Pharmacology Flashcards
Mu1, Mu2, kappa, delta
inhibit calcium transport presynapitcally and potentiating potassium transport post synaptically , reduce synaptic action potential of central/c pain fibers
Mu1
pain reduction (#1 opioid pain receptor)
Mu2, Kappa side effect
have side effect of respiratory depression “kappa Kills and Mu2 is a character that kills”
codeine metabolism
morphine and hydrocodone –> hydromorphone
morphine and hydrocodone are metabolized into
hydromorphone
side effect of opiates
hypogonadism! Low Testosterone
NMDA antagonists
methadone and ketamine
Buprenorphine
Mixed agonist/antagonist at M1,2, K and delta receptors, often combined with naloxone for opioid detoxification/weaning…8-16 mg sublingual daily
Naloxone
Opioid antagonist, 0.2-2 mg IV
Tramadol
Mu agonist, as well as SNRI reuptake inhibitor, 25 - 100 mg q4-6 hr PRN
Acetaminophen
Phospholipids –PLA2–> AA –COX1,2–> PG, acetaminophen inhibits cox centrally which stop PG formation – helps with fever, pain…bc metabolized centrally no side effects of gastric/renal dz..ceiling effect of pain reduction is at 1,000 mg….4g total daily dose max (out of hospital we rec 3 g total daily dose)
NSAIDs
Cox 2 dont affect platelets
peripherally acting on COX 1&2
Reduces inflammatory pain (bc decr PG)
Ibuprofen 200-800 mg PO q4-6 hrs
Naproxen 220-500 mg PO q12 hrs
Indomethacin 25-50 mg PO BID (good for HO)
Diclofenac 1% gel 2-4 grams topically QID PRN; useful for superficial MSK pain like trochanteric bursitis , hand, wrist, shoulder
Celecoxib (COX2 select) 100-200 mg PO BID
Meloxicam (COX2 select) 7.5-30 mg PO Daily
Steroids
Inhibit PLA2, so inhibit phospholipid to AA transformation
Steroids
Inhibit PLA2, so inhibit phospholipid to AA transformation
Corticosteroids, such as prednisone, function by inhibiting the enzyme phospholipase A2 (PLA-2), which normally produces arachidonic acid. Without arachidonic acid, prostaglandins are also no longer produced. However, the direct effect of prednisone is to inhibit arachidonic acid production, which indirectly leads to decreased prostaglandins. NSAIDs directly inhibit the COX-1 and COX-2 enzymes, the effect of which directly inhibits the production of prostaglandins.
COX2
PG produced by COX1 that protect stomach are still working, inhibit cox 2 PG
COX 2> COX1 inhibitors
meloxicam (once daily dosing) and celecoxib (protect stomach)
COX 2> COX1 inhibitors
meloxicam (once daily dosing) and celecoxib (protect stomach)
Topical meds
fentanyl, diclofenac, lidocaine usually 2% (good for SCI IBD/TID PRN), lido patch 1 patch daily comes in 4-5%
Amitriptyline/NOR
anticholinergic, dry. mouth, constipation, urinary retention, QT prolongation….amitriptyline more potenet than nortriptyline (gentler, possibly less efficiatious)….ami gets metabolized into nortrip
Gabapentin MOA
blocks L type Ca2 in CNS, cleared by kidneys, 3600 mg max daily dose..binds to the alpha 2 delta subunit of calcium channel
Pregabalin
same mechanism, blocks L type Ca2 in CNS, approved for diabetic neuropathic pain, postherpetic neuralgia, and fibromyalgia
Duloxeitine/Venlafaxine
SNRI, antidepp and anti neuropathic pain, FDA approved for diabetic peripheral neuropathic pain and fibromyalgia. 30-60 mg daily , venlafaxine 25 mg PO TID or 37.5-75-150 PO extended release
Carbamazepine
Blocks Na channels on neurons , prevents signal transmission, useful for trigeminal neuralgia, mood stabilizer in TBI, 100-200 mg BID-QID
Lidocaine infusion
Steroid injection
Inhibit sodium channels on C fibers
steroid injection blocks PLA2 so no AA or PGs, also have. DIRECT neuronal inhibition
Capsaicin MOA
depletes substance P, decr pain signal transmission
Baclofen MOA
Gaba B receptor agonist, withdrawal itchy bitchy twitchy, renally cleared
Diazepam MOA
Gaba A receptor agonist
CLACK
gaba A works on Cl
Gaba B1 works on calcium
GabaB2 works on K
tizanidine MOA
alpha 2 agonist (as is clonidine), inhibits spinal reflex arch, hepatically cleared!
dantrolene MOA
peripherally acting, binds to Ryanodine receptor in SR in muscle cells and inhibits calcium release which inhibits muscle contraction.
Botox injections MOA
inhibit presynaptic syntaxin , synaptobrevin and SNP 25 proteins which are full of NTs about to be released into the synapse. By cleaving these proteins, the toxin prevents ACh from being released….3 days onset, 3 week peak, 3 months duration.
Polyethylene glycol
osmotic laxative that pulls fluid into the bowel lumen
Lactulose
Traps NH3 in bowel to tx hepatic encephalopathy…osmotic laxative … docusate is a stool softner, senna is a stimulant
Bisacodyl
Rectal wall irritant that is used to stimulate rectal propulsion and evacuation of stool bolus, use gloved finger with lidocaine gel to sweep and dilate it more
UMN bladder tx
small, spastic, calm bladder down…Bladder empties via cholinergic, parasympathetic, pelvic nerve (S2-4) and stores via noradrenergic sympathetic hypogastric nerve (T11-L2)
Oxybutynin
anticholinergic, inhibits Muscarinic cholinergic activity, blocks detrusor squeezing, 5-10 mg daily
Tolterodine
same mech of oxybutynin, M antagonist a little gentler, 2-4 mg daily
Mirabegron “B3”
B3 agonist , agonizing those receptors you are storing urine…bladder wall selective bc B3 only on bladder wall so less systemic effects
Bethanechol
procholinergic to incr detrusor activity and promote empyting, useful in LMN/cauda equina, cholinergic side effects runny nose, hypersalivation, diarrhea
Good urinary medication for LMN/cauda equina syndrome
bethanechol (agonist cholinergic receptors on detrusor which promotes emptying)
Tamsulosin
Alpha 1 blocker, alpha blockers close bladder neck , useful in DSD
Heparin
rapid acting agent that activates antithrombin 3, which then inhibits factor Xa, rapid reversal with protamine sulfate, risk of HIT so monitor platelets
Enoxaparin
is a lower molecular weight heparin, also reversed with protamine sulfate, tx is 1 mg/kg body mass BID
Amantadine
Non-competitive antagonist of the NMDA receptor, which increases dopamine release and prevents dopamine reuptake., can decr seizure threshold
Methylphenidate
NE/D reuptake inhibitor, DOES NOT LOWER SEIZURE THRESHOLD (like amantadine)
Donepezil (Aricept)
Cholinesterase inhibitor, promotes ACh accumulation in brain, useful neurostimulant esp in anoxic brain injury
Levetiracetam
Na channel inhibiton ? but MOA unknown ,
prevents early posttraumatic seizures (7 days…. as it hasnt been shown to prevent late seizures) , sedation, used for mood stabilization
Phenytoin
possible Na channel block, good for early PTS prevention, but docs often use keppra for favorable side effect profile
Valproate
V gated Na channel blockade, good for seizures and mood stabilizer
Carbamazepine
useful for mood stabilizer and trigeminal neuralgia
Trazodone
SSRI , helps with sleep and mood
Mirtazapine
TCA ….. antagonist on central alpha 2 receptors which causes increased release of serotonin and norepinephrine
Pyridostigmine “gets RID of MG”
Anticholinesterase , so more ACh, Myasthenia gravis
Riluzole
Blocks glutamate in CNS prolongs survival by a few months
Nusinersen
alters splicing activity of SMN2 gene so it produces more SMN protein, used in SMA, shown to improve motor function and ambulation
Anesthetic duration (block Na channels which are at the nodes of Ranvier)
lidocaine 1-3 hrs
ropivacaine 4-6 hrs (least toxic to tenocytes)
bupivacaine 4-8 hrs
Prolotherapy
dextrose 25% solution, chaper than PRP, regenerative brings more blood
Which two bowel meds are osmotic laxatives
polyethylene glycol and lactulose
FDA approved for diabetic peripheral neuropathy
Duloxetine and pregabalin are FDA-approved to treat pain due to peripheral neuropathy in diabetes.
Avoid use with NSAIDs bc it may potentiate bone marrow suppression, GI side effect, hepatotoxicity
methotrexxate
GI irritation, rash, hypersensitivity, renal toxcitity, headache
sulfasalazine
GI, liver , leukopenia
azathioprine
alopecia, n/v, bladder side effect, pulm fibrosis, leukopenia, thrombocytopenia
cyclophosphamide
immunosuppression, HTN, renal insufficiency
Cyclosporine
Mucosal ulcer, rash, proteinuria, nephropathy, leukopenia, thrombocytopenia, anemia
gold salts (tx for JRA)
IL2 blocker
cyclosporine
meds that induce parkinson type symptoms
Metoclopramide (Reglan)
Lithium
Haloperidol
MS meds
Immunomodulator agents include interferon beta-1a (Avonex and Rebif), interferon beta-1b (Betaseron), and glatiramer acetate (Copaxone). These have been shown to reduce relapse rates in MS patients. Immunosuppressive agents include cyclosporine, azathioprine, methotrexate, and mitoxantrone, and can reduce relapse rate but have a greater side-effect profile and are therefore used as a second-line agent. Intravenous immunoglobulin is also an immunosuppressive agent and is still being studied for use in this patient population. Steroids can hasten recovery, but do not prevent further attacks, or alter progression.
early monitoring of what in myasthenia
spirometry
It is vital to do pulmonary function tests (PFTs) in patients diagnosed with MG. The forced vital capacity is probably the most important PFT, as it correlates to the function of the pulmonary muscles, including the diaphragm. Severe myasthenia may cause respiratory failure due to exhaustion of the respiratory muscles.
Xa inhibitor/ direct thrombin inhibitor
RIvaroxaban, apixaban, dabigatran
restless leg drugs
levodopa-carbidopa, ropinirole, pramipexole
treat huntington by waht receptors
decreasing dopamine and increasing Ach (antipsychotics, SSRI)
Parkinson
want to decrease acetylcholine and increase dopamine……benztropine anticholinergic, mao b or comt decr dopamine breakdown.
increases endogenous release of dopamine
AMANTADINE
benztropine
anticholinergic- parkinson dz
ziprasadone (geodon) increases
QT interval
selective alpha1 adrenergic inhibitor that can be used to induce urination.
(doxazosin)
TCA tox on EKG
A widened QRS complex can be seen with
particulate steroids
Triamcinolone, betamethasone acetate, and methylprednisolone
ratio of intrathecal baclofen to oral baclofen
100:1
hydrocodone 1 oxycodone 1.5 codeine 0.15 methadone 1-20 mg/day 4, 21-40 mg/day 8, 41-60 mg/day 10 tapentadol 0.4 (mu and NE reuptake inhibitor) vicodin 1 tramadol 0.1 hydromorphone 4 fentanyl patch 7.2 oxymorphone 3oxy
.
6 monoacetylmorphine
metabolite of heroin… can detect in urine.
