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Pharmacology 2 Cheat Sheet by

Tofaci­tinib

Janus kinas inhibitor PO
2x/day reduced to 1x if
Potent CYP3A4 and CYP2c19 inhibitors (e.g. flucon­azole)
 
Severe renal impairment
 
Mod liver impairment
Combined w/meth­otr­exate or nonbio DMARD
DO NOT combine w/bio DMARD

Other DMARDs in Refractory RA

Azathi­oprine, Cyclop­hos­pha­mide, Cyclos­porine, Penici­llamine
Last-line therapy in refractory disease
use is limited by higher rates of adverse effects

Anaest­hetics SE

CNS effects
Reduction of vascular resistance
Increased intrac­ranial pressure
Decrease BP
Entrorane and Halothane decrease CO
Decreased blood flow to liver and kidneys
Decrease respir­atory rate
Malignant hypert­hermia (uncon­trolled Ca release)
Treated with dantrolene

Local Anesth­etics

Interm­ediate chain linking amino to aromatic ring
block Na+ channels in nerve
sympat­hetic → sharp/dull → touch/temp → motor paralysis
More effect on small C fibers and small A fibers
Amino Esters
Surface: Benzoc­aine, cocaine
 
Short: Procaine
 
Long: Tetracaine
Amino Acids
Medium: Lidocaine
 
Long: Bupiva­caine, ropiva­caine
Lidocaine Patch
12hr on/12 off
 
3 patch max

Lipid Lowering Drugs

HMG- CoA reductase inhibitors
E.g. Atorva­statin, Rosuva­statin, red rice yeast
 
Primary agents
 
↓ LDL and TG, ↑ HDL, ↓ morbid­ity­/mo­rtality
 
antith­rom­botic effects, ↓endot­helial inflam­mation
 
SE: myopathy and hepatotox, elevated LFTs, CPK (muscle/jt pain, rhabdo), proximal muscle weakness
 
CYP450 (grape­fruit, Cimeti­dine)
 
Memory loss, diabetes
Bile acid seques­trants (resins)
E.g. Choles­tyr­amine; ↓ LDL, ↑HDL and TG; Unpleasant taste, GI effects, intxns; Other meds 1 hr before or 4 hr after
Fibrates
E.g. Gemfib­rozil, fenofi­brate
 
↓ LDL and TG, ↑ HDL
 
Toxicity additive w/statins
 
Rhabdo, myopathy, LDL increase
Nicotinic Acid
↓ LDL and TG, ↑ HDL
 
Flushing, itching, HA, Hyperu­ricemia in gout, Hyperg­lyc­emia, Hepatotox
Chol absorption inhibit
E.g. Ezetimibe
 
Decrease LDL, increase HDL
 
HA Diarrhea Upper resp infection
 
hepatotox + rhabdo with statins

Anti-F­actor Xa Inhibitors

Fondap­arinux
SC treat/­prevent DVT/PE
 
Avoid use in Crcl <30 ml/min
 
Monitor: Anti-Xa, sx of bleeding
Apixaban
Inhibit factor X
 
adjust in Afib if ⅔ >80 yo, Scr >1.5, weight <60kg
 
Intxns: phenytoin, carbam­aze­pine, flucon­azole, rifampin
 
bleeding, compliance
Rivaro­xaban
inhibit factor X
 
Take w/evening meal
 
Intxns: phenytoin, carbam­aze­pine, flucon­azole, rifampin

Reversal of antico­agu­lation

Warfarin
Vitamin K
Keparin
Protamine
Enoxaparin
Protamine (less reliable)
Dabigatran
Idaruc­izumab
Apixaban
zhzo Xa
Rivaro­xaban
zhzo Xa

Insulin

Lispro, Aspart
Regular
NPH
Glargine, Detemir, Degludec (basal)
O:<15 m
O:.5-1
O:2-4
O:2-4
P:1-2
P:2-3
P:4-10
P:N/A
D: 3-4
D:3-6
D:10-16
D:24

Thiazo­lid­ine­diones

E.g. Piogli­tazone, Rosigl­itazone (not used, ↑CVD)
↓HDL, trigly­cer­ides; neutral LDL
Decrease fasting plasma glucose 35-40
Reduce A1C ~0.5-1%
6 weeks for max effect
SE: weight ↑, edema, hypogl­ycemia
Contra­ind­icated liver problems or CHF

GLP-1 Agonist

E.g. Exenatide, Liragl­utide
↑ insulin release
↓A1C ~0.7
SE: GI upset, weight loss
Maybe pancre­atitis, gallbl­adder disease, thyroid cancer
Caution in renal disease
CV benefit

Acetam­inophen

central COX inhibitor
Analgesic & Antipy­retic
NOT anti-i­nfl­amm­atory or antith­rom­botic
SE: Hepato­tox­icity
1st line for OA
Avoid alcohol
No Raye’s syndrome
Similar to NSAIDs, better tolerated
2 wks before consid­ering treatment failure

Opioids

Act on Mu, Kappa, Delta receptors
Phenan­threnes
(natural) Codeine, Morphine
Phenan­threnes
(semis­ynt­hetic) Hydroc­odone, Hydrom­orp­hone, Oxycodone
Phenyl­pip­eri­dines
Fentanyl, Meperidine (chills)
Phenyl­eth­yla­mines
Methadone, Propox­yphene
Extended
Oxycodone, Morphine, Fentanyl
Tramadol
Mu receptor agonist, inhibit serotonin and NE reuptake
 
Mild to moderate pain
 
SE: ↓resp depression than other opioids, sedation, consti­pation, dry mouth, nausea, serotonin tox
Morphine
Controlled or immediate
 
SE: potential accumu­lation, itch
 
Not indicated in pts w/renal
Oxycodone
High oral bioava­ila­bility w/no food effect
 
No signif­icant metabo­lites
 
minimally affected by age renal or liver
Methadone
alpha 8-12, beta 24-36
 
NMDA receptor antago­nist/ Seroto­nergic properties
 
SE: Toxicity, QTc prolon­gation
Meperidine
Causes euphoria, most addictive, seizures
Agonists
Oxycodone, Codeine, Hydroc­odone
Mixed
Bupren­orphine
Antago­nists
Naltre­xone, Naloxone
SE: CNS/resp depression (5-7 days), N/V (codeine), consti­pation, itch/rash
 

Capsaicin Cream

Inhibits release of substance P in peripheral
Max effect takes 2-4 wks applic­ation 4x/day
More role in OA than RA

Viscos­upp­lim­ent­ation

E.g. hyaluronic acid
lubricant during low-stress mvmt, anti inflam
Has more role in OA than RA, esp knee
3-5 wkly injections = 1 cycle
Max effect 8-12 wks, lasts 6-12 mo

Non-Bio DMARDs

RA w/in 3 mo, max 6-12 mo
LF, HCQ, MTX need blood count, liver, Cr every 2-4wk/3mo then every 8-12 wks
Methot­rexate
1st line, 2-8 wk onset PO/IM immuno­sup­pre­ssant
 
SE: GI, liver tox, bone marrow, stomat­itis, hair loss, pulm tox
 
Folic acid decrease sx
Leflun­omide
Immuno­sup­pre­ssant effective as MTX
 
SE: GI, rash, hair loss, liver tox
 
Work w/in 1 mo, weaker
Hydrox­ych­lor­oquine
Low tox, 2-6 mo onset, min monitor
 
SE: GI, retinal, derm, HA
Sulfas­alazine
2-3x/day PO anti-i­nflam
 
SE: GI, leukop­enia, anemia, photos­ens­itive, skin, hepatitis, pneumo­nitis, agranu­loc­ytosis, hypers­ens­itivity
 
>HCQ, <DMARDs
 
poor tolerate, lots of monitoring
 
Potentiate antico­agu­lants

IV Anesth­etics

Etomidate
Hypnotic
 
Rapid onset gen anesthesia
 
Min cardiopulm SE
 
Good for CV and pulm comorbid
Propofol
Short acting hypnotic
 
Very rapid recovery
Thiopental sodium
Respir­atory depres­sant, no analgesia
 
Rapid safe induction
 
Barbit­urate
Midazolam
Benzod­iaz­epine
 
Amnesia
 
Potent­ially long halflife
Ketamine
Dissoc­iative analgesia

Local Anesth­etics Additives

Vasodi­lation prevented by vasoco­nst­rictor (e.g. epinep­hrine); prolong effect­/de­crease dose -- do not use in finger­s/toes
Bicarb­onate Decrease burning sensation during admin

Statin Monitoring

CK
Baseline: only in pts at increased risk for musc injury
 
Routine: only in pts w/musc pain/w­eakness
ALT
Routine: only if symptoms of hepatotox occur
FLP
Routine: 4-12 wks after initia­tion, then Q3-12 months as indicated
Hgb A1c
Baseline: only if diabetes status unknown

Antico­agu­lants

Heparin
Unfrac­tio­nated heparin (UFH); IV/SC
 
monitor aPTT, platelets, hgb, hct, HIT
Low-mo­lec­ula­r-w­eight heparin
Enoxap­arin, SC
 
Renal adjust Crcl <30
 
monitor less frqnt, Anti-Xa levels not aPTT
Anti-F­actor Xa inhibitor
Fondap­arinux, SC
 
Apixaban, PO
 
Rivaro­xaban, PO
Direct Thrombin Inhibitors
Argatr­oban, IV
 
Dabiga­tran, PO
Vitamin K antag
Warfarin, PO
 
Onset: slow, antico­agu­lation occurs 48-72 h after the first dose once factors are depleted
 
Monitor INR (goal 2-3), Hgb/hct, bleeding
 
Intxn: Food: green leafy vegetables Meds: cipro, bactrim, flagyl, flucon­azole, rifampin
 
Preferred in renal dysfun­ction

Direct Thrombin Inhibitors

Do not require antith­rombin
Monitor aPTT, platelets, hgb, het, bleeding
Continuous infusions
Used in HIT mgmt
Short duration
Argatroban
Falsely elevate INR
 
No monitoring or reversal agent
 
ADE: upset stomach, bleed
 
Intxns: avoid rifampin
 
Store in original container and use within 30 days of opening

Antico­agulant Dosing

DVT ppx: enoxparin 40mg q24 or 30mg q12 or heparin 5k units bid-tid.
PE/DVT tx: Enoxaparin 1.5mg/kg q24 hrs and 1mg/kg q12 hrs; heparin drip 18 units/­kg/hr

Biguanides

e.g. metformin
↓ glucose product, ↑ glucose uptake
↓ A1C 1-1.5
Low risk hypogl­ycemia
SE: Diarrh­ea/GI, ↓B12, l. acidosis, weight ↓
Contra­ind­icated GFR<30

Meglit­inides

e.g. Repagl­inide, Nategl­inide
Stimulate insulin secretion
Shorter acting, best taken after eating
↓A1C ~1
SE: Hypogl­ycemia, weight ↑
Safe w/greater renal insuff­iciency than SU

SGLT2 Inhibitors

E.g. Canagl­ifl­ozin, Empagl­iflozin
↑glucose excretion
↓A1C 0.7-1
Empagl­ifl­ozin: avoid if GFR <45
SE: Genital fungal infxn, UTI, AKI, dizzy, hypote­nsion, hyperk­alemia, hypogl­ycemia, fractures, ↓BMD, CV benefits

Non-Opioid Analgesics

NSAIDs, ASA, salicy­lates
Prosta­glandin inhibitors
 
Inhibit COX-1 and COX-2
 
GI side effects
 
ASA = antipl­atelet primarily used to prevent heart disease and stroke
 
Thromb­oxanes involved in platelet aggreg­ation and thrombus formation
Selective COX-2 inhibitor
e.g. Celecoxib
 
↑ MI and stroke
 
Rofecoxib and Valdecoxib taken off market
 
Celecoxib ↓GI SE in pt not on ASA
Do not cause tolerance, not addictive
All have ceiling effect to analgesia

Opioid Withdrawal

Body aches, weakness, fatigue
Diarrhea, stomach cramping
Insomnia
Irrita­bility
Loss of appetite
Nausea­/vo­miting
Increased BP/HR
Runny nose, sneezing, yawning
Chilliness and “goose bumps”

Patient Controlled Analgesia

e.g. Morphine, hydrom­orphone
Monitor HR, BP, RR, Pain, usage, O2
 

Glucos­ami­ne/­Cho­ndr­oitin

Glucos­amine
cartilage building block
Chondr­oitin
Increase protein synthesis
OTC, not 1st line, may improve OA knee pain
Weeks to months for effect
SE: GI upset

Cortic­ost­eroids

E.g. Dexame­tha­sone, Hydroc­ort­isone, Methyl­pre­dni­solone
Intraa­rti­cular
1-6 wk relief for OA/RA knee
 
3-4/yr limit
 
Lidocaine sometimes added
Systemic
RA, not OA
Acute SE: Hyperg­lyc­emia, HTN, euphor­ia/­psy­chosis, weight­↑/e­dema, GI bleed
Chronic SE: Cushing’s appear­ance, cataracts, hyperl­ipi­demia, muscle­/te­ndon, OP/fra­ctures, infection, HPA suppre­ssion

Bio DMARDs

Non-TNF
Abatacept SE: Pulmonary infection, allergic rxn, HA/dizzy
 
Anakinra SE: inj site rxn, infection, allergic rxn
 
Rituximab SE: rash, infection, neuro, infusion rxn, Tumor Lysis, multifocal leukoe­nce­pha­lopathy
TNF inhibit
Adalim­umab: SC every 2 wk, mild-mod inject rxn
 
Etaner­cept: SC 1-2/wk, mild-mod inject rxn
 
Inflix­imab: IV at 0,2,6,8 wk; infusion rxn
 
Increased malignancy risk
 
SE: hypers­ens­iti­vity, Lupus-­like, hepatotox, pancyt­openia, aplastic anemia, heart failure
 
MTX combo or solo
 
Mod-severe RA
Possibly reacti­vates TB, no live vaccine

NM Blocking Agents

Non-De­pol­arizing
Compet­itive Ach antag
 
Pancur­onium O: 4-6 min D: 120-180 min
 
Rocuronium O: 1-2 min D: 30-60 min
Depola­rizing
Overst­imulate receptor
 
Succin­ylc­holine O: 1-1.5 min D: 5-8 min

Anaest­hetics Pharma­cok­inetics

highly lipid soluble
When discon­tinued, drugs will continue to enter systemic circul­ation
Lethargy, confusion

Lidocaine Patch

12 hr on/12 hr off
3 at at time max

monoclonal antibo­die­s/PCSK9 inhibit

SC
Reduce LDL by additional 60% with statin
E.g. evoloc­umab, alirocumab
Advant­ages: injected once or twice/­month
SE: common cold, itching, flu, injxn site rxns, allergic rxns

Antipl­atelets

Aspirin
ADP receptor inhibitors e.g. Clopid­ogrel Prasugrel Ticagrelor
PO

Thromb­olytics

Alteplase (IV)
Dissolve clots acutel­y/clear IV line
Relative contra­ind­ica­tion: HTN
Absolute contra­ind­ica­tion: recent head trauma
ADR: bleeding, hemorrhage
C

Heparin Induced Thromb­ocy­topenia

Type 1
10-20%
 
Onset: 2-3 d
 
Platelet <50% decrease, nadir >100k
Type 2
1-3%
 
Onset: 5-10 d
 
Platelet >50% decrease, nadir 10-20k
 
Antibody mediated
 
Thromb­oem­bolic sequelae 30-80%
 
D/c all heparin products, initiate direct thrombin inhibi­tor­/co­umadin

ADP Receptor Inhibitors

Clopid­ogrel
Indica­tions: ASA + Clopid­ogrel in pts receiving stents
Prasugrel
More potent, less variable platelet response than Clopid­ogrel
 
reduction of thrombotic CV events (including stent thromb­osis) in pts w/ACS who are to be managed w/PCI
 
Risks may exceed benefits in pts w/ >75 yo Previous history of TIA or stroke <60kg
 
Likely to undergo CABG = bleed risk
 
Hold for 7 days before surgery
Ticagrelor
SE: bleeding, dyspnea, bradyc­ardia
 
2x/day
 
Avoid in pts w/hx of hemorr­hagic stroke
 
Avoid aspirin >100 mg CYP 3a4 inducers (rifampin, carbam­aze­pine, phenytoin) CYP 3A4 inhibitors (ketoc­ona­zole, ritonavir) Monitor digoxin levels

Sulfon­ylurea

e.g. Glyburide, Glimep­iride, Glipizide
↑endog­enous insulin secretion
↓A1C 1-2
SE: hypogl­ycemia, ↑weight, photos­ens­itive
Least expensive
Caution in renal, elderly
Often discon­tinued once insulin started

DPP-4 inhibitors

e.g. Sitagl­iptin, Saxagl­iptin
↑ incretin, insulin release
↓A1C ~0.7
Well tolerated, no weight gain, no hypogl­ycemia
Maybe pancre­atitis, jt pain, heart failure
Dose modifi­cation in renal impairment
CYP3a4 intera­ctions

Other Antidi­abetics

Alpha-­glu­cos­idase inhibitors
e.g. Acarbose
 
block enzymes that digest starches in small intestine
 
GI upset, flatul­ence, bloating
Amylin analogs
e.g. Pramli­ntide
 
Injectable
Bile acid seques­trants
e.g. Colese­velam
 
GI side effects

NSAIDs

1st line in RA, 2nd in OA
Aspirin
Most widely used, analgesic, antinf­lam­matory, antipy­retic, antipl­atelet
Diclofenac
more potent than other NSAIDs, ADRs occur in 20%
Ibuprofen
fever, GI side effects ~5-15%
Indome­thacin
Dose related side effects (i.e. confus­ion); 35-50% pts
Ketorolac
Orally or IM, IV doses provide postop­erative analgesia equivalent to opioids
 
not used >5 days due to ADR
Naproxen
Similar to ibuprofen, less frequent dosing 2x/day
SE: GI, acute renal failure, BP, hypers­ens­itivity
GI SE: Celecoxib < Diclofenac < Ibuprofen & Naproxen < ketorolac
Take ibuprofen at least 2 hours after ASA -- makes aspirin ineffe­ctive
GI ulcers­/bleed prophy­laxis: Misopr­ostol, Proton pump inhibitors (panto­pra­zole), H2RAs (ranit­idine)
Use with caution on pt on antico­agu­lants
Need to take contin­uously for antiinflam
2-4 wk trial needed

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