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drug action of tricyclic antidepressants
block reuptake of norepinephrine and serotonin, but also block muscarinic, dopaminergic, histaminergic, muscarinic, and serotonergic receptors
common adverse effects of tricyclic antidepressants
anticholinergic (sedation, dry mouth, impotence, orthostatic hypotension, EPS, cardiac conduction problems
risks of tricyclic antidepressants
narrow therapeutic index, toxicity affects CNS (seizures) and cardiovascular (dysrhythmias), can cause death, orthostatic hypotension (fall risk)
teaching about tricyclic antidepressants
  • may take 3-4 weeks for therapeutic effect
  • titrate up to effective range to avoid OD
  • watch for oversedation, postural hypotension
  • do not stop taking meds abruptly
  • anticholinergic effects (drying)
  • pregnancy category C, D
tricyclics are used to treat...
depression, certain chronic pain disorders, OCD, bedwetting
pregnancy category A drugs
studies show no risk to human fetus
pregnancy category B drugs
studies show no risk to animal fetus; no information re. human fetus
pregnancy category C drugs
adverse effects shown in animal fetus; no info re humans
pregnancy category D drugs
possible risk to human fetus reported
pregnancy category X drugs
should never be used in pregnant women-significant risk of fetal abnormalities
SSRIs are used to treat...
depression, bipolar, anxiety disorders, OCD, eating disorders
most common adverse effects of SSRIs
  • generally much safer than tricyclics
  • insomnia
  • weight gain
  • impotence
  • serotonin syndrome
  • renal/hepatic
teaching for SSRIs
  • taken once daily in morning
  • may take 3-4 weeks to have therapeutic effect
  • do not take with other meds
  • contraindicated in pts w/ hx kidney, liver disease
  • pregnancy class B, C
patients taking MAOIs may have potentially fatal hypertension if...
consume too much tyramine.  high tyramine content in:

aged cheeses, smoked/pickled/aged meats, yeast (dark beer), red wine, fava beans, avocado
aminoglycosides treat...
MRSA, primarily gram-, but also resistant gram+ cocci
aminoglycosides are dosed...
once daily (concentration based killing) to reduce risk of kidney damage
precautions with aminoglycosides
renal function, casts in urine, ^BUN, ^creatinine, ototoxicity.  measure trough 18-24 hrs post dose
fluoroquinolones treat...
broad gram-, select gram+, UTIs (unchanged in urine)
precautions with fluoroquinolones
can cause arrhythmias, do not take with antacids or dairy, may be associated with superinfection 
vancomycin is used to treat
only gram+: C. diff, MRSA, Staph.,
routes of vancomycin
IV-bone, joint, blood infections
PO-GI infections
precautions for vancomycin
nephrotoxicity, ototoxicity, pretreat with benadryl to prevent Red Man Syndrome
action of MAOIs
inhibit breakdown of monoamines (serotonin, norepinephrine, dopamine, tyramine), leaving more in synapse
action of lithium
alter sodium ion transport in nerve cells, affecting catecholamine metabolism
precautions of lithium use
narrow therapeutic index, renal precautions, pregnancy, electrolyte imbalance, fine tremors.  long term use can cause hypothyroidism
signs of lithium toxicity
N/V/D, tremor, confusion, seizures, dysrhythmia, movement irregularities
rivastigmine (Exelon) and donepezil (Aricept) are used to treat...
their action...
Alzheimer's disease/
cholinesterase inhibitors-delay breakdown of acetylcholine at synapse.  improves memory and cognitive function
Study of drug movement throughout the body
Pharmacokinetics
Four Basic Pharmacokinetic Processes:
•Absorption
•Distribution
•Metabolism
•Excretion
The movement of a drug from its site of administration into the blood
Absorption
The movement of the drug from the blood into cells
Distribution
Enzymatically mediated alteration of the drug’s structure
Metabolism
The movement of the drug out of the body
Excretion
Two Major Routes:
  • Enteral (via the gastrointestinal tract) By Mouth
  • –Parenteral (outside the gastrointestinal tract) Injection
Intravenous Barriers to Absorption
None
Intravenous Absorption Pattern
Instantaneous and complete
Intravenous Advantages
–Rapid onset
–Control
–Best for irritant drugs
Intravenous Disadvantages
–High cost
–Difficult
–Inconvenient
–Irreversible
–Fluid overload
–Embolism
Intramuscular Barriers to Absorption
The capillary wall
Intramuscular Absorption Pattern
–Drug’s water solubility
–Blood flow to the site of injection
Intramuscular Advantages
–Can be used for poorly soluble drugs that cannot be given IV
–Used for depot drugs
Intramuscular Disadvantages
Discomfort and inconvenience
Subcutaneous
•Essentially same pharmacokinetics as IM
•Absorption will be affected by amount of subcutaneous fatty tissue
Oral Administration Absorption Pattern
Highly variable
Oral Administration Advantages
Easy, convenient, inexpensive
Oral Administration Disadvantages
Variability of absorption
The intestinal and hepatic degradation or alteration of a drug or substance taken by mouth after absorption, removing some of the active substance from the blood before it enters the general circulation.


First-pass effect
Movement of drugs throughout the body  
Distribution
Factors that impact distribution
•Plasma protein binding 
 –Albumin (most important)
•Distribution of blood 
  –Rapid heart, liver, kidneys,brain    
  –Slow – muscle, skin, fat
Some drug molecules have an affinity for binding to protein molecules in blood stream
Plasma Protein Binding
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