mixed metabolic acidosis-respiratory alkalosis
MOA - reversibly inhibits dihydroorotate dehydrogenase, preventing pyrimidine synthesis -> suppress T-cell proliferation
Leflunomide
MOA - bisphosphonates?
Pyrophosphate analogs that bind hydroxyapatite in bone, inhibiting osteoclast activity
AE - esophagitis (if taken orally, patient should sit upright for 30 minutes)
Bisphosphonates
AE - osteonecrosis of the jaw
Bisphosphonates
MOA - recombinant PTH analog used to increase osteoblastic activity when administered in a pulsatile fashion
Teriparatide
Compare the effects of bisphosphonates vs. teriparatide.
Bisphosphonates are anti-resorptive
Teriparatide is pro-bone growth
AE - increased risk of osteosarcoma?
Teriparatide (thus contraindicated in Paget disease or unexplained ALP elevation)
Compare acetaminophen, aspirin, celecoxib, and NSAIDs regarding MOA.
Anti-pyretic: acetaminophen, intermediate dose aspirin, NSAIDs (NOT celecoxib)
Analgesic - all (intermediate dose aspirin)
Anti-platelet - only low-dose aspirin
Anti-inflammatory - all (high-dose aspirin) EXCEPT acetaminophen
Arachadonic acid pathway
- Membrane phospholipids -> arachidonic acid (via phospholipase A2)
2a. Arachidonic acid -> 5-HPETE -> Leukotrienes via 5-lipoxygenase
2b. Arachidonic acid -> cyclic endoperoxides -> prostacyclin, prostaglandins, and thromboxane via COX1 and COX2
Effect of glucocorticoids on arachidonic acid pathway
- Inhibit Phospholipase A2
2. Activate IKB -> inhibits NF-kappa B (thus inhibiting its activating effect on COX2)
Compare COX1 and COX2.
COX1 - constitutive, found in GI, kidney, platelets, endothelium
COX2 - inflammatory sites only, temporal
Compare TXA2 and PGs.
TXA2 - clotting, vasoconstriction
PGs - prevent clotting, vasodilation
MOA - inhibits reabsorption of uric acid in proximal convoluted tubule
Probenecid
MOA - allopurinol
Competitive inhibitor of XO -> decreased conversion of hypoxanthine and xanthine to urate
Which drugs does allopurinol increase the concentration of?
Azathioprine and 6-MP
MOA - recombinant uricase catalyzing uric acid to allantoin (more water-soluble)
Pegloticase
MOA - inhibits XO
Febuxostat
Rx - chronic gout (preventive)
Probenecid
Allopurinol*
Pegloticase
Febuxostat*
(Prevent a Painful Flare)
[Also colchicine]
Rx - acute gout
NSAIDs (any)
Glucocorticoids
Colchicine
MOA - binds and stabilizes tubulin -> inhibits microtubule polymerization -> impairs neutrophil chemotaxis and degranulation
Colchine
First line treatment for status epilepticus?
Benzodiazepines
First line treatment for prophylaxis of recurrent status epilepticus
Phenytoin
What is the only other drug indicated for status epilepticus?
Phenobarbitol
First line treatment for epilepsy in babies?
Phenobarbitol
First line treatment for seizures in eclampsia? Other option?
MgSO4; benzodiazepines
Most epilepsy drugs can be used to treat partial (focal) seizures. Which drug is commonly used? Which drugs are NOT indicated?
Common - carbamazepine
NOT indicated - benzos, ethosuximide
Most epilepsy drugs can be used to treat tonic-clonic seizures. Which drugs are commonly used? Which drugs are NOT indicated?
Common - valproic acid, phenytoin
NOT indicated - benzos, ethosuximide, gabapentin, tiagabine, topiramate, vigabatrin
First line treatment - trigeminal neuralgia?
Carbamazepine
Which drug is commonly used to treat absence seizures? What are two other alternatives?
Common - ethosuximide
Other - lamotrigine, VPA
Which epilepsy drugs affect (generally increase) GABA action?
- Benzodiazepines
- Phenobarbitol
- Tiagabine (inhibits reuptake)
- Topiramate
- Valproic acid
- Vigabatrin
Which epilepsy drugs increase GABA by inhibiting GABA transaminase? Which of these is irreversible?
Valproic acid, vigabatrin (irreversible)
Which epilepsy drugs act by blocking calcium channels?
Ethosuximide (thalamic T-type channels)
Gabapentin (high-voltage)
Which epilepsy drugs inhibit Na+ channels?
Carbamazepine Lamotrigine (also inhibits release of glutamate) Phenytoin Topiramate Valproic acid
Epilepsy drug with AE - permanent visual loss?
Vigabatrin
Patients on which epilepsy drug should have their LFTs monitored?
VPA
Compare MOA of barbiturates and benzodiazepines.
Both facilitate GABA-A action
Barbiturates - increase duration of chloride channel opening
Benzos - increased frequency of chloride channelingn opening
Short-acting benzos with a higher addictive potential?
ATOM (Alprazolam, Triazolam, Oxazepam, Midazolam)
Benzos with minimal first pass metabolism (can be used in elderly, patients with liver disease0?
LOT (Lorazepam, Oxazepam, Temazepam)
Rx - OD of benzodiazepines?
Flumazenil
Also reverses effects of non-benzo hypnotics
MOA - melatonin receptor agonist, binds MT1 nd MT2 in suprachiasmatic nucleus
Ramelteon
Which insomnia medication has no risk of dependence?
Ramelteon
Suvorexant has “no or low” dependence
MOA - hypocretin (orexin) receptor antagonist
Suvorexant
MOA - bind BZ1 subtype of the GABA receptor
Zolpidem, Zaleplon, Eszopiclone
Drugs used to treat Parkinson disease?
Bromocriptine Amantadine Levodopa (w/carbidopa) Selegiline (and COMT inhibitors) Antimuscarinics
BALSA
MOA - dopamine agonist (ergot and non-ergot)?
Ergot - bromocriptine
Non-ergot - pramipexole, ropinirole
MOA - increased dopamine availability via increased release and decreased reuptake?
Amantadine
MOA - prevent dopamine breakdown?
Selegiline (inhibit MAO-B)
Entacapone (inhibit central COMT)
Anti-muscarinics used in Parkinson disease to curb excess cholinergic activity?
Benztropine
Trihexyphenidyl
(Improves tremor and rigidity, little effect on bradykinesia)
Rx - increase survival in ALS?
Riluzole (decreases neuron glutamate excitotoxicity)
Rx - Huntington chorea and tardive dyskinesia?
VMAT inhibitors (tetrabenazine, reserpine)
AChE inhibitors used to treat AD?
Donepezil, rivastigmine, galantamine
NMDA receptor antagonist used to treat AD?
Memantine
Which types of anesthetics have rapid induction and recovery?
Decreased blood solubility
Minimal alveolar concentration?
[inhaled asthetic] required to prevent 50% of subjects from moving in response to a noxious stimulus
Why does N2O (nitrous oxide) have fast induction and low potency?
Decreased blood solubility
Decreased lipid solubility
Fever and severe muscle contractions induced by inhaled anesthetics or succinylcholine
Malignant hyperthermia
Rx - malignant hyperthermia?
Dantrolene
Which IV anesthetic decreases cerebral blood flow?Which increases it?
Decrease - thiopental
Increase - ketamine
Which three drugs are used to treat glaucoma by decreasing aqueous humor synthesis?
- Beta-blockers (timolol, betaxolol, carteolol)
- Alpha-agonists (epinephrine, apraclonidine, brimonidine)
- Diuretics (acetazolamide)
Which 2 drugs are used to treat glaucoma by increasing outflow of aqueous humor?
Prostaglandins (decreased resistance of flow thru uveoscleral pathway)
M3 cholinomimetics (direct - pilocarpine, carbachol, indirect - physostigmine, echothiophate) (contraction of ciliary muscle, opening of trabecular meshwork)
Which glaucoma drug is CONTRAindicated in closed-angle glaucoma?
Alpha-1 agonists (cause mydriasis)
AE (glaucoma drug) - browning of iris + eyelash growth
Prostaglandins
Rx - acute angle closure glaucoma
Pilocarpine
H2 blocker with lots of AE effects
Cimetidine (CYP450 inhibitor, anti-androgenic, cross BBB, cross placenta, decrease excretion of creatinine)
Which antacid causes constipation? Which causes diarrhea?
Constipation - aluminum hydroxide
Diarrhea - magnesium hydroxide
Drug used for prevention of NSAID-induced peptic ulcers?
Misoprostol (PGE1 analog)
MOA - combination of sulfapyridine (antibacterial) and 5-aminosalicyclic acid (anti-inflamatory), activated by colonic bacteria?
Sulfasalazine
Indication - sulfasalazine?
UC, Crohn disease (colitis component)
List the 2 bulk-forming laxatives.
Psyillium, methylcellulose
List the 4 osmotic laxatives.
Mg hydroxide, Mg citrate, polyethylene glycol, lactulose
How is lactulose, an osmotic laxative, also used to treat hepatic encephalopathy?
Gut flora degrade it into metabolites (lactic and acetic acid) that promote nitrogen excretion
1 stimulant laxative
Senna (stimulates enteric nerves)
AE - melanosis coli
Senna
1 emollient
Docusate
List the 3 first generation H1 blockers.
Diphenhydramine
Dimenhydrinate
Chlorpheniramine
List the 4 second generation H1 blockers.
Loratadine
Fexofenadine
Desloratadine
Cetirizine
Major differences between first and second generation H1 blockers?
1st - used for allergy, motion sickness, and sleep aid
2nd - used for allergy only
1st - sedation, antimuscarinic, and anti-alpha-adrenergic effects
2nd - less sedating (less entry into CNS)
MOA - expectorant that things respiratory secretions, but does not suppress cough reflex
Guaifenesin
MOA - mucolytic that disrupts disulfide bonds, used in COPD and CF
NAC
MOA - anti-tussive that antagonizes NMDA glutamate receptors
Dextromethorphan
List the 2 alpha-adrenergic agonists used as nasal decongestants
Pseudoephedrine, phenylephrine
List 3 drugs that can treat pulmonary hypertension.
- Endothelin receptor antagonists
- PDE5 inhibitors
- Prostacyclin analogs
First line treatment for chronic asthma
Inhaled corticosteroids (fluticasone, budesonide)
Indication - prevention of bronchospasm (NOT acute bronchodilation)
Mast cell stabilizers (cromolyn, nedocromil)