|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
|
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
|
|
|
Azathioprine, Cyclophosphamide, Cyclosporine, Penicillamine
|
|
|
Last-line therapy in refractory disease
|
|
|
use is limited by higher rates of adverse effects
|
|
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
|
|
|
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
|
|
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
|
|
Warfarin
|
Vitamin K
|
|
Keparin
|
Protamine
|
|
Enoxaparin
|
Protamine (less reliable)
|
|
Dabigatran
|
Idarucizumab
|
|
Apixaban
|
zhzo Xa
|
|
Rivaroxaban
|
zhzo Xa
|
|
e.g. metformin
|
|
↓ glucose product, ↑ glucose uptake
|
|
↓ A1C 1-1.5
|
|
Low risk hypoglycemia
|
|
SE: Diarrhea/GI, ↓B12, l. acidosis, weight ↓
|
|
Contraindicated GFR<30
|
|
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
|
|
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
|
|
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
|
|
|
e.g. Morphine, hydromorphone
|
|
Monitor HR, BP, RR, Pain, usage, O2
|
|
Inhibits release of substance P in peripheral
|
|
Max effect takes 2-4 wks application 4x/day
|
|
More role in OA than RA
|
|
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
|
|
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
|
|
|
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
|
|
Vasodilation prevented by vasoconstrictor (e.g. epinephrine); prolong effect/decrease dose -- do not use in fingers/toes
|
|
|
Bicarbonate Decrease burning sensation during admin
|
|
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
|
|
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
|
|
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
|
|
|
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
|
|
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
|
|
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
|
|
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
|
|
|
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
|
|
|
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
|
|
|
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
|
|
|
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
|
|
highly lipid soluble
|
|
|
When discontinued, drugs will continue to enter systemic circulation
|
|
|
Lethargy, confusion
|
|
12 hr on/12 hr off
|
|
|
3 at at time max
|
|
Aspirin
|
|
|
ADP receptor inhibitors e.g. Clopidogrel Prasugrel Ticagrelor
|
|
|
PO
|
|
Alteplase (IV)
|
|
|
Dissolve clots acutely/clear IV line
|
|
|
Relative contraindication: HTN
|
|
|
Absolute contraindication: recent head trauma
|
|
|
ADR: bleeding, hemorrhage
|
|
|
C
|
|
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
|
|
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
|
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