Pharm Mini Board Flashcards
Tacrolimus
Calcineurin inhibition preventing IL-2 transcription; used for transplant rejection prophylaxis
ADRs: Nephrotoxicity
Sirolimus
mTOR inhibitor that prevents T-cell response to IL-2; used for kidney transplant prophylaxis
ADRs: Aplastic anemia, insulin resistance, delayed wound healing
Daclizuma, basiliximab
Abs that block the IL-2 receptor
Azathioprine
Antimetabolite precursor of 6-MP; inhibits lymphocyte proliferation “Azathiopurine”
Uses: Transplant rejection prophylaxis, RA, Crohn’s
ADRs: Aplastic anemia, increased toxicity w/ allopurinol since 6-MP is degraded by xanthine oxidase
Glucocorticoids (immunosuppressive action)
Inhibits NFkB; decreases transcription of cytokines
Uses: Transplant rejection prophylaxis. AI disorders, inflammation
Cyclosporine
Binds to cyclophilin and inhibits IL-2 transcription; used to prevent transplant rejection as well as for psoriasis
ADRs: Nephrotoxicity, gingival hyperplasia, hirsutism, HTN
Alemtuzumab
CD52 antibody
Used for CLL
“lem=lymphocytic”
Bevacizumab
VEGF ab
-Used for colorectal and renal cell carcinomas
Rituximab
CD20 ab
B-cell non-Hodgkin’s lymphoma, CLL, RA, ITP
Etanercept
Decoy TNF-a receptor used for IBD, RA, ankylosing spondylitis
-Adalimumab and infliximab are TNF-a abs
Eculizumab
C5 ab
Used for PNH
Natalizumab
a4-integrin ab
Used for MS, Crohn’s
Abciximab
Glycoprotein IIb/IIIa ab
- Used for prevention of ischemic complications in pts. undergoing coronary interventions;
- also for unstable angina ya dingus
Denosumab
RANKL ab
-Used for osteoporosis; mimics osteoprotegrin by inhibiting osteoclast maturation
Omalizumab
IgE ab
Used for severe allergic asthma
Palivizumab
RSV F protein ab
-Used as prophylaxis for high risk infants
Penicillinase Resistant Drugs
Methicillin, Oxacillin, Nafcillin (IV), Cloxacillin, Dicloxacillin (PO)
-Also, general ADRs for penicillins include rash, interstitial nephritis, and seizures
DOC for Listeria
Ampicillin; aminopenicillins also have more gram neg activity and useful for enterics
Antipseudomonal penicillins
Piperacillin, Ticarcillin (taken off market due to INCREASED SODIUM)
- Also covers anaerobes, Staph/**Enterococcus, Piddly, Fence, SPACE)
- Make sure to use B-lactamase inhibitor with these
Cefazolin
1st gen Cephalosporin that covers Gram +, ^PEK
-Used as a prophylactic prior to surgery to prevent S. aureus infxns
Cefuroxime, Cefoxitin, Cefotetan
Covers Gram +, ^PEK
TAN FOX =» Also covers ANAEROBES
Ceftriaxone
3rd gen cephalosporins that cover serious Gram - inxns (^SACE)
DOC for N. meningitidis/gonorrheae and Lyme disease
Ceftazidime
3rd gen cephalosporin that covers Pseud BUT loses gram +
Cefepime
Same as ceftazidime but recovers Gram + orgs
-What does this mean it covers?
Ceftaroline
5th gen cephalosporin that covers Gram pos, neg, and MRSA
-Lose pseud tho
Cephalosporin ADRs
- Cross reactivity w/ penicillin allergy
- Bleeding due to inhibition of Vitamin-K coag factors
- Disulfarim like reaction
- Pseudoemembranous colitis
- Don’t use w/ AGCs (increases nephrotoxicity)
Imipenem
DOC for ESBL species; also used for Staph, Strep, Entero, SPACE, anaerobes
- Is metabolized in the kidneys to a nephrotoxic product; administer w/ cilastatin (to make the kill lastin’)
- Severe ADRs include: Seizures, anemia/leukopenia/thrombocytopenia
Ertapenem
Similar to meropenem and doripenem BUT adds some pseud. coverage and takes away entero
Aztreonam
DOC for penicillin allergy pts. but only covers Gram negs
Ciprofloxacin, moxifloxacin, levofloxacin
MOA: DNA gyrase inhibitor (topoisomerase II); exhibits a PAE
***CANNOT TAKE W/ ANTACIDS
ADRs: Damage cartilage (young people usually) => tendonitis and tendon rupture (old people usually)
QT prolongation Photosensitivity, rashes CI= pregnant women
Ciprofloxacin facts
Least tendency to prolong QT interval of FQNs
Highest tendency for photosensitivity
Good pseud. coverage
Levofloxacin
Good for enteric GNR inxns, atypical pneumonias
Moxifloxacin
Hs anaerobic coverage
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin,
Mean GNATS caNNOT kill anaerobes
AGCs tht bind to the 30s subunit and inhibit the initiation complex
*Bactericidal, concentration dependent killing
DOC for gram negative AEROBES (requires O2 for uptake)
ADRs: Nephrotoxicity, Ototoxicity, Teratogen
Mechanism of tetracycline resistance
Efflux of active drug, (classic question)
-Decreased absorption w/ milk and antacids
Doxycycline
Only tetracycline not cleared by the kidney or liver (can be used in renal failure); accumulates intracellular (good for rickettsia and chlamydia)
Macrolide general characteristics
Bind to 23S rRNA of the 50s subunit (bacteriostatic)
-Good for covering atypical pneumonias (mycoplasma, chlamydia, legionella) and pertussis
ADRs: Motility issues (GI) Arrhythmia (QT prolongation) Cholestatic hepatitis (estolate form; DONT USE IN PREGNANCY) Rash eOsinophilia
CYP450 inhibitors*
*MoR: Methlyation of 23s rRNA-binding site
DOC for legionella
Azithromycin (also covers other respiratory pathogens like h. flu, m. cat, s. pneumo, mycoplasma)
Telithromycin
Macrolide used against resistant S. pneumo
-Reaches high tissue conc.
Bactrim
Sulfonamide: PABA analog that inhibits dihydropteroate synthase
ADRs: Displaces warfarin from albumin
Morbilliform rash, Steven-Johnson
Tubulointerstitial nephritis (administer w/ fluids)
Kernicterus in newborns (given during late pregnancy)
Trimethoprim: Inhibits DHFR
ADRs: Megaloblastic anemia, leukopenia
Uses: Staph (+MRSA), Gram negs (UTIs), salmonella, shigella, chlamydia
*Prophylaxis for Toxoplasma gondii and PCP
Vanc ADRs
Nephrotoxicity
Ototoxicity
Thrombophlebitis (Red-Man Syndrome; slow infusion rate)
Daptomycin
Disrupts cell membrane of Gram + cocci
**Inactivated by pulmonary surfactant, so don’t use for pneumonia
***ADRs: Rhabdomyolysis (monitor CK)
Linezolid
Similar to Macrolides; useful for MRSA and VRE
ADRs: Aplastic anemia
***Serotonin syndrome w/ serotonergics
Peripheral neuropathy
Clindamycin
Used for anaerobic infxns above the diaphragm (Bacteroides, C. perfringens); typically in aspiration pneumonia or oral infxns
-But causes what classic GI infxn
Metronidazole
Generates free radicals that damage bacterial RNA
DOC for anaerobes and C.diff BELOW the diaphragm
-Also used for Giardia, entamoeba, trichomonas, gardnerella
ADRs: Dilsulfarin w/ alcohol (hypotension, flushing, tachycardia)
Chloramphenicol
***Causes aplastic anemia and gray baby syndrome (due to accumulation)
But works great against anaerobes and meningitis and stuff (just FYI)
t^1/2 equation
.693/ke
or
Vd x .693/ CL
so what does Ke equal?
Zero-order eliminated drugs
Phenytoin
Ethanol
Aspirin
-Same amnt is eliminated no matter what
Works on Gq/ PLC (autonomics)
HAVe 1 M&M
H1, a1, V1, M1, M3
Works on Gi (autonomics)
MAD 2s
M2, a2, D2
Where are M1 receptors found?
Brain
Where are M2 receptors found?
Heart
Cholinesterase inhibitor poisoning
Diarrhea Urination Miosis Bradycardia Bronchospasm Excitation of skeletal muscles and CNS Lacrimation Sweating Salivation
Muscarininic antagonist ADRs
Hot as a hare (decreased sweating)
Dry as a bone (dry mouth/skin)
Red as a beet (flushed skin)
Blind as a bat (cycloplegia)
Mad as a hatter (disorientation)
Raltegravir
HIV integrase inhibitor
-disrupts the ability of HIV dsDNA to integrate into the host cell’s chromosomes thereby preventing transcription of viral mRNA
Beer’s Criteria
Anticholinergics: 1st gen antihistamines like diphenhydramine and GI antispasmodics
CV: a-blockers, antiarrhythmics
CNS: TCAs, antipsychotics, barbiturates, benzos
Endocrine: Sulfonylureas
Pain: Indomethacin, Meperidine
Calcipotriol
Calcitriol analog that binds to the Vitamin D receptor, a nuclear transcription factor, and inhibits keratinocyte proliferation
-Can also inhibit T-cell proliferation
Dobutamine
B-agonist that primarily works on B1 receptors
=»increased inotropy, mild vasodilation, increased HR
-increased myocardial O2 demand is outweighed by heavy increased in CO
-Also has some action on B2 and a1
Ipratropium
Competitive muscarinic receptor blocker
=»Prevention of bronchoconstriction
- enhances effect of B2 agonists (albuterol) but not as good alone
- Also blocks submucosal gland secretion in the lungs
Ribavirin
Inhibits synthesis of guanine nucleotides by competitively inhibiting inosine monophosphate dehydrogenase
=»depletes intracellular GTP and overall inhibition of the duplication of viral genetic material
-Used in HCV and RSV
ADRs: Hemolytic anemia; teratogen
Drug used to decreased likelihood of calicum renal stones
HCTZ
-By reabsorbing Ca2+, there will be less in the lumen; also there will be a higher h2o content in the lumen
Sotalol
BB and a type III anti arrhythmic
***Excessive B-blockade can cause TORSADES DE POINTES
Lidocaine, Mexilitine
Class IB antiarrhythmic that Decreases the AP duration
***Preferentially affects ischemic or depolarized tissue
*DOC for post-MI arrhythmias and digitoxin-induced arrhythmias
Nimodipine
CCB useful in prevention of cerebral vasospasms following an SAH
Nitroprusside
Directly stimulates NO increasing cGMP
*Used in HTN emergencies
**OD can cause CN- toxicity =» Give thiosulfate
Dopamine doses
Low =» vasodilation of renal BF
Medium =» increased cardiac contractility
High =» Generalized vasoconstriction
Metoclopramide
D2 receptor antagonist that is used to increase LES tone, motility, and contractility of the GI tract
ADRs: Parkinsonian effects! Tardive dyskinesia
Cilostazol
PDE III inhibitor; increases the cAMP in platelets resulting in decreased aggregation
Tx: Intermittent claudication, coronary vasodilation, prevention of stroke/TIAs
ADRs: Flushing, nausea, headache e
5-FU
Pyrimidine analog activated to 5F-dUMP which complexes w/ folic acid
=»inhibition of thimidylate synthase
Uses: Solid tumors (colon cancer, pancreatic cancer, basal cell carcinoma)
ADRs: Myelosuppression (can’t be rescued)
Methotrexate
Folic acid analog that inhibits DHF
Uses: Leukemia, Lymphoma, choriocarcinoma, sarcomas, abortion, RA, psoriasis, IBD
ADRs: Myelosuppression (rescued), hepatotoxicity, pulmonary fibrosis
Azathioprine, 6-MP
Purine analog that must be activated by HGPRT; azathioprine is metabolized to 6-MP
Uses: Rejection prophylaxis, IBD, RA, SLE
ADRs: Myelosuppression; ***Increased toxicity w/ allopurinol
Bleomycin
Induces free radical formation =» breaks in dsDNA
Uses: Testicular cancer, Hodgkin’s
ADRs: ***Pulmonary fibrosis, skin hyperpigmentation
Doxorubicin
Generates free radicals that intercalate into DNA and produce breaks
Uses: Solid tumors, leukemias, lymphomas
ADRs: Dilated cardiomyopathy, alopecia
**Dexrazoxane will prevent cardiomyopathy
Cyclophosphamide
Cross link DNA; requires hepatic activation
Uses: Solid tumors
ADRs: Hemorrhagic cystitis; prevent w mesna
Carmustine, Lomustine, Streptozocin
Alkylating agent that can cross the BBB
Uses: ***Glioblastoma multiforme and other brain tumors
ADRs: Convulsions, dizziness, ataxia
Paclitaxel
Stabilize polymerized microtubules in the M phase
=»mitotic spindle cannot break down
Uses: Women cancers
ADRs: alopecia, myelosuppression
Vincristine, Vinblastine
Bind to B-tubulin and inhibit microtubule polymerization
=»prevents microtubule formation
Uses: Solid tumors
ADRs: Neurotoxicity
Kinase inhibitor suffix
-nib
Aldrenoate
Pyrophosphate analogs that bind hydroxyapetite in bones and inhibit osteoclast activity
ADRs: Corrosive esophagitis =» pts. should remain upright for 30 mins
Osteonecrosis of jaw
Pilocarpine
Cholinomimmetic that increases the outflow of aqueous humor via contraction of the ciliary muscle (produces miosis)
-Physostigmine will indirectly do this as well
DOC for acute angle closure glaucoma
Pilocarpine
Latanoprost
PGF2a that increases outflow of aqueous humor
-Darkens the Iris (browning)
Timolol, betaxolol
BBs used to decrease aqueous humor synthesis
Drugs to not use in closed-angle glaucoma
Epinephrine (produces mydriasis)
Second line tx for absence seizures
VA
Olanzapine
Atypical antipsychotic that is assoc. w weight gain
Clozapine
Atypical antipsychotic that is assoc. w/ agranulocytosis
Risperidone
Atypical antipsychotic that is assoc. w/ increased prolactin
=»gynecomastia and lactation
Neuroleptic malignant syndrome
Caused by the typical antipsychotics (haloperidol + -azines)
Fever Encephalopathy Vitals (unstable) Enzymes (increased) Rigidity of muscles (myoglobinuria too)
Tx: Dantrolene
Tardive dyskinesia
Odd, stereotypical facial movements after LONG-TERM typical antipsychotic (chlorpromazine, thioridazine, haloperidol) use
Amitryptiline, imipramine, amoxapine
TCAs that block reuptake of NER and 5-HT3
Uses: Major depression, OCD, peripheral neuropathy, migraines
ADRs: Sedation, a1 blocking effects (postural hypotension), anticholinergic effects (dry mouth, tachycardia)
*Amitryptiline can also prolong QT interval (just cause its stronger)
3 Cs of TCAs
Convulsions
Coma
Cardiotoxicity
-Also see respiratory depression
Tx: NaHCO3