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Pharmacology
N/A
100
Nursing
Undergraduate 3
12/07/2009

Additional Nursing Flashcards

 


 

Cards

Term
Urecholine (bethanechol)
Definition

* activates muscarinic receptors in the urinary tract, increases tone of smooth muscles and sphincters

* relieves urinary retention; also for GERD, ileius

* contraindicated with blockages

* Onset: 30-60min.  DOA: 60min.  make sure a bathroom is nearby!

* ADR's: CHOLINERGIC (N/V/D, cramps, urinary frequency, ^ sweating/salivation, blurred vision, brady♥, ↓HTN

Term
atropine
Definition

* anticholinergic/muscarinic antagonist - BLOCKS ACH receptors!

* Actions: ↑HR, ↓secretions, relaxes bronchi, ↓bladder tone (irritable bladder), ↓GI tone/motility (UC, crohn's), mydriasis, CNS excitation (muscarinic poisoning)

* ADR's: anticholinergic!  xerostomia, urinary retention, constipation, ↑IOP, blurred vision, photophobia, tachy♥/dysrhythmia, anhydrosis, asthma

* contraindicated with glaucoma because of ↑IOP

* antidote: physostigmine (~2mg IM/IV); ipecac syrup followed by activated charcoal

Term
echothiophosphate
Definition

* irreversible cholineresterase inhibitor - only one that is clinically significant!

* allows to have more Ach available → mydrasis (↓IOP!)

Term
myasthenic vs. cholinergic crisis
Definition

myasthenic cholinergic

* d/t inadequate meds * med OD

* poor transmission @ junction * excessive ACH

* continuous stimulation

give edrophonium (Tensilon) - fast-acting ChEI

* will get better * will get worse

  - resp support   - resp support

  - neostigmine (Prostigmin)   - atropine 

Term
Neuromuscular blocking agents (NMB's)
Definition

* Block Ach from activation Nm receptors on skeletal muscles @ NMJ

* causes motor relaxation commonly used during surgery, ET intubation, mech ventilation or other dx procedures.

* risk for resp arrest d/t possible paralysis of resp muscles!

* can't cross BBB → no effect on CNS, therefore:

   - need sedation, need analgesia and need respiratory support!

* caution use with myasthenia gravis patients bc they already have extreme muscle weakness!

Term
tubocurarine (Curare)
Definition

* non-depol. NMB

* contraindicated in cardiac/renal patients or those with significant ↑K+ (major burns, multiple skeletal m. or UMN injury)

* ADR's: ↓HTN, ↑K+, brady♥, dysrhythmias, ♥arrest

* does not cross BBB, no effect on CNS (need sedation, need analgesia and need resp support!)

* Abx - aminoglycosides, tetracycline, some non-PCN's - inhibitors (intensify response!)

* ChEI's decrease effect d/t competition with Ach receptors!

Term
succinylcholine
Definition

* depolarizing NMB  (constant state of depolarization - no repolarization!)

* no effect on CNS

* abx intensify response

* Anticholinergics potentiates effects

* risk of malignant hyperthermia - temp up to 43°C/109.4°F with succinylcholine + inhaled anesth.

  - hyperpyrexia d/t ↑ metabolic activity of muscle (constant) and ↑ release of Ca+2 (uncontrolled!)

  - d/c succs, cooling blanket, iced IV NS, dantrolene (stops muscle activity!) 

Term
epi concentrations
Definition

1:100 PO inhalation

1:1000 SQ, IM, intraspinal

1:10,000 IV, intracardiac

1:100,000 in combo with local anesthesia

 

these concentrations CANNOT be used interchangeably!

Term
anaphylactic shock
Definition

* widespread ↓HTN

* glottal edema

* bronchoconstriction

* treat with epinephrine

* β1: ↑ CO therefore ↑BP!

* β2: bronchodilation

* α1: also helps ↑BP d/t vasoconstriction (also helps with edema!)

Term
epinephrine
Definition

* drug of choice for anaphylactic shock

* nasal decongestant d/t α1 stimulation

* all adrenergic receptors (minus DA...only DA can stimulate DA!)

* MAOi's and TCA's prolong and intensify effects!

* ADR's: HTN crisis (d/t excessive α1 stimulation), dysrhythmias (β1), angina, extravasation (IV), hyperglycemia (β2 = glycogenolysis!)


Term
norepinephrine (Levophed)
Definition

*like epi, but does not activate β2; only α1, 2 & β1

*hypotensive states and cardiac arrest

Term
dobutamine (Dobutrex)
Definition

* improves CO in HF

* + inotropic effect

* adjusted based on BP

* MAOi's and TCA's prolong and intensify the effects

* specific for β1

Term
terbutaline (Brethine), albuterol (Proventil)
Definition

* β2-specific

* indicated for asthma; delay preterm labor (Ritrodine)

* ADR's: tremors; can cause tachy♥ with large doses that effect B1 (loses selectivity!)

Term
ephedrine
Definition

* stimulates all adrenergic receptors (except DA) - like epi!

* nasal decongestion

* narcolepsy

Term
phentolamine (Regitine)
Definition

* prevent necrosis d/t extravasation of vasoconstrictors (DA, Levophed/NE)

* if OD, can't give epinephrine because B activation will dominate over A....tx with NE!

Term
Therapeutic effects of α-blockade
Definition

* essential HTN - causes dilation to ↓P

* pheochromocytoma

* Raynaud's disease (peripheral vasoconstriction) - dilates these vessels; however α blockers are contraindicated in all other types of PVD!

* OD of α1 agonist, such as epinephrine - HTN secondary to excessive α1 stimulation → blockade causes vasodilation therefore ↓P!

Term
adverse effects of α-blockade
Definition

* orthostatic hypotension - Δ position slowly!!!

* reflex tachy♥ d/t baroreceptor reflex

* nasal congestion d/t vasodilation

* inhibition of ejaculation

* Na+ retention (α blockers ↓P, which ↓kidney perfusion which holds onto Na+ and H2O → ↑P!

Term
therapeutic effects of β-blockade
Definition

* ↓HR, force of contraction & velocity of conduction

* ↓ renin release

* AP, HTN, dysrhythmias, MI, HF (carvedilol, bisoprolol, metoprolol), migraine, hyperthyroidism, stage fright, glaucoma (↓ production of aqueous humor), pheochromocytoma 

Term
adverse effects of β-blockers
Definition

* brady♥

* reduced CO

* precipitation of heart failure - except with Coreg and Copressor

* AV heart block

* bronchoconstriction*

* peripheral vasocon

* inhibition of glycogenolysis

* rebound cardiac excitation

Term
what are the 3 β-blockers that are effective with HF?
Definition

* carvedilol (Coreg) - best

* bisoprolol (Zebeta) - not as common

* metoprolol (Lopressor) - very common

 

β-blocker use in HF used to be contraindicated but these 3 drugs have been proven effective!

Term
clonidine (Catapres)
Definition

* indirect α2-adrenergic blocking agent

* centrally-acting, SELECTIVE - acts w/in CNS in areas assoc. with autonomic regulation of CV systems

* primary indication: HTN

   - also used for menopausal flushing, w/d from opioids/narcotics, Tourette's and severe cancer pain (Duraclon)

* ADR's: drowsiness, rebound HTN (d/t baroreceptors), anxiety, depression; constipation!

Term
drug holiday
Definition
brief (e.g. 10 days) interruption of treatment.  Must take place in a hospital because drug holidays can be dangerous!  When a holiday is successful, beneficial effects are achieved with lower doses.
Term
carbidopa/levodopa (Sinemet)
Definition

* Levodopa is metabolized to DA and used in the periphery but only 2% is usable in the brain.

* Combined with carbidopa to prevent breakdown of levodopa → DA in the periphery, allowing more to be used by the brain

* effects in weeks to months - depends on the patient!

* ADR's: darker-colored urine, N/V, dyskinesias, dysrhythmias, orthostat hypotension

* on-off phenomenon: abrupt loss of effect at ANY time; might be r/t too much protein in the diet (spread intake t/o the day!!)

* contraindicated with malignant melanoma (can activate neoplasm) and MAOi's - can lead to HTN crisis.  If on MAOi's, w/d from hem at least 2 weeks before giving Sinemet.  Avoid B6 (pyridoxine) with only levodopa (okay with Sinemet)

* take food with stomach upset but avoid meals high in protein

Term
Anti-epileptic drugs (AED's)
Definition

* MOA: Suppresses Na+ and Ca++ influx, potentiation of GABA (neuronal inhibitor)
  - supp. of Na+ influx: phenytoin (Dilantin), carbamazepine (Tegretol), valporic acid (Depakote), lamotrigine (Lamictal)
  - supp. of Ca+ influx: valporic acid (Depakote), ethosuximide (Zarotin)

  - antagonism of glutamate (excitatory transmitter): felbamate (Felbatol), topiramate (Topamax)

  - potentiation of GABA: benzos, barbs, gabapentin (Neurotin), tiagabine (Gabatril), vigabatrin (Gabril)

* monitor plasma levels with ALL AED's
* majority are teratogenic - women of childbearing age need to use contraception!
* need to be GRADUALLY withdrawn!  Abrupt withdrawal can lead to status epilepticus
     - 20-30 min duration
     - ↑HR, BP, Temp & ↓BS and pH (acidosis!)

* withdrawal needs to be done over a period of MONTHS.  if on multiple AED's, need to d/c ONE AT A TIME

* drugs are matched based on seizure type.  EXCEPTION: valporic acid (Depakote) - effective for all types!


Term
phenytoin (Dilantin)
Definition

* for partial and 1° generalized tonic-clonic seizures

* PO, IV

   - IV: mix with NS only - it is incompatible with everything!!  Cannot be PB'ed - need its own primary line!
   - give slowly - too fast, and BP can bottom out!!
* ADR's: dysrhythmias, hypotension (IV), skin rashes → D/C! (SJS)...interferes with Vitamin D metabolism (rickets, osteomalacia), gingival hyperplasia, sedation, ataxia, hirsutism, ↓Vit K synth, teratogenic, diplopia, tremors
* phenytoin metabolism INHIBITORS = diazepam, eimetadine, ETOH, valporic acid (need ↓dose!)
* phenytoin metabolism INDUCERS = BCP's, warfarin, glucocorticoids (need ↑dose!)

* Therapeutic range: 10-20mcg/dL!

* Encourage frequent dental check-ups d/t gingival hyperplasia

Term
fosphenytoin (Cerebyx)
Definition

* prodrug for phenytoin (Dilantin) → immediately converts to phenytoin in blood
* for SE (continuous seizure, 20-30 min)
*non-irritating to veins
* prepared in 5% dextrose

Term
carbamazepine (Tegretol)
Definition

* preferred over phenytoin and phenobarbitol
* 1st choice for partial & tonic-clonic seizures (NOT absence); for bipolar disorder refractory to lithium; trigeminal & glossopharyngeal neuralgias
* ADR's: ataxia, vertigo, visual problems, H/A, myelosuppression, teratogenic (assoc. with NTD's), skin problems (SJS!)

* grapefruit juice is an inhib
* inducer of enzyme for BCP's (tell them to use another form) & warfarin
* oxcarbazepine (Trileptal) - derivative with fewer ADR's

Term
phenobarbitol
Definition

* potentiates GABA
* well-absorbed with a long T1/2 (~4 days)
* ADR's: dependence, depression, agitation, confusion, ↓Vit K&D, paradoxical hyperactivity/irritability w/ kids, drowsiness (but they build a tolerance to it!)
* OD: nystagmus, ataxia, general CNS depression, death

* abrupt w/d → SE!
* primidone (Mysoline) - nearly identical, so don't 'combo'

Term
valporic acid (Depakote)
Definition

* 1st line treatment for all major seizure types; also for bipolar disorder and migraines (prophylactic)
* ADR's: (rare) hepatotoxicity, pancreatitis, teratogenic (NTD's)...cognitive impairment, N/V, indigestion (take w/ food or use enteric-coated preparation)
* contraindicated in patients with hx of liver problems, pancreatitis

* maintain blood levels: 60-100ug/dL

Term
ethosuximide (Zarontin)
Definition

* drug of choice for absence seizures (suppresses neurons in the thalamus responsible for absence seizures)
* No signifcant ADR's aside from drowsiness, dizziness and lethargy; but pt will build a tolerance to this!!
* with N/V, tell them to take with food

* risk of SJS

Term
Skeletal Muscle Relaxants for spasm
Definition

* for localized muscle spasm
   - 2° to epilepsy, hypocalcemia, acute & chronic pain syndromes, trauma (=localized muscle injury)
* diazepam (Valium) - enhances action of GABA

   - only med appropriate for BOTH spasms  & spasicity!
* tizanidine (Zanaflex)
* ADR's for all centrally-acting relaxants (all except dantrolene): CNS depression, hepatotoxicity & physical dependence

Term
Skeletal Muscle Relaxants for spasicity
Definition

* spasicity: state of increased muscle tone with exaggerated tendon reflexes (stiff, awkward movements d/t MS, CP, SC injury)
* 3 drugs used, 2 @ CNS, 1 @ skeletal muscle

     - baclofen (Lioresal) - CNS.  NOT for CVA, PD, HD chorea!  suppresses hyperactive reflexes in the SC
          - suppresses resistance to passive movementno direct effect on skeletal muscle.
          - ADR's: drowsiness, dizziness, weakness, fatigue, nausea, constip, urinary retention

     - diazepam (Valium) - CNS.  Mimics GABA
          - ADR's: sedation, dependence (MUST do slow w/d)
     - dantrolene (Dantrium) - acts directly on skeletal muscle.  does not work in CNS.  stops Ca++ release from sarcoplasmic reticulum

          - antidote for malignant hyperthermia caused by anesth and/or succinylcholine.  N2O does not cause this.
          - ADR's: weakness, diminished strength, drowsiness, hepatotoxicity, diarrhea, acne rash

Term
local anesthetics
Definition

* suppresses pain by blocking impulse conduction along axons (Na+ channels)
*
perception of pain lost first, then cold, warmth and finally deep pressure (goes backwards when the med wears off)

* used with a vasoconstrictor (usually epinephrine) to decrease local blood flow which delays systemic absorption (prolongs anesthesia)
* procaine, lidocaine, cocaine

Term
balanced anesthesia
Definition

combo of drugs to accomplish analgesia, unconciousness, muscle relaxation, amnesia.
* Combo used: SA barb (induction), NMB, opioids + NO (analgesia) - combo induces a deeper state of anesthesia
* GABA is inhibited; blocks NMDA (excitatory)

* ADR's: (inhaled) resp/♥depression, sensitization of ♥ to catecholamines, malignant hyperthermia (risk with ALL inhaled anesthetics), aspiration, toxic to OR personnel, hepatotoxic

Term
opioid analgesics
Definition

* narcotics: MSO4, codeine, oxycodone, prophyxphene
* endogenous opioid receptors: enkephalins, endorphins, dynorphins
* M (mu) most important from a pharmacological prespective; K (kappa) weak activity; Δ none
* pentazocine (Talwin) = partial agonist/agonist-antagonist
     - ADR's: analgesia, resp depression, sedation, euphoria, constipation, urinary retention, vasodilation, ↑ICP, dependence, tolerance, orthostatic hypotension
* narcosis: OD of opioid
     - naloxone (Narcan) and nalmefene (Revex) = antidotes!  (w/ Narcan, changes are INSTANT; Revex is long-acting with a LONG w/d off med!)
* contraindicated with IBD (r/t constipation)
* with acute exacerbation of COPD - give morphine!  it relieves their discomfort & anxiety and relaxes bronchospasm w/ COPD!

Term
categories of drugs for asthma
Definition

anti-inflammatory (glucocorticoids, cromolyn) → fixed doses, CHRONIC
bronchodilators - β2 agonists → chronic or acute; fixed or PRN

Term
asthma management
Definition

* β2 agonists → bronchodilation!

* inhaled: immediate treatment and prevention
* short-acting: QUICK.  Used for exercise-induced asthma, break through symptoms (albuterol [Proventil])

     - instant effect, lasts 3-5hr, Q4-6h

* long-acting: PROPHYLACTIC.  NOT USED FOR AN ACUTE ATTACK. (salmeterol [Serevent diskus] & moterol [Foradil aerolizer])

     - in 30min, lasts 12h, Q12h.  Fixed dosing, NOT PRN.

* inhaled preps have fewer ADR's, however OD'ing will cause the drug to lose selectivity and stimulate β1: tachy♥/dysrhythmias, angina.  Most common ADR are tremors.

Term
asthma management with glucocorticoids
Definition

* most effective antiasthmatic drug available.

* prophylaxis for chronic asthma (suppress inflammation)

* decreases bronchial hyperactivity, airway mucous production

* increases # of bronchial β2 receptors and their responsiveness to their agonists

* decreases inflammation! → decreased airway edema

* ADR's: minor w/ acute use.  inhaled: Bone loss (ensure lowest dose, ensure adequate Ca+2/Vit D. intake, wt.-bearing exercises), inahled oropharyngeal candidiasis & dysphonia (gargle after each administration and use a spacer).  Oral: adrenal suppression (Addison's!), bone loss.  LT: cataracts, glaucoma, PUD, hyperglycemia.  Can decrease growth in children.

Term
flucticasone + salmeterol (Advair diskus)
Definition

* fluticasone (inhaled glucocorticoid) + salmeterol (LA inhaled β2 agonist) - chronic prophylaxis
* ADR's/salmeterol: HA, tremor, dizziness, tachy♥, palpitations, HTN, difficulty breathing, bronchospasm(risk higher in african-american population)
* Interactions/salmeterol: ensure cardioselective β-blocker (metoprolol/Lopressor) to ↓ risk of bronchospasm.  Diuretics: worsening hypoK+ & EKG abn.  Potentiated by MAOi's, TCA's, or w/in 2 weeks of d/cing either.

Term
cromolyn sodium (Intal)
Definition

* anti-allergic, anti-inflammatory properties.  mast cell stabilizer, not a bronchodilator!  stabilizes mast cell membrane, decreasing the release of histamine & other mediators

     - inhibits eosinophils, macrophages and other inflammatory cells

* do not use to abort an acute attack

* safest antiasthmatic med!
* especially effective for seasonal allergy attacks; e.g. 15min before mowing the lawn!
* ADR's: cough, bronchospasm (low incidence)

* works in 15min; 1-2 weeks to get maximum benefits!

* allergic rhinnitis: Nasalcrom (intranasally)

Term
methylxanthines
Definition

* CNS stimulation, bronchodilation, cardiac stimulation, vasodilation, diuresis
* theophylline - PO, IV (not affective by inhalation)
     - narrow therapeutic range: 10-20ug/mL.  best: 5-15ug/mL
          ≥20-25ug/mL: NVD, insomnia, irritability
         
30ug/mLvery toxic.  severe dysrhythmias (VFIB), convulsions that are very hard to tx!  Can lead to death by CV/Resp collapse!

     - MOA: adenosine blockade → sm muscle relaxation

- cimetidine & fluoroquinolones increase levels, phenobarb ↓ levels,  Smoking ↓T1/2 by 50%

Term
ipratropium (Atrovent)
Definition

* Atrovent - an atropine derivative

* approved for COPD bronchospasm

* ADR's: + charge → not really absorbed from the lungs (but systemic effects are rare!); GI tract, xerostomia, pharyngeal irritation.  very high dose → ↑IOP

Term
leukotriene modifiers
Definition

* PO

* suppresses leukotrienes  (↓infammation, bronchoconstriction, airway edema, mucous secretion, recruitment of eosinophils and other inflammatory mediators to the area)

* ADR's: liver injury (zileuton, zafirlukast), Chrug-Strauss syndrome when glucocorticoid is withdrawan (zafilukast, monelukast)

     - Chrug-Strauss: wt. loss, flu-like sx, pulmonary vascularitis

* zileuton (Zyflo), zafirlukast (Accolate), montelukast (Singulair)

Term
zileuton (Zyflo)
Definition

* leukotriene modifier

* not to be used for an actue attack

* stops production of leukotrienes

* ADR's: hepatotoxicity (↑ALT's).  Metabolized by CYP 450.

* effective in 1-2 hours.

Term
zafilukast (Accolate)
Definition

* ADR's: myalgia, P450 inhib

* increases levels of theophylline, warfarin

Term
montelukast (Singulair)
Definition

* ADR's: equivalent to placebo.  In combo w/ phenytoin: decreases montelukast levels

* effective w/in 24h.

Term
omalizumab (Xolair)
Definition

* MOA: antagonism of IgE → decreases release of inflammatory mediators

* after d/c it takes 1 year for IgE to return to pre-treatment levels

* 2nd line for allergy-related asthma > age 12 and ONLY when preferred options have failed

* SQ

Term
seasonal rhinnitis
Definition

* hay fever, rose fever: outdoor allergens

* PO antihistamines (H1-receptor antagonists)

     - most effective when taking prophylactically for sneezing, rhinorrhea & nasal itching; less effective after sx appear

     - no relief of congestion! - sedating!

     - diphenhydramine (Benadryl), fexofenadine (Allegra), azelastine (Astellin)

* intranasal glucocorticoids - prophylactic.  anti-inflammatory and suppresses all major symtpoms

     - beclomethasone (Beconase), budesonide (Rhinocort), fluticasone (Flonase), mometasone (Nasonex), triamcinolone (nasalcort AQ HFA) - watch for epistaxis!

Term
seasonal rhinnitis, cont.
Definition

* Nasalcrom - intranasal cromolyn sodium.  

     - works in 1-2 weeks.

* sympathomimetrics (PO and intranasal decongestants used adjunctively)

     - relieves stuffiness, not sneezing, runny nose or itching

     - limit use to 3-5 days or else will REBOUND (all symptoms will reappear!)

          - phenylephrine (Neo-synephrine), Sudafed PE, Afrin

     - potential for abuse (like amphetamines) - pseudoephedrine, ephedrine

     - ADR's: CNS excitation (irritability anxiety, insomnia)

Term
major antitussives
Definition

* dextromethorphan

* diphenhydramine

* codeine - opioid

 

antitussives do not suppress the productive cough of chronic lung disease (emphysema, asthma, bronchitis) - don't use them!

Term
opioid antitussives
Definition

* act in the CNS to increase cough threshold

* codeine, hydrocodone

* Schedule II controlled substance/Rx alone

* Schedule V when used in an antitussive mixture

 

↓ respiratory reserve in the elderly and those with COPD.  avoid these drugs!

antidote: Narcan!

Term
non-opioid antitussives
Definition

* dextromethorphan

* most effective, used in a lot of OTC preparations

* not as effective as codeine for acute, severe cough

* blocks receptors for NMDA in CNS → decreases pain.  also doubles the effect of opioids when used in combo.

* taken Q4-6h with normal therapeutic doses while coughing.

* diphenhydramine - can suppress cough @ high doses only

* benzonatate (Tessalon) - structural analog of tetracaine.  don't chew or else will anesthetize the mouth/pharynx!

Term
expectorants
Definition

* stimulates flow of respiratory secretions

* guaifenesin (Mucinex) - works well in high doses

Term
mucolytics
Definition

* reacts directly with mucous to thin secretions

* acetylcysteine (Mucomyst) - sulfur content (also the antidote for Tylenol OD!)

* Hypertonic Na+

Term
kinin
Definition

* vascular permeability

* chemotaxis - leukocyte

* works with PGE to produce pain**

* bronchoconstriction**

* smooth muscle contraction**

.....inducing HTN!

Term
histamine
Definition

* synth & stored in mast cells (tissues) and basophils (blood)

* plays a role in allergic reactions and GI acid secretion!

* present in skin, lungs, GI tract

* vasodilation of small vessels

* ↑capillary permeability → tissue edema!

* bronchoconstriction

* CNS effects - sedation, itching, pain, seizure suppression


Term

H1 antagonists

(classic antihistamines)

Definition

* Tx MILD allergic reactions!

* selectively blocks H1 receptors from histamines but DOES NOT block histamine from mast cells & basophils

* also antagonizes muscarainic receptors - anticholinergic effect (drying out!)

* diphenhydramine (Benadryl) - 1st generation

     - ADR's: highly sedating, pupil dilation, tachy♥, hyperpyrexia

* loratidine (Claritin) - 2nd generation

     - less sedating (does not cross BBB), longer-acting

* fexofenadine (Allegra), cetirizine HCl (Zyrtec) - also 2nd gens

* safety w/ pregnancy unknown

Term
antihistamines for motion sickness
Definition

* H1 and muscarinic receptors blocked in neuronal pathway from vestibular apparatus of inner ear to the vomiting center of the medulla

* promethazine (Phenergan)

* dimenhydrinate (Dramamine)

* meclizine (Antivert) - vertigo

 

with the common cold: only antimuscarinic activity and moderate decrease in rhinorrhea activity

Term
cyclooxygenase (COX)
Definition

* enzyme that converts arachidonic acid into prostaglandins (PGE2, PGI2) which promote inflammation and sensitize receptors to painful stimuli.

* COX1 = GOOD! =)

     - found in all tissues.  promotes plt aggregation, protects GI mucosa and supports renal fx

          - inhibit: gastric erosion & ulceration, bleeding tendencies, renal impairment, protection against MI/CVA 2º to ↓plt aggregation!

* COX2 = BAD! =(

     - produced @ site of injury.  mediates inflammation, sensitizes pain receptors

          - inhibit: supp. of inflamm, alleviates pain, dec. fever, renal impairment

Term
COX inhibitors
Definition

* non-selective - both COX1 and COX2

* NSAIDS, including ASA

* ADR's: gastric ulceration/bleeding, renal impairment, MI & CVA (but not with ASA)

* LT use: 12% ↑risk of MI/CVA (except for ASA) and 200-300% ↑ risk with LT use & smoking!

Term
acetylsalicylic acid (Aspirin)
Definition

* non-selective COX inhibitor (1, 2)

* irreversible (all other NSAIDS are reversible)

* ADR's: GIB, RI, Reye's, salicylism (tinnitus is one of the first signs!)

* ♥ protective 2° to ↓ platelet aggregation (↓risk of MI/CVA!) - 81mg/day

* acetaminophen, diclofenac (Voltaren), celecoxib (Celebrex) do not interfere with ASA's cardioprotection.  ibuprofen blocks ASA's access to COX, so don't use!

* contraindicated (ALL NSAIDS) in kids <18 y.o. with the chicken pox/flu d/t risk of Reye's.  Tyelnol is best to use! 

Term
Non-steroidal anti-inflammatory drugs (NSAIDs)
Definition

* 1st generation - non-selective

* ibuprofen (Motrin), naproxen (Naprosyn), indomethacin (Indocin), sulindac (Clinoril), meloxicam (Mobic)

* mild-moderate pain relief, including OA & RA, bursitis, pain relief, antipyretic, relieve dysmenorrhea

* ketorolak (Toradol) - IV, IM (30-60mg), PO

     - ST use only 

     - relieves pain as well as opioids

     - minimal anti-inflammatory properities

     - ADR's: GI ulceration, GIB, RI, ↑risk thrombosis, SJS

Term
Non-steroidal anti-inflammatory drugs, cont.
Definition

* 2nd generation - COX2 inhibitors only = -coxibs

* analgesia, antiypyretic, anti-inflamm W/O the bleeding, RF and GI problems with COX1.

* celecoxib (Celebrex)

     - contains sulfa.  contraindicated with sulfa allergies.

     - ↑ risk of MI and thrombotic events

Term
acetaminophen (Tylenol)
Definition

* antipyretic, analgesic - no anti-inflamm. properties

* inhibits PG synth in CNS only

* no platelet aggregation suppression

* inhibits metabolism of warfarin

* antidote: acetylcysteine (Mucomyst) mixed w/ water or juice (w/in 8-10h OD, there is good protection against the liver)

* do not exceed 4000mg (4g) day. 

Term
glucocorticoids = corticosteroids
Definition

* cortisone, prednisone

* ADR's: hyperglycemia, suppresses protein synth, breaks down fat (redistribution w/ LT use) → iatrogenic cushing's (potbelly abd, buffalo hump, moonshaped face), thinning of the skin; promotes vascular stability, increases circulating RBCs & PNMs, decreases immunity, delayed wound healing

* more stress, more glucocorticoids!

     - severe stress → glucocorticoid insuff → circulatory failure → death!

     - Na+ retention, K+ and Ca++ loss (watch with digoxin!!)

Term
glucocorticoids
Definition

* low doses tx adrenocorticol insuff (Addison's)

     - give @ 9am to mimic normal burst @ dawn (cortisol is NORMALLY released in the morning!)

* higher doses: inflammatory supression

     - RA, asthma, certain cancers, prevent donor rejection

* LT: pituitary loses ability to manufacture ACTH → endogenous cortisol

     - SLOW D/C, gradually with NSAIDs so D/C sx not interpreted as return of underlying disease

Term
ADR' of glucocorticoids
Definition
adrenal insufficiency, OP, infections, glucose intolerance, myopathy, skin lesions, fluid imbalances (edema and K+ loss!  restrict Na+ intake and increase K+ intake!), growth retardation, psychological disturbances, cataracts/glaucoma (eye exams Q6mos), peptic ulcers, fat redistribution (iatrogenic cushing's)
Term
Disease-modifying anti-rheumatic drugs (DMARDs)
Definition

* reduce joint destruction and retards disease progression in RA

* efficacy in 3wks-6mos depending on the drug

* concurrent use with NSAIDs while waiting for effects

* multiple DMARDs with persistent joint injury progression 

Term
methotrexate (Rheumatrex, Trexall)
Definition

* efficacy in 3-6 weeks

* ADR's: hepatic fibrosis, myelosuppression, GI ulcers, pneumonitis, immunosuppressive

* pregnancy category X

Term
hydroxychloroquine (Plaquenil)
Definition

* usually used in combo with methotrexate, NSAIDs

* MOA unknown

* most serious ADR: retinal damage (dose-related) - eye exams Q6mos!

* take w/ milk or food w/ GI upset

Term
sulfasalazine (Azulfadine)
Definition

* retards joint deterioration w/in 1 month

* contraindicated with allergy to sulfa

Term
etanercept (Enbrel)
Definition

* mAb, DMARD II

* TNF blocker

* ADR's: immunosupp/risk of infection, HR, demylenization disorders (MS)

* inflixamab (Remicade), adalimumab (Humira), anakira (Kineret) (an IL1 blocker)

* these drugs are very expensive!

Term
DMARDS III
Definition

* newer small molecule, less $$

* leflunomide (Avara) - contraindicated with pregnancy!

* cyclosporine (Sandimmune)

Term
DMARDs IV
Definition

* older, limited use

* gold salts - PO, IM...frequent pruritis, stomatitis, renal toxicity

* penicillamine [Cuprimine, Depen] - myelosupp, autoimmune sx

* azathioprine (Imuran) - rarely used; hepatotox, blood dyscrasias

Term
treating gout
Definition

ST - acute (< 3 yrs) → NSAIDs (1st choice), glucocorticoids

 

LT (≥ 3 years) → to decrease uric acid levels (make sure to look @ these lab values!!)

Term
allopurinol (Zyloprim) 
Definition

* for chronic tophaceous gout

* ↓ blood levels of uric acid by decreasing production

Term
probenecid
Definition

* inhibits tubular reabsorption of uric acid and ↑ uric acid excretion

* prevents excretion of penicillin and cephalosporin!!! - can lead to toxic levels, don't combo these drugs together!

Term
arterioles
Definition

* CONTROL VALVES that regulate LOCAL blood flow (everything to do with afterload!)

Term
preload
Definition

* the pool - pressure stretching the ventricle of the heart (usually refers to the L ventricle)

* the more a ventricle stretches, the more force that needs to be used to eject the blood out!

Term
afterload
Definition

* tension produced by a chamber of the heart in order to contract ("load" the heart must eject blood against!)

* ↑ afterload = ↓ SV

* ↓ afterload = ↑ SV

Term
baroreceptors
Definition

* maintain a pre-set BP

* aortic arch, carotid arteries, vena cava (Bainbridge reflex), atria

* aortic arch & carotids are the ones that primary sense the Δ in pressure!

Term
RAAS
Definition

* ↓ (renal) BP - kidneys secrete renin

* converts angiotensinogen to angiotensin I

* angiotensin I is converted to angiotensin II via ACE (angiotensin converting enzyme) from the lungs

* angiotensin II → strong vasoconstrictor!  Stimulates the release of aldosterone (saves Na+ and water (and secretes K+) which in the end ↑ blood volume, which ↑BP!

Term
normal blood pressure
Definition
<120/80
Term
prehypertension
Definition
120-139 or / 80-89
Term
hypertension stage 1
Definition
140-159 or 90-99
Term
hypertension stage 2
Definition
≥160 or ≥100
Term
digoxin (Lanoxin)
Definition

* + inotrope (↑ contractility) while ↓HR (hold med if HR <60bpm)

* HF, dysrhythmias

* Monitor kidney fx for renal insufficiency (expect a reduced dose!)

* need blood levels.  Therapeutic range: 0.5-2.0.  0.2-0.8 = BEST

* watch K+!  hold med with hypokalemia (digoxin inhibits the Na+K+ATPase pump.  Dig & K+ compete with each other.  No K+ = no competition with receptors which leads to toxicity!)

Term

s/s of impending digoxin toxicity

s/s of actual digoxin toxicity

Definition

*impending: anorexia, N/V (usually appear first), fatigue, visual Δ's (yellow tinge, halos around dark objects, blurring)

 

*actual: dysrhythmias!!!

Term
chronic stable angina
Definition

* increases with activity, emotions, large meal or cold

* stops with rest

* underlying cause: CAD

* tx with NTG, beta blockers, CCBs *AND* an anti-platelet drug (such as ASA) to reduce the incidence of MI/CVA.

Term
variant angina-prinzmetal's/vasospastic
Definition

* coronary vasospasm

* you can wake up in the middle of the night with this one!

* treatment is symptomatic only: nitrates and CCBs

Term
unstable angina
Definition

* aka acute coronary syndrome (ACS)

* medical emergency - might lead to an MI!

* occurs at rest with new onset or intensification of existing stable angina

* acute management: anti-ischemic therapy: NTG (SL→IVT), BB (if contraind, use a non-dihydropyridine), O2, morphine sulfate

Term
nitroglycerin 
Definition

* dilation of veins

* ↓ preload and (slightly) afterload

* T1/2 5-7min

* ADR's: orthostatic hypotension, reflex tachy♥, HA (pretx with Tylenol)

* can build up tolerance

* PDE5 inhibitors: Levitra, Viagra, Revadio - can cause severe ↓HTN!  contraind!

* subdue reflex tachy with β blockers

* 0.4mg NTG Q5min x3 if you're stilly having pain after the first pill, take the second pill and call 911 because you might be having an MI!

Term
calcium channel blockers (CCBs)
Definition

* all dilate arteries

* for stable angina only

* DO NOT ABRUPTLY D/C (risk of reflex tachy with nifedipine, ↑angina, MI)

* can mask hypoglycemic signs, so use caution with diabetics

* ADR's: will initially c/o fatigue, but  eventually patients will build up a tolerance!

Term
vitamin K-dependent clotting factors
Definition

VII, IX, X, prothrombin

Term
heparin
Definition

* IV, SQ

* inactivates thrombin and factor Xa

* from bovine lungs and porcine intestines (allergies, religious regions!)

* For PE, embolic CVA, MI, DIC, prophylaxis for venous clots/DVTs

* effective in minutes, T1/2 is 1.5 hours

* monitor aPTT (nl=40 sec) 1.5-2x (60-80sec) = therapeutic

* antidote: protamine sulfate

* ADR's: hypersensitivity d/t animal origin, OP w/ LT, high dose therapy, vasospasm; bruising, petechiae, look @ stool, urine...

* contraindicated with eye surgery or CNS (risk of neurological injury!)

Term
LMW heparins
Definition

* enoxaparin (Lovenox), dalteparin (Fragmin)

* antidote: protamine sulfate (except for fondaparinux (Arixtra)

* inhibits only Factor Xa (not thrombin)

* as effective as heparin

* fixed dose scheduling, no aPTT monitoring, greatly reduced risk of thrombocytopenia

Term
warfarin (Coumadin)
Definition

* Vitamin K antagonist (antidote = Vitamin K1, Aquamephyton)

* Avoid mayo, cannola oil, soybean oil, green leafy veg = good sources of Vit K

* category X

* Monitor PT (therapeutic: 18-24sec) and INR (therapeutic: 2-3; 3-4.5 w/ mech valves, recurrent emboli)


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